Diabetes mellitus is globally approaching epidemicproportions and acts as a major cause of a number ofserious health problems diagnosed as diabetic complications. The current oral drugs in the treatment of diabetesand its complications could meet some but not all of thepatients’ needs, and the development of novel drugs with ahypoglycemic effect is urgently required. Silibinin, aflavonolignan traditionally used for the treatment of gallbladderand hepatic diseases, was reported to improveglycemic homeostasis by improving the activity of pancreaticb-cells, increasing insulin sensitivity of liver andmuscle cells, and decreasing lipid deposition in adipocytes. Researches also indicated the effectiveness of silibinin incontrolling several diabetic complications including neuropathy,retinopathy, impaired healing, hepatopathy, cardiomyopathy,nephropathy, and osteoporosis. In thisreview, we summarize the recent anti-diabetes findings ofsilibinin and clarify the underlying pharmacologicalmechanisms, and update the knowledge in understandingthe role of silibinin in control of diabetic complications.