Epithalon 25 mg

Description

Epithalon (also known as Epitalon, Epithalone, or Epithalamin) is a short synthetic peptide recognized for its ability to activate the telomerase enzyme and stimulate melatonin release. First developed in Russia in the 1980s, Epithalon has demonstrated the ability to delay age-related changes in the reproductive and immune systems and to extend the lifespan of mice and rats. While primarily studied for its anti-aging potential, Epithalon has also shown significant effects in certain types of cancer, infectious diseases, and DNA regulation.

Epithalon Structure

Source: PubChem

Sequence: Ala-Glu-Asp-Gly
Molecular Formula: C₁₄H₂₂N₄O₉
Molecular Weight: 390.349 g/mol
PubChem CID: 219042
CAS Number: 307297-39-8

Epithalon Research

1. The Role of Telomerase in the Anti-Aging Effects of Epithalon

Early studies in insects and rodents revealed that Epithalon can significantly prolong lifespan. In healthy fruit flies and rats, Epithalon decreased mortality by 52%. In mice genetically predisposed to heart disease and cancer, Epithalon extended lifespan by up to 27% compared to controls[1].

A key mechanism behind these effects involves the elimination of free radicals—charged molecules that cause damage to healthy tissues.

However, antioxidant activity alone does not fully explain Epithalon’s impact on longevity. In vitro studies on human somatic cells demonstrate that Epithalon activates telomerase, an enzyme that protects telomeres, which are the critical end caps of chromosomes that maintain DNA integrity[2]. This telomerase activation results in fewer DNA errors, supporting the concept that Epithalon protects DNA from damage[3][4]. In essence, Epithalon helps prevent the accumulation of DNA damage over time—a process that leads to cell dysfunction, aging, and cancer.

2. Epithalon and DNA Activation

Beyond its antioxidant effects and telomere protection, Epithalon influences gene expression. Research in cell cultures reveals that Epithalon binds directly to DNA promoter regions of genes including CD5, IL-2, MMP2, and Tram1[5].

• CD5 and IL-2 regulate immune system function.
• MMP2 is crucial for maintaining the extracellular matrix in skin, tendons, and connective tissue.
• Tram1 supports protein production.

This suggests Epithalon may enhance immune function and the body’s ability to repair and regenerate after injury or daily stress.

Supporting this, rat studies show that Epithalon increases interferon gamma expression in aging lymphocytes[6]. Interferon gamma is essential for antiviral defense, activating macrophages, natural killer cells, and T cells.

Known DNA interactions of Epithalon include:

• CD5 — Promotes immune cell differentiation
• IL-2 — Boosts IL-2 production, regulating white blood cells
• MMP2 — Enhances MMP activity, reducing inflammation
• Tram1 — Increases protein synthesis
• Arylalkylamine-N-acetyltransferase — Stimulates melatonin production
• pCREB t — Regulates circadian rhythms and has anti-cancer effects
• Telomerase — Extends cellular longevity

3. Epithalon and Skin Health

Epithalon positively regulates MMP2, a protein vital for connective tissue like skin. Rodent studies demonstrate that Epithalon activates fibroblasts, cells responsible for producing MMP2, collagen, elastin, and other matrix components. Mice treated with Epithalon showed a 30-45% increase in fibroblast activation[7].

By activating fibroblasts, Epithalon supports faster healing and counters the natural age-related decline in skin structure and elasticity.

Additionally, Epithalon reduces caspase-3 activity, an enzyme involved in programmed cell death (apoptosis). This helps protect fibroblasts and skin cells, keeping them healthier and alive longer[8].

4. Epithalon and Tumor Growth

In cancer research, daily administration of Epithalon to rats reduced tumor growth[9] and prevented metastasis—the spread of tumors to distant tissues[10][11].

Currently, Epithalon is under investigation for treating Her-2/neu positive breast cancer and shows potential for preventing certain leukemias and testicular cancer[12][13].

Slowed tumor growth in mice exposed to epithalon compared to controls
Source: Wiley Online Library

There is evidence that Epithalon activates the gene for the PER1 protein, which is primarily found in the hypothalamus. PER1 plays a key role in regulating the circadian rhythm and is known to be under-expressed in cancer patients. It remains unclear whether this under-expression precedes cancer development—potentially contributing to tumor growth—or if it is a consequence of cancer progression.

What is clear, however, is that PER1 influences cancer growth once tumors are established. Regulating PER1 expression may provide a natural way to slow tumor growth.

Research indicates that increased PER1 expression sensitizes cancer cells to radiation therapy, potentially allowing for lower radiation doses in treatment[^14]. This reduction could minimize immediate side effects and decrease the risk of secondary tumors caused by high-dose radiation exposure.

PER1 Causes Increased Rates of Ionizing Radiation-Induced Cell Death
Source: Molecular Cell

5. Epithalon and Melatonin Secretion
Melatonin, a hormone closely linked to sleep regulation and aging, is produced by the pineal gland. Research in rats demonstrates that Epithalon and similar peptides influence both the synthesis and release of melatonin by modulating the expression of two key proteins: arylalkylamine-N-acetyltransferase (AANAT) and pCREB transcription protein[15]. Both proteins play crucial roles in melatonin production and the circadian (day/night) regulation of its release. Studies in monkeys further indicate that Epithalon can restore melatonin secretion to normal levels[16].

6. Epithalon and Eyesight
In a trial involving rats with retinitis pigmentosa, Epithalon improved outcomes in 90% of subjects[17]. The peptide appears to preserve the normal structure of the eye while enhancing the bioelectric function of the retina, which is essential for vision.

7. Safety and Usage Disclaimer:
Epithalon exhibits minimal side effects, with low oral and excellent subcutaneous bioavailability in mice. However, the per kilogram dosage used in mice does not directly scale to humans. Epithalon sold by Peptide Sciences is strictly for educational and scientific research purposes only and is not intended for human consumption. Purchase of Epithalon should be limited to licensed researchers only.

Article Author

The above literature was researched, edited, and organized by Dr. Logan, M.D. Dr. Logan holds a doctorate degree from Case Western Reserve University School of Medicine and a B.S. in Molecular Biology.

Scientific Journal Article

Professor Vladimir Khavinson is a leading figure in gerontology and peptide research. He serves as:

• President of the European region of the International Association of Gerontology and Geriatrics
• Member of the Russian and Ukrainian Academies of Medical Sciences
• Main gerontologist of the Health Committee of the Government of Saint Petersburg, Russia
• Director of the Saint Petersburg Institute of Bioregulation and Gerontology
• Vice-president of the Gerontological Society of the Russian Academy of Sciences
• Head of the Chair of Gerontology and Geriatrics at North-Western State Medical University, St. Petersburg
• Retired Colonel of Medical Service (USSR, Russia)

Prof. Khavinson is renowned for the discovery, experimental, and clinical study of new classes of peptide bioregulators, and for the development of bioregulating peptide therapy. His research focuses on the role of peptides in regulating aging mechanisms. Over his 40-year career, he has designed, and conducted pre-clinical and clinical studies on new peptide geroprotectors aimed at slowing aging and extending human lifespan.

His work has led to the introduction of six peptide-based pharmaceuticals and 64 peptide food supplements into clinical practice. He holds 196 patents (both Russian and international) and has authored 775 scientific publications. His major works include the books:

• Peptides and Ageing (NEL, 2002)
• Gerontological Aspects of Genome Peptide Regulation (Karger AG, 2005)

Prof. Khavinson also introduced the scientific specialty “Gerontology and Geriatrics” in Russia at the governmental level and has overseen over 200 Ph.D. and Doctorate theses internationally.

Disclaimer

Prof. Vladimir Khavinson is referenced as one of the leading scientists involved in the research and development of Epitalon. He does not endorse or advocate the purchase, sale, or use of this product for any reason. There is no affiliation or relationship, implied or otherwise, between Peptide Sciences and Prof. Khavinson. The citation of this scientist is solely to acknowledge and credit the extensive research and development efforts conducted by his group. Prof. Khavinson is listed under references [1], [2], [5], [6], [7], [9], [12], [13], [15], and [17].

