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Purpose Methoxyisoflavone (M), 20-hydroxyecdysone (E), and sulfo-polysaccharide (CSP3) have been marketed to athletes as dietary supplements that can increase strength and muscle mass during resistance-training. However, little is known about their potential ergogenic value. The purpose of this study was to determine whether these supplements affect training adaptations and/or markers of muscle anabolism/catabolism in resistance-trained athletes. Methods Forty-five resistance-trained males (20.5 ± 3 yrs; 179 ± 7 cm, 84 ± 16 kg, 17.3 ± 9% body fat) were matched according to FFM and randomly assigned to ingest in a double blind manner supplements containing either a placebo (P); 800 mg/day of M; 200 mg of E; or, 1,000 mg/day of CSP3 for 8-weeks during training. At 0, 4, and 8-weeks, subjects donated fasting blood samples and completed comprehensive muscular strength, muscular endurance, anaerobic capacity, and body composition analysis. Data were analyzed by repeated measures ANOVA. Results No significant differences (p > 0.05) were observed in training adaptations among groups in the variables FFM, percent body fat, bench press 1 RM, leg press 1 RM or sprint peak power. Anabolic/catabolic analysis revealed no significant differences among groups in active testosterone (AT), free testosterone (FT), cortisol, the AT to cortisol ratio, urea nitrogen, creatinine, the blood urea nitrogen to creatinine ratio. In addition, no significant differences were seen from pre to post supplementation and/or training in AT, FT, or cortisol. Conclusion Results indicate that M, E, and CSP3 supplementation do not affect body composition or training adaptations nor do they influence the anabolic/catabolic hormone status or general markers of catabolism in resistance-trained males.
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... Derivada de la Ecdisona, la Ecdisterona (Ec), β-Ecdisona o 20-Hidroxiecdisona (BE) fue catalogada como la molécula estándar de esta familia de compuestos cíclicos perhidrogenados. Ec es el ecdiesteroide con mayor actividad biológica en insectos (14,15,16) . Del mismo modo, es el PE más común, pudiendo ser aislado de los extractos de diversas especies de plantas con una relación coste/beneficio aceptable (13) . ...
... De mismo modo, la respuesta celular es dosis dependiente ya que con una posología inferior a 5ug/Kg de peso corporal no mostraban actividad significativa (27) . En modelos animales, principalmente ratas y ratones, la suplementación de la dieta con Ec durante periodos de 20 a 30 días y, en combinación con pruebas de natación, mostró que aquellos individuos suplementados eran capaces de nadar tramos más largos (14,15,25) . Estas conclusiones llevaron a la Ec a ser propuesta como molécula de estudio en humanos y dilucidar si realmente ejerce un poder anabólico y de mejora del rendimiento físico. ...
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Introducción: Los ecdiesteroides presentan cualidades únicas dentro del reino vegetal y animal. Su similitud a esteroides endógenos de mamíferos les otorga actividad biológica sobre el tejido muscular esquelético. Sin embargo, su mecanismo de acción está por definirse en su totalidad. Método: Se realizó una revisión narrativa utilizando la evidencia científica más relevante. Se consultaron de las bases de datos Medline, Google Scholar, Scielo y Wiley, incluyéndose y excluyéndose trabajos acordes a los criterios del autor. Resultados: La actividad de los ecdiesteroides, principalmente de la Ecdisterona (Ec), podría deberse a la interacción con Mas, receptor acoplado a proteína-G transmembrana (GPCR), y la posterior activación del receptor de estrógenos β (ER β) no nuclear. Dicho mecanismo de acción induce la activación de la ruta alternativa del Sistema Renina-Angiotensina-Aldosterona (RAA) aboliendo los mecanismos de degradación muscular y, mediante la activación indirecta de Erβ, se suprime la expresión del gen de la miostatina. Esta actividad biológica pudiera conferir a los ecdiesteroides propiedades farmacológicas óptimas para impedir la degradación proteico-muscular, tales como la regeneración y reparación del tejido. Conclusiones: Ec ha demostrado poseer propiedades farmacológicas interesantes para el abordaje alternativo de patologías musculodegenerativas por sus efectos anticatabólicos. Aunque prosigue la investigación para su implementación en la clínica, esta siendo utilizada en la industria deportiva y en ensayos para el tratamiento de diferentes patologías.
