TY - JOUR
T1 - Riccardin C
T2 - A natural product that functions as a liver X receptor (LXR)α agonist and an LXRβ antagonist
AU - Tamehiro, Norimasa
AU - Sato, Yoji
AU - Suzuki, Takuo
AU - Hashimoto, Toshihiro
AU - Asakawa, Yoshinori
AU - Yokoyama, Shinji
AU - Kawanishi, Tohru
AU - Ohno, Yasuo
AU - Inoue, Kazuhide
AU - Nagao, Taku
AU - Nishimaki-Mogami, Tomoko
N1 - Funding Information:
This work was supported in part by a grant (MF-16) from the Organization for Pharmaceutical Safety and Research and a grant from the Japan Health Sciences Foundation.
PY - 2005/10/10
Y1 - 2005/10/10
N2 - 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.
AB - 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.
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U2 - 10.1016/j.febslet.2005.08.054
DO - 10.1016/j.febslet.2005.08.054
M3 - Article
C2 - 16182288
AN - SCOPUS:25844438389
SN - 0014-5793
VL - 579
SP - 5299
EP - 5304
JO - FEBS Letters
JF - FEBS Letters
IS - 24
ER -