Inhibition of VHR dual-specificity protein tyrosine phosphatase activity by flavonoids isolated from Scutellaria baicalensis: structure-activity relationships.
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.
Lee
Myung Sun
MS
Korea Research Institute of Bioscience and Biotechnology (KRIBB), Daejeon, South Korea.
Oh
Won Keun
WK
Kim
Bo Yeon
BY
Ahn
Soon Cheol
SC
Kang
Dae Ook
DO
Sohn
Cheon Bae
CB
Osada
Hiroyuki
H
Ahn
Jong Seog
JS
D004305:Dose-Response Relationship, Drug; D054640:Dual Specificity Phosphatase 3; D044950:Flavanones; D047309:Flavones; D005419:Flavonoids / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D015394:Molecular Structure; D010749:Phosphoprotein Phosphatases / Q000037:antagonists & inhibitors; D008517:Phytotherapy; D010936:Plant Extracts / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D018517:Plant Roots / Q000737:chemistry; D054645:Protein Phosphatase 1; D017027:Protein Tyrosine Phosphatases / Q000037:antagonists & inhibitors*; D031364:Scutellaria baicalensis; D013329:Structure-Activity Relationship
D044950:Flavanones; D047309:Flavones; D005419:Flavonoids; D010936:Plant Extracts; C472146:dihydronorwagonin; C055505:norwogonin; C006680:baicalein; D010749:Phosphoprotein Phosphatases; D054645:Protein Phosphatase 1; D054640:Dual Specificity Phosphatase 3; D017027:Protein Tyrosine Phosphatases