Phenolic compounds are important functional bioactive substances distributed in various food plants. They have gained wide interest from researchers due to their multiple health benefits. There are two forms of phenolic compounds: free form and bound form. The latter is also called bound phenolics (BPs), which are found mainly in the cell wall and distributed in various tissues/organs of the plant body. They can either chemically bind to macromolecules and food matrixes or be physically entrapped in food matrixes and intact cells. Various isolation methods, including chemical, biological, and physical methods, have been employed to extract BPs from plants. BPs have been shown to have strong biological activities, including antioxidant, probiotic, anticancer, anti-inflammation, antiobesity, and antidiabetic effects as well as beneficial effects on central nervous system diseases. This review summarizes research findings on these topics to help in better understanding of BPs and provide comprehensive information on their health effects.