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Application of Bromodomain-containing protein 4 (BRD4) and inhibitor thereof in preparing drugs for treating fatty liver and related diseases

A technology of functional domains and inhibitors, applied in metabolic diseases, drug combinations, endocrine system diseases, etc., can solve problems such as unclear effects

Inactive Publication Date: 2018-06-22
WUHAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the role of BRD4 and its inhibitors in fatty liver is not clear

Method used

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  • Application of Bromodomain-containing protein 4 (BRD4) and inhibitor thereof in preparing drugs for treating fatty liver and related diseases
  • Application of Bromodomain-containing protein 4 (BRD4) and inhibitor thereof in preparing drugs for treating fatty liver and related diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0053] [Example 1] Effect of BRD4 inhibitor treatment on lipid accumulation in L02 cells

[0054] L02 cells were divided into three groups for culture. After the cells adhered to the wall, they were treated with DMSO, 0.5 μM JQ1, and 0.5 μM OTX015 for 3 hours, and then treated with 0.2 / 0.4 mM PAOA for 12 hours, and stained with Oil Red O.

[0055] The staining result is as figure 1 As shown, the color of the inhibitor-treated group was significantly lighter compared with the control DMSO group. The results indicated that lipid accumulation was significantly inhibited in L02 cells treated with BRD4 inhibitor. [Example 2] Effect of BRD4 inhibitor treatment on lipid accumulation in HepG2 cells

Embodiment 2

[0055] The staining result is as figure 1 As shown, the color of the inhibitor-treated group was significantly lighter compared with the control DMSO group. The results indicated that lipid accumulation was significantly inhibited in L02 cells treated with BRD4 inhibitor. [Example 2] Effect of BRD4 inhibitor treatment on lipid accumulation in HepG2 cells

[0056] HepG2 cells were divided into three groups and cultured. After the cells adhered to the wall, they were treated with DMSO, 0.5 μM JQ1, and 0.5 μMOTX015 for 3 hours, and then treated with 0.1 / 0.2 mM PA / OA for 12 hours before staining with Oil Red O.

[0057] The staining result is as figure 2 As shown, the color of the inhibitor-treated group was significantly lighter compared with the control DMSO group. The results indicated that lipid accumulation was significantly inhibited in HepG2 cells treated with BRD4 inhibitor.

[0058] The above results show that inhibiting the expression of BRD4 can significantly impro...

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Abstract

The invention discloses application of a Bromodomain-containing protein 4 (BRD4) and an inhibitor thereof in preparing drugs for treating fatty liver and related diseases. Different liver cells (L02 cell and HepG2 cell) are adopted as experimental subjects which are treated by BRD4 inhibitors, JQ1 AND OTX015 respectively; with DMSO as control, the liver cells are treated by palmitate / oleic acid (PA / OA), and then are dyed by oil red O; the dyeing results show that: in comparison with the DMSO control group, the color of the inhibitor treatment group obviously becomes light, indicating that after BRD4 is inhibited, fat accumulation can be suppressed, and the occurrence of fatty liver and related diseases can be reduced. Therefore, the BRD4 provides a target of developing drugs for preventing, relieving and / or treating fatty liver and related diseases.

Description

technical field [0001] The invention belongs to the field of gene function and application, and in particular relates to the application of BRD4 as a drug target in the screening of drugs for the treatment of fatty liver, and the use of BRD4 inhibitors in the preparation of drugs for the prevention, alleviation and / or treatment of fatty liver and related diseases Applications. Background technique [0002] With the continuous improvement of people's living standards, great changes have taken place in the diet structure, which gradually tends to be high in protein and high in fat. However, human metabolism is limited, which leads to the continuous accumulation of fat in the liver, which leads to fat accumulation. liver. In recent years, the incidence of fatty liver has been increasing day by day, and the patients will be accompanied by steatohepatitis, liver fibrosis and even liver cirrhosis, and will develop into hepatocellular carcinoma. At present, there is no specific d...

Claims

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Application Information

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IPC IPC(8): A61K45/00A61P35/00A61P1/16A61P5/50A61P3/00A61P3/04A61P3/10A61P3/06
CPCA61K45/00
Inventor 李红良李枫
Owner WUHAN UNIV
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