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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.
Afiliación
  • Yun B; Drug Delivery, Disposition and Dynamics, Monash University, Parkville, Victoria 3052, Australia. Bo.Yun@petermac.org.
  • Roberts KD; Drug Delivery, Disposition and Dynamics, Monash University, Parkville, Victoria 3052, Australia. Kade.Roberts@monash.edu.
  • Thompson PE; Medicinal Chemistry, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria 3052, Australia. Philip.Thompson@monash.edu.
  • Nation RL; Drug Delivery, Disposition and Dynamics, Monash University, Parkville, Victoria 3052, Australia. roger.nation@monash.edu.
  • Velkov T; Drug Delivery, Disposition and Dynamics, Monash University, Parkville, Victoria 3052, Australia. tony.velkov@unimelb.edu.au.
  • Li J; Monash Biomedicine Discovery Institute, Department of Microbiology, Monash University, Clayton, Victoria 3800, Australia. jian.li@monash.edu.
Sensors (Basel) ; 17(11)2017 Nov 11.
Article en En | MEDLINE | ID: mdl-29137129
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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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Idioma: En Revista: Sensors (Basel) Año: 2017 Tipo del documento: Article País de afiliación: Australia Pais de publicación: Suiza
Texto completo
Añadir a Mi BVS
Imprimir
XML
PubMed Links
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Idioma: En Revista: Sensors (Basel) Año: 2017 Tipo del documento: Article País de afiliación: Australia Pais de publicación: Suiza