沙林对猴全血乙酰胆碱酯酶抑制的老化及重活化

摘要

Objective To study the inhibition of acetylcholinesterase (AChE) by sarin,aging rates of phosphorus acy-lase and reactivation of phosphorus acylase by oxime drugs in monkey blood . Methods The activity of AChE was detected by DTNB method. Results The IC50 and IC90 value of inhibition of AChE by sarin in monkey blood was 6. 3 X 10 -8 mol/L and 1.5 ×l0-7 mol/L, respectively. At the concentration of 0. 1 mmol/L, 0. 33 mmol/L and 1 mmol/L,the reactivation rate of pralidoxime ( pyraloxime ) chloride on sarin inhibited AChE in monkey blood was 16%, 45% and 83%, respectively, the reactivation rate of obidoxime chloride on inhibited AChE was 18%, 39% and 70%, and the respectively , and the reactivation rate of pralidoxime ( pyraloxime ) iodide on inhibition of AChE was 14%, 41% and 72%, respectively. The half aging time of phosphorus acylase of sarin-inhibited AChE in monkey blood was about 12 hours using 1 mmol/L pralidoxime chloride as the reactivator. Conclusion Such oximes as pralidoxime chloride should be used soon after sarin poisoning . The reactivation effect of obidoxime chloride is better than that of pralidoxime chloride and pralidoxime iodide at low con -centrations,but pralidoxime chloride shows the best effectiveness with the increasing concentration . Acute poisoning symptoms can be controlled by pralidoxime chloride , which should be repeated within 12 hours.%目的 研究沙林对猴全血乙酰胆碱酯酶(AChE)的抑制,磷酰化酶的老化速率及肟类药物的重活化作用.方法 5,5-连硫代-双-2-硝基苯甲酸(DTNB)法测定AChE活性.结果 沙林抑制猴全血AChE的IC50值为6.3×10-8mol/L,IC90值为1.5×10-7mol/L.在0.1、0.33和1 mmol/L的浓度下,氯解磷定对沙林抑制猴全血AChE的重化活率分别为16%、45%和83%;双复磷对沙林抑制猴全血AChE的重化活率分别为18%、39%和70%;碘解磷定对沙林抑制猴全血AChE的重化活率分别为14%、41%和72%.采用1 mmol/L的氯解磷定为重活化剂时,沙林抑制猴全血AChE磷酰化酶的半老化时间约为12 h.结论 沙林中毒后应尽早使用氯解磷定等肟类重活化剂.在低浓度0.1 mmol/L时,双复磷重活化效果最好;随着不同重活化剂浓度的增加,氯解磷定显示出较好的重活化效果.氯解磷定为重活化剂时,急性中毒症状控制后,建议应在12 h内重复使用.