Potent and rapid bactericidal action of alyteserin-1c and its [E4K] analog against multidrug-resistant strains of Acinetobacter baumannii

Structural diversity and species distribution of host-defense peptides in frog skin secretions

“…The alyteserin-1 peptides show selective growth inhibitory activity against Gram-negative bacteria while displaying low hemolytic activity against human erythrocytes. Alyteserin-1c is particularly potent against multidrugresistant strains of the nosocomial pathogen Acinetobacter baumannii [26]. The alyteserin-2 peptides preferentially inhibit the growth of Gram-positive bacteria such as Staphylococcus aureus and also display low hemolytic activity [25].…”

Efficacy of six frog skin-derived antimicrobial peptides against colistin-resistant strains of the Acinetobacter baumannii group

“…Previous studies have shown that the peptides [E4K]alyteserin1c [15] and [D4K]B2RP [16] show high potency against colistinsusceptible nosocomial isolates of A. baumannii. More than 99.9% of the bacteria were killed within 30 min by the alyteserin-1c analogue at a concentration of 1× the minimum bactericidal concentration [15].…”

Confronting multidrug-resistant Acinetobacter baumannii: a review

“…The haemolytic activity of the naturally occurring peptide was relatively low. Colnon et al [138] reported that it presented bactericidal activity against MDR-AB in the MIC range of 5-10 M. Following substitution of the Glu4 residue by l-Lys, the created analogue [E4K] was found to have a four-fold increase in potency against all strains of MDR-AB tested by the authors [138]. Moreover, the haemolytic activity of the [E4K] analogue was appreciably lower than the naturally occurring peptide (lethal concentration for 50% of test population >400 M) and the analogue was extremely soluble in physiological buffers.…”

“…However, a major obstacle to the development of peptide-based anti-infective drugs, particularly if they are to be administered systemically, is their short half-lives in the circulation [137]. Efforts are constantly being made to overcome this problem, with varying results [138].…”

“…Moreover, the haemolytic activity of the [E4K] analogue was appreciably lower than the naturally occurring peptide (lethal concentration for 50% of test population >400 M) and the analogue was extremely soluble in physiological buffers. In a time-kill assay, >99.9% of the bacteria were killed within 30 min by the [E4K] analogue at a concentration of 1 × the minimum bactericidal concentration [138].…”