The consumption of plant-based diets has become a burgeoning trend, and they are increasingly consumed globally owing to their substantial energy intensity and dietetic advantages. Plants possess numerous bioactive components that have been recognized to exhibit manifold health-promoting assets. Comprehension of the synthesis of these primary and secondary metabolites by plants and their method of action against several chronic illnesses is a significant requirement for understanding their benefits to human health and disease prevention. Furthermore, the association of biologically active complexes with plants, humans, disease, medicine, and the underlying mechanisms is unexplored. Therefore, this review portrays various bioactive components derived from plant sources associated with health-promoting traits and their action mechanisms. This review paper predominantly assembles proposed plant-derived bioactive compounds, postulating valuable evidence aimed at perceiving forthcoming approaches, including the selection of potent bioactive components for formulating functional diets that are effective against several human disorders. This meticulous evidence could perhaps provide the basis for the advanced preemptive and therapeutic potential promoting human health. Hence, delivery opens possibilities for purchasers to approach the lucrative practice of plants as a remedy, produce novel products, and access new marketplaces.