BACKGROUND Zanthoxylum nitidum (Roxb.) DC. (Z. nitidum), which is known in China as Liang-Mian-Zhen, is mainly distributed in southern China and is widely used in traditional Chinese medicine. It is traditionally used for treating stomach ache, toothache, rheumatic arthralgia, traumatic injury and venomous snake bites. Additional medical applications include the treatment of inflammations, various types of cancer, bacterial and viral infections, gastric and oral ulcers and liver damage. OBJECTIVE This paper aims to offer up-to-date information on the botany, traditional uses, phytochemistry, pharmacology and toxicity of Z. nitidum. This review also discussed the perspectives for possible future research on Z. nitidum. METHODS A comprehensive review was carried out on studies about Z. nitidum conducted in the past 60 years by using different resources, including Flora of China, Pharmacopoeia of the People's Republic of China and academic databases. RESULTS At present, more than 150 chemical constituents have been separated and identified from Z. nitidum, most of which include alkaloids. Biological activities, including anti-inflammation, analgesia, haemostasis, anticancer and antibacterial, were determined via in vitro and in vivo studies. The variations in the efficacy of Z. nitidum can be attributed to the biological activities of its natural products, especially alkaloids. Toxicity studies on Z. nitidum are relatively few, thus requiring further study. CONCLUSIONS This article generalises the current research achievements related to Z. nitidum, which is an important medicinal material in China. Some traditional uses of Z. nitidum have been assessed by pharmacological studies. Unresolved problems remain, including molecular mechanisms underlying biological activities, pharmacokinetics, toxicology and therapeutic effect, which are still being studied and explored before Z. nitidum can be integrated into clinical medicine.