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Int J Biol Sci 2018; 14(6):599-607. doi:10.7150/ijbs.23419

Research Paper

Evaluation of the bioactivity of a mastoparan peptide from wasp venom and of its analogues designed through targeted engineering

Xiaoling Chen1*, Luyao Zhang1*, Yue Wu1, Lei Wang1, Chengbang Ma1✉, Xinping Xi1✉, Olaf R.P. Bininda-Emonds2, Chris Shaw1, Tianbao Chen1, Mei Zhou1✉

1. Natural Drug Discovery Group, School of Pharmacy, Queen's University Belfast, Belfast, Northern Ireland, UK
2. AG Systematik und Evolutionsbiologie, IBU—Faculty V, Carl von Ossietzky University Oldenburg, Oldenburg, Germany
* These authors contributed equally to this work

Abstract

Mastoparan is a typical cationic and amphipathic tetradecapeptide found in wasp venom and exhibits potent biological activities. Yet, compared with other insect-derived peptides, such as melittin from the bee venom, this family have been underrated. Herein, we evaluated the biological activities of mastoparan-C (MP-C), which was identified from the venom of the European Hornet (Vespa crabro), and rationally designed two analogues (a skeleton-based cyclization by two cysteine residues and an N-terminal extension via tat-linked) for enhancing the stability of the biological activity and membrane permeability, respectively. Three peptides possessed broadly efficacious inhibiting capacities towards common pathogens, resistant strains, as well as microbial biofilm. Although, cyclized MP-C showed longer half-life time than the parent peptide, the lower potency of antimicrobial activity and higher degree of haemolysis were observed. The tat-linked MP-C exhibited more potent anticancer activity than the parent peptide, but it also loses the specificity. The study revealed that MP-C is good candidate for developing antimicrobial agents and the targeted-design could improve the stability and transmembrane delivery, but more investigation would be needed to adjust the side effects brought from the design.

Keywords: mastoparan-C, peptide design, antimicrobial, anticancer

This is an open access article distributed under the terms of the Creative Commons Attribution (CC BY-NC) license (https://creativecommons.org/licenses/by-nc/4.0/). See http://ivyspring.com/terms for full terms and conditions.
How to cite this article:
Chen X, Zhang L, Wu Y, Wang L, Ma C, Xi X, Bininda-Emonds ORP, Shaw C, Chen T, Zhou M. Evaluation of the bioactivity of a mastoparan peptide from wasp venom and of its analogues designed through targeted engineering. Int J Biol Sci 2018; 14(6):599-607. doi:10.7150/ijbs.23419. Available from http://www.ijbs.com/v14p0599.htm