Bioavailability challenges associated with development of anti-cancer phenolics

Mini Rev Med Chem. 2010 Jun;10(6):550-67. doi: 10.2174/138955710791384081.

Abstract

Phenolics including many polyphenols and flavonoids have the potentials to become chemoprevention and chemotherapy agents. However, poor bioavailability limits their biological effects in vivo. This paper reviews the factors that affect phenolics absorption and their bioavailabilities from the points of view of their physicochemical properties and disposition in the gastrointestinal tract. The up-to-date research data suggested that solubility and metabolism are the primary reasons that limit phenolic aglycones' bioavailability although stability and poor permeation may also contribute to the poor bioavailabilities of the glycosides. Future investigations should further optimize phenolics' bioavailabilities and realize their chemopreventive and chemotherapeutic effects in vivo.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Anticarcinogenic Agents / chemistry
  • Anticarcinogenic Agents / pharmacokinetics
  • Anticarcinogenic Agents / therapeutic use
  • Antineoplastic Agents / chemistry*
  • Antineoplastic Agents / pharmacokinetics
  • Antineoplastic Agents / therapeutic use
  • Biological Availability
  • Clinical Trials as Topic
  • Flavonoids / chemistry*
  • Flavonoids / pharmacokinetics
  • Flavonoids / therapeutic use
  • Humans
  • Neoplasms / drug therapy
  • Phenols / chemistry*
  • Phenols / pharmacokinetics
  • Phenols / therapeutic use
  • Polyphenols
  • Rats

Substances

  • Anticarcinogenic Agents
  • Antineoplastic Agents
  • Flavonoids
  • Phenols
  • Polyphenols