26 results about "Stat3 Signaling Pathway" patented technology

The invention discloses application of (20S)-ginsenoside Rh1 in preparation of drugs for preventing and / or improving cerebral arterial thrombosis, and relates to the technical field of medical application of natural drugs. The invention verifies that (20S)-ginsenoside Rh1 up-regulates the expression of an anti-apoptosis gene by promoting STAT3 phosphorylation and translocation to a cell nucleus, so that the (20S)-ginsenoside Rh1 plays a role in protecting neuronal injury induced by sugar oxygen deprivation. In MCAO model mice, the (20S)-ginsenoside Rh1 obviously relieves the symptom of ischemic cerebral apoplexy and has positive influence on neurodegenerative events related to cerebral infarction, and the anti-apoptosis and neuroprotection effects are most prominent. Mechanism research shows that (20S)-ginsenoside Rh1 plays a therapeutic role in PC12 cell and MCAO model mice by activating a JAK2 / STAT3 signal channel.

The invention discloses application of THBS1 in preparation of pancreatic cancer diagnosis and treatment products. Wherein THBS1 in pancreatic cancer cells is high in expression, and the higher expression level of THBS1 is related to poor prognosis of pancreatic cancer patients; in addition, migration and invasion of pancreatic cancer cells can be inhibited by reducing THBS1 gene expression, and apoptosis is promoted at the same time; in addition, the THBS1 inhibitor can also be used for preparing a medicine for inhibiting a JAK2 / STAT3 signal channel (reducing phosphorylation of JAK2 and STAT3).

The invention discloses a stem cell composition and application thereof in regulating sub-health. The stem cell composition comprises mesenchymal stem cells (MSCs) modified by fusion polypeptide and an anti-IL-6R single domain antibody. The amino acid sequence of the fusion polypeptide is as shown in SEQ ID NO.1, and the fusion polypeptide is modified on the surface of stem cells through click chemistry, so that the chemotactic migration ability, collagen matrix affinity and inflammation tolerance of the stem cells are remarkably improved. The anti-IL-6R single-domain antibody is obtained through phage display screening, the VHH gene of the anti-IL-6R single-domain antibody is shown as SEQ ID NO.2, and the anti-IL-6R single-domain antibody has high affinity and activity of inhibiting an IL-6 / STAT3 signal channel. Animal experiments show that the composition can significantly reduce inflammatory factor (IL-6) and cortisol levels of chronic stress model mice, improve oxidation resistance (SOD) and recover immune homeostasis, and provides an innovative treatment strategy for adjustment of sub-health status.

The application discloses an azaphilone molecule targeting STAT3 signal pathways, a preparation method and purposes. The structural formula of the azaphilone molecule chaetoviridinol A1 is shown as formula (A). The azaphilone molecule chaetoviridinol A1 or a medicinal salt thereof has the purposes of preparing an antitumor drug.

The invention discloses application of a gp130 inhibitor in preparation of a medicine for treating virus infection, and relates to the technical field of medicines. Experiments prove that combination of IL-6 family cell factors and a gp130 receptor is inhibited, so that downward signal transmission of a JAK2 / STAT3 signal channel triggered by the IL-6 family cell factors is inhibited, the purposes of inhibiting cell fusion induced by SARS-CoV-2 spike protein and further influencing replication and propagation of SARS-CoV-2 are achieved, and a small-molecule inhibitor SC144 is an inhibitor of gp130, has a remarkable effect of inhibiting SARS-CoV-2 virus replication and has a good application prospect. Meanwhile, the traditional Chinese medicine composition also has a remarkable effect of inhibiting replication of viruses such as human immunodeficiency virus, herpes simplex virus and respiratory syncytial virus.

The present invention discloses a class of flavonoid derivatives, their preparation methods, and applications. The structural formula is shown in Formula I: wherein X is selected from CH and N, and R1 is selected from H. These compounds can significantly inhibit the activation of STAT3, a cell signaling pathway, at low doses. Experimental results show that these compounds can significantly inhibit the proliferation of various tumor cell lines, including lymphoma, multiple myeloma, cervical cancer, breast cancer, gastric cancer, lung cancer, and pancreatic cancer. They can specifically inhibit STAT3 signaling activation and the expression of the downstream target gene cyclinD1, indicating that these compounds have the potential to be developed as targeted anti-tumor drugs related to the STAT3 signaling pathway.

