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Anti-tumor activating fuling scloerotium glucan sulfate and its preparation and use

A technology of dextran sulfate and antitumor activity, applied in the fields of polymer chemistry and molecular biology, can solve the problems of few reports on derivatization modification, achieve good application prospects, short production cycle, simple and easy production process row effect

Inactive Publication Date: 2005-02-23
WUHAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there are few reports on other derivatized modifications of Poria cocos sclerotran

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Fresh Poria sclerotia were collected from Jiuzihe Town, Luotian County, Hubei Province. The sclerotia were successively refluxed with ethyl acetate and acetone for 6 hours respectively for Soxhlet extraction to remove fat. Then soak in normal saline to extract and centrifuge; the residue after centrifugation is extracted with hot water at 120°C at 0.20Mpa and centrifuged; the residue after centrifugation is washed with 0.5M NaOH (containing 0.05% NaBH 4 ) at 4°C to obtain polysaccharides, which are white powdery solids. Gas chromatography, infrared spectroscopy and13 Its structure was detected by C NMR spectrum, etc., which proved that it was a high-purity linear (1→3)-β-D-glucan.

[0039] Dissolve 600 mg of the above Poria cocos sclerotium (1→3)-β-D-glucan in 50 mL of DMSO, stir at room temperature for 12 hours, then add 9 mL of pyridine dropwise at a rate of 0.8 mL / min, and continue stirring at room temperature 30 minutes. The reaction flask was placed in an ice ba...

Embodiment 2

[0041] Fresh Poria sclerotia were collected from Jiuzihe Town, Luotian County, Hubei Province. The sclerotia were refluxed with ethyl acetate and acetone for 5 hours respectively for Soxhlet extraction to remove fat. Then soak in normal saline to extract and centrifuge; the residue after centrifugation is extracted with hot water at 120°C at 0.20Mpa and centrifuged; the residue after centrifugation is washed with 1M NaOH (containing 0.1% NaBH 4 ) at 5° C. to obtain polysaccharides, which are white powdery solids. Gas chromatography, infrared spectroscopy and 13 Its structure was detected by C NMR spectrum, etc., which proved that it was a high-purity linear (1→3)-β-D-glucan.

[0042] Dissolve 600 mg of the above Poria cocos sclerotium (1→3)-β-D-glucan in 50 mL of DMSO, stir at room temperature for 16 hours, then add 9 mL of pyridine dropwise at a rate of 1.0 mL / min, and continue stirring at room temperature 25 minutes. The reaction flask was placed in an ice bath, and 3.7 ...

Embodiment 3

[0044] Fresh Poria sclerotia were collected from Jiuzihe Town, Luotian County, Hubei Province. The sclerotia were successively refluxed with ethyl acetate and acetone for 6 hours respectively for Soxhlet extraction to remove fat. Then soak in normal saline to extract and centrifuge; the residue after centrifugation is extracted with 105°C hot water at 0.12Mpa and centrifuged; the residue after centrifugation is washed with 0.5M NaOH (containing 0.05% NaBH 4 ) at 4°C to obtain polysaccharides, which are white powdery solids. Gas chromatography, infrared spectroscopy and 13 Its structure was detected by C NMR spectrum, etc., which proved that it was a high-purity linear (1→3)-β-D-glucan.

[0045] Dissolve 600 mg of the above Poria cocos sclerotium (1→3)-β-D-glucan in 50 mL of DMSO, stir at room temperature for 12 hours, then add 9 mL of pyridine dropwise at a rate of 1.0 mL / min, and continue stirring at room temperature 30 minutes. The reaction flask was placed in an ice bat...

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Abstract

An anti-tumour activated Tuckahoe sclerotium glucan sulfuric is prepared by: taking fresh Tuckahoe sclerotium, extracting non-water soluble (1->3)-beta- D- glucan with NaOH, solving them in anhydrous dimethylsulfoxide, adding pyridine and chloro-sulfonic acid to react to get glucan sulfuric ester. The glucan sulfuric ester's substituted reaction is of non-selective substitution, occurred at C-6 position of hydroxy, the substitution value of sulfuric ester is 0.66- 1.21, weight-average molecular weight is 0.8X104-16.4X104, and has well water solubility. Testing in vivo and in vitro showed that, the glucan sulfuric ester has obvious inhibit effect for Sarcoma 180 and proliferation of adenocarcinoma of stomach. The toxic testing in small rat prove that half lethal dose of glucan sulfuric ester (LD50)>1600 mg / kg, and without toxic or side effects. The Tuckahoe sclerotium glucan sulfuric ester is capable of use in preparing anti-tumour pharmaceuticals or health food with function of increasing body immunological competence.

Description

technical field [0001] The present invention relates to Poria cocos sclerotin sulfate ester with anti-tumor activity and its preparation method and application. It belongs to the field of polymer chemistry and also belongs to the field of molecular biology. Background technique [0002] Recent studies have shown that fungal polysaccharides have significant curative effects on many diseases that endanger human health, such as immune disorders, cancer, diabetes, hypertension, hepatitis, and hyperlipidemia. However, the main component extracted from Poria cocos sclerotia is (1→3)-β-D-glucan, but it is insoluble in water and basically inactive. It is possible to improve water solubility and biological activity by modifying its structure through derivatization reactions. Chihara et al. (Nature, 225,943, 1970) chemically modified the Poria cocos glucan (Pachyman) extracted from Poria cocos through periodic acid oxidation, sodium borohydride reduction and mild hydrolysis to obtai...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/716A61P35/00C08B37/02
Inventor 张俐娜王艺峰侯晓华李云桥
Owner WUHAN UNIV
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