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Molecules 2017, 22(9), 1428;

Discovery of Phylloseptins that Defense against Gram-Positive Bacteria and Inhibit the Proliferation of the Non-Small Cell Lung Cancer Cell Line, from the Skin Secretions of Phyllomedusa Frogs

School of Chinese Materia Medica, Beijing University of Chinese Medicine, Beijing 102488, China
Natural Drug Discovery Group, School of Pharmacy, Queen’s University, Belfast BT9 7BL, UK
Authors to whom correspondence should be addressed.
Received: 3 August 2017 / Accepted: 26 August 2017 / Published: 29 August 2017
(This article belongs to the Special Issue Bioactive Natural Peptides As A Pipeline For Therapeutics)
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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. View Full-Text
Keywords: phylloseptins; antimicrobial peptides; anti-biofilm; cytostatic phylloseptins; antimicrobial peptides; anti-biofilm; cytostatic

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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

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Liu, J.; Wu, Q.; Li, L.; Xi, X.; Wu, D.; Zhou, M.; Chen, T.; Shaw, C.; Wang, L. Discovery of Phylloseptins that Defense against Gram-Positive Bacteria and Inhibit the Proliferation of the Non-Small Cell Lung Cancer Cell Line, from the Skin Secretions of Phyllomedusa Frogs. Molecules 2017, 22, 1428.

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