Epithalon, or Epitalon, is a small synthetic peptide that appears to activate the telomerase enzyme and may promote the release of melatonin. Experimental research has suggested its potential to slow alterations in reproductive and immune systems and improve the life span of mice and rats.[1] Apart from its potential in regulating cell aging, the peptide also has played an important role in research conducted upon certain classes of cancer, infectious diseases, and DNA regulation.
OTHER KNOWN TITLES: Epitalon, Epithalone, Epithalamin
MOLECULAR FORMULA: C14H22N4O9
MOLECULAR WEIGHT: 390.35 g/mol
SEQUENCE: Ala-Glu-Asp-Gly
EPITHALON AND CELL AGING
Early research on insect and rodent models hypothesized that Epithalon may improve cell span to a significant extent. Studies in rats indicated a 52% decrease in mortality upon Epithalon exposure. It appears to have been impactful in mice models of cardiac disease, where the life expectancy was reported to be increased by 27% compared to control animals. The peptide has been observed to mediate action through eliminating free radicals (charged molecules that damage tissue). Apart from studies its anti-oxidant activity, Epithalon has also been studied for its potential to activate an enzyme called telomerase in cell culture assays. Telomerase preserves the ends of chromosomes known as telomeres, which are crucial for maintaining the integrity of DNA. Epithalon has the potential to preserve the DNA from damage by activating the telomerase and decreasing the number of errors in the DNA strands.
EPITHALON AND DNA ACTIVATION
Epithalon is being researched actively to explore the various mechanisms by which this peptide mediates longevity. One of such pathways is the regulation of certain gene expressions.[2] Studies using cell culture have noted that the peptide appears to directly interact with promoter regions of certain genes such as Tram1, IL-2, CD5, and MMP2 and may also enhance their expression. CD5 and IL-2 are both involved in operations of the immune system, while MMP2 is considered to play a role in the maintenance of extracellular matrix in tendons, skin, and other connective tissue. Epithalon appears to trigger interferon-gamma synthesis from aging lymphocytes in rats. Interferon-gamma is a relevant signaling molecule of the immune system and helps prepare the animal for combating viral infections through T lymphocyte, macrophage, and natural killer cell activation.
EPITHALON AND EXTRACELLULAR MATRIX (SKIN ECM)
Experimental research suggests Epithalon’s potential to induce MMP2 expression. MMP2 is a protein found in connective tissue like skin. Research in rodents indicates that apart from activation of MMP2, the peptide may also activate fibroblasts which produce and maintain MMP2 as well as other components of the extracellular matrix such as collagen and elastin. Mice exposed to Epithalon exhibited 30-45% higher activation of fibroblasts than controls.[3] Epithalon also appears to inhibit the activity of Caspase-3, a key enzyme that promotes apoptosis or programmed cell death.
EPITHALON AND TUMOR GROWTH
Daily exposure to the peptide in rat models of cancerous tumors, reported a reduction in tumor growth with the burden apparently diminishing the metastasis of the cells to distant tissues. Epithalon is currently under research for its interaction in Her-2/neu positive breast cancer, testicular cancer, and certain types of leukemia. There is scientific research associating the peptide with the activation of PER1 protein produced in the hypothalamus.[4] The gene is involved in the regulation of the circadian rhythm and is considered to be under-expressed in cancer instances. PER1 has been suggested to influence cancer progression once cancer is established. Control of PER1 expression may potentially be employed for the reduction in tumor growth. PER1 expression in cells appears to sensitize cancer cells to radiation. This is considered to exhibit a two-fold action. It may not only bring about a decrease in tumor size and burden and decrease radiation, but also minimize the chances of secondary tumors from extensive radiation. Research is ongoing.
EPITHALON AND MELATONIN SECRETION
Melatonin is an hormone produced from the pineal gland, and it is considered to regulate sleep cycles. Studies on rats have suggested Epithalon and similar peptides may potentially regulate the synthesis and secretion of melatonin by influencing the expression of two proteins; arylalkylamine-N-acetyltransferase (AANAT) and pCREB transcription protein.[5] These genes are involved in melatonin production and the circadian (day/night) control of release of the hormone. Research in monkeys observed that Epithalon may potentially restore normal physiological levels of melatonin.
EPITHALON AND VISION
Epithalon has been studied in rat models of retinitis pigmentosa. These studies reported that the peptide appeared to improve the outcome in 90% of the cohort. Generally, research in Epithalon has suggested its potential to preserve the overall structure of the eye as well as boost the bioelectric function of the retina important for proper vision.
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