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Int. J. Mol. Sci. 2011, 12(3), 2077-2087; doi:10.3390/ijms12032077
Article

In Vitro Ability of Currently Available Oximes to Reactivate Organophosphate Pesticide-Inhibited Human Acetylcholinesterase and Butyrylcholinesterase

1,2,3,* , 4,5
, 6
 and 1,*
Received: 11 February 2011; Accepted: 9 March 2011 / Published: 23 March 2011
(This article belongs to the Section Molecular Toxicology)
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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” 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.
Keywords: acetylcholinesterase; butyrylcholinesterase; in vitro; nerve agent; organophosphate; pesticide; reactivator; oxime; scavenger acetylcholinesterase; butyrylcholinesterase; in vitro; nerve agent; organophosphate; pesticide; reactivator; oxime; scavenger
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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MDPI and ACS Style

Jun, D.; Musilova, L.; Musilek, K.; Kuca, K. In Vitro Ability of Currently Available Oximes to Reactivate Organophosphate Pesticide-Inhibited Human Acetylcholinesterase and Butyrylcholinesterase. Int. J. Mol. Sci. 2011, 12, 2077-2087.

AMA Style

Jun D, Musilova L, Musilek K, Kuca K. In Vitro Ability of Currently Available Oximes to Reactivate Organophosphate Pesticide-Inhibited Human Acetylcholinesterase and Butyrylcholinesterase. International Journal of Molecular Sciences. 2011; 12(3):2077-2087.

Chicago/Turabian Style

Jun, Daniel; Musilova, Lucie; Musilek, Kamil; Kuca, Kamil. 2011. "In Vitro Ability of Currently Available Oximes to Reactivate Organophosphate Pesticide-Inhibited Human Acetylcholinesterase and Butyrylcholinesterase." Int. J. Mol. Sci. 12, no. 3: 2077-2087.


Int. J. Mol. Sci. EISSN 1422-0067 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert