Epitalon 25mg

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Size: 25mg
Contents: Epitalon (25mg)
Form: Lyophilized powder
Purity: >99%
SKU: P-EPITALON-25
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Epitalon for Sale

Research has shown that Epitalon, also known as AEDG peptide, or tetrapeptide Epitalon, or Epithalon or Epithalone, regulates the function of the brain, the pineal gland, and the eye retina. In several studies the following Epitalon benefits have been:

  • Epitalon enhances sleep, by stimulating the pineal gland, releasing more melatonin
  • The peptide stimulates the generation of telomerase, which inhibits age-related diseases
  • It provides strong antioxidant properties
  • Epitalon extended the workable integrity of the eyes’ retina

Guide to Epitalon Research

With recent technology and ongoing advanced developments in the scientific field, methods have developed to synthesize the complex peptide preparations from the extracts of several different tissues.

One such peptide found in the tissues is ‘Epithalamin’ which is produced in the pineal gland. Epithalamin is functional in increasing the melatonin production, improving the immunological and anticarcinogenic effects in rats and mice and restoring the reproductive function in old rodents. Similar effects of the peptide were observed in human trials, representing the geroprotector activity of the peptide in human volunteers (1).

Utilizing the recent advancements in science, a peptide similar to Epithalamin was synthesized, namely ‘Epitalon.’ Interestingly, Epitalon is a common peptide belonging to both pineal gland and eye retina, hence, most likely producing beneficial effects in both organs (1).

Introduction

Epitalon (aka Epithalon or Epithalone) is a synthetic tetrapeptide, also known as AEDG peptide, composed of amino acids Ala-Glu-Asp-Gly (2).

The peptide induces effects similar to Epithalamin via various modes of actions. This mechanism and further studies are further described below.

Epitalon Peptide History

The natural peptide, Epithalamin, was discovered by a Russian professor named Vladimir Khavinson, in the 1980s. During these preliminary studies (3), it became known that the peptide was potentially useful in old people, patients with liver disorders, mental health, retinal disorders and in delaying the aging effects in men.

Interestingly, it was also noted that when the peptide was administered in fetal cells that were telomerase negative, it induced catalytic effects of the enzymes by a possible reactivation of telomerase. This fact indicated that the peptide could possibly increase the lifespan of the cells and thereby the lifespan of the whole organism (3).

Later, the synthetic peptide Epitalon was first created at St. Petersburg Institute of Bioregulation and Gerontology in Russia (4).

Several studies have been conducted at the same institute, and it has been understood that the peptide plays a key role in decreasing the mortality rate in humans and inhibiting the delay in the bodily developments with age (4). These studies have shown potential anti-aging effects of the peptide.

Mode of Action

Longevity and Anti-Carcinogenic Effects of Epitalon

Studies (2) have shown that the peptide binds with the histones - HI/6 and HI/3 – located at different sites in the human tissues, which then interact with the DNA. This binding of the peptide and the histones leads to the increment of neurogenic differentiation of gene transcription involving markers such as Nestin, Beta Tubulin III and Doublecortin, by 1.6 to 1.8 times than usual. This neuronal differentiation and protein synthesis in retinal and human ligament stem cells potentially leads to the beneficial effects of the peptide.

Epitalon Anti-Aging Effects

In order to understand the anti-aging effects of various synthetic peptides, several studies were conducted to study their effect on cell proliferation, cell regeneration and aging, cellular apoptosis, and matrix modelling (5). It was noted that Epitalon inhibited the synthesis of MM-9 that usually increases upon aging and increased the proliferation and cellular regeneration process, which usually decreases upon aging. Consequently, the peptide induces suppression of the aging process.

Epitalon Benefits

Below are the key advantages of the peptide:

  • Anti-aging effects
  • Possesses geroprotective properties (capability to protect DNA through production of telomerase)
  • Increase melatonin production in the body
  • Increases life span
  • Potential use as an anticancer agent

Many research studies have been conducted which show the above listed benefits of the peptide. Various studies have been conducted in vitro and in vivo in animals (primarily rodents) as well as in humans.

Research and Clinical Studies

In Vitro Studies on Human Fetal Cells with Epitalon

This study (6) was conducted to understand the proliferative effects of the peptide on human fetal fibroblastic cells.

Pulmonary fibroblasts were isolated from the 24-week-old fetus, and it was noted that these fibroblasts lost their proliferative function at the 34th passage. These cells possessed extremely small telomeres sizes – these telomeres size was smaller than what it originally was during the 10th passage.

