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Cytotoxic caffeic acid derivatives from the rhizomes of Cimicifuga heracleifolia

Yim, Soon-Ho, Kim, Hyun Jung, Park, Si-Hwan, Kim, Jinmi, Williams, Darren R., Jung, Da-Woon, Lee, Ik-Soo
Archives of pharmacal research 2012 v.35 no.9 pp. 1559-1565
NAD ADP-ribosyltransferase, Western blotting, anticarcinogenic activity, apoptosis, caffeic acid, colorectal neoplasms, cytotoxicity, dose response, fractionation, herbal medicines, high performance liquid chromatography, medicinal plants, neoplasm cells, nuclear magnetic resonance spectroscopy, rhizomes
Activity profiling of the n-BuOH extract from Cimicifuga heracleifolia rhizomes led to the identification of three cytotoxic caffeic acid derivatives, carboxymethyl isoferulate (2), cimicifugic acid A (3), and cimicifugic acid B (4) together with a series of structurally related inactive compounds. The extract was separated by time-based fractionation in a gradient HPLC condition, and cytotoxicity of each fraction was evaluated using HCT116 colon cancer cells in vitro. HPLChyphenated spectroscopy including LC/NMR and LC/PDA/MS provided structural information for phenolic compounds contained in the extract, and further preparative isolation of active compounds 2–4 was achieved by semi-preparative HPLC. Compounds 2–4 showed cytotoxic activity against cancer cells in a dose-dependent manner at the concentrations of 2.5–40 μM, and western blotting analysis showed that these compounds increased expression of cleaved poly ADP ribose polymerase (PARP), a critical apoptosis marker.