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Low-dosage medicine composition containing EGFR (epidermal growth factor receptor) tyrosine kinase and application thereof in preparation of anti-tumor transfer medicines

An anti-tumor metastasis and composition technology, applied in the direction of drug combinations, anti-tumor drugs, medical preparations containing active ingredients, etc., can solve the problem of failure to improve the five-year overall survival of patients with non-small cell lung cancer, and the occurrence of gefitinib Drug resistance and other issues

Active Publication Date: 2016-09-28
FUZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Gefitinib is a poorly soluble drug, and its solubility in aqueous solution is pH-dependent, that is, the lower the pH, the greater the solubility in aqueous solution, and it is almost insoluble in water with a pH value of about 7; Patients with mutations have a certain therapeutic effect, but patients generally relapse or metastasize within 1-2 years, or develop new mutations that are resistant to gefitinib, so even if gefitinib (casein amino acid kinase inhibitor) treatment still does not improve five-year overall survival in patients with non-small cell lung cancer

Method used

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  • Low-dosage medicine composition containing EGFR (epidermal growth factor receptor) tyrosine kinase and application thereof in preparation of anti-tumor transfer medicines
  • Low-dosage medicine composition containing EGFR (epidermal growth factor receptor) tyrosine kinase and application thereof in preparation of anti-tumor transfer medicines
  • Low-dosage medicine composition containing EGFR (epidermal growth factor receptor) tyrosine kinase and application thereof in preparation of anti-tumor transfer medicines

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Inhibitory effects of ursolic acid and gefitinib alone and in combination for 24 hours on the proliferation of different lung cancer cell lines: The standard MTT colorimetric method was used to measure the effect of different combination ratios of ursolic acid and gefitinib on different lung cancer cell lines Proliferation inhibitory activity, results such as Figure 1-3 shown.

[0023] Such as Figure 1-3 As shown, when ursolic acid (10 μM) and gefitinib (1-5 μM) were administered in combination at a low concentration range for 24 hours, it had no significant inhibitory effect on cancer cell proliferation and had little toxic side effects on normal cells. Therefore, in the follow-up, we chose to combine ursolic acid with a safe and effective low-dose concentration (no obvious cell killing effect) and gefitinib, and continue to study its ability to inhibit the invasion and metastasis of lung cancer cells, so as to explore its role in anti-tumor metastasis. field appli...

Embodiment 2

[0025] Effects of ursolic acid and gefitinib alone and in combination on the invasion ability of A549 cell line

[0026] A549 cells were first added with serum-free phenol red-free medium and starved overnight, and the cells collected by digestion and centrifugation were suspended in blank medium containing different drug concentrations. Take a 12-well plate and add 500 μL of cell suspension containing different drug concentrations (about 5×10 5 / well), add 500 μl culture medium containing 10% calf serum to the lower chamber, and let the drug act for 24 h, take out the small chamber, fix with 4% paraformaldehyde for 20 min, wipe off the unmigrated cells in the upper layer with a cotton swab, wash with PBS 3 times, stained with 0.1% crystal violet for 40 minutes, washed 3 times with PBS, removed the bottom membrane of the small chamber, sealed and preserved, took pictures under an inverted microscope at random 5 fields of view, counted the number of migrated cells, and the resu...

Embodiment 3

[0029] Ursolic acid and gefitinib are used alone and in combination to inhibit the invasion ability of H1975 cell line, the steps are the same as in Example 2, and the results are as follows Figure 6 shown.

[0030] Experimental results such as Figure 6 The indicated ursolic acid and gefitinib were used alone or in combination for 24 h to detect the inhibition rate of the invasion ability of H1975 cell line. The results showed that the blank control group, UA (under 10 μM condition) and gefitinib (5 μM condition) group used alone, about 70-80% of H1975 cells invaded and penetrated the chamber, when the two were administered together, only about 35% of the H1975 invaded and penetrated the chamber, the combination of the two Significantly reduced the invasion ability of H1975 cells.

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Abstract

The invention relates to a low-dosage medicine composition containing EGFR (epidermal growth factor receptor) tyrosine kinase and an application thereof in preparation of anti-tumor transfer medicines. The low-dosage medicine composition with anti-tumor transfer function is characterized by comprising ursolic acid and gefitinib according to the weight ratio of 10:(1-5). The low-dosage medicine composition has the advantage that after the gefitinib with targeting function is jointly used together with the anti-tumor natural product of ursolic acid with high efficiency and low toxicity, the good anti-tumor transfer function on cancer cells is realized, and a safe and reliable novel candidate medicine is obtained.

Description

technical field [0001] The invention belongs to the field of anti-tumor metastasis drugs, in particular, the invention relates to a low-dose pharmaceutical composition for anti-tumor metastasis. Background technique [0002] Ursolic acid is 3β-hydroxy-ursolic-12-en-28-acid (3β-hydroxy-urs-12-en-28-oic acid, referred to as UA), also known as ursolic acid, which belongs to a-amyresinol (a-amyrin) type pentacyclic triterpenoids with a relative molecular weight of 456.68 and a molecular formula of C 30 h 48 o 3 , the structure shown in formula I is a natural active compound widely distributed in nature, mainly in the form of free or glycosides, and it is widely distributed in various natural plants such as loquat leaves, bearberries, hawthorns, and Hedyotis diffusa. One of the main active ingredients of many traditional Chinese medicines, it has a wide range of pharmacological effects, such as anti-cancer, liver protection, anti-inflammation, anti-virus, anti-oxidation, etc. ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/5377A61K31/56A61P35/04
CPCA61K31/5377A61K31/56A61K2300/00
Inventor 邵敬伟郑桂容
Owner FUZHOU UNIV
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