title: Synthesis, in-vitro cytotoxic activity and DNA interactions of new dicarboxylatoplatinum(II) complexes with 2-hydroxymethylbenzimidazole as carrier ligands.
abstract: OBJECTIVE
  The aim of this study was to investigate the in-vitro cytotoxic activity of new platinum(II) complexes on the human HeLa (ER-), MCF-7 (ER+) and MDA-MB 231 (ER-) cell lines. Furthermore, we investigated plasmid DNA interactions and inhibition of BamHI and HindIII restriction enzyme activity of the complex 1-4,7.
  
  
  METHODS
  Platinum(II) complexes were synthesised from precursor complexes of [PtL2 Cl2 ] and [PtL2 I2 ]. Their cytotoxic activity was tested by MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay. Their plasmid DNA interactions and restriction enzyme activities were also investigated using the agarose gel electrophoresis method.
  
  
  RESULTS
  The growth inhibitory effect results showed that the cytotoxicity of complex 2 was found to be the most active complex among the synthesised complexes.
  
  
  CONCLUSIONS
  The MTT results showed that complex 2 was found to be cytotoxic equal to cisplatin and higher than carboplatin against the MCF-7 and MDA-MB-231 cell lines. Furthermore, the estrogen or progesterone co-treatment slightly increased the cytotoxicity of complex 2, the cisplatin and carboplatin compared with the complex 2 tested alone in 50 μm concentration. According to plasmid DNA interaction and the restriction studies, complexes 1-4,7 modified the tertiary structure of pBR322 plasmid DNA, and complexes 2-4 prevented enzyme digestion at high concentrations.
authors.affiliation: Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Mersin University, Mersin, Turkey.
authors.forename: Semra
authors.initials: S
authors.lastname: Utku
authors.forename: Azime Berna
authors.initials: AB
authors.lastname: Ozçelik
authors.forename: Fatma
authors.initials: F
authors.lastname: Gümüş
authors.forename: Sükran
authors.initials: S
authors.lastname: Yılmaz
authors.forename: Taibe
authors.initials: T
authors.lastname: Arsoy
authors.forename: Leyla
authors.initials: L
authors.lastname: Açık
authors.forename: Ayten
authors.initials: A
authors.lastname: Celebi Keskin
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000494:pharmacology / Q000627:therapeutic use*; D001562:Benzimidazoles / Q000737:chemistry*; D016190:Carboplatin / Q000494:pharmacology / Q000627:therapeutic use; D002945:Cisplatin / Q000494:pharmacology / Q000627:therapeutic use; D004247:DNA / Q000187:drug effects* / Q000378:metabolism; D004354:Drug Screening Assays, Antitumor; D004967:Estrogens / Q000494:pharmacology / Q000627:therapeutic use; D006367:HeLa Cells; D006801:Humans; D066298:In Vitro Techniques; D008024:Ligands; D061986:MCF-7 Cells; D009369:Neoplasms / Q000188:drug therapy*; D010957:Plasmids / Q000187:drug effects* / Q000235:genetics; D010984:Platinum / Q000494:pharmacology / Q000627:therapeutic use*; D011374:Progesterone / Q000494:pharmacology / Q000627:therapeutic use; D011372:Progestins / Q000494:pharmacology / Q000627:therapeutic use; D015183:Restriction Mapping
chemical_list: D000970:Antineoplastic Agents; D001562:Benzimidazoles; D004967:Estrogens; D008024:Ligands; D011372:Progestins; D010984:Platinum; D011374:Progesterone; D004247:DNA; D016190:Carboplatin; D002945:Cisplatin
keywords: DNA binding; benzimidazole; cytotoxic activity; gel electrophoresis; platinum(II) complexes