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Polysulfone derivative and preparation method and application thereof

A derivative, polysulfone technology, applied in the field of medicine, can solve rare problems and achieve the effects of good adsorption, good application prospects and good blood compatibility

Active Publication Date: 2020-11-20
CHONGQING ANTIXIN BIOTECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, blood purification materials that can simultaneously adsorb pathogen-associated molecular patterns and cytokines, especially materials that can be used for blood purification such as hemodialysis and hemofiltration, are still rare.

Method used

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  • Polysulfone derivative and preparation method and application thereof
  • Polysulfone derivative and preparation method and application thereof
  • Polysulfone derivative and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0049] Embodiment 1: the preparation of polyamine functional group

[0050] 1.1 Experimental method:

[0051]

[0052]

[0053] Weigh 50g of compound 1 and dissolve it in 200ml of ethanol, add 88.6g of Boc 2 O, react at room temperature. After the reaction was complete, the solvent was concentrated under reduced pressure to obtain 90 g of a yellow oil (compound 2). Weighed 60g of Compound 2 and dissolved it in 600ml of saturated methanolic ammonia solution, added 48g of Raney nickel, reacted under 4MPa hydrogen at 90°C for 48 hours, filtered, concentrated under reduced pressure to remove the solvent, and obtained a blue oil (Compound 3). Compound 3 was completely dissolved in 250ml of ethanol, 36ml of acrylcyanide was added, reacted at 40°C for 3 hours, concentrated under reduced pressure, and dried to obtain a golden yellow oil (compound 4). Weigh 5g of compound 4 and dissolve it in 50ml of dichloromethane, add 4ml of triethylamine and 6.76g of 3,4-dimethoxyphenylpro...

Embodiment 2

[0056] Embodiment 2: Preparation of polysulfone derivatives

[0057] 2.1 Experimental method: Dissolve 1g of polyethersulfone in 10ml of dichloromethane, then add 0.01mmol of 1,4-dichloromethoxybutane and 0.1ml of tin tetrachloride, and react at 25°C for 3 hours. Add 5ml of ethanol to precipitate the precipitate, wash with N,N-dimethylformamide, hydrochloric acid, ethanol and water successively until neutral, and dry to obtain chloromethylated polysulfone. Dissolve chloromethylated polysulfone in 10 ml of dichloromethane, add 2.5 ml of ammonia water dropwise, and continue the reaction for 4 hours. The organic layer was taken, washed with 10ml of hydrochloric acid and 10ml of sodium carbonate solution, concentrated and dried to obtain aminated polysulfone. Aminated polysulfone was dissolved in 15 ml of tetrahydrofuran, 5 mg of polyamine functional group (Example 1) was added, and reacted at room temperature for 4 hours. Then, 2.5 ml of acetic anhydride and 5 ml of triethylami...

Embodiment 3

[0061] Example 3: Detection of adsorption performance of polysulfone derivatives on bacterial lipopolysaccharide

[0062] 3.1 Experimental method: Prepare 1 μg / ml bacterial lipopolysaccharide solution, take 10 ml and place it in a stoppered Erlenmeyer flask, weigh 1 g of polysulfone derivative and put it into the bottle. The bacterial lipopolysaccharide solution was prepared in the same way, and 1 g of polysulfone was added as a control group. Shake and adsorb in a constant temperature oscillator at 37±1°C for 2 hours. According to the "Chinese Pharmacopoeia" 2015 Edition Bacterial Endotoxin Inspection Method, use Limulus reagent (dynamic turbidity method) to detect the content of bacterial lipopolysaccharide before and after adsorption, and calculate the adsorption Rate.

[0063] 3.2 Experimental results: see the results figure 1 . The adsorption of polysulfone to lipopolysaccharide is very weak, and the adsorption rate is only 14.11%, while the adsorption rate of polysulf...

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Abstract

The invention relates to a polysulfone derivative as well as a preparation method and application thereof, the polysulfone derivative is formed by covalently connecting polysulfone and a polyamine functional group, and the structural general formula of the polysulfone derivative is disclosed in the invention, wherein R1 to R5 are randomly selected from H or OH or OCH3; n1-n4 are integers ranging from 2 to 7; n5 is an integer from 0 to 2; n6 is an integer from 1 to 3; P is polysulfone. The polysulfone derivative disclosed by the invention can adsorb pathogen-related molecular patterns and cytokines, can be prepared into various blood purifiers for hemodialysis, hemofiltration and the like, and is used for removing excessive pathogen-related molecular patterns and cytokines in a human body,so that excessive immune response of the human body is avoided, and cytokine storm is avoided.

Description

technical field [0001] The invention belongs to the technical field of medicine, and particularly relates to a polysulfone derivative, a preparation method thereof, and an application in the preparation of a blood purifier capable of eliminating pathogen-related molecular patterns and / or cytokines. Background technique [0002] Pathogen-associated molecular patterns (PAMPs) produced by pathogenic microorganisms such as bacteria, viruses, and fungi, such as lipopolysaccharide, DNA, peptidoglycan, and lipoteichoic acid of bacteria, nucleic acids and structural proteins of viruses, and yeast Polysaccharides, etc., can cause excessive immune responses in the human body and produce cytokine storms. They are the main pathogenic substances that cause sepsis, new coronavirus pneumonia and other diseases. Removing these harmful substances can play a therapeutic role in related diseases. Blood purification is considered to be an effective means to remove these pathogenic substances an...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08G75/20C08G75/23A61M1/36B01J20/26B01J20/30
CPCC08G75/20C08G75/23A61M1/3679B01J20/265B01J20/30Y02A50/30
Inventor 郑玥邓军
Owner CHONGQING ANTIXIN BIOTECH CO LTD
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