Anti-tumor activity of the farnesyl-protein transferase inhibitors arteminolides, isolated from Artemisa.
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.
Lee
Seung Ho
SH
Korea Research Institute of Bioscience and Biotechnology, 52 Uendong Yoosunggu, Taejeon 305-600, South Korea.
Lee
Mi-Young
MY
Kang
Hyun-Mi
HM
Han
Dong Cho
DC
Son
Kwang-Hee
KH
Yang
Deok Cho
DC
Sung
Nack-Do
ND
Lee
Chang Woo
CW
Kim
Hwan Mook
HM
Kwon
Byoung-Mog
BM
D019883:Alkyl and Aryl Transferases / Q000037:antagonists & inhibitors*; D000818:Animals; D000970:Antineoplastic Agents / Q000737:chemistry / Q000302:isolation & purification / Q000627:therapeutic use*; D019306:Artemisia / Q000201:enzymology; D045744:Cell Line, Tumor; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000302:isolation & purification / Q000627:therapeutic use*; D051231:Farnesyltranstransferase; D006801:Humans; D007783:Lactones / Q000737:chemistry / Q000302:isolation & purification / Q000627:therapeutic use*; D051379:Mice; D008819:Mice, Nude; D009368:Neoplasm Transplantation; D008517:Phytotherapy; D012717:Sesquiterpenes / Q000737:chemistry / Q000302:isolation & purification / Q000627:therapeutic use*; D025521:Tumor Suppressor Proteins / Q000627:therapeutic use; D023041:Xenograft Model Antitumor Assays
D000970:Antineoplastic Agents; D004791:Enzyme Inhibitors; D007783:Lactones; D012717:Sesquiterpenes; D025521:Tumor Suppressor Proteins; C484914:arteminolide A; C484912:arteminolide B; C484913:arteminolide C; D019883:Alkyl and Aryl Transferases; D051231:Farnesyltranstransferase