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Sulphonated Gleditia sinensis Lam polysaccharide and application thereof

A technology of sulfation and acacia, which is applied in the directions of medical preparations containing active ingredients, organic active ingredients, antiviral agents, etc., can solve the problems of high and low anti-HIV activity, and the sulfated acacia polysaccharide has not yet been reported.

Inactive Publication Date: 2010-12-29
YUNNAN UNIV OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the complexity of the polysaccharide structure, the anti-HIV activity of the sulfated modification of a certain polysaccharide varies.
So far, there have been no reports on the sulfated acacia polysaccharides obtained from plant acacia polysaccharides through the esterification of sulfonating agents and their strong anti-HIV effects, and the application of sulfated acacia polysaccharides has not yet been reported.

Method used

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  • Sulphonated Gleditia sinensis Lam polysaccharide and application thereof
  • Sulphonated Gleditia sinensis Lam polysaccharide and application thereof
  • Sulphonated Gleditia sinensis Lam polysaccharide and application thereof

Examples

Experimental program
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Embodiment 1

[0019] Embodiment one: a kind of preparation method of compound of the present invention

[0020] Take 80 mL of sulfonating agent (chlorosulfonic acid: pyridine = 1: 8) and place it in a 250 mL three-necked flask, control the temperature at 75° C., add 8 grams of acacia (Gleditiasinensis Lam) polysaccharide, stir and react for 12 hours, take out the flask after the reaction and cool to room temperature. Neutralize with 6M NaOH solution, precipitate with ethanol, centrifuge, dissolve the precipitate in distilled water and dialyze in distilled water, distill and concentrate the inner liquid of the dialysate under reduced pressure, precipitate with ethanol, centrifuge, and dry to obtain the saponins polysaccharide sulfate ester of the present invention. The molecular weight of the product is 7.9 ×10 4 Daltons, sulfation degree 1.0. Analysis by HPLC showed that the sulfated saponins polysaccharide was composed of galactose and mannose, and the composition ratio was 1:4. Accordin...

Embodiment 2

[0021] Embodiment two: the pharmacological effect of sulfated saponins of the present invention

[0022] 1. Anti-HIV-1IIIB (X4 virus) activity of sulfated saponins polysaccharides in vitro

[0023] On a 96-well culture plate, make 5-fold dilutions of the stock solution of the sulphated saponins to be tested, and make 8 gradients in total, with 4 wells for each gradient, 100 μl per well, and set AZT positive control group and blank control group at the same time . Then, 50 μl (2×104 / well) of C8166 cells (a T lymphocyte line, donated by British Medical Research Council (MRC), AIDS Reagent Project) and HIV-1 cells were added to each well. IIIB (H9 / HIV-1IIIB, donated by the British MRC, resuscitated, cultured, collected, aliquoted and frozen according to conventional methods) virus 20 μl (MOI value 0.2), supplemented with complete medium to make the final volume of each well 200 μl. 37°C, 5% CO 2 to cultivate. On the third day, 100 μl of fresh complete medium (RPMI-1640) was a...

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Abstract

The invention relates to a sulphonated Gleditia sinensis Lam polysaccharide with bioactivity and application thereof. The sulphonated Gleditia sinensis Lam polysaccharide is characterized in that a polysaccharide chain contains galactose and mannose, a main chain is D-mannopyranose connected through a beta-(1,4)-glucosidic bond, a branched chain is D-galactopyranose connected through an alpha-(1,6)- glucosidic bond, and the degree of esterification is between 0.1 and 1.7. The sulphonated Gleditia sinensis Lam polysaccharide provided by the invention is obtained by utilizing a sulphonating agent to process a hot water extract of Gleditia sinensis Lam; and the sulphonating method thereof comprises the following steps: adding Gleditia sinensis Lam polysaccharide into the sulphonating agent, reacting while controlling the temperature and stirring, taking out a flask after the reaction is finished, cooling to room temperature, neutralizing by utilizing a NaOH solution, carrying out precipitating and washing for several times by utilizing ethanol, carrying out dialysis in distilled water, carrying out reduced pressure distillation on the dialysate, precipitating by utilizing absolute ethyl alcohol, and drying the precipitation in vacuum to obtain the sulphonated Gleditia sinensis Lam polysaccharide, wherein the sulphonating agent consists of chlorosulfonic acid and formamide or pyridine at the volume ratio of 1:5-10. The sulphonated Gleditia sinensis Lam polysaccharide obtained in the invention has higher substitution degree, stronger activity for resisting human AIDS viruses and herpes simplex viruses and low toxicity to human cells, and can be used for preparing a preparation of preventing or curing human AIDS virus and herpes simplex virus infection.

Description

technical field [0001] The invention relates to a biologically active sulfated acacia polysaccharide and its use. The sulfated acacia polysaccharide not only has a high degree of substitution, but also has strong anti-human HIV and herpes simplex virus activity, low toxicity, and is useful in preparing preparations for preventing or treating human HIV and herpes simplex virus infection. Very good application prospects. Background technique [0002] AIDS is Acquired Immunodeficiency Syndrome (AIDS), which is a fatal infectious disease caused by Human Immunodeficiency Virus (HIV). Since the first case was discovered in 1981, AIDS has spread rapidly around the world, seriously threatening human life. By the end of 2004, more than 40 million people around the world were infected with HIV. In 2004 alone, there were about 5 million new HIV infections, and about 3 million AIDS patients died. Since the first report of AIDS cases in my country in 1985, the prevalence of AIDS has s...

Claims

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Application Information

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IPC IPC(8): C08B37/00A61K31/737A61P31/18A61P31/22
Inventor 赵声兰贲昆龙陈朝银李汝润陶剑曹筱梅
Owner YUNNAN UNIV OF TRADITIONAL CHINESE MEDICINE
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