Synthesis and characterization of novel chelation-free Zn(II)-azole complexes: Evaluation of antibacterial, antioxidant and DNA binding activity

589-597Here, we synthesized novel chelation-free Zn(II)-complexes (1-3) [ZnCl2L2] of monodentate ligands with L = 2-isopropylimidazole (L1), 2-methylbenzimidazole (L2), and 2-methylbenzoxazole (L3) and evaluated their antibacterial, antioxidant and DNA binding activities. The chelation-free properties of these coordination complexes were confirmed by UV-visible spectroscopy, 1H NMR spectroscopy, single X-ray crystallography and elemental analysis. Complexes 1-3 exhibited substantial antibacterial activity against all antibiotic susceptible bacteria within a concentration range of 100-200 µg/ml while free ligands L1 and L2 exhibited weak antibacterial activity considerably concentration above 200 µg/ml. Also, both complexes 2 and 3 were twice more active against methicillin-resistant Staphylococcus aureus (MRSA) than complex 1. Furthermore, we found that complexes 1-3 showed DNA binding activity with E. coli plasmid DNA and calf thymus DNA, which may be a plausible mechanism for their antibacterial activity. We also investigated the antioxidant activity of complexes 1-3 and found that complex 2 exhibited potential antioxidant activity compared to complexes 1 and 3. All these results suggest that the chelation-free Zn(II)-complexes can be the future candidates for more advance biological studies

Nanocarrier cancer therapeutics with functional stimuli-responsive mechanisms

Presently, nanocarriers (NCs) have gained huge attention for their structural ability, good biocompatibility, and biodegradability. The development of effective NCs with stimuli-responsive properties has acquired a huge interest among scientists. When developing drug delivery NCs, the fundamental goal is to tackle the delivery-related problems associated with standard chemotherapy and to carry medicines to the intended sites of action while avoiding undesirable side effects. These nanocarriers were able of delivering drugs to tumors through regulating their pH, temperature, enzyme responsiveness. With the use of nanocarriers, chemotherapeutic drugs could be supplied to tumors more accurately that can equally encapsulate and deliver them. Material carriers for chemotherapeutic medicines are discussed in this review keeping in viewpoint of the structural properties and targeting methods that make these carriers more therapeutically effective, in addition to metabolic pathways triggered by drug-loaded NCs. Largely, the development of NCs countering to endogenous and exogenous stimuli in tumor regions and understanding of mechanisms would encourage the progress for tumor therapy and precision diagnosis in future

Plasma-Generated Nitric Oxide Water Mediates Environmentally Transmitted Pathogenic Bacterial Inactivation via Intracellular Nitrosative Stress

Over time, the proportion of resistant bacteria will increase. This is a major concern. Therefore, effective and biocompatible therapeutic strategies against these bacteria are urgently needed. Non-thermal plasma has been exhaustively characterized for its antibacterial activity. This study aims to investigate the inactivation efficiency and mechanisms of plasma-generated nitric oxide water (PG-NOW) on pathogenic water, air, soil, and foodborne Gram-negative and Gram-positive bacteria. Using a colony-forming unit assay, we found that PG-NOW treatment effectively inhibited the growth of bacteria. Moreover, the intracellular nitric oxide (NO) accumulation was evaluated by 4-amino-5-methylamino-2′,7′-dichlorofluorescein diacetate (DAF-FM DA) staining. The reduction of viable cells unambiguously indicates the anti-microbial effect of PG-NOW. The soxR and soxS genes are associated with nitrosative stress, and oxyR regulation corresponds to oxidative stress in bacterial cells. To support the nitrosative effect mediated by PG-NOW, we have further assessed the soxRS and oxyR gene expressions after treatment. Accordingly, soxRS expression was enhanced, whereas the oxyR expression was decreased following PG-NOW treatment. The disruption of cell morphology was observed using scanning electron microscopy (SEM) analysis. In conclusion, our findings furnish evidence of an initiation point for the further progress and development of PG-NOW-based antibacterial treatments