Perilla is a useful pharmaceutical and food product and is empirically consumed by humans. However, its properties have not been evaluated extensively. In this review, we summarize the progress made in research, focusing on the bioactivities of perilla. There are many in vitro and animal studies on the cytostatic activity and antiallergic effects, respectively, of perilla and its constituents. However, its influence on humans remains unclear. Hence, investigating and clarifying the physiological effects of perilla and its constituents on humans are imperative in the future to adhere to the ideals of evidence-based medicine.