title: Stabilization of G-quadruplex DNA and inhibition of telomerase activity studies of ruthenium(II) complexes.
abstract: Two ruthenium(II) complexes [Ru(IP)2(PIP)](ClO4)2·2H2O (1) and [Ru(PIP)2(IP)](ClO4)2·2H2O (2) (IP=imidazole [4, 5-f] [1,10] phenanthroline, PIP=2-phenylimidazo-[4, 5-f][1,10] phenanthroline) have been synthesized and characterized. The quadruplex binding of the compounds was evaluated by emission spectrum, CD spectroscopy, Visual detection assay and FRET (fluorescence resonance energy transfer)-melting assay. The results show that both complexes can induce the stabilization of quadruplex DNA, while complex 1 is a better G-quadruplex binder than complex 2. Furthermore, polymerase chain reaction-stop assay, electrophoretic mobility shift assay, telomerase repeat amplification protocol and MTT (3-[4,5-Dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide) assay demonstrate that complex 1 not only can stabilize dimer forms of the G-quadruplex at low concentrations but also exhibit better inhibitory activity for telomerase and cancer cells.
authors.affiliation: Department of Chemistry, Jinan University, Guangzhou 510632, PR China; GuangDong Dongguan Health School, Dongguan 523186, PR China.
authors.forename: Qian
authors.initials: Q
authors.lastname: Li
authors.forename: Jingnan
authors.initials: J
authors.lastname: Zhang
authors.forename: Licong
authors.initials: L
authors.lastname: Yang
authors.forename: Qianqian
authors.initials: Q
authors.lastname: Yu
authors.forename: Qingchang
authors.initials: Q
authors.lastname: Chen
authors.forename: Xiuying
authors.initials: X
authors.lastname: Qin
authors.forename: Fangling
authors.initials: F
authors.lastname: Le
authors.forename: Qianling
authors.initials: Q
authors.lastname: Zhang
authors.forename: Jie
authors.initials: J
authors.lastname: Liu
mesh_terms: D017209:Apoptosis / Q000187:drug effects; D002942:Circular Dichroism; D004305:Dose-Response Relationship, Drug; D024202:Electrophoretic Mobility Shift Assay; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D031541:Fluorescence Resonance Energy Transfer; D054856:G-Quadruplexes; D006367:HeLa Cells / Q000187:drug effects; D006801:Humans; D015394:Molecular Structure; D009942:Organometallic Compounds / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D012428:Ruthenium / Q000737:chemistry*; D019098:Telomerase / Q000037:antagonists & inhibitors*
chemical_list: D004791:Enzyme Inhibitors; D009942:Organometallic Compounds; D012428:Ruthenium; D019098:Telomerase
keywords: Anticancer activity; G-quadruplex DNA; Ruthenium(II) complexes; Telomerase