来自日本水杨梅的抗艾滋病毒三萜酸。

Anti-HIV triterpene acids from Geum japonicum.

作者信息

Xu H X, Zeng F Q, Wan M, Sim K Y

机构信息

Department of Chemistry, National University of Singapore, Singapore.

出版信息

J Nat Prod. 1996 Jul;59(7):643-5. doi: 10.1021/np960165e.

DOI:10.1021/np960165e

PMID:8759159

Abstract

The methanol extract from the whole plant of Geum japonicum was found to inhibit the human immunodeficiency virus (HIV-1) protease. Through bioassay-directed fractionation of the extract, a new triterpene acid along with five known triterpene acids, ursolic acid, epipomolic acid, maslinic acid, euscaphic acid, and tormentic acid, were isolated. The structure of the new compound was determined by spectral means including 1H-1H COSY, HMQC, HMBC, and NOE experiments to be 2 alpha, 19 alpha-dihydroxy-3-oxo-12-ursen-28-oic acid (1). Of these compounds, 1, ursolic acid, and maslinic acid showed potent inhibitory activity against HIV-1 protease.

摘要

发现日本水杨梅全草的甲醇提取物可抑制人类免疫缺陷病毒（HIV-1）蛋白酶。通过对该提取物进行生物活性导向分离，分离出一种新的三萜酸以及五种已知的三萜酸，即熊果酸、表波莫酸、山楂酸、优斯卡酸和 tormentic 酸。通过包括 1H-1H COSY、HMQC、HMBC 和 NOE 实验在内的光谱方法确定新化合物的结构为 2α,19α-二羟基-3-氧代-12-乌苏烯-28-酸（1）。在这些化合物中，化合物 1、熊果酸和山楂酸对 HIV-1 蛋白酶表现出强效抑制活性。