Exploration of Underlying Mechanism of Anti-adipogenic Activity of Sulfuretin

Biol Pharm Bull. 2017 Sep 1;40(9):1366-1373. doi: 10.1248/bpb.b17-00049. Epub 2017 Jun 3.

Abstract

Sulfuretin is a natural flavonoid found in the plant Rhus verniciflua STOKES. The plant has been traditionally used as medicinal agent for antiviral, cathartic, diaphoretic, anti-rheumatic and sedative activities in East Asia. In this study we isolated and identified sulfuretin from R. verniciflua and investigated its anti-adipogenic activity against 3T3-L1 preadipocytes cells. We evaluated the effects of sulfuretin on the adipogenic transcription factors like peroxisome proliferator-activated receptor γ (PPARγ), CCAAT/enhancer-binding protein α (C/EBPα), fatty acid synthase (FAS), Fabp4, adiponectin and zinc fingerprint protein (Zfp) 521 by gene expression (real-time QPCR) and Western blot analysis. Sulfuretin treatment at Day 0 and 2 showed significant reduction of lipid production in 3T3-L1 cells in concentration dependent manner. Gene expression analysis (real-time PCR) revealed that sulfuretin inhibited the both major adipogenic factors (C/EBPα, C/EBPβ and PPARγ) and minor adipogenic factors (sterol regulatory element-binding protein (SREBP1c), adiponectin, FAS, Fabp4, Zfp423, and Ebf1). Western blot analysis showed the increased expression of β-catenin and suppression of PPARγ after sulfuretin treatment. Overall, sulfuretin is a natural flavonoid having potent anti-adipogenic activity through the suppression of major adipogenic factors C/EBPα, C/EBPβ and PPARγ, which initiate adipogenesis.

Keywords: adipogenic transcription factor; anti-adipogenesis; oil-red-O; sulfuretin.

MeSH terms

  • 3T3-L1 Cells
  • Adipocytes / metabolism
  • Adipogenesis / drug effects*
  • Adipose Tissue / cytology
  • Adipose Tissue / metabolism*
  • Animals
  • Anti-Obesity Agents / pharmacology
  • Anti-Obesity Agents / therapeutic use
  • Benzofurans / pharmacology*
  • Benzofurans / therapeutic use
  • CCAAT-Enhancer-Binding Proteins / metabolism
  • DNA-Binding Proteins / metabolism
  • Flavonoids / pharmacology
  • Flavonoids / therapeutic use
  • Gene Expression / drug effects
  • Mice
  • Obesity / metabolism*
  • Obesity / prevention & control
  • PPAR gamma / metabolism
  • Phytotherapy
  • Plant Extracts / pharmacology*
  • Plant Extracts / therapeutic use
  • Rhus / chemistry*
  • Sterol Regulatory Element Binding Protein 1 / metabolism
  • Transcription Factors / metabolism
  • beta Catenin / metabolism

Substances

  • Anti-Obesity Agents
  • Benzofurans
  • CCAAT-Enhancer-Binding Proteins
  • CTNNB1 protein, mouse
  • DNA-Binding Proteins
  • Ebfaz protein, mouse
  • Flavonoids
  • PPAR gamma
  • Plant Extracts
  • Srebf1 protein, mouse
  • Sterol Regulatory Element Binding Protein 1
  • Transcription Factors
  • beta Catenin
  • sulfuretin