title: The use of tandem yeast and mammalian cell in vitro androgen bioassays to detect androgens in internet-sourced sport supplements.
abstract: Sport supplements containing steroids never approved for therapeutic use have the potential for abuse by athletes. Most are marketed online and may contain undisclosed steroids yet are readily available despite lacking toxicological or pharmacological evaluation. In this study, 18 supplements purchased online underwent organic solvent extraction to isolate any steroids they contained. From the 18 supplements, 19 steroids were identified and for each, its intrinsic androgenic potency was determined by a yeast cell (Saccharomyces cerevisiae) androgen bioassay and its potential androgenic potency was determined by a liver (HuH7) cell androgen bioassay. The yeast bioassay showed that of the 19 steroids tested, 6 demonstrated strong intrinsic bioactivity, with 4 metabolically activated to even stronger androgens. Moreover, 4 steroids with moderate and 1 with intrinsically weak androgenic bioactivity were activated to more potent androgens. Finally, 8 steroids were metabolically inactivated or deactivated into weaker androgens. Our results show that Internet-sourced sport supplements may contain intrinsically strong androgens, or precursors that can be metabolized to them. These potentially potent pharmacologically active steroids are being used without regulatory control or consumer awareness of their potential adverse effects. Copyright © 2016 John Wiley & Sons, Ltd.
authors.affiliation: School of Life Sciences, Faculty of Science, University of Technology, Broadway, NSW, Australia.
authors.forename: Elliot R
authors.initials: ER
authors.lastname: Cooper
authors.affiliation: School of Life Sciences, Faculty of Science, University of Technology, Broadway, NSW, Australia.
authors.forename: Kristine C Y
authors.initials: KC
authors.lastname: McGrath
authors.affiliation: School of Life Sciences, Faculty of Science, University of Technology, Broadway, NSW, Australia.|Department of Endocrinology, Dezhou People's Hospital, China.
authors.forename: Xiaohong
authors.initials: X
authors.lastname: Li
authors.affiliation: ANZAC Research Institute, University of Sydney, Concord Hospital, NSW, Australia.
authors.forename: Omar
authors.initials: O
authors.lastname: Akram
authors.affiliation: School of Life Sciences, Faculty of Science, University of Technology, Broadway, NSW, Australia.
authors.forename: Robert
authors.initials: R
authors.lastname: Kasz
authors.affiliation: National Measurement Institute, North Ryde, NSW, Australia.
authors.forename: Rymantas
authors.initials: R
authors.lastname: Kazlauskas
authors.affiliation: Research School of Chemistry, Australian National University, Canberra, ACT, Australia.
authors.forename: Malcolm D
authors.initials: MD
authors.lastname: McLeod
authors.affiliation: ANZAC Research Institute, University of Sydney, Concord Hospital, NSW, Australia.
authors.forename: David J
authors.initials: DJ
authors.lastname: Handelsman
authors.affiliation: Department of Physiology, Otago School of Medical Sciences., University of Otago, Dunedin, New Zealand.
authors.forename: Alison K
authors.initials: AK
authors.lastname: Heather
mesh_terms: D000728:Androgens / Q000032:analysis* / Q000494:pharmacology*; D000818:Animals; D002460:Cell Line; D019587:Dietary Supplements / Q000032:analysis*; D004300:Doping in Sports; D004353:Drug Evaluation, Preclinical / Q000379:methods; D006801:Humans; D020407:Internet; D008099:Liver / Q000166:cytology / Q000187:drug effects / Q000378:metabolism; D051379:Mice; D032446:Myoblasts / Q000166:cytology / Q000187:drug effects / Q000378:metabolism; D012441:Saccharomyces cerevisiae / Q000187:drug effects / Q000378:metabolism; D013256:Steroids / Q000032:analysis / Q000494:pharmacology
chemical_list: D000728:Androgens; D013256:Steroids
keywords: androgen; bioassays; sport supplements; sports doping