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Application of sultan-cyclohexanone spiro derivative 1-3-51 in preparation of medicine for treating gastric cancer

A technology of cyclohexanone spiro and sulphonolactam, which is applied in the field of medicine and can solve the problems of limited clinical application and low specificity

Active Publication Date: 2021-04-30
ARMY MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At the same time, studies have shown that siomycin A can also inhibit maternal embryonic leucine zipper protein kinase (MELK), and thiostrepton can also target Peroxiredoxin 3, but their specificity in targeting FOXM1 is not high, and their clinical application is limited.

Method used

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  • Application of sultan-cyclohexanone spiro derivative 1-3-51 in preparation of medicine for treating gastric cancer
  • Application of sultan-cyclohexanone spiro derivative 1-3-51 in preparation of medicine for treating gastric cancer
  • Application of sultan-cyclohexanone spiro derivative 1-3-51 in preparation of medicine for treating gastric cancer

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033]Example 1 Preparation, detection and extraction of cells

[0034]1.1 cell culture

[0035]Human gastric cancer cells BGC823, MKN45 were cultured with DMEM high sugar medium, RPMI 1640 medium (containing 10% fetal bovine serum, 100U / ml penicillin and 10 mg / L streptomycin), cultured condition: saturated humidity, 37 ° C, 5 % CO2Culture in a constant temperature incubator. When the cells grow to 80-90%, 1: 3 is digested.

[0036]1.2 CCK8 detection cytometry

[0037]The cells were inoculated with 4000 / well on the 96-well plate, and 10 μl of CCK8 was added to each well during harvesting. After the CCK81H was added, the cell activity was determined at the optical density value at the wavelength of the enzyme gauge instrument 450 nm.

[0038]1.3 Extraction Cell Total Protein

[0039]After the treatment, the cells were discarded, washed twice with pre-cooling PBS, and the PBS was discarded, and the hydromelase inhibitor-containing Ripa (strong) lysate was added, and the cells were scratched under...

Embodiment 2

[0054]Example 2 Compound 1-3-51 inhibits FOXM1 expression in gastric cancer cells

[0055]Chemical Synthesis Method (HE XL, XIAO YC, DU W, ET Al.enantioselective Formal [3 + 3] cyclic 1-azadienes by cascade enamine-enaminecatalysis [J] .chemistry-a European Journal, 2015.doi: 10.1002 / Chem.201404550) Constructing compounds 1-3-51 chemical structureFigure 1A As shown, the semi-inhibitory concentration (IC50) of 1-3-51 promotes gastric cancer cell apoptosis is detected by CCK-8 kit (IC50), and the results showed that the IC50 of Compound 1-3-51 was shown in BGC823 and MKN45 cells. 5.429 ± 0.225μm, 5.169 ± 0.239μm (Figure 1B ). The above two gastric cancer cells were then treated with DMSO, 2.5 μM, and 5 μM 1-3-15, using Western Blot and RT-QPCR to detect compounds 1-3-51 on the expression of FOXM1 protein and mRNA in gastric cancer cells. Show compounds 1-3-51 showed concentrations of inhibitory FOXM1 protein and mRNA expression (Figure 1C ). The above gastric cancer cells 0H, 24H, 48H ...

Embodiment 3

[0056]Example 3 Compound 1-3-51 inhibits expression of FOXM1 downstream target gene Cyclin D1, MMP9 in gastric cancer cells

[0057]Dimso, 2.5 μm, 5 μm were used to treat Cyclin D1, MMP9, and RT-QPCR was used to detect the mRNA expression of Foxm1 downstream target gene Cyclin D1, MMP9, and results showed that the compound 1-3-51 was concentrated in inhibiting Cyclin D1. , MMP9 mRNA expression (Figure 2A ). The above gastric cancer cells 0H, 24H, 48H were then treated with compounds 1-3-51 5 μm, and the results showed that it also decreased inhibition of Cyclin D1, MMP9 mRNA expression (Figure 2b ).

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Abstract

The invention relates to application of a Sultan-cyclohexanone spiro derivative 1-3-51 in preparation of a medicine for treating gastric cancer, the medicine remarkably inhibits expression of FOXM1 and proliferation, invasion and migration of gastric cancer cells, and after interfering with FOXM1, the capacity of inhibiting proliferation, invasion and migration of gastric cancer cells is reduced.

Description

Technical field[0001]The present invention belongs to the field of medical technology, and in particular, the application of sulfonamide-cyclohexanone screw derivatives 1-3-51 in the preparation of the treatment of gastric cancer drugs.Background technique[0002]Gastric Cancer GC is one of the world's common digestive system malignant tumors. It has made it a major issue that has become a major issue in the world, especially human public health, and serious harms human health and waste. community resource. Currently 50% of gastric cancer is diagnosed in East Asia, most cases occur in China. The global gastric cancer morbidity has risen steadily. According to global cancer statistics in 2018, the incidence of gastric cancer ranks the fifth world in the world, and the death rate ranks third in the world. It is expected that gastric cancer will become the world. 15 major causes of death. Although the comprehensive treatment of gastric cancer in recent years has made certain progress, th...

Claims

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Application Information

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IPC IPC(8): A61K31/428A61P1/00A61P35/00
CPCA61K31/428A61P1/00A61P35/00
Inventor 欧阳勤古晶王纳高梦圆陈应春胡长江杨仕明
Owner ARMY MEDICAL UNIV
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