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Anti-proliferative effects of estrogen receptor-modulating compounds isolated from Rheum palmatum

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Abstract

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 EC50 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, 2.853 µg/mL, 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) (6.3 × 10−2), followed by compound 4 (3.8 × 10−3), compound 5 (2.6 × 10−4), a compound 1 (2.1 × 10−4). 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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Correspondence to Jong Hwan Kwak or Ok Pyo Zee.

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Kang, S.C., Lee, C.M., Choung, E.S. et al. Anti-proliferative effects of estrogen receptor-modulating compounds isolated from Rheum palmatum . Arch. Pharm. Res. 31, 722–726 (2008). https://doi.org/10.1007/s12272-001-1218-1

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  • DOI: https://doi.org/10.1007/s12272-001-1218-1

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