Chemopreventive Activities of Sulforaphane and Its Metabolites in Human Hepatoma HepG2 Cells

Peng Liu, Wei Wang, Zhigang Zhou, Andrew J O Smith, Richard P Bowater, Ian Michael Wormstone, Yuqiong Chen, Yongping Bao (Corresponding Author)

Research output: Contribution to journalArticlepeer-review

17 Citations (Scopus)
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Sulforaphane (SFN) exhibits chemopreventive effects through various mechanisms. However, few studies have focused on the bioactivities of its metabolites. Here, three metabolites derived from SFN were studied, known as sulforaphane glutathione, sulforaphane cysteine and sulforaphane-N-acetylcysteine. Their effects on cell viability, DNA damage, tumorigenicity, cell migration and adhesion were measured in human hepatoma HepG2 cells, and their anti-angiogenetic effects were determined in a 3D co-culture model of human umbilical vein endothelial cells (HUVECs) and pericytes. Results indicated that these metabolites at high doses decreased cancer cell viability, induced DNA damage and inhibited motility, and impaired endothelial cell migration and tube formation. Additionally, pre-treatment with low doses of SFN metabolites protected against H₂O₂ challenge. The activation of the nuclear factor E2-related factor 2 (Nrf2)-antioxidant response element (ARE) pathway and the induction of intracellular glutathione (GSH) played an important role in the cytoprotective effects of SFN metabolites. In conclusion, SFN metabolites exhibited similar cytotoxic and cytoprotective effects to SFN, which proves the necessity to study the mechanisms of action of not only SFN but also of its metabolites. Based on the different tissue distribution profiles of these metabolites, the most relevant chemical forms can be selected for targeted chemoprevention.

Original languageEnglish
Article number585
Issue number5
Publication statusPublished - 9 May 2018


  • Acetylcysteine/metabolism
  • Anticarcinogenic Agents/pharmacology
  • Antioxidant Response Elements/drug effects
  • Cell Adhesion/drug effects
  • Cell Movement/drug effects
  • Cell Survival/drug effects
  • Comet Assay
  • DNA Damage/drug effects
  • Dose-Response Relationship, Drug
  • Glutathione/metabolism
  • Hep G2 Cells
  • Human Umbilical Vein Endothelial Cells/drug effects
  • Humans
  • Hydrogen Peroxide/toxicity
  • Isothiocyanates/pharmacology
  • NF-E2-Related Factor 2/genetics
  • Sulforaphane
  • Chemoprevention
  • Sulforaphane metabolites
  • Nrf2
  • GSH


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