Epithalon
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Apenas para Uso em Pesquisa
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Resumo da Pesquisa
Visao Geral da Pesquisa Epithalon (Ala-Glu-Asp-Gly) is a synthetic tetrapeptide geroprotector developed by Prof. Vladimir Khavinson no(a) St. Petersburg Institute of Bioregulacao and Gerontology como o(a) ativo(a) component of Epithalamin (bovine pineal gland extract). Its discovery originated from 1970s Soviet military research para proteger soldiers from radiation and acelerou aging.[4] Epithalon's mechanism is fundamentally diferente from classical receptor-ligand pharmacology. Rather do que binding a cell surface receptor, it enters the nucleus and interacts directly with DNA (targeting CAG repeats and ATTTC promoter sequences) and histone proteins (H1.3, H1.6) — functioning como um(a) epigenetic switch que converts heterochromatin to euchromatin, making silenced genes accessible for transcricao.[1][3] Research spans 10+ indication categories across gerontology, oncology, ophthalmology, endocrinology, and neuroscience — with over 50 years of study (1970s–2025). The "Epithalon Paradox" — activating telomerase enquanto simultaneamente inhibiting cancer — challenges conventional oncological assumptions and remains a principal focus of current research.[7]
Epithalon — Dados de Pesquisa em Resumo
| Propriedade | Valor |
|---|---|
| Pesquisadores Colaboradores | 3 |
| Condicoes de Armazenamento | Armazene liofilizado a -20°C (anos-estável). |
| Padrao de Pureza | ≥99% (HPLC verified, 3rd-party COA) |
| Apenas para Uso em Pesquisa | Nao destinado ao consumo humano. Apenas para uso em pesquisa. |
Compare Epithalon com Outros Peptideos
Visao Geral
Visao Geral da Pesquisa
Epithalon (Ala-Glu-Asp-Gly) is a synthetic tetrapeptide geroprotector developed by Prof. Vladimir Khavinson no(a) St. Petersburg Institute of Bioregulacao and Gerontology como o(a) ativo(a) component of Epithalamin (bovine pineal gland extract). Its discovery originated from 1970s Soviet military research para proteger soldiers from radiation and acelerou aging.[4]
Epithalon's mechanism is fundamentally diferente from classical receptor-ligand pharmacology. Rather do que binding a cell surface receptor, it enters the nucleus and interacts directly with DNA (targeting CAG repeats and ATTTC promoter sequences) and histone proteins (H1.3, H1.6) — functioning como um(a) epigenetic switch que converts heterochromatin to euchromatin, making silenced genes accessible for transcricao.[1][3]
Research spans 10+ indication categories across gerontology, oncology, ophthalmology, endocrinology, and neuroscience — with over 50 years of study (1970s–2025). The "Epithalon Paradox" — activating telomerase enquanto simultaneamente inhibiting cancer — challenges conventional oncological assumptions and remains a principal focus of current research.[7]
Mecanismo de Acao
Mecanismo de Acao
Epithalon operates via a receptor-independent, epigenetic mechanism — bypassing cell surface receptors to directly interact com o(a) genome. It penetrates the cell nucleus and liga-se a DNA and histone proteins, functioning como um(a) master gene regulator.[3][1]
Primary Epigenetic Targets
| Target | Mecanismo | Downstream Effect |
|---|---|---|
| DNA — CAG repeats & ATTTC sequences | Binds principal groove of DNA double helix | Lowers chromatin melting temperature → previne genomic "hardening" with age |
| Histone H1.3 & H1.6 | High-affinity binding → decondenses heterochromatin → euchromatin | Silenced genes become accessible for transcricao |
| hTERT gene promoter | Direct promoter binding → upregula hTERT mRNA (12-fold at 1 µg/mL) | Telomerase synthesis → TTAGGG repeat elongation |
Dual Telomere Mechanism (Al-dulaimi et al., 2025)
| Cell Type | Mecanismo | Markers |
|---|---|---|
| Normal somatic cells | Telomerase-mediated elongation (classic pathway) | ↑ hTERT mRNA → ↑ atividade da telomerase → TTAGGG addition |
| Cancer cells | ALT (Alternative Lengthening of Telomeres) via replication stress | C-circles, PML bodies — NOT aumentou atividade da telomerase |
Downstream Signaling Cascades
| Pathway | Targets | Effect |
