Kate Anup N, Kumbhar Anupa A, Khan Ayesha A, Joshi Pranaya V, Puranik Vedavati G
Department of Chemistry, University of Pune , Pune 411007, India.
Bioconjug Chem. 2014 Jan 15;25(1):102-14. doi: 10.1021/bc400385d. Epub 2013 Dec 19.
The thiosemicarbazone derivative of anthracene (ATSC, anthracene thiosemicarbazone 1) and its copper(II) complex (CuATSC, 2) were synthesized and characterized by spectroscopic, electrochemical, and crystallographic techniques. Interaction of 1 and 2 with calf thymus (CT) DNA was explored using absorption and emission spectral methods, and viscosity measurements reveal a partial-intercalation binding mode. Their protein binding ability was monitored by the quenching of tryptophan emission using bovine serum albumin (BSA) as a model protein. Furthermore, their cellular uptake, in vitro cytotoxicity testing on the HeLa cell line, and flow cytometric analysis were carried out to ascertain the mode of cell death. Cell cycle analysis indicated that 1 and 2 cause cell cycle arrest in sub-G1 phase.
合成了蒽的硫代氨基脲衍生物（ATSC，蒽硫代氨基脲1）及其铜（II）配合物（CuATSC，2），并通过光谱、电化学和晶体学技术对其进行了表征。采用吸收光谱和发射光谱法研究了1和2与小牛胸腺（CT）DNA的相互作用，粘度测量结果表明其结合模式为部分嵌入。以牛血清白蛋白（BSA）为模型蛋白，通过色氨酸发射淬灭监测它们的蛋白质结合能力。此外，还进行了它们的细胞摄取、对HeLa细胞系的体外细胞毒性测试以及流式细胞术分析，以确定细胞死亡模式。细胞周期分析表明，1和2会导致细胞周期停滞在亚G1期。
