Gentiopicroside isolated from Gentiana scabra Bge. inhibits adipogenesis in 3T3-L1 cells and reduces body weight in diet-induced obese mice

Bioorg Med Chem Lett. 2019 Jul 15;29(14):1699-1704. doi: 10.1016/j.bmcl.2019.05.038. Epub 2019 May 20.

Abstract

Gentiopicroside is a major active component of the Gentiana scabra Bge., which is commonly used as herbal medicine for the treatment of inflammation in Asia. Gentiopicroside significantly down-regulated expression of key adipogenic transcription factors (PPARγ, C/EBPα, SREBP-1c) and dose-dependently inhibited the lipid uptake-related gene (LPL), fatty acid transport-related gene (FABP4) and triglyceride (TG) synthesis-related gene (DGAT2), as well as fatty acid synthesis-related genes (FAS, SCD1), which resulted in reduced intracellular lipid droplet accumulation and TG content in 3T3-L1 cells. Gentiopicroside also down-regulated expression of inflammatory cytokine genes (NFκB1, TNFα, IL6) compared with vehicle. Oral administration of gentiopicroside (50 mg/kg) in mice fed with high-fat diet for 12 weeks resulted in reduced body weight and visceral fat mass compared with the control group. Overall, the results of this study showed that gentiopicroside had positive anti-obesity effects by regulating the expression of adipogenesis/lipogenesis-related genes and inflammatory genes in 3T3-L1, and that it effectively reduced body weight and visceral fat mass in vivo.

Keywords: 3T3-L1; Adipogenesis; Gentiopicroside; High-fat diet; Inflammation; Obesity.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • 3T3-L1 Cells / drug effects*
  • Adipogenesis / drug effects*
  • Animals
  • Anti-Obesity Agents / pharmacology
  • Anti-Obesity Agents / therapeutic use*
  • Body Weight / drug effects*
  • Gentiana / chemistry*
  • Iridoid Glucosides / pharmacology
  • Iridoid Glucosides / therapeutic use*
  • Male
  • Mice
  • Mice, Obese

Substances

  • Anti-Obesity Agents
  • Iridoid Glucosides
  • gentiopicroside