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抗疟灵芝甾体。

Antiplasmodial lanostanes from the Ganoderma lucidum mushroom.

机构信息

Institute of Pharmaceutical Biology, University of Basel, Klingelbergstrasse 50, 4056 Basel, Switzerland.

出版信息

J Nat Prod. 2010 May 28;73(5):897-900. doi: 10.1021/np100031c.

Abstract

In a screen of 880 extracts from plants and fungi for antiplasmodial, antitrypanosomal, and leishmanicidal activity, an ethyl acetate extract of the mushroom Ganoderma lucidum showed antiplasmodial activity with 79% inhibition at 4.9 microg/mL. HPLC-based activity profiling and subsequent isolation of the antiplasmodial compounds yielded seven lanostanes (1-7), of which three (2, 3, and 7) were new. A new benzofuran derivative (8) of the farnesyl hydroquinone ganomycin B was also identified. The structures and relative configurations of the new compounds were elucidated by comprehensive spectroscopic analysis and by comparison of their NMR data with those of related compounds. The lanostanes exhibited in vitro antiplasmodial activity with IC(50) values from 6 to greater than 20 microM.

摘要

在对 880 种植物和真菌提取物进行抗疟原虫、抗锥虫和杀利什曼原虫活性筛选时,发现灵芝(Ganoderma lucidum)的乙酸乙酯提取物具有抗疟原虫活性,在 4.9 μg/mL 时抑制率为 79%。基于高效液相色谱的活性分析和随后对抗疟原虫化合物的分离得到了 7 个羊毛甾烷(1-7),其中 3 个(2、3 和 7)为新化合物。还鉴定了法呢基氢醌 ganomycin B 的一种新苯并呋喃衍生物(8)。新化合物的结构和相对构型通过综合光谱分析以及与相关化合物的 NMR 数据比较来阐明。这些羊毛甾烷在体外显示出抗疟原虫活性,IC(50)值为 6 至 20 微摩尔以上。

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