133results about How to "Inhibition of clonogenicity" patented technology

The invention discloses an siRNA of a targeted long-chain noncoding RNA DDX11-AS1 and applications thereof in liver cancer treatment. Through designing and synthesizing the siRNA of the DDX11-AS1 andtransfecting a liver cancer cell line with the siRNA, it is proved that the siRNA can targetedly inhibit expression of the DDX11-AS1, can significantly suppress liver cancer cell proliferation, invasion and migration and can induce liver cancer cell apoptosis. A novel target point for research and development of a liver cancer treatment medicine is provided.

The invention discloses an application of a cyclopeptide compound for preventing tumors, and a preparation method of the cyclopeptide compound, belonging to the technical field of biological medicines. The cyclopeptide compound CP-1 or CP-2 has the functions of inhibiting cancer cell growth and proliferation, adjusting and controlling cancer cell periods and adjusting and controlling cancer cell periodic protein expression, so that the cyclopeptide compound can be used for preparing anti-cancer medicaments and / or health care products. The invention further relates to the preparation method of the cyclopeptide compound CP-1 or CP-2. The preparation method comprises the following steps of: with streptomycete as a stain, optimizing the cultivation and fermentation conditions, treating the fermented product, separating the fermented product by using a silica gel column and a reverse phase silica gel column, and finally separating by using a preparative chromatography column so as to obtain the cyclopeptide compound with activity. Compared with the prior art, the preparation method is simple, feasible, environmental-friendly, low in cost and high in yield; and according to the preparation method, the yield of microbial activity secondary metabolite is effectively increased.

The invention belongs to the biotechnical field, and concretely relates to a tumor necrosis factor family cell apoptosis protein fusion protein, and a preparation method and a use thereof. The fusion protein is composed of annexin, a connecting peptide and a tumor necrosis factor family cell apoptosis protein, and coding gene of the fusion protein is constructed through cloning. The tumor necrosis factor family cell apoptosis protein fusion protein has a substantial enhanced cell apoptosis induction effect, can induce the apoptosis of tumor cells insensitive to the cell apoptosis, and can reduce the protein administration dosage needed by the obtaining of the treatment effect.

The invention discloses application of HIP-55 protein to development of tumor inhibition drugs. DNA molecules encoding and interfering HIP-55 protein from expressing siRNA are inserted into an expression vector to obtain a recombinant vector; the amino acid sequence of the HIP-55 protein is a sequence II in a sequence table; the invention also provides application of HIP-55 protein or the recombinant vector containing the HIP-55 protein coding gene to preparation of products having the following functions of (1) promoting tumor cell migration and / or (2) promoting tumor cell invasion. Experiments prove that the HIP-55 protein gene is overexpressed in lung cancer cells to promote tumor formation, lung cancer cell migration and lung cancer cell invasion; therefore, the HIP-55 provides a new target for clinical diagnosis, treatment and development of new drugs and can be used for screening, developing and / or designing products for prevention and / or treatment of tumors.

The invention discloses application of rabdocetsin in preparing a product for inhibiting proliferation of esophageal squamous carcinoma cells. Proofed by experiment, the application has the advantages that the rabdocetsin can effectively inhibit the proliferation of the esophageal squamous carcinoma cells, the cloning formation of the esophageal squamous carcinoma cells, affecting the cycle progress of the esophageal squamous carcinoma cells, inducing the retardation of the cycle of the esophageal squamous carcinoma cells, inhibiting the DNA (deoxyribonucleic acid) restoration of the esophageal squamous carcinoma cells, inducing the withering of the esophageal squamous carcinoma cells, regulating up the expression amount of cleaved-caspase-9, regulating up the expression amount of cleaved-caspase-3, regulating up the expression amount of cleaved-PARP, inhibiting Akt signal pathways, inhibiting NF-kappa B signal pathways, and inhibiting the growth of tumors caused by the esophageal squamous carcinoma cells; the important application value is realized.

The invention relates to an application of a PNO1 inhibitor to preparation of esophagus cancer treatment medicines, belongs to the field of biopharmaceutical research, and particularly relates to an application of a PNO1 inhibitor to preparation of esophagus cancer treatment medicines. The inventor firstly finds that the PNO1 can be used as an esophagus cancer treatment target point. The PNO1 inhibitor can restrain the proliferation rate of esophagus cancer cells, can restrain the cloning and forming capacity of the esophagus cancer cells, can promote esophagus cancer apoptosis, can restrain esophagus cancer cell migration, can restrain esophagus cancer cell transfer, and can restrain esophagus cancer cell invasion and transfer, so as to treat esophagus cancer, and a new direction is opened up for treatment of esophagus cancer.

