Vilon

What it is

Vilon (Lys-Glu) is a synthetic dipeptide bioregulator originally developed from thymic peptide research. According to the reviewed abstracts, its biological activities include: (1) interaction with specific DNA sequences (GCGG, GGGC in promoter regions) via molecular docking, modulating gene expression of SIRT1, PARP1, PARP2, CD5, IL-2, MMP2, and others (PMIDs: 37042594, 4, 23484211, 37042594); (2) immunomodulatory effects including activation of T-cell differentiation and lymphocyte function (PMIDs: 9637345, 36395816, 39325560); (3) epigenetic effects — inducing deheterochromatinization (decondensation) of facultative heterochromatin in lymphocytes of aged individuals, reactivating ribosomal genes (PMIDs: 15105581, 23486604 [sic: 15085253], 15455093, 16705247, 21675094 [sic: 23486604]); (4) geroprotective effects including upregulation of SIRT1 and downregulation of PARP1/PARP2 in aging mesenchymal stem cells; (5) modulation of mitochondrial function and ribosomal protein expression in thymic cells (PMID 33342107 [sic: 8]); (6) stimulation of proliferative activity in splenic and thymic cells (PMIDs: 12820529, 15490736, 25705040); (7) antihypoxic properties in animal models; and (8) modulation of IL-2 gene expression in hypothalamic structures (PMIDs: 16224591, 17152351, 18264770). The peptide bond between Lys and Glu is critical for biological activity, as the free amino acid mixture does not replicate the peptide's effects.

