Abstract:Glycosides widely distributed in nature have many pharmacological activities. A lot of drugs belong to glycoside and the sugar chains are closely related to its pharmacological activities. The modification of sugar chains can change the pharmacological activities of glycosides, which provides tremendous glycoside resource for drug development. Because of high efficiency and low pollution, biotransformation by glycosidase is widely used in the preparation of active glycosides. This review summarized recent advances in the preparation of active glycosides by glycosidase transformation, and provided useful references for preparing active glycosides and related research work.