Inhibitory effect of gallic acid on voltage-gated Na+ channels in rat cardiomyocytes |
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Authors: | Ya-ya Du Li Zou Xiu-xiu Wang Le-yao Dai Xin-nan Ling Zheng-xin Xu |
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Affiliation: | Department of Pharmacology, School of Medicine, Yangzhou University, Yangzhou, China |
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Abstract: | Gallic acid (GA) has a protective effect on the cardiovascular system. To study its cardiac electrophysiological effects, voltage-gated Na+ channel currents (INa) were recorded in rat cardiomyocytes using whole-cell patch clamp techniques. Moreover, the effects of GA on aconitine-induced arrhythmias were assessed using electrocardiograms in vivo. We found that the current–voltage characteristic curve (I-V curve) of INa significantly shifted in the presence of 1, 3, and 10 μmol/L of GA. The peak sodium current density (INa-Peak) was reduced from −84.02 ± 5.68 pA/pF to −65.78 ± 3.96 pA/pF with 1 μmol/L, −54.45 ± 5.18 pA/pF with 3 μmol/L, and −44.20 ± 4.35 pA/pF with 10 μmol/L, respectively. GA shifted the steady-state activation curve of INa and recovery curve to the right and the steady-state inactivation curve to the left. The observed inhibitory effect was comparable to that of amiodarone. GA pre-treatment significantly prolonged the onset of fatal ventricular fibrillation. Our results indicated that GA inhibited INa in rat ventricular myocytes and aconitine-induced arrhythmias in vivo. These results suggest the potential of GA for development as a novel anti-arrhythmic therapeutic. |
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Keywords: | amiodarone arrhythmia cardiomyocytes gallic acid voltage-gated Na+ channels |
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