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灵芝孢子中萜类化合物的抗补体活性。

Anticomplement activity of terpenoids from the spores of Ganoderma lucidum.

作者信息

Min B S, Gao J J, Hattori M, Lee H K, Kim Y H

机构信息

Institute of Natural Medicine, Toyama Medical and Pharmaceutical University, Toyama, Japan.

出版信息

Planta Med. 2001 Dec;67(9):811-4. doi: 10.1055/s-2001-18854.

Abstract

A new lanostane-type terpenoid, lucidenic acid SP1 (1), was isolated from a CHCl(3)-soluble fraction of Ganoderma lucidum spores together with four other known compounds (2 - 5). The structure of lucidenic acid SP1 was determined to be 3 beta,7 beta-dihydroxy-4,4,14 alpha-trimethyl-11,15-dioxo-5 alpha-chol-8-en-24-oic acid by spectroscopic means including 2D-NMR. Twelve triterpenes (1-12) isolated from G. lucidum spores were investigated in vitro for their anticomplementary activity. Compounds 1 - 5 were inactive, whereas ganoderiol F (8), ganodermanondiol (9) and ganodermanontriol (10) showed a strong anticomplement activity against the classical pathway (CP) of the complement system with IC(50) values of 4.8, 41.7, and 17.2 microM, respectively. The potency of these triterpene alcohols (8-10) in inhibiting CP activity was improved when the number of hydroxymethyl groups on the side chain moiety is increased. On the other hand, the ganoderic acids 1-7, which contain a carboxyl group in the side chain, and lucidumols A and B (11, 12) had little activity on this system.

摘要

从灵芝孢子的氯仿可溶部分中分离出一种新的羊毛甾烷型萜类化合物,灵芝酸SP1(1),以及其他四种已知化合物(2 - 5)。通过包括二维核磁共振在内的光谱手段,确定灵芝酸SP1的结构为3β,7β - 二羟基 - 4,4,14α - 三甲基 - 11,15 - 二氧代 - 5α - 胆甾 - 8 - 烯 - 24 - 酸。对从灵芝孢子中分离出的12种三萜化合物(1 - 12)进行了体外抗补体活性研究。化合物1 - 5无活性,而灵芝二醇F(8)、灵芝酸二醇(9)和灵芝酸三醇(10)对补体系统的经典途径(CP)表现出较强的抗补体活性,IC50值分别为4.8、41.7和17.2微摩尔。当侧链部分羟甲基数量增加时,这些三萜醇(8 - 10)抑制CP活性的能力增强。另一方面,在侧链含有羧基的灵芝酸1 - 7以及灵芝醇A和B(11, 12)对该系统几乎没有活性。

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