61 results about "U251 cell" patented technology

The invention belongs to the technical field of medicines and particularly relates to a callicarpa nudiflora extract or a diterpene compound separated from an overground part of callicarpa nudiflora and medical application of pharmaceutical composition prepared from the callicarpa nudiflora extract and the diterpene compound to preparation of medicines for treating gliomas. According to in-vitro tests, the callicarpa nudiflora extract and the diterpene compound can play a role in inhibition of human brain malignant spongioblastoma U251 cells by inhibition of cell proliferation and induction of cell apoptosis and can be used for development of the medicines for treating the gliomas.

The invention relates to water caltrops polysaccharide, the extraction method and the usage, belonging to field of Chinese herbal medicine, which is characterized in comprising following preparation methods: crude polysaccharide is prepared and purified and dissolved and produced into 5% of sugar solution; volume ratio of chloroform and normal butyl alcohol solution is 1 to 0.2; crude polysaccharide solution, chloroform and normal butyl alcohol solution are mixed according to volume ratio of 2 to 5 : 1 and are added into a vessel for oscillating about 30 min and centrifuging 15 min; the aqueous phase at the upper layer is taken for storing; the chloroform phase and protein solution are thrown away; protein can be removed three times according to the above method before the polysaccharide is dried and decolored through adopting active carbon method. The water caltrops polysaccharide has the advantages of anti-tumor, obvious proliferation inhibition and apoptosis induction upon Hela and U251 through pharmacodynamics experiment showing.

The invention belongs to the technical fields of medicinal chemistry and polypeptide biology, and relates to an oligopeptide derivative P15 capable of combination of basic fibroblast growth factor (bFGF), wherein the sequence of the P15 is N'-PILQAGLGGGS-NH2-C'. The invention specifically relates to the sequence of the P15, and an application of the P15 in fields of basic research and medicine. The present invention further comprises various peptide derivatives of the P15, wherein the P21 is the peptide derivative of the P15, and the sequence of the P21 is N'-PLLQA TA GGGS-NH2-C'. With combination of the bFGF, the P15 and the P21 can provide good inhibition activities for bFGF-induced NIH3T3 cell proliferation and bFGF-induced Bable / C 3T3 cell proliferation, can significantly inhibit proliferations of bFGF-induced lung cancer A549 cells and bFGF-induced glioma U251 cells, and provide prospects for development into anti-tumor peptide drugs.

The invention relates to a medicinal diterpenoid compound separated from dried aerial parts of Callicarpa nudiflora and a preparation method of the compound. The diterpenoid compound is reported for the first time, adopts a novel structure, and can be obtained through extraction from the dried aerial parts of the Callicarpa nudiflora, separation and purification. In-vitro tests prove that the compound plays a role in inhibiting human brain glioblastoma U251 cells by inhibiting cell proliferation and inducing cell apoptosis and can be developed into drugs for treating neuroglioma.

The invention relates to a new compound with remarkable antibacterial and antineoplastic activity, which has the following structure (shown in formula I), and has good antibacterial function for methicillin-resistant staphylococcus aureus (MRSA) and methicillin sensitive staphylococcus aureus (MSSA) as well as good antineoplastic function for human cervical cancer Hela cells, human liver cancer BEL-7402 cells, human mucinous epidermoid lung cancer A549 cells, human breast cancer MCF-7 / s cells and human glioma U251 cells. (In the formula I,) R=-CH3 or CF3, X=O, S or N, and R1=-Cl, -F, -CH3, -CF3, -OCH3 and -OCF3.

The invention discloses a double-strand small activation RNA (dsLRIG-712) for activating cancer suppressor gene LRIG1 expression in brain glioma U251 cells and and application of double-strand small activation RNA (dsLRIG-712). dsLRIG-712 consists of 21 nucleotide positive-sense strands and antisense strands, two dTdT nucleotides are suspended at the 3'terminal of each strand in a protruding manner, and the other 19 nucleotides are mutually paired. The saRNA molecule can specifically activate expression of the LRIG1 gene, the target gene mRNA and the protein expression level are improved, proliferation and exercise capabilities of brain glioma cells are inhibited, and the purpose of suppressing tumor growth is achieved. Therefore, the saRNA molecule can be used for treating brain glioma.

