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Molecules 2017, 22(12), 2058; doi:10.3390/molecules22122058

PTP1B Inhibitors from the Entomogenous Fungi Isaria fumosorosea

1
College of Life Science, Key Laboratory of Medicinal Chemistry and Molecular Diagnosis of Ministry of Education, Hebei University, Baoding 071002, China
2
College of Pharmaceutical Science, Key Laboratory of Pharmaceutical Quality Control of Hebei Province, Hebei University, Baoding 071002, China
3
Institute of Tropical Bioscience and Biotechnology, Chinese Academy of Tropical Agricultural Sciences, Haikou 571101, China
*
Authors to whom correspondence should be addressed.
Received: 8 November 2017 / Revised: 22 November 2017 / Accepted: 23 November 2017 / Published: 24 November 2017
(This article belongs to the Section Medicinal Chemistry)
View Full-Text   |   Download PDF [551 KB, uploaded 24 November 2017]   |  

Abstract

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 26 were isolated from the entomogenous fungus Isaria fumosorosea. The structures of 26 were elucidated by extensive spectroscopic analysis. Fumosorinone A (1) and beauvericin (6) showed significant PTP1B inhibitory activity with IC50 value of 3.24 μM and 0.59 μM. View Full-Text
Keywords: Isaria fumosorosea; PTP1B; pyrrolidinedione Isaria fumosorosea; PTP1B; pyrrolidinedione
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Zhang, J.; Meng, L.-L.; Wei, J.-J.; Fan, P.; Liu, S.-S.; Yuan, W.-Y.; Zhao, Y.-X.; Luo, D.-Q. PTP1B Inhibitors from the Entomogenous Fungi Isaria fumosorosea. Molecules 2017, 22, 2058.

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