酶促小分子化合物β-糖基化研究进展

Research progress on enzymaticβ-glycosylation of small molecule compounds

糖基化是自然界增加小分子化合物功能多样性的有效方法,并能显著改善化合物的水溶性、稳定性等物理化学性质,其中β-糖苷类化合物广泛存在于自然界中,具有重要的生物活性。由于缺乏高效β-糖基化修饰的酶催化剂,许多β-异构体糖苷的生产主要采用天然产物的分离提取和化学合成等方法。文章主要总结了可实现小分子化合物β-糖基化的酶的特性、催化机制和底物特异性等,并概述了以廉价寡糖为供体的β-糖基化酶的定向进化,为小分子化合物的β-糖基化研究提供参考。

Glycosylation is an effective way to increase the functional diversity of small molecule compounds in nature,and can significantly improve the water solubility,stability and other physical and chemical properties of compounds.Among them,β-glycoside compounds are widely present in nature and have important biological activities.However,due to the low efficiency ofβ-anomer-selective glycosylation catalyzed by enzymes,the production of manyβ-isomer glycosides currently used to be dependent upon methods such as separation and extraction of natural products and chemical synthesis.This review focuses on the enzymatic synthesis ofβ-glycoside.The characteristics,catalytic mechanism and substrate specificity of enzymes,which can catalyzeβ-glycosylation of small molecule compounds,were summarized.Directed evolution of enzymes with cheap oligosaccharides as glycosyl donor for enhancingβ-glycosylation function was also discussed.These knowledges would be helpful for researches about enzymaticβ-glycosylation of small molecule compounds.