Application of cephalosporin antibiotics as anticancer medicines and anticancer medicines

A technology of anti-cancer drugs and antibiotics, which can be used in the field of drug research to solve problems such as sensitization of cancer patients

Active Publication Date: 2019-10-15
KUNMING MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0016] "Auxiliary anti-cancer health products" refer to health products used for the adjuvant treatment of cancer patients during the...

Method used

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  • Application of cephalosporin antibiotics as anticancer medicines and anticancer medicines
  • Application of cephalosporin antibiotics as anticancer medicines and anticancer medicines
  • Application of cephalosporin antibiotics as anticancer medicines and anticancer medicines

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0061] Example 1: Cephalosporin antibiotics (except ceftriaxone) have significant and cell-targeted anticancer effects in vitro.

[0062] In vitro anticancer test method: cephalosporin antibiotics were dissolved in sterile normal saline, and the in vitro anticancer test was carried out according to the final concentration of 25, 50, 100, 200, 400 μg / ml. Human cancer cells in the logarithmic growth phase were collected, suspended in DMEM / F12 complete culture medium without antibiotics supplemented with 10% fetal bovine serum (FBS), and inoculated on a 96-well plate, and 100 µl of cell suspension was added to each well (except for MCF-7 Inoculate 1×10 per well 4 1 cells, the rest of the cancer cell lines were inoculated with 5×10 cells per well. 3 cells). 37°C, 5% CO 2 After culturing overnight in the incubator, suck out the culture medium, and then add 200 μl of culture medium containing corresponding concentrations of cephalosporin antibiotics according to the design (the c...

Embodiment 2

[0066] Example 2: Cephalosporin antibiotics (except ceftriaxone) have selective anticancer effects in vitro

[0067] The experimental method is the same as the in vitro anti-cancer experiment in Example 1, using human normal vascular endothelial cells ECV-304 to compare the selective cytotoxicity. In vitro cell culture experiments found that under the same dose and test conditions, cephalosporin antibiotics had almost no cytotoxic effect on human normal vascular endothelial cell line ECV-304, or the cytotoxic effect was significantly lower than that on many human cancer cell lines. Cytotoxicity. The inhibitory effect of cephalosporin antibiotics (except ceftriaxone) on nasopharyngeal carcinoma CNE2 and normal cells in vitro is very significantly different, see image 3 .

Embodiment 3

[0068] Example 3: In vivo anticancer effect of cefotaxime sodium on nasopharyngeal carcinoma

[0069] Anti-transplant human nasopharyngeal carcinoma test method in nude mice: prepare human nasopharyngeal carcinoma cell samples by cell culture, adjust the cell concentration to 4×10 with sterile, FBS-free DMEM / F12 culture medium 7 cells / ml to obtain a cell suspension. For balb / c nude mice (body weight 19-21g) that had been adaptively fed for 3 days, each mouse was subcutaneously inoculated with 0.1ml of cell suspension on the right back. Nude mice were bred in SPF laboratory. Measure the long diameter (a) and transverse diameter (b) of each tumor-bearing mouse tumor with a vernier caliper with automatic reading, using the formula: V=a×b 2 / 2 to calculate the tumor volume per mouse. On the 8th day after cell inoculation, most mice had subcutaneous tumors visible to the naked eye, and the average tumor volume reached 200-250mm 3 Left and right, the tumor-bearing mice were stra...

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Abstract

The invention relates to an application of cephalosporin antibiotics as anticancer medicines and the anticancer medicines, and belongs to the technical field of medicine research. The cephalosporin antibiotics have a high specific anticancer effect on nasopharyngeal carcinoma, also have obvious anticancer effects on other various cancers, and have no toxicity to normal cells or have toxicity, farlower than toxicity to cancer cells, to normal cells. The cephalosporin antibiotics remarkably inhibit growth of nasopharyngeal carcinoma in vivo, and do not influence body weight development of animals. The combined effects of the cephalosporin antibiotics with clinical anticancer medicines on different cancers are different. The cephalosporin antibiotics have great differences in anticancer activity, and ceftriaxone does not have anticancer activity. The anti-cancer activity and selectivity of the cephalosporin antibiotics are determined by side chains of chemical structures of the cephalosporin antibiotics, and external structure modification of mother nuclei is a way for finding and synthesizing novel anticancer substances. The result shows that the cephalosporin antibiotics except ceftriaxone are specific anticancer medicines for nasopharyngeal carcinoma, can also be used as therapeutic medicines for other cancers, can be used as a combined anticancer medicine, or can be used as health-care products for adjuvant therapy of cancers.

Description

technical field [0001] The present invention belongs to the technical field of drug research, and in particular relates to the application of cephalosporin antibiotics (except ceftriaxone) in the preparation of drugs with specific and selective anti-nasopharyngeal cancer effects and the application of other cancer anti-cancer drugs, including The cephalosporin antibiotic has specific and selective anticancer drugs or a pharmaceutical composition with combined anticancer effects. Background technique [0002] Cancer is a major disease that seriously threatens human health and life safety, and is the main cause of death for human beings. According to data from the International Center for Cancer Research, in 2012, the number of malignant tumors in the world reached 14.1 million cases and 8.2 million deaths; among them, the number of nasopharyngeal cancer cases was 86,691, and the number of deaths was 50,831. In 2018, there were 18.1 million new cases of cancer worldwide and 9...

Claims

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Application Information

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IPC IPC(8): A61K31/546A61K31/43A61K31/513A61K31/282A61P35/00A61P35/02C07D501/34C07D501/06A23L33/10
CPCA61K31/546A61K31/43A61K31/513A61K31/282A61P35/00A61P35/02C07D501/34C07D501/06A23L33/10A23V2002/00A61K2300/00A23V2200/308
Inventor 贺小琼
Owner KUNMING MEDICAL UNIVERSITY
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