真菌F01-994产生的对谷胱苷肽转移酶具有抑制作用的活性化合物的研究  

Study on inhibitory active compound against glutathione S-transferase produced by one strain of fungi F01-994

作　　者：李韶菁[1] 路新华[2] 董悦生[2] 郑智慧[2] 张华[2] 

机构地区：[1]中国中医科学院中药研究所,北京100700 [2]华北制药集团新药研究开发有限责任公司微生物药物国家工程研究中心,石家庄050015

出　　处：《中国抗生素杂志》2010年第10期743-746,共4页Chinese Journal of Antibiotics

基　　金：国家重大新药创制专项资助项目"创新药物研究与开发技术体系建设"(编号:2008ZX09401-005)

摘　　要：目的筛选具有潜在的可用作抗肿瘤药物增敏剂的新的谷胱苷肽-S-转移酶-π(GST-π)的抑制剂。方法利用所建立的高通量筛选模型从微生物代谢产物中筛选对GST-π具有抑制作用的活性化合物。结果使用有机溶剂萃取、硅胶柱层析、高压液相分离等方法,从真菌的菌丝体中分离得到了一个对GST-π具有抑制作用的活性化合物994-a,其IC50为15μg/mL并经各种理化性质及NMR分析确定其与Pencolid同质。结论本文首次报道了该化合物对GST-π酶所显示出的中等强度的抑制活性。Objective Screening new glutathione S-transferase-n （GST-n） inhibitor used as potent antitumor drug sensitizing agents. Methods A high throughput screening model has been set up and used to screening inhibitory bioactive compound toward GST-n from the metabolites of microorganism. Results One bioactivity compound named 994-a with the IC50 of 15μg/mL to GST-n was isolated from the mycelium of fungi F01-994 by solvent extraction, silica column chromatography, HPLC purification etc and it was elucidated to be identical with Pencolid by means of physico-chemical properties and NMR analysis. Conclusion This compound showed moderate strength inhibitory activity against GST-n and its inhibitory activity to GST was first reported.

关 键 词：GST HTS ENZYME INHIBITOR Pencolid 

分 类 号：R379[医药卫生—病原生物学]