Title
An adamantyl amino acid containing gramicidin S analogue with broad spectrum antibacterial activity and reduced hemolytic activity
Author
Kapoerchan, V.V.
Knijnenburg, A.D.
Niamat, M.
Spalburg, E.
de Neeling, A.J.
Nibbering, P.H.
Mars-Groenendijk, R.H.
Noort, D.
Otero, J.M.
Llamas-Saiz, A.L.
van Raaij, M.J.
van der Marel, G.A.
Overkleeft, H.S.
Overhand, M.
TNO Defensie en Veiligheid
Publication year
2010
Abstract
The cyclic cationic antimicrobial peptide gramicidin S (GS) is an effective topical antibacterial agent that is toxic for human red blood cells (hemolysis). Herein, we present a series of amphiphilic derivatives of GS with either two or four positive charges and characteristics ranging between very polar and very hydrophobic. Screening of this series of peptide derivatives identified a compound that combines effective antibacterial activity with virtually no toxicity within the same concentration range. This peptide acts against both Gram-negative and Gram-positive bacteria, including several MRSA strains, and represents an interesting lead for the development of a broadly applicable antibiotic. © 2010 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.
Subject
Health
Amino acids
Antibiotics
Gramicidin
Methicillin-resistant Staphylococcus aureus (MRSA)
Peptides
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DOI
https://doi.org/10.1002/chem.201001686
TNO identifier
425161
ISSN
0947-6539
Source
Chemistry - A European Journal, 16 (40), 12174-12181
Document type
article