Laboratory of Experimental Pharmacology (LAFE), Department of Physiology and Pharmacology, Biomedical Institute, Fluminense Federal University (UFF), Room 204-A, 24420-210, Niterói, RJ, Brazil.
Laboratory of Experimental Pharmacology (LAFE), Department of Physiology and Pharmacology, Biomedical Institute, Fluminense Federal University (UFF), Room 204-A, 24420-210, Niterói, RJ, Brazil.
Eur J Pharmacol. 2020 Sep 5;882:173289. doi: 10.1016/j.ejphar.2020.173289. Epub 2020 Jun 19.
Atherosclerosis is a multifactorial chronic disease, initiated by an endothelial dysfunction. Adenosine and its analogs can change a variety of inflammatory diseases and has shown important effects at different disease models. Inosine is a stable analogous of adenosine, but its effects in inflammatory diseases, like atherosclerosis, have not yet been studied. The aim of this study was to evaluate the pharmacological properties of inosine, administered sub chronically in a hypercholesterolemic model. Male Wistar rats were divided into four groups: control group (C) and control + inosine (C + INO) received standard chow, hypercholesterolemic diet group (HCD) and HCD + inosine (HCD + INO) were fed a hypercholesterolemic diet. At 31st experimentation day, the treatment with inosine was performed for C + INO and HCD + INO groups once daily in the last 15 days. We observed that the hypercholesterolemic diet promoted an increase in lipid levels and inflammatory cytokines production, while inosine treatment strongly decreased these effects. Additionally, HCD group presented a decrease in maximum relaxation acetylcholine induced and an increase in contractile response phenylephrine induced when compared to the control group, as well as it has presented an enhancement in collagen and ADP-induced platelet aggregation. On the other hand, inosine treatment promoted a decrease in contractile response to phenylephrine, evoked an improvement in endothelium-dependent vasorelaxant response and presented antiplatelet properties. Moreover, inosine activated eNOS and reduced p38 MAPK/NF-κB pathway in aortic tissues. Taken together, the present results indicate inosine as a potential drug for the treatment of cardiovascular disorders such as atherosclerosis.
动脉粥样硬化是一种多因素的慢性疾病,由内皮功能障碍引发。腺苷及其类似物可以改变多种炎症性疾病,并在不同的疾病模型中显示出重要的效果。肌苷是腺苷的稳定类似物,但它在炎症性疾病(如动脉粥样硬化)中的作用尚未得到研究。本研究旨在评估肌苷的药理学特性,该药物在高胆固醇血症模型中进行亚慢性给药。雄性 Wistar 大鼠被分为四组:对照组(C)和对照+肌苷组(C+INO)给予标准饲料,高胆固醇饮食组(HCD)和 HCD+肌苷组(HCD+INO)给予高胆固醇饮食。在第 31 天实验日,对 C+INO 和 HCD+INO 组进行肌苷治疗,每天一次,持续 15 天。我们观察到,高胆固醇饮食促进了脂质水平和炎症细胞因子产生的增加,而肌苷治疗强烈降低了这些效果。此外,与对照组相比,HCD 组在最大松弛乙酰胆碱诱导时表现出舒张功能下降,而在苯肾上腺素诱导的收缩反应中表现出增加,并且胶原和 ADP 诱导的血小板聚集增强。另一方面,肌苷治疗促进了对苯肾上腺素的收缩反应的降低,引起了内皮依赖性血管舒张反应的改善,并表现出抗血小板特性。此外,肌苷激活了 eNOS 并减少了主动脉组织中 p38 MAPK/NF-κB 通路。综上所述,这些结果表明肌苷可能是治疗心血管疾病如动脉粥样硬化的潜在药物。