Fructus Zizyphi refers to the fruits of Zizyphus jujuba plant, and this plant is geographically distributed in East Asia and South Europe. This plant belongs to the family Rhamnaceae, and this plant is a shrub of 10 m in height. This review aimed to focus on chemical constituents, medicinal and pharmacological applications, and the toxicology of Fructus Zizyphi. The major chemical constituents of Fructus Zizyphi are triterpenes and triterpene saponins. Fructus Zizyphi treats insomnia, increases body weight, strengthens body muscle, decreases body temperature, increases urine volume, accelerates women's period, calms and reinforces agents, chases phlegm, treats vision, skin inflammation, hepatitis, respiratory diseases, diabetes, gastric ulcer, and different skin wounds. The pharmacology of Fructus Zizyphi includes experimental pharmacology and clinical pharmacology. Experimental pharmacology includes antiallergenic, anti-inflammatory, analgesic, anti-hyperglycemic, anti-hypercholesterolemic, central nervous system depressant, immune stimulation, and platelet aggregation activities. Fructus Zizyphi ethanol extracts to mice in drinking water daily for 3 months without any effect on animal death, hematology, organ weight, or sperm secretion. Fructus Zizyphi was not mutagenic. Fructus Zizyphi declined gastric adenocarcinoma progress. Fructus Zizyphi without general precautions, drug connections; drug and laboratory test relations; teratogenic or non-teratogenic effects in pregnancy; nursing mothers; or pediatric use. In conclusion, Fructus Zizyphi had antiallergenic, anti-inflammatory, analgesic, anti-hyperglycemic, anti-hypercholesterolemic, central nervous system depressant, immune stimulation, platelet aggregation activities, and without any effect on animals death, hematology, organ weight or sperm secretion.