Synthesis of a novel multivalent galactoside with high hepatocyte targeting for gene delivery

摘要

A novel bifunctional glycolipid which carried a cluster of thiogalactosides as the hepatocyte targeting ligand for gene delivery was prepared. Hexa-antennary alcohol 1 was used as the core scaffold to attach a cholesterol molecule by a poly(ethylene glycol) chain, while its remaining branches were linked with five acetylgalactosides, which would be deacetylated later to produce penta- antennary galactoside. Liposome containing the galactoside showed high affinity and transfection activity in hepatoma cells HepG2.