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Life Extension

Epitalon: The Fountain of Youth

For centuries mankind has searched for the “Fountain of Youth”; that proverbial source of everlasting life. Herodotus wrote of a spring that gave the water of youth to all who bathed in it. Juan Ponce de Leon looked for it in south Florida centuries later but didn’t find it. Man’s quest for such a fountain failed until Dr. Vladimir Khavinson discovered Epitalon in the 1980’s. The fountain turned out to be a peptide produced by the pineal gland [1].

Telomeres
Telomeres resemble the plastic tips on the ends of the shoelace that prevent it from fraying.

There are many theories of aging, one of which is the shortening of telomeres in our DNA. A telomere is like the plastic tip on the end of your shoe lace. It protects the DNA from unraveling during each cell division. Each cell division results in a slightly shorter telomere length, and eventually, the cell can no longer divide. This is called the Hayflick Limit, after Dr. Leonard Hayflick’s discovery that cells have a limited number of times that they can divide.[2] In mammals, the telomeres are protected from shortening until the onset of sexual maturity. After that, they begin to shorten with each cell division, eventually leading to an inability to divide any more in order to replace worn out, damaged or diseased cells. There is an enzyme called telomerase that is produced in the cells which stimulates the lengthening of the telomeres. The pineal gland produces a hormone called epithalamin that tells the cells to produce telomerase which in turn results in longer telomeres in our DNA. The functionality of the pineal gland declines with age, and is partly responsible for age related diseases. [3]

Dr. Vladimir Khavinson
Dr. Vladimir Khavinson
Khavinson V.” by Nikolay bilakOwn work. Licensed under CC BY-SA 3.0 via Commons.

What Dr. Khavinson found was that introducing epithalamin into mammals resulted in a reversal of age related diseases, and a reversal of the signs of aging. He was able to take geriatric female mice, who were no longer fertile, give them epithalamin, and after about two weeks of treatment, the mice became fertile again, got pregnant and had pups.[4] He showed that Epitalon induces telomerase activity in human somatic cells, proving that telomeres were lengthened by the peptide.[5] The synthetic version of epithalamin was patented by Dr. Khavinson and called “Epitalon” (also sometimes called epithalon since the original word is in Russian). It was approved for general use in the Soviet Union in 1990 and has been used in gerontology there ever since. No adverse side effects have ever been reported, according to Dr. Khavinson.

Since Epitalon is patented and trademarked, no drug company will research it. Since drug companies pay for almost all of the research on new medicines, no human clinical trials have been done in the West on it. Almost all of the research has been done by Dr. Khavinson and his associates. The results of his research are startling: for example, the application of Epithalamin diminished mortality in aged humans by 1.8 times over a 6 year period of observation. [6] Here in the West, Epitalon is sold as a research chemical, not approved by the FDA for any purpose, but unregulated for research purposes. Anyone who uses it is considered a “researcher,” in other words.

Epitalon chemical structure

Epitalon is a small peptide of 4 amino acids: Ala-Glu-Asp-Gly and can be administered via injection, as a nasal spray, or through the skin. The most effective route of administering it is via injection, either subcutaneously or intramuscularly. The peptide is typically given 2-3 times a day for 10-20 days in doses of 5-10 mg each. This cycle is repeated once every six to twelve months, but Epitalon can be given as often as desired. There are no negative side effects from the drug ever reported in over 100 studies on the peptide and from clinical use in Russia since 1990. Epitalon works mainly on the endocrine system but has effects on the entire body.[7]


 
When I first started taking it, my sense of smell returned, my digestion improved and I slept better. I have also noted positive changes in my vision and hearing. All of these functions are related to the autonomic nervous system and the endocrine system. Epitalon has been shown to restore normal melatonin production in aging monkeys, as well as restore the normal circadian rhythm for cortisol production, both of which result in better sleep at night.[8]

Epitalon is certainly one of the most interesting anti-aging substance on the market, but further studies are needed to assess the efficacy and safety of telomerase activators.