The invention belongs to the technical field of biological medicines, and provides application of combination of nicotinic acid and metformin in blocking the progress of esophageal squamous carcinoma. The invention discovers that nicotinic acid and metformin inhibit FRMD8 expression through different mechanisms for the first time so as to inhibit a JAK1-STAT3 signal channel. Nicotinic acid and metformin are combined to achieve a more remarkable inhibition effect on the ability of esophageal squamous cell carcinoma cells to subcutaneously grow in mice and generate pulmonary metastasis through caudal veins than a single drug, and a brand new drug direction is provided for prevention and treatment of esophageal squamous cell carcinoma.

This invention provides an application of *Lactobacillus paracasei* IOB413 metabiotic and its composition in gastric cancer, belonging to the field of microbial technology. *Lactobacillus paracasei* IOB413 has the preservation number CGMCC No. 16022. Its metabiotic can inhibit gastric cancer progression by suppressing epithelial-mesenchymal transition in tumor cells and regulating the IL-6 / JAK2 / STAT3 signaling pathway. The composition with folic acid has a synergistic effect, more effectively reducing tumor volume and lowering the levels of pro-inflammatory factors and tumor markers. It has high safety and is suitable as an adjuvant therapy before and after gastric cancer surgery, providing a new approach to gastric cancer treatment.

The present invention relates to an amplification enhancer, which enhancer comprises a protein molecule capable of triggering the intracellular domain, transmembrane domain and extracellular domain of the cellular STAT5 and / or STAT3 signaling pathways; the present invention also relates to lymphocytes expressing the amplification enhancer and their use as immunotherapeutic drugs.

The invention relates to the technical field of nano-drugs, in particular to a tolbuzumab / lanthanide series metal / nucleic acid nano-composite, a preparation method and application. The mass ratio of the tolbuzumab to the lanthanide series metal to the nucleic acid in the nano-composite is (0.5-5.1): 1: (10-11). The nano compound disclosed by the invention can be used for promoting the activation of a cGAS-STING-STAT1 pathway and blocking an IL6 / IL6R-STAT3 signal pathway at the same time, so that chronic inflammation caused by a CIN phenomenon of tumor cells is converted into anti-tumor immune response.

The invention belongs to the technical field of medicines, and relates to a benzimidazo 2-amino-1, 3, 4-thiadiazole carboxylic ester derivative shown as a formula I, a pharmaceutically acceptable salt and a preparation method thereof, a composition containing one or more compounds, and application of the compounds as an STAT3 signaling pathway inhibitor in treatment of STAT3 high-expression cancer diseases, and particularly relates to a preparation method of the benzimidazo 2-amino-1, 3, 4-thiadiazole carboxylic ester derivative shown as the formula I. The invention also relates to a preparation method of the benzimidazo 2-amino-1, 3, 4-thiadiazole carboxylic ester derivative.

The invention belongs to the technical field of biology, and relates to an in-vitro preliminary screening method of an IL-6 / JAK2 / STAT3 signal channel inhibitor. The method comprises the following steps: co-culturing mouse spleen lymphocytes and a to-be-detected compound, and determining the critical concentration of the to-be-detected compound which does not reduce the cell activity; dividing the mouse spleen lymphocytes into a model group, an experimental group and a control group; only 10-20ng / mL of IL-6 is added into the culture solution of the model group, 10-20ng / mL of IL-6 and a to-be-detected compound with critical concentration are added into the culture solution of the experimental group, and no additional substance is added into the culture solution of the control group; if the STAT3 mRNA expression quantity, the STAT3 and p-STAT3 protein expression quantity and the IgG content of the model group are all higher than those of the control group and the experimental group, the compound to be detected is judged to be the IL-6 / JAK2 / STAT3 signal channel inhibitor. The method can reduce resource investment of animal experiments and clinical tests.

The invention provides a method and system for detecting the malignant degree of endometrial cancer cells, and the method comprises the following steps: judging the influence mechanism of leptin on the malignant degree of cancer cells by detecting parameters such as leptin concentration, JAK2 / STAT3 pathway activation degree, cell proliferation activity, migration and invasion ability and the like; the dynamic association between the leptin concentration change and the activation state of the JAK2 / STAT3 signal channel can be systematically evaluated, the regulation and control effect of the channel on the proliferation, migration and invasion ability of cancer cells is effectively quantified, and a scientific basis is provided for developing treatment schemes and drugs for endometrial cancer.

