Molecular Formula: C14H22N4O9
Molecular Weight: 390.35 g/mol
PubChem: CID 219042
CAS Number: 307297-39-8
What Is Epithalon peptide?
Epithalon (also known as Epitalon, Epithalone, or Epithalamin) is a small synthetic peptide that activates the telomerase enzyme and promotes the release of melatonin. It was first developed in Russia in the 1980s and has been shown to slow down age-related alterations in reproductive and immune systems and improve the life span of mice and rats. Apart from its prominence in regulating aging, the peptide also has played an important role in certain classes of cancer, infectious diseases, and DNA regulation.
1. The Role of Telomerase in the Anti-Aging Effects
Early research on insect and rodent models revealed that epithalon could help improve life span to a significant extent. Normal, healthy fruit flies and rats show a 52% decrease in mortality upon epithalon treatment. It is effective even in mice suffering from both cardiac disease and cancer, wherein the life expectancy is increased by 27% compared to control animals. The peptide has been observed to mediate its effect by eliminating free radicals (charged molecules that damage healthy tissues).
Apart from its anti-oxidant activity, epithalon has been observed 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 preserves the DNA from damage by activating the telomerase, decreasing the number of errors in the DNA strands. Thus, the peptide protects DNA from accumulating errors over time, which often leads to cellular dysfunction, cancer, and aging.
2. DNA Activation
Epithalon is being researched actively to explore the various mechanisms by which this wonder peptide mediates longevity. One of such pathways is the regulation of certain gene expressions.
Studies using cell culture have highlighted that the peptide directly interacts with promoter regions of certain genes such as Tram1, IL-2, CD5, and MMP2 and enhances their expression. CD5 and IL-2 are both involved in operations of the immune system, while MMP2 plays a critical role in the maintenance of extracellular matrix in tendons, skin, and other connective tissue. Thus the drug boosts immune system function and the ability of the body to heal both from injury and everyday stress and wear and tear.
Epithalon triggers interferon-gamma synthesis from aging lymphocytes in rats. Interferon-gamma is a relevant signaling molecule of the immune system and helps prepare the body for combating viral infections through T lymphocyte, macrophage, and natural killer cell activation.
The following are known DNA interactions of epithalon:
– CD5 – Leads to immune cell differentiation
– pCREB t – Circadian rhythm regulation and anti-neoplastic effects
– IL-2 – Increases IL-2 production, which modulates white blood cells
– Arylalkylamine-N-acetyltransferase – Increases melatonin production
– MMP2 – Enhances MMP activation and reduces inflammation
– Telomerase – Telomerase activity improves cell longevity
– Tram1 – Improves protein production
3. Epithalon peptide and Skin Health
As mentioned above, epithalon induces MMP2 expression. MMP2 is a protein found in connective tissue like skin. Research in rodents indicates that apart from activation of MMP2, the peptide also activates fibroblasts which produce and maintain MMP2 as well as other components of the extracellular matrix such as collagen and elastin. Mice treated with epithalon show 30-45% higher activation of fibroblasts. The activated fibroblasts improve wound healing and help to decrease the natural aging of the skin.
Epithalon also inhibits the activity of Caspase-3, a key enzyme that promotes apoptosis or programmed cell death. The peptide thus ensures the longevity of fibroblasts and other skin cells by inhibiting their apoptosis and thus keeping the skin young and healthy.
4. Epithalon and Tumor Growth
Daily administration of the peptide on rats suffering from cancer reduces tumor growth and burden and diminishes the metastasis of the cells to distant tissues. Epithalon is currently investigated for the treatment of Her-2/neu positive breast cancer, testicular cancer, and certain types of leukemia.
There is scientific evidence associating the peptide with the activation of PER1 protein produced in the hypothalamus. The gene is involved in the regulation of the circadian rhythm and happens to be under-expressed in cancer patients. Interestingly, it is unknown whether the gene is a cause or effect of neoplastic development. PER1 has been observed to influence cancer progression once cancer is established. Control of PER1 expression can be utilized for the reduction in tumor growth. PER1 expression in cells happens to sensitize cancer cells to radiation therapy. This has two-fold effects. It not only brings about an immediate decrease in tumor size and burden and thereby decreases the radiation dose but also minimizes the chances of secondary tumors from extensive radiation therapy.
5. Melatonin Secretion
Melatonin is an important hormone produced from the pineal gland, and it regulates sleep and aging. Studies on rats have shown epithalon and similar peptides to regulate the synthesis and secretion of melatonin by influencing the expression of two proteins (arylalkylamine-N-acetyltransferase (AANAT) and pCREB transcription protein). These genes are involved in melatonin production and the circadian (day/night) control of release of the hormone. Research in monkeys shows that epithalon also restores the normal physiological level of melatonin.
6. Epithalon and Eyesight
Epithalon has been used in rats to treat a condition known as retinitis pigmentosa. The peptide has been found to improve the outcome in 90% of the cohort. To conclude, epithalon helps preserve the overall structure of the eye as well as boosts the bioelectric function of the retina important for proper vision.
Epithalon exhibits minimal adverse effects and low oral and amazing subcutaneous bioavailability in mice. The dose used in mice (per kg) does not scale to humans.