Riccardin C: a natural product that functions as a liver X receptor (LXR)alpha agonist and an LXRbeta antagonist

FEBS Lett. 2005 Oct 10;579(24):5299-304. doi: 10.1016/j.febslet.2005.08.054.

Abstract

Liver X receptors (LXRs) alpha and beta share considerable sequence homology and several functions, respond to the same endogenous and synthetic ligands, and play critical roles in maintaining lipid homeostasis. In this study, liverwort-derived riccardin C (RC) and F (RF) were identified as an LXRalpha agonist/LXRbeta antagonist and an LXRalpha antagonist, respectively. RC and RF bound to LXRs, but had different abilities to recruit a coactivator and thereby induce transactivation. Despite its unique subtype-selective activity, RC enhanced ABCA1 and ABCG1 expression and cellular cholesterol efflux in THP-1 cells. RC may provide a novel tool for identifying subtype-function and drug development.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Biological Products / pharmacology*
  • Cell Line
  • DNA-Binding Proteins / agonists*
  • DNA-Binding Proteins / antagonists & inhibitors*
  • Ethers, Cyclic / pharmacology*
  • Humans
  • Liver X Receptors
  • Orphan Nuclear Receptors
  • Receptors, Cytoplasmic and Nuclear / agonists*
  • Receptors, Cytoplasmic and Nuclear / antagonists & inhibitors*
  • Reverse Transcriptase Polymerase Chain Reaction

Substances

  • Biological Products
  • DNA-Binding Proteins
  • Ethers, Cyclic
  • Liver X Receptors
  • NR1H3 protein, human
  • Orphan Nuclear Receptors
  • Receptors, Cytoplasmic and Nuclear
  • riccardin C