When Epitalon was administered in these otherwise aging cells, it was noted that it stimulated the development of telomeres, causing them to increase and restore their normal size. As a result of this size elongation, the telomeres caused 10 extra cell divisions than usual seen in the control cells. Thus, this study suggested that Epitalon overcame the Hayflick limit and extended the normal cell cycle in human cells (6).

Epitalon Studies on Aged Lymphocytic Cells

In this study (7), the lymphocytic cells were isolated and cultured from people aged between 76 and 80 years. The purpose of this study was to determine the effect of Epitalon on ribosomal cell activity and its impact on denaturation and polymorphism of heterochromatin.

The outcome of this study, post administration of the cell culture with Epitalon, was that the peptide induced activation of the ribosomal genes and decondensation of the heterochromatin. Consequently, it induced the release of genes that were otherwise suppressed due to the aging of the chromosomal regions.

This study suggested that Epitalon has the ability to modify the chromosome regions in the aging cells, activate chromatin and restore cellular activities that were otherwise suppressed or delayed in geriatric patients.

Epitalon Studies Showing Anti-Mutagenic Effects

In this 2011 study (8), three different mice models were used to determine the effect of the peptide on chromosomal aberrations. The three mice models were – SAMP-1 female mice with accelerated aging and wild rats SAMR-1 and SHR (both female mice).

Upon administration of Epitalon, it was noticed that the incidence of the chromosomal aberrations in the bone marrow of SAMP-1 mice with accelerated aging was almost 2 times higher than the other two models. When the peptide was administered at the age of 2 months in the mice, it decreased the chromosomal aberrations in all three models, the highest being in the SAMP-1 mice with accelerated aging.

On co-administration with melatonin, given with water in the dose of 20mg/liter during night time, there was no impact on the effects of the peptide.

This study suggested that Epitalon possessed antimutagenic effects, which probably is the underlying effect of its geroprotective properties.

Epitalon Studies Showing Anti-Carcinogenic Properties

In this study (9), one-year-old female (C3H/He) mice with tumors on the reproductive organs (mammary glands and ovaries) were selected. The tumors on the mammary glands included several variants of the invasive ductal carcinogenic cells, whereas, in the ovaries, the tumors found were granulosa cell tumors. These mice, kept in standard conditions for six months, were divided into two groups – the control group and the experimental group.

The dose given to the mice belonging to the experimental group was 0.5 mg of Epitalon, administered five times in a week.

Once the study was completed, it was discovered that 3 out of the 9 mice in the control group showed metastasis and an increase in the number of tumor cells. While the peptide treated mice showed that there was a decrease in the number of tumor cells. Epitalon, upon administration, inhibited the process of metastasis in the mice, which prevented tumor cell cycle and growth. This study highlighted the antimetastatic effects of the peptide, which leads to their anti-cancer properties.

Epitalon Studies in Hypophysectomized Birds

In this study (10), hypophysectomized birds, both young and old age were selected to study the effects of Epitalon peptide on the morphology of thymus gland. Hypophysectomized birds are birds in which the pituitary gland has been surgically removed.

Upon administration of the peptide, it was discovered that the morphology of the thymus gland was restored in all birds, regardless of their age. The most effective results were observed on birds (mainly chickens) that underwent a neonatal hypophysectomy before the peptide administration. This study further supported the earlier evidence showing the geroprotective properties of the peptide.

Human Clinical Trials with Epitalon

Epitalon Peptide Effects on Melatonin Levels

This study (11) was carried out on both aging monkeys and human volunteers to determine the effects of Epitalon on melatonin levels.

With increasing age, the melatonin levels in the body tend to decrease due to reduced secretion, which causes difficulty in sleep especially during night time. This was mainly because the functioning of the pineal gland deteriorated with increasing age and the hormone circadian rhythm amplitude is also reduced.

Upon administration of Epitalon, it stimulates effects similar to that caused by the natural secretion of the pineal gland. The melatonin levels in the body increase to normal levels, especially during the night time, which induces adequate sleep in elderly patients.

Peptide Effects on Retinal Cells

With the increasing age, eye sight tends to deteriorate. In this study (12), it was discovered that when Epitalon was administered in geriatric patients, it elevated the bioelectric and functional activities in the retina, thereby preserving the morphological structure of the retina. As a result, age-related retinal degeneration could be reversed in the old patients, which was evident by the positive clinical outcome in 90% of the patients treated with the peptide.

