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Title 

Inhibition of protein tyrosine phosphatase 1B by prenylated isoflavonoids isolated from the stem bark of Erythrina addisoniae

Authors 

Eun Young BaeMin Kyun NaD NjamenJ T MbaforZ T FomumL CuiDong-Ho ChoungBo Yeon KimWon Keun OhJong Seog Ahn

Publisher 

Georg Thieme Verlag

Issue Date 

2006

Citation 

Planta Medica, vol. 72, no. 10, pp. 945-948

Keywords 

erythrina extractprotein tyrosine phosphatase 1Bprotein tyrosine phosphatase 1B inhibitorbarkdrug inhibitionenzyme inhibitionerythrinaplant stemplant stemsprotein-tyrosine-phosphatase

Abstract 

It has been suggested that protein tyrosine phosphatase IB (PTP1B) inhibitors might be a therapeutic target for the treatment of type 2 diabetes and obesity. A bioassay-guided phytochemical study of the EtOAc extract of the stem bark of Erythrina addisoniae (Leguminosae) resulted in the identification of a new PTP1B inhibitory compound, 5,2′4′-trihydroxy-6-(γ, γ-dimethylallyl)-2?,2?-dimethyldihydropyrano[5?, 6?]isoflavanone (6), along with five known prenylated isoflavonoids, orientanol E (1), senegalensin (2), warangalone (3), warangalone 4′-methyl ether (4) and 2,3-dihydroauriculatin (5). Compounds 1, 5 and 6 inhibited PTP1B with IC50 values ranging from 2.6 ± 0.5 to 10.1 ± 0.3 μM. Our results indicate that hydroxylation at both 2′- and 4′-positions in the B-ring and cyclization between a hydroxy group at C-7 and one of the prenyl groups at C-6 or C-8 in the A-ring may be important for activity. Thus, compounds 5 and 6 could be a new class of natural PTP1B inhibitors.

ISSN 

0032-0943

Link 

http://dx.doi.org/10.1055/s-2006-946674

Appears in Collections

1. Journal Articles > Journal Articles

Registered Date

2019-05-02


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