苯二甲酸:在动脉粥样硬化性心血管疾病和糖尿病中的作用机制和治疗用途

V. Serhiyenko, A. Serhiyenko
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引用次数: 0

摘要

苯二甲酸是一种新的降胆固醇药物,最近获得了美国食品药品管理局和欧洲药品管理局的批准。该药物通过下调ATP柠檬酸裂解酶和上调ATP活化蛋白激酶(AMPK)来靶向脂质和葡萄糖代谢以及炎症。它的主要作用是减少肝脏中胆固醇的合成,它的使用通常与不良的肌肉疾病无关。苯二甲酸可以减少糖异生过程,从而改善胰岛素敏感性、葡萄糖代谢和代谢综合征的特征。苯戊酸的抗炎作用主要是通过激活免疫细胞中的AMPK通路,帮助降低血浆中c反应蛋白的水平来实现的。苯戊二酸对动脉粥样硬化性心血管疾病、2型糖尿病和慢性肝病病程的影响已经在随机临床试验中进行了评估,需要进一步研究。III期临床安全性试验表明,苯甲多酸与他汀类药物、依折替米贝或蛋白转化酶subti-lisin / keexin 9型抑制剂联合使用可达到低密度脂蛋白胆固醇的目标水平。本综述的目的是分析苯戊酸的主要作用机制,潜在的临床靶点,并描述现有的临床试验证据。搜索是在Scopus, Science Direct(来自Elsevier)和PubMed数据库中完成的,包括Medline。使用了以下关键词:甲苯二甲酸,低密度脂蛋白胆固醇,动脉粥样硬化性心血管疾病,糖尿病。为了确定在网上搜索中无法找到的研究结果,使用了出版物参考书目的手动搜索。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Bempedoic acid: mechanism of action and therapeutic use in atherosclerotic cardiovascular diseases and diabetes
Bempedoic acid is a new cholesterol-lowering drug that recently received approval from the US Food and Drug Administration and the European Medicines Agency. This drug targets lipid and glucose metabolism as well as inflammation by downregulating the ATP citrate lyase and upregulating of AMP-activated protein kinase (AMPK). The main effect is to reduce cholesterol synthesis in the liver, and its use is generally not associated with undesirable muscle disorders. Bempedoic acid can reduce the processes of gluconeogenesis, which leads to an improvement in insulin sensitivity, glucose metabolism and features of the metabolic syndrome. The anti-inflammatory effect of bempedoic acid is mainly achieved by activating the AMPK pathway in immune cells, which helps reduce the level of C-reactive protein in plasma. The effects of bempedoic acid on the course of atherosclerotic cardiovascular disease, type 2 diabetes and chronic liver disease have been evaluated in randomi­zed clinical trials that require further research. Phase III clinical safety trial show that bempedoic acid is generally well tolerated in combination with statins, ezetimibe, or proprotein convertase subti­lisin/kexin type 9 inhibitors in achieving target levels of low-density lipoprotein cholesterol. The aim of this review is to analyze the main mechanisms of action, potential clinical targets of bempedoic acid and describe the existing evidence from clinical trials. The search was done in the Scopus, Science Direct (from Elsevier), and PubMed databases, including the Medline. The following keywords were used: bempedoic acid, low-density lipoprotein cholesterol, atherosclerotic cardiovascular diseases, diabetes. In order to identify research results that could not be found during the online search, a manual search of the bibliography of publications was used.
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