title: Synthesis, DNA-binding and topoisomerase inhibitory activity of ruthenium(II) polypyridyl complexes.
abstract: Two ruthenium(II) complexes [Ru(bpy)(2)(bfipH)](2+) (1) and [Ru(phen)(2)(bfipH)](2+) (2) have been synthesized and characterized. The DNA-binding behaviors of complexes were studied by using spectroscopic and viscosity measurements. Results suggested that the two complexes bind to DNA in an intercalative mode. Complexes 1 and 2 can efficiently photocleave pBR322 DNA in vitro under irradiation, singlet oxygen ((1)O(2)) was proved to contribute to the DNA photocleavage process. Topoisomerase inhibition and DNA strand passage assay confirmed that two Ru(II) complexes acted as efficient dual inhibitors of topoisomerases I and II. In MTT cytotoxicity studies, two Ru(II) complexes exhibited antitumor activity against BEL-7402, HeLa, MCF-7 tumor cells. The AO/EB staining assay indicated that Ru(II) complexes could induce the apoptosis of HeLa cells.
authors.affiliation: MOE Laboratory of Bioinorganic and Synthetic Chemistry, State Key Laboratory of Optoelectronic Materials and Technologies, School of Chemistry and Chemical Engineering, Sun Yat-Sen University, Guangzhou 510275, PR China.
authors.forename: Ke-Jie
authors.initials: KJ
authors.lastname: Du
authors.forename: Jin-Quan
authors.initials: JQ
authors.lastname: Wang
authors.forename: Jun-Feng
authors.initials: JF
authors.lastname: Kou
authors.forename: Guan-Ying
authors.initials: GY
authors.lastname: Li
authors.forename: Li-Li
authors.initials: LL
authors.lastname: Wang
authors.forename: Hui
authors.initials: H
authors.lastname: Chao
authors.forename: Liang-Nian
authors.initials: LN
authors.lastname: Ji
mesh_terms: D000818:Animals; D002417:Cattle; D045744:Cell Line, Tumor; D018360:Crystallography, X-Ray; D004247:DNA / Q000737:chemistry / Q000378:metabolism*; D053837:DNA Cleavage / Q000187:drug effects / Q000528:radiation effects; D026942:DNA Topoisomerases / Q000378:metabolism*; D006801:Humans; D020128:Inhibitory Concentration 50; D009942:Organometallic Compounds / Q000138:chemical synthesis / Q000737:chemistry / Q000378:metabolism* / Q000494:pharmacology*; D012428:Ruthenium / Q000737:chemistry*; D059003:Topoisomerase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000378:metabolism* / Q000494:pharmacology*
chemical_list: D009942:Organometallic Compounds; D059003:Topoisomerase Inhibitors; D012428:Ruthenium; D004247:DNA; D026942:DNA Topoisomerases