文献类型： 外文期刊
第一作者： Zhang, Jun
作者： Zhang, Jun;Meng, Lin-Lin;Fan, Peng;Liu, Sha-Sha;Yuan, Wei-Yu;Luo, Du-Qiang;Wei, Jing-Jing;Zhao, You-Xing
作者机构：
关键词： Isaria fumosorosea;PTP1B;pyrrolidinedione
期刊名称：MOLECULES （ 影响因子：4.411； 五年影响因子：4.587 ）
ISSN： 1420-3049
年卷期： 2017 年 22 卷 12 期
页码：
收录情况： SCI
摘要： Protein tyrosine phosphatase 1B (PTP1B) is implicated as a negative regulator of insulin receptor (IR) signaling and a potential drug target for the treatment of type II diabetes and other associated metabolic syndromes. Thus, small molecule inhibitors of PTP1B can be considered as an attractive approach for the design of new therapeutic agents of type II diabetes and cancer diseases. In a continuing search for new PTP1B inhibitors, a new tetramic acid possessing a rare pyrrolidinedione skeleton named fumosorinone A (1), together with five known ones 2-6 were isolated from the entomogenous fungus Isaria fumosorosea. The structures of 2-6 were elucidated by extensive spectroscopic analysis. Fumosorinone A (1) and beauvericin (6) showed significant PTP1B inhibitory activity with IC50 value of 3.24 M and 0.59 M.
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