Novakovic Aleksandra, Gojkovic-Bukarica Ljiljana, Peric Miodrag, Nezic Dusan, Djukanovic Bosko, Markovic-Lipkovski Jasmina, Heinle Helmut
Department of Pharmacology, Faculty of Pharmacy, University of Belgrade, Serbia and Montenegro.
J Pharmacol Sci. 2006 May;101(1):85-90. doi: 10.1254/jphs.fp0050863. Epub 2006 May 9.
Resveratrol, a stilbene polyphenol found in grapes and red wine, produces vasorelaxation in both endothelium-dependent and endothelium-independent manners. The mechanisms by which resveratrol causes vasodilatation are uncertain. The aim of this study was to investigate the mechanism(s) of endothelium-independent resveratrol-induced vasorelaxation in human internal mammary artery (HIMA) obtained from male patients undergoing coronary artery bypass surgery and to clarify the contribution of different K+ channel subtypes in resveratrol action in this blood vessel. HIMA rings without endothelium were precontracted with phenylephrine. Resveratrol induced a concentration-dependent relaxation of the HIMA. A highly selective blocker of ATP-sensitive K+ channels, glibenclamide, as well as nonselective blockers of Ca2+-sensitive K+ channels, tetraethylammonium and charybdotoxin, did not block resveratrol induced relaxation of HIMA rings. 4-Aminopyridine (4-AP), non selective blocker of voltage gated K+ (KV) channels, and margatoxin that inhibits KV1.2, KV1.3, and KV1.6 channels abolished relaxation of HIMA rings induced by resveratrol. In conclusion, we have shown that resveratrol potently relaxed HIMA rings with denuded endothelium. It seems that 4-AP- and margatoxin-sensitive K+ channels located in smooth muscle of HIMA mediated this relaxation.
白藜芦醇是一种存在于葡萄和红酒中的芪类多酚,它能以依赖内皮和不依赖内皮的方式引起血管舒张。白藜芦醇导致血管舒张的机制尚不清楚。本研究的目的是探讨在接受冠状动脉搭桥手术的男性患者获取的人乳内动脉(HIMA)中,白藜芦醇诱导的不依赖内皮的血管舒张机制,并阐明不同钾通道亚型在该血管白藜芦醇作用中的贡献。去除内皮的HIMA血管环用去氧肾上腺素预收缩。白藜芦醇诱导HIMA产生浓度依赖性舒张。ATP敏感性钾通道的高选择性阻滞剂格列本脲,以及钙敏感性钾通道的非选择性阻滞剂四乙铵和蝎毒素,均不能阻断白藜芦醇诱导的HIMA血管环舒张。电压门控钾(KV)通道的非选择性阻滞剂4-氨基吡啶(4-AP)以及抑制KV1.2、KV1.3和KV1.6通道的玛格毒素可消除白藜芦醇诱导的HIMA血管环舒张。总之,我们已经表明白藜芦醇能有效舒张去除内皮的HIMA血管环。似乎位于HIMA平滑肌中的对4-AP和玛格毒素敏感的钾通道介导了这种舒张。