A serum-resistant polyamidoamine-based polypeptide dendrimer for gene transfection.

摘要: A serum tolerant polycation gene vector, G(2) PAMAM-PGlu-G(1) PAMAMs (ALA), was designed, synthesized, characterized and evaluated. honeycomb-like molecular structure model for mechanistic explanation of ALA postulated discussed. Designed as a star-shaped polyamidoamine (PAMAM)-based polypeptide dendrimer through peptide bond linkages, with non-toxic low generation PAMAM (G(2)) its central core, polyglutamate (PGlu)s backbone branches G(1) (G(1))s branch grafts peripheral terminals. IR, (1)H NMR demonstrated successful combination. As carrier, exhibited good DNA binding condensation capacity particle size (approximately 87 nm N/P 40, approximately 170 30) ζ-potential 16 mV 30-40), negligible cytotoxicity, exciting significant serum-promoted (serum-containing 56.6%>serum-free 32.7%), cell line dependent (Hek 293 > Bel 7402 Hela), incubation period (38 h 18 12 9 4 2 1 h) sustained (peak transfection appeared at 30 incubation) efficiency. The presence had not only no inhibition on, but also prominent promotion to, the activity ALA. All above features differentiated clearly from most other serum-inhibitive nonviral carriers, proved promising challenging potential efficient vector practical clinical application.