IngredientesEcdysterone (also known as crustecdysone, beta-ecdysone, and 20-hydroxyecdysone) is a naturally occurring steroid hormone belonging to the ecdysteroid class. Ecdysteroids are a group of polar, polyhydroxylated steroid hormones essential for the growth, development, and reproduction of arthropods and are also found in high concentrations in plants, where they are termed phytoecdysteroids.
Among more than 520 known ecdysteroids, one of the most common is 20-hydroxyecdysone (20HE). Ecdysterone is a structurally characteristic ecdysteroid bearing the systematic name 2β,3β,14α,20β,22α,25β-hexahydroxycholest-7-en-6-one. Important for the biological activity of ecdysteroids are the double bond at C-7, the keto group at C-6, and the hydroxyl groups at positions C-2, C-3, C-14, and C-22; the hydroxyl group at C-20 is specifically correlated with anabolic activity.
Ecdysteroids are the moulting hormones of insects and crustaceans, and are relatively polar polyhydroxy steroids that are widely distributed in nature. The first ecdysteroid, ecdysone, was isolated by Butenandt and Karlson in 1954 from silkworm pupae, and its structure was finally elucidated in 1965 by X-ray crystallography. Over 250 ecdysteroids have been isolated from various sources, particularly plants, where they probably function as chemical defences against predatory insects.
The most prominent members of the class discussed in the dietary supplement context are:
Although many plants synthesize ecdysteroids, only a few cultivated species — emphasizing quinoa and spinach — contribute meaningfully to dietary intake, while wild species such as those from the Ajuga genus contain substantially higher concentrations.
Key botanical sources include:
Ecdysteroids such as ecdysterone, ecdysone, and turkesterone occur naturally in insects, some plants, and some fungi; in insects they regulate many processes including molting, growth, and reproduction. In plants, ecdysteroids play a role in protecting the plants from stress and from insect attacks.
Commercial dietary supplements are derived from botanical extracts including Rhaponticum carthamoides, Cyanotis arachnoidea, Ajuga turkestanica, and quinoa, spinach, kaniwa, and asparagus, which have been confirmed as natural sources of phytoecdysteroids. Supplements are sold in capsule and tablet form and are commonly standardized to a declared percentage of 20-hydroxyecdysone content, though quality control issues are prevalent (see Section 8 below).
The use of R. carthamoides for medicinal purposes dates back to ancient times, and traditional Siberian medicine has long praised the plant for its ability to treat weariness and debility after sickness. Also known as leuzea or maral root, the plant Rhaponticum carthamoides comes from the Baikal Lake region, which stretches along Eastern Siberia. Traditionally consumed by Siberians in the form of a tea mixed with Rhodiola rosea, it was used as a stimulant and to combat fatigue or general weakness following illness, or as a tonic after the long Siberian winter.
Classified as a perennial herb used for centuries in eastern Russia, R. carthamoides was formally classified as an adaptogen by Brekhman and Dardymov in 1969 — a term used to refer to a natural herb product that increases the body's resistance to stresses such as trauma, anxiety, and bodily fatigue. In 1961, after more than 25 years of research and clinical studies, Rhaponticum carthamoides was officially included in the Soviet pharmacopoeia as a remedy for increasing capacity for work, athletic performance, and recovery following strenuous muscle work.
The most active phytoecdysteroid, ecdysterone — referred to as a "Russian secret" — was already suspected to be used by Russian Olympic athletes since the 1980s. In the history of Russian scientific investigation, R. carthamoides has received considerable attention in the domain of physical performance improvement. Research over the last century has shown its muscle- and strength-building capabilities, resulting in widespread use among elite athletes in Soviet and Russian sports.
The application of traditional Chinese herbs for bone regeneration has gained popularity in recent years, with β-ecdysterone recognized as a plant sterol similar to estrogen that promotes protein synthesis in cells. Plants of the Achyranthes genus containing ecdysteroids have been used in Chinese herbal medicine for centuries, including applications related to bone health.
Several different classes of compounds have been isolated from R. carthamoides, of which the main groups are steroids, particularly ecdysteroids, and phenolics (flavonoids and phenolic acids) accompanied with polyacetylenes, sesquiterpene lactones, triterpenoid glycosides, and terpenes (essential oil).
