Antiplasmodial phenolic compounds from Piptadenia pervillei

被引:33
作者
Ramanandralbe, Voahangy
Grellier, Philippe [3 ]
Martin, Marie-Therese [2 ]
Deville, Alexandre [1 ]
Joyeau, Roger [1 ]
Ramanitrahasimbola, David
Mouray, Elisabeth [3 ]
Rasoanaivo, Philippe
Mambu, Lengo [1 ]
机构
[1] Museum Natl Hist Nat, CNRS Chim & Biochim Subst Nat, USM 0502,UMR 5154, Dept Regulat Dev & Divers Mol, F-75231 Paris 05, France
[2] CNRS, Inst Chim Subst Nat, Gif Sur Yvette, France
[3] Museum Natl Hist Nat, USM Biol Fonct Protozoaires 0504, Dept Regulat Dev & Diversite Mol, F-75231 Paris, France
关键词
Piptadenia pervillei; Fabaceae; antiplasmodial activity; (+)-catechin gallate;
D O I
10.1055/s-2008-1034328
中图分类号
Q94 [植物学];
学科分类号
071001 ;
摘要
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 mu M and 1.0 mu M, respectively, and no significant cytotoxicity against the human embryonic lung cells MRC-5 was measured (IC50 values > 75 mu M). Five analogues (5-9) of (+)-catechin 5-gallate (2) were synthesized and evaluated for their antiplasmodial activity.
引用
收藏
页码:417 / 421
页数:5
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