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Application of ZINC62678696 in preparation of medicine for inhibiting liver fibrosis

A technology of liver fibrosis and drugs, applied in the field of preparation of drugs to inhibit liver fibrosis, can solve the problems of reversing liver fibrosis and no specific drugs

Active Publication Date: 2018-12-07
TIANJIN MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] In order to solve the problems in the prior art, the present invention provides the use of ZINC62678696 in the preparation of drugs for inhibiting liver fibrosis, and solves the problem that there is no specific drug in the prior art to effectively prevent or reverse liver fibrosis

Method used

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  • Application of ZINC62678696 in preparation of medicine for inhibiting liver fibrosis
  • Application of ZINC62678696 in preparation of medicine for inhibiting liver fibrosis
  • Application of ZINC62678696 in preparation of medicine for inhibiting liver fibrosis

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0017] ZINC62678696 Add pharmaceutically acceptable excipients and make various dosage forms according to conventional methods, such as liquid injections of various specifications, powder injections, emulsions for injections, tablets, pills, capsules, ointments, creams, patches, liniments , powder, spray, implant, drop, suppository, ointment, candy, etc.

[0018] The administration routes of ZINC62678696 include various administration routes: oral administration, injection administration, implant administration, intracavitary administration, sublingual administration, anal administration, transdermal administration, internal and external application, etc.

experiment example 1

[0019] Experimental example 1: gene chip screening and verification

[0020] Differential mRNAs in fibrotic liver tissue and normal liver tissue were screened by gene chip. The chip is currently the most powerful whole-transcriptome research tool, designed with 5.5 million probes, which basically include all known classic transcripts and all predicted possible gene transcription forms. In addition, the chip is designed with multiple probes for each sequence, which increases the reliability of the signal. We extracted total RNA from 5 fibrotic liver tissues and 5 normal liver tissues, and passed the quality inspection through high-throughput chip screening. According to the expression difference between fibrotic liver tissue and normal liver tissue, the expression difference was more than 1.6 times and the P value was less than or equal to According to the standard of 0.05, 1526 mRNAs were differentially expressed between fibrotic liver tissue and normal liver tissue, among wh...

experiment example 2

[0022] Experimental Example 2: Constructing CCl 4 and bile duct ligation (BDL)-induced liver fibrosis model in mice

[0023] CCl 4Induced mouse liver fibrosis model: purchase 36 balb / c male mice, and after a week of normal feeding, they were randomly divided into 6 groups, 6 in each group: control group (injected with olive oil) and CCl 4 2, 4, 6, 8, 10 week groups. CCl 4 Group mice were intraperitoneally injected with 0.3ml / kg CCl 4 (5%, v / v, dissolved in olive oil; ), twice a week for 8 weeks. After 8 weeks of treatment, the control group and CCl were anesthetized with chloral hydrate. 4 Group mice, recorded changes in liver appearance and photographed, and liver tissues were fixed and cryopreserved for subsequent experiments.

[0024] Bile duct ligation (BDL)-induced liver fibrosis model in mice:

[0025] (1) After buying 24 balb / c male mice and feeding them normally for one week, they were randomly divided into four groups with 6 mice in each group: control group (...

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PUM

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Abstract

The invention discloses an application of ZINC62678696 in preparation of a medicine for inhibiting liver fibrosis, and provides the application of a substance, inhibitor ZINC62678696 that is capable of reducing activity of GPR65 in preparation of the medicine for treating the liver fibrosis; by researching the effect and mechanism of the GPR65 in the liver fibrosis, it is found that the disease progression of the liver fibrosis can be alleviated by inhibiting the activity of the GPR65 in macrophages. The invention has important reference significance on researching of the pathogenesis of the liver fibrosis and selection on treatment strategy in future.

Description

technical field [0001] The present invention relates to the application of ZINC62678696, an inhibitor targeting GPR65, in the preparation of drugs for inhibiting liver fibrosis. Background technique [0002] Liver fibrosis is an inevitable stage in the development of various chronic liver diseases to cirrhosis, and it is the result of various etiologies such as viral hepatitis, alcoholism, parasites, autoimmune diseases and malnutrition that lead to tissue damage such as inflammation and necrosis. Fix response. If the process of liver fibrosis is not suppressed or reversed, it may progress to decompensated liver cirrhosis, and various complications of end-stage liver disease will appear, seriously affecting the quality of life and prognosis of patients. Related studies have reported that liver cirrhosis affects 1% to 2% of the world's population and causes more than 1 million deaths worldwide each year. my country is one of the countries with the highest incidence and morta...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/506A61P1/16
CPCA61K31/506A61P1/16
Inventor 洪伟韩涛章坤姚庆斌洪宇桁韩晓辉时哲敏郑丽娜胡志梅
Owner TIANJIN MEDICAL UNIV