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Updated: May 22, 2026

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06:51

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Published on: July 21, 2018

Leonurine suppresses renal cell carcinoma progression by targeting the PDK1-mediated Warburg effect

Tiaodi Qian1,2, Xuan Zhou1,2, Jiajie Hu1,2

  • 1Department of Endoscopy Center, Sir Run Run Shaw Hospital, Zhejiang University School of Medicine, Hangzhou, China.

Translational Andrology and Urology
|May 21, 2026
PubMed
Abstract

Insights

Leonurine (Leo) inhibits renal cell carcinoma (RCC) progression by targeting pyruvate dehydrogenase kinase 1 (PDK1), suppressing the Warburg effect, and restricting tumor growth. This study reveals Leo as a novel metabolic inhibitor for RCC treatment.

Area of Science:

  • Oncology
  • Molecular Biology
  • Biochemistry

Background:

  • Leonurine (Leo), a bioactive alkaloid from Leonurus japonicus, shows anti-tumor potential.
  • Its specific role and molecular targets in renal cell carcinoma (RCC) require elucidation.
  • This study offers a novel perspective on Leo's anti-RCC mechanisms.

Purpose of the Study:

  • To investigate the anti-tumor effects of Leonurine (Leo) in renal cell carcinoma (RCC).
  • To identify the molecular targets and metabolic pathways affected by Leo in RCC.
  • To provide insights for developing new anti-RCC drugs.

Main Methods:

  • Evaluated Leo's efficacy in RCC cell lines using CCK-8, colony formation, flow cytometry, and Transwell assays.
  • Identified potential targets via in silico prediction (ChEMBL) and validated using MST, molecular docking, and CETSA.
  • Assessed glycolytic flux and confirmed the PDK1-mediated metabolic axis involvement through rescue experiments and in vivo xenograft models.

Main Results:

  • Leonurine significantly inhibited RCC cell proliferation and migration, inducing apoptosis.
  • Leo directly interacted with pyruvate dehydrogenase kinase 1 (PDK1), downregulating its protein levels.
  • Leo suppressed the Warburg effect, and PDK1 overexpression abrogated Leo's inhibitory effects; in vivo studies confirmed restricted tumor growth.

Conclusions:

  • Leonurine (Leo) acts as a novel metabolic inhibitor in RCC.
  • It targets the PDK1-mediated glycolytic pathway.
  • Leo demonstrates therapeutic potential for renal cell carcinoma treatment.
Keywords:
Leonurine (Leo)glycolysispyruvate dehydrogenase kinase 1 (PDK1)renal cell carcinoma (RCC)

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