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首页> 外文期刊>Dalton transactions: An international journal of inorganic chemistry >Functionalized nonporous silica nanoparticles as carriers for Pt(IV) anticancer prodrugs
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Functionalized nonporous silica nanoparticles as carriers for Pt(IV) anticancer prodrugs

机译：功能化的无孔二氧化硅纳米粒子作为Pt（IV）抗癌前药的载体

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摘要

Nonporous silica nanoparticles (SNPs) with an external shell containing primary amino groups were proposed as potential delivery systems for Pt(IV) antitumor prodrugs. Spherical SNPs containing two different external arms, i.e. 3-aminopropyl and N-(6-aminohexyl) aminomethylene, of around 125 nm hydrodynamic diameter were loaded with two different cisplatin-based Pt(IV) complexes, namely (OC-6-44)-diamminedichloridoethoxidosuccinatoplatinum(IV) and IV(OC-6-44)-diamminedichloridoacetylamidosuccinatoplatinum(IV), through the formation of amide bonds between the pendant amino groups on SNPs and the free carboxylic group of the complexes. In the presence of the N-(6-aminohexyl) aminomethylene arm, the Pt(IV)-SNP conjugates showed a negligible (unwanted) Pt release by hydrolysis, whereas in the presence of ascorbic acid the reduction of Pt(IV) -> Pt(II) caused the substantial release of the active metabolite cisplatin. Conjugate Pt(IV)-SNP exhibited better antiproliferative activity on the Pt-sensitive A2780 human ovarian cancer cell line than the parent cisplatin and their free Pt(IV) precursors, due to their more efficient cellular uptake, likely by endocytosis.
机译：带有外壳的含伯氨基的无孔二氧化硅纳米粒子（SNP）被提议作为Pt（IV）抗肿瘤前药的潜在传递系统。包含两个不同外臂（即3-氨基丙基和N-（6-氨基己基）氨基亚甲基）的球形SNP，其流体动力学直径约为125 nm，装有两种不同的基于顺铂的Pt（IV）配合物，即（OC-6-44）通过在SNPs侧链氨基上的酰胺键与配合物的游离羧基之间形成酰胺键，可生成-diamminedichloridoethoxidosuccinatoplatinum（IV）和IV（OC-6-44）-diamminedichloridoethyloxidamideamidosuccinatoplatinum在N-（6-氨基己基）氨基亚甲基臂的存在下，Pt（IV）-SNP共轭物通过水解显示出可忽略的（不需要的）Pt释放，而在抗坏血酸的存在下，Pt（IV）的减少-> Pt（II）导致活性代谢物顺铂的大量释放。共轭Pt（IV）-SNP对Pt敏感的A2780人卵巢癌细胞系比其母体顺铂及其游离Pt（IV）前体表现出更好的抗增殖活性，这是由于它们更有效的细胞摄取（可能是胞吞作用）。

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