来自海洋真菌的潜在抗疟先导结构。

Potential antimalarial lead structures from fungi of marine origin.

作者信息

Wright Anthony D, Lang-Unnasch Naomi

机构信息

Australian Institute of Marine Science, Townsville MC, Queensland 4810, Australia.

出版信息

Planta Med. 2005 Oct;71(10):964-6. doi: 10.1055/s-2005-864181.

DOI:10.1055/s-2005-864181

PMID:16254832

Abstract

Antiplasmodial and cytotoxicity testing of five highly oxygenated natural products (6R,12R,14R-colletoketol, 6R,11R,12R,14R-colletoketodiol, dihydrobotrydial, pycnidione, and 3R,4S-hydroxymellein), all derived from fungi of marine origin, showed one of them, pycnidione, to have activities against three different strains of Plasmodium falciparum in the sub-micromolar (microM) range. Although the mean selectivity index of 1 for the observed antiplasmodial activity of 4 is low, pycnidione's usefulness as a potential lead structure should not be ignored.

摘要

对五种高度氧化的天然产物（6R,12R,14R - 胶孢炭疽醇、6R,11R,12R,14R - 胶孢炭疽二醇、二氢葡萄孢盘菌素、密挤青霉二酮和3R,4S - 羟基水曲霉毒素）进行抗疟原虫和细胞毒性测试，所有这些天然产物均源自海洋真菌，结果显示其中一种，即密挤青霉二酮，在亚微摩尔（μM）范围内对三种不同的恶性疟原虫菌株具有活性。尽管观察到的密挤青霉二酮抗疟活性的平均选择性指数为1，较低，但它作为潜在先导结构的实用性不应被忽视。