Peptide preparations of Pineal Gland in age-Prevention

October 14, 2021

Pineal gland – what is it? 

Pineal gland (lat. Corpus pineale, epiphysis cerebri) is one of the most famous endocrine glands in the scientific community, and interest in it continues to grow: there is a Journal of Pineal Research and international conferences and symposia devoted to this topic are held annually. The rapid development of chronobiology (the science of cyclic processes in the body) imposed the leading role of the pineal gland and its hormone melatonin in the implementation of circadian, seasonal and annual rhythms of various functional systems of the body [2]. 

Pineal gland as a morphological structure has been known for more than 2,000 years. Ancient philosophers considered it to be a means of clairvoyance and reflection of the soul reincarnation. [8] The term “pineal gland” was first introduced by Claudius Galenus a Greek physician, surgeon and philosopher. The term comes from the name “glandula pinealis” (pinea – Italian pine). In appearance, the pineal gland indeed resembles a pine cone, has a slightly bumpy surface and a grayish-red color, its average length is 8-10 mm, width – 6 mm.

Epiphysis is located in the epithalamus, near the center of the brain, between the two hemispheres, tucked in a groove where the two halves of the thalamus join. Epiphysis is especially noticeable at a young age, the size of the gland grows until 2 y.o. and remains more or less constant until 18-20 y.o., later calcium and magnesium salts are deposited in it. The mass of the pineal gland in adults is approximately 120 mg.

The pineal gland is a neuroendocrine transducer that responds to nerve impulses by producing hormones, including:

• secretion of serotonin (“hormone of happiness”);
• secretion of melatonin (“hormone of youth”);
• secretion of antigonadotropins mostly used in gynecology;
• secretion of adrenoglomerular hormone, which affects the adrenal glands and regulates blood pressure.

There is a book devoted to pineal gland peptides and age-related aspects. It is written by Dr Vladimir Khavinson and his colleagues and titled “Peptide Preparations of Thymus and Pineal Gland in Prevention of Accelerated Aging”. Dr Khavinson is an honored Soviet and Russian scientist, European Chair (President) of the International Association of Gerontology and Geriatrics (2011-2015), Director of the Saint-Petersburg Institute of Bioregulation and Gerontology who dedicated his life to the issues of accelerated aging and its prevention.

This book generalizes results of the authors’ research work of many years devoted to the study of effectiveness of pineal gland and thymus peptide preparations in human aging. The up-to-date approaches to accelerated aging and main directions in its prevention are outlined. The physiological and pharmacological effectiveness of pineal gland preparation in particular, their influence on the functional state of cardiovascular and central nervous systems, immune and endocrine status of the organism, lipid and carbohydrate metabolism, hepatic detoxicating capacity, and functional age of the organism’s physiological systems are thoroughly reviewed. The patterns of epithalamin application for the prevention of accelerated aging as well as of the treatment of age-dependent pathology are proposed. The book may be of interest for physiologists, pharmacists, immunologists, geriatric specialists and nootropic enthusiasts. 

We thought it might be interesting for you to get acquainted with the English contents of the book. Though the main text is in Russian, we have summarized a few ideas and given links to research below.  

Epiphysis peptides or How can I support my pineal gland? 

Peptides are biologically active substances, protein compounds of several amino acids that regulate intracellular processes and ensure the normal functioning of organs and tissues. There are short peptides consisting of 2–4 amino acids called cytogens, and peptides consisting of more ones. More than 7,000 naturally occurring peptides are known nowadays. Many of them have important functions in the body, including acting as hormones, neurotransmitters, growth factors, ion channel ligands, or anti-infective agents. [6] 

We get peptides from food every day. Food that we eat contains proteins. In the stomach they are split into short peptides, which are not further degraded. These short peptides are absorbed in the intestine, enter the bloodstream, then into cells, bind to specific surface receptors of cells, such as G-protein-coupled receptors (GPCR) or ion channels, thereby triggering intracellular reactions. This is the essence of proper nutrition.

Advantages of peptides

Peptides do not replace the function of organs, but help to normalize and prolong their work. Peptides are easily and organically “incorporated” into the vital processes of the human body. The peptides of the research are said to have no side effects. They work on certain organs (tissues) in a targeted manner, have a mild normalizing action and do not accumulate in the body. Given their attractive pharmacological profile and other properties such as safety, good tolerability and efficacy, peptides represent an optimal base for the development of new therapeutic agents.

It is believed that the most important function of the pineal gland is the production of Melatonin. If the synthesis of melatonin is normal, the hormonal status of the body is stable. This means that the endocrine, immune, reproductive and nervous body systems function correctly, the process of cell proliferation and differentiation takes place without pathological changes, this reduces the risk of developing cancer and prolongs the active phase of healthy longevity.

