title: A novel antimicrobial peptide derived from membrane-proximal external region of human immunodeficiency virus type 1.
abstract: With increasing microbial drug resistance worldwide, antimicrobial peptides (AMPs) are considered promising alternatives to addressing this problem. In this study, a series of synthetic peptides were designed based on the membrane-disrupting properties of the membrane-proximal external region (MPER) of human immunodeficiency virus type 1 (HIV-1) envelope protein. The peptide AP16-A was found to exhibit the most effective antimicrobial activities against both Gram-negative and Gram-positive bacteria. The minimal bactericidal concentration (MBC) of AP16-A ranged from 2 μg/ml to 16 μg/ml. AP16-A had no detectable cytotoxicity in various tissue cultures and a mouse model. Furthermore, results of confocal fluorescence microscopy and the SYTOX Green uptake assay indicated that AP16-A killed Gram-negative bacteria by the combined effects of relatively slow membrane permeabilization and interaction with an intracellular target, while it killed Gram-positive bacteria by a fast membrane permeabilization process, which achieved relatively more rapid bacterial killing kinetics. The results of this study support the potential use of AP16-A as an AMP.
authors.affiliation: National Engineering Laboratory for AIDS Vaccine, School of Life Sciences, Jilin University, Changchun, Jilin, China.
authors.forename: Xiaoqiu
authors.initials: X
authors.lastname: He
authors.affiliation: National Engineering Laboratory for AIDS Vaccine, School of Life Sciences, Jilin University, Changchun, Jilin, China.
authors.forename: Huayan
authors.initials: H
authors.lastname: Zhang
authors.affiliation: National Engineering Laboratory for AIDS Vaccine, School of Life Sciences, Jilin University, Changchun, Jilin, China.
authors.forename: Yuhua
authors.initials: Y
authors.lastname: Shi
authors.affiliation: National Engineering Laboratory for AIDS Vaccine, School of Life Sciences, Jilin University, Changchun, Jilin, China.
authors.forename: Xin
authors.initials: X
authors.lastname: Gong
authors.affiliation: National Engineering Laboratory for AIDS Vaccine, School of Life Sciences, Jilin University, Changchun, Jilin, China.
authors.forename: Shanshan
authors.initials: S
authors.lastname: Guan
authors.affiliation: National Engineering Laboratory for AIDS Vaccine, School of Life Sciences, Jilin University, Changchun, Jilin, China.
authors.forename: He
authors.initials: H
authors.lastname: Yin
authors.affiliation: National Engineering Laboratory for AIDS Vaccine, School of Life Sciences, Jilin University, Changchun, Jilin, China.
authors.forename: Lan
authors.initials: L
authors.lastname: Yang
authors.affiliation: National Engineering Laboratory for AIDS Vaccine, School of Life Sciences, Jilin University, Changchun, Jilin, China.
authors.forename: Yongjiao
authors.initials: Y
authors.lastname: Yu
authors.affiliation: National Engineering Laboratory for AIDS Vaccine, School of Life Sciences, Jilin University, Changchun, Jilin, China.
authors.forename: Ziyu
authors.initials: Z
authors.lastname: Kuai
authors.affiliation: National Engineering Laboratory for AIDS Vaccine, School of Life Sciences, Jilin University, Changchun, Jilin, China.
authors.forename: Dongni
authors.initials: D
authors.lastname: Liu
authors.affiliation: Department of Hepatology, The First Hospital, Jilin University, Changchun, Jilin, China.
authors.forename: Rui
authors.initials: R
authors.lastname: Hua
authors.affiliation: State Key Laboratory of Theoretical and Computational Chemistry, Institute of Theoretical Chemistry, Jilin University, Changchun, Jilin, China.
authors.forename: Song
authors.initials: S
authors.lastname: Wang
authors.affiliation: National Engineering Laboratory for AIDS Vaccine, School of Life Sciences, Jilin University, Changchun, Jilin, China; Key Laboratory for Molecular Enzymology and Engineering, The Ministry of Education, School of Life Sciences, Jilin University, Changchun, Jilin, China. Electronic address: shanym@jlu.edu.cn.
authors.forename: Yaming
authors.initials: Y
authors.lastname: Shan
mesh_terms: D000595:Amino Acid Sequence; D000818:Animals; D000890:Anti-Infective Agents / Q000302:isolation & purification / Q000494:pharmacology*; D005260:Female; D015497:HIV-1 / Q000737:chemistry*; D051379:Mice; D008807:Mice, Inbred BALB C; D010455:Peptides / Q000302:isolation & purification / Q000494:pharmacology*
chemical_list: D000890:Anti-Infective Agents; D010455:Peptides
keywords: Antimicrobial activity; Antimicrobial peptides; Bacterial killing kinetics; Membrane permeabilization