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THE 13 th SYMPOSIUM OF THE NATURAL<br />
PRODUCTS RESEARCH NETWORK FOR EASTERN<br />
AND CENTRAL AFRICA (NAPRECA)<br />
Theme “DRUG DISCOVERY FROM AFRICAN<br />
RAINFOREST”<br />
August 10-14, 2009<br />
Tel: 00243999942710<br />
Kinshasa/Gombe, DR Congo<br />
BOOK OF ABSTRACTS
13th NAPRECA SYMPOSIUM BOOK OF ABSTRACTS August 10-14, 2009<br />
>>>> SCOPE OF THE SYMPOSIUM >>>><br />
Role of ethnopharmacology in drug discovery<br />
Target identification and validation for diseases<br />
of concern to African countries<br />
Screening of extracts for bioactivity<br />
Herbal remedies<br />
Vector control agents and repellents<br />
Monitoring the isolation of active constituents<br />
Structure elucidation of bioactive compounds<br />
Ethics of Drug development<br />
Bringing active compounds into drug development<br />
Green Chemistry<br />
Kinshasa/Gombe, DR Congo<br />
ii
13th NAPRECA SYMPOSIUM BOOK OF ABSTRACTS August 10-14, 2009<br />
Local Organizing Committee<br />
Prof. Dr. Dibungi T. Kalenda - Chairman<br />
Prof. Dr. Mudogo Virima - Secretary and<br />
Vice Chairman<br />
Prof. Dr. Kokengo Bokolo - Treasurer<br />
Members<br />
Prof. Dr. Kambu Kabangu,<br />
Prof. Dr. Tona Lutete,<br />
Prof. Dr. Takaisi Kikuni,<br />
Prof. Dr. Mpuza Kapundu,<br />
Prof. Dr. Kasende Okuma,<br />
Prof. Dr. Yav Gushimana,<br />
Prof. Dr. Taba Kalulu,<br />
Prof. Dr. Molisho Ngongo,<br />
Prof. Dr. Kunyima Badibanga,<br />
Prof. Dr. Mpiana Tshimakinda,<br />
Dr. Ndjoko Karine et Pn Manga Opondjo<br />
Fernand.<br />
Prof. Dr. Dr. h.c. G. Bringmann<br />
Prof. B. Abegaz (Botswana)<br />
Prof. E. Dagne (Ethiopia)<br />
Prof. Philippe Rasoanaivo<br />
(Madagascar)<br />
Prof. J. Midiwo (Kenya)<br />
Prof. R. T. Majinda (Botswana)<br />
Prof. Joseph Moswa (DR Congo)<br />
NAPRECA Advisory Panel<br />
Contact Person<br />
Regional Coordinating Office Committee<br />
Professor Dr. J.O. Midiwo (Executive<br />
Secretary, NAPRECA)<br />
Professor Dr. C. Thoruwa (Assistant<br />
Secretary/Treasurer)<br />
Professor Dr. Abiy Yenesew (Programme<br />
Officer, NAPRECA)<br />
Dr Solomon Derese (Member)<br />
Dr. Joseph Mwaniki (Member)<br />
Prof. Dibungi Kalenda (DR Congo)<br />
Dr. Maud K. Mugisha (Uganda)<br />
Dr. J. Magadula (Tanzania)<br />
Prof. Sami Khalid (Sudan)<br />
Prof. Joseph Mbafor (Cameroon)<br />
Prof. Dr. Abiy Yenesew (Programme Officer, NAPRECA)<br />
ayenesew@uonbi.ac.ke<br />
Kinshasa/Gombe, DR Congo<br />
iii
13th NAPRECA SYMPOSIUM BOOK OF ABSTRACTS August 10-14, 2009<br />
SPONSORS OF THE THIRTEENTH NAPRECA<br />
SYMPOSIUM<br />
Université de Kinshasa<br />
Kinshasa/Gombe, DR Congo<br />
iv
13th NAPRECA SYMPOSIUM BOOK OF ABSTRACTS August 10-14, 2009<br />
FOREWORD<br />
We take this opportunity to welcome delegates to the 13 th NAPRECA Symposium to<br />
the Democratic Republic of Congo. The theme of the Symposium “Drug discovery<br />
from African rain forest” could not have been better used; the African biodiversity<br />
still offers great opportunity for doing what the them says. The amount of research<br />
that has been done on African medicinal plants and their development to<br />
phytomedicines or phytopharmaceuticals is still quite limited. The Congo basin is<br />
also the centre of the “African Rain Forest” by all consideration and has a<br />
bewildering array of biodiversity which needs to be tapped by us for the benefit of<br />
mankind.<br />
There is a large rapporteur of topics to be covered during this Symposium as<br />
indicated by the titles. We also have some luminary leading researchers and people<br />
of different disciplines in the field amongst us and we should seize the opportunity<br />
to explore collaboration for more effective and productive research activity as we<br />
usually endevour to carry out. It is clear to all of us that while the resolution and<br />
identification of active ingredients is gaining momentum in our institutions, we are<br />
not moving quickly enough to what should be our ultimate goal which should be<br />
getting the “product”. We should spend time at this Symposium reflecting the<br />
difficulties of doing this amongst ourselves.<br />
Finally, many of you, we are sure, are eagerly awaiting their first social experiences<br />
in the Congo. We wish that you will cease the opportunity to see as much as possible<br />
and leave with a positive impression.<br />
Enjoy your stay in Kinshasa. Seize your chance.<br />
Pascal Dibungi Kalenda- President, NAPRECA - Congo<br />
Jacob Ogweno Midiwo- Executive Secretary, NAPRECA.<br />
Kinshasa/Gombe, DR Congo<br />
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13th NAPRECA SYMPOSIUM BOOK OF ABSTRACTS August 10-14, 2009<br />
PROGRAMME FOR THE 13 TH NAPRECA SYMPOSIUM<br />
16:00 – 18:00 COCKTAIL<br />
SUNDAY, AUGUST 9 TH 2009<br />
ARRIVAL<br />
REGISTRATION, CERCLE ELAEÏS<br />
MONDAY, AUGUST 10 TH 2009<br />
SESSION I<br />
Chairperson: Prof. Dr. Virima Mudogo (Secretary and Vice Chairman, Organizing<br />
Committee)<br />
08:00 – 09:00<br />
09:00 – 09:10<br />
09:10 – 09:20<br />
09:20 – 09:30<br />
09:30 – 09:35<br />
09:35 – 09:45<br />
09:45 – 10:00<br />
10:00 – 10:45<br />
Registration Continues<br />
Welcome and Introductory Remark by Prof. Dr. Dibungi Kalenda<br />
Remark by Prof. J.O.Midiwo (Executive Secretary, NAPRECA)<br />
Remarks by sponsors<br />
Official of UNIKIN<br />
Rector, UNIKIN<br />
Government Official from DRC<br />
Keynote address by Prof. Dr. Dibungi Kalenda<br />
10:45 – 11:00 TEA BREAK<br />
SESSION II<br />
PLENARY LECTURES (PL)<br />
Chairperson: Prof. Dr. Dibungi Kalenda (Chairman, Organizing Committee)<br />
PL 1<br />
PL 2<br />
PL 3<br />
11:00 – 11:40<br />
11:40 – 12:20<br />
12:20 – 13:00<br />
Prof. Dr. Berhanu Abegaz<br />
Novel metabolites from Rhus pyroides from<br />
Botswana and Morus mesozyga from Cameroon<br />
Prof. Kurt Hostettmann<br />
The potential of African medicinal plants as source of<br />
new drugs.<br />
Dr. Karine Ndjoko<br />
Application of LC-MS and LC-NMR Techniques to<br />
the Identification of Bioactive Natural Products<br />
Kinshasa/Gombe, DR Congo<br />
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13th NAPRECA SYMPOSIUM BOOK OF ABSTRACTS August 10-14, 2009<br />
13:00 – 14:00 LUNCH<br />
SESSION III<br />
Chairperson: Prof. Dr. Abiy Yenesew<br />
PL 4 14:00 – 14:40 Prof. Dr. Dr. h.c. G. Bringmann<br />
Anthraquinones and alkaloids –acetogenic, antiinfective,<br />
and axially chiral!<br />
SL 1<br />
SL 2<br />
SL 3<br />
14:40 – 15:00<br />
15:00 – 15:20<br />
15:20 – 16:00<br />
Steinert, C.<br />
Isolation of bioactive compounds from the tropical<br />
liana Ancistrocladus congolensis<br />
Irmer, A.<br />
The biosynthetic origin of naphthylisoquinoline<br />
alkaloids<br />
Ngombe, N.K.<br />
Vasoconstrictor and inotropic effects induced by<br />
the root bark extracts of Anthocleista<br />
schweinfurthii (Gilg) (Gentianaceae)<br />
16:00 – 16:30 TEA BREAK<br />
SESSION IV<br />
Chairperson: Prof. Dr. Ermias Dagne<br />
PL 5 16:30 – 17:10 Prof. Dr. P. Okinda Owuor<br />
Optimising yields and quality of tea in different<br />
locations<br />
************End of day one**************<br />
Kinshasa/Gombe, DR Congo<br />
vii
13th NAPRECA SYMPOSIUM BOOK OF ABSTRACTS August 10-14, 2009<br />
TUESDAY, AUGUST 11 TH 2009<br />
SESSION V<br />
Chairperson: Prof. Dr. Berhanu Abegaz<br />
PL 6 08:30 – 09:10 Prof. Philippe Rasoanaivo<br />
Drug discovery at IMRA: Recent results and way<br />
forward<br />
PL 7<br />
SL 4<br />
SL 5<br />
09:10 – 09:50<br />
09:50 – 10:10<br />
10:10 – 10:30<br />
Prof. Dulcie A Mulholland<br />
Terpenoids from African Medicinal Plants<br />
Mpiana, P.T.<br />
Antisickling activity of Justicia secunda Vahl<br />
Merhatibeb, B.<br />
HPLC analysis and NMR identification of homoisoflavonoids<br />
and stilbenoids from the inter-bulb<br />
surface of Scilla nervosa.<br />
10:30 – 11:00 TEA BREAK<br />
SESSION VI<br />
Chairperson: Prof. Dr. Dr. h.c. G. Bringmann<br />
SL 6 11:00 – 11:20 Bwire, R.N.<br />
Radical scavenging principles from Cassia abbreviata<br />
beareana holmes and Vangueria parvifolia sond & a facile<br />
palladium catalysed transfer hydrogenation protocol of<br />
prochiral alkenes.<br />
SL 7<br />
SL 8<br />
SL 9<br />
11:20 – 11:40<br />
11:40 – 12:00<br />
12:00 – 12:20<br />
Yagi, S.<br />
Phytochemical and biological studies of Gegeria alata<br />
Kabera, J.N.<br />
Phytomedicine development from plants of Rwanda<br />
Namutebi, A.<br />
The role of nutraceutical-implied empirical grades of plant<br />
foods in eliciting plant biodiversity on women small<br />
holder farms<br />
Kinshasa/Gombe, DR Congo<br />
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13th NAPRECA SYMPOSIUM BOOK OF ABSTRACTS August 10-14, 2009<br />
SL 10<br />
SL 11<br />
12:20 – 12:40<br />
12:40 – 13:00<br />
Chairperson: Dr. Karine Ndjoko<br />
PL 8 14:00 – 14:40<br />
SL 12<br />
SL 13<br />
SL 14<br />
SL 15<br />
14:40 – 15:00<br />
15:00 – 15:20<br />
15:20 – 15:40<br />
15:40 – 16:00<br />
Mapitse, R.<br />
Synthesis of methoxystilbenes<br />
Shetonde, O.M.<br />
Total synthesis of biarylchalcones: Rhuschalcone VI and its<br />
analogues<br />
13:00 – 14:00 LUNCH<br />
SESSION VII<br />
Prof. Abiy Yenesew<br />
Red hot compounds from the red hot poker plants,<br />
Kniphofia species<br />
Magadula, J.J.<br />
Bioactive extracts and compounds from some<br />
Garcinia species growing in Tanzania<br />
Byamukama, R.<br />
Anthocyanins from selected plant species in<br />
Uganda<br />
Sivakumar, T.<br />
An application of mass spectra in natural products<br />
Ngombe, N.K.<br />
Screening of antibacterial and antifungal activities<br />
of fifteen extracts from Anthocleista schweinfurthii<br />
(Gilg.) (Gentianaceae)<br />
16:00 - 16:30 TEA BREAK<br />
Chairperson: Prof. Dr. Dibungi Kalenda<br />
PL 9 16:30 – 17:10 Prof. Dr. Joe Conolly<br />
Lifetime of Natural Products<br />
************End of day two**************<br />
Kinshasa/Gombe, DR Congo<br />
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13th NAPRECA SYMPOSIUM BOOK OF ABSTRACTS August 10-14, 2009<br />
Chairperson:<br />
PL 10 08:30 – 09:10<br />
PL 11<br />
PL 12<br />
09:10 – 09:50<br />
09:50 – 10:30<br />
Chairperson:<br />
SL 16 11:00 – 11:20<br />
SL 17<br />
SL 18<br />
SL 19<br />
SL 20<br />
11:20 – 11:40<br />
11:40 – 12:00<br />
12:00 – 12:20<br />
12:20 – 12:40<br />
WEDNESDAY, AUGUST 12 TH 2009<br />
SESSION VIII<br />
Prof. Ermias Dagne<br />
Quality control of Natural Products<br />
Prof. Sabrina Krief<br />
From plants to bioactive compounds - through the<br />
study of great apes- ecology, chemistry and<br />
conservation of Tropical forest<br />
Prof. J. Quetin-Leclercq<br />
Croton zambesicu: isolation and quantification of<br />
active diterpenes and structure-activity<br />
relationships<br />
10:30 – 11:00 TEA BREAK<br />
SESSION IX<br />
Derese, S.<br />
Antiplasmodial -hydroxydihydrochalcone from<br />
seedpods of Tephrosia elata<br />
Kerubo, L.<br />
Phytochemical investigation of surface exudates of<br />
Dodonaea angustifoliafor in vitro antiplasmodial<br />
and mosquito larvicidal activity<br />
Mukanganyama, S.<br />
The role of natural products as modulators of drug<br />
efflux in pathogenic microbes<br />
Kamatenesi-Mugisha Maud<br />
Nutri-medicinal plants usage in the management of<br />
immuno-compromised ailments in Uganda<br />
Ngadjui, B.T.<br />
Chemistry and biological evaluation of Morus<br />
Kinshasa/Gombe, DR Congo<br />
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13th NAPRECA SYMPOSIUM BOOK OF ABSTRACTS August 10-14, 2009<br />
SL 21<br />
12:40 – 13:00<br />
mesozygia and Dorstenia spp (Moraceae)<br />
Chiteva, R.<br />
Phytochemical investigation of resins from<br />
Commiphora holtziana in Kenya<br />
13:00 – 14:00 LUNCH<br />
SESSION X<br />
Chairperson: Prof. Dr. Tana Lutete<br />
SL 22 14:00 – 14:20 Nindi, M.M.<br />
Phytochemistry, analytical chemistry and medicinal<br />
plants: challenges in Africa<br />
SL 23<br />
SL 24<br />
14:20 – 14:40<br />
14:40 – 15:00<br />
K. B. Kubata<br />
Trypanosomiasis and African indigenous<br />
knowledge<br />
Ngombe, N.K.<br />
A n t i b a c t e r i a l a n d a n t i f u n g a l a c t i v i t i e s<br />
o f c a r d i a c g l y c o s i d e s e x t r a c t o f<br />
S n t h o c l e i s t a s c h w e i n f u r t h i i ( G i l g )<br />
( G e n t i a n a c e a e )<br />
15:00 – 16:00 POSTER SESSION<br />
16:00 – 16:30 TEA BREAK<br />
Chairperson: Prof. Dr. Kokengo Bokolo<br />
16:30 – 17:30 ROUND TABLE DISCUSSION<br />
************End of day three**************<br />
Kinshasa/Gombe, DR Congo<br />
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13th NAPRECA SYMPOSIUM BOOK OF ABSTRACTS August 10-14, 2009<br />
THURSDAY, AUGUST 13 TH 2009<br />
SESSION XI<br />
Chairperson:<br />
08:30 – 10:30 GREEN CHEMISTRY WORK<br />
SHOP<br />
10:30 – 10:45 TEA BREAK<br />
10:45 – 13:00 GREEN CHEMISTRY WORK<br />
SHOP CONTINUES<br />
13:00 – 14:00 LUNCH<br />
Chairperson:<br />
14:00 – 14:45<br />
14:45 – 15:30<br />
Chairperson:<br />
16:00 – 17:30<br />
SESSION XII<br />
15:30 – 16:00 TEA BREAK<br />
19:00 DINNER<br />
Medicinal Plants in the Congolese Art<br />
(DRC)<br />
Prof. Dr. Dr. h.c. G. Bringmann<br />
Our Congolese-German partnership – a<br />
model case for other universities?<br />
Round Table Discussion<br />
************End of day four**************<br />
FRIDAY, AUGUST 14 TH 2009<br />
EXCURSION<br />
Kinshasa/Gombe, DR Congo<br />
xii
13th NAPRECA SYMPOSIUM BOOK OF ABSTRACTS August 10-14, 2009<br />
PLENARY LECTURES<br />
Kinshasa/Gombe, DR Congo<br />
1
13th NAPRECA SYMPOSIUM BOOK OF ABSTRACTS August 10-14, 2009<br />
[PL -1] NOVEL METABOLITES FROM RHUS PYROIDES FROM<br />
BOTSWANA AND MORUS MESOZYGA FROM CAMEROON<br />
Berhanu M. Abegaz a , O. M. Shetonde a , G.D.W.E.Kapche b , W. Mammo c , and K.<br />
Marobela d<br />
a Department of Chemistry, d Department of Biological Sciences, University of<br />
Botswana, Gaborone, Botswana; b Department of Chemistry, Higher Teachers’<br />
Training College, University of Yaounde1, P.O. Box 47, Yaounde Cameroon;<br />
c Department of Chemistry, Addis Ababa University, P.O. Box 1176, Addis Ababa,<br />
Ethiopia.<br />
abeazb@mopipi.ub.bw<br />
We have recently completed a phytochemical investigation of the medicinal plant<br />
known as Rhus pyroides as well as the total synthesis of the major constituents [1, 2,<br />
3]. Our studies have resulted in the isolation of two kinds of unique bichalcones: one<br />
set containing an oxygen bridge between the chalcone moieties (1-4); and the<br />
second set (5, 6) consisting of two directly linked chalcones. The plant has<br />
demonstrated fairly strong biological activities and these properties appear to be<br />
attributed to these novel metabolites. We have therefore undertaken and<br />
successfully achieved the total synthesis of these compounds and their derivatives. A<br />
full investigation of the biological activities of these compounds is currently<br />
underway. We have also completed the investigation of the Moraceous plant,<br />
Morus mesozyga from Cameroon which yielded 13 metabolites of which five were<br />
found to be novel 2-aryl benzofuran derivatives [4]. The structural features of these<br />
metabolites and their significance will be discussed.<br />
References<br />
1. B. Masesane, S. O. Yeboah, J. Liebscher, C. Muegge and B. M. Abegaz. 1999. A<br />
Bichalcone from the twigs of Rhus pyroidesPhytochemistry, 53, 1005-1008.<br />
Kinshasa/Gombe, DR Congo<br />
2
13th NAPRECA SYMPOSIUM BOOK OF ABSTRACTS August 10-14, 2009<br />
2. Ladislaus K. Mdee, Samuel O. Yeboah, and Berhanu M. Abegaz 2003.<br />
Rhuschalcones II-VI, Five New Bichalcones from the Root Bark of Rhus pyroides, J.<br />
Nat. Prod. 66(5) pp 599 – 604.<br />
3. O. M. Shetonde, W. Mammo, M. Bezabih, K. Marobela, d and B. M. Abegaz, Total<br />
Synthesis and anti-protozoal activities of Rhuschalcone VI and derivatives, 2009<br />
manuscript under to be submitted.<br />
4. G.D.W.E.Kapche, C.D. Fozin, J.H. Donfack, G.W. Fotso, D. Amadou, A>k. Tchana,<br />
M. Bezabih, P.F. Moundipa, B.T. Nadjui, B.M. Abeaz, Prenylated arylbenzofuran<br />
derivatives from Morus mesozyia, Phytochemistry, 2009, 70, 216-221.<br />
[PL -2] THE POTENTIAL OF AFRICAN MEDICINAL PLANTS AS<br />
SOURCE OF NEW DRUGS<br />
Kurt Hostetmann<br />
Laboratory of Pharmacognosy and Phytochemistry, School of Pharmaceutical<br />
Sciences, University of Geneva, University of Lausanne, CH-1211 Geneva 4,<br />
Switzerland<br />
Kurt.Hostettman@pharm.unige.ch<br />
The African continent with tropical forests, coastal regions, desertic regions and high<br />
mountains has a very wide biodiversity which is not yet fully exploited. The most<br />
famous plant issued from Africa is without any doubt coffee (various species of the<br />
genus Coffea, Rubiaceae) which is now well-implanted in South America. A couple of<br />
African plants have provided important molecules such as the alkaloids of<br />
Catharanthus roseus (Apocynaceae) used worldwide for the treatment of leukaemia<br />
and various cancers. To fight arthritic pains, extracts of devil’s claw (Harpagophytum<br />
procumbens, Pedaliaceae) are widely used in Europe and are now recognized as<br />
registered drugs and not as food supplements anymore. The same applies for<br />
Umckaloabo (Pelargonium sidoides, Geraniaceae), a plant used in the Zulu traditional<br />
medicine. Extracts of this plant have been introduced with great success in the<br />
Western medicine for the efficient treatment of acute bronchitis and other problems<br />
of the respiratory tract. Hoodia gordonii (Apocynaceae) is used as food supplement<br />
to inhibit appetite. Many other exemples could be cited.<br />
The approach to find new bioactive compounds from higher plants will be described<br />
and illustrated with the search for new antifungal compounds from various African<br />
plants. The potential of these plants is important in the fight against neglected<br />
diseases such as parasitic diseases which still affect millions of people in Africa. In<br />
Kinshasa/Gombe, DR Congo<br />
3
13th NAPRECA SYMPOSIUM BOOK OF ABSTRACTS August 10-14, 2009<br />
Mali, a plant introduced long times ago from Central America, Argemone mexicana<br />
(Papaveraceae) is now used by traditional healers to treat malaria. The<br />
phytochemical investigation of this plant will also be presented.<br />
[PL -3] APPLICATION OF LC-MS AND LC-NMR TECHNIQUES TO THE<br />
IDENTIFICATION OF BIOACTIVE NATURAL PRODUCTS<br />
Karine Ndjoko<br />
[PL -4] ANTHRAQUINONES AND ALKALOIDS –ACETOGENIC, ANTI-<br />
INFECTIVE, AND AXIALLY CHIRAL!<br />
Gerhard Bringmann et al.<br />
Institute of Organic Chemistry, University of Würzburg, Germany<br />
bringman@chemie.uni-wuerzburg.de<br />
Natural products chemistry is a stimulating and future-oriented field of research,<br />
providing new chemical and biological challenges and inspirations, but also new drug<br />
candidates and, thus, new chances to overcome diseases and suffering of mankind.<br />
We pursue natural products chemistry in a broad, multi-disciplinary way, with<br />
analytical, synthetic, biosynthetic, computational, and pharmaceutical facets. This<br />
high degree of interdisciplinarity is, exemplarily, depicted for different classes of<br />
compounds that possess unusual, stereochemically intriguing structures, new or<br />
