Back to Search
Start Over
Cytotoxicity of hexahelicene and its effect on the aryl hydrocarbon receptor pathway
- Source :
- Toxicology in vitro : an international journal published in association with BIBRA. 57
- Publication Year :
- 2018
-
Abstract
- Carbohelicenes are a group of helical-shaped polycyclic aromatic hydrocarbons. This study examined the effect of hexahelicene (or [6]helicene) and of its imidazolium derivative, 1-butyl-3-(2-methyl[6]helicenyl)-imidazolium bromide (I[6]H), on the activity of the aryl hydrocarbon receptor (AhR) and expression of cytochrome P450 1A1 (CYP1A1) in human hepatoma HepG2 cells. An MTT viability assay showed that both [6]helicene and I[6]H were cytotoxic to HepG2 cells after 24 h of exposure, with IC50 values of 0.9 and 8.4 μM, respectively. Using a gene reporter assay performed in transiently transfected HepG2 cells, we found that 1 μM [6]helicene, unlike I[6]H, significantly increased the activity of AhR to 2.1-fold compared to the control after 24 h of exposure. Moreover, [6]helicene induced a small but significant increase in the level of CYP1A1 mRNA. On the other hand, neither the protein level nor activity of CYP1A1 were affected by [6]helicene in HepG2 cells. The effect of [6]helicene on the AhR pathway was thus much lower than that of 2,3,7,8-tetrachlorodibenzo-p-dioxin, a potent AhR activator. We conclude that [6]helicene is a poor activator of the AhR pathway in HepG2 cells, and that the possible activation of the AhR pathway in vivo remains to be investigated.
- Subjects :
- 0301 basic medicine
Toxicology
03 medical and health sciences
chemistry.chemical_compound
0302 clinical medicine
Cytochrome P-450 CYP1A1
Cytotoxic T cell
Humans
Polycyclic Compounds
Viability assay
Cytotoxicity
biology
Activator (genetics)
Imidazoles
Cytochrome P450
General Medicine
Transfection
Hep G2 Cells
respiratory system
Aryl hydrocarbon receptor
Molecular biology
030104 developmental biology
Helicene
chemistry
Receptors, Aryl Hydrocarbon
030220 oncology & carcinogenesis
biology.protein
Signal Transduction
Subjects
Details
- ISSN :
- 18793177
- Volume :
- 57
- Database :
- OpenAIRE
- Journal :
- Toxicology in vitro : an international journal published in association with BIBRA
- Accession number :
- edsair.doi.dedup.....88029d4c9a866aefe859f775ea5ced24