Antiplasmodial Phenolic compounds from Piptadenia pervillei

 

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Abstract

Piptadenia pervillei Vatke (Fabaceae) was selected from a screening programme devoted to the search of naturally-occuring antimalarial compounds from plants of Madagascar. Bioassay-guided fractionation of the ethyl acetate extract of the leaves led to the isolation of four phenolic compounds, (+)-catechin (1), (+)-catechin 5-gallate (2), (+)-catechin 3-gallate (3) and ethyl gallate (4). Structures were determined by NMR and mass spectroscopy. Compounds 2 and 3 displayed the highest in vitro activity against the chloroquine-resistant strain FcB1 of Plasmodium falciparum with IC₅₀ values of 1.2 μM and 1.0 μM, respectively, and no significant cytotoxicity against the human embryonic lung cells MRC-5 was measured (IC₅₀ values > 75 μM). Five analogues (5 - 9) of (+)-catechin 5-gallate (2) were synthesized and evaluated for their antiplasmodial activity.

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Dr. Lengo Mambu

USM 0502-UMR 5154

CNRS Chimie et Biochimie des Substances Naturelles

Département Régulations,

Développement et Diversité Moléculaire

Muséum National d’Histoire Naturelle

CP 54, 57 rue Cuvier

75231 Paris Cedex 05

France

Phone: +33-1-4079-5607

Fax: +33-1-4079-3135

Email: mambu@mnhn.fr