The invention discloses a tricyclic diterpene analogue shown as formula (I) and a preparation method of the analogue. The preparation method comprises the following steps: taking a tricyclic diterpene analogue (1) as a raw material, carrying out an esterification reaction, a Friedel-Crafts acylation reaction, a haloform reaction, a hydrolysis reaction and an amidation reaction so as to prepare a compound (4); and taking the compound (4) as a raw material, carrying out the amidation reaction under catalysis of DMAP, EDCI and HOBt, thereby obtaining the tricyclic diterpene analogue shown as formula (I). The invention further provides application of the tricyclic diterpene analogue in preparation of anti-prostate cancer drugs. The structural formula is as shown in the specification.

The invention belongs to the technical field of medicine and pharmacy, and discloses an application of a micromolecule compound WZ-2-033 shown as below to medicines for treating breast cancer and stomach cancer. The compound can restrain proliferation, clone formation, migration and invasion of breast cancer cells and stomach cancer cells, and can induce apoptosis of the breast cancer cells and the stomach cancer cells. The compound exerts effects through influencing an STAT3 signal channel, can reduce the phosphorylation level (Y705) of the STAT3, can reduce STAT3 dimer formation, can reduceDNA combining capacity and transcriptional activity of the STAT3, and can further reduce the expression level of STAT3 target genes c-Myc, Bcl-xL and Mcl-1 so as to restrain activation of STAT3 signals and restrain the growth of the breast cancer cells and the stomach cancer cells. In an animal model, the compound can restrain the growth of stomach cancer cell transplanted tumors and has favorableapplication prospects.

Liposarcomas are treated using HIV protease inhibitors, particularly nelfinavir. The protease inhibitors may be used alone or in combination with traditional cancer treatments, such as chemotherapy, radiotherapy, or surgery.

The invention provides an application of a long-chain non-coding RNA RP11-224O19.2 inhibitor in preparation of a drug for treating tumors. The invention further provides a drug for treating the tumors, and a kit for liver cancer screening and / or liver cancer prognosis diagnosis. The application shows that the RNA RP11-224O19.2 inhibitor has a significant treatment effect on the tumors. In addition, the expression level of RNA RP11-224O19.2 is detected, and the long-chain non-coding RNA RP11-224O19.2 inhibitor can be applied to auxiliary diagnosis and prognosis judgment of a clinical liver cancer and is good in application prospect.

The invention discloses application of etomoxir to treatment of colorectal cancer and particularly relates to application of etomoxir to preparation of medicines for preventing and treating colorectalcancer, especially medicines for inhibiting colorectal cancer metastasis. The research shows that etomoxir is capable of obviously inhibiting colony formation under anoikis of colorectal cancer cells, accelerating anoikis of colorectal cancer cells and inhibiting metastasis capability of the colorectal cancer cells in the body, has an obvious effect of treating the colorectal cancer and especially has an obvious effect of inhibiting colorectal cancer metastasis, so that etomoxir can be used for treating colorectal cancer metastasi. The invention provides novel application of etomoxir, expandsthe clinical application fields of etomoxir and further provides a novel manner for treating colorectal cancer metastas; etomoxir has good popularization and application prospects.

The invention relates to a method for slowing down ovarian surface epithelial cell vicious transformation. During ovarian surface epithelial cell vicious transformation, active vitamin D (1,25(OH)2D3) is added through each passage and after each culture medium replacement so as to slow down the ovarian surface epithelial cell vicious transformation. The invention further provides application of the vitamin D in the preparation of medicine for treating ovarian cancer. By the long-term use of low dosage of vitamin D, 25-hydroxyvitamin D or active vitamin D, the tumorigenic ability of ovarian surface epithelial cells in the body of a nude mouse can be weakened effectively.

The invention belongs to the field of chemistry, particularly relates to an application of an SIRT1 inhibitor and sorafenib in preparing medicaments for treating liver cancer. The method of the invention can inhibit proliferation, differentiation and cloning of liver cancer stem cells, improve sensibility of liver cancer stem cells to sorafenib, reduce drug resistance of liver cancer stem cells to sorafenib, and enhance damage of sorafenib to liver cancer stem cells, so as to kill tumor stem cells from the source and bring new hope for eliminating tumors.

