Enzyme-catalyzed Synthesis of Galactose Ligands Targeted Kupffer Cells

NIE Hua; CHENG Yi; ZHENG Pin-jing; ZHAO Ju-xiang; WU Qiong

doi:10.11653/syfj2013100021

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Enzyme-catalyzed Synthesis of Galactose Ligands Targeted Kupffer Cells

更新时间：2024-01-04

- Enzyme-catalyzed Synthesis of Galactose Ligands Targeted Kupffer Cells
- Chinese Journal of Experimental Traditional Medical Formulae Vol. 19, Issue 10, Pages: 21-24(2013)
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- DOI：10.11653/syfj2013100021
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- Published：2013
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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：

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.

摘要

目的: 采用酶催化法在非水相介质中合成半乳糖配体。方法: 通过IR

质谱

核磁共振(1H-NMR

1C-NMR)对产物结构进行表征;以底物转化率为指标

采用单因素试验考察酶种类、反应介质、酶加入量、底物摩尔比、反应温度等对配体合成的影响。结果: 通过表征分析显示经酶的催化反应

半乳糖C1'位的羟基发生了酯化反应

所得产物为目标产物。优选的反应条件为反应介质四氢呋喃(THF)-二甲基亚砜(DMSO)(3:1)

Novozym 435 固定化脂肪酶为催化剂

酶加入量600 U·mL-1

半乳糖-硬脂酸乙烯酯的摩尔比1:4

于55 ℃反应8 h

半乳糖的转化率达>0%。结论: 酶促催化法可用于合成肝靶向脂质体配体。

Abstract

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.

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