title: Riccardin C: a natural product that functions as a liver X receptor (LXR)alpha agonist and an LXRbeta antagonist.
abstract: Liver X receptors (LXRs) alpha and beta 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 LXRalpha agonist/LXRbeta antagonist and an LXRalpha 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.
authors.affiliation: National Institute of Health Sciences, Setagaya-ku, Tokyo, Japan.
authors.forename: Norimasa
authors.initials: N
authors.lastname: Tamehiro
authors.forename: Yoji
authors.initials: Y
authors.lastname: Sato
authors.forename: Takuo
authors.initials: T
authors.lastname: Suzuki
authors.forename: Toshihiro
authors.initials: T
authors.lastname: Hashimoto
authors.forename: Yoshinori
authors.initials: Y
authors.lastname: Asakawa
authors.forename: Shinji
authors.initials: S
authors.lastname: Yokoyama
authors.forename: Tohru
authors.initials: T
authors.lastname: Kawanishi
authors.forename: Yasuo
authors.initials: Y
authors.lastname: Ohno
authors.forename: Kazuhide
authors.initials: K
authors.lastname: Inoue
authors.forename: Taku
authors.initials: T
authors.lastname: Nagao
authors.forename: Tomoko
authors.initials: T
authors.lastname: Nishimaki-Mogami
mesh_terms: D001688:Biological Products / Q000494:pharmacology*; D002460:Cell Line; D004268:DNA-Binding Proteins / Q000819:agonists* / Q000037:antagonists & inhibitors*; D004988:Ethers, Cyclic / Q000494:pharmacology*; D006801:Humans; D000071518:Liver X Receptors; D057093:Orphan Nuclear Receptors; D018160:Receptors, Cytoplasmic and Nuclear / Q000819:agonists* / Q000037:antagonists & inhibitors*; D020133:Reverse Transcriptase Polymerase Chain Reaction
chemical_list: D001688:Biological Products; D004268:DNA-Binding Proteins; D004988:Ethers, Cyclic; D000071518:Liver X Receptors; C000605213:NR1H3 protein, human; D057093:Orphan Nuclear Receptors; D018160:Receptors, Cytoplasmic and Nuclear; C505660:riccardin C