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Application of dapivirine to preparation of drugs used for treating glioblastoma

A technology for glioblastoma and dapivirine, which is used in drug combinations, antitumor drugs, pharmaceutical formulations, etc.

Inactive Publication Date: 2017-09-15
NANFANG HOSPITAL OF SOUTHERN MEDICAL UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0007] So far, no relevant literature has confirmed that dapivirine has anti-glioma activity

Method used

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  • Application of dapivirine to preparation of drugs used for treating glioblastoma
  • Application of dapivirine to preparation of drugs used for treating glioblastoma
  • Application of dapivirine to preparation of drugs used for treating glioblastoma

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Embodiment 2

[0060] Embodiment 2 detects the in vivo antitumor activity of dapivirine

[0061] 6.1. Male nude mice from 4 to 6 weeks old were raised in an SPF animal laboratory for one week to adapt to the environment. U87 cells were cultured in DMEM medium (containing 10% fetal calf serum, 100 kU / L penicillin and 100 mg / L streptomycin) at 37° C., 5% CO2, and a saturated humidity incubator. Before inoculating nude mice, they were digested and passaged with 0.25% trypsin, centrifuged and mixed with PBS, and centrifuged again. Then pipette the homogeneous cells into a suspension with pre-cooled PBS, put them in an ice bath on crushed ice, and set aside. The tumor cell suspension was inoculated subcutaneously on the right back of nude mice, and the number of tumor cells inoculated in each nude mouse was about 5×10 7 , to observe the tumor formation, such as Figure 7 (A). After 2 weeks, a tumor with a diameter of 0.3 cm was formed on the right back of the nude mouse, and the drug was star...

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Abstract

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.

Description

technical field [0001] The invention belongs to the field of biomedicine and relates to the application of dapivirine in medicine for treating glioblastoma. technical background [0002] Glioblastoma (glioblastoma, GBM) is the most malignant glioma, belonging to WHO grade IV. Glioblastoma is mainly treated with surgery, radiotherapy, chemotherapy and other comprehensive treatments, and the most important treatment method is surgery. (Comprehensive genomic characterization defines human glioblastoma genes and core pathways. Nature, 2008.455(7216):p.1061-8). Drug therapy develops the fastest among the three major therapies for malignant tumors. Temozolomide (TMZ) is currently widely used in clinical glioma chemotherapeutic drugs. Although the survival period of glioma patients has been greatly changed after TMZ treatment, it is the same as other chemotherapeutic drugs. The drug resistance of TMZ severely limits the therapeutic effect and leads to tumor recurrence, which has ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/505A61P35/00
CPCA61K31/505
Inventor 刘亚伟刘蔚雯
Owner NANFANG HOSPITAL OF SOUTHERN MEDICAL UNIV
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