even unprecedented biosynthetic origins and, in particular, promising bioactivities.<br />
Our strategy to find novel-type compounds is spectroscopy-assisted, rather than<br />
bioactivity-guided, with the structural novelty as the primary search criterion. The<br />
lecture describes the strategy for such an online search for novel-type structures by<br />
HPLC-MS/MS-NMR-CD (in combination with quantum chemical CD calculations), 1,2<br />
exemplarily for different classes of metabolites (see Figure). These involve<br />
acetogenic alkaloids and anthraquinones from plant or marine sources, possessing<br />
unprecedented biosynthetic origins and/or stereochemically intriguing C,C- or C,Naxes<br />
(sp 2 -sp 2 or sp 2 -sp 3 ), which are configurationally stable or semi-stable. 3-5<br />
Kinshasa/Gombe, DR Congo<br />
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13th NAPRECA SYMPOSIUM BOOK OF ABSTRACTS August 10-14, 2009<br />
The work shows the synergy of these interdisciplinary facets of natural products<br />
research in the isolation, structural elucidation (online or offline), biosynthesis,<br />
synthesis, and bioactivity discovery and optimization of natural products.<br />
1. G. Bringmann, T. Bruhn, K. Maksimenka, Y. Hemberger; The Assignment of<br />
Absolute Stereostructures by Quantum Chemical Circular Dichroism<br />
Calculations; Eur. J. Org. Chem. 2009, 17, 2717-2727.<br />
2. G. Bringmann, T.A.M. Gulder, M. Reichert, T. Gulder; The Online Assignment<br />
of the Absolute Configuration of Natural Products: HPLC-CD in Combination<br />
with Quantum Chemical CD Calculations; Chirality 2008, 20, 628- 642.<br />
3. G. Bringmann, B. Abegaz, M. Knauer, J. Mutanyatta; Knipholone and related<br />
4-phenylanthraquinones: structurally, pharmacologically, and biosynthetically<br />
remarkable natural products; Nat. Prod. Rep. 2008, 25, 696-718.<br />
4. G. Bringmann, J. Mutanyatta-Comar, K. Maksimenka, J. M. Wanjohi, M.<br />
Heydenreich, R. Brun, W.E.G. Müller, M.G. Peter, J. O. Midiwo, A. Yenesew;<br />
Joziknipholones A and B, the First Dimeric Phenylanthraquinones, from the<br />
Roots of Bulbine frutescens; Chem. Eur. J. 2008, 14, 1420-1429.<br />
5. G. Bringmann, I. Kajahn, M. Reichert, S.E.H. Pedersen, J.H. Faber, T. Gulder, R.<br />
Brun, S.B. Christensen, A. Ponte- Sucre, H. Moll, G. Heubl, V. Mudogo;<br />
Ancistrocladinium A and B, the First N,C-Coupled<br />
Naphthyldihydroisoquinoline Alkaloids, from a Congolese Ancistrocladus<br />
Species; J. Org. Chem. 2006, 71, 9348-9356.<br />
Keywords: Naphthylisoquinoline alkaloids; anthraquinones; atropisomerism;<br />
synthesis; biosynthesis; anti-infective activity<br />
Schrott:<br />
G. Bringmann, A. Irmer; Acetogenic Anthraquinones: Biosynthetic Convergence and<br />
Chemical Evidence of Enzymatic Cooperation in Nature; Phytochem. Rev. 2008, 7,<br />
499-511.<br />
Kinshasa/Gombe, DR Congo<br />
5
13th NAPRECA SYMPOSIUM BOOK OF ABSTRACTS August 10-14, 2009<br />
[PL -5] OPTIMISING YIELDS AND QUALITY OF TEA IN DIFFERENT<br />
LOCATIONS<br />
P. Okinda Owuor<br />
Department of Chemistry, Maseno University,<br />
Private Bag, Maseno 40105, Kenya<br />
owuorpo@africaonline.co.ke<br />
Tea (Camellia sinensis (L)) is grown under tropical and sub-tropical environments<br />
with large variations in climatic conditions resulting in yields and quality differences.<br />
These differences are attributed changes to soil types, altitudes, solar radiation,<br />
rainfall, seasonal conditions and agronomic in-puts. Further away from the equator,<br />
the seasonal variations are much larger than close to the equator. Consequently,<br />
seasonal yield distributions and quality become more variable as distance from the<br />
equator increases. Close to the equator, growth is more uniform, and it was assumed<br />
growth and leaf chemical composition which control yields and quality, respectively,<br />
do not vary much. As a result, agronomic inputs and processing technology<br />
recommendations have been uniform to a large extent. But recent research have<br />
demonstrated large variations in quality and yields in the different environments<br />
within East and Central African tea growing areas implying need for region specific<br />
agronomic recommendations and processing technologies. This report reviews<br />
results of studies to establish the variations in yields and quality of black tea in<br />
different locations within the region due to agronomic inputs and processing<br />
technologies. For same cultivars grown in different locations, there were differences<br />
in yields and quality suggesting variations in growth pattern and differences in the<br />
chemical composition of the same cultivar in the different regions. Growth and green<br />
leaf chemical composition resulting in differences in yields and black tea quality were<br />
observed in the same cultivars grown at different altitudes even within a 10 km<br />
radius at different altitudes. Yields declined but quality improved with rise in<br />
altitude. When the same cultivar was subjected to different rates on nitrogenous<br />
fertiliser and plucking intervals, response depended on the location of growth.<br />
Indeed, the optimal yields and quality were obtained at different nitrogenous<br />
fertiliser rates and plucking intervals demonstrating the growth and green leaf<br />
chemical composition varied with location of production. Fermentation is a critical<br />
stage in black tea processing as most noticeable chemical transformations occur at<br />
this stage. Using same cultivar grown in Kenya and Malawi, and processed under<br />
identical conditions, large differences in the resultant black tea chemical<br />
composition hence quality were recorded, at the same fermentation duration.<br />
Indeed, optimal fermentation durations in the same cultivars were arrived at after<br />
same fermentation duration in the two countries. Generally, optimal fermentation<br />
durations were much shorter in Malawi than in Kenya under identical fermentation<br />
Kinshasa/Gombe, DR Congo<br />
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13th NAPRECA SYMPOSIUM BOOK OF ABSTRACTS August 10-14, 2009<br />
conditions. The data suggest that the there is need to develop region specific<br />
agronomic inputs, cultivars and processing technologies. Adoption of agronomic<br />
inputs and processing technologies recommendations develop away from the<br />
farming area may be subjecting some tea growers to perpetual low production<br />
and/or production of low quality black tea. This subjects the producers to continuous<br />
poverty.<br />
Keywords<br />
Black tea, Camellia sinensis, environment, genotypes, cultural and agronomic<br />
practices, processing technologies, yields, quality.<br />
[PL -6] DRUG DISCOVERY AT IMRA: RECENT RESULTS AND WAY<br />
FORWARD<br />
Philippe Rasoanaivo 1 , Solofoniaina Razafimahefa 1 , Benoît Rasolondratovo 2 , Jarl<br />
Wikberg 3<br />
1<br />
Institut Malgache de Recherches Appliquées, BP 3833; 101-Antananarivo,<br />
Madagascar, rafita@moov.mg<br />
2<br />
Département de Chimie, Faculté des Sciences, Université de Toliara, BP 304, 601<br />
Toliara, Madagascar ; rasolobe@moov.mg<br />
3<br />
Department of Pharmaceutical Biosciences, Uppsala University, Box 591,<br />
Biomedicum, SE 751 24 Uppsala, Sweden; jarl.wikberg@farmbio.uu.se<br />
One of main activities of the Institut Malgache de Recherches Appliquées (acronym<br />
IMRA) is drug discovery which is focussed on tropical diseases (malaria and<br />
chikungunya) and diseases of ageing (diabetes of ageing, erectile dysfunction in old<br />
men, and memory and cognitive dysfunction). The presentation will be focussed on<br />
erectile dysfunction. The work has been carried out in collaboration with Uppsala<br />
University. The arrival of the synthetic drug Sildenafil citrate and its chemical<br />
analogues has captivated the public imagination, and has drawn tremendous<br />
medical attention to the concept of sex male dysfunction. A search of PubMed, using<br />
the search term erectile dysfunction (ED) and comparing the results for the period<br />
1961-1997 with that of 1998-2009, 1997 being the year when sildenafil was<br />
launched, reveals a dramatic 15-fold steep increase in frequency of papers, and this<br />
includes papers in ‘‘high impact factor’’ peer-reviewed journals. In response to<br />
recent advances in synthetic medication, there has been a recent growing interest<br />
towards the search of traditionally herbs, which are being constantly claimed for the<br />
treatment of erectile and libido dysfunction. At this point, Neobegua mahafalensis<br />
(Meliaceae) is used in the South and West parts of Madagascar for the treatment of<br />
erectile dysfunction in old men. We used the physiology-based approach to<br />
Kinshasa/Gombe, DR Congo<br />
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13th NAPRECA SYMPOSIUM BOOK OF ABSTRACTS August 10-14, 2009<br />
demonstrate activities, and the mating behaviour test to assess the efficacy of<br />
different extracts from the species. Bioassay-guided fractionation led to the isolation<br />
of three pharmaco-active constituents as limonoids with unprecedented structures<br />
[1]. They were active even at very low doses, i.e. 0.4 down to 0.04mg/kg, and had<br />
long lasting effects after three days consecutive treatment. Preliminary<br />
investigations suggest that the lippophilic bioactive compounds probably act in the<br />
brain, which precludes any direct vascular effects. Acute and sub-acute toxicological<br />
studies in rodents demonstrated the safety of the active constituents. A<br />
phytomedicine under the trade name Dangitsyl ® was formulated with the active<br />
constituents. Under the regulations regarding the clinical evaluation of traditional<br />
medicine preparations in Madagascar, the clinical efficacy of Dangitsyl was verified<br />
at daily dosages ranging from 10mg to 60mg in preliminary trials. The effect of<br />
Dangitsyl is delayed; most subjects experience a pronounced improvement of sexual<br />
performance on the 4 th or 5 th day following the start of the treatment, and the effect<br />
may persist for several weeks. This corroborates the effects observed in animal<br />
models. The duration of the effect of Dangitsyl is therefore very long (several weeks<br />
to even months), and may vary with patient, and as well as over time with repeated<br />
treatment for the same patient. Several pharmacological studies are underway to<br />
further clarify the mechanism of action of the active limonoids.<br />
References<br />
1. J.E.S. Wikberg, P. Rasoanaivo, S. A. Razafimahefa, B. Rasolondratovo<br />
(4/12/2008) Novel compounds and pharmaceutical preparations. PCT patent<br />
WO 2008/145996 A2.<br />
[PL -7] TERPENOIDS FROM AFRICAN MEDICINAL PLANTS<br />
Dulcie A Mulholland<br />
Division of Chemical Sciences, Faculty of Health and Medical Sciences, University of Surrey,<br />
Guildford, GU27XH, Surrey, United Kingdom<br />
D.Mulholland@surrey.ac.uk<br />
Phytochemical investigations of the genus Croton (Euphorbiaceae) and Phyllanthus<br />
(Phyllanthaceae) have yielded a range of di- and tri-terpenoids. Of particular interest is the<br />
range of novel cembranoids isolated from Croton gratissimus, as shown below, which<br />
include the first example of a cembrane-derived diterpenoid with a C-2, C-12 bond. Croton<br />
sylvaticus has yielded clerodane diterpenoids including a novel lactonized clerodane<br />
furanoditerpenoid and Croton pseudopulchellus has yielded ent-kaurane diterpenoids<br />
Kinshasa/Gombe, DR Congo<br />
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13th NAPRECA SYMPOSIUM BOOK OF ABSTRACTS August 10-14, 2009<br />
including two novel ent-kaur-16-en-19-oic acid derivatives. The variation in diterpenoid<br />
classes isolated from the different Croton species investigated will be discussed.<br />
Cembranoids from Croton gratissimus.<br />
H O<br />
O<br />
H O<br />
H O<br />
O<br />
H<br />
O<br />
O<br />
H<br />
[PL -8] RED HOT COMPOUNDS FROM THE RED HOT POKER<br />
PLANTS, KNIPHOFIA SPECIES<br />
Abiy Yenesew, a Immaculate Achieng a , Meron Gebru, a Matthias Heydenreich, b Martin<br />
G. Peter, b Ermias Dagne, c Michael Knauer d , Gerhard Bringmann d<br />
a<br />
Department of Chemistry, University of Nairobi, PO Box 30197, Nairobi, Kenya<br />
b<br />
Institut für Chemie, Universität Potsdam, PO Box 60 15 53, D-14415 Potsdam,<br />
Germany<br />
c<br />
Department of Chemistry, Addis Ababa University, PO Box 30270, Addis Ababa,<br />
Ethiopia<br />
d<br />
Institut für Organische Chemie, Universität Würzburg, Am Hubland, D-97074<br />
Würzburg,Germany<br />
ayenesew@uonbi.ac.ke<br />
Knipholone, the first 4-arylanthraquinone was discovered from the stem of Kniphofia<br />
foliosa (Asphodelaceae) in 1984 [1]. Since then a number of 4-arylanthraquinones<br />
including knipholone anthrone have been isolated from this plant [2, 3] and other<br />
members of the Asphodelaceae, namely from Bulbine [4] and from Bulbinela species<br />
[5]. Compounds belonging to this new class of anthraquinones have rotationally<br />
hindered biaryl linkages. The absolute configuration of knipholone and the other<br />
members was established by the use of advanced quantum chemical CD calculations<br />
[6]. Recently the first dimeric arylanthraquinones, named joziknipholones A and B,<br />
have been discovered from the roots of Bulbine frutescens [7]. We have now<br />
reinvestigated Kniphofia foliosa and identified joziknipholone A and other<br />
anthraquinones. More significantly, we have discovered an unprecedented<br />
tetrameric phenylanthraquinone, named jozi-joziknipholone. The structures and<br />
antiprotozoal activities of these compounds will be discussed.<br />
H<br />
HO<br />
O<br />
H<br />
H<br />
HO<br />
HO<br />
O<br />
Kinshasa/Gombe, DR Congo<br />
OH<br />
9
13th NAPRECA SYMPOSIUM BOOK OF ABSTRACTS August 10-14, 2009<br />
References<br />
1. Dagne, E.; Steglich, W. Phytochemistry 1984, 23, 1729-1731.<br />
2. Dagne, E.; Yenesew, A. Phytochemistry 1993, 34, 1440-1441.<br />
3. Yenesew, A.; Dagne, E.; Müller, M.; Steglich, W. Phytochemistry 1994, 37, 525-<br />
528.<br />
4. Kuroda, M.; Mimaki, Y.; Sakagami, H.; Sashida, Y. J. Nat. Prod. 2003, 66, 895-897.<br />
5. Mutanyatta, J.; Bezabih, M.; Abegaz, B. M.; Dreyer, M.; Brun, R., Kocher, N.;<br />
Bringmann, G. Tetrahedron 2005, 61, 8575-8484.<br />
6. Bringmann, G.; Maksimenka, K.; Mutanyatta-Comar, J.; Knauer, M.; Bruhn, T.<br />
Tetrahedron 2007, 63, 9810-9824.<br />
7. Bringmann, G.; Mutanyatta-Comar, J.; Maksimenka, K.; Wanjohi, J.M.;<br />
Heydenreich, M.; Brun, R.; Müller, W.E.G.; Peter, M.G.; Midiwo, J.O.; Yenesew,<br />
A. Chem. Eur. J. 2008, 14, 1420-1429.<br />
[PL -9] LIFETIME OF NATURAL PRODUCTS<br />
Joe Conolly<br />
Scotland, UK<br />
joec@chem.gla.ac.uk<br />
In almost fifty years of natural product research I have met a lot of very nice people<br />
and a lot of very nice compounds. In my talk I want to look back and to highlight<br />
some of the major changes I have seen over the years. Then I shall discuss some of<br />
the compounds isolated by my Cameroon colleagues in their quest for anti-malarial<br />
activity. Finally I shall mention some of my favorite compounds from other parts of<br />
the world.<br />
Kinshasa/Gombe, DR Congo<br />
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13th NAPRECA SYMPOSIUM BOOK OF ABSTRACTS August 10-14, 2009<br />
[PL -10] QUALITY CONTROL OF NATURAL PRODUCTS<br />
Ermias Dagne<br />
African Laboratory for Natural Products (ALNAP), Department of Chemistry,<br />
Addis Ababa University, P.O. Box 30270, Addis Ababa Ethiopia. Fax: 251 111<br />
239468.<br />
edagne@ethionet.et<br />
The worldwide demand for high quality, safe, effective, and clean natural plant<br />
products has grown significantly in recent years. Although there is rich heritage in<br />
the use of medicinal plants in Africa, not much economic benefit has been derived<br />
from this area despite the rapidly expanding international market.<br />
In the past, herbs and essential oil bearing plants were largely harvested from the<br />
wild and brought to the market without questions being asked about their origin,<br />
botanical identity, methods of cultivation, safety, efficacy, sustainable harvesting,<br />
loss of genetic diversity resulting from extensive wild harvesting etc. Botanical<br />
misidentification, inappropriate methods of collection and processing and presence<br />
of pesticide and microbial residues have all negatively contributed to the marketing<br />
of African natural products.<br />
The export of raw plant materials requires product-tracking system for the<br />
cultivation and sustainable harvesting. Processed products, which usually give better<br />
returns, need to be backed by quality control data, which usually require trained<br />
manpower and sophisticated technology, both not readily available in Africa. The<br />
role local and regional universities could play in alleviating the problem of quality<br />
control of natural products cannot be overemphasized.<br />
The main purpose of this talk is to present recent results in quality control of natural<br />
products achieved in our laboratory.<br />
Kinshasa/Gombe, DR Congo<br />
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13th NAPRECA SYMPOSIUM BOOK OF ABSTRACTS August 10-14, 2009<br />
[PL -11] FROM PLANTS TO BIOACTIVE COMPOUNDS<br />
THROUGH THE STUDY OF GREAT APES- ECOLOGY, CHEMISTRY AND<br />
CONSERVATION OF TROPICAL FOREST<br />
Sabrina Krief<br />
Departement Hommes Natures, Sociétés, UMR 7206- Muséum National d’Histoire Naturelle,<br />
57 rue Buffon, 75005 Paris, France- tel: +33 1 40 79 53 37-<br />
krief@mnhn.fr<br />
Tropical forests are being threatened by accelerating rate of forest conversion and<br />
degradation. They contain however 50 to 90 % of the animal and vegetal species and<br />
remain the main source for medicinal products. Of all the primates, 90% live in<br />
tropical forests and one in five is endangered or critically endangered. The unique<br />
habitat of six species of great apes is tropical forests. In the framework of the<br />
partnership between French and Ugandan institutions (Museum National d’Histoire<br />
Naturelle, France- Institut de Chimie des Substances Naturelles, France- Makerere<br />
University, Uganda- Uganda Wildlife University, Uganda) we aim at implementing<br />
the knowledge on phytochemistry and biodiversity of Ugandan plants using<br />
chimpanzees as “guides”. In Kibale National Park, Uganda, we monitor the<br />
chimpanzee (Pan troglodytes schweinfurthii) diet since 1999. Of the 250 plant parts,<br />
some are rarely consumed and have a low nutritive value. We thus explore the<br />
relationship between health and plant selection to target plants and to isolate<br />
bioactive compounds. Several bioactive extracts of plants species eaten by<br />
chimpanzees were investigated some of them leading to novel molecules. Bioguided<br />
fractionation of the leaves’ extract of Trichilia rubescens (Meliaceae) provided new<br />
antiplasmodial limonoids, novel cytotoxic oleanane-type triterpene saponins were<br />
isolated from extract of leaves and bark of Albizia grandibracteata (Fabaceae) and<br />
ten novel cycloartanes triterpenoids from Markhamia platycalyx (Bignoniaceae)<br />
