Preparation, characterization and biological evaluation of two chiral binuclear copper(II) complexes

October 11, 2018

Title

Preparation, characterization and biological evaluation of two chiral binuclear copper(II) complexes

Author

Jing-Jing Suo, Zhong-Ying Ma, Jing-Yuan Xu, Jin-Lei Tian, Xin Liu

Year

2017

Journal

Applied Organometallic Chemistry

Abstract

Two chiral Cu(II) complexes of [Cu2(R-L)2](PF6)2·2C2H5OH (1) and [Cu2(S-L)2](PF6)2·2C2H5OH (2) (HL = 2-(Bis(quinolin-2-ylmethyl)amino)-1-propanol) were designed and synthesized to serve as chemical nucleases and anticancer drugs. X-ray crystallography revealed that two complexes contain chiral binuclear cations and PF6− anions. The interaction of two complexes with CT-DNA was researched via various spectroscopic techniques and viscosity measurement, indicating that the complexes were bound to CT-DNA by a classical intercalation binding mode. In addition, the two complexes exhibited remarkable DNA cleavage activity with an optimal dosage of 10 μM in the absence of any exogenous oxidant agent. Both of the complexes showed excellent in vitro cytotoxicity on A549 cell lines with IC50values in the low micromolar range. Moreover, complex 2 could damage DNA of A549 cells into fragmentation and then induced cell apoptosis in a dose-dependent manner, which was demonstrated by comet assay and Hoechst 33342 staining experiment. Further research showed that complex 2 could also induce G2 and S phase cell cycle arrest.

Instrument

J-715

Keywords

Circular dichroism, Stereochemistry, Inorganic chemistry