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

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Title
Protein tyrosine phosphatase 1B inhibitory activity of amentoflavone and its cellular effect on tyrosine phosphorylation of insulin receptors
Author(s)
M K Na; K A Kim; H Oh; Bo Yeon Kim; Won Keun Oh; Jong Seog Ahn
Bibliographic Citation
Biological & Pharmaceutical Bulletin, vol. 30, no. 2, pp. 379-381
Publication Year
2007
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.
Keyword
amentoflavonenon-competitive inhibitorprotein tyrosine phosphatase 1Bselaginella tamariscinaselaginellaceaetyrosine phosphorylation of insulin receptor
ISSN
0918-6158
Publisher
Pharmaceutical Soc Japan
DOI
http://dx.doi.org/10.1248/bpb.30.379
Type
Article
Appears in Collections:
Ochang Branch Institute > Chemical Biology Research Center > 1. Journal Articles
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