Preparation method and application of coumarin glycoside compounds

A technology for coumarin glycosides and compounds, applied in the field of medicine, can solve problems such as no public reports, and achieve the effects of remarkable economic and social benefits, good reproducibility and simple preparation method

Inactive Publication Date: 2019-06-18
HENAN UNIV OF CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The coumarin glycoside compounds involved in the present invention and their biological activity have not been reported so far

Method used

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  • Preparation method and application of coumarin glycoside compounds
  • Preparation method and application of coumarin glycoside compounds
  • Preparation method and application of coumarin glycoside compounds

Examples

Experimental program
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Embodiment 1

[0012] In the specific implementation of the present invention, a method for preparing coumarin glycoside compounds is made from 20 kg of small bark bone as raw material, and the weight of the raw material and the volume ratio of 95% ethanol are heated and refluxed at 90°C for 3 times. The extraction time is 1 hour each time. The ethanol is recovered under reduced pressure to obtain the extract-like ethanol extract, which is suspended in 4.8L of distilled water, and extracted with petroleum ether, ethyl acetate and n-butanol for 3 times, 4.8L each time , The time is 1.5 hours; the extraction part of n-butanol is separated by AB-8 macroporous adsorption resin column chromatography, and the volume ratio is 0:100, 30:70, 95:5 ethanol-water mixed solvent for gradient elution. Use 5.0L eluent for each gradient with a flow rate of 10mLmin -1 , The water eluate was discarded, and the eluted fractions with volume ratios of 30:70 and 95:5 ethanol-water were collected. After concentration...

Embodiment 2

[0014] In the specific implementation of the present invention, a method for preparing coumarin glycoside compounds is made from 15 kg of small bark bone, and extracted 3 times with 3 times the weight of the raw material and 75% volume concentration of ethanol at 95°C under reflux, each time The extraction time is 1 hour. The ethanol is recovered under reduced pressure to obtain the extract-like ethanol extract, which is suspended in 3.6L of distilled water, and extracted with petroleum ether, ethyl acetate and n-butanol three times, 3.6L each time. It is 1.5 hours; the extraction part of n-butanol is separated by AB-8 macroporous adsorption resin column chromatography, and the volume ratio is 0:100, 30:70, 95:5 ethanol-water mixed solvent for gradient elution, each The gradient uses 3.8L eluent, the flow rate is 5mLmin -1 , The water eluate was discarded, and the eluted fractions with volume ratios of 30:70 and 95:5 ethanol-water were collected. After concentration under reduce...

Embodiment 3

[0016] In the specific implementation of the present invention, a method for preparing coumarin glycoside compounds is made from 18kg of small bark bone, and extracted 3 times with 4 times the weight of the raw material and 85% volume concentration of ethanol at 92°C under reflux, each time The extraction time is 1 hour. The ethanol is recovered under reduced pressure to obtain the extract-like ethanol extract, which is suspended in 4.5L of distilled water, and extracted with petroleum ether, ethyl acetate and n-butanol three times, 4.5L each time. It is 1.5 hours; the extraction part of n-butanol is separated by AB-8 macroporous adsorption resin column chromatography, and the volume ratio is 0:100, 30:70, 95:5 ethanol-water mixed solvent for gradient elution, each The gradient uses 4.5L eluent, the flow rate is 8mLmin -1 , The water eluate was discarded, and the eluted fractions with volume ratios of 30:70 and 95:5 ethanol-water were collected. After concentration under reduced...

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Abstract

The invention relates to a preparation method and an application of coumarin glycoside compounds and can effectively solve the problems about preparation of novel coumarin glycoside compounds with liver protection activity and the application of the coumarin glycoside compounds in preparation of liver protection drugs. The novel coumarin glycoside compounds with the liver protection activity are genglycoside A I, genglycoside B II and genglycoside D III which are separated from the medicinal material of common gendarussa herb. The preparation method is simple, the reproducibility is good, theobtained compounds have high purity and are favorable for further pharmacological and clinical research, the prepared novel coumarin glycoside compounds with the liver protection activity, namely, genglycoside A I, genglycoside B II and genglycoside D III, are effectively used for preparing the liver protection drugs, a new way of the liver protection drugs and medicinal value and commercial valueof the common gendarussa herb are opened up, and the economic and social benefits are remarkable.

Description

Technical field [0001] The invention relates to medicine, in particular to a preparation method and application of a coumarin glycoside compound of a novel coumarin glycoside compound with anti-protective activity. Background technique [0002] The liver converts a variety of endogenous or exogenous toxic substances in the human body into non-toxic or low-toxic substances through oxidation, reduction, and hydrolysis, and is an important metabolic organ. The liver is susceptible to viruses, drugs, poisons, and immunopathological factors. For example, long-term living in a toxic environment or excessive alcohol consumption can induce various liver diseases, which will lead to liver damage. Liver injury is the direct cause of hepatitis, cirrhosis and liver cancer. The clinical incidence is increasing year by year. It has become one of the main diseases that seriously endanger human health in the world. At present, the important cause of the disease is generally considered to be the...

Claims

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Application Information

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IPC IPC(8): C07H17/065C07H1/08A61P1/16
Inventor 孙彦君高美玲陈豪杰冯卫生韩瑞杰崔卫东赵晨弓建红王俊敏刘延霆陈辉郝志友赵悦亮
Owner HENAN UNIV OF CHINESE MEDICINE
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