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Inhibition of protein tyrosine phosphatase 1B by lignans from Myristica fragrans
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AbstractInhibition 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 IC50 values of 19.6 ± 0.3 and 48.9 ± 0.5 µm, 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. Copyright © 2006 John Wiley & Sons, Ltd.
Title: Inhibition of protein tyrosine phosphatase 1B by lignans from Myristica fragrans
Description:
AbstractInhibition 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 IC50 values of 19.
6 ± 0.
3 and 48.
9 ± 0.
5 µm, 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.
Copyright © 2006 John Wiley & Sons, Ltd.
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