应用膜片钳技术研究豆腐果苷对hERG钾通道电生理功能的影响

Using patch clamp technique to investigate influence of helicid to electrophysiological function of hERG potassium channel

目的:探讨豆腐果苷对hERG钾离子电流的影响及潜在心脏毒性。方法:使用稳定转染hERG基因的CHO细胞,通过全细胞膜片钳技术检测不同浓度豆腐果苷对hERG通道电流活动的作用。结果:豆腐果苷对hERG钾通道的IC50约为47μmol/L,比临床常规剂量下人体内峰浓度高1 000倍以上。结论:临床常用剂量下,豆腐果苷发生与hERG通道抑制作用相关的心脏安全性问题的可能性非常小。

AIM：To investigate the impact of natural medicine helicid on hERG potassium currents and potential cardiac toxicity.METHODS：hERG gene was stably transfected in CHO cells.The whole-cell patch-clamp technique was applied to detect effects on hERG channel current of different concentrations helicid.RESULTS：IC50of helicid on hERG channels was 47μmol/L,which was more than 1000 times higher than the peak concentration in human body at clinical dose.CONCLUSION：It is less likely to encounter cardiac safety issues via the hERG channel inhibition of helicid in clinical application.