Cationic facial amphiphiles: a promising class of transfection agents
| Autor: | Babu Suresh D, Leigh Wierichs, Suzanne Walker, Natan A. Kogan, Michael J. Sofia, Karen Bruker, Ramesh Kakarla, Helena R. Axelrod, Clifford B. Longley, Sunita Midha, Daniel Kahne |
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| Rok vydání: | 1996 |
| Předmět: |
Cell Membrane Permeability
Chemical Phenomena medicine.drug_class DNA Recombinant Gene delivery Biology Transfection law.invention Bile Acids and Salts chemistry.chemical_compound Genes Reporter law Cations Chlorocebus aethiops Amphiphile Polyamines medicine Animals Particle Size Cell Line Transformed Multidisciplinary Molecular Structure Bile acid Chemistry Physical Phosphatidylethanolamines Cationic polymerization Quaternary Ammonium Compounds Membrane Biochemistry chemistry Drug Design Recombinant DNA DNA Research Article |
| Zdroj: | Proceedings of the National Academy of Sciences. 93:1585-1590 |
| ISSN: | 1091-6490 0027-8424 |
| Popis: | A promising class of compounds for DNA transfection have been designed by conjugating various polyamines to bile-acid-based amphiphiles. Formulations containing these compounds were tested for their ability to facilitate the uptake of a beta-galactosidase reporter plasmid into COS-7 cells. Dioleoyl phosphatidyl ethanolamine (DOPE) formulations of some of the compounds were several times better than Lipofectin at promoting DNA uptake. The most active compounds contained the most hydrophilic bile acid components. The activity is clearly not related to affinity for DNA: the hydrophobic bile acid conjugates were found to form stable complexes with DNA at lower charge ratios than the hydrophilic conjugates. We suggest that the high activity of the best compounds is related to their facial amphiphilicity, which may confer an ability to destabilize membranes. The success of these unusual cationic transfection agents may inspire the design of even more effective gene delivery agents. |
| Databáze: | OpenAIRE |
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