References

1. V. N. Anisimov, S. V. Mylnikov, and V. K. Khavinson, “Pineal peptide preparation epithalamin increases the lifespan of fruit flies, mice and rats,” Mech. Ageing Dev., vol. 103, no. 2, pp. 123–132, Jun. 1998. [PubMed]
2. V. K. Khavinson, I. E. Bondarev, and A. A. Butyugov, “Epithalon peptide induces telomerase activity and telomere elongation in human somatic cells,” Bull. Exp. Biol. Med., vol. 135, no. 6, pp. 590–592, Jun. 2003. [PubMed]
3. T. A. Dzhokhadze, T. Z. Buadze, M. N. Gaiozishvili, M. A. Rogava, and T. A. Lazhava, “[Functional regulation of genome with peptide bioregulators by hypertrophic cardiomyopathy (by patients and relatives)],” Georgian Med. News, no. 225, pp. 94–97, Dec. 2013. [PubMed]
4. V. N. Anisimov et al., “Effect of Epitalon on biomarkers of aging, life span and spontaneous tumor incidence in female Swiss-derived SHR mice,” Biogerontology, vol. 4, no. 4, pp. 193–202, 2003. [PubMed]
5. V. K. Khavinson, S. I. Tarnovskaya, N. S. Linkova, V. E. Pronyaeva, L. K. Shataeva, and P. P. Yakutseni, “Short cell-penetrating peptides: a model of interactions with gene promoter sites,” Bull. Exp. Biol. Med., vol. 154, no. 3, pp. 403–410, Jan. 2013. [PubMed]
6. N. S. Lin’kova, B. I. Kuznik, and V. K. Khavinson, “[Peptide Ala-Glu-Asp-Gly and interferon gamma: their role in immune response during aging],” Adv. Gerontol. Uspekhi Gerontol., vol. 25, no. 3, pp. 478–482, 2012. [PubMed]
7. N. I. Chalisova, N. S. Lin’kova, A. N. Zhekalov, A. O. Orlova, G. A. Ryzhak, and V. K. Khavinson, “[Short peptides stimulate skin cell regeneration during ageing],” Adv. Gerontol. Uspekhi Gerontol., vol. 27, no. 4, pp. 699–703, 2014. [PubMed]
8. N. S. Lin’kova et al., “Peptide Regulation of Skin Fibroblast Functions during Their Aging In Vitro,” Bull. Exp. Biol. Med., vol. 161, no. 1, pp. 175–178, May 2016. [PubMed]
9. I. A. Vinogradova, A. V. Bukalev, M. A. Zabezhinski, A. V. Semenchenko, V. K. Khavinson, and V. N. Anisimov, “Effect of Ala-Glu-Asp-Gly peptide on life span and development of spontaneous tumors in female rats exposed to different illumination regimes,” Bull. Exp. Biol. Med., vol. 144, no. 6, pp. 825–830, Dec. 2007. [PubMed]
10. G. Kossoy, V. N. Anisimov, H. Ben-Hur, N. Kossoy, and I. Zusman, “Effect of the synthetic pineal peptide epitalon on spontaneous carcinogenesis in female C3H/He mice,” Vivo Athens Greece, vol. 20, no. 2, pp. 253–257, Apr. 2006. [PubMed]
11. V. N. Anisimov et al., “Inhibitory effect of the peptide epitalon on the development of spontaneous mammary tumors in HER-2/neu transgenic mice,” Int. J. Cancer, vol. 101, no. 1, pp. 7–10, 2002. [PubMed]
12. V. N. Anisimov, V. K. Khavinson, I. N. Alimova, A. V. Semchenko, and A. I. Yashin, “Epithalon decelerates aging and suppresses development of breast adenocarcinomas in transgenic her-2/neu mice,” Bull. Exp. Biol. Med., vol. 134, no. 2, pp. 187–190, Aug. 2002. [PubMed]
13. I. A. Vinogradova, A. V. Bukalev, M. A. Zabezhinski, A. V. Semenchenko, V. K. Khavinson, and V. N. Anisimov, “Geroprotective effect of ala-glu-asp-gly peptide in male rats exposed to different illumination regimens,” Bull. Exp. Biol. Med., vol. 145, no. 4, pp. 472–477, Apr. 2008. [PubMed]
14. S. Gery, N. Komatsu, L. Baldjyan, A. Yu, D. Koo, and H. P. Koeffler, “The circadian gene per1 plays an important role in cell growth and DNA damage control in human cancer cells,” Mol. Cell, vol. 22, no. 3, pp. 375–382, May 2006. [PubMed]
15. V. K. Khavinson, L. K. Shataeva, and A. A. Chernova, “Effect of regulatory peptides on gene transcription,” Bull. Exp. Biol. Med., vol. 136, no. 3, pp. 288–290, Sep. 2003. [PubMed]
16. O. V. Korkushko et al., “[Normalizing effect of the pineal gland peptides on the daily melatonin rhythm in old monkeys and elderly people],” Adv. Gerontol. Uspekhi Gerontol., vol. 20, no. 1, pp. 74–85, 2007. [PubMed]
17. V. Khavinson, M. Razumovsky, S. Trofimova, R. Grigorian, and A. Razumovskaya, “Pineal-regulating tetrapeptide epitalon improves eye retina condition in retinitis pigmentosa,” Neuro Endocrinol. Lett., vol. 23, no. 4, pp. 365–368, Aug. 2002. [PubMed]

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The products offered on this website are furnished for in-vitro studies only. In-vitro studies (Latin: in glass) are performed outside of the body. These products are not medicines or drugs and have not been approved by the FDA to prevent, treat, or cure any medical condition, ailment, or disease. Bodily introduction of any kind into humans or animals is strictly forbidden by law.