Application of otilonium bromide to preparation of antitumor medicines

An anti-tumor drug, octilonium bromide technology, applied in anti-tumor drugs, drug combinations, pharmaceutical formulations and other directions, can solve the problems of no patent application, no report on the effect of tumor proliferation and growth, etc.

Active Publication Date: 2020-10-23
ZHENGZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, there is currently no report on the effect of this drug on inhibiting the proliferation and growth of gastrointestinal tumors such as esophageal cancer and gastric cancer, and there is no related patent application

Method used

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  • Application of otilonium bromide to preparation of antitumor medicines
  • Application of otilonium bromide to preparation of antitumor medicines
  • Application of otilonium bromide to preparation of antitumor medicines

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Example 1 In vitro experiment of otilonium bromide inhibiting the proliferation of esophageal cancer cells

[0041] Cytotoxicity test

[0042] The experimental process is: KYSE150 cells were treated with 8×10 3 cells / well were inoculated in a 96-well plate for culture (10% FBS / 1640, 37°C, 5% CO 2 ), KYSE450 cells at 1.2×10 4 Each well was inoculated in a 96-well plate for culture (10% FBS / DMEM, 37°C, 5% CO 2 ), after 14-16 hours, replace the fresh medium and add otilonium bromide (DMSO solution), so that the final concentration of otilonium bromide in the medium is 0 μM, 3.125 μM, 6.25 μM, 12.5 μM, 25 μM, 50 μM, 75 μM, 100 μM, cultured for 24 and 48 hours respectively, the cells were taken out of the incubator, the original medium was discarded, and washed twice with 1×PBS. Then discard the PBS, add 100 μL / well of 4% paraformaldehyde, fix for 30 minutes, discard the paraformaldehyde, and wash twice with 1×PBS. Then discard the PBS, stain with DAPI (DAPI stock solut...

Embodiment 2

[0047] Example 2 In vitro experiments of otilonium bromide inhibiting the ability of esophageal cancer cell colony formation

[0048] The experimental process is as follows: spread 3 mL of BME medium (containing 10% FBS and 0.5% agar) in each well of a 6-well plate, and spread suspension of esophageal cancer cells (KYSE150: 8×10 3 pcs / hole or KYSE450: 8×10 3 pcs / well) top layer gel (the top layer gel contains 1 mL BME medium, the medium contains 10% FBS and 0.33% agar, and the final concentrations of drugs in the medium are 0 μM, 2.5 μM, 5 μM, 10 μM, 20 μM), in an incubator (37°C, 5% CO 2 ) After 7-14 days of culture or according to the condition of the cells, when clones are formed, use IN Cell Analyzer 3000 to count the clones ( figure 2 For the results obtained after culturing for 10 days).

[0049] Experimental results such as figure 2 shown. from figure 2 It can be seen that the number of cell clones decreased after treatment with otilonium bromide, and the size ...

Embodiment 3

[0050] Example 3 In Vitro Experiment of Otilonium Bromide Inhibiting the Proliferation of Gastric Cancer Cells

[0051] Cytotoxicity test

[0052] The experimental process is: HGC27 cells were divided into 6×10 3 cells / well were inoculated in a 96-well plate for culture (10% FBS / 1640, 37°C, 5% CO 2 ), AGS cells in 8×10 3 Each well was inoculated in a 96-well plate for culture (10% FBS / F12k, 37°C, 5% CO 2 ), after 14-16 hours, replace the fresh medium and add otilonium bromide (DMSO solution), so that the final concentration of otilonium bromide in the medium is 0 μM, 3.125 μM, 6.25 μM, 12.5 μM, 25 μM, 50 μM, 100 μM), cultured for 24 and 48 hours respectively, the cells were taken out of the incubator, the original medium was discarded, and washed twice with 1×PBS. Then discard the PBS, add 100 μL / well of 4% paraformaldehyde, fix for 30 minutes, discard the paraformaldehyde, and wash twice with 1×PBS. Then discard the PBS, stain with DAPI (DAPI stock solution: 1×PBS=1:5000...

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Abstract

The invention discloses an application of otilonium bromide to preparation of antitumor medicines. The otilonium bromide is chemically named as N,N-diethyl-N-methyl-2-[[4[[2- (octyl ) benzoyl]amino]benzoyl] oxyl] ethanaminium bromide, CAS No. is 26095-59-0, the molecular formula is C29H43BrN2O4, and the molecular weight is 563.56. The antitumor medicines are medicines for treating esophagus canceror gastric cancer. Experiments confirm that when the otilonium bromide is used for esophageal squamous cell carcinoma cells (KYSE150 cells and KYSE450 cells) or gastric cancer cells ( HGC27 cells andAGS cells), the otilonium bromide can achieve the effects of restraining growth and transformation of the esophageal squamous cell carcinoma cells or the gastric cancer cells, and the appropriate concentration of the otilonium bromide for restraining proliferation and transformation of the esophageal squamous cell carcinoma cells or the gastric cancer cells is 2.5-20 [mu]M.

Description

technical field [0001] The invention belongs to the technical field of tumor treatment and prevention, and in particular relates to the application of otilonium bromide in the preparation of antitumor drugs. Background technique [0002] Cancer seriously threatens human health. In recent years, the incidence of cancer has continued to rise, becoming the second deadliest disease after cardiovascular and cerebrovascular diseases. Cancer treatment is one of the intractable diseases that are difficult to overcome in the current world. Not only is it difficult to cure completely, but there are also many difficulties in improving the survival period of patients. [0003] Cancer has become the first cause of death in China and is a serious public health problem. According to statistical results, esophageal cancer and gastric cancer are the most common types of cancer and the most common cause of cancer death in China. [0004] Globally, the incidence of esophageal cancer ranks e...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/245A61P35/00
CPCA61K31/245A61P35/00
Inventor 刘康栋包卓董子钢赵继敏江亚南
Owner ZHENGZHOU UNIV
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