Barbaloin inhibits ventricular arrhythmias in rabbits by modulating voltage-gated ion channels

Zhen-zhen CAO1, You-jia TIAN1, Jie HAO1, Pei-hua ZHANG1, Zhi-pei LIU1, Wan-zhen JIANG1, Meng-liu ZENG1, Pei-pei ZHANG1, Jihua MA1
1 The Cardio-Electrophysiological Research Laboratory, Medical College, Wuhan University of Science and Technology, Wuhan 430065, China
Correspondence to: Jihua MA:,
DOI: 10.1038/aps.2017.93
Received: 28 February 2017
Accepted: 17 June 2017
Advance online: 26 October 2017


Barbaloin (10-β-D-glucopyranosyl-1,8-dihydroxy-3-(hydroxymethyl)-9(10H)-anthracenone) is extracted from the aloe plant and has been reported to have anti-inflammatory, antitumor, antibacterial, and other biological activities. Here, we investigated the effects of barbaloin on cardiac electrophysiology, which has not been reported thus far. Cardiac action potentials (APs) and ionic currents were recorded in isolated rabbit ventricular myocytes using whole-cell patch-clamp technique. Additionally, the antiarrhythmic effect of barbaloin was examined in Langendorff-perfused rabbit hearts. In current-clamp recording, application of barbaloin (100 and 200 μmol/L) dose-dependently reduced the action potential duration (APD) and the maximum depolarization velocity (Vmax), and attenuated APD reverse-rate dependence (RRD) in ventricular myocytes. Furthermore, barbaloin (100 and 200 μmol/L) effectively eliminated ATX II-induced early afterdepolarizations (EADs) and Ca2+-induced delayed afterdepolarizations (DADs) in ventricular myocytes. In voltageclamp recording, barbaloin (10–200 μmol/L) dose-dependently inhibited L-type calcium current (ICa.L) and peak sodium current (INa.P) with IC50 values of 137.06 and 559.80 μmol/L, respectively. Application of barbaloin (100, 200 μmol/L) decreased ATX II-enhanced late sodium current (INa.L) by 36.6%±3.3% and 71.8%±6.5%, respectively. However, barbaloin up to 800 μmol/L did not affect the inward rectifier potassium current (IK1) or the rapidly activated delayed rectifier potassium current (IKr) in ventricular myocytes. In Langendorff-perfused rabbit hearts, barbaloin (200 μmol/L) significantly inhibited aconitine-induced ventricular arrhythmias. These results demonstrate that barbaloin has potential as an antiarrhythmic drug.
Keywords: arrhythmias; aloe; barbaloin; ventricular myocytes; late sodium current; peak sodium current; L-type calcium current; afterdepolarization; ATX II; aconitine

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