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Biological activities of cationicity-enhanced and hydrophobicity-optimized analogues of an antimicrobial peptide, dermaseptin-PS3, from the skin secretion of phyllomedusa sauvagii
Tan Y.2; Chen X.2; Ma C.2; Xi X.2; Wang L.2; Zhou M.2; Burrows J.F.2; Kwok H.F.1; Chen T.2
2018-08-07
Source PublicationToxins
ISSN20726651
Volume10Issue:8
Abstract

The skin secretions of the subfamily Phyllomedusinae have long been known to contain a number of compounds with antimicrobial potential. Herein, a biosynthetic dermaseptin-precursor cDNA was obtained from a Phyllomedusa sauvagii skin secretion-derived cDNA library, and thereafter, the presence of the mature peptide, namely dermaseptin-PS3 (DPS3), was confirmed by LC–MS/MS. Moreover, this naturally occurring peptide was utilized to design two analogues, K-DPS3 (introducing two lysine residues at positions 5 and 17 to replace acidic amino acids) and L-DPS3 (replacing two neutral amino acids with the hydrophobic amino acid, leucine), improving its cationicity on the polar/unipolar face and hydrophobicity in a highly conserved sequence motif, respectively. The results in regard to the two analogues show that either increasing cationicity, or hydrophobicity, enhance the antimicrobial activity. Also, the latter analogue had an enhanced anticancer activity, with pretreatment of H157 cells with 1 µM L-DPS3 decreasing viability by approximately 78%, even though this concentration of peptide exhibited no haemolytic effect. However, it must be noted that in comparison to the initial peptide, both analogues demonstrate higher membrane-rupturing capacity towards mammalian red blood cells.

KeywordAnticancer Activity Antimicrobial Activity Antimicrobial Peptide (Amp) Anuran Skin Secretion Dermaseptin Drug Design
DOI10.3390/toxins10080320
URLView the original
Indexed BySCI
Language中文
WOS Research AreaFood Science & Technology ; Toxicology
WOS SubjectFood Science & Technology ; Toxicology
WOS IDWOS:000443617800016
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Cited Times [WOS]:2   [WOS Record]     [Related Records in WOS]
Document TypeJournal article
CollectionFaculty of Health Sciences
Affiliation1.Universidade de Macau
2.Queen's University Belfast
Recommended Citation
GB/T 7714
Tan Y.,Chen X.,Ma C.,et al. Biological activities of cationicity-enhanced and hydrophobicity-optimized analogues of an antimicrobial peptide, dermaseptin-PS3, from the skin secretion of phyllomedusa sauvagii[J]. Toxins,2018,10(8).
APA Tan Y..,Chen X..,Ma C..,Xi X..,Wang L..,...&Chen T..(2018).Biological activities of cationicity-enhanced and hydrophobicity-optimized analogues of an antimicrobial peptide, dermaseptin-PS3, from the skin secretion of phyllomedusa sauvagii.Toxins,10(8).
MLA Tan Y.,et al."Biological activities of cationicity-enhanced and hydrophobicity-optimized analogues of an antimicrobial peptide, dermaseptin-PS3, from the skin secretion of phyllomedusa sauvagii".Toxins 10.8(2018).
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