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Title 

Protein tyrosine phosphatase 1B inhibitory activity of 24-norursane triterpenes isolated from Weigela subsessilis

 

PTP1b 저해 24-noursane triterperne 화합물

Authors 

M NaP T ThuongI H HwangK BaeBo Yeon KimH OsadaJong Seog Ahn

Publisher 

Wiley-Blackwell

Issue Date 

2010

Citation 

Phytotherapy Research, vol. 24, no. 11, pp. 1716-1719

Keywords 

CaprifoliaceaeIlekudinol AIlekudinol BNon-competitive inhibitorsProtein tyrosine phosphatase 1BWeigela subsessilis

Abstract 

During the screening effort to discover new types of protein tyrosine phosphatase 1B (PTP1B) inhibitors, it was found that a MeOH extract of the leaves and stems of Weigela subsessilis (Caprifoliaceae) inhibited the enzyme activity. By means of an in vitro bioassay-guided fractionation on the MeOH extract, two 24-norursane triterpenes, ilekudinol A (1) and ilekudinol B (2), were isolated as active metabolites. Compounds 1 and 2 inhibited PTP1B with IC50 values of 29.1 ± 2.8 and 5.3 ± 0.5 μM, respectively. Kinetic studies suggest that both 1 and 2 are non-competitive inhibitors of PTP1B. The findings indicate that the free carboxyl group at C-28 in this type of triterpenes plays a critical role in the inhibition of PTP1B.

ISSN 

0951-418X

Link 

http://dx.doi.org/10.1002/ptr.3203

Appears in Collections

1. Journal Articles > Journal Articles

Registered Date

2017-04-19


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