Jun Daniel, Musilova Lucie, Pohanka Miroslav, Jung Young-Sik, Bostik Pavel, Kuca Kamil
Faculty of Military Health Sciences, University of Defence, Hradec Kralove, Czech Republic.
Int J Mol Sci. 2010 Aug 3;11(8):2856-63. doi: 10.3390/ijms11082856.
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.
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。
