College of Life Science, Key Laboratory of Medicinal Chemistry and Molecular Diagnosis of Ministry of Education, Hebei University, Baoding 071002, China
College of Pharmaceutical Science, Key Laboratory of Pharmaceutical Quality Control of Hebei Province, Hebei University, Baoding 071002, China
Molecules. 2017 Nov 24;22(12):2058. doi: 10.3390/molecules22122058.
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 (), together with five known ones - were isolated from the entomogenous fungus The structures of - were elucidated by extensive spectroscopic analysis. Fumosorinone A () and beauvericin () showed significant PTP1B inhibitory activity with IC value of 3.24 μM and 0.59 μM.
蛋白酪氨酸磷酸酶 1B（PTP1B）被认为是胰岛素受体（IR）信号的负调节剂，也是治疗 II 型糖尿病和其他相关代谢综合征的潜在药物靶点。因此，PTP1B 的小分子抑制剂可被视为设计 II 型糖尿病和癌症疾病新型治疗剂的一种有吸引力的方法。在继续寻找新的 PTP1B 抑制剂的过程中，一种新型的四元酸，含有罕见的吡咯烷二酮骨架，名为 fumosorinone A ()，与五种已知的化合物——从昆虫病原真菌 中分离出来。通过广泛的光谱分析阐明了 - 的结构。Fumosorinone A () 和 beauvericin () 表现出显著的 PTP1B 抑制活性，IC 值分别为 3.24 μM 和 0.59 μM。
