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Monoamine oxidase inhibition by selected dye compounds.
Chemical Biology & Drug Design ( IF 3.2 ) Pub Date : 2019-12-13 , DOI: 10.1111/cbdd.13654 Franciska de Beer 1 , Jacobus P Petzer 1, 2 , Anél Petzer 1, 2
Chemical Biology & Drug Design ( IF 3.2 ) Pub Date : 2019-12-13 , DOI: 10.1111/cbdd.13654 Franciska de Beer 1 , Jacobus P Petzer 1, 2 , Anél Petzer 1, 2
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Monoamine oxidase (MAO) is an important drug target as the MAO isoforms play key roles in neurodegenerative disorders such as Alzheimer's disease and Parkinson's disease, as well as in neuropsychiatric diseases such as depression. Methylene blue is an inhibitor of MAO-A, while azure B, the major metabolite of methylene blue, and various other structural analogues retain the ability to inhibit MAO-A. Based on this, the present study evaluated 22 dyes, many of which are structurally related to methylene blue, as potential inhibitors of human MAO-A and MAO-B. The results highlighted three dye compounds as good potency competitive and reversible MAO inhibitors, and which exhibit higher MAO inhibition than methylene blue: acridine orange, oxazine 170 and Darrow red. Acridine orange was found to be a MAO-A specific inhibitor (IC50 = 0.017 μM), whereas oxazine 170 is a MAO-B specific inhibitor (IC50 = 0.0065 μM). Darrow red was found to be a non-specific MAO inhibitor (MAO-A, IC50 = 0.059 μM; MAO-B, IC50 = 0.065 μM). These compounds may be advanced for further testing and preclinical development, or be used as possible lead compounds for the future design of MAO inhibitors.
中文翻译：
选定的染料化合物抑制单胺氧化酶。
单胺氧化酶 (MAO) 是一个重要的药物靶点，因为 MAO 亚型在阿尔茨海默病和帕金森病等神经退行性疾病以及抑郁症等神经精神疾病中发挥着关键作用。亚甲蓝是 MAO-A 的抑制剂，而亚甲蓝的主要代谢物 azure B 和各种其他结构类似物保留了抑制 MAO-A 的能力。基于此，本研究评估了 22 种染料作为人类 MAO-A 和 MAO-B 的潜在抑制剂，其中许多染料在结构上与亚甲基蓝相关。结果表明，三种染料化合物是具有良好效力的竞争性和可逆性 MAO 抑制剂，并且比亚甲蓝表现出更高的 MAO 抑制作用：吖啶橙、恶嗪 170 和达罗红。发现吖啶橙是一种 MAO-A 特异性抑制剂 (IC50 = 0.017 μM)，而 恶嗪 170 是一种 MAO-B 特异性抑制剂 (IC50 = 0.0065 μM)。 Darrow red 被发现是一种非特异性 MAO 抑制剂（MAO-A，IC50 = 0.059 μM；MAO-B，IC50 = 0.065 μM）。这些化合物可用于进一步测试和临床前开发，或用作未来 MAO 抑制剂设计的可能先导化合物。
更新日期：2019-12-27
中文翻译：
选定的染料化合物抑制单胺氧化酶。
单胺氧化酶 (MAO) 是一个重要的药物靶点，因为 MAO 亚型在阿尔茨海默病和帕金森病等神经退行性疾病以及抑郁症等神经精神疾病中发挥着关键作用。亚甲蓝是 MAO-A 的抑制剂，而亚甲蓝的主要代谢物 azure B 和各种其他结构类似物保留了抑制 MAO-A 的能力。基于此，本研究评估了 22 种染料作为人类 MAO-A 和 MAO-B 的潜在抑制剂，其中许多染料在结构上与亚甲基蓝相关。结果表明，三种染料化合物是具有良好效力的竞争性和可逆性 MAO 抑制剂，并且比亚甲蓝表现出更高的 MAO 抑制作用：吖啶橙、恶嗪 170 和达罗红。发现吖啶橙是一种 MAO-A 特异性抑制剂 (IC50 = 0.017 μM)，而 恶嗪 170 是一种 MAO-B 特异性抑制剂 (IC50 = 0.0065 μM)。 Darrow red 被发现是一种非特异性 MAO 抑制剂（MAO-A，IC50 = 0.059 μM；MAO-B，IC50 = 0.065 μM）。这些化合物可用于进一步测试和临床前开发，或用作未来 MAO 抑制剂设计的可能先导化合物。
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