Tsipouras A, Adefarati A A, Tkacz J S, Frazier E G, Rohrer S P, Birzin E, Rosegay A, Zink D L, Goetz M A, Singh S B, Schaeffer J M
Department of Cell Biochemistry and Physiology, Merck Research Laboratories, Rahway, NJ 07065, USA.
Bioorg Med Chem. 1996 Apr;4(4):531-6. doi: 10.1016/0968-0896(96)00036-3.
A series of ophiobolins were isolated from a fungal extract based on their nematocidal activity. These compounds are non-competitive inhibitors of ivermectin binding to membranes prepared from the free-living nematode, Caenorhabditis elegans, with an inhibition constant of 15 microM. The ophiobolins which were most potent in the biological assays, ophiobolin C and ophiobolin M, were also the most potent compounds when evaluated in a C. elegans motility assay. These data suggest that the nematocidal activity of the ophiobolins is mediated via an interaction with the ivermectin binding site. The isolation, structure and biological activity of ophiobolins have been described.
基于杀线虫活性，从一种真菌提取物中分离出了一系列蛇孢菌素。这些化合物是非竞争性抑制剂，可抑制伊维菌素与从自由生活线虫秀丽隐杆线虫制备的膜结合，抑制常数为15微摩尔。在生物学试验中最有效的蛇孢菌素，即蛇孢菌素C和蛇孢菌素M，在秀丽隐杆线虫运动试验中评估时也是最有效的化合物。这些数据表明，蛇孢菌素的杀线虫活性是通过与伊维菌素结合位点的相互作用介导的。蛇孢菌素的分离、结构和生物活性已有描述。
