In silico and in vitro evaluation of potential agonistic and antagonistic estrogenic and androgenic activities of pure cyanotoxins, microcystin-LR and cylindrospermopsin
Casas Rodríguez, Antonio | Cascajosa Lira, Antonio | Puerto Rodríguez, María | Cameán Fernández, Ana María | Jos Gallego, Ángeles Mencía | Universidad de Sevilla. Departamento de Nutrición y Bromatología, Toxicología y Medicina Legal | Ministerio de Ciencia, Innovación y Universidades (MICINN). España | Agencia Estatal de Investigación. España | European Union (UE)
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.
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