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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.
N-asetil epitalon mengumpulkan struktur
Urutan asam amino:Ala-glu-asp-glyFormula Kimia:C14H22N4HAI9Massa molekul:390.349 g/molPubchem CID: 219042
Massa molekul:446.45 g/molNomor CAS:307297-39-8Sinonim:Epitalon, Epithalon, Epithalamine, EpithalamineSumber:PubchDi sini, dalam urutan, "Ac-" mewakili kelompok asetil yang melekat pada N-terminus peptida, dan "-NH2" mewakili kelompok yang di tengah di C-terminus. Urutan asam amino "Agagaaga" sesuai dengan inti epitalon peptida. Acetyl-Epitalon-Amidate adalah versi yang dimodifikasi dari Epitalon, peptida sintetis dengan sifat anti-penuaan dan aktivasi telomerase yang potensial. Penambahan asetil dan kelompok yang di tengah dapat meningkatkan stabilitas, ketersediaan hayati, dan kemanjurannya.
Epithalon N-Acetyl Amidasi: Modifikasi
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
Epithalon N-asetil mengumpulkan dan otak
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.
Nestin - Protein filamen menengah ini diekspresikan dalam sel saraf dan memainkan peran penting dalam pertumbuhan radial akson. Ini juga membantu sel induk untuk berdiferensiasi menjadi sel -sel saraf, sehingga merangsang pertumbuhan jaringan dalam sistem saraf pusat (SSP).
GAP43 - GAP43 sering disebut protein "plastisitas" karena memainkan peran penting dalam kerucut pertumbuhan neuron selama pengembangan dan regenerasi aksonal. Ini memainkan peran penting dalam belajar. Penghapusan bahkan satu alel gen GAP43 mengarah pada kecacatan intelektual.
β Tubulin III - Elemen mikrotubulus ini ditemukan dalam neuron dan sel testis di mana ia terlibat dalam pembentukan mikrotubulus dan respons stres oksidatif. Penelitian menunjukkan bahwa penting dalam adaptasi seluler terhadap stres molekuler dan bahwa kekurangan dalam protein ini dapat memainkan peran kunci dalam agresivitas tumor.
DoubleCortin-Doublecortin adalah protein terkait mikrotubulus yang ditemukan pada neuron yang belum matang. Sangat penting untuk pengembangan struktur otak yang kompleks. Kekurangan dalam doublecortin telah dikaitkan dengan sindrom korteks ganda di mana kurangnya migrasi neuron yang belum matang menyebabkan otak yang halus pada pria dan neuron yang salah tempat pada wanita. Hasil kekurangan adalah kecacatan intelektual yang mendalam.
Dengan meningkatkan akses ke daerah DNA yang mengandung gen yang mengontrol protein di atas, epithalon telah dikaitkan dengan peningkatan pembelajaran, meningkatkan pemulihan dari cedera SSP, dan berpotensi dengan pengurangan efek jangka panjang penuaan pada otak. Fitur terakhir ini hanyalah salah satu dari banyak cara di mana epithalon ditemukan secara positif mempengaruhi proses penuaan. Secara khusus, epithalon telah terbukti mempengaruhi diferensiasi sel induk neuron dengan mempromosikan pertumbuhan dan perkembangan neuron dari progenitor sel induk [2]. Dengan waktu paruh yang lebih panjang dan penetrasi yang lebih baik di SSP, potensi, dan efek epithalon N-asetil yang dinamai akan ditingkatkan dibandingkan dengan epithalon standar.
Epithalon N-asetil mengumpulkan dan kesehatan kulit
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].
Epithalon N-asetil mengumpulkan dan kesehatan kekebalan tubuh
Area lain di mana Epithalon memainkan peran aktif dalam regulasi gen adalah sistem kekebalan tubuh. Penelitian kultur sel menunjukkan bahwa epithalon mengubah ekspresi molekul pensinyalan kekebalan seperti CD5, IL-2, arylalkylamine-N-acetyltransferase, interferon gamma, dan tram1. Masing -masing protein ini mempengaruhi sistem kekebalan tubuh sebagai berikut.
