Anti-proliferative effects of estrogen receptor-modulating compounds isolated from Rheum palmatum.
Kang, Se Chan 1,2; Lee, Chang Min 3; Choung, Eui Su 3; Bak, Jong Phil 3; Bae, Jong Jin 3; Yoo, Hyun Sook 3; Kwak, Jong Hwan 3; Zee, Ok Pyo 3
[Article] Archives of Pharmacal Research. 31(6):722-726, June 2008.

(Format: HTML, PDF)

: 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 [mu]g/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.

(C) 2008 Springer. Part of Springer Science Business Media