新型强效免疫抑制剂西罗莫司F904的研究

Novel macrolide immunosuppressant, sirolimus F904

从福建省福州市的土壤中分离到的链霉菌 FC90 4 ,经分类鉴定、菌株培养确定为吸水链霉菌。其发酵代谢产物 F90 4具有抗真菌、抗增殖和比环孢素强的免疫抑制活性。分离、纯化、结晶 ,得 F90 4 ,经理化性质、光谱分析和 X-射线单晶衍射研究证明 F90 4为三烯大环内酯新型强效免疫抑制剂西罗莫司。

In the course of screening program for novel immunosuppressants, a macrolide F904 has been isolated from the fermentation broth of a Streptomyces FC904 drived from Fuzhou, Fujian province. The strain was identified as Streptomyces hygroscopicus . The macrolide F904 showed very potent activities against fungi and proliferation, and the immunosuppressive potency of F904 was higher than that of ciclosporin. The culture broth of Streptomyces hygroscopicus FC904 was extracted, purified and crystallized. Based on physico chemical properties, spectral analysis and X ray diffraction, F904 was identified as sirolimus, a powerful immunosuppressive macrolide.