The invention discloses a small molecule compound cyy-260 and application thereof in preparation of antitumor drugs; the small molecule compound is a JAKs inhibitor, the structure of the small molecule compound is shown as a formula (I), and the small molecule compound has an inhibition effect in occurrence and development of non-small cell lung cancer. Experiments prove that cyy-260 can inhibit lung cancer cell proliferation, clone formation and migration in a concentration-dependent manner and induce apoptosis. The anti-tumor biological activity is achieved at lower concentration.

The invention discloses application of a small molecular compound WB460 shown in a formula (I).in preparation of a medicine for treating pancreatic cancer In vitro, the compound can inhibit proliferation, migration, invasion and colon of pancreatic cancer cells, and can induce pancreatic cancer cells to generate apoptosis and cell cycle arrest; in vivo, WB460 inhibits growth and transferring of pancreatic cancers. The WB460 has good application prospect.

The invention specifically relates to application of losmapimod to non-small cell lung cancer, belonging to the field of chemoprophylaxis of tumors. Losmapimod and a tyrosine kinase receptor inhibitorfor non-small cell lung cancer are combined and applied to non-small cell lung cancer, so tumor cells are enhanced in sensibility to the tyrosine kinase receptor inhibitor for non-small cell lung cancer, and formation of drug resistance is delayed. In the invention, it is proved for the first time that formation of gefitinib-resistant cell strains and gefitinib resistance is dependent on formation of tetraploid cells. When losmapimod and gefitinib are applied to tumor cells of non-small cell lung cancer together, tumor cells are obviously enhanced in sensibility to gefitinib, and multiplication and clone formation capabilities of tumor cells are inhibited; and thus, when gefitinib is applied to treatment of non-small cell lung cancer, the occurrence of gefitinib resistance is delayed, andthe application effect of gefitinib in treatment of non-small cell lung cancer is enhanced.

The invention relates to a drug composition containing a AKT inhibitor and an IRE1 inhibitor and application of the drug composition in preparing drug for preventing and treating tumor. The AKT inhibitor is selected from MK-2206, Perifosine, Ipatasertib or AZD5363, and is MK-2206 preferably; the IRE1 inhibitor is selected from STF-083010, APY29 or 4u8C, and is STF-083010 preferably. The drug composition combines MK-2206 with STF-083010, a new treatment scheme is provided for tumor patients, growing of tumor cells and forming of cell cloning can be inhibited effectively, the drug composition has effect remarkably better than single use of MK-2306 or STF-083010, has additive or synergistic effect, has low toxic and side effect on normal cells, is high in safety and can be applied in the field of preparing anti-tumor drug.

The invention discloses application of macrocarpal I to preparation of an anti-tumor drug. In an experiment, the inventor finds that the macrocarpal I can effectively inhibit proliferation in vitro orinvasion of colorectal cancer cells, can inhibit the clonality of the colorectal cancer cells, can reduce the growth rate of the subcutaneous tumor of a naked mouse and has certain specificity to thecolorectal cancer cells. In addition, the macrocarpal I is extremely high in safety and expected to be a natural anti-tumor micro-molecular compound applied to the treatment of the metastatic colorectal cancer.

The invention discloses an application of pectolinarigenin in the preparation of an anti-esophageal cancer drug. Pectolinarigenin is named as 5,7-dihydroxy-4',6-dimethoxyflavone. The invention verifies the inhibition effect of pectolinarigenin on esophageal squamous cell carcinoma cells, and verifies the remarkable effect of pectolinarigenin on the prevention and treatment of esophageal cancer ona patient derived xenograft model (PDX). Research results show that pectolinarigenin can inhibit the proliferation of esophageal squamous cell carcinoma cells KYSE150 and KYSE450 and inhibit the cloneformation of the esophageal squamous cell carcinoma cells. Compared with a tumor volume of a control group, a tumor volume of a mouse treated by pectolinarigenin has a remarkable statistical difference. Therefore, the situation that pectolinarigenin has remarkable inhibition effects on esophageal squamous cell carcinoma cells and remarkable effects of preventing and treating esophageal cancer isshown. Therefore, pectolinarigenin can be used as an existing clinical use drug to play a role in preventing and treating esophageal squamous cell carcinoma.

