Abstract
Copper-based compounds are promising entities for target-specific next-generation anticancer and NSAIDS therapeutics. In lieu of this, benzimidazole scaffold plays an important role, because of their wide variety of potential functionalizations and coordination modes. Herein, we report three copper complexes 1–3 with benzimidazole-derived scaffolds, a biocompatible molecule, and secondary ligands viz, 1–10-phenanthroline and 2,2′-bipyridyl. All the copper complexes have been designed, synthesized and adequately characterized using various spectroscopic techniques. In-vitro, human serum albumin (HSA) binding was also carried out using fluorescence technique and in-silico molecular modeling studies, which exhibited significant binding affinities of the complexes with HSA. Furthermore, copper complexes 1–3 were tested for biological studies, i.e., anticancer as well as NSAIDS. In vitro cytotoxicity results were carried out on cultured MCF-7 cell lines. To get the insight over the mechanism of action, GSH depletion and change in lipid peroxidation were tested and thus confirmed the role of ROS generation, responsible for the cytotoxicity of the complexes 1–3. Moreover, the copper complexes 1–3 were tested for potential to act as NSAIDS on albino rats and mice in animal studies in-vivo. Additionally, we also predicted the mechanism of action of the copper complexes 1–3 using molecular modeling studies with COX-2 inhibitor.
Highlights
The essential trace element-copper has a key role in numerous physiological cellular processes
We have synthesized an organic motif, Schiff base of 2-aminobenzimidazole with o-vanillin[34] and three copper complexes using copper (II), Schiff base as a primary ligand (1), and with 1,10-phenanthroline and 2,2′-bipyridyl as co-ligand (2 and 3). We have studied their potential to act as an anti-cancer chemotherapeutic as well as non-steroidal inflammatory drugs (NSAIDs) candidates using In vitro and in vivo studies
The morphological images of the MCF-7 cancer cells, upon treatment with complexes 1–3 displayed nuclear blebbing and fragmentation of the nuclei, which is typical of late, apoptosis
Summary
We have monitored the quenching in the fluorescence properties of HSA in the presence of metal complexes (Figs 2 and S6). For the three metal complexes were of the order of 1013 M−1 s−1 which were at least 1000 times more than the maximum collision constant of 1010 M−1 s−1 43 These results clearly indicate that the quenching of HSA fluorescence in the presence of the studied metal complexes was due to the formation of a complex rather than merely a collision event.
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