Pharmacokinetics and tissue distribution of 14C-Labeled grape polyphenols in the periphery and the central nervous system following oral administration

Elsa M. Janle, Mary Ann Lila, Michael Grannan, Lauren Wood, Aine Higgins, Gad G. Yousef, Randy B. Rogers, Helen Kim, George S. Jackson, Lap Ho, Connie M. Weaver

Research output: Contribution to journalArticlepeer-review

73 Scopus citations


Grape polyphenols confer potential health benefits, including prevention of neurodegenerative diseases. To determine the absorption and tissue distribution of the complex grape polyphenol mixture, 14C-labeled polyphenols were biosynthesized by grape cell suspension cultures, during co-incubation with radioisotopically labeled sucrose, and fractionated into polyphenolic subfractions. The pharmacokinetics and distribution of grape polyphenols into blood, brain, and peripheral interstitial fluid were determined by tracking the 14C label. The blood peak 14C concentration of the fractions ranged from 15 minutes to 4 hours. Absorption and tissue distribution varied greatly between fractions. Concentrations in interstitial fluid were lower than in blood. The amount of residual label in the brain at 24 hours ranged from 0.1% to 1.7% of the dose, depending on the fraction. 14C label found in the brain tissue and brain microdialysate indicated that grape polyphenols or their metabolites are able to cross the blood-brain barrier. Using 14C-labeled plant polyphenols it is possible to track the compounds or their metabolic products into any tissue and determine distribution patterns in spite of low concentrations. A central question regarding the potential role of dietary polyphenolics in neurodegenerative research is whether they are bioavailable in the brain. Our observations indicate that some grape-derived polyphenolics do reach the brain, which suggests their potential value for applications in neurodegenerative disorders.

Original languageEnglish
Pages (from-to)926-933
Number of pages8
JournalJournal of Medicinal Food
Issue number4
StatePublished - 1 Aug 2010


  • blood-brain barrier
  • brain kinetics
  • grape
  • grape cell culture
  • interstitial fluid kinetics
  • neurodegenerative diseases
  • pharmacokinetics
  • polyphenols
  • tissue distribution


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