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

Urinary Elimination of Ecdysterone and Its Metabolites Following a Single-Dose Administration in Humans / Gabriella Ambrosio, Tasha Yuliandra, Bernhard Wuest, Monica Mazzarino, Xavier de la Torre, Francesco Botrè, Patrick Diel, Eduard Isenmann, Maria Kristina Parr. - (Metabolites 11 (2021) 6 (9 June); p. 1-15)

  • PMID: 34207569
  • PMCID: PMC8227119
  • DOI: 10.3390/metabo11060366


Abstract

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.

Original document

Parameters

Science
Study
Date
9 June 2021
People
Ambrosio, Gabriella
Botrè, Francesco
de la Torre, Xavier
Diel, Patrick
Isenmann, Eduard
Mazzarino, Monica
Parr, Maria Kristina
Wuest, Bernhard
Yuliandra, Tasha
Country
Germany
Italy
Switzerland
Language
English
Legal Terms
WADA Monitoring List
Other organisations
Deutsche Sporthochschule Köln (DSHS) - German Sport University Cologne
Freie Universität Berlin (FU Berlin) - Free University of Berlin
Université de Lausanne (UNIL) - University of Lausanne
Laboratories
Roma, Italia: Laboratorio Antidoping FMSI
Analytical aspects
Half-life / excretion time of substance
Mass spectrometry analysis
Metabolization
New substance, not on prohibited list
Doping classes
S1. Anabolic Agents
Substances
Ecdysterone
Document category
Scientific article
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Pdf file
Date generated
31 August 2021
Date of last modification
1 September 2021
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  • Legal Source
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  • Statistics
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  • ADRV
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