Alteration of hepatic carboxylesterase activity by soman: inhibition in vitro and enhancement in vivo.
Xenobiotica
; 19(1): 115-21, 1989 Jan.
Article
em En
| MEDLINE
| ID: mdl-2756715
ABSTRACT
1. Hydrolysis of the drug esters procaine, chloramphenicol succinate, and prednisolone succinate was studied. Addition of soman to guinea pig liver microsomes caused a dose-dependent inhibition of hydrolysis of all three substrates; at the highest soman concentration (1 microM), ester hydrolysis was totally abolished. 2. Ester hydrolysis was also measured in liver microsomes from guinea pigs pretreated with soman at a low dose (10% of LD50) or at a high dose (90% of LD50) either 1 h or 12 h before killing. Plasma-cholinesterase activity was decreased in all pretreated animals. Liver carboxylesterase activity, measured with the three drug substrates and by hydrolysis of 4-nitrophenyl acetate was increased by all pretreatments. 3. This enhancing effect varies with the substrate and increases with dose of soman. The 12 h pretreatment produced a greater increase in activity than did the 1 h pretreatment. 4. These studies indicate that soman is a potent inhibitor of carboxylesterase activity in vitro but increases the activity of the liver enzyme when administered in vivo.
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Soman
/
Microssomos Hepáticos
/
Hidrolases de Éster Carboxílico
Limite:
Animals
Idioma:
En
Revista:
Xenobiotica
Ano de publicação:
1989
Tipo de documento:
Article