Suzen Sibel, Bozkaya Pinar, Coban Tulay, Nebioğu Doğu
Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Ankara University, Tandogan, Ankara 06100, Turkey.
J Enzyme Inhib Med Chem. 2006 Aug;21(4):405-11. doi: 10.1080/14756360500381210.
Oxidative stress has been implicated in the development of many neurodegenerative diseases and also responsible from aging and some cancer types. Indolic compounds are a broad family of substances present in microorganisms, plants and animals. They are mainly related to tryptophan metabolism, and present particular properties that depend on their respective chemical structures. Due to free radical scavenger and antioxidant properties of indolic derivatives such as indolinic nitroxides and melatonin, a series of 2-phenyl indole derivatives were prepared and their in vitro effects on rat liver lipid peroxidation levels, superoxide formation and DPPH stable radical scavenging activities were determined against melatonin, BHT and alpha-tocopherol. The compounds significantly inhibited (72-98%) lipid peroxidation at 10(-3) M. These values were similar to that observed with BHT (88%). Possible structure-activity relationships of the compounds were discussed.
氧化应激与许多神经退行性疾病的发展有关，也与衰老和某些癌症类型有关。吲哚类化合物是存在于微生物、植物和动物中的一大类物质。它们主要与色氨酸代谢有关，并具有取决于其各自化学结构的特殊性质。由于吲哚类衍生物如吲哚啉氮氧化物和褪黑素具有自由基清除剂和抗氧化特性，制备了一系列2-苯基吲哚衍生物，并测定了它们对大鼠肝脏脂质过氧化水平、超氧形成和DPPH稳定自由基清除活性的体外作用，以与褪黑素、丁基羟基甲苯（BHT）和α-生育酚进行对比。这些化合物在10⁻³ M时能显著抑制（72 - 98%）脂质过氧化。这些数值与BHT（88%）所观察到的相似。讨论了这些化合物可能的构效关系。