If the pineal gland is unbalanced and does not produce melatonin and other hormones in sufficient quantities, hormonal disruption and imbalance in the work of organs and systems of the human body occurs, which entails accelerated aging and the development of diseases of various origins.

Before the appearance of pineal gland peptides, the issue of insufficient production of melatonin was solved by the prescription of hormonal preparations containing synthetic melatonin in the form of a pure artificial hormone. There are also melatonin pills as well as sublingual melatonin sprays. But excessive use of exogenous melatonin is not recommended. Hence, we can conclude that a more optimal solution is to create conditions for the body to produce melatonin on its own. 

Endogenous melatonin is produced by the pineal gland in the required amount, and influences the body in a beneficial and physiological manner, preventing the excess of optimal norms. Therefore, the intake of natural and safe pineal gland peptides (Endoluten, Pineamin, Epifamin) is becoming more and more popular among nootropic enthusiasts. 

Anti-aging mechanisms of epiphysis peptides

Various functions of the pineal gland suggest that it plays an important role in the regulation of life expectancy. The aging of the pineal gland, which begins after puberty, leads to the aging of the whole organism. Therefore, it is important that the cells of the pineal gland remain intact as long as possible and perform all their functions in full. 

Proteins are very important for every cell of our body, pineal gland cells are no exception. Proteins form the DNA of the cell and participate in its metabolic processes. Thanks to the discovery made in 1999 by Günter Blobel, who received the Nobel Prize for his scientific work, it was established that proteins control the processes of intercellular interaction and determine the ability of the cell to heal itself. Lack of peptides (caused by age or pathology) accelerates tissue wear, aging processes and leads to the development of diseases. 

The information about how much a cell is supposed to divide is encoded in its genetic apparatus – DNA. It is located in the cell nucleus and has an X-shaped structure. The “shoulder” of DNA is called the telomere, which physically shortens as the number of divisions is spent.

Once in the body, the peptide freely passes through all tissue barriers: the cell membrane, the nuclear membrane and is embedded in the DNA structure, at the point of telomere shortening according to the principle of complementarity. The peptide “lengthens” telomeres by almost a half (42%) and restores the ability of DNA to synthesize protein, thus extending the life of the cell. The longer it divides, the longer it lives. [3]

In terms of the tissue (organ), which consists of these cells, it means the restoration of its structure and function. And in terms of the whole body – it is life extension, improvement of its quality, prevention and treatment of age-related diseases.

In “Peptide Preparations of Thymus and Pineal Gland in Prevention of Accelerated Aging” prof. Khavinson and his colleagues described a study of geroprotective properties of pineal gland peptides (namely Epithalamin) on mice. It was established that these peptides stimulate immune system cells and inhibit their aging; eliminate some age-related disturbances in fat and carbohydrate metabolism; prolonge ovarium cyclic activity and reproduction in senile mice. An important property of these peptides was their ability to prevent different types of tumors. [3]

The use of pineal gland peptides in Oncological practice

The effectiveness of epiphyseal peptides such as Endoluten, for maintaining vital functions in cancer patients after radiation and chemotherapy has been established. Considering the powerful antioxidant activity of melatonin, its use in oncological practice is a promising area.

It is possible to use melatonin as an independent agent (to a lesser extent), capable of slowing down the growth of some malignant tumors (for example, prostate cancer) by direct and indirect cytostatic effect on cancer cells (through a decrease in the production of tumor growth factors – prolactin and insulin-like growth factor 1) and as a symptomatic agent (melatonin or melatonin in combination with interleukin-2), allowing to reduce the severity of side effects (thrombocytopenia, asthenia, stomatin, neuropathy, but not alopecia and nausea) when using chemotherapy in cancer patients. [1] 

Endoluten

The peptide preparation of the pineal gland Endoluten® is designed to normalize the level of melatonin secretion, which decreases with age.

It is a natural pineal gland peptide for the hormonal system, created by the technology of regulatory peptides of Dr Vladimir Khavinson. Endoluten contains natural extracted A-8 peptides obtained from pineal gland tissues of healthy young animals.

According to the manufacturer Endoluten has the following properties:

• Its use helps to reduce the severity of pathologies and the manifestation of symptoms associated with hormonal disruptions.
• It works on the pituitary gland, which has an impact on the metabolism and reproductive function in women and men, therefore it is used in preparation for conceiving.

• It is recommended for use in case of increased stress, impaired immunity and bad habits.
• It is an anti-age drug with geroprotective properties.

