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Two cytotoxic sesquiterpene
lactones from the leaves of Xanthium strumarium and their in vitro
inhibitory activity on farnesyltransferase.
Kim
YS, Kim
JS, Park
SH, Choi
SU, Lee
CO, Kim
SK, Kim
YK, Kim
SH, Ryu
SY.
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:
PMID: 12709909 [PubMed - indexed for MEDLINE]
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