| Title | Anti-proliferative effects of estrogen receptor-modulating compounds isolated from Rheum palmatum. | | Author(s) | Kang SC, Lee CM, Choung ES, Bak JP, Bae JJ, Yoo HS, Kwak JH, Zee OP | | Institution | Gyeonggi Pharmaceutical Research Center, Suwon, 443-766, Korea. | | Source | Arch Pharm Res 2008 Jun; 31(6):722-6. | | 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 EC(50) 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 microg/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 x 10(-2)), followed by compound 4 (3.8 x 10(-3)), compound 5 (2.6 x 10(-4)), a compound 1 (2.1 x 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. | | Language | eng | | Pub Type(s) | Journal Article
| | PubMed ID | 18563353 |
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