exhibiting antitrypanosomal activities were elucidated. In addition, there is a large<br />
overlap between the ingested plant parts by chimpanzees and those used in<br />
traditional medicine. Studying and preserving the interactions between humans,<br />
animals and flora is of major interest for the human health and the planet welfare in<br />
the future. For this reason, the Association ‘Projet pour la Conservation des Grands<br />
Singes’ in partnership with UNESCO, and MAEE currently conduct a sensitization<br />
programme using kits with 120kg of educative tools in African countries which are<br />
home range of great apes. In Gabon and Uganda, 15 000 kids from 120 schools in<br />
remote areas participated in 2008 to sessions where Apes are ambassadors for<br />
tropical forests. DRC, Congo as well as Cameroun will be soon partners of the<br />
programme through ECOFAC partnership. The motivation of participants for<br />
preserving forests for a sustainable use of their resources as well as Apes survival<br />
greatly increased following the programme. It is the challenge of the seventh species<br />
Kinshasa/Gombe, DR Congo<br />
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13th NAPRECA SYMPOSIUM BOOK OF ABSTRACTS August 10-14, 2009<br />
of Great Apes, present worldwide and threatening the others, human beings, to save<br />
their closest parents, umbrella and keystone species in tropical forests.<br />
[PL -12] CROTON ZAMBESICUS : ISOLATION AND QUANTIFICATION<br />
OF ACTIVE DITERPENES AND STRUCTURE-ACTIVITY RELATIONSHIPS<br />
J. Quetin-Leclercq<br />
UCL- Belgium<br />
Croton zambezicus Muell. Arg. (Euphorbiaceae) (Syn.C. amabilis Muell. Arg., C.<br />
gratissimus Burch.) is a shrub or small tree reaching 10 m in height. It is a Guineo-<br />
Congolese species widespread in Tropical Africa. The leaf decoction is used in Benin<br />
as anti-hypertensive, anti-microbial (urinary infections) and to treat fever associated<br />
with malaria.<br />
The genus Croton is well known for its diterpenoid content and a lot of different<br />
types of diterpenes (phorbol esters, clerodane, labdane, kaurane, trachylobane,<br />
pimarane, etc.) have been isolated from this genus.<br />
There was very little literature concerning the phytochemical content of Croton<br />
zambesicus although this plant is widely used in African traditional medicine.<br />
Labdane, clerodane and trachylobane diterpenes have been identified in its stem<br />
bark.<br />
During our research, we isolated from the leaves three new trachylobanes, one<br />
isopimarane together with trans- -amyrin and sterols, as well as a mixture of<br />
two diterpenes that inhibits the KCl-induced contraction of male Wistar rat aorta in a<br />
concentration-dependent manner with an IC50 of 1 μg/mL. As the dichloromethane<br />
fraction of the aqueous extract of the leaves show some antihypertensive properties<br />
on mice, we decided to test the diterpenes isolated from the leaves of Croton<br />
zambesicus to evaluate their vasorelaxant activity on Wistar rat aorta. Their<br />
vasorelaxant effect was compared to a series of synthetic trachylobanes on<br />
KCl-induced contractions in order to evaluate the structure-activity relationships.<br />
The cytotoxicity of all these compounds has also been evaluated on HeLa cells as<br />
some trachylobanes were shown to be cytotoxic ant pro-apoptotic.<br />
We showed for the first time the vasorelaxant properties of some pure trachylobane<br />
diterpenes at low concentration (IC50 < 5 µg/mL) on KCl-induced contractions but<br />
none of them have an effect on noradrenaline-induced contractions. We also<br />
observed that a carbonyl group at C-14 associated to a hydroxyl or ketonic function<br />
Kinshasa/Gombe, DR Congo<br />
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13th NAPRECA SYMPOSIUM BOOK OF ABSTRACTS August 10-14, 2009<br />
at C-15 or a carbonyl at C-3 associated to a hydroxymethyl group at C-4 plays an<br />
important role on the vasorelaxant activity of trachylobane diterpenes. We did not<br />
observe a marked effect of the absolute configuration nor of the cleavage of the<br />
C13-C16 cyclopropane bond. Our work also shows that cytotoxic activities of these<br />
diterpenes were not correlated to their vasorelaxant properties.<br />
To quantify these compounds in plants and extracts, a sensitive and accurate<br />
method, combining Soxhlet extraction, solid-phase extraction and capillary gas<br />
chromatography was developed and fully validated for the quantitative<br />
determination of four diterpenes (ent-trachyloban-3β -ol, ent-18-hydroxytrachyloban-3-one,<br />
ent-trachyloban-3-one and isopimara-7,15-dien-3β-ol) in the<br />
leaves of Croton zambesicus.<br />
These results indicate that C. zambesicus leaves contain vasorelaxant diterpenes<br />
which could account, at least partially, for their use to treat hypertension.<br />
Nevertheless, as some of these compounds are cytotoxic, this plant has to be used<br />
with caution and in vivo toxicity studies are needed before this plant could be<br />
recommended in medicine<br />
Schematic SAR model for the vasorelaxant activity of synthetic trachylobane<br />
diterpenes.<br />
References<br />
1. Adjanohoun, E.J et al. Contribution aux Etudes Ethnobotaniques et<br />
Floristiques en République Populaire du Bénin, Vol. 1 (1989).<br />
2. Baccelli C et al., Journal of Naturals Products (2007) 70:910-917<br />
3. Baccelli C et al. Planta Medica (2005) 71:1036-1039<br />
4. Block S et al. Phytochemical Analysis (2005) 16:342-348<br />
Kinshasa/Gombe, DR Congo<br />
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13th NAPRECA SYMPOSIUM BOOK OF ABSTRACTS August 10-14, 2009<br />
5. Block S et al. Anticancer Research (2005) 25:363-368<br />
6. Block S et al. Phytochemistry (2004) 65:1165-1171<br />
7. Block S et al. Planta Medica (2002) 68:647-649<br />
8. Ngadjui, B.T. et al. Phytochemistry (2002) 60: 345–349.<br />
[PL 13] OUR CONGOLESE-GERMAN PARTNERSHIP – A MODEL CASE<br />
FOR OTHER UNIVERSITIES?<br />
Gerhard Bringmann 1 , Virima Mudogo 2 , Dibungi Kalenda 2<br />
1<br />
Institute of Organic Chemistry, University of Würzburg, Germany,<br />
bringman@chemie.uni-wuerzburg.de<br />
2<br />
Université de Kinshasa, mudogov@yahoo.fr, dibungikalenda@daad-alumni.de<br />
The University of Kinshasa (UNIKIN), once a leading university in Subsaharan Africa,<br />
presently suffers from difficult conditions concerning staff age and replacement,<br />
shortage of scientific instrumentation, and insufficient infrastructure in general.<br />
Starting with an intense cooperation on the biodiversity of Congolese plants and the<br />
resulting chemical diversity, and guided by our personal dreams to find solutions to<br />
these difficult problems, we have, together with our friends, built up a multi-faceted<br />
joint program, which consists of essentially 9 'columns':<br />
1. The scientific cooperation as such,<br />
since 1994.<br />
2. A joint university-university<br />
agreement since 2003.<br />
3. Joint lecture courses, seminars, and<br />
excursions.<br />
4. The organization of scientific<br />
symposia, starting with the first<br />
chemistry and pharmacy<br />
symposium in 2005, and, in 2009,<br />
hosting the 13th NAPRECA<br />
symposium.<br />
5. The collection and donation of<br />
scientific books (30 tons, more than<br />
10 further tons en route).<br />
6. A first German-Congolese joint<br />
highschool-highschool project.<br />
7. Likewise just starting: a joint bee<br />
Kinshasa/Gombe, DR Congo<br />
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13th NAPRECA SYMPOSIUM BOOK OF ABSTRACTS August 10-14, 2009<br />
project near the UNIKIN campus.<br />
8. Intense public relations work (i.a.,<br />
at the European Parliament).<br />
9. An excellence-scholarship system (BEBUK), a probably unique, privately financed<br />
program, which will enable young outstanding Congolese students to study<br />
rapidly and efficiently and then to go abroad and come back for an academic<br />
career in Africa. After a first pilot phase I (students of chemistry and pharmacy),<br />
and encouraged by the excellent results of the first 4 scholars, the scholarship<br />
system has been extended to presently 10 students of chemistry, pharmacy,<br />
medicine, laws, and letters, and will be enlarged to all other subjects and<br />
disciplines of the UNIKIN.<br />
In Würzburg (Germany), the joint program is paralleled by the foundation of the<br />
Africa Circle at the University of Würzburg (www.afrikakreis.uni-wuerzburg.de),<br />
which involves scientists from all 10 faculties, by an own NGO ("Support for the<br />
UNIKIN", see logo), and by a research network SFB 630 "Agents against Infectious<br />
Diseases" (www.sfb-630.uni-wuerzburg.de); coordinator of all these institutions is G.<br />
Bringmann.<br />
Keywords: Partnership UNIKIN-UNIWUE; BEBUK; excellence scholarship;<br />
biodiversity; agents against infectious diseases<br />
Speaker: Prof. Dr. Dr. h.c. Gerhard Bringmann, Institut für Organische Chemie, Am<br />
Hubland, 97074 Würzburg, Germany, bringman@chemie.uni-wuerzburg.de<br />
Kinshasa/Gombe, DR Congo<br />
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13th NAPRECA SYMPOSIUM BOOK OF ABSTRACTS August 10-14, 2009<br />
SHORT LECTURES<br />
Kinshasa/Gombe, DR Congo<br />
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13th NAPRECA SYMPOSIUM BOOK OF ABSTRACTS August 10-14, 2009<br />
[SL - 1] ISOLATION OF BIOACTIVE COMPOUNDS FROM THE<br />
TROPICAL LIANA ANCISTROCLADUS CONGOLENSIS<br />
C. Steinert, Asfaw Debella + , K. Messer, G. Bringmann*<br />
Institute of Organic Chemistry, University of Würzburg, Am Hubland, D-97074<br />
Würzburg<br />
+ present address: Ethiopian Health and Nutrition Research Institute, P.O. Box 1242,<br />
Addis Ababa, Ethiopia<br />
The small plant family of the Ancistrocladaceae comprises approximately 18 species<br />
in the palaeotropic regions and, up to now, one single genus named<br />
Ancistrocladus.[1] These lianas feature hooked branches as climbing implements,<br />
and are closely related to the Dioncophyllaceae, tropical lianas with hooked leaves.<br />
The two plant families are used in traditional African and Asian medicine against<br />
dysentery, malaria, African sleeping sickness and leishmaniasis.[2] The bioactivity<br />
results from naphthylisoquinoline alkaloids, an extraordinary class of biaryls, only<br />
found in Ancistrocladaceae and Dioncophyllaceae species. The naphthylisoquinolines<br />
consist of a naphthalene and an isoquinoline moiety, coupled via a biaryl axis. The<br />
axis joins the two molecule halves at various positions and usually is rotationally<br />
hindered. Several naphthylisoquinolines, C,C-coupled ones, like dioncophylline A and<br />
C and ancistrolikokine B, and N,C-coupled ones, like ancistrocladinium B, have shown<br />
in vitro and in vivo activities against pathogens of tropical diseases.<br />
Previous work in our research group on Ancistrocladus congolensis showed the<br />
presence of numerous interesting naphthylisoquinolines and also<br />
naphthylisoquinoline dimers, which are known for their anti-HIV activity. Recently,<br />
the structures of two new compounds, a 7,8’- coupled naphthylisoquinoline and a<br />
dimer, were elucidated, three more are in progress. In addition, the naphthoquinone<br />
malvone A was isolated from plant material for the first time.<br />
Kinshasa/Gombe, DR Congo<br />
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13th NAPRECA SYMPOSIUM BOOK OF ABSTRACTS August 10-14, 2009<br />
References<br />
1. C. M. Taylor, R. E. Gereau, G. M. Walters; Ann. Missouri Bot. Gard. 2005, 92,<br />
360-399.<br />
2. G. François, G. Timperman, W. Eling, L. Aké Assi, J. Holenz, G. Bringmann;<br />
Antimicrob. Agents Chemother. 1997, 41(11), 2533-2539.<br />
[SL - 2] THE BIOSYNTHETIC ORIGIN OF NAPHTHYLISOQUINOLINE<br />
ALKALOIDS<br />
A. Irmer , S. Rüdenauer, J. Mutanyatta-Comar, T. F. Noll, G. Bringmann*<br />
Institute of Organic Chemistry, University of Würzburg, Am Hubland, D-97074<br />
Würzburg<br />
The small palaeotropical plant families Dioncophyllaceae and Ancistrocladaceae<br />
comprise most peculiar lianas. They are the only plants known to produce<br />
naphthylisoquinoline alkaloids, like, e.g., dioncophylline A. These remarkable natural<br />
products are characterized by their unprecedented structures, usually with<br />
rotationally hindered and thus stereogenic biaryl axes, by their promising<br />
antiprotozoal bioactivities (e.g., against Plasmodium, Leishmania, and Trypanosoma<br />
species), and by the unique biosynthetic origin of both, the isoquinoline and the<br />
naphthalene portions, each from six acetate units .[1]<br />
To evidence this acetogenic origin by biosynthetic experiments was possible only by<br />
the establishment of cell cultures of these sensitive tropical lianas, thus providing a<br />
sterile in vitro system that reliably produces the alkaloids. More detailed insight into<br />
the biosynthetic pathway was now gained by the synthesis and incorporation of two<br />
advanced 13C2-labeled isoquinoline precursors .[2] The unambiguous incorporation of<br />
these precursors into dioncophylline A and two other naphthylisoquinolines was<br />
achieved by spectroscopic methods ( 1 H NMR, 13 C NMR, and INADEQUATE<br />
experiments).<br />
Kinshasa/Gombe, DR Congo<br />
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13th NAPRECA SYMPOSIUM BOOK OF ABSTRACTS August 10-14, 2009<br />
The results thus obtained suggest that the initially formed dihydroisoquinoline is<br />
efficiently and highly stereoselectively reduced to the corresponding transconfigured<br />
tetrahydroisoquinoline, which is then further coupled oxidatively with the<br />
naphthalene moiety to form the complete naphthylisoquinoline alkaloids.<br />
1. G. Bringmann, M. Wohlfarth, H. Rischer, M. Grüne, J. Schlauer, Angew. Chem.<br />
Int. Ed. 2000, 39, 1464-1466.<br />
2. G. Bringmann, J. Mutanyatta-Comar, M. Greb, S. Rüdenauer, T. F. Noll, A.<br />
Irmer, Tetrahedron 2007, 63, 1755-1761.<br />
[SL – 3] VASOCONSTRICTOR AND INOTROPIC EFFECTS INDUCED BY<br />
THE ROOT BARK EXTRACTS OF ANTHOCLEISTA SCHWEINFURTHII (GILG)<br />
(GENTIANACEAE)<br />
Nadege Kabamba Ngombe a,b , Dibungi T. Kalenda b , Joelle Quetin-Leclercq a , Nicole<br />
Morel c,<br />
a<br />
Laboratoire de pharmacognosie, Louvain Drug Research Institute, Université<br />
catholique de Louvain, Av.E. Mounier 72, 1200 Bruxelles, Belgium<br />
b<br />
Centre d’Etudes des Substances Naturelles d’Origine Végétale, Université de<br />
Kinshasa<br />
BP202 KIN IX, Kinshasa, Democratic Republic of Congo.<br />
c Laboratoire de physiologie cellulaire, Université catholique de Louvain,<br />
Av.Hipppocrate 55, 1200 Bruxelles, Belgium.<br />
The present study was performed to evaluate the cardiovascular effects of three<br />
extracts from the root bark of A. schweinfurthii (Gilg) positive to kedde reagent<br />
considered as specific for cardiac glycosides. Plant extracts which contains “digital<br />
like” compounds present a possible cardiotoxicity due to inhibition of the Na + ,K +<br />
ATPase pump. Nowadays, there is no evidence of cardio-vascular activity of the<br />
extracts of A. schweinfurthii (Gilg.). This big tree of tropical regions are eaten by<br />
bonobo (Pan paniscus), an endemic pigmee chimpanzee of the Democratic Republic<br />
of Congo and also used in folk medicine to treat several disorders (malaria, tumors,<br />
cancers, venereal diseases, bacterial diseases…). The effects of dichloromethane<br />
soluble fraction of the ethanolic extract (DCMR), cardiac glycoside-rich fraction<br />
(CARDAN) and aqueous extract (AE ) on the vascular responses of isolated rat aorta<br />
and the cardiac functions in isolated frog heart were evaluated. In isolated rat aortic<br />
preparations, the contraction evoked by AE was completely reversed by<br />
phentolamine (1µM), whereas the contractile response to CARDAN was inhibited by<br />
the addition of verapamil (1µM). Effect of DCMR was transient and contraction<br />
relaxed spontaneously. In frog isolated heart, A.schweinfurthii extracts exhibited<br />
Kinshasa/Gombe, DR Congo<br />
20
13th NAPRECA SYMPOSIUM BOOK OF ABSTRACTS August 10-14, 2009<br />
positive inotropic effect in isolated frog heart. The effect of AE and DCMR was<br />
depressed in the presence of propranolol. The inotropic effect of CARDAN was<br />
unaffected by the beta blocker. The present results showed for the first time the<br />
cardiovascular effect of three extracts isolated from A. schweinfurthii (Gilg)<br />
containing cardiac glycosides type compounds as indicated by a positive reaction<br />
with Kedde reagent.<br />
KEY WORDS: Anthocleista schweinfurthii- cardiac glycosides extracts- asoconstrictor<br />
effect-inotropic effect.<br />
[SL - 4] ANTISICKLING ACTIVITY OF JUSTICIA SECUNDA VAHL<br />
P.T. Mpiana, K.N. Ngbolua, M.T. Bokota, T.K. Kasonga, E.K. Atibu, and V. Mudogo<br />
Anthocyanins extracts from some Congolese plants used in traditional medicine<br />
against sickle cell anemia had recently showed antisickling activity in vitro 1,2 Justicia<br />
secunda is one of them. Its use is even advised by some religions congregation to<br />
bypass blood transfusions.<br />
SS erythrocytes treated using anthocyanins extracts of J. secunda indicated the reappearance<br />
of the biconcave shape of erythrocytes with a mean radius value of<br />
3.3±0.3µm similar to that of normal ones. The solubility of Deoxyhemoglobin S<br />
erythrocytes and their osmotic fragility increased upon treatment with anthocyanins<br />
extracts.<br />
These findings suggest that anthocyanins extract play a role in both stabilizing<br />
erythrocyte membrane and inhibiting polymerization of hemoglobin S. This provides<br />
a possible molecular basis for earlier reports on the antisickling properties of<br />
anthocyanins and their use in the management of sickle cell disease.<br />
Key words: Justicia secunda, Antisickling activity, Anthocyanins extracts.<br />
REFERENCES<br />
1. Mpiana PT, Mudogo V, Tshibangu DST, Ngbolua KN, Atibu EK, Kitwa EK,<br />
Kanangila AB, Makelele LK; Activité antifalcémiante et thermodégradation<br />
d’une fraction d’anthocyanes extraits de Zizyphus mucronata; Annales<br />
Africaines de Médecine 2009, 2, N°2, 91-97.<br />
Kinshasa/Gombe, DR Congo<br />
21
13th NAPRECA SYMPOSIUM BOOK OF ABSTRACTS August 10-14, 2009<br />
2. Mpiana PT, Tshibangu DST, Shetonde OM and Ngbolua KN; In vitro<br />
antidrepanocytary activity (anti-sickle cell anaemia) of some Congolese<br />
plants; Phytomed 2007, 14, 192-195.<br />
[SL - 5] HPLC ANALYSIS AND NMR IDENTIFICATION OF HOMOISO-<br />
FLAVONOIDS AND STILBENOIDS FROM THE INTER-BULB SURFACE OF<br />
SCILLA NERVOSA<br />
Merhatibeb Bezabih, Samson O. Famuyiwa and Berhanu M. Abegaz<br />
Department of Chemistry, University of Botswana, P. Bag UB00704, Gaborone,<br />
Botswana<br />
Scilla nervosa (Burch.) Jessop [syn. Scilla regidifolia (Kunth), Schizocarphus nervosus<br />
(Burch.) Van der Merwe] (Hyacinthaceae) is an important traditional medicinal plant<br />
in Southern Africa where it is native to Botswana, Namibia, South Africa and<br />
Swaziland. It is used to treat infections and rheumatic fever. On the other hand it is<br />
also recognized to be poisonous to livestock [1-3].<br />