... The administration of alcoholic extract leads to an increase in uterus diameter and thickness of the endometrium, suggesting mild estrogenic activity (Pare et al. 2013). In another study, Wilborn et al. (2006) opined that more studies on human beings should be conducted to assess the antifertility potential of T. portulacastrum. ...
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Medicinal plants have remained a promising panacea for various health problems since ancient times. Trianthema portulacastrum L. (Family: Aizoaceae) is a small, diffused, annual and branched weed native to South Africa and also distributed in America, Baluchistan, India and West Asia. It is one of the significant medicinal herbs used for a variety of culinary and healthcare practices all over the world. Traditionally, it was used for the treatment of jaundice, asthma, throat infections and rheumatism. It is also helpful in treating alcohol poisoning. Its fleshy leaves are used for wound healing. The medicinal herb is a rich reservoir of therapeutically useful bioactive constituents, viz. flavonoids, saponins, alkaloids, steroids, terpenoids, tannins, glycosides and phenols. This plant possesses several pharmacological activities, such as antioxidant, antimicrobial, anti-inflammatory, analgesic, anti-fungal, anti-pyretic, anticancer, hypoglycemic and hepatoprotective. The present review is an effort to consolidate the available information on its ethnobotany, phytochemistry, pharmacological actions with possible mechanisms of action, toxicological studies, and recent advances. The phytotoxic potential of this weed has also been highlighted which may serve as a source for developing potent herbicides. The findings of this article may provide useful leads for pharmaceutical scientists, food scientists and herbal health practitioners to search for new drugs. The findings may also be beneficial for preparing a monograph of plants for future research aspects. Further comprehensive research is needed to evaluate molecular modes of action and ascertain efficacious doses of T. portulacastrum. Graphical abstract
... PLA decreased by 0.9% and 0.7% below baseline at 60 and 120 min post-ingestion, respectively, and, at 180 min, it increased 3.6% above baseline. Wilborn et al. [46] examined the effects of methoxyisoflavone, 20E, and sulfo-polysaccharide supplementation, similarly failing to find changes in catecholamine synthesis-associated cortisol across an 8-week resistance training protocol [47]. Nevertheless, the data are mixed on these metabolic effects and it thus remains possible that turkesterone supplementation in our investigation may have decreased cortisol and catecholamines, resulting in the equivocally observed RMR and substrate utilization results [10]. ...
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Turkesterone is a naturally occurring plant steroid touted for its medicinal, pharmacological, and biological properties with no reported adverse side effects compared with traditional anabolic androgenic steroids (AAS). However, this ostensible enhancement to increase muscle protein synthesis and facilitate augmented thermogenesis remains undescribed despite uninformed and potentially haphazard consumption. To investigate whether turkesterone enhances insulin-like growth factor-1 (IGF-1) and resting metabolic rate (RMR), eleven apparently healthy males (23.3 ± 2.2) volunteered to participate in the present study with samples collected pre-, 3H post-, and 24H post-ingestion. Subsequent analyses failed to reveal any significant main condition, time, or interaction main effects for serum IGF-1, RMR, lipid, and carbohydrate metabolism (p > 0.05). However, non-significant serum IGF-1 concentrations increased with both turkesterone conditions and remained elevated when compared with placebo. Similarly, RMR remained elevated above baseline across the 3 h assessed. Although these data fail to fully support turkesterone as a potent anabolic supplement, nevertheless, our findings are foundational to persistently tease apart this supplement's purported ergogenic effects and underscore its favorable hemodynamic and gastrointestinal tolerability profile. Future investigations should, therein, aim to assess turkesterone-mediated IGF-1 increases on long-term whole-muscle growth across several training sessions to further substantiate its efficacy on anabolism.
... In addition, in a WADA-funded study performance-enhancing and anabolic effects were determined in humans (Isenmann et al. 2019). A dose-dependent effect was observed in muscle mass and performance (Isenmann et al. 2019;Wilborn et al. 2006). Moreover, the use of phytosteroids such as ECDY as an alternative to anabolic steroids is recommended by secondary literature (Fahey, 1991;Kampitsch and Zippel, 2016). ...
