Authors: BaoLi Fei Bin Yin DongDong Li WuShuang Xu Yang Lu
Publish Date: 2016/09/14
Volume: 21, Issue: 8, Pages: 987-996
Abstract
To develop chiral anticancer drug candidates for molecular target DNA the synthesis and characterization of a novel enantiomerically pure copperII complex Cu 1 Cl 2 2 of an optically pure ligand Npyridin2ylmethylene dehydroabietylamine 1 was carried out The coordination geometry of the copper center is a distorted squareplanar arrangement The interactions of 1 and 2 with salmon sperm DNA were investigated by viscosity measurements UV fluorescence and circular dichroism CD spectroscopic techniques All the results reveal that 1 and 2 interacted with DNA through intercalation and 2 exhibited a higher DNA binding ability Further 1 and 2 could cleave supercoiled pBR322 DNA by single strand and 2 displayed stronger cleavage ability in the presence of ascorbic acid In vitro cytotoxicity of 1 and 2 against HeLa SiHa HepG2 and A431 cancer cell lines was studied using CCK8 assay The results indicate that 2 had a superior cytotoxicity than 1 and the widely used drug cisplatin under identical conditions Flow cytometry analysis demonstrates 2 produced death of HeLa cancer cells through an apoptotic pathway Cell cycle analysis shows that 2 mainly arrested HeLa cells at the S phaseThe authors gratefully acknowledge the financial support from State Key Laboratory of Coordination Chemistry of Nanjing University the Priority Academic Program Development of Jiangsu Higher Education Institutions and College and University Graduate Research Innovation Project of Jiangsu Province
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