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Flavonoids are widely-distributed polyphenolic secondary metabolites with diverse biological activities in plants and benefit human health as protective dietary agents. They participate in plants' responses to harsh environmental conditions and effectively regulate the cell differentiation and growth. In plants, the majority of their functions are attributed to their strong antioxidative properties. Similarly, dietary flavonoids protect the human body against free radicals which are associated with the development of cancer and atherosclerosis. Plants rich in polyphenols have been used to cure various diseases because of their antibacterial, antiviral, antifungal and anticancer properties. This review summarizes the up-to-date research trends and development on flavonoids and its derivatives, working mechanisms and potential functions and applications particularly in relation to plant protection and human health. Towards the end, notable concluding remarks with a close-up look at the future research directions have also been presented briefly.