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

被引：66
作者：
Tamehiro, N
Sato, Y
Suzuki, T
Hashimoto, T
Asakawa, Y
Yokoyama, S
Kawanishi, T
Ohno, Y
Inoue, K
Nishimaki-Mogami, T
机构：
[1] Natl Inst Hlth Sci, Setagaya Ku, Tokyo 1588501, Japan
[2] Tokushima Bunri Univ, Fac Pharmaceut Sci, Tokushima 770, Japan
[3] Nagoya City Univ, Grad Sch Med Sci, Nagoya, Aichi 467, Japan
来源：
FEBS LETTERS | 2005年 / 579卷 / 24期
关键词：
liver X receptor; ATP-binding cassette transporter; A1; ATP-binding cassette transporter G1; HDL; cholesterol;
D O I：
10.1016/j.febslet.2005.08.054
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
Liver X receptors (LXRs) a and 0 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 LXR alpha( agonist/ LXR beta antagonist and an LXR alpha 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. (c) 2005 Published by Elsevier B.V. on behalf of the Federation of European Biochemical Societies.
引用
收藏
页码：5299 / 5304
页数：6
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