Title
The value of central-African traditional medicine for lead finding : some case studies The value of central-African traditional medicine for lead finding : some case studies
Author
Faculty/Department
Faculty of Pharmaceutical, Biomedical and Veterinary Sciences. Pharmacy
Publication type
article
Publication
Lausanne ,
Subject
Biology
Pharmacology. Therapy
Human medicine
Source (journal)
Journal of ethnopharmacology. - Lausanne
Volume/pages
174(2015) , p. 607-617
ISSN
0378-8741
ISI
000365050900060
Carrier
E
Target language
English (eng)
Full text (Publishers DOI)
Affiliation
University of Antwerp
Abstract
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.
Full text (open access)
https://repository.uantwerpen.be/docman/irua/5d5a06/128934.pdf
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