Reactivation of human acetylcholinesterase and butyrylcholinesterase inhibited by leptophos-oxon with different oxime reactivators in vitro |
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| Authors: | Jun Daniel Musilova Lucie Pohanka Miroslav Jung Young-Sik Bostik Pavel Kuca Kamil |
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| Affiliation: | 1 Faculty of Military Health Sciences, University of Defence, Hradec Kralove, Czech Republic;2 Faculty of Environmental Sciences, Czech University of Life Sciences Prague, Praha, Czech Republic;3 Faculty of Pharmacy in Hradec Kralove, Charles University in Prague, Hradec Kralove, Czech Republic;4 Medicinal Science Division, Korea Research Institute of Chemical Technology, Yuseong, Taejon, Korea |
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| 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. |
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| Keywords: | acetylcholinesterase butyrylcholinesterase nerve agent pesticide reactivator oxime scavenger leptophos-oxon |
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