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1kits（10Vials）
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▎Thymogen Structure
Source: PubChem | Sequence: EW Molecular Formula: C16H19N3O5 Molecular Weight: 333.34 g/mol CAS Number: 38101-59-6 PubChem CID：100094 Synonyms: Oglufanide |
▎Thymogen Research
What is the research background of Thymogen?
Since the 1960s, core organs of the animal immune system—such as bone marrow, thymus, and spleen—have attracted significant scientific attention due to their potential to produce bioactive compounds that influence immune function and hold medicinal promise. In the mid-1960s, researchers discovered a component within acetone extracts of calf thymus exhibiting significant biological activity capable of restoring suppressed immune responses in mice. Subsequently, similar compounds like thymosin, thymopeptide, and T-activator emerged, finding limited application in medical practice as first-generation broad-spectrum immunostimulants.
Subsequent in-depth research on thymosin component 5 led scientists to discover the first peptide hormones regulating mammalian immune system function, including thymosin α1 (containing 28 amino acid residues), thymosin β4 (containing 43 residues), and thymosin beta (containing 49 residues). Amid this research surge, Thymogen emerged. Thymogen is a short peptide composed solely of two amino acids (glutamic acid-tryptophan, Glu-Trp), with its active substance being the monosodium salt of L-α-glutamine - L-tryptophan monosodium salt, identical to the natural compound chromatographically isolated from thymus extract. Its unique molecular structure and potential immunomodulatory properties have prompted ongoing scientific exploration into its mechanisms of action in immune regulation, tissue repair, and cellular signaling pathways, aiming to achieve prevention and treatment of various diseases.
What is the mechanism of action of Thymogen?
Immune Regulation:
Activation of Immune Receptors and Signaling Pathways: Studies indicate that Thymogen activates immune TLR/RLR receptors and their signaling factor genes. In cultures of THP-1 monocyte leukemia cells and healthy donor blood, Thymogen stimulates the expression of endosomal TLR3/7/8/9 receptors, cytoplasmic sensors RIG1/MDA5, and signaling factors NFκB1 and MAVS[1]. This indicates that Thymogen modulates the body's immune response and enhances immune defense capabilities by activating these critical immune-related receptors and signaling pathways. For example, NFκB1 participates in inflammatory responses and immune regulation; Thymogen's stimulation of its signaling factor genes helps initiate relevant immune responses to defend against pathogen invasion.
Modulation of Cytokine Secretion: In the aforementioned cell culture systems, Thymogen induces the secretion of inflammatory cytokines TNF-α and IL-1β. Cytokines play crucial communication and regulatory roles in the immune system. TNF-α and IL-1β are involved in initiating and modulating inflammatory responses. Their increased secretion indicates that Thymogen can guide the body's immune response toward pathogen defense by regulating cytokine secretion[1].
Regulation of Gene Expression: Components of Thymogen, such as the EW dipeptide (i.e., Thymogen itself), can modulate gene expression. It regulates the synthesis of heat shock proteins, cytokines, fibrinolysis, senescence genes, and other factors, as well as cellular processes including differentiation, proliferation, and apoptosis. For example, heat shock proteins play a crucial role in cellular stress responses. Thymogen's regulation of their synthesis helps cells better adapt to environmental changes and resist damage [2].
Antiviral Effects:
Direct Antiviral Activity: In vitro experiments demonstrate that Thymogen spray exhibits local antiviral activity against SARS-CoV-2 at a viral titer of 5.2 log TCID50 in Vero CCL81 cell cultures. This occurs through direct interaction with the virus, affecting processes such as adsorption, invasion, and replication, thereby inhibiting viral infection and transmission[3].
Enhanced Immune-Mediated Indirect Antiviral Effects: Due to its immunomodulatory properties, Thymogen activates immune receptors and signaling pathways, regulates cytokine secretion, and enhances the body's immune defense capabilities. It indirectly combats viral infections by boosting overall immune function. For instance, activated immune cells can more effectively recognize and eliminate virus-infected cells, thereby achieving antiviral effects [1].
Figure 1 TRH-TSH-T3 feedback loop[3].
Cell Repair and Regeneration:
Antioxidant Effects: In acute toxic liver injury experiments, Thymogen suppresses oxidative peroxidation reactions. When administered following carbon tetrachloride-induced liver injury, Thymogen reduced malondialdehyde (MDA) concentrations, indicating its capacity to mitigate oxidative stress-induced cellular damage. This occurs because oxidative stress generates excessive free radicals that attack intracellular biomolecules—such as lipids, proteins, and DNA—leading to cellular injury and dysfunction. Thymogen's antioxidant properties protect cells from free radical damage [5].
