高效合成及首次区域选择性 C-6 直接芳基化咪唑并[2,1-c][1,2,4]三嗪骨架及其在 HO 诱导氧化应激中的评价。
Efficient synthesis and first regioselective C-6 direct arylation of imidazo[2,1-c][1,2,4]triazine scaffold and their evaluation in HO-induced oxidative stress.
机构信息
Institut de Chimie Organique et Analytique, Université d'Orléans, UMR-CNRS 7311, BP 6759, rue de Chartres, 45067, Orléans Cedex 2, France; Equipe de Chimie Bioorganique & Analytique, URAC 22 Université Hassan II Mohammedia-Casablanca, BP 146, 28800, Mohammedia, Morocco.
Institut de Chimie Organique et Analytique, Université d'Orléans, UMR-CNRS 7311, BP 6759, rue de Chartres, 45067, Orléans Cedex 2, France; Laboratoire de Chimie Organique et Analytique, Université Sultan Moulay Slimane - Faculté des Sciences et Techniques, BP 523, 23000, Beni-Mellal, Morocco.
出版信息
Eur J Med Chem. 2018 Feb 10;145:113-123. doi: 10.1016/j.ejmech.2017.12.081. Epub 2017 Dec 27.
Oxidative stress and apoptosis are both associated with various acute and chronic disorders. Thus, the aim of the present study is to synthesize imidazo[2,1-c][1,2,4]triazines derivatives and to evaluate their effects in HO-induced oxidative stress in human neuroblastoma cell line (SH-SY5Y cells). The effects of the compounds on cell viability were measured by MTT assay and the changes in stress and apoptosis-related proteins were investigated by PathScan Stress and Apoptosis Signaling Antibody Array kit and Western Blot technique. In particular, four compounds were found to protect SH-SY5Y cells from HO-induced toxicity by increasing Bcl-2/Bax ratio, regulating PI3-K/Akt cascade and inhibiting the ERK pathway.
氧化应激和细胞凋亡都与各种急性和慢性疾病有关。因此，本研究的目的是合成咪唑并[2,1-c][1,2,4]三嗪衍生物，并评估它们在 HO 诱导的人神经母细胞瘤细胞系 (SH-SY5Y 细胞) 氧化应激中的作用。通过 MTT 测定法测量化合物对细胞活力的影响，并通过 PathScan 应激和细胞凋亡信号转导抗体阵列试剂盒和 Western Blot 技术研究应激和凋亡相关蛋白的变化。特别地，发现四种化合物通过增加 Bcl-2/Bax 比值、调节 PI3-K/Akt 级联和抑制 ERK 途径来保护 SH-SY5Y 细胞免受 HO 诱导的毒性。
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