Abstract: Gardenia is a kind of medicinal and edible plant resource. Gardenia yellow pigment is an active ingredient isolated from gardenia fruit and belongs to natural water-soluble carotenoids. Studies have shown that gardenia yellow pigment has multiple active functions such as antioxidant, anti-tumor, anti-depressant, anti-inflammatory, and lowering blood sugar and blood pressure. Therefore, it has great development potential in the fields of food and medicine. However, the current research on the pharmacological activity of gardenia yellow pigment is not systematic enough, and it is necessary to analyze and summarize it in detail. This article briefly reviewed the extraction and purification methods of gardenia yellow pigment, such as traditional solvent extraction, ultrasonic extraction, column chromatography, and membrane separation, and so on. On this basis, the pharmacological activity of gardenia yellow pigment was systematically discussed, and its mechanism of treatment of diseases was summarized, in order to provide theoretical guidance for the in-depth research and application of gardenia yellow pigment.