Ziziphi Spinosae Semen (ZS, the seeds of Ziziphus jujuba Mill. var. spinosa (Bunge) Hu ex H. F. Chou) is used as a traditional Chinese medicine referred to as Suan zao ren (). This paper aims to provide a systematic review of its traditional uses and its botanical, phytochemical, pharmacological, pharmacokinetic, and toxicological characteristics. The future development and research prospects for ZS have also been discussed in detail. To date, over 150 compounds have been identified in this plant, including terpenoids, alkaloids, flavonoids, fatty acids, volatile oils, polysaccharides, and others. Both extracts and purified compounds have excellent biological activities, especially sedative and hypnotic effects. Other effects include ameliorating effect of learning and memory, anti-inflammation, antioxidation, blood pressure and lipid lowering, antiaging, and antitumor effects. Thus, this traditional Chinese medicine can be used to treat many diseases such as insomnia, forgetfulness, headaches, and dizziness. Although many of the traditional uses of ZS are well established, the relationship between structure and function still needs to be further studied. In order to better pave the way for research and the establishment of quality control standards for ZS, it will be very important to elucidate its pharmacological mechanisms of action and explore new clinical effects. © 2020 Su-Rong He et al.