TGFβ1-mediated suppression of cytochrome P450(CYP) induction responses in rat hepatocyte-fibroblast co-cultures

Toxicol In Vitro. 2018 Aug:50:47-53. doi: 10.1016/j.tiv.2018.01.015. Epub 2018 Jan 31.

Abstract

Co-culture of hepatocyte and fibroblasts has shown distinct advantages in enhancing certain liver specific functions and maintaining hepatic polarity. However, the utility of hepatocyte co-culture models for studies, such as drug-drug interaction studies, has not been completely elucidated. In this study the induction of Cyp1a2, Cyp2b1/2, and Cyp3a2, the three major cytochrome P450 (CYP) isoforms in the rat liver, was evaluated in randomly mixed co-cultures and micropatterned co-cultures. We found that in both co-culture configurations, the drug-induced Cyp1a2, Cyp2b1/2, Cyp3a2 mRNA and activity were suppressed relative to those in monocultured hepatocytes. Further, we observed a significant increase in TGFβ1 production in the co-cultures. Addition of 100 pg/ml TGFβ1 to hepatocyte monocultures resulted in the suppression of Cyp1a2, Cyp2b1/2, and Cyp3a2 induction. These findings implicate TGFβ1 as one of the important factors impairing drug induced CYP induction in co-cultures and suggests that caution needs to be exercised in the use of hepatocyte-fibroblast co-cultures for CYP induction studies.

Keywords: CYP 450; Co-cultures; Drug interactions; Hepatocytes; TGF-Beta 1.

MeSH terms

  • Animals
  • Cells, Cultured
  • Coculture Techniques
  • Cytochrome P-450 Enzyme Inducers / pharmacology
  • Cytochrome P-450 Enzyme System / genetics
  • Cytochrome P-450 Enzyme System / metabolism*
  • Enzyme Induction*
  • Fibroblasts / metabolism*
  • Hepatocytes / metabolism*
  • Male
  • Mice
  • NIH 3T3 Cells
  • Rats, Wistar
  • Transforming Growth Factor beta1 / metabolism*

Substances

  • Cytochrome P-450 Enzyme Inducers
  • Tgfb1 protein, rat
  • Transforming Growth Factor beta1
  • Cytochrome P-450 Enzyme System