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Delivery of suramin as an antiviral agent through liposomal systems

By Eloise Mastrangelo, Stefania Mazzitelli, Jacopo Fabbri, Jacques Rohayem, Janne Ruokolainen, Antti Nykänen, Mario Milani, Margherita Pezzullo, Claudio Nastruzzi and Martino Bolognesi


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

Topics: antiviral agents, drug delivery, liposomes, norovirus, RNA-dependent RNA polymerase, Animals, Antiviral Agents, Cell Line, Cell Proliferation, Dose-Response Relationship, Drug, Liposomes, Macrophages, Mice, Microbial Sensitivity Tests, Norovirus, Structure-Activity Relationship, Suramin, Virus Replication, Drug Delivery Systems, Pharmacology, Toxicology and Pharmaceutics (all), Organic Chemistry, Molecular Medicine, Medicine (all)
Year: 2014
DOI identifier: 10.1002/cmdc.201300563
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