Silanetriols as in vitro inhibitors for AChE

Three stable silanetriols with increasing steric protection of the silicon atom have been tested for inhibition of acetylcholinesterase (AChE). For all tested silanetriols we found reversible inhibition of the AChE activity at a 100 μM concentration. The highest inhibition rate was found for the ste...

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Detalles Bibliográficos
Autores principales: Blunder, Martina, Hurkes, Natascha, Spirk, Stefan, List, Martina, Pietschnig, Rudolf
Formato: Texto
Lenguaje:English
Publicado: Elsevier Science Ltd 2011
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3013380/
https://www.ncbi.nlm.nih.gov/pubmed/21111617
http://dx.doi.org/10.1016/j.bmcl.2010.10.139
Descripción
Sumario:Three stable silanetriols with increasing steric protection of the silicon atom have been tested for inhibition of acetylcholinesterase (AChE). For all tested silanetriols we found reversible inhibition of the AChE activity at a 100 μM concentration. The highest inhibition rate was found for the sterically least hindered cyclohexylsilanetriol with 45% inhibition relative to galanthamine hydrobromide for which an IC(50) value of 121 ± 3 μM was determined as well. The cytotoxicity of the silanetriols used was found to be negligible at concentrations relevant for inhibition.

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