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Article

Urinary Elimination of Ecdysterone and Its Metabolites Following a Single-Dose Administration in Humans

1
Institute of Pharmacy, Pharmaceutical and Medicinal Chemistry (Pharmaceutical Analysis), Freie Universitaet Berlin, 14195 Berlin, Germany
2
Agilent Technologies, 76337 Waldbronn, Germany
3
Laboratorio Antidoping FMSI, 00197 Rome, Italy
4
REDs—Research and Expertise in Anti-Doping Sciences, ISSUL—Institute of Sport Sciences, University of Lausanne, 1015 Lausanne, Switzerland
5
Department for Molecular and Cellular Sports Medicine, Institute for Cardiovascular Research and Sports Medicine, German Sport University Cologne, 50933 Cologne, Germany
*
Author to whom correspondence should be addressed.
Academic Editor: Anthony Tsarbopoulos
Metabolites 2021, 11(6), 366; https://doi.org/10.3390/metabo11060366
Received: 30 April 2021 / Revised: 3 June 2021 / Accepted: 6 June 2021 / Published: 9 June 2021
(This article belongs to the Special Issue Analysis and Metabolism of Bioactive Compounds)
Ecdysterone is a phytosteroid widely discussed for its various pharmacological, growth-promoting, and anabolic effects, mediated by the activation of estrogen receptor beta (ERbeta). Performance-enhancement in sports was demonstrated recently, and ecdysterone was consequently included in the Monitoring Program, to detect potential patterns of misuse in sport. Only few studies on the pharmacokinetics of ecdysterone in humans have been reported so far. In this study, post-administration urine samples in twelve volunteers (single dose of 50 mg of ecdysterone) were analyzed using dilute-and-inject liquid-chromatography–tandem mass spectrometry. Identification and quantitation of ecdysterone and of two metabolites, 14-deoxy-ecdysterone and 14-deoxy-poststerone, was achieved. Ecdysterone was the most abundant analyte present in post-administration urine samples, detected for more than 2 days, with a maximum concentration (Cmax) in the 2.8–8.5 h urine (Cmax = 4.4–30.0 µg/mL). The metabolites 14-deoxy-ecdysterone and 14-deoxy-poststerone were detected later, reaching the maximum concentrations at 8.5–39.5 h (Cmax = 0.1–6.0 µg/mL) and 23.3–41.3 h (Cmax = 0.1–1.5 µg/mL), respectively. Sex-specific differences were not observed. Cumulative urinary excretion yielded average values of 18%, 2.3%, and 1.5% for ecdysterone, 14-deoxy-ecdysterone, and 14-deoxy-poststerone, respectively. Ecdysterone and 14-deoxy-ecdysterone were excreted following first-order kinetics with half-lives calculated with three hours, while pharmacokinetics of 14-deoxy-poststerone needs further evaluation. View Full-Text
Keywords: ecdysterone; metabolites; excretion profile; urinary pharmacokinetics ecdysterone; metabolites; excretion profile; urinary pharmacokinetics
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MDPI and ACS Style

Ambrosio, G.; Yuliandra, T.; Wuest, B.; Mazzarino, M.; de la Torre, X.; Botrè, F.; Diel, P.; Isenmann, E.; Parr, M.K. Urinary Elimination of Ecdysterone and Its Metabolites Following a Single-Dose Administration in Humans. Metabolites 2021, 11, 366. https://doi.org/10.3390/metabo11060366

AMA Style

Ambrosio G, Yuliandra T, Wuest B, Mazzarino M, de la Torre X, Botrè F, Diel P, Isenmann E, Parr MK. Urinary Elimination of Ecdysterone and Its Metabolites Following a Single-Dose Administration in Humans. Metabolites. 2021; 11(6):366. https://doi.org/10.3390/metabo11060366

Chicago/Turabian Style

Ambrosio, Gabriella, Tasha Yuliandra, Bernhard Wuest, Monica Mazzarino, Xavier de la Torre, Francesco Botrè, Patrick Diel, Eduard Isenmann, and Maria K. Parr 2021. "Urinary Elimination of Ecdysterone and Its Metabolites Following a Single-Dose Administration in Humans" Metabolites 11, no. 6: 366. https://doi.org/10.3390/metabo11060366

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