A Library Approach to Cationic Amphiphilic Polyproline Helices that Target Intracellular Pathogenic Bacteria.
ACS Infect Dis
; 4(9): 1300-1305, 2018 09 14.
Article
em En
| MEDLINE
| ID: mdl-29979033
ABSTRACT
A number of pathogenic bacteria reproduce inside mammalian cells and are thus inaccessible to many antimicrobial drugs. Herein, we present a facile method to a focused library of antibacterial agents known as cationic amphiphilic polyproline helices (CAPHs). We identified three CAPHs from the library with superior cell penetration within macrophages and excellent antibacterial action against both Gram-positive and Gram-negative bacteria. These cell-penetrating antibacterial CAPHs have specific subcellular localizations that allow for targeting of pathogenic bacteria at their intracellular niches, a unique feature that promotes the successful clearance of intracellular pathogens ( Salmonella, Shigella, and Listeria) residing within macrophages. Furthermore, the selected CAPHs also significantly reduced bacterial infections in an in vivo model of Caenorhabditis elegans, with minimal in vivo toxicity.
Palavras-chave
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Peptídeos
/
Infecções Bacterianas
/
Peptídeos Catiônicos Antimicrobianos
/
Bibliotecas de Moléculas Pequenas
/
Antibacterianos
Limite:
Animals
/
Humans
Idioma:
En
Revista:
ACS Infect Dis
Ano de publicação:
2018
Tipo de documento:
Article
País de afiliação:
Estados Unidos