Department of Chemistry, National Institute of Technology, Hamirpur (H.P.)-177005, India.
Department of Biotechnology, Deenbandhu Chhotu Ram University of Science and Technology Murthal (Sonepat) Haryana-131039, India.
Anticancer Agents Med Chem. 2018;18(5):739-746. doi: 10.2174/1871520618666171219122431.
After the discovery of cisplatin, first non platinum anticancer drugs having excellent efficacy were budotitane and TiCl2(cp)2 but action mechanism is not clear. Therefore, we hereby reporting synthesis and biological activities novel titanium complexes to explore their mode of action.
Synthesis, spectral characterization, antibacterial and anticancer activity of some titanium complexes. Antibacterial studies on various bacterial strains and anticancer studies on HeLa, C6, CHO cancerous cell lines have been performed. Further, the cell death mechanistic study was done on CHO cell lines.
Titanium complexes with and without labile groups have been synthesized by reacting of TiCl4 with nitrogen containing ligands viz. 1,2-diaminocyclohexane, 1,10-Phenanthroline, adamantylamine, 2,2'-bipyridine, 4,4'-dimethyl-2,2'-bipyridine in predetermined molar ratios. Antibacterial and anticancer studies were performed by agar well diffusion method and MTT assay respectively. Cell cycle analysis is done by using flow cytometry.
Complex 2 i.e TiCl2(Phen)2 showed better activity than other complexes as an antibacterial as well as anticancer agent. Phase contrast imaging indicates that observed morphological changes of cells was dose dependent. Cell death mechanistic study have shown the increase in sub G0 phase population as well as formation of blebbing and fragmentation of chromatin material which is an indicative measure of apoptosis.
Complex 2 proved to be more effective bactericide and cytotoxic agent. Cell cycle analysis showed cell arrest in G0 phase. Apoptosis percentage was found to increase in a dose dependent manner. So, prepared titanium complexes can be put to use as an important chemotherapeutic agents.
顺铂发现后，具有优异疗效的首批非铂类抗癌药物是布托他滨和 TiCl2(cp)2，但作用机制尚不清楚。因此，我们在此报告合成和生物活性新型钛配合物，以探索其作用模式。
合成、光谱表征、一些钛配合物的抗菌和抗癌活性。对各种细菌菌株进行了抗菌研究，对 HeLa、C6、CHO 癌细胞系进行了抗癌研究，并对 CHO 细胞系进行了细胞死亡机制研究。
用 TiCl4 与含氮配体 1,2-二氨基环己烷、1,10-菲咯啉、金刚烷胺、2,2'-联吡啶、4,4'-二甲基-2,2'-联吡啶反应，合成具有和不具有易位基团的钛配合物，以预定的摩尔比。采用琼脂孔扩散法和 MTT 法进行抗菌和抗癌研究。用流式细胞术进行细胞周期分析。
配合物 2 即 TiCl2(Phen)2 作为一种抗菌和抗癌剂的活性优于其他配合物。相差显微镜观察表明，观察到的细胞形态变化具有剂量依赖性。细胞死亡机制研究表明，亚 G0 期细胞群增加以及染色质物质的起泡和碎片化，这是细胞凋亡的一个指示性指标。
配合物 2 被证明是更有效的杀菌剂和细胞毒性剂。细胞周期分析显示细胞在 G0 期停滞。凋亡百分比呈剂量依赖性增加。因此，所制备的钛配合物可作为重要的化疗药物使用。
