Protein tyrosine phosphatase 1B inhibitors isolated from Morus bombycis

  • Bioorg Med Chem Lett. 2009 Dec 1;19(23):6759-61. doi: 10.1016/j.bmcl.2009.09.102.
Duc Manh Hoang  1 ,  Tran Minh Ngoc ,  Nguyen Tien Dat ,  Do Thi Ha ,  Young Ho Kim ,  Hoang Van Luong ,  Jong Seog Ahn ,  KiHwan Bae
Affiliations
  • 1. Functional Metabolite Research Center, Korea Research Institute of Bioscience and Biotechnology, Yuseong-gu, Daejeon 305-333, Republic of Korea.
PMID: 19846295 DOI: 10.1016/j.bmcl.2009.09.102
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.

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