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Application of gold nanoparticles in preparing anticoagulants or antiplatelet drugs

A gold nanoparticle and antiplatelet agent technology, applied in the field of biomedicine, can solve problems such as complex synthesis process, and achieve the effects of simple preparation method, high efficiency, small side effects, and small particle size distribution

Active Publication Date: 2014-08-13
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 the same time, pyrimidine is also the synthetic precursor of some anticoagulant drugs currently being studied. These anticoagulant drugs have shown more effective anticoagulant activity than existing drugs in previous studies, and are not easy to cause bleeding side effects. However, the synthesis process Too complex (Abdelhafez, O.M., et al., Bioorg. Med. Chem. 2010, 18(10), 3371-3378)

Method used

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  • Application of gold nanoparticles in preparing anticoagulants or antiplatelet drugs
  • Application of gold nanoparticles in preparing anticoagulants or antiplatelet drugs
  • Application of gold nanoparticles in preparing anticoagulants or antiplatelet drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Example 1 Preparation of substituted pyrimidine-modified gold nanoparticles Au_DAPT

[0028] (1) Configure the reaction solution

[0029] Configure 5mM chloroauric acid methanol solution: dissolve 41mg chloroauric acid in 20mL anhydrous methanol;

[0030] Prepare 10 mM 2-mercapto-4,6-diaminopyrimidine solution: add 14 mg of 2-mercapto-4,6-diaminopyrimidine (DAPT) into 10 mL of anhydrous methanol, and add 200 μL of anhydrous acetic acid and 50 μL of Tween 80, ultrasonic dissolution;

[0031] Prepare 60mM sodium borohydride methanol solution: dissolve 12mg sodium borohydride in 3mL methanol, ready to use;

[0032] (2) Reduction reaction to prepare gold nanoparticles

[0033] Under an ice bath, mix 20 mL of chloroauric acid methanol solution and 10 mL of 2-mercapto-4,6-diaminopyrimidine solution into a 50 mL round bottom flask, and stir for 10 min with a magnet;

[0034] Increase the stirring speed, add sodium borohydride methanol solution dropwise, drop it within 2 mi...

Embodiment 2

[0037] Preparation of Example 2 Substituted Pyrimidine Modified Gold Nanoparticles Au_APT and Au_DHPT

[0038] The synthesis method of Au_APT (APT is 2-mercapto-4-aminopyrimidine) and Au_DHPT (DHPT is 2-mercapto-4,6-dihydroxypyrimidine) is similar to Au_DAPT, just replace DAPT with equimolar APT and DHPT.

Embodiment 3

[0039] Example 3 Investigation of Gold Nanoparticles with Different Molar Content Ratio of Gold Elements and Substituted Pyrimidine Molecules

[0040] The molar content ratios of Au and DAPT were respectively prepared as 1:0.125, 1:0.25, 1:0.5, 1:1, and 1:2, and were characterized by transmission electron microscopy, as shown in image 3 shown. , when the ratio of Au and DAPT is 1:0.125 to 1:0.25, some gold nanoparticles have larger particle size and are more likely to agglomerate. When the ratio of Au and DAPT is 1:0.5 to 1:2, the dispersion of gold nanoparticles is better, and the particle size is about 3nm.

[0041] Table 1 Surface molecular density of different gold nanoparticles

[0042]

[0043] According to the XPS results, the surface molecular density of gold nanoparticles was calculated, and the surface molecular density was the highest when the ratio of Au and DAPT was 1:1.

[0044] The above-mentioned gold nanoparticles with different ratios were tested toget...

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Abstract

The invention discloses application of substituted pyrimidine molecule modified gold nanoparticles in preparing anticoagulants or antiplatelet drugs. The substituted pyrimidine molecule for modifying the gold nanoparticles is one or a mixture of at least two of 2-thiol-4,6-diaminopyrimidine, 2-thiol-4-aminopyrimidine and 2-thiol-4,6-dihydroxylpyrimidine. According to the gold nanoparticles, the substituted pyrimidine part without anticoagulant activity is connected with gold nanoparticles without anticoagulant activity through an S-Au bond to be applied to the anticoagulation field for the first time; the substituted pyrimidine molecule modified gold nanoparticles obtain unexpected anticoagulation effect, the preparation method is simple, the nanoparticles are small in diameter distribution and can be well dispersed in water, cannot cause bleeding side effect in normal dosage, and can be used for preparing anticoagulants or antiplatelet drugs.

Description

technical field [0001] The invention belongs to the field of biomedicine and relates to the application of gold nanoparticles, more specifically, the application of a substituted pyrimidine-modified gold nanoparticle in the preparation of anticoagulant or antiplatelet agent. Background technique [0002] Venous thrombosis is the third leading killer of human death due to cardiovascular-related diseases, and anticoagulant drugs are currently the most effective preventive and therapeutic drugs (Mackman, N., Nature 2008, 451(7181), 914-918). Currently commonly used anticoagulant drugs such as heparin and warfarin sodium are likely to cause side effects such as bleeding during use, and are likely to interact with other things and drugs, affecting the efficacy of the drug. Drug monitoring is required when using it ( Goldhaber, S.Z.; Bounameaux, H., Lancet 2012, 379(9828), 1835-1846; Palareti, G., et al., Lancet 1996, 348(9025), 423-428). People have always wanted to solve the pr...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K31/555A61P7/02
Inventor 蒋兴宇田月赵玉云张伟
Owner THE NAT CENT FOR NANOSCI & TECH NCNST OF CHINA
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