51 results about "U87" patented technology

The invention provides a bionic nanocarrier for treating GBM (glioblastoma) and a preparation method of the bionic nanocarrier and belongs to the field of biomedical engineering. According to the bionic nanocarrier for treating the GBM and the preparation method of the bionic nanocarrier, Ang-RBCm-CA / siRNA comprises Ang-RBCm (Ang (Angiopep-2) polypeptide modified red blood cell membrane) and citraconic anhydride grafted polylysine and polyethylenimine-siRNA compound (CA / siRNA). Ang-RBCm-CA / siRNA can effectively carry siRNA and protect siRNA against degradation. The Ang-RBCm-CA / siRNA has prolonged blood circulation time and high blood brain barrier penetrability, can be efficiently taken in by U87MG brain glial cells over-expressed by a low-density LPR (lipoprotein receptor) and can realizerapid charge conversion in endosome / lysosome, effectively release siRNA and effectively treat in-situ U87MG GBM.

The invention provides application of sinomenine to preparation of a medicament for treating human brain glioma. As proved by experiments, the sinomenine has a function of restraining human-derived glioma U87MG and SF767 cell strains, and the function is improved along with the increase of dose and time. Moreover, the sinomenine can induce the increase of autophagosomes, increase the quantity of autophagic vesicles, prompt the expression increase of human glioma cells LC3B-II, induce autophagic death of human glioma cells, and restrain the growth of U87MG cell xenograft tumors. The sinomenine is a novel and effective glioma-resisting medicament with a great potential, and can be used for preparing a human brain glioma medicament; by adopting the sinomenine, a new way is created for medical treatment of human brain glioma, and the medical application of the sinomenine is expanded.

The invention discloses an antisense oligonucleotide used for inhibiting the expression of micro RNA-485-5p, and an application thereof. The antisense oligonucleotide comprises the sequence of 5'-GAAUUCAUCACGGCCAGCCUCU-3' which can be specifically combined with human miR-485-5p. The antisense oligonucleotide can be ribonucleotide, deoxyribonucleotide or chimera of the ribonucleotide and the deoxyribonucleotide, and can be used for modifying any nucleotide in the chain. The miR-485-5p antisense oligonucleotide can be used for effectively inhibiting the expression of miR-485-5p in a human brainglioma cell U87 as well as the growth and propagation of the human brain glioma cell U87, thus effectively treating the brain glioma and other tumours with high expression of miR-485-5p.

The invention discloses a nucleic acid aptamer specifically bound with a human epidermal growth factor receptor III-type mutant and an application of the nucleic acid aptamer. The nucleotide sequence of the nucleic acid aptamer is any one of SEQ ID NO:1, SEQ ID NO:2, SEQ ID NO:3 and SEQ ID NO:4. The nucleic acid aptamer specifically bound with the human epidermal growth factor receptor (EGFRv) III-type mutant is only specifically bound with U87-delta cell lines rather than U87 cell lines, so that the nucleic acid aptamer can be effectively applied to preparing a sensor or a kit for diagnosing tumor cells for expressing EGFRv III. Furthermore, the nucleic acid aptamer can be adopted as a medicine carrying tumor cells resistant to express EGFRv III or a carrier of siRNA (Small Interfering RNA) for entering tumor cells or tissues capable of expressing EGFRv III so as to play a role of a targeted matter, thereby having broad application prospects.

The invention provides a water-soluble monodemethoxycurcumin derivative as shown in general formula I and a pharmaceutically acceptable salt thereof. The compound has higher water solubility as well as high antitumor activity, has a function of inhibiting human gastric carcinoma cells MGC-803, human hepatocellular carcinoma cells Bel-7402, human chronic leukemia granulocytes K562 and human glioma U87 to different extents, and can be used for preparing an antitumor medicament, and the IC50 (Inhibitory Concentration 50) reaches the level of 1 [mu]M.

