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Puerarin: a novel antagonist to inward rectifier potassium channel (I K1)

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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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Acknowledgments

We thank Prof. Jia JiDong for helpful discussions and guidance in electrophysiological techniques.

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Correspondence to Hua Zhang or TingZhong Wang.

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Hua Zhang, Li Zhang and Qing Zhang have contributed equally to this study.

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Zhang, H., Zhang, L., Zhang, Q. et al. Puerarin: a novel antagonist to inward rectifier potassium channel (I K1). Mol Cell Biochem 352, 117–123 (2011). https://doi.org/10.1007/s11010-011-0746-0

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  • DOI: https://doi.org/10.1007/s11010-011-0746-0

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