Protein Tyrosine Phosphatase 1B Inhibitory Activity of 24-Norursane Triterpenes Isolated from Weigela subsessilis

Title
Protein Tyrosine Phosphatase 1B Inhibitory Activity of 24-Norursane Triterpenes Isolated from Weigela subsessilis
Author(s)
나민균Phuong Thien Thuong[Phuong Thien Thuong]황인현배기환[배기환]김보연[김보연]Hiroyuki Osada[Hiroyuki Osada]안종석[안종석]
Keywords
INSULIN SIGNAL-TRANSDUCTION; OBESITY; RESISTANCE
Issue Date
201011
Publisher
JOHN WILEY & SONS LTD
Citation
PHYTOTHERAPY RESEARCH, v.24, no.11, pp.1716 - 1719
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 IC(50) values of 29.1 +/- 2.8 and 5.3 +/- 0.5 mu M, 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. Copyright (C) 2010 John Wiley & Sons, Ltd.
URI
http://hdl.handle.net/YU.REPOSITORY/23342http://dx.doi.org/10.1002/ptr.3203
ISSN
0951-418X
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약학대학 > 약학부 > Articles
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