Jiaxing Hospital of Traditional Chinese Medicine, Jiaxing 314000, China.
Zhejiang Chinese Medical University, Academy of Chinese Medicine & Institute of Comparative Medicine, Hangzhou 310053, China.
J Appl Biomed. 2023 Sep;21(3):137-149. doi: 10.32725/jab.2023.014. Epub 2023 Sep 18.
Myocardial hypertrophy may lead to heart failure and sudden death. As traditional Chinese medicine, Guanxinning tablets (GXN) have significant pharmacological effects in the prevention and treatment of cardiovascular diseases. However, the anti-cardiac hypertrophy efficacy of GXN and its mechanism of action are still unclear. Therefore, we established a heart failure rat model and isolated primary cardiomyocytes of neonatal rat to observe the protective effect of GXN on heart failure rat model and the intervention effect on myocardial cell hypertrophy, and to explore the possible mechanism of GXN preventing and treating myocardial hypertrophy. The results of in vivo experiments showed that GXN could significantly reduce the degree of cardiac hypertrophy, reduce the size of cardiomyocytes, inhibit the degree of myocardial remodeling and fibrosis, and improve cardiac function in rats with early heart failure. The results of in vitro experiments showed that GXN was safe for primary cardiomyocytes and could improve cardiomyocyte hypertrophy and reduce the apoptosis of cardiomyocytes in pathological state, which may be related to the inhibition of the over-activation of MEK-ERK1/2 signaling pathway. In conclusion, GXN may inhibit cardiac hypertrophy and improve early heart failure by inhibiting the over-activation of MEK-ERK1/2 signaling pathway.
心肌肥厚可导致心力衰竭和猝死。作为中药，冠心宁片（GXN）在心脑血管疾病的防治方面具有显著的药理作用。然而，GXN 的抗心肌肥厚作用及其作用机制尚不清楚。因此，我们建立了心力衰竭大鼠模型，并分离新生大鼠原代心肌细胞，观察 GXN 对心力衰竭大鼠模型的保护作用及对心肌细胞肥大的干预作用，并探讨 GXN 防治心肌肥厚的可能机制。体内实验结果表明，GXN 可显著减轻心肌肥厚程度，减小心肌细胞大小，抑制心肌重构和纤维化程度，改善心力衰竭大鼠心功能。体外实验结果表明，GXN 对原代心肌细胞安全，可改善病理状态下心肌细胞肥大和减少心肌细胞凋亡，这可能与抑制 MEK-ERK1/2 信号通路的过度激活有关。综上所述，GXN 可能通过抑制 MEK-ERK1/2 信号通路的过度激活来抑制心肌肥厚，改善早期心力衰竭。
