Antioxidant activity of nimesulide and its main metabolites.
Drugs
; 46 Suppl 1: 15-21, 1993.
Article
em En
| MEDLINE
| ID: mdl-7506157
ABSTRACT
The antioxidant activity of nimesulide and its main metabolites, 4'-hydroxynimesulide (M1) and 2-(4'-hydroxyphenoxy)-4-N-acetylamino-methansulfonanilide (M2), was investigated using 2 in vitro models NADPH-supported lipid peroxidation in rat liver microsomes (marker MDA formation) and xanthine/xanthine oxidase, iron-promoted depolymerisation of hyaluronic acid, determined by gel permeation chromatographic analysis (marker molecular weight distribution). In the lipid peroxidation model, all the compounds inhibited MDA formation in a concentration-dependent manner, although with different potencies; the maximum scavenging effect was observed for M1 [50% inhibitory concentration (IC50) = 30 mumol/L; M2 IC50 = 0.5 mmol/L; nimesulide = 0.8 mmol/L]. Nimesulide was more active than its metabolites in preventing OH-induced depolymerisation of hyaluronic acid, with a 50% effective concentration of approximately 230 mumol/L, which was fairly comparable to that of tenoxicam. This protective effect was due to the OH.-entrapping capacity of the drug, which, in the Fenton-driven model, is easily converted, via OH. attack, to M1 and putatively to 2-hydroxy-4-nitro-methansulfonanilide.
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Base de dados:
MEDLINE
Assunto principal:
Sulfonamidas
/
Anti-Inflamatórios não Esteroides
/
Antioxidantes
Limite:
Animals
Idioma:
En
Revista:
Drugs
Ano de publicação:
1993
Tipo de documento:
Article
País de afiliação:
Itália