Thymalfasin
Thymalfasin
CAS: 69440-99-9
Molecular Formula: C129H215N33O55
Thymalfasin - Names and Identifiers
Thymalfasin - Physico-chemical Properties
| Molecular Formula | C129H215N33O55 |
| Molar Mass | 3108.31 |
Thymalfasin - Reference Information
| Overview | Thymosin is a protein and polypeptide hormone with immune enhancement function produced by superficial thymic cortex and medullary epithelial cells. It is an acidic polypeptide composed of 28 amino acids. It is a biological response regulator with a wide range of biological activities. It is mainly used clinically for the treatment of immunodeficiency, viral infections and tumors, it is the first-line drug for the treatment of hepatitis B, and can also be used as a vaccine adjuvant drug with significant therapeutic effect. It has the advantages of extremely high activity, less toxic side effects and a wide range of applicable symptoms. The new trade name of Thymopeptide is Ridaxian. It is a chemically synthetic drug that is consistent with the human body's natural thymosin α1 in chemical structure and spatial structure, thus ensuring that its biological activity is completely consistent with the human body's natural thymosin α1. In other words, thymosin can play a role in the formation of T cells, including the transformation from stem cells to T cells, the further differentiation and maturation of T cells, and the antiviral and anti-tumor activities after maturity. At the same time, it also has immunomodulatory effects. Therefore, Thymus Faxin is currently the most widely used and most based drug in clinical practice. Thymosin is an old drug with a history of decades. It is different from other thymosin in terms of mechanism, principle and clinical characteristics. Thymopentin has a half-life of nearly 2 hours. It can be used 2-3 times a week to ensure the required blood concentration, while the half-life of thymopentin is only more than 40 seconds. Clinically, daily administration is not necessarily guaranteed. The required blood concentration. (Yao Yao) |
| mechanism of action | the exact mechanism of action of thymosin in the treatment of chronic hepatitis B has not been fully studied, but various experiments show that thymosin plays an obvious role in the immune response. It is mainly realized by enhancing the function of T cells, which runs through the whole process of T cell generation, differentiation and maturation, and apoptosis. Thymosin plays an immunomodulatory role by increasing the absolute number of natural killer, CD3 and CD4 cells in lymph and liver. Thymosin can promote the maturation and differentiation of bone marrow-derived DC cells, and then promote the maturation and differentiation of T cells. Thymosin can increase the production of interferon human interleukin IL2 and IL3 and other cytokines. By activating mitogen or antigen, the expression of human interleukin IL2 receptor is increased, and CD4 T cells are differentiated into Thl,Thl has significant antiviral effect. Thymosin promotes the generation of lymphocytes in the body by increasing the effect of P cells, regulates the proportion of P cell subsets, U cell differentiation and antibody production, stimulates the production of other antiviral lymphokines and macrophages and enhances phagocytic function, and improves the cellular immune system function of tumor patients. It can also remove bacteria, fungi and viruses from the body. Thymosin acts on the nervous system and around the endothelium, and regulates the synaptic transmission of hippocampal neurons. Thymus new affects the transmission of excitatory synapses and the nervous system, and can be used to prevent neurotoxicity caused by anti-cancer treatments such as chemotherapy in cancer patients. Thymosin has gene regulation, which can induce kinase cascade genes, up-regulate cytokine genes and immune response regulatory genes. The upregulation of Thymosin on Toil-like receptor gene indicates that Thymosin has a stimulating effect on antigen presenting cells. The role of thymosin in the growth of immune cells is reflected in the up-regulation of stem cell growth factor and hematopoietic protein gene expression. |
| preparation method | 1. biochemical extraction method thymosin preparations (a mixture of various peptides) are basically obtained from animal tissues, so the activity is very different. because it contains animal proteins, the possibility of allergic reactions is also relatively large. The thymus of human embryo is used as raw material, and the thymus is extracted by biochemical method. The yield is very low, but the curative effect is good. Considering the limited raw materials, high prices, low yield, complex extraction steps, etc., large-scale production is difficult, and the development prospects are not optimistic. 2. Chemical synthesis method The new main SPSS method of thymus on the market was synthesized and purified by appropriate technology. Using resin as a carrier, Fmoc was used for solid phase synthesis, 28 amino acids were sequentially coupled and synthesized according to thymosin, N-terminal amino acids were acetylated with acetic anhydride, and TFA was used as the main lysis reagent to obtain crude products. The crude products were prepared and separated by HPLC to obtain thymosin new pure products, and then further purified to obtain thymosin new raw materials. 