中国抗生素杂志2024,Vol.49Issue(9) :1013-1018.

西罗莫司新类似物FIM-R140的分离和结构鉴定

Isolation and identification of sirolimus analogue FIM-R140

陈夏琴 陈晓明 刘颖 应加银 李夸良 黄捷 杨国新
中国抗生素杂志2024,Vol.49Issue(9) :1013-1018.

西罗莫司新类似物FIM-R140的分离和结构鉴定

Isolation and identification of sirolimus analogue FIM-R140

陈夏琴 1陈晓明 1刘颖 1应加银 1李夸良 1黄捷 1杨国新1
扫码查看

作者信息

  • 1. 福建省微生物研究所,福州 350007
  • 折叠

摘要

目的 从西罗莫司产生菌吸水链霉菌FC904发酵液的粗提物中分离纯化未知杂质FIM-R140,鉴定其化学结构.方法 采用硅胶柱层析和制备液相分离纯化获得FIM-R140,进行理化性质以及IR、UV、NMR和HRMS等波谱分析,鉴定该杂质的化学结构.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 纯化获得HPLC纯度为97.05%的FIM-R140,结构鉴定为31-差向雷帕霉素,为首次报道的西罗莫司同分异构体.FIM-R140的抗肿瘤活性较西罗莫司略低,对白念珠菌的抑菌作用弱于西罗莫司.

Abstract

Objective To isolate and identify FIM-R140,a metabolite from the broth of the sirolimus producing strain Streptomyces hygroscopicus FC904.Methods FIM-R140 was separated and purified by silica gel chromatography and preparative liquid chromatography.Its chemical structure was determined by physicochemical properties and spectral analysis including IR,UV,NMR,and HRMS.The anti-cancer activity of FIM-R140 was determined by the SRB method in vitro,and the antifungal activity was evaluated by the serial two-fold broth dilution method.Results and Conclusion FIM-R140 with HPLC of 97.05%was obtained,and it was identified as 31-epi-rapamycin,a sirolimus isomer,which was reported for the first time.The anti-cancer activity and anti-fungus activity of FIM-R140 were slightly weaker than those of sirolimus.

关键词

西罗莫司/31-差向雷帕霉素/吸水链霉菌FC904/分离纯化/结构鉴定

Key words

Sirolimus/31-epi-rapamycin/Streptomyces hygroscopicus FC904/Isolation and purification/Structure identification

引用本文复制引用

出版年

2024
中国抗生素杂志
中国医药集团总公司四川抗菌素工业研究所,中国医学科学院医药生物技术研究所

中国抗生素杂志

CSTPCDCSCD北大核心
影响因子:1.08
ISSN:1001-8689
参考文献量15
段落导航相关论文