| 钩藤碱对human ether-a-go-go相关基因通道的抑制作用 |
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| 作者姓名： | Gui L Li ZW Du R Yuan GH Li W Ren FX Li J Yang JG |
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| 作者单位： | 桂乐（南通大学附属医院心内科,南通,226000）
李之望（华中科技大学同济医学院神经生物学教研室,武汉,430030）
杜戎（华中科技大学同济医学院协和医院心血管病研究所,武汉,430030）
袁国会（华中科技大学同济医学院协和医院心血管病研究所,武汉,430030）
李伟（华中科技大学同济医学院协和医院心血管病研究所,武汉,430030）
任法鑫（华中科技大学同济医学院协和医院心血管病研究所,武汉,430030）
李婧（华中科技大学同济医学院协和医院心血管病研究所,武汉,430030）
杨钧国（华中科技大学同济医学院协和医院心血管病研究所,武汉,430030） |
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| 摘 要： | 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.
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| 关 键 词： | human ether-a-go-go相关基因 钩藤碱 卵母细胞 双电极电压钳 |
| 收稿时间： | 2004-09-06 |
| 修稿时间： | 2005-07-27 |
Inhibitory effect of rhynchophylline on human ether-a-go-go related gene channel |
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| Gui L,Li ZW,Du R,Yuan GH,Li W,Ren FX,Li J,Yang JG.Inhibitory effect of rhynchophylline on human ether-a-go-go related gene channel[J].Acta Physiologica Sinica,2005,57(5):648-652. |
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| Authors: | Gui Le Li Zhi-Wang Du Rong Yuan Guo-Hui Li Wei Ren Fa-Xin Li Jing Yang Jun-Guo |
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| Institution: | GUI Le,LI Zhi-Wang,DU Rong,YUAN Guo-Hui,LI Wei,REN Fa-Xin,LI Jing,YANG Jun-Guo Department of Cardiology,Affiliated Hospital,Nantong University,Nantong 226000,China Department of Neurobiology,Huazhong University of Science and Technology,Wuhan 430030,China Institute of Cardiovascular Medicine,Union Hospital,Tongji Medical College,Huazhong University of Science and Technology,Wuhan 430030,China |
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| Abstract: | We studied the effects of Chinese traditional medicine rhynchophylline (Rhy) on human ether-a-go-go related gene (HERG)channel and characterized the electrophysiological properties of Rhy's pharmacological effect on HERG channel using Xenopus oocytes. Xenopus oocytes were injected with either 23 nl (5.75 ng) HERG cRNA or 23 nl distilled water. Xenopus oocytes were randomly assigned to receive one of the following different concentrations of Rhy: (1) control, (2)10 μmol/L Rhy, (3)100 μmol/L Rhy,(4) 500 μmol/L Rhy, (5) 1 000 μmol/L Rhy, (6) 10 000 μmol/L Rhy. Cell currents were recorded in oocytes. The peak tail currents of HERG channel were inhibited by Rhy. The inhibition was in a dose-dependent manner IC50=(773.4 ± 42.5) μmol/L]. Experiment with 100 μmol/L Rhy indicated that the degree of HERG blockade showed some voltage dependence (within -40 mV to -20 mV ). Kinetic analyses revealed that Rhy decreased the rate of channel activation. The findings indicate that Rhy inhibits HERG encoded potassium channels. It may underline the molecular mechanism of myocardial electrophysiological characteristics associated with this drug. |
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| Keywords: | HERG rhynchophylline oocyte two-microelectrode voltage clamp |
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