Alkenylboronic acids have shown important biological activities that contribute to neuroprotection. We have determined their influence on the β-amyloid (βA) aggregation process, β-secretase and acethylcholinesterase activities on cell-free systems, on the redox and lipid peroxidation status, and on the vulnerability to apoptotic death in an APPswe neuroblastoma cell line, before and after hydrogen peroxide treatment. We have discovered that 2-arylvinylboronic acids and some of their esters possess a set of properties which makes them highly useful as neuroprotective agents affecting multiple biological targets involved in AD. These properties are not paralleled by the related 2-arylboronic acids.

译文

烯基硼酸已显示出重要的生物活性,可促进神经保护作用。我们已经确定了它们对β-淀粉样蛋白(βA)聚集过程,β-分泌酶和乙酰胆碱酯酶活性对无细胞系统,氧化还原和脂质过氧化状态的影响,以及对APPswe神经母细胞瘤细胞株凋亡死亡的脆弱性的影响,过氧化氢处理前后。我们已经发现2-芳基乙烯基硼酸及其某些酯具有一组特性,这使得它们非常有用地用作影响涉及AD的多个生物学靶标的神经保护剂。这些性能是相关的2-芳基硼酸无法比拟的。

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