|---|---|---|
| Melatonin Synthesis | ↑ AANAT + pCREB in pinealocytes | Restores nighttime melatonin production |
| Antioxidant Defense | Keap1/Nrf2 pathway ativacao | ↑ SOD, Catalase, Glutathione Peroxidase |
| Immune Signaling | ↑ STAT1 + ERK1/2 fosforilacao; ↑ IL-2 mRNA (within 5h) | T-proliferacao celular; NO STAT3 ativacao |
| Circadian Clock | Modulates Clock, Cry2, Csnk1e genes | Restores youthful circadian rhythms |
No opioid ligacao ao receptor — Epithalon nao interact with µ or δ opioid receptors apesar de being a peptide. Its STAT1 fosforilacao is acreditado(a) para be receptor-independent.[3]
Aplicacoes de Pesquisa
Aplicacoes de Pesquisa
Epithalon research spans 10+ indication categories with over 50 years of investigation (1970s–2025):
- Telomere Extension & Cellular Senescence — Cells surpass Hayflick limit; telomere elongation confirmou in subjects aged 60–80 (9.61→10.72 kb and 7.51→8.91 kb, p<0.05).[5]
- Cancer Prevention Paradox — Inhibits spontaneous tumors in HER-2/neu mice; reduz oncoexpressao genica 3.7-fold; anti-metastatic — apesar de telomerase ativacao.[7][14]
- Retinal Degeneration / Retinitis Pigmentosa — observacoes relatadas in 162 research subjects; visual field expanded 90–120°.[9]
- Circadian Rhythm & Sleep Regulation — Restores youthful melatonin secretion; normalizes cortisol rhythms in aged monkeys and humans.[11][15]
- Neuroprotection & Neurogenesis — Upregula Nestin, GAP43, Beta-Tubulin III in celulas-tronco; promove neuronal diferenciacao.[3]
- Immune System Rejuvenation — ↑ IL-2, T-proliferacao celular; corrects age-related CD4+/CD8+ ratios.[4]
- Antioxidant Defense — ↑ SOD (+41%), catalase (+20%), glutathione peroxidase; ↓ lipid peroxidation and ROS.[6]
- Diabetic Retinopathy / Wound Healing — Inhibits EMT and fibrose in high-glucose RPE cells.[12]
- Reproductive Health — Restores estrous cycles in ratos idosos; melhora oocyte quality and blastocyst hatching.[10]
- Geroprotection / Anti-Aging — Maximum lifespan aumentou 12–13% in mice; up to 24% in CBA model; reduziu chromosomal aberrations.[7][8]
Caracteristicas Bioquimicas
| Propriedade | Valor |
|---|---|
| Molecular Formula | C₁₄H₂₂N₄O₉ |
| Molecular Weight | 390.35 Da |
| CAS Number | 307297-39-8 |
| PubChem CID | 219042 |
| Sequence (1-Letter) | AEDG |
| Sequence (3-Letter) | Ala-Glu-Asp-Gly |
| Structure | Linear tetrapeptide; four L-aminoacidos; no ponte dissulfetos |
| InChI Key | HGHOBRRUMWJWCU-FXQIFTODSA-N |
| Origin | Synthetic analog of Epithalamin (bovine pineal gland extract) |
| Classification | Peptide Bioregulator / Geroprotector / Research Peptide |
| Dose-Response | Bell-shaped / non-linear — peak activity at ultra-low concentrations (10⁻¹⁷ to 10⁻¹⁵ M) |
Identificadores
| Purity Standard | |
|---|---|
| SMILES | |
| IUPAC Name | |
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Resumo da Pesquisa Pre-clinica
Resumo da Pesquisa Pre-clinica
Key Preclinical Studies
| Estudo | Modelo | Principais Achados | Ref |
|---|---|---|---|
| Anisimov/Popovich et al. (2003) | SHR mice — 1 µg/mouse SC × 5d/month from 3 mo | Last 10% lifespan aumentou 13.3%; chromosomal aberrations ↓17.1%; leukemia inibiu 6-fold | [7] |
| Anisimov et al. (2002) | HER-2/neu camundongos transgenicos — 1 µg/mouse SC monthly | HER-2/neu mRNA reduziu 3.7-fold; breast adenocarcinoma incidence reduziu significativamente | [14] |
| Kossoy et al. (2006) | C3H/He mice — 0.1 µg/mouse SC × 5x/wk × 6.5 mo | Reduced tumor metastasis and multiplicity | [8] |
| Anisimov et al. (2001) | CBA mice — 0.1 µg/mouse SC monthly | Oldest treated mouse lived 34 months vs 24 mo control; mice reaching 23 mo aumentou 4-fold | [8] |
| Khavinson et al. (2002–03) | Campbell rats — 1 µg/rat parabulbar injection | Retinal function prolonged 43.9%; 90% of retinal layers preservou at day 41 vs complete destruction | [9] |
| Zamorskii et al. (2014–19) | Rats with agudo(a) kidney failure — 7 µg/kg IM/IP × 7–10d | Nephroprotective — aumentou diuresis, diminuiu proteinuria, ↑ catalase and glutathione peroxidase | [13] |
| Goncharova et al. (2001–05) | Old female rhesus monkeys — 10 µg/kg IM | Restored nighttime melatonin synthesis; normalized cortisol circadian rhythm; melhorou glucose tolerance | [11] |
