Dissection of the antimicrobial and hemolytic activity of Cap18: Generation of Cap18 derivatives with enhanced specificity

PLoS One. 2018 May 31;13(5):e0197742. doi: 10.1371/journal.pone.0197742. eCollection 2018.

Abstract

Due to the rapid emergence of resistance to classical antibiotics, novel antimicrobial compounds are needed. It is desirable to selectively kill pathogenic bacteria without targeting other beneficial bacteria in order to prevent the negative clinical consequences caused by many broad-spectrum antibiotics as well as reducing the development of antibiotic resistance. Antimicrobial peptides (AMPs) represent an alternative to classical antibiotics and it has been previously demonstrated that Cap18 has high antimicrobial activity against a broad range of bacterial species. In this study we report the design of a positional scanning library consisting of 696 Cap18 derivatives and the subsequent screening for antimicrobial activity against Y. ruckeri, A. salmonicida, S. Typhimurium and L. lactis as well as for hemolytic activity measuring the hemoglobin release of horse erythrocytes. We show that the hydrophobic face of Cap18, in particular I13, L17 and I24, is essential for its antimicrobial activity against S. Typhimurium, Y. ruckeri, A. salmonicida, E. coli, P. aeruginosa, L. lactis, L. monocytogenes and E. faecalis. In particular, Cap18 derivatives harboring a I13D, L17D, L17P, I24D or I24N substitution lost their antimicrobial activity against any of the tested bacterial strains. In addition, we were able to generate species-specific Cap18 derivatives by particular amino acid substitutions either in the hydrophobic face at positions L6, L17, I20, and I27, or in the hydrophilic face at positions K16 and K18. Finally, our data showed the proline residue at position 29 to be essential for the inherent low hemolytic activity of Cap18 and that substitution of the residues K16, K23, or G21 by any hydrophobic residues enhances the hemolytic activity. This study demonstrates the potential of generating species-specific AMPs for the selective elimination of bacterial pathogens.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Aeromonas salmonicida / drug effects
  • Amino Acid Substitution
  • Animals
  • Anti-Infective Agents / chemistry
  • Anti-Infective Agents / pharmacology*
  • Antimicrobial Cationic Peptides / chemistry
  • Antimicrobial Cationic Peptides / genetics
  • Antimicrobial Cationic Peptides / pharmacology*
  • Cathelicidins
  • Drug Design
  • Erythrocytes / drug effects
  • Hemolytic Agents / chemistry
  • Hemolytic Agents / pharmacology*
  • Horses
  • Microbial Sensitivity Tests
  • Peptide Library
  • Salmonella typhimurium / drug effects
  • Yersinia ruckeri / drug effects

Substances

  • Anti-Infective Agents
  • Antimicrobial Cationic Peptides
  • Hemolytic Agents
  • Peptide Library
  • Cathelicidins

Grants and funding

This work was supported by Danish Ministry of Food, Agriculture and Fisheries programme supporting Green Development and Demonstration (GUDP grant nr.: 3405-10-0124) (http://mst.dk/erhverv/groen-virksomhed/groent-udviklings-og-demonstrationsprogram-gudp/). This work was also supported by Innovation Fund Denmark (https://innovationsfonden.dk/en), grant number 7045-00021B. The funders had no role in study design, data collection and analysis, decision to publish, or preparation of the manuscript.