Related Experiment Video
Updated: May 12, 2026
Exploring the Pharmacological Action and Molecular Mechanism of Salidroside in Inhibiting MCF-7 Cell Proliferation and Migration
Published on: June 9, 2023
2-Hydroxychalcone and xanthohumol inhibit invasion of triple negative breast cancer cells
Sun Young Kim1, Ik-Soo Lee, Aree Moon
1College of Pharmacy, Duksung Women's University, Seoul 132-714, Republic of Korea.
Abstract:
Breast cancer is estimated as one of the most common causes of cancer death among women. In particular, triple negative breast cancers (TNBCs), which do not express the genes for estrogen/progesterone receptors (ER/PR) and human epidermal growth factor receptor 2 (HER2), have been associated with poor prognosis and metastasis. Chalcones, the biosynthetic precursors of flavonoids present in edible plants, exert cytotoxic and chemopreventive activities. Although mounting evidence suggests the anticancer properties of chalcones, limited information is available regarding the inhibitory effects of chalcones on the aggressiveness of breast cancer cells. The present study aimed to investigate the effects of chalcone and its derivatives on the growth and the invasiveness of TNBC cells. Here, we showed that treatment with chalcone, 2-hydroxychalcone, and xanthohumol for 24h inhibited the growth of MDA-MB-231 cells with IC50 values of 18.1, 4.6, and 6.7 μM, respectively. Similarly, Chalcone, 2-hydroxychalcone, and xanthohumol also exerted cytotoxicity in another TNBC cell line, Hs578T. Neohesperidin dihydrochalcone, 4-methoxychalcone, and hesperidin methylchalcone did not show the cytotoxicity on the MDA-MB-231 cells. Xanthohumol and 2-hydroxychalcone induced apoptosis by Bcl-2 downregulation. Importantly, 2-hydroxychalcone and xanthohumol exerted more potent inhibitory effects on the proliferation, MMP-9 expression and invasive phenotype of MDA-MB-231 than chalcone. These results suggest a potential application of these chalcones as anticancer agents that can alleviate malignant progression of TNBC.
Insights
Chalcones, natural compounds from plants, show promise in fighting triple-negative breast cancer (TNBC). Specific derivatives like 2-hydroxychalcone and xanthohumol effectively inhibited TNBC cell growth and invasiveness, suggesting potential therapeutic applications.
Area of Science:
- Biochemistry
- Pharmacology
- Oncology
Background:
- Triple-negative breast cancer (TNBC) is an aggressive subtype with limited treatment options and poor prognosis.
- Chalcones, natural flavonoids, possess known cytotoxic and chemopreventive properties.
- Limited research exists on chalcones' effects on breast cancer cell aggressiveness.
Purpose of the Study:
- To investigate the inhibitory effects of chalcone and its derivatives on the growth and invasiveness of TNBC cells.
- To evaluate the potential of specific chalcones as therapeutic agents against TNBC progression.
Main Methods:
- Treatment of MDA-MB-231 and Hs578T TNBC cell lines with various chalcones.
- Determination of IC50 values for growth inhibition.
- Assessment of apoptosis induction via Bcl-2 downregulation.
- Evaluation of effects on MMP-9 expression and invasive phenotype.
Main Results:
- Chalcone, 2-hydroxychalcone, and xanthohumol inhibited MDA-MB-231 cell growth with IC50 values of 18.1, 4.6, and 6.7 μM, respectively.
- 2-hydroxychalcone and xanthohumol induced apoptosis and downregulated Bcl-2.
- 2-hydroxychalcone and xanthohumol demonstrated superior inhibition of proliferation, MMP-9 expression, and invasion compared to chalcone.
- Other tested chalcones showed no significant cytotoxicity.
Conclusions:
- 2-hydroxychalcone and xanthohumol exhibit potent anti-proliferative and anti-invasive effects on TNBC cells.
- These chalcones show potential as therapeutic agents to mitigate the malignant progression of TNBC.
- Further research into chalcone derivatives is warranted for TNBC treatment strategies.
