NDLI: Comparison of the reactivation rates of acetylcholinesterase modified by structurally different organophosphates using novel pyridinium oximes

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Comparison of the reactivation rates of acetylcholinesterase modified by structurally different organophosphates using novel pyridinium oximes

Content Provider	Scilit
Author	Bharate, Sandip B. Chao, Chih-Kai Thompson, Charles M.
Copyright Year	2019
Description	Journal: Environmental toxicology and pharmacology A novel panel of oximes were synthesized, which have displayed varying degree of reactivation ability towards different organophosphorus (OP) modified cholinesterases following insecticide exposures. In the present article, we report a comparative reactivation profile of a series of quaternary pyridinium-oximes for electric eel acetylcholinesterase (EEAChE) inhibited by the organophosphorus (OP) inhibitors methyl paraoxon (MePOX), ethyl paraoxon (POX; paraoxon) and diisopropyl fluorophosphate (DFP) that are distinguishable as dimethoxyphosphoryl, diethoxyphosphoryl and diisopropoxyphosphoryl AChE-OP-adducts. Most of the 59-oximes tested led to faster and more extensive reactivation of MePOX- and POX-inhibited EEAChE as compared to DFP-modified EEAChE. All were effective reactivators of three OP-modified EEAChE conjugates showing 18–21% reactivation for DFP-inhibited AChE and ≥45% reactivation for MePOX- and POX-inhibited EEAChE. Oximes 7 and 8 showed kr values better than pralidoxime (1) for DFP-inhibited EEAChE. Reactivation rates determined at different inhibition times showed no significant change in kr values during 0–90 min incubation with three OP’s. However, a 34–72% decrease in kr for MePOX and POX and > 95% decrease in kr for DFP-inhibited EEAChE was observed after 24 h of OP-exposure (aging).
Related Links	https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6736693/pdf
Ending Page	103218
Page Count	1
Starting Page	103218
ISSN	13826689
e-ISSN	18727077
DOI	10.1016/j.etap.2019.103218
Journal	Environmental toxicology and pharmacology
Volume Number	71
Language	English
Publisher	Elsevier BV
Publisher Date	2019-10-01
Access Restriction	Open
Subject Keyword	Journal: Environmental toxicology and pharmacology Medicinal Chemistry Pyridinium Oximes Electric Eel Ache Diisopropyl Fluorophosphates
Content Type	Text
Resource Type	Article
Subject	Health, Toxicology and Mutagenesis Medicine Toxicology Pharmacology

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