CD5 - CD5 mempengaruhi diferensiasi sel -sel dari sistem kekebalan tubuh, membantu sel induk untuk beralih ke sel -sel fungsional yang melawan infeksi dan memerangi peradangan.
IL-2-IL-2 adalah regulator yang kuat dari produksi sel darah putih.
Arylalkylamine-N-acetyltransferase-enzim ini sangat penting untuk produksi melatonin, yang tidak hanya penting dalam tidur tetapi juga memainkan peran penting dalam regulasi sistem kekebalan tubuh.
Interferon Gamma - Penelitian pada tikus menunjukkan bahwa interferon gamma penting dalam melawan infeksi melalui aktivasi makrofag, sel pembunuh alami, dan sel T. Ini seperti memainkan peran penting dalam respons tubuh terhadap infeksi virus khususnya [5].
Kerusakan respons imun adalah salah satu penanda utama dan pendorong penuaan. Fungsi kekebalan yang tidak teratur menyebabkan peradangan kronis dan berperan dalam pengembangan penyakit kardiovaskular dan demensia. Kemampuan epithalon untuk mengatur sistem kekebalan adalah salah satu cara di mana ia menggagalkan efek penuaan. Sekali lagi, kemampuan Epithalon N-asetil turun ke SSP membantu memastikan bahwa efek peningkatan kekebalannya dialami di otak, di mana regulasi peradangan dapat membantu meredam proses yang menyebabkan demensia.
Epithalon N-asetil mengumpulkan dan kanker
Penelitian dalam model tikus berbagai tumor telah menunjukkan bahwa pemberian epithalon harian mengurangi pertumbuhan tumor [6]. Peptida saat ini sedang diselidiki sebagai bahan pembantu potensial untuk pengobatan kanker payudara HER-2/Neu positif (hormon positif) serta leukemia dan kanker testis. Menariknya, salah satu tindakan utama epithalon pada kanker tampaknya melalui regulasi gen per1. PER1, yang ditemukan di hipotalamus, mengatur ritme sirkadian dan telah ditemukan kurang terekspresikan pada pasien kanker [7].
Epithalon N-asetil mengumpulkan dan tidur
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.
Epithalon N-asetil mengumpulkan dan menua
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.
N-Acetyl Epithalon Amidasi: Ringkasan
Sementara Epithalon bukan jawaban tunggal untuk menghentikan proses penuaan, itu memberikan wawasan tentang bagaimana menangkal beberapa proses dasar yang menyebabkan DNA dan kerusakan protein dapat membantu menggagalkan proses penuaan secara keseluruhan. Menurut Dr. Vladimir Khavison, ayah baptis pengembangan epithalon, ketika penelitian epithalon terus berlanjut, sains mendapatkan pemahaman yang lebih dalam, lebih bernuansa tentang apa yang menyebabkan mamalia, secara umum, dan manusia untuk menua dan akhirnya mati. Epithalon adalah kunci penting untuk memahami bagaimana proses biokimia dapat diubah untuk memperlambat atau bahkan menghentikan beberapa penyebab mendasar penuaan. Pengembangan N-asetil Epithalon Amidasi adalah bagian penting dari penelitian epithalon karena kemampuannya untuk menembus SSP akan memudahkan para peneliti untuk mengeksplorasi efek epithalon pada penuaan di otak. Ini kemungkinan akan memberikan wawasan tentang bagaimana proses biokimia seperti tidur dan pertumbuhan neuron mempengaruhi pembelajaran, memori, ketahanan kognitif, dan banyak lagi.
Penulis artikel
Literatur di atas diteliti, diedit dan diselenggarakan oleh Dr. E. Logan, M.D. Dr. E. Logan memegang gelar doktor dariCase Western Reserve University School of Medicinedan seorang B.S. dalam biologi molekuler.