The invention discloses antisense oligonucleotide for suppressing the expression of micro ribonucleic acid (RNA)-150 and application thereof. The antisense oligonucleotide comprises a sequence, namely, 5'-CACUGGUACAAGGGUUGGGAGA-3', wherein the sequence can be specifically combined with human miR-150. The antisense oligonucleotide can be ribonucleotide, deoxyribonucleotide or the chimera of the ribonucleotide and the deoxyribonucleotide and can modify any nucleotide in a chain. MiR-150 antisense oligonucleotide can effectively suppress the expression of miR-150 in a human glioma cell U87, suppresses the growth and multiplication of the cell and can effectively treat brain glioma and other tumors with high miR-150 expression.

The invention provides application of a non-nucleoside reverse transcriptase inhibitor dapivirine (TMC120) to preparation of drugs used for treating glioblastoma. According to the invention, in-vitro experiments are carried out to detect cytotoxic effect of dapivirine on a human glioblastoma cell strain U87 and influence of dapivirine on the migration and invasion ability of U87, on proliferation, apoptosis and autophagy of U87 cells, on expression of epithelial-mesenchymal transition-associated proteins and on signal channels in the U87 cells, so the potential antineoplastic effect of dapivirine is preliminarily revealed; and the in-vivo anti-glioblastoma activity of dapivirine is confirmed via a nude-mouse in-vivo transplantation tumor model. Dapivirine provided by the invention can be used for development of novel anti-glioblastoma drugs.

The invention provides application of compound of any one or more of a formula I, a formula II and a formula III for the preparation of a medicament for treating brain malignant gliomas or melanoma and belongs to the technical field of tumor medicines. The compound shown in the formula I, the formula II and the formula III is a monomer ingredient in an annona squamosa total lactones extract. The invention further provides a method for preparing an annona squamosa seed extract for treating human brain malignant gliomas or melanoma and a product thereof. The compound shown in the formula I, theformula II and the formula III and the extract (including effective parts) have an efficient killing effect on the brain malignant gliomas or melanoma. Particularly, the compound shown in the formulaI has an IC 50 value of only 0.4044 nM for brain malignant gliomas U87-MG, and an IC50 value of only 0.5152 nM for melanoma SK-MEL-28, while the IC50 for most other tumors is often between 1uM and 100uM, and the difference is more than three orders of magnitude, showing a selective and efficient killing effect on brain malignant gliomas U87-MG and melanoma SK-MEL-28.

The invention discloses a new application of isojacareubin. The new application is meant that isojacareubin as an active ingredient is used in preparation of an antitumor pharmaceutical preparation. Pharmacological tests prove that, isojacareubin has an obvious inhibition effect on growth of U87 human brain glioma cell lines, BXPC-3 human pancreatic cancer cell lines, NCI-2126 human lung cancer cell lines, PANC-1 human pancreatic cancer cell lines, A549 human non small cell lung cancer cell lines, AGs human gastric cancer cell lines, A375 human melanoma cell lines, MCF-7 human breast cancer cell lines, MDA-MB-231 human breast cancer cell lines and SMMC-7721 human liver cancer cell lines, has significant antitumor activity, can be expected to be used as the active ingredient for the preparation of the antitumor pharmaceutical preparation, and has medicinal prospects.

The invention discloses a nucleic acid aptamer for specific binding with a human epidermal growth factor receptor type III variant and an application of the nucleic acid aptamer. The nucleotide sequence of the nucleic acid aptamer is as shown in any one of SEQ ID NO: 1, SEQ ID NO: 2, SEQ ID NO: 3 and SEQ ID NO: 4. The nucleic acid aptamer for specific binding with the EGFRvIII is only specifically bound with the cell line U87 delta and not bound with the cell line U87, and therefore, the nucleic acid aptamer can be effectively applied to preparing a sensor or a kit for diagnosing tumor cells in which the EGFRv III is expressed. Besides, the nucleic acid aptamer also can be used as a carrier carrying a drug for resisting the tumor cells in which the EGFRv III is expressed or carrying siRNA to go into the tumor cells or tissue in which the EGFRv III is expressed; the nucleic acid aptamer for specific binding with the EGFRv III has a targeting effect and wide application prospect.

