Gold M E, Wood K S, Byrns R E, Fukuto J, Ignarro L J
Department of Pharmacology, University of California, School of Medicine, Los Angeles 90024.
Proc Natl Acad Sci U S A. 1990 Jun;87(12):4430-4. doi: 10.1073/pnas.87.12.4430.
The objective of this study was to determine whether the vascular smooth muscle contractile effect of NG-methyl-L-arginine (NMA) is endothelium dependent and attributed to a decline in smooth muscle levels of cyclic GMP. Vascular smooth muscle levels of cyclic GMP are severalfold greater in endothelium-intact than in endothelium-denuded preparations because of the continuous formation and release of a lipophilic endothelium-derived chemical factor that diffuses into the underlying smooth muscle and activates cytosolic guanylate cyclase. This chemical substance, believed to be nitric oxide (NO) or a labile nitroso precursor, appears to account for the biological actions of endothelium-derived relaxing factor. NMA inhibits the formation of NO from endogenous L-arginine in endothelial cells. In the present study, NMA caused marked endothelium-dependent contraction of isolated rings of bovine pulmonary artery and vein, and this was similar to the contraction elicited by hemoglobin, an inhibitor of the relaxant action of NO. Both NMA and hemoglobin caused endothelium-dependent potentiation of contractile responses to phenylephrine in artery and vein. NMA caused endothelium-dependent decreases in the resting or basal levels of cyclic GMP in artery and vein to levels that were characteristic of those in endothelium-denuded vessels. Finally, NMA inhibited endothelium-dependent relaxant responses and cyclic GMP formation stimulated by acetylcholine and bradykinin. These observations reveal that interference with the continuous or basal generation of endothelium-derived NO in artery and vein can cause marked increases in vascular smooth muscle tone as a result of inhibition of cyclic GMP formation.
本研究的目的是确定NG-甲基-L-精氨酸(NMA)对血管平滑肌的收缩作用是否依赖于内皮,以及是否归因于平滑肌中环状鸟苷酸(cGMP)水平的下降。由于一种亲脂性内皮衍生化学因子的持续形成和释放,完整内皮的血管平滑肌中cGMP水平比去内皮制剂中的高出几倍,该化学因子扩散到下层平滑肌并激活胞质鸟苷酸环化酶。这种化学物质,被认为是一氧化氮(NO)或一种不稳定的亚硝基前体,似乎可以解释内皮衍生舒张因子的生物学作用。NMA抑制内皮细胞中内源性L-精氨酸生成NO。在本研究中,NMA引起牛肺动脉和静脉离体环明显的内皮依赖性收缩,这与血红蛋白(一种NO舒张作用的抑制剂)引起的收缩相似。NMA和血红蛋白均引起动脉和静脉对去氧肾上腺素收缩反应的内皮依赖性增强。NMA使动脉和静脉中cGMP的静息或基础水平呈内皮依赖性降低,降至去内皮血管特有的水平。最后,NMA抑制了乙酰胆碱和缓激肽刺激的内皮依赖性舒张反应和cGMP形成。这些观察结果表明,干扰动脉和静脉中内皮衍生NO的持续或基础生成,可因抑制cGMP形成而导致血管平滑肌张力显著增加。