Dibenzocyclooctadiene lignans are important active constituents in genus Schisandra, exhibit remarkable biological activities including hepatoprotective, antioxidant, anti-inflammatory, central nervous system-modulating, and antitumor activities, demonstrating significant clinical potential. China serves as both the diversity center and distribution center for genus Schisandra, to conserve existing resources, the biosynthesis of dibenzocyclooctadiene lignans has gradually become a research hotspot. This review systematically summarizes the chemical structures and pharmacological activities of dibenzocyclooctadiene lignans from genus Schisandra, while critically discussing recent advances in elucidating their biosynthetic pathways and characterizing key catalytic components. The integration of phytochemistry and synthetic biology approaches discussed herein provides theoretical references for the sustainable utilization of Schisandra resources, the advancement of lignan biosynthesis technologies, and the development of new pharmaceuticals.