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Low-molecular-weight fucosylated chondroitin sulfate, preparation method thereof and application of low-molecular-weight fucosylated chondroitin sulfate to preparation of medicine for resisting Trousseau syndrome

A chondroitin sulfate and fucosification technology, which is applied in the application field of medicine, can solve the problem that no relevant reports have been reported on the research and application of fucosylated chondroitin sulfate, the pH of the reaction system is unstable, and the content of fucose sulfate is reduced. To achieve the effect of inhibiting lung metastasis, relieving Trusseau syndrome, and easy to prepare in large quantities

Inactive Publication Date: 2017-01-25
OCEAN UNIV OF CHINA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] There are many literatures and patents on the extraction, separation and preparation of fucosylated chondroitin sulfate, such as: Chinese patent application (publication number CN102993327A) and Chinese patent application (publication number CN101624426A) both disclose enzymatic extraction of fucosylated chondroitin sulfate method, but the product has high molecular weight, unclear structure and low bioavailability
Fucosylated chondroitin sulfate can be depolymerized by physical or chemical methods to obtain low molecular weight fucosylated chondroitin sulfate, which can reduce the hemorrhagic side effects of fucosylated chondroitin sulfate and improve its bioavailability, such as: Chinese patent application (publication number CN103285031A) discloses a method for preparing low-molecular-weight fucosylated chondroitin sulfate by free radical degradation. Reduced sugar sulfate content, thereby reducing various biological activities
Although the Chinese patent (publication number CN101057859A and publication number CN104147040A) discloses the application of fucosylated chondroitin sulfate in the preparation of antithrombotic drugs, but about low molecular weight fucosylated chondroitin sulfate in the anti-Trousseau's syndrome (Trousseau's syndrome) There are no relevant reports on the research and application of

Method used

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  • Low-molecular-weight fucosylated chondroitin sulfate, preparation method thereof and application of low-molecular-weight fucosylated chondroitin sulfate to preparation of medicine for resisting Trousseau syndrome
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  • Low-molecular-weight fucosylated chondroitin sulfate, preparation method thereof and application of low-molecular-weight fucosylated chondroitin sulfate to preparation of medicine for resisting Trousseau syndrome

Examples

Experimental program
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Effect test

Embodiment 1

[0048] Example 1: Preparation of low molecular weight fucosylated chondroitin sulfate

[0049] 1. Take 100 g of North Atlantic dried sea cucumber, homogenize it, defat it, add 0.1 mol / L NaOH solution, stir and react at 50 ℃ for 3 h;

[0050] After cooling at room temperature, add hydrochloric acid to neutralize, add 500 mg papain, 5 mmol / L Na 2 EDTA solution and 5 mmol / L cysteine ​​solution were stirred and reacted at 50 °C for 12 h;

[0051] Combine the extracts, add 3 times the volume of 95% ethanol to precipitate, centrifuge, wash the precipitate 3 times with 95% ethanol and absolute ethanol, and dry at 60 °C;

[0052] Take the dried sample, add appropriate amount of water to dissolve, add 0.1 mol / L KOH solution to adjust the pH to 9, add 30% H 2 o 2 , decolorize at 30°C for 2 h;

[0053] After the reaction solution was cooled, hydrochloric acid was added to adjust the pH to 1-2, and the precipitate was removed by centrifugation;

[0054] Add 95% ethanol until the alco...

Embodiment 2

[0062] Example 2: The effect of low molecular weight fucosylated chondroitin sulfate against Trusso syndrome

[0063] 1. Passage Lewis lung cancer cells in vivo: Take Lewis lung cancer cells in the logarithmic growth phase, digest with 0.25% trypsin, and adjust to 1×10 with normal saline 7 cells / ml of single-cell suspension, and inoculated 0.2 ml subcutaneously in the right axillary of mice. 10 days after inoculation, take the Lewis lung cancer solid tumor under sterile conditions, make a single cell suspension according to the ratio of tumor block (g): normal saline (ml) 1:3, take 0.2 ml (containing tumor cells 2×10 6 ) were inoculated subcutaneously in the right axilla of C57BL / 6J mice, and passaged ten times in vivo.

[0064] 2. Replication and experiment of animal model: take the Lewis lung cancer solid tumor that has been passaged ten times in vivo under sterile conditions, make a single-cell suspension according to the ratio of tumor mass (g): normal saline (ml) at 1:3...

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Abstract

The invention provides low-molecular-weight fucosylated chondroitin sulfate, a preparation method thereof and application of the low-molecular-weight fucosylated chondroitin sulfate to the preparation of medicine for resisting Trousseau syndrome. Sulfated polysaccharide with the main chain using beta-1,4-D-glucuronic acid and beta-1,3-D-acetamino galactose as disaccharide repeating units and the branch chain being alpha-1,3-L-fucus oligosaccharide sulfate. Experiments show that the fucosylated chondroitin sulfate has an evident inhibiting effect on the Trousseau syndrome. The fucosylated chondroitin sulfate is rich in raw material source, simple in preparation process, easy in industrialization, high in product safety, good in stability, unique in activity, promising in technical prospect in the development of medicine for resisting the Trousseau syndrome, and the like.

Description

technical field [0001] The invention belongs to the field of marine medicines, and relates to a low-molecular-weight fucosylated chondroitin sulfate, a preparation process thereof, and an application in preparation of anti-Trusau syndrome medicines. Background technique [0002] Cardiovascular and cerebrovascular thrombotic disease is the number one killer of human health. With the improvement of people's living standards, its incidence rate is also increasing year by year, and it is showing a younger trend. According to the American Heart Association (AHA) 2016 academic annual meeting report, between 2003 and 2013, about 1 / 3 of patients who died of diseases each year died of cardiovascular and cerebrovascular diseases. About 2 million people die of cardiovascular and cerebrovascular diseases in my country every year, and more than 3 million people need thrombolytic therapy. Malignant tumors are the second cause of human death in today's society. The World Health Organizat...

Claims

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Application Information

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IPC IPC(8): C08B37/08A61K31/737A61P7/02A61P35/00A61P35/04
CPCA61K31/737C08B37/0069
Inventor 于广利刘潇潇郝杰杰蔡超李国云李芹英
Owner OCEAN UNIV OF CHINA
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