20-hydroxyecdysone was discovered as the major biologically active insect steroid hormone half a century ago, yet much remains to be learned about its biosynthesis and its activities. 20-hydroxyecdysone controls many biological processes, including progression between larval stages, entry to pupariation and metamorphosis. Ecdysteroids are compounds related to 20-hydroxyecdysone, the insect moulting hormone. Surprisingly, they have been found in serum and urine of patients infected with helminths. In these cases, the substances are assumed to be produced by the parasites and, therefore, might be used as a marker of parasitic infection. Ecdysteroids produced by schistosomes are released in biological fluids of infected hosts. In the sera, the concentration of ecdysteroids correlates with the permissiveness of the host to schistosome infection.
Function in plants
Phytoecdysteroids are a family of about 200 plant steroids related in structure to the invertebrate steroid hormone 20-hydroxyecdysone. Typically, they are C27, C28 or C29 compounds. Phytoecdysteroid has been found to protect spinach from plant-parasitic nematodes and may confer a mechanism for nematode resistance. It is possible that phytoecdysteroids are found in plants to protect them from insects. Pfaffia glomerata is one plant of many that has ecdysteroids.
Biol Sport. 2015. Ecdysteroids: A novel class of anabolic agents? Increasing numbers of dietary supplements with ecdysteroids are marketed as "natural anabolic agents". Results of recent studies suggested that their anabolic effect is mediated by estrogen receptor (ER) binding. Within this study the anabolic potency of ecdysterone was compared to well characterized anabolic substances. Effects on the fiber sizes of the soleus muscle in rats as well the diameter of C2C12 derived myotubes were used as biological readouts. Ecdysterone exhibited a strong hypertrophic effect on the fiber size of rat soleus muscle that was found even stronger compared to the test compounds metandienone (dianabol), estradienedione (trenbolox), and SARM S 1, all administered in the same dose. To clarify its status in sports, ecdysterone should be considered to be included in the class "S1.2 Other Anabolic Agents" of the list of prohibited substances of the World Anti-Doping Agency.
Brain neuron protection
Neurosci Res. 2014 Jan 27. Ecdysterone protects gerbil brain from temporal global cerebral ischemia/reperfusion injury via preventing neuron apoptosis and deactivating astrocytes and microglia cells.
Ecdysterone was shown to improve the learning and memory of the rats and increase the expression of c-fos. Very little human research has been published regarding ecdysterone. Therefore little is known about the full benefits and side effects of ecdysterone.
Effect of ecdysterone on glucose metabolism in vitro.
Life Sci. 2005.
The aims of this study was to investigate whether ecdysterone is able to exert glucose-lowering effect on hepatocytes or stimulate the secretion of insulin. HepG2 cell line was used for glucose consumption (GC) studies. At moderate high glucose concentration, GC of HepG2 cells was increased by 44% to 77% with ecdysterone, which was comparable to that with metformin. The glucose-lowering effect of ecdysterone decreased as the glucose concentration of medium increased. The results indicate that ecdysterone is able to exert the glucose-lowering effect in hepatocytes which is insulin-independent, but has no effect on insulin release.
Ecdysteroids during early embryonic development in
silkworm Bombyx mori: metabolism and functions.
Zoolog Sci. 2004.
It has been well established that eggs of insects, including those of the silkworm Bombyx mori, contain various molecular species of ecdysteroids in free and conjugated forms. In B. mori eggs, 20-hydroxyecdysone (20E) is a physiologically active molecule. In nondiapause eggs, 20E is produced by the conversion of maternal conjugated ecdysteroids (ecdysteroid-phosphates) and by de novo biosynthesis. In contrast, in diapause eggs, neither of these metabolic processes occurs. In de novo biosynthesis of 20E in B. mori eggs, hydroxylation at the C-20 position of ecdysone, which is catalyzed by ecdysone 20-hydroxylase, is a rate-limiting step. Furthermore, we found that a novel enzyme, called ecdysteroid-phosphate phosphatase (EPPase), specifically catalyzes the conversion of ecdysteroid-phosphates to free ecdysteroids. The developmental changes in the expression pattern of EPPase mRNA correspond closely to changes in the enzyme activity and in the amounts of free ecdysteroids in eggs. EPPase is localized in the cytosol of yolk cells, and the bulk of maternal ecdysteroid-phosphates is bound to vitellin and stored in yolk granules. The vitellin-bound ecdysteroid-phosphates are scarcely hydrolyzed by EPPase. Therefore, to examine how ecdysteroid-phosphates are hydrolyzed by EPPase during embryonic development further investigations were focused on yolk granules. Recent data indicate that acidification in yolk granules, induced by vacuolar H(+)-ATPase, triggers the dissociation of ecdysteroid -phosphates from the vitellin-ecdysteroid -phosphates complex and the dissociated ecdysteroid-phosphates are released from yolk granules to the cytosol. To explain the process of the increase in the level of 20E during embryonic development in B. mori eggs, a possible model is proposed.
Study of excretion of ecdysterone in human urine.
Rapid Commun Mass Spectrom. 2001.
Doping Control Laboratory of Athens, Olympic Athletic Center of Athens, Kifissias, Maroussi, Greece.
