N-Acetyl Epithalon Amidate is a modified version of the synthetic peptide Epithalon (a.k.a. Epitalon). Epithalon itself is a component of naturally occurring cow pineal gland extract that is now produced synthetically. It is well known in research settings for its anti-aging properties and significant effects on cancer, infectious disease, DNA (primarily telomere) regulation, and skin health.
Even though Epithalon was discovered roughly forty years ago at the St. Petersburg Institute of Bioregulation and Gerontology, the peptide is still under active research and providing new insights. Most recently, scientists proposed potential epigenetic mechanisms to explain the influence that Epithalon has on neuronal differentiation of stem cells.
The modifications to Epithalon do not alter the peptide’s overall function, but they do alter the half-life, stability, and efficacy of Epithalon. Only two modifications are made to the native peptide: N-acetylation and amidation. Each has specific benefits that make Epithalon more potent and allow for lower dosing of the peptide.
Acetylation is a common, natural process that occurs to many proteins in the body. It is also a process used by the pharmaceutical industry to help a compound to reach the central nervous system. Acetylated molecules are much more capable of crossing the blood-brain barrier (BBB). Acetylation has been shown to increase the rate at which a compound crosses the BBB, thereby increasing the intensity of the compound’s effects and helping reduce the dosage of a compound required to achieve a specific outcome. Aspirin, for instance is the acetylated form of salicylic acid. Research shows that acetylation of salicylic acid increases the anti-inflammatory effects of the molecule.
Amidation is another natural protein modification that has been coopted by the pharmaceutical industry to improve the half-life of compounds. Amidated proteins are less sensitive to proteolytic degradation in the blood stream. They also tend to bind more strongly to their receptors, making amidation an excellent means of increasing potency and efficacy of a compound.
By altering Epithalon via acetylation and amidation, it is possible to increase the penetration of the peptide into the central nervous and protect it from degradation during the process. The result is increased potency of a given dose of Epithalon as well as increased efficacy of the compound due to improved receptor binding
n-アセチルエピタロンは、脳と脳
Research in cell culture shows that Epithalon influences gene expression in neurogenetic differentiation as well as protein synthesis. Molecular modeling suggests that occurs through epigenetic modulation of a handful of genes coding for the proteins Nestin, GAP43, β Tubulin III, and Doublecortin. Epithalon increases expression of these peptides by as much as 1.8 times via binding with specific histone proteins and allowing the genes to be accessed more easily[1]. The result of easier access to the DNA in those regions is increased expression of the genes and thus increased protein production.
The proteins being affected by Epithalon are important in the growth and development of neurons as follows.
The ability of Epithalon to regulate gene expression patterns is hardly limited to the CNS. Research in skin stem cell cultures shows that Epithalon, even at very low concentrations increases proliferation of stems cells in rats regardless of age. In particular, fibroblast proliferation rates increase by as much as 45%[3].
It isn’t just the growth of fibroblasts that is affected, however. Research shows that Epithalon (and other short polyfunctional peptides) decrease rates of apoptosis and increase functional activity of fibroblasts[4]. This leads to “normalization” of the intracellular matrix. In other words, Epithalon restores homeostasis (biological balance) to the skin and helps to shift the balance in aging skin toward more youthful production of things like collage, elastin, and other proteins[4]. The net result is improved skin health. In fact, Epithalon has opened up a new field in research, referred to as gerontocosmetology, focused on skin health in age.
It is important to note that while cosmetology has a definite component focused on appearance, the field is much deeper than that. The visual effects of cosmetology overlay the deeper components of skin health. Aging skin appears wrinkled, for instance, because of a loss of extracellular matrix proteins like collagen and elastin. Replacement of these proteins, among others, reduces the appearance of wrinkles but also improves the strength and integrity of skin. Skin is the first line of defense against infection and is often referred to as the large organ of the immune system. Healthy skin means less infection, faster wound healing, better insulation against cold, improved response to heat, and much more. Thus, the field of gerontocosmetology is focused not just on the surface, but on the holistic health of the skin and thus the human body[3].
As noted above, Epithalon regulates the production of the protein PER1, which plays an important role in circadian rhythm. This should come as no surprise given that Epithalon was first isolated from the pineal gland of cows and the primary role of the pineal gland is to regulate the sleep-wake cycle and the response of many animals to light. Research in rats shows that Epithalon also regulates the production and release of melatonin, which is a potent regulator of sleep.