In Botswana the bulbs of S. nervosa are claimed to enhance female fertility. One will<br />
find the bulbs offered for sale in open markets at bus stations and other public<br />
places in Botswana. Our earlier investigation of the dried and powdered bulbs of S.<br />
nervosa purchased at the Gaborone bus station in Botswana yielded 13<br />
homoisoflavonoids and 3 stilbinoids [4]. Additionally two homoisoflavonoids and<br />
two stilbenoids were reported from whole bulbs of S. nervosa collected in South<br />
Africa [5]. Twenty one isoflavonoids are reported from the genus Scilla.<br />
The yellow inter-bulb deposits from Scilla nervosa were anaylsed by HPLC and found<br />
to contain 19 components. Twelve of the 19 were identified by comparison of Rt<br />
values with those of authentic homoisoflavonoids and stilbenoids, co-elution and by<br />
Kinshasa/Gombe, DR Congo<br />
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13th NAPRECA SYMPOSIUM BOOK OF ABSTRACTS August 10-14, 2009<br />
preparative isolation followed by NMR and MS. Two new homoisoflavonoids, 3-(4hydroxyoxybenzyl)-5,7-dimethoxy-6-hydroxychroman-4-one<br />
and 3-(4methoxybenzyl)-6,7-dimethoxy-5-hydroxychroman-4-one<br />
were also identified.<br />
References<br />
1. Abegaz BM (2002)Novel phenylanthraquinones, isofuranonaphthoquinones,<br />
homoisoflavonoids, and biflavonoids from African plants in the genera<br />
Bulbine, Scilla, Ledebouria, and Rhus, Phytochemistry Reviews 1, 299–310.<br />
2. Kellerman TS, Coetzer JAW, Naude TW (1988). In Plant poisonings and<br />
mycotoxicoses of livestock in Southern Africa (p. 96). Cape Town: Oxford<br />
University Press.<br />
3. Watt J M, Breyer-Brandwijk M G (1962). In Medicinal and poisonous plants of<br />
Southern and Eastern Africa (2nd ed.) (p. 713). Edinburgh: E and S Livingstone<br />
Ltd.<br />
4. Silayo A, Ngadjui BT, Abegaz BM (1999) Homoisoflavonoids and stilbenes from<br />
the bulbs Scilla nervosa subsp. rigigitolla. Phythochemistry, 52, 947-955.<br />
5. Bangani B, Crouch NR, Mulholland DA (1999) Homoisoisoflavanones and<br />
stilbenoids from Scilla nervosa. Phytochemistry, 51, 947-951.<br />
[SL - 6] RADICAL SCAVENGING PRINCIPLES FROM CASSIA<br />
ABBREVIATA BEAREANA HOLMES AND VANGUERIA PARVIFOLIA SOND<br />
& A FACILE PALLADIUM CATALYSED TRANSFER HYDROGENATION<br />
PROTOCOL OF PROCHIRAL ALKENES<br />
Regina N. Bwire 1 Majinda R.T. Runner 2 and Masesane B Ishmael 2<br />
1<br />
Department of Physical Science, Masinde Muliro University of Science and<br />
Technology(MMUST), Box 190, Kakamega – Kenya.<br />
2<br />
Chemistry Department, University of Botswana, Private bag, 00704, Gaborone –<br />
Botswana.<br />
Corresponding Author: Email: nabwire2002@yahoo.com<br />
The extracts and compounds isolated from two medicinal plants in use in Eastern<br />
and Southern Africa were assayed for antioxidant activity. They showed very good to<br />
appreciable activity and this is reported here. Both the rapid TLC analysis and the UV<br />
spectrophotometric method were used to assay these compounds for radical<br />
scavenging activity. A facile stereoselective palladium catalysed transfer<br />
hydrogenation protocol of prochiral alkenes was also developed<br />
Kinshasa/Gombe, DR Congo<br />
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13th NAPRECA SYMPOSIUM BOOK OF ABSTRACTS August 10-14, 2009<br />
Key word index: Cassia abbreviata Beareana Holmes, Vangueria parvifolia Sond,<br />
Radical scavenging, Antioxidants, Stereoselective.<br />
[SL - 7] PHYTOCHEMICAL AND BIOLOGICAL STUDIES OF GEGERIA<br />
ALATA<br />
Randa Babiker a , Rostand Manfouo b , Sakina Yagi a,c , Igbal Choudhary b , Françoise<br />
Chrétien c , Yves Chapleur c , Dominique Laurain-Mattar c<br />
a Department of Botany, Faculty of Science, University of Khartoum, P.O. Box 321,<br />
Sudan. b International Center for Chemical Sciences, HEJ Research Institute of<br />
Chemistry, University of Karachi, Karachi, Pakistan, c Groupe S.U.C.R.E.S., UMR 7565<br />
CNRS-Nancy-Université, BP 70239,54506 Nancy-Vandoeuvre, France<br />
Plants form the main ingredients of medicines in traditional systems of healing and<br />
have been the source of inspiration for several major pharmaceutical drugs. Gegeria<br />
alata (DC), Oliv & Hiern (Asteraceae) has been used as traditional medicine for many<br />
applications such as epilepsy, spasms, pneumonia and rheumatism 1 . Also, the whole<br />
plant is used as insecticidal and in food as spices. Repeated column chromatography<br />
of the chloroform extract of the roots of G. alata yielded two new sesquiterpene<br />
lactones [1&2] together with the known Geigerane (sesquiterpene lactone) and<br />
Flavonol: 7-O- methylkaempferol. Six components were detected in the oil of G.<br />
alata roots representing 99% of the total oil.<br />
Extracts from the leaves and roots were screened for different biological activities<br />
such as antibacterial, antifungal, cytotoxicity, and insecticidal activities. All extracts<br />
of the roots and the ethanol extract of the leaves showed significant activity against<br />
S. aureus and K. pneumonia. The former bacterium was also susceptible to<br />
chloroform extract of leaves. Also the ethanol extract of the roots displayed<br />
significant activity against E. coli. The hexane and ethanol extracts of leaves showed<br />
moderate antifungal activity against C. albicans.<br />
The chloroform extract of the roots showed significant insecticidal activity against<br />
Tribolium castaneum and Callosbruchus analis while the volatile oil exhibited only a<br />
significant activity against C. analis. The brine shrimp lethality assay showed absence<br />
of any measurable cytotoxicity of the hexane and chloroform extracts of the leaves<br />
whereas, both extracts as well as volatile oil obtained from roots showed significant<br />
cytotoxicity. Thus G. alata, as shown by in-vitro assays, could be a potential source<br />
for natural antibacterial, insecticidal and anticancer agents.<br />
Kinshasa/Gombe, DR Congo<br />
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13th NAPRECA SYMPOSIUM BOOK OF ABSTRACTS August 10-14, 2009<br />
Keywords: Gegeria alata, sesquiterpene lactones, flavonol, biological activity.<br />
Reference<br />
El Ghazali, G.E.B., El Tohami, M.S. & El Egami, A.A.B. 1997. Medicinal plants of Sudan,<br />
Part III, Medicinal plants of the eastern Nuba Mountains. Khartoum Univrsity<br />
Press.<br />
[SL - 8] PHYTOMEDICINE DEVELOPMENT FROM PLANTS OF<br />
RWANDA<br />
Justin N. KABERA, Polycarpe NYETERA<br />
IRST/Research centre in Phytomedicines and Life sciences, Butare- RWANDA<br />
kajust68@yahoo.fr, jkabera@irst.ac.rw<br />
In Rwanda, the first scientific work on the pharmacopoeia and traditional medicine<br />
started in the year 1972, at the National University of Rwanda (UNR), more precisely<br />
within the Faculty of Medicine by a small group of researchers-teachers. In 1975, this<br />
group is reinforced by a few teachers of the Faculty of Science, in particular those<br />
from the Department of Chemistry. In the years 1980, these researchers put in place<br />
the University Research Centre on the Pharmacopoeia and Traditional Medicine<br />
known as CURPHAMETRA. In 1989, this centre became the centre Pharmacopoeia of<br />
the Institute of scientific and technological research (IRST) by law Nr 06/1989 of<br />
March 15, 1989. Very recently, this centre was named “Research Center in<br />
Phytomedicines and Life sciences” (CRP&SV).<br />
Since 1989, several drugs containing plant extracts were developed, components<br />
with new structures were isolated and were given names inspired by the vernacular<br />
names of the plants; such as for example: Idomaïn de Gutenbergia coridifolia<br />
(vernacular name :Idoma).<br />
Kinshasa/Gombe, DR Congo<br />
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13th NAPRECA SYMPOSIUM BOOK OF ABSTRACTS August 10-14, 2009<br />
The studies undertaken on the medicinal plants are mainly based on information<br />
provided by traditional healers during ethno-botanic investigations. First, these<br />
plants are the subject of a botanical study for the exact scientific identification. Then,<br />
the extracts of these plants prepared using various solvents are subjected to a series<br />
of biological and pharmacological tests in order to detect a biological activity. The<br />
plants having revealed a particularly interesting activity are the subject of a chemical<br />
study including isolation, purification and structural identification of active<br />
ingredients having the initially detected biological activity. The isolation of the active<br />
ingredients is generally carried out using various methods of extraction, column and<br />
thin layer chromatography, preparative chromatography and purification by<br />
crystallization. The determination of chemical structures is carried out, in<br />
collaboration with foreign laboratories better equipped than ours, by various<br />
techniques of spectrometry: infra-red (IR), ultraviolet (UV), gas chromatography<br />
coupled with mass spectrometry (GC-MS) and by nuclear magnetic resonance<br />
(NMR). The biological and pharmacological tests are mainly carried out on laboratory<br />
mice, in our “Research Centre in Phytomedicines and Life sciences” (CRP&SV).<br />
Essential oils are extracted by the method of steam distillation. Their chemical<br />
composition is established by gas chromatography coupled with mass spectroscopy.<br />
The antimicrobial activity is tested by the traditional biological methods. The results<br />
of this research led to the manufacture of drugs containing the local plants extracts<br />
and also aroused the interest to continue research because the potentialities are<br />
enormous.<br />
[SL - 9] THE ROLE OF NUTRACEUTICAL-IMPLIED EMPIRICAL<br />
GRADES OF PLANT FOODS IN ELICITING PLANT BIODIVERSITY ON<br />
WOMEN SMALL HOLDER FARMS<br />
AGNES NAMUTEBI*, LEVI. S. M. AKUNDABWENI 1 and JUDITIH KIMIYWE 2<br />
Department of Food Science & Technology, Makerere University, PO Box 7062,<br />
Kampala, Uganda; asnamutebi@agric.mak.ac.ug, asnamutebi@yahoo.co.uk<br />
1 Department of Plant Science and Crop Protection-University of Nairobi, P.O. Box<br />
30197-00100 Nairobi; proflevi@uonbi.ac.ke<br />
2 Department of Food Nutrition and Dietetics, Kenyatta University, P.O. Box 43844,<br />
Nairobi; email: jokimiywe@yahoo.com:<br />
A range of plant biodiversity species, produced for household food and nutrition<br />
security, characterize women small-holder farms of the Lake Victoria Basin. The<br />
Kinshasa/Gombe, DR Congo<br />
26
13th NAPRECA SYMPOSIUM BOOK OF ABSTRACTS August 10-14, 2009<br />
usefulness of nutraceutical-implied grades computed from micro-nutrient mineral<br />
concentrations of plant germplasm in eliciting plant biodiversity is presented. Plant<br />
foods were sampled from women small-holder farms in Iganga (Uganda) and Vihiga<br />
(Kenya) districts. Mineral concentrations were measured using Energy dispersive Xray<br />
fluorescence spectroscopy (XRF), converted to nutrametric scores (1-10) and<br />
grades (low, medium and high). Six minerals were consistently found in a decreasing<br />
concentration order (p>0.05) viz.: potassium, calcium, iron, Zinc, manganese and<br />
strontium and used to elicit plant biodiversity variation on the farms. The<br />
nutrametric grades computed using the If logic function have been coined as units of<br />
biodiversity. A single mineral exhibited a wide plant biodiversity on the farms.<br />
Similarly, a combination of the six minerals exhibited wide plant biodiversity. Plant<br />
foods were from Acanthaceae, Amaranthaceae, Asteraceae, Basellaccae,<br />
Cucurbitaceae, Dioscoreaccae, Moraceae, Musaceae and Solanacea families. The<br />
plant foods captured on these farms with medium to high nutraceutical grades have<br />
been identified for phyto-chemical profiling to further qualify their nutraceutical<br />
value to in order to conserve the seed and share among farmers.<br />
Key words: Biodiversity, Nutraceutical, Small-holder, Mineral<br />
[SL - 10] SYNTHESIS OF METHOXYSTILBENES<br />
Mapitse, R.; Chacha, M.; Home, P.; Masesane, I. B.; Majinda, R. R. T. and Mutisya, D.<br />
Department of Chemistry, University of Botswana, P/Bag UB 00704, Gaborone,<br />
Botswana.<br />
gabaitsr@mopipi.ub.bw<br />
Polyhydroxystilbenes are among the naturally occurring bioactive compounds often<br />
isolated from plant materials. Examples include resveratrol 1 and its analogues. The<br />
observed biological activities range from antibacterial, antifungal and anticancer<br />
properties, to name just a few. Some methoxystilbenes have been found to possess<br />
superior biological activities compared to the polyhydroxy analogues. In some cases<br />
the introduction of the methoxy groups has led to a 100-fold improvement 2 in<br />
biological activity. This paper describes the synthesis of methoxystilbenes using the<br />
Wittig reaction. It was found that the substitution pattern of both the ylide and<br />
aldehyde affected the cis/trans ratio of the stilbene product. Biological activity of the<br />
compounds is currently being investigated.<br />
Kinshasa/Gombe, DR Congo<br />
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13th NAPRECA SYMPOSIUM BOOK OF ABSTRACTS August 10-14, 2009<br />
MeO<br />
CH 2PPh 3 CHO<br />
Br<br />
+<br />
OMe<br />
NaOH<br />
H 2O, rt<br />
References<br />
1. Gosslau, A.; Chen, M.; Ho, Ci-T.; Chen, K. Y., British Journal of Cancer, (2005),<br />
92(3), 513-521.<br />
2. Park, E-U.; Min, H-Y.; Ahn, Y-H.; Bae, C-M.; Pyee, J-H.; Lee, S. K., Bioorganic<br />
and Medicinal Chemistry Letters, (2004), 14, 5895-5898.<br />
[SL - 11] TOTAL SYNTHESIS OF BIARYLCHALCONES: RHUSCHALCONE<br />
VI AND ITS ANALOGUES<br />
MeO<br />
MeO<br />
MeO<br />
Oscar M. Shetonde, a,b Merhatibeb Bezabih, b Wendimagegn Mammo, c Kerstin<br />
Marobela, d and Berhanu M. Abegaz b,*<br />
a On study leave from Department of Chemistry, Universite′ de Kinshasa, P.O.Box:<br />
119, Kinshasa XI, DR Congo, b Department of Chemistry, University of Botswana,<br />
P/B 00704, Gaborone, Botswana. c Department of Chemistry, Addis-Ababa University,<br />
P.O.Box: 1176, Addis-Ababa, Ethiopia. d Department of Biological Sciences, University<br />
of Botswana, P/B 00704, Gaborone, Botswana.<br />
Rhus pyroides Burch. (Anacardiaceae) is a shrub to a medium-sized tree widely<br />
distributed in the eastern part of Botswana and South Africa, and is used against<br />
epilepsy in traditional medicine. 1,2 R. pyroides is an exceptionally rich source of<br />
bioactive bichalcones with novel structural characteristics. 1 Rhuschalcone VI (1) is a<br />
naturally occurring biarylchalcone composed of two molecules of isoliquiritigenin (2).<br />
The natural material was reported for the first time by Mdee et al. 1 from the root<br />
bark of R. pyroides and was shown to have a strong anti-plasmodial activity and a<br />
moderate antiproliferative activity against two colorectal cancer cells. 1 However, the<br />
quantities obtained from natural sources were limited, and it is remarkable that<br />
+<br />
Kinshasa/Gombe, DR Congo<br />
OMe<br />
28
13th NAPRECA SYMPOSIUM BOOK OF ABSTRACTS August 10-14, 2009<br />
whereas a number of flavonoids have been employed in Suzuki reactions, 3 the use of<br />
chalcones and the synthesis of any biaryl-type Rhuschalcones has not yet been<br />
reported. In order to provide ready access to sufficient quantities of material for<br />
more complete biological studies, as well as a general route for the preparation of<br />
Rhuschalcone VI and its structural analogues, the total synthesis of Rhuschalcone VI<br />
has been achieved starting from simple and available resorcinol and 4hydroxybenzaldehyde.<br />
Since a previous report 1 on Rhuschalcone VI has shown that it possesses interesting<br />
biological activities, unnatural Rhuschalcone VI analogues may show similar and/or<br />
other pharmacological activities, which would warrant additional investigation.<br />
Within this context, and in order to demonstrate the applicability of our strategy, we<br />
undertook and successfully completed the preparation of a few such Rhuschalcone<br />
VI analogues that would be of value in SAR studies. The first total syntheses of eight<br />
Rhuschalcone VI-type bichalcones were achieved, indicating that the general<br />
methodology developed by our group is of practical use in the syntheses of more<br />
congeners carrying the same carbon-framework and the creation of biologically<br />
more potent substances. The lecture will describe our strategy, which involves the<br />
solvent-free Aldol syntheses of chalcones, and the first time use of the Suzuki-<br />
Miyaura coupling reaction in the synthesis of bichalcones.<br />
Key words: Synthesis, Rhuschalcone VI, Biarylchalcones, Suzuki-Miyaura reaction.<br />
1. Mdee, L.K.; Yeboah, S.O.; Abegaz, B.M. J. Nat. Prod. 2003, 66, 599-604.<br />
2. Svenningsen, A.B.; Madsen, K.D.; Liljefors, T.; Stafford, G.I.; Staden, J.V.;<br />
Jäger, A.K. J. Ethnopharmacology. 2006, 103, 276-280.<br />
3. Chen, J.; Chang, H.W.; Kim, H.P.; Park, H. Bioorg. Med. Chem. Lett. 2006, 16,<br />
2373-2375.<br />
Kinshasa/Gombe, DR Congo<br />
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13th NAPRECA SYMPOSIUM BOOK OF ABSTRACTS August 10-14, 2009<br />
[SL - 12] BIOACTIVE EXTRACTS AND COMPOUNDS FROM SOME<br />
GARCINIA SPECIES GROWING IN TANZANIA<br />
Joseph J. Magadula a *, Ester Innocent a , Supinya Tewtrakul b , Kuo-Hsiung Lee c<br />
a<br />
Institute of Traditional Medicine, Muhimbili University of Health and Allied Sciences,<br />
P.O. Box 65001, Dar es salaam, Tanzania<br />
b<br />
Department of Pharmacognosy and Pharmaceutical Botany, Faculty of<br />
Pharmaceutical Sciences, Prince of Songkla University, Hat-Yai, Songkhla, 90112,<br />
Thailand<br />
c<br />
Natural Products Laboratory, School of Pharmacy, University of North Carolina,<br />
Chapel Hill, North Carolina 27599, USA<br />
The genus Garcinia is a member of the Clusiaceae (Gutiferae) family that comprises<br />
of plant species growing mainly in tropical Africa and Southeast Asia 1 . Trees or<br />
shrubs of this genus usually produce yellow resin of medicinal importance while<br />
fruits of most species of the genus Garcinia are edible. Phytochemically, the genus is<br />
well known to contain prenylated xanthones 2 , flavonoids 3 , isoprenylated<br />
benzophenones 4 and triterpenoids 5 .<br />
In our continued efforts to search for novel and bioactive compounds from the<br />
genus Garcinia, we recently investigated 17 crude extracts from 9 Garcinia species<br />
growing in Tanzania for their potential against 4 human cancer cell lines, HIV-1<br />
protease inhibitors, antioxidants and antimicrobial activities. Furthermore,<br />
phytochemical studies on the stem bark of Garcinia semseii gave three novel<br />
isoprenylated benzophenones (1-3) while from the root barks of Garcinia edulis and<br />
Garcinia volkensis, three bioactive prenylated xanthones (4-6) were isolated. The<br />
results for biological activities exhibited by crude extracts and compounds together<br />
with structure elucidation of new compounds will be presented and discussed.<br />
References<br />
1. Perry, LM, Metzger, J (Eds.), 1980. Medicinal Plants of East and South-East<br />
Asia. MIT Press, London, p. 175.<br />
