Polysaccharide sulfate selenide compound and its preparation method and application

A technology of polysaccharide sulfate and selenized polysaccharide, which is applied in the direction of drug combination, antineoplastic drugs, etc., can solve the problems of cumbersome preparation and low selenium content, and achieve the effect of a wide range of physiological functions

Inactive Publication Date: 2008-01-16
陈艺新
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  • Polysaccharide sulfate selenide compound and its preparation method and application
  • Polysaccharide sulfate selenide compound and its preparation method and application

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Embodiment 1

[0032] Example 1 In vitro detection of selenated polysaccharide sulfate anticancer drug susceptibility test by MTT method

[0033] Cells in the logarithmic growth phase were diluted to 2.0×106 cells mL-1 with RPMI-1640 medium containing 10% fetal bovine serum, inoculated in a 96-well plate, 100 μL per well, and then added the drug to be tested and the negative control in sequence group, positive control group, and keep the blank group with medium only. Subsequently, culture was continued for 24 hours in an incubator at 37° C. and 5% CO 2 , and then 10 μL of 5 mg·mL −1 MTT solution was added to each well, and culture was continued for 4 hours. Aspirate the supernatant, add 100 μL of DMSO to each well, and measure the absorbance (A) value with a microplate reader at a wavelength of 570 nm. Calculate the cell proliferation inhibition rate with the following formula, and use the formula T / C (%)=100×A 阴性 / A 样品 The half inhibitory concentration (IC50) inhibitory rate=(A 空白 -A 给...

Embodiment 2

[0035] Embodiment 2 antioxidant activity research

[0036] 1. to O 2 · The scavenging effect

[0037] Contains selenated polysaccharide sulfate (1mg·mL -1 ) Tris-HCl buffer solution of pH 8.2 was incubated at 25°C for 20 minutes, and 0.1mol·L -1 10mmol·L of pyrogallol -1 Hydrochloric acid solution, shake quickly, measure the absorbance at 319nm at 25°C, and continuously measure A p .

[0038] Do not add selenized polysaccharide sulfate, operate as above, measure its contrast absorbance value A s . The test showed that the absorbance A p Relative Absorbance A s reduce.

[0039] The results showed that: selenized polysaccharide sulfate can effectively scavenge active oxygen.

[0040] 2. Scavenging effect on hydroxyl radicals and protecting DNA

[0041]Using Fenton system, take 0.2mL F eSO4-EDTA mixed solution (10mmol L -1 ) into the test tube, add 0.5mL of DNA (10mmol·L -1 ), then add selenated polysaccharide sulfate (1mg·mL -1 ), with phosphate buffer (pH 7.4, 0.1...

Embodiment 3

[0044] The chemical synthesis of embodiment 3 polysaccharide sulfate.

[0045] in N 2 Under protection, 1 g of polysaccharide was added into 150 mL of tetrahydrofuran (N, N-dimethylformamide, DMF), and stirred at room temperature for 14 h. N 2 Under protection, sulfur trioxide·pyridine was added while stirring (the molar ratio of sulfur trioxide·pyridine to hydroxyl groups in the polysaccharide was 10:1), and then reacted at 40°C for 10 h. Crude polysaccharide sulfate pyridinium salt was prepared by treating with 500 ml of methanol and stirring for 1 hour. Filter with a sintered glass funnel equipped with an aspirator, and wash with methanol continuously until the filtrate becomes colorless, and dry in the air. The crude polysaccharide sulfate pyridinium salt was dissolved in 6.5 ml of 30% sodium acetate solution; 7 ml of double distilled water was added to replace the pyridinium salt with sodium salt. Then the salt solution was slowly added into 100 ml of anhydrous methan...

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Abstract

Disclosed are a selenium polysaccharide sulfate compound and a preparation method and applications of the selenium polysaccharide sulfate compound, belonging to the polysaccharide selenide technical field. The selenium polysaccharide sulfate compound is characterized in containing pyran sugar units or/and furan sugar units. The preparation method adopts reaction between polysaccharide sulfate and selenide reagent which is selenous acid and selenite. Molar ratio of the selenide reagent and groups of the polysaccharide sulfate is 1: 0.1-10. The compound of the invention is applied in preparing anticancer drug and ant-oxidation drug. The polysaccharide selenide sulfate of the invention is produced by substitution reaction between selenous acid and sugar unit sulfate radicals. Therefore, the yield and the quality of the product are both higher than that of the product produced by other methods. The invention also has advantage of high selenium content: the highest content of the selenium can reach to 45 percent which is much higher than 12.5 percent reported in literature.

Description

technical field [0001] The invention belongs to the technical field of selenated polysaccharides, and in particular relates to a selenized polysaccharide sulfate compound, a preparation method thereof, and an application in preparing anticancer drugs and antioxidant drugs. Background technique [0002] Polysaccharides are another important biological macromolecule in addition to proteins and nucleic acids in organisms. They have anti-infection, immune promotion, tumor prevention and treatment, viral hepatitis, rheumatoid disease, AIDS and other immune damage or immune deficiency diseases and anti-oxidation. Various functions and biological activities. Structural factors that affect the biological activity of polysaccharides include the properties of the main chain of polysaccharides, the properties of branched chains, and the higher-order structure of polysaccharide molecules. The composition of sugar units in the main chain of polysaccharides and the type of glycosidic bond...

Claims

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Application Information

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IPC IPC(8): C08B37/00A61K31/717A61P35/00
Inventor 陈艺新
Owner 陈艺新
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