Synthesis and evaluation of vitamin D-based cationic lipids for gene delivery in vitro.
A new panel of steroidal cationic lipids has been synthesized for gene delivery. Using commercially available vitamin D2 (calciferol) or vitamin D3 (cholecalciferol) as hydrophobic motifs and a variety of cationic head groups as binding sites for negatively charged phosphate groups in DNA, we demonstrated that the transfection activity of the synthetic vitamin D-based cationic lipids 1d, 2d formulated with dioleoylphosphatidylethanolamine (DOPE) as a co-lipid is comparable to that of 3-(-[N-N',N'-dimethylaminoethane)carbamoyl]cholesterol (DC-Chol). These synthetic lipids are effective in transfecting a variety of cell lines. These results suggest that vitamin D-based cationic lipids are useful transfection reagents for in vitro gene transfer studies.
Ren
T
T
Department of Pharmaceutical Sciences, School of Pharmacy, University of Pittsburgh, PA 15261, USA.
Zhang
G
G
Liu
F
F
Liu
D
D
D016475:3T3 Cells; D000818:Animals; D002412:Cations; D002460:Cell Line; D002762:Cholecalciferol / Q000737:chemistry; D004872:Ergocalciferols / Q000737:chemistry; D015870:Gene Expression / Q000187:drug effects; D018390:Gene Targeting; D006367:HeLa Cells; D006801:Humans; D008055:Lipids / Q000138:chemical synthesis / Q000737:chemistry*; D051379:Mice; D014162:Transfection; D014407:Tumor Cells, Cultured; D014807:Vitamin D / Q000138:chemical synthesis / Q000737:chemistry*
D002412:Cations; D004872:Ergocalciferols; D008055:Lipids; D014807:Vitamin D; D002762:Cholecalciferol