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PTP1B Inhibitors from the Entomogenous Fungi Isaria fumosorosea

文献类型: 外文期刊

作者: Zhang, Jun 1 ; Meng, Lin-Lin 1 ; Wei, Jing-Jing 2 ; Fan, Peng 1 ; Liu, Sha-Sha 1 ; Yuan, Wei-Yu 1 ; Zhao, You-Xing 3 ; Lu 1 ;

作者机构: 1.Hebei Univ, Coll Life Sci, Key Lab Med Chem & Mol Diag, Minist Educ, Baoding 071002, Peoples R China

2.Hebei Univ, Coll Pharmaceut Sci, Key Lab Pharmaceut Qual Control Hebei Prov, Baoding 071002, Peoples R China

3.Chinese Acad Trop Agr Sci, Inst Trop Biosci & Biotechnol, Haikou 571101, Hainan, Peoples R China

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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