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Title
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The value of central-African traditional medicine for lead finding : some case studies
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Author
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Abstract
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| Ethnoparmaological relevance: One of the possible methodologies for the discovery of novel drugs is the screening of selected plant extracts for a broad array of pharmacological activities. Materials and Methods: The selection based on enthnomedicinal uses, combined with a follow-up of existing literature on the plants chemotaxonomic properties, would seem to be the most cost-effective strategy for finding active plant extracts. A bioassay-guided fractionation of the active extracts should subsequently lead to the isolation and identification of the active lead constituent(s). Results and Discussion: Taking into account the enormous number and the amazing structural diversity of the currently known plant constituents, one might hope that promising model compounds with new structures and/or novel mechanisms of action might be found. In order, however, to optimize such a natural product drug discovery methodology, dereplication and selectivity of activity should be included in the screening system. Dereplication by which known compounds can rapidly be identified from a partially purified mixture prevents a research group from wasting resources by rediscovering known compounds. The use of single-target specific bioassays such as tests on isolated enzymes or on receptor-binding, or multiple target functional bioassays on isolated organs or intact cells must allow at an early stage to isolate compounds with specific pharmacological properties. Conclusions: In this publication, several examples of bioassay-guided isolation and identification of pharmacologically active lead compounds from plants used in Central-African traditional medicine by our research group will be presented and discussed. |
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Language
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English
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Source (journal)
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Journal of ethnopharmacology. - Lausanne
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Publication
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Lausanne
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2015
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ISSN
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0378-8741
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DOI
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10.1016/J.JEP.2015.06.004
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Volume/pages
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174
(2015)
, p. 607-617
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ISI
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000365050900060
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Pubmed ID
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26079563
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Full text (Publisher's DOI)
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Full text (open access)
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Full text (publisher's version - intranet only)
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