Resveratrol analog 4-[2-(3,5-dimethoxyphenyl)vinyl]pyridine reduces differentiation of the 3T3-L1 adipocyte

Pharm Biol. 2013 Jan;51(1):96-9. doi: 10.3109/13880209.2012.711841. Epub 2012 Oct 5.

Abstract

Context: Resveratrol (3,5,4'-trihydroxystilbene) is a phytoalexin synthesized by plants, most notably grapes, against microbial invasion or ultraviolet stimulation, and is known to exert antioxidant, anticancer, and antiobesity effects.

Objective: This study was conducted to find resveratrol derivatives with higher anti-obesity activity compared to resveratrol and to verify their mechanism of action.

Materials and methods: The inhibitory effect of resveratrol and its derivatives on adipocyte differentiation in 3T3-L1 cells was studied using Oil Red O staining, and the effects on the intracellular expression of fatty acid synthase (FAS) and acetyl-CoA carboxylase (ACC) were measured via Western blot analysis.

Results: A derivative of resveratrol, 4-[2-(3,5-dimethoxyphenyl)vinyl]pyridine (DPVP), exerted inhibitory effects against 3T3-L1 adipocyte differentiation (IC(50) = 13.5 µM) and FAS expression. Notably, it displayed higher activity at concentrations lower than 25 µM compared to resveratrol.

Discussion and conclusion: DPVP is considered to have greater potential as an anti-obesity substance, as it exhibits excellent activity at low concentrations compared to resveratrol.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • 3T3-L1 Cells
  • Acetyl-CoA Carboxylase / genetics
  • Adipocytes / drug effects*
  • Animals
  • Anti-Obesity Agents / administration & dosage
  • Anti-Obesity Agents / pharmacology
  • Blotting, Western
  • Cell Differentiation / drug effects*
  • Dose-Response Relationship, Drug
  • Fatty Acid Synthases / genetics
  • Gene Expression Regulation, Enzymologic / drug effects
  • Inhibitory Concentration 50
  • Mice
  • Pyridines / administration & dosage
  • Pyridines / pharmacology*
  • Resveratrol
  • Stilbenes / administration & dosage
  • Stilbenes / pharmacology*
  • Vinyl Compounds / administration & dosage
  • Vinyl Compounds / pharmacology*

Substances

  • 4-(2-(3,5-dimethoxyphenyl)vinyl)pyridine
  • Anti-Obesity Agents
  • Pyridines
  • Stilbenes
  • Vinyl Compounds
  • Fatty Acid Synthases
  • Acetyl-CoA Carboxylase
  • Resveratrol