Abstract
We describe a strategy to boost anticancer activity and reduce normal cell toxicity of short antimicrobial peptides by adding positive charge amino acids and non-nature bulky amino acid β-naphthylalanine residues to their termini. Among the designed peptides, K4R2-Nal2-S1 displayed better salt resistance and less toxicity to hRBCs and human fibroblast than Nal2-S1 and K6-Nal2-S1. Fluorescence microscopic studies indicated that the FITC-labeled K4R2-Nal2-S1 preferentially binds cancer cells and causes apoptotic cell death. Moreover, a significant inhibition in human lung tumor growth was observed in the xenograft mice treated with K4R2-Nal2-S1. Our strategy provides new opportunities in the development of highly effective and selective antimicrobial and anticancer peptide-based therapeutics.
Highlights
The development of cationic antimicrobial peptides (CAPs) as functional therapeutics to fight against infectious diseases and cancer has become an important area [1,2,3]
CAPs are normally characterized by their positive charges and amphipathic features, which enable them to bind to negatively charged bacterial cell membranes and cause the disruption of the membrane, the death of bacteria [7, 8]
Only a few studies were reported on the development and application of CAPs in cancer treatment and most of these studies were focused on CAPs derived from natural amino acids [39,40,41,42,43]
Summary
The development of cationic antimicrobial peptides (CAPs) as functional therapeutics to fight against infectious diseases and cancer has become an important area [1,2,3]. Tremendous efforts have been put into the development of new treatments, cancer remains the major cause of death [9]. Chemotherapies, despite their severe side effects to normal cells and tissues, and the easy formation of multi-drug resistances, are still the principal drugs used to treat cancer in the advanced or metastatic stages [9]. The outer membranes of cancer cells have been reported to carry more negatively charged molecules, PLOS ONE | DOI:10.1371/journal.pone.0126390 May 13, 2015
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