2. Yang, NY, Han, QB, Cao, XW, Qiao, CF, Song, JZ, Chen, SL, Yang, DJ, H, Xu, HX,<br />
2007. Two new xanthones isolated from the stem bark of Garcinia lancilimba.<br />
Chem. Pharm. Bull. 55, 950–952.<br />
3. Babu, V, Ali, SM, Sultana, S, Ilyas, M, 1988. A biflavonoid from Garcinia<br />
nervosa. Phytochemistry 27, 3332–3335.<br />
4. Oliveira, CMA, Porto, ALM, Biurich, V, Marsaioli, AJ, 1999. Two prenylated<br />
benzophenones from the floral resins of three Clusia species. Phytochemistry<br />
50, 1073–1079.<br />
Kinshasa/Gombe, DR Congo<br />
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13th NAPRECA SYMPOSIUM BOOK OF ABSTRACTS August 10-14, 2009<br />
5. Nyemba, AM, Mpondo, TN, Connolly, JD, Rycroft, DS, 1990. Cycloartane<br />
derivatives from Garcinia lucida. Phytochemistry 29, 994–997.<br />
[SL - 13] ANTHOCYANINS FROM SELECTED PLANT SPECIES IN<br />
UGANDA<br />
Robert Byamukama a , Monica Jordheim b , Bernard Kiremire a and Oyvind Andersen b .<br />
a Chemistry Department, Makerere University, P.O. Box 7062, Kampala, Uganda<br />
b Department of Chemistry, University of Bergen, Allegt. 41, 5007, Bergen, Norway<br />
rbyamukama@chemistry.mak.ac.ug<br />
Anthocyanins comprise a diverse group of intensely coloured pigments responsible<br />
for the appealing and often spectacular orange, red purple and blue colours of many<br />
fruits, vegetables, cereal grains, flowers, leaves, roots and other plant storage<br />
organs. The most common food colorants that have been used worldwide are<br />
synthetic ones some of which are deemed to be carcinogenic. Because of this, the<br />
safety of synthetic colorants has been questioned in the past years, and this has<br />
significantly increased the interest in natural colorants as food colour additives such<br />
as anthocyanins. Today, interest in anthocyanin pigments has also intensified<br />
because of their possible health benefits. Anthocyanins are potent antioxidants and<br />
may be chemoprotective.<br />
This presentation will give the results of anthocyanin analysis (isolation and structure<br />
elucidation) from a number of plants plant species in Uganda including the novel<br />
compounds whose structure has been elucidated (Hippeastrum cultivars, Castor-<br />
Ricinus communis, Acalypha hispida, Rubus Pinnatus, R. Rigidus) from Uganda. The<br />
presentation summarise the following Publications<br />
1. Robert Byamukama, Monica Jordheim, Bernard Kiremire and Øyvind M.<br />
Andersen (2008). New anthocyanins from the stem bark of Castor, Ricinus<br />
communis. Natural Product Communications , 3 (9), 1497-1500.<br />
2. Robert Byamukama, Jane Namukobe and Bernard Kiremire (2009).<br />
Anthocyanins from leaf stalks of cassava (Manihot esculenta Crantz). African<br />
Journal of Pure and Applied Chemistry Vol. 3 (2), 020-025.<br />
3. Robert Byamukama, Bernard T. Kiremire, Øyvind M. Andersen and Andreas<br />
Steigen (2005). Anthocyanins from fruits of Rubus pinnatus and Rubus rigidus.<br />
Journal of Food Composition and Analysis, 18, 599–605.<br />
4. Robert Byamukama, Monica Jordheim, Bernard Kiremire, Jane Namukobe<br />
and Øyvind M. Andersen (2006). Anthocyanins from flowers of Hippeastrum<br />
cultivars. Scientia Horticulturae, 109, 262–266.<br />
Kinshasa/Gombe, DR Congo<br />
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13th NAPRECA SYMPOSIUM BOOK OF ABSTRACTS August 10-14, 2009<br />
5. Bergitte Reiersen, Bernard T. Kiremire, Robert Byamukama and Øyvind M.<br />
Andersen (2003). Anthocyanins acylated with gallic acid from chenille plant,<br />
Acalypha hispida.. Phytochemistry , 64, 867–871.<br />
[SL - 14] AN APPLICATION OF MASS SPECTRA IN NATURAL<br />
PRODUCTS<br />
T. Sivakumar, R.Rajavel, K.Srinivasan,Jagadeeswaran M, Saravanan.R<br />
Nandha college of pharmacy, Perundurai main road, Erode, Tamilnadu, India -<br />
638052<br />
Natural flavonoids, alkaloids, saponins and sesquiterpenoids have been extensively<br />
investigated because of their biological and physiological significances, as well as<br />
their promising clinical uses. It is designed to improve the productivity and quality of<br />
results to facilitate wise decisions for use of MS data. Interpretation of mass<br />
spectrometry (MS) data can help to solve the problems. The successful hyphenation<br />
of LC and MS, which was thought as "the bird wants to marry with fish", has been<br />
conducted widely in natural product sample analysis. The application of mass<br />
spectrometry in the natural health products industry is, however, sparse. Given the<br />
complexity of the chemical composition of these products, the use of mass<br />
spectrometry as a chromatographic detector is essential for the proper identification<br />
and quantification of their bioactive components. It is also important to monitor the<br />
fate of the bioactive components of natural health products during processing, as<br />
processing conditions may modify their structure and activity. Mass spectrometric<br />
evaluations of commercial health food products show that most products are lacking<br />
in quality, indicates that the methods presently used for quality control and<br />
quantitative analysis are not adequate. This paper examines the use of biomolecular<br />
mass spectrometry for analysis of the bioactive components in functional foods,<br />
neutraceuticals, and herbal health products. With the health and safety of<br />
consumers at stake, mass spectrometry should be made mandatory for analysis of<br />
those products.<br />
Keywords: alkaloids, mass spectrometry, natural products<br />
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13th NAPRECA SYMPOSIUM BOOK OF ABSTRACTS August 10-14, 2009<br />
[SL – 15] SCREENING OF ANTIBACTERIAL AND<br />
ANTIFUNGAL ACTIVITIES OF FIFTEEN EXTRACTS FROM ANTHOCLEISTA<br />
SCHWEINFURTHII (GILG.) (GENTIANACEAE)<br />
Nadege Kabamba Ngombe a,b , Erick Francisco Rakotoniriana a , Dibungi T. Kalenda b<br />
and Joelle Quetin-Leclercq a<br />
a<br />
Unité CHAM, Louvain drug research institute, Université catholique de Louvain,<br />
Av.E.Mounier 72, Bruxelles 1200, Belgium<br />
b<br />
Centre d’Etudes des Substances Naturelles d’Origine Végétale,Université de<br />
Kinshasa BP 202 KIN IX, Kinshasa, Democratic Republic of Congo.<br />
Anthocleista schweinfurtii (Gilg) is a common plant of tropical regions, whose<br />
leaves, stem bark and root bark are eaten by bonobo (Pan paniscus), an endemic<br />
pigmee chimpanzee of the Democratic Republic of Congo and also used in folk<br />
medicine to treat several disorders (malaria, tumors, cancers, venereal diseases,<br />
bacterial diseases…). Only few studies on the chemical and biological activities of this<br />
plant have been performed. The development of multiple resistances in human<br />
pathogenic microorganisms to the indiscriminate use of antibiotic drugs commonly<br />
employed in the treatment of infectious diseases, have conducted scientists into<br />
looking for new antimicrobial substances from various sources like medicinal plants.<br />
The screening of plant extracts for antimicrobial activity has shown that higher plants<br />
represent a potential source of new anti-microbial agents. The present study was<br />
conducted to investigate antibacterial and antifungal activities of fifteen extracts<br />
from A.schweinfurtii (Gilg). Inhibition of bacterial growth and fungal growth was<br />
investigated using agar diffusion methods (paper disc method). The microorganisms<br />
used in this study consisted of reference strains of Staphylococcus aureus,<br />
Escherichia coli, Pseudomonas aeruginosa, Klebsilla pneumonie , Klebsiella<br />
oxytocica, Yercinia enterolytica, Enterobacter aerugines and Candida albicans. Most<br />
extracts of Anthocleista Schweinfuthii showed antimicrobial activity against S.aureus<br />
and E.coli and antifungal activity against C. albicans at the concentrations tested. The<br />
least effective were the most polar fractions (EtOAc extracts and aqueous residues)<br />
indicating that most active molecules were lipophilic.<br />
KEY WORDS: Anthocleista schweinfurthii- antifungal activity-antibacterial activity<br />
Kinshasa/Gombe, DR Congo<br />
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13th NAPRECA SYMPOSIUM BOOK OF ABSTRACTS August 10-14, 2009<br />
[SL - 16] ANTIPLASMODIAL -HYDROXYDIHYDROCHALCONE FROM<br />
SEEDPODS OF TEPHROSIA ELATA<br />
Lois M. Muiva a,b , Abiy Yenesew a , Solomon Derese a , Matthias Heydenreich c , Martin G. Peter c ,<br />
Hosea M. Akala d , Norman C. Waters d , Charles Mutai e , Joseph M. Keriko b , Douglas Walsh d<br />
a<br />
Department of Chemistry, University of Nairobi, P. O. Box 30197-00100, Nairobi,<br />
Kenya<br />
b<br />
Department of Chemistry, Jomo Kenyatta University of Agriculture and Technology,<br />
P.O. Box 62000, Nairobi, Kenya<br />
c<br />
Institut für Chemie, Universität Potsdam, PO Box 60 15 53, D-14415 Potsdam,<br />
Germany<br />
d<br />
United States Army Medical Research Unit-Kenya, Walter Reed Project), Kisumu,<br />
MRU 64109, APO, AE 09831-4109, USA<br />
e<br />
Centre of Traditional Medicine, Kenya Medical Research Institute, P.O. Box 54840-<br />
00200, Nairobi, Kenya<br />
sderese@uonbi.ac.ke<br />
Tephrosia species (Leguminosae) in East Africa are used in traditional medicinal<br />
practice to treat infectious diseases. It is estimated that there are between 300 and<br />
400 Tephrosia species, of which some 30 are found in Kenya. The genus Tephrosia is<br />
rich in flavonoids and isoflavonoids including rotenoids. Previous phytochemical<br />
investigation of the roots of T. elata yielded flavanones, a flavone, pterocarpans and<br />
rotenoids.<br />
In this study from the seedpods of Tephrosia elata, a new -hydroxydihydrochalcone<br />
named (S)-elatadihydrochalcone (1) was isolated. In addition, the known flavonoids<br />
obovatachalcone, obovatin, obovatin methyl ether and deguelin were identified. The<br />
structures were determined on the basis of spectroscopic evidence. The crude<br />
extract and the flavonoids obtained from the seedpods of this plant showed<br />
antiplasmodial activities. The literature NMR data on -hydroxydihydrochalcones is<br />
reviewed and the identity of some of the compounds assigned -<br />
hydroxydihydrochalcone skeleton is questioned. These results will be discussed during<br />
the short lecture.<br />
Kinshasa/Gombe, DR Congo<br />
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13th NAPRECA SYMPOSIUM BOOK OF ABSTRACTS August 10-14, 2009<br />
Key Words: Tephrosia elata; Leguminosae; seedpods; (S)-elatadihydrochalcone; βhydroxydihydrochalcone;<br />
Antiplasmodial Activity.<br />
[SL - 17] PHYTOCHEMICAL INVESTIGATION OF SURFACE EXUDATES<br />
OF DODONAEA ANGUSTIFOLIAFOR IN VITRO ANTIPLASMODIAL AND<br />
MOSQUITO LARVICIDAL ACTIVITY<br />
Kerubo, L. O a , Midiwo, J. O a , Derese, S a , Yenesew, A a , Matthias, H b , Peter, M. G b ,<br />
Akala, H. M. c , Eyase, F c , Waters, N. C. c , Kabaru, J d<br />
a Department of Chemistry, Nairobi University, Box 30197-00100, Nairobi, Kenya<br />
b Institut für Chemie, Potsdam Universitat, P Bag 60 15 53, D-14415 Potsdam,<br />
Germany<br />
c<br />
United States Army Medical Research Unit-Kenya, Walter Reed Project, Kisumu,<br />
MRU<br />
64109, APO, AE 09831-4109, USA<br />
d<br />
Department of Zoology, Nairobi University, P Bag 30197-00100, Nairobi, Kenya.<br />
lkerubo@uonbi.ac.ke<br />
Dodonaea angustifolia in study belongs to the family sapindaceae distributed in the<br />
tropical and subtropical regions of the world. Traditionally this plant is used as an<br />
analgesic, laxative, antipyretic, in rheumatism, eczema, and skin ulcers. The most<br />
common secondary metabolites of these plants are terpenoids and flavonoids<br />
usually deposited on the surface of the leaves, and are known to have antioxidant,<br />
antibacterial and antiviral activities. The surface exudes of Dodonaea angustifolia is<br />
up to 12% surface exudates and has yielded seven methylated flavonoids and two<br />
clerodane terpenoids. The surface exudates showed anti-plasmodial activity with<br />
IC50 values of 41.5 3.9 g/ml against chloroquine-sensitive (D6) strain of the P.<br />
falciparum. The crude extract did not show good larvicidal activity, against the larvae<br />
of Aedes aegypti, as its LC50 value was > 60 μg/ml after 24 hours. Most of the<br />
isolated compounds showed moderate anti-plasmodial activity against the D6 strain<br />
of Plasmodium falciparum (Table 1.0). Among the compounds tested for larvicidal<br />
activity against Aedes aegypti; rhamnocitrin (5) and santin (4) showed good dose<br />
dependent activity with an LC50 value of 1.75 and 5.1 g/ml (Table 1.0), respectively,<br />
after 24 hours.<br />
In this presentation the chemistry, antiplasmodial and mosquito larvicidal activity of<br />
some isolated compounds will be discussed.<br />
Kinshasa/Gombe, DR Congo<br />
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13th NAPRECA SYMPOSIUM BOOK OF ABSTRACTS August 10-14, 2009<br />
Keywords: Dodonaea angustifolia, surface exudates, in vitro antiplasmodial,<br />
mosquito larvicide.<br />
Kinshasa/Gombe, DR Congo<br />
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13th NAPRECA SYMPOSIUM BOOK OF ABSTRACTS August 10-14, 2009<br />
[SL - 18] THE ROLE OF NATURAL PLANT PROD UCTS AS<br />
MOD ULATORS OF DRUG EFFLUX IN PATHOGENIC<br />
MICROBES<br />
Rumbidzai Mangoyi, Sungai Mazando, Tariro Chitemerere, Elaine Chirisa, Theresa<br />
Chimponda and Stanley Mukanganyama<br />
Biomolecular Interactions Analyses, Department of Biochemistry, University of<br />
Zimbabwe, Box MP 167, Mount Pleasant, Harare, Zimbabwe. Email:<br />
smukanganyama@medic.uz.ac.zw<br />
The success of infectious disease chemotherapy has been dimmed ever since the<br />
dawn of the antimicrobial drug era because of the anti-infective resistance.<br />
Numerous diseases caused by microorganisms have become difficult to treat<br />
including microorganisms responsible for severe infections in hospitalized patients,<br />
food borne pathogens, and sexually transmitted pathogens are resistant to most<br />
available antimicrobial drugs. Among the mechanisms of drug resistance observed<br />
clinically, enhanced drug efflux from the pathogenic organisms has been noted to<br />
play a significant role. Among these drug efflux pumps are ATP-binding cassette<br />
(ABC) family which is found in most microorganisms. Several studies now show a<br />
common cause of high-level drug efflux in clinical isolates of pathogenic organisms<br />
and this is correlated to the over-expression of drug efflux proteins. Efflux pumps<br />
can be specific for a class of antibiotics or responsible for multidrug resistance. They<br />
are attractive antibacterial targets and co-administration of an efflux pump inhibitor<br />
(EPI) with an antibiotic can potentially be used to modulate or enhance the effects of<br />
the antibiotic. The existence of every class of the five existing families of efflux<br />
pumps has been demonstrated in Mycobacterium tuberculosis, Candida albicans,<br />
Escherichia coli and other bacterial species. Using Mycobacterium aurum, Candida<br />
albicans and several bacterial species, we have investigated the role of plant extracts<br />
in the efflux of ciprofloxacin (CIP) or Rhodamine 6G (R6G) from these cells. The<br />
study was performed to set up both ciprofloxacin efflux assay and Rhodamine 6G<br />
efflux assay in Mycobacterium aurum, Candida albicans, E. coli for testing plant<br />
natural compounds as efflux pump inhibitors (EPIs). After determining the MICs and<br />
MBCs for the putative EPIs, they were tested for their effects as inhibitors of the<br />
efflux pumps. Our results show the both compounds (CIP and R6G) are pumped out<br />
from these cells via an ATP-dependent pathway. The efflux of ciprofloxacin from C.<br />
albicans was inhibited by standard efflux inhibitors such as reserpine, cccp and<br />
verapamil. Several plant extracts (Syzigium cordatum, Cussonia natalensis, and<br />
Combretum zeyhrii) were shown to modulate the effects of these pumps in Candida<br />
albicans. Further work is being carried out on to assess the effects of plant extracts<br />
on the efflux of drugs from the other model organisms such as S. aureus, E. coli, C.<br />
Kinshasa/Gombe, DR Congo<br />
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13th NAPRECA SYMPOSIUM BOOK OF ABSTRACTS August 10-14, 2009<br />
glutamicum, P. aeruginosa, M. aurum and Bacillus species. This study provides<br />
evidence for the role of plant compounds not just as inhibitors of growth but also as<br />
modulators of drug efflux from the cells and this may provide an additional<br />
mechanism for the action of natural plant compounds as anti-infective agents.<br />
[SL - 19] NUTRI-MEDICINAL PLANTS USAGE IN THE MANAGEMENT<br />
OF IMMUNO-COMPROMISED AILMENTS IN UGANDA<br />
Kamatenesi-Mugisha Maud, Acipa Annabel & Oryem-Origa Hannington<br />
Department of Botany, Makerere University. P.O. Box 7062, Kampala, Uganda.<br />
Tel: 256-772-438905<br />
mkamatenesi@botany.mak.ac.ug<br />
To regard food as medicine is part of cultural heritage. Today, more advanced<br />
scientific research reveals that human health is directly connected to nutrition<br />
(Johns, 2003, Lentini et al., 2007). There is no definitive resource available containing<br />
this information for African food plants. FAO, (2003) observed that wild food plants<br />
have a potential in the mitigation of HIV/AIDS impact, especially among the rural<br />
poor. In Uganda, 80% of mothers use traditional medicine to provide health care for<br />
themselves and children (Kamatenesi et al, 2005, Kamatenesi and Oryem-Origa<br />
2006). For instance, in the treatment of ailments that women suffer especially in<br />
rural areas, herbal medicines are the first line treatment unless the condition<br />
deteriorates then they seek modern health facilities. This study inventoried<br />
nutritional medicinal plants and performed the nutritional analysis of some nutrimedicinal<br />
plants used in most parts of Uganda. The research findings revealed that<br />
vegetables such as Amaranthus graecizans Auct.Non L, Solanum nigrum Acerb. ex.<br />
Dunal, Cleome gynandra L., are rich in nutrients and micronutrients such as iron,<br />
calcium, phosphorus, potassium, beta carotene and vitamin C, proteins and dietary<br />
fibre. These plants were found to be favoured by immuno-compromised people<br />
including pregnant women for immune boosting and restoration of appetite. This<br />
paper will present the value of food plants that double as medicinal plants in health<br />
care delivery in Uganda.<br />
Key words: Nutri-medicinal plants; immune boosting; nutritional analysis; Uganda.<br />
Kinshasa/Gombe, DR Congo<br />
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13th NAPRECA SYMPOSIUM BOOK OF ABSTRACTS August 10-14, 2009<br />
[SL – 20] CHEMISTRY AND BIOLOGICAL EVALUATION OF MORUS<br />
MESOZYGIA AND DORSTENIA SPP (MORACEAE)<br />
B. T. Ngadjui a G.D.W.F. Kapche b , M. –T. Bezabih c and B. M. Abegaz c<br />
a<br />
Department of Organic Chemistry, Faculty of Science, University of Yaounde 1<br />
BP 812, Yaounde, Cameroon,<br />
b<br />
Department of Chemistry, Higher Teachers’ training College, University of Yaoundé<br />
1, P.O Box 47, Yaoundé, Cameroon<br />
c<br />
