Modulation of rat hepatic CYP3A by nonylphenol

Xenobiotica. 1996 Aug;26(8):831-8. doi: 10.3109/00498259609046753.

Abstract

1. In in vitro assays, nonylphenol (NP) inhibited microsomal 5 alpha-reductase and steroid hydroxylase activities from the liver of dexamethasone-treated rats. The inhibition was specific in that 6 beta-hydroxylase was affected the most followed by 16 alpha-hydroxylase. The activity of 17 alpha-hydroxylase remained unchanged. 2. Enzyme kinetic analyses (Lineweaver Burke plots) using different NP concentrations with graded increases in the concentrations of the substrate, progesterone, showed that the inhibition was of a mixed competitive and non-competitive type. 3. In in vivo studies, treatment of rats with NP resulted in a dose dependent increase in the hepatic microsomal progesterone hydroxylase activity and CYP3A proteins as measured by Western blot analysis. 4. The mixed competitive and non-competitive nature of inhibition by NP on hepatic microsomal progesterone hydroxylase activity indirectly suggests that this compound may behave as a partial substrate of the CYP3A enzyme. More importantly, nonylphenol induces the expression of rat hepatic CYP3A which may then affect its own metabolism and that of other steroid substrates.

Publication types

  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Age Factors
  • Animals
  • Aryl Hydrocarbon Hydroxylases*
  • Binding, Competitive
  • Blotting, Western
  • Cholestenone 5 alpha-Reductase
  • Cytochrome P-450 Enzyme System / drug effects
  • Cytochrome P-450 Enzyme System / metabolism*
  • Dose-Response Relationship, Drug
  • Female
  • Microsomes, Liver / drug effects
  • Microsomes, Liver / metabolism*
  • Oxidoreductases / drug effects
  • Oxidoreductases / metabolism
  • Phenols / metabolism*
  • Phenols / pharmacology*
  • Pregnancy
  • Progesterone / metabolism
  • Rats
  • Rats, Sprague-Dawley
  • Steroid 16-alpha-Hydroxylase
  • Steroid 17-alpha-Hydroxylase / drug effects
  • Steroid 17-alpha-Hydroxylase / metabolism
  • Steroid Hydroxylases / drug effects
  • Steroid Hydroxylases / metabolism*
  • Substrate Specificity

Substances

  • Phenols
  • Progesterone
  • nonylphenol
  • Cytochrome P-450 Enzyme System
  • Oxidoreductases
  • Steroid Hydroxylases
  • Aryl Hydrocarbon Hydroxylases
  • Steroid 16-alpha-Hydroxylase
  • steroid 16-beta-hydroxylase
  • steroid hormone 6-beta-hydroxylase
  • Steroid 17-alpha-Hydroxylase
  • Cholestenone 5 alpha-Reductase