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  • 标题:Baicalein Potently Inhibits Rho Kinase Activity and Suppresses Actin Stress Fiber Formation in Angiotensin II-Stimulated H9c2 Cells
  • 本地全文:下载
  • 作者:Kwang-Seok Oh ; Byung Koo Oh ; Cheon Ho Park
  • 期刊名称:Biological and Pharmaceutical Bulletin
  • 印刷版ISSN:0918-6158
  • 电子版ISSN:1347-5215
  • 出版年度:2012
  • 卷号:35
  • 期号:8
  • 页码:1281-1286
  • DOI:10.1248/bpb.b12-00121
  • 出版社:The Pharmaceutical Society of Japan
  • 摘要:Baicalein is a flavonoid (5,6,7-trihydroxy-2-phenyl-4 H -1-benzopyran4-one) and an active principle in Scutellaria baicalensis . The present study was performed to investigate the mechanisms underlying the anti-fibrotic effects of baicalein with a focus on Rho kinase (ROCK) inhibition. The effect of baicalein on ROCK activity was analyzed using an immobilized metal affinity for phosphochemicals (IMAP)-based time-resolved fluorescence resonance energy transfer (TR-FRET) assay. The underlying mechanisms of baicalein were examined using angiotensin II-stimulated H9c2 cells. Rho kinase (ROCK1 and ROCK2) studies using IMAP-TR-FRET showed that baicalein possesses potent ROCK inhibitory activity with IC50 values of 6.55 and 2.82 µ M , respectively. Pretreatment with baicalein (for 2 h) concentration-dependently decreased the angiotensin II-induced phosphorylation of myosin phosphatase (MYPT) and myosin light chain (MLC). Furthermore, baicalein also concentration-dependently suppressed actin stress fiber formation in angiotensin II-stimulated H9c2 cells. These results suggest that baicalein potently inhibits ROCK and that by so doing it modulates actin stress fiber formation. These anti-fibrotic effects of baicalein explain, at least in part, its pharmacology and mode of action.
  • 关键词:baicalein;Rho kinase;angiotensin II;actin stress fiber;H9c2 cell
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