Epithalon | Reviews, Clinical Trials, and Safety

Epithalon is classified as a research chemical outside of Russia, where it is used to treat menopause-related symptoms, anovulatory infertility, and hormone-dependent tumors [9].

As noted by the Alzheimer’s Drug Discovery Foundation (ADDF), the bulk of research involving epithalamin and epithalon has been conducted in Russia (or formerly, the Soviet Union) and has not been subject to independent confirmation [1].

The ADDF further notes that its review of epithalon has excluded roughly half of the approximately 110 epithalon/epithalamin articles published in the Russian language, though efforts have been made to refer to English translations where possible.

Below, we present a summary of key epithalon benefits based on the research available.

Epithalon and longevity

It is known that epithalon regulates gene expression and protein synthesis, with the general effect of reducing mortality and delaying the progression of age-associated diseases in the elderly [4].

In an in vitro study conducted by Professor Khavinson and colleagues in 2003, the team demonstrated that epithalon elongates telomeres and induces telomerase activity when introduced to telomerase-negative human fetal fibroblast cultures. The researchers concluded that epithalon may prolong the lifespan of cell populations through anti-senescence activity [2].

In a human study published that same year, Khavinson and colleagues observed that elderly human subjects who received epithalamin treatment for two to three years experienced a 1.6-1.8 fold decreased mortality rate compared with a control group. Additionally, the researchers found that the epithalamin-treated patients exhibited reduced rates of:

• Coronary artery disease
• Hypertension
• Osteoarthritis
• Osteoporosis

The researchers concluded that epithalon may be used for “health maintenance and age-related pathology prevention” in the elderly [10].

Epithalon and sleep

Animal studies have shown that the peptide increases melatonin may therefore enhance sleep and promote brain health.

• A 1992 study by Anisimov et al. investigated the effect of epithalamin on the pineal and serum melatonin levels in elderly rats. The team noted that epithalamin increased melatonin production in rats, referencing past research showing that the administration of melatonin had the effect of increasing the rodents’ longevity [9].
• A 2001 study by Khavinson et al. investigated the regulatory effect of epithalon on the production of melatonin and cortisol in senescent monkeys, finding that the peptide significantly stimulated melatonin synthesis, thus normalizing the circadian rhythm of cortisol secretion [11].
• A 2004 study by Korkushko et al. found that epithalamin could be used to increase melatonin production by modulating the melatonin-producing function of the pineal gland [12].
• In a 2013 study by Korenevsky et al., the researchers administered a combination of melatonin and epithalon to female rats exposed to suboptimal environmental factors, such as light pollution, finding that the combined therapy rectified various impairments of the hypothalamic-pituitary-gonadal axis [13].

The link between melatonin and brain health has been clarified in more recent research by Chitimus et al., noting that melatonin has antioxidant properties and can help protect the brain from oxidative stress [14].

Since oxidative stress may contribute to neurodegenerative disorders, there is strong research interest in epithalon’s role in optimizing sleep and maintaining overall brain health.

Epithalon and DNA repair

Research indicates that epithalon may be used to protect against and repair DNA damage, given its potent antioxidant activity. For example, it has been shown to:

• Decrease levels of DNA damage when administered to senescence-accelerated mice [15];
• Stimulate cortical neurons when administered intranasally to rodents [16];
• Increase levels of the DNA-binding protein phosphor-CREB [17]; and,
• Improve antioxidant defense systems in flies and rats [18, 19, 20]

Epithalon and cancer research

Preclinical studies in rats and cancer-prone mice suggest that epithalon may have utility in cancer prevention.

• In a 2002 study by Anisimov et al., female transgenic FVB mice carrying the breast cancer gene HER-2/neu were given monthly injections of either vilon or epithalon. Researchers found that epithalon “markedly inhibited neoplasm development” and reduced the maximum size of breast adenocarcinomas by 33% compared with the control group [21].
• A 2006 study by Kossoy et al. investigated the potential preventive effect of epithalon on spontaneous tumorigenesis in mice, finding that the peptide delayed development of metastases from spontaneous tumors, without any metastases found in the experimental mice [22].
• A pair of studies conducted by Vinogradova et al. found that epithalon significantly inhibited the development of spontaneous tumors in rats exposed to constant natural light, thus prolonging their mean lifespan [23, 24].

These studies highlight the potential anti-cancer properties of eptihalon in animal models and suggest that further research in this area remains warranted.