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Title 

Isolation of the protein tyrosine phosphatase 1B inhibitory metabolite from the marine-derived fungus Cosmospora sp. SF-5060

Authors 

C SeoJ H SohnH OhBo Yeon KimJong Seog Ahn

Publisher 

Elsevier

Issue Date 

2009

Citation 

Bioorganic & Medicinal Chemistry Letters, vol. 19, no. 21, pp. 6095-6097

Keywords 

Competitive inhibitorCosmospora sp.Fungal metaboliteMarine-derived fungusProtein tyrosine phosphatase 1B (PTP1B)

Abstract 

In the course of bioassay-guided study on the EtOAc extract of a culture broth of the marine-derived fungus Cosmospora sp. SF-5060, aquastatin A (1) was isolated as a protein tyrosine phosphatase 1B (PTP1B) inhibitory component produced by the fungus. The compound was isolated by various chromatographic methods, and the structure was determined mainly by analysis of NMR spectroscopic data. Compound 1 exhibited potent inhibitory activity against PTP1B with IC50 value of 0.19 μM, and the kinetic analyses of PTP1B inhibition by compound 1 suggested that the compound is inhibiting PTP1B activity in a competitive manner. Aquastatin A (1) also showed modest but selective inhibitory activity toward PTP1B over other protein tyrosine phosphatases, such as TCPTP, SHP-2, LAR, and CD45. In addition, the result of hydrolyzing aquastatin A (1) suggested that the dihydroxypentadecyl benzoic acid moiety in the molecule is responsible for the inhibitory activity.

ISSN 

0960-894X

Link 

http://dx.doi.org/10.1016/j.bmcl.2009.09.025

Appears in Collections

1. Journal Articles > Journal Articles

Registered Date

2019-05-02


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