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An antibacterial agent based on gold nanoparticles surface-modified nitrogen-heterocyclic small molecules

A technology of gold nanoparticles and nitrogen heterocycles, which is applied in the field of gold nanoparticles, can solve the problems of affecting the experimental repeatability and antibacterial effect, and has no effect, so as to avoid poor biocompatibility, good antibacterial property, and strong antibacterial active effect

Active Publication Date: 2022-04-15
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

Compared with antibiotics themselves, the antibacterial activity of gold nanoparticles modified by antibiotics is significantly enhanced, but this kind of gold nanoparticles still has no effect on drug-resistant bacteria
[0004] In order to synthesize effective gold nanoparticles with antibacterial activity, applicants have invented a series of gold nanoparticles modified with mercaptopyrimidines with antibacterial activity, which are effective against Gram-negative bacteria, Gram-positive bacteria and super Drug-resistant bacteria have good antibacterial effects, but these gold nanoparticles have some serious shortcomings, for example, two small molecule ligands are required to modify gold nanoparticles at the same time, and the functionalization of the two ligands with different effects seriously affects the experimental results. Repeatability and antimicrobial effect

Method used

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  • An antibacterial agent based on gold nanoparticles surface-modified nitrogen-heterocyclic small molecules
  • An antibacterial agent based on gold nanoparticles surface-modified nitrogen-heterocyclic small molecules
  • An antibacterial agent based on gold nanoparticles surface-modified nitrogen-heterocyclic small molecules

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0057] This example is used to illustrate the surface-modified 3-amino-5-mercapto-1,2,4-triazole gold nanoparticles (ATT-Au) of the present invention and its preparation method.

[0058] The preparation method that this embodiment adopts can refer to figure 1 The schematic diagram in , specifically:

[0059] (1) 3-amino-5-mercapto-1,2,4-triazole is completely dissolved in methanol and then mixed with chloroauric acid to form a mixed solution, the 3-amino-5-mercapto-1,2, The molar ratio of 4-triazole and the chloroauric acid is shown in Table 1.

[0060] (2) Stir the mixed solution described in step (1) under an ice-bath magnetic stirrer, add Tween 80 and fully mix and dissolve, add sodium borohydride, the mol ratio of the Tween 80 to the chloroauric acid and The molar ratio of the sodium borohydride to the chloroauric acid is shown in Table 1, and the stirring was continued for 1 hour to obtain the crude gold nanoparticles.

[0061] (3) Methanol was removed by a rotary evap...

Embodiment 2

[0064] This example is used to illustrate the surface-modified 3-amino-5-mercapto-1,2,4-triazole gold nanoparticles (ATT-Au) of the present invention and its preparation method.

[0065] The preparation method of this embodiment is basically the same as that of Example 1, the only difference being the molar ratio of the nitrogen heterocyclic small molecules specified in the following table 1, the nitrogen heterocyclic small molecules to the chloroauric acid, the Tween 80 and the mol ratio of the chloroauric acid, the mol ratio of the sodium borohydride and the chloroauric acid are prepared.

[0066] Measured by TEM, the particle diameter of the gold nanoparticles is about 1-5nm, and the measurement results are as follows: Figure 4 shown. As determined by X-ray energy spectrometer, the molar ratio of the small nitrogen heterocyclic molecules in the finally obtained gold nanoparticles to gold is 0.53:1.

Embodiment 3

[0068] This example is used to illustrate the surface-modified 4-amino-3-hydrazine-5-mercapto-1,2,4-triazole gold nanoparticles (AHMT-Au) of the present invention and its preparation method.

[0069] The preparation method of this embodiment is basically the same as that of Example 1, the only difference being the molar ratio of the nitrogen heterocyclic small molecules specified in the following table 1, the nitrogen heterocyclic small molecules to the chloroauric acid, the Tween 80 and the mol ratio of the chloroauric acid, the mol ratio of the sodium borohydride and the chloroauric acid are prepared.

[0070] Measured by TEM, the particle size of the gold nanoparticles is about 2 to 15nm, and the measurement results are as follows: Figure 5 shown. Measured by an X-ray energy spectrometer, the molar ratio of the nitrogen heterocyclic small molecule to gold in the finally obtained gold nanoparticles is 0.31:1.

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Abstract

The present invention provides a gold nanoparticle. The surface of the gold nanoparticle is modified with a nitrogen heterocyclic small molecule, preferably selected from triazoles with mercapto groups, imidazoles with mercapto groups, purines with mercapto groups and benzothiazoles with mercapto groups. one or more of. The gold nanoparticles prepared by the present invention have good antibacterial properties against Gram-negative bacteria, Gram-positive bacteria and / or clinically isolated bacteria with multidrug resistance, and can have good biocompatibility. The invention also provides a preparation method of the gold nanoparticle, an antibacterial composition containing the gold nanoparticle, a kit, and an application of the gold nanoparticle and the antibacterial composition in preparing antibacterial products or medicines.

Description

technical field [0001] The present invention relates to a gold nanoparticle, in particular to a gold nanoparticle surface-modified nitrogen heterocyclic small molecule, a preparation method of the gold nanoparticle, an antibacterial composition containing the gold nanoparticle, a kit, the gold nanoparticle and Application of the antibacterial composition in the preparation of antibacterial products or medicines. Background technique [0002] Bacterial infection is one of the most important causes of threats to human health, but the abuse of traditional antibiotics based on small organic molecules has led to the emergence of super-resistant bacteria. Antimicrobial resistance has caused serious morbidity and mortality, especially in hospital-associated infections, and a corresponding increase in public healthcare costs. In this way, there is an urgent need to invent new and effective antibacterial agents, especially for super-resistant bacteria. [0003] Nanomaterials have s...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/54A61K33/242A61K9/51A61P31/04
CPCA61K9/51A61K33/24A61K31/53C09K11/02C09K11/58Y02A50/30
Inventor 蒋兴宇冯艳
Owner THE NAT CENT FOR NANOSCI & TECH NCNST OF CHINA
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