Key result
Suramin delivered through liposomes effectively inhibited murine norovirus replication in cell-based assays, overcoming the poor cell permeability of the free drug.
Liposomal delivery of suramin overcomes its poor cell permeability, enabling effective inhibition of norovirus replication in vitro.
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Liposomal suramin may enable norovirus inhibition; leaves open translation to in vivo models or clinical use.
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.
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Mastrangelo et al. (2014) studied Norovirus infection. Suramin-loaded liposomes was evaluated on Inhibition of murine norovirus replication. Suramin delivered through liposomes effectively inhibited murine norovirus replication in cell-based assays, overcoming the poor cell permeability of the free drug.
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