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Dihydroartemisinin represses esophageal cancer glycolysis by down-regulating pyruvate kinase M2

Shumin Li1, Peng Huang1, Junqing Gan1

  • 1Department of Gastrointestinal Oncology, Harbin Medical University Cancer Hospital, Harbin, Heilongjiang, 150081, PR China.

European Journal of Pharmacology
|April 21, 2019
PubMed

Insights

Dihydroartemisinin (DHA) shows promise against esophageal squamous cell carcinoma (ESCC) by inhibiting cancer cell glycolysis. This novel therapy targets pyruvate kinase M2 (PKM2), a key factor in ESCC progression.

Area of Science:

  • Oncology
  • Biochemistry
  • Pharmacology

Background:

  • Esophageal squamous cell carcinoma (ESCC) poses a significant health burden, particularly in China, with limited treatment options.
  • Previous research indicated dihydroartemisinin (DHA) possesses anticancer properties against esophageal cancer, but the underlying mechanisms remain unclear.
  • Cancer cells often exhibit altered metabolism, including enhanced glycolysis (the Warburg effect), which supports rapid proliferation.

Purpose of the Study:

  • To investigate the effect of dihydroartemisinin (DHA) on cancer cell glycolysis in esophageal squamous cell carcinoma (ESCC).
  • To explore the role of pyruvate kinase M2 (PKM2), a key regulator of glycolysis, in the context of DHA treatment for ESCC.
  • To determine if targeting PKM2 mediates the anti-glycolytic effects of DHA in ESCC.

Main Methods:

  • Assessed the expression levels of pyruvate kinase M2 (PKM2) in ESCC patient samples and cell lines.
  • Treated ESCC cells with dihydroartemisinin (DHA) and measured changes in PKM2 expression, glucose uptake, and lactate production.
  • Utilized lentiviral transfection to overexpress PKM2 in ESCC cells to evaluate its impact on DHA's inhibitory effects.

Main Results:

  • Pyruvate kinase M2 (PKM2) was found to be significantly overexpressed in ESCC patients and cell lines.
  • DHA treatment led to down-regulation of PKM2, reduced glucose uptake, and inhibited lactate production in ESCC cells.
  • Overexpression of PKM2 counteracted the inhibitory effects of DHA on glycolysis, suggesting PKM2 mediates DHA's action.

Conclusions:

  • Dihydroartemisinin (DHA) exhibits anti-glycolytic effects in esophageal squamous cell carcinoma (ESCC) partly through the down-regulation of pyruvate kinase M2 (PKM2).
  • Targeting PKM2 represents a potential therapeutic strategy for managing ESCC.
  • DHA holds promise as a prospective therapeutic agent for esophageal cancer treatment.
Keywords:
DihydroartemisininEsophageal cancerGlycolysisPyruvate kinase M2

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