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Application of flavonone compounds in preparation of farnesol X receptor stimulant

A receptor agonist and dihydroflavonoid technology, applied in the field of natural medicines, can solve the problems such as the application of dihydroflavonoids in cholestatic liver disease, which has not been reported, and achieve the improvement of inflammatory cell infiltration, the improvement of inhibition of bile excretion, and the improvement of effect of treatment

Inactive Publication Date: 2017-11-28
CATCH BIO SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] However, the application of dihydroflavonoids in the preparation of medicines for the treatment of cholestatic liver disease has not been reported

Method used

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  • Application of flavonone compounds in preparation of farnesol X receptor stimulant
  • Application of flavonone compounds in preparation of farnesol X receptor stimulant
  • Application of flavonone compounds in preparation of farnesol X receptor stimulant

Examples

Experimental program
Comparison scheme
Effect test

experiment example 1

[0045] Experimental example 1 Study on the activation of farnesoid X receptor (FXR) by dihydroflavonoids

[0046] 1. Experimental materials

[0047] Take dihydromyricetin, astilbin, isoastilbin, chrysanthemum glycoside, isoflavin, dihydroquercetin, and dihydrokaempferol as test substances.

[0048] 2. Experimental method

[0049] 2.1 Test product configuration

[0050] Prepare dihydromyricetin, astilbin, isoastilbin, citrusin, isoglucoside, dihydroquercetin and dihydrokaempferol as 50 μg / mL aqueous solutions respectively.

[0051] 2.2 FXR model screening experiment

[0052] 2.2.1 Cell Seeding

[0053] HepG2 liver cancer cells in the logarithmic growth phase were used for experiments, and seeded in 96-well plates at 50,000 / well; each group made 3 replicate wells, and transfected when the coverage rate of cells in the 96-well plates reached 80%-85%. dye.

[0054] 2.2.2 Plasmid transfection

[0055] According to the instructions of LipofectamineTM 2000 reagent, the trans...

experiment example 2

[0070] Experimental example 2 Therapeutic effect of dihydroflavonoids on rats with cholestatic liver disease

[0071] 1. Experimental materials

[0072] Male SD rats, weighing 190-240g, were provided by Shanghai Lingchang Biotechnology Co., Ltd.; they were reared in separate cages in plastic cages, free to eat and drink for 7 days, and allowed them to adapt to the environment and quarantine.

[0073] 2. Experimental method

[0074] In this experiment example, 1-naphthyl isothiocyanate (ANIT) was used to establish a rat model of acute intrahepatic cholestatic hepatitis, and the effects of dihydroflavonoids on the model rats were studied.

[0075] 2.1 Experimental grouping

[0076] Rats were randomly divided into experimental group 1, experimental group 2, experimental group 3, experimental group 4, experimental group 5, experimental group 6, experimental group 7, model control group and normal control group, experimental group 1-7, 4 rats in each group, the test products ...

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Abstract

The invention relates to application of flavonone compounds in the preparation of a farnesol X receptor stimulant. The flavonone compounds including dihydromyricetin, astilbin, isoastilbin, engeletin, isoengeletin, dihydroquercetin and dihydrokaempferol have a relatively strong FXR stimulation effect and can be used as a potential farnesol X receptor stimulant. The flavonone compounds including dihydromyricetin, astilbin, isoastilbin, engeletin, isoengeletin, dihydroquercetin and dihydrokaempferol have a remarkable inhibition effect to the active increase of Tbil, ALT, APL and gamma-GT caused due to ANIT-induced cholestasis, are capable of obviously improving the inhibition to ANIT-induced hepatic cell injury, inflammatory cell infiltration and bile excretion, have a relatively good treatment effect to cholestasis type hepatitis and can be used as potential drugs for treating the cholestasis type hepatitis.

Description

technical field [0001] The invention belongs to the field of natural medicines, and in particular relates to the application of dihydroflavone compounds in the preparation of medicines for treating cholestatic liver disease. Background technique [0002] Cholestatic liver disease is a group of common clinical diseases with cholestasis as the main manifestation. Causes bile excretion disorder, bile flow reduction, bile components back into the blood, causing a series of organic damage, leading to jaundice, skin itching, glucose metabolism and lipid metabolism disorders, etc., mainly involving middle-aged and elderly people, pregnant women, children etc., seriously endanger people's health, even death. [0003] Dihydroflavones, also known as flavanones, belong to flavonoids and are distributed in angiosperms such as Rosaceae, Rutaceae, Zingiberaceae, Compositae, Rhododendronaceae, and Fabaceae. Dihydroflavonoids have a wide range of biological activities such as sterilizatio...

Claims

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Application Information

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IPC IPC(8): A61K31/353A61P1/16
CPCA61K31/353
Inventor 温尧林刘晓宇
Owner CATCH BIO SCI & TECH
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