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.
Highlights
IntroductionEcdysterone (chemical structure Figure 1a) is a steroid hormone naturally present in plants
Ecdysterone is a steroid hormone naturally present in plants
The analysis of the urine samples has been performed using LC–MS/MS and the mass spectrometer was operated in multiple reaction monitoring (MRM) acquisition mode, using positive ionization (ESI+)
Summary
Ecdysterone (chemical structure Figure 1a) is a steroid hormone naturally present in plants. It is the most widely used active ecdysteroid, and its pharmacological effects have been discussed since the 1980s [1,2]. Studies reported the ability of this natural steroid hormone to stimulate protein synthesis, and change carbohydrate and lipid metabolism [3,4]. In vitro and in silico studies have shown that the anabolic effect of ecdysterone is mediated by activation of estrogen receptor beta (ER beta) [8,24,25,26,27]. Ecdysterone is marketed as able to increase strength and muscle mass and Metabolites 2021, 11, 366.
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