A study of excretion in human urine of ecdysterone, which is the active component of several over-the-counter supplements such as "Ecdysten", reportedly used by athletes, is presented. The study was performed after oral administration of 20 mg of ecdysterone. The collected urine samples were prepared using the standard screening extraction procedure for the free and conjugated fraction of anabolic steroids, and analyzed by gas chromatography (GC) coupled with quadrupole mass spectrometry (MS) and also with high-resolution mass spectrometry (HRMS). Two ecdysterone metabolites were identified and detected along with unchanged ecdysterone. Accurate mass measurements were made for diagnostic ions, including the molecular ion of the main metabolite of ecdysterone, deoxyecdysone, which, to our knowledge, has not previously been reported in the literature. These accurate mass measurements support the proposed fragmentation scheme.
A new ecdysteroid named rhapontisterone R1 together with two known phytoecdysones, rhapontisterone and ecdysterone were isolated from the roots of Rhaponticum uniflorum.
The ecdysone -inducible gene switch is a useful tool for modulating gene expression in mammalian cells and transgenic animals. We have identified inducers derived from plants as well as certain classes of insecticides that increase the versatility of this gene regulation system. Phytoecdysteroids share the favorable kinetics of steroids, but are inert in mammals. The gene regulation properties of one of these ecdysteroids have been examined in cell culture and in newly developed strains of ecdysone -system transgenic mice. Ponasterone A is a potent regulator of gene expression in cells and transgenic animals, enabling reporter genes to be turned on and off rapidly. A number of nonsteroidal insecticides have been identified that also activate the ecdysone system.
Effect of ecdystene on parameters of the sexual function
under experimental and clinical conditions.
Eksp Klin Farmakol. 2000.
Institute of the Chemistry of Plant Substances, Academy of Sciences of the Republic of Uzbekistan, Tashkent, Uzbekistan.
The effects of ecdysterone and the related drug ecdysten on the sexual activity were studied under experimental and clinical conditions. A 10-day administration of ecdysterone (5 and 10 mg/kg, p.o.) improved behavioral characteristics of the sexual function in rats, the effect being especially pronounced during the fist days of experiment. The administration of ecdysten to men with the infertility diagnosis (disturbed spermatogenesis as a complication of some urologic diseases) increased the copulative function and improved the sperm quality. The administration of ecdysten to patients in the stage of recovery upon myocardial infarction also improved the sexual function.
Q. I use herbal medicinals to treat the long-term side effects of an Accutane treatment I underwent in 2002. I currently take Epimedium grandiflorum, Mucuna pruriens, Maca, and Polypodium vulgare. The Epimedium is not as a effective as it was when I first began using it; this may be due to downregulation of ACh receptors; I am considering substituting it with Huperzine A. My main concern though is with the use of Polypodium. I have heard that this particular species contains carcinogens. However, I have not found any information in pharmacopeias or journals that substantiate that it does. James Duke's Phytochemical and Ethnobotanical Databases does not list any. Are you aware of any carcinogenic constituents to this botanical? I am also concerned about using ecdysteroids. Do you know if their are any negative side effects associated with the use of ecdysteroids, viz. gynecomastia, testicular atrophy, or abnormal liver functions? If it increases testosterone levels, would this not lead to an increase in estradiol levels? Wouldn't the increase in testosterone lead to negative feedback of GnRH, decreasing LH levels? I am aware, however, that antigonadotropins are present in Polypodium vulgare. Do they effect LH signaling pathways?
A. Most herbs have dozens and more compounds in them, each influencing various parts of the body and hormonal system. It is too difficult to answer such questions since human trials are lacking in most cases.
Q. I am a track and
field coach in Canada. My athletes use suma and ecdysterone and have great
results from it. The product is not on the World Anti Doping List of Banned
Substances (WADA), the NCAA list, or the IOC list. Question. I'm curious as to
why it was used in the study mentioned on your site done in Athens? Correct me
if i'm wrong but the test at the Olympic Doping centre was to just pick up
metabolites?. I'm a bit confused. The Olympic testing system has programed in it
about 400 plus items , in other words they are "looking" for those items. Now
wouldn't one have to add the molecular configuration of ecdysterone to pick up
ecdysterone on the tests? I'm confused as to the entire premise of the Olympic
test of 20mg of ectysterone. Lastly, what is you opinion of it for athletes, do
you think it is a useful product and why. Would you know also where I could get
the molecular picture of ecdysterone and compare it to something like Nandralone.
A. These are questions that are beyond my range of knowledge. Ecdysterone is a new substance for me that I recently came across so I don't know too many details about it at this time.
Q. I read your review of creatine online and found it
very informational. I am wondering if you can share some information about the
recent body-building supplement Ecdy Bolin. I have been using it for a couple
months (both with creatine and also without). It is promoted as has other
benefits aside from muscle-building, such as nerve function. Anyway, I would
like to know if you feel this supplement is a safe and a quality addition and
how you feel about it in general. At the moment, I am not using creatine, only
A. An internet search reveals Ecdy Bolin has 100 mg of ecdysterone. I have not seen any human studies with Ecdy Bolin or ecdysterone, so I have no opinion on this supplement at this time.
Q. I always find your articles informative an most
helpful to my Type-1 diabetes. I noticed this comment in one your articles on
20-hydroxyecdysone and helminths and it struck a bell with Type-1 diabetes
resistance due to a Helminth infection. Just wanted to know if you know of any
research in this direction?
A. I have not studied this topic in any great detail.
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