Beta-ecdysterone and its anabolic role

Beta-ecdysterone and its anabolic role

Beta-Ecdysterone, also called Ecdysterone or 20-hydroxyecdysone, belongs to the group of ecdysteroids, natural steroids found in some plants and insects.

Beta-Ecdysterone, the ultimate anabolic substance

Something virtually unknown until a couple of months ago, where it began to echo through social networks, which ignited like wildfire under the claim of:

“Ecdysterone, a new non-banned anabolic steroid with no side-effects.”

Does Ecdysterone improve sports performance?

Ecdysterone does not induce gene expression like anabolic steroids but influences biochemical pathways outside the nuclei of muscle cells and the end result is increased muscle protein synthesis, thus promoting the building of lean mass.

Beta-Ecdysterone is commonly included in some supplements in combination with other natural extracts such as tribulus terrestris, tongkat ali and rhodiola rosea, to improve all sports performance parameters.

But really, what’s the truth in all this? Have we moved beyond traditional anabolic steroids and found a safe alternative? In this article, we’ll see that this isn’t the case…

What is Ecdysterone?

Firstly, Ecdysteroids, especially Ecdysterone and Turkesterone, have been widely used for decades by performance athletes around the world, under the claim of their potential to improve body composition and thus athletic performance.

The concept of Ecdysteroid comes from:

  • Ecdysis, which is the hormone-controlled moulting process by which insects shed their exoskeleton, and
  • Steroid, referring to their molecular structure, which are synthesised in arthropods from cholesterol.

Hence any type of Ecdysteroid, although the most commonly consumed is Ecdysterone, are known as “insect steroids”.

Anabolic effects in training

They do not actually come from these, as Ecdysteroid production for consumption is extracted from a wide variety of coniferous and angiosperm plants.

The ecdysteroidogenic metabolic pathway is dependent on a set of genes known as “Halloween”, encoded by cytochrome P450 enzymes and which humans do not possess, just as we do not possess the Ecdysterone receptors present in arthropods which complete a metabolic pathway that we do not have in our own bodies

How do ecdysteroids work?

Ecdysteroids presumably have the potential to modulate immune system response, increase oxidative metabolism of carbohydrates and fatty acids, protein synthesis and physical performance.

But to understand whether this is true or not it’s important to know how they do it.

Parr et al. (2014) wrote a study explaining the metabolic pathway that ecdysteroids (Ecdysterone) use in mammals to cause these effects; they administered 5mg/kg of Ecdysterone intravenously to a group of rats for 21 days.

The authors explain that the effects that ecdysteroids have on arthropods (such as moulting, or mediation of sexual functions) cannot be mediated in mammals, as we lack the nuclear receptor complexes USP and EcR; therefore, the effects that ecdysteroids exert in mammals must be mediated by another pathway.

This pathway is through agonism with the estrogen receptors beta (ERBs), which appear to be responsible for the anabolic effects of oestrogens in the human body.

There is another subtype of estrogen receptor, the alpha; homologous in amino acid sequence and with similar affinity for oestradiol (E2), but different distribution in body tissues (it’s assumed that, for example, this subtype is responsible for the appearance of gynaecomastia due to its dominance in breast tissue.

However, Ecdysterone does not (a priori) have an affinity for this type of receptor.

Hydroxy-Ecdysterone

Figure I. Mechanism of action of 20-Hydroxy-Ecdysterone (20HE) in increasing muscle protein synthesis. (Gorelick-Feldman, Cohick, & Raskin, 2010)

Ecdysterone induces a non-genomic response that activates a G-protein-coupled receptor, which initiates a cascade of reactions that forces calcium out of the sarcoplasmic reticulum into the cell cytosol.

In addition to the opening of cell membrane calcium channels that generate a positive gradient allowing Ca2+ to enter the cell; this increase in intracellular calcium concentrations activates the PI3K/AKT transduction pathway, which subsequently activates mTORC1, P70S6K and subsequent metabolic reactions resulting in increased protein synthesis.

To get an idea, it shares a mechanism of action (at least the PI3K-dependent one) with the famous IGF-1 (Increlex). In addition, it has the advantage that it doesn’t inhibit HPTA, since despite the hypotheses that have existed, Ecdysterone does not agonise with androgen receptors (as do anabolic steroids and SARMs), so it would not be necessary to restore the hormonal axis after consumption of the same

Effects

In vitro, in animals and in humans.

On paper, intravenous infusion of 5mg/kg Ecdysterone in mice increases IGF-1 and LH concentrations; reduces E2 and Corticosterone; and does not affect concentrations of other hormones such as prolactin, thyroxine, or testosterone.

Ecdisterone

Figure II. A- Effects of Ecdysterone vs Control on soleus muscle fibre size. B- Effects of Ecdysterone (E) vs Control (K) on the size of different muscle fibre types (I, II, IIa, IIb) of the soleus. (Parr et al., 2014)

The results are shocking, in 21 days the rats significantly increased the cross-sectional area of the soleus musculature, through the increase (significantly higher) of the type II muscle fibres (fast, those with the greatest potential for hypertrophy).

