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Int. J. Mol. Sci. 2010, 11(8), 2856-2863; doi:10.3390/ijms11082856
Article

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

1,2,* , 3, 1, 4, 1 and 1,*
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
* Authors to whom correspondence should be addressed.
Received: 29 June 2010 / Revised: 25 July 2010 / Accepted: 29 July 2010 / Published: 3 August 2010
(This article belongs to the Section Bioinorganic Chemistry)
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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.
Keywords: acetylcholinesterase; butyrylcholinesterase; nerve agent; pesticide; reactivator; oxime; scavenger; leptophos-oxon acetylcholinesterase; butyrylcholinesterase; nerve agent; pesticide; reactivator; oxime; scavenger; leptophos-oxon
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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Jun, D.; Musilova, L.; Pohanka, M.; Jung, Y.-S.; Bostik, P.; Kuca, K. Reactivation of Human Acetylcholinesterase and Butyrylcholinesterase Inhibited by Leptophos-Oxon with Different Oxime Reactivators in Vitro. Int. J. Mol. Sci. 2010, 11, 2856-2863.

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