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Sulfonated changium root polysaccharides and preparing method and use thereof

A technology of polysaccharide sulfuric acid and esterification, which is applied in the direction of drug combinations, pharmaceutical formulas, and medical preparations containing active ingredients, etc., and can solve the problems of increased anti-/01 activity, insufficient content, and low activity

Inactive Publication Date: 2006-10-11
NANJING UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In vivo and in vitro experiments, sulfated polysaccharides have shown good antiviral effects, but the immune-promoting activity of sulfated polysaccharides is considered to be one of the important mechanisms of antiviral and anti-tumor effects in the overall situation. Therefore, Japanese scholars have studied discovered the natural sulfated polysaccharide in seaweed, and found that it has anti-tumor effect in vivo, but it has no effect in vitro (Tian Gengyuan, Li Shoutong, Song Maili, et al. Synthesis and antiviral activity of Achyranthes bidentata polysaccharide sulfate [J]. Acta Pharmaceutica Sinica, 1995 , 30(2):107-111)
[0006] Natural heparin has anti-HIV-1 activity, but the activity is very low. Although its anticoagulant activity can be removed by chemical structure modification, it does not help to improve the anti-HIV-1 activity. This is because SO 4 2- Insufficient content, it is generally believed that each monosaccharide unit needs 2~3 SO 4 2- , in order to have good anti-HIV-1 activity, which has aroused great interest of pharmacologists and microbiologists

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Embodiment 1: the preparation method of Mingtangshen polysaccharide sulfate ester, the steps of its preparation method are as follows:

[0029] (1) Extraction of Codonopsis polysaccharide:

[0030] Take Ming Codonopsis medicinal material, knock it into small pieces, weigh 500g and put it in a flask, add 4000ml of 95% ethanol to soak for 1.5h, then reflux on a water bath for 3h, filter, and filter the residue once as above, then filter again, and dry the filter residue, Add 4000ml of distilled water and boil for 2h, pour out the extract, and centrifuge; add 2000ml of distilled water to the filter residue and boil for 2h, pour out the extract, and centrifuge (3000r·min -1 ) for 20 minutes, discard the precipitate, combine the supernatant, and put it in the refrigerator overnight;

[0031] Suction filter the extract in the refrigerator, place the filtrate in two 5000ml large beakers, heat on a water bath, concentrate, stop heating when solids are about to appear, add 0.6 ...

Embodiment 2

[0033] Embodiment 2: the preparation method of Mingtangshen polysaccharide sulfate ester, the steps of its preparation method are as follows:

[0034] (1) Extraction of Codonopsis polysaccharide, same as Example 1;

[0035] (2) Sulfation of polysaccharides: Measure 75ml of concentrated sulfuric acid and 25ml of n-butanol, put them in a 500ml three-necked bottle with a drying tube and a stirring device, add 1.25g of ammonium sulfate, stir, and cool in an ice bath to 0°C , slowly add 10g of 50% alcohol-precipitated polysaccharide (B) powder, react at 0°C for 120 minutes, neutralize the reaction solution with NaOH to PH7, centrifuge and dialyze with distilled water for 24 hours, concentrate under reduced pressure, alcohol-precipitate, let stand and centrifuge to collect the precipitate The product is the sulfated product (B1), and it is 62.35% through the determination of sulfate group content.

Embodiment 3

[0036] Embodiment 3: the preparation method of Mingtangshen polysaccharide sulfate ester, the steps of its preparation method are as follows:

[0037] (1) Extraction of Codonopsis polysaccharide, same as Example 1;

[0038] (2) Sulfation of polysaccharides: Measure 75ml of concentrated sulfuric acid and 25ml of n-butanol, put them in a 500ml three-necked bottle with a drying tube and a stirring device, add 1.25g of ammonium sulfate, stir, and cool in an ice bath to 0°C , slowly add 10g of 70% alcohol-precipitated polysaccharide (C) powder, and react at 0°C for 120 minutes. After neutralization and centrifugation, the reaction solution is dialyzed with distilled water for 24 hours, concentrated under reduced pressure, alcohol-precipitated, and the precipitate is collected by centrifugation. The sulfated product (C1) was determined to be 40.16% by sulfate group content.

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Abstract

In this invention, we extract raw polysaccharides from changium root named A B C respectively, and purify to get 6 polysaccharides I,II,III,IV,V,VI. After sulfation, we get sulfated polysaccharides A1, B1,C1. A1 has two sulfate groups on each monosaccharide at the average while B1 and C1 have three. The sulfated polysaccharides' molecular weight is more than 2 million D. The glycoside link is alpha type. The whole procedure of changium root sulfated polysaccharides is as followings: extract raw polysaccharides from changium root, and then get the polysaccharides sulfated. It is advantageous in simplied-manipulation and low cost. The pharmacological experiments prove its obvious suppression on rat transplanting tumor(S-180) and the reduction of platelet aggregation ratio and whole blood viscosity. It also reduces coagulant time.

Description

1. Technical field [0001] The invention relates to a natural polysaccharide sulfate, in particular to a sulfated polysaccharide extracted from Mingdangshen and its preparation method and application. 2. Background technology [0002] Mingdangshen is the dry root of Changium smyrnioides Wolff, a single species of Umbelliferae. It has been used as a medicine since the Ming and Qing Dynasties, and it is used to "invigorate the lungs and move downward" ("Materia Medica Congxin"); "to treat dizziness and general evil, stroke and fainting" ("New Ginseng of Decoction Pieces"); it is recorded in "Chinese Pharmacopoeia", which is called: " Nourishes the lungs and resolves phlegm, nourishes yin and harmonizes the stomach, calms the liver, and detoxifies." Ming Codonopsis is a commonly used traditional Chinese medicine recorded in the "Chinese Pharmacopoeia". It is a specialty in Jiangsu. It is an authentic medicinal material production area and has the reputation of "Done Peak Ming P...

Claims

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Application Information

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IPC IPC(8): C08B37/00A61K31/715A61P35/00A61P7/02
Inventor 李祥陈建伟
Owner NANJING UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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