Abstract: Selenium (Se) is an essential micronutrient for human body that plays an important physiological function in life. Compared with inorganic selenium, organic selenium has high bioavailability and low toxicity, making it a superior source of selenium supplementation. Bioactive selenium-containing peptides are important forms of organic selenium, mainly be isolated from selenium-enriched plants and obtained from synthetic pathway, which have become a research hotspot in recent years due to their multiple healthful biological activities. In this review, the isolation and artificial chelating preparation, and the common sources of plant-derived bioactive selenium-containing peptides, as well as their various bioactivities such as antioxidant, hepatoprotective, immunomodulatory, anticancer, hypotensive are summarized. This review would provide a theoretical reference for the development and utilization of plant-derived bioactive selenium-containing peptides in functional foods and medicines.