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Published on: March 30, 2018
Wedelolactone Targets EZH2-mediated Histone H3K27 Methylation in Mantle Cell Lymphoma
Nadezhda Romanchikova1, Peteris Trapencieris2
1Latvian Institute of Organic Synthesis, Riga, Latvia nadezhda.romanchikova@gmail.com.
Background/Aim:
Enhancer of zeste homolog 2 (EZH2), the catalytic subunit of polycomb repressive complex 2 (PRC2), possesses histone N-methyltransferase (HMT) activity and plays an essential role in cancer initiation and development. The aim of the present study was to investigate the potential of Wedelolactone (WL) to inhibit the methylation activity of EZH2.
Materials And Methods:
The mantle cell lymphoma (MCL) cell line, Mino, was treated with WL, while untreated cells were used as control. HMT activity and EZH2 amount were measured in nuclear extracts from WL-treated and control Mino cells.
Results:
WL was found to target EZH2-mediated histone H3K27 methylation. Along with the inhibition of H3K27 methylation in vitro (IC50=0.3 μM), WL suppressed HMT activity in Mino cells with an IC50 value of 3.2 μM. We detected a reduced amount of EZH2 in Mino cells treated with WL, compared to untreated control cells.
Conclusion:
This is the first study to show that WL induces inhibition of H3K27 methylation via EZH2 modulation and decreases cell proliferation in MCL, in vitro. WL is proposed as a promising agent and a novel epigenetic approach in MCL investigation and treatment.
Insights
Wedelolactone (WL) inhibits EZH2-mediated H3K27 methylation and reduces cell proliferation in mantle cell lymphoma (MCL). This epigenetic approach shows promise for MCL treatment.
Area of Science:
- Epigenetics
- Cancer Biology
- Pharmacology
Background:
- Enhancer of zeste homolog 2 (EZH2) is crucial for cancer development.
- EZH2's histone N-methyltransferase (HMT) activity drives tumorigenesis.
Purpose of the Study:
- To investigate Wedelolactone's (WL) potential to inhibit EZH2's HMT activity.
- To explore WL as a novel therapeutic agent for mantle cell lymphoma (MCL).
Main Methods:
- Mantle cell lymphoma (MCL) cells (Mino) were treated with WL.
- Histone N-methyltransferase (HMT) activity and EZH2 levels were quantified in nuclear extracts.
Main Results:
- Wedelolactone (WL) inhibited EZH2-mediated histone H3K27 methylation in vitro (IC50=0.3 μM).
- WL suppressed HMT activity in Mino cells (IC50=3.2 μM) and reduced EZH2 levels.
- WL treatment decreased cell proliferation in MCL cells.
Conclusions:
- WL demonstrates inhibitory effects on H3K27 methylation through EZH2 modulation.
- WL shows potential as a novel epigenetic therapeutic strategy for mantle cell lymphoma (MCL).
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