twitter

Tuesday, 21 April 2015

Botanical compounds and their regulation of nuclear receptor action: The case of traditional Chinese medicine

Volume 401, 5 February 2015, Pages 221–237
Review

Botanical compounds and their regulation of nuclear receptor action: The case of traditional Chinese medicine


Highlights

Nuclear receptors are targets of compounds from traditional Chinese herbal remedies.
We review the mechanisms of action of botanical compounds on nuclear receptors.
We exemplify actions mediated by steroid receptors, metabolic receptors and RXR.
We draw a parallel between TCMs and phytoestrogens or endocrine disruptors.
We define common principle and highlight potential and limits of active compounds.

Abstract

Nuclear receptors (NRs) are major pharmacological targets that allow an access to the mechanisms controlling gene regulation. As such, some NRs were identified as biological targets of active compounds contained in herbal remedies found in traditional medicines. We aim here to review this expanding literature by focusing on the informative articles regarding the mechanisms of action of traditional Chinese medicines (TCMs). We exemplified well-characterized TCM action mediated by NR such as steroid receptors (ER, GR, AR), metabolic receptors (PPAR, LXR, FXR, PXR, CAR) and RXR. We also provided, when possible, examples from other traditional medicines. From these, we draw a parallel between TCMs and phytoestrogens or endocrine disrupting chemicals also acting via NR. We define common principle of action and highlight the potential and limits of those compounds. TCMs, by finely tuning physiological reactions in positive and negative manners, could act, in a subtle but efficient way, on NR sensors and their transcriptional network.

Abbreviations

  • AR, androgen receptor;
  • CAR, constitutive androstane receptor;
  • DBD, DNA-binding domain;
  • EDC, endocrine disrupting chemical;
  • ER, estrogen receptor;
  • FXR, farnesoid X receptor;
  • GR, glucocorticoid receptor;
  • HRE, hormone responsive elements;
  • LBD, ligand-binding domain;
  • LXR, liver X receptor;
  • NGF-IB, nerve growth factor-IB;
  • NR, nuclear receptor;
  • NURR1, nuclear receptor related 1;
  • PPAR, peroxisome proliferator activated receptor;
  • PXR, pregnane X receptor;
  • RAR, retinoid acid receptor;
  • RXR, retinoid X receptor;
  • SERM, selective estrogen receptor modulator;
  • SHP, small heterodimer partner;
  • SNuRMs, selective nuclear receptor modulators;
  • SRC, steroid receptor coactivator;
  • TCM, traditional Chinese medicine;
  • TR, thyroid receptor;
  • VDR, vitamin D receptor

Keywords

  • Nuclear receptor;
  • Traditional Chinese medicine;
  • Pharmacology;
  • Agonist;
  • Antagonist

Corresponding author. Institut de Génomique Fonctionnelle de Lyon, Ecole Normale Supérieure de Lyon, 46 allée d'Italie, 69364 Lyon 07, France. Tel.: 33 (0)4 26 73 13 76; fax: 33 (0)4 26 73 13 75.