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The outer membrane permeability-increasing action of deacylpolymyxins

P Viljanen1, H Matsunaga, Y Kimura

  • 1Department of Fisheries, Faculty of Agriculture, Miyazaki University, Japan.

Insights

Deacylpolymyxins, like deacylpolymyxin B (DAPB), are potent outer membrane permeabilizers, enhancing antibiotic effectiveness against bacteria like Escherichia coli and Salmonella typhimurium.

Area of Science:

  • Microbiology
  • Drug Discovery
  • Antimicrobial Resistance

Background:

  • Polymyxins are crucial antibiotics targeting Gram-negative bacteria.
  • Outer membrane permeability is a key factor in antibiotic efficacy.
  • Polymyxin B nonapeptide (PMBN) is a known potent permeabilizer.

Purpose of the Study:

  • To compare the outer membrane permeability-increasing activity of deacylpolymyxins with PMBN.
  • To evaluate the effectiveness of deacylpolymyxin B (DAPB) and deacylcolistin (DAC) as permeabilizers.

Main Methods:

  • Deacylpolymyxin B (DAPB) was prepared by treating polymyxin B with polymyxin acylase.
  • Bacterial sensitization assays were performed using probe antibiotics (rifampin, fusidic acid, erythromycin, clindamycin, novobiocin).
  • Comparative analysis of DAPB and PMBN as outer membrane permeabilizers.

Main Results:

  • DAPB demonstrated slightly higher permeabilizing activity than PMBN.
  • Low concentrations of DAPB (1 microgram/ml) significantly sensitized Escherichia coli (30-100 fold) and Salmonella typhimurium (10-100 fold) to antibiotics.
  • Higher DAPB concentrations (3 micrograms/ml) resulted in further sensitization.
  • Deacylcolistin (DAC) was also identified as an effective permeabilizer.

Conclusions:

  • Deacylpolymyxins, particularly DAPB, are highly effective agents for increasing outer membrane permeability.
  • DAPB shows promise as a sensitizer to enhance the efficacy of existing antibiotics against Gram-negative bacteria.
  • Further research into deacylpolymyxins could lead to novel strategies for combating antimicrobial resistance.

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