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

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

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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.

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