Abstract
The growing occurrence of bacterial resistance to conventional antibiotics has called for the development of new classes of antimicrobial agents. Antimicrobial peptides (AMPs) with broad antimicrobial spectrum derived from frog skin secretions have been demonstrated to be promising candidates for new antibiotic development. A proven rich source of these compounds are the skin secretions of the frogs in the Phyllomedusa genus. In this study, two novel phylloseptin peptides—phylloseptin-PTa and phylloseptin-PHa—were isolated from the skin secretions of the South American frogs, Phyllomedusa tarsius (P. tarsius) and Phyllomedusa hypochondrialis (P. hypochondrialis) through parallel transcriptomic and peptidomic studies. Replicates obtained by chemical synthesis were structurally analysed and shown to adopt an α-helix configuration in an amphiphilic environment. Both peptides demonstrated antimicrobial activities against planktonic Gram-positive bacteria strains, including Staphylococcus aureus, Enterococcus faecalis and methicillin-resistant Staphylococcus aureus , biofilms, as well as cytostatic effects on the non-small cell lung cancer cell line, NCI-H157, with relatively low haemolysis on horse erythrocytes and low cytotoxicity on the human microvascular endothelial cell line, HMEC-1. The discovery of phylloseptin peptides may further inspire the development of new types of antibiotics.
Highlights
Decades of research has revealed amphibian skin secretions as great natural sources of bioactive compounds, such as peptides, steroids, alkaloids and biogenic amines [1]
The results revealed that both phyllospetins were capable to eradicate the formed biofilm at the concentrations of their respective minimum biofilm eradication concentration (MBEC) and 2 × MBEC
The increase in antibiotic resistance incidents worldwide poses a severe threat to the fight against infectious diseases, urging the development of alternative antimicrobial drugs with low resistance induction potential
Summary
Decades of research has revealed amphibian skin secretions as great natural sources of bioactive compounds, such as peptides, steroids, alkaloids and biogenic amines [1]. Antimicrobial peptides (AMPs) comprise the group with the most immediate therapeutic potential owing to their antimicrobial superiority over conventional antibiotics. The AMPs derived from amphibian skin secretions have remarkable activities against a great range of microorganisms, falling into the categories of bacteria, fungi, protozoa and even viruses [2,3]. Molecules 2017, 22, 1428 these distinctive membrane interactions may represent a powerful weapon in the fight against resistant pathogenic microorganisms. The skin secretions of neotropical frogs of the subfamily Phyllomedusinae, which have attracted research attention worldwide in recent decades, contain an abundant variety of active peptides [6]
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