| 螺卷毛壳霉代谢产物的抗菌活性研究(英文) |
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| 引用本文： | 杨恩超,杨涛,李宗珍,刘光烨,李国友. 螺卷毛壳霉代谢产物的抗菌活性研究(英文)[J]. 天然产物研究与开发, 2008, 20(6) |
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| 作者姓名： | 杨恩超 杨涛 李宗珍 刘光烨 李国友 |
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| 作者单位： | 中国科学院成都生物研究所,成都,610041 |
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| 基金项目： | This research was financially supported by the Knowledge Innovation Program of the Chinese Academy of Sciences. |
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| 摘 要： | 采用管碟法首次对螺卷毛壳霉（Chaetomium cochloides）的含硫次生代谢产物（1—5）进行了体外抗细菌和抗真菌活性测定，并对其构效关系进行了研究。活性测定显示化合物1—5对革兰氏阳性细菌（Staphylococcus aureus）具有较强的抑制活性，其中化合物1的抑菌活性最强。构效关系研究表明位于C-3’和C-6’之间的二硫桥为化合物的抑菌活性中心，C-3与C-11a之间的二硫桥和N-6与O—3’之间的大环结构能够增强活性。
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| 关 键 词： | 螺卷毛壳霉 抗细菌活性 抗真菌活性 构效关系 |
Antimicrobial Activity of the Epipolythiodioxopiperazines from Chaetomium cochliodes |
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| YANG En-chao,YANG Tao,LI Zong-zhen,LIU Guang-ye,LI Guo-you. Antimicrobial Activity of the Epipolythiodioxopiperazines from Chaetomium cochliodes[J]. Natural Product Research and Development, 2008, 20(6) |
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| Authors: | YANG En-chao YANG Tao LI Zong-zhen LIU Guang-ye LI Guo-you |
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| Affiliation: | YANG En-chao,YANG Tao,LI Zong-zhen,LIU Guang-ye,LI Guo-you*Chengdu Institute of Biology,Chinese Academy of Sciences,Chengdu 610041,China |
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| Abstract: | The in vitro antibacterial and antifungal activities of the epipolythiodioxopiperazines (1-5) isolated from Chaetomium cochliodes were evaluated using the cup-plate method for the first time. The structure-activity relationship (SAR) of compounds 1-5 was investigated. Compounds 1-5 exhibited a good activity profile versus Staphylococcus au-reus, and among them 1 showed the strongest activity. The SAR study of compounds 1-5 suggested that the disulfer bridge between C-3' and C-6'(1) is the active center for the antibacterial activity against S. aureus, and the S-S bridge between C-3 and C-11a(1,2 and 4) and the cyelization between N-6 and 0-3'(4 and 5) can enhance the activity. |
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| Keywords: | Chaetomium cochloides antibacterial antifungal structure-activity relationship |
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