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A study on the antibacterial activity and antimicrobial resistance of pyridinium cationic pillar[5]arene against Staphylococcus aureus and Escherichia coli

Abstract

An increasing number of infections caused by multidrug-resistant (MDR) Staphylococcus aureusS. aureus) and Escherichia coliE. 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.

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Abbreviations

CL:

Cardiolipin

CFU:

Colony-forming units

CLSM:

Confocal laser scanning microscope

CV:

Crystal violet

DSC:

Differential scanning calorimetry

DMSO:

Dimethyl sulfoxide

E. coli:

Escherichia coli

LUV:

Large unilamellar liposomes

LB:

Luria Broth

MRSA:

Methicillin-resistant Staphylococcus aureus

MBC:

Minimum bactericidal concentration

MIC:

Minimum inhibitory concentration

PM:

Polymyxin B

MDR:

Multidrug-resistant

MDR-SA:

Multidrug-resistant Staphylococcus aureus

POPG:

1-palmitoyl-2-oleoyl-phosphatidylglycerol

PDI:

Polydispersity index

PI:

Propidium iodide

P. aeruginosa:

Pseudomonas aeruginosa PAO1

PP5:

Pyridine-based pillar[5]arene

SD:

Standard deviations

S. aureus:

Staphylococcus aureus

SI:

Supporting information

Tm:

Temperature

TEM:

Transmission electron microscopy

TP5:

Trimethylamine based pillar[5]arene

TSB:

Tryptic soy broth

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Funding

This work was supported by the Natural Science Foundation of Zhejiang Province of China (LY20B040001), the Project of Public Welfare Technology of Zhejiang Province of China (LGN19C200008), and the Science & Technology Innovation Program of Zhejiang Province (2018R52051).

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Authors and Affiliations

Authors

Contributions

Hua Yang and Dengqi Zhao conducted the lab work, data analysis, and drafted the manuscript. Lijun Yang contributed partly to the lab work. Shuping Wang conducted the MTT. Jianying Huang, Zibin Zhang, and Shijun Li conceived of the study, performed data review, and contributed to the manuscript writing. All authors have read and approved the final manuscript.

Corresponding authors

Correspondence to Jianying Huang or Zibin Zhang.

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The authors declare no competing interests.

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Yang, H., Zhao, D., Wang, S. et al. A study on the antibacterial activity and antimicrobial resistance of pyridinium cationic pillar[5]arene against Staphylococcus aureus and Escherichia coli. Int Microbiol (2022). https://doi.org/10.1007/s10123-022-00269-2

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  • DOI: https://doi.org/10.1007/s10123-022-00269-2

Keywords

  • Pillar[5]arenes
  • Pyridinium
  • Biofilm
  • Antibacterial agents
  • Drug-resistant bacteria
  • Liposome