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.
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Authors | Minkyun Na, Bo Yeon Kim, Hiroyuki Osada, Jong Seog Ahn |
Journal | Journal of enzyme inhibition and medicinal chemistry
(J Enzyme Inhib Med Chem)
Vol. 24
Issue 4
Pg. 1056-9
(Aug 2009)
ISSN: 1475-6374 [Electronic] England |
PMID | 19548777
(Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
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Chemical References |
- Enzyme Inhibitors
- Pentacyclic Triterpenes
- Plant Extracts
- Triterpenes
- lupenone
- Protein Tyrosine Phosphatase, Non-Receptor Type 1
- lupeol
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Topics |
- Binding, Competitive
- Enzyme Activation
(drug effects)
- Enzyme Inhibitors
(isolation & purification, pharmacology)
- Molecular Structure
- Pentacyclic Triterpenes
(pharmacology)
- Plant Bark
(chemistry)
- Plant Extracts
(chemistry)
- Plant Stems
(chemistry)
- Protein Tyrosine Phosphatase, Non-Receptor Type 1
(antagonists & inhibitors)
- Sorbus
(chemistry)
- Triterpenes
(pharmacology)
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