Within these, subtype B appears to be the most sensitive to the effects of Ecdysterone

Dexamethasone

Figure III. Effects of different doses of dexamethasone (a corticosteroid) (Dexa 5, Dexa 6), dihydrotestosterone (DHT), Insulin-like growth factor type 1 (IGF-1) and Ecdysterone (Ecdy) on the diameter of rat C2C12 cell myotubes, In Vitro. (Parr et al., 2014)

Effects on myotube diameter are similar when incubated in 100nM Dihydrotestosterone, 10ng/ml IGF-1 and 1 mcM Ecdysterone.

Beta-Ecdysterone and Anabolic Effect

So we have a substance that increases muscle fibre size, of similar potency to IGF-1, so highly sought after and considered by some to be the cornerstone of musculo-skeletal hypertrophy (and possible hyperplasia), without inhibition of the hormonal axis…

Do we have the ultimate compound?

Parr et al. (2015) repeated these same conclusions by showing that Ecdysterone had the potential to significantly increase the size of soleus muscle fibres in rats compared to other substances that are so widely used for this purpose such as methandienone (dianabol) or S1 (SARM).

Effects of Ecdysterone

Figure IV. Effects of Ecdysterone vs DHT vs IGF-1 vs Control on myotube diameter and relative size increase between estradienodione (EDD), methandienone (MD), SARMS S1 (S1) and Ecdysterone (Ecdy); left and right graph, respectively. (Parr et al., 2015)

Well, there we have it, the ultimate compound….

On paper; in vitro tests on animal models… In vitro studies are a good starting point, they allow us to elucidate the biomolecular mechanisms through which certain responses observed in living organisms occur.

But conclusions reached from isolated tissue responses in a laboratory should never be extrapolated to a living body, especially if the studies have been performed in vitro using tissues from animal models.

This, unfortunately, is the case with Ecdysterone; as after all its great potential in rats, in humans it shows… Nothing?

Body Composition

Figure V. Changes in body composition of subjects after 8 weeks of training and supplementation. (E) is the Ecdysterone supplemented group. FFM- Fat free mass; FM- Fat mass; BF (%)- Body Fat Percentage. (Colin et al. 2006)

Colin et al. (2006) showed that oral supplementation of 200mg. of Ecdysterone per day in 45 trained men did not generate any significant difference after 8 weeks of training and supplementation versus the placebo group, neither in body composition, nor in performance in strength exercises (kg) nor in the Wintgate test (w).

Performance Table

Figure VI. Changes in performance of subjects after 8 weeks of training and supplementation in Bench Press and Leg Press. (E) is the group supplemented with Ecdysterone. (Colin et al. 2006)

Likewise, as expected, it did not affect serum concentrations of free and available testosterone, but neither did it affect cortisol concentrations, which presumably should decrease following Ecdysterone consumption.

Is Ecdysterone legal?

Ecdysterone cannot be crossed off the list of substances potentially beneficial to athletic performance either.

The WADA (World Anti-Doping Agency) has pursued this substance hard after the publication of the aforementioned studies, for its possible benefit on sporting performance, in order, of course, to ban it.

Isenmann et al. (2019) published a WADA-supported study in which a total of 46 trained young people underwent 10 weeks of weight training and were administered oral Ecdysterone to test the effects of Ecdysterone on body composition, athletic performance and serum hormone concentrations.

The sample was divided into 4 groups: PL- Placebo, training, no supplementation. EC1 – Ecdysterone low dose, train, supplement with 200mg. EC2 – Ecdysterone high dose, train, supplement with 800mg. CON – Control, no training, supplement with 200mg.

In this case, Ecdysterone supplementation resulted in a significant increase in body weight in both the low and high dose versus the control; and although not significant, it resulted in a greater increase in body weight versus the placebo group.

It also resulted in a significantly greater increase in muscle mass than the placebo group.

Changes in body composition

Figure VII. Changes in body composition in the different groups subjected to training and/or supplementation. On the left body weight, on the right muscle mass. (Issenmann et al., 2019)

Beta-Ecdysterone and Sports Performance

Similarly, squat performance increased more in the dose-dependent Ecdysterone-consuming groups, although with a non-linear dependence, i.e. Ecdysterone loses efficiency at higher doses.

And they increased bench press performance significantly more than the placebo group.

Changes in the RM Squat and Bench Press

Figure VIII. Changes in performance of the different groups subjected to training and/or supplementation. On the left 1RM squat, on the right 1RM bench press. (Issenmann et al., 2019)

With regard to hormonal changes, there are none that can be attributed to the consumption of Ecdysterone, due to the variability between intervention groups (Ec1 and Ec2), and we can only hypothesise that Ecdysterone may have the potential to attenuate the negative (acute) effects of intense strength training on IGF-1 concentrations.

IGF

Figure IX. Changes in IGF-1 concentrations in the different groups subjected to training and/or supplementation. (Issenmann et al., 2019)

So increases in athletic performance may be due to risk of bias in this study, or mechanisms potentially elucidated in In Vitro trials.

