Protein tyrosine phosphatase 1B inhibitory activity of 24-norursane triterpenes isolated from Weigela subsessilis = PTP1b 저해 24-noursane triterperne 화합물

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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
Author(s)
M Na; P T Thuong; I H Hwang; K Bae; Bo Yeon Kim; H Osada; Jong Seog Ahn
Bibliographic Citation
Phytotherapy Research, vol. 24, no. 11, pp. 1716-1719
Publication Year
2010
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.
Keyword
CaprifoliaceaeIlekudinol AIlekudinol BNon-competitive inhibitorsProtein tyrosine phosphatase 1BWeigela subsessilis
ISSN
0951-418X
Publisher
Wiley
DOI
http://dx.doi.org/10.1002/ptr.3203
Type
Article
Appears in Collections:
Ochang Branch Institute > Chemical Biology Research Center > 1. Journal Articles
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