Inhibition of protein tyrosine phosphatase 1B by lupeol and lupenone isolated from Sorbus commixta

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Title
Inhibition of protein tyrosine phosphatase 1B by lupeol and lupenone isolated from Sorbus commixta
Author(s)
M Na; Bo Yeon Kim; H Osada; Jong Seog Ahn
Bibliographic Citation
Journal of Enzyme Inhibition and Medicinal Chemistry, vol. 24, no. 4, pp. 1056-1059
Publication Year
2009
Abstract
Protein tyrosine phosphatase 1B (PTP1B) appears to be an attractive target for the development of new drugs for type 2 diabetes and obesity. In our preliminary test, a MeOH extract of the stem barks of Sorbus commixta Hedl. (Rosaceae) showed strong PTP1B inhibitory activity. Bioassay-guided fractionation of the MeOH extract resulted in the isolation of two lupane-type triterpenes, lupenone (1) and lupeol (2). Compounds 1 and 2 inhibited PTP1B with IC(50) values of 13.7 +/- 2.1 and 5.6 +/- 0.9 microM, respectively. Kinetic studies revealed that both the compounds 1 and 2 are non-competitive inhibitors of PTP1B that decrease V(max) values with no effect on K(m) values.
ISSN
1475-6366
Publisher
T&F (Taylor & Francis)
DOI
http://dx.doi.org/10.1080/14756360802693312
Type
Article
Appears in Collections:
Ochang Branch Institute > Anticancer Agent Research Center > 1. Journal Articles
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