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

Chao Zhang, Tiziana Schilirò, Marta Gea, Silvia Bianchi, Angelo Spinello, Alessandra Magistrato, Gianfranco Gilardi and Giovanna Di Nardo
Additional contact information
Chao Zhang: Department of Life Sciences and Systems Biology, University of Torino, 10123 Torino, Italy
Tiziana Schilirò: Department of Public Health and Pediatrics, University of Torino, 10126 Torino, Italy
Marta Gea: Department of Public Health and Pediatrics, University of Torino, 10126 Torino, Italy
Silvia Bianchi: Department of Life Sciences and Systems Biology, University of Torino, 10123 Torino, Italy
Angelo Spinello: National Research Council-Institute of Materials (CNR-IOM) at International School for Advanced Studies (SISSA), 34165 Trieste, Italy
Alessandra Magistrato: National Research Council-Institute of Materials (CNR-IOM) at International School for Advanced Studies (SISSA), 34165 Trieste, Italy
Gianfranco Gilardi: Department of Life Sciences and Systems Biology, University of Torino, 10123 Torino, Italy
Giovanna Di Nardo: Department of Life Sciences and Systems Biology, University of Torino, 10123 Torino, Italy

IJERPH, 2020, vol. 17, issue 16, 1-18

Abstract: 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 17β-estradiol, thiacloprid and imidacloprid induced an estrogenic activity at the highest concentrations tested with a relative potency of 5.4 × 10 −10 and 3.7 × 10 −9 , respectively. Molecular dynamics and docking simulations predicted the potential binding sites and the binding mode of the three pesticides on the structure of the two key targets, providing a rational for their mechanism as EDCs. The results demonstrate that the three pesticides are potential EDCs as glyphosate acts as an aromatase inhibitor, whereas imidacloprid and thiacloprid can interfere with estrogen induced signaling.

Keywords: aromatase; estrogen receptor; endocrine disrupting chemical; pesticides; neonicotinoids; estrogenic activity; gene reporter assay; MELN allosteric inhibition; molecular dynamics (search for similar items in EconPapers)
JEL-codes: I I1 I3 Q Q5 (search for similar items in EconPapers)
Date: 2020
References: View references in EconPapers View complete reference list from CitEc
Citations: View citations in EconPapers (5)

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