Characterization of the in vitro kinetic interaction of chlorpyrifos-oxon with rat salivary cholinesterase: a potential biomonitoring matrix

Toxicology
A A KousbaC Timchalk

Abstract

The primary mechanism of action for organophosphorus (OP) insecticides such as chlorpyrifos (CPF) involves the inhibition of acetylcholinesterase (AChE) by their active oxon metabolites resulting in a wide range of neurotoxic effects. These oxons also inhibit other cholinesterases (ChE) such as butyrylcholinesterase (BuChE), which represents a detoxification mechanism and a potential biomarker for OP insecticide exposure/response. Salivary biomonitoring has recently been explored as a practical method for examination of chemical exposure, however, there are few studies exploring the use of saliva for OP insecticides. To evaluate the use of salivary ChE as a biological monitor for OP insecticide exposure, a modified Ellman assay in conjunction with a pharmacodynamic model was used to characterize salivary ChE in adult male Sprague-Dawley rats. Comparison of rat saliva, brain, and plasma ChE activity in the presence of selective inhibitors of AChE and BuChE (BW284C51 and iso-OMPA, respectively) with different ChE substrates indicated that rat salivary ChE activity is primarily associated with BuChE (>95%). Further characterization of rat salivary BuChE kinetics yielded an average total BuChE active site concentration of 1.20+/-0....Continue Reading

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Citations

Nov 20, 2008·Journal of Exposure Science & Environmental Epidemiology·Richard C BarryCharles A Timchalk
Aug 15, 2006·Journal of Toxicology and Environmental Health. Part a·Birgit Claus HennStephanie Padilla
May 12, 2010·Basic & Clinical Pharmacology & Toxicology·Ayhan BozkurtSirri Bilge
Jun 7, 2006·Comparative Biochemistry and Physiology. Toxicology & Pharmacology : CBP·Federico CaselliElena Fabbri
Jul 26, 2005·Toxicology and Applied Pharmacology·Shakil A SaghirJames S Bus
Jul 23, 2011·Comparative Biochemistry and Physiology. Toxicology & Pharmacology : CBP·P ValbonesiE Fabbri
Oct 28, 2016·Comparative Biochemistry and Physiology. Toxicology & Pharmacology : CBP·Elvira MennilloCarlo Pretti
Oct 5, 2006·Toxicological Sciences : an Official Journal of the Society of Toxicology·Ahmed A KousbaCharles Timchalk
Dec 9, 2004·Toxicology Letters·Turhan YavuzAli Kutsal
Aug 21, 2007·Human & Experimental Toxicology·Mehmet GüneyIrfan Altuntas
Apr 4, 2013·Journal of Zhejiang University. Science. B·Yan-xia YangShao-nan Li
Mar 17, 2007·The International Journal of Neuroscience·Fatih GultekinNamik Delibas
Jan 21, 2017·Research in Veterinary Science·Saša M TrailovićJelena Nedeljković Trailović

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