Epithalon
C14H22N4O9
H-Ala-Glu-Asp-Gly-OH
Key Benefits
Biologic Description
Epithalon, also known as Epitalon or Epithalone, is a tetrapeptide with the amino acid sequence Ala-Glu-Asp-Gly. This sequence mimics that of a natural peptide, epithalamin, which is extracted from the pineal gland of bovines. Epithalon is primarily recognized for its potential role in the modulation of telomerase activity, a key enzyme involved in the maintenance and elongation of telomeres.
Chemically, Epithalon is categorized as a polypeptide, consisting of four amino acid residues: alanine, glutamic acid, aspartic acid, and glycine. The peptide bonds formed between these amino acids result in a molecule with a low molecular weight, which enables it to cross the blood-brain barrier. The structure of Epithalon is characterized by its linear, non-branching arrangement, allowing it to interact with specific receptors and enzymatic complexes within cells.
Functionally, Epithalon is hypothesized to exert its biological effects primarily through the activation of telomerase, an enzyme that adds specific DNA sequence repeats ("TTAGGG" in all vertebrates) to the 3' end of DNA strands in the telomere regions, which are found at the ends of eukaryotic chromosomes. This activity is crucial in maintaining genomic stability and preventing chromosomal degradation, thereby potentially influencing cellular aging and longevity.
Additionally, Epithalon has been associated with a variety of other biological processes, including the regulation of gene expression, antioxidative defense mechanisms, and neuroendocrine activity. It has shown potential in modulating melatonin production and circadian rhythm regulation, due to its pineal origin.
At the cellular level, Epithalon's impact on telomere elongation is of particular interest in the study of aging and age-related diseases. By potentially stabilizing telomere length, it may contribute to the extension of cellular lifespan and the delay of senescence in human cells.
However, it is important to note that much of the research on Epithalon is in its early stages, with a majority of studies conducted in vitro or in animal models. The full extent of its effects, particularly in human physiology, is not yet fully understood, and its therapeutic applications are still under investigation. As with any compound impacting fundamental cellular processes, the potential for unintended consequences or side effects remains a critical area of ongoing research.
Dosage Guidelines
The Russian Protocol, as derived from the research conducted by Professor Khavinson and his team and cited by the International Peptide Society for anti-aging research, involves a specific regimen for administering Epithalon.
In this protocol, the total dosage of Epithalon prescribed is 100mg, spread over a study period of 10 days. The administration is carried out daily, with each day's dosage being 10mg.
This can either be administered in one subcutaneous injection or split into two injections, one in the morning and the other at night, depending on the preference or requirement of the study design. Researchers employing this protocol typically repeat it up to twice a year, ensuring that there is a pause of at least four months between each course.
This protocol is specifically tailored for research focused on exploring the anti-aging effects of Epithalon and provides a structured approach for scientists and researchers in this field.
10 mg
Daily
10-Days
Side Effects
Regarding the side effects of Epithalon, it's important to recognize that the comprehensive understanding of its adverse effects is still emerging, primarily due to the limited scope of clinical studies and the peptide's predominant use in research settings. However, from the available data and anecdotal reports, some potential side effects have been noted.
Firstly, as with any substance administered via subcutaneous injection, there's a risk of local reactions at the injection site. These can include redness, itching, or swelling, although such reactions are generally mild and transient. In rare cases, more severe local reactions could occur, necessitating further medical attention.
Systemically, Epithalon's effects on the body are not fully understood, but some users have reported a range of symptoms that may be linked to its use. These include fluctuations in energy levels, alterations in sleep patterns, and changes in emotional states, like increased irritability or mood swings. It's crucial to note that these reports are largely anecdotal and may not be directly attributable to Epithalon itself.
Another concern with the use of Epithalon, as with any agent that potentially influences cellular mechanisms, is the long-term impact on cellular and genomic stability. While Epithalon is studied for its role in telomere elongation and potential anti-aging effects, the broader implications of these changes at the cellular level are not completely understood. There is a theoretical risk that manipulating telomerase activity could have unintended consequences on cellular proliferation and stability, although no direct evidence has yet established such effects in the context of Epithalon use.
Furthermore, the impact of Epithalon on hormonal and immune systems is not well-defined. Given its origin and structural similarity to naturally occurring peptides in the body, there could be complex interactions with various physiological systems, which need to be explored further in rigorous clinical studies.
Finally, individuals with pre-existing health conditions or those on concurrent medications should approach the use of Epithalon with caution, as the interactions and side effects in such scenarios are largely unknown.
References:
Epithalon peptide induces telomerase activity and telomere elongation in human somatic cells
Addition of Epithalon peptide in telomerase-negative human fetal fibroblast culture induced expression of the catalytical subunit, enzymatic activity of telomerase, and telomere elongation, which can be due to reactivation of telomerase gene in somatic cells and indicates the possibility of prolonging life span of a cell population and of the whole organism.
Author: V Kh Khavinson, I E Bondarev, A A Butyugov
Publication Date: 2003 Jun
Effect of Epitalon on biomarkers of aging, life span and spontaneous tumor incidence in female Swiss-derived SHR mice
The results of this study show that treatment with Epitalon did not influence food consumption, body weight or mean life span of mice. However, it slowed down the age-related switching-off of estrous function and decreased the frequency of chromosome aberrations in bone marrow cells (by 17.1%, P<0.05). It also increased by 13.3% the life span of the last 10% of the survivors (P<0.01) and by 12.3% the maximum life span in comparison with the control group. We also found that treatment with Epitalon did not influence total spontaneous tumor incidence, but inhibited the development of leukemia (6.0-fold), as compared with the control group. The data obtained suggest a geroprotector activity of Epitalon and the safety of its long-term administration in mice.
Authors: Vladimir N Anisimov, Vladimir Kh Khavinson, Irina G Popovich, Mark A Zabezhinski, Irina N Alimova, Svetlana V Rosenfeld, Natalia Yu Zavarzina, Anna V Semenchenko, Anatoli I Yashin
Published: 2003
Inhibitory effect of the peptide epitalon on the development of spontaneous mammary tumors in HER-2/neu transgenic mice
The data demonstrate the inhibitory effect of Epitalon in the development of spontaneous mammary tumors in HER-2/neu mice, suggesting that a downregulation of HER-2/neu gene expression in mammary adenocarcinoma may be responsible, at least in part, for the antitumor effect of the peptide.Authors: T. Badenhorst, D. Svirskis, M. Merrilees, L. Bolke, Zimei Wu
Published: 2002 Sep
Effect of the synthetic pineal peptide epitalon on spontaneous carcinogenesis in female C3H/He mice
Treatment with Epitalon decreased the number of tumor-bearing mice with malignant tumors and prevented the development of metastases.
Authors: L. Pickart, Jessica Michelle Vasquez-Soltero, A. Margolina
Published: 2015-07-07