Ruthenium(II) complexes: DNA-binding, cytotoxicity, apoptosis, cellular localization, cell cycle arrest, reactive oxygen species, mitochondrial membrane potential and western blot analysis

作者：Li Wei; Jiang Guang Bin; Yao Jun Hua; Wang Xiu Zhen; Wang Ji; Han Bing Jie; Xie Yang Yin; Lin Gan Jian; Huang Hong Liang^*; Liu Yun Jun

来源：Journal of Photochemistry and Photobiology B: Biology , 2014, 140: 94-104.

DOI：10.1016/j.jphotobiol.2014.07.011

• Ru(II) polypyridyl complex
• Cytotoxicity in vitro
• Cell cycle arrest
• Reactive oxygen species
• Western blot analysis
• DNA-binding

The aim of our study was to investigate DNA-binding and cytotoxic activity of the four new Ru(II) polypyridyl complexes [Ru(dmb)(2)(HMHPIP)](ClO4)(2) (1), [Ru(bpy)(2)(HMHPIP)I(ClO4)(2) (2), [Ru(Phen)(2) (HMHPIP)](ClO4)(2) (3) and [Ru(dmp)(2)(HMHPIP)](ClO4)(2) (4). The complexes interact with DNA through intercalative mode and show relatively high cytotoxic activity against A549 cells, no cytotoxicity toward MG-63 cells. Complexes 1-4 can enhance the levels of ROS in A549 cells and induce the decrease of the mitochondrial membrane potential. These complexes inhibit the cell growth in A549 cells at G0/G1 or S phase. Complex 3 activated caspase 7, and down-regulated the expression of the anti-apoptotic protein Bcl-2. Complexes 1-4 induce apoptosis in A549 cells through ROS-mediated mitochondrial dysfunction pathway.

• 单位
  广东药学院