title: Anticancer activity for targeting telomeric G-quadruplex and antiangiogenesis of a novel Ru(II)-Se complex.
abstract: A new Ru(II)-Se complex, Ru(bpy)2L2Cl2 (bpy = 2,2'-bipyridine, L = 1,10-phenanthrolineselenazole) (Ru-Se) has been synthesized and characterized. The G-quadruplex DNA-binding properties of the complex and its selenium ligand (Phen-Se) were evaluated by thermal denaturation study, polymerase chain reaction (PCR) stop assay, and telomerase repeat amplification protocol (TRAP). The results showed that the obtained complex could induce and stabilize G-quadruplex structure as well as exhibit potent inhibitory activity against telomerase. In vitro cytotoxicity studies showed that complex Ru-Se inhibited the cancer cell growth through apoptosis. However, the presence of the ligand Phen-Se did not appear to have a significant effect either on G-quadruplex binding or on biological activity. Furthermore, the cell migration assay and the tube formation assay also demonstrated that the complex Ru-Se significantly inhibited human umbilical vascular endothelial cell (HUVEC) proliferation, migration, and tube formation. These findings indicate that the Ru-Se complex may be a potential telomerase inhibitor and a viable drug candidate in antiangiogenesis for anticancer therapies.
authors.affiliation: College of Chemistry and Biology, Beihua University, Jilin, 132013, People's Republic of China.
authors.forename: Lijun
authors.initials: L
authors.lastname: Wang
authors.forename: Chuping
authors.initials: C
authors.lastname: Zheng
authors.forename: Yanyu
authors.initials: Y
authors.lastname: Liu
authors.forename: Fangling
authors.initials: F
authors.lastname: Le
authors.forename: Fang
authors.initials: F
authors.lastname: Yang
authors.forename: Xiuying
authors.initials: X
authors.lastname: Qin
authors.forename: Chuan
authors.initials: C
authors.lastname: Wang
authors.forename: Jie
authors.initials: J
authors.lastname: Liu
mesh_terms: D015082:2,2'-Dipyridyl / Q000737:chemistry; D020533:Angiogenesis Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects; D045744:Cell Line, Tumor; D002465:Cell Movement / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D056831:Coordination Complexes / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D054856:G-Quadruplexes / Q000187:drug effects*; D061307:Human Umbilical Vein Endothelial Cells; D006801:Humans; D008024:Ligands; D008968:Molecular Conformation; D009691:Nucleic Acid Denaturation / Q000187:drug effects; D016566:Organoselenium Compounds / Q000737:chemistry*; D010618:Phenanthrolines / Q000737:chemistry; D012428:Ruthenium / Q000737:chemistry*; D016615:Telomere / Q000187:drug effects* / Q000235:genetics
chemical_list: D020533:Angiogenesis Inhibitors; D056831:Coordination Complexes; D008024:Ligands; D016566:Organoselenium Compounds; D010618:Phenanthrolines; D015082:2,2'-Dipyridyl; D012428:Ruthenium; C025205:1,10-phenanthroline