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Title 

Protein tyrosine phosphatase 1B inhibitory activity of amentoflavone and its cellular effect on tyrosine phosphorylation of insulin receptors

Authors 

M K NaK A KimH OhBo Yeon KimWon Keun OhJong Seog Ahn

Publisher 

Pharmaceutical Society of Japan

Issue Date 

2007

Citation 

Biological & Pharmaceutical Bulletin, vol. 30, no. 2, pp. 379-381

Keywords 

amentoflavonenon-competitive inhibitorprotein tyrosine phosphatase 1Bselaginella tamariscinaselaginellaceaetyrosine phosphorylation of insulin receptorinsulin receptorprotein tyrosine phosphatase 1B inhibitortyrosine

Abstract 

Inhibition of protein tyrosine phosphatase 1B (PTP1B) has been proposed as a strategy for the treatment of type 2 diabetes and obesity. Bioassay-guided fractionation of MeOH extract of Selaginella tamariscina (Selaginellaceae) afforded a PTP1B inhibitory compound, amentoflavone. The compound inhibited PTP1B with an IC50 value of 7.3±0.5 μM. Kinetic study suggested that amentoflavone is a non-competitive inhibitor of PTP1B, with a Ki value of 5.2 μM. Treatment of 32D cells overexpressing the insulin receptor (IR) with amentoflavone resulted in a dose-dependent increase in tyrosine phosphorylation of IR. These results indicate that amentoflavone may enhance insulin-induced intracellular signaling possibly through inhibition of PTP1B activity.

ISSN 

0918-6158

Link 

http://dx.doi.org/10.1248/bpb.30.379

Appears in Collections

1. Journal Articles > Journal Articles

Registered Date

2017-04-19


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