Application of indacaterol maleate to preparation of tumor resisting medicines

An anti-tumor drug, the technology of acid indene, applied in the field of medicine, can solve the problems that have not yet been reported on cancer cell research, and achieve the effect of inhibiting tumor growth

Inactive Publication Date: 2019-07-16
JINAN UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there is no research report on the effect of indacaterol maleate on cancer cells (especially colorectal cancer)

Method used

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  • Application of indacaterol maleate to preparation of tumor resisting medicines
  • Application of indacaterol maleate to preparation of tumor resisting medicines
  • Application of indacaterol maleate to preparation of tumor resisting medicines

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Example 1 In vitro experiment: growth inhibitory effect of indacaterol maleate on colorectal cancer cells.

[0027] The detection is carried out by the WST-1 method, and the specific steps are as follows:

[0028] 1) Spread colorectal cancer cells HT29, RKO, DLD-1, and HCT116 into 96-well plates, with 3000 cells per well.

[0029] 2) Dissolve indacaterol maleate (purchased from Shanghai Taosu Biochemical Technology Co., Ltd.) in dimethyl sulfoxide (DMSO) to prepare a stock solution with a concentration of 10 mM, and then use RPMI1640 cell culture medium (containing 10% (v / v) FBS) to dilute the stock solution to prepare working solutions with final concentrations of 0 μM, 15 μM, 20 μM, 30 μM and 40 μM.

[0030] 3) After the cells in step (1) adhere to the wall, add the working solution of different concentrations prepared in step (2) into the corresponding wells in a volume of 100 μL per well. After the working solution is treated for 24, 48, and 72 hours, use WST respe...

Embodiment 2

[0033] Example 2 In vitro experiment: the cycle arrest effect of indacaterol maleate on colorectal cancer cells.

[0034] The steps are as follows: spread HT29 and RKO cells into 12-well plates, 2×10 per well 5 After the cells adhered to the wall, the cells were treated with a working solution of a certain concentration gradient (0 μM, 7.5 μM, 15 μM, 30 μM), and 1 mL of the working solution of the corresponding concentration was added to each well for 48 hours, and the cell cycle detection kit ( (purchased from Beyond Biotechnology Co., Ltd.) was used to detect cell cycle with C6Flow Cytometer flow cytometer (purchased from BD Accuri Company) after treating the cells.

[0035] The above experimental steps were biologically repeated three times. The sources of HT29 and RKO cells used in this step and the preparation method of the working solution were the same as in Example 1.

[0036] The results of the cell experiments figure 2 As shown, indacaterol maleate has obvious cyc...

Embodiment 3

[0037] Example 3 In vivo experiment: the inhibitory effect of indacaterol maleate on the growth of xenografted human colorectal cancer cells in nude mice.

[0038] (1) Select 18 6-week-old female nude mice (balb / c-nu / nu) (purchased from Southern Medical University), and randomly divide them into control group, experimental group 1 and experimental group 2, with 6 mice in each group, used to construct tumor models.

[0039] (2) HCT116 cells were digested, counted and resuspended in PBS buffer (pH=7.4, 0.01M), and the cell concentration in the cell suspension was 1×10 8 cells / mL, mix the cell suspension with Matrigel at a volume ratio of 1:1. Before the experiment, the nude mice were anesthetized, and the degree of anesthesia was evaluated through painless and painful stimulation to ensure that the nude mice were under anesthesia. HCT116 cells resuspended in PBS buffer and mixed with Matrigel were subcutaneously injected into nude mice with a micro-syringe with a 25G needle, a...

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Abstract

The invention discloses an application of indacaterol maleate to preparation of tumor resisting medicines. According to the application of the invention, the situation that the indacaterol maleate canrestrain the growth of colorectal cancer is found for the first time. The indacaterol maleate can restrain the reproductive activity of colorectal cancer cells, block the cell cycle of the colorectalcancer, cause G1-period blocking to restrain tumor growth of in vivo colorectal cancer. Besides, the effect of the indacaterol maleate for restraining the cell proliferation activity of the colorectal cancer is more significant along with the increase of the concentration of the indacaterol maleate and prolonging of medication time, and the indacaterol maleate has concentration dependence on thecycle checking effect and in vivo growth of colorectal cancer cells. Besides, the indacaterol maleate is a medicine which is approved by FDA for sale, is lower in cost than developing new medicines, and does not have any obvious toxic or side effects, and when the indacaterol maleate is used for auxiliary treatment of the colorectal cancer, a new medicine source can be provided for auxiliary treatment of cancer.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to the application of indacaterol maleate in the preparation of antitumor drugs. Background technique [0002] Colorectal cancer (CRC) is a common malignant tumor of the digestive tract and one of the main tumor types with a high mortality rate worldwide. At present, radiotherapy and chemotherapy are still the main treatment methods for colorectal cancer. Although chemotherapy and radiotherapy can inhibit most cancer cells, it also kills normal cells while killing cancer cells. It also has toxic side effects such as gastrointestinal dysfunction and bone marrow suppression, which greatly reduces the quality of life of patients. Therefore, it is very urgent to explore safer and more effective treatment options. [0003] Chronic obstructive pulmonary disease is a disease of persistent and progressive airflow limitation (Donald PT. Indacaterolmaleate for the treatment of ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4704A61K31/194A61P35/00
CPCA61K31/194A61K31/4704A61P35/00A61K2300/00
Inventor 李斌何庆瑜李杨葭
Owner JINAN UNIVERSITY
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