Overview
Vilon is a short synthetic dipeptide composed of two amino acids — lysine and glutamic acid (Lys-Glu) — giving it the molecular formula C11H21N3O5 and a molecular weight of approximately 275.3 Da. It belongs to a class of compounds known as peptide bioregulators, a category of small signaling peptides that have been studied for their potential roles in cellular and gene regulation processes. Vilon has appeared in scientific literature exploring topics such as epigenetic modification, stem cell aging, and gene expression related to proteins like SIRT1 and PARP1, suggesting researchers are interested in understanding how it may interact with cellular aging mechanisms at a molecular level. Like other peptide bioregulators, it is sometimes discussed alongside peptides such as Epitalon and Livagen in the context of chromatin and cellular biology research. Vilon is intended strictly for laboratory and research purposes and is not approved for human use or consumption.
Research & Bioactivity
Vilon (Lys-Glu) is a dipeptide that has attracted research interest primarily in the areas of aging biology, immunology, and cellular regulation. Studies have examined its potential role as a geroprotective and immunomodulatory agent, with in vitro research investigating how it influences gene expression and protein synthesis related to aging processes in human mesenchymal stem cells, including the regulation of SIRT1, PARP1, and PARP2. Researchers have also studied Vilon's effects on epigenetic modification, particularly its influence on condensed chromatin in lymphocytes derived from older individuals, using molecular-cytogenetic methods to characterize these changes. Additional in vitro research has investigated Vilon's activity in monocyte and macrophage cell models, examining its potential role in modulating inflammatory and proliferative pathways in the THP-1 human leukemia monocytic cell line. Across these studies, Vilon has been characterized as a peptide bioregulator, a class of short peptides that researchers study for their proposed roles in tissue-specific gene regulation and cellular homeostasis.
Published Research
Graphene oxide nanosheets conjugated PEG-Glu-Lys-Glu copolymer drug delivery system improves drug-loading rates and enables reduction-sensitive drug release and drug tracking.
Xu Q, Chen H, Zhu J, Li X, Yang J, et al. — 2024
In this study, the PEG-Glu-Lys-Glu copolymer drug delivery system (GO/PEG-Glu-Lys-Glu) is prepared using glutamate-lysine-glutamate (Glu-Lys-Glu) modified polyethylene glycol (PEG) and connected graphene oxide nanosheets (GO). The multiple carboxyl groups of Glu-Lys-Glu and π-π interactions of GO can increase drug loading rate, and the fluorescence characteristics of GO could monitor the distribution of drug-loading systems in cells and the uptake of cells without the need for external dyes. Paclitaxel (PTX) is loaded reduction-responsive disulfide bonds as a model medicine to examine the drug delivery potential of GO/PEG-Glu-Lys-Glu. The results showed that the drug loading content of PEG-Glu-Lys-Glu and GO/PEG-Glu-Lys-Glu to PTX is 7.11% and 8.97%, and the loading efficiency is 71.05% and 89.68%, respectively. It's speculated that the π-π interaction between GO and PTX improved the drug-loading capacity and efficiency of GO/PEG-Glu-Lys-Glu. in a simulated drug release test, at 48 h, the release of PTX was 85.51% at pH 5.0, 65.12% and 38.32% at pH 6.5 and 7.4, respectively. The cytotoxicity assay results showed that GO/PEG-Glu-Lys-Glu cell inhibition rate to MCF-7 cells was 7.36% at 72 h. The cell inhibition rate of GO/PEG-Glu-Lys-Glu/PTX system at 72 h was 92%, equivalent to free PTX. Therefore, the GO/PEG-Glu-Lys-Glu drug delivery system has the characteristics of good biocompatibility and sustainable release of PTX, which is expected to be applied in the field of tumor therapy.
[KE peptide regulates SIRT1, PARP1, PARP2 gene expression and protein synthesis in human mesenchymal stem cells aging.].
Khavinson VK, Linkova NS, Ashapkin VV, Shilovsky GA, Borushko NV, et al. — 2023
It was shown that KE peptide (Lys-Glu, vilon) has immunomodulatory, oncostatic and geroprotective effects. The aim of this work is to evaluate the effect of the KE peptide on gene expression and protein synthesis of SIRT1, PARP1, PARP2 during aging of human mesenchymal stem cells (MSC). The KE peptide increased gene expression and synthesis of the SIRT1 protein in «young» MSCs by 6 and 8,2 times, respectively. The KE peptide reduced gene expression and PARP1 protein synthesis during MSC aging by 2,1 and 5,3 times, respectively; and also reduced gene expression and PARP2 protein synthesis by 2,1 and 4,7 times, respectively. According to molecular modeling data, the KE peptide can interact with the GCGG sequence of double-stranded DNA (dsDNA) in the classical B-form and with the GGGC sequence of the curved dsDNA nucleosome. The indicated dsDNA sequences were found in the promoters of the human SIRT1, PARP1, PARP2 genes. Thus, the KE peptide regulates gene expression and synthesis of SIRT1, PARP1, PARP2 proteins in human mesenchymal stem cells during replicative ageing, which underlies the biological activity and geroprotective effect of this peptide.