Via action at the genes for arylalkylamine-N-acetyltransferase and pCREM, Epithalon increases melatonin production and can restore normal sleep-wake cycles[8]. Melatonin and sleep patterns often become dysregulated because of age, a phenomenon that is more than likely a result of changes in DNA expression patterns. By restoring DNA expression to a more youthful state, Epithalon helps to offset age-related changes in sleep. This, in turn, as a tremendous impact on everything from cognitive function to wound healing, the immune response, growth hormone secretion, weight gain, bone structure, and cardiovascular health.
n-アセチルエピタロンの環境と老化
Each of the above sections has dealt with a specific feature of Epithalon function, but each has also made note of the fact that Epithalon helps to restore DNA expression patterns in aging animals to those seen in younger animals. Indeed, restoration of youthful DNA expression patterns is the overarching theme associated with Epithalon. Production of this peptide by the pineal gland appears to decline with age, resulting in many of the age-related changes that impact health and longevity. Supplementation with Epithalon in insects and rodents has shown that Epithalon can decrease mortality by more than half and prolong life by as much as 27%[9].
The above changes in DNA expression patterns, possibly through epigenetic changes that result of histone protein binding, is at least part of the reason that Epithalon has such profound effects on aging. It is not the whole story though. Research shows that Epithalon also impacts antioxidant activity and telomere health.
In rat models. Injection of Epithalon has been shown to decrease LPO production and reduce oxidative modification of proteins[10]. LPO production (lipid peroxidation products) result from lipid peroxidation, which is a normal biological process known to production free radicals. LPO is necessary for several normal biological functions, such as the destruction of invading pathogens and the recycling of damaged proteins. The production of potentially dangerous free radicals is offset by the equal production of antioxidants. With aging, however, antioxidant production wanes thus cellular and protein damage from free radical production increases. Epithalon offsets the decline in antioxidant production and thus helps to maintain the homeostatic balance that prevents damage from free radicals.
Research in human somatic cells shows that Epithalon activates an enzyme called telomerase[11]. Telomerase is important for maintain the end caps of DNA called telomeres. Telomeres are regions of the DNA that don not contain genes, but instead protect DNA during the process of replication. Replication slowly erodes DNA so having telomeres helps to prevent functional DNA from being damaged. Unfortunately, telomeres themselves degrade over time and when they get too short, cells stop functioning and eventually die. Telomerase helps to repair telomeres and thus helps to extend the lifespan of cells. By increasing activity of telomerase, Epithalon is directly impacting the health of DNA and thus how long cells live[12], [13].
Aging, in general, can be divided into several categories, but they are all interlinked. In general, DNA damage leads to protein malfunction. This, combined with direct protein damage, leads to cellular dysfunction. As cellular dysfunction accumulates, cells are either killed or become non-functional in a process known as senescence. Over time, both processes lead to tissue and organ dysfunction that eventually produces signs of aging like changes in sleep patterns, weight gain, wrinkling, greying of the hair, and increased incidence of chronic disease. The accumulation of this “macro-damage” is what eventually leads to death as the body becomes unable to sustain normal biological function. Epithalon helps to offset much of this dysfunction by regulating DNA and protein damage at a fundamental level.
ウラジミール・ハビンソン老年学と老年学の国際協会の欧州地域の教授であり、ヨーロッパ地域の会長です。のメンバー医学科学のロシア語とウクライナのアカデミー;ロシア州政府政府の保健委員会の主要老年学者。聖ペテルブルク生物調節および老年学研究所のディレクター。老年学会の副会長ロシア科学アカデミー;セントペテルブルクの老年医学および老年科学老年科学部長。医療サービス大佐（ロシア、ソ連）、退職。VladimirKhavinsonは、新しいクラスの発見、実験、臨床研究で知られていますペプチド生体調節因子と生体育成ペプチド療法の開発。彼は、老化のメカニズムの調節におけるペプチドの役割を研究することに従事しています。彼の主な行動分野は、新しいペプチドの設計、臨床前、臨床研究ですゼロゲロテクター. A 40-year-long investigation resulted in a multitude of methods of application of peptide bioregulators to slow down the process of ageing and increase human life span. Six peptide-based pharmaceuticals and 64 peptide food supplements have been introduced into clinical practice by V. Khavinson. He is an author of 196 patents (Russian and international) as well as of 775 scientific publications.His major achievements are presented in two books: “Peptides and Ageing” (NEL, 2002)and “Gerontological aspects of genome peptide regulation” (Karger AG, 2005).Vladimir Khavinson introduced scientific specialty “Gerontology and Geriatrics” in the Russian Federation on the governmental level. Academic Council headed by V. Khavinson has oversighted over 200 Ph.D. and Doctorate theses from many different countries.
Prof. Vladimir Khavinson is being referenced as one of the leading scientists involved in the research and development of N-Acetyl Epithalon Amidate. In no way is this doctor/scientist endorsing or advocating the purchase, sale, or use of this product for any reason. There is no affiliation or relationship, implied or otherwise, between
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