In Vitro Estrogenic and Breast Cancer Inhibitory Activities of Chemical Constituents Isolated from Rheum undulatum L.
- Authors
- Lee, Dahae; Park, SeonJu; Choi, Sungyoul; Kim, Seung Hyun; Kang, Ki Sung
- Issue Date
- May-2018
- Publisher
- MDPI
- Keywords
- Rheum undulatum L; menopause; estrogen receptor; hormone replacement therapy
- Citation
- MOLECULES, v.23, no.5
- Journal Title
- MOLECULES
- Volume
- 23
- Number
- 5
- URI
- https://scholarworks.bwise.kr/gachon/handle/2020.sw.gachon/3817
- DOI
- 10.3390/molecules23051215
- ISSN
- 1420-3049
- Abstract
- We investigated the estrogenic and breast cancer inhibitory activities of chemical constituents isolated from Rhei undulati Rhizoma (roots of Rheum undulatum L.), which is used as a laxative, an anti-inflammatory, and an anti-blood stagnation agent. Estrogen-like activity was studied using the well characterized E-screen assay in estrogen receptor (ER)-positive MCF-7 cells. The mechanism underlying the breast cancer inhibitory activity of the compounds was studied using human ER-negative MDA-MB-231 and ER-positive MCF-7 cells. The activation of apoptosis pathway-related proteins was investigated by western blotting, using extracts of R. undulatum prepared in three solvent conditions (EX1, EX2, and EX3). The R. undulatum chemical constituents (compounds 1-3) showed estrogen-like activity in the concentration range of 10 to 50 M, by increasing the proliferation of human ER-positive MCF-7 cells. These effects were attenuated by co-treatment with 100 nM fulvestrant, an ER antagonist. Compounds 1-3 decreased the viability of MCF-7 cells in a concentration-dependent manner. Compounds 1 (aloe emodin) and 2 (rhapontigenin) induced mitochondria-independent apoptosis by activating the caspase-8 pathway, whereas the cytotoxic effect of compound 3 (chrysophanol 1-O--d-glucopyranoside) was mediated through the mitochondria-dependent apoptotic pathway.
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