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Application of lomitapide in preparation of antitumor drugs

An anti-tumor drug, the technology of lomitapide, applied in the field of biomedicine, can solve the problems of high price of cancer drugs, drug resistance of malignant tumor cells, and lower quality of life of patients, so as to achieve good prospects for development and utilization, inhibit intestinal Cancer growth, high safety effect

Inactive Publication Date: 2021-09-24
JINAN UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although chemotherapy and radiotherapy can inhibit most cancer cells, it will kill normal cells while killing cancer cells, and can also cause toxic side effects such as gastrointestinal dysfunction and bone marrow suppression, greatly reducing the quality of life of patients and causing long-term Chemotherapy, malignant tumor cells are prone to drug resistance
Most of the drugs for the treatment of cancer are expensive, which also limits the application of drugs

Method used

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  • Application of lomitapide in preparation of antitumor drugs
  • Application of lomitapide in preparation of antitumor drugs
  • Application of lomitapide in preparation of antitumor drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Embodiment 1: in vitro test

[0026] Colorectal cancer cells were treated with different concentrations of lomitapide, and then the cell viability was detected by WST-1 assay to study the effects of different concentrations of lomitapide on the proliferation of colorectal cancer cells. At the same time, flow cytometry was used to detect cell apoptosis, and the effect of different concentrations of lomitazine on the apoptosis of intestinal cancer cells was studied.

[0027] 1. WST-1 experiment

[0028] (1) Plating: Human colon cancer cells HCT116 (purchased from ATCC) and human colon cancer cells HT29 (purchased from ATCC) were digested into suspended single cells with 0.25% trypsin, counted according to 100 μL per well, 3000 Cells were seeded in 96-well plates at 37°C, 5% CO 2 cultivated under conditions.

[0029] (2) Drug treatment: Add 1640 medium (purchased from Sigma-Aldrich Company) containing different concentrations (0, 1.25 μM, 2.5 μM, 5 μM, 10 μM) of lomitap...

Embodiment 2

[0037] Example 2: In vivo test

[0038] Select 12 6-week-old female nude mice (BALB / c nu / nu immunodeficient mice, purchased from the Institute of Model Animals, Nanjing University, 6 mice in the control group and 6 mice in the experimental group, to construct a subcutaneous tumor formation model: (1 ) Human colon cancer cells HT29 were resuspended in PBS buffer (pH=7.4, 0.1M) to obtain resuspended cells; (2) Nude mice were anesthetized before the experiment, and the degree of anesthesia was evaluated by painless and painful stimulation , make sure that the nude mice are under anesthesia; (3) Mix the resuspended cells with Matrigel at a volume ratio of 1:1 to obtain a mixed solution, use a micro-syringe with a 25G needle to take 100 μL containing 2×10 6 The mixture of individual colon cancer cells HT29 was subcutaneously injected into nude mice; (4) lomitapide treatment: ten days after the subcutaneous injection, administration was started by intragastric administration. In th...

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Abstract

The invention discloses an application of lomitapide in preparation of antitumor drugs, and belongs to the technical field of biological medicine. Belongs to the technical field of biological medicine. The lomitapide can be applied to the antitumor drugs. The lomitapide is an FDA approved clinical medicine, and is high in safety, good in development and utilization prospect, small in toxic and side effects and low in price. The invention provides the application of lomitapide in the preparation of the antitumor drugs, and the lomitapide can be dissolved in water and orally taken for adjuvant therapy of colon cancer. In-vitro and in-vivo experiments show that the lomitapide can inhibit growth of intestinal cancer. The invention provides new application of the lomitapide, and provides a new drug source for adjuvant therapy of cancers.

Description

technical field [0001] The invention belongs to the technical field of biomedicine, and in particular relates to the application of lomitapide in the preparation of antitumor drugs. Background technique [0002] Lomitapide was approved on December 21, 2012 to be used together with low-fat diet and other lipid-lowering drugs for the treatment of homozygous familial hypercholesterolemia. The mechanism is that the drug can directly bind and inhibit MTP, thereby preventing Assembly of apoB-containing lipoproteins in enterocytes and hepatocytes, inhibition of synthesis of chylomicrons and very low-density lipoproteins. Inhibition of very low-density lipoprotein synthesis can reduce plasma low-density lipoprotein. At present, there is no application of lomitapide in inhibiting tumor proliferation. [0003] Cancer is one of the most difficult diseases in the world to treat. The mortality rate of colorectal cancer (CRC) ranks second in the global malignancy mortality rate. In my...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/445A61P35/00A61P1/00
CPCA61K31/445A61P35/00A61P1/00
Inventor 许雯雯李斌左谦
Owner JINAN UNIVERSITY
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