The invention belongs to the technical field of medicine and particularly relates to a pharmaceutical composition for treating glioma.The pharmaceutical composition comprises a component A, a component B, a component C and a component D, wherein the component A is diterpenoids (I) extracted from callicarpa nudiflora, the component B is withanolides (II) extracted from the dried whole herb of asiatic plantain, the component C is triterpenoid saponins echinoside A purchased from the market, and the component D is flavonoids (IV) extracted from the overground part of vervain.In-vitro experiment prove that the pharmaceutical composition can inhibit the human brain malignant glioblastoma U251 cells by inhibiting cell proliferation and inducing cell apoptosis and can be developed into medicine for treating the glioma.

The invention relates to a novel application of fusion protein TAT-DCF1. By judging dcf1-induced U251 cell line apoptosis by virtue of such methods as immuno-electron microscope, atomic force microscope, CCK8 proliferation assay, JC-1 dyeing, nude mouse tumor heterotopic transplantation and the like, results show that dcf1, which is positioned in mitochondria, can cause pathological change of the mitochondria structure and result in drop in membrane potential, so that expression amounts of related genes are changed, and the apoptosis is finally induced. Nude mouse experiments show that them dcf1 can obviously diminish tumor volume of glioma, so that tumor growth is inhibited.

The invention discloses a clerodane type diterpene compound for treating neuroglioma, belongs to the field of medicine, and specifically relates to a novel clerodane type diterpene compound which is separated from dry nearly-matured fruits of cardamom, a preparation method and medical applications thereof. The compound is reported for the first time and is extracted from the dry nearly-matured fruits of cardamom, the extract is separated and purified, and the purity is high. The in-vitro experiment results show that the compound can inhibit human brain malignant glioblastoma U251 cell by inhibiting cell proliferation and inducing apoptosis and can be further developed to prepare drugs for treating neuroglioma.

The invention discloses a preparation method and medicinal application of CHB which is an effective component of bupleurum Chinese and particularly relates to an application of CHB in preparation of a product for treating depression. The CHB which is the effective component of the bupleurum Chinese has a good effect on treating depression caused by various factors, has a certain protection effect on a U251 cell damaged by corticosterone and has the effects of shortening the tail-suspending immobility time and the swimming immobility time of a mouse and improving the decrease of the body temperature of the mouse due to reserpine. Each dose group is significantly and statistically different from the model group, is dose-dependent and has a good antidepressant function.

The invention discloses application of a Wuling capsule in the preparation of a medicament for inhibiting proliferation of a U251 cell. The Wuling capsule comprises various main components such as Wuling fungus powder, vitamins of VitE, B1, B6, K1 and the like and trace elements of Zn, Fe, Ca and the like, wherein the Wuling fungus powder contains 19 kinds of amino acids, such as adenosine, polysaccharide, sterols, glutamic acid, Y-aminobutyric acid and lysine. The Wuling capsule has the functions of reinforcing the kidney and brain and tranquilizing mind by nourishing the heart and is suitable for treating disharmony of heart and kidney of neurasthenia, insomnia, amnesia, physical and mental fatigue, soreness and weakness of waist and knees, minor veins or myasthenia gravis and the like. The Wuling capsule is orally taken by thee granules each time, with three times each day or follows the advice of doctors; the weight of each granule is 0.33g; and the Wuling capsule is found to have the efficacy of inhibiting the proliferation of the U251 cell.

The present invention relates the application of a human source dcf1 gene in the inhibition of U251 glioma cell line proliferation and in the induction of U251 glioma cell line apoptosis. The present invention makes judgments for dcf1-induced U251 cell line apoptosis by the methods of immune electron microscope, atomic force microscope, CCK8 proliferation detection, JC-1 staining, and nude mouce tumor heterotopic transplantation. The results show that: the dcf1 causes mitochondrial structure lesion and membrane potential reduction by locating in mitochondria, thereby causing apoptosis-related gene expression change, and eventually leading to apoptosis. The nude mouce experiments show that the dcf1 can significantly reduce glioma tumor volume and inhibit tumor growth.

The invention provides an application of TMSB10 in diagnosis and treatment of glioma. Specifically, research finds that expression of TMSB10 increases with malignancy degree of glioma and is negativecorrelation with the survival rate. The TMSB10 silences and inhibits proliferation, attack and migration (MMP-9 and N-Cadherin) in U87MG and U251 cell lines, induces cell apoptosis, inhibits in-vitrocell cycles (p21, CDK4 and cyclin D1) through PI3K-AKT / ERK signal pathways (PI3K, P-AKT and p-ERK) and reduces in-vivo tumorigenicity. It indicates that the TMSB10 is an oncogene participating in occurrence and development of glioma and can be used as a biomarker and treatment target of the glioma.

