Bioavailability of Sulforaphane Following Ingestion of Glucoraphanin-Rich Broccoli Sprout and Seed Extracts with Active Myrosinase: A Pilot Study of the Effects of Proton Pump Inhibitor Administration

Nutrients. 2019 Jun 29;11(7):1489. doi: 10.3390/nu11071489.

Abstract

We examined whether gastric acidity would affect the activity of myrosinase, co-delivered with glucoraphanin (GR), to convert GR to sulforaphane (SF). A broccoli seed and sprout extract (BSE) rich in GR and active myrosinase was delivered before and after participants began taking the anti-acid omeprazole, a potent proton pump inhibitor. Gastric acidity appears to attenuate GR bioavailability, as evidenced by more SF and its metabolites being excreted after participants started taking omeprazole. Enteric coating enhanced conversion of GR to SF, perhaps by sparing myrosinase from the acidity of the stomach. There were negligible effects of age, sex, ethnicity, BMI, vegetable consumption, and bowel movement frequency and quality. Greater body mass correlated with reduced conversion efficiency. Changes in the expression of 20 genes in peripheral blood mononuclear cells were evaluated as possible pharmacodynamic indicators. When grouped by their primary functions based on a priori knowledge, expression of genes associated with inflammation decreased non-significantly, and those genes associated with cytoprotection, detoxification and antioxidant functions increased significantly with bioavailability. Using principal components analysis, component loadings of the changes in gene expression confirmed these groupings in a sensitivity analysis.

Keywords: chemoprevention; crucifer; nutritional supplement; pharmacodynamics; pharmacokinetics.

Publication types

  • Clinical Trial

MeSH terms

  • Adult
  • Aged
  • Biological Availability
  • Brassica* / chemistry
  • Dietary Supplements* / adverse effects
  • Drug Interactions
  • Female
  • Gastric Acid / metabolism
  • Gene Expression Regulation / drug effects
  • Glucosinolates / administration & dosage*
  • Glucosinolates / adverse effects
  • Glucosinolates / isolation & purification
  • Glucosinolates / metabolism
  • Glycoside Hydrolases / administration & dosage*
  • Glycoside Hydrolases / adverse effects
  • Glycoside Hydrolases / metabolism
  • Humans
  • Hydrogen-Ion Concentration
  • Imidoesters / administration & dosage*
  • Imidoesters / adverse effects
  • Imidoesters / isolation & purification
  • Imidoesters / metabolism
  • Isothiocyanates / metabolism*
  • Leukocytes, Mononuclear / drug effects
  • Leukocytes, Mononuclear / metabolism
  • Male
  • Middle Aged
  • Omeprazole / administration & dosage*
  • Omeprazole / adverse effects
  • Oximes
  • Pilot Projects
  • Plant Extracts / administration & dosage*
  • Plant Extracts / adverse effects
  • Plant Extracts / isolation & purification
  • Plant Extracts / metabolism
  • Proton Pump Inhibitors / administration & dosage*
  • Proton Pump Inhibitors / adverse effects
  • Seedlings* / chemistry
  • Seeds* / chemistry
  • Sulfoxides
  • Young Adult

Substances

  • Glucosinolates
  • Imidoesters
  • Isothiocyanates
  • Oximes
  • Plant Extracts
  • Proton Pump Inhibitors
  • Sulfoxides
  • Glycoside Hydrolases
  • thioglucosidase
  • sulforaphane
  • Omeprazole
  • glucoraphanin