Assessing the receptor-mediated activity of PAHs using AhR-, ERα- and PPARγ- CALUX bioassays
Autor: | Marc Elskens, E. Van Hoeck, Imke Boonen, Heidi Demaegdt, K. Van Langenhove, A. Van Heyst, M.S. Denison, Birgit Mertens |
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Přispěvatelé: | Faculty of Sciences and Bioengineering Sciences, Chemistry, Analytical, Environmental & Geo-Chemistry, R&D centraal, Mathematics, Operational Research, Statistics and Information Systems for Management, Experimental Pharmacology |
Jazyk: | angličtina |
Rok vydání: | 2020 |
Předmět: |
Agonist
Chrysene medicine.drug_class Toxicology 03 medical and health sciences chemistry.chemical_compound Mice 0404 agricultural biotechnology Cell Line Tumor medicine CALUX Animals Humans Polycyclic Aromatic Hydrocarbons Carcinogen 030304 developmental biology Fluoranthene 0303 health sciences Anthracene Estrogen Receptor alpha 04 agricultural and veterinary sciences General Medicine Phenanthrene 040401 food science Rats PPAR gamma chemistry Biochemistry Receptors Aryl Hydrocarbon Pyrene Biological Assay Food Science Signal Transduction |
DOI: | 10.1016/j.fct.2020.111602 |
Popis: | Polycyclic aromatic hydrocarbons (PAH) are a complex group of organic compounds, consisting of at least three fused aromatic rings, which are formed during combustion of organic matter. While some PAHs have been reported to have carcinogenic and/or mutagenic properties, another possible negative health impact is their endocrine disrupting potential. Therefore, the aim of this study was to determine both the agonistic and antagonistic endocrine activity of 9 environmentally relevant PAHs using three different CALUX bioassays: The AhR-CALUX, The ERα-CALUX and PPARγ-CALUX. For the PPARγ-CALUX anthracene, fluoranthene, pyrene and fluorene showed weak agonistic activity, whilst benzo(a)pyrene (B(a)P) was the only one exhibiting weak antagonistic activity. For the AhR-CALUX, chrysene was the only PAH that showed relatively strong agonist activity (except for B(a)P which was used as a standard). Pyrene, anthracene and fluoranthene showed weak AhR agonist activity. In the ERα-CALUX bioassay, fluoranthene had agonistic activity whilst B(a)P exhibited both agonistic and antagonistic activity (lowering E2 activity by 30%). Phenanthrene and anthracene had weak ERα agonist activities. These results indicate that certain PAHs have multiple modes of action and can activate/inhibit multiple receptor signaling pathways known to play critical roles in mediating endocrine disruption. |
Databáze: | OpenAIRE |
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