In vitro and in vivo antioxidant properties of chlorogenic acid and caffeic acid

Int J Pharm. 2011 Jan 17;403(1-2):136-8. doi: 10.1016/j.ijpharm.2010.09.035. Epub 2010 Oct 7.


Dietary polyphenols are thought to be beneficial for human health as antioxidants. Coffee beans contain a common polyphenol, chlorogenic acid. Chlorogenic acid is the ester of caffeic acid and quinic acid. Although these polyphenols have received much attention, there is little evidence indicating a relationship between the effect and the rate of absorption. In this study, we focused on the beneficial effects of chlorogenic acid and caffeic acid, a major metabolite of chlorogenic acid. We carried out in vitro and in vivo experiments. In the in vitro study, caffeic acid had stronger antioxidant activity than that of chlorogenic acid. The uptake of chlorogenic acid by Caco-2 cells was much less than that of caffeic acid. The physiological importance of an orally administered compound depends on its availability for intestinal absorption and subsequent interaction with target tissues. We then used an intestinal ischemia-reperfusion model to evaluate antioxidant activities in vivo. We found that both chlorogenic acid and caffeic acid had effects on intestinal ischemia-reperfusion injury. Since caffeic acid has a stronger antioxidant activity than that of chlorogenic acid and chlorogenic acid is hydrolyzed into caffeic acid in the intestine, it is possible that caffeic acid plays a major role in the protective effect of chlorogenic acid against ischemia-reperfusion injury.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antioxidants / chemistry
  • Antioxidants / pharmacokinetics
  • Antioxidants / pharmacology*
  • Antioxidants / therapeutic use
  • Caco-2 Cells
  • Caffeic Acids / chemistry
  • Caffeic Acids / pharmacokinetics
  • Caffeic Acids / pharmacology*
  • Caffeic Acids / therapeutic use
  • Capillary Permeability
  • Chlorogenic Acid / chemistry
  • Chlorogenic Acid / pharmacokinetics
  • Chlorogenic Acid / pharmacology*
  • Chlorogenic Acid / therapeutic use
  • Humans
  • Intestinal Absorption
  • Intestine, Small / blood supply
  • Intestine, Small / drug effects
  • Intestine, Small / metabolism*
  • Male
  • Oxidation-Reduction
  • Rats
  • Rats, Wistar
  • Reperfusion Injury / metabolism
  • Reperfusion Injury / prevention & control*
  • Superoxides / analysis


  • Antioxidants
  • Caffeic Acids
  • Superoxides
  • Chlorogenic Acid
  • caffeic acid