Abstract
Three flavonoids: norwogonin, dihydronorwogonin and baicalein, were isolated from the roots of Scutellaria baicalensis, as potential inhibitors of VHR dual-specificity protein tyrosine phosphatase (DS-PTPase). Norwogonin (IC 50 = 1.1 microM), dihydronorwogonin (IC 50 = 2.9 microM) and baicalein (IC 50 = 2.4 microM) showed potent inhibitory activity toward VHR, but had no inhibitory activity against T-cell protein tyrosine phosphatase or serine/threonine protein phosphatase 1. From comparisons to the inhibitory activities of other similar flavonoids, it could be suggested that the presence of a hydroxy group in the B ring of flavonoids interferes with the inhibitory activity toward VHR DS-PTPase.
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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Dual Specificity Phosphatase 3
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Flavanones*
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Flavones
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Flavonoids / chemistry
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Flavonoids / isolation & purification
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Flavonoids / pharmacology*
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Molecular Structure
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Phosphoprotein Phosphatases / antagonists & inhibitors
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Phytotherapy
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Plant Extracts / chemistry
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Plant Extracts / isolation & purification
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Plant Extracts / pharmacology
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Plant Roots / chemistry
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Protein Phosphatase 1
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Protein Tyrosine Phosphatases / antagonists & inhibitors*
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Scutellaria baicalensis*
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Structure-Activity Relationship
Substances
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Flavanones
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Flavones
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Flavonoids
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Plant Extracts
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dihydronorwagonin
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norwogonin
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baicalein
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Phosphoprotein Phosphatases
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Protein Phosphatase 1
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Dual Specificity Phosphatase 3
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Protein Tyrosine Phosphatases