Riccardin C: A natural product that functions as a liver X receptor (LXR)α agonist and an LXRβ antagonist
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- 作者：Norimasa Tamehiro ; Yoji Sato ; Takuo Suzuki ; Toshihiro Hashimoto ; Yoshinori Asakawa ; Shinji Yokoyama ; Tohru Kawanishi ; Yasuo Ohno ; Kazuhide Inoue ; Taku Nagao and Tomoko Nishimaki-Mogami
- 关键词：Liver X receptor ; ATP-binding cassette transporter A1 ; ATP-binding cassette transporter G1 ; HDL ; Cholesterol
- 刊名：FEBS Letters
- 出版年：2005
- 出版时间：2005
- 年：2005
- 卷：579
- 期：24
- 页码：5299-5304
- 全文大小：322 K
文摘
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.