Epitalon, also known as Epithalone or Epithalon, is a synthetic tetrapeptide (Ala–Glu–Asp–Gly) derived from a naturally occurring pineal gland extract (epithalamin) [1].
Structurally, epitalon mimics endogenous peptides that influence the activity of telomerase, the enzyme responsible for maintaining telomere length. Epitalon may also modulate oxidative stress regulation, circadian rhythm stabilization, and neuroendocrine function.
One of the most widely studied aspects of epitalon is its potential influence on cellular aging through multiple biochemical pathways.
A cell study investigated whether Epithalon can influence two processes central to dementia, cholinesterase activity and the formation of the soluble form of amyloid precursor protein (sAPP) in human neuroblastoma (SH-SY5Y) cells [2].
Results showed that Epithalon:
These effects suggest that epitalon may delay or prevent mechanisms underlying conditions like Alzheimer’s disease.
Similar anti-aging effects are also seen in other tissues, such as in the prevention of age-based pigmentary retinal dystrophy in genetically predisposed rats [3].
Oxidative stress is a central contributor to cellular aging and carcinogenesis, as unmanaged oxidative species can damage lipids, proteins, and DNA.
Epitalon can mitigate such damages by enhancing endogenous antioxidant defenses.
In a fruit fly study, synthetic Epithalon’s antioxidant activities were compared with the crude pineal extract, epithalamin [4].
Epitalon was added to larval nutrient medium at 0.00001 wt%, while epithalamin was added at concentrations 1000-fold higher. Epitalon addition resulted in:
A study evaluated the effect of epitalon on tumor development and oncogene expression in 80 transgenic HER-2/neu mice, a model predisposed to breast cancer and accelerated aging [5].
Mice were either given saline as negative control, Vilon as a positive control, or Epithalon (1 µg, subcutaneous) for 5 consecutive days monthly. Results showed that epitalon:
A defining feature of epitalon is its reported influence on telomerase activity.
Telomerase is the ribonucleoprotein enzyme responsible for elongating telomeric DNA, maintaining chromosomal stability.
In most somatic cells, telomerase activity is repressed, which leads to progressive telomere shortening during replication. When telomeres become critically short, cells enter senescence, a hallmark of aging [6].
An in vitro study evaluated whether epitalon can activate telomerase and elongate telomeres in human somatic cells [7]. Human fetal fibroblasts were exposed to epitalon at varying concentrations, resulting in:
Epitalon has been linked to pineal gland regulation through melatonin, a hormone that regulates sleep–wake cycles and seasonal biological rhythms. Melatonin naturally declines with age.
An animal study evaluated whether epitalon can restore melatonin secretion and normalize circadian rhythms of cortisol production in aged female rhesus monkeys [8].
The experimental group received 10 µg of epitalon intramuscularly, once daily for 10 days, while the control group received saline. epitalon administration resulted in:
Age-related changes in mitochondria, nutrient sensing, and hormone signaling may underpin metabolic changes that result in insulin resistance and other related diseases. Epitalon works partly by addressing these mechanisms, according to a study in rhesus monkeys [9].
Seven young (6–8 years) and seven old (20–27 years) monkeys were administered epitalon intramuscularly (10 µg/day for 10 days). After administration, older monkeys had:
Glucose tolerance improvements persisted for 1–2 months post-treatment, even after epitalon withdrawal.
Research Use Only. All findings described above are derived from preclinical studies (animal models and in vitro experiments). Epitalon is not approved by the FDA for any diagnostic or therapeutic use in humans. Genesis Peptides makes no claims regarding human clinical efficacy. This product is sold exclusively for laboratory research.
Every lot undergoes six independent assays before release. Results are published in the lot-specific Certificate of Analysis.
Epitalon, also called Epithalon or Epithalone, is a synthetic tetrapeptide with the sequence Ala-Glu-Asp-Gly (AEDG). It is a short peptide made of four amino acids: alanine, glutamic acid, aspartic acid, and glycine. It was synthesized based on the amino acid composition of Epithalamin, a bovine pineal gland extract, before its discovery in a pineal gland polypeptide complex solution.
