Enzymatic tailoring of prebiotic oligosaccharides, flavonoids, and terpenoids for enhanced physiological effects.

Next-generation functional foods provide a paradigm shift from generalized healthcare to personalized nutrition. Rational design of functional ingredients based on structure-activity relationships is essential for their further development. Because of high substrate specificity and selectivity, enzymes enable the precise conversion of food components into targeted bioactive molecules. Among diverse functional ingredients, prebiotic oligosaccharides (OSs), flavonoids, and terpenoids are particularly suitable for enzyme-guided design because their biological activities strongly depend on structural features. In this review, we overview enzymatic approaches for developing degree-of-polymerization-controlled prebiotic OSs and for modifying flavonoids and terpenoids to enhance their biological activities with brief perspectives on structure-activity relationships for rational design. Representative biocatalytic strategies, including synthetic route selection and suitable enzyme engineering, are discussed for structural control and enhanced biocatalytic performance. The approaches presented here extend beyond the selected examples, highlighting the potential of enzyme-guided design to expand the repertoire of structurally defined functional food ingredients.