Pseudo-ginsengenin DQ ameliorated aconitine-induced arrhythmias by influencing Ca(2+) and K(+) currents in ventricular myocytes.

Pseudo-ginsengenin DQ ameliorated aconitine-induced arrhythmias by influencing Ca(2+) and K(+) currents in ventricular myocytes.
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DOI:
10.1039/d0ra01683g
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发表时间:
2020-07-03
期刊:
影响因子:
3.9
通讯作者:
--
中科院分区:
化学3区
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拟人参素DQ(PDQ)是原人参二醇氧化环化的产物。 PDQ具有多种生物活性,包括逆转癌症的多药耐药性、针对急性肾毒性的肾脏保护作用以及减轻异丙肾上腺素或冠状动脉结扎引起的心肌缺血损伤,但其对心律失常的作用迄今为止尚不清楚。由于人参对心血管系统的影响复杂,因此有必要研究PDQ是否会影响心律失常,而心律失常总是与其他心脏病同时发生。乌头碱用于诱发体内心律失常。为了了解其电生理学原理,采用全细胞膜片钳记录大鼠心室肌细胞中的L型钙电流(ICa,L)和钾电流(IK和IK1)。口服PDQ具有明显的抗心律失常作用,表现为室性心动过速和室性心动过速的发生率降低、发生次数减少、持续时间缩短,死亡率降低,生存时间延长。 PDQ 处理抑制 ICa、L 和 IK,而 IK1 不受影响。综上所述,PDQ可能通过抑制ICa、L和IK发挥抗心律失常作用。拟人参素DQ(PDQ)是原人参二醇氧化环化的产物。 PDQ 可以通过影响心室肌细胞中的 Ca2+ 和 K+ 电流来改善乌头碱诱导的心律失常。
Pseudo-ginsengenin DQ (PDQ) is the product of the oxidative cyclization of protopanaxadiol. PDQ exhibits various bioactivities, including reversal of multidrug resistance in cancer, renal protective effects against acute nephrotoxicity and attenuating myocardial ischemia injury induced by isoproterenol or ligation of coronary arterials, but its effect on arrhythmias has not been clear until now. Because of the complicated effects of ginseng on the cardiovascular system, it is necessary to investigate whether PDQ affects arrhythmias, which are always concomitant with other cardiac diseases. Aconitine was used to induce arrhythmia in vivo. To understand its electrophysiological fundamental, whole-cell patch-clamp was used to record the L-type calcium current (ICa,L) and potassium currents (IK and IK1) in the ventricular myocytes in rats. Oral administration of PDQ exerted obvious antiarrhythmic effects, as indicated by the decreased incidence rate, lower number of occurrences, and shorter duration time of ventricular tachycardia and ventricular tachycardia, decreased mortality rate and increased survival time. ICa,L and IK were inhibited by PDQ treatment while IK1 was not affected. To conclude, PDQ may have an anti-arrhythmia effect through inhibiting ICa,L and IK. Pseudo-ginsengenin DQ (PDQ) is the product of the oxidative cyclization of protopanaxadiol. PDQ could ameliorate aconitine-induced arrhythmias by influencing Ca2+ and K+ currents in ventricular myocytes.
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