Application of nicergoline and derivative thereof in preparation of medicine for treating tumors

A kind of nicergoline, the application technology, applied in the field of the preparation of nicergoline and its derivatives to treat tumor drugs, can solve the problem of limited treatment options, no obvious improvement in patient survival rate, etc.

Pending Publication Date: 2022-05-17
SHANGHAI HI TECH BIOENG +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Because of limited treatment options, the survival rate of patients has not improved significantly in recent years, and the five-year survival rate of LUSC patients is only 15%. There is an urgent need to develop new drugs for squamous cell carcinoma of the lung to improve the clinical efficacy of LUSC patients

Method used

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  • Application of nicergoline and derivative thereof in preparation of medicine for treating tumors
  • Application of nicergoline and derivative thereof in preparation of medicine for treating tumors
  • Application of nicergoline and derivative thereof in preparation of medicine for treating tumors

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] Survival analysis of squamous cell carcinoma of the lung

[0044] The clinical information data and sample sequencing data of TCGA lung squamous cell carcinoma cases were downloaded, and the cases with incomplete survival data were deleted to obtain the sequencing data of 490 lung squamous cell carcinoma cases, each sample containing 20530 gene expression data. Survival analysis was performed on these 20,530 genes in batches, and it was found that 180 genes were associated with longer survival (P<0.01), including 149 up-regulated genes and 31 down-regulated genes. Table 1 and Table 2 list the top 50 up-regulated genes and 31 down-regulated genes, respectively.

[0045] Table 1 List of top 50 up-regulated genes

[0046]

[0047]

[0048] Table 2 List of 31 down-regulated genes

[0049]

Embodiment 2

[0051] Drug repositioning calculation for lung squamous cell carcinoma

[0052] The gene profile obtained from the survival analysis (149 up-regulated, 31 down-regulated) was used for drug repositioning calculation based on the profile, and the top 20 candidate drugs in the calculation results are shown in Table 3. The top 20 candidate drugs include 6 tumor treatment drugs used or in research, which illustrate the feasibility of the calculation method of the present invention as a positive reference. The drug repositioning calculation method is a reference (Wu H, Huang J, Zhong Y, et al.DrugSig: Aresource for computational drug repositioning utilizing gene expression signatures[J].Plos One,2017,12(5):e0177743.)

[0053] Table 3 The top 20 drug candidates for profile repositioning

[0054]

[0055]

[0056] in,

[0057] The 18 genes targeted by Nicergoline are NTRK3, PRKCDBP, PCDHA2, PDE1B, PDZK1IP1, TIMP3, JPH2, NAV3, KIAA0408, CD14, DPP4, RNASE1, PTGIR, GLP1R, CRTAC1,...

Embodiment 3

[0078] Repositioning Drug Screening Experiments

[0079] Cell culture:

[0080] NCI-H1650, A549, NCI-H1703 were cultured in RPMI-1640 medium containing 10% fetal bovine serum, SK-MES-1 were cultured in MEM medium containing 10% fetal bovine serum, all of the above media were supplemented with penicillin -Streptomycin double antibody, the final concentration of penicillin 100IU / mL, streptomycin 100μg / mL. Cell culture at 37 °C, 5% CO 2When the cells reached 80% confluence, 0.25% trypsin was added for digestion and passage.

[0081] Add PBS (1-2mL) to the cells to be tested in the culture dish, then add medium (1-2mL) containing trypsin and EDTA to digest for about 2-5min, add medium to neutralize, transfer to a 10mL centrifuge tube and constant volume to 10mL, mix the cells at the same time, take 10uL for cell counting, and centrifuge the rest (1000rpm, 5min) to prepare a concentration of 5×10 4 cell suspension per mL, according to 10 4 Each well was inoculated in a 96-well...

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Abstract

The invention relates to the technical field of preparation of medicines for treating tumors, in particular to application of nicergoline and derivatives thereof in preparation of medicines for treating tumors. The nicergoline is used as a medicine for treating tumors and can be used for effectively treating tumors, especially lung squamous cell carcinoma, so that the lifetime of tumor patients, especially lung squamous cell carcinoma patients, is prolonged.

Description

technical field [0001] The invention relates to the technical field of preparing medicines for treating tumors, in particular to the use of nicergoline and derivatives thereof in preparing medicines for treating tumors. Background technique [0002] Lung cancer is a malignant tumor with the highest morbidity and mortality today. In 2018, there were 2.094 million new cases of lung cancer in the world and 1.761 million deaths, ranking first in the incidence and mortality of malignant tumors. Lung cancer is classified according to histopathology, mainly including non-small cell lung cancer (NSCLC) and small cell lung cancer (SCLC). Among them, NSCLC accounts for about 85% of the total number of lung cancers. In NSCLC, adenocarcinoma (Lungadenocarcinoma, LUAD) and squamous cell carcinoma (Lung squamous cell carcinoma, LUSC) are the two main types, and LUSC is the second most common subtype of lung cancer, accounting for about 30% of the total number of NSCLC. It kills about 4...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/48A61P35/00
CPCA61K31/48A61P35/00
Inventor 吴宏宇王薇张继恩黄晋江
Owner SHANGHAI HI TECH BIOENG
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