Disclosed is an anti-interleukin 11 (IL-11) antibody or a fragment thereof, which has high affinity for antigen IL-11, can block the formation of an IL-11 / IL-11Rα / GP130 complex and inhibit the activation of the STAT3 signal pathway. Therefore, the anti-interleukin 11 antibody or the fragment thereof can effectively neutralize the activity of IL-11, and can be used for preventing, treating and / or improving diseases or conditions related to IL-11 expression (including overexpression).

The present application relates to the technical field of organic synthesis, and particularly provides an indole compound, a preparation method and application thereof. The chemical structural formula of the indole compound is shown as formula I. The provided indole compound can inhibit the growth of Jurkat leukemia cells in combination with dexamethasone at different concentrations, and the indole compound in combination with dexamethasone can activate the phosphorylation level of glucocorticoid, inhibit the PI3K / AKT and JAK2 / STAT3 signal pathways related to glucocorticoid resistance to overcome the drug resistance of glucocorticoid, and make the leukemia cells die.

The present disclosure discloses the use of Tegaserod or a pharmaceutically acceptable salt thereof as a JAK-STAT3 signaling pathway inhibitor and an immunomodulator in the preparation of an anti-tumor drug. Tegaserod and the pharmaceutically acceptable salt thereof show a very excellent inhibitory effect on the growth of various tumor cells in vivo and in vitro, and are expected to be used in the treatment of various cancers.

The invention provides an application of an IGFBP5 (Insulin-like Growth Factor Binding Protein 5) gene in preparation of a medicine for improving endometrial receptivity impairment, and the IGFBP5 gene is used for preparing the medicine for improving the endometrial receptivity impairment. The number of embryo implantation sites can be effectively increased, abnormal proliferation of endometrial epithelial cells is reduced, and the relative expression level of estrogen response genes and progestational hormone response genes is improved. The IGFBP5 gene disclosed by the invention is a key downstream effector molecule of an IL-22-STAT3 signal channel, and the endometrial receptivity can be enhanced by supplementing IGFBP5 protein so as to save embryo implantation failure.

The invention relates to the technical field of traditional Chinese medicines, and discloses a traditional Chinese medicine composition for treating atherosclerosis as well as a preparation method and application thereof. The invention provides a traditional Chinese medicine composition for preventing and / or treating atherosclerosis. The traditional Chinese medicine composition is prepared from the following raw materials: rhizoma zingiberis, cassia twig, radix salviae miltiorrhizae, caulis spatholobi, semen persicae, rhizoma chuanxiong, rhizoma atractylodis macrocephalae, poria cocos, fructus crataegi, medicated leaven, rhizoma atractylodis and rhizoma acori graminei. The traditional Chinese medicine composition provided by the invention has the effects of warming yang, activating blood, tonifying spleen and reducing phlegm, is mainly used for treating atherosclerosis caused by yang deficiency, blood stasis, spleen deficiency and phlegm stagnation, and is preferably suitable for a subclinical stage. Researches find that the traditional Chinese medicine composition regulates polarization of macrophages and inhibits development of an inflammation process by inhibiting a JAK2 / STAT3 signal channel, so that the progress of AS is relieved. The traditional Chinese medicine composition provided by the invention provides a safe and effective traditional Chinese medicine early intervention scheme convenient for long-term application for huge SAS people.

The invention belongs to the field of biological medicines, and particularly relates to a cortex ailanthi extract, a quassin compound, and a preparation method, application and a pharmaceutical composition thereof. The quassin compound shown in the formula I is extracted from cortex ailanthi, can be used as a novel JAK2 inhibitor, can be combined with JAK2 protein in a high affinity manner, and blocks JAK2 kinase activity and a downstream STAT3 signal channel, so that triple negative breast cancer cell proliferation and clone formation are inhibited, and cancer cell apoptosis is induced. Therefore, the quassin compound disclosed by the invention is expected to provide a new strategy for targeted therapy of the triple negative breast cancer, and has a good application prospect. Formula I

The present invention discloses a class of piperazinamide derivatives, their preparation methods, and applications, belonging to the field of targeted tumor therapeutics. The structural formula is shown in General Formula I: #imgabs0#, wherein n=1, 2, 3, 4, 5, ..., 10, and R1 is selected from #imgabs1##imgabs2#. These compounds can significantly inhibit the activation of the STAT3 signaling pathway in cell signaling at low doses. Experimental results show that these compounds can significantly inhibit the proliferation of various tumor cell lines, including lymphoma, multiple myeloma, leukemia, breast cancer, gastric cancer, lung cancer, and pancreatic cancer. They can specifically inhibit STAT3 signaling activation and the expression of the downstream target gene C-myc, indicating that these compounds have the potential to be developed as targeted anti-tumor drugs related to the STAT3 signaling pathway.

