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SYNTHETIC MELANOCORTINS WITH ANTIMICROBIAL ACTIVITY

Antimicrobial actionCandidiasisDermatological infectionsSynthetic melanocortins

Introduction

Synthetic melanocortins (8 amino acid peptides, chemically stable) with antimicrobial effects to treat infective disorders.

Technical features

The widespread use of antibiotics has caused a growing problem of antimicrobial resistance in the community and in hospital settings. Fungal and bacterial resistance to current therapies are observed particularly in immunocompromised patients. The melanocortins are endogenous peptides that exert pleiotropic effects on the host. Chemically stable synthetic derivatives with more selective activity could form the basis for novel antimicrobial therapies. Structure-activity relation (SAR) studies on α-MSH-derived sequences were performed in order to design synthetic molecules with enhanced potency and broad spectrum of antimicrobial activity. These synthetic peptides had anti-Candida properties, including azole-resistant Candida strains, and exerted killing activity against bacterial strains including gram-positive and gram-negative organisms.

Possible Applications

  • Dermatological infections (gram-positive/negative bacteria and fungi such as pressure sores, burns and scalds, and many other conditions);
  • Dental and periodontal diseases;
  • Vaginal infections;
  • Immunocompromised host with multiple resistance to conventional antibiotics.

Advantages

  • Broad spectrum of antimicrobial action that includes yeasts, bacteria and low toxicity;
  • Concomitant anti-inflammatory action.