BACKGROUND Gold nanoparticles (AuNPs) have been proposed for many applications in medicine and bioanalysis. For use in all these applications, maintaining the stability of AuNPs in solution by suppressing aggregation is paramount. Herein, the effects of amino acids were investigated in stabilizing AuNPs by rationally designed peptide scaffolds. RESULTS Compared to other tested amino acids, phosphotyrosine (pY) significantly stabilized AuNPs. Our results indicated that pY modified AuNPs presented a high level of stability in various solutions, and had good biocompatibility. When a pY-peptide was used in stabilizing AuNPs, the phosphate group could be removed by phosphatases, which subsequently caused the aggregation and the cargo release of AuNPs. In vitro study showed that AuNPs formed aggregation in a phosphatase concentration depending manner. The aggregation of AuNPs was well correlated with the enzymatic activity (R2 = 0.994). In many types of cancer, a significant increase in phosphatases has been observed. Herein, we demonstrated that cancer cells treated with pY modified AuNPs in conjunction with doxorubicin killed SGC-7901 cells with high efficiency, indicating that the pY peptide stabilized AuNPs could be used as carriers for targeted drug delivery. CONCLUSION In summary, pY peptides can act to stabilize AuNPs in various solutions. In addition, the aggregation of pY-AuNPs could be tuned by phosphatase. These results provide a basis for pY-AuNPs acting as potential drug carriers and anticancer efficacy.

中文翻译：

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磷酸肽对金纳米颗粒稳定性和药物递送的影响。

背景技术已经提出了金纳米颗粒（AuNP）在医学和生物分析中的许多应用。为了在所有这些应用中使用，最重要的是通过抑制聚集来维持溶液中AuNP的稳定性。本文中，通过合理设计的肽支架研究了氨基酸在稳定AuNPs中的作用。结果与其他测试氨基酸相比，磷酸酪氨酸（pY）可以显着稳定AuNPs。我们的结果表明，pY修饰的AuNPs在各种溶液中均显示出高水平的稳定性，并具有良好的生物相容性。当使用pY肽稳定AuNPs时，磷酸基团可被磷酸酶去除，随后引起AuNPs的聚集和货物释放。体外研究表明，AuNPs以磷酸酶浓度依赖的方式形成聚集体。AuNPs的聚集与酶活性有很好的相关性（R2 = 0.994）。在许多类型的癌症中，已观察到磷酸酶的显着增加。在本文中，我们证明了用pY修饰的AuNPs与阿霉素协同处理的癌细胞高效杀伤了SGC-7901细胞，这表明pY肽稳定的AuNPs可以用作靶向药物递送的载体。结论总而言之，pY肽可以在各种溶液中起到稳定AuNPs的作用。另外，可以通过磷酸酶调节pY-AuNP的聚集。这些结果为pY-AuNPs充当潜在的药物载体和抗癌功效提供了基础。我们证明了用pY修饰的AuNP与阿霉素联合处理的癌细胞能高效杀伤SGC-7901细胞，这表明pY肽稳定的AuNP可以用作靶向药物递送的载体。结论总而言之，pY肽可以在各种溶液中起到稳定AuNPs的作用。另外，可以通过磷酸酶调节pY-AuNP的聚集。这些结果为pY-AuNPs作为潜在的药物载体和抗癌功效提供了基础。我们证明了用pY修饰的AuNP与阿霉素联合处理的癌细胞能高效杀伤SGC-7901细胞，这表明pY肽稳定的AuNP可以用作靶向药物递送的载体。结论总而言之，pY肽可以在各种溶液中起到稳定AuNPs的作用。另外，可以通过磷酸酶调节pY-AuNP的聚集。这些结果为pY-AuNPs充当潜在的药物载体和抗癌功效提供了基础。pY-AuNPs的聚集可以通过磷酸酶调节。这些结果为pY-AuNPs充当潜在的药物载体和抗癌功效提供了基础。pY-AuNPs的聚集可以通过磷酸酶调节。这些结果为pY-AuNPs作为潜在的药物载体和抗癌功效提供了基础。