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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.