Novel antimicrobial peptides with high anticancer activity and selectivity.

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.

• Authors: Hung-Lun Chu, Bak-Sau Yip, Kuan-Hao Chen, Hui-Yuan Yu, Ya-Han Chih, Hsi-Tsung Cheng, Yu-Ting Chou, Jya-Wei Cheng
• Journal: PloS one (PLoS One) Vol. 10 Issue 5 Pg. e0126390 ( 2015) ISSN: 1932-6203 [Electronic] United States
• PMID: 25970292 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Anti-Bacterial Agents
• Antibiotics, Antineoplastic
• Antimicrobial Cationic Peptides

Topics

• Animals
• Anti-Bacterial Agents (pharmacology)
• Antibiotics, Antineoplastic (pharmacology)
• Antimicrobial Cationic Peptides (pharmacology)
• Apoptosis
• Cell Line, Tumor
• Escherichia coli (drug effects)
• Humans
• Lung Neoplasms (drug therapy)
• Male
• Mice, Inbred BALB C
• Mice, Nude
• Microbial Sensitivity Tests
• Pseudomonas aeruginosa (drug effects)
• Staphylococcus aureus (drug effects)
• Xenograft Model Antitumor Assays