Dios-Arg (trifluoroacetate salt)

Dios-Arg is a steroid-based cationic lipid that contains a diosgenin skeleton coupled to an L-arginine head group.¹ It forms a complex with plasmid DNA and decreases plasmid DNA migration in an agarose-gel retardant assay at charge ratio greater than or equal to 4.² Dios-Arg facilitates transfection of plasmid DNA into H1299 and HeLa cells in the presence and absence of fetal bovine serum, an effect that is reversed by the lipid raft-mediated endocytosis inhibitor methyl-β-cyclodextrin and the caveolae-mediated endocytosis inhibitor genistein . It has been used, coupled to 1,2-dioleoyl-sn-glycero-3-PE (DOPE; ), to bind siRNA and plasmid DNA to for cationic lipid nanoparticles (LNPs) for intracellular transport. Dios-Arg is cytotoxic to H1299 and HeLa cells (IC₅₀s = 83.5 and 74.1 μg/ml, respectively).²

1. Sheng, R., Zhuang, X., Wang, Z., et al. Cationic nanoparticles assembled from natural-based steroid lipid for improved intracellular transport of siRNA and pDNA Nanomaterials (Basel) 6(4),(2016).
2. Sheng, R., Wang, Z., Luo, T., et al. Skeleton-controlled pDNA delivery of renewable steroid-based cationic lipids, the endocytosis pathway analysis and intracellular localization Int. J. Mol. Sci. 19(2),(2018).