The invention belongs to the field of traditional Chinese medicine preparations, relates to a novel use of juglone having a structure shown in a formula (I) in pharmacy, and particularly relates to a use of the juglone in preparation of medicines treating brain tumor. In-vitro U87 spongioblastoma cell line killing tests and animal tests on a spongioblastoma model are performed. Results of the tests show that: the IC50 of the juglone in the killing tests is 6 [mu]g / mL; in the animal tests, the lifetime of a juglone group is longer than that of a contrast group; and by systematic antitumor medicine evaluation, the results prove that the juglone has significant inhibiting functions for the spongioblastoma in vitro and in vivo, and can be used for preparation of chemotherapeutics for treating the brain tumor especially the spongioblastoma. The formula (I) is shown in the specification.

The invention provides a triterpenoid saponins compound, the molecular formula of which is C52H84O20 and the chemical name of which is 3b-O-[b-D-xylopyranose-(1-3)-a-L-rhamnopyranosyl-(1-2)-[b-D-glucopyranesyl-(1-4)]-a-L-arabopyranose] oleanolic acid (3b-O-[b-D-xylopyranosyl-(1-3)-a-L-rhamnopyranosyl-(1-2)-[b-D-glucopyranosyl-(1-4)]-a-L-arabinopyranosyl]oleanolicacid). An in-vitro antitumor test proves that the triterpenoid saponins compound has obvious inhibitory action on C6 rat spongioblastoma cell and four spongioblastoma cells: U87MG, U251MG, BT325 and SHG44, but has no influence on the growth of primarily cultured human neurogliocyte. The triterpenoid saponins compound can be used for preparing medicaments for treating glioma.

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 provides a target cell U87MG-EGRL for evaluating a targeting EGFRvIII antigen and a construction method and application of the target cell U87MG-EGRL, and belongs to the technical fieldof cellular immunity. The target cell U87MG-EGRL is a glioma cell which can express fusion protein genes of CAR-T cell target antigen EGFRvIII genes, GFP and Red Luciferase. The target cell can efficiently express the EGFRvIII antigen, both GFP genes and luciferase genes are expressed, and the killing effect of CAR-T cells can be evaluated by the luciferase reaction, therefore, the target cell canbe applied to the pharmacodynamic evaluation of CAR-T in vivo and in vitro.

The invention provides an adeno-associated virus mutant suitable for specific infection of U87-MG cells. According to the invention, the AAV serotype mutant capable of efficiently and specifically infecting U87-MG is obtained through library screening by utilizing a peptide fragment mutation library of AAV 2 / 2. An in-vitro killing experiment proves that the AAV serotype mutant obtained by screening can specifically infect and kill U87-MG cells, and has wide application in the aspects of in-vitro research on the occurrence and development mechanism of glioma and development of glioma treatment drugs.

The invention illuminates the inhibition effect and mechanism of celastrol on glioma vasculogenic mimicry for the first time. Observation by PAS-CD31 double-staining method indicates that celastrol can inhibit the formation of nude mouse tumor tissue VM (vasculogenic mimicry) and also can lower the expression of naked mouse glioma mimicry related proteins EphA2 and VE-cadherin, and in-vitro experiments verify that celastrol can inhibit the formation of U87 and U251 glioma cell VM through a PI3K / AKT / mTOR pathway.

The invention provides an application of a flavonoid derivative GL-V9 in preparation of anti-glioma drugs. Further research finds that GL-V9 can significantly inhibit the growth activity of glioma cells, can significantly promote early and late apoptosis of glioma U87 cells, and has application prospects in development of anti-glioma drugs.

