In an organic phase system, an enzymes lipase was used as a catalyst to synthesize galactosylated cholesterol, （5-cholesten-3b-yl）[（4-O-/%u-galactopyranosyl）u-glucitol-6] sebacate （CHS-SE-LA）, which contains gal...In an organic phase system, an enzymes lipase was used as a catalyst to synthesize galactosylated cholesterol, （5-cholesten-3b-yl）[（4-O-/%u-galactopyranosyl）u-glucitol-6] sebacate （CHS-SE-LA）, which contains galactose residues. Its chemical structure was characterized by ESI-MS, and NMR. For HepG2 cells, the cellular fluorescence intensities of liposomes modified with CHS-SE-LA （GAL-FL） were as much as 2.6-fold （p 〈 0.01） control liposomes （FL）. Moreover, the presence of excess galactose significantly inhibited the uptake of GAL-FL suggesting ASGPR mediated uptake. In conclusion, the novel galactosylated ligand CHS-SE-LA was synthesized by lipase-catalyzation and revealed a great potential as drug carrier materials for hepatocyte-selective targeting.展开更多
基金financially supported by the Ph.D.Programs Foundation of Ministry of Education of China(No.20134425110010)the Special Funds from Central Finance of China in Support of Local Colleges and University[No.276(2014)]
文摘In an organic phase system, an enzymes lipase was used as a catalyst to synthesize galactosylated cholesterol, （5-cholesten-3b-yl）[（4-O-/%u-galactopyranosyl）u-glucitol-6] sebacate （CHS-SE-LA）, which contains galactose residues. Its chemical structure was characterized by ESI-MS, and NMR. For HepG2 cells, the cellular fluorescence intensities of liposomes modified with CHS-SE-LA （GAL-FL） were as much as 2.6-fold （p 〈 0.01） control liposomes （FL）. Moreover, the presence of excess galactose significantly inhibited the uptake of GAL-FL suggesting ASGPR mediated uptake. In conclusion, the novel galactosylated ligand CHS-SE-LA was synthesized by lipase-catalyzation and revealed a great potential as drug carrier materials for hepatocyte-selective targeting.
