Reactivation of Human Acetylcholinesterase and Butyrylcholinesterase Inhibited by Leptophos-Oxon with Different Oxime Reactivators in Vitro

International Journal of Molecular Sciences

Daniel Jun¹  Lucie Musilova²  Miroslav Pohanka¹  Young-Sik Jung³  Pavel Bostik¹ 

[1] Faculty of Military Health Sciences, University of Defence, Hradec Kralove, Czech Republic;Faculty of Pharmacy in Hradec Kralove, Charles University in Prague, Hradec Kralove, Czech Republic;Medicinal Science Division, Korea Research Institute of Chemical Technology, Yuseong, Taejon, Korea

关键词: acetylcholinesterase;    butyrylcholinesterase;    nerve agent;    pesticide;    reactivator;    oxime;    scavenger;    leptophos-oxon;   

DOI  :  10.3390/ijms11082856

来源: mdpi

【 摘 要 】

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.

【 授权许可】

CC BY   
© 2010 by the authors; licensee Molecular Diversity Preservation International, Basel, Switzerland.