Use of chidamide analogue in preparation of anti-tumor drug

A technology similar in structure to chidamide, applied in the field of biomedicine, can solve problems such as decreased activity of tumor suppressor factors, abnormal gene expression, and abnormal local conformation of chromosomes

Inactive Publication Date: 2019-01-18
CHINA PHARM UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

In tumor cells, the overexpression of histone deacetylases makes most of histones hypoacetylated, resulting in abnormal chromosome conformation, resulting in abnormal expression of som...

Method used

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  • Use of chidamide analogue in preparation of anti-tumor drug
  • Use of chidamide analogue in preparation of anti-tumor drug
  • Use of chidamide analogue in preparation of anti-tumor drug

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Experimental program
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Effect test

Embodiment

[0016] The effects of LT-548-133-1 and chidamide on the expression of Ace-H3 and p21 of MCF-7 were detected by western blotting:

[0017] MCF-7 cells were cultured in DMEM medium containing 10% fetal bovine serum at 37°C, 5% CO 2 cultured in a cell culture incubator. The medium was changed in 1-2 days, and after the cells were congested, they were digested with 0.25% trypsin and passaged at 1:3. The cells were divided into control group, positive drug (chidamide) group and administration group (10, 5, 2.5 μM). cells in 5 x 10 6 Cells / well were spread in a six-well plate overnight until the cells adhered to the wall, and then administered. After incubation for 24 hours, the cells were digested with 0.25% trypsin to collect the cells. Add 150 μL of RIPA cell lysate to each tube of cells, make the lysate fully contact with the cells, and place on ice for 30 min to lyse. Centrifuge at 12,000 rpm at 4°C for 10 min, and take the supernatant, which is the extracted total protein....

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Abstract

The invention relates to use of a chidamide analogue LT-548-133-1 ((E)-N-(2-aminophenyl)-4-[[3-(3-chlorophenylmethylene)-2-oxopiperidin-1-yl] methyl] benzamide) in preparation of anti-tumor drugs, andbelongs to the field of biomedical technology. The invention adopts different concentrations of LT-548-133-1 on human breast cancer cell MCF-7. The results showed that LT-548-133-1 up-regulates the acetylation level of histone H3 in a dose-dependent manner while decreasing the expression of p21, resulting in cell cycle arrest in G2/M phase and ultimately in MCF-Cell proliferation is inhibited. The study may provide a new approach for the treatment of tumor rapid proliferation.

Description

technical field [0001] The invention relates to the application of chidamide structural analogue LT-548-133-1 in the preparation of antitumor drugs, and belongs to the technical field of biomedicine. Background technique [0002] Histone deacetylase (HDAC) hydrolyzes the acetyl group on the N-terminal lysine residue ε-amino group of histone, restores the positive charge density of histone to increase the attraction between histone and DNA, and makes the nuclear small The structure of the body becomes more compact, which in turn prevents the entry of transcription factors, RNA polymerase, and assembly of the basic transcription complex, thereby inhibiting the transcription of specific genes. In tumor cells, the overexpression of histone deacetylases makes most of histones hypoacetylated, resulting in abnormal chromosome conformation, resulting in abnormal expression of some genes, including tumor suppressor genes, and the activity of related tumor suppressor factors. also de...

Claims

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Application Information

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IPC IPC(8): A61K31/44A61P35/00C07D211/86
Inventor 何书英吴纲万辛雨朱雍耿爱新
Owner CHINA PHARM UNIV
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