Elnagar Mohamed M, Abou-El-Sherbini Khaled S, Samir Safia, Sharmoukh Walid, Abdel-Aziz Mohamed S, Shaker Yasser M
Institute of Electrochemistry, Ulm University, Albert-Einstein-Allee 47, 89081, Ulm, Germany.
Department of Inorganic Chemistry, National Research Centre, 33 El Bohouth St. (former Tahrir St.), 12622, Dokki, Giza, Egypt.
ChemMedChem. 2025 Feb 1;20(3):e202400680. doi: 10.1002/cmdc.202400680. Epub 2024 Nov 21.
Ruthenium complexes incorporating 2,2' : 6',2''-terpyridine ligands have emerged as promising candidates due to their versatile biological activities including DNA-binding, anti-inflammatory, antimicrobial, and anticancer properties. In this study, three new 4'-functionalized bis(terpyridine) Ru(II) complexes were synthesized. These complexes feature one ligand as 4-(2,2' : 6',2''-terpyridine-4'-yl) benzoic acid and the second ligand as either 4'-(2-thienyl)-2,2' : 6',2''-terpyridine, 4'-(3,4-dimethoxyphenyl)-2,2' : 6',2''-terpyridine, or 4'-(4-dimethylaminophenyl)-2,2' : 6',2''-terpyridine. Besides the chemical characterization by H and C NMR, mass spectrometry, and absorption and emission spectroscopy, the complexes were tested for their biological activity as anti-inflammatory, anticancer, and antimicrobial agents. Moreover, the toxicity of the Ru(II) complexes was assessed and benchmarked against diclofenac potassium and ibuprofen using a haemolysis assay. Biological evaluations demonstrate that these ruthenium complexes exhibit promising therapeutic potential with reduced haemolytic activity compared to standard drugs. They demonstrate substantial anti-inflammatory effects through inhibition of albumin denaturation along with moderate cytotoxicity against cancer cell lines and broad-spectrum antimicrobial activity. These findings highlight the multifaceted biomedical applications of 4'-functionalized bis(terpyridine) Ru(II) complexes, suggesting their potential for further development as effective and safe therapeutic agents.
由于具有包括DNA结合、抗炎、抗菌和抗癌特性在内的多种生物活性,含有2,2':6',2''-三联吡啶配体的钌配合物已成为有前景的候选物。在本研究中,合成了三种新型的4'-官能化双(三联吡啶)Ru(II)配合物。这些配合物的一个配体为4-(2,2':6',2''-三联吡啶-4'-基)苯甲酸,第二个配体为4'-(2-噻吩基)-2,2':6',2''-三联吡啶、4'-(3,4-二甲氧基苯基)-2,2':6',2''-三联吡啶或4'-(4-二甲基氨基苯基)-2,2':6',2''-三联吡啶。除了通过氢谱和碳谱、质谱以及吸收和发射光谱进行化学表征外,还测试了这些配合物作为抗炎、抗癌和抗菌剂的生物活性。此外,使用溶血试验评估了Ru(II)配合物的毒性,并与双氯芬酸钾和布洛芬进行了对比。生物学评估表明,与标准药物相比,这些钌配合物具有良好的治疗潜力且溶血活性降低。它们通过抑制白蛋白变性表现出显著的抗炎作用,同时对癌细胞系具有中等细胞毒性和广谱抗菌活性。这些发现突出了4'-官能化双(三联吡啶)Ru(II)配合物多方面的生物医学应用,表明它们作为有效且安全的治疗剂具有进一步开发的潜力。