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

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

Research output: Contribution to journalArticle

57 Citations (Scopus)

Abstract

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.

Original languageEnglish
Pages (from-to)5299-5304
Number of pages6
JournalFEBS Letters
Volume579
Issue number24
DOIs
Publication statusPublished - Oct 10 2005

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Biological Products
Liver
Hepatophyta
Sequence Homology
Transcriptional Activation
Homeostasis
Cholesterol
riccardin C
Liver X Receptors
Ligands
Lipids
Pharmaceutical Preparations
riccardin F

All Science Journal Classification (ASJC) codes

  • Biophysics
  • Structural Biology
  • Biochemistry
  • Molecular Biology
  • Genetics
  • Cell Biology

Cite this

Tamehiro, N., Sato, Y., Suzuki, T., Hashimoto, T., Asakawa, Y., Yokoyama, S., ... Nishimaki-Mogami, T. (2005). Riccardin C: A natural product that functions as a liver X receptor (LXR)α agonist and an LXRβ antagonist. FEBS Letters, 579(24), 5299-5304. https://doi.org/10.1016/j.febslet.2005.08.054

Riccardin C : A natural product that functions as a liver X receptor (LXR)α agonist and an LXRβ antagonist. / Tamehiro, Norimasa; Sato, Yoji; Suzuki, Takuo; Hashimoto, Toshihiro; Asakawa, Yoshinori; Yokoyama, Shinji; Kawanishi, Tohru; Ohno, Yasuo; Inoue, Kazuhide; Nagao, Taku; Nishimaki-Mogami, Tomoko.

In: FEBS Letters, Vol. 579, No. 24, 10.10.2005, p. 5299-5304.

Research output: Contribution to journalArticle

Tamehiro, N, Sato, Y, Suzuki, T, Hashimoto, T, Asakawa, Y, Yokoyama, S, Kawanishi, T, Ohno, Y, Inoue, K, Nagao, T & Nishimaki-Mogami, T 2005, 'Riccardin C: A natural product that functions as a liver X receptor (LXR)α agonist and an LXRβ antagonist', FEBS Letters, vol. 579, no. 24, pp. 5299-5304. https://doi.org/10.1016/j.febslet.2005.08.054
Tamehiro, Norimasa ; Sato, Yoji ; Suzuki, Takuo ; Hashimoto, Toshihiro ; Asakawa, Yoshinori ; Yokoyama, Shinji ; Kawanishi, Tohru ; Ohno, Yasuo ; Inoue, Kazuhide ; Nagao, Taku ; Nishimaki-Mogami, Tomoko. / Riccardin C : A natural product that functions as a liver X receptor (LXR)α agonist and an LXRβ antagonist. In: FEBS Letters. 2005 ; Vol. 579, No. 24. pp. 5299-5304.
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