A kind of mangiferin cholic acid derivative and its preparation method and application

A technology of glycoside cholic acid and derivatives, which is applied in the field of mangiferin cholic acid derivatives and its preparation, can solve the problem that esterified derivatives cannot be used as targeted preparations for the treatment of liver and gallbladder inflammation, and achieve the purpose of improving the inhibition of liver and gallbladder inflammation and improving the efficacy of drugs. effect of concentration

Active Publication Date: 2022-03-01
GUANGXI UNIV OF CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, esterified derivatives cannot be used as targeted agents for the treatment of hepatobiliary inflammation

Method used

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  • A kind of mangiferin cholic acid derivative and its preparation method and application
  • A kind of mangiferin cholic acid derivative and its preparation method and application
  • A kind of mangiferin cholic acid derivative and its preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Described mangiferin cholic acid derivative, its preparation method comprises the following steps:

[0036] (1) Mangiferin and p-aminophenylboronic acid were fed at a ratio of 1:1, anhydrous magnesium sulfate was used as a catalyst, and reacted in an anhydrous organic solvent, stirred at room temperature to react, and the reaction process was detected by thin-layer chromatography; the reaction After completion, filter, freeze-dry, and recrystallize with DMSO to obtain the primary product;

[0037] (2) Take the primary product obtained in step (1), mix it with 1.2 equivalents of cholic acid, use EDCI as a dehydrating agent, use DMAP as a catalyst, react in an anhydrous organic solvent, stir evenly at room temperature, and monitor with a thin-layer chromatography plate Reaction process; after the reaction, add organic solvent dichloromethane or chloroform, wash with saturated brine for several times, and dry in vacuum to obtain crude product;

[0038] (3) Take the crude ...

Embodiment 2

[0042] Described mangiferin cholic acid derivative, its preparation method comprises the following steps:

[0043] (1) Take 1g of mangiferin, 324mg of p-aminophenylboronic acid, and 5g of anhydrous magnesium sulfate, react in 30mL of anhydrous organic solvent, stir at room temperature to react, use thin-layer chromatography to detect the reaction process; filter after the reaction, Freeze-dried and recrystallized with DMSO to obtain the primary product;

[0044](2) Take the primary product obtained in step (1), mix it with 1.2 equivalents of cholic acid, use EDCI as a dehydrating agent, use DMAP as a catalyst, react in an anhydrous organic solvent, stir evenly at room temperature, and monitor with a thin-layer chromatography plate Reaction process; after the reaction, add organic solvent dichloromethane or chloroform, wash with saturated brine for several times, and dry in vacuum to obtain crude product;

[0045] (3) Take the crude product obtained in step (2), and recrystall...

Embodiment 3

[0049] Described mangiferin cholic acid derivative, its preparation method comprises the following steps:

[0050] (1) Take 1g of mangiferin, 324mg of p-aminophenylboronic acid, and 5g of anhydrous magnesium sulfate, react in 30mL of anhydrous organic solvent, stir at room temperature to react, use thin-layer chromatography to detect the reaction process; filter after the reaction, Freeze-dried and recrystallized with DMSO to obtain the primary product;

[0051] (2) Take the primary product obtained in step (1), mix it with 1.2 equivalents of cholic acid, use EDCI as a dehydrating agent, use DMAP as a catalyst, react in an anhydrous organic solvent, stir evenly at room temperature, and monitor with a thin-layer chromatography plate Reaction process; after the reaction, add organic solvent dichloromethane or chloroform, wash with saturated brine for several times, and dry in vacuum to obtain crude product;

[0052] (3) Take the crude product obtained in step (2), and recrystal...

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Abstract

The invention discloses a mangiferin cholic acid derivative, its preparation method and application, and discloses its chemical structure and chemical synthesis method. The mangiferin derivatives prepared by the present invention have liver-targeting properties, and can be targetedly accumulated in the liver and gallbladder through the enterohepatic circulation mechanism of cholic acid, thereby increasing the drug concentration and improving the ability of the mangiferin cholic acid derivatives to inhibit hepatobiliary inflammation. Effect.

Description

technical field [0001] The invention relates to the technical field of mangiferin derivatives, in particular to a mangiferin cholic acid derivative and its preparation method and application. Background technique [0002] Targeting agents ( targeting drug delivery system ), also known as targeted drug delivery system, is a preparation that can deliver therapeutic drugs targetedly to the site where the therapeutic effect needs to be exerted (that is, the target area), but has no or almost no drug effect on the non-target area . Targeting agents are divided into active targeting agents, passive targeting agents and physicochemical targeting agents. Targeted preparations have the characteristics of strong targeting, high efficiency and low toxicity, good drug compliance, and fast drug efficacy. They have always been a hot spot in the field of pharmaceutical research and a research goal pursued by pharmaceutical workers. Most of the targeted drugs studied in the early stage a...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07J17/00A61P29/00A61P1/16
CPCC07J17/00A61P29/00A61P1/16
Inventor 李学坚张子谦蒋凌风银江林
Owner GUANGXI UNIV OF CHINESE MEDICINE
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