Introduction: Kola nitida (KN) is a tropical plant belonging to the familyMalvaceae. Aim: To explore the metabolic profile and health benefits of KN leaf. Methods: The active metabolites were employed by HPLC-UV-MS/MS. The hepatoprotective of the hydromethanolic KN leaf extract (KNLE) was tested against CCl4-induced hepatotoxicity in rats. Besides, KNLE antihyperglycemic and antihyperlipidemic properties were studied in streptozotocin (STZ)-induced diabetic rats. Results: Eight phenolics were detected quantitatively. KNLE (100 mg/kg) significantly reduced liver index, serum ALT, AST, ALP, total bilirubin, ACP, β-GAL, and β-NAG relative to CCL4. The biochemical results were corroborated with the liver histopathology. Diabetic rats pretreated with KNLE (200 mg/kg) significantly lowered serum glucose, HbA1c, triglyceride, total cholesterol, and very-low-density lipoproteins compared to diabetic rats. Conclusion: KNLE protected the liver against CCl4 induced hepatotoxicity compared to silymarin. Besides, KNLE exerted antihyperglycemic and antihyperlipidemic properties in diabetic rats compared to glibenclamide.