Journal
BIOLOGICAL & PHARMACEUTICAL BULLETIN
Volume 30, Issue 2, Pages 379-381Publisher
PHARMACEUTICAL SOC JAPAN
DOI: 10.1248/bpb.30.379
Keywords
protein tyrosine phosphatase 1B; Selaginella tamariscina; Selaginellaceae; amentoflavone; non-competitive inhibitor; tyrosine phosphorylation of insulin receptor
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Inhibition of protein tyrosine phosphatase IB (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 mu m. Kinetic study suggested that amentoflavone is a non-competitive inhibitor of PTP1B, with a K-i value of 5.2 mu m. 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.
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