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
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Research Support, Non-U.S. Gov't
MeSH terms
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Alkyl and Aryl Transferases / antagonists & inhibitors*
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Animals
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Antineoplastic Agents / chemistry
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Antineoplastic Agents / isolation & purification
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Antineoplastic Agents / therapeutic use*
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Artemisia / enzymology
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Cell Line, Tumor
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Enzyme Inhibitors / chemistry
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Enzyme Inhibitors / isolation & purification
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Enzyme Inhibitors / therapeutic use*
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Farnesyltranstransferase
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Humans
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Lactones / chemistry
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Lactones / isolation & purification
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Lactones / therapeutic use*
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Mice
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Mice, Nude
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Neoplasm Transplantation
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Phytotherapy
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Sesquiterpenes / chemistry
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Sesquiterpenes / isolation & purification
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Sesquiterpenes / therapeutic use*
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Tumor Suppressor Proteins / therapeutic use
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Xenograft Model Antitumor Assays
Substances
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Antineoplastic Agents
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Enzyme Inhibitors
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Lactones
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Sesquiterpenes
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Tumor Suppressor Proteins
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arteminolide A
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arteminolide B
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arteminolide C
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Alkyl and Aryl Transferases
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Farnesyltranstransferase