What is Epithalon and How Does it Protect Telomeres?
What is Epithalon?
Epithalon is a short, 4 amino acid chain peptide used to regulate the cell cycle through the upregulation of telomerase activity. It has been shown to have distinctive anti-aging and anti-tumor activity across many animal and human studies. Known as the synthetic version of the tetrapeptide epithalamin, which naturally occurs in the pineal gland in our body, Epithalon (also known as Epitalon or Epithalone) was first discovered in the late 1980’s by Prof. Vladimir Khavinson from The Sankt Petersburg University, Russia.
As the most prominent tasks of the pineal gland are to maintain different kind of processes in our body, such as to normalize the activity of anterior pituitary and to maintain the levels of calcium, gonadotropins, and melatonin, its activity is highly regulated by a series of feedback mechanisms. Epithalamin acts as an antioxidant and increases the resistance to stress and lowers the levels of corticosteroids. The life extension and anti-aging properties, amongst a variety of different clinical indications, of epithalon are incredible.
Mechanism of Action
Epithalon regulates the cell cycle through up-regulation of telomerase activity. Upregulating telomerase activity has a vast amount of effects on the body because it allows all the cells in the body to be maintained due to inhibiting the shortening of telomeres, which are fundamentally involved in the aging process. Telomerase is a RNA-dependent polymerase that elongates and maintains the length of telomeres by adding tandem repeats on the 3’ end of chromosomes. Telomere elongation promotes indefinite cellular proliferation and that can promote neoplastic cells. However, it has been shown that maintaining proper telomere length acts as a prominent effector of anti-aging and inhibitor of tumorigenesis; and, this is precisely what epithalon does.
Epithalon has also been shown to affect the aging process by exerting an antioxidant effect. This is implicated in the slowing of the aging process because cytotoxicity due to reactive oxygen species can lead to damaging DNA, leading to cellular death and/or mutations leading to the formation of cancerous cells.
It has also been reported to show significant anti-tumor effects in breast and colorectal cancer by inhibiting carcinogenic receptor expression and attenuation of metastasis.
Further, epithalon has been reported to play a key role in the regulation of important biomolecules such as cytokines, C-reactive protein, and other acute phase reactants to attenuate the inflammatory response. This regulation of the inflammation process is pivotal to human health because dysregulation and potentiation can cause a broad spectrum of disorders including, but not limited to, rheumatoid arthritis, ulcerative colitis, amongst others.
Lastly, it has been found that epithalon plays a very important role in the regulation of the endocrine system in the body. The vast amount of effect different hormones have in the body is fundamental to different processes in the body. And, any loss in hormones can result in different aspects of disease. But, in the realm of aging, we tend to lose production of hormones due to shortening of telomeres. So, epithalon can increase endogenous levels of hormones that we lose. For example, a study was done on elderly patients to determine the effect of epithalon administration on levels of melatonin, a natural regulator of the sleep cycle. This study showed that levels of melatonin increased and restoration of sleep was achieved. Other studies have reported that epithalon has effects on other hormones such as gonadotropic hormones (FSG, LG, prolactin) to improve sexual and reproductive functions.
What have Research Studies Shown?
Scientific research has revealed that epithalon affects the following:
- Upregulate telomerase activity
- Normalize antioxidant indices
- Reduce peroxide lipid oxidation products
- Increase activity of glutathione peroxidase
- Improve melatonin and immunity (cellular and humoral)
- Improve insulin sensitivity
- Decrease LDL and VLDL
- Improve tissue repair
- Anti-tumor effects
- Decrease mortality and increases life expectancy
Epithalon in Research (Expanded)
Aging Decleration
Epithalon induces telomerase activity and telomere elongation in human somatic cells. In a study it was shown to induce a 33% increase in telomere elongation which is directly involved in the aging process. There was a human trial done over a 12-year period with patients treated with epithalon and a placebo group. The results of this study demonstrated a 28% decrease in overall mortality with those treated with epithalamin, and a 2-fold decrease in cardiovascular mortality by decreasing the functional age and degree of cardiovascular aging. Another study was done to show that those treated with thymalin and epithalamin over a 6-year period had a mortality rate that was 4.1 times lower than the control group.
Tumor Suppression
There has been a lot of scientific research made and still is being made on the use of epithalon against cancer. It was found that epithalon has inhibitory effects on the development and growth of tumors with studies done on mammary tumors, colon carcinogenesis, prostate cancer just to name a few. Tumors exposed to epithalon have been shown to shrink in size. Treatment with epithalon stopped the metastases of tumors in mice and it has oncostatic properties, halting the spread of cancer. Due to its role in telomerase activity along with endocrine and immune function, epithalon has been implicated for its anti-tumor properties in hormone dependent cancer. A study was done on patients with uterus, cervix, and ovarian cancer and it was shown that treatment of epithalon restored cellular immunity, decreased recurrence and metastasis of the cancer, and decreased the size of tumors.
Anti-Oxidant Effects
Research has shown that epithalon is a powerful antioxidant that eliminates oxygen free radicals responsible for damaging and killing cells. This process, known as oxidative stress, is the root cause of a wide variety of age-related diseases. It is important to note that the human lifespan is inversely related to the number of oxygen free radicals in the human body, and epithalon is responsible for slowing down and killing these killer radicals. Since free radicals are the main source of degenerative diseases, eliminating them prevents diseases such as cancer, dementia, Alzheimer’s, muscle and joint pain, heart disease, and more.
Restoring Normal Sleep Patterns
As we age, melatonin content in our blood decreases considerably. Epithalon plays a key role in our bio-rhythm control and affects the endocrine, nervous and immune systems. In fact, reduced melatonin production leads to age-related neurodegenerative changes and certain diseases. Melatonin's importance is clear, however, supplementing melatonin, in some cases, can provoke considerable side-effects, such as neoplastic growth. Finding a suitable way to safely increase melatonin levels is an important endeavor. Epithalon stimulates production of melatonin through its action on the pineal gland, and this is why people taking epithalon have reported better sleep patterns and increased deep sleep, which is essential for the body to repair itself and strengthen the immune system.
Regulation of Inflammation
There are countless disorders that arise due to dysregulation of the immune system and inflammatory processes. Therefore, obtaining therapies that have the ability to help regulate the inflammatory pathway through control of different mediators in the process can help treat disorders. Epithalon has extensively been shown to help regulate the function of mediators such as cytokines, C-reactive protein, and other acute phase reactants.
Insulin and Cholesterol
Due to epithalon’s variety of activity amongst different cells in the endocrine system, amongst other systems, due to telomerase upregulation and pineal gland activation, it has been shown that epithalon significantly improves insulin sensitivity, glucose utilization, and overall cholesterol health. In regard to cholesterol health, it has been shown to significantly decrease LDL and VLDL while significantly increasing levels of HDL.
References
Khavinson VKh, Bioregulating therapy as a new direction in Medicine,Proceedings of the National conference of Gerontology and Geriatrics;May 28-31, 1997 Bucharest, Romainia;1997 p205
Peptide regulation of Aging.Proceedings of the 17th World Congress of the International Association of Gerontology,July 1-6 2001,Vancouver Canada, Gerontology 2001, 47(1) pg 545
Anisimov VN, Arutjunyan AV, Khavinson VK. Effects of pineal peptide preparation Epithalamin on free-radical processes in humans and animals. Neuro Endocrinol Lett. 2001;22(1):9-18.
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