BACKGROUND The genus Ziziphus (Rhamnaceae) contains 58 accepted species that are extensively used by local people and medicinal practitioners in arid and semi-arid regions for the treatment of diarrhoea, dysentery, cholera, diabetic, hypertension, inflammation, intestinal spasm, liver, malaria and other diseases. Aims of this review: This review article documents and critically assesses, for the first time; up to date categorized information about botanical traits, distribution, traditional uses, phytochemistry, pharmacological and toxicological effects of Ziziphus species. METHODS Information was collected systematically from electronic scientific databases including Google Scholar, Science Direct, PubMed, Web of Science, ACS Publications, Elsevier, SciFinder, Wiley Online Library and CNKI, as well as other literature sources (e.g., books). RESULTS The phytochemical investigations of plants of this genus have led to the identification of about 431 chemical constituents. Cyclopeptide alkaloids and flavonoids are the predominant groups. The crude extracts and isolated compounds exhibit a wide range of in vitro and in vivo pharmacologic effects, including antimicrobial, antitumour, antidiabetic, antidiarrhoeal, anti-inflammatory, antipyretic, antioxidant and hepatoprotective activities. Toxicity studies indicate that Ziziphus species seems to be non-toxic at typical therapeutic doses. CONCLUSIONS Phytochemical and pharmacological studies have demonstrated that Ziziphus species are important medicinal herbs with prominent bioactivities. The focus so far has only been on ten species; however, plants of this genus can potentially yield a wide range of other products with different properties. Meticulous studies on pharmaceutical standardisation, mode of action of the active constituents and toxicity of Ziziphus species are needed to meet the growing demands of the pharmaceutical industry and to exploit their preventive and therapeutic potential fully.