Abstract |
It has been suggested that protein tyrosine phosphatase 1B (PTP1B) inhibitors might be a therapeutic target for the treatment of type 2 diabetes and obesity. A bioassay-guided phytochemical study of the EtOAc extract of the stem bark of Erythrina addisoniae (Leguminosae) resulted in the identification of a new PTP1B inhibitory compound, 5,2',4'-trihydroxy-6-(gamma,gamma-dimethylallyl)-2''',2'''-dimethyldihydropyrano[5''',6'''] isoflavanone ( 6), along with five known prenylated isoflavonoids, orientanol E ( 1), senegalensin ( 2), warangalone ( 3), warangalone 4'-methyl ether ( 4) and 2,3-dihydroauriculatin ( 5). Compounds 1, 5 and 6 inhibited PTP1B with IC (50) values ranging from 2.6 +/- 0.5 to 10.1 +/- 0.3 microM. Our results indicate that hydroxylation at both 2'- and 4'-positions in the B-ring and cyclization between a hydroxy group at C-7 and one of the prenyl groups at C-6 or C-8 in the A-ring may be important for activity. Thus, compounds 5 and 6 could be a new class of natural PTP1B inhibitors.
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Authors | Eun Young Bae, Minkyun Na, Dieudonné Njamen, Joseph Tanyi Mbafor, Zacharias Tanee Fomum, Long Cui, Dong Ho Choung, Bo Yeon Kim, Won Keun Oh, Jong Seog Ahn |
Journal | Planta medica
(Planta Med)
Vol. 72
Issue 10
Pg. 945-8
(Aug 2006)
ISSN: 0032-0943 [Print] Germany |
PMID | 16972201
(Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
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Chemical References |
- Enzyme Inhibitors
- Isoflavones
- Plant Extracts
- PTPN1 protein, human
- Protein Tyrosine Phosphatase, Non-Receptor Type 1
- Protein Tyrosine Phosphatases
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Topics |
- Enzyme Inhibitors
(chemistry, isolation & purification, pharmacology)
- Erythrina
(chemistry)
- Humans
- Isoflavones
(chemistry, isolation & purification, pharmacology)
- Plant Extracts
(chemistry, isolation & purification, pharmacology)
- Plant Stems
(chemistry)
- Protein Tyrosine Phosphatase, Non-Receptor Type 1
- Protein Tyrosine Phosphatases
(antagonists & inhibitors)
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