Hyperglycemia and advanced glycation end products (AGEs) have considerable effects in diabetic patients. So, the recognition of anti-glycation property of compounds has a substantial benefit. Here, desferal, an iron chelator which is one of the most effective drugs in β-thalassemia patients, was chosen to explore its effects on the fructation process of hemoglobin (Hb). The results indicated that desferal had a retardation effect on the functional and structural changes of Hb during fructation. It can prevent the AGE and carbonyl formations and helix depletion during the Hb fructation process. Moreover, desferal can preserve peroxidase and esterase activities of fructated Hb similar as native Hb. Therefore, desferal can be introduced as an anti-glycation drug to prevent the AGE formation.