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Updated: Jun 4, 2026

High-throughput Screening for Small-molecule Modulators of Inward Rectifier Potassium Channels
Published on: January 27, 2013
Puerarin: a novel antagonist to inward rectifier potassium channel (IK1)
Hua Zhang1, Li Zhang, Qing Zhang
1Department of Cardiology, Shaanxi Provincial Corps Hospital of Chinese People's Armed Police Forces, Xi'an, People's Republic of China. zl1017@126.com
Abstract:
Puerarin, isolated from the root of pueraria, had been widely used to prevent and treat arrhythmia. We show that puerarin effectively prevents and reverses aconitine-induced arrhythmias in perfused heart in vitro and in rats in vivo. To study the mechanisms of antiarrhythmic action of puerarin, we investigated the electrophysiological actions of puerarin using whole-cell clamp in isolated rodent ventricular myocytes and two electrode voltage-clamp (TEV) in I(K1)-expressing Xenopus oocytes. Puerarin had no prominent effect on action potentials of ventricular myocytes from guinea pig. However, puerarin (1.2 mM) significantly inhibited the I(K1) current in rat ventricular cells. Consistently, puerarin blocked I(K1) expressed in Xenopus oocytes in a dose-dependent manner. Puerarin competed with barium, an open-channel blocker of I(K1), to inhibit I(K1) currents. Thus, our data demonstrated that puerarin is a novel open-channel blocker of I(K1), which may underlie the antiarrhythmic action of puerarin.
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