Premium
Riccardin C: A natural product that functions as a liver X receptor (LXR)α agonist and an LXRβ antagonist
Author(s) -
Tamehiro Norimasa,
Sato Yoji,
Suzuki Takuo,
Hashimoto Toshihiro,
Asakawa Yoshinori,
Yokoyama Shinji,
Kawanishi Tohru,
Ohno Yasuo,
Inoue Kazuhide,
Nagao Taku,
Nishimaki-Mogami Tomoko
Publication year - 2005
Publication title -
febs letters
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.593
H-Index - 257
eISSN - 1873-3468
pISSN - 0014-5793
DOI - 10.1016/j.febslet.2005.08.054
Subject(s) - liver x receptor , abcg1 , transactivation , abca1 , agonist , coactivator , antagonist , nuclear receptor , chemistry , biology , pharmacology , receptor , endocrinology , biochemistry , transcription factor , transporter , gene
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.