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Application of GL-V9 in preparation of anti-glioma drugs

A technology for GL-V9 and glioma, applied in the field of anti-tumor drugs, can solve problems such as easy recurrence, poor prognosis, and fast growth, and achieve the effect of promoting early and late apoptosis

Inactive Publication Date: 2021-08-13
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0003] The World Health Organization (WHO) divides brain gliomas into four grades, more than half of which are the most malignant glioblastoma multiforme (GBM). GBM is locally heterogeneous and highly invasive, with fast growth. It makes complete surgical resection difficult, easy to relapse, and easy to develop drug resistance
And due to the existence of the blood-brain barrier, most drugs cannot directly reach the tumor site. At present, because the structure of the blood-brain barrier is not very clear, especially the mechanism of diversion is not clear, so not all drugs can pass through the blood-brain barrier. Difficult treatment and poor prognosis for malignant glioma
[0004] Temozolomide is an alkylating agent and is currently the first-line chemotherapy drug commonly used in clinical treatment of glioma. It has good central nervous system permeability and biological availability when taken orally. However, according to the current evidence of circulatory medicine, its The clinical effect is poor. Using the current standard temozolomide adjuvant chemotherapy, the 5-year survival rate of newly diagnosed GBM is only 9.8%, and drug resistance and systemic side effects are more likely to occur, and the vast majority of patients are still difficult to avoid tumor recurrence

Method used

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  • Application of GL-V9 in preparation of anti-glioma drugs
  • Application of GL-V9 in preparation of anti-glioma drugs
  • Application of GL-V9 in preparation of anti-glioma drugs

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] Embodiment 1 MTT experiment

[0044] MTT solution can be reduced to blue-purple crystalline formazan by mitochondrial dehydrogenase in living cells, DMSO can dissolve formazan, and the color of the formed solution is proportional to the cell viability, so the cell viability can be detected. Cells were cultured in a 96-well ELISA plate according to the appropriate cell density, and the volume of cells in each well was 100 μl, and 100 μl of GL-V9 at a specified concentration was added to it at the same time; the cells given the drug were continued to be cultured in the incubator for 24 hours Afterwards, 20 μl MTT solution was added to each well; the supernatant was removed after continued incubation for 4 h, and 100 μl DMSO was added to each well, placed in a micro-oscillator to vibrate, and after the crystals were completely dissolved, the absorbance was detected with a wavelength of 570 nm. After sorting out the detected absorbance values, calculate the growth inhibitio...

Embodiment 2

[0047] Example 2 Annexin V / PI apoptosis double staining experiment

[0048] After the specified time of drug action, centrifuge at 2000rpm for 5min to collect the cell suspension, discard the medium, wash the cells twice with pre-cooled PBS solution, add 400μL 1×Binding Buffer to suspend the cells, and the cell density is about 1×10 6 individual / mL. Add 5 μL of Annexin V to the cell suspension of each group, mix gently and incubate at 2-8°C in the dark for 15 minutes, then add 5 μL of PI, mix gently and incubate at 2-8°C in the dark for 5 minutes. Within 1 h, it was detected by flow cytometry.

[0049] The effect of natural product derivative GL-V9 on the apoptosis of glioma cell line U87 at 24h time point was determined by flow cytometry. The results of Annexin V / PI double staining experiment showed that ( figure 2 ), GL-V9 can significantly promote early and late apoptosis of U87 cells. These results preliminarily confirmed that GL-V9 plays an anti-glioma role by induci...

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Abstract

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.

Description

technical field [0001] The invention belongs to the field of antitumor drugs, and in particular relates to the application of a compound GL-V9 in the preparation of anti-glioma drugs. Background technique [0002] Glioma is the most common primary brain tumor arising from the canceration of glial cells in the brain and spinal cord. The annual incidence is about 3-8 per 100,000 population. Glioma is caused by the interaction of innate genetic risk factors and environmental carcinogenic factors. Some known genetic diseases, such as neurofibromatosis (type I) and tuberculous sclerosis, are genetic susceptibility factors for glioma. [0003] The World Health Organization (WHO) divides brain gliomas into four grades, more than half of which are the most malignant glioblastoma multiforme (GBM). GBM is locally heterogeneous and highly invasive, with fast growth. Make complete surgical resection difficult, easy to relapse, and easy to produce drug resistance. And due to the exis...

Claims

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Application Information

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IPC IPC(8): A61K31/4025A61P35/00
CPCA61K31/4025A61P35/00
Inventor 郭青龙惠慧李慧杨林周煜新魏立彬张小博徐澍吴焘高源
Owner CHINA PHARM UNIV
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