Department of Chemical Biology, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China.
Bioorg Med Chem Lett. 2013 Jul 1;23(13):3700-3. doi: 10.1016/j.bmcl.2013.05.016. Epub 2013 May 16.
E-3,4-Dihydroxy styryl aralkyl ketones as well as their 3,4-diacetylated derivatives as the analogues of neuroprotective agent CAPE were designed and synthesized for improving stability and lipid solubility. The neuroprotective activities of target compounds 10a-g and 11a-g were tested by three models in vitro, including 1,1-diphenyl-2-picrylhydrazyl radical scavenging capacity, neuronal protecting effect against damage induced by H2O2 in PC12 cells and nitric oxide suppression effect in BV2 microglial cells. The results demonstrated that compounds 10f and 11f exhibited the most potent neuroprotective effect against oxidative stress and inflammation, which is higher than that of the lead compound CAPE.
E-3,4-二羟基苯乙烯芳烷基酮及其 3,4-二乙酰化衍生物作为神经保护剂 CAPE 的类似物被设计和合成，以提高其稳定性和脂溶性。目标化合物 10a-g 和 11a-g 的神经保护活性通过三种体外模型进行测试，包括 1,1-二苯基-2-苦基肼自由基清除能力、PC12 细胞中过氧化氢诱导的神经元保护作用和 BV2 小胶质细胞中一氧化氮抑制作用。结果表明，化合物 10f 和 11f 对氧化应激和炎症具有最强的神经保护作用，高于先导化合物 CAPE。