The invention discloses a 3,5-disubsitutued 2-amino-pyrazine compound. The compound has the structure shown in the formula I; in the formula I, NR1R2 is n-propylamino, cyclopropylamino, cyclopentylamino, cyclohexylamino, morpholinyl, 4-methyl piperazine, anilino, 4-chloroaniline or 3-chloroaniline; Ar is 3,5-dimethyl-isoxazolyl-4 or 1-methyl-1H-pyrazolyl-4; and the invention further provides the preparation technology and application thereof. The compound has the outstanding inhibiting effect on growth of four kinds of cancer cells including a human cervical cancer cell HeLa, a human brain glioma cell U87, a human hepatoma cancer cell HepG2 and a human colon cancer cell LoVo, wherein a large part of the compound has an obviously higher inhibiting effect on proliferation of the cancer cellsthan positive control VX-680, particularly the compound Ih and Ii have relatively high activity on the four kinds of cancer cells, and have prominent activity inhibiting effect on aurora kinase A andaurora kinase B, and therefore the compound can be applied to preparation of anti-cancer drugs.

The invention discloses a technetium-99m labeled FAPI derivative containing D-proline glycine polypeptide modification and a preparation method and application of the technetium-99m labeled FAPI derivative containing D-proline glycine polypeptide modification, wherein the structural general formula of the technetium-99m labeled FAPI derivative is 99mTc (HYNIC-PGn-FAPI) (Tricine / TPPTS). The < 99m > Tc (HYNIC-PGn-FAP) (trickine / TPPTS) complex is prepared by the following two steps: synthesis of a ligand HYNIC-PGn-FAPI and preparation of the < 99m > Tc (HYNIC-PGn-FAP) (trickine / TPPTS), and the < 99m > Tc (HYNIC-PGn-FAP) (trickine / TPPTS) complex is obtained. The complex is simple and convenient to prepare, high in radiochemical purity and good in stability, has very high uptake and target-to-non-target ratio at the tumor site of a U87MG tumor-bearing mouse, has specific binding with FAP in tumors, and is a novel tumor radiopharmaceutical with clinical application value.

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 invention provides a triterpenoid saponins compound, the molecular formula of which is C52H84O20 and the chemical name of which is 3b-O-[b-D-xylopyranose-(1-3)-a-L-rhamnopyranosyl-(1-2)-[b-D-glucopyranesyl-(1-4)]-a-L-arabopyranose] oleanolic acid (3b-O-[b-D-xylopyranosyl-(1-3)-a-L-rhamnopyranosyl-(1-2)-[b-D-glucopyranosyl-(1-4)]-a-L-arabinopyranosyl]oleanolicacid). An in-vitro antitumor test proves that the triterpenoid saponins compound has obvious inhibitory action on C6 rat spongioblastoma cell and four spongioblastoma cells: U87MG, U251MG, BT325 and SHG44, but has no influence on the growth of primarily cultured human neurogliocyte. The triterpenoid saponins compound can be used for preparing medicaments for treating glioma.

The invention discloses an application of low-temperature plasma combined with metformin, in particular the application of low-temperature plasma combined with metformin to non-therapeutically induce glioma cell death in vitro. The application of the combination of low-temperature plasma and metformin in in vitro non-therapeutic induction of glioma cell death provided by the present invention shows that the combination of low-temperature plasma and metformin has obvious effects on glioma cell lines U251 and U87 cells cultured in vitro Synergistic inhibitory effect, can significantly induce cell death. The present invention is used for non-disease treatment, but for in vitro research. The scheme of the application of the combination of metformin and low-temperature plasma in inducing the death of glioma provided by the present invention can be used to study the combination of low-temperature plasma and metformin in glioma. It provides a new strategy for the application of glioma treatment, in order to provide new ideas for the design of new products or new programs for the treatment of glioma.

