The cytotoxicity of the dominant lignans and sesquiterpenoids from Taiwania (Taiwania cryptomerioides Hayata) was investigated. Three human tumor cells including A-549 lung carcinoma, MCF-7 breast adenocarcinoma and HT-29 colon adenocarcinoma were selected to illustrate the structure cytotoxicity relationships of Taiwania's dominant compounds. Taiwanin A, taiwanin E and dimethylmatairesinol exhibited significant cytotoxicity against three human tumor cells. Among them, taiwanin A possesses the strongest cytotoxic activity. In addition, the morphology-based evaluation, flow cytometric analysis, and DNA fragmentation assays demonstrated that the turner cell death induced by taiwanin A was due to apoptosis.