The pineal gland in cross-section, from which epithalon was originally derived.

The pineal gland in cross-section, from which epithalon was originally derived. "Pineal gland - high mag" by Nephron - Own work. Licensed under CC BY-SA 3.0 via Commons -

Introduction

Epithalon (also referred to as epitalon or AEDG) is a small peptide made of four amino acids (i.e. a sequence of Ala-Glu-Asp-Gly). Some researchers, particularly those involved in the isolation of this tetrapeptide, claim that epithalon confers beneficial effects in the areas of cancer prevention, the treatment of age-related physiological changes and nerve cell activity1. Epithalon may have some advantages as a research peptide, mostly due to its relatively small mass. However, its role in the management of states such as tumorigenesis and aging is uncertain at best. 

Epithalon and its purported effects in Cancer Development

Some scientists have claimed that epithalon may prevent tumor development in animal models of carcinogenesis. A study used an inbred mouse strain to assess this property2. 61 female mice were treated with 0.5μg/ml subcutaneous epithalon five days a week for 26 weeks. The number of spontaneously-forming tumors in these mice was compared to those in 56 identical mice receiving saline as a control. The mice receiving epithalon developed fewer tumors compared to controls, and exhibited no metastases compared to three in the control mice2. However, no significant differences were reported here2. Treatment with epithalon was shown to have no effect in the rate of malignant lymphoma in another study using a mouse line susceptible to this condition3. Other researchers have claimed that 0.1μg epithalon given five times a week prevented spontaneous tumor formation in rats living in ambient environmental light, but not those exposed to standard laboratory or constant illumination4.

Epithalon and Aging

Aging in animals is characterized by an increased susceptibility to DNA damage, (e.g. mutations) shorter telomeres (which essentially measure the ability of the cell to replicate its DNA in the course of proliferation) and other deficiencies in normal processes that protect cells from damage and death. There are some reports claiming evidence that epithalon may conserve cell survival through the restoration of telomere and telomerase structure and function, which degrade as a cell ages5. The authors of another study claimed a significant (20%) decrease in the chromosomal aberration (another marker of aging) of mice carrying mutations that promote aging (SAMP-1 mice) compared to identical untreated controls6. Another study compared female SAMR-1 and SAMP-1 mice treated with either melatonin (a neurotransmitter that is also linked to increased protection against aging and age-related physiological irregularities) or epithalon five times weekly for four weeks to untreated control mice (although the group size was unreported)3. These authors observed no difference between the treated or control animals of either strain in metabolic parameters. However, they claimed that both epithalon and melatonin alleviated irregularities in the estrous cycle of the treated animals compared to controls3. The last 10% of the SAMP-1 mice to die exhibited an increased rate of aging and a decreased mean life span compared to SAMR-1 mice, although treatment with epithalon or melatonin resulted in increased mean and maximum lifespan in these SAMP-1 mice compared to their untreated controls3. A study of aging under different lighting conditions claimed that, while treatment with 0.1μg epithalon five times a week did not affect the survival of rats living under standard laboratory illumination regimens, it did increase the maximum survival times of rats living under either constant or ambient (i.e. natural to the surrounding environment) illumination by 24 and 95 days respectively4.

References:

1. Vanhee C, Moens G, Van Hoeck E, Deconinck E, De Beer JO. Identification of the small research tetra peptide Epitalon, assumed to be a potential treatment for cancer, old age and Retinitis Pigmentosa in two illegal pharmaceutical preparations. Drug testing and analysis. 2015;7(3):259-264.

2. Kossoy G, Anisimov VN, Ben-Hur H, Kossoy N, Zusman I. Effect of the synthetic pineal peptide epitalon on spontaneous carcinogenesis in female C3H/He mice. In vivo (Athens, Greece). 2006;20(2):253-257.

3. Anisimov VN, Popovich IG, Zabezhinskii MA, et al. [Effect of epitalon and melatonin on life span and spontaneous carcinogenesis in senescence accelerated mice (SAM)]. Voprosy onkologii. 2005;51(1):93-98.

4. Vinogradova IA, Bukalev AV, Zabezhinski MA, Semenchenko AV, Khavinson V, Anisimov VN. Effect of Ala-Glu-Asp-Gly peptide on life span and development of spontaneous tumors in female rats exposed to different illumination regimes. Bulletin of experimental biology and medicine. 2007;144(6):825-830.

5. Khavinson V, Bondarev IE, Butyugov AA. Epithalon peptide induces telomerase activity and telomere elongation in human somatic cells. Bulletin of experimental biology and medicine. 2003;135(6):590-592.

6. Rosenfeld SV, Togo EF, Mikheev VS, Popovich IG, Khavinson V, Anisimov VN. Effect of epithalon on the incidence of chromosome aberrations in senescence-accelerated mice. Bulletin of experimental biology and medicine. 2002;133(3):274-276.