As the main active component of Zanthoxylum bungeanum, its volatile oil (ZEO) exhibits diverse pharmacological activities, including insecticidal, antibacterial, anti-inflammatory, and anti-tumor effects. These properties support its traditional functions, such as “expelling worms” and “warming the Middle Jiao to alleviate pain and relieve itching.” However, modern research mainly validates individual components or effects, leaving notable gaps in understanding this complex system. This review integrates research on ZEO, summarizing its composition, influencing factors, and mechanisms of action. By framing the “composition–activity–mechanism–application” continuum, this review analyzes the basis for the holistic, multi-component, multi-target therapeutic model of traditional Chinese medicine (TCM). It clarifies the core TCM principles of pharmacological symbiosis and synergy through formula compatibility. These insights form a theoretical basis for further development and wider application of ZEO in fields such as medicine, food, and daily chemical products.

As the primary active component of Zanthoxylum bungeanum, its volatile oil (ZEO) exhibits diverse pharmacological activities, including insecticidal, antibacterial, anti-inflammatory, and anti-tumor effects. These properties provide a scientific foundation for its traditional functions, such as "expelling worms" and "warming the Middle Jiao to alleviate pain and relieve itching."However, contemporary research predominantly focuses on validating individual active constituents or specific pharmacological effects, highlighting substantial gaps in elucidating this complex chemical system. This review systematically synthesizes existing research on ZEO and delineates the chemical composition, influencing factors, and mechanisms of action of ZEO. Thus, by integrating the "composition-activity-mechanism-application" continuum, this review provides an in-depth analysis of the modern scientific essence of the holistic therapeutic model of traditional Chinese medicine (TCM) — multi-component and multi-target actions. This precisely expounds the theoretical core of TCM concepts of pharmacological symbiosis and synergistic effects via formula compatibility. Together, these insights establish a robust theoretical foundation for the further development and broader application of ZEO in fields such as medicine, food, and daily chemical products.