Synthesis and delivery activity of new cationic cholesteryl glucosides
| Autor: | Marina A. Zenkova, N. G. Morozova, Evgeniya I. Chizhik, Galina A. Serebrennikova, Elena I. Ryabchikova, Mikhail A. Maslov, Dmitriy A. Rapoport |
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| Rok vydání: | 2010 |
| Předmět: |
Chemical Phenomena
Stereochemistry Chemistry Pharmaceutical Alkylation Gene delivery Transfection Biochemistry Cell Line Analytical Chemistry chemistry.chemical_compound Heterocyclic Compounds Amphiphile Animals Cationic liposome RNA Small Interfering Drug Carriers Liposome Base Sequence Chemistry Oligonucleotide Organic Chemistry Cationic polymerization General Medicine Combinatorial chemistry Cholesterol Liposomes Pyridinium Fluorescein-5-isothiocyanate |
| Zdroj: | Carbohydrate Research. 345:2438-2449 |
| ISSN: | 0008-6215 |
| Popis: | Cholesterol amphiphiles containing positively charged groups (pyridinium, N-methylimidazolium, N-methylmorpholinium, and N-methylpiperidinium) linked via β-glucosyl spacer were prepared by alkylation of the corresponding bases with 6-О-mesyl-β- d -cholesteryl glucopyranoside. IC50 values were in the range 20–35 μM for the series of compounds and liposomal formulations with DOPE (1:1) were significantly less toxic. The liposomal formulations provided the accumulation of FITC-labeled oligonucleotide in cells, and the efficiency of this process was comparable to that of Lipofectamine® 2000. Cationic liposomes were able to deliver siRNA into the cells, and the liposomal formulation 7d/DOPE provided the most pronounced down-regulation of EGFP expression both in the presence and in the absence of serum (up to 30%). |
| Databáze: | OpenAIRE |
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