NIE Hua, CHENG Yi, ZHENG Pin-jing, et al. Enzyme-catalyzed Synthesis of Galactose Ligands Targeted Kupffer Cells[J]. Chinese journal of experimental traditional medical formulae, 2013, 19(10): 21-24.
NIE Hua, CHENG Yi, ZHENG Pin-jing, et al. Enzyme-catalyzed Synthesis of Galactose Ligands Targeted Kupffer Cells[J]. Chinese journal of experimental traditional medical formulae, 2013, 19(10): 21-24. DOI: 10.11653/syfj2013100021.
Objective: To synthesize galactose ligand in non-aqueous medium by enzyme-catalyzed method. Method: Structure of the product was confirmed by IR
ESI-MS
1H-NMR and1C-NMR;With conversion rate of substrate as index
effects of enzyme species
reaction medium
the amount of enzyme
molar ratio of substrate
reaction temperature on ligand synthesis was investigated by single factor tests. Result: Characterization by catalytic reaction
C1' bit hydroxyl of galactose occurred esterification
the received products was the target product.Optimized reaction conditions were as followings:tetrahydrofuran(THF)-dimethyl sulfoxide(DMSO)3:1 as reaction medium
Novozym 435 immobilized lipase as catalyst
the amount of enzyme of 600 U·mL-1
molar ratio of galactose to vinyl stearate at 1:4
and reacted at 55 ℃ for 8 h
the conversion rate of galactose reached more than 70%. Conclusion: Enzyme catalysis method could be used for synthesizing ligand of liver targeted liposomes.