Obesity, modifiable and an avertable medical condition, has become a global threat due to rapid modernization and industrialization. Swift growth in modernization not only eases the day-to-day life, it also mandates sedentary lifestyle, which leads to various noncommunicable diseases. At present one in eight people in global population are obese, and these booming obese individuals are prone to various other micro- and macrovascular diseases such hyperglycemia, myocardial infraction, hypertension, stroke, and so forth. Ample research had unveiled an intricate association perceived between obesity and Type 2 diabetes mellitus pathogenesis. Although the intake of anti-obesity drugs along with anti-diabetic drugs had effectively regulated the hyperglycemic conditions in diabetic patients, it causes various side effects on long-term usage. Coumarins are phytochemicals that have demonstrated pharmacological properties including anti-inflammatory, antioxidant, anti-tumor, and so forth. In this analysis, we assessed anti-obesity and anti-diabetic potency of aesculetin, a courmarin derivative. The rats were induced obesity with high-fat diet and subjected to streptozotocin infusion to induce hyperglycemia. Obese diabetic induced rats were treated with aesculetin and assessed for its anti-diabetic effect. BMI were assessed in the rats to analyze the anti-obesity effect of aesculetin. Diabetic profile test and lipid profile test were performed to evaluate the anti-diabetic effect of aesculetin. Ameliorative effect of aesculetin in obese rats during hyperglycemic conditions was assessed with renal profile test, hepatic function biomarkers, and by histopathological analysis of cardiac tissue. The anti-inflammatory and antioxidant property were also assessed to determine the mechanism of action of aesculetin. To confirm the anti-obesity potency of aesculetin, adipokines levels were estimated. Aesculetin eminently decreased the BMI, HbA1c, cholesterol levels, and intensified secretion of insulin in obese diabetic rats. It also regulated the renal, hepatic functional markers and prevented cardiac tissue injury in obese diabetic rats. It regulated the adipokines, increased antioxidants, and decreased level of proinflammatory cytokines, thereby prevented obesity-induced hyperglycemic effects in rats. To conclude, our findings had confirmed the supplementary intake of aesculetin prevents obesity-induced hyperglycemic disorder in rats.© 2025 International Union of Biochemistry and Molecular Biology, Inc.