Muthukumarasamyvel Thangavel, Rajendran Ganapathy, Santhana Panneer Devendrapandi, Kasthuri Jayapalan, Kathiravan Krishnan, Rajendiran Nagappan
Department of Polymer Science and Department of Biotechnology, University of Madras, Guindy Campus, Chennai 600025, Tamil Nadu, India.
Department of Chemistry, Quaid-E-Millath Government College for Women (Autonomous), Chennai 600002, Tamil Nadu, India.
ACS Omega. 2017 Jul 31;2(7):3527-3538. doi: 10.1021/acsomega.7b00353. Epub 2017 Jul 25.
Herein, we report the surface functionality of dicationic cysteamine conjugated cholic acid (DCaC), dicationic cysteamine conjugated deoxycholic acid (DCaDC), and dicationic cysteamine conjugated lithocholic acid (DCaLC) templated gold nanoparticles (AuNPs) on mammalian cells. The haemocompatibility of the synthesized NPs was evaluated by in vitro hemolysis and erythrocyte sedimentation rate using human red blood cells (RBCs). In all of the systems, no toxicity was observed on human erythrocytes (RBCs) up to the concentration of 120 μg/mL. The anticancer activity of these dicationic amphiphile-stabilized AuNPs on A549 lung cancer cells was demonstrated by in vitro cell viability assay, intracellular reactive oxygen species estimation by DCFH-DA, apoptosis analysis using AO-EtBr fluorescence staining, DNA fragmentation analysis by agarose gel electrophoresis, and western blot analysis of caspase-3 expression. These results suggest that the cytotoxicity of AuNPs to A549 cells increase with the dose and hydrophobicity of amphiphiles and were found to be in the order: DCaLC-AuNPs > DCaDC-AuNPs > DCaC-AuNPs.
在此,我们报告了二价半胱胺共轭胆酸(DCaC)、二价半胱胺共轭脱氧胆酸(DCaDC)和二价半胱胺共轭石胆酸(DCaLC)模板化金纳米颗粒(AuNPs)在哺乳动物细胞上的表面功能。使用人红细胞(RBCs)通过体外溶血和红细胞沉降率评估合成纳米颗粒的血液相容性。在所有系统中,在浓度高达120μg/mL时,未观察到对人红细胞(RBCs)的毒性。通过体外细胞活力测定、DCFH-DA法测定细胞内活性氧、AO-EtBr荧光染色法进行凋亡分析、琼脂糖凝胶电泳法进行DNA片段分析以及caspase-3表达的蛋白质印迹分析,证明了这些二价两亲物稳定的AuNPs对A549肺癌细胞的抗癌活性。这些结果表明,AuNPs对A549细胞的细胞毒性随着两亲物的剂量和疏水性增加而增加,并且发现顺序为:DCaLC-AuNPs > DCaDC-AuNPs > DCaC-AuNPs。