The invention discloses application of a lamprey CRBGP in the preparation of a drug for resisting malignant glioma. The application finds that natural and recombinant lamprey CRBGPs are capable of effectively inhibiting processes of multiplication, adhesion, migration, infiltration and the like of U251 cells of the malignant glioma and present a dose-dependent property. Therefore, the lamprey CRBGP can be used as a sodium ion channel blocking agent in the application of the preparation of the drug for resisting the malignant glioma and has the advantages of low toxicity, high efficiency and the like.

The invention provides an epoxide sterol composition comprising epoxide sterol A and epoxide sterol B, of which the total content is greater than 95%. The epoxide sterol composition is prepared by percolation extraction, concentration and column chromatography isolation purification of a marine animal, namely green sea anemone. Experimental results show that the epoxide sterol composition (ESC) remarkably refrains the growth of rat glioma cells C6 and human glioma cells U251, induces tumor cell apoptosis or necrosis, and can be used for preparing medicines for curing brain gliomas.

The invention discloses an anti-tumor Chinese medicine extract, a preparation method and an application thereof; pulverized clematis terniflora is used or a clematis terniflora decoction piece is directly adopted, added with water or ethanol, heated, treated with reflux extraction for 2-5 times and then filtered; extract is merged, filtered or centrifugated, and then passes through macroporous resin; then water is firstly used for washing the resin, the water eluent is removed, then hydrous ethanol with the volume percentage of 30-95% is used for eluting, and the ethanol eluent is collected and concentrated into thick paste under reduced pressure, the thick paste undergoes decompressed concentration or spray drying so as to obtain the clematis terniflora extract which contains flavone and rutin no less than 20% and 0.1% respectively. The extract of the invention shows good in vitro inhibiting effect on the proliferation of leukemia Molt-4 cell strain, leukemia cell HL60, cerebral cancer U251 cell strain, esophagus cancer Eca-109 cell strain as well as liver cancer BEL-7402 cell strain. The anti-tumor Chinese medicine extract can be used for preparing the medicines for treating tumor, especially digestive system malignant tumor and the like diseases.

The invention discloses a model in vitro which can simulate the metastasis of human neuroglioma dynamically. The construction steps comprise the construction of an anti-cell adherence model by using human neuroglioma cell line U251; the construction of in vitro metastasis model of human neuroglioma cell and the identification for the constructed metastasis model in vitro of human neuroglioma. The model of the invention can be used for the control research between the in situ cancer and the tumor in metastasis; the invention can further be used as a monitoring system for the biological behavior detection of the tumor cell in metastasis and the judgment of tumor prognosis. The model has important value for the research of neuroglioma metastasis mechanism and the screening for metastasis control drugs. The model can also be used as the screening technology platform for the preparation of anti-neuroglioma transgenic vaccine and the construction of anti-tumor metastasis drugs.

The invention relates to the medical field of genes and especially relates to circSPECC1 for brain glioma treatment and a usage thereof. The invention provides the usage of the circSPECC1 for brain glioma treatment in preparation of medicines for brain glioma treatment. The beneficial effects are as follows: the circSPECC1 can realize targeted regulation of expression of genes HIP1 and Caspase 9 through interactions with miR-615 and can play an important role in invasion and proliferation of gliomas, and capabilities of proliferation and invasion of a glioma U251 cell can be effectively suppressed through suppression of the circSPECC1 as found in the project based on a YB-1 gene of a glioma U251 cell. Implementation of the project is of decisive significance to filling up vacancy in gliomabiological treatment and perfecting current glioma comprehensive treatment measures and is also of profound significance to prevention and control of tumors in other tissues and organs.

The invention discloses a research method of a Crosstalk mechanism of VEGF-CXCL8-Akt and application thereof. The research method comprises the following steps of firstly, detecting the influence of U87MG, U251 and secretion factors VEGF thereof on secretion of CXCL8 by HBMEC by using ELISA, secondly, respectively adding a specific agonist CXCL8 and an inhibitor LY294002 of a CXCL8-Akt signal pathinto a co-culture system, and detecting the influence of co-culture and activation / inhibition on expression of Akt proteins of U87MG and U251 cells and phosphorylation activation state P-Akt thereofby using Western blotting, and then using CCK-8 and Transwell invasion experiments for respectively detecting the influence of co-culture and activation / inhibition on proliferation and invasion of U87MG and U251 cells.

