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.