Cationic Nucleoside Lipids Based on a 3-Nitropyrrole Universal Base for siRNA Delivery

Cationic nucleoside lipids based on a 3-nitropyrrole universal base were prepared from d-ribose using a straightforward chemical synthesis. Several studies including DLS, TEM, and ethidium bromide (EthBr) assay demonstrated that these amphiphilic molecules form supramolecular organizations of nanometer size in aqueous solutions and are able to bind nucleic acids. siRNA knockdown experiments were performed with these nucleolipids, and we observed protein knockdown activity similar to the siPORT NeoFX positive control. No significant cytotoxicity was found.