The effect of obesity and repeated exposure on pharmacokinetic response to grape polyphenols in humans

Mol Nutr Food Res. 2017 Nov;61(11):10.1002/mnfr.201700043. doi: 10.1002/mnfr.201700043. Epub 2017 Aug 29.

Abstract

Scope: Evidence suggests that dietary pattern may affect polyphenol absorption and/or metabolism. Further, obesity is associated with lower circulating nutrients, though the reason is unclear. We investigated the pharmacokinetic (PK) response of polyphenols in obese/overweight versus lean individuals before and after repeated dosing of grape polyphenols.

Methods and results: A pilot study was conducted in which PK challenges were administered before and after 10 days of repeated dosing with polyphenols. Volunteers (6 lean, 6 overweight/obese) consumed resveratrol, grape seed extract, and grape juice (2125 mg total polyphenols) daily. On days 1 and 11, blood samples were collected for 6 h after the polyphenol dose and analyzed for deconjugated catechin, epicatechin, resveratrol, and quercetin. Area under the plasma polyphenol mass by time curves (AUCs) were greater for catechin, epicatechin, and quercetin on day 11 versus day 1 for low BMI individuals (p = 0.039) but not high BMI individuals. Further, AUCs were greater for epicatechin and resveratrol for low versus high BMI individuals (p = 0.041), with a similar trend for catechin (p = 0.065), on day 11 but not day 1.

Conclusion: These results suggest that that obesity and repeated exposure may modify polyphenol absorption and/or metabolism in humans.

Trial registration: ClinicalTrials.gov NCT01751750.

Keywords: BMI; Bioavailability; Catechin; Epicatechin; Polyphenol; Quercetin; Resveratrol.

Publication types

  • Comparative Study

MeSH terms

  • Aged
  • Anti-Obesity Agents / administration & dosage*
  • Anti-Obesity Agents / blood
  • Anti-Obesity Agents / metabolism
  • Anti-Obesity Agents / therapeutic use
  • Area Under Curve
  • Body Mass Index
  • Dietary Supplements*
  • Female
  • Fruit / chemistry*
  • Fruit and Vegetable Juices
  • Humans
  • Kinetics
  • Male
  • Middle Aged
  • Obesity / blood
  • Obesity / diet therapy
  • Obesity / metabolism*
  • Overweight / blood
  • Overweight / diet therapy
  • Overweight / metabolism*
  • Pilot Projects
  • Plant Extracts / administration & dosage
  • Plant Extracts / metabolism
  • Plant Extracts / therapeutic use
  • Polyphenols / administration & dosage*
  • Polyphenols / blood
  • Polyphenols / metabolism
  • Polyphenols / therapeutic use
  • Resveratrol
  • Seeds / chemistry
  • Stilbenes / administration & dosage
  • Stilbenes / blood
  • Stilbenes / metabolism
  • Stilbenes / therapeutic use
  • Vitis / chemistry*

Substances

  • Anti-Obesity Agents
  • Plant Extracts
  • Polyphenols
  • Stilbenes
  • Resveratrol

Associated data

  • ClinicalTrials.gov/NCT01751750