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

Author

Listed:
  • 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)

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.

Suggested Citation

  • Chao Zhang & Tiziana Schilirò & Marta Gea & Silvia Bianchi & Angelo Spinello & Alessandra Magistrato & Gianfranco Gilardi & Giovanna Di Nardo, 2020. "Molecular Basis for Endocrine Disruption by Pesticides Targeting Aromatase and Estrogen Receptor," IJERPH, MDPI, vol. 17(16), pages 1-18, August.
    • Handle: RePEc:gam:jijerp:v:17:y:2020:i:16:p:5664-:d:395043
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    References listed on IDEAS

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    1. Francisco Sánchez-Bayo & Henk A. Tennekes, 2020. "Time-Cumulative Toxicity of Neonicotinoids: Experimental Evidence and Implications for Environmental Risk Assessments," IJERPH, MDPI, vol. 17(5), pages 1-20, March.
    2. Wissem Mnif & Aziza Ibn Hadj Hassine & Aicha Bouaziz & Aghleb Bartegi & Olivier Thomas & Benoit Roig, 2011. "Effect of Endocrine Disruptor Pesticides: A Review," IJERPH, MDPI, vol. 8(6), pages 1-39, June.
    3. Nicolas Defarge & Eszter Takács & Verónica Laura Lozano & Robin Mesnage & Joël Spiroux de Vendômois & Gilles-Eric Séralini & András Székács, 2016. "Co-Formulants in Glyphosate-Based Herbicides Disrupt Aromatase Activity in Human Cells below Toxic Levels," IJERPH, MDPI, vol. 13(3), pages 1-17, February.
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    Cited by:

    1. Monica Lopes-Ferreira & Adolfo Luis Almeida Maleski & Leticia Balan-Lima & Jefferson Thiago Gonçalves Bernardo & Lucas Marques Hipolito & Ana Carolina Seni-Silva & Joao Batista-Filho & Maria Alice Pim, 2022. "Impact of Pesticides on Human Health in the Last Six Years in Brazil," IJERPH, MDPI, vol. 19(6), pages 1-19, March.
    2. Marta Gea & Chao Zhang & Roberta Tota & Gianfranco Gilardi & Giovanna Di Nardo & Tiziana Schilirò, 2022. "Assessment of Five Pesticides as Endocrine-Disrupting Chemicals: Effects on Estrogen Receptors and Aromatase," IJERPH, MDPI, vol. 19(4), pages 1-10, February.
    3. Neeranuch Suwannarin & Tippawan Prapamontol & Tomohiko Isobe & Yukiko Nishihama & Yuki Hashimoto & Ampica Mangklabruks & Tawiwan Pantasri & Somporn Chantara & Warangkana Naksen & Shoji F. Nakayama, 2021. "Exposure to Organophosphate and Neonicotinoid Insecticides and Its Association with Steroid Hormones among Male Reproductive-Age Farmworkers in Northern Thailand," IJERPH, MDPI, vol. 18(11), pages 1-16, May.
    4. Lucia Coppola & Sabrina Tait & Enrica Fabbrizi & Monia Perugini & Cinzia La Rocca, 2022. "Comparison of the Toxicological Effects of Pesticides in Non-Tumorigenic MCF-12A and Tumorigenic MCF-7 Human Breast Cells," IJERPH, MDPI, vol. 19(8), pages 1-18, April.

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