In vitro protein tyrosine phosphatase 1B inhibitory phenols from the seeds of Psoralea corylifolia

Abstract Protein tyrosine phosphatase 1B plays a major role in the negative regulation of insulin signaling, and this establishes protein tyrosine phosphatase 1B as an attractive therapeutic target for diabetes. Bioassay-guided fractionation of the EtOAc-soluble extract of the seeds of PSORALEA CORY...

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Veröffentlicht in:	Planta medica 2005, Vol.71 (1), p.87-89
Hauptverfasser:	Kim, Y.C, Oh, H, Kim, B.S, Kang, T.H, Ko, E.K, Han, Y.M, Kim, B.Y, Ahn, J.S
Format:	Artikel
Sprache:	eng
Schlagworte:	bakuchiol chemical structure Cullen corylifolium Dose-Response Relationship, Drug enzyme inhibition enzyme inhibitors Enzyme Inhibitors - administration & dosage Enzyme Inhibitors - pharmacology Enzyme Inhibitors - therapeutic use enzyme kinetics Faboideae Humans Letter medicinal plants phenols Phenols - administration & dosage Phenols - pharmacology Phenols - therapeutic use phosphoric monoester hydrolases phytochemicals Phytotherapy plant extracts Plant Extracts - administration & dosage Plant Extracts - pharmacology Plant Extracts - therapeutic use protein tyrosine phosphatase 1B Protein Tyrosine Phosphatase, Non-Receptor Type 1 Protein Tyrosine Phosphatases - antagonists & inhibitors Psoralea psoralidin Seeds
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Zusammenfassung:	Abstract Protein tyrosine phosphatase 1B plays a major role in the negative regulation of insulin signaling, and this establishes protein tyrosine phosphatase 1B as an attractive therapeutic target for diabetes. Bioassay-guided fractionation of the EtOAc-soluble extract of the seeds of PSORALEA CORYLIFOLIA afforded two protein tyrosine phosphatase 1B inhibitory compounds, psoralidin (1) and bakuchiol (2), along with inactive corylin. Compounds 1 and 2 inhibited PTP1B activity in a dose-dependent manner, displaying IC 50 values of 9.4 ± 0.5 μM and 20.8 ± 1.9 μM, respectively.
ISSN:	0032-0943 1439-0221
DOI:	10.1055/s-2005-837759