Browsing by Author "Kavukcu, SB"

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    Ruthenium compounds: Are they the next-era anticancer agents?
    Kavukcu, SB; Özverel, CS; Kiyak, N; Vatansever, HS; Türkmen, H
    This study focuses on the cytotoxic activity of ruthenium(II) complexes, denoted as Ru1-8, which exhibit coordination with nitrogen (amine and amide), oxygen, and sulfur donor atoms, coupled with aryl and aliphatic wingtips. Specifically, the complexes were evaluated for their impact on the MCF-7 breast cancer cell line. A systematic exploration of various parameters, including solubility, donor atom type, metal number, carbon chain length, aromatic ring presence, and molecular weight, was conducted to discern their influence on cytotoxic activity. The investigation involved assessing the cell viability across five concentrations (100, 50, 25, 10, and 5 mu M) for five distinct monometallic and three bimetallic ruthenium complexes. Notably, Ru3, characterized by an extended carbon chain length (dodecyl) and favorable oil solubility facilitating cellular membrane penetration, demonstrated particularly promising results with the IC50 value of 1.03 mu M. This research underscores the critical role of ligand design in shaping the cytotoxic potential of ruthenium(II) complexes and emphasizes the suitability of the Ru(II) p-cymene complexes, as demonstrated by their robust activity against breast cancer in this specific investigation. Novel Ru(II) arene complexes were prepared. The cytotoxic activities of these complexes were investigated on MCF-7 cell line. The structure-activity relationships for the complexes containing Namine/Namine, Namine/Namide, Namide/Oamide, and Namide/Sthiolate/Sthiolate-chelating ligands were investigated. The promising results were obtained. image
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    Synthesis and cytotoxic activities of organometallic Ru(II) diamine complexes
    Kavukcu, SB; Sahin, O; Vatansever, HS; Kurt, FO; Korkmaz, M; Kendirci, R; Pelit, L; Türkmen, H
    A series of mono and bimetallic ruthenium(II) arene complexes bearing diamine (Ru1-6) were prepared and fully characterized by H-1, C-13, F-19, and P-31 NMR spectroscopy and elemental analysis. The crystal structure of the bimetallic complex (Ru-5) was determined by X-ray crystallography. Monometallic analogues (Ru1-3) were synthesized to investigate the contributions of ruthenium and the other organic groups (aren, ethylenediamine, butyl) to the activity. The electrochemical behaviors of mono and bimetallic complexes were obtained from the relationship between cyclic voltammetry (CV) and the biological activities of the compounds. The cytotoxic activities of the complexes (Ru1-6) were tested against wide-scale cancer cell lines, namely HeLa, MDA-MB-231, DU-145, LNCaP, Hep-G2, Saos-2, PC-3, and MCF-7, and normal cell lines 3T3-L1 and Vero. Diamine Ru(II) arene complexes have unique biological characteristics and they are promising models for new anticancer drug development. MTT analysis reveals that each synthesized Ru complex showed cytotoxic activity towards the different cancer cells. In particular, three Ru complexes (Ru-3, Ru-5 and Ru-6) showed less toxic effects on the cancer cells than the others. These novel Ru complexes affected both cancer and normal cell lines. As they had a toxic effect on the cells, the dosage applied should be tested before being used for in vivo applications. Cytotoxicity tests have shown that the bimetallic complex Ru-6 was effective on all cancer cells. The effect of bimetallic enhancement on cancer cell lines, the systematic variation of the intermetallic distance and the ligand donor properties of the mono and bimetallic complexes were explored based on the cytotoxic activity. The interaction with FS-DNA and the stability/aquation of the complexes (Ru-3 and Ru-6) were investigated with H-1 NMR spectroscopy. The binding modes between the complexes (Ru-3 and Ru-6) and DNA were investigated via UV-Vis spectroscopy.
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    Cell Death Mechanism of Organometallic Ruthenium(II) and Iridium(III) Arene Complexes on HepG2 and Vero Cells
    Kavukcu, SB; Ensarioglu, HK; Karabiyik, H; Vatansever, HS; Türkmen, H
    Due to side effects and toxicity associated with platinum-derived metal-based drugs, extensive research has been conducted on ruthenium (Ru) complexes. We aim to synthesize a highly oil soluble Ru(II)-p-cymene complex (Ru1) with an aliphatic chain group, a bimetallic Ru(II)-p-cymene complex (Ru2) with N,S,S triple-coordination and a bimetallic Ir(III)-pentamethylcyclopentadienyl complex (Ir1) with S,S double-coordination. Subsequently, we investigate the effects of these complexes on Vero and HepG2 cell lines, focusing on cell death mechanisms. Characterization of the complexes is performed through nuclear magnetic resonance spectroscopy (H-1 and C-13 NMR) and Fourier-transform infrared spectroscopy. The effective doses are determined using the (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide) (MTT) assay, applying different doses of the complexes to the two cell lines for 24 and 48 h, respectively. Immunoreactivities of Bax, Bcl2, caspase-3, RIP3, and RIPK1 are analyzed using the indirect immunoperoxidase technique. Notably, all the complexes (Ru1, Ru2, and Ir1) exhibit distinct cell death mechanisms, showing greater effectiveness than cisplatin. This study reveals the diverse mechanisms of action of Ru and Ir complexes based on different ligands. To the best of our knowledge, this study represents the first investigation of a novel RAED-type complex (Ru1) and unexpected bimetallic complexes (Ru2 and Ir1).