Department of Pharmacy, The First Affiliated Hospital of Harbin Medical University, Harbin, Heilongjiang 150001, P.R. China.
Department of Pharmacology, The State‑Province Key Laboratories of Biomedicine‑Pharmaceutics of China, Key Laboratory of Cardiovascular Research, Ministry of Education, Harbin Medical University, Harbin, Heilongjiang 150081, P.R. China.
Mol Med Rep. 2019 May;19(5):3527-3536. doi: 10.3892/mmr.2019.10034. Epub 2019 Mar 14.
Myocardial infarction (MI) is the most common event in cardiovascular disease. Carvedilol, a β‑blocker with multiple pleiotropic actions, is widely used for the treatment cardiovascular diseases. However, the underlying mechanisms of carvedilol on alleviating MI are not fully understood. The aim of the present study was to investigate whether the beneficial effects of carvedilol were associated with regulation of microRNA‑1 (miR‑1). It was demonstrated that carvedilol ameliorated impaired cardiac function and decreased infarct size in a rat model of MI induced by coronary artery occlusion. Similarly, carvedilol reversed the H2O2‑induced decrease in cardiomyocyte viability in a dose‑dependent manner. The in vivo and in vitro models demonstrated the downregulation of miR‑1 following treatment with carvedilol. Overexpression of miR‑1, a known pro‑apoptotic miRNA, decreased cell viability and induced cell apoptosis. Transfection of miR‑1 abolished the beneficial effects of carvedilol. The expression of heat shock protein 60 (HSP60), a direct target of miR‑1, was identified to be decreased in MI and H2O2‑induced apoptosis, which was associated with a decrease in Bcl‑2 and an increase in Bax; expression was restored following treatment with carvedilol. It was concluded that carvedilol partially exhibited its beneficial effects by downregulating miR‑1 and increasing HSP60 expression. miR‑1 has become a member of the group of carvedilol‑responsive miRNAs. Future studies are required to fully elucidate the potential overlapping or compensatory effects of known carvedilol‑responsive miRNAs and their underlying mechanisms of action in the pathophysiology of cardiovascular diseases.
心肌梗死(MI)是心血管疾病中最常见的事件。卡维地洛是一种具有多种多效作用的β受体阻滞剂,广泛用于治疗心血管疾病。然而,卡维地洛缓解 MI 的潜在机制尚不完全清楚。本研究旨在探讨卡维地洛的有益作用是否与 microRNA-1(miR-1)的调节有关。研究表明,卡维地洛可改善冠状动脉闭塞诱导的 MI 大鼠模型的心脏功能障碍和梗死面积减小。同样,卡维地洛以剂量依赖性方式逆转 H2O2 诱导的心肌细胞活力下降。体内和体外模型均表明卡维地洛治疗后 miR-1 下调。miR-1 是一种已知的促凋亡 miRNA,其过表达降低了细胞活力并诱导细胞凋亡。miR-1 的转染消除了卡维地洛的有益作用。miR-1 的直接靶标热休克蛋白 60(HSP60)的表达在 MI 和 H2O2 诱导的细胞凋亡中降低,这与 Bcl-2 减少和 Bax 增加有关;卡维地洛治疗后表达得到恢复。研究结论为,卡维地洛通过下调 miR-1 和增加 HSP60 表达部分发挥其有益作用。miR-1 已成为卡维地洛反应性 miRNA 组的一员。未来的研究需要充分阐明已知卡维地洛反应性 miRNA 的潜在重叠或补偿作用及其在心血管疾病病理生理学中的作用机制。