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

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. Com...

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Autores principales: Jun, Daniel, Musilova, Lucie, Pohanka, Miroslav, Jung, Young-Sik, Bostik, Pavel, Kuca, Kamil
Formato: Texto
Lenguaje:English
Publicado: Molecular Diversity Preservation International (MDPI) 2010
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Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2996742/
https://www.ncbi.nlm.nih.gov/pubmed/21152278
http://dx.doi.org/10.3390/ijms11082856
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author Jun, Daniel
Musilova, Lucie
Pohanka, Miroslav
Jung, Young-Sik
Bostik, Pavel
Kuca, Kamil
author_facet Jun, Daniel
Musilova, Lucie
Pohanka, Miroslav
Jung, Young-Sik
Bostik, Pavel
Kuca, Kamil
author_sort Jun, Daniel
collection PubMed
description 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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spelling pubmed-29967422010-12-08 Reactivation of Human Acetylcholinesterase and Butyrylcholinesterase Inhibited by Leptophos-Oxon with Different Oxime Reactivators in Vitro Jun, Daniel Musilova, Lucie Pohanka, Miroslav Jung, Young-Sik Bostik, Pavel Kuca, Kamil Int J Mol Sci Article 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. Molecular Diversity Preservation International (MDPI) 2010-08-03 /pmc/articles/PMC2996742/ /pubmed/21152278 http://dx.doi.org/10.3390/ijms11082856 Text en © 2010 by the authors; licensee Molecular Diversity Preservation International, Basel, Switzerland. http://creativecommons.org/licenses/by/3.0 This article is an open-access article distributed under the terms and conditions of the Creative Commons Attribution license (http://creativecommons.org/licenses/by/3.0/).
spellingShingle Article
Jun, Daniel
Musilova, Lucie
Pohanka, Miroslav
Jung, Young-Sik
Bostik, Pavel
Kuca, Kamil
Reactivation of Human Acetylcholinesterase and Butyrylcholinesterase Inhibited by Leptophos-Oxon with Different Oxime Reactivators in Vitro
title Reactivation of Human Acetylcholinesterase and Butyrylcholinesterase Inhibited by Leptophos-Oxon with Different Oxime Reactivators in Vitro
title_full Reactivation of Human Acetylcholinesterase and Butyrylcholinesterase Inhibited by Leptophos-Oxon with Different Oxime Reactivators in Vitro
title_fullStr Reactivation of Human Acetylcholinesterase and Butyrylcholinesterase Inhibited by Leptophos-Oxon with Different Oxime Reactivators in Vitro
title_full_unstemmed Reactivation of Human Acetylcholinesterase and Butyrylcholinesterase Inhibited by Leptophos-Oxon with Different Oxime Reactivators in Vitro
title_short Reactivation of Human Acetylcholinesterase and Butyrylcholinesterase Inhibited by Leptophos-Oxon with Different Oxime Reactivators in Vitro
title_sort reactivation of human acetylcholinesterase and butyrylcholinesterase inhibited by leptophos-oxon with different oxime reactivators in vitro
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2996742/
https://www.ncbi.nlm.nih.gov/pubmed/21152278
http://dx.doi.org/10.3390/ijms11082856
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