A plant with important ethnomedical applications, Oxystelma esculentum, has garnered interest due to its numerous therapeutic benefits. This study examines its phytochemical composition, which includes alkaloids, flavonoids, glycosides, and saponins. These compounds support its anti-inflammatory, anticancer, antioxidant, and antibacterial properties. Potential health benefits, including immune regulation, wound healing, and digestive health, are associated with the plant's bioactive constituents. This study discusses the pharmacological uses of Oxystelma esculentum along with scientific data supporting its historical use in treating a variety of diseases. New therapeutic opportunities for contemporary medicine may arise from further investigation of its bioactive constituents and modes of action.