Epithalon (Epitalon)
Epithalon | Epithalone | Ala-Glu-Asp-Gly
Mechanism of Action
Epitalon is a synthetic tetrapeptide based on the naturally occurring peptide epithalamin, which is extracted from the pineal gland. Developed by Professor Vladimir Khavinson at the St. Petersburg Institute of Bioregulation and Gerontology, epitalon is the most extensively studied of the Khavinson peptide bioregulators. Its primary mechanism of action involves activation of telomerase, the enzyme responsible for maintaining telomere length at chromosome ends.
Telomeres shorten with each cell division, and this progressive shortening is considered a key hallmark of cellular aging. When telomeres become critically short, cells enter senescence or undergo apoptosis. Khavinson and colleagues demonstrated that epitalon can activate telomerase in human somatic cells, leading to elongation of telomeres and extension of cellular lifespan beyond the Hayflick limit. This was shown in human fetal fibroblast cultures where epitalon-treated cells underwent significantly more population doublings than controls.
Epitalon also influences melatonin production. As a pineal bioregulator, it has been shown to restore the nocturnal melatonin peak in aged primates, which normally declines with age. This melatonin-related activity provides a secondary mechanism through which epitalon may affect aging processes, given melatonin's roles as an antioxidant and circadian regulator.
Key Research Findings
- Khavinson et al. (2003) demonstrated epitalon activated telomerase and elongated telomeres in human fetal fibroblasts, extending their replicative lifespan by 44%.
- Anisimov et al. (2001) showed chronic epitalon administration extended maximum lifespan and inhibited spontaneous tumor development in female mice.
- Khavinson & Morozov (2003) reported that long-term treatment with epithalamin (the natural extract) increased maximum lifespan in aged rhesus monkeys.
- Goncharova et al. (2005) demonstrated epitalon restored the nocturnal melatonin peak in old female macaques to levels comparable to young animals.
References
Dosage in Research
Animal studies have used doses of 0.1-1 mcg per animal in rodents. In primate studies, epithalamin was administered at doses equivalent to 10-20 mg of the natural extract. In vitro telomerase activation studies used micromolar concentrations.
Storage & Handling
Store lyophilized powder at -20C. Reconstituted solution should be refrigerated at 2-8C. As a small tetrapeptide, epitalon is relatively stable compared to larger peptides.
Frequently Asked Questions
What is Epitalon?
Epitalon is a synthetic four-amino-acid peptide (Ala-Glu-Asp-Gly) based on epithalamin, a natural pineal gland extract. It was developed by Russian gerontologist Vladimir Khavinson and has been studied primarily for its effects on telomerase activation and aging biomarkers.
What is the relationship between epitalon and telomerase?
Research has shown epitalon can activate telomerase, the enzyme that maintains telomere length. Telomere shortening is a hallmark of cellular aging, and telomerase activation can extend the replicative capacity of cells. Khavinson et al. demonstrated this directly in human fibroblast cultures.
How does N-Acetyl Epitalon Amidate differ from standard Epitalon?
N-Acetyl Epitalon Amidate is a modified version with N-terminal acetylation and C-terminal amidation, modifications designed to increase resistance to enzymatic degradation and potentially improve cellular uptake and bioavailability.
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