Epitalon (also marked as Epithalon) is a synthetic tetra-peptide with amino acid sequence Ala-Glu-Asp-Gly, molecular formula C14H22N4O9 and a molecular weight 390.35 g/mol. Epitalon is derived from Epithalamin (Epithalamine), a naturally occurring polypeptide in the body, which is produced in pineal gland. A very valuable and unique main property of Epitalon is its ability to increase telomerase activity in somatic cells. This helps cells reproduce telomeres, which are the essential “protective parts” of our DNA, which eventually results in a slowdown in the aging process.
In addition, scientific studies have also shown other great possible benefits of Epitalon as prevention of cancer and age-related diseases, restoration and normalization of melatonin levels, promotion of deeper sleep and strong anti-oxidant properties. Epitalon is patented by its discoverer Professor Khavinson and was approved for general use in Russia in 1990 and has since been used in gerontology. Many scientific studies and clinical trials of Epitalon have been conducted in both animals and humans, and no adverse side effects have ever been reported to date.
Mechanism of action of Epitalon
Telomerase activator peptide Epitalon directly stimulates cells in the body to produce a telomerase enzyme, that renew and extends telomeres at the ends of chromosomes. This ultimately leads to a slowing of the aging of cell populations, and the aging of cell populations correlate with the overall physical aging of an organism. Clinical studies conducted with Epitalon have shown that administration of Epitalon to mammals has not only reversed the symptoms of aging but also reversed many age-related diseases. Epitalon has also been shown to help restore and normalize melatonin production by the pineal gland, as well as restoring the normal circadian rhythm of cortisol production, both of which result in better sleep at night.
DNA & Chromosomes
DNA (Deoxyribonucleic acid) is a molecule composed of 2 polynucleotide chains that coil around each other to form a double helix carrying genetic instructions for the development, functioning, growth and reproduction of all known organisms and many viruses. DNA and RNA (Ribonucleic acid) are nucleic acids. Alongside proteins, lipids and complex carbohydrates (polysaccharides), nucleic acids are one of the four major types of macromolecules that are essential for all known forms of life.
Chromosome is a DNA molecule with part or all of the genetic material (genome) of an organism: Within eukaryotic cells (animals, plants, fungi and protists), DNA is organized into long structures called chromosomes. Before typical cell division, these chromosomes are duplicated in the process of DNA replication, providing a complete set of chromosomes for each daughter cell. Eukaryotic organisms store most of their DNA inside the cell nucleus as nuclear DNA, and some in the mitochondria as mitochondrial DNA or in chloroplasts as chloroplast DNA.
Telomere is important region of repetitive nucleotide sequences at each end of a chromosome, which protects the end of the chromosome from deterioration or from fusion with neighboring chromosomes. However, as a result of each cell division, the ends of the telomeres are shortened: During chromosome replication, the enzymes that duplicate DNA cannot continue their duplication all the way to the end of a chromosome, so in each duplication the end of the chromosome is shortened (this is because the synthesis of Okazaki fragments requires RNA primers attaching ahead on the lagging strand). This means, each cell division (each time a cell undergoes mitosis), the telomeres on the ends of each chromosome again shorten. After many divisions, the telomeres reach a critical length, resulting in the cell eventually losing its ability to divide further to replace worn, damaged or diseased cells. Further cell division becomes impossible and the cell becomes senescent. At this point, the cell reached its so-called Hayflick limit.
The Hayflick limit
The Hayflick limit, or Hayflick phenomenon, is the number of times a normal human cell population will divide before cell division stops. The concept of the Hayflick limit was advanced by American anatomist Leonard Hayflick in 1961, at the Wistar Institute in Philadelphia, Pennsylvania, United States. Hayflick demonstrated that a normal human fetal cell population will divide between 40 and 70 times in cell culture before entering a senescence phase. The aging of cell populations appears to correlate with the overall physical aging of an organism.
Hayflick was also the first to report that only cancer cells are immortal. Cellular senescence does not occur in most cancer cells due to expression of an enzyme telomerase, when telomerase extends telomeres / preventing the telomeres of cancer cells from shortening and by this way giving them infinite replicative potential. One of the proposed treatment for cancer is the usage of telomerase inhibitors in the cancer cells, that would prevent the restoration of their telomeres, and allows the cancer cells to die like other body cells.
Telomerase is a ribonucleoprotein that adds a species-dependent telomere repeat sequence to the 3′ end of telomeres. It is a reverse transcriptase enzyme that carries its own RNA molecule (e.g., with the sequence 3′-CCCAAUCCC-5′ in Trypanosoma brucei) which is used as a template when it elongates telomeres. Telomerase is active in gametes and most cancer cells, but is normally absent from, or at very low levels in, most somatic cells.
