| 19846295 |
Hoang DM, Ngoc TM, Dat NT, Ha do T, Kim YH, Luong HV, Ahn JS, Bae K: Protein tyrosine phosphatase 1B inhibitors isolated from Morus bombycis. Bioorg Med Chem Lett. 2009 Dec 1;19(23):6759-61. Epub 2009 Oct 7.
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. |
35(0,1,1,5) |