Reduction of stress responses in honey bees by synthetic ligands targeting an allatostatin receptor
Abstract Honey bees are of great economic and ecological importance, but are facing multiple stressors that can jeopardize their pollination efficiency and survival. Therefore, understanding the physiological bases of their stress response may help defining treatments to improve their resilience. We...
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| Format: | Article |
| Language: | English |
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Nature Portfolio
2022-10-01
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| Series: | Scientific Reports |
| Online Access: | https://doi.org/10.1038/s41598-022-20978-y |
| _version_ | 1811194827256102912 |
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| author | Adrià Sánchez-Morales Véronique Gigoux Minos-Timotheos Matsoukas Laura Perez-Benito Daniel Fourmy Ramón Alibes Félix Busqué Arnau Cordomí Jean-Marc Devaud |
| author_facet | Adrià Sánchez-Morales Véronique Gigoux Minos-Timotheos Matsoukas Laura Perez-Benito Daniel Fourmy Ramón Alibes Félix Busqué Arnau Cordomí Jean-Marc Devaud |
| author_sort | Adrià Sánchez-Morales |
| collection | DOAJ |
| description | Abstract Honey bees are of great economic and ecological importance, but are facing multiple stressors that can jeopardize their pollination efficiency and survival. Therefore, understanding the physiological bases of their stress response may help defining treatments to improve their resilience. We took an original approach to design molecules with this objective. We took advantage of the previous identified neuropeptide allatostatin A (ASTA) and its receptor (ASTA-R) as likely mediators of the honey bee response to a biologically relevant stressor, exposure to an alarm pheromone compound. A first series of ASTA-R ligands were identified through in silico screening using a homology 3D model of the receptor and in vitro binding experiments. One of these (A8) proved also efficient in vivo, as it could counteract two behavioral effects of pheromone exposure, albeit only in the millimolar range. This putative antagonist was used as a template for the chemical synthesis of a second generation of potential ligands. Among these, two compounds showed improved efficiency in vivo (in the micromolar range) as compared to A8 despite no major improvement in their affinity for the receptor in vitro. These new ligands are thus promising candidates for alleviating stress in honey bees. |
| first_indexed | 2024-04-12T00:34:01Z |
| format | Article |
| id | doaj.art-5ff99a956aef4b80a9f931d76725ad60 |
| institution | Directory Open Access Journal |
| issn | 2045-2322 |
| language | English |
| last_indexed | 2024-04-12T00:34:01Z |
| publishDate | 2022-10-01 |
| publisher | Nature Portfolio |
| record_format | Article |
| series | Scientific Reports |
| spelling | doaj.art-5ff99a956aef4b80a9f931d76725ad602022-12-22T03:55:14ZengNature PortfolioScientific Reports2045-23222022-10-0112111410.1038/s41598-022-20978-yReduction of stress responses in honey bees by synthetic ligands targeting an allatostatin receptorAdrià Sánchez-Morales0Véronique Gigoux1Minos-Timotheos Matsoukas2Laura Perez-Benito3Daniel Fourmy4Ramón Alibes5Félix Busqué6Arnau Cordomí7Jean-Marc Devaud8Departament de Química, Universitat Autònoma de BarcelonaCentre de Recherches en Cancérologie de Toulouse (CRCT), INSERM Unité Mixte de Recherche UMR-1037, CNRS Equipe de Recherche Labellisée ERL5294, Université de ToulouseUnitat de Bioestadística, Universitat Autònoma de BarcelonaUnitat de Bioestadística, Universitat Autònoma de BarcelonaCentre de Recherches en Cancérologie de Toulouse (CRCT), INSERM Unité Mixte de Recherche UMR-1037, CNRS Equipe de Recherche Labellisée ERL5294, Université de ToulouseDepartament de Química, Universitat Autònoma de BarcelonaDepartament de Química, Universitat Autònoma de BarcelonaUnitat de Bioestadística, Universitat Autònoma de BarcelonaCentre de Recherches Sur La Cognition Animale (CRCA), Centre de Biologie Intégrative, 9 (CBI), Université de Toulouse, CNRSAbstract Honey bees are of great economic and ecological importance, but are facing multiple stressors that can jeopardize their pollination efficiency and survival. Therefore, understanding the physiological bases of their stress response may help defining treatments to improve their resilience. We took an original approach to design molecules with this objective. We took advantage of the previous identified neuropeptide allatostatin A (ASTA) and its receptor (ASTA-R) as likely mediators of the honey bee response to a biologically relevant stressor, exposure to an alarm pheromone compound. A first series of ASTA-R ligands were identified through in silico screening using a homology 3D model of the receptor and in vitro binding experiments. One of these (A8) proved also efficient in vivo, as it could counteract two behavioral effects of pheromone exposure, albeit only in the millimolar range. This putative antagonist was used as a template for the chemical synthesis of a second generation of potential ligands. Among these, two compounds showed improved efficiency in vivo (in the micromolar range) as compared to A8 despite no major improvement in their affinity for the receptor in vitro. These new ligands are thus promising candidates for alleviating stress in honey bees.https://doi.org/10.1038/s41598-022-20978-y |
| spellingShingle | Adrià Sánchez-Morales Véronique Gigoux Minos-Timotheos Matsoukas Laura Perez-Benito Daniel Fourmy Ramón Alibes Félix Busqué Arnau Cordomí Jean-Marc Devaud Reduction of stress responses in honey bees by synthetic ligands targeting an allatostatin receptor Scientific Reports |
| title | Reduction of stress responses in honey bees by synthetic ligands targeting an allatostatin receptor |
| title_full | Reduction of stress responses in honey bees by synthetic ligands targeting an allatostatin receptor |
| title_fullStr | Reduction of stress responses in honey bees by synthetic ligands targeting an allatostatin receptor |
| title_full_unstemmed | Reduction of stress responses in honey bees by synthetic ligands targeting an allatostatin receptor |
| title_short | Reduction of stress responses in honey bees by synthetic ligands targeting an allatostatin receptor |
| title_sort | reduction of stress responses in honey bees by synthetic ligands targeting an allatostatin receptor |
| url | https://doi.org/10.1038/s41598-022-20978-y |
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