In vitro estrogenic and breast cancer inhibitory activities of chemical constituents isolated from rheum undulatum L.

Dahae Lee, Seon Ju Park, Sungyoul Choi, Seung Hyun Kim, Ki Sung Kang

Research output: Contribution to journalArticle

2 Citations (Scopus)

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 µM, 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-β-D-glucopyranoside) was mediated through the mitochondria-dependent apoptotic pathway.

Original languageEnglish
Article number1215
JournalMolecules
Volume23
Issue number5
DOIs
Publication statusPublished - 2018 Jan 1

Fingerprint

Rheum
estrogens
MCF-7 Cells
breast
Estrogen Receptors
cancer
Breast Neoplasms
Mitochondria
Estrogens
Apoptosis
mitochondria
Laxatives
apoptosis
Chemical compounds
Caspase 8
cells
Assays
Blood
Anti-Inflammatory Agents
multiple docking adapters

All Science Journal Classification (ASJC) codes

  • Analytical Chemistry
  • Chemistry (miscellaneous)
  • Molecular Medicine
  • Pharmaceutical Science
  • Drug Discovery
  • Physical and Theoretical Chemistry
  • Organic Chemistry

Cite this

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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 µM, 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-β-D-glucopyranoside) was mediated through the mitochondria-dependent apoptotic pathway.",
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In vitro estrogenic and breast cancer inhibitory activities of chemical constituents isolated from rheum undulatum L. / Lee, Dahae; Park, Seon Ju; Choi, Sungyoul; Kim, Seung Hyun; Kang, Ki Sung.

In: Molecules, Vol. 23, No. 5, 1215, 01.01.2018.

Research output: Contribution to journalArticle

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