Gomisin N is the most abundant dibenzocyclooctadiene lignan present in the traditional Chinese medicinal herb Schisandra chinensis (Turcz.) Baill. In vitro assays demonstrated that Gomisin N could inhibit TGF-β induced epithelial-mesenchymal transition of 4T1 cells and of primary human breast cancer cells. Gomisin N could maintain membrane stability of rat hepatocytes under oxidative stress. Gomisin N can reduce inflammation, inhibit apoptosis, and improve cardiac function after ischemic injury. It represents a potential novel therapeutic approach for treatment of ischemic heart disease. Gomisin N produced beneficial sedative and hypnotic bioactivity, which might be mediated by the modification of the serotonergic and GABAergic system.