OBJECTIVE The objective of this study was to evaluate the therapeutic effects of balanitoside in diabetic rats. METHODS Twenty-five rats were divided into five groups. Rats in groups 2 to 5 were treated with streptozotocin to induce hyperglycemia. In addition, rats in groups 1 and 2 received 1 mL of distilled water, whereas those in groups 3, 4, and 5 received 10 and 20 mg/kg balanitoside and 6 U/kg insulin, respectively, for 14 days. All rats were sacrificed on day 15, blood samples were collected, and serum levels of alkaline phosphatase (ALP), alanine aminotransferase (ALT), and aspartate aminotransferase (AST) were measured. The liver was processed for examination under a light microscope. RESULTS The results showed a significant decrease in liver protein concentrations in diabetic control rats, compared to those in the normal control rats and rats treated with 10 mg/kg balanitoside (p < 0.05). There was no significant difference in ALP levels among all groups. However, a significant increase in ALT and AST levels was observed in the diabetic control rats, compared to those in the normal control rats (p < 0.05). Photomicrographs of the liver of the diabetic control rats showed fat and glycogen droplets, vacuolated nuclei, and loss of cellular boundaries, whereas those of the rats treated with balanitoside or insulin showed a small amount of microvesicular fat droplets and slight infiltration of lymphocytes. CONCLUSIONS The findings of this study suggest the therapeutic effects of balanitoside in the liver of diabetic rats.