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Medicinal composition for resisting non-small cell lung cancer, and application thereof

A technology for non-small cell lung cancer and a composition, which is applied in the field of medical applications to achieve the effect of inhibiting the phosphorylation level and solving the problem of partial drug resistance

Inactive Publication Date: 2017-05-17
JIANGSU PROVINCE INST OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] So far, there is no report on the application of the pharmaceutical composition combined with artemisinin derivatives and EGFR-TKI in the treatment of lung cancer

Method used

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  • Medicinal composition for resisting non-small cell lung cancer, and application thereof
  • Medicinal composition for resisting non-small cell lung cancer, and application thereof
  • Medicinal composition for resisting non-small cell lung cancer, and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Example 1: Artemisinin derivatives inhibit STAT3 phosphorylation

[0032] Take PC-9 and H1975 cells and use RPMI 1640 medium containing 10% FBS, 100 U / mL penicillin and 100 μg / mL streptomycin, at 37 °C, 5% CO 2maintained in an incubator. After the cells grow to the logarithmic growth phase, they are digested with 0.25% trypsin-EDTA solution to prepare a single cell suspension, and 4×10 5 Inoculate a six-well plate at a cell density of 1 cell / well, and after culturing for 24 hours, add different concentrations of artemisinin derivatives, and select 4 concentrations around the IC50 value, specifically: 20 μM, 40 μM, 60 μM, 80 μM, DMSO as a solvent control group. After 24 hours of drug intervention, remove the supernatant, wash twice with PBS, add RIPA lysate containing protease and phosphatase inhibitors, and lyse on ice for 30 minutes. The cell lysate was collected with a cell scraper, and centrifuged at 12000 r / min for 10 min at 4°C. Take the supernatant, measure th...

Embodiment 2

[0034] Example 2: Artemisinin derivatives can inhibit EGFR-TKI-induced STAT3 phosphorylation

[0035] Take PC-9 and H1975 cells and use RPMI 1640 medium containing 10% FBS, 100U / mL penicillin and 100ug / mL streptomycin at 37°C, 5% CO 2 maintained in an incubator. After the cells grow to the logarithmic growth phase, they are digested with 0.25% trypsin-EDTA solution to prepare a single cell suspension, and 4×10 5 The cell density of each cell / well was inoculated into a six-well plate, and after culturing for 24 hours, the concentration of the IC50 value of each compound was added, specifically: DHA (40 μM), EGFR-TKI (for PC-9 cells, the concentration of Gef was 0.1 μM, and the concentration of Erl 0.1 μM, Afa concentration 0.0038 μM, Osi concentration 0.04 μM; for H1975 cells, Gef concentration 8 μM, Erl concentration 8 μM, Afa concentration 0.3 μM, Osi concentration 0.04 μM) or a combination of both, DMSO as solvent control group. After 24 hours of drug intervention, remove...

Embodiment 3

[0037] Example 3: Artemisinin derivatives and EGFR-TKI synergistically promote cell death in non-small cell lung cancer

[0038] Take PC-9 cells and use RPMI1640 medium containing 10% FBS, 100U / mL penicillin and 100ug / mL streptomycin at 37°C, 5% CO 2 maintained in an incubator. After the cells grow to the logarithmic growth phase, they are digested with 0.25% trypsin-EDTA solution to prepare a single cell suspension, with a volume of 100 μL per well, 2×10 3 A cell concentration of 100 cells was seeded in a 96-well plate. After culturing for 24 hours, different concentrations of artemisinin derivatives (dihydroartemisinin concentration gradient as follows: 5, 10, 20, 25, 30, 35, 40, 60, 80 μM; artemether concentration gradient as follows: 12.5 , 25, 50, 62.5, 70, 87.5, 100, 150, 200μM; artether concentration gradient is as follows: 12.5, 25, 50, 62.5, 70, 87.5, 100, 150, 200μM) and different concentrations of EGFR-TKI (ji The concentration gradient of nontinib is as follows:...

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Abstract

The invention discloses a medicinal composition for resisting non-small cell lung cancer. The active components of the medicinal composition comprise an artemisinin derivative and EGFR-TKI (epidermal growth factor receptor-tyrosine kinase inhibitor), wherein the artemisinin derivative is selected from one of dihydroartemisinin, artesunate, artemether and arteether; and the EGFR-TKI is selected from one of gefitinib, erlotinib, afatinib and osimertinib. The invention also discloses application of the medicinal composition to preparation of medicines for treating and resisting the non-small cell lung cancer. When the medicinal composition provided by the invention is used for treating the non-small cell lung cancer, the medicinal effect which is more excellent than that of the singly used EGFR-TKI can be achieved, the sensitizing effect is achieved, the problem of partial medicine resistance of the non-small cell lung cancer EGFR-TKI is solved, and a scientific basis is provided for the development of new medicines.

Description

technical field [0001] The invention belongs to the field of medical applications, in particular to a pharmaceutical composition for resisting non-small cell lung cancer and its application. Background technique [0002] At present, the morbidity and mortality of lung cancer in all countries in the world are increasing year by year. According to the statistics of the World Health Organization (WHO), the incidence of lung cancer ranks first among malignant tumors, which seriously threatens human health. Lung cancer can be divided into small cell lung cancer (SCLC) and non-small cell lung cancer (NSCLC) according to pathological classification, and NSCLC accounts for about 80%-90% of lung cancer. For a long time, patients with advanced NSCLC could only receive "platinum-containing chemotherapy". Compared with supportive care, although it increased the overall survival of patients to a certain extent, its upper limit was limited to 20% response rate and median survival of 8-10...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K45/06A61K31/357A61K31/5377A61K31/517A61P35/00
CPCA61K45/06A61K31/357A61K31/517A61K31/5377A61K2300/00
Inventor 曹鹏蔡雪婷杨杰
Owner JIANGSU PROVINCE INST OF TRADITIONAL CHINESE MEDICINE
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