Evidence for the activation of organophosphate pesticides by cytochromes P450 3A4 and 2D6 in human liver microsomes

Toxicology Letters

Volumn 116, Issue 3, 2000, Pages 217-221

  Sams, Craig ^a   Mason, Howard J ^a   Rawbone, Roger ^b  

^a HEALTH AND SAFETY LABORATORY   (United Kingdom)

^b HEALTH AND SAFETY EXECUTIVE   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

CHLORPYRIFOS; CHOLINESTERASE; CYTOCHROME P450 2D6; CYTOCHROME P450 3A4; CYTOCHROME P450 ISOENZYME; DIMPYLATE; KETOCONAZOLE; ORGANOPHOSPHATE PESTICIDE; PARATHION; QUINIDINE; UNCLASSIFIED DRUG;

ARTICLE; BIOTRANSFORMATION; CATALYSIS; CONTROLLED STUDY; ENZYME ACTIVITY; ENZYME INHIBITION; HUMAN; HUMAN CELL; LIVER MICROSOME; PRIORITY JOURNAL; STRUCTURE ANALYSIS;

BIOTRANSFORMATION; CHOLINESTERASE INHIBITORS; CYTOCHROME P-450 CYP2D6; CYTOCHROME P-450 ENZYME SYSTEM; DOSE-RESPONSE RELATIONSHIP, DRUG; HUMAN; INSECTICIDES, ORGANOPHOSPHATE; KETOCONAZOLE; MICROSOMES, LIVER; MIXED FUNCTION OXYGENASES; QUINIDINE;

EID: 0034674894     PISSN: 03784274     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0378-4274(00)00221-6     Document Type: Article

References (12)

1. Bourrie M., Meunier V., Berger Y., Fabre G. Cytochrome P450 isoform inhibitors as a tool for the investigation of metabolic reactions catalysed by human liver microsomes. J. Pharmacol. Exp. Ther. 277:1996;321-332.
2. Butler A.M., Murray M. Biotransformation of parathion in human liver:participation of CYP3A4 and its inactivation during microsomal parathion oxidation. J. Pharmacol. Exp. Ther. 280:1997;966-973.
3. Eagling V.A., Tjia J.F., Back D.J. Differential selectivity of cytochrome P450 inhibitors against probe substrates in human and rat liver microsomes. Br. J. Clin. Pharmacol. 45:1998;107-114.
4. Eto M. Organophosphorus Pesticides: Organic and Biological Chemistry. 1974;CRC Press, Cleveland.
5. Gonzalez F.J., Skoda R.C., Kimura S., Umeno M., Zanger U.M., Nebert D.W., Gelboin H.V., Hardwick J.P., Meyer U.A. Characterisation of the common genetic defect in humans deficient in debrisoquine metabolism. Nature. 331:1988;442-446.
6. Heath A.J.W., Vale J.A. Ballantyne B., Marrs T.C. Organophosphates and Carbamates. 1992;513-519 Butterworth-Heinemann, Oxford.
7. Lewis P.J., Lowing R., Gompertz D. Automated discrete kinetic method for erythrocyte acetylcholinesterase and plasma cholinesterase. Clin. Chem. 27:1981;926-929.
8. Lewis D.F.V. Cytochromes P450: Structure, Function and Mechanism. 1996;Taylor and Francis, Basingstoke.
9. Mutch E., Blain P.G., Williams F.M. The role of metabolism in determining susceptibility to parathion toxicity in man. Toxicol. Lett. 107:1999;177-187.
10. Neal R.A. Studies on the metabolism of diethyl-4-nitrophenyl phosphorothionate (parathion) in vitro. Biochem. J. 103:1967;183-191.
11. Sams C., Mason H.J. Detoxification of organophosphates by A-esterases in human serum. Hum. Exp. Toxicol. 18:1999;653-658.
12. Smith D.A., Abel S.M., Hyland R., Jones B.C. Human cytochrome P450s: selectivity and measurement in vivo. Xenobiotica. 28:1998;1095-1128.