Gut microbiota is essential in the metabolism of glycosides in vivo.It is open to metabolism by metabolic enzymes,through deglycosylation,demethylation,dehydroxylation,hydrolysis and other reactions.It is generally believed that glycosides are converted to the corresponding aglycones,secondary glycosides,or other metabolites by the gut microbiota and/or by the metabolic enzymes,and as such absorbed from the small intestine.In this review,we summarize our existing knowledge of the rules underlying the metabolic regulation of gut microbiota in different types of glycosides.The significance of gut microbiota and metabolic enzymes on the glycoside metabolism is also discussed.This paper provides a basis for the understanding of the therapeutic basis and mechanism of glycosides,and development of new drugs by microbial transformation.