The negative effects of bile acids and tumor necrosis factor-alpha on the transcription of cholesterol 7alpha-hydroxylase gene (CYP7A1) converge to hepatic nuclear factor-4: a novel mechanism of feedback regulation of bile acid synthesis mediated by nuclear receptors

J Biol Chem. 2001 Aug 17;276(33):30708-16. doi: 10.1074/jbc.M103270200. Epub 2001 Jun 11.

Abstract

Bile acids regulate the cholesterol 7alpha-hydroxylase gene (CYP7A1), which encodes the rate-limiting enzyme in the classical pathway of bile acid synthesis. Here we report a novel mechanism whereby bile acid feedback regulates CYP7A1 transcription through the nuclear receptor hepatocyte nuclear factor-4 (HNF-4), which binds to the bile acid response element (BARE) at nt -149/-118 relative to the transcription start site. Using transient transfection assays of HepG2 cells with Gal4-HNF-4 fusion proteins, we show that chenodeoxycholic acid (CDCA) dampened the transactivation potential of HNF-4. Overexpression of a constitutive active form of MEKK1, an upstream mitogen-activated protein kinase (MAPK) module triggered by stress signals, strongly repressed the promoter activity of CYP7A1 via the consensus sequence for HNF-4 embedded in the BARE. Similarly, MEKK1 inhibited the activity of HNF-4 in the Gal4-based assay. The involvement of the MEKK1-dependent pathway in the bile acid-mediated repression of CYP7A1 was confirmed by co-transfecting a dominant negative form of the stress-activated protein kinase kinase, SEK, which abolished the effect of CDCA upon CYP7A1 transcription. Treatment of transfected HepG2 cells with tumor necrosis factor alpha (TNF-alpha), an activator of the MEKK1 pathway, led to the repression of CYP7A1 via the HNF-4 site in the BARE. TNF-alpha also inhibited the transactivation potential of HNF-4. Collectively, our results demonstrate for the first time that HNF-4, in combination with a MAPK signaling pathway, acts as a bile acid sensor in the liver. Furthermore, the effects of CDCA and TNF-alpha converge to HNF-4, which binds to the BARE of CYP7A1, suggesting a link between the cascades elicited by bile acids and pro-inflammatory stimuli in the liver.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Basic Helix-Loop-Helix Leucine Zipper Transcription Factors
  • Bile Acids and Salts / biosynthesis
  • Bile Acids and Salts / pharmacology*
  • Cells, Cultured
  • Cholesterol 7-alpha-Hydroxylase / genetics*
  • DNA-Binding Proteins*
  • Feedback
  • Hepatocyte Nuclear Factor 4
  • Humans
  • MAP Kinase Kinase Kinase 1*
  • Phosphoproteins / physiology*
  • Protein Serine-Threonine Kinases / physiology
  • Response Elements
  • Transcription Factors / physiology*
  • Transcription, Genetic / drug effects*
  • Transcriptional Activation
  • Tumor Necrosis Factor-alpha / pharmacology*

Substances

  • Basic Helix-Loop-Helix Leucine Zipper Transcription Factors
  • Bile Acids and Salts
  • DNA-Binding Proteins
  • Hepatocyte Nuclear Factor 4
  • MLX protein, human
  • Phosphoproteins
  • Transcription Factors
  • Tumor Necrosis Factor-alpha
  • Cholesterol 7-alpha-Hydroxylase
  • Protein Serine-Threonine Kinases
  • MAP Kinase Kinase Kinase 1
  • MAP3K1 protein, human