| Khavinson et al. (2000–01) | Drosophila — 0.00001–0.001% in medium | Mean lifespan +11–16%, max +14%; mortality ↓52%; SOD +41%, catalase +20% | [6] |
| Ullah et al. (2025) | Bovine oocytes in vitro | Activated telomerase; melhorou blastocyst hatching; reduziu ROS | [10] |
Clinical / Human Studies
| Ensaio | Population | Intervention | Key Results | Ref |
|---|---|---|---|---|
| Retinitis Pigmentosa | n=162 subjects | 5.0 µg parabulbar daily × 10 days | Reported positivo(a) observations; visual acuity and visual field improvements observado(a) in study | [9] |
| Circadian Rhythm | n=75 women, age 60–74 | 0.5 mg sublingual daily × 20 days | Melatonin +1.6-fold; Clock ↓1.8×, Cry2 ↑2×, Csnk1e ↓2.1× | [15] |
| Telomere Elongation | Subjects aged 60–80 | Standard protocol | Ages 60–65: 9.61→10.72 kb; Ages 75–80: 7.51→8.91 kb (ambos(as) p<0.05) | [5] |
| Pulmonary Tuberculosis | TB subjects | Not specified | Protective effect against further chromosomal aberrations (mixed outcome) | [16] |
Safety Summary
| Parametro | Finding |
|---|---|
| Long-term Animal Studies | No toxicity in mice/rats from 3 months of age until natural death; reduziu mortality and spontaneous tumors |
| Clinical Trials | No severe eventos adversos in retinitis pigmentosa (n=162) or circadian rhythm trials; mild injection site reactions relatado(a) anecdotally |
| Cancer Risk Paradox | Apesar de telomerase ativacao, animal studies consistently show ANTI-tumor and anti-metastatic effects |
| Degradation | N-terminal glutamic acid can cyclize to pyroglutamate; TFA salt affects net peptide content |
| Routes Studied | Subcutaneous, intramuscular, parabulbar (eye), sublingual, oral, intranasal |
Autores e Atribuicao
✍️ Autor do Artigo
Prof. Vladimir Khavinson, M.D., Ph.D.
Prof. Vladimir Khavinson e o(a) Director do(a) St. Petersburg Institute of Bioregulacao and Gerontology, a Member do(a) Russian Academy of Sciences, e um(a) retired Colonel of Medical Service. He is o(a) principal inventor and pioneer of peptide bioregulators, leading the original discovery of Epithalamin (pineal gland extract) e o(a) subsequente synthesis of Epithalon (Ala-Glu-Asp-Gly). His research estabeleceu the 'peptide theory of aging,' demonstrating Epithalon's ability to reactivate telomerase, elongate telomeres, and regulate expressao genica no(a) epigenetic level. Foundational research began no(a) 1970s no(a) S.M. Kirov Military Medical Academy no(a) Soviet Union. Key publications include 'Epithalon Peptide Induces Telomerase Activity and Telomere Elongation in Human Somatic Cells' (2003) and 'AEDG Peptide Stimulates Gene Expression during Neurogenesis' (2020). Prof. Vladimir Khavinson is referenced como o(a) leading scientist in Epithalon research. De forma alguma este(a) médico(a)/cientista endossa ou defende a compra, venda ou uso deste produto por qualquer motivo. Não existe afiliação ou relação, implícita ou de outra forma, entre a Pure US Peptide e este(a) médico(a).
Ver Perfil Completo do Pesquisador →🎓 Autor de Revista Cientifica
Prof. Vladimir N. Anisimov, M.D., Ph.D.
Prof. Vladimir N. Anisimov is a researcher no(a) N.N. Petrov Research Institute of Oncology (St. Petersburg, Russia). He has been instrumental in characterizing the geroprotective and oncostatic properties of Epithalon em modelos animais, providing decades of critico(a) evidence que enquanto Epithalon extends telomeres, it nao promote cancer — paradoxically inhibiting spontaneous tumor development and extending lifespan in mice. His work estabeleceu the 'Epithalon Paradox' in gerontological research. Key publications include 'Effect of Epitalon on biomarcadors of aging, life span and spontaneous tumor incidence in SHR mice' (Biogerontology, 2003) and 'Inhibitory effect on HER-2/neu mammary tumors' (2002). Prof. Vladimir Anisimov é referenciado(a) como um(a) cientista líder na pesquisa de Epithalon. De forma alguma este(a) médico(a)/cientista endossa ou defende a compra, venda ou uso deste produto por qualquer motivo. Não existe afiliação ou relação, implícita ou de outra forma, entre a Pure US Peptide e este(a) médico(a).
