Delivery of suramin as an antiviral agent through liposomal systems.
ChemMedChem
; 9(5): 933-9, 2014 May.
Article
en En
| MEDLINE
| ID: mdl-24616282
ABSTRACT
Norovirus RNA-dependent RNA polymerase (RdRp) is a promising target enzyme for the development of new antiviral drugs. Starting from the crystal structure of norovirus RdRp, we had previously performed an in silico docking search using a library of low-molecular-weight compounds that enabled us to select molecules with predicted enzyme inhibitory activity. Among these, the polysulfonated naphthylurea suramin proved to inhibit in vitro both murine and human norovirus polymerases, with IC50 values in the low micromolar range. The negatively charged inhibitor, however, displayed poor cell permeability in cell-based experiments. Therefore, we produced different suramin-loaded liposome formulations and evaluated their activities in cell-based assays using murine norovirus cultivated in RAW 264.7 macrophages, as a model for norovirus genus. The results obtained show that suramin, when delivered through liposomes, can effectively inhibit murine norovirus replication.
Palabras clave
Texto completo:
1
Bases de datos:
MEDLINE
Asunto principal:
Antivirales
/
Suramina
/
Sistemas de Liberación de Medicamentos
/
Norovirus
Tipo de estudio:
Prognostic_studies
Límite:
Animals
Idioma:
En
Revista:
ChemMedChem
Asunto de la revista:
FARMACOLOGIA
/
QUIMICA
Año:
2014
Tipo del documento:
Article