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Compound 2,3,4,6,8-pentamethoxyl-dibenzofuran and its use

A pentamethoxy, diphenyl technology, applied in the field of natural medicinal chemistry, can solve problems such as toxicity, and achieve significant social and economic benefits.

Active Publication Date: 2009-05-13
BEIJING INSTITUTE OF TECHNOLOGYGY +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, the compound that has a good inhibitory effect on SSAO enzyme activity is dibromoethylamine, but this compound has certain toxicity to the human body and has not been developed as a drug.

Method used

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  • Compound 2,3,4,6,8-pentamethoxyl-dibenzofuran and its use
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  • Compound 2,3,4,6,8-pentamethoxyl-dibenzofuran and its use

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] 1. Preparation of 2,3,4,6,8-pentamethoxy-dibenzofuran

[0040] (1) 5Kg of the root of the natural plant Rosaceae Hawthorn plant Hawthorn is weighed and pulverized, and the pulverization refers to pulverization by a common pulverizer;

[0041] (2) adding 50L of 80% ethanol to reflux extraction of crushed plant fragments for 3 hours to obtain ethanol extract;

[0042] (3) The extract is filtered with a clarification plate, the filtrate is recovered under vacuum and reduced pressure to remove the solvent, the weight of the obtained extract is weighed to be 0.5Kg, and the extract is pulverized into fine powder by an ordinary pulverizer;

[0043] (4) add petroleum ether, chloroform, ethyl acetate successively to extract by the weight percentage of extract and petroleum ether, chloroform, ethyl acetate is 1:20, the petroleum ether of gained, chloroform extraction solution adopts vacuum decompression recovery to remove solvent respectively , to obtain the crude product;

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Embodiment 2

[0089] 1. Preparation of 2,3,4,6,8-pentamethoxy-dibenzofuran

[0090] (1) 5Kg of the root of the natural plant Rosaceae Hawthorn plant Hawthorn is weighed and pulverized, and the pulverization refers to pulverization by a common pulverizer;

[0091] (2) adding 50L of 95% ethanol to reflux extraction of crushed plant fragments for 3 hours to obtain ethanol extract;

[0092] (3) The extract is filtered with a clarification plate, the filtrate is recovered under vacuum and decompression to remove the solvent, and the weight of the obtained extract is weighed to be 0.45Kg, and the extract is pulverized into fine powder by an ordinary pulverizer;

[0093] (4) Add petroleum ether, chloroform, and ethyl acetate to extract in sequence according to the weight percentage of the extract and petroleum ether, chloroform, and ethyl acetate at 1:20, and wherein the petroleum ether and chloroform extracts obtained are respectively removed by vacuum decompression recovery Solvent, obtain crud...

Embodiment 3

[0097] 1. Preparation of 2,3,4,6,8-pentamethoxy-dibenzofuran

[0098] (1) 5Kg of the root of the natural plant Rosaceae Hawthorn plant Hawthorn is weighed and pulverized, and the pulverization refers to pulverization by a common pulverizer;

[0099] (2) adding the crushed plant fragments to 60L water for reflux extraction for 3 hours to obtain a water extract;

[0100] (3) The extract is filtered with a clarification plate, the filtrate is recovered under vacuum and decompression to remove the solvent, and the weight of the obtained extract is weighed to be 0.38Kg, and the extract is pulverized into fine powder by an ordinary pulverizer;

[0101] (4) Add petroleum ether, chloroform, and ethyl acetate to extract in sequence according to the weight percentage of the extract and petroleum ether, chloroform, and ethyl acetate at 1:20, and wherein the petroleum ether and chloroform extracts obtained are respectively removed by vacuum decompression recovery Solvent, obtain crude pr...

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Abstract

The present invention discloses new type of compounds 2, 3, 4, 6, 8-pentamethoxyl-dibenzofuran extracted from haw root and its medicinal use. These compounds have activity of inhibiting semicarbazide sensitive amine oxidase (SSAO). The raised activity of SSAO is related with several kinds of serious diseases, and in the case of existing transition metal, the deaminated products of SSAO, formaldehyde and hydrogen peroxide, will generate free radicals, the accumulation of which may result in oxidizing damage to human body and cause diseases, such as stress ulcer, atherosclerosis, heart disease, malignant tumor, etc.

Description

Technical field: [0001] The present invention relates to 2,3,4,6,8-pentamethoxy-dibenzofuran and its use, in particular to the new compound 2,3,4,6,8-5 extracted and isolated from natural plants Methoxy-dibenzofuran and its use in inhibiting the activity of semicarbazide-Sensitive Amine Oxidase (SSAO enzyme, Semicarbazide-Sensitive Amine Oxidase) belong to the field of natural medicinal chemistry. Background technique: [0002] 1. Research progress of natural products [0003] What the present invention researches is the root of Hawthorn, a plant of the Rosaceae Hawthorn genus. Hawthorn is distributed in the northern temperate zone, and there are more than 280 species of this genus in the world. Its fruit is a commonly used traditional Chinese medicine. According to the "Compendium of Materia Medica": this product is "sweet and sour, warm in taste, relieves food accumulation, and nourishes the spleen". It is cultivated all over the country and is a homologous plant for me...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D307/91A61K31/343A61K36/734A61P9/10A61P35/00A61P37/02A61K125/00
Inventor 邓玉林徐志慧戴荣继禹玉洪刘洋
Owner BEIJING INSTITUTE OF TECHNOLOGYGY
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