Department of Chemistry, Faculty of Science, University of Botswana, Private Bag,<br />
0022, Gaborone, Botswana<br />
ngadjuibt@yahoo.fr<br />
The study of natural products is an important area of scientific activity in Cameroon.<br />
This study embraces the disciplines of Taxonomic botany, pharmacology,<br />
pharmacognosy and chemistry. The selection of the plant material for investigation<br />
has been guided by its uses in the traditional medicine. We have been able to isolate<br />
and identified many novel structures and biological properties such as anti-malarial,<br />
anti- inflammatory, antimicrobial. Summary of the recent work on Morus mesozygia,<br />
and Dorstenia ssp (Moraceae) will be presented.<br />
Morus mesozygia<br />
Morus or Mulberry (Moraceae) is a genus of 10-16 species of deciduous trees native<br />
to Warm, Temperate and Subtropical regions of Asia, Africa and the America. Leaves<br />
of Morus species, especially, of M. alba have been an indispensable food source for<br />
silk-worms. Morus mesozygia is a small to medium sized forest tree of Tropical<br />
Africa; its leaves and fruit provide food for Monkey and Chimpanzee[1]. M.<br />
mesozygia is used to cure venereal diseases stomach troubles [1]. Repeated column<br />
chromatography of the trunk bark organic extract yielded several prenylated<br />
arylbensofuran derivatives such as 5-(2,3-dihydroxy-3-methylbuthyl)-2-(3,5dihydroxyphenyl)benzofuran-6-ol<br />
[1].<br />
Dorstenia spp<br />
The genus Dorstenia(Moraceae), represented by about 170 species worldwide,<br />
contains many plants that are used as anti-snakebite, anti-infection and antirheumatism<br />
remedies in the medicinal plant therapy of many countries in Africa,<br />
Central and South America. The genus is now recognized as a rich source of prenyl<br />
and geranyl-substituted coumarins and flavonoids [2]. There is now increasing<br />
interest in the genus Dorstenia; during the last decade close to 40 papers have<br />
appeared dealing with investigations of over 29 Dorstenia species. We have so far<br />
investigated 16 species out of 23 identified in Cameroon. The results of our studies<br />
Kinshasa/Gombe, DR Congo<br />
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13th NAPRECA SYMPOSIUM BOOK OF ABSTRACTS August 10-14, 2009<br />
yielded: triterpenoids, styrenes, coumarins and mainly flavonoids [2]. Eleven<br />
diprenylated flavonoids have so far been isolated from Dorstenia and all of them are<br />
reported from the twigs the twigs of D. mannii. The pharmacological data of this<br />
genus are scanty. Extracts of D. multiradiata show antileishmanial activity.<br />
1. G.W.F. Kapche, C.D. Fozing, J.H. Donfack, G.W. Fotso, D. Amadou,<br />
A.N.Tchana, M.-T. Bezabih, P. moundipa, B.T. Ngadjui, B.M. Abegaz;<br />
Phytochemistry;70,216-221 (2009).<br />
2. Ngadjui, B. T. Abegaz, B.M. “The chemistry and pharmacology of the genus<br />
Dorstenia (Moraceae)” in studies in Natural Products Chemistry (ed. Atta-Ur-<br />
Rahman, Elsevier, vol 29 Bioactive Natural Products (Part J), pp. 761-805<br />
(2003)<br />
[SL – 21] PHYTOCHEMICAL INVESTIGATION OF RESINS FROM<br />
COMMIPHORA HOLTZIANA IN KENYA<br />
Rose Chiteva a,b , Abiy Yenesew b , John Wanjohi b and Ben Chikamai c<br />
a Forest Products Research Center, Karura, Kenya Forestry Research Institute (KEFRI), P.<br />
O. Box 64636, 00620, Nairobi, Kenya ;<br />
b Department of Chemistry, University of Nairobi, P. O Box 30197, Nairobi, Kenya;<br />
c Kenya Forestry Research Institute (KEFRI), P. O. Box 20142, 00200, Nairobi, Kenya<br />
In the antimicrobial analysis, the crude extracts of Commiphora holtziana showed an<br />
appreciable activity against Gram positive (Bacillus pumilis, Bacillus subtilis and<br />
Staphylococcus aureus) and Gram negative (E. coli) bacteria, and the fungus<br />
Sacharamyces cervisiae. A new compound, 11–hydroxyl-γ-muurolene (1) was<br />
isolated and characterized from the hexane extract. In addition, two known<br />
compounds, (1E)-3-methoxy-8,12-epoxygermacra-1,7,10,11-tetraen-6-one (2) and<br />
(1E)-3-methoxy-8,12-epoxygermacra-1,7,10,11-tetraen-6-one (3) were also<br />
identified. Furthermore, a total of 174 compounds were detected by GC – MS<br />
analysis, and some 14 of these were identified by the comparison of their mass<br />
spectra with data available in the GC – MS library. The details of these results will be<br />
presented.<br />
Kinshasa/Gombe, DR Congo<br />
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13th NAPRECA SYMPOSIUM BOOK OF ABSTRACTS August 10-14, 2009<br />
1<br />
OH<br />
CH 3 O<br />
O<br />
2<br />
O<br />
CH 3 O<br />
[SL - 22] PHYTOCHEMISTRY, ANALYTICAL CHEMISTRY AND<br />
MEDICINAL PLANTS: CHALLENGES IN AFRICA<br />
Mathew Muzi Nindi<br />
Department of Chemistry, University of South Africa, P. Box 392, Pretoria, 0003, RSA<br />
Medicinal plants have for a long time played an essential role to a variety of<br />
communities in Africa. It is not surprising that tremendous research on medicinal<br />
plants have been studied extensively by African researchers as well as other<br />
scientists worldwide. The pharmaceutical industry in developed countries has<br />
invested heavily in the development of novel drug entities for the treatment of<br />
disease from large supply banks of compounds for new screens. However, drug<br />
development through natural product research is challenging and requires a multidisciplinary<br />
approach that would include expertise in phytochemistry and analytical<br />
chemistry. There is a need for analytical chemists to play a role in the isolation,<br />
sample pre-treatment, characterization and quantification of isolated compounds.<br />
Elimination of problematic common natural products such as saponins, tannins, from<br />
plant extracts prior to characterization, quantification and testing using biological<br />
screening procedures require an analytical approach. The partnership of analytical<br />
chemistry and phytochemistry should lead to providing the missing analytical data<br />
such as percentage composition of active metabolites present in plants. Such<br />
information is invaluable especially in biologically active extracts that have<br />
demonstrated reduced activities when tested as pure components.<br />
The presentation would review the currently available technology that could be used<br />
in the phytochemistry research of natural products. Examples will be given of some<br />
of the work that we have already done. The challenges faced by African scientists in<br />
this area of research will also be reviewed.<br />
3<br />
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13th NAPRECA SYMPOSIUM BOOK OF ABSTRACTS August 10-14, 2009<br />
[SL - 23] TRYPANOSOMIASIS AND AFRICAN INDIGENOUS<br />
KNOWLEDGE<br />
K. B. Kubata<br />
NEPAD/Biosciences eastern and central Africa, Nairobi, Kenya<br />
b.kubata@africabiosciences.org<br />
Lipid mediators (Prostaglandins, Thromboxane A2, etc.) comprise a family of<br />
structurally related biologically active compounds involved in various symptoms<br />
associated with parasitic diseases. The molecular mechanisms of Lipid mediators<br />
Lipid mediators’ biosynthesis in animals have been studied extensively. Currently,<br />
several lines of evidence link their production with parasitic infections. The author<br />
will discuss Prostaglandins (PGs) production in parasitic protozoa and their roles in<br />
pathogenesis and parasite physiology as well as the recent advances in our<br />
understanding of the enzymology of PG production in various parasites. The author<br />
will also discuss the role of some African tropical plants in the control of parasitic<br />
infections such as trypanosomiasis and malaria.<br />
[SL – 24] ANTIBACTERIAL AND ANTIFUNGAL ACTIVITIES OF CARDIAC<br />
GLYCOSIDES EXTRACT OF ANTHOCLEISTA SCHWEINFURTHII (GILG)<br />
(GENTIANACEAE)<br />
Nadege Kabamba Ngombe a,b , Erick Francisco Rakotoniriana a , Dibungi T. Kalenda b<br />
and Joelle Quetin-Leclercq a *<br />
a<br />
Unité CHAM, Louvain drug research institute, Université catholique de Louvain,<br />
Av.E.Mounier 72, Bruxelles 1200, Belgium<br />
b<br />
Centre d’Etudes des Substances Naturelles d’Origine Végétale,Université de<br />
Kinshasa BP 202 KIN IX, Kinshasa, Democratic Republic of Congo.<br />
Anthocleista schweinfurthii (Gilg) is one of the food plants of Bonobo(Pan paniscus),<br />
an endemic chimpanzee pygmee of the Democratic Republic of Congo. In folk<br />
medicine, this plant is used to treat several disorders (malaria, tumors, cancers,<br />
venereal diseases, bacterial diseases. Little is known about the chemical<br />
compositions or biological activities of Anthocleista schweinfurthii (Gilg).<br />
Phytochemical screening showed that some extracts of this plant were positive to<br />
Kedde reagent, so were likely to contain cardiac glycosides. Cardiac glycosides could<br />
derive from plants, skins and parotid gland of amphibians. They are used as cardiac<br />
stimulant. Few studies on the antibacterial and antifungal activities of cardiac<br />
glycosides have been performed. The present investigation was carried out to<br />
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13th NAPRECA SYMPOSIUM BOOK OF ABSTRACTS August 10-14, 2009<br />
evaluate antibacterial and antifungal activities of cardiac glycoside type compounds<br />
rich-extract (CARDAN) from the root bark of Anthocleista schweinfurthii (Gilg) against<br />
two strains of bacteria (Bacillus substilis and Escherichia coli), the pathogenic fungus<br />
Cladosporium cucumerinum and the pathogenic yeasts Candida albicans. Inhibition<br />
of bacterial and fungal growth was assessed in semi quantitative fashion by<br />
bioautography on TLC plates. CARDAN showed interesting antibacterial activity<br />
against both bacteria when tested at concentration of 50 and 100µg. We observed<br />
no activity of this extract against fungi at the same concentration.<br />
KEY WORDS: Anthocleista schweinfurthii- cardiac glycosides extract- antifungal<br />
activity-antibacterial activity-bioautography<br />
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13th NAPRECA SYMPOSIUM BOOK OF ABSTRACTS August 10-14, 2009<br />
YOUNG SCIENTIS<br />
Kinshasa/Gombe, DR Congo<br />
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13th NAPRECA SYMPOSIUM BOOK OF ABSTRACTS August 10-14, 2009<br />
[YS 1] THE ANTI-PROLIFERATIVE EFFECTS OF PLANT PRODUCTS<br />
ON HUMAN LEUKEMIA CELL LINES JURKAT AND WIL2<br />
Simbiso C.Dumbura 1 , Lesilane. Mampuru 2 and Stanley Mukanganyama 1<br />
1<br />
Biomolecular Interactions Analyses Group ,Department of Biochemistry, University<br />
of Zimbabwe, P.O.MP167 Mount Pleasant, Harare, Zimbabwe<br />
2<br />
Medicinal Plant Research Group, Department of Biochemistry ,Microbiology, and<br />
Biotechnology ,University of Limpopo, Private Bag X1106,Sovenga 0727,South Africa,<br />
sdumbura@science.uz.ac.zw<br />
Background Cancer is a worldwide problem with treatment being undermined by<br />
drug resistance and drug toxicity in patients. With most therapeutic drugs being<br />
derived from plant sources researchers have turned to plants for discovery of less<br />
expensive and less toxic chemotherapeutic compounds that alone or used with<br />
conventional drugs induce apoptosis, inhibit proliferation or increase drug sensitivity<br />
of cancer cells. Plants that are used as traditional medicines are under investigation<br />
to validate claims of disease treatment and test them on other diseases.<br />
Objectives To screen for plant extracts that inhibit proliferation of leukaemia cell<br />
lines Jurkat and Wil 2<br />
Methodology Medicinal plants used in Zimbabwe were screened for their ability to<br />
inhibit cell proliferation as compared to anticancer drug doxorubicin. Methanolic<br />
extracts from 14 plants were screened for ability to inhibit Wil2 and Jurkat cell<br />
growth at concentrations 0, 50,100,250,500 and 1000 µg/mL. Trypan blue assay was<br />
used for cell counting and cell viability determination. Doxorubicin was used as the<br />
positive control at a concetration of 10 µg/ml.<br />
Results and Discussion The 5 most active of the extracts were found to be potent in<br />
this order: Parinari curatellifolia>Aloe forex >Croton >Vernonia adoensis >Euphobia<br />
traculli >Cajanus cajan. The extract from Parinari curatellifolia reduced cell<br />
proliferation by half at a concetration of 50 µg/ml after 3 hours as compared to the<br />
anticancer drug doxorubicin that halved cell proliferation after 5 hours of incubation<br />
in comparison to the control. The extract from Parinari curatellifolia was the most<br />
potent at reducing proliferation of the cell lines. The leaves of this plant are used by<br />
locals for treating stomach ailments and fever. Aloe forex the second most potent is<br />
used locally for treating skin ailments, coughs, liver and spleen diseases<br />
Conclusion. The extracts from Parinari curatellifolia and the other four plants<br />
exhibited anticancer activity and could, therefore, serve as source of active chemical<br />
species that can potentially be used as anti-cancer drug leads.<br />
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13th NAPRECA SYMPOSIUM BOOK OF ABSTRACTS August 10-14, 2009<br />
Key words: Leukemia cell lines, anti-proliferative, medicinal plants, plant extracts,<br />
doxorubicin<br />
[YS -2] ANTIBACTERIAL ACTIVITY OF SELECTED PLANTS FROM<br />
ZIMBABWE<br />
Tariro Chitemerere and Stanley Mukanganyama<br />
Biomolecular Interactions Analyses Laboratory, Department of Biochemistry,<br />
University of Zimbabwe, P.O.MP 167, Mount Pleasant, Harare, Zimbabwe<br />
alisonsiyaz@gmail.com<br />
Background The indiscriminate use of antibiotics has led to the emergence of drug<br />
resistant pathogens. For instance, 90-95 % of methicillin-resistant Staphylococcus<br />
aureus (MRSA) have been reported. The emergence of drug and multidrug resistance<br />
means that bacterial infections that were once easy to treat have now become<br />
difficult to treat as well as expensive because patients stay longer in hospitals. The<br />
search for new antibacterial agents is a matter of urgency to successfully manage<br />
and contr ause of the diversity of chemicals found in plants. Furthermore, ethnomedicinal<br />
use ol bacterial infections and pathogens. Nature is a source of new<br />
antibacterial agents bec of plants has been practiced by many cultural divides the<br />
world over since ancient times. These practices could give leads for the development<br />
of new antibacterials. However, only a small fraction of these chemicals have been<br />
discovered yet with the majority of them still to be exploited.<br />
Objectives The aims of the study were to screen for plant extracts exhibiting<br />
antibacterial activity and to determine extract concentrations that are bactericidal to<br />
five bacterial species: Escherichia coli ATCC 11229, Pseudomonas aeruginosa ATCC<br />
27853, Staphylococcus aureus ATCC 9144, Bacillus subtilis ATCC 6633 and Bacillus<br />
cereus ATCC 11778.<br />
Methodology Seventeen plant extracts selected from Zimbabwe were screened for<br />
antibacterial activity using the disc diffusion assay. Minimum inhibitory<br />
concentrations (MICs) and minimum bactericidal concentrations (MBCs) of top five<br />
potent extracts were determined using the microdilution and agar dilution methods<br />
respectively. Ampicillin was used as a reference antibiotic in all experiments. Serial<br />
two-fold dilution of plant extracts ranged from a concentration of 1000 µg/ml to<br />
1.95 µg/ml.<br />
Results Initial screening by the disc diffusion assay, showed the following to be the<br />
top five most potent plant extracts.<br />
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13th NAPRECA SYMPOSIUM BOOK OF ABSTRACTS August 10-14, 2009<br />
E. Coli ; Callistemon sp > Vernonia adoensis > Parinari curatellifolia > Parinari<br />
curatellifolia> Mangifera indica.<br />
P. aeruginosa; Vernonia adoensis >Callistemon sp > Parinari curatellifolia > Parinari<br />
curatellifolia> Mangifera indica.<br />
S. aureus; Vernonia adoensis >Callistemon sp > Parinari curatellifolia > Parinari<br />
curatellifolia> Faurea sp<br />
B. subtilis; Callistemon sp > Asteraceae family > Vernonia adoensis > Parinari<br />
curatellifolia > Faurea sp> Mangifera indica.<br />
B. cereus; Vernonia adoensis >Callistemon sp > Parinari curatellifolia > Xeroderris<br />
stuhlmannii > Parinari curatellifolia.<br />
These extracts were then used to determine the MIC and MBC.<br />
MIC and MBC results showed that Mangifera indica and Callistemon sp were the<br />
most potent extracts for P. aeruginosa, E. coli and B. subtilis. Callistemon sp and<br />
Vernonia adoensis were the most potent for S. aureus and B. cereus.<br />
Conclusion The most potent extracts among all species of bacteria were Callistemon<br />
sp, Mangifera indica and Vernonia adoensis. The active antibacterial compounds in<br />
these plant species will be isolated using bio-guided fractionation assays. The<br />
extracts from the three species will also be used to determine their effects on the<br />
efflux of ciprofloxacin from the bacterial cells.<br />
Key words: natural plant products, ethno- medicinal, antibacterial, screening,<br />
bioassay<br />
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13th NAPRECA SYMPOSIUM BOOK OF ABSTRACTS August 10-14, 2009<br />
POSTERS<br />
Kinshasa/Gombe, DR Congo<br />
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13th NAPRECA SYMPOSIUM BOOK OF ABSTRACTS August 10-14, 2009<br />
[PS – 1] ABIETANE DITERPENOIDS FROM CLERODENDRUM<br />
ERIOPHYLLUM<br />
Francis Machumi, Abiy Yenesew and Jacob O. Midiwo<br />
Department of Chemistry, University of Nairobi, P.O. Box 30197 (00100), Nairobi,<br />
Kenya<br />
francis.machumi@gmail.com<br />
Clerodendrum eriophyllum is a tree/shrub that grows to a height of about 8m high. It<br />
is widely used in Kenya’s traditional medicine for treatment of fever and malaria. Invitro<br />
anti-plasmodial tests on methanol/dichloromethane (1:1) extract of the roots of<br />
this plant showed activities against chloroquine sensitive (D6) and chloroquine<br />
resistant (W2) clones of Plasmodium falciparum parasites.<br />
Chromatographic separation on the extract, aimed at isolating the anti-plasmodial<br />
constituents, led to isolation of eight abietane diterpenoids, whose structures were<br />
elucidated using spectroscopic methods.<br />
[PS – 2] PURIFICATION OF 2-ARYLBENZOFURANS FROM AFRICAN<br />
MULBERRY MORUS MESOZYGIA (MORACEAE) BY CENTRIFUGAL<br />
PARTITION CHROMATOGRAPHY<br />
Gilbert Deccaux Kapche a , Pierre Waffo-Teguo b , Victor Kuete c , Bonaventure Ngadjui d<br />
and Jean-Michel Mérillon b<br />
a<br />
Department of Chemistry, Higher Teachers’ Training College (ENS), University of<br />
Yaounde I, P.O. Box 47, Yaounde, Cameroon<br />
b<br />
GESVAB, EA 3675, ISVV, UFR des Sciences Pharmaceutiques, Université Victor<br />
Segalen Bordeaux 2, 146 rue Léo Saignat, 33076 Bordeaux Cedex, France<br />
c<br />
Department of Biochemistry, University of Dschang, P.O. Box 67 Dschang,<br />
Cameroon<br />
d<br />
Department of Organic Chemistry, Faculty of Science, University of Yaounde I, P.O.<br />
Box 812, Yaounde, Cameroon<br />
Six 2-aryl benzofurans derivatives were isolated from the twigs of a Cameroonian<br />
