Preprint Article Version 1 Preserved in Portico This version is not peer-reviewed

Urinary Elimination of Ecdysterone and its Metabolites following a Single-Dose Administration in Humans

Version 1 : Received: 3 May 2021 / Approved: 6 May 2021 / Online: 6 May 2021 (15:20:04 CEST)

A peer-reviewed article of this Preprint also exists.

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. 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.

Journal reference: Metabolites 2021, 11, 366
DOI: 10.3390/metabo11060366

Abstract

Ecdysterone is a phytosteroid widely discussed for its various pharmacological, growth-promoting and anabolic effects mediated by 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 urines 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 urines, detected for more than 2 days with a maximum concentration (Cmax) in the 2.8-8.5 h urines (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. 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.

Subject Areas

ecdysterone; metabolites; excretion profile; urinary pharmacokinetics

Comments (0)

We encourage comments and feedback from a broad range of readers. See criteria for comments and our diversity statement.

Leave a public comment
Send a private comment to the author(s)
Views 0
Downloads 0
Comments 0
Metrics 0


×
Alerts
Notify me about updates to this article or when a peer-reviewed version is published.
We use cookies on our website to ensure you get the best experience.
Read more about our cookies here.