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Application of toluylene dimer in preparing medicine for treating liver related diseases

A stilbene dimer and drug technology, applied in the direction of drug combination, resistance to vector-borne diseases, antiviral agents, etc., can solve the problems that the activity has not been reported in the literature

Pending Publication Date: 2018-07-03
INST OF MATERIA MEDICA AN INST OF THE CHINESE ACAD OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There are few relevant reports on Gns-1 in the literature, especially its activity in the treatment and / or prevention of liver-related diseases has not been reported in the literature

Method used

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  • Application of toluylene dimer in preparing medicine for treating liver related diseases
  • Application of toluylene dimer in preparing medicine for treating liver related diseases
  • Application of toluylene dimer in preparing medicine for treating liver related diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Example 1 Detection of Gns-1 using APAP-induced liver cell injury model in vitro

[0025] 1. Experimental method: MTT method is adopted. HepG2 cells are human liver cancer cells, which retain most of the characteristics of normal human liver cells, and are often used in the study of liver cell injury. HepG2 cells were inoculated in 96-well cell culture plates, and after 24 hours of culture, non-toxic concentrations of Gns-1 and paracetamol (APAP, final concentration 8mM) were added, and the positive drug bicyclol control group, solvent control group and model group were set at the same time. Continue to act on the cells for 48h. Discard the culture medium, add 100 μL of MTT (0.5 mg / mL) solution to each well, continue to incubate for 4 h, discard the MTT solution, add 150 μL of DMSO to each well, shake with a mixing oscillator, and measure the absorbance value at a wavelength of 570 nm on a microplate reader. Cell survival rate (%)=100×average OD of administration grou...

Embodiment 2

[0030] Example 2 Detection of Gns-1 by triptolide-induced liver cell injury model in vitro

[0031] 1. Experimental method: MTT method is adopted. HepG2 cells were seeded in 96-well cell culture plates, and after 24 hours of culture, non-toxic concentrations of Gns-1 and triptolide (TPL, final concentration 180nM) were added, and the positive drug bicyclol control group, solvent control group and model were set at the same time. Group. Continue to act on the cells for 48h. Discard the culture medium, add 100 μL of MTT (0.5 mg / mL) solution to each well, continue to incubate for 4 h, discard the MTT solution, add 150 μL of DMSO to each well, shake with a mixing oscillator, and measure the absorbance value at a wavelength of 570 nm on a microplate reader. Cell survival rate (%)=100×average OD of administration group / average OD of blank control group. Experiments were repeated 3-4 times.

[0032]2. Experimental results: The results are shown in Table 2. TPL 180nM acted on HepG...

Embodiment 3

[0037] Example 3 Using concanavalin A (ConA)-induced acute immune liver injury model to detect Gns-1

[0038] 1. Experimental methods and detection indicators

[0039] 1.1 Establishment of ConA-induced acute immune liver injury model in mice and administration method

[0040] SPF male ICR mice (20-22g) were randomly divided into 4 groups after adapting to the environment, blank control group, ConA model group, Gns-1 100mg / kg group by intragastric administration, and positive control drug bicyclol intragastric administration 200mg / kg group. The Gns-1 administration group started administration 3 days before modeling, and administered once a day for a total of 3 days. The bicyclol group administered once in the afternoon of the day before modeling, and in the morning and afternoon of the same day. , Blank control group and model group animals were given the same amount of 0.5% CMC-Na solution. Two hours after the last administration, except the blank control group, the mice i...

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Abstract

The invention discloses application of an indene type toluylene dimer Gns-1 (gnetulin) shown by formula (I) in preparation of a medicine for preventing and / or treating liver related diseases.

Description

technical field [0001] The present invention relates to the new medical application of the compound stilbene dimer (Gnetulin, Gns-1) represented by formula (I), specifically the application of Gns-1 in the preparation of treatment and / or prevention of liver-related diseases. [0002] Background technique [0003] Liver disease is a worldwide disease, and my country is a big country with liver disease. At present, there are a large number of patients with liver injury and liver inflammation caused by various reasons in my country, mainly viral hepatitis. In recent years, the incidence of drug-induced liver disease, alcoholic and non-alcoholic fatty liver disease, autoimmune liver disease, etc. increasing trend year by year. It is well known that liver disease is a progressive disease, and various evidences have suggested that liver inflammation occurs in almost all causes of liver disease, and often throughout the course of liver disease. However, for a long time, the res...

Claims

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Application Information

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IPC IPC(8): A61K31/09A61P1/16A61P31/20A61P31/14A61P35/00
CPCA61K31/09Y02A50/30
Inventor 孙华姚春所杨庆云李芳芳程桂芳张丹亢玉龙
Owner INST OF MATERIA MEDICA AN INST OF THE CHINESE ACAD OF MEDICAL SCI
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