medicinal plant Morus mesozygia (Moraceae) in a preparative-scale using centrifugal<br />
partition chromatography (CPC). In this study, we have successfully used the<br />
quaternary Arizona solvent systems (n-heptane-EtOAc-MeOH-water) for the<br />
Kinshasa/Gombe, DR Congo<br />
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13th NAPRECA SYMPOSIUM BOOK OF ABSTRACTS August 10-14, 2009<br />
purification of moracin C (1), moracin M (2), moracin Q (3), moracin R (4), moracin T<br />
(5) and moracin U (6). Their structure was elucidated using MS, 1D and 2D NMR.<br />
Their antimicrobial activity was evaluated, and all non cyclised prenylated<br />
compounds (1, 4, and 5) were found to be active on at least 60 % of the tested<br />
microbial strains.<br />
Key words: Antimicrobial activity, 2-arylbenzofurans, centrifugal partition<br />
chromatography, Moraceae, moracin, Morus mesozygia.<br />
KINETIC STUDY OF THE ANTI-DIABETIC PROPERTIES OF BRYOPHYLLUM<br />
PINNATUM LEAVES<br />
*ARANSIOLA Elizabeth Funmilayo 1 , IWALEWA Ezekiel Olugbenga 2 , DARAMOLA<br />
Michael Olawale 1 , SELUWA Aanuoluwapo Mary 1 and OLUFOWOBI Olugbenga<br />
Oluwaseun 1<br />
1 Department of Chemical Engineering, O.A.U., Ile-Ife. Nigeria<br />
2 Department of Pharmacology, O.A.U., Ile-Ife. Nigeria<br />
Tel: +2348039537535<br />
aransiola4@yahoo.com & earansi@oauife.edu.ng<br />
Diabetes is one of the major degenerative diseases in the world today. Conventional<br />
drugs used for its treatment are expensive and unaffordable by the rural populace.<br />
This work was aimed at studying the anti-diabetic properties of Bryophyllum<br />
pinnatum leaves using animal models. Since albino rats have similar blood to<br />
humans, they were used as model.<br />
The rats were made diabetic by injecting them with glucose to raise their blood<br />
glucose level. Aqueous extract of the leaf was administered on several rats with<br />
dosages of different concentrations.<br />
The measurement of the rats’ blood glucose level after administering the extract<br />
showed significant drop in glucose level to a value close to normal in about 120mins.<br />
These results were competitive with results obtained when a mixture of the extract<br />
and Glibenclamide was administered.<br />
This study revealed that when 200mg/Kg concentration of the extract was used, it<br />
gave a better reduction in the glucose level than the higher concentrations of the<br />
extract. The results also obtained from a combination of Glibenclamide and extract<br />
sample showed large drop in the blood glucose level. This now concludes how the<br />
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13th NAPRECA SYMPOSIUM BOOK OF ABSTRACTS August 10-14, 2009<br />
extract and its combination with existing diabetes drug can lead to better<br />
normalization of the glucose level.<br />
Key words: Anti-diabetics, Bryophyllum pinnatum, Blood glucose level, albino rats<br />
ANIMAL SELF-MEDICATION: A BIO-RATIONAL FOR DRUG DISCOVERY<br />
Michael A. Huffman, Primate Research Institute, Kyoto University<br />
Plant secondary metabolites (PSM) are traditionally viewed as the means by which<br />
plants inhibit or limit damage done to them by herbivores. This stimulated research<br />
into how animals are sometimes able to detoxify PSM in order to utilize the plant’s<br />
nutritional properties. Some herbivorous species also exploit PSM for their curative<br />
value, as humans traditionally do around the world. A growing body of research<br />
shows that primates ingest PSM for positive benefits, in particular for their<br />
therapeutic and passive preventative properties. A growing body of evidence for this<br />
comes from the emerging field of animal self-medication, particularly from the study<br />
of primates. Self-medication primarily take on three forms, ingestion of plants for<br />
their structural barriers to digestion (e.g. silicate) or bioactive / toxic properties and /<br />
or external application of PSMs. African great apes, and chimpanzees in particular,<br />
practice the first two forms in response to parasite infections. A substantial number<br />
of such plant species have been recorded and are also known to be traditionally<br />
utilized by some African cultures for the treatment of similar symptoms / diseases.<br />
New PSM have also been discovered which may have potential use for humans.<br />
Thirteen novel compounds and their biological activities have been discovered from<br />
the investigation of one species alone; Vernonia amygdalina. Other examples exist<br />
from research on a variety of wild and domestic animals species. Traditionally<br />
humans around the world have looked to animals as a source of medicinal wisdom.<br />
In this two pronged approach, natural products chemistry has much to benefit from<br />
the study of animal self-medication.<br />
PHYTOCHEMICAL PROFILE AND MOSQUITO LARVICIDAL ACTIVITIES OF<br />
THREE KOTSCHYA SPECIES.<br />
Innocent E, a* Kaale EA b , Mgeniwaho B b and Mbwambo ZK c<br />
a Department of Biological and Pre-clinical Studies, Institute of Traditional Medicine,<br />
Muhimbili University of Health and Allied Sciences, P.O. Box 65001, Dar es salaam<br />
Kinshasa/Gombe, DR Congo<br />
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13th NAPRECA SYMPOSIUM BOOK OF ABSTRACTS August 10-14, 2009<br />
b<br />
Department of Medicinal Chemistry, School of Pharmacy, Muhimbili University of<br />
Health and Allied Sciences, P.O. Box 65001, Dar es salaam<br />
c<br />
Department of Natural Products Development and Formulation, Institute of<br />
Traditional Medicine, Muhimbili University of Health and Allied Sciences, P.O. Box<br />
65001, Dar es salaam<br />
Due to resistance of mosquito vectors to chemical insecticides previously used, it is<br />
becoming necessary to identify safe, eco-friendly and effective alternative sources of<br />
larvicides in order to reduce mosquito menace. Previous studies have shown that<br />
polar extracts of Kotschya uguenensis show larvicidal & growth disruption<br />
activities of immature stages of Anopheles. In this study, it was hypothesized that,<br />
other Kotschya species may contain the responsible bioactive compounds in varying<br />
amounts. Hence need to compare the chemical profiles of the ethanolic root extracts<br />
of Kotschya uguenensis, K. speciosa and K. strigosa and conduct further studies on<br />
their mosquito larviciding properties. Reverse phase plates (Uniplate-HPTLC-RP8F uv<br />
254) were used for qualitative analysis of the crude extracts. The plates were<br />
developed and placed under a CAMAG TLC scanner 3 controlled by an external<br />
computer equipped with WINCAT software and scanned at UV 360 nm.<br />
Larvicidal assay against Culex quinquefascintus was done according to WHO 1996<br />
protocol. Higher activity was shown for the root extract of K. uguenensis attaining<br />
100% mortality on 4 th day at 500 and 250 g/ml. K. speciosa attained greater effect<br />
(≥ 45%) on 8 th day compared to K. strigosa ( ≤ 35%) especially at 250 g/ml.<br />
Densitometric evaluation revealed a presence of a common peak at RF 0.28 whose<br />
composition in Kotschya uguenensis, K. speciosa, and K. strigosa agreed with the<br />
trend of larvicidal results for the three plant species. This confirmed presence of<br />
similar bioactive compound responsible for larvicidal activity in the three extracts.<br />
However, further studies should be done to isolate, characterize and quantify this<br />
compound to know whether it works alone or in synergism with other compounds<br />
present in the extract.<br />
Key words: Kotshya uguenensis, K. strigosa, K. speciosa, Verbenaceae, Mosquito<br />
Larvicidal activities, HPLTC<br />
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13th NAPRECA SYMPOSIUM BOOK OF ABSTRACTS August 10-14, 2009<br />
ANTI-PARASITIC ACTIVITY AND CYTOTOXICITY OF SELECTED MEDICINAL<br />
PLANTS FROM KENYA<br />
Elizabeth V.M. Kigondu a,b , Geoffrey M. Rukunga b , Joseph M. Keriko c , Willy K. Tonui d ,<br />
Jeremiah W. Gathirwa b , Peter G. Kirira b , Beatrice Irungu b , Johnstone M. Ingonga d ,<br />
Isaiah O. Ndiege e .<br />
a<br />
Institute of Tropical Medicine and Infectious Diseases (ITROMID), P.O. Box 54840,<br />
Nairobi 00200, Kenya<br />
b<br />
Center for Traditional Medicine and Drug Research, Kenya Medical Research<br />
Institute (KEMRI), P.O. Box 54840, Nairobi 00200, Kenya<br />
c<br />
Department of Chemistry, Jomo Kenyatta University of Agriculture and Technology<br />
(JKUAT), P.O. Box 62000, Nairobi 00200, Kenya<br />
d<br />
Center for Biotechnology Research and Development, Kenya Medical Research<br />
Institute, P.O. Box 54840, Nairobi 00200, Kenya<br />
e<br />
Department of Chemistry, Kenyatta University, P.O. Box 43844, Nairobi 00100,<br />
Kenya<br />
Extracts from 6 selected plant species, used as medicinal plants by indigenous local<br />
communities in Kenya, were screened for in vitro anti-plasmodial and antileishmanial<br />
activity, against 2 laboratory-adapted Plasmodium falciparum isolates<br />
(D6, CQ-sensitive and W2, CQ-resistant) and Leishmania major (IDU/KE/83 = NLB-144<br />
strain), respectively. The methanol extract of Suregada zanzibariensis leaves<br />
exhibited good anti-plasmodial activity (IC50 4.66 0.22 and 1.82 0.07µg/ml for D6<br />
and W2, respectively). Similarly, the methanol extracts of Albizia coriaria (IC50<br />
37.83 2.11µg/ml for D6) and Asparagus racemosus (32.63 2.68 and<br />
33.95 2.05µg/ml for D6 and W2, respectively) had moderate anti-plasmodial<br />
activity. Although the leishmanicidal activity of extracts were lower than for<br />
pentostam (80%), reasonable activity was observed for Aloe nyeriensis methanol<br />
(68.4 6.3%), Albizia coriara water (66.7 5.0%), Maytenus putterlickoides methanol<br />
(60.0 6.23%), Asparagus racemosus methanol and water (58.3 8.22 and<br />
56.8 6.58%, respectively), Aloe nyeriensis water (53.3 5.1%) and Acacia tortilis<br />
water (52.9 6.55%) extracts at 1000µg/ml. Leishmania major infected macrophages<br />
treated with methanol extracts of Suregada zanzibariensis and Aloe nyeriensis var<br />
kedongensis and Pentostam ® had infection rates of 28 2.11, 30 1.22 and 40 3.69%,<br />
respectively at 1000µg/ml, indicating better anti-leishmanial activity for the extracts.<br />
Multiplication indices for Leishmania major amastigotes treated with methanol<br />
extracts of Albizia coriaria, Suregada zanzibariensis and Aloe nyeriensis var<br />
kedongensis, aqueous extract of Acacia tortilis and pentosam were 28.5 1.43,<br />
29.4 2.15, 31.1 2.22, 35.9 3.49 and 44.0 3.27%, respectively, at 1000µg/ml,<br />
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13th NAPRECA SYMPOSIUM BOOK OF ABSTRACTS August 10-14, 2009<br />
confirming better anti-leishmanial activity for the extracts. All extracts exhibited very<br />
low cytotoxicity (CC50 >500µg/ml) against human embryonic lung fibroblast (HELF)<br />
cells. The investigations demonstrated the efficacy and safety of some extracts of<br />
plants that are used by rural indigenous communities for the treatment of parasitic<br />
diseases.<br />
EVALUATION OF SOME TANZANIAN PLANT SPECIES AS SOURCES OF<br />
BOTANICAL LARVICIDAL FOR ANOPHELES GAMBIAE GILES S.S<br />
Charles Kihampa 1 , Cosam C. Joseph 2 , Mayunga H.H. Nkunya 2 , Stephen Magesa 3 ,<br />
Ahmed Hassanali 4 , Matthias Heydenreich 5 and Erich Kleinpeter 5<br />
1<br />
School of Environmental Science and Technology, Ardhi University, Tanzania<br />
2 Department of Chemistry, University of Dar es Salaam, Tanzania<br />
3<br />
Amani Research Centre, National Institute for Medical Research, Tanzania<br />
4<br />
International Centre of Insect Physiology and Ecology (ICIPE), Kenya<br />
5 Institut für Chemie, Universität Potsdam, Germany<br />
In many isolated areas of the world indigenous people have historically relied on<br />
locally sourced natural plant-based remedies to kill, repel or prevent biting insects<br />
entering their homes. Although synthetic insecticides ruled the plant protection<br />
scene, their replacement either partially or totally is now considered a necessity<br />
because of the adverse effects associated with their use. This presentation will give<br />
detailed mosquitocidal properties of some Tanzanian plant species. Extracts from<br />
those plant species and different fractions thereof were compared for their<br />
immediate toxicity and longer-term effects on Anopheles gambiae Giles sensu stricto<br />
(Diptera: Culicidae). Larvicidal effects of the extracts appeared to be associated with<br />
components of low polarity extracted by pet ether and chloroform than those of<br />
high polarity extracted by methanol. Farther investigations that are needed and<br />
possible use of the results in terms of development of larval control strategies for<br />
malaria vectors are discussed.<br />
Keywords: Botanical mosquitocides; Anopheles gambiae s.s.; igr activity<br />
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13th NAPRECA SYMPOSIUM BOOK OF ABSTRACTS August 10-14, 2009<br />
UNUSUAL SESQUITERPENE KETONE FOUND IN THE ESSENTIAL OIL OF<br />
CYPERUS DISTANS L. (CYPERACEAE) FROM SOUTH AFRICA<br />
Oladipupo A. Lawal 1 , Adebola O. Oyedeji 1 and Andy R. Opoku 2<br />
1<br />
Department of Chemistry, University of Zululand, KwaDlangezwa 3886, South<br />
Africa<br />
2<br />
Department of Biochemistry & Microbiology, University of Zululand, KwaDlangezwa<br />
3886, South Africa<br />
ladilawal@hotmail.com<br />
The essential oil from the rhizomes of Cyperus distans growing wild in KwaZulu-Natal<br />
Province, South Africa was obtained by hydrodistillation and analyzed by GC and<br />
GC/MS for the first time. Twenty-three constituents were identified, representing<br />
88.4% of the oil composition. The chemical profile of the oil was very different from<br />
the essential oils of several species of the genus Cyperus, with little amount of<br />
cyperene (3.1%) detected. The most interesting feature of the oil was the presence<br />
of an unusual and rarely occurring sesquiterpene ketone, zierone (33.9%).<br />
Keywords: Cyperus distans, Cyperaceae, essential oil composition, zierone.<br />
ANTI-PROTOZOAL CONSTITUENTS OF ACRIDOCARPUS CHLOROPTERUS<br />
OLIVER<br />
Hamisi M. Malebo 1,2,4,5 , Wenzler Tanja 2 , Monical Cal 2 , Sauda M. Swaleh 1 , Maurice O.<br />
Omolo 3 , Ahmed Hassanali 4 , , Urs Séquin 5 , Daniel Häussinger 5 , Petur Dalsgaard 6 ,<br />
Matthias Hamburger 6 , Reto Brun 1 , Isaiah O. Ndiege 1<br />
1<br />
Department of Chemistry, Kenyatta University, P.O. Box 43844, Nairobi, Kenya.<br />
2<br />
Medical Parasitology and Infection Biology, Parasite Chemotherapy Unit, Swiss<br />
Tropical Institute, University of Basel, Socinstrasse 57, CH-4002, Basel, Switzerland.<br />
3<br />
Department of Physical Sciences. Masinde Muliro University of Science & Technology,<br />
P. O. Box 190, Kakamega, Kenya<br />
4<br />
International Centre for Insect Physiology and Ecology, P.O. Box 30772, Nairobi,<br />
Kenya.<br />
5<br />
Institute of Organic Chemistry, University of Basel, St Johanns Ring 19 , CH-4052,<br />
Basel, Switzerland.<br />
6<br />
Institute of Pharmaceutical Biology, University of Basel, Klingelbergstrasse 50 , CH-<br />
4056, Basel, Switzerland.<br />
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13th NAPRECA SYMPOSIUM BOOK OF ABSTRACTS August 10-14, 2009<br />
Protozoal diseases like malaria, trypanosomiasis and leishmaniasis caused by<br />
Plasmodium, Trypanosoma and Leishmania, respectively, have overwhelming impact<br />
on public health in developing regions. Due to their prevalence, virulence and drug<br />
resistance, they are the most serious and widespread parasitic diseases encountered<br />
by mankind. The inadequate armory of drugs, high cost and lack of new drugs are<br />
the major limiting factors in the fight against the 3 diseases. Consequently, there is<br />
continuing need of research on the discovery and development of new effective and<br />
safe anti-protozoal drugs. In this work, extract from Acridocarpus chloropterus was<br />
tested for its anti-protozoal activity. Anti-protozoal bioassays revealed inactivity.<br />
Chromatography of A. chloropterus extract led to the isolation and identification of 5<br />
triterpenes: β-sitosterol (1), stigmasterol (2), friedelin (3), oleanolic acid (4), ursolic<br />
acid (5); and 5 flavonoids: apigenin (6), luteolin (7), vitexin (8), kaempferol (9) and<br />
quercetin (10). Quercetin (10) exhibited moderate in vitro anti-plasmodial activity<br />
(IC50 2.6+0.05 μg/ml) while the rest of compounds were inactive. Mild to weak in<br />
vitro anti-trypanosomal activity was observed in quercetin (10) (IC50 3.60+0.00001<br />
μg/ml), ursolic acid (5) (IC50 7.80+0.0001 μg/ml) and apigenin (6) (IC50 9.0+0.00001<br />
μg/ml). Good in vitro anti-leishmanial activity (IC50 0.80+0.00001, 2.10+0.00001,<br />
2.20+0.00001, 5.90+ 0.0001 and 3.5+0.00002 μg/ml) and favourable selectivity were<br />
observed in ursolic acid (5), quercetin (10), kaempferol (9), apigenin (6) and oleanolic<br />
acid (4), respectively. SAR comparisons in the isolated triterpenoids confirmed that,<br />
the OH at C-3 with, 23-CH3, 25-CH3, 26-CH3, C-12/C-13 double bond, 28-CO2H, H-20<br />
and 30-CH3 in the molecular framework of ursolic acid (5) are the structural motifs<br />
responsible for the strong anti-leishmanial activity whereas in the isolated<br />
flavonoids, the 3-OH and 3′-OH in the apigenin (6) molecular framework are the<br />
structural motifs responsible for the observed strong anti-protozoal activity. The<br />
strong to moderate anti-leishmanial activity of the isolated triterpenes and<br />
flavonoids render them good candidates as molecular templates for SAR studies<br />
which could lead to new drug development.<br />
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13th NAPRECA SYMPOSIUM BOOK OF ABSTRACTS August 10-14, 2009<br />
IN VIVO EFFICACY OF ORAL AND INTRAPERITONEAL ADMINISTRATION<br />
OF EXTRACTS OF WARBURGIA UGANDENSIS (CANELLACEAE) IN<br />
EXPERIMENTAL TREATMENT OF OLD WORLD CUTANEOUS<br />
LEISHMANIASIS CAUSED BY LEISHMANIA MAJOR<br />
Peter Kamau 1 , Zipporah Ng’ang’a 3 , Johnstone Ingonga 2 and Geoffrey Rukunga 2 and<br />
Willy Kiprotich Tonui 2<br />
1 Daystar University, Science department, P.O. Box 44400, 00100, Nairobi. 2 Kenya<br />
Medical Research Institute.<br />
3 Jomo Kenyatta University of Agriculture and Technology.<br />
*E-mail: ngure2001us@yahoo.com<br />
The antileishmanial activity of extracts of Warburgia ugandensis Spraque<br />
(Canellaceae), a known traditional therapy in Kenya was evaluated in vivo. Treatment<br />
of infected BALB/c mice with W. ugandensis extracts orally resulted in a reduction of<br />
the size of lesions compared to the untreated control. The lesion sizes differed<br />
significantly for the four extracts (p=0.039) compared to the untreated control. For<br />
mice treated by intraperitoneal injection, the lesion sizes increased initially for the<br />
hexane, dichloromethane and ethyl acetate extracts and healed by day 42. The<br />
lesion sizes for mice treated with methanol extract increased steadily from 2.47mm<br />
to 3.57mm. The parasitic burden was significantly higher (p
13th NAPRECA SYMPOSIUM BOOK OF ABSTRACTS August 10-14, 2009<br />
