Development of an aptamer-ampicillin conjugate for treating biofilms

Biochem Biophys Res Commun. 2017 Feb 5;483(2):847-854. doi: 10.1016/j.bbrc.2017.01.016. Epub 2017 Jan 6.

Abstract

Biofilm formation involves the development of extracellular matrix and initially depends on adherence and tropism by flagellar movement. With the widespread development of antibiotic resistance and tolerance of biofilms, there is a growing need for novel anti-infective strategies. No currently approved medications specifically target biofilms. Aptamers are single-stranded nucleic acid molecules that may bind to their targets with high affinity and affect the target functions. We developed a bifunctional conjugate by linking an aptamer targeting bacterial flagella with ampicillin. We investigated its influence on biofilm prevention and dissolution by ultraviolet-visible spectrophotometry, inverted microscopy, and atomic force microscopy. This conjugate had distinctive antibacterial activity. Notably, the conjugate was more active than either component, and thus had a synergistic effect against biofilms.

Keywords: Antibiofilm; Conjugate; Flagella; S. choleraesuis.

MeSH terms

  • Ampicillin / administration & dosage*
  • Ampicillin / chemical synthesis
  • Anti-Bacterial Agents / administration & dosage*
  • Anti-Bacterial Agents / chemical synthesis
  • Aptamers, Nucleotide / administration & dosage*
  • Aptamers, Nucleotide / chemical synthesis
  • Aptamers, Nucleotide / genetics
  • Bacillus thuringiensis / drug effects
  • Bacillus thuringiensis / physiology
  • Bacteria / drug effects*
  • Bacteria / pathogenicity
  • Bacterial Load
  • Base Sequence
  • Biofilms / drug effects*
  • Biofilms / growth & development
  • Drug Synergism
  • Escherichia coli / drug effects
  • Escherichia coli / physiology
  • Flagella / drug effects
  • Humans
  • SELEX Aptamer Technique
  • Salmonella / drug effects
  • Salmonella / genetics
  • Salmonella / physiology
  • Salmonella paratyphi A / drug effects
  • Salmonella paratyphi A / physiology

Substances

  • Anti-Bacterial Agents
  • Aptamers, Nucleotide
  • Ampicillin