Design, synthesis and in vitro bioactivity of mixed ligand Ru(II) complexes bearing the fluoroquinolone antibacterial agents
| Autor: | Sarmita Jana, Soumya Ranjan Dash, Debjani Chakraborty, Ramadevi Pulipaka, Priyanka Khanvilkar, Ranjitsinh V. Devkar |
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| Rok vydání: | 2019 |
| Předmět: |
Denticity
biology Chemistry Stereochemistry Phenanthroline Metals and Alloys 010403 inorganic & nuclear chemistry 01 natural sciences In vitro 0104 chemical sciences Catalysis Inorganic Chemistry Metal chemistry.chemical_compound visual_art Materials Chemistry visual_art.visual_art_medium biology.protein Moiety Bovine serum albumin Organometallic chemistry |
| Zdroj: | Transition Metal Chemistry. 44:721-735 |
| ISSN: | 1572-901X 0340-4285 |
| DOI: | 10.1007/s11243-019-00341-3 |
| Popis: | Mixed ligand Ru(II) phenanthroline complexes of the type [Ru(1,10-phen)2Flq]ClO4 (RPFlq-1-3) and “piano-stool”-type Ru(II) arene complexes [Ru(η6-p-cymene)Cl(Flq)] (RAFlq-1-3), where Flq = fluoroquinolone, have been synthesized, characterized and studied for their anticancer potential. DFT calculations were in line with the proposed structures, wherein the fluoroquinolones are coordinated to the metal through the ring carbonyl and one of the carboxylic oxygen atoms in a bidentate fashion. Binding efficacies of the synthesized complexes with bovine serum albumin (BSA) and CT-DNA were studied spectroscopically, and it has been established that the arene complexes, though have moderate binding propensities to CT-DNA (Kb = 0.8–1.7 × 103 M−1), have 102–103-fold better binding efficacies toward BSA (Ka = 3.2 × 105–2.1 × 106 M−1) due to the presence of the hydrophobic arene moiety. These results further prompted a study in their in vitro cytotoxicity assay on A-549 non-small cell lung cancer and MCF7 breast cancer cell lines. Furthermore, gene expression studies on BAX and BCL-2 genes and FACS analysis confirmed apoptosis as the mode of cell death. |
| Databáze: | OpenAIRE |
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