Application of sodium alginate oligose and derivative to treatment of vascular dementia

A technology for oligosaccharides and derivatives of alginate, applied in the directions of sugar derivatives, sugar derivatives, sugar derivatives preparation, etc., can solve the problems of drug application limitation, large molecular weight of alginate, etc.

Active Publication Date: 2017-01-25
GREEN VALLEY (SHANGHAI) PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] However, due to the large molecular weight of alginate, its application in medicine is limited to a certain extent.

Method used

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  • Application of sodium alginate oligose and derivative to treatment of vascular dementia
  • Application of sodium alginate oligose and derivative to treatment of vascular dementia
  • Application of sodium alginate oligose and derivative to treatment of vascular dementia

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] Embodiment 1 Preparation of algin oligosaccharides

[0048] Weigh 1 g of polymannuronic acid sodium salt (weight average molecular weight 8235 Da, provided by Shanghai Green Valley Pharmaceutical Co., Ltd.), and add appropriate amount of distilled water to prepare a 1% (weight percent) aqueous solution of polymannuronate sodium. The pH value of the 1% aqueous sodium polymannuronate solution was adjusted to 4 with hydrochloric acid, and then the aqueous solution was placed in an autoclave. The reaction was heated at 110°C for 4 hours. The reacted solution was taken out from the autoclave and allowed to cool. After cooling, the pH value of the reacted solution was adjusted with NaOH solution to obtain a neutral liquid. Under the condition of stirring, the neutral liquid was slowly added into ethanol in an amount 4 times the volume of the liquid, alcohol precipitation was carried out and the mixture was allowed to stand overnight. The solid matter obtained by alcohol pr...

Embodiment 2

[0050] Example 2 Preparation of algin oligosaccharide oxygen hydrolysis product

[0051] Take 5 g of the above-mentioned crude alginate oligosaccharides that have not been separated by molecular exclusion chromatography to prepare a 5% (weight percent) aqueous solution. Fresh oxidant copper hydroxide was prepared by adding 25 ml of 5% (weight percent) copper sulfate solution to 50 ml of 10% (weight percent) sodium hydroxide solution and mixing immediately. The fresh oxidant copper hydroxide was immediately added to 40ml of the above-mentioned 5% (weight percent) alginate oligosaccharide solution, and heated in a boiling water bath until no brick-red precipitate was produced. The reaction system was centrifuged to remove precipitates to obtain a supernatant. Get a little supernatant and add the oxidizing agent again to check whether there is brick red precipitate. If there is still a brick-red precipitate, then continue to react all the supernatant obtained by the centrifugat...

Embodiment 3

[0053] Example 3 Effect of alginate oligosaccharides on mice with vascular dementia induced by bilateral common carotid artery ligation (BCCAo)

[0054] 1 Experimental materials

[0055] 1.1 Test drugs

[0056] According to the method of Example 2, a mixture of alginic oligosaccharides (n=2-8, ie components 4-10 in the figure) of formula (II) was prepared. The mixture is off-white powder, easily soluble in water; nimodipine is produced by Shandong Health Pharmaceutical Co., Ltd.

[0057] 1.2 Experimental Instruments

[0058] The Morris water maze was designed and manufactured by the Institute of Materia Medica, Chinese Academy of Medical Sciences;

[0059] Brain stereotaxic instrument is a product of Narishige Company in Japan;

[0060] The dark avoidance tester is designed and manufactured by the Institute of Materia Medica, Chinese Academy of Medical Sciences.

[0061] 1.3 Experimental animals

[0062] C57BL / 6 mice, male, weighing 22±2 g, were provided by the Experimen...

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Abstract

The invention relates to application of sodium alginate oligose and a derivative to treatment of vascular dementia. The sodium alginate oligose and the derivative of the sodium alginate oligose are particularly mannuronic acid oligose or mannuronic acid oligose with a carboxyl at a 1-position of a reducing end and the derivative or a pharmaceutically acceptable salt, formed by connecting a beta-D-mannuronic acid through a 1,4-glucosidic bond.

Description

technical field [0001] The invention relates to algin oligosaccharides and derivatives thereof and their application in treating vascular dementia. Background technique [0002] Vascular dementia (VD) is a severe cognitive impairment syndrome caused by cerebrovascular disease. The prevalence of VD in my country is 1.1% to 3.0%, and the annual incidence is 5 to 9 / 1000 people. Its clinical practice mainly focuses on the treatment of primary cerebrovascular diseases and the prevention of VD. For VD patients, vitamin E, vitamin C and ginkgo biloba preparations are mainly used as adjuvant therapy, but there is no good drug for treatment at present. [0003] Alginate is the main component of the cell wall of brown algae. It is a linear anionic polysaccharide formed by connecting β-D-mannuronic acid and α-L-guluronic acid through 1,4-glycosidic bonds. Alginate is a kind of polymer compound with relatively large molecular weight, generally between tens of thousands to several mil...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/7016A61K31/702A61K31/734A61P25/28A61P9/00C08B37/04C07H3/04C07H3/06C07H1/00
Inventor 耿美玉辛现良丁健
Owner GREEN VALLEY (SHANGHAI) PHARM CO LTD
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