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Polyrotaxane-structured NO donor material and preparation method and application thereof

A polyrotaxane, donor technology, applied in the field of biomedical engineering materials, can solve problems such as neglect

Active Publication Date: 2019-12-03
JINAN UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0004] However, at present, a large number of researchers regard the drug loading and long release period of NO donor materials as a breakthrough in the application of NO antibacterial agents in the antibacterial field, thus ignoring the special structural properties of the donor materials themselves. More efficient antibacterial effect of NO donor material

Method used

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  • Polyrotaxane-structured NO donor material and preparation method and application thereof
  • Polyrotaxane-structured NO donor material and preparation method and application thereof
  • Polyrotaxane-structured NO donor material and preparation method and application thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0078] (1) The anhydrous triblock copolymer PEG-PPG-PEG was added to anhydrous dichloromethane under nitrogen protection and dissolved completely. Then, p-toluenesulfonyl chloride was added at 5°C, and the stirring was continued for 20 minutes, followed by the addition of 4-dimethylaminopyridine (DMAP) and triethylamine (NeT 3 ), the reaction was continued for 48 h, the reaction was terminated, and 30 mL of saturated NaHCO was used. 3 Washed twice, evaporated to remove dichloromethane, and vacuum-dried at 50 °C for 24 h to obtain p-toluenesulfonylated PEG-PPG-PEG(PEG-(OTs) 2 );

[0079] Among them, the number average molecular weight of the anhydrous triblock copolymer PEG-PPG-PEG is 1000, and m:n is 1:0.5; the anhydrous triblock copolymer PEG-PPG-PEG, p-toluenesulfonyl chloride, 4-dimethylformaldehyde Aminopyridine (DMAP) and triethylamine (NeT 3 ) in a molar ratio of 1:2:0.05:5; the anhydrous dichloromethane consumption is calculated by dissolving 0.5g of anhydrous triblo...

Embodiment 2

[0092] PEG-PPG-PEG amination (PEG-PPG-PEG-NH 2 )preparation

[0093] (1) Add the anhydrous triblock copolymer PEG-PPG-PEG to anhydrous dichloromethane under nitrogen protection and dissolve it completely; then add p-toluenesulfonyl chloride at 20°C and continue to stir to stabilize After 30min, continue to add 4-dimethylaminopyridine (DMAP) and triethylamine (NeT 3 ), the reaction was continued for 72 h, the reaction was terminated, and 60 mL of saturated NaHCO was used. 3 Washed 3 times, evaporated to remove dichloromethane, and then vacuum-dried at 60 °C for 36 h to obtain p-toluenesulfonated PEG-PPG-PEG(PEG-(OTs) 2 );

[0094] Among them, the number average molecular weight of the anhydrous triblock copolymer PEG-PPG-PEG is 15000, and m:n is 1:1.5; the anhydrous triblock copolymer PEG-PPG-PEG, p-toluenesulfonyl chloride, 4-dimethylformaldehyde Aminopyridine (DMAP) and triethylamine (NeT 3 ) molar ratio is 1:10:0.1:15; the amount of dichloromethane is calculated by diss...

Embodiment 3

[0111] Take 1 mg of triblock copolymer PEG-PPG-PEG (raw material in Example 1) and the aminated PEG-PPG-PEG (PEG-PPG-PEG-NH) prepared in Example 1 respectively. 2 ), interlocking supramolecular polyrotaxane (β-CD@PEG-PPG-PEG-DNFB), cationized interlocking supramolecular polyrotaxane (β-CD@PEG-PPG-PEG@PEHA) and interlocking Supramolecular polyrotaxane NO donor (β-CD@PEG-PPG-PEG@PEHA / NONOate) was dispersed in 1 mL of pure water, and the surface potential changes of the corresponding materials were measured. The results are as follows: image 3 As shown, it was found that the potential of the aminated PEG-PPG-PEG changed significantly, proving that tris(2-aminoethyl)amine was successfully modified to both ends of PEG-PPG-PEG. The interlocked supramolecular polyrotaxane (β- The potential of CD@PEG-PPG-PEG-DNFB) was compared with that of aminated PEG-PPG-PEG (PEG-PPG-PEG-NH 2 ) was significantly reduced, and was significantly lower than that of PEG-PPG-PEG, which proved that the ...

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Abstract

The invention discloses a polyrotaxane-structured NO donor material and a preparation method and application thereof. The polyrotaxane-structured NO donor material is an internal lock supramolecule formed by sleeving a dumbbell-shaped PEG-PPG-PEG linear molecule with a cationized beta-cyclodextrin molecule, wherein the beta-cyclodextrin molecule can freely slide on the PEG-PPG-PEG linear molecule.The internal lock supramolecule serving as an NO donor material can effectively inhibit growth and reproduction of bacteria and fungi, has a remarkable inhibiting effect on common pathogenic bacteria, dermatophytes, wound infection bacteria and the like, has functions of promoting wound healing, diminishing inflammation and the like, and can be applied to preparation of biomedical engineering materials.

Description

technical field [0001] The invention belongs to the field of biomedical engineering materials, and in particular relates to a polyrotaxane structure NO donor material and a preparation method and application thereof. Background technique [0002] Bacterial resistance to antibiotics is a growing threat to human health. The irrational use of antibacterial drugs will lead to the reduction or even disappearance of the sensitivity of bacteria to antibacterial drugs, the reduction or even ineffectiveness of the efficacy of antibacterial drugs, and the emergence of bacterial resistance. Bacterial drug resistance will lead to a series of serious problems. For example, patients with drug-resistant bacterial infection will face more complex treatment problems, prolong hospital stay, increase mortality, and increase personal and social economic burden. Bacterial drug resistance may lead to no available drugs; multi-drug resistance with no cure can cause epidemics of infectious disease...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08G83/00A61K33/00A61P31/04A61P31/10
CPCA61K33/00A61P31/04A61P31/10C08G83/008
Inventor 马栋李国巍张武
Owner JINAN UNIVERSITY
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