Application of cholesterol transport inhibitor U18666A as sensitizer in preparation of antitumor products

A technology of U18666A, anti-tumor products, applied in the field of anti-tumor drugs, can solve the problems of lack of relevant reports on U18666A anti-tumor, and achieve the effect of improving tumor inhibition effect, significant curative effect and simple cost

Pending Publication Date: 2022-07-29
SHANDONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there are still no relevant reports on the anti-tumor application of U18666A

Method used

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  • Application of cholesterol transport inhibitor U18666A as sensitizer in preparation of antitumor products
  • Application of cholesterol transport inhibitor U18666A as sensitizer in preparation of antitumor products
  • Application of cholesterol transport inhibitor U18666A as sensitizer in preparation of antitumor products

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0062] 1. Cell culture

[0063] The human hepatocellular carcinoma HepG2 cell line was cultured in DMEM medium containing 100 U / mL streptomycin, 100 U / mL penicillin and 10% bovine serum in 5% CO 2 , aseptic culture in an incubator at a constant temperature of 37°C and saturated humidity.

[0064] 2. Cell crystal violet staining experiment

[0065] HepG2 cells press 1 ⅹ 10 5 The cells / well were inoculated into a 24-well plate and cultured at 37°C overnight; the medium was replaced on the next day, the control group was not given any drug, and the experimental group was added with GPNA (0.5 mM), U18666A (1 μM), GPNA (0.5 mM) and U18666A ( 1 μM), incubate at 37°C for 24 h; aspirate and discard the medium, add 500 μL of pre-cooled PBS, aspirate and discard, add 500 μL methanol, fix at room temperature for 10 min; aspirate and discard methanol, add 500 μL crystal violet staining solution (0.5%), and stain at room temperature for 15 min; Remove the dyeing solution, rinse the resi...

Embodiment 2

[0073] 1. Animal model establishment and grouping

[0074] H22 cells were resuscitated in mouse ascites, and under sterile conditions, 0.1mL / 5x10 5 The mice were subcutaneously injected into the left and right sides of the back of the mice. After the tumor modeling was successful, they were randomly divided into four groups, including the blank control group, the GPNA treatment group, the U18666A treatment group, and the GPNA and U18666A combined treatment group.

[0075] Among them, the administration methods and routes of different administration groups are shown in Table 1, and the blank control group was given the same amount of PBS.

[0076] Table 1 Dosing methods and routes of different experimental groups

[0077]

[0078] Note: i.p.: intraperitoneal injection, intraperitoneal injection; qd: quadue die, once a day

[0079] 2. Determination of tumor volume

[0080] The long diameter (L) and short diameter (W) of the tumor nodules in each group were measured with ve...

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Abstract

The invention relates to an application of a cholesterol transport inhibitor U18666A as a sensitizer in preparation of an anti-tumor product. The invention discloses an application of GPNA and U18666A drug combination in tumor resistance, U18666A improves the killing effect of GPNA on tumor cells, and a new method for overcoming the defect that the anti-tumor drug effect of GPNA is reduced is provided. The application specifically comprises the following steps: (1) the GPNA and U18666A combined medication has a better anti-tumor effect; 2, the U18666A is used for increasing the sensitivity of tumor cells to glutamine limitation; 3, GPNA and U18666A are combined for use, so that the inhibition effect of GPNA on tumor cell proliferation can be enhanced; and 4, the GPNA and U18666A are combined for use, so that the death of tumor cells is remarkably promoted. Compared with the prior art, the pharmaceutical composition has a more remarkable anti-tumor effect.

Description

technical field [0001] The invention belongs to the technical field of antitumor drugs, in particular to the application of cholesterol transport inhibitor U18666A as a sensitizer in the preparation of antitumor products, and the application of a pharmaceutical composition of U18666A and GPNA in antitumor products. Background technique [0002] The information disclosed in this Background section is only for enhancement of understanding of the general background of the invention and should not necessarily be taken as an acknowledgement or any form of suggestion that this information forms the prior art already known to a person of ordinary skill in the art. [0003] Malignant tumor is the main killer of human health and one of the most important diseases that seriously threaten human life. Rapidly growing tumors are metabolically reprogrammed to generate sufficient structural molecules and energy. In normal cells, glutamine (Gln) is a non-essential amino acid. However, tum...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/5685A61K45/06A61P35/00A23L33/10A61K31/198
CPCA61K31/5685A61K31/198A61K45/06A61P35/00A23L33/10A61K2300/00
Inventor 岳学田孔佑姿
Owner SHANDONG UNIV
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