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 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.
Institut für Chemie, Karl-Franzens-Universität Graz, Schubertstrasse 1, 8010 Graz, Austria.
Martina
M
Blunder
Natascha
N
Hurkes
Stefan
S
Spirk
Martina
M
List
Rudolf
R
Pietschnig
D000110:Acetylcholinesterase / Q000737:chemistry* / Q000378:metabolism; D002460:Cell Line; D002800:Cholinesterase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000633:toxicity; D006801:Humans; D017646:Organosilicon Compounds / Q000737:chemistry* / Q000633:toxicity; D012821:Silanes / Q000737:chemistry*
D002800:Cholinesterase Inhibitors; D017646:Organosilicon Compounds; D012821:Silanes; C082343:silanol; D000110:Acetylcholinesterase