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In vitro ability of currently available oximes to reactivate organophosphate pesticide-inhibited human acetylcholinesterase and butyrylcholinesterase.

Jun D, Musilova L, Musilek K, Kuca K - Int J Mol Sci (2011)

Bottom Line: Methamidophos and leptophos-oxon were quite easily reactivatable by all tested reactivators.Therefore, we evaluated the reactivation ability of obidoxime in a concentration range of 10(-3)-10(-7) M.In the case of BChE, no reactivator exceeded 15% reactivation ability and therefore none of the oximes can be recommended as a candidate for "pseudocatalytic" bioscavengers with BChE.

View Article: PubMed Central - PubMed

Affiliation: Center of Advanced Studies, Faculty of Military Health Sciences, University of Defence, Trebesska 1575, Hradec Kralove, 500 01, Czech Republic.

ABSTRACT
We have in vitro tested the ability of common, commercially available, cholinesterase reactivators (pralidoxime, obidoxime, methoxime, trimedoxime and HI-6) to reactivate human acetylcholinesterase (AChE), inhibited by five structurally different organophosphate pesticides and inhibitors (paraoxon, dichlorvos, DFP, leptophos-oxon and methamidophos). We also tested reactivation of human butyrylcholinesterase (BChE) with the aim of finding a potent oxime, suitable to serve as a "pseudocatalytic" bioscavenger in combination with this enzyme. Such a combination could allow an increase of prophylactic and therapeutic efficacy of the administered enzyme. According to our results, the best broad-spectrum AChE reactivators were trimedoxime and obidoxime in the case of paraoxon, leptophos-oxon, and methamidophos-inhibited AChE. Methamidophos and leptophos-oxon were quite easily reactivatable by all tested reactivators. In the case of methamidophos-inhibited AChE, the lower oxime concentration (10(-5) M) had higher reactivation ability than the 10(-4) M concentration. Therefore, we evaluated the reactivation ability of obidoxime in a concentration range of 10(-3)-10(-7) M. The reactivation of methamidophos-inhibited AChE with different obidoxime concentrations resulted in a bell shaped curve with maximum reactivation at 10(-5) M. In the case of BChE, no reactivator exceeded 15% reactivation ability and therefore none of the oximes can be recommended as a candidate for "pseudocatalytic" bioscavengers with BChE.

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Relationship between obidoxime concentration and corresponding reactivation ability of DFP-inhibited AChE.
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f5-ijms-12-02077: Relationship between obidoxime concentration and corresponding reactivation ability of DFP-inhibited AChE.


In vitro ability of currently available oximes to reactivate organophosphate pesticide-inhibited human acetylcholinesterase and butyrylcholinesterase.

Jun D, Musilova L, Musilek K, Kuca K - Int J Mol Sci (2011)

Relationship between obidoxime concentration and corresponding reactivation ability of DFP-inhibited AChE.
© Copyright Policy - open-access
Related In: Results  -  Collection

License 1 - License 2
Show All Figures
getmorefigures.php?uid=PMC3111652&req=5

f5-ijms-12-02077: Relationship between obidoxime concentration and corresponding reactivation ability of DFP-inhibited AChE.
Bottom Line: Methamidophos and leptophos-oxon were quite easily reactivatable by all tested reactivators.Therefore, we evaluated the reactivation ability of obidoxime in a concentration range of 10(-3)-10(-7) M.In the case of BChE, no reactivator exceeded 15% reactivation ability and therefore none of the oximes can be recommended as a candidate for "pseudocatalytic" bioscavengers with BChE.

View Article: PubMed Central - PubMed

Affiliation: Center of Advanced Studies, Faculty of Military Health Sciences, University of Defence, Trebesska 1575, Hradec Kralove, 500 01, Czech Republic.

ABSTRACT
We have in vitro tested the ability of common, commercially available, cholinesterase reactivators (pralidoxime, obidoxime, methoxime, trimedoxime and HI-6) to reactivate human acetylcholinesterase (AChE), inhibited by five structurally different organophosphate pesticides and inhibitors (paraoxon, dichlorvos, DFP, leptophos-oxon and methamidophos). We also tested reactivation of human butyrylcholinesterase (BChE) with the aim of finding a potent oxime, suitable to serve as a "pseudocatalytic" bioscavenger in combination with this enzyme. Such a combination could allow an increase of prophylactic and therapeutic efficacy of the administered enzyme. According to our results, the best broad-spectrum AChE reactivators were trimedoxime and obidoxime in the case of paraoxon, leptophos-oxon, and methamidophos-inhibited AChE. Methamidophos and leptophos-oxon were quite easily reactivatable by all tested reactivators. In the case of methamidophos-inhibited AChE, the lower oxime concentration (10(-5) M) had higher reactivation ability than the 10(-4) M concentration. Therefore, we evaluated the reactivation ability of obidoxime in a concentration range of 10(-3)-10(-7) M. The reactivation of methamidophos-inhibited AChE with different obidoxime concentrations resulted in a bell shaped curve with maximum reactivation at 10(-5) M. In the case of BChE, no reactivator exceeded 15% reactivation ability and therefore none of the oximes can be recommended as a candidate for "pseudocatalytic" bioscavengers with BChE.

Show MeSH
Related in: MedlinePlus