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...
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Elsevier
2025-01-01
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| Series: | Ecotoxicology and Environmental Safety |
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| Online Access: | http://www.sciencedirect.com/science/article/pii/S014765132401532X |
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| author | Antonio Casas-Rodríguez Antonio Cascajosa-Lira María Puerto Ana María Cameán Angeles Jos |
| author_facet | Antonio Casas-Rodríguez Antonio Cascajosa-Lira María Puerto Ana María Cameán Angeles Jos |
| author_sort | Antonio Casas-Rodríguez |
| collection | DOAJ |
| description | 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. |
| format | Article |
| id | doaj-art-dc20f7882b86402ab77eb91da37fc17a |
| institution | Kabale University |
| issn | 0147-6513 |
| language | English |
| publishDate | 2025-01-01 |
| publisher | Elsevier |
| record_format | Article |
| series | Ecotoxicology and Environmental Safety |
| spelling | doaj-art-dc20f7882b86402ab77eb91da37fc17a2025-01-23T05:25:38ZengElsevierEcotoxicology and Environmental Safety0147-65132025-01-01289117456In silico and in vitro evaluation of potential agonistic and antagonistic estrogenic and androgenic activities of pure cyanotoxins, microcystin-LR and cylindrospermopsinAntonio Casas-Rodríguez0Antonio Cascajosa-Lira1María Puerto2Ana María Cameán3Angeles Jos4Area of Toxicology, Faculty of Pharmacy, University of Sevilla, Profesor García González nº 2, Sevilla 41012, SpainArea of Toxicology, Faculty of Pharmacy, University of Sevilla, Profesor García González nº 2, Sevilla 41012, SpainCorresponding author.; Area of Toxicology, Faculty of Pharmacy, University of Sevilla, Profesor García González nº 2, Sevilla 41012, SpainArea of Toxicology, Faculty of Pharmacy, University of Sevilla, Profesor García González nº 2, Sevilla 41012, SpainArea of Toxicology, Faculty of Pharmacy, University of Sevilla, Profesor García González nº 2, Sevilla 41012, SpainThe 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.http://www.sciencedirect.com/science/article/pii/S014765132401532XMC-LRCYNEstrogensAndrogensDocking |
| spellingShingle | Antonio Casas-Rodríguez Antonio Cascajosa-Lira María Puerto Ana María Cameán Angeles Jos In silico and in vitro evaluation of potential agonistic and antagonistic estrogenic and androgenic activities of pure cyanotoxins, microcystin-LR and cylindrospermopsin Ecotoxicology and Environmental Safety MC-LR CYN Estrogens Androgens Docking |
| title | In silico and in vitro evaluation of potential agonistic and antagonistic estrogenic and androgenic activities of pure cyanotoxins, microcystin-LR and cylindrospermopsin |
| title_full | In silico and in vitro evaluation of potential agonistic and antagonistic estrogenic and androgenic activities of pure cyanotoxins, microcystin-LR and cylindrospermopsin |
| title_fullStr | In silico and in vitro evaluation of potential agonistic and antagonistic estrogenic and androgenic activities of pure cyanotoxins, microcystin-LR and cylindrospermopsin |
| title_full_unstemmed | In silico and in vitro evaluation of potential agonistic and antagonistic estrogenic and androgenic activities of pure cyanotoxins, microcystin-LR and cylindrospermopsin |
| title_short | In silico and in vitro evaluation of potential agonistic and antagonistic estrogenic and androgenic activities of pure cyanotoxins, microcystin-LR and cylindrospermopsin |
| title_sort | in silico and in vitro evaluation of potential agonistic and antagonistic estrogenic and androgenic activities of pure cyanotoxins microcystin lr and cylindrospermopsin |
| topic | MC-LR CYN Estrogens Androgens Docking |
| url | http://www.sciencedirect.com/science/article/pii/S014765132401532X |
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