1. Design, synthesis and evaluation of anticancer activity of ruthenium (II) polypyridyl complexes.
- Author
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Tang B, Wan D, Lai SH, Yang HH, Zhang C, Wang XZ, Zeng CC, and Liu YJ
- Subjects
- A549 Cells, Antineoplastic Agents chemistry, Apoptosis drug effects, Autophagy drug effects, Cell Cycle Checkpoints drug effects, Cell Line, Tumor, HeLa Cells, Hep G2 Cells, Humans, Magnetic Resonance Spectroscopy, Membrane Potential, Mitochondrial drug effects, Proto-Oncogene Proteins c-bcl-2 metabolism, Reactive Oxygen Species metabolism, Spectrometry, Mass, Electrospray Ionization, Antineoplastic Agents pharmacology, Ruthenium Compounds chemistry, Ruthenium Compounds pharmacology
- Abstract
A new ligand PFPIP (PFPIP=2-(2,3,4,5,6-pentafluorophenyl)[4,5-f]imadazo [1,10]phenanthroline) and its four ruthenium(II) polypyridyl complexes [Ru(NN)
2 (PFPIP)](ClO4 )2 (NN=dmb: 4,4'-dimethyl-2,2'-bipyridine, 1; bpy: 2,2'-bipyridine, 2; phen: 1,10-phenanthroline, 3; dmp: 2,9-dimethyl-1,10-phenanthroline, 4) were synthesized and characterized by elemental analysis, IR,1 H NMR,13 C NMR and ESI-MS. The cytotoxic activity in vitro of the ligand and complexes toward BEL-7402, A549, HeLa, HepG2 and MG-63 cell lines was evaluated using MTT method (MTT=(3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide). Complexes 1, 3 and 4 show moderate cytotoxic effect on the cell growth in BEL-7402 cells with IC50 values of 32.1±0.9, 37.9±1.7 and 42.1±3.0μM, respectively. The apoptosis in BEL-7402 cell was investigated with AO/EB and Hoechst 33,258 staining methods. The autophagy in BEL-7402 cell induced by complexes was assayed using MDC staining cell nuclei. The cell invasion, reactive oxygen species (ROS), mitochondrial membrane potential, cell cycle arrest, cellular uptake, comet assay and wound healing were studied under a fluorescent microscope. The complexes can cause autophagy and inhibit the cell invasion, and increase the ROS levels and induce a decrease in the mitochondrial membrane potential. The expression of the proteins related with apoptosis induced by the complexes was assayed by western blot analysis., (Copyright © 2017 Elsevier Inc. All rights reserved.)- Published
- 2017
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