Stimulation of Cell Regeneration: Similarly, in acute toxic liver injury models, Thymogen stimulates reparative regeneration of hepatocytes. This likely occurs by regulating the expression of genes associated with cell proliferation, differentiation, and apoptosis. For instance, it promotes hepatocyte proliferation, accelerating the repair and regeneration of damaged liver tissue to restore normal liver function[5].
Effects on Mineral, Pigment, and Lipid Metabolism: In studies of domesticated moose with hoof injuries, incorporating Thymogen into treatment protocols for severely injured moose facilitated greater normalization of mineral metabolism while minimizing disturbances in pigment and lipid metabolism. This indicates that Thymogen influences mineral, pigment, and lipid metabolic processes by regulating key points in relevant metabolic pathways, thereby maintaining metabolic equilibrium [6].
Effects on Protein, Nitrogen, and Carbohydrate Metabolism: In castration experiments on boars, Thymogen significantly mitigated the intensity of pathological catabolic phase changes and facilitated normalization of biochemical indicators during the final experimental stage. This indicates Thymogen's regulatory effect on protein, nitrogen, and carbohydrate metabolism, potentially maintaining metabolic stability by influencing the activity or gene expression of relevant metabolic enzymes[6].
What are the applications of Thymogen?
Antiviral Field: In studies targeting the novel coronavirus, experiments conducted on Vero CCL81 cell cultures compared Thymogen® spray with the antiseptic Miramistin® solution to investigate their local antiviral activity against SARS-CoV-2. Results showed no toxic effects on Vero cells at the concentrations studied. Furthermore, across a series of experiments, Thymogen® spray demonstrated local antiviral activity against SARS-CoV-2 at a viral titer of 5.2 log TCID50. This indicates significant potential for Thymogen® nasal spray as a topical agent for preventing and treating COVID-19 [3].
Liver Disease Treatment: In studies of acute toxic liver disease, continuous intraperitoneal administration of carbon tetrachloride for 5 days induced hepatic steatosis, reduced catalase activity, and elevated malondialdehyde levels. Administration of Thymogen and its structural analogues (obtained by attaching the amino acid D-Ala to the N- or C-terminus of the peptide molecule) inhibited oxidative peroxidation reactions and stimulated hepatocyte repair and regeneration. Among these, Thymogen analogues demonstrated more pronounced hepatotropic and antioxidant effects compared to Thymogen. The effect was most pronounced when the amino acid was added to the C-terminus of the molecule. This demonstrates that Thymogen and its analogues exert positive effects in liver injury repair[5].
Immunomodulation and Infection Therapy: The peptide drug thymalin can be applied to various conditions associated with immune dysfunction, viral and bacterial infections, normalization of regeneration, immunosuppression, and hematopoietic suppression following chemotherapy and radiotherapy. One of its components, the EW dipeptide (i.e., the drug Thymogen), regulates gene expression, heat shock protein synthesis, cytokines, fibrinolysis, senescence genes, and cellular differentiation, proliferation, and apoptosis. Thymogen is effective against various viral infections and demonstrates therapeutic efficacy in the comprehensive treatment of COVID-19 caused by coronavirus infection[2].
Conclusion
Thymogen exhibits multidimensional biological activity. It maintains immune homeostasis and enhances anti-infective capacity by activating immune TLR/RLR receptors, regulating cytokine secretion (e.g., TNF-α, IL-1β), and modulating immune cell function. It demonstrates in vitro antiviral activity against SARS-CoV-2. Additionally, it mitigates damage by suppressing oxidative stress and stimulating tissue cell repair/regeneration (e.g., hepatocytes). while regulating mineral, pigment, and lipid metabolism to maintain metabolic balance. It can assist in COVID-19 prevention and treatment, repair liver damage, and be used for preoperative immune conditioning in elderly cancer patients to reduce postoperative complications and shorten recovery time. This makes it beneficial for interventions in immune-related diseases and tissue repair.
About The Author
The above-mentioned materials are all researched, edited and compiled by Cocer Peptides.
Scientific Journal Author
Kim H is a researcher focusing on the field of bone biology and the physiological functions of thyroid hormones. Their research mainly centers on the regulatory role of thyroid hormones in skeletal development-related biological processes, with a focus on exploring the underlying molecular and cellular mechanisms. Kim H often uses a combination of experimental methods such as molecular biology techniques and biological model systems to conduct in-depth studies, aiming to enrich the theoretical understanding of the interaction between endocrine factors and skeletal health. Kim H is listed in the reference of citation [4].
