Design and evaluation of novel polymyxin fluorescent probes

Research output: Contribution to journalArticleResearchpeer-review

1 Citation (Scopus)

Abstract

Polymyxins (polymyxin B and colistin) are cyclic lipopeptide antibiotics that serve as a last-line defence against Gram-negative “superbugs”. In the present study, two novel fluorescent polymyxin probes were designed through regio-selective modifications of the polymyxin B core structure at the N-terminus and the hydrophobic motif at positions 6 and 7. The resulting probes, FADDI-285 and FADDI-286 demonstrated comparable antibacterial activity (MICs 2-8 mg/L) to polymyxin B and colistin (MICs 0.5-8 mg/L) against a panel of gram-negative clinical isolates of Acinetobacter baumannii, Klebsiella pneumoniae and Pseudomonas aeruginosa. These probes should prove to be of considerable utility for imaging cellular uptake and mechanistic investigations of these important last-line antibiotics.

Original languageEnglish
Article number2598
Number of pages8
JournalSensors
Volume17
Issue number11
DOIs
Publication statusPublished - 11 Nov 2017

Keywords

  • Dansyl
  • Fluorescent
  • Gram-negative
  • Polymyxins
  • Probe

Cite this

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title = "Design and evaluation of novel polymyxin fluorescent probes",
abstract = "Polymyxins (polymyxin B and colistin) are cyclic lipopeptide antibiotics that serve as a last-line defence against Gram-negative “superbugs”. In the present study, two novel fluorescent polymyxin probes were designed through regio-selective modifications of the polymyxin B core structure at the N-terminus and the hydrophobic motif at positions 6 and 7. The resulting probes, FADDI-285 and FADDI-286 demonstrated comparable antibacterial activity (MICs 2-8 mg/L) to polymyxin B and colistin (MICs 0.5-8 mg/L) against a panel of gram-negative clinical isolates of Acinetobacter baumannii, Klebsiella pneumoniae and Pseudomonas aeruginosa. These probes should prove to be of considerable utility for imaging cellular uptake and mechanistic investigations of these important last-line antibiotics.",
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Design and evaluation of novel polymyxin fluorescent probes. / Yun, Bo; Roberts, Kade D.; Thompson, Philip E.; Nation, Roger L.; Velkov, Tony; Li, Jian.

In: Sensors, Vol. 17, No. 11, 2598, 11.11.2017.

Research output: Contribution to journalArticleResearchpeer-review

TY - JOUR

T1 - Design and evaluation of novel polymyxin fluorescent probes

AU - Yun, Bo

AU - Roberts, Kade D.

AU - Thompson, Philip E.

AU - Nation, Roger L.

AU - Velkov, Tony

AU - Li, Jian

PY - 2017/11/11

Y1 - 2017/11/11

N2 - Polymyxins (polymyxin B and colistin) are cyclic lipopeptide antibiotics that serve as a last-line defence against Gram-negative “superbugs”. In the present study, two novel fluorescent polymyxin probes were designed through regio-selective modifications of the polymyxin B core structure at the N-terminus and the hydrophobic motif at positions 6 and 7. The resulting probes, FADDI-285 and FADDI-286 demonstrated comparable antibacterial activity (MICs 2-8 mg/L) to polymyxin B and colistin (MICs 0.5-8 mg/L) against a panel of gram-negative clinical isolates of Acinetobacter baumannii, Klebsiella pneumoniae and Pseudomonas aeruginosa. These probes should prove to be of considerable utility for imaging cellular uptake and mechanistic investigations of these important last-line antibiotics.

AB - Polymyxins (polymyxin B and colistin) are cyclic lipopeptide antibiotics that serve as a last-line defence against Gram-negative “superbugs”. In the present study, two novel fluorescent polymyxin probes were designed through regio-selective modifications of the polymyxin B core structure at the N-terminus and the hydrophobic motif at positions 6 and 7. The resulting probes, FADDI-285 and FADDI-286 demonstrated comparable antibacterial activity (MICs 2-8 mg/L) to polymyxin B and colistin (MICs 0.5-8 mg/L) against a panel of gram-negative clinical isolates of Acinetobacter baumannii, Klebsiella pneumoniae and Pseudomonas aeruginosa. These probes should prove to be of considerable utility for imaging cellular uptake and mechanistic investigations of these important last-line antibiotics.

KW - Dansyl

KW - Fluorescent

KW - Gram-negative

KW - Polymyxins

KW - Probe

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