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探讨一种新型氟喹诺酮类抗菌剂盐酸昌欣沙星(chinfloxacin hydrochloride,CFX)对HERG(human ether-à-go-go-related gene)钾离子通道动力学的影响。利用全细胞膜片钳技术,在HEK293细胞中记录异源表达的HERG钾电流,观察CFX对通道的抑制作用,分析其对通道激活、失活和去激活等动力学过程的影响。结果表明,CFX作用于HERG钾离子通道的开放状态,以浓度依赖的方式抑制HERG钾电流,半有效抑制浓度(IC50)为(162.1±14.2)μmol.L?1,是其改造前体盐酸莫西沙星的2倍,但CFX不改变通道动力学特性。由于改变细胞外液K+浓度,CFX对HERG钾电流抑制作用增强。
To investigate the effect of a novel fluoroquinolone antibacterial agent chinfloxacin hydrochloride (CFX) on K (superscript 2+) channel kinetics of HERG (human ether-a-go-go-related gene) The whole cell patch clamp technique was used to record the heterologously expressed HERG potassium currents in HEK293 cells. The inhibitory effect of CFX on the channels was observed and its effects on the activation, inactivation and deactivation of channels were analyzed. The results showed that CFX inhibited the HERG potassium current in a dose-dependent manner in the open state of HERG potassium channel, and the IC50 value was (162.1 ± 14.2) μmol·L -1. Cisaprine 2 times, but CFX does not change the channel dynamics. Due to the change of K + concentration in extracellular fluid, CFX can inhibit HERG potassium current.