Ver Perfil Completo do Pesquisador →Prof. Vladimir N. Anisimov, M.D., Ph.D. is being referenced as one of the leading scientists involved in the research and development of Epithalon. 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 Pure US Peptide and this doctor. The purpose of citing the doctor is to acknowledge, recognize, and credit the exhaustive research and development efforts conducted by the scientists studying this peptide.
🔬 Pesquisador Colaborador
Prof. Natalia S. Linkova
Prof. Natalia S. Linkova is a Doctor of Biological Sciences no(a) St. Petersburg Institute of Bioregulacao and Gerontology e o(a) Academy of Postgraduate Education under FSBU FSCC of FMBA of Russia. She is a prominent researcher no(a) molecular mechanisms of peptide bioregulators, focusing on how Epithalon interage com DNA and histone proteins para regular expressao genica, neurogenese, and cell diferenciacao — providing the mechanistic explanation for o peptideo's broad biological effects. Key publications include 'AEDG Peptide Stimulates Gene Expression and Protein Synthesis during Neurogenesis: Possible Epigenetic Mechanism' (Molecules, 2020) and 'Peptide Regulation of Gene Expression: A Systematic Review' (2021). Prof. Natalia Linkova é referenciado(a) como um(a) cientista líder na pesquisa de Epithalon. De forma alguma este(a) médico(a)/cientista endossa ou defende a compra, venda ou uso deste produto por qualquer motivo. Não existe afiliação ou relação, implícita ou de outra forma, entre a Pure US Peptide e este(a) médico(a).
Ver Perfil Completo do Pesquisador →Prof. Natalia S. Linkova is being referenced as one of the leading scientists involved in the research and development of Epithalon. 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 Pure US Peptide and this doctor. The purpose of citing the doctor is to acknowledge, recognize, and credit the exhaustive research and development efforts conducted by the scientists studying this peptide.
Aviso de Uso em Pesquisa
Apenas para Uso em Pesquisa (RUO). Nao destinado ao consumo humano, uso clinico, ou como medicamento, alimento, cosmetico ou dispositivo medico. Este produto nao foi avaliado pelo FDA e e fornecido exclusivamente para pesquisa laboratorial in vitro por profissionais qualificados.
Certificado de Analise
Each lot is independently tested by accredited third-party laboratories (ISO 17025) at 99%+ purity.
Ultimo Relatorio de Laboratorio
Armazenamento e Manuseio
Resumo
Armazene liofilizado a -20°C (anos-estável). Proteja da umidade e light. Reconstituído: 4°C até 20 dias; evite ciclos de congelamento-descongelamento.
❄️ Liofilizado Powder Storage
Store Epithalon (Epitalon) liofilizado powder at -20°C in a sealed container, protegeu from light and moisture. Under these conditions, o peptideo is estável por varios(as) years. For longo prazo archival storage, -80°C is recommended. Keep vials desiccated; the tetrapeptide Ala-Glu-Asp-Gly is hygroscopic and will absorb atmospheric moisture if exposed.
🧪 Reconstituted Solution Storage
Após reconstituição, store at 4°C (refrigerator temperature). Reconstituted Epithalon is estável por aproximadamente 2–20 days depending on solvent and conditions. Bacteriostatic water extends working solution stability. Prepare aliquots of stock solution to avoid repeated freeze-thaw cycles, que accelerate degradacao.
⚗️ Reconstitution Notes
Epithalon is water-soluble como o(a) free peptide. If supplied como o(a) TFA (trifluoroacetic acid) salt, the TFA counterion contribui para the mass — net peptide content is lower do que the stated weight. If supplied como o(a) acetate salt, net peptide content is higher. Reconstitua com sterile water or agua bacteriostatica. Typical research concentrations: 1–5 mg/mL in aqueous solution.
⚠️ Degradation Pathway
The N-terminal glutamic acid (Glu) residue no(a) AEDG sequence can cyclize to pyroglutamate, a spontaneous non-enzymatic degradacao pathway. This reaction is acelerou by heat and repeated freeze-thaw cycles. Storage at -20°C and prompt use after reconstitution minimizes this pathway. Purity verification deve ser performed by RP-HPLC and mass spectrometry before use.
💉 Administration Forms Studied
Peer-reviewed research has investigated Epithalon via multiplos(as) administration routes, incluindo subcutaneo(a) injection, intramuscular injection, parabulbar (periocular) injection for retina studies, sublingual, oral, and intranasal delivery. Route selection in research protocols significantly affects biodisponibilidade and tissue distribuicao.
For Research Use Only. This product is furnished for in-vitro laboratory studies only. Not aprovado(a) por the FDA for qualquer medical indication.
“Resumo da Pesquisa Pre-clinica Key Preclinical Studies Estudo Modelo Principais Achados Ref Anisimov/Popovich et al.”
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