title: DNA- and BSA-binding studies and anticancer activity against human breast cancer cells (MCF-7) of the zinc(II) complex coordinated by 5,6-diphenyl-3-(2-pyridyl)-1,2,4-triazine.
abstract: Binding studies of a mononuclear zinc(II) complex, [Zn(dppt)2Cl2] (dppt is 5,6-diphenyl-3-(2-pyridyl)-1,2,4-triazine), with DNA and bovine serum albumin (BSA) have been investigated under physiological conditions. The binding properties of the complex with fish sperm DNA (FS-DNA) have been investigated by UV-Vis absorption, thermal denaturation, competitive DNA-binding studies with ethidium bromide (EB) by fluorescence, and gel electrophoresis techniques. The competitive study with (EB) shows that the complex can displace EB from the DNA-EB system and compete for the DNA-binding sites with EB, which is usually characteristic of the intercalative interaction of compounds with DNA. The value of the fluorescence quenching constant (Ksv) was obtained as 3.1×10(4)M(-1), indicating that this complex shows a high quenching efficiency and a significant degree of binding to DNA. Moreover, the intercalative binding mode has also been verified by the results of UV-Vis absorption, thermal denaturation and gel electrophoresis. The value of Kb at room temperature was calculated to be 1.97×10(5)M(-1), indicating that the complex possesses strong tendency to bind with DNA. This value is very greater than to the values obtained for other zinc(II) complexes. The interaction of the complex with BSA has been studied by UV-Vis absorption, fluorescence and circular dichroism (CD) spectroscopic techniques. The results indicate that the complex has a quite strong ability to quench the fluorescence of BSA and the binding reaction is mainly a static quenching process. The quenching constants (KSV), the binding constants (Kb), the number of binding sites at different temperatures, the binding distance between BSA and the complex (r), and the thermodynamic parameters (ΔH(o), ΔS(o) and ΔG(o)) between BSA and the complex were calculated. The complex exhibits good binding propensity to BSA showing relatively high binding constant values. The positive ΔH(o) and ΔS(o) values indicate that the hydrophobic interaction is main force in the binding of the complex to BSA. Moreover, to evaluate the anticancer properties, the cytotoxicity of the complex has been tested against the human breast adenocarcinoma (MCF-7) cell lines using the MTT assay. The results indicate that the parent complex displays cytotoxicity against human breast cancer cell lines (MCF-7) with an IC50 value of 10.44μM. 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, 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
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
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology; D001943:Breast Neoplasms / Q000188:drug therapy* / Q000378:metabolism / Q000473:pathology; D002417:Cattle; D045744:Cell Line, Tumor; D004273:DNA, Neoplasm / Q000737:chemistry* / Q000378:metabolism; D005260:Female; D006576:Heterocyclic Compounds, 4 or More Rings / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D007364:Intercalating Agents / Q000737:chemistry / Q000494:pharmacology; D012710:Serum Albumin, Bovine / Q000737:chemistry*; D014227:Triazines / Q000737:chemistry / Q000494:pharmacology; D015032:Zinc / Q000737:chemistry / Q000494:pharmacology
chemical_list: D000970:Antineoplastic Agents; D004273:DNA, Neoplasm; D006576:Heterocyclic Compounds, 4 or More Rings; D007364:Intercalating Agents; D014227:Triazines; D012710:Serum Albumin, Bovine; D015032:Zinc
keywords: 5,6-Diphenyl-3-(2-pyridyl)-1,2,4-triazine(dppt); Anticancer; BSA binding; DNA binding; MCF-7; Zinc(II) complex