梭曼、沙林对鸭血清丁酰胆碱酯酶的动力学研究  

Kinetic study of the inhibition of duck serum butyrylcholinesterase by soman and sarin

作　　者：吴方晖[1] 高川[1] 张靖[1] 宋云扬[1] 王惠芳[1] 李艳军[1] 董兆君[2] 

机构地区：[1]北京药物化学研究所,北京102205 [2]第三军医大学预防医学系军事毒理学研究室,重庆400038

出　　处：《第三军医大学学报》2004年第12期1058-1060,共3页Journal of Third Military Medical University

摘　　要：目的　从酶反应动力学方面揭示梭曼、沙林对丁酰胆碱酯酶的毒性强弱 ,比较两者对丁酰胆碱酯酶的抑制强度。方法　通过改进的Ellman法验测定了鸭血清丁酰胆碱酯酶的km 值 ,以及梭曼、沙林对该酶抑制反应的解离常数kd、膦酰化常数k2 和抑制速率常数ki值。结果　虽然梭曼和沙林在可逆的酶 抑制剂反应过程中反应速度相差不大 ,但梭曼对该酶的亲和力与抑制能力均比沙林强。Objective To investigate the toxicity of soman and sarin to butyrylcholinesterase and to compare the intensity of their inhibitory effect on butyrylcholinesterase. Methods k m value of the duck serum butyrylcholinesterase was detected by modified Ellman method. The dissociation (k d), phosphonylation (k 2), and biomolecular reaction (k i) constants were determined for the inhibitory kinetics of soman and sarin. Results Under the experiment conditions, the k m value of cholinesterase was 1.44×10 -5 mol/L. The k d values of soman and sarin to cholinesterase were 0.88×10 -8 mol/L and 1.87×10 -8 mol/L. The k 2 values were 9.89/min and 11.70/min. Conclusion Although there is little difference between the reactive velocities of soman and sarin when the reversible enzyme inhibitor complex is transformed to covalence phosphonylated enzyme, the affinity and inhibitory capacity of soman are higher than those of sarin. This may be the reason why the toxicity of soman is higher than that of sarin.

关 键 词：梭曼 沙林 丁酰胆碱酯酶 

分 类 号：R556.1[医药卫生—血液循环系统疾病] R996[医药卫生—内科学]