ArticleMolecular pharmaceutics
Hydrophobic moiety of cationic lipids strongly modulates their transfection activity.
Article in Molecular pharmaceutics. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 papers.
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Who cites it
21 citing papers in PubMed, 95 citations in OpenAlex.
- Triarylphosphonium-conjugated Sn(iv)-porphyrins for antimicrobial photodynamic therapy: impact of substituents on lipophilicity, aggregation, and photoantibacterial activity.RSC medicinal chemistry · 2026Article
- mRNA delivery enabled by metal-organic nanoparticles.Nature communications · 2024Article
- The interplay of quaternary ammonium lipid structure and protein corona on lung-specific mRNA delivery by selective organ targeting (SORT) nanoparticles.Journal of controlled release : official journal of the Controlled Release Society · 2023Article
- Atherosclerosis: The Involvement of Immunity, Cytokines and Cells in Pathogenesis, and Potential Novel Therapeutics.Aging and disease · 2023Review
- Cationic Liposomes as Vectors for Nucleic Acid and Hydrophobic Drug Therapeutics.Pharmaceutics · 2021Review
- Charge-Conversion Strategies for Nucleic Acid Delivery.Advanced functional materials · 2021Article
- Article
- Green Transfection: Cationic Lipid Nanocarrier System Derivatized from Vegetable Fat, Palmstearin Enhances Nucleic Acid Transfections.ACS omega · 2017Article
- Synthesis and evaluation of L-arabinose-based cationic glycolipids as effective vectors for pDNA and siRNA in vitro.PloS one · 2017Article
- Synthesis of linear and cyclic peptide-PEG-lipids for stabilization and targeting of cationic liposome-DNA complexes.Bioorganic & medicinal chemistry letters · 2016Article
- On the possible involvement of bovine serum albumin precursor in lipofection pathway.Journal of biosciences · 2014Article
- Cationic polyene phospholipids as DNA carriers for ocular gene therapy.BioMed research international · 2014Article
- Influence of charge density on bilayer bending rigidity in lipid vesicles: a combined dynamic light scattering and neutron spin-echo study.The European physical journal. E, Soft matter · 2013Article
- Quantitative silencing of EGFP reporter gene by self-assembled siRNA lipoplexes of LinOS and cholesterol.Molecular pharmaceutics · 2012Article
- Cubic phases in membrane lipids.European biophysics journal : EBJ · 2012Review
- Highly efficient cationic ethylphosphatidylcholine siRNA carrier for GFP suppression in modified breast cancer cells.Anticancer research · 2012Article
- Asymmetric 1-alkyl-2-acyl phosphatidylcholine: a helper lipid for enhanced non-viral gene delivery.International journal of pharmaceutics · 2012Article
- Article
- Differentially charged hollow core/shell lipid-polymer-lipid hybrid nanoparticles for small interfering RNA delivery.Angewandte Chemie (International ed. in English) · 2011Article
- Self-Assembled Lipoplexes of Short Interfering RNA (siRNA) Using Spermine-Based Fatty Acid Amide Guanidines: Effect on Gene Silencing Efficiency.Pharmaceutics · 2011Article
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Authors and funding
4 authors at 2 institutions in 2 countries.
Funding
Abstract
Synthetic cationic lipids are widely used components of nonviral gene carriers, and the factors regulating their transfection efficiency are the subject of considerable interest. In view of the important role that electrostatic interactions with the polyanionic nucleic acids play in formation of lipoplexes, a common empirical approach to improving transfection has been the synthesis and testing of amphiphiles with new versions of positively charged polar groups, while much less attention has been given to the role of the hydrophobic lipid moieties. On the basis of data for approximately 20 cationic phosphatidylcholine (PC) derivatives, here we demonstrate that hydrocarbon chain variations of these lipids modulate by over 2 orders of magnitude their transfection efficiency. The observed molecular structure-activity relationship manifests in well-expressed dependences of activity on two important molecular characteristics, chain unsaturation and total number of carbon atoms in the lipid chains, which is representative of the lipid hydrophobic volume and hydrophilic-lipophilic ratio. Transfection increases with decrease of chain length and increase of chain unsaturation. Maximum transfection was found for cationic PCs with monounsaturated 14:1 chains. It is of particular importance that the high-transfection lipids strongly promote cubic phase formation in zwitterionic membrane phosphatidylethanolamine (PE). These remarkable correlations point to an alternative, chain-dependent process in transfection, not related to the electrostatic cationic-anionic lipid interactions.
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Registered trials
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