Teixeira-Fonseca Jorge Lucas, Santos-Miranda Artur, Marques Ivan Lobo Sousa, Marques Leisiane Pereira, Alcantara Fabiana, de Lima Conceição Michael Ramon, Souza Diego Santos, Santana Gondim Antonio Nei, Roman-Campos Danilo
Laboratório de Cardiobiologia, Departamento de Biofísica, Universidade Federal de São Paulo (UNIFESP), São Paulo, São Paulo, Brazil.
Departamento de Fisiologia, Universidade Federal de Minas Gerais, Belo Horizonte, Brazil.
Basic Clin Pharmacol Toxicol. 2023 Nov;133(5):565-575. doi: 10.1111/bcpt.13941. Epub 2023 Sep 19.
Eugenol is an aromatic compound used in the manufacture of medicines, perfumes, cosmetics and as an anaesthetic due to the ability of the drug to block the neuronal isoform of voltage-gated Na channels (Na ). Some arrhythmias are associated with gain of function in the sodium current (I ) found in cardiomyocytes, and antiarrhythmic sodium channel blockers are commonly used in the clinical practice. This study sought to elucidate the potential mechanisms of eugenol's protection in the arrhythmic model of ouabain-induced arrhythmias in guinea pig heart. Ex vivo arrhythmias were induced using 50 μM of ouabain. The antiarrhythmic properties of eugenol were evaluated in the ex vivo heart preparation and isolated ventricular cardiomyocytes. The compound's effects on cardiac sodium current and action potential using the patch-clamp technique were evaluated. In all, eugenol decreased the ex vivo cardiac arrhythmias induced by ouabain. Furthermore, eugenol showed concentration dependent effect upon peak I , left-shifted the stationary inactivation curve and delayed the recovery from inactivation of the I . All these aspects are considered to be antiarrhythmic. Our findings demonstrate that eugenol has antiarrhythmic activity, which may be partially explained by the ability of eugenol to change de biophysical properties of I of cardiomyocytes.
丁香酚是一种芳香化合物，因其能够阻断电压门控钠通道（Na ）的神经元亚型，而被用于制造药品、香水、化妆品以及用作麻醉剂。一些心律失常与心肌细胞中钠电流（I ）的功能增强有关，抗心律失常的钠通道阻滞剂在临床实践中常用。本研究旨在阐明丁香酚在豚鼠心脏哇巴因诱导的心律失常模型中发挥保护作用的潜在机制。使用50μM哇巴因诱导离体心律失常。在离体心脏标本和分离的心室心肌细胞中评估丁香酚的抗心律失常特性。使用膜片钳技术评估该化合物对心脏钠电流和动作电位的影响。总体而言，丁香酚可减少哇巴因诱导的离体心脏心律失常。此外，丁香酚对I 的峰值呈浓度依赖性影响，使稳态失活曲线左移，并延迟I 失活后的恢复。所有这些方面都被认为具有抗心律失常作用。我们的研究结果表明，丁香酚具有抗心律失常活性，这可能部分归因于丁香酚改变心肌细胞I 生物物理特性的能力。
