In silico and in vitro evaluation of potential agonistic and antagonistic estrogenic and androgenic activities of pure cyanotoxins, microcystin-LR and cylindrospermopsin
The potential endocrine disruption activity of cyanotoxins, particularly their effects on estrogen and androgen receptors (ER, AR), remains poorly understood. In the present study, the potential agonistic/antagonistic estrogenic and androgenic activities of MC-LR and CYN have been determined for the...
| Authors: | , , , , |
|---|---|
| Format: | article |
| Status: | Published version |
| Publication Date: | 2025 |
| Country: | España |
| Institution: | Universidad de Sevilla (US) |
| Repository: | idUS. Depósito de Investigación de la Universidad de Sevilla |
| OAI Identifier: | oai:idus.us.es:11441/172705 |
| Online Access: | https://hdl.handle.net/11441/172705 https://doi.org/10.1016/j.ecoenv.2024.117456 |
| Access Level: | Open access |
| Keyword: | MC-LR CYN Estrogens Androgens Docking |
| Summary: | The potential endocrine disruption activity of cyanotoxins, particularly their effects on estrogen and androgen receptors (ER, AR), remains poorly understood. In the present study, the potential agonistic/antagonistic estrogenic and androgenic activities of MC-LR and CYN have been determined for the first time with validated OECD Test Guidelines No. 455 and 458, respectively. The data show that only MC-LR demonstrated weak estrogenic agonistic effects (LogPC10 value of − 9.85 M), while both toxins displayed antagonistic effects on the ER, with LogIC30 values of − 4.4 and − 6.4 for MC-LR and CYN, respectively. In addition, neither MC-LR nor CYN exhibited agonistic/antagonistic activities in AR. Docking studies revealed potential interactions between both toxins and AR, with CYN showing a higher predicted affinity for this receptor. In vivo studies, particularly those investigating androgen disruption, are warranted to confirm the endocrine disrupting potential of MC-LR and CYN. |
|---|