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KMID : 0043320120350091559
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Archives of Pharmacal Research
2012 Volume.35 No. 9 p.1559 ~ p.1565
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Cytotoxic caffeic acid derivatives from the rhizomes of Cimicifuga heracleifolia
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Yim Soon-Ho
Kim Hyun-Jung
Park Si-Hwan
Kim Jin-Mi
Williams Darren R.
Jung Da-Woon
Lee Ik-Soo
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Abstract
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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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KEYWORD
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Cimicifuga heracleifolia, Activity profiling, Caffeic acid derivatives, Carboxymethyl isoferulate, Cimicifugic acid A, Cimicifugic acid B, Cytotoxicity, Poly ADP ribose polymerase (PARP)
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