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Application of avasimibe in preparation of medicine for preventing or treating glioblastoma

A technology for glioblastoma and drugs, applied in drug combinations, antineoplastic drugs, active ingredients of anhydrides/acids/halides, etc.

Inactive Publication Date: 2020-05-01
INST OF MATERIA MEDICA AN INST OF THE CHINESE ACAD OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] So far, there has been no report about the anti-tumor effect of avasimibe inducing glioblastoma apoptosis through the mitochondrial pathway and non-specifically blocking the cell cycle through a p53-dependent pathway

Method used

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  • Application of avasimibe in preparation of medicine for preventing or treating glioblastoma
  • Application of avasimibe in preparation of medicine for preventing or treating glioblastoma
  • Application of avasimibe in preparation of medicine for preventing or treating glioblastoma

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] (1) Dilute avasimibe to the concentration of Table 1 with the DMEM high-glucose culture medium containing 10% fetal bovine serum, 100kU / L penicillin, and 100mg / L streptomycin respectively, and the avasimibe of different concentrations is respectively See figure 1 and Table 1.

[0041] Table 1 The cell inhibition rate of avasimibe acting on U251-MG for different time at different dosages

[0042]

[0043] It can be seen that avasimibe inhibited the proliferation of glioblastoma U251-MG in a concentration- and time-dependent manner, and the half maximal inhibitory concentration (IC 50 ) is about 20.29 μΜ.

[0044] Dilute avasimibe to the concentration shown in Table 2 with the DMEM high-sugar culture medium containing 10% fetal bovine serum, 100kU / L penicillin, and 100mg / L streptomycin respectively, and different concentrations of avasimibe act on U251 respectively Apoptotic changes of -MG cells after 48 hours see figure 2 and Table 2.

[0045] Table 2 The apopto...

Embodiment 2

[0058] (1) Dilute avasimibe to the concentration of Table 4 with the DMEM high-glucose culture medium containing 10% fetal bovine serum, 100kU / L penicillin, and 100mg / L streptomycin respectively, and the avasimibe of different concentrations is respectively See Figure 7 and Table 4.

[0059] Table 4 The cell inhibition rate of avasimibe acting on U87-MG for different time at different dosages

[0060]

[0061] It can be seen that avasimibe inhibited the proliferation of glioblastoma U87-MG in a concentration- and time-dependent manner, and the half maximal inhibitory concentration (IC 50 ) is about 28.27 μΜ.

[0062] Dilute avasimibe to the concentration shown in Table 5 with the DMEM high-sugar culture medium containing 10% fetal bovine serum, 100kU / L penicillin, and 100mg / L streptomycin, respectively, and the different concentrations of avasimibe act on U87- The apoptosis rate of MG cells after 48 hours is shown in Figure 8 and Table 5.

[0063] Table 5 The apoptos...

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Abstract

The invention relates to an anti-tumor medicine for treating glioblastoma, wherein the medicine is avasimibe. The medicine provided by the invention induces apoptosis through a mitochondrial pathway to realize the activity against the glioblastoma; the medicine provided by the invention induces the apoptosis by non-specifically blocking a cell cycle; and the medicine provided by the invention induces the cell cycle to be blocked in a G0 / G1 phase and a G2 / M phase through a p53-dependent pathway.

Description

technical field [0001] The invention relates to an antitumor drug, in particular to avasimibe and its application in the preparation of drugs for preventing or treating glioblastoma. Background technique [0002] Glioma is the most common primary intracranial tumor, accounting for about 81% of intracranial tumors. Among them, malignant glioma (glioblastoma, GBM) is the most common glioma (accounting for about 45% of all gliomas), and has the characteristics of short disease course and high mortality. Although the incidence rate of malignant glioma (4.67-5.73 / 100,000) is lower than that of most other systemic tumors, it grows rapidly and can invade important life-regulating centers around the tumor. Temozolomide (TMZ) is the most effective chemotherapy drug for malignant glioma. TMZ concurrent radiotherapy combined with adjuvant chemotherapy is the standard treatment for malignant glioma, but it can only increase the 2-year survival rate from 10.4% to 26.5%. The survival pe...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/185A61P35/00
CPCA61K31/185A61P35/00
Inventor 王金华刘金宜杜冠华庞晓丛李婉
Owner INST OF MATERIA MEDICA AN INST OF THE CHINESE ACAD OF MEDICAL SCI
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