title: The fungus Cunninghamella elegans can produce human and equine metabolites of selective androgen receptor modulators (SARMs).
abstract: 1. Selective androgen receptor modulators (SARMs) are a group of substances that have potential to be used as doping agents in sports. Being a relatively new group not available on the open market means that no reference materials are commercially available for the main metabolites. In the presented study, the in vitro metabolism of SARMs by the fungus Cunninghamella elegans has been investigated with the purpose of finding out if it can produce relevant human and equine metabolites. 2. Three different SARMs, S1, S4 and S24, were incubated for 5 days with C. elegans. The samples were analysed both with and without sample pretreatment using ultra performance liquid chromatography coupled to high resolution mass spectrometry. 3. All the important phase I and some phase II metabolites from human and horse were formed by the fungus. They were formed through reactions such as hydroxylation, deacetylation, O-dephenylation, nitro-reduction, acetylation and sulfonation. 4. The study showed that the fungus produced relevant metabolites of the SARMs and thus can be used to mimic mammalian metabolism. Furthermore, it has the potential to be used for future production of reference material.
authors.affiliation: Department of Medicinal Chemistry, Division of Analytical Pharmaceutical Chemistry, Uppsala University, Uppsala, Sweden.
authors.forename: Axel
authors.initials: A
authors.lastname: Rydevik
authors.forename: Mario
authors.initials: M
authors.lastname: Thevis
authors.forename: Oliver
authors.initials: O
authors.lastname: Krug
authors.forename: Ulf
authors.initials: U
authors.lastname: Bondesson
authors.forename: Mikael
authors.initials: M
authors.lastname: Hedeland
mesh_terms: D000728:Androgens / Q000378:metabolism*; D000818:Animals; D020093:Cunninghamella / Q000378:metabolism* / Q000502:physiology; D004300:Doping in Sports; D006736:Horses; D006801:Humans; D058573:Performance-Enhancing Substances / Q000378:metabolism*; D011944:Receptors, Androgen / Q000378:metabolism; D015813:Substance Abuse Detection
chemical_list: D000728:Androgens; D058573:Performance-Enhancing Substances; D011944:Receptors, Androgen