Novel ceramides, together with nine known compounds were isolated from aerial parts of the Saussurea involucrata Kar. et. Kir. The novel structures were determined by spectroscopic methods and microscale chemical degradation. The ceramides showed appreciable cytotoxicity against three human tumor cell lines including human promyelocytic leukemia (HL-60), human melanoma (A375-S2) and human cervical carcinoma (HeLa) cell lines. The results suggested that this class of ceramides may have potential as an antitumor agent.