Endoluten peptide is recommended for people starting from 25-30 y.o. to maintain the health of the hormonal system and the quantitative production of hormones at a normal level, as well as to curb the development of genetic predispositions associated with the diseases of the hormonal system. 

Pineamin

Pineamin® (drug analogue – Epithalamin)  is an injectable preparation containing Polypeptides of Pineal Gland (PPG), which helps to restore the optimal functional density of pineal gland cells, which, indirectly through the activation of internal inhibitory structures, can solve the problem of menopause symptoms without resorting to synthetic substitutes or analogs of female hormones. The preparation is produced by GeroPharm, one of the leading Russian pharmaceutical companies.

The traditional method of dealing with the manifestations of menopause is hormonal therapy. However, despite its effectiveness (up to 96%), a large number of patients do not agree to be treated with hormones because there are a serious number of restrictions, contraindications and side effects. In these cases, prescribing centrally-acting drugs, in particular Pineamin, is justified.

One of the features of Pineamin is the absence of a proliferative effect on target organs (cervix, endometrium) even with prolonged use, which was shown in a study conducted on 120 patients [9].

The results of an open comparative randomized controlled clinical study of the use of combination therapy, including Pineamin, in postmenopausal women showed that at all stages of the study, a more pronounced effect of the treatment was established in the group receiving combination therapy (1 mg estradiol + 5 mg dydrogesterone) with Pineamin, which was achieved more quickly for both vasomotor and other menopausal symptoms. Importantly, a more significant clinical effect was obtained without increasing the dose of menopausal hormone therapy. [13] It is important to note that before prescribing Pineamin, it is necessary to conduct a standard examination to exclude the so-called “menopause masks”, when similar symptoms are caused by other diseases.

Close analogue of Pineamin is Epithalamin developed by Dr Khavinson too. They both have a unidirectional stimulating effect on the melatonin-producing function of the pineal gland in elderly patients. [10] According to the research it can be recommended not only as part of the combination therapy of menopause but also as a means to restore the level of melatonin secretion in the elderly. 

Epifamin

Epifamin® is another endocrine bioregulator derived from the pineal gland of cattle. It is a complex of proteins and nucleoproteins that are identical to those in humans. Both Epifamin and Pineamin mentioned earlier are produced by GeroPharm. Though being a food supplement Epifamin is known to be less effective in comparison to Pineamin injections.

How does Epifamin work? It has a selective effect on the pineal gland cells, contributing to the regulation of hormonal metabolism, as well as the correction of immunity and the blood coagulation system, and the production of melatonin.

Due to the mechanism of transcytosis, the incoming protein in unchanged form enters its target – the cell of the pineal gland. Once in the cell, Epifamin saturates them with an optimal protein “diet”, allowing them to recover faster and normalize the performance of their functions – the production of melatonin, the maintenance of normal immunity and hormonal balance.

Clinical trials of Epifamin were carried out in 167 patients with asthenia, pronounced manifestations of the female climacteric period, dyshormonal myocardial dystrophy, as well as in cancer patients after radiation- and chemo-therapy. According to the results of the use of Epifamin for the treatment of asthenia, its high efficiency in getting rid of astheno-neurotic syndrome has been established. A good effect from the use of Epifamin was found in patients with headache syndrome, signs of dizziness and emotional instability. [7]

During the course of administration of Epifamin in patients with dyshormonal myocardial dystrophy, a decrease in the number and intensity of heart pain attacks, an increase in efficiency and normalization of the psycho-emotional state, and a positive dynamics of ECG indicators were found.

Why are epiphysis peptides so Expensive?

Although the price of many epiphysis peptides is quite high, it should be noted that the pineal gland is very small in size and weight. Accordingly, even one capsule of that same Endoluten per day is more than enough. The most effective scheme for using Endoluten is considered to be: 1 capsule in 2 days for a month. There is also a lingual Endoluten. It is recommended to take 5-6 drops sublingually prior to meals 3-4 times a day for a period of 1 month.

The course of peptide drugs (Pineamin, Endoluten, Epifamin) should be taken twice a year upon necessity. This approach guarantees the maximum effect and will provide an opportunity to save an impressive sum of money.

Currently, many therapeutic peptides and proteins are obtained by recombinant methods or synthetically, which is a new direction for scientific development. For example, the pineal gland peptide Epitalon is a synthetic peptide made of four amino acids: alanine, glutamic acid, aspartic acid and glycine (Ala-Glu-Asp-Gly). It is aimed to restore the proper functioning of the pineal gland and trigger the production of the necessary amount of melatonin.

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 Bibliography

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