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Application of parthenolide in preparation of lung cancer treating drug

A parthenolide, small cell lung cancer technology, applied in the directions of drug combination, antitumor drugs, pharmaceutical formulations, etc., can solve the problem of unreported pharmacological characteristics of parthenolide in the treatment of lung cancer, and achieve remarkable results, weakened ability, The effect of inhibiting metastasis

Inactive Publication Date: 2016-06-15
NANKAI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] However, the application of parthenolide in the treatment of lung cancer and its pharmacological characteristics have not been reported yet.

Method used

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  • Application of parthenolide in preparation of lung cancer treating drug
  • Application of parthenolide in preparation of lung cancer treating drug
  • Application of parthenolide in preparation of lung cancer treating drug

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Example 1 Detection of the inhibitory effect of parthenolide on the proliferation of lung cancer cell lines NCI-H446, NCI-H460 and A549

[0040] Experiment method: MTT colorimetric method

[0041] The specific experimental steps are as follows: the cells were seeded on a 96-well culture plate (5×103 cells / well), placed at 37°C, CO 2(5%) overnight in the incubator. On the second day, discard the culture medium, add parthenolide cell culture medium with concentrations of 0, 4, and 8 μM parthenolide respectively, and set control wells without adding drugs. Placed at 37°C, CO 2 (5%) After culturing in an incubator for 48 hours, add 20 μL tetramethylazozolate (MTT) mother solution (mother solution concentration: 5 mg / mL) to each well and continue to incubate for 4 hours. Then the culture solution was sucked out, and 150 μ L DMSO was added to each hole as a solvent to dissolve formazan. After dissolving, the absorbance at 490 nm was measured with a microplate reader, and t...

Embodiment 2

[0044] Example 2 In vitro detection of the effect of parthenolide on the migration ability of lung cancer cell lines NCI-H446, NCI-H460 and A549 at the cell level

[0045] Experimental method: cell scratch method

[0046] The specific experimental steps are: inoculate the cells in a 35mm petri dish and culture the monolayer cells to 100%, use the tip of a sterile pipette tip to make a 100μm scratch blank area, discard the liquid, wash twice with 1×PBS, and add the concentration of 0 , 4, 8μM parthenolide cell culture medium, and set control wells without drugs, placed at 37 ° C, CO 2 (5%) Cultured in an incubator for 24 hours, at 0 hours, 12 hours and 24 hours, placed on an optical microscope at a fixed position to take samples, took pictures, and recorded the changes in the distance between cells at both ends of the scratch.

[0047] Relative starting position ratio (Ratioto0h)=S xh / S 0h ; Use Excel software to draw the cell migration distance-time curve, and each index i...

Embodiment 3

[0050] Example 3 Effects of parthenolide on the expression levels of EMT-related marker molecules in three cell lines

[0051] The expression of EMT-related marker molecules included: epithelial marker molecules Occludin, claudin3 and EMA, mesenchymal marker molecules N-cadherinCD34 and VEGFR1, Vimentin.

[0052] Experimental method: Immunofluorescence staining

[0053] The specific experimental steps are as follows: the cells were seeded on a 96-well culture plate (8×10 3 cells / well), placed at 37°C, CO 2 (5%) overnight in the incubator. The next day, discard the culture medium, add parthenolide cell culture medium with a concentration of 0, 4, and 8 μM respectively, and set up control wells without adding drugs, place them in an incubator for 24 hours, wash 4 times with 1×PBS, 10% formaldehyde (prepared in 1×PBS) was fixed at room temperature for 20-30min, washed twice with 1×PBS, permeabilized by adding 0.1% NP-40 (prepared in 1×PBS) for 2-5min, 3% BSA (prepared in 1×PBS...

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Abstract

The invention discloses an application of parthenolide in preparation of a lung cancer treating drug. EMT (epithelial-mesenchymal transition) of lung cancer cells is reversed through parthenolide, so that growth, invasion or metastasis of the lung cancer cells is inhibited. Embodiments of the invention comprise experimental study including an MTT test, Transwell, a scratch test, immunofluorescence and the like on cells and animals, and results show that parthenolide can reverse EMT of the lung cancer cells, so that parthenolide inhibits invasion and metastasis of the lung cancer cells of small cell lung cancer and non-small cell lung cancer and can have a remarkable effect on tumor cancer treatment.

Description

technical field [0001] The invention belongs to the field of medicinal chemistry, and in particular relates to the application of parthenolide in the preparation of drugs for treating lung cancer. Background technique [0002] Lung cancer is the most common in the world, and it is one of the malignant tumors with the fastest increasing morbidity and mortality, and the greatest threat to the health and life of the population. In recent years, the morbidity and mortality of lung cancer have increased significantly. The reason is generally believed to be due to its high local recurrence rate and high distant metastasis rate, and its malignancy is largely due to its High metastasis rate, but currently there are few drugs that can inhibit tumor metastasis clinically, and it is accompanied by problems such as poor prognosis, so it is urgent to develop new therapeutic drugs. [0003] Parthenolide is a sesquiterpene lactone compound purified from tansy. Molecular formula: C 15 h ...

Claims

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Application Information

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IPC IPC(8): A61K31/365A61P35/00A61P35/04A61P11/00
CPCA61K31/365
Inventor 杨诚孙涛周红刚刘慧娟刘艳荣陈双秦源仲威龙王玮赵冬谷文光竞香艳孟晶荆学双胡雪姣
Owner NANKAI UNIV
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