Jujube (Ziziphus jujuba Mill.) originated in China and is very popular for its rich nutrition. Jujube is also a traditional Chinese medicine, with a variety of pharmacological activities. This paper systematically reviews its biologically active components and the mechanism of pharmacological action. Jujube is abundant in many biological components including flavonoids, alkaloids, polysaccharides, triterpenoids, cylic nucleosides, polyphenols, etc. Some studies proved that the active compounds of these bioactive compounds produce obvious anti-inflammatory, anti-oxidative, anti-inflammatory, hypoglycemic, hypolipidemic and anti-cancer effects. Moreover, it improves oxygen insufficiency supply of the heart muscle and improves sleep. The purpose of this review is to provide concrete information about active components and mechanism of pharmacological effects of jujube on the basis of scientific literature. This review provides a foundation for further study of biological activity and its mechanism of jujube. © 2022 International Society for Horticultural Science. All rights reserved.