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

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.

Biomarker Exploration in Human Peripheral Blood Mononuclear Cells for Monitoring Sulforaphane Treatment Responses in Autism Spectrum Disorder

“…Conversion of GR to SF (bioavailability) was calculated as percent of dose excreted in collected urine samples, and was normalized on a molar equivalence basis (moles of GR to moles of SF plus its metabolites as determined in the cyclocondensation reaction). Conversion efficiencies varied among subjects from 8.2% to 68.4% of the administered dose, which is consistent with the data we and others have previously reported on bioavailability in adults 11,68,69 . Post-dose plasma DTC levels were closely related to the time between last dose and blood draw, with lower levels at less than 2 h or more than 14 h, and higher levels between 9-10 h after the last dose (Table 1).…”

BMI Is Associated With Increased Plasma and Urine Appearance of Glucosinolate Metabolites After Consumption of Cooked Broccoli

“…To the best of our knowledge, it has not been established whether gut content of myrosinase-expressing bacteria varies with BMI. When active myrosinase is included in glucosinolate-rich meals as in our earlier study (25) and in that of Fahey et al (41), ITCs and ITC metabolites are rapidly produced and then absorbed in the upper digestive tract. Neither study reported a main effect of BMI.…”

Bioactive Compounds and Bioactivities of Brassica oleracea L. var. Italica Sprouts and Microgreens: An Updated Overview from a Nutraceutical Perspective

“…In broccoli sprouts, two of the most abundant GLSs are glucoraphanin and glucoerucin, and myrosinase hydrolysis of these GLSs form SFN and ERN, respectively. SFN, distinguished ITCs in broccoli sprouts, is one of the most potent naturally occurring inducers of phase 2 detoxification enzymes, boost antioxidant status, and protect animals against chemically induced cancer [40,90]. Its modes of action are involved with the repressor protein Kelch-like ECH associated protein 1 (Keap1), nuclear factor erythroid 2 p45-related factor 2 (Nrf2), and genes, which contain an antioxidant responsive element (ARE) [62].…”