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Titolo:
Mechanism of acetaminophen inhibition of cyclooxygenase isoforms
Autore:
Ouellet, M; Percival, MD;
Indirizzi:
Merck Frosst Ctr Therapeut Res, Dept Biochem & Mol Biol, Kirkland, PQ H9R 4P8, Canada Merck Frosst Ctr Therapeut Res Kirkland PQ Canada H9R 4P8 H9R 4P8, Canada
Titolo Testata:
ARCHIVES OF BIOCHEMISTRY AND BIOPHYSICS
fascicolo: 2, volume: 387, anno: 2001,
pagine: 273 - 280
SICI:
0003-9861(20010315)387:2<273:MOAIOC>2.0.ZU;2-K
Fonte:
ISI
Lingua:
ENG
Soggetto:
PROSTAGLANDIN-H SYNTHASE; NONSTEROIDAL ANTIINFLAMMATORY DRUGS; PEROXIDASE REACTION; REACTION-KINETICS; RADICALS; ANALOGS; COX-2; PURIFICATION; PARACETAMOL; SYNTHETASE;
Keywords:
acetaminophen; cyclooxygenase; glutathione; peroxidase; reducing agent; hydroperoxide; NSAID; analgesic; antipyretic; antiinflammatory;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
39
Recensione:
Indirizzi per estratti:
Indirizzo: Ouellet, M Merck Frosst Ctr Therapeut Res, Dept Biochem & Mol Biol, POB 1005, Kirkland, PQ H9R 4P8, Canada Merck Frosst Ctr Therapeut Res POB 1005 Kirkland PQ Canada H9R 4P8
Citazione:
M. Ouellet e M.D. Percival, "Mechanism of acetaminophen inhibition of cyclooxygenase isoforms", ARCH BIOCH, 387(2), 2001, pp. 273-280

Abstract

Acetaminophen has similar analgesic and antipyretic properties to nonsteroidal antiinflammatory drugs (NSAIDs), which act via inhibition of cyclooxygenase enzymes. However, unlike NSAIDs, acetaminophen is at best weakly antiinflammatory, The mechanism by which acetaminophen exerts its therapeutic action has yet to be fully determined, as under most circumstances, acetaminophen is a very weak cyclooxygenase inhibitor. The potency of acetaminophenagainst both purified ovine cyclooxygenase-1 (oCOX-1) and human cyclooxygenase-2 (hCOX-2) was increased approximately 30-fold by the presence of glutathione peroxidase and glutathione to give IC50 values of 33 muM and 980 muM, respectively. Acetaminophen was found to be a good reducing agent of both oCOX-1 and hCOX-2, The results are consistent with a mechanism of inhibition of acetaminophen in which it acts to reduce the active oxidized form ofCOX to the resting form. Inhibition would therefore be more effective under conditions of low peroxide concentration, consistent with the known tissue selectivity of acetaminophen, (C) 2001 Academic Press.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 28/09/20 alle ore 05:46:34