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Open AccessArticle

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

1
School of Pharmacy, Queen’s University Belfast, Belfast BT9 7BL, UK
2
Department of Natural Sciences, Faculty of Science and Technology, Middlesex University, London NW4 4BT, UK
*
Author to whom correspondence should be addressed.
Antibiotics 2020, 9(9), 627; https://doi.org/10.3390/antibiotics9090627
Received: 26 August 2020 / Revised: 15 September 2020 / Accepted: 17 September 2020 / Published: 21 September 2020
(This article belongs to the Special Issue Synthesis and Utility of Antimicrobial Peptides)
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. View Full-Text
Keywords: antimicrobial peptide; D-amino acid; protease stability; Galleria mellonella larva model antimicrobial peptide; D-amino acid; protease stability; Galleria mellonella larva model
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MDPI and ACS Style

Zai, Y.; Ying, Y.; Ye, Z.; Zhou, M.; Ma, C.; Shi, Z.; Chen, X.; Xi, X.; Chen, T.; Wang, L. Broad-Spectrum Antimicrobial Activity and Improved Stability of a D-Amino Acid Enantiomer of DMPC-10A, the Designed Derivative of Dermaseptin Truncates. Antibiotics 2020, 9, 627.

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