Identification of key pathways involved in the toxic response of the cyanobacterial toxin cylindrospermopsin in human hepatic HepaRG cells

Toxicol In Vitro. 2019 Aug:58:69-77. doi: 10.1016/j.tiv.2019.03.023. Epub 2019 Mar 21.

Abstract

The hepatotoxin cylindrospermopsin (CYN) has been involved in cases of poisoning in humans following ingestion. As its liver toxicity process is complex, we studied the transcriptomic profile of HepaRG cells exposed to CYN. The affected pathways were confirmed through the expression of key genes and the investigation of toxicity markers. In addition, CYP450 activities and cell redox homeostasis were investigated following acute and repeated exposure. CYN induced the down-regulation of genes involved in xenobiotic metabolism and cell cycle progression. There was cell cycle disturbance characterised by an accumulation of G1/S and G2/M cells and an increase in phospho-H3-positive cells. This was linked to the induction of DNA damage demonstrated by an increase in γH2AX-positive cells as well as an accumulation of sub-G1 cells indicating apoptosis but not involving caspase-3. While glutathione (GSH) content sharply decreased following acute exposure to CYN, it increased following repeated exposure, reflecting an adaptive response of cell redox homeostasis. However, our data also suggested that CYN induced the down-regulation of phase I and II metabolism gene products, and CYP450 activities were affected following both acute and repeated exposure to CYN. Our study indicated that repeated exposure of liver cells to low concentrations of CYN may affect their detoxification capacities.

Keywords: Cell cycle; Cylindrospermopsin; Hepatotoxicity; Transcriptomic; Xenobiotic metabolism.

MeSH terms

  • Alkaloids
  • Bacterial Toxins / toxicity*
  • Cell Cycle / drug effects
  • Cell Line
  • Cyanobacteria
  • Cyanobacteria Toxins
  • Cytochrome P-450 Enzyme System / metabolism
  • DNA Damage
  • Glutathione / metabolism
  • Hepatocytes / drug effects*
  • Hepatocytes / metabolism
  • Humans
  • Metabolic Networks and Pathways / drug effects
  • Transcriptome / drug effects
  • Uracil / analogs & derivatives*
  • Uracil / toxicity

Substances

  • Alkaloids
  • Bacterial Toxins
  • Cyanobacteria Toxins
  • cylindrospermopsin
  • Uracil
  • Cytochrome P-450 Enzyme System
  • Glutathione