Next Article in Journal
Improved Synthesis of N-Methylcadaverine
Next Article in Special Issue
Nutraceuticals in Periodontal Health: A Systematic Review on the Role of Vitamins in Periodontal Health Maintenance
Previous Article in Journal
Antioxidants from the Brown Alga Dictyopteris undulata
Previous Article in Special Issue
Tetragonia tetragonioides (Pall.) Kuntze Regulates Androgen Production in a Letrozole-Induced Polycystic Ovary Syndrome Model
Article Menu
Issue 5 (May) cover image

Export Article

Open AccessArticle
Molecules 2018, 23(5), 1215; https://doi.org/10.3390/molecules23051215

In Vitro Estrogenic and Breast Cancer Inhibitory Activities of Chemical Constituents Isolated from Rheum undulatum L.

1
School of Pharmacy, Sungkyunkwan University, Suwon 16419, Korea
2
College of Pharmacy, Yonsei Institute of Pharmaceutical Sciences, Yonsei University, Incheon 21983, Korea
3
College of Korean Medicine, Gachon University, Seongnam 13120, Korea
These authors contributed equally to this work.
*
Authors to whom correspondence should be addressed.
Received: 29 March 2018 / Revised: 16 May 2018 / Accepted: 17 May 2018 / Published: 18 May 2018
(This article belongs to the Special Issue Nutraceuticals and Their Medicinal Importance)
Full-Text   |   PDF [3591 KB, uploaded 18 May 2018]   |  

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 13) 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 13 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. View Full-Text
Keywords: Rheum undulatum L.; menopause; estrogen receptor; hormone replacement therapy Rheum undulatum L.; menopause; estrogen receptor; hormone replacement therapy
Figures

Graphical abstract

This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).
SciFeed

Share & Cite This Article

MDPI and ACS Style

Lee, D.; Park, S.; Choi, S.; Kim, S.H.; Kang, K.S. In Vitro Estrogenic and Breast Cancer Inhibitory Activities of Chemical Constituents Isolated from Rheum undulatum L.. Molecules 2018, 23, 1215.

Show more citation formats Show less citations formats

Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.

Related Articles

Article Metrics

Article Access Statistics

1

Comments

[Return to top]
Molecules EISSN 1420-3049 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert
Back to Top