Urushi polysaccharide sulfation and its preparation method and uses

A sulfation and raw lacquer technology, which is applied in pharmaceutical formulations, medical preparations containing active ingredients, and extracellular fluid diseases, etc. The effect of good reproducibility, high degree of substitution and anticoagulant activity

Inactive Publication Date: 2004-11-10
WUHAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The amount of sulfation reagent used in this method is large, and degradation is serious in the reaction process, and product molecular weight is little (<10000), and biological activity is relatively poor

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0010] Example 1: 486 mg of lacquer polysaccharide was suspended in 48.6 ml of dimethyl sulfoxide, stirred at 60° C. for 30 min, and then 1.92 g of sulfur trioxide pyridine complex was added. After reacting for 1 h, the reaction mixture was cooled to room temperature with an ice-water bath, 30 ml of ice water was added, neutralized with 15 wt % NaOH, and then dialyzed in distilled water for 120 hours. The dialyzed internal solution was concentrated by distillation under reduced pressure at 45°C, followed by precipitation with absolute ethanol; precipitation was carried out with P 2 o 5 The product was obtained after vacuum drying. The molecular parameters and anticoagulant properties of the obtained product are listed in Table 1.

Embodiment 2

[0011] Example 2: 486 mg of lacquer polysaccharide was suspended in 48.6 ml of dimethyl sulfoxide, stirred at 60° C. for 30 min, and then 1.92 g of sulfur trioxide pyridine complex was added. After reacting for 3 h, the reaction mixture was cooled to room temperature with an ice-water bath, 30 ml of ice water was added, neutralized with 15 wt % NaOH, and then dialyzed in distilled water for 120 hours. The dialyzed internal solution was concentrated by distillation under reduced pressure at 45°C, followed by precipitation with absolute ethanol; precipitation was carried out with P 2 o 5 The product was obtained after vacuum drying. The molecular parameters and anticoagulant properties of the obtained product are listed in Table 1.

Embodiment 3

[0012] Example 3: 162 mg of lacquer polysaccharide was suspended in 16.2 ml of dimethyl sulfoxide, stirred at 40° C. for 30 min, and then 0.64 g of sulfur trioxide pyridine complex was added. After reacting for 3 h, the reaction mixture was cooled to room temperature with an ice-water bath, 10 ml of ice water was added, neutralized with 15 wt% NaOH, and dialyzed in distilled water. The dialyzed inner liquid was concentrated by vacuum distillation, followed by precipitation with absolute ethanol, and the product was obtained after vacuum drying. The molecular parameters and anticoagulant properties of the obtained product are listed in Table 1.

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PUM

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Abstract

The invention relates to a sulfation raw lacquer polysaccharide with biological activity prepared through the steps of, (2) dissolving or suspending the raw lacquer polysaccharide in 50-100 times weight ratio of drying solvent, stiring 10-30 min at 40-100 deg. C, charging trioxide pyridine compound of 1-4 times molar weight of raw lacquer polysaccharide residue or 1:2-4:1 volumetric ratio of sulfuric chlorohydrin pyridine mixture, reacting 0.5-4 hrs, cooling down the reaction mixture through ice bath, charging ice water with 1/3-1/2 times of solvent volume, neutralizing with 5-20wt% of NaOH, dialyzing in distilled water, subjecting the dialysate to vacuum distillation concentration at 30-70 deg. C, settling with anhydrous alcohol, and vacuum drying with P2O5.

Description

technical field [0001] The invention relates to a biologically active sulfated lacquer polysaccharide, a preparation method and application thereof. The sulfated polysaccharide has anticoagulant activity and antiviral activity, and has application prospects as a medicine in the treatment of cardiovascular diseases, HIV and the like. Background technique [0002] Thromboembolism can be resolved with anticoagulant therapy. For deep vein thrombosis and pulmonary embolism, it is estimated that approximately 0.2-0.4% of people require anticoagulant therapy each year. The most commonly used anticoagulant drug is heparin, a sulfated natural polysaccharide. At present, heparin has become the second largest natural therapeutic drug after insulin. However, although heparin has a very good anticoagulant effect, its use is limited in some clinical conditions due to the congenital lack of antithrombin and heparin's role in some patients and heparin often causes thrombocytopenia and bl...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/715A61P7/02C08B37/00
Inventor 杜予民杨建红
Owner WUHAN UNIV
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