Synergistic anti-cancer effects of galangin and berberine through apoptosis induction and proliferation inhibition in oesophageal carcinoma cells

Biomed Pharmacother. 2016 Dec:84:1748-1759. doi: 10.1016/j.biopha.2016.10.111. Epub 2016 Nov 18.


Galangin is an active pharmacological ingredient from propolis and Alpinia officinarum Hance, and has been reported to have anti-cancer and antioxidative properties. Berberine, a major component of Berberis vulgaris extract, exhibits potent anti-cancer activities through distinct molecular mechanisms. However, the anticancer effect of galangin in combination with berberine is still unknown. In the present study, we demonstrated that the combination of galangin with berberine synergistically resulted in cell growth inhibition, apoptosis and cell cycle arrest at G2/M phase with the increased intracellular reactive oxygen species (ROS) levels in oesophageal carcinoma cells. Pretreatment with ROS scavenger promoted the apoptosis dramatically induced by co-treatment with galangin and berberine. Treatment with galangin and berberine alone caused the decreased expressions of Wnt3a and β-catenin. Interestingly, combination of galangin with berberine could further suppress Wnt3a and β-catenin expression and induce apoptosis in cancer cells. Additionally, in nude mice with xenograft tumors, the combinational treatment of galangin and berberine significantly inhibited the tumor growth without obvious toxicity. Overall, galangin in combination with berberine presented outstanding synergistic anticancer role in vitro and in vivo, indicating that the beneficial combination of galangin and berberine might provide a promising treatment for patients with oesophageal carcinoma.

Keywords: Berberine; Combination; Galangin; Oesophageal carcinoma.

MeSH terms

  • Animals
  • Antineoplastic Combined Chemotherapy Protocols / pharmacology*
  • Apoptosis / drug effects*
  • Berberine / pharmacology*
  • Carcinoma, Squamous Cell / drug therapy*
  • Carcinoma, Squamous Cell / genetics
  • Carcinoma, Squamous Cell / metabolism
  • Carcinoma, Squamous Cell / pathology
  • Cell Line, Tumor
  • Cell Proliferation / drug effects*
  • Dose-Response Relationship, Drug
  • Drug Synergism
  • Esophageal Neoplasms / drug therapy*
  • Esophageal Neoplasms / genetics
  • Esophageal Neoplasms / metabolism
  • Esophageal Neoplasms / pathology
  • Esophageal Squamous Cell Carcinoma
  • Flavonoids / pharmacology*
  • G2 Phase Cell Cycle Checkpoints
  • Humans
  • Male
  • Mice, Inbred BALB C
  • Mice, Nude
  • Oxidative Stress / drug effects
  • RNA Interference
  • Reactive Oxygen Species / metabolism
  • Time Factors
  • Transfection
  • Tumor Burden / drug effects
  • Wnt Signaling Pathway / drug effects
  • Wnt3A Protein / genetics
  • Wnt3A Protein / metabolism
  • Xenograft Model Antitumor Assays
  • beta Catenin / genetics
  • beta Catenin / metabolism


  • CTNNB1 protein, human
  • Flavonoids
  • Reactive Oxygen Species
  • WNT3A protein, human
  • Wnt3A Protein
  • beta Catenin
  • Berberine
  • galangin