Class: Synthetic dipeptide / peptide bioregulator / thymomimetic

What it's studied for

• Immunomodulation / thymic function support Mixed
  • Vilon, a novel immunomodulatory dipeptide, activated T-cell differentiation and T-cell recognition of peptide-MHC complexes, induced changes in intracellular cyclic nucleotides and cytokine (IL-2, IFN) excretion of blood lymphocytes, and activated neutrophil chemotaxis and phagocytosis. PMID 9637345 Morozov VG, Khavinson VK. International journal of immunopharmacology (1997)
  • Dipeptide vilon stimulated differentiation of precursors into T-helpers, cytotoxic T lymphocytes, and B cells in organotypic pineal gland culture, suggesting a compensatory role in age-related thymic atrophy. PMID 22803057 Linkova NS et al. Bulletin of experimental biology and medicine (2011)
  • Vilon dipeptide modulated proliferative patterns and inhibited TNF and IL-6 cytokine expression stimulated by LPS in THP-1 monocyte/macrophage cells; reduced monocyte adhesion to activated endothelial cells. PMID 35408963 Avolio F et al. International journal of molecular sciences (2022)
  • Vilon activated T-helpers in spleen during aging, with the effect mediated by decreased apoptosis. PMID 28976144 Chervyakova NA et al. Advances in gerontology (2014)
• Geroprotection / anti-aging Mixed
  • KE peptide increased SIRT1 gene expression and protein synthesis ~6–8-fold in young MSCs; reduced PARP1 and PARP2 gene expression and protein synthesis ~2–5-fold during MSC aging, underlying geroprotective effects. PMID 37042594 Khavinson VK et al. Advances in gerontology = Uspekhi gerontologii (2023)
  • KE peptide (at nanomolar concentrations) modulated expression of IGF1, FOXO1, TERT, TNKS2, and NFκB genes in human embryonic bone marrow MSCs in aging culture models. PMID 32399807 Ashapkin V et al. Molecular biology reports (2020)
  • Review summarizing long-term clinical studies showing peptide bioregulators including Vilon can serve as geroprotectors for prevention of diseases and treatment of elderly patients. PMID 24003726 Khavinson VK et al. Advances in gerontology = Uspekhi gerontologii (2013)
  • KE dipeptide increased collagen type I expression area in old skin fibroblasts by 83% and increased sirtuin-6 expression in young and old fibroblasts by 1.6 and 2.6 times, respectively, promoting functional activity and inhibiting aging. PMID 29322736 Fridman NV et al. Advances in gerontology (2017)
• Chromatin reactivation / epigenetic modulation in aging lymphocytes In vitro only
  • Vilon induced deheterochromatinization of total and facultative heterochromatin and reactivated ribosomal genes in cultured lymphocytes from individuals aged 75–88 years; did not induce decondensation of pericentromeric structural heterochromatin. PMID 15105581 Lezhava T et al. Biogerontology (2004)
  • Vilon activated synthetic processes via reactivation of ribosomal genes (deheterochromatinization of NORs), induced unrolling of total heterochromatin, and released repressed genes in cultured lymphocytes from old people (75–88 years). PMID 16705247 Lezhava T et al. Georgian medical news (2006)
  • Vilon induced activation of ribosome genes, decondensation of heterochromatin fibrils, and deheterochromatinization of facultative chromatin in leukocytes from subjects aged 75–88 years. PMID 15085253 Khavinson VK et al. Bulletin of experimental biology and medicine (2004)
• Oncostatic / cancer-related effects Animal studies only
  • Vilon at 10 µg/kg reduced 1,2-dimethylhydrazine-induced tumor incidence from 60% (control) to 14.3% in mice surviving to first tumor detection (46 weeks); inhibited preneoplastic alterations in kidneys. PMID 16308980 Pliss GB et al. Voprosy onkologii (2005)
  • Vilon at 0.5 µg significantly increased apoptosis of transplanted sarcoma M-1 tumor cells in old rats. PMID 15490736 Barykina OP et al. Advances in gerontology (2004)
  • Vilon at 1 mg/kg significantly increased survival in mice with transplanted Lewis lung carcinoma. Synchronous injection of Vilon and cyclophosphamide (100 mg/kg) decreased survival; Vilon should not be used simultaneously with cytostatic drugs. PMID 14743610 Barykina OP et al. Advances in gerontology (2003)
  • In transgenic erbB-2/NEU mice, Vilon (1 µg s.c., 5 days per month from age 2 months) showed no significant inhibition of mammary carcinogenesis; lung metastasis incidence was 2.6 times higher in the Vilon group than in Epitalon-treated animals. PMID 12101568 Alimova IN et al. Voprosy onkologii (2002)
  • Preliminary clinical experience suggested Vilon inclusion in complex radical treatment of elderly stage III rectal/colon cancer patients may improve 2-year survival and prevent post-operative complications. PMID 16075684 Ias'kevich LS et al. Advances in gerontology (2005)
• Diabetes mellitus — immune status and hemostasis Human observational
  • Vilon as adjunct to complex therapy in elderly type 1 diabetes patients optimized coagulation hemostasis (increased antithrombin III and protein C, stimulated fibrinolysis), reduced insulin dose required, and normalized T- and B-lymphocyte levels. PMID 18306698 Kuznik BI et al. Advances in gerontology (2007)
  • Vilon (Lys-Glu) significantly reduced or eliminated DIC syndrome in type 1 diabetes patients at various ages; effect on coagulative hemostasis was less pronounced in elderly patients with severe disease. PMID 17152731 Kuznik BI et al. Advances in gerontology (2006)
