Distance of Hydroxyl Functionality from the Quaternized Center Influence DNA Binding and in Vitro Gene Delivery Efficacies of Cationic Lipids with Hydroxyalkyl Headgroups
| Autor: | Sunkara Sakunthala Madhavendra, Mukthavaram Rajesh, Arabinda Chaudhuri, Yenugonda Venkata Mahidhar |
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| Rok vydání: | 2004 |
| Předmět: |
Gene delivery
Transfection Cell Line Structure-Activity Relationship Cricetulus Microscopy Electron Transmission Genes Reporter Cations Cricetinae Chlorocebus aethiops Drug Discovery Animals Deoxyribonuclease I Humans Reporter gene Liposome Histocytochemistry Chemistry Chinese hamster ovary cell Genetic transfer Gene Transfer Techniques Cationic polymerization DNA beta-Galactosidase Lipids In vitro Quaternary Ammonium Compounds Biochemistry Molecular Medicine Drug carrier |
| Zdroj: | Journal of Medicinal Chemistry. 47:5721-5728 |
| ISSN: | 1520-4804 0022-2623 |
| DOI: | 10.1021/jm049656j |
| Popis: | In vitro gene delivery efficacies of cationic amphiphiles 1-7 (Scheme 1) were measured by both the reporter gene expression assays in CHO, COS-1, HepG2, and MCF7 cells and by the whole cell histochemical X-gal staining of representative Chinese hamster ovary cells. Our results demonstrated that in vitro gene delivery efficiencies of cationic lipids with hydroxyalkyl headgroups are adversely affected by increased covalent distances between the hydroxyl functionality and the cationic centers. Findings in the DNase I protection experiments and transmission electron microscopic study support the notion that such compromised gene delivery efficacies may originate from poor lipid-DNA binding interactions and significantly increased lipoplex nanosizes. |
| Databáze: | OpenAIRE |
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