Apparent induction of microsomal carboxylesterase activities in tissues of clofibrate-fed mice and rats

https://doi.org/10.1016/0041-008X(87)90155-4Get rights and content

Abstract

Treatment with 0.5% (ww) dietary clofibrate, a peroxisome proliferator, for 14 days induced microsomal carboxylesterase activities for five substrates including malathion, clofibrate, diethylsuccinate, diethylphthalate, and p-nitrophenylacetate in liver and kidney of male Swiss-Webster mice and Sprague-Dawley rats. The induction was substrate, tissue, and species dependent. The carboxylesterase activity was induced in mouse from 1.2- to 2.2-fold (liver) and from 1.1- to 1.7-fold (kidney) depending upon substrate used. Analogous values from rat ranged from 1.0- to 1.4-fold (liver) and from 1.1- to 1.8-fold (kidney). Enzyme activities were either decreased or not affected in testes of treated mice and rats. Substituted trifluoroketones (“transition-state” inhibitors of carboxylesterase) were found to be very potent inhibitors of clofibrate-metabolizing carboxylesterase(s) and to be potentially useful in distinguishing among isozymes. The inhibition data suggested that changes in carboxylesterase activity following clofibrate treatment were both qualitative and quantitative.

References (24)

Cited by (25)

  • Renal Xenobiotic Metabolism

    2018, Comprehensive Toxicology: Third Edition
  • Renal Xenobiotic Metabolism

    2010, Comprehensive Toxicology, Second Edition
  • Effect of clofibrate administration on the esterification and deesterification of steroid hormones by liver and extrahepatic tissues in rats

    2002, Biochemical Pharmacology
    Citation Excerpt :

    Carboxylesterase catalyzes the hydrolysis of a large number of xenobiotics, and many isozymes have been isolated and characterized. The induction of carboxylesterase by peroxisome proliferators is substrate dependent [21,22]. In this study, we determined esterase activity for the hydrolysis of an estradiol fatty acid ester by using estradiol-oleoyl ester as the substrate.

View all citing articles on Scopus
1

Permanent address: Department of Plant Protection, College of Agriculture, University of Zagazig, Zagazig, Egypt.

2

Current address: Center for Human Toxicology, University of Utah, Salt Lake City, UT 84112.

View full text