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Application of a compound in cancer treatment medicine

A cancer treatment and compound technology, applied in the field of biomedicine, can solve the problems of high heterogeneity drugs in breast cancer that cannot meet targeted and precise treatment

Active Publication Date: 2022-06-21
CHONGQING MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0004] The present invention intends to provide the application of a compound in cancer treatment drugs to solve the problem that existing drugs cannot meet the needs of targeted and precise treatment due to the high heterogeneity of breast cancer

Method used

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  • Application of a compound in cancer treatment medicine
  • Application of a compound in cancer treatment medicine
  • Application of a compound in cancer treatment medicine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] Example 1: Study of the effect of drugs on cell activity

[0044] The human breast cancer cells MCF-7, ZR-75-1 and T47D cells in the logarithmic growth phase were taken to prepare single cell suspensions, which were inoculated in 96-well culture plates, 180 μl per well, and 12.5, 25, 50, and 100 cells were added to each well. 200 μmol / l of candidate compounds were cultured for 24 h, 48 h, and 72 h, respectively, and 20 μl of MTT was added to each well. After culturing for 4 h, the medium was discarded, and 150 μl of DMSO was added to mix well. The OD value of the well at 570nm wavelength was used to calculate the cell growth inhibition ratio (IR) and IC50.

[0045] In this experimental example, MTT experiments were performed on 14 compounds. In fact, when the inventor was conducting research, the inventor screened 2 million compounds in the library, and screened out a total of 14 potential compounds. In the follow-up MTT experiment, it was further found that four compo...

Embodiment 2

[0055] Example 2: In vitro cytotoxicity evaluation of Zinc-09

[0056] Using the commonly used anticancer drug paclitaxel (PTX) as a positive control, the concentration of PTX was 0.5 μM, and taking normal breast epithelial cells MCF-10A as the research object, the cytotoxicity of Zinc-09 was detected by MTT method. The experimental results are as follows Figure 8 As shown (the data in the figure is in the form of mean±SE, n=6), the results show that in normal mammary epithelial cells MCF-10A, the inhibitory effect of PTX on the cells for 48h is 32.3%, and 200 μM Zinc-09 on MCF-10A The inhibition rate of cells was 40.7%, and when Zinc-09 was lower than 200 μM, the inhibitory effect of the drug on MCF-10A cells was less than that of PTX, indicating that compared with the clinical anti-breast cancer drug PTX, Zinc-09 has less cytotoxicity.

Embodiment 3

[0057] Example 3: Confirmation of the target of Zinc-09

[0058] In this example, conventional western blot was used for detection. The basic process was as follows: cells were inoculated into T25 culture flasks, and after the cells adhered to the wall, different concentrations of test drugs were added to treat them for different times, and then the cells were collected, and RIPA (plus PMSF) was used to collect the cells. After lysing on ice for 1 h, centrifuge at 4 °C for 20 min, take the supernatant, add 5× loading buffer, and cook at 100 °C for 5 min to denature the protein. After separation by SDS-PAGE, the membrane was transferred to PVDF membrane, blocked and incubated with primary and secondary antibodies for color development.

[0059] In the occurrence and development of breast cancer, the expression of SGK3 is regulated by estrogen. Therefore, we first detected 6 breast cancer cell lines (MCF-7, ZR-75-1, T47D, MDA-MB-231, MDA-MB -453, CAL-148) expression of SGK3 pro...

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Abstract

The invention relates to the field of biomedicine, in particular to the application of a compound in cancer treatment drugs. The compound Zinc‑09 in this program has good anticancer activity and SGK3 (serum and glucocorticoid-induced protein kinase 3) targeting, can target the downstream pathway of SGK3, and inhibit the SGK3-mediated cancer cell Occurrence and development have an inhibitory effect. Zinc‑09 in this program can solve the problem that existing drugs cannot meet the demand for targeted and precise therapy due to the high heterogeneity of breast cancer. Zinc‑09 and its derivatives can be developed as inhibitors targeting SGK3 to exert its anticancer effect.

Description

technical field [0001] The invention relates to the field of biomedicine, in particular to the application of a compound in a cancer therapeutic drug. Background technique [0002] Breast cancer has become one of the most common tumors that seriously threaten women's health and even life, and its mortality rate has ranked first among women's cancer deaths. The occurrence and development of breast cancer and its mechanism are extremely complex. With the deepening of the understanding of the biological behavior of breast cancer and the transformation and update of the treatment concept, the treatment of breast cancer has entered the era of comprehensive treatment of surgery, chemotherapy and radiotherapy. Among them, drug chemotherapy is still one of the main means of clinical treatment of breast cancer. [0003] Compared with comprehensive chemotherapy, targeted therapy is an emerging and more efficient treatment method. For example, based on receptor tyrosine kinase famil...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/513A61P35/00A61P35/04
CPCA61K31/513A61P35/00A61P35/04
Inventor 周维英李小丽周端方宋燚张欢龙良源
Owner CHONGQING MEDICAL UNIVERSITY
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