In vitro comparison of aldicarb oxidation in various food-producing animal species.
Aldicarb (ALD) metabolism was studied in vitro using hepatic microsomes from chickens, rabbits, sheep and pigs. The microsomal activities of mono-ooxygenase enzymes (flavin-containing and cytochrome P-450-dependent mixed function oxygenases) were compared by measuring the quantity of the 2 oxidized metabolites, ALD sulfoxide and ALD sulfone, produced during 60 min of incubation. Pig microsomes produced the greatest quantity of ALD sulfoxide and the lowest quantity of ALD sulfone; the latter being produced in greater quantities in sheep than in chickens and rabbits. Aldicarb and its metabolites were degraded fastest in rabbits, probably by hydrolytic reactions. These in vitro results, which are consistent both with the levels of cytochrome P450 found in hepatic microsomes and previous in vivo data on ALD kinetics in pigs, rabbits and chickens, indicate that preliminary in vitro studies can limit the necessary use of animals for drug metabolism experiments.
Institute of Pharmacology, Pharmacokinetics and Toxicology, Faculty of Veterinary Medicine, Bologna, Italy.
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Montesissa
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De Liguoro
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Amorena
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Lucisano
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Carli
D000448:Aldicarb / Q000378:metabolism* / Q000493:pharmacokinetics / Q000633:toxicity; D000826:Animal Testing Alternatives; D000818:Animals; D002645:Chickens; D002851:Chromatography, High Pressure Liquid; D003577:Cytochrome P-450 Enzyme System / Q000378:metabolism*; D005415:Flavins / Q000378:metabolism; D066298:In Vitro Techniques; D007306:Insecticides / Q000378:metabolism* / Q000493:pharmacokinetics / Q000633:toxicity; D007527:Isoenzymes / Q000378:metabolism; D008297:Male; D008862:Microsomes, Liver / Q000187:drug effects / Q000201:enzymology*; D010084:Oxidation-Reduction; D011817:Rabbits; D012756:Sheep; D013045:Species Specificity; D013552:Swine
D005415:Flavins; D007306:Insecticides; D007527:Isoenzymes; D000448:Aldicarb; D003577:Cytochrome P-450 Enzyme System