Abstract: Natural polyphenols are widely found in plants and have biological activities such as antioxidant, anti-inflammatory and anticancer. Polyphenols can be categorized into free polyphenols and bound polyphenols according to their solubility characteristics. Compared with free polyphenols that can be directly extracted, bound polyphenols have a higher proportion and wider distribution, which have potential application value and are increasingly being paid attention to. Therefore, this paper summarizes and analyzes the in vitro release of bound polyphenols, and briefly reviews the release mechanism of bound polyphenols in the human body, and focuses on the mechanisms and research progress of the functional activities of bound polyphenols, such as antioxidant, anti-inflammatory, anticancer, and regulate of the intestinal environment. It is expected to provide reference and guidance for future research and application of bound polyphenols.