Geroprotective Effects of Epitalon

This study (13) was conducted in 266 elderly patients (over the age of 60 years) over the course of 6 to 8 years, where some patients were treated with peptide bioregulator Thymalin, others with Epitalon and the rest were treated with the combination of the two.

After the study, it was confirmed that both the peptides had the ability to restore the basic bodily functions in geriatric patients – including improving the cardiovascular, endocrinal, immune, and nervous systems, along with the metabolic and hemostatic activities. What's more, the peptide treated group showed a 2-fold decrease in the common geriatric disorders such as acute respiratory disorder, heart diseases and bone disorders.

As a result of these results, the mortality rate in the peptide treated patient significantly decreased – 2-fold decrease in the Thymalin treated patients, 1.8-fold decrease in the Epitalon treated patients, and 2.5-fold decrease in the patients treated with both peptides.

This study suggested that the peptide ingestion in elderly patients is safe and efficient, and could be potentially used in maintaining and treating age-related common disorders.

Epitalon Side Effects

Studies have been conducted (on both healthy adults and geriatric patients) which have determined the long-term efficacy and safety of the Epitalon peptide with negligible side effects. Limited side effects of the peptide have been noted during the clinical trials.

Common side effects of the use of the peptide are as follows, which are usually observed in overly sensitive people:

  • Pain, swelling and redness at the injection site
  • Headaches
  • Dizziness
  • Fatigue
  • Flu-like symptoms may occur temporarily

Epitalon Long Term Safety and Efficacy Profile

A randomized clinical trial (14) was conducted for 12 years on elderly patients suffering from coronary disease and increased aging of the cardiovascular system. Some elderly patients were treated with the Epitalon peptide, for 12 continuous years, and some patients were part of the control group (i.e., not treated with the peptide, but monitored for 12 years).

During these 12 years, the number of elderly patients who died (due to natural causes) were 28% less in the peptide treated group, despite the basic therapy in both groups being identical. There was a 2-fold decrease in cardiovascular failure and respiratory diseases in the peptide treated elderly patients. No severe adverse events were reported during this study.

This study depicted that the peptide not only possessed geroprotective properties but could be used long term in the life prognosis of the old patients without any severe adverse effect.

Epitalon Recommended Dosage

Various clinical trials have been conducted in humans with various doses and dosage forms.

In the long-term efficacy study in geriatric patients (14), the peptide was administered subcutaneously in patients at doses of 10mg every 3 days. Furthermore, in one of the clinical trials conducted (11), the peptide was administered during the evening time, to increase the melatonin levels in elderly patients.

While these studies have resulted in positive outcomes, the dosage form and the dose would be dependent on each case and purpose of application.

Summary

Epitalon, also known as AEDG, is a synthetic tetrapeptide composed of amino acids Ala-Glu-Asp-Gly. This peptide is highly similar to the naturally occurring peptide, Epithalamin, producing similar effects in the human body. Epithalamin was first discovered and thereby synthetically developed in Russia. Several research studies for Epitalon have also been conducted here, to determine the full potency and efficacy of the peptide in humans.

Analogous to Epithalamin, this peptide causes anti-aging effects by increasing cell proliferation and growth, possesses geroprotective properties as it elongates the activities of the telomerase cells and has anticarcinogenic properties as it inhibits the metastasis and development of the tumor cells in the body.

Several research studies, both in vivo and in vitro, have been conducted to determine the extent and mechanism of the peptide effects in humans. Long term efficacy and safety profile of the medication has been established with minimal to no side effects reported in geriatric patients.

All studies conducted in geriatric patients have yielded positive outcomes – causing restoration of the bodily functions to normal rate (which otherwise decline with increasing age) and decline in the rate of common disorders caused in elderly patients. Consequently, studies have shown that Epitalon causes a decrease in the mortality rate – with no severe adverse effects. It's one of the highlights of this peptide, making it a promising candidate in the medical field for treating old patients.

