title: 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.affiliation: Institute of Biotechnology and Department of Medical Science, National Tsing Hua University, Hsinchu, 300, Taiwan.
authors.forename: Hung-Lun
authors.initials: HL
authors.lastname: Chu
authors.affiliation: Institute of Biotechnology and Department of Medical Science, National Tsing Hua University, Hsinchu, 300, Taiwan; Department of Neurology, National Taiwan University Hospital Hsinchu Branch, Hsinchu, 300, Taiwan.
authors.forename: Bak-Sau
authors.initials: BS
authors.lastname: Yip
authors.affiliation: Institute of Biotechnology and Department of Medical Science, National Tsing Hua University, Hsinchu, 300, Taiwan.
authors.forename: Kuan-Hao
authors.initials: KH
authors.lastname: Chen
authors.affiliation: Institute of Biotechnology and Department of Medical Science, National Tsing Hua University, Hsinchu, 300, Taiwan.
authors.forename: Hui-Yuan
authors.initials: HY
authors.lastname: Yu
authors.affiliation: Institute of Biotechnology and Department of Medical Science, National Tsing Hua University, Hsinchu, 300, Taiwan.
authors.forename: Ya-Han
authors.initials: YH
authors.lastname: Chih
authors.affiliation: Institute of Biotechnology and Department of Medical Science, National Tsing Hua University, Hsinchu, 300, Taiwan.
authors.forename: Hsi-Tsung
authors.initials: HT
authors.lastname: Cheng
authors.affiliation: Institute of Biotechnology and Department of Medical Science, National Tsing Hua University, Hsinchu, 300, Taiwan.
authors.forename: Yu-Ting
authors.initials: YT
authors.lastname: Chou
authors.affiliation: Institute of Biotechnology and Department of Medical Science, National Tsing Hua University, Hsinchu, 300, Taiwan.
authors.forename: Jya-Wei
authors.initials: JW
authors.lastname: Cheng
mesh_terms: D000818:Animals; D000900:Anti-Bacterial Agents / Q000494:pharmacology*; D000903:Antibiotics, Antineoplastic / Q000494:pharmacology*; D023181:Antimicrobial Cationic Peptides / Q000494:pharmacology*; D017209:Apoptosis; D045744:Cell Line, Tumor; D004926:Escherichia coli / Q000187:drug effects; D006801:Humans; D008175:Lung Neoplasms / Q000188:drug therapy*; D008297:Male; D008807:Mice, Inbred BALB C; D008819:Mice, Nude; D008826:Microbial Sensitivity Tests; D011550:Pseudomonas aeruginosa / Q000187:drug effects; D013211:Staphylococcus aureus / Q000187:drug effects; D023041:Xenograft Model Antitumor Assays
chemical_list: D000900:Anti-Bacterial Agents; D000903:Antibiotics, Antineoplastic; D023181:Antimicrobial Cationic Peptides