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Application of compound EPZ5676 and related inhibitor thereof in preparing drug for preventing and treating pulmonary fibrosis diseases

A technology of EPZ5676, pulmonary fibrosis, is applied in the field of preparing medicines for preventing and treating pulmonary fibrosis, which can solve the problems of harming patients' health and postoperative rehabilitation, lack of treatment and intervention measures, etc.

Inactive Publication Date: 2018-11-02
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Clinical practice shows that pulmonary fibrosis is the final stage of the development of most lung diseases, which seriously endangers the health of patients and postoperative rehabilitation, and there is still a lack of effective therapeutic interventions in clinical practice; the current main treatment strategies are: anti-inflammatory, anti-fibrotic oxidation and anti-oxidation

Method used

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  • Application of compound EPZ5676 and related inhibitor thereof in preparing drug for preventing and treating pulmonary fibrosis diseases
  • Application of compound EPZ5676 and related inhibitor thereof in preparing drug for preventing and treating pulmonary fibrosis diseases
  • Application of compound EPZ5676 and related inhibitor thereof in preparing drug for preventing and treating pulmonary fibrosis diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] This example shows that EPZ5676 can significantly improve the survival rate and weight loss of mice, reduce inflammatory infiltration and fibrous thickening of alveolar walls and bronchioles in the process of pulmonary fibrosis, and inhibit collagen production in lung tissue and the expression of fibrotic effector protein .

[0025] The experiment was made with Bleomycin (bleomycin). The specific method was as follows: male C57BL / 6J mice weighing 25-30g were anesthetized with 10% chloral hydrate and fixed on their back, and the neck skin was prepared; a 1cm opening was cut in the middle of the trachea, Separate the trachea bluntly, do a tracheal puncture, inject 30μL Bleomycin (2.5mg / kg), inject about 1ml of gas to make the Bleomycin evenly distributed, suture the neck skin, disinfect and avoid infection; routinely make the Bleomycin distribution more uniform; then keep the mouse After the body temperature was awake, they were raised in separate cages in a sterile breeding...

Embodiment 2

[0028] EPZ5676 inhibits TGF-β-induced fibrosis-related protein expression in WI38 and mLFs cells

[0029] The mouse primary fibroblasts mLFs and WI38 (human embryonic fibroblast cell line) extracted by the tissue patch method were cultured in DMEM and MEM medium containing 10% fetal bovine serum, respectively, and placed at 37℃, 5 Cultured in a %CO2 incubator, the cells reached an appropriate density and then passaged; the experiment was divided into a control group, a model group stimulated by TGF-β (4ng / ml), EPZ5676 (10mM) was given in advance for 4 hours and then TGF-β (4ng / ml) was added In the stimulated administration group, DOT1LshRNA lentivirus was transfected in advance and then added to the TGF-β (4ng / ml) stimulated lentiviral transfection group, and the changes in the expression of fibrosis-related proteins were detected by Western Blotting and immunofluorescence;

[0030] The results show that Western Blotting and immunofluorescence detection both show that EPZ5676 and D...

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Abstract

The invention belongs to the field of pharmacy and relates to novel application of a compound EPZ5676 in pharmacy, in particular to application of a compound EPZ567 (C30H42N8O3) and a related inhibitor thereof in preparing a drug for preventing and treating pulmonary fibrosis diseases. According to the application, the result of a therapeutic effect experiment of the compound EPZ5676 for pulmonaryfibrosis in vivo and in vitro shows that the effect of the EPZ5676 on pulmonary fibrosis resistance is realized by inhibiting histone transmethylase DOT1L; experiment results prove that the EPZ5676 is used as an inhibitor for the histone transmethylase DOT1L and shows better pulmonary fibrosis resistance in vivo and in vitro. The compound EPZ5676 has better pulmonary fibrosis resistance in vivo and in vitro. Furthermore, the compound EPZ5676 and the related inhibitor thereof can be used for preparing a drug for preventing and treating the pulmonary fibrosis diseases.

Description

Technical field [0001] The present invention belongs to the field of pharmacy, relates to the new use of compound EPZ5676 in pharmacy, and specifically relates to compound EPZ567(C 30 H 42 N 8 O 3 ), CAS number 1380288-87-8 and its related inhibitors in the preparation of drugs for preventing and treating pulmonary fibrosis. Background technique [0002] The prior art discloses that pulmonary fibrosis is a group of destructive lung diseases caused by different causes, mainly manifested as diffuse alveolitis, structural disorder of alveolar units, and pulmonary fibrosis, which ultimately leads to severe damage to lung structure and function. The pathogenesis has not been fully elucidated. Studies have shown that pulmonary fibrosis, especially idiopathic pulmonary fibrosis (IPF), is an interstitial lung disease, which seriously endangers the lives of patients. According to statistics, the survival rate after diagnosis of IPF is only 3 years, which exceeds most malignant tumors. Cl...

Claims

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Application Information

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IPC IPC(8): A61K31/7076A61P11/00
CPCA61K31/7076
Inventor 朱依谆刘新华徐鹏
Owner FUDAN UNIV
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