Kamisah Yusof, Che Hassan Hamat H
Department of Pharmacology, Faculty of Medicine, Universiti Kebangsaan Malaysia, Kuala Lumpur 56000, Malaysia.
Department of Medicine, Faculty of Medicine, Universiti Kebangsaan Malaysia, Kuala Lumpur 56000, Malaysia.
Pharmaceuticals (Basel). 2024 Apr 5;17(4):464. doi: 10.3390/ph17040464.
Endothelial dysfunction is a hallmark of cardiovascular diseases, contributing to impaired vasodilation, altered hemodynamics, and atherosclerosis progression. Trimetazidine, traditionally used for angina pectoris, exhibits diverse therapeutic effects on endothelial dysfunction. This review aims to elucidate the mechanisms underlying trimetazidine's actions and its potential as a therapeutic agent for endothelial dysfunction and associated cardiovascular disorders. Trimetazidine enhances vasodilation and hemodynamic function by modulating endothelial nitric oxide synthase activity, nitric oxide production, and endothelin-1. It also ameliorates metabolic parameters, including reducing blood glucose, mitigating oxidative stress, and dampening inflammation. Additionally, trimetazidine exerts antiatherosclerotic effects by inhibiting plaque formation and promoting its stability. Moreover, it regulates apoptosis and angiogenesis, fostering endothelial cell survival and neovascularization. Understanding trimetazidine's multifaceted mechanisms underscores its potential as a therapeutic agent for endothelial dysfunction and associated cardiovascular disorders, warranting further investigation for clinical translation.
内皮功能障碍是心血管疾病的一个标志,会导致血管舒张受损、血流动力学改变和动脉粥样硬化进展。传统上用于治疗心绞痛的曲美他嗪,对内皮功能障碍具有多种治疗作用。本综述旨在阐明曲美他嗪作用的潜在机制及其作为内皮功能障碍及相关心血管疾病治疗药物的潜力。曲美他嗪通过调节内皮型一氧化氮合酶活性、一氧化氮生成和内皮素-1来增强血管舒张和血流动力学功能。它还能改善代谢参数,包括降低血糖、减轻氧化应激和抑制炎症。此外,曲美他嗪通过抑制斑块形成并促进其稳定性发挥抗动脉粥样硬化作用。此外,它还调节细胞凋亡和血管生成,促进内皮细胞存活和新生血管形成。了解曲美他嗪的多方面机制凸显了其作为内皮功能障碍及相关心血管疾病治疗药物的潜力,值得进一步研究以实现临床转化。