Application of 2-(2,2,2-trifluoroethylidene)-1,3-diketone compound in preparation of anti-lung cancer drugs

A technology of trifluoroethylene and compounds, applied in the field of medicine, can solve problems such as unclear anti-lung cancer activity

Active Publication Date: 2020-10-20
GUANGXI MEDICAL UNIVERSITY +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But at present, whether 2-(2,2,2-trifluoroethylene)-1,3-d

Method used

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  • Application of 2-(2,2,2-trifluoroethylidene)-1,3-diketone compound in preparation of anti-lung cancer drugs
  • Application of 2-(2,2,2-trifluoroethylidene)-1,3-diketone compound in preparation of anti-lung cancer drugs
  • Application of 2-(2,2,2-trifluoroethylidene)-1,3-diketone compound in preparation of anti-lung cancer drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Example 1 Screening of 2-(2,2,2-trifluoroethylene)-1,3-dione compound

[0031] Use MTT colorimetric experiment.

[0032] Measuring principle:

[0033] The succinate dehydrogenase in the mitochondria of living cells can reduce the exogenous MTT to water-insoluble blue-purple crystal formazan (Formazan) and deposit it in the cells, while dead cells have no such function. Dimethyl sulfoxide (DMSO) can dissolve the formazan in the cells, and the OD value can be detected and read by the enzyme-linked immunoassay at 490nm, which can indirectly reflect the number of living cells. Within a certain range of cell numbers, the amount of MTT crystal formation is directly proportional to the number of living cells.

[0034] test methods:

[0035] 1) In the preliminary screening stage, four lung cancer cells A549, H1299, HCC827, and PC9 were respectively inoculated into a 96-well plate, the number of cells was 3000-8000 per well, the cell suspension was 100 μL per well, and 3 multiple wells ...

Embodiment 2

[0045] Example 2 The inhibitory effect of 2-(2,2,2-trifluoroethylene)-1,3-dione compound 3e on lung cancer cells cultured in vitro was carried out by using MTT colorimetric test.

[0046] test methods:

[0047] 1) The six lung cancer cell lines A549, H1299, HCC827, PC9, H460, H1688 all use RPMI1640 medium containing 10% FBS, 1% penicillin streptomycin mixture, at 37℃, 5% CO 2 Culture in a constant temperature cell incubator. Perform cell exchange, digestion and passage, seeding, dosing and other experimental operations in a sterile ultra-clean table, and change the medium in a timely manner according to the cell proliferation speed and density.

[0048] 2) Using the MTT method to detect the anti-lung cancer activity of 2-(2,2,2-trifluoroethylene)-1,3-dione compound 3e, the six strains A549, H1299, HCC827, PC9, H460, H1688 Lung cancer cells were respectively inoculated in 96-well plates, the number of cells was 3000-8000 per well, the cell suspension was 100 μL per well, 3 multiple w...

Embodiment 3

[0056] Example 3 Molecular docking and activity verification of 2-(2,2,2-trifluoroethylene)-1,3-dione compound 3e and TrxR1 protein

[0057] Use MOE molecular docking software and DTNB experiment.

[0058] Measuring principle:

[0059] 1) Molecular docking (Molecular Docking) refers to the process of mutual recognition between ligands and receptors through energy matching and geometric matching, which mainly includes electrostatic interaction, hydrogen bonding, hydrophobic interaction force, van der Waals force and so on. In recent years, with the rapid development of computer-aided drug design technology, molecular docking technology has become one of the important methods of structure-based drug design and computer-aided drug design.

[0060] 2) DTNB is an Ellman reagent, which is used for colorimetric determination of sulfhydryl groups in biological samples. It is easily soluble in water. In the presence of sulfhydryl compounds, the colorless DTNB will be converted into yellow 5-m...

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Abstract

The invention discloses an application of a 2-(2,2,2-trifluoroethylidene)-1,3-diketone compound in preparation of anti-lung cancer drugs, and relates to an application in the field of medicines. The compound is preferably 1,3-bis(4-(tert-butyl) phenyl)-2-(2,2,2-trifluoroethylidene) propane-1,3-diketone, can inhibit the growth and proliferation of a human lung cancer cell line, is combined with a TrxR1 protein specific region of human lung cancer cells, inhibits the functional activity of the human lung cancer cells, up-regulates the ROS level of the cells, finally blocks the cycle of the humanlung cancer cells to a G1 stage or a G2/M stage, promotes apoptosis or non-apoptotic death of the human lung cancer cells, and is a potential new anti-lung cancer drug.

Description

Technical field [0001] The present invention relates to the field of medical technology, in particular to the application of 2-(2,2,2-trifluoroethylene)-1,3-dione compound in the preparation of anti-lung cancer drugs. Background technique [0002] Lung cancer is a malignant tumor with the highest incidence and mortality in the world and in my country. It is also the main cause of cancer deaths and seriously endangers human life and health. Lung cancer can be divided into two categories: one is non-small cell lung cancer (NSCLC), which accounts for about 85% of lung cancer. Non-small cell lung cancer can be divided into adenocarcinoma, squamous cell carcinoma and large cell carcinoma; One is small cell lung cancer (SCLC), which accounts for about 15% of lung cancer. At present, the treatment methods for lung cancer are mainly divided into: surgery, chemotherapy, radiotherapy, molecular targeted therapy and immunotherapy. Surgical treatment is an ideal treatment plan for early-st...

Claims

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Application Information

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IPC IPC(8): A61K31/12A61P11/00A61P35/00
CPCA61K31/12A61P11/00A61P35/00
Inventor 阳洁翁志强潘颖星莫孝成林棋吴伟黎骊莫小香
Owner GUANGXI MEDICAL UNIVERSITY
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