Unknown

Dataset Information

0

Broad-Spectrum Antimicrobial Activity and Improved Stability of a D-Amino Acid Enantiomer of DMPC-10A, the Designed Derivative of Dermaseptin Truncates.


ABSTRACT: DMPC-10A (ALWKKLLKK-Cha-NH2) is a 10-mer peptide derivative from the N-terminal domain of Dermaseptin-PC which has shown broad-spectrum antimicrobial activity as well as a considerable hemolytic effect. In order to reduce hemolytic activity and improve stability to endogenous enzymes, a D-amino acid enantiomer (DMPC-10B) was designed by substituting all L-Lys and L-Leu with their respective D-form amino acid residues, while the Ala1 and Trp3 remained unchanged. The D-amino acid enantiomer exhibited similar antimicrobial potency to the parent peptide but exerted lower cytotoxicity and hemolytic activity. Meanwhile, DMPC-10B exhibited remarkable resistance to hydrolysis by trypsin and chymotrypsin. In addition to these advantages, DMPC-10B exhibited an outstanding antibacterial effect against Methicillin-resistant Staphylococcus aureus (MRSA) and Klebsiella pneumoniae using the Galleria mellonella larva model and displayed synergistic activities with gentamicin against carbapenem-resistant K. pneumoniae strains. This indicates that DMPC-10B would be a promising alternative for treating antibiotic-resistant pathogens.

PROVIDER: S-EPMC7557582 | BioStudies |

REPOSITORIES: biostudies

Similar Datasets

| S-EPMC8348142 | BioStudies
| S-EPMC6920804 | BioStudies
| S-EPMC7451071 | BioStudies
| S-EPMC6535564 | BioStudies
| S-EPMC5573263 | BioStudies
| S-EPMC6021629 | BioStudies
| S-EPMC5913935 | BioStudies
| S-EPMC6195691 | BioStudies
| S-EPMC8319832 | BioStudies
| S-EPMC2778059 | BioStudies