Tianjin Key Laboratory of Ionic-Molecular Function of Cardiovascular disease, Department of Cardiology, Tianjin Institute of Cardiology, the Second Hospital of Tianjin Medical University, Tianjin, China.
Clin Exp Pharmacol Physiol. 2022 Aug;49(8):848-857. doi: 10.1111/1440-1681.13672. Epub 2022 Jun 14.
LCZ696, an angiotensin receptor-neprilysin inhibitor, has shown promising clinical efficacy in patients with heart failure (HF) with reduced ejection fraction. However, its potential effects on heart failure with preserved ejection fraction (HFpEF) are still not fully understood. We evaluated the effect of LCZ696 on HFpEF in transverse aortic constriction mice and compared it with the effect of the angiotensin receptor blocker, valsartan. We found that LCZ696 improved cardiac diastolic function by reducing ventricular hypertrophy and fibrosis in mice with overload-induced diastolic dysfunction. In addition, there was superior inhibition of LCZ696 than stand-alone valsartan. As a potential underlying mechanism, we demonstrated that LCZ696 behaves as a potent suppressor of calcium-mediated calcineurin-nuclear factor of activated T cells (NFAT) signalling transduction pathways. Hence, we demonstrated the protective effects of LCZ696 in overload-induced HFpEF and provided a pharmaceutical therapeutic strategy for related diseases.
LCZ696,一种血管紧张素受体-脑啡肽酶抑制剂,在射血分数降低的心力衰竭(HF)患者中显示出有前景的临床疗效。然而,其对射血分数保留的心力衰竭(HFpEF)的潜在影响仍不完全清楚。我们评估了 LCZ696 在主动脉缩窄小鼠中对 HFpEF 的影响,并将其与血管紧张素受体阻滞剂缬沙坦的效果进行了比较。我们发现 LCZ696 通过减少心室肥厚和纤维化改善了心脏舒张功能,在超负荷诱导的舒张功能障碍的小鼠中。此外,LCZ696 的抑制作用优于单独的缬沙坦。作为一个潜在的潜在机制,我们证明 LCZ696 是一种有效的钙介导的钙调神经磷酸酶-活化 T 细胞核因子(NFAT)信号转导通路的抑制剂。因此,我们证明了 LCZ696 在超负荷诱导的 HFpEF 中的保护作用,并为相关疾病提供了一种药物治疗策略。