Gold nanoparticle with Gram selectivity and modified with phenylboronic acid and derivatives of phenylboronic acid and preparation method and application of gold nanoparticle

A gram-selective, gold nanoparticle technology, applied in non-active ingredients medical preparations, active ingredients-containing medical preparations, drug combinations, etc. Process complexity and other problems, to achieve the effect of less drug resistance, excellent biocompatibility, and high biosafety

Active Publication Date: 2019-11-01
THE NAT CENT FOR NANOSCI & TECH NCNST OF CHINA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, the prior art discloses a composite nano-antibacterial agent with bacteria-specific recognition ability and its application. Bacillus influenzae and Staphylococcus aureus have selective recognition ability, but nano-silver is unstable and has strong toxicity to the human body. The US FDA has explicitly banned the use of nano-silver in medical applications. restricted
The prior art also discloses a composition for preparing antibacterial polyurethane, antibacterial polyurethane and a preparation method thereof, which can selectively kill Gram-positive bacteria, but the raw material components include polymer diol, diisocyanate, Chain extender and benzisothiazoline, the composition is complex, and the influence between various components is not clear
The prior art discloses a selective bactericide of composite nanoparticles and its preparation and application. The antibiotic is modified by a chemical cross-linking agent to achieve selective sterilization, but it is unavoidable that the use of antibiotics will lead to the emergence of bacterial drug resistance, and there is an induced The hidden danger of superbugs
The prior art discloses a myrrh alkane-type sesquiterpene compound and its preparation method and its application as a selective antibacterial agent. It has the activity of inhibiting various bacteria, but it needs to undergo fermentation culture, filtration, concentration, extraction, and chromatographic separation. and the eluent are concentrated, the product preparation process is complicated, and the degree of purification is difficult to determine

Method used

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  • Gold nanoparticle with Gram selectivity and modified with phenylboronic acid and derivatives of phenylboronic acid and preparation method and application of gold nanoparticle
  • Gold nanoparticle with Gram selectivity and modified with phenylboronic acid and derivatives of phenylboronic acid and preparation method and application of gold nanoparticle
  • Gold nanoparticle with Gram selectivity and modified with phenylboronic acid and derivatives of phenylboronic acid and preparation method and application of gold nanoparticle

Examples

Experimental program
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Effect test

Embodiment 1

[0066] This example is used to illustrate the preparation method of phenylboronic acid modified gold nanoparticles of the present invention.

[0067] Proceed as follows:

[0068] (1) In a round-bottom flask, dissolve 0.05 millimoles of phenylboronic acid (PBA, molecular weight 121.93, Sigma) in 10 milliliters of deionized aqueous solution, and then add 0.05 millimoles of chloroauric acid trihydrate (molecular weight 393.83, Sinopharm Chemical Reagent Co., Ltd.), 50 microliters of triethylamine and 30 mg of Tween 80, and mix in an ice water bath for 10 minutes until the molecules are completely dissolved.

[0069] (2) Dissolve 6 mg of sodium borohydride in 2 ml of deionized water, add it dropwise to a round bottom flask under vigorous stirring at 1000 revolutions per minute. The color of the solution in the bottle immediately changes from colorless to brown. Keep this reaction Conditions reacted for another 2 hours.

[0070] (3) Dialysis the obtained phenylboronic acid-modified gold n...

Embodiment 2

[0073] This example is used to illustrate the preparation method of carboxyphenylboronic acid modified gold nanoparticles of the present invention.

[0074] Proceed as follows:

[0075] (1) In a round-bottom flask, dissolve 0.05 millimoles of carboxyphenylboronic acid (CBA molecular weight 165.94, Sigma) in 10 milliliters of deionized aqueous solution, then add 0.05 millimoles of chloroauric acid trihydrate, and 50 microliters of trihydrate. Ethylamine and 30 mg of Tween 80 are mixed in an ice water bath for 10 minutes until the molecules are completely dissolved.

[0076] (2) The synthesis and particle characterization of carboxyphenylboronic acid modified gold nanoparticles are the same as those in Example 1. The results are as follows figure 2 As shown in A-B, the average particle size of the gold nanoparticles modified with carboxyphenylboronic acid is 7±2.1 nm.

[0077] (3) The antibacterial properties of the gold nanoparticles modified with carboxyphenylboronic acid are the sam...

Embodiment 3

[0079] This example is used to illustrate the preparation method of hydroxyphenylboronic acid modified gold nanoparticles of the present invention.

[0080] Proceed as follows:

[0081] (1) In a round-bottom flask, dissolve 0.05 millimoles of hydroxyphenylboronic acid (HBA molecular weight 137.93, Sigma) in 10 milliliters of deionized aqueous solution, then add 0.05 millimoles of chloroauric acid trihydrate, and 50 microliters of trihydrate. Ethylamine and 30 mg of Tween 80 are mixed in an ice water bath for 10 minutes until the molecules are completely dissolved.

[0082] (2) The synthesis and particle characterization of gold nanoparticles modified by hydroxyphenylboronic acid are the same as those in Example 1. The results are as follows figure 2 As shown in A-B, the average particle diameter of gold nanoparticles modified with hydroxyphenylboronic acid is 17±7.8 nm.

[0083] (3) The antibacterial properties of gold nanoparticles modified by hydroxyphenylboronic acid are the same ...

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Abstract

The invention provides a gold nanoparticle with Gram selectivity and modified with phenylboronic acid and derivatives of the phenylboronic acid, and further provides a preparation method and application of the gold nanoparticle. The gold nanoparticle modified with the phenylboronic acid and the derivatives of the phenylboronic acid has high biological safety, and the identification and targeting of bacteria are improved; the stability between small molecules and the gold nanoparticle is ensured, the preparation method is simple, the bacteria are not prone to being induced to produce drug resistance, the antibacterial activity of Gram-negative bacterium selection and identification is achieved, and the antibacterial effect against drug-sensitive strains and multi-drug resistant strains is obvious; and the gold nanoparticle co-modified with the two ligands has a broad-spectrum antibacterial effect, synthesized particles are stable and easy to store, and the potential for large-scale production and broad clinical application prospects are achieved.

Description

Technical field [0001] The invention belongs to the field of nano biomaterials, and specifically relates to a gold nanoparticle modified with phenylboronic acid and its derivatives with Gram selectivity, and a preparation method and application thereof. Background technique [0002] Gram-negative bacteria (e.g. Escherichia coli) can cause infections of the urinary tract, gastrointestinal and lungs, while gram-positive bacteria (e.g. Staphylococcus aureus) can cause skin and cartilage infections. With the reduction in the efficiency of conventional antibiotics and the intensification of clinical infections, bacterial infections and antibiotic resistance have become major issues of global concern. Therefore, there is an urgent need to develop a new generation of antibacterial agents that are selective for Gram bacteria and are not easy to induce bacterial resistance. Antibacterial agents designed by exchanging ligands have been used to prepare many types of antibacterial agents, i...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K33/242A61K47/24A61K47/54A61K9/16A61P31/04A61P17/02A61P1/02
CPCA61K33/24A61K9/1617A61P31/04A61P17/02A61P1/02Y02A50/30
Inventor 蒋兴宇王乐
Owner THE NAT CENT FOR NANOSCI & TECH NCNST OF CHINA
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