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

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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{norm of matrix} 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 ofmethamidophos-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. © 2011 by the authors; licensee MDPI, Basel, Switzerland.

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Jun, D., Musilova, L., Musilek, K., & Kuca, K. (2011). In Vitro ability of currently available oximes to reactivate organophosphate pesticide-inhibited human acetylcholinesterase and butyrylcholinesterase. International Journal of Molecular Sciences, 12(3), 2077–2087. https://doi.org/10.3390/ijms12032077

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