Phytoecdysteroids: A Novel, Non-Androgenic Alternative for Muscle Health and Performance

McBride, Jeffrey M.

doi:10.4172/2157-7536.s12-e001

Cited by 6 publications

(3 citation statements)

References 52 publications

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“…It has also been highlighted that ecdysterone is correlated with an increased cell immunity, and that it is also endowed with adaptogenic, anti-diabetic, hepatoprotective, and anti-tumor properties [4,5]. Moreover, growth-promoting and anabolic effects in animals and in humans have been reported [5][6][7][8][9][10][11][12][13][14][15][16][17][18][19][20][21][22][23]. 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].…”

Section: Introductionmentioning

confidence: 99%

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

et al. 2021

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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.

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Section: Introductionmentioning

confidence: 99%

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

et al. 2021

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“…Ecdysterone (chemical structure in Figure 1) is widely marketed as a "natural anabolic agent", advertised to increase strength and muscle mass during resistance training, to reduce fatigue and to ease recovery. Growth promoting and anabolic effects in various animal species including humans have been reported [1][2][3][4][5][6][7][8][9][10][11][12][13][14][15][16][17][18]. Ecdysterone appeared to promote an anabolic effect that was reported to be even stronger than that of the anabolic androgenic steroid (AAS) metandienone [19,20].…”

Section: Introductionmentioning

confidence: 99%

Targeting the administration of ecdysterone in doping control samples

et al. 2019

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The phytosteroid ecdysterone was recently reported to enhance performance in sports and may thus be considered as a substance of relevance in anti-doping control. To trace back an administration of ecdysterone from urine samples analytical properties have been investigated to assess its integration into initial testing procedures (ITP) in doping control laboratories. MethodsAnalytical properties of ecdysterone were evaluated using GC-QTOF-MS and LC-QTOF-MS.Its metabolism and elimination in human were studied using urines collected after administration. ResultsThe detectability of ecdysterone by GC-MS (after derivatization) and/or LC-MS(/MS) has been demonstrated and sample preparation methods were evaluated. Dilute-and-inject for LC-MS(/MS) or SPE using Oasis HLB for GC-MS or LC-MS were found most suitable, while liquidliquid extraction was hampered by the high polarity of ecdysteroids.Most abundantly, ecdysterone was detected in the post administration urines as parent compound besides the metabolite desoxy-ecdysterone. Additionally desoxy-poststerone was tentatively assigned as minor metabolite, however further investigations are needed. ConclusionAn administration of ecdysterone can be targeted using existing procedures of anti-doping laboratories. Ecdysterone and desoxy-ecdysterone appeared as suitable candidates for integration in ITP. Using dilute-and-inject a detection of the parent compound was possible for more than two days after the administration of a single dose of ~50 mg.

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“…Unfortunately, the decline can become a vicious circle, since declining muscle strength results in ever less inclination to remain active, with many only recognizing the problem once it has become established, and it is perhaps too late to pursue a more active lifestyle. Biochemically, the rate of skeletal muscle protein synthesis declines with aging, owing largely to decreased activation of the PI3K/Akt/mTORC1 signalling pathway (Zwetsloot et al 2014). Hence, the potential attractiveness of mild anabolic agents, such as the ecdysteroids, which activate this signalling pathway through a G-proteincoupled receptor, and, unlike the androgenic anabolic steroids, and does not require a concomitant exercise regime for effect and does not produce unpleasant physical and psychological side effects.…”

Section: Agingmentioning

confidence: 99%