Abstract:Acarbose, an α-glucosidase inhibitor, regulates the postprandial blood glucose level by competitively inhibiting the activities of sucrase, maltase, and glucamylase in the intestine, serving as an ideal drug ingredient with blood glucose-lowering activity. Acarbose is mainly produced by the fermentation of Actinoplanes sp., and its biosynthetic pathway is mainly divided into four modules: C7-cyclitol synthesis, deoxyglucosamine synthesis, maltose integration, and extracellular transport of acarbose and its homologues (carbophore cycle). This paper reviewed the advances in the research fields mentioned above, aiming to provide ideas for further exploring the biosynthetic pathways of acarbose, catalytic mechanisms of related enzymes, and molecular modification of fermentation strains.