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Title 

Protein tyrosine phosphatase 1B inhibitors isolated from Morus bombycis

Authors 

D M HoangT M NgocN T DatD T HaY H KimH V LuongJong Seog AhnK Bae

Publisher 

Elsevier

Issue Date 

2009

Citation 

Bioorganic & Medicinal Chemistry Letters, vol. 19, no. 23, pp. 6759-6761

Keywords 

2-Arylbenzofuran derivativesChalcone-derived Diels-Alder typesMorus bombycisProtein tyrosine phosphatase 1B (PTP1B)

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.

ISSN 

0960-894X

Link 

http://dx.doi.org/10.1016/j.bmcl.2009.09.102

Appears in Collections

1. Journal Articles > Journal Articles

Registered Date

2017-04-19


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