Telomerase restores short bits of DNA known as telomeres, which are otherwise shortened when a cell divides via mitosis. In normal circumstances, where telomerase is absent, if a cell divides recursively, at some point the progeny reach their Hayflick limit, which is believed to be between 40–70 cell divisions. At the limit the cells become senescent and cell division stops.
But Telomerase allows each offspring to replace the lost bit of DNA, allowing the cell line to divide without ever reaching the limit – allowing senescent cells that would otherwise become postmitotic and undergo apoptosis to exceed the Hayflick limit and become potentially immortal, as is often the case with cancerous cells.
Embryonic stem cells express telomerase, which allows them to divide repeatedly and form the individual. In adults, telomerase is highly expressed only in cells that need to divide regularly, especially in male sperm cells but also in epidermal cells, in activated T cell and B cell lymphocytes, as well as in certain adult stem cells, but in the great majority of cases somatic cells do not express telomerase.
The pineal gland is a small endocrine gland in the brain of most vertebrates. It is located in the epithalamus, near the center of the brain, between the two hemispheres, tucked in a groove where the two halves of the thalamus join. The pineal gland is one of the neuroendocrine secretory circumventricular organs in which there does not exist the blood–brain barrier at the capillary level.
The primary function of the pineal gland is to produce Melatonin, that has various functions in the central nervous system, the most important of which is to help modulate sleep patterns. The pineal gland also produces polypeptide Epithalamin, that stimulates cells in the body to produce a telomerase enzyme, that extends telomeres at the ends of chromosomes in their DNA. This ultimately leads to a slowing of the aging of cell populations.
Epitalon was discovered and developed by the Russian scientist and gerontologist Professor, Doctor of Medical sciences Vladimir Khavinson of St. Petersburg Institute of Bioregulation and Gerontology, whose research is focused on the development of peptide preparations used to restore function in various organs in order to prevent and reverse the aging process. Epitalon was identified as active component of a bovine pineal gland extract (known as Epithalamin).
Low-molecular peptides isolated from pineal gland and Epithalamin of animals were studied in different biologic models. Most all performed scientific studies and clinical trials of Epitalon and Epithalamin have been conducted just by already mentioned St. Petersburg Institute of Bioregulation and Gerontology in Russia, primarily overseen by Professor Vladimir Khavinson, who has been involved in this research already for over 35 years, and has merit not only in the discovery of epitalon, but also in its highly advanced scientific and clinical review. Throughout this time, Epitalon has been extensively investigated in animal and human clinical trials and today is one of the best scientifically investigated peptides.
Scientific studies, clinical trials and Epitalon results
Scientific studies in animals:
An in vivo study in aging mice found that epitalon treatment significantly reduced the incidence of chromosomal aberrations, both for wild-type mice and for mice characterized by an accelerated aging phenotype, which is consistent with increases in telomere length.
Another study in aging rats found that epitalon increased the activities of the antioxidant enzymes superoxide dismutase, glutathione peroxidase, and glutathione-S-transferase. In male rats, epithalamin increased total antioxidant capacity by 36% and superoxide dismutase (SOD, a powerful endogenous antioxidant) by 19%. Oxidative stress, which occurs when the body has a deficit in antioxidants to counteract the effects of free radicals (damaging molecules that are missing electrons), plays a causative role in many diseases, including heart disease, cancer, diabetes, and even neurodegenerative diseases such as Alzheimer’s and Parkinson’s diseases. One of the most potent endogenous antioxidants produced by the body is Melatonin. Epitalon’s antioxidant effects are thought to be in part due to its ability to stimulate Melatonin production as well as mechanisms other than through the action of Melatonin.
Epitalon reduced the number of spontaneous tumors and the number of metastases in mice that did develop spontaneous tumors in an experiment on one-year-old female C3H/He mice, and is speculated to have oncostatic and anti-metastatic properties.
In a study of chickens subjected to neonatal hypophysectomy and subsequent maturation, epitalon promoted the recovery of the morphological structures of the thymus, as well as the structure and function of the thyroid gland. Epitalon appears to increase the proliferation of lymphocytes in the thymus, putatively increasing production of interferon gamma by T-cells. Another study in aging rats demonstrated extension of life span for rats subjected to constant illumination or to a natural light regimen typical of northern regions.
Scientific studies in humans:
In human clinical studies, epitalon and epithalamin both significantly increased telomere lengths in the blood cells of patients of ages 60-65 and 75-80, and their efficacy was comparable to one another.
Epitalon and epithalamin appear to restore melatonin secretion by the pineal gland in both aged monkeys and humans.
A human clinical trial conducted on a sample of retinitis pigmentosa patients found that epitalon produced a positive clinical effect in 90% of cases in the treated group.
In another human clinical trial conducted on a sample of pulmonary tuberculosis patients, epitalon did not appear to correct pre-existing structural aberrations of chromosomes associated with telomere degradation, but did appear to exert a protective effect against the future development of additional chromosomal aberrations.
