title: Sulforaphane Bioavailability from Glucoraphanin-Rich Broccoli: Control by Active Endogenous Myrosinase.
abstract: Glucoraphanin from broccoli and its sprouts and seeds is a water soluble and relatively inert precursor of sulforaphane, the reactive isothiocyanate that potently inhibits neoplastic cellular processes and prevents a number of disease states. Sulforaphane is difficult to deliver in an enriched and stable form for purposes of direct human consumption. We have focused upon evaluating the bioavailability of sulforaphane, either by direct administration of glucoraphanin (a glucosinolate, or β-thioglucoside-N-hydroxysulfate), or by co-administering glucoraphanin and the enzyme myrosinase to catalyze its conversion to sulforaphane at economic, reproducible and sustainable yields. We show that following administration of glucoraphanin in a commercially prepared dietary supplement to a small number of human volunteers, the volunteers had equivalent output of sulforaphane metabolites in their urine to that which they produced when given an equimolar dose of glucoraphanin in a simple boiled and lyophilized extract of broccoli sprouts. Furthermore, when either broccoli sprouts or seeds are administered directly to subjects without prior extraction and consequent inactivation of endogenous myrosinase, regardless of the delivery matrix or dose, the sulforaphane in those preparations is 3- to 4-fold more bioavailable than sulforaphane from glucoraphanin delivered without active plant myrosinase. These data expand upon earlier reports of inter- and intra-individual variability, when glucoraphanin was delivered in either teas, juices, or gelatin capsules, and they confirm that a variety of delivery matrices may be equally suitable for glucoraphanin supplementation (e.g. fruit juices, water, or various types of capsules and tablets).
authors.affiliation: Department of Pharmacology and Molecular Sciences, Johns Hopkins University School of Medicine, Baltimore, Maryland, United States of America; Department of International Health, Johns Hopkins University Bloomberg School of Public Health, Baltimore, Maryland, United States of America.
authors.forename: Jed W
authors.initials: JW
authors.lastname: Fahey
authors.affiliation: Department of Pharmacology and Molecular Sciences, Johns Hopkins University School of Medicine, Baltimore, Maryland, United States of America.
authors.forename: W David
authors.initials: WD
authors.lastname: Holtzclaw
authors.affiliation: Department of Pharmacology and Molecular Sciences, Johns Hopkins University School of Medicine, Baltimore, Maryland, United States of America.
authors.forename: Scott L
authors.initials: SL
authors.lastname: Wehage
authors.affiliation: Department of Pharmacology and Molecular Sciences, Johns Hopkins University School of Medicine, Baltimore, Maryland, United States of America.
authors.forename: Kristina L
authors.initials: KL
authors.lastname: Wade
authors.affiliation: Department of Pharmacology and Molecular Sciences, Johns Hopkins University School of Medicine, Baltimore, Maryland, United States of America.
authors.forename: Katherine K
authors.initials: KK
authors.lastname: Stephenson
authors.affiliation: Department of Pharmacology and Molecular Sciences, Johns Hopkins University School of Medicine, Baltimore, Maryland, United States of America; Department of International Health, Johns Hopkins University Bloomberg School of Public Health, Baltimore, Maryland, United States of America.
authors.forename: Paul
authors.initials: P
authors.lastname: Talalay
mesh_terms: D000328:Adult; D001682:Biological Availability; D001937:Brassica / Q000737:chemistry*; D019587:Dietary Supplements; D016503:Drug Delivery Systems; D005260:Female; D005961:Glucosinolates / Q000008:administration & dosage* / Q000493:pharmacokinetics; D006026:Glycoside Hydrolases / Q000008:administration & dosage* / Q000378:metabolism; D006801:Humans; D007096:Imidoesters / Q000008:administration & dosage* / Q000493:pharmacokinetics; D017879:Isothiocyanates / Q000493:pharmacokinetics / Q000652:urine*; D008297:Male; D008875:Middle Aged; D010091:Oximes; D010936:Plant Extracts / Q000032:analysis / Q000493:pharmacokinetics; D036226:Seedlings / Q000378:metabolism; D012639:Seeds / Q000378:metabolism; D013454:Sulfoxides
chemical_list: D005961:Glucosinolates; D007096:Imidoesters; D017879:Isothiocyanates; D010091:Oximes; D010936:Plant Extracts; D013454:Sulfoxides; D006026:Glycoside Hydrolases; C022739:thioglucosidase; C016766:sulforaphane; C119494:glucoraphanin