源自中国山楂的抗疟原花青素衍生物。

Antiplasmodial procyanidins derivatives from Chinese Hawthorn.

机构信息

Division of Environmental and Resource, College of Environmental and Bioresource Sciences, Chonbuk National University, Iksan, South Korea.

出版信息

Immunopharmacol Immunotoxicol. 2010 Dec;32(4):607-10. doi: 10.3109/08923971003631417. Epub 2010 Feb 22.

DOI:10.3109/08923971003631417

PMID:20175642

Abstract

The methanolic extract of the leaves of Chinese Hawthorn was investigated for its activity against chloroquine-sensitive strains of Plasmodium falciparum using the method of parasite lactate dehydrogenase assay. Four oligomeric procyanidins, such as epicatechin-(4β→8)-epicatechin-(4β→8)-epicatechin (1), epicatechin-(4β→8)-epicatechin-(4β→6)-epicatechin (2), epicatechin-(4β→6)-epicatechin-(4β→8)-epicatechin (3), and epicatechin-(4β→8)-epicatechin-(4β→8)-epicatechin-(4β→8)-epicatechin-(4β→8) (4), were isolated and evaluated for in vitro antiplasmodial activity, as well as for their cytotoxic potential on SK-OV-3 cancer cell lines. Three procyanidins showed notable growth inhibitory activity against chloroquine-sensitive strains of P. falciparum with IC(50) values of 2.7 μM (SI values of >55.5). The compounds showed no significant cytotoxicity (IC(50) > 150 μM) toward the SK-OV-3 cancer cell line. This is the first report on the antiplasmodial activity of these oligomeric procyanidins from Chinese Hawthorn.

摘要

采用疟原虫乳酸脱氢酶检测法，研究了山楂叶的甲醇提取物对氯喹敏感株疟原虫的抑制活性。分离并评价了四种低聚原花青素，即表儿茶素-(4β→8)-表儿茶素-(4β→8)-表儿茶素（1）、表儿茶素-(4β→8)-表儿茶素-(4β→6)-表儿茶素（2）、表儿茶素-(4β→6)-表儿茶素-(4β→8)-表儿茶素（3）和表儿茶素-(4β→8)-表儿茶素-(4β→8)-表儿茶素-(4β→8)-表儿茶素-(4β→8)（4），对其体外抗疟原虫活性及对 SK-OV-3 癌细胞系的细胞毒性进行了评价。三种原花青素对氯喹敏感株疟原虫具有显著的生长抑制活性，IC50 值分别为 2.7 μM（SI 值>55.5）。这些化合物对 SK-OV-3 癌细胞系无明显细胞毒性（IC50 >150 μM）。这是山楂中这些低聚原花青素具有抗疟原虫活性的首次报道。