The invention belongs to the field of chemistry, particularly discloses application of SIRT1 expression interfering agent in preparation of medicine for inhibiting self renewal of liver cancer stem cell. The self renewal of liver cancer stem cells is inhibited by inhibiting SIRT1 expression in liver cancer stem cells to remarkably reduce proliferation capacity, cloning capacity and balling capacity of liver cancer stem cells, so that the SIRT1 expression interfering agent can be used for preparing medicaments for targeting treatment of liver cancer.

The invention relates to an Eps8-SH3 structural domain-based dual antitumor polypeptide. The polypeptide has an amino acid sequence of Lys-Tyr-Ala-Lys-Ser-Lys-Tyr-Asp-Phe (SEQ ID No: 1). The dual antitumor polypeptide can induce cytotoxic T cells, effectively kill HLA-A*2402 positive and Eps8 positive tumors, directly inhibit HLA-A*2402 positive and Eps8 positive tumor cell proliferation and be used for preparation of dual antitumor drugs.

The invention discloses a cell strain capable of stably secreting and expressing IL-24 recombinant protein, and construction and application thereof, belonging to the technical field of gene engineering. The construction method of the cell strain comprises the following steps: subcloning CDS region sequence of IL-24 gene into pcDNA5 / FRT plasmid of an Flp-In targeted integration system, transfecting into Flp-In-CHO cell together with plasmid pOG44, and screening the stable-expression cell strain by using antibiotic Hygromycin B; purifying the recombinant protein in the cultured supernatant of the cell strain by affinity chromatography; and finally, carrying out in-vivo and in-vitro activity experiments to prove that the recombinant protein has an action on inhibiting esophagus cancer cells and melanoma cells from proliferation and can induce the apoptosis of the esophagus cancer cells and melanoma cells, thereby developing an effective new drug for treating tumors.

The invention discloses an application of mozavaptan in preparation of anti-digestive tract tumor drugs, the chemical name of the mozavaptan is 5-(dimethylamino)-1-[4-(2-methylbenzamido)benzoyl]-2,3,4,5-tetrahydro-1H-benzazephe, and experiments prove that the mozavaptan can inhibit esophageal squamous cell carcinoma cells KYSE150 and KYSE450, proliferation of gastric cancer cells HGC27 and AGS, clone formation of esophageal squamous carcinoma cells and induce the cell apoptosis. Therefore, it is shown that mozavaptan has a remarkable inhibition effect on esophageal squamous cell carcinoma cells. Therefore, the mozavaptan can be used as an existing clinical medicine to play a role in preventing and treating tumors. The invention provides a new application of mozavaptan in tumor treatment and prevention.

The invention relates to an application of 2,2',2''-((2,4,6-trihydroxybenzene-1,3,5-triyl)tris(methanylylidene))tris(hydrazinecarbothioamide) in the preparation of antitumor drugs, especially in the preparation of anti-liver cancer drugs. Cell proliferation, cell morphology, cell colony formation, apoptosis, cell cycle, molecular biology and other experiments prove that the compound can effectively inhibit the proliferation of tumor cells, inhibit the tumor cell cloning formation, induce tumor cell apoptosis and affect the cycle of the tumor cells, has significant influences on proteins associated with tumor apoptosis, and has significant antitumor activity. The application provides a basis for the development of novel antitumor drugs, and the compound has a good clinical application prospect. The 2,2',2''-((2,4,6-trihydroxybenzene-1,3,5-triyl)tris(methanylylidene))tris(hydrazinecarbothioamide) which can be used as a pharmaceutically active ingredient and a pharmaceutically acceptablecarrier can be used to prepare an antitumor medicinal composition.