The principal bioactive ecdysteroids identified in supplement-relevant plant sources are:
β-ecdysterone can stimulate protein synthesis, promote carbohydrate and lipid metabolism, control blood glucose level, inhibit cell apoptosis, and improve intervertebral disc degeneration, and also has good biocompatibility.
Emerging evidence indicates that, unlike traditional anabolic steroids that act primarily via the Androgen Receptor (AR), ecdysterone's anabolic effects may be mediated through estrogen receptors (ERs), particularly estrogen receptor beta (ERβ). Hypertrophy induced by estradiol and ecdysterone could be antagonized with an antiestrogen but not by an antiandrogen. In HEK293 cells transfected with ERα or ERβ, ecdysterone treatment transactivated a reporter gene. To elucidate the role of ERβ, C2C12 myotubes were treated with ERα- and ERβ-selective ligands; ecdysterone treatment and the ERβ-selective ligand but not the ERα-selective ligand induced hypertrophy.
Molecular docking experiments have supported the ERβ-mediated action of ecdysterone. These findings underscore the pivotal role of ERβ in mediating ecdysterone's anabolic effects, distinguishing it from traditional androgenic steroids.
Ecdysterone has been demonstrated to increase protein synthesis in skeletal muscle. Gorelick et al. proposed direct or indirect stimulation of the PI3K/Akt signaling pathway as the mechanism for this increased protein synthesis. Studies have shown that ecdysterone can stimulate protein synthesis in skeletal muscle cells, potentially through direct or indirect activation of the PI3K/Akt signaling pathway. The binding of ecdysterone to human ERβ has been demonstrated in cell culture experiments, further supporting this non-androgenic mechanism of action.
Conversely to anabolic-androgenic steroids (AAS) that increase muscle mass mainly through their binding to the androgen receptor (AR), no nuclear receptor that is homologous to the ecdysone nuclear receptor found in insects has yet been described in mammals. Unlike anabolic steroids, ecdysteroids are believed to promote muscle growth and enhance physical performance without the severe side effects commonly associated with synthetic steroids, making them particularly appealing to athletes.
β-ecdysterone is a plant sterol similar to estrogen that promotes protein synthesis in cells. Studies have investigated its function on osteoblast differentiation and bone regeneration in vitro and in vivo. Preclinical research indicates involvement of the BMP-2/SMAD/RUNX2/Osterix signaling pathway in ecdysterone-mediated effects on bone tissue.
20-Hydroxyecdysone is an arthropod steroid hormone that possesses a number of beneficial pharmacological activities in humans, including anabolic, antioxidant, hypoglycemic, cardioprotective, hepatoprotective, neuroprotective, and antineoplastic properties. While several studies have explored the anabolic activity of 20E in muscle cells, others have demonstrated that 20E boosts both catabolism and anabolism, coupling energy-producing and biosynthetic metabolic processes in mouse myoblasts and fibroblasts.
In rats, ecdysterone exhibited a strong hypertrophic effect on the fiber size of the soleus muscle that was found even stronger compared to the test compounds metandienone (Dianabol), estradienedione (trenbolox), and SARM S1, all administered at the same dose (5 mg/kg body weight, for 21 days). In C2C12 myotubes, ecdysterone at 1 µM induced a significant increase in diameter comparable to dihydrotestosterone (1 µM) and IGF-1 (1.3 nM). These are preclinical findings and do not establish equivalent effects in humans.
Isenmann et al. (2019) — WADA-Funded RCT: A 10-week intervention study of strength training in young men (n = 46) was carried out, in which different doses of ecdysterone-containing supplements were administered. Analysis of blood and urine samples for ecdysterone and potential biomarkers of performance enhancement was conducted. Significantly higher increases in muscle mass were observed in those participants who were dosed with ecdysterone, and the same hypertrophic effects were also detected in vitro in C2C12 myotubes. Notably, research participants supplemented with high-dose ecdysterone (48 mg of ecdysterone) showed a significant increase in muscle mass (2.0 kg delta). The authors suggested that ecdysterone should be included in the WADA Prohibited List as "other anabolic agent." Interestingly, the actual amount of ecdysterone in the capsule was found to be only 6 mg, whereas the declared amount was 100 mg. This is a significant methodological limitation, as the true dose delivered to participants may have differed substantially from the nominal dose.
