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New application of Apiosylskimmin in preparation of medicine for treating cholestasis

A technology for cholestasis and drugs, applied in the field of preparation of drugs for treating cholestasis, can solve problems such as lack of expression of CYP2B, increase of serum bilirubin level, etc., and achieve broad application prospects and good safety effects

Pending Publication Date: 2021-12-31
THE FIRST HOSPITAL OF LANZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Studies have found that CAR activation can up-regulate the expression of bilirubin-converting enzyme CYP2B and bilirubin efflux transporter multidrug resistance-related protein family; CAR gene deletion can cause loss of CYP2B expression and increase serum bilirubin levels

Method used

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  • New application of Apiosylskimmin in preparation of medicine for treating cholestasis
  • New application of Apiosylskimmin in preparation of medicine for treating cholestasis
  • New application of Apiosylskimmin in preparation of medicine for treating cholestasis

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047]Example 1 Determination of FXR agonistic activity

[0048] Establish a dual-luciferase reporter gene assay for FXR agonist screening cell verification method, the specific experimental steps are as follows:

[0049] 1. HepG2 cells were inoculated in a 96-well plate at a concentration of 15,000 cells / well, cultured in complete DMEM medium for 24 hours, and then transfected when the cells grew to about 70%; the transfection reagent X-tremegene (Roche), overexpressed in advance Plasmid FXR, reporter gene plasmid BSEP, renilla luciferase plasmid, and Opti-MEM were cultured based on a room temperature of 15-25 ° C for 20 minutes; the transfection mixture was prepared in proportion, each 100 μL Opti-MEM medium contained 1 μg of each plasmid, 4 μL of transfection reagent, the ratio of plasmid and transfection reagent is 1:2, mix gently; take out the 96-well plate, add 10 μL of transfection mixed reagent to each well, and continue to incubate for 24 hours; after 24 hours, add 20...

Embodiment 2

[0052] Example 2 Determination of CAR agonistic activity

[0053] Establish a dual-luciferase reporter gene assay for CAR agonist screening cell verification method, the specific experimental steps are as follows:

[0054] 1. HepG2 cells were inoculated in a 96-well plate at a concentration of 15,000 cells / well, cultured in complete DMEM medium for 24 hours, and then transfected when the cells grew to about 70%; the transfection reagent X-tremegene (Roche), overexpressed in advance Plasmid CAR, reporter gene plasmid CYP2B6 and Renilla luciferase plasmid, and Opti-MEM culture were based on a room temperature of 15-25°C and equilibrated for 20 minutes; the transfection mixture was prepared in proportion, each 100 μL Opti-MEM medium contained 1 μg of each plasmid, Transfection Reagent 4 μL of plasmid and transfection reagent at a ratio of 1:2, mix gently; take out the 96-well plate, add 10 μL of transfection mixed reagent to each well, and continue to incubate for 24 hours; add 2...

Embodiment 3

[0057] Example 3 Apiosylskimmin's therapeutic effect on cholestasis mice

[0058] 1. Experimental materials

[0059] Male C57BL / 6 mice, weighing 18±2g, were provided by the Gansu Provincial Institute for Drug Control; they were housed in separate cages in plastic cages, free to eat and drink for 7 days, and allowed them to adapt to the environment and quarantine.

[0060] 2. Experimental method

[0061] In this experiment, 1-naphthyl isothiocyanate (ANIT) was used to establish a mouse model of acute cholestasis, and the therapeutic effect of Apiosylskimmin on this model mouse was studied.

[0062] 2.1 Experimental grouping

[0063] The mice were randomly divided into normal control group, model control group, low-dose Apiosylskimmin group, middle-dose Apiosylskimmin group, high-dose Apiosylskimmin group, and positive drug obeticholic acid (OCA) group, with 8 mice in each group.

[0064] 2.2 Administration method

[0065] Apiosylskimmin low-dose group, Apiosylskimmin middle...

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Abstract

The invention belongs to the technical field of biological medicines and particularly relates to novel application of Apiosylskimmin in preparation of a medicine for treating cholestasis. Firstly, the invention discovers that the Apiosylskimmin can be used for exciting FXR and CAR in a targeted manner and can be used for preparing FXR and CAR agonists; secondly, it is found that the Apiosylskimmin can be used for remarkably inhibiting the content of total bilirubin (TBIL) and total bile acid (TBA) of cholestasis model mice and inhibiting the activity of alanine transaminase (ALT), aspartate transaminase (AST), alkaline phosphatase (ALP) and glutamyl transferase (GGT), the Apiosylskimmin has the remarkable double effects of benefiting gallbladder and removing jaundice, and the effect of the Apiosylskimmin is equivalent to or better than that of existing clinical medicine obeticholic acid; and in addition, the Apiosylskimmin is basically non-toxic and good in safety, and can be used for preparing the medicine for treating the cholestasis and related complications thereof.

Description

technical field [0001] The invention belongs to the technical field of biomedicine, and in particular relates to a new application of Apiosylskimmin for preparing a drug for treating cholestasis. Background technique [0002] Cholestasis refers to the pathological state of bile formation, secretion and excretion disorders caused by various reasons, causing bile to enter the blood, and the clinical manifestations are itching, fatigue and jaundice. Cholestasis has no obvious symptoms in the early stage, and hyperbilirubinemia may occur as the disease progresses, and severe cases may cause liver failure or even death. At present, the main method of treating cholestasis is to remove the cause and choleretic therapy. The commonly used western medicine for cholestasis is ursodeoxycholic acid, and the medicine for treating jaundice is glucuronidase inducer, activated charcoal and albumin. Traditional Chinese medicine has a unique understanding of the etiology and pathogenesis of "...

Claims

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Application Information

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IPC IPC(8): A61K31/7048A61P1/16
CPCA61K31/7048A61P1/16
Inventor 魏玉辉席莉莉沈阗阗李汛石阿茜夏文彬
Owner THE FIRST HOSPITAL OF LANZHOU UNIV
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