The invention discloses application of a curcumenol derivative in preparation of antitumor drugs. Curcumenol is an important component of traditional Chinese medicine curcuma zedoary volatile oil, andis separated from various plants at present. Researches show that curcumenol has various activities and can inhibit proliferation of various tumor cells. It is found that the curcumenol derivative 4awith the chemical structure shown in the figure 1 has good inhibitory activity on glioma U251 cells and has the prospect of being developed into anti-glioma drugs.

The invention provides a graphene-based nanomaterial for an antitumor drug carrier and a preparation method of the graphene-based nanomaterial. The graphene-based nanomaterial is characterized in thatthrough the combination of an X-ray diffractometer, a Fourier transform infrared spectrometer, an atomic force microscope and an ultraviolet spectrophotometer test, it is found that a functionalizedgraphene oxide nanosheet has a lateral dimension less than 200nm and a thickness less than 2nm, drug is successfully supported on the graphene oxide nanosheet, a complex does not aggregate in large area in a cell culture medium and can enter a cell; through the combination of a CCK-8 method and an inverted fluorescence microscope in-vitro detection test, it is shown that a complex solution has a stronger anti-human glioma U251 cell effect. Based on the unique nanostructure and excellent physical and chemical properties and biological properties of the graphene-based nanomaterial, the graphene-based nanomaterial is a potential molecular targeted therapeutic drug.

The invention discloses cell-penetrating peptide modified enzyme-sensitive PDC type PROTAC as well as a preparation method and application thereof, and belongs to the technical field of tumor targeted therapy. The cell-penetrating peptide modified enzyme-sensitive PDC type PROTAC is obtained by modifying a target protein ligand with a cell-penetrating peptide and an enzyme-sensitive Linker (GFLG) as an antitumor drug, has the capability of releasing the PDC type PROTAC under the catalysis of cathepsin B, has small influence on the cell activity of U251 cells, U87 cells and HEK293 cells, has proliferation inhibition activity on the U251 cells and the U87 cells, and can be used for preparing an antitumor drug. The polypeptide can degrade target proteins in U251 cells and U87 cells, can induce apoptosis of the U251 cells and the U87 cells, has an influence on the cycle of the U251 cells, can be used for preparing antitumor drugs (in the aspects of targeted protein degradation and membrane permeation), has a good application prospect in preparation of drugs targeting human brain glioma cells, and can be used in another important field of PROTAC drug development.

The invention relates to the field of medicine, in particular to artemisinin derivatives containing isothiocyanate group and application thereof, namely artemisinin-isothiocyanate derivatives that mayrelease hydrogen sulfide messenger molecules in a body. Two types of derivatives are provided according to an embodiment; artemisinin and NCS (isothiocyanate) group are linked via an ether(ester) bridge chain, the multi-target glioma treatment action is given to play, and accordingly, small-molecular drugs effective to treat gliomas are acquired. The artemisinin derivatives are suitable for the preparation of anti-glioma drugs and have higher cytotoxicity for malignant gliomas U87 and U251 than dihydroartemisinin.

The invention relates to the field of marine drugs and specifically discloses a method for extracting, separating and purifying lutein from porphyra haitanensis, a research on in vitro activity of lutein to malignant glioma cells and the research on the mechanism of lutein in restraining U87 cell migration. According to the invention, the lutein is acquired in the manner of using an ultrasonic-assisted organic solvent for extracting porphyra haitanensis and combining silica-gel column chromatography with SephadexLH-20 chromatography. The acquired lutein has higher purity and is capable of obviously restraining proliferation of U87 cells and U251 cells, obviously restraining migration capacity of U87 cells, obviously boosting apoptosis of U87 cells and effectively reducing the expression ofmigration-related signaling proteins, such as p-p38, MAPK, p-ERK1 / 2 and p-MEK in U87 cells.

The invention provides a marine anti-glioma natural active substance Streptomyces naphthyridine A as well as preparation and application thereof, the marine anti-glioma natural active substance Streptomyces naphthyridine A is separated from a metabolite of streptomycete in marine sediments, the classification name of the streptomycete is Streptomyces sp.SY2111, and the preservation number is CCTCC M 2021154. The Streptomyces naphthyridine A can significantly inhibit proliferation of human glioma U87MG and U251 cells, can be used for preparing anti-glioma drugs, and provides a new drug molecule for treatment of glioma. The chemical structural formula of the Streptomyces naphthyridine A is shown in the specification.

