title: 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.affiliation: Orthopedics Department, Guangdong Provincial Hospital of Traditional Chinese Medicine, 111 Dade Road, Guangzhou 510120, Guangdong (China).
authors.forename: Yanxin
authors.initials: Y
authors.lastname: Du
authors.forename: Xiaoyan
authors.initials: X
authors.lastname: Fu
authors.forename: Hong
authors.initials: H
authors.lastname: Li
authors.forename: Bolai
authors.initials: B
authors.lastname: Chen
authors.forename: Yuhai
authors.initials: Y
authors.lastname: Guo
authors.forename: Guoyi
authors.initials: G
authors.lastname: Su
authors.forename: Hu
authors.initials: H
authors.lastname: Zhang
authors.forename: Feipeng
authors.initials: F
authors.lastname: Ning
authors.forename: Yongpeng
authors.initials: Y
authors.lastname: Lin
authors.forename: Wenjie
authors.initials: W
authors.lastname: Mei
authors.forename: Tianfeng
authors.initials: T
authors.lastname: Chen
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects; D049109:Cell Proliferation / Q000187:drug effects; D056831:Coordination Complexes / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D061986:MCF-7 Cells; D008928:Mitochondria / Q000187:drug effects* / Q000378:metabolism; D015394:Molecular Structure; D011108:Polymers / Q000737:chemistry*; D011725:Pyridines / Q000737:chemistry*; D012428:Ruthenium / Q000737:chemistry*; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured
chemical_list: D000970:Antineoplastic Agents; D056831:Coordination Complexes; D011108:Polymers; D011725:Pyridines; D012428:Ruthenium
keywords: anticancer agents; apoptosis; mitochondria membrane potential; mitochondrial fragmentation; ruthenium polypyridyl complexes