Ethnopharmacological relevance: Perilla frutescens (Linnaeus) Britton, Mem. Torrey Bot. Club 5: 277. 1894., is famous as a worldwide plant with multiple medical parts, including leaves, stems, fruits, etc. Perillae Fructus, the desiccative ripe fruit of P. frutescens, is locally called Zisuzi in Chinese Pharmacopoeia. It is a popularly used herb for relieving cough and asthma, dissipating phlegm and treating constipation in some Asian countries, such as China, Japan, India, South Korea, etc. Various chemical compounds were isolated and identified from Perillae Fructus.

The aim of the review: This review aims to summarize the botany, ethnopharmacological applications, phytochemistry, pharmacology, toxicity and quality control of Perillae Fructus to provide scientific evidence for development and utilization Perillae Fructus.

Materials and methods: Relevant information about Perillae Fructus was collected from ScienceDirect, PubMed, Web of science, CNKI, WanFang data, ancient classics and clinical reports. Some electronic databases were also retrieved.

Results: Perillae Fructus was exerted to treat cough and asthma in traditional application. It also had the effect on moistening intestine to relieve constipation for tremendous lipid substances. Up to now, 193 compounds have been isolated and identified from Perillae Fructus, mainly including fatty acids, flavonoids, phenolic acids, phytosterols, triterpenoids and volatile oils. As for its pharmacological activities, prevalent traditional applications of Perillae Fructus have been supported by modern pharmacological experiments in vivo or in vitro, such as anti-inflammatory and anti-oxidant effects. Besides, Perillae Fructus also has hypolipidemic, anti-tumor, antibacterial effects, etc. This review will provide a scientific basis for further studies and rational applications of Perillae Fructus in the future.

Conclusions: According to its traditional applications, phytochemicals and pharmacological activities, Perillae Fructus was regarded as a valuable herb for application in medicine and food fields. Although some ingredients have been confirmed to have multiple pharmacological activities, their mechanisms of action are still unclear. Further studies on the material basis and mechanism of action are clearly warranted.