Abstract: Tectochrysin is an important active ingredient in plants. It belonging to flavonoids, and it has multiple bioactivities, such as anti-tumor, anti-oxidant, anti-inflammatory, anti-diarrheal, anti-bacterial, anti-allelopathy, trypanocidal and other effects. And the anti-tumor effects are deeply studied and found its effect on different tumor cells with different mechanisms. In recent years, newly discovered pharmacological activities such as anti-allergy, anti-osteoporosis, neuroprotective and other pharmacological activities gradually emerged. In addition, it can undergo demethoxylation leading to produce chrysin according to the metabolic process study, but studies on pharmacokinetics remain poor. This review summarizes research progress of the bioactivities and pharmacokinetics of tectochrysin for the first time in order to provide a reference for researchers to understand the research progress of tectochrysin.