Design, synthesis and in vitro evaluation of d-glucose-based cationic glycolipids for gene delivery.
Org Biomol Chem
; 14(5): 1611-22, 2016 Feb 07.
Article
en En
| MEDLINE
| ID: mdl-26670704
ABSTRACT
A cationic lipid consists of a hydrophilic headgroup, backbone and hydrophobic tails which have an immense influence on the transfection efficiency of the lipid. In this paper, two novel series of cationic cyclic glycolipids with a quaternary ammonium headgroup and different-length hydrophobic tails (dodecyl, tetradecyl, hexadecyl) have been designed and synthesized for gene delivery. One contains lipids 1-3 with two hydrophobic alkyl chains linked to the glucose ring directly via an ether link. The other contains lipids 4-6 with two hydrophobic chains on the positively charged nitrogen atoms. All of the lipids were characterized for their ability to bind to DNA, size, ζ-potential, and toxicity. Atomic force microscopy showed that the lipids and DNA-lipid complexes were sphere-like forms. The lipids were used to transfer enhanced green fluorescent protein (EGFP-C3) to HEK293 cells without a helper lipid, the results indicated that lipids 4-6 have better transfection efficiency, in particular lipids 5-6 have similar or better efficiency, compared with the commercial transfection reagent lipofectamine 2000.
Texto completo:
1
Banco de datos:
MEDLINE
Asunto principal:
Glucolípidos
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Transfección
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Diseño de Fármacos
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Glucosa
Límite:
Humans
Idioma:
En
Año:
2016
Tipo del documento:
Article