Bioavailability of Sulforaphane from two broccoli sprout beverages: results of a short-term, cross-over clinical trial in Qidong, China

One of several challenges in design of clinical chemoprevention trials is the selection of the dose, formulation, and dose schedule of the intervention agent. Therefore, a cross-over clinical trial was undertaken to compare the bioavailability and tolerability of sulforaphane from two of broccoli sp...

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Published in:Cancer prevention research (Philadelphia, Pa.) Pa.), 2011-03, Vol.4 (3), p.384-395
Main Authors: Egner, Patricia A, Chen, Jian Guo, Wang, Jin Bing, Wu, Yan, Sun, Yan, Lu, Jian Hua, Zhu, Jian, Zhang, Yong Hui, Chen, Yong Sheng, Friesen, Marlin D, Jacobson, Lisa P, Muñoz, Alvaro, Ng, Derek, Qian, Geng Sun, Zhu, Yuan Rong, Chen, Tao Yang, Botting, Nigel P, Zhang, Qingzhi, Fahey, Jed W, Talalay, Paul, Groopman, John D, Kensler, Thomas W
Format: Article
Language:English
Subjects:
Adult
Aged
Anticarcinogenic Agents - pharmacokinetics
Anticarcinogenic Agents - urine
Beverages
Biological Availability
Brassica
China
Cross-Over Studies
Female
Genotype
Glucosinolates - metabolism
Glycoside Hydrolases - chemistry
Humans
Imidoesters - metabolism
Isothiocyanates
Male
Middle Aged
Oximes
Raphanus - metabolism
Reproducibility of Results
Signal Transduction
Sulfhydryl Compounds - chemistry
Sulfoxides
Thiocyanates - pharmacokinetics
Thiocyanates - urine
Treatment Outcome
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Summary:One of several challenges in design of clinical chemoprevention trials is the selection of the dose, formulation, and dose schedule of the intervention agent. Therefore, a cross-over clinical trial was undertaken to compare the bioavailability and tolerability of sulforaphane from two of broccoli sprout-derived beverages: one glucoraphanin-rich (GRR) and the other sulforaphane-rich (SFR). Sulforaphane was generated from glucoraphanin contained in GRR by gut microflora or formed by treatment of GRR with myrosinase from daikon (Raphanus sativus) sprouts to provide SFR. Fifty healthy, eligible participants were requested to refrain from crucifer consumption and randomized into two treatment arms. The study design was as follows: 5-day run-in period, 7-day administration of beverages, 5-day washout period, and 7-day administration of the opposite intervention. Isotope dilution mass spectrometry was used to measure levels of glucoraphanin, sulforaphane, and sulforaphane thiol conjugates in urine samples collected daily throughout the study. Bioavailability, as measured by urinary excretion of sulforaphane and its metabolites (in approximately 12-hour collections after dosing), was substantially greater with the SFR (mean = 70%) than with GRR (mean = 5%) beverages. Interindividual variability in excretion was considerably lower with SFR than with GRR beverage. Elimination rates were considerably slower with GRR, allowing for achievement of steady-state dosing as opposed to bolus dosing with SFR. Optimal dosing formulations in future studies should consider blends of sulforaphane and glucoraphanin as SFR and GRR mixtures to achieve peak concentrations for activation of some targets and prolonged inhibition of others implicated in the protective actions of sulforaphane. Cancer Prev Res; 4(3); 384-95. ©2011 AACR.
ISSN:1940-6207
1940-6215
DOI:10.1158/1940-6207.capr-10-0296