Hepatic biotransformation of the flukicidal agent nitroxynil (3-iodo-4-hydroxy-5-nitrobenzonitrile) (I) has been studied with rat liver subcellular fractions as the source of enzymes: two metabolites, 3-iodo-4--hydroxy-5-aminobenzonitrile (II) and 3-iodo-4-hydroxy-5-nitrobenzamide (III) have been identified by standard analytical techniques (TLC, GLC and MS). The nitroaromatic reduction product (II) is formed in the hepatocyte in a process in which cytosol and endoplasmic reticulum enzymes cooperate. This formation is maximal in anaerobic conditions, but takes also place aerobically and in the absence of electrogenic cofactors. Cytochrome P-450 plays a major role in the denitrification process, and consequently could be the cellular site most exposed to damage by the intermediate arylhydroxylamine formed by reduction.

The reductive metabolism of the nitroaromatic flukicidal agent nitroxinil by liver microsomal cytochrome P-450 / R. Maffei Facino, D. Pitrè, M. Carini. - In: IL FARMACO. EDIZIONE SCIENTIFICA. - ISSN 0430-0920. - 37:7(1982), pp. 463-474.

The reductive metabolism of the nitroaromatic flukicidal agent nitroxinil by liver microsomal cytochrome P-450

R. Maffei Facino;M. Carini
1982

Abstract

Hepatic biotransformation of the flukicidal agent nitroxynil (3-iodo-4-hydroxy-5-nitrobenzonitrile) (I) has been studied with rat liver subcellular fractions as the source of enzymes: two metabolites, 3-iodo-4--hydroxy-5-aminobenzonitrile (II) and 3-iodo-4-hydroxy-5-nitrobenzamide (III) have been identified by standard analytical techniques (TLC, GLC and MS). The nitroaromatic reduction product (II) is formed in the hepatocyte in a process in which cytosol and endoplasmic reticulum enzymes cooperate. This formation is maximal in anaerobic conditions, but takes also place aerobically and in the absence of electrogenic cofactors. Cytochrome P-450 plays a major role in the denitrification process, and consequently could be the cellular site most exposed to damage by the intermediate arylhydroxylamine formed by reduction.
Settore CHIM/08 - Chimica Farmaceutica
IL FARMACO. EDIZIONE SCIENTIFICA
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Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/2434/183074
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