螺卷毛壳霉代谢产物的抗菌活性研究

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0-3'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 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.