ABSTRACT
An increasing number of infections caused by multidrug-resistant (MDR) Staphylococcus aureus （S. aureus） and Escherichia coli （E. coli） have severely affected human society. Thus, it is essential to develop an alternative type of antibacterial agents that has a different bacterial resistance mechanism from that of traditional antibiotics. After the synthesis and structural characterization of a cationic pillar[5]arene with pyridinium groups (PP5), the antibacterial and antibiofilm activities as well as its microbial resistance were systematically investigated. In-depth evaluation of biological studies revealed that PP5 was an active antibacterial agent, with surprising antibiofilm formation ability against E. coli and S. aureus. From the results of differential scanning calorimetry and transmission electron microscopy, it was concluded that the microbicidal activity of PP5 was due to the physical disruption of the pathogens membrane and the subsequent leakage of cytoplasmic components, which could greatly reduce the rapid generation of resistance. It was presented that the easily available PP5 has high activity to inhibit Gram-positive and Gram-negative bacteria and/or their biofilms with low cytotoxicity. This pillar[5]arene derivative can be used as a good candidate for controlling drug-resistant pathogenic bacterial infections and treating MDR bacteria.(AU)
Subject(s)
Humans , Staphylococcus aureus , Escherichia coli , Anti-Bacterial Agents , Drug Resistance, Bacterial , Calorimetry , Microscopy, Electron , Biofilms , Microbiology , Bacterial InfectionsABSTRACT
An increasing number of infections caused by multidrug-resistant (MDR) Staphylococcus aureus ï¼S. aureusï¼ and Escherichia coli ï¼E. coliï¼ have severely affected human society. Thus, it is essential to develop an alternative type of antibacterial agents that has a different bacterial resistance mechanism from that of traditional antibiotics. After the synthesis and structural characterization of a cationic pillar[5]arene with pyridinium groups (PP5), the antibacterial and antibiofilm activities as well as its microbial resistance were systematically investigated. In-depth evaluation of biological studies revealed that PP5 was an active antibacterial agent, with surprising antibiofilm formation ability against E. coli and S. aureus. From the results of differential scanning calorimetry and transmission electron microscopy, it was concluded that the microbicidal activity of PP5 was due to the physical disruption of the pathogen's membrane and the subsequent leakage of cytoplasmic components, which could greatly reduce the rapid generation of resistance. It was presented that the easily available PP5 has high activity to inhibit Gram-positive and Gram-negative bacteria and/or their biofilms with low cytotoxicity. This pillar[5]arene derivative can be used as a good candidate for controlling drug-resistant pathogenic bacterial infections and treating MDR bacteria.
Subject(s)
Anti-Bacterial Agents , Staphylococcal Infections , Humans , Anti-Bacterial Agents/pharmacology , Anti-Bacterial Agents/chemistry , Staphylococcus aureus , Escherichia coli , Drug Resistance, Bacterial , Gram-Negative Bacteria , Gram-Positive Bacteria , Biofilms , Microbial Sensitivity TestsABSTRACT
In this study, we prepared chitosan (CS)-coated iron oxide (Fe3O4) nanocomposites (NCs) by employing the aqueous leaf extract of Brassica oleracea L. and evaluated its antimicrobial potential. The characterization of hybrid CS-Fe3O4 NCs was performed using Fourier-transform infrared spectroscopy (FTIR) analysis to evaluate the chemical bonding of chitosan to nanoparticles (NPs). X-ray photoelectron spectroscopy (XPS) studies revealed the presence of oxidation state elements Fe 2p, O 1s, N 1s, and C 1s, and the zeta potential analysis was found to have well-colloidal stability (+ 76.9 mV) of NCs. Transmission electron microscopy (TEM) analysis determined that CS-Fe3O4 NCs were spherical with an average particle size of 27 nm. The X-ray diffractometer (XRD) spectrum ascertained the crystallinity of the hybrid NCs and the vibrating sample magnetometer (VSM) inferred the ferromagnetic behavior of the synthesized NCs. Furthermore, the significant antibacterial efficacy of NPs was demonstrated against foodborne bacterial pathogens, such as Staphylococcus aureus (S. aureus) and Escherichia coli (E. coli), and the highest zone of inhibition was observed to be 11.5 mm and 13.5 mm in CS-Fe3O4 NCs, respectively. In comparison with Fe3O4 NPs, synergistic impacts of CS-Fe3O4 NCs displayed great antibacterial potential as exhibited by a clearly enlarged zone. Thus, CS-Fe3O4 NCs could be used as efficacious antimicrobial agents in food packaging and food preservation fields.
ABSTRACT
An omnipresent pathogenic bacterium, Pseudomonas aeruginosa (P. aeruginosa PAO1), is easy to contaminate environmental water or foods, causing daily food spoilage and infections. The biofilm-forming ability and bacterial resistance of P. aeruginosa PAO1 make it difficult to be eradicated by traditional bacteriostatic agents. In this work, we designed and synthesized a pyridinium-based pillar[5]arene (PP5), while trimethylammonium-based pillar[5]arene (TP5) was used as a control compound. After clear characterization, the antibacterial and antibiofilm activities as well as the microbial resistance of TP5 and PP5 against P. aeruginosa PAO1 were extensively examined. It was revealed that PP5 exhibited good inhibition activity with the minimum inhibitory concentration (MIC) of 0.051 mmol/L, while no significant antibacterial and biofilm formation activity for TP5 against P. aeruginosa PAO1 was observed. More importantly, PP5 had negligible antimicrobial resistance even after 18th passages. A transmission electron microscope (TEM) showed that PP5 could physically disrupt the cell membranes, causing the leakage of internal constituents, which is possibly ascribed to the synergistic penetrability and π-π interactions of strain, thus greatly reduced the development of bacterial resistance. Overall, the presented studies indicated that pyridinium moieties could facilitate the cationic pillar[5]arene to generate surprising antibacterial and antibiofilm formation ability against P. aeruginosa PAO1.
