Epitalon, also known as epithalon and epithalone, is a synthetic tetra-peptide version of epithalamin (epithalon tetra), which is naturally produced by the pineal gland in the brain. The epitalon tetra peptide is made up of four amino acid building blocks (alanine, glutamic acid, aspartic acid, and glycine) and has been shown to have a wide range of beneficial biological activities in animal and human studies . Long-term exposure to epithalamin was followed by an increase in the mean and maximum life spans of aging of rats, mice, and flies. In human cells, epitalon stimulates enzymatic activity of telomerase, and telomere elongation, which can be due to reactivation of the telomerase gene. Telomerase extends the length of human DNA to make cells biologically younger, which provides the possibility of prolonging the life span of a cell population and of the entire body . Results of a 12-month study following patients with accelerated aging treated with epitalon showed that the peptide reduced mortality, normalised metabolism and improved the condition of various metabolic systems . The peptide was also shown to reduce serum insulin and fatty acid levels in rabbits and improve glucose tolerance in these animals. Epitalon stimulates the immune system by increasing the number of antibody producing cells, which fight infection . Epitalon is a potent antioxidant able to stimulate the production of multiple antioxidant enzymes inside the body to improve antioxidant defence . Overall, results show a high efficiency of epithalamin therapy for reducing age-related illnesses, including various cancers, metabolic syndromes and heart conditions. These studies demonstrate that the peptide has the potential to slow down disease processes and to extend human lifespan.
Epitalon should be dosed subcutaneously or intramuscularly for maximum potency as it is digested when orally administered. 5 mg of the peptide can be injected either once or twice per day and this should be carried out in the morning and afternoon if dosing twice per day. Epitalon can be injected for 20 days at a time followed by a four to six month pause in between cycles. Once the peptide has been reconstituted in BAC water then it is stable for a full 20-day treatment cycle if stored at 4-8°C. The peptide will lose potency after this time and should be discarded.
Long-term clinical trials in humans have reported no side effects of epithalon. In these trials, the peptide was administered every 3 days at 10 mg in 2 ml saline intramuscularly, with a 6-month interval between courses .
- Khavinson, V.K., V.G. Morozov, and V.N. Anisimov, Experimental Studies of the Pineal Gland Preparation Epithalamin, in The Pineal Gland and Cancer: Neuroimmunoendocrine Mechanisms in Malignancy, C. Bartsch, et al., Editors. 2001, Springer Berlin Heidelberg: Berlin, Heidelberg. p. 294-306.
- Kh Khavinson, V., I. E Bondarev, and A.A. Butyugov, Epithalon Peptide Induces Telomerase Activity and Telomere Elongation in Human Somatic Cells. Vol. 135. 2003. 590-2.
- Korkushko, O.V., et al., Peptide geroprotector from the pituitary gland inhibits rapid aging of elderly people: results of 15-year follow-up. Bull Exp Biol Med, 2011. 151(3): p. 366-9.
- Khavinson, V.K., et al., Modulating effects of epithalamin and epithalon on the functional morphology of the spleen in old pinealectomized rats. Bull Exp Biol Med, 2001. 132(5): p. 1116-20.
- Kozina, L.S., A.V. Arutjunyan, and V. Khavinson, Antioxidant properties of geroprotective peptides of the pineal gland. Arch Gerontol Geriatr, 2007. 44 Suppl 1: p. 213-6.