Changes in hepatic cytosolic glutathione S-transferase enzymes induced by clotrimazole treatment in rats

Clin Exp Pharmacol Physiol. 1989 Nov;16(11):867-71. doi: 10.1111/j.1440-1681.1989.tb01526.x.

Abstract

1. The influence of the antifungal agent clotrimazole on cytosolic glutathione S-transferase activities was studied in male Wistar rats. 2. Animals received clotrimazole by gastric lavage for 3 days (75 mg/kg per day). Hepatic glutathione S-transferase activity was determined with five different substrates: 1-chloro-2,4-dinitrobenzene (CDNB), 1,2-dichloro-4-nitrobenzene (DCNB), p-nitro-benzyl chloride (PNBC), ethacrynic acid (EA) and trans-4-phenyl-3-buten-2-one (TPBO). 3. The largest increases in glutathione S-transferase activity were found with CDNB, DCNB and PNBC (+61%, +50% and +50%, respectively, when expressed per mg of cytosolic protein). Enzyme activity toward EA was induced to a lower extent (+33%). Changes in the formation of the conjugate of TPBO were relatively small (+22%). 4. These data indicate a differential induction of glutathione S-transferase isoenzymes and suggest that clotrimazole is a phenobarbital-type inducer of enzyme activity.

MeSH terms

  • Animals
  • Clotrimazole / pharmacology*
  • Cytosol / enzymology*
  • Enzyme Induction
  • Glutathione Transferase / biosynthesis
  • Glutathione Transferase / metabolism*
  • Imidazoles / pharmacology*
  • In Vitro Techniques
  • Liver / drug effects
  • Liver / enzymology*
  • Male
  • Rats
  • Rats, Inbred Strains

Substances

  • Imidazoles
  • Glutathione Transferase
  • Clotrimazole