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Resveratrol from red grapes - pedestrian polyphenol or useful anticancer agent?

Andreas J Gescher1

  • 1Cancer Biomarkers and Prevention Group, Department of Cancer Studies and Molecular Medicine, University of Leicester, Leicester, U.K. ag15@le.ac.uk

Planta Medica
|May 1, 2008
PubMed

Insights

Resveratrol, a natural compound, shows promise in preventing cancer by affecting cell cycles and reducing inflammation. Its effectiveness may be enhanced by developing new resveratrol derivatives with improved properties.

Area of Science:

  • Phytochemistry
  • Cancer Chemoprevention
  • Pharmacology

Background:

  • Resveratrol is a phytoalexin found in plants, known for its potential cancer chemopreventive properties.
  • Its proposed mechanisms include inhibiting enzymes, angiogenesis, and modulating cellular processes like cell cycle and apoptosis.
  • Resveratrol's low bioavailability and the prevalence of its conjugates in circulation are key pharmacokinetic considerations.

Purpose of the Study:

  • To explore the cancer chemopreventive properties of resveratrol.
  • To investigate the mechanisms underlying resveratrol's efficacy.
  • To examine the potential of resveratrol analogues for improved pharmacological activity.

Main Methods:

  • Preclinical models of carcinogenesis were utilized.
  • Mechanisms of action including enzyme inhibition, angiogenesis, drug metabolism, antioxidation, cell cycle, and apoptosis were studied.
  • Pharmacokinetic studies in rodents and humans were conducted.
  • Development and evaluation of resveratrol analogues with modified aryl substituents were performed.

Main Results:

  • Resveratrol demonstrated cancer chemopreventive properties in preclinical models.
  • Key mechanisms involve inhibition of cyclooxygenase, angiogenesis, and modulation of drug-metabolizing enzymes, alongside antioxidant effects and alterations in cell cycle and apoptosis.
  • Pharmacokinetic data indicate low bioavailability of resveratrol, with conjugates being the primary circulating forms.
  • Novel stilbene derivatives with modified substituents showed enhanced pharmacological properties compared to resveratrol.

Conclusions:

  • Resveratrol exhibits significant potential as a cancer chemopreventive agent through multiple biological pathways.
  • The low bioavailability of resveratrol necessitates further research into its metabolites and the development of more effective analogues.
  • Optimized resveratrol derivatives hold promise for enhanced therapeutic applications in cancer chemoprevention.

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