Institut für Chemie, Karl-Franzens-Universität Graz, Schubertstrasse 1, 8010 Graz, Austria.
Bioorg Med Chem Lett. 2011 Jan 1;21(1):363-5. doi: 10.1016/j.bmcl.2010.10.139. Epub 2010 Nov 5.
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.
已经测试了三种具有增加的硅原子空间位阻保护的稳定硅三醇,以抑制乙酰胆碱酯酶(AChE)。对于所有测试的硅三醇,我们发现其在 100μM 浓度下对 AChE 活性具有可逆抑制作用。对于空间位阻最小的环己基硅三醇,抑制率最高,达到 45%,相对溴化加兰他敏,其 IC50 值为 121±3μM。在抑制相关浓度下,所用硅三醇的细胞毒性可以忽略不计。