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在体外使用不同肟类重活化剂对被水胺硫磷氧抑制的人乙酰胆碱酯酶和丁酰胆碱酯酶进行重活化

Reactivation of human acetylcholinesterase and butyrylcholinesterase inhibited by leptophos-oxon with different oxime reactivators in vitro.

作者信息

Jun Daniel, Musilova Lucie, Pohanka Miroslav, Jung Young-Sik, Bostik Pavel, Kuca Kamil

机构信息

Faculty of Military Health Sciences, University of Defence, Hradec Kralove, Czech Republic.

出版信息

Int J Mol Sci. 2010 Aug 3;11(8):2856-63. doi: 10.3390/ijms11082856.

Abstract

We have evaluated in vitro the potency of 23 oximes to reactivate human erythrocyte acetylcholinesterase (AChE) and plasma butyrylcholinesterase (BChE) inhibited by racemic leptophos-oxon (O-[4-bromo-2,5-dichlorophenyl]-O-methyl phenyl-phosphonate), a toxic metabolite of the pesticide leptophos. Compounds were assayed in concentrations of 10 and 100 μM. In case of leptophos-oxon inhibited AChE, the best reactivation potency was achieved with methoxime, trimedoxime, obidoxime and oxime K027. The most potent reactivators of inhibited BChE were K033, obidoxime, K117, bis-3-PA, K075, K074 and K127. The reactivation efficacy of tested oximes was lower in case of leptophos-oxon inhibited BChE.

摘要

我们已经在体外评估了23种肟类化合物对被消旋溴苯磷-氧磷(O-[4-溴-2,5-二氯苯基]-O-甲基苯基膦酸酯)抑制的人红细胞乙酰胆碱酯酶(AChE)和血浆丁酰胆碱酯酶(BChE)的重新激活能力,溴苯磷-氧磷是杀虫剂溴苯磷的一种有毒代谢产物。化合物的检测浓度为10μM和100μM。对于被溴苯磷-氧磷抑制的AChE,甲氧肟、三甲肟、双复磷和肟K027的重新激活能力最佳。抑制的BChE的最有效重新激活剂是K033、双复磷、K117、双-3-PA、K075、K074和K127。在溴苯磷-氧磷抑制BChE的情况下,所测试肟类化合物的重新激活效果较低。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/3e58/2996742/627818deff49/ijms-11-02856f1a.jpg

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