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Application of demethylenetetrahydroberberine hydrochloride in preparation of medicine for preventing or treating liver injury

A technology for methylenetetrahydroberberine and liver damage, applied in the field of biomedicine, can solve the problems of reversing the process of liver fibrosis, blocking, etc., and achieve the effect of improving compliance, reducing effective dose, and good anti-inflammation

Inactive Publication Date: 2020-04-17
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there is no specific and effective method for the treatment of liver fibrosis clinically. The main treatment plan is to prevent or alleviate liver damage, and then block or even reverse the process of liver fibrosis.

Method used

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  • Application of demethylenetetrahydroberberine hydrochloride in preparation of medicine for preventing or treating liver injury
  • Application of demethylenetetrahydroberberine hydrochloride in preparation of medicine for preventing or treating liver injury
  • Application of demethylenetetrahydroberberine hydrochloride in preparation of medicine for preventing or treating liver injury

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] Example 1. Desmethylenetetrahydroberberine hydrochloride (DMTHB) cellular level antioxidant activity

[0047] Method: The ability of desmethylenetetrahydroberberine hydrochloride to scavenge ROS was detected at the cellular level by using the ROS probe method. We first pre-incubated normal liver cells (L02) with 40 μM desmethylene berberine hydrochloride and des methylenetetrahydroberberine hydrochloride for 4 h. Hydrogen peroxide H was then added to the Petri dish 2 o 2 (1mM) continuously stimulate the hepatic cell line (L02) for 1h to make it produce a large amount of ROS and cause cell damage. Using the principle of fluorescent probe DCFH-DA (50 μM) combined with ROS to generate fluorescence, the scavenging effect of ROS was observed under a fluorescence microscope.

[0048] Results: Fluorescence microscopy showed that various concentrations of DMTHB can significantly inhibit the ROS produced by peroxide in L02 cells, the results are as follows figure 1 .

Embodiment 2

[0049] Example 2. The protective effect of desmethylenetetrahydroberberine (DMTHB) on thioacetamide-induced acute mild liver injury

[0050] Method: In this experiment, male ICR mice, weighing 22-24 g, were randomly divided into 6 groups, with 8 mice in each group. Each group was normal control group, model group, silymarin (SILY) positive drug group (150mg / kg), desmethylenetetrahydroberberine hydrochloride low-dose group (50mg / kg), desmethylenetetrahydrochloride hydrochloride group Berberine medium dose group (150mg / kg), demethylenetetrahydroberberine hydrochloride high dose group (300mg / kg). The administration group was given intragastric administration for 5 consecutive days, while the control group and the model group were given the same dose of excipients by intragastric administration for 5 days. On the fourth day of gavage, the mice in the model group and the treatment group were injected intraperitoneally with thioacetamide at a dose of 150 mg / kg, and the mice in the ...

Embodiment 3

[0054] Example 3. The protective effect of desmethylenetetrahydroberberine hydrochloride (DMTHB) on the pathological changes of acute mild liver injury induced by thioacetamide

[0055] Method: In this experiment, male ICR mice, weighing 22-24 g, were randomly divided into 6 groups, with 8 mice in each group. Each group was normal control group, model group, silymarin (SILY) positive drug group (150mg / kg), desmethylenetetrahydroberberine hydrochloride low-dose group (50mg / kg), desmethylenetetrahydrochloride hydrochloride group Berberine medium dose group (150mg / kg), demethylenetetrahydroberberine hydrochloride high dose group (300mg / kg). The administration group was given intragastric administration for 5 consecutive days, while the control group and the model group were given the same dose of excipients by intragastric administration for 5 days. On the fourth day of gavage, the mice in the model group and the treatment group were injected intraperitoneally with thioacetamide...

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Abstract

The invention relates to the field of biological medicines, and concretely relates to application of demethylenetetrahydroberberine hydrochloride in the preparation of a medicine for preventing and / ortreating liver injury induced by thioacetamide. The demethylenetetrahydroberberine hydrochloride medicine has the advantages of good solubility, good medicine absorptivity and good anti-inflammatoryand antioxidant activity, and has a remarkable treatment effect on thioacetamide-induced acute mild and chronic liver injury; and compared with the traditional liver protection medicine, the demethylenetetrahydroberberine hydrochloride can achieve the treatment purpose under a low oral administration dosage, can improve the patient compliance, and achieves the treatment effect on diseases.

Description

technical field [0001] The invention relates to the field of biomedicine, in particular to the application of desmethylenetetrahydroberberine hydrochloride in the preparation of drugs for preventing and / or treating liver damage induced by thioacetamide. Background technique [0002] The liver is the most important metabolic organ in the human body and participates in the metabolism of various substances such as carbohydrates, lipids, and vitamins. There are also many drug-metabolizing enzymes in the liver, and the liver must be involved in the metabolic elimination of almost all drugs and exogenous chemical substances. Therefore, the excessive use or abuse of drugs and the inadvertent intake of hepatotoxic substances will lead to acute, chronic or explosive damage to the liver. Moreover, acute liver failure has the characteristics of rapid onset, multiple complications, and high mortality, which poses a huge threat to human health. Faced with severe liver damage, liver tran...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4375A61P1/16
CPCA61K31/4375A61P1/16
Inventor 张玉彬朱倩倩张元强闻婧
Owner CHINA PHARM UNIV
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