Abstract
Two xanthanolide sesquiterpene lactones, 8- epi-xanthatin (1) and 8- epi-xanthatin epoxide (2), isolated from the leaves of Xanthium strumarium (Compositae), demonstrated a significant inhibition on the proliferation of cultured human tumor cells, i. e., A549 (non-small cell lung), SK-OV-3 (ovary), SK-MEL-2 (melanoma), XF498 (central nervous system) and HCT-15 (colon) in vitro. They were also found to inhibit the farnesylation process of human lamin-B by farnesyltransferase (FTase), in a dose-dependent manner in vitro (IC 50 value was calculated as 64 and 58 microM, respectively). Due to the relatively high concentrations of 1 and 2 required to obtain an FTase inhibition as compared with those necessary for a cytotoxic effect on tumor cells, it remains unclear whether a relationship between these two activities exists.
Publication types
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Letter
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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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Alkyl and Aryl Transferases / drug effects*
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Antineoplastic Agents / administration & dosage
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Antineoplastic Agents / pharmacology*
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Antineoplastic Agents / therapeutic use
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Dose-Response Relationship, Drug
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Farnesyltranstransferase
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Humans
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Inhibitory Concentration 50
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Lactones / administration & dosage
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Lactones / pharmacology
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Lactones / therapeutic use
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Phytotherapy*
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Plant Extracts / administration & dosage
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Plant Extracts / pharmacology*
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Plant Extracts / therapeutic use
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Plant Leaves
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Sesquiterpenes / administration & dosage
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Sesquiterpenes / pharmacology
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Sesquiterpenes / therapeutic use
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Tumor Cells, Cultured / drug effects
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Xanthium*
Substances
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Antineoplastic Agents
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Lactones
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Plant Extracts
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Sesquiterpenes
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Alkyl and Aryl Transferases
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Farnesyltranstransferase