Evosterone, the definitive Beta-Ecdysterone from HSN

HSN’s SportSeries range includes an exclusive formula based on Ecdysterone (Beta-Ecdysterone) from the Rhaponticum carthamoides plant.

Unlike other products on the market, the raw material of Ecdysterone from which Evosterone is manufactured has been standardised to 95% using high-performance liquid chromatography measurement methods (HPLC).

This makes sure the concentration indicated on the product is guaranteed and there is no possibility of error.

Why is this important?

Because, as mentioned in the article, the quality controls of the ecdysterone supplements sold are not sufficient, and other companies, in order to buy cheap raw materials to reduce costs, offer products with a lower quantity than indicated.

Evosterone by SportSeries by HSN

Don’t miss our out on our latest products! Always in our online shop.

You can check it in this external analysis where we compare the concentration of the 2 authorised suppliers of ecdysterone (supplier 1 and supplier 2) for the manufacture of Evosterone, and a known product of another brand on the market (end product brand 2) that claims to have 20.9mg per capsule, when in fact it has only 12.5mg (40% less).

At HSN, we work with the highest certified quality standards, and therefore the dosage and control of our products is outstanding.

Evosterone contains 50mg of Ecdysterone per daily dose, and it’s dosed according to the Ec2 dose (the most effective) from the study by Isenmann et al. (2019).

New product developments are carried out by HSN’s specialist R+D+I department, with dosages and formulations backed by scientific evidence.

Evosterone also contains black pepper extract (100% piperine) to partially and temporarily inhibit the metabolisation of the compound ecdysterone so that its effects are greater.

It also contains zinc, which contributes to the maintenance of normal concentrations of testosterone, and vitamin B6 which contributes to the regulation of hormonal activity.

It is impossible to have any doubts! At HSN, we offer you premium quality products at the right price.

Who Evosterone is for

When to take Ecdysterone?

It’s important to highlight how little control the marketed Ecdysterone supplements are undergoing.

The authors explained that the quantification of actual Ecdysterone per capsule after laboratory analysis revealed an amount of 6mg per capsule; which is considerably less than the 100mg advertised on the product. So the Ec1 group was consuming 12mg/day; and Ec2 48mg/day actually.

Dose

The dosage of the substance should be limited to 0.15-0.6mg/kg/day

Interestingly, the study by Parr et al. (2014) shows that any ERb-selective agonist loses this affinity when consumed in high amounts, causing it to bind to ERa indiscriminately.

Side effects

If you end up suffering from gynecomastia or somatic symptoms of excess oestrogen, it’s possible you’re consuming more than the established dose, which causes Ecdysterone to bind to receptors in breast tissue, for example; or contamination of the product with other substances which can cause these effects, as you know.

Conclusions

We don’t knowfor sure if Ecdysterone really is a substance that represents a great advantage at a sporting level compared to not consuming it.

How to take ecdysterone

HSN, We are nutrition!

The studies that report great benefits are being subsidised by WADA, who have an interest in banning it (albeit pre-emptively) to avoid competitive irregularities; an independent study concluded that Ecdysterone has no effect on any parameters that are likely to influence sporting performance.

It may also be because the product they bought had no active ingredient at all, as there are no reports of analysis of the contents of the capsules.

Ecdysterone is a substance that has a very interesting mechanism of action in animal models, with significant effects on body composition and sports performance in animal models; but has seriously mixed evidence in humans

Bibliographic sources

  1. Gorelick-Feldman, J., Cohick, W., & Raskin, I. (2010). Ecdysteroids elicit a rapid Ca2+ flux leading to Akt activation and increased protein synthesis in skeletal muscle cells. Steroids, 75(10), 632–637.
  2. Isenmann, E., Ambrosio, G., Joseph, J. F., Mazzarino, M., de la Torre, X., Zimmer, P., … Parr, M. K. (2019). Ecdysteroids as non-conventional anabolic agent: performance enhancement by ecdysterone supplementation in humans. Archives of Toxicology, 93(7), 1807–1816.
  3. Parr, M. K., Botrè, F., Naß, A., Hengevoss, J., Diel, P., & Wolber, G. (2015). Ecdysteroids: A novel class of anabolic agents? Biology of Sport, 32(2), 169–173.
  4. Parr, M. K., Zhao, P., Haupt, O., Ngueu, S. T., Hengevoss, J., Fritzemeier, K. H., … Diel, P. (2014). Estrogen receptor beta is involved in skeletal muscle hypertrophy induced by the phytoecdysteroid ecdysterone. Molecular Nutrition & Food Research, 58(9), 1861–1872.
  5. Wilborn, C. D., Taylor, L. W., Campbell, B. I., Kerksick, C., Rasmussen, C. J., Greenwood, M., & Kreider, R. B. (2006). Effects of Methoxyisoflavone, Ecdysterone, and Sulfo-Polysaccharide Supplementation on Training Adaptations in Resistance-Trained Males. Journal of the International Society of Sports Nutrition, 3(2), 19.

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About Alfredo Valdés
Alfredo Valdés
A specialist in Pathophysiology and biomolecular effects on nutrition and sportive activity who will show you the elaborate world of sports nutrition in his articles, employing a simple and critical writing.
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