The invention provides a combination capable of efficiently inducing differentiation of hematopoietic stem / progenitor cells to megakaryocyte lineage cells. The combination comprises three components: a first component, a second component and a third component, wherein the first component is an HSE7 gene or protein, mRNA of HSE7, an HSE7 expression cassette or an HSE7 accelerant; the second component is a histone deacetylase inhibitor; and the third component is a gamma-aminobutyric acid agonist. Also provided is a method for efficiently inducing differentiation of hematopoietic stem / progenitor cells into meganuclear lineage cells, comprising overexpressing HSE7, inhibiting HDAC expression and / or activity, and administering a GABA agonist.

The present invention provides a gene / drug co-loaded liposome and a preparation method and use thereof. The liposome of the present invention comprises a lipid membrane, a small molecule drug and a gene; the lipid membrane is a cationic lipid membrane; the small molecule drug is a STAT3 pathway inhibitor; the gene targets the JAK / STAT3 signaling pathway. The co-loaded liposome provided by the present invention can simultaneously load genes and small molecule drugs targeting the key signaling pathway JAK / STAT3 in psoriasis, deliver the gene and the small molecule drug into the cell together, block the STAT3 signaling pathway from the gene and protein levels respectively, exert a synergistic effect, have good biocompatibility and safety, and achieve the purpose of better treating psoriasis.

The invention belongs to the technical field of traditional Chinese medicine anti-tumor, and discloses insoluble traditional Chinese medicine small molecule icaritin HP (ICT) loaded hydrogel as well as a preparation method and application thereof. The HP-coated ICT hydrogel has the characteristics of good injectability, thermosensitivity, stability, excellent degradation capability, in-vivo biocompatibility and the like, meanwhile, long-acting slow release can be realized, and the drug can be retained in a tumor for one week. The HP (at) ICT can effectively reverse the tumor immunosuppressive microenvironment by inhibiting a JAK2 / STAT3 signal channel. In-vivo experiments prove that the HP (at) ICT can obviously inhibit the growth of residual hepatocellular carcinoma after radiofrequency ablation of mice and the polarization of tumor-related neutrophil (TAN) in residual cancer tissues from N2 type and PMN-MDSC type to N1 type, and meanwhile inhibit Treg cell infiltration, collect CD8 + T cells and promote the functions of the CD8 + T cells, so that the anti-tumor immunity of the organism is enhanced, and the growth and metastasis of tumors are inhibited.

The invention discloses application of moutan bark derived carbon dots in a medicine for treating acute myelogenous leukemia. The moutan bark derived carbon dots obtained by high-temperature heating through a one-step hydrothermal method can significantly inhibit the cell activity of acute myelogenous leukemia, and show excellent oxidative damage resistance and STAT3 signal channel activation inhibition ability in an in-vivo acute myelogenous leukemia resistance experiment. The moutan bark derived carbon dots can significantly inhibit infiltration of acute myelogenous leukemia cells in the liver, spleen and bone marrow, greatly prolong the lifetime of mice with acute myelogenous leukemia, and have no significant toxicity to the weight, main tissue and blood biochemical indexes of the mice. The invention is expected to provide a new technology and a new preparation for acute myelogenous leukemia.

The application discloses tegaserod or a pharmaceutically acceptable salt thereof as a JAK-STAT3 signal pathway inhibitor, an immunomodulator and application thereof in preparation of an antitumor drug. Tegaserod and the pharmaceutically acceptable salt thereof have very good inhibiting effect on the growth of various tumor cells in vivo and in vitro, and are expected to be used in the treatment of various cancers.

The invention belongs to the technical field of medicines, and relates to a benzimidazo 2-amino-1, 3, 4-thiadiazole compound and a pharmaceutical application thereof, in particular to a benzimidazo 2-amino-1, 3, 4-thiadiazole derivative shown as a formula I, a pharmaceutical salt thereof, a preparation method of the benzimidazo 2-amino-1, 3, 4-thiadiazole derivative, a composition containing one or more of the compounds, and a pharmaceutical application of the benzimidazo 2-amino-1, 3, 4-thiadiazole compound. The invention also discloses application of the compound as an STAT3 signal channel inhibitor in the aspect of treating tumor diseases. # imgabs0 #