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

Bioorg Med Chem. 2003 Oct 15;11(21):4545-9. doi: 10.1016/j.bmc.2003.08.008.

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.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

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

Substances

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