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 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.
Keywords: Antibacterial agents; Biofilm; Drug-resistant bacteria; Liposome; Pillar[5]arenes; Pyridinium.
© 2022. The Author(s), under exclusive licence to Springer Nature Switzerland AG.