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。
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 aureus, 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 cyclization between N-6 and 0-3＇（4 and 5） can enhance the activity.
出处
《天然产物研究与开发》
CAS
CSCD
2008年第6期953-955,963,共4页
Natural Product Research and Development
基金
This research was financially supported by the Knowledge Innovation Program of the Chinese Academy of Sciences.
关键词
螺卷毛壳霉
抗细菌活性
抗真菌活性
构效关系
Chaetomium cochloides
antibacterial
antifungal
structure-activity relationship