Epitalon is not approved by the FDA and should not be used to treat or cure any disease.

For more in-depth information about Epitalon check out Epitalon, Part II: Mechanism of Action and the Epitalon’s Facebook group.

References   [ + ]

Categories
Life Extension

Epitalon, Part II: Mechanism of Action

Peptide bioregulators, like Epitalon, Cortexin or Thymalin work via pleiotropic mechanisms, providing support to diverse areas of day-to-day cellular and tissue-related functions. The culmination of these small supportive mechanisms is believed to produce the purported anti-ageing effect of peptide bioregulators and, in particular, Epitalon. In this article, a few central mechanisms contributing to this preserving effect will be highlighted.

Physiology

To begin, peptides are small chains of amino acids (the basic units of organic matter) linked by amide bonds, & can be thought of as «small proteins». Proteins are larger macromolecules comprised of many more amino acids linked together. Despite their size, however, peptides play many important roles in the normal functioning of the human body. Some examples include insulin, which is responsible for controlling levels of glucose within the blood, and substance P, a peptide playing a major role in the perception of pain.

Telomere Elongation

With each cellular replication, the telomeres (in green) are shortened. The maximum number of times that DNA can be replicated is called the Hayflick Limit. Once this number is reached, the cell undergoes apoptosis or programmed cell death. Telomerase is an enzyme which restores telomere length.

Epitalon is a synthetic peptide which were originally developed based upon the action of epithalamin, a hormone produced by the pineal gland. This hormone was found to stimulate the production of telomerase, an enzyme which plays a role in maintaining telomere length. Telomeres are non-coding terminal regions of DNA strands which preserve the integrity of the strand. With each revision, telomeres are shortened until the DNA strand cannot be further replicated. This process is highly implicated in the ageing process. Elongating telomeres theoretically extend the lifespan of a copy of DNA and allows it to replicate more times than usual. This was the theory behind the development of Epitalon®, a synthetic version of epithalamin which also stimulates the production of telomerase. Indeed, this theory has been confirmed in vitro in human cell cultures[1].

Neutralisation of Harmful Free Radicals

The role of antioxidants in mitigating damage from free radicals.

Cytotoxicity secondary to free radical damage has been implicated in the ageing process[2]. Administration of epithalon has also been shown to exert an antioxidant effect[3]. The presence of toxic compounds within the body can lead to the formation of reactive oxygen species (ROS) which can damage DNA, leading to cellular death &/or mutations leading to the formation of cancerous cells.

Inhibition of Cancer Formation & Growth

Maintaining the integrity of the genetic information stored in DNA is one of the mechanisms in which peptide bioregulators work to prevent cancer.

The anti-carcinogenic effect of Epitalon has also been explored in several animal studies. Epitalon has shown beneficial effects in animal models of breast[4] & colorectal cancer[5] without significant rates of adverse effects. Purported mechanisms include inhibition of carcinogenic receptor expression (Human Epithelial growth factor Receptor 2, also known as HER2, which is over-expressed in breast cancer) & retardation of metastasis[6],[7].

Attenuation of Inflammation

fire

Inflammation is a normal immune response that can become dysregulated and potentiated in a broad spectrum of disorders from rheumatoid arthritis to ulcerative colitis and even has been implicated in psychiatric disorders. The inflammatory process is dependent upon intercellular communication mediated by biomolecules such as cytokines, C-reactive protein, and other acute phase reactants[8]. Epithalamin has been observed to play a role in the regulation of these molecules[9] & thus attenuate the inflammatory response[10].

Endocrine Regulation

Hormones released by endocrine glands play signalling roles that coordinate different organs of the body.

