Aurantii Fructus (called Zhiqiao, ZQ in Chinese), the dried unripe fruit of Citrus aurantium L. or its cultivated variety, is a common traditional edible-medicinal herb in regulating visceral functions for thousands of years. As a widely used ethnomedicine in Asia including China, Japan and Korea, ZQ possesses ideal therapeutic effect on digestive system diseases, and is also used as a condiment in food for regular consumption to benefit health. Amounts of investigations on different aspects have been done for ZQ in the past decades. However, there has no literature systematic comparison on the similarity concerning research achievements of ZQ. Herein, this review comprehensively presents the up-to-date information on botany, ethnopharmacology, phytochemistry, pharmacological activity, clinical use, quality control and toxicology of ZQ to identify their therapeutic potential and directs future research opportunities. So far, about 62 compounds has been isolated and identified from ZQ, in which flavonoids, alkaloids and coumarins would be the main bioactive ingredients for its pharmacological properties, such as regulating gastrointestinal motility, anti-gastric ulcer effect, regulating blood pressure, cardioprotective effects, anti-atherosclerotic activity, anti-vascular damage activity, anti-depression activity, anti-obesity activity, anti-inflammatory, anti-oxidant, anti-tumor, immunomodulatory activity and affecting enzyme activities. Even so, the variety of sources and origins, ZQ has defects in quality control and clinical application.