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Epithalon (also known as Epitalon) is a synthetic derivative of Epithalamin and holds the potential to modulate telomerase, the enzyme responsible for safeguarding and preserving the telomere caps situated at the ends of DNA chromosomes. This effect directly protects the DNA and prevents errors.
Scientists also showed it regulates the function of pineal gland and the retina as it induces cell differentiation and has a profound effect on gene expression and protein synthesis in animals.
References:
Khavinson VKh, Bondarev IE, Butyugov AA. Epithalon peptide induces telomerase activity and telomere elongation in human somatic cells. Bull Exp Biol Med. 2003 Jun;135(6):590-2. doi: 10.1023/a:1025493705728. PMID: 12937682.
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Epithalon, also known as Epitalon or Epithalone, is a synthetic tetra-peptide with the structure Ala-Glu-Asp-Gly. The peptide was developed based on a naturally occurring peptide produced in the pineal gland of the brain called epithalamin.
Epithalon exhibits potential anti-aging properties and has been studied for possible health benefits. A study on rats showed that it extended their life and delayed age-related degenerative changes in both the immune and reproductive systems.
Even though their primary focus was on anti-aging research, researchers reported other benefits in this study, benefits ranging from condition improvements in some types of cancers, infectious diseases and DNA regulation.
Epithalon and Anti-Aging Effects
Research using insects and rodents proved that epithalon can extend life. Research in fruit flies, mice, and rats has also shown promising results.
This research found that epithalon reduced mortality rate by as much as 52% in normal healthy fruit flies and rats! It’s also proven that epithalamion stimulates the synthesis and secretion of melatonin in rats and inhibits free radical production in rats and fruit flies. These antioxidative properties help enhance the lifespan of the three kinds of animal test subjects we mentioned.
Epithalon and DNA Activation
Understanding the effects of epithalon on longevity and extending lifespan needs more scientific investigation.
Research in cell cultures implies that epithalon interacts directly with DNA to turn on and enhance the expression of certain genes. As cell research has proven, Epithalon interacts directly with DNA with the promoter regions of CD5, IL-2, MMP2 and Tram1 genes to increase their expression.
CD5 and IL-2 both affect the immune system, while MMP2 helps in maintaining the extracellular matrix in skin, tendons and other connective tissue. Because of this we can assume that peptides affect immune response, and the ability of the body to heal itself.
It’s safe to say that epithalon has an impact on the immune system. Research in rats implies that epithalon boosts the expression of interferon gamma in aging lymphocytes. Interferon gamma is very important for fighting off infections through the activation of macrophages, natural killer cells, and T cells.
Epithalon and Skin Cell Regeneration
As we already discussed, epithalon has a positive effect on the gene that regulates MMP2. MMP2 is found in the skin that regulates this protein; even other components, such as collagen and elastin, are activated.
The impact on organotypic skin cell cultures proliferation in young and old animals were also investigated. Young and old rats exposed to epithalon had stimulated skin fibroblast proliferation by up to 29-45%. So it's clear that the peptide is helping by activating fibroblasts in order to increase the speed of skin healing and to compensate for the processes in the structure and integrity of the skin that often occurs during aging.
Another proof of epithalon’s benefit for the skin is the fact that it decreases caspase-3 activity.Caspase-3 is a critical enzyme in the process of apoptosis, which is the programmed cell death essential for the development and maintenance of healthy tissues. By decreasing it, the epithalon helps protect fibroblasts and other skin cells, keeping them alive and healthy for long periods.
Epithalon and Tumorigenensis
Daily administration of Ephitalon to rats with cancer has been investigated due to tumor growth and its effect on lifespan in different illumination regimes. As it turns out, the peptide not only reduces tumor growth but also prevents metastasis.
Epithalon is being researched as a potential drug for the treatment of Her-2/neu positive breast cancer and also the development of certain types of leukemia and testicular cancer. Epithalon not only decelerates aging, but it also suppresses the growth of breast adenocarcinomas in transgenic Her-2/neu.
One experiment showed that rats that got peptide injections five times a week, experienced suppressed formation of neoplasms, decreased lung metastases by 1,6 times, multiple tumors by two times, 3,7-fold increase of mice without breast tumors and decrease of mice with 6 or more tumors by three times.
There Is evidence that epithalon activates the gene for the PER-1 protein, which is found in the hypothalamus. PER1 affects cancer growth and causes an increased rate of ionizing radiation-induced cell death. However, it is unknown whether its lack of expression precedes and contributes to cancer development or is the only source of cancer.
Melatonin Secretion and Epithalon Influence
The hormone Melatonin, which is produced by the pineal gland, can be linked with aging and sleep. Experiment done on rats showed that epithalon and similar peptides affect both the synthesis and release of melatonin by affecting the expression of two proteins arylalkylamine-N-acetyltransferase (AANAT) and the transcriptional protein pCREB.
Both play a very important role not only in the production of melatonin but also in the circadian control of its release during the day and night. Additional research done on monkeys shows that epithalon restores melatonin production to normal rates. Because of disorders in the pineal gland in elderly age in monkeys and humans, melatonin release decreases.
Epithalon and Eyesight
Epithalon can also help maintain and improve normal structure of the eye retina condition while also improving the bioelectric and functional activity of the retina due to the preservation of its morphological structure.
A study done on rats suffering from retinitis pigmentosa found that epithalon improves outcomes in 90% of patients. As it turns out, the peptide helps to preserve normal structure of the eye while also boosting the bioelectric function of the retina which is necessary for vision.
References:
- https://pmc.ncbi.nlm.nih.gov/articles/PMC7037223/
- https://pubmed.ncbi.nlm.nih.gov/14501183/
- https://www.sciencedirect.com/science/article/abs/pii/S0047637400002177
- https://www.researchgate.net/publication/9087984_Effect_of_Epitalon_on_biomarkers_of_aging_life_span_and_spontaneous_tumor_incidence_in_female_Swiss-derived_SHR_mice
- https://www.sciencedirect.com/science/article/abs/pii/S0304383502000903
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