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Evodia alkaloids suppress gluconeogenesis and lipogenesis by activating the constitutive androstane receptor

Lushan Yu1, Zhangting Wang1, Minmin Huang1

  • 1Department of Pharmaceutical Analysis and Drug Metabolism, Zhejiang Province Key Laboratory of Anti-Cancer Drug Research, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, China.

Biochimica Et Biophysica Acta
|October 13, 2015
PubMed

Insights

Evodia alkaloids rutaecarpine and evodiamine activate human constitutive androstane receptor (hCAR), suppressing glucose and fat production. This suggests potential for treating hyperglycemia and type 2 diabetes.

Area of Science:

  • Nuclear receptor signaling
  • Metabolic regulation
  • Pharmacology

Background:

  • Constitutive androstane receptor (CAR) is crucial for metabolism and detoxification.
  • CAR influences hepatic gluconeogenesis and lipogenesis.
  • Evodia alkaloids rutaecarpine (Rut) and evodiamine (Evo) are potential therapeutic agents.

Purpose of the Study:

  • To investigate the effects of Rut and Evo on gluconeogenesis and lipogenesis via hCAR activation.
  • To explore the therapeutic potential of Rut and Evo for metabolic disorders.

Main Methods:

  • In vitro studies using hyperlipidemic HepG2 cells treated with Rut and Evo.
  • Assessment of hCAR activation and its role using antagonists.
  • Analysis of gene promoter recruitment (FoxO1, HNF4α) for gluconeogenic genes (PEPCK, G6Pase).
  • In vivo studies involving glucose tolerance tests in mice.

Main Results:

  • Rut and Evo demonstrated anti-lipogenic and anti-gluconeogenic effects in HepG2 cells.
  • Both alkaloids potently activated hCAR, with effects reversed by antagonists.
  • CAR-mediated inhibition of FoxO1 and HNF4α recruitment to PEPCK and G6Pase promoters was observed.
  • Rut treatment improved glucose tolerance in mice in a CAR-dependent manner.

Conclusions:

  • Rut and Evo exert anti-metabolic effects through hCAR activation.
  • These alkaloids modulate key transcription factors involved in gluconeogenesis.
  • Evodia alkaloids show promise for managing hyperglycemia and type 2 diabetes.
Keywords:
Constitutive androstane receptorEvodiamineGluconeogenesisLipogenesisRutaecarpine

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