Epithalon (25mg)

What is the Epithalon peptide?

Epithalon (also known as Epitalon, Epithalone, or Epithalamin) 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 down age-related alterations in reproductive and immune systems and improve the life span of mice and rats^[1]. Apart from its potential in regulating aging, the peptide also has played an important role in research conducted upon certain classes of cancer, infectious diseases, and DNA regulation.

Specifications

AKA: Epitalon

Molecular Formula: C14H22N4O9

Molecular Weight: 390.35 g/mol

Sequence: Ala-Glu-Asp-Gly

PubChem: CID 219042

CAS Number: 307297-39-8

Reconstitution: Required

Research

Epithalon and Anti-Aging
Early research on insect and rodent models hypothesized 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 appears effective even in mice suffering from both cardiac disease and cancer, where 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 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. Thus, the peptide may protect DNA from accumulating errors over time, which often leads to cellular dysfunction, cancer, and aging.

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 plays a critical role in the maintenance of extracellular matrix in tendons, skin, and other connective tissue. Thus the peptide may boost immune system functionality and assist the body to heal both from injury and everyday stress and wear and tear. 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 body for combating viral infections through T lymphocyte, macrophage, and natural killer cell activation.
The following are potential DNA interactions of Epithalon:
– CD5 – Leads to immune cell differentiation
– pCREB t – Circadian rhythm regulation and anti-neoplastic effects
– IL-2 – Increase in IL-2 production, which modulates white blood cells
– Arylalkylamine-N-acetyltransferase – Increase in melatonin production
– MMP2 – Enhancement of MMP activation and inflammation reduction
– Telomerase – Telomerase activity to improve cell longevity
– Tram1 – Improve protein production

Epithalon and Skin Health
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 treated with Epithalon exhibited 30-45% higher activation of fibroblasts^[3]. The activated fibroblasts improve wound healing and help to decrease the natural aging of the skin. Epithalon also appears to inhibit the activity of Caspase-3, a key enzyme that promotes apoptosis or programmed cell death. Epithalon therefore has the potential to increase the longevity of fibroblasts and other skin cells by inhibiting their apoptosis, and thus keep the skin young and healthy.

Epithalon and Tumor Growth
Daily administration of the peptide on rats suffering from cancer reduces tumor growth and burden appeared to diminish the metastasis of the cells to distant tissues. Epithalon is currently under investigation as a potential treatment of 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 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.

Epithalon and Melatonin Secretion
Melatonin is an important hormone produced from the pineal gland, and it regulates sleep and aging. Studies on rats have sugggested Epithalon and similar peptides may help 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 also restore the normal physiological level of melatonin.

Epithalon and Eyesight
Epithalon has been studied in rat models to treat a condition known as 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. Experimental research has reported that Epithalon appears to exhibit minimal adverse effects and low oral and high subcutaneous bioavailability in mice. The dose used in mice (per kg) does not scale to humans.

References