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KMID : 0043320080310060722
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Archives of Pharmacal Research
2008 Volume.31 No. 6 p.722 ~ p.726
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Anti-Proliferative Effects of Estrogen Receptor-Modulating Compounds Isolated from Rheum palmatum
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Kang Se-Chan
Lee Chang-Min
Choung Eui-Su
Bak Jong-Phil
Bae Jong-Jin
Yoo Hyun-Sook
Kwak Jong-Hwan
Zee Ok-Pyo
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Abstract
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The Rheum palmatum L., a traditional medicine in Korea, was screened for their estrogenic activity in a recombinant yeast system with a human estrogen receptor (ER) expression plasmid and a reporter plasmid used in a previous study. The values of the n-hexane, dichloromethane, ethyl acetate, n-butanol, and water fractions of the methanolic extract of R. palmatum in the yeast-based estrogenicity assay system were 0.145, 0.093, 0.125, 1.459, , respectively, with marked estrogenic activity in the dichloromethane fraction. Using an activity-guided fractionation approach, five known anthraquinones, chrysophanol (1), physcion (2), emodin (3), aloe-emodin (4) and rhein (5), were isolated from the dichloromethane fraction. Compound 3 had the highest estrogenic relative potency (RP, 17bestradiol = 1.00) (), followed by compound 4 (), compound 5 (), and compound 1 (). Also, compound 3 and fraction 3 (which contained compound 3) of the dichloromethane fraction of R. palmatum showed strong cytotoxicity in both ER-positive (MCF-7) and -negative (MDA-MB-231) breast cancer cell lines.
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KEYWORD
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Rheum palmatum L., Anthraquinones, Yeast-based estrogenicity assay, Anti-proliferative effects
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