锁阳成分及相关三萜衍生物对HIV-1蛋白酶的抑制作用。

Inhibitory effects of constituents from Cynomorium songaricum and related triterpene derivatives on HIV-1 protease.

作者信息

Ma C, Nakamura N, Miyashiro H, Hattori M, Shimotohno K

机构信息

Research Institute for Wakan-Yaku (Traditional Sino-Japanese Medicines), Toyama Medical and Pharmaceutical University, Japan.

出版信息

Chem Pharm Bull (Tokyo). 1999 Feb;47(2):141-5. doi: 10.1248/cpb.47.141.

DOI:10.1248/cpb.47.141

PMID:10071849

Abstract

From CH2Cl2 and MeOH extracts of the stems of Cynomorium songaricum RUPR. (Cynomoriaceae), ursolic acid and its hydrogen malonate were isolated as inhibitors of human immunodeficiency virus type 1 (HIV-1) protease, with 50% inhibitory concentrations (IC50) of 8 and 6 microM, respectively. Amongst various synthesized dicarboxylic acid hemiesters of related triterpenes, inhibitory activity tended to increase in the order of oxalyl, malonyl, succinyl and glutaryl hemiesters, for triterpenes such as ursolic acid, oleanolic acid and betulinic acid. The most potent inhibition was observed for the glutaryl hemiesters, with an IC50 of 4 microM. From the water extract of the stems of C. songaricum, flavan-3-ol polymers, consisting of epicatechin as their extender flavan units, were also found to be potent inhibitory principles against HIV-1 protease.

摘要

从锁阳（锁阳科）茎的二氯甲烷和甲醇提取物中，分离得到了熊果酸及其氢丙二酸酯，它们是人类免疫缺陷病毒1型（HIV-1）蛋白酶的抑制剂，50%抑制浓度（IC50）分别为8和6微摩尔。在相关三萜类化合物的各种合成二羧酸半酯中，对于熊果酸、齐墩果酸和桦木酸等三萜类化合物，抑制活性倾向于按草酸半酯、丙二酸半酯、琥珀酸半酯和戊二酸半酯的顺序增加。观察到戊二酸半酯的抑制作用最强，IC50为4微摩尔。从锁阳茎的水提取物中，还发现由表儿茶素作为其延伸黄烷单元组成的黄烷-3-醇聚合物是抗HIV-1蛋白酶的有效抑制成分。