Compound having anti-hepatic injury activity and preparation method and application thereof

A compound and liver damage technology, which is applied in the field of natural medicine and drug therapy, can solve the problems of GAA's weak anti-liver damage activity, large dosage, and low absorption, so as to achieve good repair and protection effects, promote repair function, and improve repair Effect

Active Publication Date: 2017-11-24
佛山市第五人民医院 +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the influence of solubility, the natural GAA has relatively weak anti-liver damage activity, and the dosage is large. In order to further improve the anti-liver damage activity of GAA, people have carried out structural modification and transformation on it, and obtained some GAA derivatives with higher activity. has become a hot topic
At present, GAA has low activity, low absorption, poor solubility and low bioavailability in the body, these characteristics greatly limit its application

Method used

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  • Compound having anti-hepatic injury activity and preparation method and application thereof
  • Compound having anti-hepatic injury activity and preparation method and application thereof
  • Compound having anti-hepatic injury activity and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] The synthesis of embodiment 1 target compound

[0024] Glycyrrhetinic acid (1.1mmole) and biotin (1.3eq) were dissolved in anhydrous dichloromethane (30ml), under the catalysis of pyridine (0.5g) and 4-dimethylaminopyridine (0.5g), room temperature 25 React overnight at -30°C, filter, pass through a silica gel chromatographic column (the elution solvent used is ethyl acetate and petroleum ether with a volume ratio (3-9):7), rotary evaporation, and dry to obtain the white solid target compound . Through liquid chromatography mass spectrometry and NMR analysis, the newly prepared white solid target compound is a compound with a structure shown in formula (I):

[0025]

Embodiment 2

[0026] Example 2 Evaluation of the Anti-hepatic Injury Effect of the Target Compound

[0027] In this example, the mouse liver injury model induced by carbon tetrachloride was used for evaluation.

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Abstract

The present invention belongs to the field of natural medicines and medicine treatment, and discloses a compound having anti-hepatic injury activity and a preparation method and application thereof. The compound is prepared by coupling glycyrrhetinic acid and vitamin biotin, and the structural formula is shown in formula (I). The preparation method comprises the following steps: dissolving the glycyrrhetinic acid and the biotin in anhydrous dichloromethane, under catalysis of pyridine and 4-dimethylaminopyridine, reacting at room temperature overnight, filtering, performing silica gel column chromatography, performing rotary evaporation, and drying to obtain the target compound. Mouse experiments show that the compound has a good therapeutic effect on liver injury diseases.

Description

technical field [0001] The invention belongs to the field of natural medicine and drug treatment, and in particular relates to a compound with anti-liver damage activity and its preparation method and application. Background technique [0002] Aging, neurological diseases, viral infections, drugs or chemical poisons, alcoholism and other factors can all cause liver damage, and then induce hepatitis, liver cirrhosis and even liver cancer, seriously affecting the quality of life and health. Some commonly used hepatoprotective and anti-inflammatory drugs include: cell membrane protective agents, such as polyene phosphatidylcholine; detoxifying and hepatoprotective drugs: such as silymarin, glutathione, etc.; anti-inflammatory and hepatoprotective drugs, including glycyrrhizic acid preparations, hexanone cocoa alkali, bicyclol, etc.; choleretic and hepatoprotective drugs, such as S-adenosylmethionine, ursodeoxycholic acid, etc. And through reasonable drug compatibility, multi-c...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J63/00A61K31/58A61P1/16
Inventor 严文黄文柱刘连王志军刘腾彭咏波
Owner 佛山市第五人民医院
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