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.
Development of multidrug resistance among pathogens has become a global problem for chemotherapy of bacterial infections. Extended-spectrum β-lactamase- (ESβL-) producing enteric bacteria and methicillin-resistant Staphylococcus aureus (MRSA) are the two major groups of problematic MDR bacteria that have evolved rapidly in the recent past. In this study, the aqueous extract of Murraya koenigii leaves was used for synthesis of silver nanoparticles. The synthesized MK-AgNPs were characterized using UV-vis spectroscopy, FTIR, XRD, SEM, and TEM, and their antibacterial potential was evaluated on multiple ESβL-producing enteric bacteria and MRSA. The nanoparticles were predominantly found to be spheroidal with particle size distribution in the range of 5–20 nm. There was 60.86% silver content in MK-AgNPs. Evaluation of antibacterial activity by the disc-diffusion assay revealed that MK-AgNPs effectively inhibited the growth of test pathogens with varying sized zones of inhibition. The MICs of MK-AgNPs against both MRSA and methicillin-sensitive S. aureus (MSSA) strains were 32 μg/ml, while for ESβL-producing E. coli, it ranged from 32 to 64 μg/ml. The control strain of E. coli (ECS) was relatively more sensitive with an MIC of 16 μg/ml. The MBCs were in accordance with the respective MICs. Analysis of growth kinetics revealed that the growth of all tested S. aureus strains was inhibited (∼90%) in presence of 32 μg/ml of MK-AgNPs. The sensitive strain of E. coli (ECS) showed least resistance to MK-AgNPs with >81% inhibition at 16 μg/ml. The present investigation revealed an encouraging result on in vitro efficacy of green synthesized MK-AgNPs and needed further in vivo assessment for its therapeutic efficacy against MDR bacteria.
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.
Cancer and the associated secondary bacterial infections are leading cause of mortality, due to the paucity of effective drugs. Here, we have synthesized silver nanoparticles (AgNPs) from organic resource and confirmed their anti-cancer and anti-microbial potentials. Microwave irradiation method was employed to synthesize AgNPs using
Pandanus odorifer
leaf extract. Anti-cancer potential of AgNPs was evaluated by scratch assay on the monolayer of rat basophilic leukemia (RBL) cells, indicating that the synthesized AgNPs inhibit the migration of RBL cells. The synthesized AgNPs showed MIC value of 4–16 μg/mL against both Gram +ve and Gram -ve bacterial strains, exhibiting the anti-microbial potential. Biofilm inhibition was recorded at sub-MIC values against Gram +ve and Gram -ve bacterial strains. Violacein and alginate productions were reduced by 89.6 and 75.6%, respectively at 4 and 8 μg/mL of AgNPs, suggesting anti-quorum sensing activity. Exopolysaccharide production was decreased by 61–79 and 84% for Gram -ve and Gram +ve pathogens respectively. Flagellar driven swarming mobility was also reduced significantly. Furthermore,
In vivo
study confirmed their tolerability in mice, indicating their clinical perspective. Collective, we claim that the synthesized AgNPs have anti-metastasis as well as anti-microbial activities. Hence, this can be further tested for therapeutic options to treat cancer and secondary bacterial infections.
The resistance and pathogenesis of bacteria could be related to their ability to sense and respond to population density, termed quorum sensing (QS). Inhibition of the QS system is considered as a novel strategy for the development of antipathogenic agents, especially for combating drug-resistant bacterial infections. In the present study, the anti-QS activity of Onion peel ethylacetate fraction (ONE) was tested against Chromobacterium violaceum CV12472 and Pseudomonas aeruginosa PAO1. ONE inhibit the QS-mediated virulence factors production such as violacein in C. violaceum and elastase, pyocyanin in P. aeruginosa. Further, the treatment with sub-MICs of ONE significantly inhibited the QS-mediated biofilm formation, EPS (Extracellular polymeric substances) production and swarming motility. Further, quercetin 4′-O-β-D glucopyranoside (QGP) was isolated from ONE and its anti-QS potential was confirmed after observing significant inhibition of QS-controlled virulence factors such as violacein, elastase, pyocyanin and biofilm formation in test pathogens. Molecular docking analysis predicted that QGP should be able to bind at the active sites of Vfr and LasR, and if so blocks the entry of active sites in Vfr and LasR.
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.
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