Anti-tumor activity of the farnesyl-protein transferase inhibitors arteminolides, isolated from Artemisa.

Abstract

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.

• Authors: Seung Ho Lee, Mi-Young Lee, Hyun-Mi Kang, Dong Cho Han, Kwang-Hee Son, Deok Cho Yang, Nack-Do Sung, Chang Woo Lee, Hwan Mook Kim, Byoung-Mog Kwon
• Journal: Bioorganic & medicinal chemistry (Bioorg Med Chem) Vol. 11 Issue 21 Pg. 4545-9 (Oct 15 2003) ISSN: 0968-0896 [Print] England
• PMID: 14527550 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Antineoplastic Agents
• Enzyme Inhibitors
• Lactones
• Sesquiterpenes
• Tumor Suppressor Proteins
• arteminolide A
• arteminolide B
• arteminolide C
• Alkyl and Aryl Transferases
• Farnesyltranstransferase

Topics

• Alkyl and Aryl Transferases (antagonists & inhibitors)
• Animals
• Antineoplastic Agents (chemistry, isolation & purification, therapeutic use)
• Artemisia (enzymology)
• Cell Line, Tumor
• Enzyme Inhibitors (chemistry, isolation & purification, therapeutic use)
• Farnesyltranstransferase
• Humans
• Lactones (chemistry, isolation & purification, therapeutic use)
• Mice
• Mice, Nude
• Neoplasm Transplantation
• Phytotherapy
• Sesquiterpenes (chemistry, isolation & purification, therapeutic use)
• Tumor Suppressor Proteins (therapeutic use)
• Xenograft Model Antitumor Assays