Epitalon has been shown to help regulate endocrine activity in the body. Hormones are responsible for many key signalling circuits between cells which on a larger scale comprise the functions of large organs. For example, melatonin is a hormone which regulates the circadian rhythm, an internal biological clock. Endogenous melatonin production has been observed to decrease with ageing. A 2007 study of Epitalon administration in elderly patients found that the compound helped to restore pineal gland function & increased release of melatonin[11], which is purported to be the mechanism behind the restoration of sleep. Other studies have found that Epitalon exerts regulatory effects on gonadotropic hormones (FSG, LG, prolactin), which are involved in sexual & reproductive functions[12].

Summary

These are but a few of the many mechanisms by which Epitalon support normal functioning of the human body, and ultimately produce their anti-ageing effect. Telomerase activation, neutralisation of free radicals, oncostasis, modulation of inflammatory mediators, and endocrine regulation are all ways in which peptide bioregulators can help to ultimately prolong life. Peptide bioregulators as a class are still relatively uncharacterised, and most of the available clinical data are from Russian studies. As interest in this class of drugs grows, more mechanisms of action may be discovered, and the true treatment effects of Epitalon and peptide bioregulators may begin to be better understood.

References   [ + ]

1. Khavinson VK, Bondarev IE, Butyugov AA. Epithalon peptide induces telomerase activity & telomere elongation in human somatic cells. Bull Exp Biol Med. 2003 Jun;135(6):590-2.
2. Hekimi S, Lapointe J, Wen Y. Taking a “good” look at free radicals in the aging process. Trends In Cell Biology. 2011;21(10) 569-76.
3. Anisimov VN, Arutjunyan AV, Khavinson VK. Effects of pineal peptide preparation Epithalamin on free-radical processes in humans and animals. Neuro Endocrinol Lett. 2001;22(1):9-18.
4. Anisimov VN, Khavinson VK, Provinciali M, Alimova IN, Baturin DA, Popovich IG, et al. Inhibitory effect of the peptide epitalon on the development of spontaneous mammary tumours in HER-2/neu transgenic mice. Int J Cancer. 2002 Sep 1;101(1):7-10.
5. Anisimov VN, Khavinson VK, Popovich IG, Zabezhinski MA. Inhibitory effect of peptide Epitalon on colon carcinogenesis induced by 1,2-dimethylhydrazine in rats. Cancer Lett. 2002 Sep 8;183(1):1-8.
6. Kossoy G, Zandbank J, Tendler E, Anisimov V, Khavinson V, Popovich I, et al. Epitalon and colon carcinogenesis in rats: proliferative activity & apoptosis in colon tumors & mucosa. Int J Mol Med. 2003 Oct;12(4):473-7.
7. Kossoy G, Anisimov VN, Ben-Hur H, Kossoy N, Zusman I. Effect of the synthetic pineal peptide epitalon on spontaneous carcinogenesis in female C3H/He mice. In Vivo. 2006 Mar-Apr;20(2):253-7.
8. Owen JA, Punt J, Stranford SA. Immunology. 7th ed. New York: W.H. Freeman & Company; (c) 2013.
9. Labunets IF, Butenko GM, Korkushko OV, Shatilo VB. Effect of epithalamin on the rhythm of immune and endocrine systems functioning in patients with chronic coronary disease. Bull Exp Biol Med. 2007 Apr;143(4):472-5.
10. Khavinson VKh. Peptide regulation of aging. Proceedings of the 17th World Congress of the International Association of Gerontology; Jul 1–6 2001; Vancouver, Canada. Gerontology: 2001; 47(1).
11. Korkushko OV, Lapin BA, Goncharova ND, Khavinson VK, Shatilo VB, Vengerin AA, et al. Normalizing effect of the pineal gland peptides on the daily melatonin rhythm in old monkeys & elderly people. Adv Gerontol. 2007;20(1):74-85.
12. Slepushkin VD, Mordovin VF, Zoloev GK, Iakovleva RA, Khavinson VK. Effect of the epiphysial preparation epithalamin on the gonadotropic function of the hypophysis. Probl Endokrinol (Mosk). 1983 Nov-Dec;29(6):51-4.