Perilla frutescens (L.) Britt., a worldwide distributed plant, is an important economic crop and with a long cultivation history in China as well as some other countries in Asia. Except for the edible applications, the plant of P. frutescens is also traditionally used as a medicinal herb in China for thousands years. The leaves, seeds and stems of P. frutescens are recommended by the Chinese Pharmacopeia as three medicinal materials for various therapeutic applications. In the past decades, amount investigations have been done about different aspects for P. frutescens. However, no literature review about these works has been compiled. This review aims to present the findings of research conducted up-to-date (2015) on the traditional use, phytochemicals, pharmacological activities and toxicities of P. frutescens to provide scientific evidence for well-understanding and future research of P. frutescens. It was found that more than 100 compounds have been reported for P. frutescens and most of them are contributed to its medical benefits such as anti-allergic, anti-inflammatory, anti-oxidant, anticancer, anti-microbial, anti-depressive and anti-cough effects. Toxicology studies have been conducted to evaluate the safety of P. frutescens to provide information on their dosages and usages.