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Plant steroids such as ecdysterone (ECDY) or diosgenin (DIO) have been associated with anabolic and performance-enhancing effects for years. However, the molecular mechanisms have not yet been extensively studied in skeletal muscle cells. Consequently, the anabolic activity and associated molecular mechanisms of ECDY and DIO alone and in combination were investigated in C2C12 myotubes. Dose-dependent effects of both compounds on myotube diameter, mRNA expression of IGF-1 and PI3KR1 as well as expression of myosin heavy chain (MHC) proteins were analyzed in differentiated C2C12 cells. In addition, the binding affinities to androgen and estrogen receptors were analyzed. Treatment with ECDY and DIO significantly induced hypertrophy of C2C12 myotubes. Partially additive effects were observed. This is supported by the mRNA expression of IGF-1 and PI3KR1 as well as in the expression of MHC. However, no clear statement can be made regarding which combination has the strongest additive effects. Besides, the results suggest that, in contrast to ECDY, DIO has antiandrogenic effects and bind on AR. Consequently, it indicates that two different mechanisms of action are activated in ECDY and DIO combinations. However, this must be confirmed in further cell cultures studies and human interventions concerning anti-doping regulations.
... In contrast, Wilborn et al. examined the effects of methoxyisoflavone, 20-hydroxyecdysone (E), and sulfopolysaccharide (CSP3) on strength and muscle mass 15 . Forty-five resistance-trained males (average age 20.5 years, height 179 cm, weight 84 kg, body fat 17.3%) were matched based on fat-free mass (FFM) and randomly assigned, in a double-blind manner, to receive either a placebo (P), 800 mg/day of methoxyisoflavone, 200 mg/day of 20hydroxyecdysone, or 1,000 mg/day of sulfur-polysaccharide for 8 weeks during their training. ...
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Introduction: It has been suggested that supplementation with turkesterone, a type of ecdysteroid, may have anabolic properties that promote improvements in body composition. Thus, the purpose of this investigation was to determine if four weeks of Turkesterone (500 mg daily dose) supplementation affected body composition in healthy males and females. Methods: Thirty-one active males (n=14) and females (n=17) volunteered for this investigation. Research participants were assessed pre and four weeks post for body composition (i.e., dual-energy X-ray absorptiometry). After pre-testing, they were randomized into a placebo (rice flour) or treatment group (i.e., 500 mg per day of turkesterone [Ajuga Extract]). Subjects were instructed to maintain the same diet and exercise habits during the study. Results: The delta scores of the treatment and placebo groups were compared using an independent samples t-test. There were no between-group differences (p>0.05) at baseline for age, height, or body mass. There were no between-group differences in the delta score between the turkesterone and placebo groups in body mass (p=0.38), lean body mass (p=0.68), fat mass (p=0.06), or percent body fat (p=0.14); (Delta score, mean±SD: body mass kg – treatment -0.4±1.8, placebo 0.1±1.8; lean body mass kg - treatment -0.6±1.4, placebo -0.3±1.7; fat mass kg - treatment 0.1±0.6, placebo 0.5±0.6, % fat treatment 0.3±0.6, placebo 0.7±0.9). Conclusions: Four weeks of supplementation with 500 mg of turkesterone did not affect body composition in active, healthy males and females
... However, the real content of ecdysterone has not been confirmed in analytical testsbased only on the information from the label. [72] One of the most thoroughly conducted studies, performed by Isenmann et al., showed that 10-week supplementation of ecdysterone at 12 mg daily and 48 mg daily in young men contributed to the improvement of anthropometric and performance parameters in the performed exercises. Significantly higher increases in muscle mass were observed in participants dosed with ecdysterone. ...
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... Thus, authors strongly suggested the inclusion of ECD in class S1.2 of the WADA prohibited list [8]. Surprisingly, another quite similar study found the opposite result, namely, ECD supplementation had no effect on training adaptation and anabolic/catabolic hormone status [9]. The significant difference can presumably be explained by incorrect labeling, namely, that the real ECD content was much lower than those indicated on the product, as found by Ambrosio et al. [10]. ...
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... Also, a structural role of ecdysterone in the mitochondrial membranes was reported [6]. However, positive therapeutic effects of ecdysterone were doubted in the literature [16]. ...
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