Anti-tumor activity of the farnesyl-protein transferase inhibitors arteminolides, isolated from Artemisa Original Research Article

Members of the Artemisia genus are important medicinal plants found throughout the world. Arteminolides A–D (1–4), isolated from the aerial parts of Artemisia, have an inhibitory activity on farnesyl-protein transferase (FPTase; EC 2.5.1.29) in in vitro assay. This study was carried out with the purpose of validating anti-tumor effects of the compounds in human tumor cells and mouse xenograft model. The arteminolides inhibited tumor cell growth in a dose-dependent manner. Furthermore, arteminolide C (3) blocked in vivo growth of human colon and lung tumor xenograft without the loss of body weight in nude mice.