title: [Enhancement of cytotoxicity of cantionic antimicrobial peptide in tumor cells by conjugation to cell-penetrating peptide].
abstract: Due to their lower risk for induction of resistance, membrane-active antimicrobial peptides with anticancer effect are attractive in cancer therapy. Because cell binding contributes to the cytotoxicity of peptide, it is possible to enhance the cytotoxicity of antimicrobial peptide in tumor cells by conjugation to a cell-penetrating peptide (CPP). In this paper, a fusion peptide MPGA by conjugation of antimicrobial peptide MP to CPP Antp at its N-terminus was constructed. After compared the cytotoxicity of unconjugated MP with that of the fusion peptide, it was found that MPGA showed higher cytotoxicity than that of unconjugated MP. And the fusion peptide MPGA induced cell death in tumor cells by membrane disruption. These results demonstrated that the cytotoxicity of antimicrobial peptide can be significantly enhanced by conjugation to CPP, which might be an effective way to develop novel anticancer drugs.
authors.affiliation: Key Lab of Transplant Engineering and Immunology, Ministry of Health, West China Hospital, Sichuan University, Chengdu 610041, China.
authors.forename: Shan
authors.initials: S
authors.lastname: Liu
authors.forename: Hao
authors.initials: H
authors.lastname: Yang
authors.forename: Huawei
authors.initials: H
authors.lastname: Cai
authors.forename: Lin
authors.initials: L
authors.lastname: Wan
authors.forename: Xiaofeng
authors.initials: X
authors.lastname: Lu
mesh_terms: D023181:Antimicrobial Cationic Peptides / Q000493:pharmacokinetics / Q000494:pharmacology*; D000970:Antineoplastic Agents / Q000493:pharmacokinetics / Q000494:pharmacology*; D045744:Cell Line, Tumor; D002463:Cell Membrane Permeability / Q000187:drug effects*; D006801:Humans
chemical_list: D023181:Antimicrobial Cationic Peptides; D000970:Antineoplastic Agents