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.

中文翻译：

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含氟喹诺酮类抗菌剂的混合配体 Ru(II) 配合物的设计、合成和体外生物活性

[Ru(1,10-phen)2Flq]ClO4 (RPFlq-1-3) 型混合配体 Ru(II) 菲咯啉配合物和“钢琴凳”型 Ru(II) 芳烃配合物 [Ru(η6-p -cymene)Cl(Flq)] (RAFlq-1-3)，其中 Flq = 氟喹诺酮，已被合成、表征和研究其抗癌潜力。DFT 计算与所提出的结构一致，其中氟喹诺酮类通过环羰基和一个羧基氧原子以二齿方式与金属配位。合成的复合物与牛血清白蛋白 (BSA) 和 CT-DNA 的结合功效进行了光谱研究，并且已经确定芳烃复合物虽然对 CT-DNA 具有中等结合倾向（Kb = 0.8–1.7 × 103 M−） 1)，对 BSA 的结合效率提高 102-103 倍（Ka = 3.2 × 105-2。1 × 106 M-1) 由于疏水芳烃部分的存在。这些结果进一步促进了对 A-549 非小细胞肺癌和 MCF7 乳腺癌细胞系的体外细胞毒性试验的研究。此外，BAX 和 BCL-2 基因的基因表达研究和 FACS 分析证实细胞凋亡是细胞死亡的方式。