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Alkaloid compounds, preparation method and application thereof

A technology for medicines and preparations, applied in the field of alkaloid compounds and their effective parts, can solve the problems of easy generation of tolerance and addiction, and achieve the effects of affirmative drug efficacy, controllable quality, and simple and easy separation process

Inactive Publication Date: 2010-11-03
PHARMA FACTORY GUANGXI MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, the drugs for treating insomnia are mainly benzodiazepines. Although the curative effect is good, they are prone to tolerance and long-term use will cause addiction.

Method used

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  • Alkaloid compounds, preparation method and application thereof
  • Alkaloid compounds, preparation method and application thereof
  • Alkaloid compounds, preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0064] 1 kg of cat bean coarse powder, add 10 times the amount of 0.1mol / L sulfuric acid solution and soak for 15 hours, shake it from time to time to obtain the extract, filter with suction, concentrate the filtrate under reduced pressure, and use the concentrated solution to pass through a strong acidic cation exchange resin column (weaker cation exchange resin column can also be used) Acidic cation exchange resin, strong basic or weak basic anion exchange resin) adsorption, wash with 0.1% ammonia water and elute, collect the eluate containing compound I, concentrate under reduced pressure, dry to obtain refined extract and effective fraction . The refined extract or effective part is dissolved, and the strong acidic cation exchange resin chromatography column (weak acidic cation exchange resin, strong basic or weak basic anion exchange resin can also be used), and 0.1% ammonia water is eluted to obtain compound I.

Embodiment 2

[0066] Add 5 times the amount of 0.1mol / L hydrochloric acid solution to immerse for 5 hours, then use 15 times the amount of 0.1mol / L hydrochloric acid solution to percolate, collect the percolation liquid, suction filter, concentrate under reduced pressure, and concentrate Super-strongly acidic cation exchange resin column (weakly acidic cation exchange resin, strongly basic or weakly basic anion exchange resin can also be used) adsorption, wash with 0.1% sodium hydroxide after washing, collect the eluate containing compound I, reduce Concentrate under pressure and dry to obtain refined extracts and effective fractions. The refined extract or effective part was dissolved, subjected to silica gel column chromatography, eluted with methanol, and compound I was isolated.

Embodiment 3

[0068] Add 15 times the amount of cat bean coarse powder and soak it in an acidic ethanol solution for 10 hours, shake it from time to time to obtain an extract, filter it with suction, concentrate the filtrate under reduced pressure, and dry to obtain a crude extract, which is subjected to silica gel column chromatography. Elute with methanol or ethanol, collect the eluate containing compound I, concentrate under reduced pressure, and dry to obtain a refined extract and effective fraction. The refined extract or effective fraction was dissolved, subjected to silica gel column chromatography, and eluted with different gradient mixed solvents of chloroform-methanol-water or ethyl acetate-methanol-water to obtain compound I.

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PUM

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Abstract

The invention relates to an alkaloid compound extracted and prepared from a cat bean and a valid target, wherein, the cat bean is used as a raw material, the valid target is obtained through crushing, solvent extraction, separation and purification by resin or silica gel column chromatography and other methods, and the compound, 1, 2-dihydro-3-guanido-6-hydroxymethyl-1-methylpyrazine-2-ketone, namely cat-bean guanidine, is obtained by separation of the valid target. Pharmacodynamical experiments prove that: the compound has sedative-hypnotic function, and can be used as a pharmaceutical and chemical raw material and be prepared into sedative-hypnotic preparation.

Description

Technical field: [0001] The invention belongs to the fields of natural medicinal chemistry and medicine, and relates to an alkaloid compound extracted and prepared from cat bean, its effective part and its application in sedative and hypnotic effects. Background technique: [0002] Cat bean is the seed of Stizolobium cochinchinensis (Lour) Tang et Wang, a plant of the leguminous genus Stizolobium cochinchinensis (Lour) Tang et Wang. It is a characteristic medicinal and edible resource and a commercial crop in Guangxi. Cat bean is the most important raw material for extracting levodopa. Extracting levodopa from cat bean has become the main source of levodopa raw material in the world. The research on the key technology of high-purity and efficient extraction of levodopa completed by the applicant has been transformed, making Guangxi an international production base of levodopa. The research on other chemical components of cat bean is of great significance to the extension of...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D241/20A61K31/4965A61K36/48A61P25/20
Inventor 蒋伟哲黄增琼黄兴振黄敏巫世红吕立李迪王健
Owner PHARMA FACTORY GUANGXI MEDICAL UNIV
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