Synthesis and transfection activity of novel galactosylated polycationic lipid

• Published in: Bioorganic & medicinal chemistry letters Vol. 21; no. 10; pp. 2937 - 2940
• Main Authors: Maslov, M.A., Medvedeva, D.A., Rapoport, D.A., Serikov, R.N., Morozova, N.G., Serebrennikova, G.A., Vlassov, V.V., Zenkova, М.A.
• Format: Journal Article
• Language: English
• Published: England Elsevier Ltd 15-05-2011
• Subjects: Aggregation behavior; Animals; Cationic lipids; Cell Line; Cell Survival - drug effects; Compaction; Cricetinae; DNA; EGFP expression; Flow Cytometry; Galactose; Galactose - chemistry; gene expression; Gene silencing; Gene Transfer Techniques; Humans; Lipids; Lipids - chemical synthesis; Lipids - chemistry; Lipids - toxicity; Liposomes - chemistry; Mammalian cells; mammals; Microscopy, Atomic Force; Molecular Structure; nucleic acids; Oligonucleotides; Plasmids; Polyamines - chemistry; siRNA; small interfering RNA; Spermine; toxicity; Transfection; Transfection efficiency; Transgenes; siRNA; EGFP expression; Transfection efficiency; Cationic lipids; Oligonucleotides
• ISSN: 0960-894X; 1464-3405
• DOI: 10.1016/j.bmcl.2011.03.056

In this study, we synthesized a new galactosylated cationic lipid and investigated its biological activity. The structure of lipid combines both spermine residue for DNA compaction and galactose moiety for the improvement of aggregation behavior of lipoplexes. Lipid was low toxic for different mammalian cells, and was able both to compact plasmid DNA and to mediate cellular accumulation of various nucleic acids (ODN, pDNA and siRNA) exhibiting biological activity (transgene expression, gene silencing).