Diabetes mellitus is one of the prominent metabolic disorders nowadays worldwide and it is characterized by an increase in blood glucose, disturbances in metabolism, and alteration in insulin secretion. Nowadays, phytopharmaceuticals have become a significant treatment mode for diabetes, and bioactive compounds have expanded an increasing amount of consideration to this end for they have multiple biological potentials, including the sustained secretion of insulin and revival of pancreatic islets cells. In this review article, we explained the role of bioactive compounds in the treatment and management of diabetes and their mechanisms in prevention.