Ecdysteroids: A novel class of anabolic agents?
Arch Insect Biochem Physiol. The percentage of trabecular area in the metaphysis of tibia was significantly increased in Ecd and E 2 treated animals. Abstract Increasing numbers of dietary supplements with ecdysteroids are marketed as "natural anabolic agents". Anabolic effect of ecdysterone Ecdy expressed as fiber size of soleus muscle in intact rats. Showing of 5 extracted citations. Piperine downregulates enzymes that eliminate bioactive compounds from the body, so their bioavailability is enhanced.
The control groups were injected with vehicle only. The animals were handled in compliance with accepted veterinary medical practice and with the approval of the Animal Welfare Committee. Further experimental details were performed as described earlier [ 2 ]. The anabolic potency of ecdysterone was determined using the muscle fiber size of the soleus muscle of male Wistar rats as measure.
The effect was compared to the anabolic androgenic steroids metandienone dianabol and estradienedione trenbolox as well as the selective androgen receptor modulator S-1 chemical structures in Figure 1. These crystal structures represent complexes with estradiol for the ER and testosterone for the AR to make sure they represent the protein conformation relevant for agonism. The docking experiment was performed using the software GOLD [ 19 ] allowing side chain flexibility in the binding regions to allow adaptions to the significantly larger ligand ecdysterone.
Binding poses were analyzed for key interaction features using the 3D pharmacophore modeling platform LigandScout [ 20 , 21 ]. Statistical data evaluation was performed by Kruskal—Wallis test followed by pair-wise comparison with the Mann—Whitney U-test. Box and whisker plots in Figure 2 and Figure 3 represent minimum, 25 th , 50 th median , 75 th percentile, and maximum of the distribution.
C2C12 derived myotubes were used as in-vitro model for testing anabolic activities. Incubation with ecdysterone showed significantly increased myotube diameters compared to vehicle treated control cells Figure 2. Comparing the effect with the endogenous anabolic androgenic steroid dihydrotestosterone at the same concentration and the anabolic growth factor IGF-1 concentration for comparison was 1.
To mimic the situation in athletes, intact male Wistar rats were treated with the test components for 21 days. Significantly increased fiber sizes of the soleus muscle were determined following treatment with ecdysterone. Comparison with the animals treated with the anabolic androgenic steroids metandienone or estradienedione and the SARM S-1 yielded a significantly higher effect in the ecdysterone treated animals when the same doses were applied Figure 3.
At those positions where methyl groups are found for the endogenous ligand testosterone, hydroxyl groups sterically interfere with the receptor in case of ecdysterone.
In addition, a water molecule mediating important interaction in the testosterone complex is replaced by a methyl group for the ecdysterone docking pose resulting in an unfavorable interaction pattern.
In contrast, both ER isoforms offer a binding side shape more suitable to accommodate ecdysterone. Docking poses in both subtypes share several interactions shown in Figure 4. The data reported in here demonstrate that ecdysterone induces hypertrophy of muscles with a comparable or even higher potency as shown for anabolic androgenic steroids, SARMs or IGF Analogous findings were also reported by Syrov et al. An anabolic activity of ecdysterone was clearly confirmed by our investigation.
Moreover in-silico docking experiments support the postulated non-androgenic mechanism of ecdysterone. More likely and in agreement to the experimental data anabolic activity of ecdysterone is mediated via binding to the ER particularly ER beta. The authors declared no conflict of interests regarding the publication of this manuscript.
The snippet could not be located in the article text. This may be because the snippet appears in a figure legend, contains special characters or spans different sections of the article. Published online March This article has been cited by other articles in PMC. Chemical structure of ecdysterone A as well as of the other anabolic agents used for comparison B: Statistics Statistical data evaluation was performed by Kruskal—Wallis test followed by pair-wise comparison with the Mann—Whitney U-test.
Determination of diameters of 47 myotubes per group. Anabolic effect of ecdysterone Ecdy expressed as fiber size of soleus muscle in intact rats. Conflict of interests The authors declared no conflict of interests regarding the publication of this manuscript. Anabolic effect of ecdysterone results in hypertrophy of C2C12 myotubes by an estrogen receptor mediated pathway.
