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Usually found bound to other complex molecules (e.g., lignin, hemicellulose), phenolic compounds (PC) are widely present in agro-industrial by-products, and their extraction is challenging. In recent times, research is starting to highlight the bioactive roles played by bound phenolics (BPC) in human health. This review aims at providing a critical update on recent advances in green techniques for the recovery of BPC, focusing on enzymatic-assisted (EAE) and fermentation-assisted extraction (FAE) as well as in the combination of technologies, showing variable yield and features. The present review also summarizes the most recent biological activities attributed to BPC extracts until now. The higher antioxidant activity of BPC—compared to FPC—coupled with their affordable by-product source make them medicinally potent and economically viable, promoting their integral upcycling and generating new revenue streams, business, and employment opportunities. In addition, EAE and FAE can have a biotransformative effect on the PC itself or its moiety, leading to improved extraction outcomes. Moreover, recent research on BPC extracts has reported promising anti-cancer and anti-diabetic activity. Yet further research is needed to elucidate their biological mechanisms and exploit the true potential of their applications in terms of new food products or ingredient development for human consumption. [ABSTRACT FROM AUTHOR]