The plant Aegle marmelos belongs to the family of Rutaceae. From the leaves of A. marmelos an alkaloidal-amide, Aegeline 2, was isolated and found to have antihyperglycemic activity as evidenced by lowering the blood glucose levels by 12.9% and 16.9% at 5 and 24 h, respectively, in sucrose challenged streptozotocin induced diabetic rats (STZ-S) model at the dose of 100 mg/kg body weight. Aegeline 2 has also significantly decreased the plasma triglyceride (Tg) levels by 55% (P < 0.001), total cholesterol (TC) by 24% (P < 0.05), and free fatty acids (FFA) by 24%, accompanied with increase in HDL-C by 28% and HDL-C/TC ratio by 66% in dyslipidemic hamster model at the dose of 50 mg/kg body weight. The reasonable mapping of compound 2 to validated pharmacophoric hypothesis and 3D QSAR model with an estimated activity (283 nM) suggest that the compound 2 might be a β3-AR agonist.