摘要
目的从雷帕霉素产生菌吸水链霉菌FC904的发酵粗提物中,分离纯化在HPLC图谱中与雷帕霉素相对保留时间(RRT)为0.88的化合物FIM-R24并鉴定其化学结构。方法采用硅胶柱层析和制备液相分离FIM-R24,并对其进行NMR、UV、IR和HRMS等波谱分析。用SRB测定化合物体外抗肿瘤活性,用沙氏液体培养基二倍稀释法测定化合物的抗真菌活性。结果与结论 FIM-R24的结构为雷帕霉素二醛。FIM-R24的抗肿瘤活性仅比雷帕霉素略低,抗酵母样真菌的活性仅为雷帕霉素的1/8~15。
Objective To isolate and identify a chemical compound, FIM-R24, extracted from the fermentation broth of rapamycin producing strain Streptomyces hygroscopicus FC904, which showed a RRT of 0.88 in the rapamycin HPLC analysis. Methods FIM-R24 was isolated by silica gel chromatography and preparative liquid chromatography, and its chemical structurewas determined by the spectral analysis including NMR, UV, IR, and HRMS. The anti-cancer activity of FIM-R24 was determined by the SRB method in vitro, and the antifungal activity was evaluated by the serial two-foldbroth dilution method. Result and Conclusion FIM-R24 was identical with rapamycin dialdehyde. By comparison, the anti-cancer activity of FIM-R24 was slightly weaker than that of rapamycin, and its anti-fungal activity was 8-15 times weaker than that of rapamycin.
作者
杨国新
陈夏琴
余辉
陈晓明
李夸良
金东伟
程元荣
黄捷
Yang Guo-xin;Chen Xia-qin;Yu hui;Chen Xiao-ming;Li Kua-liang;Jin Dong-wei;Cheng Yuan-rong;Huang Jie(Fujian Institute of Microbiology, Fuzhou 35000)
出处
《中国抗生素杂志》
CAS
CSCD
2018年第4期450-456,共7页
Chinese Journal of Antibiotics
基金
福建省化药技术重大研发平台(No.2014Y2001)
福州市生物制药行业技术创新中心(No.2016-PT-36)
关键词
雷帕霉素
雷帕霉素二醛
吸水链霉菌FC904
分离纯化
结构鉴定
Rapamycin analogue
Rapamycin dialdehyde
Streptomyces hygroscopicus FC904
Isolation and purification
Structure identification