Objective: To analyze and summarize the latest research progress regarding pharmacological and toxicological effects of bavachin. Methods: Through retrieval of all bavachin-related reports on pubmed, CNKI, Wanfang database and other databases, the pharmacologic and toxicological effects of bavachin were sorted out and concluded accordingly. Results: The study showed that bavachin had a wide range of pharmacological activities, including estrogen-like, anti-inflammatory, anti-tumor, immunoregulatory, anti-diabetes and its complications effects. The toxicological effects of bavachin were mainly manifested in three aspects: hepatotoxicity, reproductive toxicity and nephrotoxicity. Conclusions: Bavachin has the characteristics of multi-function and multi-target monomer similar to traditional Chinese medicine, and broad application prospects, but also has certain toxicological effects. How to avoid toxicity, as well as enhance strengths and avoid weaknesses is the direction of development and utilization of bavachin. This review provides reference for further development and utilization of bavachin.