Stearylated antimicrobial peptide melittin and its retro isomer for efficient gene transfection.
Bioconjug Chem
; 24(11): 1805-12, 2013 Nov 20.
Article
em En
| MEDLINE
| ID: mdl-24107137
ABSTRACT
A crucial bottleneck in nonviral vector-mediated gene delivery is poor endosomal escape. Here, we constructed novel gene vectors by coupling the stearyl moiety to the N-terminus of the antimicrobial peptide melittin (stearyl-Mel) and its retro isomer (stearyl-rMel) due to their high membrane-lytic activity. As expected, stearyl-Mel showed obvious increases in endosome-lytic activity and transfection efficiency compared with the reported stearyl-TP10. More gratifyingly, the transfection efficiency of stearyl-rMel was around 10-fold greater than that of stearyl-Mel and almost reached the transfection levels of Lipofectamine 2000 due to the enhanced endosome-lytic activity. Furthermore, the stearyl-rMel/p53 plasmid complex exhibited higher p53 expression and antitumor activity than stearyl-Mel, confirming the fact that stearyl-rMel displayed higher transfection efficiency. Taken together, the combination of the stearyl moiety with retro melittin provides a novel framework for the development of excellent nonviral gene vectors.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Ácidos Esteáricos
/
Peptídeos Catiônicos Antimicrobianos
/
Vetores Genéticos
/
Meliteno
/
Antineoplásicos
Limite:
Animals
/
Humans
Idioma:
En
Revista:
Bioconjug Chem
Assunto da revista:
BIOQUIMICA
Ano de publicação:
2013
Tipo de documento:
Article
País de afiliação:
China