The invention provides a bionic nanocarrier for treating GBM (glioblastoma) and a preparation method of the bionic nanocarrier and belongs to the field of biomedical engineering. According to the bionic nanocarrier for treating the GBM and the preparation method of the bionic nanocarrier, Ang-RBCm-CA / siRNA comprises Ang-RBCm (Ang (Angiopep-2) polypeptide modified red blood cell membrane) and citraconic anhydride grafted polylysine and polyethylenimine-siRNA compound (CA / siRNA). Ang-RBCm-CA / siRNA can effectively carry siRNA and protect siRNA against degradation. The Ang-RBCm-CA / siRNA has prolonged blood circulation time and high blood brain barrier penetrability, can be efficiently taken in by U87MG brain glial cells over-expressed by a low-density LPR (lipoprotein receptor) and can realizerapid charge conversion in endosome / lysosome, effectively release siRNA and effectively treat in-situ U87MG GBM.

The present invention provides an adeno-associated virus recombinant vector for knocking out the CXCL12 gene, the recombinant vector at least includes the following sequence elements operably linked: 5' terminal inverted repeat sequence, CMV promoter, sacas9 sequence, polyA signal sequence, U6 promoter sequence, gRNA sequence, 3'-end inverted repeat sequence. The inventors found that the CXCL12 gene knockout vector can effectively inhibit the growth of transplanted tumors and tumor angiogenesis in the U87 cell glioma model, and can effectively inhibit the tumor growth and tumor angiogenesis in the U87 cell subcutaneous glioma model in nude mice. It shows that the technical scheme of the present invention can be applied to the treatment of glioma diseases.

The invention relates to application of CH223191 in inhibition of cell migration, in particular to application of CH223191 or a pharmaceutical composition containing the CH223191 in preparation of a medicine for inhibiting glioma cell migration. It is found for the first time that the CH223191 with a specific concentration can inhibit migration of a glioblastoma cell line U87, and a new choice is provided for treatment of glioblastoma.

The invention discloses application of amentoflavone in preparation of a drug for treating glioma. The amentoflavone is used for influencing activation of a JAK2STAT3 pathway of glioblastoma and apoptosis and proliferation of tumor cells. The method comprises the following steps: treating glioblastoma cell lines U87MG 24, 48 and 72 hours by using 0 [mu]M, 50 [mu]M, 100 [mu]M, 150 [mu]M and 200 [mu]M amentoflavone, then respectively detecting the influence of the glioblastoma cell lines on cell proliferation and apoptosis by using CCK8 and Annexin V / PI staining, and detecting the influence of the glioblstoma cell lines on cell JAK2-STAT3 pathway activation and the apoptosis related protein of the downstream regulation by using Western blotting. The amentoflavone is used for blocking a JAK2-STAT3 signal path, promoting tumor cell apoptosis and inhibiting proliferation of tumor cells, and is a novel method for glioblastoma treatment or adjuvant therapy.

The invention discloses application of combination of a low-temperature plasma and metformin, in particular to application of the combination of the low-temperature plasma and metformin to in-vitro non-therapeutic induction of glioma cell death. The application of the combination of the low-temperature plasma and the metformin to in-vitro non-therapeutic induction of glioma cell death shows that the combination of the low-temperature plasma and the metformin has an obvious synergistic inhibition effect on glioma cell lines U251 and U87 cultured in vitro, and can remarkably induce cell death. The application is used for non-disease treatment, but for in vitro studies, through the scheme of the application of the combination of the metformin and the low-temperature plasma to inducing gliomadeath, a new strategy can be provided for researching the application of the combination of the low-temperature plasma and the metformin to glioma treatment, and a new thought is expected to be provided for designing a new product or a new scheme for treating glioma.

The invention discloses a novel spxiterpenoid saponin type compound extracted from Ardisia pusilla and the application thereof in treating glioma. A chemical structure of the compound is determined by adopting such spectroscopic technologies as high-resolution mass spectrum and two-dimensional nuclear magnetic resonance spectroscopy and the like as well as a chemical method. An in vitro anti-tumor experiment shows that the compound has remarkable effect on inhibiting four human malignant glioma cells comprising U87MG, U251MG, BT325 and SHG44 without affecting the growth of the primary cultured human neuroglial cells. The novel spxiterpenoid saponin type compound is expected to be a drug for curing glioma.