title: A mononuclear Ni(II) complex with 5,6-diphenyl-3-(2-pyridyl)-1,2,4-triazine: DNA- and BSA-binding and anticancer activity against human breast carcinoma cells.
abstract: DNA- and BSA-binding properties of a mononuclear Ni(II) complex, [Ni(dppt)2Cl2] (dppt = 5,6-diphenyl-3-(2-pyridyl)-1,2,4-triazine), have been investigated under physiological conditions. The interaction of the complex with the fish sperm DNA (FS-DNA) has been studied by UV-Vis absorption, thermal denaturation, viscosity measurement, competitive DNA-binding studies with ethidium bromide (EB) by fluorescence, and gel electrophoresis technique. The experimental results indicate that the complex interacts with DNA by intercalative binding mode. The competitive study with ethidium bromide (EB) shows that the complex competes for the DNA-binding sites with EB and displaces the DNA-bound EB molecule. The interactions of the dppt ligand and the complex with BSA have been studied by UV-Vis absorption and fluorescence spectroscopic techniques. The values of Kb for the BSA-dppt and the BSA-complex systems at room temperature were calculated to be 0.14×10(4) M(-1) and 0.32×10(5) M(-1), respectively, indicating that the complex has stronger tendency to bind with BSA than the dppt ligand. The quenching constants (Ksv), binding constants (Kbin), and number of binding sites (n) at different temperatures, as well as the binding distance (r) and thermodynamic parameters (ΔH°, ΔS° and ΔG°) have been calculated for the BSA-dppt and the BSA-complex systems. The cytotoxicities of the dppt ligand and the complex have been also tested against the human breast adenocarcinoma (MCF-7) cell line using the MTT assay. The results indicate that the dppt ligand and the complex display cytotoxicity against human breast cancer cell lines (MCF-7) with the IC50 values of 17.35 μM and 13.00 μM, respectively. It is remarkable that the complex can introduce as a potential anticancer drug.
authors.affiliation: Department of Chemistry, Shahid Bahonar University of Kerman, Kerman 76169-133, Iran.
authors.forename: Marzieh
authors.initials: M
authors.lastname: Anjomshoa
authors.affiliation: Department of Chemistry, Isfahan University of Technology, Isfahan 84156-83111, Iran. Electronic address: hadad@cc.iut.ac.ir.
authors.forename: Hassan
authors.initials: H
authors.lastname: Hadadzadeh
authors.affiliation: Department of Chemistry, Shahid Bahonar University of Kerman, Kerman 76169-133, Iran.
authors.forename: Seyed Jamilaldin
authors.initials: SJ
authors.lastname: Fatemi
authors.affiliation: Department of Biotechnology, Institute of Science, High Technology & Environmental Science, Graduate University of Advance Technology, Kerman, Iran. Electronic address: m.torkzadeh@kgut.ac.ir.
authors.forename: Masoud
authors.initials: M
authors.lastname: Torkzadeh-Mahani
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology*; D001667:Binding, Competitive / Q000187:drug effects; D001943:Breast Neoplasms / Q000473:pathology*; D002417:Cattle; D056831:Coordination Complexes / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D004247:DNA / Q000378:metabolism*; D004583:Electrons; D024202:Electrophoretic Mobility Shift Assay; D004996:Ethidium / Q000378:metabolism; D005260:Female; D005399:Fishes; D006801:Humans; D007700:Kinetics; D061986:MCF-7 Cells; D009532:Nickel / Q000494:pharmacology*; D009691:Nucleic Acid Denaturation / Q000187:drug effects; D011485:Protein Binding / Q000187:drug effects; D012710:Serum Albumin, Bovine / Q000378:metabolism*; D013050:Spectrometry, Fluorescence; D013056:Spectrophotometry, Ultraviolet; D013696:Temperature; D014227:Triazines / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology; D014783:Viscosity
chemical_list: D000970:Antineoplastic Agents; D056831:Coordination Complexes; D014227:Triazines; C000600058:dichloro(5,6-diphenyl-3-(2-pyridyl)-1,2,4-triazine)nickel(II); D012710:Serum Albumin, Bovine; C093444:1,2,4-triazine; D009532:Nickel; D004247:DNA; D004996:Ethidium
keywords: 5,6-Diphenyl-3-(2-pyridyl)-1,2,4-triazine (dppt); Anticancer; BSA-binding; DNA-binding; MCF-7 cells; Nickel(II) complex