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Enhancement of anticancer potential of polyphenols by covalent modifications

Urszula Lewandowska1, Jakub Fichna1, Sylwia Gorlach1

  • 1Department of Biochemistry, Medical University of Lodz, Lodz, Poland.

Biochemical Pharmacology
|January 19, 2016
PubMed

Insights

Chemoprevention using modified natural polyphenols shows promise for cancer prevention and therapy. Covalent modifications enhance their anticancer effects, warranting clinical trials.

Area of Science:

  • Biochemistry
  • Pharmacology
  • Oncology

Background:

  • Chemoprevention is a valued approach to cancer prevention using natural or synthetic compounds.
  • Natural polyphenols exhibit anticancer properties and could be used in cancer prevention and therapy.
  • Covalent modifications of polyphenols can enhance their anticancer potential.

Purpose of the Study:

  • To review covalent modifications of polyphenols for increasing their anticancer activity.
  • To discuss how modifications like hydroxylation, methylation, acylation, and galloylation impact polyphenol efficacy.
  • To explore the potential of modified polyphenols in cancer prevention and therapy.

Main Methods:

  • Review of scientific literature on polyphenol modifications and their anticancer effects.
  • Analysis of in vitro studies on cytotoxic, antiproliferative, and proapoptotic activities.
  • Examination of in vivo studies on tumor growth and metastasis suppression.

Main Results:

  • Covalent modifications (hydroxylation, methylation, acylation, galloylation) enhance polyphenol activities.
  • Modified polyphenols show increased cytotoxic, pro-oxidant, antiproliferative, proapoptotic, proautophagic, and antimigratory effects in vitro.
  • Some derivatives exhibit stronger tumor suppression and metastasis inhibition in animal models than parent compounds.
  • Modifications can improve absorption and tissue distribution of phenolic compounds in vivo.

Conclusions:

  • Covalent modification is a viable strategy to enhance the anticancer potential of polyphenols.
  • Modified polyphenols demonstrate significant promise for both cancer prevention and therapy.
  • Further clinical trials with polyphenol derivatives are warranted based on preclinical evidence.
Keywords:
Anticancer drugCarcinogenesisChemopreventionDerivativePolyphenol

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