title: Ruthenium (II) polypyridyl complexes stabilize the bcl-2 promoter quadruplex and induce apoptosis of Hela tumor cells.
abstract: In the present study, the interaction between GC-rich sequence of bcl-2 gene P1 promoter (Pu39) and two ruthenium (II) polypyridyl complexes, [Ru(bpy)₂(tip)]²⁺ (1) and [Ru(phen)₂(tip)]²⁺ (2), was investigated by UV-Visible, fluorescence spectroscopy, circular dichroism, fluorescence resonance energy transfer melting assay and polymerase chain reaction stop assay. Those experimental results indicated that the two complexes can effectively stabilize the G-quadruplex of Pu39. It was found that the complex 2 exhibited greater cytotoxic activity than 1 against human Hela cells and can enter into Hela cells in a short period of time to effectively induce apoptosis of cells. Further experiments found that complexes 1 and 2 had as potent inhibitory effects on ECV-304 cell migration as suramin. Those noteworthy results provide new insights into the development of anticancer agents for targeting G-quadruplex DNA.
authors.affiliation: Department of Chemistry, Jinan University, Guangzhou 510632, People's Republic of China.
authors.forename: Chuan
authors.initials: C
authors.lastname: Wang
authors.forename: Qianqian
authors.initials: Q
authors.lastname: Yu
authors.forename: Licong
authors.initials: L
authors.lastname: Yang
authors.forename: Yanyu
authors.initials: Y
authors.lastname: Liu
authors.forename: Dongdong
authors.initials: D
authors.lastname: Sun
authors.forename: Yongchao
authors.initials: Y
authors.lastname: Huang
authors.forename: Yanhui
authors.initials: Y
authors.lastname: Zhou
authors.forename: Qianling
authors.initials: Q
authors.lastname: Zhang
authors.forename: Jie
authors.initials: J
authors.lastname: Liu
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects*; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D054856:G-Quadruplexes / Q000187:drug effects*; D006367:HeLa Cells; D006801:Humans; D008958:Models, Molecular; D009942:Organometallic Compounds / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D011401:Promoter Regions, Genetic / Q000187:drug effects* / Q000235:genetics; D019253:Proto-Oncogene Proteins c-bcl-2 / Q000235:genetics*; D011725:Pyridines / Q000737:chemistry*; D012428:Ruthenium / Q000737:chemistry*; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D009942:Organometallic Compounds; D019253:Proto-Oncogene Proteins c-bcl-2; D011725:Pyridines; D012428:Ruthenium