The invention relates to a model building method and application of a G protein coupled receptor (GPCR) on a new platform, in particular to model building and application of two subtypes, namely an Atype (ETA receptor) and a B type (ETB receptor), of an endothelin receptor on different cell lines by using an unmarked cell dynamic mass reset technology. The ETA receptor model is constructed on anSH-SY5Y cell line and a PC3 cell line for endogenously expressing ETA receptors respectively, and the ETB receptor model is constructed on a U251 cell line for endogenously expressing ETB receptors. The method has the characteristics of being close to the real environment in vivo, unmarked, real-time in monitoring, high in flux and simple to operate, can screen the ETA receptor and ETB receptor ligands (including agonists and antagonists) with subtype selectivity, and can compare the results of the same compound on the two receptors in the same ratio.

The invention discloses a combined medication mode for synergistically treating human brain glioma, and belongs to the technical field of pharmacology. Through the combined use of two tumor cell inhibiting drugs, i.e. Perphenazine and temozolomide are combined to treat human brain glioma cells, a model is established to quantify a combined effect. By selecting different concentrations of a stem cell inhibitor perphenazine and a human brain glioma chemotherapeutic drug temozolomide, the proliferation of U87 cells and U251 cells is inhibited by combined administration, the combination index (CI) value obtained by model quantification after the two drugs are combined for use reaches 0.3299 + / -0.002, and a strong synergistic effect is achieved; through colony formation experiment detection, the cell clone formation rate of a drug combination group is obviously lower than that of a control group and a single drug administration group, and a novel and creative drug administration mode can provide a novel drug administration strategy for treating human brain glioma.

The present invention relates to an sgRNA sequence for targeted knockout of the IGFL3 gene and its application in enhancing the radiosensitivity of glioblastoma, belonging to the field of biotechnology. The sgRNA sequence is IGFL3-sgRNA-1 or IGFL3-sgRNA-3, and a CRISPR / Cas9 vector for targeted knockout of the IGFL3 gene is constructed using this sgRNA. The above vector was transfected into human glioblastoma cell line U251, and it was identified that the IGFL3 gene could be efficiently knocked out in this cell, and 2 U251 cell lines with knocked-out IGFL3 gene were screened. By targeted knockout of the IGFL3 gene, the radiosensitivity of human glioblastoma cell line U251 can be effectively enhanced. The present invention lays a foundation for studying the role of the IGFL3 gene in the radiosensitivity of glioblastoma, and also provides a powerful tool for developing this gene as a potential molecular target for enhancing the radiosensitivity of glioblastoma.

The invention relates to a sgRNA sequence for targeted knockout of IGFL3 gene and application of the sgRNA sequence in improvement of radiosensitivity of glioblastoma, and belongs to the technical field of biology. The sequence of the sgRNA is IGFL3-sgRNA-1 or IGFL3-sgRNA-3, and a CRISPR (clustered regularly interspaced short palindromic repeats) / Cas9 (clustered regularly interspaced short palindromic repeats) vector of which the IGFL3 gene is knocked out in a targeted manner is constructed by utilizing the sgRNA. The vector is transfected into a human glioblastoma cell U251, the IGFL3 gene can be efficiently knocked out from the cell through identification, and two strains of IGFL3 gene knocked-out U251 cell lines are obtained through screening. Through targeted knockout of the IGFL3 gene, the radiosensitivity of the human glioblastoma cell U251 can be effectively improved, a foundation is laid for researching the effect of the IGFL3 gene in the radiosensitivity of the glioblastoma, and a powerful tool is provided for developing the gene as a potential molecular target for improving the radiosensitivity of the glioblastoma.

The invention provides a ceritinib derivative, a preparation method and application thereof and a medicine, and relates to the technical field of pharmacy. According to the invention, a boric acid derivative or a boric acid ester derivative is used for modifying a piperidine region of ceritinib, and a reversible covalent bond is formed by an empty orbit of sp2 of a boron atom and nucleophilic residues in protein, so that cytotoxicity caused by off-target and cytotoxicity to normal cells are reduced; meanwhile, the compound has broad-spectrum cytotoxicity on tumor cells. Experimental data show that when the ceritinib derivative provided by the invention is applied as a medicine, the ceritinib derivative has cytotoxicity to tumor cells such as H228 cells, MCF7 cells, HeLa cells, U251 cells, MDA-MB-231 cells and the like, and has relatively low cytotoxicity to normal LO2 cells of a human body. # imgabs0 #