Protein tyrosine phosphatase 1B inhibitors isolated from Morus bombycis

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Title
Protein tyrosine phosphatase 1B inhibitors isolated from Morus bombycis
Author(s)
D M Hoang; T M Ngoc; N T Dat; D T Ha; Y H Kim; H V Luong; Jong Seog Ahn; K Bae
Bibliographic Citation
Bioorganic & Medicinal Chemistry Letters, vol. 19, no. 23, pp. 6759-6761
Publication Year
2009
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 IC50 values ranging from 2.7 to 13.8 μM. 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.
Keyword
2-Arylbenzofuran derivativesChalcone-derived Diels-Alder typesMorus bombycisProtein tyrosine phosphatase 1B (PTP1B)
ISSN
0960-894X
Publisher
Elsevier
DOI
http://dx.doi.org/10.1016/j.bmcl.2009.09.102
Type
Article
Appears in Collections:
Ochang Branch Institute > Chemical Biology Research Center > 1. Journal Articles
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