Recent Advances in Dope Analysis 20 Cologne: Stress-protective properties of phytoecdysteroids. In the liver of stressed animals, phytoecdysteroids prevented sharp decrease in the glycogen concentration, showed a clear trend toward normalization of the ratio of lactic and pyruvic acids, maintained homeostasis of macroergic phosphorus compounds, and increased the activity of antioxidant enzymes that inhibit lipid peroxidation. With respect to the stress-protective activity, the studied phytoecdysteroids are in some cases superior to eleutherococcus extract.
Ecd reduced caspase 3 activity. Ecdysterone promotes wound healing in rabbits. Ecdysterone can obviously promote wound healing in rabbits, which may offer a clinical alternative for promoting wound healing. Ecdysterone and its activity on some degenerative diseases.
The most interesting of these is that on degenerative diseases, one of which, up to now not clarified in detail, is 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 is the possibility of suppression of neurodegenerative processes and protection of the cardiovascular system metabolic syndrome symptom suppression, antidiabetic activity, and protection of heart and blood vessels.
Ecdysteroid induction of sex pheromone biosynthesis in the housefly, Musca domestica—Are other factors involved? These results show that juvenile hormone neither induced nor modified sex pheromone production in the housefly. Ecdysteroids or their agonist, by themselves, induce sex pheromone production in the housefly.
In pigs, doses of 0. Indeed it stimulates muscle growth , provided that protein supply is adequate. Such anabolic effects result in increased physical performance without training Chermnykh et al. This was for instance demonstrated using the forced swimming test with rats: Wound-healing effects of ecdysteroids have been described. It was shown early on that 20E given per os to rats reduces hyperglycaemia induced either by glucagon or by alloxan treatment.
In fact, 20E stimulates the incorporation of glucose into glycogen and protein in mouse liver and more generally it enhances glucose utilization by tissues. The mechanism involved seems to be an increase of tissue sensitivity to insulin and preparations containing phytoecdysteroids have been proposed as oral antidiabetics. Ecdysteroids display hypocholesterolaemic effects , through a reduction of cholesterol biosynthesis and an increase of its catabolism.
In connection with these effects, ecdysteroids may also have antiatherosclerotic actions. Ecdysteroids are not toxic to vertebrates: Du kommentierst mit Deinem WordPress. Du kommentierst mit Deinem Twitter-Konto. Du kommentierst mit Deinem Facebook-Konto. Benachrichtigung bei weiteren Kommentaren per E-Mail senden.
Chinesische Medizin Traditionelle und moderne Heilkunde. A novel class of anabolic agents? Estrogen receptor beta is involved in skeletal muscle hypertrophy induced by the phytoecdysteroid ecdysterone.
Adipositas Metabolic effects of OH-ecdysone in ovariectomized rats. Diabetes Estimation of the hypoglycemic effect of phytoecdysteroids A series of phytoecodysteroids, including alpha-ecdysone, 2-deoxy-alpha-ecdysone, and 2-deoxyecdysterone isolated from Silene praemixta, integristerone A and ecdysterone isolated from Rhaponticum carthamoides and acetylcyasterone and turkesterone isolated from Ajuga turkestanica, exhibit a pronounced hypoglycemic effect in experiments on intact male rats.
Klimakterium Metabolic effects of OH-ecdysone in ovariectomized rats.
Iamges: ecdysteroids a novel class of anabolic agents
J Nutr Biochem, Piperine inhibits cytochrome P enzymes, which play essential roles in the elimination of many compounds. Comparison with the animals treated with the anabolic androgenic steroids metandienone or estradienedione and the SARM S-1 yielded a significantly higher effect in the ecdysterone treated animals when the same doses were applied Figure 3.
Docking poses in both subtypes share several interactions shown in Figure 4.
Journal of Animal and Veterinary Advances, It was shown early on that 20E given per os to rats reduces hyperglycaemia induced either by glucagon or by alloxan treatment. J Nutr Biochem, Natural Anabolic anabolic steroids dianabol uk Androgenic Complex Increase muscle ecdysteroids a novel class of anabolic agents and size Improve protein synthesis and ecdysetroids. According to our results 20E may provide an alternative for substitution of anabolic-androgenic steroids in therapeutic treatments against muscle atrophy. Syrov Pharmaceutical Chemistry Journal