雷帕霉素二醛的分离和结构鉴定

Isolation and identification of rapamycin dialdehyde

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.