3. genetic engineering methods there are three kinds of genetically engineered bacteria: (1) multi-string gene is cloned into the host to obtain the target gene bacteria, and finally expressed in the form of inclusion bodies. It has been reported that a new multi-string gene of thymus was constructed by random annealing and PCR, and cloned into Escherichia coli. (2) The synthesized fusion protein gene is recombined into the vector, and the vector is transformed into the host to construct genetically engineered bacteria. For example, according to the signal peptide gene in the plasmid, the expression plasmid was constructed, transformed into Pichia pastoris by electric excitation, and then the fusion protein was induced to express with methanol, and then the thymus was processed by enzyme digestion. (3) firstly, the expression vector was constructed and transferred into the host to make it become genetically engineered bacteria, and then fermented and cultured to obtain the target product. The synthetic thymus new monomer gene is connected to the corresponding plasmid to construct an expression vector, and then it is integrated into Pichia pastoris. The target product is directly secreted into the fermentation broth, and then purified in two steps to obtain high-purity thymus new, separation The steps are few, the cost is low, and the scale production is easy. |
| application | 1. thymus fasin is currently mainly used for the treatment or adjuvant treatment of various liver diseases, including hepatitis B, hepatitis c, liver cirrhosis, primary liver cancer and viral severe hepatitis. The treatment of thymosin has low side effects and is well tolerated. At the same time, thymosin is a national medical insurance class B drug for the treatment of hepatitis B and hepatitis C, and the economic burden of patients is small. 2. Thymosin is widely used in the treatment of tumors, mainly because it can significantly reduce the recurrence rate of tumors and the side effects of radiotherapy and chemotherapy. 3. Thymosin can be used to treat malignant tumors such as pancreatic cancer, lung cancer, metastatic brain tumor, rheumatism, rheumatoid, lupus erythematosus and other immune-related diseases such as leukemia. After treatment, the recurrence rate is obviously reduced, and the side effects of radiotherapy and chemotherapy are reduced. Figure 2 is a brief introduction to Ridaxin drugs 4. Radiotherapy is a commonly used method for the treatment of esophageal cancer, nasopharyngeal cancer, cervical cancer, advanced lung cancer and other diseases. Radiotherapy can also cause immune dysfunction. Combined application of thymosin can prolong the interval of chemotherapy and has clinical significance for improving the survival rate of patients. 5. chemotherapy combined with thymosin can become a new treatment for patients with advanced tumors. For malignant lymphoma, cardia cancer, gastric cancer, breast cancer, pancreatic cancer, rectal cancer and other chemotherapy combined with thymosin can improve the cellular immune function of patients and reduce adverse reactions. 6. Thymosin can also be combined with other drugs for anti-infection treatment. Compared with conventional anti-infection treatment, the number of respiratory infections is reduced, the use of antibiotics is shortened, and the effective rate is significantly improved. Thymosin has a high auxiliary synergistic effect on the treatment of refractory pulmonary tuberculosis; the addition of thyosin in the treatment of herpes zoster has a definite effect. In terms of treatment, it is better than conventional treatment methods in terms of blistering, skin lesion healing and pain relief time; Vaccination with influenza vaccine and the use of thymosin can improve the disease resistance immunity of the elderly and reduce respiratory diseases, and the older the age, the more obvious the effect. 7. Thymosin can treat condyloma acuminatum, the recurrence of laser combined with thymosin group is lower than that of conventional laser group, and can shorten the treatment time, thus reducing the pain of patients. |
| contraindications | thymosin contraindications are very few, and are forbidden for patients with a history of allergy to thymosin itself or other ingredients in thymosin for injection. Thymus is newly contraindicated in patients treated with immunosuppressive therapy such as organ transplant recipients. |
| Main references | [1] Song Jiyong, Du Guosheng, Zhu Zhidong, Zheng Dehua, Cui Hongtao, Feng Likui, Shi Bingyi. Safety of thymalfasin in patients with tumor after liver transplantation [J]. Chinese Journal of Injury and Repair (Electronic Edition),2014,9(02):166-168. [2] Li Yuanyuan. Preparation and in vitro and in vivo evaluation of thymosin microemulsion [D]. Chinese People's Liberation Army Medical College, 2013. [3] Tian Nina. Quality Analysis of Thymus Method [D]. Lanzhou University, 2015. [4] Cheng Hu, Wei Ping, Zhu Yishen. Solid Phase Synthesis of Thymosin α_1[J]. Journal of Nanjing University of Technology (Natural Science Edition),2004,(02):78-80. |
Last Update：2024-04-10 22:29:15
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CAS: 69440-99-9
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QQ: 2850607228
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QQ: 2850607228
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