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RESEARCH PRODUCT

Molecular Basis for Endocrine Disruption by Pesticides Targeting Aromatase and Estrogen Receptor

Angelo SpinelloTiziana SchiliròChao ZhangAlessandra MagistratoGianfranco GilardiMarta GeaSilvia BianchiGiovanna Di Nardo

subject

aromatasemedicine.drug_classHealth Toxicology and Mutagenesislcsh:MedicineEstrogen receptorMixed inhibitionEndocrine Disruptors010501 environmental sciencesPharmacology01 natural sciencesArticle03 medical and health scienceschemistry.chemical_compoundImidaclopridReceptorsmedicineHumansAromataseestrogenic activity030304 developmental biology0105 earth and related environmental sciences0303 health sciencesAromatase inhibitorendocrine disrupting chemicalbiologyAromatase Inhibitorslcsh:RPublic Health Environmental and Occupational HealthEstrogenspesticidesPesticideThiaclopridEstrogenmolecular dynamicsReceptors EstrogenchemistryEstrogenMELN allosteric inhibitionbiology.proteingene reporter assayAromatase; Endocrine disrupting chemical; Estrogen receptor; Estrogenic activity; Gene reporter assay; MELN allosteric inhibition; Molecular dynamics; Neonicotinoids; Pesticides; Aromatase; Aromatase Inhibitors; Estrogens; Humans; Receptors Estrogen; Endocrine Disruptors; Pesticidesneonicotinoidsestrogen receptor

description

The intensive use of pesticides has led to their increasing presence in water, soil, and agricultural products. Mounting evidence indicates that some pesticides may be endocrine disrupting chemicals (EDCs), being therefore harmful for the human health and the environment. In this study, three pesticides, glyphosate, thiacloprid, and imidacloprid, were tested for their ability to interfere with estrogen biosynthesis and/or signaling, to evaluate their potential action as EDCs. Among the tested compounds, only glyphosate inhibited aromatase activity (up to 30%) via a non-competitive inhibition or a mixed inhibition mechanism depending on the concentration applied. Then, the ability of the three pesticides to induce an estrogenic activity was tested in MELN cells. When compared to 17&beta

yearjournalcountryeditionlanguage
2020-08-05International Journal of Environmental Research and Public Health
https://doi.org/10.3390/ijerph17165664