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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 Na; K A Kim; H Oh; Bo Yeon Kim; Won Keun Oh; Jong Seog Ahn |
Publisher | Pharmaceutical Society of Japan |
Issue Date | 2007 |
Citation | Biological & Pharmaceutical Bulletin, vol. 30, no. 2, pp. 379-381 |
Keywords | amentoflavone; non-competitive inhibitor; protein tyrosine phosphatase 1B; selaginella tamariscina; selaginellaceae; tyrosine phosphorylation of insulin receptor; insulin receptor; protein tyrosine phosphatase 1B inhibitor; tyrosine |
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 | |
Appears in Collections | |
Registered Date |
2019-05-02 |
| Files in This Item: | Size | Format | |
|---|---|---|---|
| 6913.pdf | 197Kb | Adobe PDF | 
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