Decrease in hepatic microsomal UDP-glucuronosyl-transferase activity in rats and cattle with fascioliasis: impaired in vitro glucuronidation of oxyclozanide

Toxicol Lett. 1985 Jul;26(1):65-71. doi: 10.1016/0378-4274(85)90186-9.

Abstract

The effects of liver fluke infection (Fasciola hepatica) on hepatic microsomal UDP-glucuronosyl-transferase activity have been studied in microsomes from experimentally infected rats and naturally infected cattle to see if they explain the toxic episodes observed in parasite-infected animals subjected to intensive chemotherapy with the flukicidal drug oxyclozanide. Dramatic decreases in the activity of this enzyme system with the typical substrate p-nitrophenol were observed in both animal species, even when little or no degenerative lesions could be seen in the liver parenchyma. In vitro there was a similar loss of glucuronic acid conjugation of oxyclozanide by hepatic microsomes from infected cattle. In vivo this would result in slower elimination of the drug and in drug accumulation.

MeSH terms

  • Animals
  • Cattle
  • Cattle Diseases / drug therapy*
  • Cattle Diseases / enzymology
  • Fasciola hepatica / isolation & purification
  • Fascioliasis / drug therapy*
  • Fascioliasis / enzymology
  • Fascioliasis / veterinary
  • Feces / parasitology
  • Glucuronates / metabolism
  • Glucuronic Acid
  • Glucuronosyltransferase / metabolism*
  • Kinetics
  • Male
  • Microsomes, Liver / drug effects*
  • Microsomes, Liver / enzymology
  • Microsomes, Liver / metabolism
  • Nitrophenols / metabolism
  • Oxyclozanide / metabolism
  • Oxyclozanide / therapeutic use*
  • Rats
  • Rats, Inbred Strains
  • Salicylamides / therapeutic use*

Substances

  • Glucuronates
  • Nitrophenols
  • Salicylamides
  • Oxyclozanide
  • Glucuronic Acid
  • Glucuronosyltransferase
  • 4-nitrophenol