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目的 了解对硫磷与对氧磷在试管内对人脑乙酰胆碱酯酶 (AChE)的抑制 ,膦酰化酶的老化速率及肟类药物的重活化效能有何差别。方法 微量羟胺比色法测定AChE活性。结果 对硫磷与对氧磷抑制人脑AChE 5 0 %活性的摩尔浓度的负对数值(pI50 )分别为 4 .10及 7.5 1,抑制人脑AChE 90 %活性的摩尔浓度的负对数值 (pI90 )值分别为 2 .5 5及6 .5 7。氯磷定、双复磷、双磷定和酰胺磷定 4种重活化剂对对硫磷与对氧磷抑制的人脑AChE的重活化作用有较大差异 ,等摩尔浓度条件下 ,其对对氧磷的重活化作用普遍好于对硫磷。且双肟类重活化剂作用普遍强于单肟类重活化剂 ;对硫磷与对氧磷的最佳重活化剂均为双复磷。对硫磷与对氧磷人脑AChE磷酰化酶的半老化时间 (t0 .5)分别为 14及 12h ,老化达到 99%的时间 (t0 .99)分别为 95及 81h。结论 对硫磷或对氧磷中毒时应尽早使用双复磷或双磷定。且在急性中毒症状控制后 ,仍须连续使用重活化剂 4d。
Objective To understand the inhibitory effect of parathion and paraoxon on human brain acetylcholinesterase (AChE), the aging rate of phosphonylase and the reactivation of oximes in vitro. Methods Micro hydroxylamine colorimetry was used to measure the activity of AChE. Results The negative logarithm (pI50) of the molar concentrations of parathion and paraoxon that inhibited human AChE 50% activity were 4.10 and 7.51, respectively. The negative logarithm of the molar concentration of AChE 90% inhibition of human brain ( pI90) values of 2.55 and 6.57, respectively. Four kinds of heavy activators such as chlorophosphatidylcholine, diphosphorus, diphosphatidylcholine and amidopidil have significant differences on AChE reactivation in human brain inhibited by parathion and paraoxon. Under equimolar conditions, The reactivation of paraoxon is generally better than parathion. And the bi-oxime reactivator was generally stronger than the mono-oxime reactivator. The best reactivators of parathion and paraoxon were bisphosphorus. The half-aging time (t0.5) for parathion and paraoxon-phosphorylated human brain AChE phosphorylase was 14 and 12 h, respectively, and the aging time (t0.99) was 95 and 81 h, respectively. Conclusion Parathion or paraoxon poisoning should be used as soon as possible bis-or dual-phosphorus fixed. And in the control of symptoms of acute poisoning, still need to continue to use heavy activator 4d.