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探究二甲双胍的多效性活性。对止血作用的一瞥。

An investigation into the pleiotropic activity of metformin. A glimpse of haemostasis.

机构信息

Laboratory of Bioanalysis, Department of Pharmaceutical Chemistry, Drug Analysis and Radiopharmacy, Medical University of Lodz, ul. Muszyńskiego 1, 90-151, Lodz, Poland.

Students Research Group, Laboratory of Bioanalysis, Department of Pharmaceutical Chemistry, Drug Analysis and Radiopharmacy, Medical University of Lodz, ul. Muszyńskiego 1, 90-151, Lodz, Poland.

出版信息

Eur J Pharmacol. 2020 Apr 5;872:172984. doi: 10.1016/j.ejphar.2020.172984. Epub 2020 Feb 1.

Abstract

The most characteristic features of type 2 diabetes mellitus (T2DM) are hyperglycaemia and insulin resistance, however, patients with T2DM are at higher risk of cardiovascular disease (CVD) and atherosclerosis. Diabetes, frequently related to metabolic and vascular impairments, is also associated with thrombosis, increased blood coagulation and an imbalance between coagulation and fibrinolysis. Metformin is the most often used oral glucose-lowering agent; its beneficial properties include lowering insulin resistance, weight reduction and cardioprotection. Available data suggest that the advantageous properties of metformin stem from its favourable effects on endothelium, and anti-oxidative and anti-inflammatory properties. This paper reviews the favourable impact of metformin on endothelial function, with particular emphasis on the release of endogenous molecules modulating the state of the vascular endothelium and coagulation. It also summarizes the present knowledge on the influence of metformin on platelet activity and plasma haemostasis, including clot formation, stabilization and fibrinolysis. Its findings confirm that metformin should constitute first line therapy of T2DM subjects; however, more comprehensive methodical studies are required to discover the full potential of this drug.

摘要

2 型糖尿病(T2DM)的最典型特征是高血糖和胰岛素抵抗,但 T2DM 患者发生心血管疾病(CVD)和动脉粥样硬化的风险更高。糖尿病常与代谢和血管损伤有关,也与血栓形成、凝血增加以及凝血和纤维蛋白溶解失衡有关。二甲双胍是最常用的口服降血糖药物;其有益特性包括降低胰岛素抵抗、减轻体重和心脏保护。现有数据表明,二甲双胍的有益特性源于其对内皮的有利作用,以及抗氧化和抗炎特性。本文综述了二甲双胍对内皮功能的有利影响,特别强调了释放调节血管内皮和凝血状态的内源性分子。还总结了目前关于二甲双胍对血小板活性和血浆止血的影响的知识,包括血栓形成、稳定和纤维蛋白溶解。其研究结果证实,二甲双胍应成为 T2DM 患者的一线治疗药物;然而,需要更全面的方法学研究来发现这种药物的全部潜力。

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