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  • 标题:Vasodilatation Produced by Orientin and Its Mechanism Study
  • 本地全文:下载
  • 作者:Xiao-Chun Fu ; Min-Wei Wang ; Shao-Peng Li
  • 期刊名称:Biological and Pharmaceutical Bulletin
  • 印刷版ISSN:0918-6158
  • 电子版ISSN:1347-5215
  • 出版年度:2005
  • 卷号:28
  • 期号:1
  • 页码:37-41
  • DOI:10.1248/bpb.28.37
  • 出版社:The Pharmaceutical Society of Japan
  • 摘要:In this paper we investigated the vascular activity and possible mechanism of Orientin, from bamboo leaves ( Phyllostachys nigra ), in isolated thoracic aortic rings from New Zealand rabbit. Among the four compounds, studied, only Orientin relaxed phenylephrine-induced contractions with an IC50 value of 2.28 μ M in the endothelium intact and with an IC50 value around 7.27 μ M in the endothelium removed aortic rings. The vasorelaxant effect of Orientin on endothelium-intact thoracic aortic rings was attenuated by the nitric oxide (NO) synthase inhibitor N G-nitro- L -arginine methyl ester, but not by indomethacin (a cyclooxygenase inhibitor), tetraethylammonium chloride (K+ channels inhibitor) or propranolol (β-receptor inhibitor). Furthermore, Orientin inhibited norepinephrine (NE), CaCl2 and KCl-induced vasoconstriction concentration dependently in a non-competitive manner, and also reduced both the initial fast release and the sustained phases of phenylephrine-induced contractions. Orientin can stimulate NO production from endothelial cells. Orientin also increased cyclic guanosine 3,5-cyclic monophosphate (cGMP) levels without changes in adenosine-3′,5′-cyclic phosphoric acid (cAMP) in rabbit aorta. The results showed that Orientin relaxed thoracic aortic rings by the nitric oxide-cGMP pathway, and in the vascular smooth muscle inhibited the contraction induced by the activation of receptor-operating and voltage-dependent Ca2+ channels. Cyclooxygenase pathway, potassium channels, β-receptors and cAMP pathway, on the other hand, had no apparent roles. The inhibition of both intracellular Ca2+ release and extracellular Ca2+ influx may be one of the main vasorelaxant mechanisms of Orientin.
  • 关键词:orientin;vasorelaxant;endothelium;nitric oxide (NO);rabbit thoracic aorta;cyclic nucleotide
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