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Phytother Res. 2006 Aug;20(8):680-2.

Inhibition of protein tyrosine phosphatase 1B by lignans from Myristica fragrans.

Author information

1
Korea Research Institute of Bioscience and Biotechnology (KRIBB), 52 Eoeun-dong, Yusong-gu, Daejeon 305-333, Korea.

Abstract

Inhibition of protein tyrosine phosphatase 1B (PTP1B) has been proposed as one of the drug targets for treating type 2 diabetes and obesity. Bioassay-guided fractionation of a MeOH extract of the semen of Myristica fragrans Houtt. (Myristicaceae) afforded PTP1B inhibitory compounds, meso-dihydroguaiaretic acid (1) and otobaphenol (2). Compounds 1 and 2 inhibited PTP1B with IC(50) values of 19.6 +/- 0.3 and 48.9 +/- 0.5 microM, respectively, in the manner of non-competitive inhibitors. Treatment with compound 1 on 32D cells overexpressing the insulin receptor (IR) resulted in a dose-dependent increase in the tyrosine phosphorylation of IR. These results indicate that compound 1 can act as an enhancing agent in intracellular insulin signaling, possibly through the inhibition of PTP1B activity.

PMID:
16752372
DOI:
10.1002/ptr.1935
[Indexed for MEDLINE]

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