Novel insights into the anti-cancer effects of 3-bromopyruvic acid against castration-resistant prostate cancer

Hsin Chih Yeh, Chia Cheng Su, Yen Hsuan Wu, Cheng Hsueh Lee, Bo Ying Bao, Wei Chung Cheng, Shu Chi Wang, Po Len Liu, Chien Chih Chiu, Chih Pin Chuu, Chien Chih Ke, Hsin En Wu, Yuan Ru Chen, Wei Ju Chung, Shu Pin Huang, Chia Yang Li

Research output: Contribution to journalArticlepeer-review


3-bromopyruvic acid (3-BP), a small molecule alkylating agent, has been emerged as a glycolytic inhibitor with anticancer activities. However, the effects of 3-BP on the growth and metastasis in prostate cancer have not been well investigated. Here we investigated the anti-cancer effects of 3-BP on prostate cancer in vitro and in vivo. Cell growth, apoptosis, migration, motility, and invasion were examined. The tumor growth ability was determined using a xenograft murine model. Transcriptome analysis using RNA-seq was performed to explore the mechanism of action of 3-BP. Our experimental results showed that 3-BP effectively inhibits prostate cancer cell growth, especially in castration-resistant prostate cancer (CRPC) cells. Moreover, 3-BP induces apoptosis and suppresses cell migration, motility, epithelial-mesenchymal transition (EMT), and invasion in CRPC cells. In addition, 3-BP also attenuates tumor growth in a xenograft murine model. Through transcriptome analysis using RNA-seq, 3-BP significantly regulates the cell cycle pathway and decreases the expression of downstream cycle cycle-associated genes in CRPC cells. The results of cell cycle analysis indicated that 3-BP arrests cell cycle progression at G2/M in CRPC cells. These results suggest that 3-BP has the potential in inhibiting CRPC progression and might be a promising drug for CRPC treatment.

Original languageEnglish (US)
Article number174929
JournalEuropean Journal of Pharmacology
StatePublished - May 15 2022
Externally publishedYes


  • 3-Bromopyruvic acid
  • Anticancer
  • Cell metastasis
  • Prostate cancer
  • Transcriptome analysis

ASJC Scopus subject areas

  • Pharmacology


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