Diabetes mellitus is globally approaching epidemic proportions and acts as a major cause of a number of serious health problems diagnosed as diabetic complications. The current oral drugs in the treatment of diabetes and its complications could meet some but not all of the patients' needs, and the development of novel drugs with a hypoglycemic effect is urgently required. Silibinin, a flavonolignan traditionally used for the treatment of gallbladder and hepatic diseases, was reported to improve glycemic homeostasis by improving the activity of pancreatic β-cells, increasing insulin sensitivity of liver and muscle cells, and decreasing lipid deposition in adipocytes. Researches also indicated the effectiveness of silibinin in controlling several diabetic complications including neuropathy, retinopathy, impaired healing, hepatopathy, cardiomyopathy, nephropathy, and osteoporosis. In this review, we summarize the recent anti-diabetes findings of silibinin and clarify the underlying pharmacological mechanisms, and update the knowledge in understanding the role of silibinin in control of diabetic complications.