ArticlePloS one2019
Design, antimicrobial activity and mechanism of action of Arg-rich ultra-short cationic lipopeptides.
Article in PloS one, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.
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Who cites it
19 citing papers in PubMed, 51 citations in OpenAlex.
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- Proline-Modified RWn Peptides: Enhanced Antifungal Efficacy and Synergy with Conventional Antibiotics for Combating Resistant Fungal Infections.ACS omega · 2024Article
- Antibacterial efficacy and membrane mechanism of action of theMicrobiology spectrum · 2024Article
- Mechanism of Action of Oxazoline-Based Antimicrobial Polymers Against Staphylococcus aureus: In Vivo Antimicrobial Activity Evaluation.Advanced healthcare materials · 2023Article
- Evaluation of the Effect of Antibacterial Peptides on Model Monolayers.International journal of molecular sciences · 2023Article
- Structural and biological characterization of shortened derivatives of the cathelicidin PMAP-36.Scientific reports · 2023Article
- Development of novel broad-spectrum antimicrobial lipopeptides derived from plantaricin NC8 β.Scientific reports · 2023Article
- Antimicrobial activities and phylogenetic study ofBiotechnologia · 2023Article
- An Optimized Workflow for the Discovery of New Antimicrobial Compounds Targeting Bacterial RNA Polymerase Complex Formation.Antibiotics (Basel, Switzerland) · 2022Article
- Induction of Systemic Resistance in Maize and Antibiofilm Activity of Surfactin FromFrontiers in microbiology · 2022Article
- Gemini Lipopeptide Bearing an Ultrashort Peptide for Enhanced Transfection Efficiency and Cancer-Cell-Specific Cytotoxicity.ACS omega · 2021Article
- Effects of Lipidation on a Proline-Rich Antibacterial Peptide.International journal of molecular sciences · 2021Article
- Biological and Physico-Chemical Characteristics of Arginine-Rich Peptide Gemini Surfactants with Lysine and Cystine Spacers.International journal of molecular sciences · 2021Article
- DBAASP v3: database of antimicrobial/cytotoxic activity and structure of peptides as a resource for development of new therapeutics.Nucleic acids research · 2021Article
- Lipidation of Antimicrobial Peptides as a Design Strategy for Future Alternatives to Antibiotics.International journal of molecular sciences · 2020Review
- Effect of Disulfide Cyclization of Ultrashort Cationic Lipopeptides on Antimicrobial Activity and Cytotoxicity.International journal of molecular sciences · 2020Article
- Vancomycin-Lipopeptide Conjugates with High Antimicrobial Activity on Vancomycin-Resistant Enterococci.Pharmaceuticals (Basel, Switzerland) · 2020Article
- Ultrashort Cationic Lipopeptides-Effect ofMolecules (Basel, Switzerland) · 2020Article
Corrections and comments
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Authors and funding
8 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The increasing emergence of multidrug-resistant microorganisms represents one of the greatest challenges in the clinical management of infectious diseases, and requires the development of novel antimicrobial agents. To this aim, we de novo designed a library of Arg-rich ultra-short cationic antimicrobial lipopeptides (USCLs), based on the Arg-X-Trp-Arg-NH2 peptide moiety conjugated with a fatty acid, and investigated their antibacterial potential. USCLs exhibited an excellent antimicrobial activity against clinically pathogenic microorganisms, in particular Gram-positive bacteria, including multidrug resistant strains, with MIC values ranging between 1.56 and 6.25 μg/mL. The capability of the two most active molecules, Lau-RIWR-NH2 and Lau-RRIWRR-NH2, to interact with the bacterial membranes has been predicted by molecular dynamics and verified on liposomes by surface plasmon resonance. Both compounds inhibited the growth of S. aureus even at sub MIC concentrations and induced cell membranes permeabilization by producing visible cell surface alterations leading to a significant decrease in bacterial viability. Interestingly, no cytotoxic effects were evidenced for these lipopeptides up to 50-100 μg/mL in hemolysis assay, in human epidermal model and HaCaT cells, thus highlighting a good cell selectivity. These results, together with the simple composition of USCLs, make them promising lead compounds as new antimicrobials.
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