References:

1. Khavinson VKh. Peptides and Ageing. Neuro Endocrinol Lett. 2002;23 Suppl 3:11-144. PMID: 12374906. https://pubmed.ncbi.nlm.nih.gov/12374906/

2. Khavinson, Vladimir et al. “AEDG Peptide (Epitalon) Stimulates Gene Expression and Protein Synthesis during Neurogenesis: Possible Epigenetic Mechanism.” Molecules (Basel, Switzerland) vol. 25,3 609. 30 Jan. 2020, doi:10.3390/molecules25030609. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7037223/

3. Khavinson VKh, Bondarev IE, Butyugov AA. Epithalon peptide induces telomerase activity and telomere elongation in human somatic cells. Bull Exp Biol Med. 2003 Jun;135(6):590-2. doi: 10.1023/a:1025493705728. https://pubmed.ncbi.nlm.nih.gov/12937682/

4. Khavinson VKh, Kuznik BI, Tarnovskaia SI, Lin'kova NS. [Peptides and CCL11 and HMGB1 as molecular markers of aging: literature review and own data]. Adv Gerontol. 2014;27(3):399-406. Russian. https://pubmed.ncbi.nlm.nih.gov/25826983/

5. Lin’kova, N.S., Drobintseva, A.O., Orlova, O.A. et al. Peptide Regulation of Skin Fibroblast Functions during Their Aging In Vitro . Bull Exp Biol Med 161, 175–178 (2016). https://doi.org/10.1007/s10517-016-3370.

6. Khavinson VKh, Bondarev IE, Butyugov AA, Smirnova TD. Peptide promotes overcoming of the division limit in human somatic cell. Bull Exp Biol Med. 2004 May;137(5):503-6. doi: 10.1023/b:bebm.0000038164.49947.8c. PMID: 15455129. https://pubmed.ncbi.nlm.nih.gov/15455129/

7. Khavinson VKh, Lezhava TA, Monaselidze JR, Jokhadze TA, Dvalishvili NA, Bablishvili NK, Trofimova SV. Peptide Epitalon activates chromatin at the old age. Neuro Endocrinol Lett. 2003 Oct;24(5):329-33. PMID: 14647006. https://pubmed.ncbi.nlm.nih.gov/14647006/

8. Rosenfeld SV, Togo EF, Mikheev VS, Popovich IG, Khavinson VKh, Anisimov VN. Effect of Epithalon on the incidence of chromosome aberrations in senescence-accelerated mice. Bull Exp Biol Med. 2002 Mar;133(3):274-6. doi: 10.1023/a:1015899003974. PMID: 12360351. https://pubmed.ncbi.nlm.nih.gov/12360351/

9. Kossoy G, Anisimov VN, Ben-Hur H, Kossoy N, Zusman I. Effect of the synthetic pineal peptide Epitalon on spontaneous carcinogenesis in female C3H/He mice. In Vivo. 2006 Mar-Apr;20(2):253-7. PMID: 16634527. https://pubmed.ncbi.nlm.nih.gov/16634527/

10. Pateyk AV, Baranchugova LM, Rusaeva NS, Obydenko VI, Kuznik BI. Effect of peptides Lys-Glu-Asp-Gly and Ala-Glu-Asp-Gly on the morphology of the thymus in hypophysectomized young and old birds. Bull Exp Biol Med. 2013 Mar;154(5):681-5. doi: 10.1007/s10517-013-2029-0. PMID: 23658898. https://pubmed.ncbi.nlm.nih.gov/23658898/

11. Korkushko OV, Lapin BA, Goncharova ND, Khavinson VKh, Shatilo VB, Vengerin AA, Antoniuk-Shcheglova IA, Magdich LV. [Normalizing effect of the pineal gland peptides on the daily melatonin rhythm in old monkeys and elderly people]. Adv Gerontol. 2007;20(1):74-85. Russian

12. Khavinson V, Razumovsky M, Trofimova S, Grigorian R, Razumovskaya A. Pineal-regulating tetrapeptide Epitalon improves eye retina condition in retinitis pigmentosa. Neuro Endocrinol Lett. 2002 Aug;23(4):365-8. PMID: 12195242. https://pubmed.ncbi.nlm.nih.gov/12195242/

13. Khavinson VKh, Morozov VG. Geroprotektornaia éffektivnost' timalina i épitalamina [Geroprotective effect of thymalin and Epithalamin]. Adv Gerontol. 2002;10:74-84. Russian. PMID: 12577695. https://pubmed.ncbi.nlm.nih.gov/12577695/

14. Korkushko OV, Khavinson VKh, Shatilo VB, Antonyuk-Shcheglova IA. Geroprotective effect of Epithalamine (pineal gland peptide preparation) in elderly subjects with accelerated aging. Bull Exp Biol Med. 2006 Sep;142(3):356-9. English, Russian. doi: 10.1007/s10517-006-0365-z. PMID: 17426848. https://pubmed.ncbi.nlm.nih.gov/17426848/


 

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