A quinoline-based FtsZ inhibitor for the study of antimicrobial activity and synergistic effects with β-lactam antibiotics

Zhiyuan Fang; Li Ban; Yanan Li; Wenchang Yuan; Zhihua Liu; Ting Liu; Xiaomei Li; Kwok yin Wong; Yujing Lu; Ning Sun; Xingang Yao

doi:10.1016/j.jphs.2018.07.005

A quinoline-based FtsZ inhibitor for the study of antimicrobial activity and synergistic effects with β-lactam antibiotics

Zhiyuan Fang, Li Ban, Yanan Li, Wenchang Yuan, Zhihua Liu, Ting Liu, Xiaomei Li, Kwok yin Wong, Yujing Lu, Ning Sun, Xingang Yao

Research output: Journal article publication › Journal article › Academic research › peer-review

28 Citations (Scopus)

Abstract

The antibacterial activity and the synergistic effect with β-lactam antibiotics of a new 1-methylquinolinium iodide derivative were investigated. The experimental results indicate that the compound possesses a strong antibacterial activity against a panel of bacteria including methicillin-resistant Staphylococcus aureus, vancomycin-resistant Enterococcus and NDM-1 Escherichia coli with the MIC values from 0.75 μg/mL to 6 μg/mL. In addition, this compound combined with β-lactam antibiotics shows strong synergistic antimicrobial activities against antibiotic-resistant strains of S. aureus. The results of biochemical studies also reveal that this compound can effectively disrupt GTPase activity, polymerization of FtsZ, and cell division to cause cell death. The compound shows high potential for further development as a new generation of antibacterial agents to fight against the emergence of multidrug-resistant bacteria.

Original language	English
Pages (from-to)	283-289
Number of pages	7
Journal	Journal of Pharmacological Sciences
Volume	137
Issue number	3
DOIs	https://doi.org/10.1016/j.jphs.2018.07.005
Publication status	Published - Jul 2018

Keywords

Antibacterial activity
Bacterial resistance
Cell division
FtsZ inhibitor
Synergistic effect

ASJC Scopus subject areas

Molecular Medicine
Pharmacology

More information

10.1016/j.jphs.2018.07.005

http://hdl.handle.net/10397/80029

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title = "A quinoline-based FtsZ inhibitor for the study of antimicrobial activity and synergistic effects with β-lactam antibiotics",

abstract = "The antibacterial activity and the synergistic effect with β-lactam antibiotics of a new 1-methylquinolinium iodide derivative were investigated. The experimental results indicate that the compound possesses a strong antibacterial activity against a panel of bacteria including methicillin-resistant Staphylococcus aureus, vancomycin-resistant Enterococcus and NDM-1 Escherichia coli with the MIC values from 0.75 μg/mL to 6 μg/mL. In addition, this compound combined with β-lactam antibiotics shows strong synergistic antimicrobial activities against antibiotic-resistant strains of S. aureus. The results of biochemical studies also reveal that this compound can effectively disrupt GTPase activity, polymerization of FtsZ, and cell division to cause cell death. The compound shows high potential for further development as a new generation of antibacterial agents to fight against the emergence of multidrug-resistant bacteria.",

keywords = "Antibacterial activity, Bacterial resistance, Cell division, FtsZ inhibitor, Synergistic effect",

author = "Zhiyuan Fang and Li Ban and Yanan Li and Wenchang Yuan and Zhihua Liu and Ting Liu and Xiaomei Li and Wong, {Kwok yin} and Yujing Lu and Ning Sun and Xingang Yao",

year = "2018",

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doi = "10.1016/j.jphs.2018.07.005",

language = "English",

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AU - Fang, Zhiyuan

AU - Ban, Li

AU - Li, Yanan

AU - Yuan, Wenchang

AU - Liu, Zhihua

AU - Liu, Ting

AU - Li, Xiaomei

AU - Wong, Kwok yin

AU - Lu, Yujing

AU - Sun, Ning

AU - Yao, Xingang

PY - 2018/7

Y1 - 2018/7

N2 - The antibacterial activity and the synergistic effect with β-lactam antibiotics of a new 1-methylquinolinium iodide derivative were investigated. The experimental results indicate that the compound possesses a strong antibacterial activity against a panel of bacteria including methicillin-resistant Staphylococcus aureus, vancomycin-resistant Enterococcus and NDM-1 Escherichia coli with the MIC values from 0.75 μg/mL to 6 μg/mL. In addition, this compound combined with β-lactam antibiotics shows strong synergistic antimicrobial activities against antibiotic-resistant strains of S. aureus. The results of biochemical studies also reveal that this compound can effectively disrupt GTPase activity, polymerization of FtsZ, and cell division to cause cell death. The compound shows high potential for further development as a new generation of antibacterial agents to fight against the emergence of multidrug-resistant bacteria.

AB - The antibacterial activity and the synergistic effect with β-lactam antibiotics of a new 1-methylquinolinium iodide derivative were investigated. The experimental results indicate that the compound possesses a strong antibacterial activity against a panel of bacteria including methicillin-resistant Staphylococcus aureus, vancomycin-resistant Enterococcus and NDM-1 Escherichia coli with the MIC values from 0.75 μg/mL to 6 μg/mL. In addition, this compound combined with β-lactam antibiotics shows strong synergistic antimicrobial activities against antibiotic-resistant strains of S. aureus. The results of biochemical studies also reveal that this compound can effectively disrupt GTPase activity, polymerization of FtsZ, and cell division to cause cell death. The compound shows high potential for further development as a new generation of antibacterial agents to fight against the emergence of multidrug-resistant bacteria.

KW - Antibacterial activity

KW - Bacterial resistance

KW - Cell division

KW - FtsZ inhibitor

KW - Synergistic effect

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DO - 10.1016/j.jphs.2018.07.005

M3 - Journal article

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SN - 1347-8613

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A quinoline-based FtsZ inhibitor for the study of antimicrobial activity and synergistic effects with β-lactam antibiotics

Abstract

Keywords

ASJC Scopus subject areas

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