1. Academic Validation
  2. Anti-biofilm and anti-adherence properties of novel cyclic dipeptides against oral pathogens

Anti-biofilm and anti-adherence properties of novel cyclic dipeptides against oral pathogens

  • Bioorg Med Chem. 2019 Jun 15;27(12):2323-2331. doi: 10.1016/j.bmc.2018.11.042.
Gaëlle Simon 1 Christopher Bérubé 2 Normand Voyer 3 Daniel Grenier 4
Affiliations

Affiliations

  • 1 Groupe de Recherche en Écologie Buccale, Faculté de Médecine Dentaire, Université Laval, 2420, rue de la Terrasse, Québec, QC G1V 0A6, Canada; Département de Chimie and PROTEO, Université Laval, Québec, QC G1V 0A6, Canada.
  • 2 Département de Chimie and PROTEO, Université Laval, Québec, QC G1V 0A6, Canada.
  • 3 Département de Chimie and PROTEO, Université Laval, Québec, QC G1V 0A6, Canada. Electronic address: [email protected].
  • 4 Groupe de Recherche en Écologie Buccale, Faculté de Médecine Dentaire, Université Laval, 2420, rue de la Terrasse, Québec, QC G1V 0A6, Canada. Electronic address: [email protected].
Abstract

Microorganisms embedded in a biofilm are significantly more resistant to antimicrobial agents and the defences of the human immune system, than their planktonic counterpart. Consequently, compounds that can inhibit biofilm formation are of great interest for novel therapeutics. In this study, a screening approach was used to identify novel cyclic dipeptides that have anti-biofilm activity against oral pathogens. Five new active compounds were identified that prevent biofilm formation by the cariogenic bacterium Streptococcus mutans and the pathogenic fungus Candida albicans. These compounds also inhibit the adherence of Microorganisms to a hydroxylapatite surface. Further investigations were conducted on these compounds to establish the structure-activity relationship, and it was deduced that the common cleft pattern is required for these molecules to act effectively against biofilms.

Keywords

Adherence; Anti-biofilm; Biofilm; C. albicans; Candidiasis; Cyclic dipeptides; Dental caries; Quorum sensing; S. mutans.

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