Epithalon is a short peptide consisting of just four amino acids (Alanine-Glutamate-Asparagine-Glycine). In animal studies, epithalon has been shown to affect melatonin secretion as well as telomerase activity. The molecule is sometimes referred to as epithalone, epitalon, LS-72251, and CID2192042. Epithalon was developed in Russia (isolated from the bovine (cow) pineal gland) and has received attention for its anti-aging and anti-carcinogenic properties as well as for its ability to regulate melatonin secretion.
A 2002 study on transgenic mice prone to cancer produced surprising results. Epithalon prolonged the average lifetime of the cancer-prone her2/neu mice by 13.5% when administered subcutaneously 5 times per week. The molecule appeared to suppress the development of cancer and reduce metastasis (spread) of existing cancers. Overall, cancer rates in mice that were provided epithalon were 3.7 times lower than in mice who did not receive the peptide. The mice that did develop cancer lived 1.7 times longer if they received epithalon compared to mice that did not. Epithalon also extended the life of mice without cancer substantially1 .
The Anti-Aging Effects of Epithalon
The anti-aging effects of epithalon appear to be a result of its ability to activate telomerase. Telomerase is an enzyme, found in all cells, that maintains the length of telomeres. Telomeres are specialized sequences of the DNA that protect chromosomes from damage, but shorten over time as an organism ages. Maintenance of telomere length has been associated with longevity, disease-free survival, and a reduction in the physical manifestations of aging.
Two studies in birds, published in 2012 and 2013, found that epithalon can impact thymus health and function. The thymus is a gland that functions in the development of T-lymphocytes (T-cells). By improving thymus function, epithalon improves lymphocyte function and boosts T-cell proliferation. The result is increased levels of interferon gamma, a molecule important in immune fucntion2,3 .
Epithalon and Melatonin
Catecholamines, like norepinephrine and dopamine, are critical in regulating the hypothalamus, a small region of the brain responsible for much of the hormone secretion in mammalian and avian organisms. The pineal gland, found in another region of the brain, is responsible for melatonin release, which regulates the normal day/night cycle of most living things. Inappropriate melatonin release leads to fluctuations in catecholamine release, which in turn affects the hypothalamus.
A 2012 study found that epithalon is capable of influencing melatonin release and can diurnal rhythms in female rats. Epithalon proved to be more effective than melatonin supplementation in correcting experimentally induced disturbances in circadian rhythm, thereby lessening impact on normal reproductive function and even reducing the risk of premature aging in female rats4 .
What Is Epithalon, Really?
Epithalon is a small peptide consisting of just four amino acids. It was developed from isolates of bovine pineal gland extract. It has shown promise as a potential anti-cancer agent. It is also being investigated as a means of controlling circadian rhythm disturbances and as a potential anti-aging treatment.
A Note on Naming
While epithalon is sometimes referred to as AGAG because of its amino acid sequence, such an abbreviation violates scientific convention and is incorrect. The appropriate shorthand for epithalon is AERG. The abbreviation AGAG would refer to a peptide with the sequence Alanine-Glycine-Alanine-Glycine rather than to epithalon, which is Alanine-Glutamate-Asparagine-Glycine.
- Anisimov, V. N., Khavinson, V. K., Alimova, I. N., Semchenko, A. V. & Yashin, A. I. Epithalon decelerates aging and suppresses development of breast adenocarcinomas in transgenic her-2/neu mice. Bull. Exp. Biol. Med.134, 187-190 (2002).
- Pateyk, A. V., Baranchugova, L. M., Rusaeva, N. S., Obydenko, V. I. & Kuznik, B. I. Effect of peptides Lys-Glu-Asp-Gly and Ala-Glu-Asp-Gly on the morphology of the thymus in hypophysectomized young and old birds. Bull. Exp. Biol. Med.154, 681-685 (2013).
- Lin’kova, N. S., Kuznik, B. I. & Khavinson, V. K. [Peptide Ala-Glu-Asp-Gly and interferon gamma: their role in immune response during aging]. Adv. Gerontol. Uspekhi Gerontol. Ross. Akad. Nauk Gerontol. Obshchestvo25, 478-482 (2012).
- Arutjunyan, A. et al. Melatonin and pineal gland peptides are able to correct the impairment of reproductive cycles in rats. Curr. Aging Sci.5, 178-185 (2012).