Stilbene analogs as inducers of apolipoprotein-I transcription

Eur J Med Chem. 2010 May;45(5):2018-23. doi: 10.1016/j.ejmech.2009.12.076. Epub 2010 Jan 14.

Abstract

Based on the naturally occurring stilbene, Resveratrol, a series of novel stilbene derivatives were synthesized, which have the ability to induce the expression of the ApoA-I gene. Several compounds equally or more potent than Resveratrol were identified. trans-4,4'-dihydroxy-2-methoxystilbene was the most potent (4.6x more potent than Resveratrol). These compounds provide an early lead into new drugs to treat atherosclerosis.

MeSH terms

  • Apolipoprotein A-I / genetics*
  • Caco-2 Cells
  • Humans
  • Molecular Structure
  • Promoter Regions, Genetic / drug effects
  • Promoter Regions, Genetic / genetics
  • Stereoisomerism
  • Stilbenes / chemical synthesis
  • Stilbenes / chemistry*
  • Stilbenes / pharmacology*
  • Structure-Activity Relationship
  • Transcription, Genetic / drug effects*
  • Transcription, Genetic / genetics
  • Up-Regulation / drug effects*
  • Up-Regulation / genetics

Substances

  • Apolipoprotein A-I
  • Stilbenes