文冠果木材成分对HIV-1蛋白酶的抑制作用。

Inhibitory effects on HIV-1 protease of constituents from the wood of Xanthoceras sorbifolia.

作者信息

Ma C, Nakamura N, Hattori M, Kakuda H, Qiao J, Yu H

机构信息

Institute of Natural Medicine, Toyama Medical and Pharmaceutical University, 2630 Sugitani, Toyama 930-0194, Japan.

出版信息

J Nat Prod. 2000 Feb;63(2):238-42. doi: 10.1021/np9902441.

DOI:10.1021/np9902441

PMID:10691716

Abstract

From a methanolic extract of the wood of Xanthoceras sorbifolia, two new compounds, 29-hydroxy-3-oxotirucalla-7,24-dien-21-oic acid (3, xanthocerasic acid) and epigallocatechin-(4beta-->8, 2beta-->O-7)-epicatechin (6), were isolated, together with 11 known compounds. Of the isolated compounds, 3-oxotirucalla-7, 24-dien-21-oic acid (2), oleanolic acid (4), and 6 were found to be inhibitory substances against human immunodeficiency virus (HIV-1) protease, with their 50% inhibitory concentrations (IC(50)) being 20, 10, and 70 microg/mL, respectively. Condensed tannins of high molecular weights with epicatechin and epiafzelechin as the main extender units were found to be the most active principles of this plant (IC(50) values ca. 6.0 microg/mL).

摘要

从文冠果木材的甲醇提取物中，分离出两种新化合物，即29-羟基-3-氧代-羽扇豆-7,24-二烯-21-酸（3，文冠果酸）和表没食子儿茶素-（4β→8，2β→O-7）-表儿茶素（6），以及11种已知化合物。在分离出的化合物中，3-氧代-羽扇豆-7,24-二烯-21-酸（2）、齐墩果酸（4）和6被发现是抗人类免疫缺陷病毒（HIV-1）蛋白酶的抑制物质，它们的50%抑制浓度（IC50）分别为20、10和70μg/mL。以表儿茶素和表阿夫儿茶素为主要延伸单元的高分子量缩合单宁被发现是该植物最具活性的成分（IC50值约为6.0μg/mL）。