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Updated: May 5, 2026

Assays for Validating Histone Acetyltransferase Inhibitors
Published on: August 6, 2020
Triptolide inhibits histone methyltransferase EZH2 and modulates the expression of its target genes in prostate
Ousman Tamgue1, Cheng-Sen Chai, Lin Hao
1Key Laboratory of Agricultural Molecular Biology, College of Life Science, Northwest A and F University, Yangling, China E-mail : leiming70@hotmail.com, weiyanming2005@aliyun.com.
Abstract:
The histone methyltransferase EZH2 (enhancer of zeste homolog 2) plays critical roles in prostate cancer (PCa) development and is a potential target for PCa treatment. Triptolide possesses anti-tumor activity, but it is unknown whether its therapeutic effect relates with EZH2 in PCa. Here we described EZH2 as a target for Triptolide in PCa cells. Our data showed that Triptolide suppressed PCa cell growth and reduced the expression of EZH2. Overexpression of EZH2 attenuated the Triptolide induced cell growth inhibition. Moreover, Triptolide treatment of PC-3 cells resulted in elevated mRNA levels of target genes (ADRB2, CDH1, CDKN2A and DAB2IP) negatively regulated by EZH2 as well as reduced mRNA levelsan of EZH2 positively regulated gene (cyclin D1). Our findings suggest the PCa cell growth inhibition mediated by Triptolide might be associated with downregulation of EZH2 expression and the subsequent modulation of target genes.
Insights
Triptolide inhibits prostate cancer cell growth by downregulating EZH2 (enhancer of zeste homolog 2). This suggests EZH2 is a therapeutic target for prostate cancer treatment.
Area of Science:
- Oncology
- Molecular Biology
- Pharmacology
Background:
- Enhancer of zeste homolog 2 (EZH2) is crucial in prostate cancer (PCa) progression.
- EZH2 is a potential therapeutic target for PCa.
- Triptolide exhibits anti-tumor properties, but its mechanism in PCa involving EZH2 was unclear.
Purpose of the Study:
- To investigate if EZH2 is a therapeutic target for Triptolide in prostate cancer cells.
- To elucidate the relationship between Triptolide treatment and EZH2 expression in PCa.
Main Methods:
- Prostate cancer cell lines were treated with Triptolide.
- EZH2 expression levels were analyzed.
- The impact of EZH2 overexpression on Triptolide's efficacy was assessed.
- mRNA levels of EZH2 target genes were quantified.
Main Results:
- Triptolide suppressed prostate cancer cell proliferation.
- Triptolide treatment led to decreased EZH2 expression.
- Overexpression of EZH2 partially reversed Triptolide-induced growth inhibition.
- Triptolide modulated the expression of EZH2 target genes, including ADRB2, CDH1, CDKN2A, DAB2IP, and cyclin D1.
Conclusions:
- Triptolide's anti-cancer effect in prostate cancer cells is associated with the downregulation of EZH2.
- Modulation of EZH2 and its target genes by Triptolide offers a potential therapeutic strategy for PCa.
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