Mitochondrial fragmentation is an important cellular event induced by ruthenium(II) polypyridyl complexes in osteosarcoma cells.

Abstract

A series of ruthenium(II) polypyridyl complexes were synthesized and evaluated for their in vitro anticancer activities. The results showed that ruthenium polypyridyl complexes, especially [Ru(bpy)2 (p-tFPIP)](2+) (2 a; bpy=bipyridine, tFPIP=2-(2-trifluoromethane phenyl)imidazole[4,5-f][1,10]phenanthroline), exhibited novel anticancer activity against human cancer cell lines, but with less toxicity to a human normal cell line. The results of flow cytometry and caspase activities analysis indicated that the 2 a-induced growth inhibition against MG-63 osteosarcoma cells was mainly caused by mitochondria-mediated apoptosis. DNA fragmentation and nuclear condensation as detected by TUNEL-DAPI co-staining further confirmed 2 a-induced apoptotic cell death. Further, fluorescence imaging revealed that ruthenium(II) polypyridyl complexes could target mitochondria to induce mitochondrial fragmentation, accompanied by depletion of mitochondrial membrane potential. Taken together, these findings suggest a potential application of theses ruthenium(II) complexes in the treatment of cancers.

• Authors: Yanxin Du, Xiaoyan Fu, Hong Li, Bolai Chen, Yuhai Guo, Guoyi Su, Hu Zhang, Feipeng Ning, Yongpeng Lin, Wenjie Mei, Tianfeng Chen
• Journal: ChemMedChem (ChemMedChem) Vol. 9 Issue 4 Pg. 714-8 (Apr 2014) ISSN: 1860-7187 [Electronic] Germany
• PMID: 24403015 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
• Copyright: © 2014 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

Chemical References

• Antineoplastic Agents
• Coordination Complexes
• Polymers
• Pyridines
• Ruthenium

Topics

• Antineoplastic Agents (chemical synthesis, chemistry, pharmacology)
• Apoptosis (drug effects)
• Cell Proliferation (drug effects)
• Coordination Complexes (chemical synthesis, chemistry, pharmacology)
• Dose-Response Relationship, Drug
• Drug Screening Assays, Antitumor
• Humans
• MCF-7 Cells
• Mitochondria (drug effects, metabolism)
• Molecular Structure
• Polymers (chemistry)
• Pyridines (chemistry)
• Ruthenium (chemistry)
• Structure-Activity Relationship
• Tumor Cells, Cultured