Lignans are plant-derived compounds, sharing structural similarity with wide-ranging properties and contain two or more phenylpropanoid units, that form a core scaffold. Major lignans include secoisolariciresinol, matairesinol, pinoresinol, and lariciresinol. Lignans possess diverse pharmacological properties ranging from antidiabetic, anti-inflammatory, antioxidant, anticancer, antimicrobial, neuroprotective, and antiparasitic activities. Some lignans and synthetic derivates also find possible applications in chemotherapy against cancer. Larger clinical trials are needed to confirm their applications and understand their mechanisms of action in humans. Research on bioavailability and optimal dosing is crucial to maximize their therapeutic potential. In conclusion, bioactive phytolignans hold significant promise for enhancing human health, but further research and development are needed to fully harness their potential. Advances in clinical studies, functional food development, and personalized nutrition are likely to shape the future landscape of lignan utilization.