β-半乳糖苷酶催化氟尿苷高区域选择性半乳糖化。
Highly regioselective galactosylation of floxuridine catalyzed by beta-galactosidase from bovine liver.
机构信息
State Key Laboratory of Pulp and Paper Engineering, College of Light Industry and Food Sciences, South China University of Technology, Guangzhou 510640, China.
出版信息
Biotechnol Lett. 2010 Sep;32(9):1251-4. doi: 10.1007/s10529-010-0302-0. Epub 2010 May 18.
5'-O-beta-D-Galactosyl-floxuridine, a potential novel prodrug, was synthesized with a yield of 75% through beta-galactosidase-catalyzed transgalactosylation. This enzyme displayed absolute regioselectivity toward the 5'-position of floxuridine. For the reaction, the optimal conditions were pH 6.5 at 45 degrees C for 60 h with floxuridine to o-nitrophenyl-beta-D-galactoside at 2:1 (mol/mol). Under these conditions, the initial reaction rate and the maximum yield were 0.28 mM h(-1) and 75%, respectively.
5'-O-β-D-半乳糖基氟尿苷，一种潜在的新型前药，通过β-半乳糖苷酶催化的转半乳糖基化反应以 75%的产率合成。该酶对氟尿苷的 5'-位具有绝对的区域选择性。对于该反应，最佳条件为 pH6.5、45°C 下反应 60 小时，氟尿苷与邻硝基苯-β-D-半乳糖苷的摩尔比为 2:1。在这些条件下，初始反应速率和最大产率分别为 0.28mM h(-1)和 75%。
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