Riccardin C: A natural product that functions as a liver X receptor (LXR)α agonist and an LXRβ antagonist

Norimasa Tamehiro, Yoji Sato, Takuo Suzuki, Toshihiro Hashimoto, Yoshinori Asakawa, Shinji Yokoyama, Tohru Kawanishi, Yasuo Ohno, Kazuhide Inoue, Taku Nagao, Tomoko Nishimaki-Mogami

Research output: Contribution to journalArticlepeer-review

60 Citations (Scopus)

Abstract

Liver X receptors (LXRs) α and β 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 LXRα agonist/LXRβ antagonist and an LXRα 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.

Original languageEnglish
Pages (from-to)5299-5304
Number of pages6
JournalFEBS Letters
Volume579
Issue number24
DOIs
Publication statusPublished - Oct 10 2005
Externally publishedYes

All Science Journal Classification (ASJC) codes

  • Biophysics
  • Structural Biology
  • Biochemistry
  • Molecular Biology
  • Genetics
  • Cell Biology

Fingerprint Dive into the research topics of 'Riccardin C: A natural product that functions as a liver X receptor (LXR)α agonist and an LXRβ antagonist'. Together they form a unique fingerprint.

Cite this