Application of aripiprazole in preparation of antineoplastic drug

An anti-tumor drug, the technology of aripiprazole, which is applied in the field of medicine, can solve the problems of aripiprazole and cancer cells, and achieve the effects of inhibiting growth in the body, reducing the number of clone formation, and low cost

Inactive Publication Date: 2019-07-09
JINAN UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] So far, there is no relevant literature report on the relationship between aripiprazole and the proliferation of cancer cells (especially colorectal cancer cells)

Method used

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  • Application of aripiprazole in preparation of antineoplastic drug
  • Application of aripiprazole in preparation of antineoplastic drug
  • Application of aripiprazole in preparation of antineoplastic drug

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Embodiment 1 in vitro experiment

[0029] (1) Effect of aripiprazole on the proliferation activity of colorectal cancer cells

[0030] The detection is carried out by the WST-1 method, and the specific steps are as follows:

[0031] HCT116 cells, HT29 cells and DLD-1 cells were plated into 96-well plates, with 3000 cells per well, and the medium used was RPMI1640 medium containing 10% (v / v) FBS. After the cells were completely adhered to the wall, the medium was discarded, and the cells were treated with aripiprazole at a certain concentration gradient (0 μM, 10 μM, 15 μM, 20 μM, 30 μM, 40 μM, respectively) (that is, 1 mM aripiprazole was added to 1 mL of RPMI1640 cell culture medium, respectively). Prazole 0 μL, 10 μL, 15 μL, 20 μL, 30 μL and 40 μL, and then added to the corresponding 96-well plate at a volume of 100 μL per well). After 24, 48 and 72 hours of treatment, the cell viability was detected with WST-1 cell proliferation and cytotoxicity detection kit (purc...

Embodiment 2

[0035] Embodiment 2 in vivo experiments

[0036] The effect of aripiprazole on the proliferation of human colorectal cancer cells in nude mice was further studied through animal experiments.

[0037] (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 and experimental group, with 6 mice in the control group, experimental group 1 and experimental group 2, 6 each, used to construct tumor models.

[0038](2) Digest and count HT29 cells, resuspend in PBS buffer (pH=7.4, 0.01M), and the cell concentration in the cell suspension is 4×10 7 cells / mL, and mix the cell suspension with Matrigel at a volume ratio of 1:1. Each nude mouse was subcutaneously injected with 2×10 6 HT29 cells. Nude mice were anesthetized before the experiment, and the degree of anesthesia was evaluated by painless and painful stimulation to ensure that the nude mice were under anesthesia. The HT29 cells resuspend...

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Abstract

The invention discloses application of aripiprazole in preparation of an antineoplastic drug. According to the application, it is found for the first time that the aripiprazole can inhibit the proliferative activity of colorectal cancer cells, reduce the clone formation number of the colorectal cancer cells, and inhibit growth of tumors of colorectal cancer. The colorectal cancer proliferative activity inhibiting effect of the aripiprazole is more remarkable along with the increase of the concentration of the aripiprazole and prolonging of the medication time, and has concentration dependencyon the cycle arrest function and in-vivo inhibiting function on the colorectal cancer cells. Meanwhile, the aripiprazole is a drug ratified by FDA for sale; compared with new medicine development, thecost is low, no obvious toxic or side effect exists, the aripiprazole is used for assisting in treatment of colorectal cancer, and a new drug source can be provided for adjuvant therapy of cancer.

Description

technical field [0001] The invention belongs to the technical field of medicine, in particular to the application of aripiprazole in the preparation of antitumor drugs. Background technique [0002] Aripiprazole (Aripiprazole) is a second-generation atypical antipsychotic drug developed by Japan's Otsuka Pharmaceutical Company (Otsuka) in 1988, and was approved by the U.S. Food and Drug Administration (FDA) on November 15, 2002. , trade name Abilify, for the treatment of schizophrenia. Aripiprazole is a derivative of quinolinone (Quinolinone), which has partial agonistic activity on dopamine D2 and 5-hydroxytryptamine 5-H1A receptors, and is also a 5-hydroxytryptamine 5-HT2A receptor antagonist (Ro Rong. Aripiprazole - a new type of antipsychotic [J]. Modern Diagnosis and Treatment, 2003,14(6):372-373.). Aripiprazole is widely used to treat psychiatric disorders such as steroid mania and schizophrenia. It has been reported that aripiprazole can reduce the increase of lipi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/496A61P35/00
CPCA61K31/496A61P35/00
Inventor 李斌何庆瑜张微瑕
Owner JINAN UNIVERSITY
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