Protein Tyrosine Phosphatase 1B Inhibitory Activity of Amentoflavone and Its Cellular Effect on Tyrosine Phosphorylation of Insulin Receptors(Pharmacognosy)

概要

論文の詳細を見る
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 tamarisdna (Selaginellaceae) afforded a PTP1B inhibitory compound, amentoflavone. The compound inhibited PTP1B with an IC_<50> value of 7.3±0.5μM. Kinetic study suggested that amentoflavone is a non-competitive inhibitor of PTP1B, with a K_i value of 5.2μM. 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.
社団法人日本薬学会の論文
2007-02-01