Quantitative analysis of absorption, metabolism, and excretion of benzoxazinoids in humans after the consumption of high- and low-benzoxazinoid diets with similar contents of cereal dietary fibres: a crossover study

Eur J Nutr. 2017 Feb;56(1):387-397. doi: 10.1007/s00394-015-1088-6. Epub 2015 Oct 30.

Abstract

Purpose: Benzoxazinoids (BXs) are a group of wholegrain phytochemicals with potential pharmacological properties; however, limited information exists on their absorption, metabolism, and excretion in humans. The aim of this study was to investigate the dose-dependent uptake and excretion of dietary BXs in a healthy population.

Methods: Blood and urine were collected from 19 healthy participants from a crossover study after a washout, a LOW BX diet or HIGH BX diet, and analysed for 12 BXs and 4 phenoxazinone derivatives.

Results: We found that the plasma BX level peaked approximately 3 h after food intake, whereas BXs in urine were present even at 36 h after consuming a meal. No phenoxazinone derivatives could be detected in either plasma or urine. The dominant BX metabolite in both plasma and urine was 2-β-D-glucopyranosyloxy-1,4-benzoxazin-3-one (HBOA-Glc), even though 2-β-D-glucopyranosyloxy-4-hydroxy-1,4-benzoxazin-3-one (DIBOA-Glc) was the major component in the diet.

Conclusion: The dietary BX treatment correlated well with the plasma and urine levels, illustrating strong dose-dependent BX absorption, which also had a rapid washout, especially from the plasma compartment.

Keywords: Benzoxazinoids; Metabolism; Rye bread; Weight loss; Wholegrain.

MeSH terms

  • Adolescent
  • Adult
  • Aged
  • Benzoxazines / blood
  • Benzoxazines / pharmacokinetics*
  • Benzoxazines / urine
  • Body Mass Index
  • Cross-Over Studies
  • Diet*
  • Dietary Fiber / administration & dosage*
  • Edible Grain / chemistry
  • Evaluation Studies as Topic
  • Female
  • Humans
  • Male
  • Middle Aged
  • Phytochemicals / blood
  • Phytochemicals / pharmacokinetics
  • Phytochemicals / urine
  • Young Adult

Substances

  • (2R)-2-O-beta-D-glucopyranosyl-2H-1,4-benzoxazin-3(4H)-one
  • (2R)-2-O-beta-D-glucopyranosyl-4-hydroxy-2H-1,4-benzoxazin-3(4H)-one
  • Benzoxazines
  • Dietary Fiber
  • Phytochemicals