Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Ankara University, 06100 Tandogan, Ankara, Turkey.
Chem Biol Drug Des. 2012 Jan;79(1):76-83. doi: 10.1111/j.1747-0285.2011.01216.x. Epub 2011 Nov 4.
Increased levels of reactive oxygen species attributed to oxidative stress have been found to be responsible for the development of some vital diseases such as cardiovascular, neurodegenerative and autoimmune diseases. Recently, it was observed that melatonin is a highly important antioxidant, and melatonin analogues are under investigation to find out improved antioxidant activity. In this study, 14 melatonin -based analogue indole amino acid and N-protected amino acid derivatives were synthesized and elucidated spectrometrically. To investigate the antioxidant activity of the synthesized compounds and to compare with melatonin, butylhydroxytoluene and vitamin E, lipid peroxidation inhibition and 2,2-diphenyl-1-picrylhydrazyl radical-scavenging activities were tested. The results indicated that the synthesized new indole amino acid derivatives have similar activities to melatonin in 2,2-diphenyl-1-picrylhydrazyl radical-scavenging activity assay but more potent activities in lipid peroxidation inhibition assay.
研究发现，氧化应激导致的活性氧水平升高与心血管疾病、神经退行性疾病和自身免疫性疾病等一些重要疾病的发生有关。最近，人们观察到褪黑素是一种非常重要的抗氧化剂，正在研究褪黑素类似物以寻找具有更高抗氧化活性的物质。在这项研究中，合成了 14 种基于褪黑素的吲哚氨基酸和 N-保护氨基酸衍生物，并通过光谱法进行了阐明。为了研究合成化合物的抗氧化活性并与褪黑素、丁基羟基甲苯和维生素 E 进行比较，测试了它们对脂质过氧化的抑制作用和对 2,2-二苯基-1-苦基肼自由基的清除活性。结果表明，所合成的新型吲哚氨基酸衍生物在 2,2-二苯基-1-苦基肼自由基清除活性测定中与褪黑素具有相似的活性，但在脂质过氧化抑制测定中具有更强的活性。