ANALYSIS OF NUTRITIONAL AND PHARMACOLOGICAL STATUS OF<br />
SELECTED PLANTS USED FOR TREATING HIV/AIDS AND OPPORTUNISTIC<br />
INFECTIONS IN EASTERN UGANDA<br />
Cyprian Osinde, Maud Kamatenesi Mugisha and Hannington Oryem-Origa<br />
DEPARTMENT OF BOTANY MAKERERE UNIVERSITY. P.O.BOX 7062, KAMPALA<br />
UGANDA.<br />
osindecyprian@yahoo.co.uk<br />
This paper presents an inventory of medicinal and nutritional plants used in<br />
treatment of opportunistic infections for HIV/AIDS patients and their mode of use,<br />
parts of plants used and the management status of these plants. People use herbs<br />
as food to treat opportunistic infections and this is reflected by the number of herbs<br />
mentioned. Sixty five species of plants belonging to sixty three genera and forty<br />
three families were mentioned. Plants used as medicine are in the categories of wild,<br />
indigenous, shrubs, cultivated, introduced, herbs, trees and lianas. The plant parts<br />
most frequently used for treating opportunistic infections due to HIV/AIDS are<br />
leaves, bark, and roots. Medications are mostly prepared as infusions, decoctions<br />
and topical applications. Some selected plants were analyzed for nutrients and they<br />
showed a variety of nutrients ranging from proteins, fibers and minerals. A<br />
comparative study on the antibacterial activities of the extracts was also done on<br />
Escherichia coli (ATCC 25922), Pseudomonas auriginosa (ATCC 27853) and<br />
Staphylococcus aureus (ATCC 25923). All the plant extracts were found to have<br />
considerable activities against the test organisms by use of the agar well diffusion<br />
assay. They showed inhibition zones ranging from 3.5mm to 20.1mm. Their MIC<br />
values were determined by use of serial dilution method and it ranged from<br />
0.0009g/ml to 0.125g/ml.<br />
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13th NAPRECA SYMPOSIUM BOOK OF ABSTRACTS August 10-14, 2009<br />
IN VIVO ANTIVIRAL AND LARVICIDAL POTENCY OF URSANE<br />
TRITERPENOIDS AND A GARLIC ACID DERIVATIVE FROM TOUSSAINTIA<br />
PATRICIAE<br />
*Samwel, S., Nkunya M.H.H., Joseph, C.C., Innocent E. and Msoffe, P.L.M<br />
Department of Chemistry, University of Dar es Salaam, P.O.Box 35061, Dar es<br />
Salaam, Tanzania.<br />
Tel: +255 22 2410038<br />
Mobile +255 754 206 560 or +255 718 944 724<br />
Fax: +255 22 2410038<br />
E-mail: samwel@chem.udsm.ac.tz or samnyandoro@yahoo.com<br />
Ursolic acid, its two hydroxylated derivatives as well as garlic acid derivative (ethyl<br />
3,4,5-trihydroxybenzoate) isolated from the leaves of Toussaintia patriciae<br />
(Annonaceae) exhibited in ovo antiviral potency against Newcastle Disease Virus<br />
(NDV) and (IBDV) at 360μg/mL. The three ursane triterpenoids also exhibited<br />
larvicidal activity against Anophelese gambiae mosquito larvae at their late 3 rd and<br />
early 4 th instar whereas the garlic acid derivative was inactive up to 50μg/mL. The<br />
larvicidal LC50 values will be presented in the results and discussion section. The<br />
structural determination was achieved based on the spectroscopic data.<br />
Key words: Ursane triterpenoids, garlic acid derivative, antiviral, larvicidal,<br />
Toussaintia patriciae.<br />
IN VITRO ANTILEISHMANIAL ACTIVITY OF EXTRACTS OF WARBURGIA<br />
UGANDENSIS (CANELLACEAE), A KENYAN MEDICINAL PLANT<br />
*Willy Kiprotich Tonui 1 , Peter Kamau Ngure 2 , Johnstone Ingonga 1 , Charles Mutai 1 ,<br />
Elizabeth Kigondu 1 , Zipporah Ng’ang’a 3 ,Geoffrey Rukunga 1 and Albert Kimutai 1 .<br />
1<br />
Center for Biotechnology Research and Development, Kenya Medical Research<br />
Institute, Nairobi, Kenya<br />
2<br />
Daystar University, Science department, P.O. Box 44400, 00100, Nairobi, Kenya<br />
3<br />
Jomo Kenyatta University of Agriculture and Technology, Nairobi, Kenya<br />
*Email: wtonui@kemri.org<br />
The antileishmanial activity of extracts of W. ugandensis (Family Canellaceae), a<br />
known traditional therapy and one of the commonly used medicinal plants in Kenya<br />
was evaluated. We tested extracts of this plant for possible antileishmanial activity in<br />
vitro. Different doses of hexane, dichloromethane, ethyl acetate and methanol<br />
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13th NAPRECA SYMPOSIUM BOOK OF ABSTRACTS August 10-14, 2009<br />
extracts of W. ugandensis were tested against Leishmania major and Leishmania<br />
donovani promastigotes and amastigotes. The hexane extract had the best activity<br />
against L. major promastigotes and amastigotes with IC50 value of 9.95 for<br />
promastigotes and 8.65 for amastigotes and minimum inhibition concentrations of<br />
62.5 µg/ml. The activity of the hexane extract on amastigotes was comparable<br />
(p>0.05) to that of pentostam and amphotericin B. Similar results were obtained for<br />
L. donovani with IC50 values of 8.67 for promastigotes and 100-fold reduction of<br />
amastigotes in macrophage cultures. Warburgia ugandensis had lower levels of<br />
toxicities compared to pentostam and amphotericin B. This study scientifically<br />
demonstrates the potential of W. ugandensis in the treatment of leishmaniasis.<br />
Key words: Warburgia ugandensis; Leishmaniasis; Promastigote; Amastigote<br />
INNOVATION SYSTEMS AND CLUSTER APPROACHES FOR<br />
EXPLOITATION OF THE INDIGENOUS AND EXOTIC EDIBLE AND<br />
MEDICINAL MUSHROOMS OF THE LAKE VICTORIA BASIN<br />
Olila, D., Kabasa, JD., Kisovi, L., Engola, A. and Munishi, PKT<br />
* Department of Veterinary Physiological Sciences,<br />
Makerere University,<br />
P.O. Box 7062, Kampala<br />
olilad@vetmed.mak.ac.ug<br />
Mushrooms are used as food and medicine in many societies. They are also of<br />
considerable biotechnological value and important nutraceuticals, particularly in<br />
immuno-compromised patients (e.g. HIV cases). However, the nutritional, ecological,<br />
medicinal and biotechnological importance of indigenous Ugandan mushrooms are<br />
not adequately studied and documented.<br />
Faced with poor and rapidly growing population in Uganda, the competition for<br />
natural resources by different producer groups is increasing. Expansion of crop and<br />
animal production has adverse effects on the environment. There is increasing<br />
pressure on land, leading to loss of indigenous mushroom bio-diversity without<br />
understanding their contribution to present and future generations.<br />
This paper will present some data on characterisation of indigenous mushroom<br />
ecology, their cultivation, indigenous knowledge, domestication and assessment of<br />
their potential as sources of nutrients, novel antibiotics and metabolites for<br />
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13th NAPRECA SYMPOSIUM BOOK OF ABSTRACTS August 10-14, 2009<br />
improved health and socio-economic benefits. The information was gathered<br />
through reconnaissance surveys, participatory appraisals and standard laboratory<br />
techniques involving assessment of nutritional and pharmacological potential.<br />
Innovation systems and cluster approaches are presented as a way forward to<br />
maximise exploitation of the indigenous African mushroom biodiversity. This is<br />
because today, economic development policies that target individual firms or<br />
industries are no longer the most viable option for regions. Cluster development has<br />
gained considerable attention over the past decade, as an operational means to<br />
systematically enhance the competitiveness of regions. The new economy of clusters<br />
has to do with speed, quality, flexibility, innovation, networks, and building critical<br />
mass. This new style demands a team approach at local level, a clustering approach.<br />
This clusters approach is the missing link in the indigenous mushroom industry in<br />
Africa. It is only through developing of viable clustering that even small firms are able<br />
to gain the necessary critical mass to service world markets.<br />
PHYTOCHEMICAL ANALYSIS OF COMMIPHORA HOLTZIANA OLEO-GUM<br />
RESIN<br />
Sylvia A. Opiyo 1 , Lawrence O. A. Manguro 1 , Peter Lemmen 2 and Eberhardt Herdweck 3<br />
1<br />
Maseno University, Department of Chemistry, P. O. Box 333, Maseno, Kenya<br />
2<br />
Technical University Munich, Institute of Organic Chemistry and Biochemistry,<br />
Lichtenbergstrasse 4, 85747- Garching, Germany<br />
3<br />
Technical University Munich, Institute of Inorganic Chemistry, Lichtenbergstrasse 4, 85747-<br />
Garching, Germany<br />
sylvopiyo@yahoo.com<br />
An investigation on the acetone extract of Commiphora holtziana gum resin yielded eleven<br />
known compounds namely cabraleadiol monoacetate, mansumbinol, 3β-acetylamyrin, 3αacetylboswellic<br />
acid, 2-methoxy-8,12-epoxygermacra-1(10),trine-6-one, 2-methoxy-5acetylfuranogermacra-1(10),7,11-trien-6-one,<br />
furadienone, 2-methoxy-5-acetyt-4furanogermacra-(10)<br />
Z-en-6-one, α-amyrin, sitosterol and stigmasterol together with four<br />
new triterpenes characterized as methyl 3-oxo-1α,19α,28-trihydroxyurs-12-en-24-oate (1),<br />
methyl 3β-acetyl-2α,11α,19α,28-tetrahydroxyurs-12-en-24-oate (2), methyl 3β,11α-diacetyl-<br />
1α,2α,28-trihydroxyurs-12-en-24-oate (3) and 3β,28-diacetyl-1α,2α,25-trihydroxydammar-<br />
23-ene (4).The structures were determined using spectroscopic and physical methods as<br />
well as by comparison with data from the literature.<br />
Keywords: Commiphora holtziana; Burseraceae; triterpenes; gum-oleo-resin exudates.<br />
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13th NAPRECA SYMPOSIUM BOOK OF ABSTRACTS August 10-14, 2009<br />
INTERSPECIFIC CHEMICAL SIGNALS INFLUENCING OVIPOSITION BY THE<br />
MALARIA MOSQUITO, ANOPHELES GAMBIAE<br />
Sabina W. Wachira 1,2 , Mary Ndung'u 3 , P.G. N. Njagi 1 and Ahmed Hassanali 1,4<br />
1<br />
International Centre of Insect Physiology and Ecology (ICIPE), PO Box 30772-00100,<br />
Nairobi, Kenya:<br />
2<br />
Kenya Medical Research Institute (KEMRI), PO Box 54840-00200, Nairobi, Kenya<br />
3<br />
Department of Chemistry, Jomo Kenyatta University of Agriculture and Technology,<br />
PO Box 62000, Nairobi, Kenya<br />
4<br />
Chemistry Department, Kenyatta University, P.O. Box 43844-00100, Nairobi, Kenya.<br />
Email: swachira@kemri.org<br />
Gravid Anopheles gambiae Giles makes a choice of an appropriate oviposition site. The<br />
presence of Culex quinquifasciatus in an oviposition site influences gravid An. gambiae<br />
decision to oviposit at a specific site or not. The effect of volatiles emanating from varying<br />
numbers of egg rafts and/or larvae of C. quinquifasciatus in relation to oviposition by An.<br />
gambiae was evaluated using double cup oviposition assay. The oviposition response had<br />
various patterns depending on the number of egg rafts and/or larvae used in test water.<br />
Oviposition was observed to increase in the presence of C. quinquifasciatus egg rafts at low<br />
density. At increased density the oviposition activity index decreased to negative value. The<br />
presence of C. quinquifasciatus larvae deterred the oviposition by gravid An. gambiae even<br />
at low density. However when both Culex quinquifasciatus larvae and egg rafts were used<br />
with varying density of egg rafts and constant number of larvae the deterrent was more than<br />
when the two were used separately.<br />
Key words: Anopheles gambiae, Culex quinquifasciatus, oviposition, egg rafts, larvae,<br />
deterrence.<br />
LEAF-SURFACE DEPOSITED COMPOUNDS AS ALTERNATIVE ANIMAL<br />
FEED PRESERVATIVES<br />
*Onemus M. Wanjau a , Simon M. Mahungu b , and Richard W. Mwangi c<br />
a Department of Chemistry, Egerton University<br />
b Department of Dairy and Food Science, Egerton University<br />
c Department of Zoology, University of Nairobi.<br />
owanjau@yahoo.com<br />
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13th NAPRECA SYMPOSIUM BOOK OF ABSTRACTS August 10-14, 2009<br />
The presence of an array of secondary metabolites in the leaf-surface exudates has<br />
elicited phytochemical screening. The constituent compounds, supposedly, serve a<br />
protective role on the plant lipids against autoxidation occasioned by UV radiation.<br />
Some flavonoids, Polsen 1, Polsen 3 and Polsen 5, isolated from the leaf-surface<br />
exudate of Polygonum senegalense were investigated for antioxidant effect on<br />
edible oils, heated to about 200 0 C. Polsen 1 enhanced the induction period and thus<br />
could be used as an animal feed additive for the purpose of retarding oxidative<br />
destruction of the naturally occurring carotenes and vitamin E in animal feeds.<br />
One compound (Polsen 5) showed a cytotoxic effect against a mammarian cell-line,<br />
Chine Hamster Ovarian (CHO), using the 3-(4,5-dimethylthiazol-2yl)-2,5diphenyltetrazoliumbromide.<br />
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13th NAPRECA SYMPOSIUM BOOK OF ABSTRACTS August 10-14, 2009<br />
GREEN CHEMISTRY WORKSHOP<br />
SPONSORED BY THE PAN AFRICAN CHEMISTRY<br />
NETWORK (PACN)<br />
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13th NAPRECA SYMPOSIUM BOOK OF ABSTRACTS August 10-14, 2009<br />
GREEN CHEMISTRY AND METAL COMPLEXES/MATERIALS<br />
Neil Coville<br />
University of Witwatersrand, Johannesburg<br />
Neil.Coville@wits.ac.za<br />
Green Chemistry is a philosophy at how to approach a chemical problem. It is<br />
possible to use the ‘12 Principles of Green Chemistry’ (and also Green Engineering)<br />
to evaluate whether a reaction is more ‘green’ than other approaches. In this talk<br />
two aspects relating to the synthesis of, mainly inorganic compounds, will be<br />
discussed. The one issue will relate to the topic of solventless/solvent-free<br />
chemistry; the other to the use of ‘green’ principles in making nanomaterials.<br />
GREEN CHEMISTRY: A TOOL FOR ENVIRONMENTAL POLLUTION<br />
PREVENTION CAUSED BY CHEMICAL MANUFACTURING<br />
PROCESSES<br />
Joseph M. Keriko<br />
Jomo Kenyatta University of Agriculture and Technology,Nairobi, Kenya<br />
kerikojm@yahoo.co.uk<br />
Green chemistry is a particular type of pollution prevention that has solutions to<br />
the current global warming problems. It is an approach that provides a fundamental<br />
methodology for changing the intrinsic nature of a chemical product or process so<br />
that it is inherently of less risk to human health and the environment.<br />
Green chemistry involves the design and redesign of chemical syntheses and<br />
chemical products to prevent pollution and thereby solve environmental problems.<br />
It is therefore, a particular type of pollution prevention.<br />
Synthetic chemists, those who design new chemicals and their manufacturing<br />
processes, have not been particularly environmentally conscious. This is primarily<br />
due to the fact that they are at the beginning of the process, identifying ways to<br />
make chemicals, while the problems have traditionally been identified with the end<br />
of the process, the waste stream. Thus, the role of synthetic chemists has<br />
historically been to design synthetic pathways to produce target molecules for the<br />
least cost in the greatest yield. However, synthetic chemists should play a more<br />
central role in developing Green chemical methods for pollution prevention rather<br />
than end-of-pipe control.<br />
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13th NAPRECA SYMPOSIUM BOOK OF ABSTRACTS August 10-14, 2009<br />
In this paper therefore, I will discuss the current global ecological footprint<br />
situations, introduction to green chemistry, tools and the principles of green<br />
chemistry. The role that chemists need to play in preventing environmental<br />
pollution based on the Green chemistry methods will also be mentioned.<br />
THE SEARCH FOR GREEN CATALYSTS<br />
Egid B. Mubofu<br />
University of Dar es Salaam, Chemistry Department, P. O. Box 35061, Dar es Salaam,<br />
Tanzania<br />
mubofu@chem.udsm.ac.tz or ebmubofu@yahoo.co.uk<br />
The importance of catalysis makes it one of the most intensely studied and pursued<br />
field in both chemical engineering and applied chemistry. The development and<br />
advancement of catalysis holds the key for improvement of economic,<br />
environmental and for the sustainability of the world. The use of principles of Green<br />
Chemistry on the design of chemical products and processes puts catalysis as one of<br />
the cornerstone of pollution prevention by design. This presentation gives a brief<br />
description of green chemistry in relation to design of products and sustainability.<br />
The clean technology pool and the green chemical technologies and hot spots are<br />
briefly introduced. This is followed by examples of various catalysts that have been<br />
designed based on green chemical technologies and hot spots. These catalysts are<br />
mostly chemically anchored onto the surface of micelle templated silica (MTS)<br />
support. Some examples of atom economy and green chemistry matrix drawn from<br />
other workers are given so as to illustrate the concept. The supported catalysts have<br />
been tested on Heck, Suzuki, epoxidation of norbonene, oxidation of maleic acid and<br />
enzyme catalysed reactions. The paper concludes by giving the key messages about<br />
the importance of green chemistry for sustainable development.<br />
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13th NAPRECA SYMPOSIUM BOOK OF ABSTRACTS August 10-14, 2009<br />
GREEN CHEMISTRY PARADIGM: THE ROLE OF NATURAL PRODUCTS<br />
Jacob O Midiwo, Joe Mwaniki, Isaac Chogii, Leonidah Kerubo, Bernard Juma<br />
Department of Chemistry, University of Nairobi, P. O. Box 30197, Nairobi.<br />
jmidiwo@uonbi.ac.ke<br />
The world is going green and chemists are being asked to ‘shift’ their thinking to<br />
Green Chemistry for sustainable development- design processes that ‘--- meet the<br />
needs of the present without compromising the ability of the future generations to<br />
meet their own needs’. To give guidelines on sustainability, the 12 principles have<br />
been enunciated by Paul Anastas and John Warner; the seventh principle says - “a<br />
raw material should be renewable rather than depleting whenever technically and<br />
economically practicable”. Certain natural products provided in large amounts by<br />
higher plants and fungi secondary metabolism should be highlighted as raw<br />
materials for synthesis (structural modification) of fine chemicals such as drugs and<br />
other biologically active products to propagate green.<br />
Many plant species scattered amongst different plant families produce in large<br />
amounts what may be referred to as surface exudates- non polymeric organic<br />
molecules that seem to have protective function to the plants. These exudates in the<br />
aerial parts have functionality that make them attractive to be considered as green<br />
synthons. Examples of surface exudates plants studied (Polygonum senegalense,<br />
Psiadia punctulata, Dodonaea angustifolia, Senecio roseiflorus) for quantities of<br />
exudates and structural diversity will be given in this lecture; structural derivatisation<br />
of the natural compounds for activity optimization, in certain cases, under green<br />
conditions will be alluded to. Other examples of plants with high yielding potential<br />
sources of starter compounds will also be mentioned.<br />
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67