Effects of baicalein isolated from Scutellaria baicalensis Radix on adhesion molecule expression induced by thrombin and thrombin receptor agonist peptide in cultured human umbilical vein endothelial cells.
We examined the effects of various flavonoids isolated from the roots of Scutellaria baicalensis Georgi on adhesion molecule expression induced by thrombin and thrombin receptor agonist peptide (SFLLRNPNDKYEPF, TRAP) in cultured human umbilical vein endothelial cells. Thrombin and thrombin receptor agonist peptide induced endothelial leukocyte adhesion molecule-1 (ELAM-1) expression. Intercellular adhesion molecule-1 (ICAM-1) expression was also induced by thrombin, but not by TRAP. Baicalein isolated from Scutellariae Radix inhibited ELAM-1 expression induced by thrombin and thrombin receptor agonist peptide dose-dependently, with 50% inhibitory concentrations (IC50) of 5.53 +/- 1.68 microM and 2.44 +/- 1.08 microM, respectively. Furthermore, baicalein inhibited thrombin-induced ICAM-1 expression with an IC50 of 9.67 +/- 1.28 microM. In addition, baicalein inhibited the expressions of ELAM-1 and ICAM-1 stimulated by protein kinase C (PKC) activator phorbol myristate acetate (PMA).
Kimura
Y
Y
2nd Department of Medical Biochemistry, School of Medicine, Ehime University, Ehime, Japan. yokim@m.ehime-u.ac.jp
Matsushita
N
N
Yokoi-Hayashi
K
K
Okuda
H
H
D000595:Amino Acid Sequence; D000704:Analysis of Variance; D002478:Cells, Cultured / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D019040:E-Selectin / Q000187:drug effects; D004730:Endothelium, Vascular / Q000166:cytology / Q000187:drug effects; D005260:Female; D044950:Flavanones; D005419:Flavonoids / Q000302:isolation & purification* / Q000494:pharmacology; D006801:Humans; D018799:Intercellular Adhesion Molecule-1 / Q000187:drug effects; D008516:Medicine, Chinese Traditional; D018517:Plant Roots / Q000737:chemistry; D010946:Plants, Medicinal / Q000737:chemistry*; D011493:Protein Kinase C / Q000037:antagonists & inhibitors / Q000187:drug effects; D011506:Proteins / Q000494:pharmacology; D018179:Receptors, Thrombin; D013755:Tetradecanoylphorbol Acetate / Q000494:pharmacology; D013917:Thrombin / Q000494:pharmacology; D014471:Umbilical Veins / Q000187:drug effects
D019040:E-Selectin; D044950:Flavanones; D005419:Flavonoids; D011506:Proteins; D018179:Receptors, Thrombin; D018799:Intercellular Adhesion Molecule-1; C006680:baicalein; D011493:Protein Kinase C; D013917:Thrombin; D013755:Tetradecanoylphorbol Acetate