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Application of ligustrazine derivant in preparing medicine for treating hepatic fibrosis

A liver fibrosis and anti-fibrosis technology, applied in the field of ligustrazine derivatives

Inactive Publication Date: 2011-09-28
NANJING UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] There are no reports on the use of ligustrazine derivatives for anti-hepatic fibrosis

Method used

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  • Application of ligustrazine derivant in preparing medicine for treating hepatic fibrosis
  • Application of ligustrazine derivant in preparing medicine for treating hepatic fibrosis
  • Application of ligustrazine derivant in preparing medicine for treating hepatic fibrosis

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Example 1: Observing H 168 Effect on liver fibrosis in rats

[0020] 1.1 Animals

[0021] Sixty clean-grade SD rats, male, weighing (200±20) g, were provided by Shanghai Slack Company, license number: SCXK (Shanghai) 2007-0005.

[0022] 1.2 Drugs and main reagents

[0023] h 168 (Gifted by Professor Li Wei, Nanjing University of Traditional Chinese Medicine), CCl 4 (Nanjing Chemical Reagent Factory product batch number: 20090120), ALT, AST, ALP assay kits (purchased from Nanjing Jiancheng Bioengineering Research Institute), LN, HA, PCIII ELISA kits (from Shanghai Sino Biotechnology Co., Ltd.).

[0024] 1.3 Main instruments

[0025] Automatic biochemical analyzer (Hitachi model: 7020).

[0026] 1.4 Animal grouping

[0027] Randomly divided into 5 groups, 12 in each group.

[0028] 1.5 Establishment of animal models

[0029] CCl 4 Make 50% olive oil preparation, inject intraperitoneally in every rat by 1ml / kg body weight, three times in the first, twice a week a...

Embodiment 2

[0063] Example 2: H 168 Cytotoxic effect on hepatic stellate cells (cytotoxicity assay)

[0064] 2.1 The main cells used in the experiment

[0065] HSC-T6 (purchased from Shanghai Cell Institute, Chinese Academy of Sciences).

[0066] 2.2 Experimental drugs and main reagents

[0067] h 168 (gifted by Professor Li Wei, Nanjing University of Traditional Chinese Medicine), ligustrazine hydrochloride (Zhejiang Hangzhou Zhongxiang Chemical Co., Ltd. batch number: 20070323).

[0068] DMEM (GIBCO company batch number: 1340114), PBS (self-made in the laboratory), calf serum (Tianjin Yang Biological Products Technology Co., Ltd. batch number: QWTC0701), Trypsin (AMRESCO company batch number: 2009 / 08), normal saline (Shanghai Yuanchangfu Pharmaceutical Co., Ltd. batch number: 070405045), lactate dehydrogenase assay kit (Nanjing Jiancheng batch number: JC-A0020).

[0069] 2.3 Main instruments

[0070] Leica inverted fluorescence microscope (German Leica company model: DM1L), precis...

Embodiment 3

[0076] Example 3: H 168 Detection of induced hepatic stellate cell apoptosis (measurement of cell apoptosis rate by flow cytometry)

[0077] 3.1 The main cells used in the experiment

[0078] HSC-T6 (purchased from Shanghai Cell Institute, Chinese Academy of Sciences).

[0079] 3.2 Experimental drugs and main reagents

[0080] h 168 (gifted by Professor Li Wei, Nanjing University of Traditional Chinese Medicine), ligustrazine hydrochloride (Zhejiang Hangzhou Zhongxiang Chemical Co., Ltd. batch number: 20070323).

[0081] DMEM (GIBCO company batch number: 1340114), PBS (self-made in the laboratory), calf serum (Tianjin Yang Biological Products Technology Co., Ltd. Yuanchangfu Pharmaceutical Co., Ltd. (batch number: 070405045), KGI Annevin V-FITC cell apoptosis detection kit (KGI biological batch number: KGA107).

[0082] 3.3 Main instruments

[0083] Leica inverted fluorescence microscope (German Leica company model: DM1L), precision pipette (French Gilson company model: ...

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Abstract

The invention belongs to the pharmacy field, and discloses application of a ligustrazine derivant (2,5-dihydromethyl-3,6-dimethyl pyrazine) in preparing a medicine for treating hepatic fibrosis. The chemical name of the ligustrazine derivant is 2,5-dihydromethyl-3,6-dimethyl pyrazine, and the molecular formula is C8H12N2O2. In vitro and in vivo test researches prove that the ligustrazine derivant has a favorable function of preventing hepatic fibrosis.

Description

technical field [0001] The present invention relates to a kind of ligustrazine derivative (H 168 ), especially involving H 168 Application in the preparation of anti-hepatic fibrosis drugs. Background technique [0002] Hepatic fibrosis is a compensatory response in the tissue repair process secondary to various forms of chronic liver injury (including viral hepatitis, alcoholism, drug effects, and metabolic diseases), and it is also a necessary condition for the development of chronic liver disease to cirrhosis. pathological process. Hepatitis is one of the diseases with a relatively high morbidity rate in our country. Currently, the status of liver disease in our country is not optimistic. The incidence of liver fibrosis continues to rise, which has become one of the most concerned and important topics of our health department. [0003] The essence of fibrosis is that the synthesis of extracellular matrix (ECM) in the liver is greater than the degradation, resulting in ...

Claims

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Application Information

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IPC IPC(8): A61K31/4965A61P1/16C07D241/12
Inventor 郑仕中陆茵倪春艳李伟吕旋张峰严令耕王爱云
Owner NANJING UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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