Androgen regulation of renal uridine diphosphoglucuronosyltransferase 1A1 in rats

Drug Metab Dispos. 2008 Sep;36(9):1737-9. doi: 10.1124/dmd.108.020610. Epub 2008 May 30.


Many phase I and II enzymes are under hormonal regulation, resulting in sex-related expression patterns. This sex-related enzyme expression can result in differential metabolism of physiologically active endogenous substances, altered xenobiotic clearance, and differences in susceptibility to drug toxicities. Treatment of female Sprague-Dawley (SD) rats with 5 mg testosterone propionate/kg/day, 2 ml/kg s.c. for 8 days resulted in induction of renal uridine diphosphoglucuronosyltransferase (UGT) 1A1, as determined by immunoblot and probe substrate activity. Glucuronidation activity for mycophenolic acid, a substrate for rat UGT1A1, 1A6, and 1A7, was significantly elevated approximately 2-fold in renal microsomes from testosterone propionate-treated animals. Protein expression of rat UGT1A1 was also dramatically increased, whereas 1A6 and 1A7 remained unchanged as a result of treatment. Male SD rats were determined to express greater renal UGT1A1 than age-matched female rats. These data support the androgen regulation of rat renal UGT1A1.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Androgens / pharmacology*
  • Animals
  • Blotting, Western
  • Female
  • Glucuronosyltransferase / metabolism*
  • Kidney / drug effects*
  • Kidney / enzymology
  • Male
  • Rats
  • Rats, Sprague-Dawley


  • Androgens
  • UGT1A1 enzyme
  • Glucuronosyltransferase