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Molecules 2014, 19(2), 1663-1671; doi:10.3390/molecules19021663
Article

Penostatin Derivatives, a Novel Kind of Protein Phosphatase 1B Inhibitors Isolated from Solid Cultures of the Entomogenous Fungus Isaria tenuipes

1,2, 1,2, 1,2, 1,2, 1,2,* , 3 and 3
1 College of Life Science, Key Laboratory of Medicinal Chemistry and Molecular Diagnosis of Ministry of Education, Hebei University, Baoding 071002, China 2 Biotechnology Center of Hebei Province, Hebei University, Baoding 071002, China 3 New Drug Research and Development Center, North China Pharmaceutical Group Corporation, Shijiazhuang 051007, China
* Author to whom correspondence should be addressed.
Received: 20 December 2013 / Revised: 22 January 2014 / Accepted: 23 January 2014 / Published: 29 January 2014
(This article belongs to the Section Metabolites)
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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. Therefore, small molecular inhibitors of PTP1B can be considered as an attractive approach for the design of new therapeutic agents of type II diabetes diseases. In a continuing search for new protein phosphatase inhibitors from fungi, we have isolated a new compound, named penostatin J (1), together with three known ones, penostatin C (2), penostatin A (3), and penostatin B (4), from cultures of the entomogenous fungus Isaria tenuipes. The structure of penostatin J (1) was elucidated by extensive spectroscopic analysis. We also demonstrate for the first time that penostatin derivatives exhibit the best PTP1B inhibitory action. These findings suggest that penostatin derivatives are a potential novel kind of PTP1B inhibitors.
Keywords: Isaria tenuipes; penostatin derivatives; protein phosphatase 1B inhibitor Isaria tenuipes; penostatin derivatives; protein phosphatase 1B inhibitor
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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Chen, Y.-P.; Yang, C.-G.; Wei, P.-Y.; Li, L.; Luo, D.-Q.; Zheng, Z.-H.; Lu, X.-H. Penostatin Derivatives, a Novel Kind of Protein Phosphatase 1B Inhibitors Isolated from Solid Cultures of the Entomogenous Fungus Isaria tenuipes. Molecules 2014, 19, 1663-1671.

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