丁卡因对人红细胞膜乙酰胆碱酯酶的抑制作用及其与膜脂的关系  

Relationship between Membrane Lipid and the Inhibition of Acetylcholinesterase on Human Erythrocyte by Tetracaine

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作  者:姚尚龙[1] 朱砂[2] 杜虹[2] 张诗海[1] 周慧[2] 曾邦雄[1] 刘敏谷[2] 

机构地区:[1]同济医科大学附属协和医院麻醉学教研室,武汉430022 [2]同济医科大学环境毒理学研究室,武汉430030

出  处:《华中科技大学学报(医学版)》1994年第S2期85-88,92,共5页Acta Medicinae Universitatis Scientiae et Technologiae Huazhong

摘  要:本文以人红细胞膜为材料,应用荧光探针(ANS)及酶学研究方法,研究了丁卡因对AchE及红细胞膜脂之间的关系。结果显示,丁卡因对红细胞膜AchE有明显抑制作用,其半数抑制浓度为525μmol/L。丁卡因还能増加膜-ANS复合物荧光强度,双倒数及Scatchard作图分析表明,其使膜ANS复合物荧光强度增强的原因并非ANS荧光量子产率的改变,而是膜上ANS结合数量增加所致,这一效应与其时膜流动性影响是一致的。Relationship between the inhibition of acetylcholinesterase (AchE) on human erythrocyte and membrane lipid by tetracaine with fluorescence(ANS)and enzymatic kinetics was studied .The results showed that tetracaine was a potent inhibitor of AchE and its IC_(50) is approximately 525 μmol/L.Tetracaine enhanced the fluorescence intensity of the ANS-membrane complex.A graphical analysis of this effect shows that it was due to an increase in the amount of ANS bound to the membrane ,not to an increase in the quantum yield of ANS.The Scatchard plots further confirmed that tetracaine increases the number of ANS binding sites and affinity of ANS to the membranes .This effect is consistent with its effect on the lipid fluidity of membrane.

关 键 词:丁卡因 红细胞膜 膜脂质 乙酰胆碱酯酶 

分 类 号:R971.2[医药卫生—药品]

 

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