Objective: To examine the hepatoprotective effects of gedunin in streptozotocin (STZ)-induced diabetic rats. Methods: Rats were divided into 4 groups: control, STZ, gedunin, and STZ+gedunin. Biochemical parameters for liver function and liver histology were studied. The molecular interaction of gedunin with the liver glucose transporters GLUT2 and SGLT1 was examined using AutoDock Vina. Results: Gedunin attenuated STZ-induced increase in the levels of aspartate transaminase, alanine transaminase, alkaline phosphatase, lactate dehydrogenase and gamma-glutamyl transferase in the serum and liver tissue, reduced lipid peroxidation, and enhanced antioxidant activity. Histopathological studies showed considerable restoration of liver architecture in gedunin-treated diabetic rats. In silico studies revealed stable binding of gedunin with GLUT2 and SGLT1. Conclusions: Gedunin exerts hepatoprotective effects in STZ-induced diabetic rats by reducing liver enzymatic activities and oxidative stress. Further studies are warranted to verify the mechanism of its hepatoprotective action.