Star-shaped polypeptides exhibit potent antibacterial activities

Yu Fon Chen, Ying Da Lai, Chien-Hsiang Chang, Yu Cheng Tsai, Chen Chi Tang, Jeng-Shiung Jan

Research output: Contribution to journalArticle

Abstract

Peptide-based biomaterials are a promising class of antimicrobial agents that work by physically damaging bacterial cell membranes rather than targeting intracellular factors, resulting in less susceptibility to drug resistance. Herein we report the synthesis of cationic, star-shaped polypeptides with 3 to 8 arms and their evaluation as antimicrobial agents against different types of bacteria. The effects of the arm number and side chain group on their antimicrobial activities were systematically investigated. Compared to their linear counterparts, these star-shaped polypeptides exhibited potent antibacterial activity (which may involve adhesion and disruption processes). The increase of the arm number can efficiently increase the antibacterial activities up until 8 arms, which did not exhibit further improvement of antibacterial activities. Poly(l-lysine) (PLL) modified with an indole group (PLL-g-indo) exhibited the best antibacterial activity among all grafted copolypeptides and improved cytotoxic selectivity towards pathogens over mammalian cells without compromising their hemolytic activities. In vivo studies showed that the star-shaped PLL-g-indo can effectively suppress Enterohaemorrhagic E. coli (EHEC) infection and attenuate the clinical symptoms in mice, suggesting that they are promising antimicrobial agents.

Original languageEnglish
Pages (from-to)11696-11708
Number of pages13
JournalNanoscale
Volume11
Issue number24
DOIs
Publication statusPublished - 2019 Jun 28

Fingerprint

Antimicrobial agents
Polypeptides
Phase locked loops
Anti-Infective Agents
Stars
Peptides
Biocompatible Materials
Pathogens
Cell membranes
Biomaterials
Escherichia coli
Lysine
Bacteria
Adhesion
Cells
Pharmaceutical Preparations

All Science Journal Classification (ASJC) codes

  • Materials Science(all)

Cite this

Chen, Yu Fon ; Lai, Ying Da ; Chang, Chien-Hsiang ; Tsai, Yu Cheng ; Tang, Chen Chi ; Jan, Jeng-Shiung. / Star-shaped polypeptides exhibit potent antibacterial activities. In: Nanoscale. 2019 ; Vol. 11, No. 24. pp. 11696-11708.
@article{9c34fedd48264cadb0877ba68ea4da00,
title = "Star-shaped polypeptides exhibit potent antibacterial activities",
abstract = "Peptide-based biomaterials are a promising class of antimicrobial agents that work by physically damaging bacterial cell membranes rather than targeting intracellular factors, resulting in less susceptibility to drug resistance. Herein we report the synthesis of cationic, star-shaped polypeptides with 3 to 8 arms and their evaluation as antimicrobial agents against different types of bacteria. The effects of the arm number and side chain group on their antimicrobial activities were systematically investigated. Compared to their linear counterparts, these star-shaped polypeptides exhibited potent antibacterial activity (which may involve adhesion and disruption processes). The increase of the arm number can efficiently increase the antibacterial activities up until 8 arms, which did not exhibit further improvement of antibacterial activities. Poly(l-lysine) (PLL) modified with an indole group (PLL-g-indo) exhibited the best antibacterial activity among all grafted copolypeptides and improved cytotoxic selectivity towards pathogens over mammalian cells without compromising their hemolytic activities. In vivo studies showed that the star-shaped PLL-g-indo can effectively suppress Enterohaemorrhagic E. coli (EHEC) infection and attenuate the clinical symptoms in mice, suggesting that they are promising antimicrobial agents.",
author = "Chen, {Yu Fon} and Lai, {Ying Da} and Chien-Hsiang Chang and Tsai, {Yu Cheng} and Tang, {Chen Chi} and Jeng-Shiung Jan",
year = "2019",
month = "6",
day = "28",
doi = "10.1039/c9nr02012h",
language = "English",
volume = "11",
pages = "11696--11708",
journal = "Nanoscale",
issn = "2040-3364",
publisher = "Royal Society of Chemistry",
number = "24",

}

Star-shaped polypeptides exhibit potent antibacterial activities. / Chen, Yu Fon; Lai, Ying Da; Chang, Chien-Hsiang; Tsai, Yu Cheng; Tang, Chen Chi; Jan, Jeng-Shiung.

In: Nanoscale, Vol. 11, No. 24, 28.06.2019, p. 11696-11708.

Research output: Contribution to journalArticle

TY - JOUR

T1 - Star-shaped polypeptides exhibit potent antibacterial activities

AU - Chen, Yu Fon

AU - Lai, Ying Da

AU - Chang, Chien-Hsiang

AU - Tsai, Yu Cheng

AU - Tang, Chen Chi

AU - Jan, Jeng-Shiung

PY - 2019/6/28

Y1 - 2019/6/28

N2 - Peptide-based biomaterials are a promising class of antimicrobial agents that work by physically damaging bacterial cell membranes rather than targeting intracellular factors, resulting in less susceptibility to drug resistance. Herein we report the synthesis of cationic, star-shaped polypeptides with 3 to 8 arms and their evaluation as antimicrobial agents against different types of bacteria. The effects of the arm number and side chain group on their antimicrobial activities were systematically investigated. Compared to their linear counterparts, these star-shaped polypeptides exhibited potent antibacterial activity (which may involve adhesion and disruption processes). The increase of the arm number can efficiently increase the antibacterial activities up until 8 arms, which did not exhibit further improvement of antibacterial activities. Poly(l-lysine) (PLL) modified with an indole group (PLL-g-indo) exhibited the best antibacterial activity among all grafted copolypeptides and improved cytotoxic selectivity towards pathogens over mammalian cells without compromising their hemolytic activities. In vivo studies showed that the star-shaped PLL-g-indo can effectively suppress Enterohaemorrhagic E. coli (EHEC) infection and attenuate the clinical symptoms in mice, suggesting that they are promising antimicrobial agents.

AB - Peptide-based biomaterials are a promising class of antimicrobial agents that work by physically damaging bacterial cell membranes rather than targeting intracellular factors, resulting in less susceptibility to drug resistance. Herein we report the synthesis of cationic, star-shaped polypeptides with 3 to 8 arms and their evaluation as antimicrobial agents against different types of bacteria. The effects of the arm number and side chain group on their antimicrobial activities were systematically investigated. Compared to their linear counterparts, these star-shaped polypeptides exhibited potent antibacterial activity (which may involve adhesion and disruption processes). The increase of the arm number can efficiently increase the antibacterial activities up until 8 arms, which did not exhibit further improvement of antibacterial activities. Poly(l-lysine) (PLL) modified with an indole group (PLL-g-indo) exhibited the best antibacterial activity among all grafted copolypeptides and improved cytotoxic selectivity towards pathogens over mammalian cells without compromising their hemolytic activities. In vivo studies showed that the star-shaped PLL-g-indo can effectively suppress Enterohaemorrhagic E. coli (EHEC) infection and attenuate the clinical symptoms in mice, suggesting that they are promising antimicrobial agents.

UR - http://www.scopus.com/inward/record.url?scp=85067829875&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=85067829875&partnerID=8YFLogxK

U2 - 10.1039/c9nr02012h

DO - 10.1039/c9nr02012h

M3 - Article

VL - 11

SP - 11696

EP - 11708

JO - Nanoscale

JF - Nanoscale

SN - 2040-3364

IS - 24

ER -