Antiplasmodial Phenolic compounds from Piptadenia pervillei

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.

Key words

Piptadenia pervillei - Fabaceae - antiplasmodial activity - (+)-catechin gallate

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