NDLI: In vitro reactivation of trichlorfon-inhibited butyrylcholinesterase using HI-6, obidoxime, pralidoxime and K048

Content Provider	Taylor & Francis Online
Author	Pohanka, Miroslav Jun, Daniel Kuca, Kamil
Abstract	Trichlorfon is a specific inhibitor of cholinesterases. It was typically used as an insecticide; however, trichlorfon was described as useful for symptomatic treatment of Alzheimer's disease some years ago. The presented study is aimed at reactivation of trichlorfon-inhibited butyrylcholinesterase since this enzyme play an important role in Alzheimer's disease as deputy for acetylcholinesterase and furthermore it could be applied as a scavenger in case of overdosing. We used in vitro reactivation test for considering only reactivation efficacy of butyrylcholinesterase that is inhibited by trichlorfon and not reactivation of butyrylcholinesterase inhibited by trichlorfon metabolic products. Four reactivators were used: HI-6, pralidoxime, obidoxime, and K048. Although all of the reactivators seem to be effective at 1 mM concentration, a lower concentration was not able ensure sufficient reactivation. There was also an observed lowering of reactivation efficacy when butyrylcholinesterase was exposed to trichlorfon for a longer time interval.
Starting Page	680
Ending Page	683
Page Count	4
File Format	PDF HTM / HTML
ISSN	14756366 14756374
DOI	10.1080/14756360802328315
Journal	Journal of Enzyme Inhibition and Medicinal Chemistry
Volume Number	24
Issue Number	3
Language	English
Publisher	Taylor & Francis
Publisher Date	2009-06-01
Access Restriction	Open
Subject Keyword	Metrifonate Chlorophos Alzheimer's disease Reactivation Oxime Butyrylcholinesterase Trichlorfon
Content Type	Text
Resource Type	Article
Subject	Drug Discovery Medicine Pharmacology

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