Emodin Inhibits the Proliferation of MCF-7 Human Breast Cancer Cells Through Activation of Aryl Hydrocarbon Receptor (AhR)

Abstract

Natural products have proved to be a promising source for the development of potential anticancer drugs. Emodin, a natural compound from Rheum palmatum, is used to treat several types of cancers, including lung, liver, and pancreatic. However, there are few reports regarding its use in the treatment of breast cancer. Thus, the therapeutic effect and mechanism of emodin on MCF-7 human breast cancer cells were investigated in this study. Morphological observations and cell viability were evaluated to determine the anti-proliferation activity of emodin. Network pharmacology and molecular docking were performed to screen the potential targets. Western blot analysis was used to explore a potential antitumor mechanism. The results showed that emodin (50–100 μmol/L) could significantly inhibit the proliferation of MCF-7 cells in a time and dose-dependent manner. Furthermore, virtual screening studies indicated that emodin was a potent aryl hydrocarbon receptor (AhR) agonist in chemotherapy for breast cancer. Finally, when MCF-7 cells were treated with emodin (100 μmol/L) for 24 h, the AhR and cytochrome P450 1A1 (CYP1A1) protein expression levels were significantly upregulated compared with the control group. Our study indicated that emodin exhibited promising antitumor activity in MCF-7 cells, likely through activation of the AhR-CYP1A1 signaling pathway. These findings lay a foundation for the application of emodin in breast cancer treatment.

Comparative Evidence for Intrahepatic Cholestasis of Pregnancy Treatment With Traditional Chinese Medicine Therapy: A Network Meta-Analysis

“…Rhubarb is also named dahuang in China. Rhubarb also contains many active constituents with pharmacological activities such as rhein, emodin, and danthron ( Xian et al, 2020 ; Zhang N. et al, 2020 ; Ma et al, 2021 ). Rhein is the main active constituent of Rhubarb with pharmacological activity.…”

The versatile emodin: A natural easily acquired anthraquinone possesses promising anticancer properties against a variety of cancers

“…found that emodin is an effective aromatic hydrocarbon receptor (AhR) agonist. Subsequent in vitro experiments also found that the expression levels of AhR and cytochrome P450 1A1 (CYP1A1) in MCF-7 cells were significantly upregulated by emodin treatment, suggesting that the antitumor effects of emodin against BC might be related to the AhR-CYP1A1 signaling pathway 120 .…”

The Health Benefits of Emodin, a Natural Anthraquinone Derived from Rhubarb—A Summary Update

“…The effect of emodin on cell proliferation was studied and confirmed for many cancer cell lines, including breast [40], skin [41], pancreas [42], colon [43,44], ovarian [45], prostate [46], esophageal [47], bladder [48], and endometrial [49]. For example, the IC50 values for MCF-7 (breast) and HepG2 (liver) cancer cells were 52.72 μM and 43.87 μM, respectively [50].…”