Brazdova Barbora, Tan Nikmala S, Samoshina Nataliya M, Samoshin Vyacheslav V
Department of Chemistry, University of the Pacific, Stockton, CA 95211, USA.
Carbohydr Res. 2009 Feb 17;344(3):311-21. doi: 10.1016/j.carres.2008.11.009. Epub 2008 Nov 25.
Glycosidases are very important enzymes involved in a variety of biochemical processes with a special importance to biotechnology, food industry, and pharmacology. Novel structurally simple inhibitors derived from cyclohexane-1,2-dicarboxylic acids were synthesized and tested against several fungal glycosidases from Aspergillus oryzae and Penicilliumcanescens. The presence of at least two carboxylic groups and one hydroxy group was essential for efficient inhibition. Significant selective inhibition was observed for alpha- and beta-glucosidases, the magnitude of which depended on the configuration of substituents; inhibition increased for beta-glucosidase by lengthening the alkoxy group of the inhibitor.
糖苷酶是非常重要的酶，参与多种生物化学过程，对生物技术、食品工业和药理学具有特殊重要性。合成了源自环己烷-1,2-二羧酸的新型结构简单的抑制剂，并针对米曲霉和灰绿青霉的几种真菌糖苷酶进行了测试。至少两个羧基和一个羟基的存在对于有效抑制至关重要。观察到对α-和β-葡萄糖苷酶有显著的选择性抑制，其程度取决于取代基的构型；通过延长抑制剂的烷氧基，β-葡萄糖苷酶的抑制作用增强。
