Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

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
View PDF1 Cites 1 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

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 some genes, including tumor suppressor genes, and the activity of related tumor suppressor factors. Also reduce accordingly
But there is no report about LT-548-133-1 can prepare anti-tumor drugs

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • 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

Examples

Experimental program
Comparison scheme
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....

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

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

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
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
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com