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 IC50 values of 9.4 +/- 0.5 microM and 20.8 +/- 1.9 microM, respectively.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Dose-Response Relationship, Drug
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Enzyme Inhibitors / administration & dosage
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Enzyme Inhibitors / pharmacology*
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Enzyme Inhibitors / therapeutic use
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Humans
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Phenols / administration & dosage
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Phenols / pharmacology
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Phenols / therapeutic use
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Phytotherapy*
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Plant Extracts / administration & dosage
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Plant Extracts / pharmacology*
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Plant Extracts / therapeutic use
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Protein Tyrosine Phosphatase, Non-Receptor Type 1
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Protein Tyrosine Phosphatases / antagonists & inhibitors*
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Psoralea*
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Seeds
Substances
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Enzyme Inhibitors
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Phenols
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Plant Extracts
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PTPN1 protein, human
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Protein Tyrosine Phosphatase, Non-Receptor Type 1
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Protein Tyrosine Phosphatases