The invention discloses an aegiceras corniculatum stem ethyl acetate extract and a preparation method thereof. The method includes: soaking aegiceras corniculatum stems into ethanol to obtain aegiceras corniculatum stem ethanol extract; after volatilization of ethanol in the aegiceras corniculatum stem ethanol extract, adding petroleum ether for extraction to obtain a lower water phase; adding ethyl acetate into the lower water phase, continuing extraction to obtain upper ethyl acetate part extract, and performing water bath drying to obtain the aegiceras corniculatum stem ethyl acetate extract. According to in-vitro molecular biological experiment researches, the aegiceras corniculatum stem ethyl acetate extract has an anti-proliferation effect on human prostatic cancer cells PC3 and DU145 and is capable of evidently inhibiting clone formation of the human prostatic cancer cells PC3 and DU145. Therefore, the aegiceras corniculatum stem ethyl acetate extract has a potential application prospect in preparation of medicines for treating prostatic cancer and can be used for preparation of the medicines for treating prostatic cancer. Deeply developing the aegiceras corniculatum stem ethyl acetate extract can expand an aegiceras corniculatum utilization range to create a novel approach for cancer treatment.

The invention belongs to the field of biological medicines and discloses a pharmaceutical composition and application thereof in preparation of medicaments for treating tumors. The pharmaceutical composition is a group of compositions containing chemical drugs and / or containing siRNA or recombinant viruses expressing shRNA, wherein the pharmaceutical composition containingthe chemical drugs comprises (i) sodium dichloroacetate or analogues thereof and (ii) chloroquine or analogues thereof, and the pharmaceutical composition containing the siRNA or the recombinant viruses expressing the shRNAcomprises a) siRNA and / or shRNA of an integrin subunit, or an inhibitor thereof, or an antibody, or b) an expression vector constructed based on a target sequence of the siRNA or the shRNA of the integrin subunit. The pharmaceutical composition has anti-cancer effects of inhibiting tumor cell proliferation, improving tumor cell metabolism, inhibiting autophagy and generation of neovascularizationin tumor microenvironment.

The invention relates to a pharmaceutical composition for treating the cancer and an application of the pharmaceutical composition. The pharmaceutical composition comprises methotrexate as an active ingredient and a BRD4 protein inhibitor, and the mass ratio of the methotrexate to the BRD4 protein inhibitor ranges from 10:1 to 1:8. The pharmaceutical composition obviously improves the chemotherapeutic effect of the methotrexate, the similar chemotherapeutic effect is achieved by using the methotrexate at the relatively low concentration, therefore, the toxicity on a nude mouth is obviously reduced, and the injury of the pharmaceutical composition on the organism is reduced, so that the pharmaceutical composition is applied to preparation of anti-tumor drugs.

The invention discloses use of nitazoxanide or pharmaceutically acceptable salt thereof in preparation of a drug for treating bladder cancers. The nitazoxanide or the pharmaceutically acceptable saltthereof is capable of inhibiting proliferation and clonality of different bladder tumor cell lines, so that the potential of a mitochondrial membrane is decreased, ROS is generated and increased, andapoptosis of bladder cancer cells is caused; meanwhile, the nitazoxanide or the pharmaceutically acceptable salt is capable of effectively inhibiting stemness maintenance of the bladder cancer cells;and the nitazoxanide and the pharmaceutically acceptable salt still have an effect of inhibiting growth of bladder tumors in vivo, appearances of reduction of activities and feeding and the like of nude mice do not appear under a therapeutic dose, and phenomenon of obvious sliming or death of the nude mice do not appear as well, so that the nitazoxanide and the pharmaceutically acceptable salt have better treatment and application prospects to the bladder cancers.

The invention belongs to the field of biomedical technologies, provides a function of DNA (deoxyribonucleic acid) damage repair related genes for cervical cancer, and further relates to application of TIMELESS siRNA [small interfering RNA (ribonucleic acid)] and medicine compositions to treating cervical cancer. The medicine compositions comprise effective dose of siRNA nucleotide fragments and pharmaceutically acceptable excipients. The application has the advantages that obvious correlation between the gene TIMELESS expression level and the progress of the cervical cancer is confirmed by the aid of molecular biology means for the first time, and the TIMELESS genes are hardly expressed in normal cervical tissues; the siRNA with the TIMELESS genes used as targets at gene level is screened, and siRNA sequences capable of efficiently and specifically knocking down the TIMELESS expression are provided; the proliferation and clone formation ability of cervical cancer cells can be obviously inhibited by the TIMELESS siRNA, apoptosis and senescence of the cervical cancer cells can be promoted, and the cisplatin sensitivity of the SiHA (human cervical squamous carcinoma) cells can be promoted; expression of Cleaved Caspase-3 and p21 can be up-regulated by the siRNA, and accordingly the apoptosis and senescence of the cervical cancer cells can be ultimately promoted.