| 蜂毒肽对豚鼠心肌线粒体Na~ 、K~ -ATP酶的影响(英文) |
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| 引用本文： | 杨申,张雪梅,江明华.蜂毒肽对豚鼠心肌线粒体Na~ 、K~ -ATP酶的影响(英文)[J].中国药理学报(英文版),2001,22(3):279-282. |
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| 作者姓名： | 杨申 张雪梅 江明华 |
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| 作者单位： | 上海复旦大学药学院药理教研室，上海复旦大学药学院药理教研室，上海复旦大学药学院药理教研室 上海 中国 200032，上海 中国 200032，上海 中国 200032 |
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| 基金项目： | Project Supported by National Natural Science Foundation China, № 39770885. |
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| 摘 要： | 目的:研究蜂毒肽对豚鼠心肌线粒体Na~ ,K~ -ATP酶活性的影响。方法:应用光电比色法测定Na~ ,K~ -ATP酶活性。以Line-weaver-burk双倒数作图法分析酶动力学参数。结果:蜂毒肽抑制心肌Na~ ,K~ -ATP酶表现为浓度和时间依赖性,IC_(50)为2.60μmol/L。酶动力学研究表明,蜂毒肽对Na~ ,K~ -ATP酶有抑制作用,对K~ 表现为竞争性结合,对Na~ 及ATP表现为非竞争性结合。结论:蜂毒肽对心肌Na~ ,K~ -ATP酶有抑制作用,其抑制机制主要是与K~ 竞争结合酶外侧的K~ 结合位点。
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| 关 键 词： | 蜂毒肽 蜂毒液类 Na~ K~ -交换ATP酶 心肌 线粒体 |
Inhibitory effect of melittin on Na~ , K~ -ATPase from guinea pig myocardial mitochondria |
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| YANG Shen,ZHANG Xue-Mei,JIANG Ming-Hua.Inhibitory effect of melittin on Na~ , K~ -ATPase from guinea pig myocardial mitochondria[J].Acta Pharmacologica Sinica,2001,22(3):279-282. |
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| Authors: | YANG Shen ZHANG Xue-Mei JIANG Ming-Hua |
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| Institution: | Department of Pharmacology, School of Pharmacy, Fudan University, Shanghai 200032, China. mhjiang@shmu.edu.cn |
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| Abstract: | AIM: To investigate the effect of melittin (Mel) of Na+,K+-ATPase activity and it's kinetic mode of action on guinea pig myocardial mitochondria. METHODS: Effect of Mel on heart mitochondrial Na+,K+-ATPase activity was determined with colorimetry method. RESULTS: Mel inhibited Na+,K+-ATPase in a concentration and time dependent manner, IC50 was 2.60 micromol/L. Kinetic studies of interaction between Mel and K+, Na+, ATP revealed that inhibitory effect of Mel was competitive with K+, but not with Na+ and ATP. CONCLUSION: Mel polypeptide potently inhibits Na+,K+-ATPase, possibly by binding to the K+ site. |
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| Keywords: | melittin bee venoms Na~ K~ -exchanging ATPase myocardium mitochondna |
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