• Endometriosis treatment (animal model) Animal studies only
  • Surgery combined with intraperitoneal Vilon demonstrated promising results for treatment of experimental endometriosis in rats as assessed by reproductive function parameters. PMID 25778659 Aleksinskaya ES et al. Bulletin of experimental biology and medicine (2015)
• Neuroendocrine modulation / sexual function in aging males Animal studies only
  • Regular Vilon administration at 50 µg/rat activated sexual function in old male hemigonadectomised rats, significantly affected neuroendocrine status including levels of LH, prolactin, and ACTH, and changed neurotransmitters in the hypothalamus. PMID 17152729 Kudriavtseva TA et al. Advances in gerontology (2006)
• Stress resistance (emotional stress, hypoxia) Animal studies only
  • Intraperitoneal Vilon injection increased resistance to emotional stress in rats, inhibited adrenal hypertrophy and thymic involution, and reduced Fos-immunoreactive neurons in paraventricular hypothalamus. PMID 12587272 Koplik EV et al. Rossiiskii fiziologicheskii zhurnal (2002)
  • Short regulatory peptides including vilon manifested antihypoxic properties in a model of hypobaric hypoxia in rats. PMID 18546825 Kozina LS. Advances in gerontology (2008)
• Chronic renal failure — TGF-β and microvascular permeability Animal studies only
  • Subcutaneous Vilon significantly decreased serum TGF-β1 concentration and permeability of mesenteric microvessels in rats 2 months after onset of chronic renal failure, indicating a homeostatic effect in the early period. PMID 16142267 Gavrisheva NA et al. Bulletin of experimental biology and medicine (2005)
• Radioprotection / protection from ecotoxicant exposure Animal studies only
  • Vilon administration normalized lymphocyte number by day 30 after repeated radioactive and mercuric exposure in rats and reduced morbidity over 15 months post-exposure. PMID 16075682 Ivanov SD et al. Advances in gerontology (2005)
• Intestinal enzyme activity and absorption improvement in aged animals Animal studies only
  • Oral Vilon (Lys-Glu) for 1 month significantly increased maltase, alkaline phosphatase, and glycyl-L-leucine dipeptidase activity in small intestine of aged Wistar rats. PMID 12660839 Khavinson VK et al. Bulletin of experimental biology and medicine (2002)
  • Oral Vilon for 1 month improved transport characteristics of the small intestine in aged rats, enhancing passive and active glucose accumulation in specific segments. PMID 12420071 Khavinson VK et al. Bulletin of experimental biology and medicine (2002)
• Dental diseases in elderly — bioregulatory therapy Human observational
  • Vilon is referenced among thymomimetic peptide bioregulators used in complex treatment of dental diseases in the elderly, with immunopharmacological effects described in a narrative review. PMID 32362097 Pinelis IS et al. Advances in gerontology (2020)
• Neuronal differentiation of stem cells In vitro only
  • A compound of peptides including KE (Lys-Glu), AEDG, AED, and KED promoted neuronal differentiation of human periodontal ligament stem cells (hPDLSCs), with increased GAP43 and Nestin expression; KE alone had a smaller effect than the compound. PMID 30791821 Caputi S et al. International journal of immunopathology and pharmacology (2019)
• Melatonin synthesis modulation in pinealocytes Animal studies only
  • Vilone peptide, combined with norepinephrine, potentiated expression of AANAT and pCREB in rat pinealocyte culture; Vilone alone had minimal independent effect on melatonin synthesis in this study. PMID 22816096 Khavinson VK et al. Bulletin of experimental biology and medicine (2012)
• Plant growth regulation (Nicotiana tabacum) In vitro only
  • Exogenous vilon (Lys-Glu) at 10⁻¹⁰ M significantly influenced growth, development, and differentiation of tobacco callus cultures and modulated expression of CLE, KNOX1, and GRF family genes. PMID 28371610 Fedoreyeva LI et al. Biochemistry (2017)

Community-reported dosing

Tier key: Research = PMID-cited study · [C] = scraped community source · [S] = model-synthesized from aggregate community reports (softer evidence). How we source.

Safety signals

• Synchronous administration of Vilon with cyclophosphamide (100 mg/kg) decreased survival in Lewis lung carcinoma mice; Vilon antagonized cytostatic effects when given simultaneously PMID 14743610
• In transgenic erbB-2/NEU mice, lung metastasis incidence was 2.6 times higher in the Vilon group than in the Epitalon group; Vilon did not significantly inhibit mammary carcinogenesis in this model PMID 12101568
• Short peptides including Vilon elevated stationary level of intracellular reactive oxygen species in neuronal populations in vitro, while decreasing percentage of dead cells; implications for in vivo conditions are uncertain PMID 18546826
• No direct antioxidant activity detected for Vilon in in vitro model experiments; biological effects operate through lipoprotein structure modification rather than direct free radical scavenging PMID 18546826

Contraindications

• Concurrent use with cytostatic chemotherapy (e.g., cyclophosphamide) is not recommended based on animal data showing decreased survival when Vilon and cyclophosphamide were given simultaneously PMID 14743610