Bitter compounds in food produce a distinct bitter taste that significantly influences overall flavor and quality, while also possessing valuable biological activities. Therefore, a systematic review summarizing recent research advances on bitter compounds is necessary for a better understanding of them. This review discusses the sources of bitter substances in food, the mechanism of bitterness perception, their biological activities and key issues for future research. Bitter compounds in food mainly include polyphenols, alkaloids, terpenoids, bitter peptides and Maillard reaction products. Bitter substances bind to specific sites on bitter taste receptors (TAS2Rs), activating G protein-mediated downstream signaling pathways that lead to the perception of bitterness. Additionally, many bitter compounds possess biological activities, such as regulating food intake and exhibiting anti-cancer, anti-inflammatory and antioxidant activities. This review highlights the potential to exploit the bioactivity of bitter compounds to enhance the nutritional value and functionality of food.
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