Recent studies suggest that the anabolic effect of ecdysterone, a naturally occurring steroid hormone claimed to enhance physical performance, is mediated by estrogen receptor (ER) binding. In comparison with the prohibited anabolic agents (e.g., metandienone and others), ecdysterone revealed to be even more effective in a recent study performed in rats. However, scientific studies in humans are very rarely accessible. Thus, our project aimed at investigating the effects of ecdysteronecontaining products on human sport exercise. A 10-week intervention study of strength training of young men (n = 46) was carried out. Different doses of ecdysterone-containing supplements have been administered during the study to evaluate the performance-enhancing effect. Analysis of blood and urine samples for ecdysterone and potential biomarkers of performance enhancement has been conducted. To ensure the specificity of the effects measured, a comprehensive screening for prohibited performance-enhancing substances was also carried out. Furthermore, the administered supplement has been tested for the absence of anabolic steroid contaminations prior to administration. Significantly higher increases in muscle mass were observed in those participants that were dosed with ecdysterone. The same hypertrophic effects were also detected in vitro in C2C12 myotubes. Even more relevant with respect to sports performance, significantly more pronounced increases in one-repetition bench press performance were observed. No increase in biomarkers for liver or kidney toxicity was noticed. These data underline the effectivity of an ecdysterone supplementation with respect to sports performance. Our results strongly suggest the inclusion of ecdysterone in the list of prohibited substances and methods in sports in class S1.2 "other anabolic agents".
The number of people suffering from being overweight or obese has risen steadily in recent years. Consequently, new forms of nutrition and diets were developed as potential solutions. In the last years, the time-restricted feeding and continuous energy restriction via macronutrient-based diets were increasingly popular. Both diets were exclusively studied separately. A comparison of the two diets for people with a high body mass index despite regular physical activity has not yet been studied in detail. Therefore, this study aimed to compare the effects of these two diets on body composition and adherence. For this study, a total of 42 subjects (m = 21, f = 21) with a BMI above 25 were recruited from a local fitness gym. After a two-week familiarisation period, one of the two diets was followed over 14 weeks. Dietary behaviour was monitored throughout the period with a food diary. The primary measurement parameters were body weight, lean body mass, fat mass, body mass index, and waist and hip circumference. In addition, adherence was assessed and calculated by food diary and questionnaire. In total, the data of 35 participants (m = 14, f = 21) were analysed. Significant reductions in body weight, fat mass, body mass index, and waist and hip circumference were observed in both groups (p < 0.05). No significant change could be observed in lean body mass in either category. No group and gender differences were detected in any of the primary parameters. For the secondary parameters, a significantly higher adherence was observed in the time-restricted feeding group (p < 0.05). In addition, it can be assumed that an adherence of 60–70% cannot lead to positive changes in body composition. In conclusion, there were no differences between the two diets on the primary parameters. However, it seemed that time-restricted feeding can be better implemented in everyday life, and an adherence of more than 70% is required for both diets to prove effective.
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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