Protein tyrosine phosphatase 1B inhibitors isolated from Morus bombycis.
Basic Information
ID: ALA1156122
Journal: Bioorg Med Chem Lett
Title: Protein tyrosine phosphatase 1B inhibitors isolated from Morus bombycis.
Authors: Hoang DM, Ngoc TM, Dat NT, Ha do T, Kim YH, Luong HV, Ahn JS, Bae K.
Abstract: Bioassay-guided fractionation of the chloroform-soluble fraction of Morus bombycis, using an in vitro PTP1B inhibitory assay led to the identification of three 2-arylbenzofurans, albafuran A (1), mulberrofuran W (2) and mulberrofuran D (6), along with three chalcone-derived Diels-Alder products, kuwanon J (3), kuwanon R (4), and kuwanon V (5). Compounds 1-6 showed remarkable inhibitory activity against PTP1B with IC(50) values ranging from 2.7 to 13.8 microM. Inhibition kinetics were analyzed by Lineweaver-Burk plots, which suggested that compounds 1-6 inhibited PTP1B in a mixed-type manner. The present results indicate that the respective lipophilic and hydroxyl groups of 2-arylbenzofurans and chalcone-derived Diels-Alder products play an important role in inhibition of PTP1B.
CiteXplore: 19846295
DOI: 10.1016/j.bmcl.2009.09.102
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