摘要
天然产物具有广泛的生物活性,是新药发现的重要来源。然而很多天然产物活性不够强、溶解性差、生物利用度低,需要通过结构修饰提高成药性。糖基化是一种重要的结构修饰反应。微生物催化具有选择性强、反应条件温和、环境友好等特点。对微生物全细胞及重组表达酶催化的天然产物糖基化反应的最新进展进行综述。
As an important source of new drugs, natural products exhibit extensive biological activities. However, most of them suffer from less potent activity, poor water solubility, and low bioavailability. Consequently, structural modification is needed to improve their druggability, Glycosylation is an important reaction for structural modification. Microbial transformation has the advantages of high selectivity, mild reaction conditions, and environmental friendliness. The recent progress in the field of glycosylation of natural products catalyzed by both whole cells and recombinant enzymes of microorganisms were reviewed.
作者
刘爽
李凯
王双
乔雪
叶敏
LIU Shuang;LI Kai;WANG Shuang;QIAO Xue;YE Min(State Key Laboratory of Natural and Biomimetie Drugs School of Pharmaeeutical Sciences, Peking University Beijing 100191. China)
出处
《药学进展》
CAS
2018年第1期14-20,共7页
Progress in Pharmaceutical Sciences
关键词
天然产物
微生物
糖基转移酶
糖苷酶
糖基化
natural product
microorganism
glycosyltransferase
glycosidase
glycosylation
