ArticlePharmaceutical research2010
N1,N12-Diacyl spermines: SAR studies on non-viral lipopolyamine vectors for plasmid DNA and siRNA formulation.
Article in Pharmaceutical research, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 6 papers.
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Who cites it
6 citing papers in PubMed, 19 citations in OpenAlex.
- Cationic Glucan Dendrimer Gel-Mediated Local Delivery of Anti-OC-STAMP-siRNA for Treatment of Pathogenic Bone Resorption.Gels (Basel, Switzerland) · 2024Article
- Covalent functionalization of graphene sheets for plasmid DNA delivery: experimental and theoretical study.RSC advances · 2023Article
- Lipophilic Polyamines as Promising Components of Liposomal Gene Delivery Systems.Pharmaceutics · 2021Review
- Quantitative silencing of EGFP reporter gene by self-assembled siRNA lipoplexes of LinOS and cholesterol.Molecular pharmaceutics · 2012Article
- Self-Assembled Lipoplexes of Short Interfering RNA (siRNA) Using Spermine-Based Fatty Acid Amide Guanidines: Effect on Gene Silencing Efficiency.Pharmaceutics · 2011Article
- Efficient Gene Silencing by Self-Assembled Complexes of siRNA and Symmetrical Fatty Acid Amides of Spermine.Pharmaceutics · 2011Article
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Authors and funding
3 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
purposeTo study the efficiency of novel synthetic N(1),N(12)-diacyl spermines on DNA and siRNA binding, and to compare their transfection efficiency with viability in cell lines.
methodsFive long chain N(1),N(12)-diacyl lipopolyamines: N(1),N(12)-[didecanoyl, dimyristoyl, dimyristoleoyl, distearoyl and dioleoyl]-1,12-diamino-4,9-diazadodecane were synthesized from the naturally occurring polyamine spermine. Their abilities to condense DNA and to form nanoparticles were characterized. Transfection efficiencies were studied in FEK4 primary skin cells and in an immortalized cancer cell line (HtTA), and compared with N(4),N(9)-regioisomers. Also, the abilities of these novel compounds to bind to siRNA-forming nanoparticles were studied using a RiboGreen intercalation assay, and their abilities to deliver fluorescein-tagged siRNA into cells were quantified and compared with TransIT-TKO.
resultsBy incorporating two long aliphatic chains and varying their acylation position, length, and oxidation state in a stepwise manner, we show efficient p and siRNA formulation and delivery to primary skin and cancer cell lines. Although two C14 chains (both saturated or both mono-cis-unsaturated) were efficient transfecting agents, they were highly toxic.
conclusionsN(1),N(12)-Dioleoyl spermine efficiently binds to and delivers pDNA and siRNA with high cell viability even in a primary skin cell line. It is a novel, efficient non-viral vector in the presence of serum.
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