High content and high activity oral polysaccharide-peptide and preparing method and application of the same

A technology of versicolor glycopeptide and high activity, which is applied in the field of pharmaceuticals, and can solve the problems of product yield reduction, loss of active ingredients, loss of active glycopeptide, etc., and achieve the effect of simple preparation process, good protective effect and low cost

Inactive Publication Date: 2008-08-27
江苏百草堂药业有限公司 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, its product and its purification process still have three deficiencies: First, although the free protein can be removed by using the Savege method for deproteinization, it inevitably removes some polysaccharide peptides and polysaccharides with physiological activity, resulting in active ingredients Second, the use of ultrafiltration membranes with a molecular weight of 30Kd and 300Kd to cut off and remove substances with a molecular weight less than 30Kd and greater than 300Kd also caused a corresponding loss of active glycopeptides, and the product yield further decreased
Third, after multiple purifications, although the polysaccharide content in the product has increased from 35-40% to more than 75%, the product yield has doubled and the cost has doubled, so it can only be used as a raw material for traditional Chinese medicine for injection, and its Glycopeptides, especially glycopeptide traditional Chinese medicine injections containing some free proteins and a large amount of unknown impurities, inevitably produce allergic reactions and other toxic and side effects during injection administration, which increases the clinical risk of tumor patients

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Take 10kg of Yunzhi glycopeptide, add 100L of water, dissolve and extract at 90°C for 2 hours, adjust the pH to 4-8, and filter through a 0.5μm microporous membrane to obtain a clear extract. The residue was extracted twice, the clarified extracts were combined, concentrated under reduced pressure to a density of 1.2; while stirring, slowly added 3 times the volume of 95% ethanol for precipitation, continued stirring for 1 hour, centrifuged to separate the precipitate, dried under reduced pressure at 60°C, and pulverized , that is, high-content, high-activity oral versicolor glycopeptide. 1g of this glycopeptide can be completely dissolved in 5ml of water, wherein the total amount of glycopeptides is 75.6%, the sugar content is 52.4%, the peptide content is 23.2%, and the polysaccharide peptides with a molecular weight above 10kd account for 84.6% of the total glycopeptides.

Embodiment 2

[0030] Take 10kg polysaccharides of Yunzhi polysaccharide, add 40L water, dissolve and extract at 100°C for 0.5 hours, adjust pH to 4, and centrifuge at 5000 rpm to obtain a clarified extract. Repeat the extraction of the residue 3 times, combine the clarified extracts, concentrate under reduced pressure to a density of 1.05, slowly add 4 times the volume of 80% ethanol to precipitate while stirring, continue stirring for 2 hours, centrifuge to separate the precipitate, and dry under reduced pressure at 50°C. Pulverized, that is high content, high activity oral versicolor glycopeptide. 1g of the glycopeptide can be completely dissolved in 5ml of water, wherein the total amount of glycopeptides is 72.2%, the sugar content is 51.9%, the peptide content is 20.3%, and the polysaccharide peptides with a molecular weight above 10kd account for 81.8% of the total glycopeptides.

Embodiment 3

[0032] Take 10kg of intracellular glycopeptides of Yunzhi, add 200L of water, dissolve and extract at 80°C for 6 hours, adjust the pH to 8, and filter through a 5μm microporous membrane to obtain a clarified extract. Repeat the extraction of the residue once, combine the clarified extracts, concentrate under reduced pressure to a density of 1.3, slowly add 2 times the volume of absolute ethanol to precipitate while stirring, continue stirring for 0.5 hours, filter and separate the precipitate, freeze-dry, and pulverize to obtain the high content, high activity oral versicolor glycopeptide. 1g of the glycopeptide can be completely dissolved in 5ml of water, wherein the total amount of glycopeptides is 75.1%, the sugar content is 50.8%, the peptide content is 24.3%, and the polysaccharide peptides with a molecular weight above 10kd account for 86.8% of the total glycopeptides.

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PUM

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Abstract

The invention relates to a polysaccharide-peptide with high content and high activity, a preparation method thereof and an application thereof. The polysaccharide-peptide is freely soluble in water; the total amount of glycopeptides is equal to or more than 70 percent; the polysaccharide-peptide with the average weight over 10kd takes up more than 80 percent of the total amount of glycopeptides, wherein, the sugar content is 50 to 80 percent, and the peptide content is 16 to 30 percent; the preparation method is as follows: (1) manyzoned polypore crude extract is made available to be suspended or dissolved in the water at the temperature of 80 to 100 DEG C; the manyzoned polypore crude extract solution is refined and separated, or the hot water with the temperature of 80 to 100 DEG C is used for extracting polyporus versicolor mycelium or manyzoned polypore fruit body for producing the manyzoned polypore crude extract solution; (2) the pH value of the manyzoned polypore crude extract solution or the manyzoned polypore crude extract suspended solution is controlled to be between 4 to 8; the lauter extracting solution can be obtained after filtering or centrifugal separation, which is concentrated to the specific gravity of 1.05 to 1.3; (3) a decoction and alcohol sedimentation method is used for purification. Compared with prior polysaccharide-peptide, the product obtained has more effective anti-tumor effect and better protective effect on marrow function and immune function, which are suitable for preventing and treating tumors.

Description

technical field [0001] The invention belongs to the field of medicines, and in particular relates to an orally absorbed high-content and high-activity versicolor glycopeptide, a preparation method and application thereof. Background technique [0002] Yunzhi glycopeptide is a crude glycopeptide extracted from Yunzhi submerged mycelium by water extraction and alcohol precipitation. It is one of the few glycopeptide immune enhancers that can be orally absorbed. It can inhibit the proliferation of various cancer cells such as human lung cancer, gastric cancer, esophageal cancer, leukemia, ascites cancer, etc. At the same time, it can effectively improve human immune function, increase appetite, relieve pain, improve hypoxia resistance, and reduce toxic and side effects caused by radiotherapy and chemotherapy , has been marketed as an adjuvant therapy drug for tumors in China. Chinese patent 89105471.5 reports "a production method of versicolor glycopeptide", the extraction met...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/14A61K36/06A61K9/14A61K9/20A61K9/16A61K9/48A61K9/10C07K1/30C07K1/34C07K1/16A61P35/00A61P37/04
Inventor 袁萍茅仁刚张雷张华周海宾刘瑶
Owner 江苏百草堂药业有限公司
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