Penulis Jurnal Ilmiah
Vladimir Khavinsonadalah seorang profesor, presiden wilayah Eropa dari Asosiasi Internasional Gerontologi dan Geriatri; AnggotaAkademi Ilmu Kedokteran Rusia dan Ukraina; Gerontologist utama Komite Kesehatan Pemerintah Ofsaint Petersburg, Rusia; Direktur Institut Bioregulasi dan Gerontologi Saint Petersburg; Wakil presiden masyarakat gerontologisAkademi Ilmu Pengetahuan Rusia; Kepala Ketua Gerontology dan Geriatrics dari Universitas Kedokteran Negara Bagian Thenorth-Western, St-Petersburg; Kolonel Layanan Medis (USSR, Rusia), pensiunan. Vladimir Khavinson dikenal karena penemuan, studi eksperimental dan klinis kelas baru dariPeptidaBioregulator serta untuk pengembangan terapi peptida bioregulasi. Dia terlibat dalam mempelajari peran peptida dalam regulasi mekanisme penuaan. Bidang tindakan utamanya adalah desain, pra-klinis dan studi klinis peptida baruGeroprotektor. 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
Guru peptidadan dokter ini. Tujuan dari mengutip dokter adalah untuk mengakui, mengenali, dan menghargai penelitian lengkap dan upaya pengembangan yang dilakukan oleh para ilmuwan yang mempelajari peptida ini.
Kutipan yang direferensikan
V. Khavinsonet al.,AEDG Peptide (Epitalon) Stimulates Gene Expression and Protein Synthesis during Neurogenesis: Possible Epigenetic Mechanism ,”Mol. Basel Switz., vol. 25, no. 3, p. E609, Jan. 2020, doi: 10.3390/molecules25030609.
S. Caputiet al., “Effect of short peptides on neuronal differentiation of stem cells,”Int. J. Immunopathol. Pharmacol., vol. 33, p. 2058738419828613, Feb. 2019, doi: 10.1177/2058738419828613.
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.
V. K. Khavinson, N. S. Linkova, A. S. Diatlova, E. O. Gutop, and O. A. Orlova, “[Short peptides: regulation of skin function during aging.],”Adv. Gerontol. Uspekhi Gerontol., vol. 33, no. 1, Art. no. 1, 2020.
N. Lin’kova, B. Kuznik, and V. Khavinson, “The peptide Ala-Glu-Asp-Gly and interferon gamma: Their role in immune response during aging,”Adv. Gerontol., vol. 3, Apr. 2013, doi: 10.1134/S2079057013020100.
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, doi: 10.1007/s10517-007-0441-z.
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, doi: 10.1016/j.molcel.2006.03.038.
O. Korkushkoet al., “[Normalizing effect of the pineal gland peptides on the daily melatonin rhythm in old monkeys and elderly people],”Adv. Gerontol. Uspekhi Gerontol. Ross. Akad. Nauk Gerontol. Obshchestvo, vol. 20, pp. 74–85, Feb. 2007.
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, doi: 10.1016/S0047-6374(98)00034-7.
L. S. Kozina, “Effects of bioactive tetrapeptides on free-radical processes,”Bull. Exp. Biol. Med., vol. 143, no. 6, Art. no. 6, Jun. 2007, doi: 10.1007/s10517-007-0230-8.
V. Kh. 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, Art. no. 6, Jun. 2003, doi: 10.1023/A:1025493705728.
T. A. Dzhokhadze, T. Z. Buadze, M. N. GaÄozishvili, 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, Art. no. 225, Dec. 2013.
V. N. Anisimov, “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, doi: 10.1023/a:1025114230714.Semua artikel dan informasi produk yang disediakan di situs web ini hanya untuk tujuan informasi dan pendidikan.Produk yang ditawarkan di situs web ini dilengkapi hanya untuk studi in-vitro. Studi in-vitro (Latin: dalam kaca) dilakukan di luar tubuh. Produk -produk ini bukan obat -obatan atau obat -obatan dan belum disetujui oleh FDA untuk mencegah, mengobati atau menyembuhkan kondisi medis, penyakit atau penyakit apa pun. Pengenalan tubuh dalam bentuk apa pun ke dalam manusia atau hewan dilarang secara ketat oleh hukum.
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