title: Design, synthesis, DNA-binding affinity, cytotoxicity, apoptosis, and cell cycle arrest of Ru(II) polypyridyl complexes.
abstract: A novel polypyridyl ligand CNPFIP (CNPFIP=2-(5(4-chloro-2-nitrophenyl)furan-2-yl)-1H-imidazo[4,5f][1,10]phenanthroline) and its mononuclear Ru(II) polypyridyl complexes of [Ru(phen)2CNPFIP](2+)(1) (phen=1,10-phenanthroline), [Ru(bpy)2CNPFIP](2+)(2) (bpy=2,2'-bipyridine), and [Ru(dmb)2CNPFIP](2+)(3) (dmb=4,4'-dimethyl-2,2'-bipyridine) have been synthesized successfully and characterized thoroughly by elemental analysis, UV/Vis, IR, NMR, and ESI-MS. The interaction of the Ru(II) complexes with calf thymus DNA (CT-DNA) was investigated by absorption titration, fluorescence, viscosity measurements. The experimental results suggest that three complexes bind to CT-DNA through an intercalative mode and the DNA-binding affinity of complex 1 is greater than that of complexes 2 and 3. The photocleavage of plasmid pBR322 DNA by ruthenium complexes 1, 2, and 3 was investigated. We have also tested three complexes for their antimicrobial activity against Escherichia coli (Gram-negative) and Staphylococcus aureus (Gram-positive) bacteria. The in vitro cytotoxicity of these complexes was evaluated by MTT assay, and complex 1 shows higher cytotoxicity than 2 and 3 on HeLa cells. The induced apoptosis and cell cycle arrest of HeLa cells were investigated by flow cytometry for 24h. The molecular docking of ruthenium complexes 1, 2, and 3 with the active site pocket residues of human DNA TOP1 was performed using LibDock.
authors.affiliation: Department of Chemistry, Osmania University, Hyderabad 500007, Telangana State, India.
authors.forename: Putta
authors.initials: P
authors.lastname: Venkat Reddy
authors.affiliation: Department of Chemistry, Osmania University, Hyderabad 500007, Telangana State, India.
authors.forename: Mallepally Rajender
authors.initials: MR
authors.lastname: Reddy
authors.affiliation: Department of Chemistry, Osmania University, Hyderabad 500007, Telangana State, India.
authors.forename: Srishailam
authors.initials: S
authors.lastname: Avudoddi
authors.affiliation: Department of Chemistry, Osmania University, Hyderabad 500007, Telangana State, India.
authors.forename: Yata
authors.initials: Y
authors.lastname: Praveen Kumar
authors.affiliation: Department of Chemistry, Osmania University, Hyderabad 500007, Telangana State, India.
authors.forename: Chintakuntla
authors.initials: C
authors.lastname: Nagamani
authors.affiliation: Department of Chemistry, Osmania University, Hyderabad 500007, Telangana State, India.
authors.forename: Nancherla
authors.initials: N
authors.lastname: Deepika
authors.affiliation: Department of Biochemistry, Osmania University, Hyderabad 500007, Telangana State, India.
authors.forename: K
authors.initials: K
authors.lastname: Nagasuryaprasad
authors.affiliation: Department of Biochemistry, Osmania University, Hyderabad 500007, Telangana State, India.
authors.forename: Surya Satyanarayana
authors.initials: SS
authors.lastname: Singh
authors.affiliation: Department of Chemistry, Osmania University, Hyderabad 500007, Telangana State, India. Electronic address: ssnsirasani@gmail.com.
authors.forename: Sirasani
authors.initials: S
authors.lastname: Satyanarayana
mesh_terms: D017209:Apoptosis / Q000187:drug effects*; D059447:Cell Cycle Checkpoints / Q000187:drug effects*; D003603:Cytotoxins / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D004926:Escherichia coli / Q000254:growth & development*; D006367:HeLa Cells; D006801:Humans; D011725:Pyridines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D012428:Ruthenium / Q000737:chemistry*; D013211:Staphylococcus aureus / Q000254:growth & development*
chemical_list: D003603:Cytotoxins; D011725:Pyridines; D012428:Ruthenium
keywords: Antimicrobial activity; Apoptosis and cell cycle arrest; Cytotoxicity; Mononuclear Ru(II) polypyridyl complexes; Photocleavage