title: Cytotoxicity of gold(III) complexes on A549 human lung carcinoma epithelial cell line.
abstract: We have studied the kinetics of the complex formation of gold(III) complexes, [Au(en)Cl2]+ (dichlorido( ethylendiamine)aurate(III)-ion) [Au(dach)Cl2] (dichloride(1,2-diaminocyclohexane)aurate(III)-ion) and [Au(bipy)Cl2]+ (dichlorido(2,2'-bipyridyl)aurate(III)-ion) with guanosine5'-monophosphate (5'-GMP). It was shown that 5'-GMP have a high affinity for gold(III) complex, which may have important biological implications, since the interactions of Au(III) with DNA are thought to be responsible for the anti-tumor activity. The [Au(bipy)Cl2]+ complex is more reactive than [Au(en)Cl2]+ or [Au(dach)Cl2]+. The activation parameters for all studied reactions suggest an associative substitution mechanism. The cytotoxicity of gold(III) complexes was tested on A549 human lung carcinoma epithelial cell line and was evaluated by cytotoxic (MTT and LDH test) and apoptotic assays. The results showed that all tested gold(III) complexes displayed cytotoxic effect on A549 cells. Among the tested gold (III) complexes, AuBIPY showed the best cytotoxic effects.
authors.affiliation: Faculty of Medicine, University of Kragujevac, Kragujevac, Serbia. arne@medf.kg.ac.rs
authors.forename: Milos
authors.initials: M
authors.lastname: Arsenijević
authors.forename: Marija
authors.initials: M
authors.lastname: Milovanovic
authors.forename: Vladislav
authors.initials: V
authors.lastname: Volarevic
authors.forename: Ana
authors.initials: A
authors.lastname: Djeković
authors.forename: Tatjana
authors.initials: T
authors.lastname: Kanjevac
authors.forename: Nebojsa
authors.initials: N
authors.lastname: Arsenijević
authors.forename: Svetlana
authors.initials: S
authors.lastname: Dukić
authors.forename: Zivadin D
authors.initials: ZD
authors.lastname: Bugarcić
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects; D002294:Carcinoma, Squamous Cell / Q000188:drug therapy* / Q000473:pathology; D049109:Cell Proliferation / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D004847:Epithelial Cells / Q000187:drug effects* / Q000473:pathology; D006801:Humans; D008175:Lung Neoplasms / Q000188:drug therapy* / Q000473:pathology; D050607:Organogold Compounds / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured
chemical_list: D000970:Antineoplastic Agents; D050607:Organogold Compounds