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Antitumor medicament containing glycolysis inhibitor and preparation method and application of antitumor medicament

An anti-tumor drug and glycolysis technology, applied in the field of anti-tumor drugs, can solve the problems of tumor recurrence and metastasis, and the inability to effectively eradicate tumor stem cells

Inactive Publication Date: 2012-03-21
黄蓬 +3
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Since traditional chemotherapy drugs cannot effectively eradicate tumor stem cells, the remaining tumor stem cells in the body after chemotherapy are an important cause of tumor recurrence and metastasis

Method used

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  • Antitumor medicament containing glycolysis inhibitor and preparation method and application of antitumor medicament
  • Antitumor medicament containing glycolysis inhibitor and preparation method and application of antitumor medicament
  • Antitumor medicament containing glycolysis inhibitor and preparation method and application of antitumor medicament

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] The preparation method of propyl 3-bromopyruvate.

[0040] The Chinese name of compound 3-BOPr provided by the present invention is 3-bromopyruvate propyl ester; English name is 3-Br-2-oxopropionic propyl ester; Molecular formula C 6 o 3 h 9 Br, molecular weight 209, colorless or light yellow transparent liquid, structural formula is as follows:

[0041]

[0042] The process step of its synthetic method of 3-bromopyruvate propyl ester is: 3-bromopyruvate and 1-propanol are mixed in the flask, and the mol ratio of 3-bromopyruvate and 1-propanol is 1: 3, in Add a small amount of concentrated hydrochloric acid (HCl) into the flask as a catalyst, heat the flask to 45°C, and keep stirring for 1 hour, then cool the reaction system to 30°C, and continue stirring for 8 hours. After the reaction, the product was cooled to 0°C on ice, and solid Na 2 CO 3Make it just neutralize the residual hydrochloric acid, and evaporate the excess 1-propanol under low pressure to obtain...

Embodiment 2

[0044] The preparation method of 3-bromopentyl pyruvate.

[0045] The Chinese name of the compound 3-BOPe provided by the present invention is 3-bromopyruvate pentyl ester; the English name is: 3-Br-2-oxopropionic pentyl ester; molecular formula C 8 o 3 h 13 Br, molecular weight 237, light yellow transparent liquid, structural formula is as follows:

[0046]

[0047] The processing step of its synthetic method of 3-bromopyruvate pentyl ester is: 3-bromopyruvate and 1-pentanol are mixed in the flask, and the mol ratio of 3-bromopyruvate and 1-pentanol is 1: 3, in Add a small amount of concentrated hydrochloric acid into the flask as a catalyst, heat the flask to 50°C, and keep stirring for 1 hour, then cool the reaction system to 30°C, and continue stirring for 8 hours. After the reaction, the product was cooled to 0°C on ice, and solid Na 2 CO 3 Make it just to neutralize the residual concentrated hydrochloric acid, and evaporate the excess 1-pentanol under low pressur...

Embodiment 3

[0051] The combination of 3-bromopyruvate propyl ester and BCNU can obviously kill tumor stem cells in vitro.

[0052] The selected cell line is the human glioma stem cell GSC11 cell isolated from the tumor of a glioma patient. Tumor stem cells were taken to make a certain concentration of cell suspension and inoculated in a 6-well plate, and a certain concentration of 3-bromopyruvate propyl ester (3-BOPr 10uM, 20uM), BCNU (100uM) or a combination of both (3-BOPr) was added to each well. -Propyl bromopyruvate 10uM, 20uM+BCNU 100uM) the drug to be tested, no drug was added to the control wells, and 3 parallel wells were set for each concentration. Cultured for 24 hours, the cells were taken out and centrifuged, stained with Annexin-v and PI, and detected by flow cytometry, the results are shown in figure 1 ; The experimental results show that the combination of 10uM 3-BOPr and 100uMBCNU has a strong synergistic effect; 20uM 3-BOPr alone has a strong effect of killing tumor ste...

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Abstract

The invention provides an antitumor medicament. The antitumor medicament is a glycolysis inhibitor, and the glycolysis inhibitor is 3-bromacetone acid ester. According to the antitumor medicament, the aim of killing tumor stem cells is fulfilled by efficiently blocking the energy metabolism of the tumor stem cells. The invention further provides application of the glycolysis inhibitor to the preparation of antitumor medicaments, a preparation method of the glycolysis inhibitor and application of the glycolysis inhibitor to tumor treatment.

Description

technical field [0001] The invention relates to the technical field of anti-tumor drugs, in particular to anti-tumor drugs containing glycolysis inhibitors and the application of the glycolysis inhibitors in the preparation of anti-tumor drugs. Background technique [0002] Cancer has replaced cardiovascular disease as the disease that causes the largest number of deaths. According to the World Health Organization, the number of cancer deaths in 2004 reached 7.4 million. It is expected that the number of cancer deaths worldwide will continue to increase in the future. Chemotherapy is one of the main treatment methods for cancer. In recent decades, cancer drug treatment has made significant progress, and a variety of anti-tumor drugs have been developed, which effectively prolong the survival period of patients or improve the patient's life expectancy. Quality of Life. However, the effect of tumor drug therapy is still unsatisfactory, and the drug resistance of tumor cells i...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/22A61P35/00C07C69/716C07C67/08A61K31/17
Inventor 黄蓬徐瑞华王峰曾益新
Owner 黄蓬
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