Characterisation of a novel peptide, Brevinin-1H, from the skin secretion of Amolops hainanensis and rational design of several analogues

Xinjie Pei, Zijian Gong, Qing Wu, Xiaoling Chen, Lei Wang, Chengbang Ma, Xinping Xi, Tianbao Chen, Christopher Shaw, Mei Zhou

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1 Citation (Scopus)
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Abstract

As drug-resistant bacteria have become a serious health problem and have caused thousands of deaths, finding new antibiotics has become an urgent research priority. A novel antimicrobial peptide, named Brevinin-1H, was identified in the skin secretion of Amolops hainanensis through ‘shotgun’ cloning. It has broad-spectrum antimicrobial activity against tested microorganisms and has anticancer cell activity. To improve its bioactivity and decrease its cytotoxicity, two structural analogues – Brevinin-1Ha and Brevinin-1HY - were designed based on the secondary structure of the natural peptide. Brevinin-1HY, in which tyrosine substituted Pro11, had similar activity to the natural peptide against Gram-negative bacteria and cancer cells, but showed a dramatic increase in haemolytic activity and cytotoxicity at its MIC. Brevinin-1Ha, which transferred the Rana-box from the C-terminal to a central position, had significantly decreased haemolytic activity, but also in antimicrobial and anticancer activity. The present data suggests that increasing the proportion of α-helix structure in an AMP can increase its target microorganism bioactivity to some extent.
Original languageEnglish
JournalChemical Biology & Drug Design
Early online date19 Aug 2020
DOIs
Publication statusEarly online date - 19 Aug 2020

Keywords

  • amphibian, anticancer activity, antimicrobial activity, peptide modification

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Pharmacology
  • Drug Discovery
  • Organic Chemistry

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