The farnesoid X-receptor is an essential regulator of cholesterol homeostasis

J Biol Chem. 2003 Jan 24;278(4):2563-70. doi: 10.1074/jbc.M209525200. Epub 2002 Nov 5.

Abstract

To address the importance of the farnesoid X-receptor (FXR; NR1H4) for normal cholesterol homeostasis, we evaluated the major pathways of cholesterol metabolism in the FXR-deficient (-/-) mouse model. Compared with wild-type, FXR(-/-) mice have increased plasma high density lipoprotein (HDL) cholesterol and a markedly reduced rate of plasma HDL cholesterol ester clearance. Concomitantly, FXR(-/-) mice exhibit reduced expression of hepatic genes involved in reverse cholesterol transport, most notably, that for scavenger receptor BI. FXR(-/-) mice also have increased: (i) plasma non-HDL cholesterol and triglyceride levels, (ii) apolipoprotein B-containing lipoprotein synthesis, and (iii) intestinal cholesterol absorption. Surprisingly, biliary cholesterol elimination was increased in FXR(-/-) mice, despite decreased expression of hepatic genes thought to be involved in this process. These data demonstrate that FXR is a critical regulator of normal cholesterol metabolism and that genetic changes affecting FXR function have the potential to be pro-atherogenic.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Apolipoproteins B / blood
  • Biological Transport
  • Blotting, Northern
  • Blotting, Western
  • Cholesterol / blood
  • Cholesterol / metabolism*
  • DNA-Binding Proteins
  • Ileum / metabolism
  • Kinetics
  • Lipid Metabolism
  • Liver / metabolism
  • Mice
  • Mice, Inbred C57BL
  • Mice, Transgenic
  • Models, Biological
  • RNA, Messenger / metabolism
  • Receptors, Cytoplasmic and Nuclear / genetics
  • Receptors, Cytoplasmic and Nuclear / metabolism*
  • Receptors, Cytoplasmic and Nuclear / physiology*
  • Time Factors
  • Transcription Factors
  • Triglycerides / blood

Substances

  • Apolipoproteins B
  • DNA-Binding Proteins
  • RNA, Messenger
  • Receptors, Cytoplasmic and Nuclear
  • Transcription Factors
  • Triglycerides
  • farnesoid X-activated receptor
  • Cholesterol