Wilborn et al. (2006) — Null Result RCT: 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, 800 mg/day of methoxyisoflavone, 200 mg of 20-hydroxyecdysone, or 1,000 mg/day of sulfo-polysaccharide for 8 weeks during training. The major finding of this study was that dietary supplementation of commercially available supplements containing methoxyisoflavone, ecdysterone, and sulfopolysaccharide did not significantly affect anabolic or catabolic responses to resistance training, body composition, or training adaptations. These findings do not support contentions that ecdysterone supplementation during resistance training enhances gains in strength, power, or muscle mass.
Asparagus-Derived 20HE Study: One human study found that supplementing with 200 mg/day of 20E for 8 weeks had no effect on lean mass, muscle strength, or muscle power adaptations, nor did it affect anabolic or catabolic hormone status in resistance-trained men. However, a separate study in young men found that supplementing with 48 mg/day of ecdysterone for 10 weeks increased muscle mass and strength. When comparing muscle mass development after the resistance training period, that latter study found no significant differences between the placebo and the 20E groups at the doses used.
Human evidence is sparse and conflicting. Extensive research on the potential anabolic-promoting effects of ecdysterone in various animal models and cell cultures has been reported; in contrast, supplementation with ecdysterone to enhance performance has not yet been widely studied in humans. The total number of human RCTs is very small, populations and doses vary, and at least one key study was complicated by severe label inaccuracy regarding actual ecdysterone content. The overall evidence base is preliminary and insufficient to establish efficacy.
In 1969, Brekhman and Dardymov classified R. carthamoides as an adaptogen, now widely used in herbal medicine to promote resistance to stress, such as trauma, anxiety, and fatigue. Adaptogens are pharmacologically active compounds or plant extracts that have the ability to enhance the body's stability against physical loads without increasing oxygen consumption.
Research conducted in Russia suggests that extract of R. carthamoides may significantly increase muscle mass while decreasing fat mass in athletes when taken during training, and studies show it may help boost capacity for work and endurance, and reduce physical and mental fatigue. The bulk of this evidence is from older Soviet-era research, much of which was published in Russian-language literature and has not been replicated in modern, independently conducted, double-blind placebo-controlled trials. Evidence strength for anti-fatigue effects in humans remains preliminary.
In vivo studies suggest that ecdysterone possesses effects on Alzheimer's disease, lipid metabolism, as well as having anti-obesity, anti-diabetic, and neuroprotective effects. A controlled randomized study has investigated the utilization of 20HE in metabolic syndrome.
Ecdysteroids are polyhydroxylated steroids present in invertebrates and plants. 20-Hydroxyecdysone (20E) is the most common and the main biologically active compound of ecdysteroids. Previous studies have demonstrated anabolic and metabolic effects of 20E in mammals, though it was not fully established whether 20E has a positive effect on all aspects of cardiometabolic syndrome.
A number of favorable non-hormonal biological effects on mammals have been reported for ecdysterone, including the so-called adaptogenic effect (protection of the organism against adverse stress factors) associated with anabolic, gastroprotective, and antioxidant effects. A second group of favorable effects involves the suppression of neurodegenerative processes and protection of the cardiovascular system (metabolic syndrome symptom suppression, antidiabetic activity, and protection of heart and blood vessels).
The vast majority of metabolic and cardiovascular evidence remains at the animal model and cell culture level. No large-scale human clinical trials have established efficacy for these indications, and evidence strength is weak to preliminary.
β-ecdysterone is a plant sterol similar to estrogen that promotes protein synthesis in cells. Studies have investigated its function on osteoblast differentiation and bone regeneration in vitro and in vivo, using MC3T3-E1 cells. The results suggest that the proliferation of MC3T3-E1 cells was promoted by β-ecdysterone. Tissue sections of the liver and kidney of rats treated with 72 mg/kg of β-ecdysterone for 4 weeks showed no signs of abnormality and toxicity, further confirming that β-ecdysterone did not exert any undesirable toxic effects on the animals at this dose.
All bone-related evidence is currently preclinical (cell culture and animal models). No controlled human trials have investigated ecdysterone specifically for bone health outcomes. Evidence strength is very preliminary.
