Zanthoxylum bungeanum Maxim (ZBM) belongs to Rutaceae family and has been used as traditional spice and herb for hundreds of years in China. Accumulating evidence suggests a series of pharmacological effects associated with ZBM. This review aims to provide a systematic analysis of the composition, structural properties, pharmacology, and pharmacokinetics of ZBM. Chemical composition analysis of ZBM showed that the main compositions were volatile oil, amide compounds, flavonoids, alkaloids, coumarins, lignans, and phenylpropanoids. Interestingly, ZBM exhibits a wide range of significant biological activities including anti-inflammatory and analgesic effect, anesthetic effect, neuroprotective effect, antiobesity activity, antineoplastic activity, antibacterial, and other activities. However, there is currently no comprehensive review available on ZBM. Therefore, an up-to-date research was accomplished through systematic searching of multiple electronic databases. In a word, this review summarizes the recent researches investigating the chemical composition and biological properties which will provide a better understanding about the health benefits and preclinical assessment of novel application of ZBM.