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Epithalon exhibits a broad spectrum of biological activity: it induces telomere lengthening, can slow the aging process, reduce the manifestations of atherosclerosis, and improve cognitive function regardless of age. This peptide also exhibits anticancer activity in animal models. Like epithalamin, epithalon increases melatonin production by the pineal gland, as demonstrated in experiments on aged monkeys and humans. In trials, epithalon influenced nocturnal melatonin production, and its effectiveness was 500 times greater than that of epithalamin. The peptide demonstrated normalization of circadian rhythms of norepinephrine and dopamine production in the hypothalamus.
Epitalon (also known as Epitalon or Epithalamin) is a short synthetic peptide known for its ability to activate the enzyme telomerase and stimulate the release of melatonin. First developed in Russia in the 1980s, epitalon has been shown to slow age-related changes in the reproductive and immune systems, as well as extend the lifespan of mice and rats. Although primarily of interest to anti-aging researchers, epitalon has also demonstrated significant effects on certain types of cancer, infectious diseases, and DNA regulation.
Epitalon is of interest in anti-aging medicine due to its potential benefits:
The Role of Telomerase in the Anti-Aging Effects of Epitalon
Early studies in insects and rodents have shown that epithalon can significantly extend lifespan. In normal, healthy flies and rats, epithalon reduces mortality by 52%. In mice prone to heart disease and cancer, epithalon increases lifespan by 27% compared to control groups.[1] At least part of the answer to how epithalon achieves these significant effects lies in its scavenging of free radicals (charged molecules that damage healthy tissue). However, antioxidant activity is not the only reason epithalon extends lifespan. There is good evidence from in vitro experiments in human somatic cells showing that epithalon activates an enzyme called telomerase.[2] Telomerase protects telomeres, the ends of chromosomes that are critical for maintaining DNA health. Activation of telomerase by epithalon directly results in a reduction in DNA strand errors, supporting the notion that epithalon protects DNA from damage.[3],[4] In short, epithalon protects DNA from the accumulation of errors over time, a process that ultimately leads to cellular dysfunction, aging, and even cancer in some cases.
Epitalon and DNA Activation
Neither its action on free radicals nor its effects on telomeres seem sufficient to explain the profound effects of epithalon on longevity. Indeed, scientists are working diligently to understand how this short peptide achieves these effects so that the mechanisms can be studied in more depth. It turns out that at least part of the answer may lie in epithalon’s alteration of the expression of certain genes. Studies in cell cultures show that epithalon directly interacts with DNA, turning on and enhancing the expression of certain genes. Epithalon interacts with the promoter regions of genes for CD5, IL-2, MMP2, and Tram1[5]. CD5 and IL-2 both influence immune function, while MMP2 plays a critical role in maintaining the extracellular matrix in skin, tendons, and other connective tissues. These findings suggest that epithalon may influence immune function and the body’s ability to recover not only from injury but also from typical everyday stress. It’s not surprising that epithalon affects the immune system. Studies in rats show that epithalon enhances interferon gamma expression in senescent lymphocytes[6]. Interferon gamma is a critical signaling molecule in the immune system. It is important for fighting viral infections by activating macrophages, natural killer cells, and T cells. Epithalon’s known interactions with DNA include:
As mentioned above, epitalon has a positive effect on the gene that regulates MMP2. MMP2 is a protein found in connective tissue, such as skin. Rodent studies show that epitalon not only activates this gene, but also activates fibroblasts, the cells that produce and maintain MMP2, as well as other extracellular matrix components such as collagen and elastin. Mice exposed to epitalon show a 30-45% increase in fibroblast activation [7]. By activating fibroblasts, epitalon may help accelerate healing processes and offset the natural decline in skin structure and integrity that occurs with aging. Further evidence of epitalon’s benefits for skin is that it reduces caspase-3 activity. Caspase-3 is an enzyme involved in the apoptotic pathway, or programmed cell death. By reducing caspase-3 activity, epitalon helps protect fibroblasts and other skin cells, keeping them alive and healthy for longer periods of time[8].
Daily administration of epithalon to rats with cancer has been found to reduce tumor growth.[9] The peptide not only reduces tumor growth, but also prevents these tumors from metastasizing to distant tissues.[10], [11] Epithalon is currently being investigated as a potential treatment for Her-2/neuron-positive breast cancer and is of interest in preventing the development of certain types of leukemia, as well as testicular cancer.[12], [13] There is some evidence that epithalon activates the gene for the PER1 protein, which is found in the hypothalamus. PER1, which helps regulate circadian rhythms, is underexpressed in cancer patients. It is unclear whether this underexpression precedes cancer development and therefore promotes cancer growth, or is a consequence of cancer development. What is clear is that the protein influences cancer growth once cancer is established. Controlling PER1 expression may be one way to naturally slow tumor growth. Studies show that PER1 expression sensitizes cells to the effects of radiation and may therefore help reduce the radiation doses needed to treat certain types of cancer, a fact that would not only reduce immediate side effects but also reduce the occurrence of secondary tumors after high doses of radiation[14].
Melatonin, which is associated with sleep and aging, is produced by the pineal gland. Studies in rats show that epithalon and similar peptides influence both the synthesis and release of melatonin by affecting the expression of two proteins (arylalkylamine-N-acetyltransferase (AANAT) and the pCREB transcription protein)[15]. Both of these genes play important roles in melatonin production and the circadian (day/night) control of its release. Studies in monkeys indicate that epithalon restores normal melatonin secretion.[16]
A study on rats suffering from retinitis pigmentosa showed that Epithalon improved outcomes in 90% of patients [17]. The peptide appears to help maintain normal ocular structure while simultaneously enhancing the retinal bioelectric function necessary for vision. Epithalon exhibits minimal side effects, low oral bioavailability, and excellent subcutaneous bioavailability in mice. The dosage per kilogram of body weight in mice is not proportional to that in humans. Epithalon sold by Pure Peptides is intended for educational and scientific research purposes only, not for human consumption. Purchase Epithalon only if you are a licensed researcher.
1-2 sprays in each nostril in the first half of the day Purity : more than 98% Storage : after opening no more than +5 °C Synonyms : Epitalon, Epithalamin, Epitalon, Epytalamin, AGAG, AEDG
The above literature was researched, edited, and compiled by Dr. E. Logan, MD Dr. E. Logan holds a PhD from Case Western Reserve University School of Medicine and a Bachelor of Science in molecular biology.
| Dose | 20mg, 50mg |
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