To investigate the acute toxicity and antidiabetic potentials of various extracts of the leaves of Ficus sur Forssk on alloxan-induced diabetic rats. Powdered leaves were successively extracted with n-hexane, chloroform and 70% ethanol for three consecutive days respectively and the obtained extracts were assessed for phytochemicals, acute toxicity and antidiabetic activity on albino rats. The acute toxicity was assessed by Lorke’s method. Diabetes was achieved by intraperitoneal injection of alloxan monohydrate (120mg/kg). Blood glucose was determined daily for seven days using a glucometer. On the seventh day of treatment, blood samples were obtained and the serum triglycerides (TG), total cholesterol (TC), glycosylated heamoglobin (GH), urea and high density lipoprotein (HDL) were determined. The active N-hexane fraction was further fractionated by column chromatography packed with silica gel G (60-80mesh) eluting with gradient mixture of n-hexane, dichloromethane and ethanol. The phytochemical screening revealed the presence of terpenoids, tannins, flavonoid and carbohydrates. The lethal dose (LD50) was recorded at 2154mg/kg in the toxicity study. The n-hexane extract showed the highest significant (p<0.05) reduction of 77.7% in blood glucose which was comparable to Glibenclamide (78.3%). Further fractionation yielded five fractions (F1-F5) in which fraction F4 and F5 were the most active with 54.7 and 55.9% reduction of blood glucose. The lipid profile of fraction F4 also exhibited decrease in TG, TC, GH, Urea and increase in HDL. This study reports the LD50 of F. sur to be2154 mg/kg and further confirms its ethnobotanical use of in the treatment of diabetes mellitus and its potential in preventing cardiovascular diseases