Sunday, 9 August 2015

6. skeletal muscle and physical performance

6. skeletal muscle and physical performance

Nucific Bio X4. Protein synthesis


Ecdysterone (under the skin or into a vein), at about 5 mg / kg of body weight seems to be able to carry the protein synthesis in animal organs such as the liver [44] [45] or skeletal muscle. [46] This is likely to increase the efficiency of mRNA translation rather than increasing mRNA synthesis (copying). [38] Moreover, ecdysteroids may be able to increase the integration of lysine in cells at a dose of 5 mg / kg of body weight (Study of the Liver investigation). [47]

In vitro studies on muscle cells observed (20 hydroxyecdysone and turkesterone) statistically significant differences in protein synthesis dose-dependent manner of 0.08nM improvements, peaking at 0.1 nm to 110-120% in the control of protein synthesis and plateauing at concentrations OT 1 and 10 nm. [48] ​​It seems that the mechanism of action to be indirectly through PI3K, also preventing the achievement of PI3K gains inhibitor in muscle mass and grip strength (mice) and metabolism 20 hydroxysterone, rubrosterone, it seems to be as strong as you look in the mouse liver. [44]

In direct comparison studies, and ecdysteroid-called 'Turkesterone' seems to be more robust with respect to other ecdysteroids studied [49] [8] followed by cyasterone then 20 hydroxysterone. [50] [15]

For the control, and increase the growth of mice turkesterone (on mg / day) increased by 63.5%, 51.9% by ecdysterone, 2-deoxyecdysterone by 21.2% and Alpha ecdystone 19.2%. This study used Methylandrostenediol (51.9%) and Nerobol (57.7% equivalent), and vehicles comparison, although the effects were more local Nerobol in skeletal muscle while ecdysteroids increased protein synthesis systemic (body and muscles). [8] Ecdysterones in this study did not suppress or cause prostate or seminal vesicle development, and have no prompt the effects of the uterus in female rats. Increase the weight of the thymus gland also 23-35%, while decreased by 20% with Nerobol. The doses used in this study, 5 mg / kg of body weight for all ecdysteroids and 10 mg / kg of body weight for Methylandrostenediol and Nerobol. [8]

As for the mechanisms of action, they appear to be able to ecydsteroids cause rapid flow of CA2 + in myocytes leading to AKT phosphorylation and thus protein synthesis. [1] This effect occurs after 10 seconds of incubation, and prevent them PI3K inhibitors, as we have seen in other studies, but inhibitors GPCR and PLC. When deplete calcium inside cells phosphoraylized AKT failure cells, free of calcium binding with EGTA down protein synthesis from 16% to 8%. [1] calcium in itself may be an important mediator of AKT and protein synthesis [51], and it seems to work ecdysteroids indirectly through CA2 + and AKT. [52]

This flow of calcium increases the phosphorylation of AKT more than 3 times the concentration of 0.1um, with low dose reponse for up to 5 times in 1-10uM. [1] reached its peak effect in 1 or 20 AKT Hydroxyecdysterone in 2-4 hours, but higher than the baseline for up to 24 hours. [1]

It was also noted in the discussion of the study [17] "tail" of ecdysteroids (γ- Hidroxa- γ-methylpentanoate), when separated from the spine of steroids, so why lysine anabolic metabolism HMB (beta-hydroxy-methyl butyrate).

If ecdysteroids up to the cells, which increases the protein synthesis. Quickly, strongly, and for a long time.

6.2. In laboratory studies and inclusive growth

Vivo studies they have noticed an increase in anabolism in a wide variety of animals such as mice and rats [45] [53] [54] pigs [55] and quail. [56] effects on improving strength and appears to be independent of the activity, according to the assessment of the time and forced to swim in improving the mice without a coherent training. According to [48] Some previous studies (before 2000) that may increase the protein synthesis in humans as well. As it noted [57] improvements in performance in rats. [58]

In sheep, and the oral dose of 0.02mcg / kg in ecdysteroids today able to increase the body's growth and wool production rate [15], and was more pronounced with the poor nutrients. A similar small dose of 0.4 mg / kg of body weight is able to increase nitrogen retention and maintaining lean mass (to 112-116% of control) when food consumption has been reduced by 11 to 17 per cent by the pigs. [55]



7. bone health and joint
Increased alkaline phosphatase activity resulting from Ecdysterone shows through estrogen receptors. [59] Through this future, and the activity of the reporter gene estrogen also increases by ecdysterone.

The increased activity in the expression of type I collagen, osteocalcin, Runx2 and do not speak with each other through the estrogen receptor. [59]



8. interact with hormones

Bio X4. Androgens


At the present time, it has been one human study was conducted only with ecdysterone. Dosed at 200 mg per day, did not observe any results in males of resistance training in total and free testosterone respect of, or change the body composition as compared with placebo. [60] Upon binding to the androgen receptor test, 20-Hydroxyecdysterone seems to have no binding affinity, and therefore can not activate the androgen receptor. [48]

He said, although no effect on testosterone itself ecdisterona may be capable of a similar practice of testosterone through the effects paths signal transfer (although the exact mechanism is still not known); at the end of the day, and work with the same biological such as hormone importance testosterone. [61]

There is little evidence to suggest there is useful for in vitro protein synthesis in muscle and strength gains ecdisterona. [62]


8.2. Estrogen

When tested in the laboratory in C2C12, 1 or 20 hydroxyecdysone (20-HE) increasing the diameter of a central myotube independent manner for the androgen receptor. So estrogen blockers corticosteroids receptors and prevented the 20-HE to promote muscle growth [46] and when I tested seemed more than 20 variables active alpha estrogen receptor (ER; 25.7nM EC50). And beta variables (ERbeta; EC50 13 nm) and 10 nm 20 found to promote muscle growth through ERbeta. [46]

When tested in the laboratory, 20 hydroxyecdysone appears to promote muscle cell hyperplasia because it works on the estrogen receptor beta. It seems that this molecule is also working on the alpha receptor, and when it is the work of each of the receivers at the same time continuing to meet the muscle cell hyperplasia


9. oxidation reactions

9.1. Lipid peroxidation

There Ecdysterone also a protective effect against fat by free radicals peroxide, resulting in a state of antioxidants. [63] It has been observed this effect with a very low dose of 0.1 mg / kg of body weight, it was more effective than vitamin D on a per molecule basis.



10. Peripheral Systems

10.1. Liver

Ecdysterone, 5 mg / kg of body weight, and can restore normal glomerular filtration rate and albuminuria suppression in mice treated with a mixture kidneys [38] and can ease the symptoms of uremia associated with liver damage. [50]

As discussed in the metabolism of fat section, ecdysterone is able to increase the secretion of bile and improve the rates of liver after the renewal of the poison (heliotrine) damage. [38]


10.2. Skin

With regard to the skin, ecdysterone seem able to enhance the keratinocytes differentiation of cells and speed up small wounds and burns when applied externally. [38]



11. Longevity and Life Extension

Bio X4

Ecdysteroids one of the pairs of insect hormones (the other is the youth hormone) which seems to be involved in the lives of insects, with ecdisterona being the agent which increases life expectancy. [64] [65] and transfection of cells with the Drosophila ecdysone receptor than life. [66] However, studies in humans and other animal models are very preliminary.



12. Safety and Toxicology

12.1. Public

Ecdysteroids, in total, they are completely safe for ingestion. The benefits appear to show a dose of 10 mg / kg of body weight, while the established toxicity in mammals (rodents) are kg body / weight 6400mg weight when injected and> 9000mg / kg of body weight when taken by mouth. [42] [41]

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