Favaloro Joanne L, Kemp-Harper Barbara K
Discipline of Pharmaceutical Sciences, School of Medical Sciences, Royal Melbourne Institute of Technology, Univ., PO Box 71, Bundoora West, Victoria 3083, Australia.
Am J Physiol Heart Circ Physiol. 2009 May;296(5):H1274-80. doi: 10.1152/ajpheart.00008.2009. Epub 2009 Feb 27.
The free radical form of nitric oxide (NO(.)) is a well-known mediator of vascular tone. What is not so well recognized is that NO(.) exists in several different redox forms. There is considerable evidence that NO(.) and its one-electron reduction product, nitroxyl (HNO), have pharmacologically distinct actions that extend into the regulation of the vasculature. The aim of this study was to compare the vasorelaxation mechanisms of HNO and NO(.), including an examination of the ability of these redox variants to hyperpolarize and repolarize vascular smooth muscle cells from rat mesenteric arteries. The HNO donor Angeli's salt (0.1 nM-10 microM) caused a concentration-dependent hyperpolarization of vessels at resting tone and a simultaneous, concentration-dependent vasorelaxation and repolarization of vessels precontracted and depolarized with methoxamine. Both vasorelaxation and repolarization responses to Angeli's salt were significantly attenuated by both the HNO scavenger l-cysteine (3 mM) and the voltage-dependent K(+) (K(v)) channel inhibitor 4-aminopyridine (4-AP; 1 mM) and virtually abolished by the soluble guanylate cyclase (sGC) inhibitor 1H-[1,2,4]oxadiazolo[4,3-a]quinoxalin-1-one (ODQ; 10 microM) or 30 mM K(+). In contrast, NO(.) (0.01-1 microM) repolarized arteries to a lesser extent than HNO, and these responses were resistant to inhibition by ODQ (10 microM) and 4-AP (1 mM). Blockade of K(v) channels (1 mM 4-AP) also significantly inhibited the repolarization response to YC-1 (0.1-10 microM), confirming a role for sGC/cGMP in the activation of K(v) channels in this preparation. We conclude that HNO causes vasorelaxation via a cGMP-dependent activation of K(v) channels and that there are different profiles of vasorelaxant activity for the redox siblings HNO and NO(.).
一氧化氮的自由基形式(NO(.))是一种众所周知的血管张力介质。但不太为人所知的是,NO(.)以几种不同的氧化还原形式存在。有大量证据表明,NO(.)及其单电子还原产物硝酰(HNO)具有药理学上不同的作用,这些作用延伸到血管系统的调节。本研究的目的是比较HNO和NO(.)的血管舒张机制,包括研究这些氧化还原变体使大鼠肠系膜动脉血管平滑肌细胞超极化和复极化的能力。HNO供体安吉利盐(0.1 nM - 10 microM)在静息张力下引起血管浓度依赖性超极化,并同时引起用甲氧明预收缩和去极化的血管浓度依赖性血管舒张和复极化。HNO清除剂L-半胱氨酸(3 mM)和电压依赖性钾(K(+))通道抑制剂4-氨基吡啶(4-AP;1 mM)均显著减弱了对安吉利盐的血管舒张和复极化反应,而可溶性鸟苷酸环化酶(sGC)抑制剂1H-[1,2,4]恶二唑并[4,3-a]喹喔啉-1-酮(ODQ;10 microM)或30 mM钾几乎完全消除了这些反应。相比之下,NO(.)(0.01 - 1 microM)使动脉复极化的程度小于HNO,并且这些反应对ODQ(10 microM)和4-AP(1 mM)的抑制具有抗性。阻断K(+)通道(1 mM 4-AP)也显著抑制了对YC-1(0.1 - 10 microM)的复极化反应,证实了sGC/cGMP在该制剂中激活K(+)通道的作用。我们得出结论,HNO通过cGMP依赖性激活K(+)通道引起血管舒张,并且氧化还原同源物HNO和NO(.)具有不同的血管舒张活性谱。