EPIGENETIC MODIFICATION UNDER THE INFLUENCE OF PEPTIDE BIOREGULATORS ON THE "OLD" CHROMATIN.
Lezhava T, Jokhadze T, Monaselidze J, Buadze T, Gaiozishvili M, et al. — 2023
In the present study, on the one hand, the epigenetic modification of condensed "old" chromatin was determined, and on the other hand, the influence of peptide bioregulators (Ala-Glu-Asp-Gly-Epitalon; Lys-Glu-Asp-Ala-Livagen; Ala-Glu-Asp-Pro - Cortagen and Lys-Glu - Vilon) on condensed chromatin in lymphocytes from old individuals. Were used molecular-cytogenetic methods: differential scanning calorimetry; activity of ribosomal genes of acrocentric chromosome satellite stalks-NORs; polymorphism of structural pericentromeric C-heterochromatin; variability of the facultative heterochromatin (sister chromatid exchanges - SCE) in the culture of lymphocytes from 75-88-year-old individuals. The analysis of results shows the chromosome progressive heterochromatinization (condensation of eu - and heterochromatin regions) occur in aging. Epigenetics process - heterochromatinization can deactivate many previously functioning active genes. It blocks certain stages of normal metabolic processes in the cell, which inhibits many specific enzymes and leads to aging pathologies. We show that peptide bioregulators induced unrolling deheterochromatinization (decondensation) of total heterochromatin, deheterochromatinization of satellite stalks of acrocentric chromosome, activating synthetic processes of ribosomal genes, does not cause deheterochromatinized of pericentromeric structural heterochromatin. This data also indicates that each of the studied peptide bioregulators (Ala-Glu-Asp-Gly; Lys-Glu-Asp-Ala; Ala-Glu-Asp-Pro and Lys-Glu) has a selective effect on definite regions of chromosomes. Thus, short peptide bioregulators induce selective heterochromatinization and deheterochromatinization of chromosome regions (remodeling of facultative heterochromatin) in individuals 75-88 years old that opens up new opportunities in the treatment of aging diseases.
ViLoN-a multi-layer network approach to data integration demonstrated for patient stratification.
Kańduła MM, Aldoshin AD, Singh S, Kolaczyk ED, Kreil DP — 2023
With more and more data being collected, modern network representations exploit the complementary nature of different data sources as well as similarities across patients. We here introduce the Variation of information fused Layers of Networks algorithm (ViLoN), a novel network-based approach for the integration of multiple molecular profiles. As a key innovation, it directly incorporates prior functional knowledge (KEGG, GO). In the constructed network of patients, patients are represented by networks of pathways, comprising genes that are linked by common functions and joint regulation in the disease. Patient stratification remains a key challenge both in the clinic and for research on disease mechanisms and treatments. We thus validated ViLoN for patient stratification on multiple data type combinations (gene expression, methylation, copy number), showing substantial improvements and consistently competitive performance for all. Notably, the incorporation of prior functional knowledge was critical for good results in the smaller cohorts (rectum adenocarcinoma: 90, esophageal carcinoma: 180), where alternative methods failed.
Peptides Regulating Proliferative Activity and Inflammatory Pathways in the Monocyte/Macrophage THP-1 Cell Line.
Avolio F, Martinotti S, Khavinson VK, Esposito JE, Giambuzzi G, et al. — 2022
This study evaluates the effects of five different peptides, the Epitalon tetrapeptide, the Vilon dipeptide, the Thymogen dipeptide, the Thymalin peptide complex, and the Chonluten tripeptide, as regulators of inflammatory and proliferative processes in the human monocytic THP-1, which is a human leukemia monocytic cell line capable of differentiating into macrophages by PMA in vitro. These peptides (Khavinson Peptides), characterized by Prof. Khavinson from 1973 onwards, were initially isolated from animal tissues and found to be organ specific. We tested the capacity of the five peptides to influence cell cultures in vitro by incubating THP-1 cells with peptides at certain concentrations known for being effective on recipient cells in culture. We found that all five peptides can modulate key proliferative patterns, increasing tyrosine phosphorylation of mitogen-activated cytoplasmic kinases. In addition, the Chonluten tripeptide, derived from bronchial epithelial cells, inhibited in vitro tumor necrosis factor (TNF) production of monocytes exposed to pro-inflammatory bacterial lipopolysaccharide (LPS). The low TNF release by monocytes is linked to a documented mechanism of TNF tolerance, promoting attenuation of inflammatory action. Therefore, all peptides inhibited the expression of TNF and pro-inflammatory IL-6 cytokine stimulated by LPS on terminally differentiated THP-1 cells. Lastly, by incubating the THP1 cells, treated with the peptides, on a layer of activated endothelial cells (HUVECs activated by LPS), we observed a reduction in cell adhesion, a typical pro-inflammatory mechanism. Overall, the results suggest that the Khavinson Peptides cooperate as natural inducers of TNF tolerance in monocyte, and act on macrophages as anti-inflammatory molecules during inflammatory and microbial-mediated activity.