The cited findings concern melatonin, a hormone made by the pineal gland. In a clinical trial in middle-aged people, the AEDG peptide increased urinary 6-sulfatoxymelatonin (6-SOMT) excretion by 1.7 times. In a clinical trial in people with reduced melatonin-producing epiphysis function, the AEDG peptide normalized hyperexpression of the circadian Clock and Csnk1e genes in leukocytes by 1.9-2.1 times and increased Cry2 gene hypoexpression in peripheral blood lymphocytes 2 times. These trial findings are reported for the AEDG peptide, and the cited sources do not state that the AEDG peptide is Epitalon. An earlier study reported that Epithalamin, another name for Epitalon, produced an effect similar to that of Pineamin on pineal melatonin synthesis in elderly people. Another report stated that Epithalamin restored melatonin levels in humans and animals during aging.
None of the available findings report that Epitalon causes oxidative stress. In aging oocytes studied in vitro, Epitalon was reported to modulate mitochondrial activity and reactive oxygen species levels. In aging mouse oocytes, adding 0.1mM Epitalon to the culture medium reduced intracellular reactive oxygen species. A review describes Epitalon as a potent antioxidant, comparable to melatonin.
Epitalon, also known as Epithalon or Epithalone, is a tetrapeptide with the sequence Ala-Glu-Asp-Gly (AEDG). Epitalon is also written as Ala-Glu-Asp-Gly (AEDG) and is a synthetic tetrapeptide.
In cell cultures from patients with ductal breast cancer, the peptide bioregulator Ala-Glu-Asp-Gly (Epitalon) and nickel ions showed a protective effect. This was reported as suggesting prospects for further study of these agents in combined therapy of this form of cancer. Ala-Glu-Asp-Gly was also studied alone and in combination with nickel for its correctional influence on genome stability in lymphocyte cultures from ductal breast cancer patients.
In bovine oocytes studied in vitro, Epitalon treatment was reported to significantly improve the oocyte maturation rate compared with the control group. In bovine in vitro studies, the authors concluded that telomerase activation via Epitalon improves bovine in vitro embryo production. In post-thawed bovine embryos studied in vitro, telomerase activity was significantly compromised, and Epitalon treatment significantly improved the blastocyst hatching rate and implantation potential.
A review identifies epitalon as associated with telomere biology among nine peptides spanning diverse aging interventions. The review states that Epitalon enhances the activity of several enzymes, including telomerase, but notes it remains uncertain whether these are the sole mechanisms of action of this compound. In an in vitro study using bovine embryos, the authors concluded that telomerase activation via Epitalon improves in vitro embryo production.
In an in vitro study using human lymphocytes from old individuals, Epitalon (Ala-Glu-Asp-Gly) was reported to induce unrolling deheterochromatinization, meaning decondensation, of total heterochromatin, the tightly packed part of chromosomes. The same in vitro human study reported that Epitalon has a selective effect on definite chromosome regions, distinct from the other tested peptides. Separately from the Epitalon finding, the same study reported progressive heterochromatinization during aging, a condensation process that can deactivate previously active genes.
In an in vitro study of tobacco cells, Epitalon was found to differently modulate the expression of CLE family genes, KNOX1 genes, and GRF genes. The KNOX1 genes are transcription factor genes, and the GRF genes code for DNA-binding proteins such as topoisomerases and nucleases. In the same tobacco cell studies, Epitalon modulated the expression of other genes, including those responsible for tissue formation and cell differentiation.
In an in vitro study, the Khavinson peptides, including Epitalon, were reported to act on macrophages as anti-inflammatory molecules during inflammatory and microbial-mediated activity. The study suggests these peptides cooperate as natural inducers of TNF tolerance in monocytes. Because the findings were reported for the peptides together, this study does not report Epitalon's effect separately from the other peptides.
FOR RESEARCH USE ONLY — Products are sold exclusively for in vitro and preclinical laboratory research. Not for human consumption or administration. Not intended for diagnostic or therapeutic use. These statements have not been evaluated by the FDA.