Department of Chemistry, Art & Science Faculty, Pamukkale University, 20160, Denizli, Turkey.
Department of Biology, Art & Science Faculty, Pamukkale University, 20160, Denizli, Turkey.
Biometals. 2021 Jun;34(3):701-713. doi: 10.1007/s10534-021-00307-y. Epub 2021 Apr 26.
This study represents synthesis, characterization, screening of antibiofilm efficacy, and cytotoxicity of iridium bis-terpyridine complexes. The complexes were characterized by NMR, MS, FTIR, UV/Visible, and fluorescence spectroscopies. The efficacy of biofilm inhibition and eradication of iridium complexes was evaluated using a crystal violet assay test and verified by fluorescence microscopy. Cytotoxicity and apoptosis analysis of iridium complexes were determined in this study. The results of our study revealed that three iridium complexes had the potential to inhibit biofilm formation and moderate the ability to destroy pre-formed biofilm of S. aureus ATCC 29,213. 250 µM concentration of synthesized complexes showed the highest antibiofilm activity (75% for Ir1, 90% for Ir2, and 71% for Ir3). The significant inhibition obtained at 6.25 µM concentration of Ir2 and Ir3 revealed the potential of our samples. Also, Ir1 and Ir2 complexes had a good capacity to destroy pre-formed biofilm. The results clearly showed that iridium complexes have cytotoxic activity towards colon cancer (Caco-2) and liver cancer (HepG2) cell lines without affecting non-cancerous cells (HEK293) at applied doses. Moreover, tested compounds induced apoptosis in these cancer cells. All of these results showed that iridium complexes had possessed the ability to inhibit or destroy pre-formed biofilm and could be developed as an effective agent against bacterial biofilms. Moreover, these pure substances may have valuable anti-cancer activity and it should be confirmed with further studies for therapeutic effects.
本研究代表了铱双三联吡啶配合物的合成、表征、抗生物膜活性筛选和细胞毒性研究。配合物通过 NMR、MS、FTIR、UV/Vis 和荧光光谱进行了表征。采用结晶紫测定法评估了配合物抑制生物膜形成和消除生物膜的效果，并通过荧光显微镜进行了验证。本研究还测定了配合物的细胞毒性和细胞凋亡。研究结果表明，三种铱配合物具有抑制生物膜形成的潜力，并具有中等程度的破坏金黄色葡萄球菌 ATCC 29,213 形成的生物膜的能力。250 µM 浓度的合成配合物表现出最高的抗生物膜活性（Ir1 为 75%，Ir2 为 90%，Ir3 为 71%）。Ir2 和 Ir3 在 6.25 µM 浓度下的显著抑制作用表明了我们样品的潜力。此外，Ir1 和 Ir2 配合物具有破坏已形成生物膜的良好能力。结果清楚地表明，铱配合物对结肠癌（Caco-2）和肝癌（HepG2）细胞系具有细胞毒性活性，而在应用剂量下对非癌细胞（HEK293）没有影响。此外，测试化合物在这些癌细胞中诱导了细胞凋亡。所有这些结果表明，铱配合物具有抑制或破坏已形成生物膜的能力，可开发为抗细菌生物膜的有效药物。此外，这些纯物质可能具有有价值的抗癌活性，应该通过进一步的研究来确认其治疗效果。
