Application of urolithin compound in preparing medicine for treating glioblastoma

A glioblastoma, urolithin technology, applied in the field of urolithin compounds

Pending Publication Date: 2020-11-27
CAPITAL UNIVERSITY OF MEDICAL SCIENCES
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, less than 3%-5% of people can live beyond 5 years, and there is still a lack of effective means to treat glioblastoma

Method used

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  • Application of urolithin compound in preparing medicine for treating glioblastoma
  • Application of urolithin compound in preparing medicine for treating glioblastoma
  • Application of urolithin compound in preparing medicine for treating glioblastoma

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0013] Example 1: Preparation of compound urolithin compounds: Take 100 g of ellagitannin, add 1000 ml of water and stir at room temperature for 30 days, and centrifuge the extract. Centrifugation conditions: 15000 rpm, 10 min, to obtain urolithin Compound.

[0014] Mass spectrometry-guided preparative liquid chromatography separates urolithin compounds. The main positive ions in the positive ion mode can be obtained from the UPLC spectrum. The MSD value to be detected is input into the workstation: 930, drying gas flow rate 12 L / min, drying gas The temperature is 350°C, the atomizing gas pressure is 350 psig, and the capillary voltage is 3000 V. Equilibrium: equilibrate the preparative column with the ratio of A phase 50% and B phase 50%, and the time is about 15 minutes. The injection volume is set to 4.5 mL, and the target fraction is collected by manual sampling, and the target fraction enters the fraction collector. Dry under reduced pressure and vacuum to obtain compound ...

Embodiment 2

[0015] Example 2: Antigenic glioblastoma effect of urolithin B

[0016] After the mice were modeled with C6 cells, the T2 phase of the mouse brain was scanned with a small animal NMR scanning system on the 7th day. Most of the mice had abnormal biological production in the left caudate nucleus, and there was liquefaction inside. There is edema with clear boundaries. The NMR image was screened and 12 mice with tumors growing and similar in size were obtained. Their initial tumor size was recorded and marked. Among the 12 ICR model mice, 6 were used as the negative control group, with 0.2 mL of normal saline per day, and 6 were used as the urolithin B group. The dosage was 40 mg / kg according to the reference. The drug was administered for 14 days, and an MRI scan was performed every 7 days and the tumor size was recorded. The mice in the control group were in good condition at 0-5 days without obvious abnormal activities. After 5 days, the mice in the control group showed signif...

Embodiment 3

[0021] Example 3: Preparation of capsules

[0022] Take milligrams of the compound urolithin compound obtained in Example 1 and 280 milligrams of finely powdered silica gel, mix them and sieving, add an appropriate amount of magnesium stearate, mix well, granulate by dry granulation, sieving, and sieve 40 -The granules between 80 meshes are packed into capsules, each granule is 0.3g.

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PUM

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Abstract

The invention relates to a urolithin compound which has a structure as shown in the specification. The compound shows very strong anti-glioblastoma activity in vitro, can be matched with a medicinal carrier, and is used for preparing various medicinal dosage forms for treating anti-glioblastoma, such as capsules, granules, oral liquid or tablets.

Description

Technical field [0001] The invention relates to the field of medicine, in particular to a urolithin compound with anti-glioblastoma effect. Background technique [0002] Glioma is the most common aggressive tumor of the central nervous system. Glioblastoma (GBM), also known as glioblastoma multiforme, is a grade four glioma classified by the World Health Organization (WHO). It accounts for 15% of brain tumors and is highly malignant. Recurrent brain tumor. Glioblastoma can develop from normal cells or from existing low-grade astrogliomas. The median survival time is 14.6 months. Usually, the treatment of glioma includes surgery, chemotherapy and radiotherapy after surgery. Temozolomide is currently the first-line chemotherapy drug for the treatment of glioblastoma. However, less than 3%-5% of people can live for 5 years, and there is still a lack of effective means to treat glioblastoma. Therefore, it is particularly urgent to find new drugs for the treatment of glioblastoma....

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D311/80A61K31/37A61P35/00
CPCC07D311/80A61K31/37A61P35/00
Inventor 赵文华郭志坤王丽雪
Owner CAPITAL UNIVERSITY OF MEDICAL SCIENCES
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