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新型 1,2,4-三嗪衍生物的合成及体外评价作为神经保护剂。

Synthesis and in vitro evaluation of novel 1,2,4-triazine derivatives as neuroprotective agents.

机构信息

Department of Medicinal Chemistry, Faculty of Pharmacy, and Drug Design & Development Research Center, Tehran University of Medical Sciences, Tehran, Iran.

出版信息

Bioorg Med Chem. 2010 Jun 15;18(12):4224-30. doi: 10.1016/j.bmc.2010.04.097. Epub 2010 May 8.

Abstract

The role of novel triazine derivatives against oxidative stress exerted by hydrogen peroxide on differentiated rat pheochromocytoma (PC12) cell line was examined and a consistent protection from H(2)O(2)-induced cell death, associated with a marked reduction in caspase-3 activation, was observed. Moreover, activation of NF-kappaB, a known regulator of a host of genes that involves in specific stress and inflammatory responses by H(2)O(2), was greatly impaired by triazine pretreatment in differentiated PC12 cells. Neuroprotective effect of such compounds may represent a promising approach for treatment of neurodegenerative diseases.

摘要

研究了新型三嗪衍生物对过氧化氢引起的分化大鼠嗜铬细胞瘤(PC12)细胞系氧化应激的作用,观察到其对 H ₂ O₂ 诱导的细胞死亡具有一致的保护作用,同时伴有 caspase-3 激活的显著减少。此外,三嗪预处理可显著抑制 NF-κB 的激活,NF-κB 是一种已知的调节因子,可调节 H₂ O₂ 引起的特定应激和炎症反应中的一系列基因。这种化合物的神经保护作用可能代表了治疗神经退行性疾病的一种有前途的方法。

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