Stearyl-(homoarginine)8 is a cell-penetrating peptide conjugated to stearic acid that has been used in the generation of liposomes for plasmid DNA or siRNA delivery in vitro.1,2 Liposomes containing stearyl-(homoarginine)8 and in complex with plasmid DNA enter NIH3T3 cells via the endocytosis pathway.1 Liposomes containing a high density, but not a low density, of stearyl-(homoarginine)8 and encapsulating plasmid DNA increase plasmid DNA expression without being degraded by lysosomes in NIH3T3 cells.2 Stearyl-(homoarginine)8-containing liposomes encapsulating siRNA targeting the mRNA encoding GAPDH decrease GAPDH levels in primary human aortic smooth muscle cells.3
References:
[1]. Khalil, I.A., Futaki, S., Niwa, M., et al.Mechanism of improved gene transfer by the N-terminal stearylation of octaarginine: Enhanced cellular association by hydrophobic core formationGene Ther.11(7)636-644(2004).
[2]. Khalil, I.A., Kogure, K., Futaki, S., et al.High density of octaarginine stimulates macropinocytosis leading to efficient intracellular trafficking for gene expressionJ. Biol. Chem.281(6)3544-3551(2006).
[3]. Fisher, R.K., Mattern-Schain, S.I., Best, M.D., et al.Improving the efficacy of liposome-mediated vascular gene therapy via lipid surface modificationsJ. Surg. Res.219136-144(2017).