Lipase-catalyzed synthesis of novel galactosylated cholesterol |
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Authors: | Hua Nie Yi Cheng Pin-Jing Zheng Li-Hua Luo Sheng-Yuan Zhang |
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Institution: | a College of Traditional Chinese Medicine, Guangzhou University of Chinese Medicine, Guangzhou 510006, China;
b Medical College of Jiaying University, Meizhou 514031, China |
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Abstract: | In an organic phase system, an enzymes lipase was used as a catalyst to synthesize galactosylated cholesterol, (5-cholesten-3b-yl)(4-O-β-D-galactopyranosyl)D-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. |
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Keywords: | Cholesterol derivative Liposomes Asialoglycoprotein receptor Lipase-catalyzed |
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