Simple Strategy for Taming Membrane-Disrupting Antibiotics.
Bioconjug Chem
; 27(12): 2850-2853, 2016 Dec 21.
Article
em En
| MEDLINE
| ID: mdl-27801580
ABSTRACT
A strategy has been devised for increasing the cellular selectivity of membrane-disrupting antibiotics based on the attachment of a facially amphiphilic sterol. Using Amphotericin B (AmB) as a prototype, covalent attachment of cholic acid bound to a series of α,ω-diamines has led to a dramatic reduction in hemolytic activity, a significant reduction in toxicity toward HEK293T cells, and significant retention of antifungal activity.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Membrana Celular
/
Antibacterianos
Limite:
Humans
Idioma:
En
Ano de publicação:
2016
Tipo de documento:
Article