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Inhibition of protein tyrosine phosphatase 1B by lignans from Myristica fragrans
Author(s) -
Yang Senugmi,
Min Kyun Na,
Jang Jun Pil,
Kim Kyung Ah,
Kim Bo Yeon,
Sung Nak Ju,
Oh Won Keun,
Ahn Jong Seog
Publication year - 2006
Publication title -
phytotherapy research
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.019
H-Index - 129
eISSN - 1099-1573
pISSN - 0951-418X
DOI - 10.1002/ptr.1935
Subject(s) - protein tyrosine phosphatase , myristica fragrans , pharmacology , fractionation , biochemistry , phosphorylation , insulin receptor , tyrosine , chemistry , biology , insulin , traditional medicine , medicine , endocrinology , chromatography , insulin resistance
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 µ m , 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.