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The GPR55 antagonist CID16020046 protects against ox-LDL-induced inflammation in human aortic endothelial cells (HAECs).
Archives of Biochemistry and Biophysics ( IF 3.9 ) Pub Date : 2020-01-03 , DOI: 10.1016/j.abb.2020.108254
Yaowen Wang 1 , Wei Pan 2 , Yan Wang 3 , Yuehui Yin 1
Affiliation  

Atherosclerosis is a commonplace cardiovascular disease which affects most people in old age. While its causes are currently poorly understood, continuous study is being performed in order to elucidate both the pathogenesis and treatment of this insidious disease. Atherosclerosis is presently thought to be linked to several factors such as endothelial dysfunction, monocyte adhesion to the intima of the artery, and increased oxidative stress. Oxidized low-density lipoprotein (ox-LDL), colloquially known as the "bad cholesterol", is known to play a critical role in the previously mentioned atherosclerotic processes. In this study, our goal was to elucidate the role of the lysophospholipid receptor G protein-coupled receptor 55 (GPR55) and its antagonist, the cannabinoid CID16020046, in endothelial dysfunction. While their existence and especially their role in atherosclerosis has only semi-recently been elucidated, a growing body of research has begun to link their interaction to antiatherosclerosis. In our research, we found CID16020046 to have distinct atheroprotective properties such as anti-inflammation, antioxidant, and inhibition of monocyte attachment to endothelial cells. While there was previously a small body of research regarding the potential of cannabinoids to treat or prevent atherosclerosis, studies on the treatment potential of CID16020046 were even fewer. Thus, this study is one of the first to explore the effects of cannabinoids in atherosclerosis. Our findings in the present study provide a strong argument for the use of CID16020046 in the treatment of atherosclerosis as well as a basis for further experimentation using cannabinoids as therapy against atherosclerosis.

中文翻译:

GPR55拮抗剂CID16020046可防止ox-LDL诱导的人主动脉内皮细胞(HAEC)炎症。

动脉粥样硬化是一种常见的心血管疾病,会影响大多数老年人。尽管目前尚不清楚其病因,但仍在进行持续研究以阐明这种潜伏性疾病的发病机理和治疗方法。目前认为动脉粥样硬化与多种因素有关,例如内皮功能障碍,单核细胞粘附在动脉内膜上以及氧化应激增加。俗称“坏胆固醇”的氧化型低密度脂蛋白(ox-LDL)在前面提到的动脉粥样硬化过程中起着关键作用。在这项研究中,我们的目标是阐明溶血磷脂受体G蛋白偶联受体55(GPR55)及其拮抗剂大麻素CID16020046在内皮功能障碍中的作用。尽管仅在最近才阐明了它们的存在,尤其是它们在动脉粥样硬化中的作用,但越来越多的研究已开始将它们的相互作用与抗动脉粥样硬化联系起来。在我们的研究中,我们发现CID16020046具有独特的抗动脉粥样硬化特性,例如抗炎,抗氧化和抑制单核细胞附着于内皮细胞。尽管以前对大麻素治疗或预防动脉粥样硬化的潜力的研究很少,但对CID16020046的治疗潜力的研究甚至更少。因此,这项研究是第一个探索大麻素在动脉粥样硬化中作用的研究。
更新日期:2020-01-04
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