Application of tegaserod maleate in preparation of antitumor drug

A technology of tegaserod maleate and anti-tumor drugs, which is applied in the field of tumor treatment and prevention, and can solve problems such as lack of research

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

AI Technical Summary

Problems solved by technology

[0007] Tegaserod maleate is an indole selective 5-HT 4 receptor agonist, which is suitable for the short-term treatment of patients with irritable bowel syndrome, and the relationship between tegaserod maleate and esophageal cancer There is a lack of corresponding research on the relationship between

Method used

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  • Application of tegaserod maleate in preparation of antitumor drug
  • Application of tegaserod maleate in preparation of antitumor drug
  • Application of tegaserod maleate in preparation of antitumor drug

Examples

Experimental program
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Effect test

Embodiment 1

[0026] Embodiment 1: Cytotoxicity experiment

[0027] Experimental process: KYSE 150 cells were seeded in 96-well plates at 8,000 per well and cultured with 1640 medium, KYSE450 cells were inoculated at 12,000 per well in 96-well plates and cultured with DMEM medium (37°C, 5% CO 2 ), after 16-18 hours, the final concentration of 50 mM tegaserod maleate plus DMSO solution was gradiently diluted to 0, 3.125, 6.25, 12.5, 25 mM, and the drug-containing medium was prepared according to 1:1000, so that The drug concentration of tegaserod maleate in the medium reached 0, 3.125, 6.25, 12.5, 25, 50 μM, added the above-mentioned drug-containing medium, cultured for 24 hours and 48 hours respectively, and then treated with 4% paraformaldehyde Fix the cells at 100 μL per well, then add DAPI staining solution (DAPI stock solution: 1×PBS=1:5000 dilution, Beijing Suolaibao Technology Co., Ltd.), 100 μL per well, and incubate at 37°C for at least 20 min After staining, put the 96-well plate ...

Embodiment 2

[0029] Embodiment 2: cell proliferation experiment

[0030] Experimental process: KYSE 150 cells were seeded in 96-well plates at 2000 per well and cultured with 1640 medium, KYSE450 cells were seeded at 4000 per well in 96-well plates and cultured with DMEM medium (37°C, 5% CO 2), after 16-18 hours, replace the fresh medium (KYSE 150 cells use 1640 medium; KYSE 450 cells use DMEM medium), and add different amounts of tegaserod maleate (0, 0.25, 0.5, 1, 2.5 μM is the final concentration), after culturing for 0, 24, 48, 72, and 96 hours respectively, fix the cells with 4% paraformaldehyde at 100 μL per well, and then prepare DAPI staining solution (DAPI stock solution) at 1:5000 : 1×PBS=1:5000 dilution, Beijing Soleibao Technology Co., Ltd.), 100 μL per well, incubate at 37°C for at least 20 minutes for staining, and finally put the 96-well plate into IN Cell Analyzer 3000, take pictures and count.

[0031] Experimental results such as figure 1 B, figure 2 Shown in B. It ...

Embodiment 3

[0032] Embodiment 3: soft agar colony formation experiment

[0033] Experimental process: Spread 3 ml of drug-containing medium in each well of a 6-well plate (KYSE 150 cells use 1640 medium; KYSE450 cells use DMEM medium), so that the final concentration of tegaserod maleate reaches 0, 0.25, 0.5, 1, 2.5 μM, after solidification, spread into the upper layer gel with 8000 esophageal cancer cells KYSE 150 or KYSE 450 suspended (the upper layer gel composition: 40% 2×BME; 40% Agar glue; 10% FBS; 9% Sterile water; 1% glutamine; 0.1% gentamicin), put it into the incubator (37°C, 5% CO 2 ) culture, choose an appropriate time to terminate the culture according to the colony formation, and use IN Cell Analyzer 3000 to take pictures and count and analyze.

[0034] Experimental results such as figure 1 C, figure 2 C shown. It can be found that as the concentration of tegaserod maleate increases, the number of clones gradually decreases, indicating that at low toxic concentrations, ...

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Abstract

The invention discloses application of tegaserod maleate in preparation of an antitumor drug. The drug tegaserod maleate has a CAS number of 189188-57-6, a chemical name of 2-[(-5 methoxy-1H-indole-3-group) methylene]-N-pentylcarbazide maleate, a molecular formula of C20H27N5O5, and a molecular weight of 417.46. Experiments prove that when the tegaserod maleate is used for esophageal squamous cellcarcinoma cells (KYSE150 cells and KYSE450 cells), the tegaserod maleate can play a role in inhibiting the growth of esophageal squamous cell carcinoma cells, and the suitable concentration of the tegaserod maleate in inhibiting the proliferation of esophageal squamous cell carcinoma cells and the number and size of clone formation is 0.25-2.5 micrometers.

Description

technical field [0001] The invention belongs to the technical field of tumor treatment and prevention, and in particular relates to the application of tegaserod maleate in the preparation of antitumor drugs. Background technique [0002] According to the data released by the World Health Organization, the global tumor morbidity and mortality are still rising rapidly. Specifically, the incidence rates of tumors in the total global population (collectively referring to the population of both sexes) are ranked as follows: lung cancer, breast cancer, colorectal cancer, prostate cancer, gastric cancer, liver cancer, and esophageal cancer; : Lung cancer, colorectal cancer, gastric cancer, liver cancer, breast cancer, esophageal cancer. The Asia-Pacific region accounts for 45% of new cancer patients and 50% of the world's deaths. The global tumor incidence map shows that the incidence of cancer in China is at the middle level in the world, and the case fatality rate is at the upp...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/404A61P35/00
CPCA61K31/404A61P35/00
Inventor 刘康栋董子钢武想雨赵继敏董子明江亚南张静
Owner ZHENGZHOU UNIV
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