钩藤碱对human ether-a-go-go相关基因通道的抑制作用(英文)

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将human ether-a-go-go相关基因(HERG)cRNA注射到非洲爪蟾卵母细胞,采用双电极电压钳技术,观察钩藤碱对 表达电流的影响。结果显示:(1)钩藤碱抑制HERG通道的表达是浓度依赖性的,IC50为(773.4±42.5)μmol/L。(2)钩藤碱抑 制HERG通道的表达是电压依赖性的,最大抑制率在-20 mV,为15%。上述结果提示,钩藤碱抑制HERG编码的钾通道, 导致心室复极时间延长,揭示了与钩藤碱相关的心肌钾通道的分子生物学基础。 Human ether-a-go-go-related gene (HERG) cRNA was injected into Xenopus laevis oocytes and double-electrode voltage clamp technique was used to observe the effect of rhynchophylline on the expression current. The results showed that: (1) rhynchophylline inhibited HERG channel expression was concentration-dependent, IC50 was (773.4±42.5) μmol/L. (2) Rhynchophylline inhibited HERG channel expression in a voltage-dependent manner, with a maximum inhibition rate of -20 mV at 15%. The above results suggest that rhynchophylline inhibits the HERG-encoded potassium channel, resulting in prolonged ventricular repolarization, revealing the molecular biological basis of rhodamine-related cardiac potassium channels.
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