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Article

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

by
Chao Zhang
1,
Tiziana Schilirò
2,
Marta Gea
2,
Silvia Bianchi
1,
Angelo Spinello
3,
Alessandra Magistrato
3,
Gianfranco Gilardi
1 and
Giovanna Di Nardo
1,*
1
Department of Life Sciences and Systems Biology, University of Torino, 10123 Torino, Italy
2
Department of Public Health and Pediatrics, University of Torino, 10126 Torino, Italy
3
National Research Council-Institute of Materials (CNR-IOM) at International School for Advanced Studies (SISSA), 34165 Trieste, Italy
*
Author to whom correspondence should be addressed.
Int. J. Environ. Res. Public Health 2020, 17(16), 5664; https://doi.org/10.3390/ijerph17165664
Submission received: 10 July 2020 / Revised: 1 August 2020 / Accepted: 3 August 2020 / Published: 5 August 2020
(This article belongs to the Special Issue Endocrine Disruptor Chemicals and Estrogenic Activity in the Context of Health Risk Assessment)
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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 aromatase; estrogen receptor; endocrine disrupting chemical; pesticides; neonicotinoids; estrogenic activity; gene reporter assay; MELN allosteric inhibition; molecular dynamics
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MDPI and ACS Style

Zhang, C.; Schilirò, T.; Gea, M.; Bianchi, S.; Spinello, A.; Magistrato, A.; Gilardi, G.; Di Nardo, G. Molecular Basis for Endocrine Disruption by Pesticides Targeting Aromatase and Estrogen Receptor. Int. J. Environ. Res. Public Health 2020, 17, 5664. https://doi.org/10.3390/ijerph17165664

AMA Style

Zhang C, Schilirò T, Gea M, Bianchi S, Spinello A, Magistrato A, Gilardi G, Di Nardo G. Molecular Basis for Endocrine Disruption by Pesticides Targeting Aromatase and Estrogen Receptor. International Journal of Environmental Research and Public Health. 2020; 17(16):5664. https://doi.org/10.3390/ijerph17165664

Chicago/Turabian Style

Zhang, Chao, Tiziana Schilirò, Marta Gea, Silvia Bianchi, Angelo Spinello, Alessandra Magistrato, Gianfranco Gilardi, and Giovanna Di Nardo. 2020. "Molecular Basis for Endocrine Disruption by Pesticides Targeting Aromatase and Estrogen Receptor" International Journal of Environmental Research and Public Health 17, no. 16: 5664. https://doi.org/10.3390/ijerph17165664

APA Style

Zhang, C., Schilirò, T., Gea, M., Bianchi, S., Spinello, A., Magistrato, A., Gilardi, G., & Di Nardo, G. (2020). Molecular Basis for Endocrine Disruption by Pesticides Targeting Aromatase and Estrogen Receptor. International Journal of Environmental Research and Public Health, 17(16), 5664. https://doi.org/10.3390/ijerph17165664

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