Popov A M, Osipov A N, Korepanova E A, Krivoshapko O N, Shtoda Yu P, Klimovich A A
Biofizika. 2015 Jul-Aug;60(4):700-7.
A comparative study of antioxidant (radical-interceptor) properties of tryptanthrin (quinazoline alkaloid shows a high anti-inflammatory activity and it is found in many types of different families of higher plants and microorganisms, including the human microbiome) in the systems of 2,2'-azo-bis(2-methylpropionamidin)dihydrochloride-luminol and hemoglobin-hydrogen peroxide-luminol has been conducted and the influence on the permeability of planar bilayer lipid membranes is evaluated. Trolox was used as a reference antioxidant, and ascorbic acid and dihydroquercetin were taken as standards. Tryptanthrin exhibits very weak antioxidant activity, being markedly inferior to the reference standard and antioxidants while testing antioxidant activity in both studied systems. By the efficacy of antioxidative action the substrates in the systems studied can be arranged in the following order: dihydroquercetin > trolox > ascorbic acid > tryptanthrin. Antioxidant potential of tryptanthrin is approximately 1000 and 3000 times lower than that of trolox and bioflavonoid dihydroquercetine, respectively. Tryptanthrin causes no significant changes in the permeability of planar bilayer membranes in a dose range of 0.5 to. 10 μg/ml. Our data show that tryptanthrin displays no significant radical-interceptor and membranotropic activities. It can be assumed that the observed high anti-inflammatory activity of tryptanthrin is not related to the neutralizing effect against reactive oxygen species and the influence on the permeability of cell membranes. The anticipated mechanisms of biological activity of tryptanthrin are discussed.
对色胺酮(喹唑啉生物碱,具有高抗炎活性,存在于许多不同科的高等植物和微生物中,包括人类微生物群)在2,2'-偶氮二(2-甲基丙脒)二盐酸盐-鲁米诺体系和血红蛋白-过氧化氢-鲁米诺体系中的抗氧化(自由基拦截剂)特性进行了比较研究,并评估了其对平面双层脂质膜通透性的影响。使用Trolox作为参考抗氧化剂,以抗坏血酸和二氢槲皮素作为标准品。在两个研究体系中测试抗氧化活性时,色胺酮表现出非常弱的抗氧化活性,明显低于参考标准品和抗氧化剂。根据抗氧化作用的效果,所研究体系中的底物可按以下顺序排列:二氢槲皮素>Trolox>抗坏血酸>色胺酮。色胺酮的抗氧化潜力分别比Trolox和生物类黄酮二氢槲皮素低约1000倍和3000倍。在0.5至10μg/ml的剂量范围内,色胺酮不会引起平面双层膜通透性的显著变化。我们的数据表明,色胺酮没有显著的自由基拦截和膜otropic活性。可以假定,观察到的色胺酮的高抗炎活性与对活性氧的中和作用以及对细胞膜通透性的影响无关。文中讨论了色胺酮预期的生物活性机制。