Ramanandraibe Voahangy, Grellier Philippe, Martin Marie-Thérèse, Deville Alexandre, Joyeau Roger, Ramanitrahasimbola David, Mouray Elisabeth, Rasoanaivo Philippe, Mambu Lengo
Laboratoire de Bio-thérapeutique, Institut Malgache de Recherches Appliquées, Antananarivo, Madagascar.
Planta Med. 2008 Mar;74(4):417-21. doi: 10.1055/s-2008-1034328.
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 IC (50) values of 1.2 microM and 1.0 microM, respectively, and no significant cytotoxicity against the human embryonic lung cells MRC-5 was measured (IC (50) values > 75 microM). Five analogues ( 5 - 9) of (+)-catechin 5-gallate ( 2) were synthesized and evaluated for their antiplasmodial activity.
佩氏猴耳环（Piptadenia pervillei Vatke，豆科）是从一项旨在从马达加斯加植物中寻找天然抗疟化合物的筛选计划中挑选出来的。对该植物叶子的乙酸乙酯提取物进行生物测定导向的分级分离，得到了四种酚类化合物，（+）-儿茶素（1）、（+）-儿茶素5-没食子酸酯（2）、（+）-儿茶素3-没食子酸酯（3）和没食子酸乙酯（4）。通过核磁共振和质谱确定了其结构。化合物2和3对恶性疟原虫耐氯喹菌株FcB1显示出最高的体外活性，其半数抑制浓度（IC50）值分别为1.2微摩尔和1.0微摩尔，并且未检测到对人胚肺细胞MRC-5有明显的细胞毒性（IC50值>75微摩尔）。合成了（+）-儿茶素5-没食子酸酯（2）的五个类似物（5 - 9），并对其抗疟活性进行了评估。
