Copper-based compounds are promising entities for target-specific next-generation anticancer and NSAIDS therapeutics.In lieuof this, benzimidazole scaffold plays an important role, because of their wide variety of potential functionalizations and coordination modes. Herein, we report three copper complexes1–3with 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 andin-silicomolecular modeling studies, which exhibited significant binding affinities of the complexes with HSA. Furthermore, copper complexes1–3were tested for biological studies, i.e., anticancer as well as NSAIDS.In vitrocytotoxicity 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 complexes1–3. Moreover, the copper complexes1–3were tested for potential to act as NSAIDS on albino rats and mice in animal studiesin-vivo. Additionally, we also predicted the mechanism of action of the copper complexes1–3using molecular modeling studies with COX-2 inhibitor.

Bacterial spoilage of food products is regulated by density dependent communication system called quorum sensing (QS). QS control biofilm formation in numerous food pathogens and Biofilms formed on food surfaces act as carriers of bacterial contamination leading to spoilage of food and health hazards. Agents inhibiting or interfering with bacterial QS and biofilm are gaining importance as a novel class of next-generation food preservatives/packaging material. In the present study, Zinc nanostructures were synthesised using Nigella sativa seed extract (NS-ZnNPs). Synthesized nanostructures were characterized hexagonal wurtzite structure of size ~24 nm by UV-visible, XRD, FTIR and TEM. NS-ZnNPs demonstrated broad-spectrum QS inhibition in C. violaceum and P. aeruginosa biosensor strains. Synthesized nanostructures inhibited QS regulated functions of C. violaceum CVO26 (violacein) and elastase, protease, pyocyanin and alginate production in PAO1 significantly. NS-ZnNPs at sub-inhibitory concentrations inhibited the biofilm formation of four-food pathogens viz. C. violaceum 12472, PAO1, L. monocytogenes, E. coli. Moreover, NS-ZnNPs was found effective in inhibiting pre-formed mature biofilms of the four pathogens. Therefore, the broad-spectrum inhibition of QS and biofilm by biogenic Zinc oxide nanoparticles and it is envisaged that these nontoxic bioactive nanostructures can be used as food packaging material and/or as food preservative.

Current exanimation reports, green fabrication of silver doped TiO2 nanoparticles (Ag/TiO2) using aqueous extract of Acacia nilotica as bio-reductant and assess its potential as antimicrobial and anticancer agent. The obtained spherical Ag/TiO2 were characterized by various analytical techniques including FTIR, (XRD), (FE-SEM EDS), and (TEM). Synthesized Ag/TiO2 demonstrated broad spectrum antibacterial and anticandidal activity. The order of antimicrobial activity was found to be E. coli > C. albicans > MRSA > P. aeruginosa. In addition, cytotoxicity and oxidative stress of Ag/TiO2 nanoparticles in (MCF-7) cells was also investigated. Outcomes of MTT assay showed concentration dependent reduction in cell viability. Further, synthesized NPs reduced the level of glutathione, induced ROS generation and lipid peroxidation in the treated cells. Therefore, it is envisaged that these spherical nanoparticles may be exploited in drug delivery, pharmaceutical, and food industry.

A new chromone-appended Cu(II) drug entity (1) was designed and synthesized as a potential anticancer chemotherapeutic agent. The structural elucidation was carried out thoroughly by elemental analysis, FT-IR, EPR, ESI-MS and single crystal X-ray crystallography. Complex 1 resulted from the in situ methoxylation reaction of the 3-formylchromone ligand and its subsequent complexation with the copper nitrate salt in a 2 : 1 ratio, respectively. 1 crystallized in the monoclinic P2₁/c space group possessing the lattice parameters, a = 8.75 Å, b = 5.07 Å, c = 26.22 Å, α = γ = 90°, β = 96.3° per unit cell. Furthermore, in vitro interaction studies of 1 with ct-DNA and tRNA were carried out which suggested more avid binding propensity towards the RNA target via intercalative mode, which was reflected from its K_b, K and K_sv values. The gel electrophoretic mobility assay was carried out on the pBR322 plasmid DNA substrate, to ascertain the cleaving ability and the mechanistic pathway in the presence of additives, and the results revealed the efficient cleaving ability of 1via the oxidative pathway. In vitro cell growth inhibition via the MTT assay was carried out to evaluate the cytotoxicity of complex 1 and IC₅₀ values were found to be in the range of 5–10 μg mL⁻¹ in HepG2 and MCF-7 cancer cell lines, which were found to be much lower than the IC₅₀ values of previously reported similar Cu(II) complexes. Additionally, in the presence of 1, reactive oxygen species (ROS) and thiobarbituric acid reactive substance (TBARS) levels in the tested cancer cell lines increased significantly, coupled with reduced glutathione (GSH) levels. Thus, our results suggested that ROS plays an important role in cell apoptosis induced by the Cu(II) complex 1 and validates its potential to act as a robust anticancer drug entity.