Additional pharmacological effects, including potential roles in breast cancer therapy and Alzheimer's disease, have been described for ecdysteroids. The therapeutic potential of phytoecdysteroid-rich extracts extends beyond sports nutrition, with promising applications in treating chronic fatigue, cardiovascular diseases, and neurodegenerative disorders.
Evidence for neuroprotection remains at in vitro and animal model stages. No human clinical trials have been completed for neurological indications, and evidence strength is very preliminary.
Ecdysteroids are widely marketed to athletes as dietary supplements, advertising to increase strength and muscle mass during resistance training, to reduce fatigue, and to ease recovery. The following dosages have been specifically reported in human and animal studies:
No standardized, officially recommended human dosage has been established. Further research on ecdysteroids is required to elucidate their mechanisms of action, confirm the absence of adverse effects, and establish reference urinary concentration ranges that allow differentiation between diet-related metabolites and those derived from drug use.
Regarding human toxicity, current evidence suggests a highly favorable safety profile. The administration of elevated ecdysterone concentrations has not been linked to any documented acute or chronic adverse events. There is evidence showing that ecdysterone does not have toxic effects on the liver or kidneys, due to the absence of biomarkers for liver or kidney toxicity after 10 weeks of administration.
Safety evaluation in the Isenmann et al. trial was performed on the basis of serum concentrations of selected biomarkers of kidney and liver function, and those markers did not significantly change during the 10-week intervention period.
The most frequently reported adverse effect is mild gastrointestinal distress, including nausea or an upset stomach. This reaction is usually transient and dose-dependent, often resolving as the body adjusts to the supplement.
The long-term safety of ecdysteroid supplementation remains undetermined due to the limited duration of current human studies. Ecdysteroids are generally considered non-toxic in humans; however, analysis of commercial supplements frequently reveals poor quality control.
This is among the most practically significant safety-adjacent concerns with ecdysterone supplements. A broad variety of products labelled to contain ecdysterone can be found on the market. In one study it was found that most of those products do not meet the desired quality and safety standard concerning the correspondence of their actual ecdysterone content with the value reported on the labeling; the content was found to be generally much lower than the amount indicated on the label.
Twenty-one ecdysterone-containing dietary supplements from ten brands were analysed. In all cases, the measured ecdysterone content was much lower than labelled, and 20% of the samples contained a prohibited substance. The concentration of ecdysterone and contaminations varied randomly from batch to batch.
Following oral ingestion, ecdysterone and its principal metabolites — namely poststerone, 14-deoxy-ecdysterone, 14-deoxypoststerone, and their various reduced derivatives — are cleared from the rat organism within a 48-hour window, primarily via fecal excretion. Ecdysterone and its metabolites, 14-deoxy-ecdysterone and 14-deoxy-poststerone, are detectable in urine for more than two days depending on dosage.
Ecdysterone has been monitored by the World Anti-Doping Agency (WADA) since 2020 because of its suspected anabolic properties and potential to enhance athletic performance in both professional and non-professional contexts. At present, WADA has not added ecdysteroids to the Prohibited List; however, there has been increasing interest in their potential performance-enhancing effects, with WADA adding them to the WADA Monitoring List in 2020. At present, there are no FDA-approved medications that contain ecdysteroids.
Some researchers have suggested that, to clarify its status in sports, ecdysterone should be considered for inclusion in the class "S1.2 Other Anabolic Agents" of the list of prohibited substances of the World Anti-Doping Agency. Unlike synthetic anabolic steroids, which are classified as controlled substances, ecdysteroids remain largely unregulated in many countries and are widely marketed as dietary supplements.
Based on earlier results, ecdysterone was included in the 2020 Monitoring Program. As ecdysterone-containing plants may be part of common human diet, discrimination between common dietary levels, excessive dietary intake of ecdysterone, and supplementation for misuse is highly desired in anti-doping contexts.
Condiciones de salud que Ecdysteroids puede ayudar a apoyar.
Ecdysteroids are polyhydroxylated steroids found in plants (phytoecdysteroids) and insects with demonstrated anabolic and ergogenic properties. RCT evidence shows improvements in muscle mass and strength. WADA placed them on its monitoring list. They act via estrogen receptor beta to stimulate muscle protein synthesis.
Sistemas corporales que Ecdysteroids puede ayudar a apoyar.
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