Semen Ziziphi Spinosae ZSS a natural medicinal and edible plant with a long history of use contains diverse phytochemicals such as saponins flavonoids alkaloids and fatty acids among which saponins e. g. jujubosides A and B have been most extensively studied. These phytochemicals exhibit a wide range of biological activities including sedative - hypnotic neuroprotective anti-inflammatory antioxidant antiarrhythmic antiplatelet aggregation lipid-lowering antitumor hypoglycemic and metabolic regulatory effects. Bioactive components of ZSS have demonstrated health-promoting functions such as improving sleep alleviating anxiety and depression enhancing learning and memory modulating immunity and combating oxidative stress. Moreover they show significant therapeutic potential across multiple disease models such as neurological disorders e. g. seizures Alzheimer􀆶 s disease Parkinson􀆶 s disease cardiovascular diseases e. g. arrhythmias coronary atherosclerosis infections inflammatory conditions malignancies e. g. lung breast and colorectal cancers and metabolic disorders e. g. diabetes polycystic ovary syndrome . In recent years the application of traditional compound formulas and the development of new products using food-medicine homologous substances have seen rapid progress. This review summarizes the pharmacology and underlying mechanisms of ZSS bioactive components providing a reference for future scientific investigations. Current research and development of these bioactive components remain at a preclinical stage necessitating further fundamental studies and clinical trials to validate their efficacy and safety thereby facilitating in-depth exploration and utilization in healthcare applications.