| 手动膜片钳检测HMS-01对HEK293细胞hERG通道电流的影响 |
| 投稿时间：2021-10-25 修订日期：2022-01-12 点此下载全文 |
| 引用本文：张慧敏,向科发,史小飞,秦臻,刘霞.手动膜片钳检测HMS-01对HEK293细胞hERG通道电流的影响[J].药学实践杂志,2022,40(2):132~135,142 |
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| 基金项目:国家自然科学基金项目（82073842）; 上海市2021年度“科技创新行动计划”优秀学术/技术带头人计划项目(21XD1404700) |
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| 中文摘要:目的 检测新化合物HMS-01有无心脏毒性，对其进行临床前安全评价研究，为进入临床试验做准备。方法 用手动膜片钳检测转染后hERG钾通道稳定表达的HEK293细胞的电流，西沙必利做阳性药，将HMS-01依次稀释成0.3、1、3、10、30 μmol/L，依次作用于细胞，记录电流变化，计算抑制率。结果 HMS-01在实验设计的最高浓度30 μmol/L时，对细胞hERG钾通道的抑制率低于30%，与阳性对照药西沙必利相比，无明显抑制作用。结论 新化合物HMS-01对hERG通道无明显抑制作用，不具有心脏毒性。 |
| 中文关键词:手动膜片钳 HEK293细胞 hERG通道 |
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| The effect of HMS-01 on stably expressed hERG channel currents in HEK293 cells detected with the manualpatch clamp method |
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| Abstract:Objective To test the cardiac toxicity of new compound HMS-01 and evaluate the safety profile for clinical trials. Methods Manualpatch clamp method was used to measure human Ether-a-go-go-Related Gene (hERG) potassium channel currents with different concentrations of HMS-01. Cisapride was selected as the positive control drug. HMS-01 was diluted to the concentration of 0.3, 1, 3, 10 and 30 μmol/L and applied to the cells. The changes in electrical currents were recorded and the inhibition rate was calculated. Results At the highest concentration of 30μmol/L, the inhibitory rate of HMS-01 on hERG channel was less than 30%. There was no obvious inhibitory effect compared with cisapride. Conclusion Compared with the cisapride, HMS-01 has no obvious inhibitory effect on hERG channel and has no cardiotoxicity. |
| keywords:manualpatch clamp method HEK293 cells hERG channel |
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