Analytical strategy for the detection of ecdysterone and its metabolites in vivo in uPA(+/+)-SCID mice with humanised liver, human urine samples and estimation of prevalence of its use in anti-doping samples / S. Kraiem, M.Y. Al-Jaber, H. Al-Mohammed, A.S. Al-Menhali, N.J. AlThani, M. Helaleh, W. Samsam, S. Touil, A. Beotra, C. Georgakopoulas, S. Bouabdallah, V. Mohamed-Ali, M. Almaadheed, - (Drug Testing and Analysis (2021) 23 March)
- PMID: 33759363
- DOI: 10.1002/dta.3032
Ecdysteroids are of interest as potential sport performance enhancers, due to their anabolic effects. The current study aimed to analyse levels of the most abundant ecdysteroid, ecdysterone (20-hydroxyecdysone, 20-OHE) in easily available dietary supplements, and, outline an analytical strategy for its detection, and that, of its metabolites, 1) following administration of pure 20-OHE to uPA(+/+)-SCID mice with humanised liver, 2) in a human volunteer after ingestion of two supplements, one with a relatively low, and the other a high, concentration of 20-OHE, and, 3) to estimate the prevalence of use of 20-OHE in elite athletes (n=1000). Of the 16 supplements tested, only five showed detectable levels of 20-OHE, with concentrations ranging from undetectable up to 2.3 mg per capsule. Urine of uPA(+/+)-SCID urine showed the presence of 20-OHE and its metabolite, 14 deoxy ecdysterone, within 24 hours (h) of ingestion. In humans, both the parent and the metabolite were detectable within 2 to 5 h of ingestion, with the metabolite being detectable for longer than the parent. After ingestion of a low dose supplement, the parent and metabolite were detectable for 70 h and 48 h, while following the higher dose it was 96 h and 48 h, respectively. Analysis of urines from athletes (n=1000) confirmed four positives for 20-OHE, suggesting a prevalence of use of 0.4%. Prevalence of its use by elite athletes was relatively low, however, this needs to be confirmed in other populations, and with other related ecdysteroids.