Cytotoxic caffeic acid derivatives from the rhizomes of Cimicifuga heracleifolia
- Arch Pharm Res. 2012 Sep;35(9):1559-65. doi: 10.1007/s12272-012-0906-0.
- 1. College of Pharmacy and Research Institute of Drug Development, Chonnam National University, Gwangju, 500-757, Korea.
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.
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