Novel application of nifuroxazide or salt thereof

A technology of nifurazide and its application, which can be applied to medical preparations containing active ingredients, respiratory diseases, organic active ingredients, etc., and can solve problems such as poor patient compliance and poor curative effect.

Inactive Publication Date: 2019-03-01
WEST CHINA HOSPITAL SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The object of the present invention is to provide the use of nifurazide or its salt in the preparation of medicines for treating and / or preventing pulmonary fibrosis, so as to solve the problems of poor curative effect and poor patient compliance of existing medicines for treating pulmonary fibrosis

Method used

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  • Novel application of nifuroxazide or salt thereof
  • Novel application of nifuroxazide or salt thereof
  • Novel application of nifuroxazide or salt thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Example 1 Cellular Experiment of Nifuzide Inhibiting Pulmonary Fibrosis

[0034] 1. Experimental principle

[0035] The excessive proliferation of mouse embryonic fibroblasts (NIH3T3), human alveolar basal epithelial cells (A549) and murine lung fibroblasts will cause collagen deposition, so inhibiting their proliferation can inhibit collagen deposition.

[0036] After A549 is stimulated by TGF-β1, it will accelerate its EMT conversion, and then accelerate the formation of pulmonary fibrosis. Therefore, inhibiting EMT conversion can reduce the formation of pulmonary fibrosis.

[0037] This experiment confirmed the effect of nifurazide on inhibiting pulmonary fibrosis from the above two aspects.

[0038] 2. Experimental method

[0039] 1. Cell culture

[0040] Mouse embryonic fibroblasts (NIH3T3) were cultured in DMEM high-glucose medium containing 10% FBS; pancreatic cancer human alveolar basal epithelial cells (A549) were cultured in 1640 medium with 10% FBS; mouse ...

Embodiment 2

[0052] Example 2 Animal Experiments of Nifurazide Treating Pulmonary Fibrosis Induced by Bleomycin

[0053] Multifocal necrosis of type 1 alveolar epithelial cells with fibrotic exudation into the alveoli after bronchial instillation of bleomycin. Proliferation and metaplasia of type 2 epithelial cells, fibroblastic organization of alveolar fibrin and interstitial fibrosis within 2 to 2 weeks. Endothelial cells became edematous and separated from the underlying basement membrane by large foams, and capillary endothelial blebbing and interstitial edema were observed after 4 weeks. The consistent induction of changes similar to diffuse pulmonary fibrosis or fibrotic alveolitis in humans suggests that bleomycin-induced injury may provide a suitable model for studying this ill-defined disease group. Based on this, the C57 mouse model of bleomycin-induced pulmonary fibrosis (CNV) was established to evaluate the effect of nifurazide in the treatment of pulmonary fibrosis in vivo. ...

Embodiment 3

[0071] Example 3 Hepatotoxicity Experiment of Nifurazide

[0072] 1. Cell Culture

[0073] Human normal hepatocytes (LO2) were cultured in DMEM high-glucose medium containing 10% FBS, and 100 U / mL of penicillin and streptomycin were required to be added during the culture and experiment process. in the incubator.

[0074] 2. MTT method to detect the effect of nifurazide on the proliferation of normal human liver cells (LO2)

[0075]Select cells in good logarithmic growth state, inoculate a 96-well plate according to the cell growth rate, about 1500-2000 cells per well, 100 μL per well, and culture in a 37°C, 5% CO2 incubator. On the second day after inoculation, add 100 μL of nifurazide diluted with the corresponding medium to each well to make the final concentration of 0 μg / mL, 1.25 μg / mL, 2.5 μg / mL, 5 μg / mL, 10 μg / mL, 20 μg / mL mL, set 6 replicate wells at the same concentration, culture in 37°C, 5% CO2 incubator for 24, 48, and 72 hours respectively, add 20 μL of MTT sto...

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Abstract

The invention relates to novel application of nifuroxazide or salt thereof, and belongs to the field of medicine. The problems that the existing pulmonary fibrosis medicine treatment effect is not good, and the compliance of a patient is poor are solved. According to the technical scheme, the invention provides application of nifuroxazide or salt thereof for preparing medicine for treating and/orpreventing pulmonary fibrosis. In-vitro and in-vivo experiments prove that nifuroxazide has the remarkable effect of preventing pulmonary fibrosis, is good in safety, is the potential treatment medicine for pulmonary fibrosis and has the great clinic application value.

Description

technical field [0001] The invention relates to a new application of nifurazide or a salt thereof, belonging to the field of medicine. Background technique [0002] Pulmonary fibrosis (Lung Fibrosis) is the end-stage change of a large class of lung diseases characterized by fibroblast proliferation and a large amount of extracellular matrix accumulation accompanied by inflammatory damage and tissue structure destruction. Abnormal repair leads to structural abnormalities (scarring). It seriously affects the respiratory function of the human body, manifested as dry cough and progressive dyspnea (perceived insufficient energy), and with the aggravation of the disease and lung damage, the patient's respiratory function continues to deteriorate. Pulmonary fibrosis is a multiple and common disease, which can involve all ages. At present, with the aggravation of factors such as pollution and environmental deterioration, the number of cases is increasing year by year. According t...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/345A61P11/00
CPCA61K31/345A61P11/00
Inventor 叶庭洪魏于全甘彩玲于艳刘志昊余洛汀谢永美姚于勤
Owner WEST CHINA HOSPITAL SICHUAN UNIV
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