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Evaluating the Bioactivity of a Novel Antimicrobial and Anticancer Peptide, Dermaseptin-PS4(Der-PS4), from the Skin Secretion of Phyllomedusa sauvagii

1
Natural Drug Discovery Group, School of Pharmacy, Queen’s University, Belfast BT9 7BL, UK
2
Department of Nutrition, Henry Fok School of Food Science and Engineering, Shaoguan University, Shaoguan 512005, China
3
School of Life Sciences and Technology, China Pharmaceutical University, Nanjing 211198, China
*
Authors to whom correspondence should be addressed.
Theses authors contributed equally to this work.
Molecules 2019, 24(16), 2974; https://doi.org/10.3390/molecules24162974
Received: 25 July 2019 / Revised: 11 August 2019 / Accepted: 15 August 2019 / Published: 16 August 2019
(This article belongs to the Special Issue Peptide Chemistry Ⅱ)
Dermaseptins belonging to a large family of cationic membrane-disruption antimicrobial peptides display extensive antibacterial and antiproliferative activities depending on a coil-to-helix transition and the specific structural parameters. Herein, a novel dermaseptin peptide named Der-PS4 was discovered from the skin secretion of the waxy monkey tree frog, Phyllomedusa sauvagii. The complementary DNA (cDNA)-encoding precursor was obtained relying on “shotgun” cloning, and afterwards, a mature peptide amino acid sequence was identified by reverse-phase high performance liquid chromatography (RP-HPLC) and MS/MS. Specimens were chemically synthesized and applied for further functional studies. Structural analysis demonstrated a higher α-helical content in the membrane-mimetic environment compared with that in the ammonium acetate/water circumstance. Der-PS4 displayed a broad spectrum of antimicrobial activities against tested pathogenic microorganisms, however, exhibiting slight membrane-damaging effectiveness towards horse red blood cells. Coincident with the inhibitory activities on pathogens, Der-PS4 also showed considerable biofilm eradicating impact. Also, Der-PS4 penetrated cell membrane in a relative short period under each minimum bactericidal concentration. In addition, Der-PS4 possessed antiproliferative capacity against five cancer cell lines, while presenting slight suppressing effect on human microvascular endothelial, HMEC-1. These findings provide a promising insight for the discovery and development of novel drugs from a natural source. View Full-Text
Keywords: dermaseptin; molecular cloning; antimicrobial peptide; anticancer peptide; frog skin secretion dermaseptin; molecular cloning; antimicrobial peptide; anticancer peptide; frog skin secretion
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Chen, D.; Zhou, X.; Chen, X.; Huang, L.; Xi, X.; Ma, C.; Zhou, M.; Wang, L.; Chen, T. Evaluating the Bioactivity of a Novel Antimicrobial and Anticancer Peptide, Dermaseptin-PS4(Der-PS4), from the Skin Secretion of Phyllomedusa sauvagii. Molecules 2019, 24, 2974.

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Molecules, EISSN 1420-3049, Published by MDPI AG
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