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Application of silicon dioxide nanoparticles modified with tumor-targeting ligands for cellular delivery of nucleoside triphosphate analogues
Journal of Saudi Chemical Society ( IF 5.8 ) Pub Date : 2019-09-24 , DOI: 10.1016/j.jscs.2019.09.007
Svetlana V. Vasilyeva , Albina S. Petrova , Alexander A. Shtil , Dmitry A. Stetsenko

A key advantage of amino-modified SiO2 nanoparticles for delivery of phosphorylated nucleosides is a broad possibility for functionalization. It can be modified with ligands currently investigated in targeted drug delivery. To improve the efficacy for intracellular delivery, SiO2 nanoparticles were functionalized with tumor-targeting ligands folic acid, biotin or 5-fluorouracil. Studies of accumulation of these conjugates in HCT116 colon carcinoma cells revealed that the uptake of modified conjugates was significantly bigger compared to unmodified nanoparticles, with the biotinylated conjugate as the preferred compound. The nanocomposites of biotin modified SiO2 and 2′,3′-dideoxyuridine triphosphate showed a pronounced antiproliferative potency relative to the unmodified nanocomposites. Thus, multi-functionalization of SiO2 nanoparticle based conjugates has a major potential for delivery of nucleoside triphosphate analogues, therefore tentatively enhancing their bioactivity.



中文翻译:

肿瘤靶向配体修饰的二氧化硅纳米粒子在细胞内传递核苷三磷酸类似物的应用

用于递送磷酸化核苷的氨基改性的SiO 2纳米颗粒的关键优势是功能化的广泛可能性。可以用目前在靶向药物递送中研究的配体对其进行修饰。为了提高细胞内递送的功效,将SiO 2纳米颗粒用靶向肿瘤的配体叶酸,生物素或5-氟尿嘧啶功能化。这些缀合物在HCT116结肠癌细胞中积累的研究表明,与未修饰的纳米颗粒相比,修饰的缀合物的摄取明显更大,其中生物素化的缀合物是优选的化合物。生物素修饰的SiO 2纳米复合材料相对于未修饰的纳米复合材料,和2',3'-二脱氧尿苷三磷酸酯显示出显着的抗增殖能力。因此,基于SiO 2纳米颗粒的缀合物的多功能化具有递送核苷三磷酸酯类似物的主要潜力,因此初步增强了它们的生物活性。

更新日期:2019-09-24
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