Design, synthesis and in vitro bioactivity of mixed ligand Ru(II) complexes bearing the fluoroquinolone antibacterial agents
- 21 Downloads
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.
The authors gratefully acknowledge the University Grants Commission RFSMS-BSR fellowship [UGC No. F.4-1/2006 (BSR)/5-68/2007 (BSR)], New Delhi, for financial assistance. The authors are thankful to the Head, Department of Chemistry and Department of Zoology, Faculty of Science, The Maharaja Sayajirao University of Baroda, for providing us with the necessary laboratory facilities and required instrumentation facilities to carry out the research work. The authors thank DBT-MSUB-ILSPARE project, Dr. Vikram Sarabhai Science Block, M. S. University of Baroda, for providing the ESI MS analysis of the complexes and FACS analysis.
Compliance with ethical standards
Conflict of interest
The authors declare that they have no conflict of interest.
- 1.Allardyce CS, Dyson PJ (2001) Platinum Metals Rev. 45:62Google Scholar
- 5.Zanzi I, Srivastava SC, Meinken GE, Robeson W, Mausner LF, Fairchild RG, Margouleff D (1989) Nucl Med Biol 16:397Google Scholar
- 10.Y.Yaw Kai, Chem. Comm. 2005, 38, 4764Google Scholar
- 11.Soni K (2012) Indo Glob J Pharm Sci 2:43Google Scholar
- 13.Kwok Y, Sun D, Clement JJ, Hurley LH (1999) Anti-Cancer Drug Des 14:443Google Scholar
- 19.Bennett MA, Smith AK (1974) J Chem Soc Dalton Trans (2):233Google Scholar
- 20.Bennett MA, Huang TN, Matheson TW, Smith AK (1983) Inorg Synth 21:74Google Scholar
- 37.Adebayo AA, Ajibade PA (2016) J Chem 2016:15, Article ID 3672062Google Scholar