A human prospective cohort study conducted on a sample of 266 people over age 60 demonstrated that treatment with epithalamin, the pineal gland extract upon which epitalon is based, produced a 1.6–1.8-fold reduction in mortality during the following 6 years, a 2.5-fold reduction in mortality when combined with thymulin, and a 4.1-fold reduction in mortality when combined with thymulin and administered annually instead of only once at study onset.
Another prospective cohort study on a sample of 79 coronary patients spanning in excess of 12 years found improved metrics of physical endurance, circadian rhythm, and carbohydrate and lipid metabolism in the treated group relative to the control group following 3 years of biannual epithalamin treatments, as well as a 50% lower rate of cardiovascular mortality, a 50% lower rate of cardiovascular failure and serious respiratory disease, and a 28% lower rate of overall mortality.
Elongation of telomeres by epitalon was sufficient to surpass the Hayflick limit in a cell culture of human fetal fibroblast cells, extending their proliferative potential from termination at the 34th passage in the control cell population to beyond the 44th passage in the treated cell population, while increasing the lengths of their telomeres to levels comparable to those of cells in the original culture.
Epitalon induces decondensation of heterochromatin near the centromeres in cultured lymphocytes originating from samples taken from humans of ages 76 to 80 years.
Epitalon appears to inhibit the synthesis of the MMP9 protein in vitro in aging skin fibroblasts.
Scientifically investigated possible benefits of Epitalon
Slows the aging of cell populations by stimulating the renew and elongation of telomeres at the ends of chromosomes in DNA
Slowing of aging / anti-aging effect, rejuvenation
Prevention of cancer and age-related diseases
Restores and normalizes Melatonin production by the Pineal gland
Strong anti-oxidant properties, protects against oxidative stress, act against the effects of free radicals
Increases the activities of the antioxidant enzymes superoxide dismutase, glutathione peroxidase, and glutathione-S-transferase
Reduces lipid oxidation and ROS (reactive oxygen species) together with normalization of T cell function (increases interferon gamma production by T cells)
Better, deeper sleep and its quality
Improves metrics of physical endurance, circadian rhythm, and carbohydrate and lipid metabolism
Healthier skin, inhibits the synthesis of the MMP9 protein in vitro in aging skin fibroblasts
Positive clinical effect in Retinitis pigmentosa disease
Epitalon possible side-effects
Performed scientific studies and clinical trials to date have not shown any significant side, undesirable or toxic effects when investigating the Epitalon peptide.
What is Epitalon used for?
Epitalon is used for increase the natural production of telomerase, a natural enzyme that helps cells reproduce telomeres, which are the protective parts of our DNA. This ultimately leads to a slowing of the aging of cell populations, and the aging of cell populations correlate with the overall physical aging of an organism. However, epitalone can also be used to restore and normalize melatonin levels or to protect against cell oxidative stress.
Can Epitalon slow down aging?
Scientific research and performed clinical trials have demonstrated Epitalon slows the aging and has strong anti-aging properties.
Can Epitalon prevent cancer?
Yes, Epitalon has the ability to prevent cancer.
Can Epitalon improve sleep?
Yes, Epitalon supports and normalize production of Melatonin, which leads to a better and deeper sleep.
How do you administer Epitalon?
Epitalon is usually administered by intravenous, intramuscular or transdermal / subcutaneous (under the skin, through the skin) injection. Oral administration is not effective because the peptides are broken down / cleaved in the gastrointestinal tract. This means: They cannot pass through the gastrointestinal tract in functional and intact state, up to the bloodstream to exert their effects.
Where can I buy Epitalon?
We offer Epitalon of the highest purity for bargain price.
Does Epitalon have side effects?
Clinical trials to date have not shown any significant side, undesirable or toxic effects when Epitalon was used.
In the scientific studies and clinical trials performed, the optimal dose of Epitalon is often reported as 5 – 10 mg daily, over a period of 10-20 days. The frequency of administration is one injection per day at lower doses and two injections per day at higher doses, which may be divided between morning and evening. Each course of use should be followed by a pause of 4-6 months before the course is repeated.
Synthetic tetra-peptide Epitalon is an activator of telomerase production. Telomerase helps cells renew telomeres, which are the essential “protective parts” of our DNA, which eventually results in a slowdown in the aging process. Epitalon was discovered and developed by the Russian scientist and gerontologist Professor, Doctor of Medical sciences Vladimir Khavinson of St. Petersburg Institute of Bioregulation and Gerontology. Epitalon has been extensively investigated in animal and human clinical trials. Scientific research and performed clinical trials have demonstrated Epitalon slows the aging of cell populations, has strong anti-aging effect and anti-oxidant properties, helps protect against cancer and age-related diseases, normalizes Melatonin production by the Pineal gland and provides quality sleep.