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叶酸季铵盐壳聚糖修饰的正电荷金纳米粒子的合成、细胞毒性及癌细胞摄取。

Positively charged gold nanoparticles capped with folate quaternary chitosan: Synthesis, cytotoxicity, and uptake by cancer cells.

机构信息

Biomedical Engineering Program, Graduate Institute of Applied Science and Technology, National Taiwan University of Science and Technology, Taipei City, 10607, Taiwan, ROC.

Institute of Preventive Medicine, National Defense Medical Center, New Taipei City, 23742, Taiwan, ROC, Taiwan, ROC; Department of Chemistry, National Taiwan University, Taipei 10617, Taiwan, ROC.

出版信息

Carbohydr Polym. 2018 Mar 1;183:140-150. doi: 10.1016/j.carbpol.2017.11.096. Epub 2017 Dec 8.

DOI:10.1016/j.carbpol.2017.11.096
PMID:29352869
Abstract

In this study, we synthesized various quaternary chitosan derivatives and used them to stabilize gold nanoparticles (AuNPs). These chitosan derivatives comprised N-(2-hydroxy)propyl-3-trimethylammonium chitosan chloride (HTCC), folate-HTCC, galactosyl-HTCC, and their fluorescein isothiocyanate-conjugated derivatives. Various positively surface-charged AuNPs were prepared under alkaline conditions using glucose as a reducing agent in the presence of the HTCC derivatives (HTCCs). The effects of the concentration of NaOH, glucose, and HTCCs on the particles size, zeta potential, and stability were studied in detail. Cell cycle assays verify that none of the HTCCs or HTCCs-AuNPs was cytotoxic to human umbilical vein endothelial cells. Flow cytometry analysis showed that the folate HTCC-AuNPs were internalized in Caco-2, HepG2, and HeLa cancer cells to a significantly greater extent than AuNPs without folate. But, galactosyl HTCC-AuNPs only showed high cell uptake by HepG2 cells.

摘要

在这项研究中,我们合成了各种季铵化壳聚糖衍生物,并将其用于稳定金纳米粒子(AuNPs)。这些壳聚糖衍生物包括 N-(2-羟丙基)-3-三甲基氯化铵壳聚糖(HTCC)、叶酸-HTCC、半乳糖基-HTCC 及其荧光素异硫氰酸酯缀合衍生物。在碱性条件下,使用葡萄糖作为还原剂,在 HTCC 衍生物(HTCCs)存在下,制备了各种带正电荷的 AuNPs。详细研究了 NaOH、葡萄糖和 HTCCs 的浓度对颗粒尺寸、ζ电位和稳定性的影响。细胞周期测定验证了 HTCC 或 HTCC-AuNPs 对人脐静脉内皮细胞均无细胞毒性。流式细胞术分析表明,叶酸 HTCC-AuNPs 被 Caco-2、HepG2 和 HeLa 癌细胞内吞的程度明显大于没有叶酸的 AuNPs。但是,半乳糖基 HTCC-AuNPs 仅显示出对 HepG2 细胞的高细胞摄取。

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