Malterud K E, Farbrot T L, Huse A E, Sund R B
Department of Pharmacognosy, University of Oslo, Norway.
Pharmacology. 1993 Oct;47 Suppl 1:77-85. doi: 10.1159/000139846.
The activity of seven anthraquinones and four anthrones against nonenzymatic and enzymatic lipid peroxidation in vitro and their ability to scavenge free radicals have been studied. In nonenzymatic peroxidation in rat hepatocytes induced by t-butyl hydroperoxide, dithranol and anthrone were the strongest antioxidants, having IC50 values of 8 +/- 1 and 24 +/- 5 mumol/l, respectively. Rhein (IC50 64 +/- 2 mumol/l) and aloe-emodin (IC50 65 +/- 3 mumol/l) showed the highest inhibitory activity against peroxidation of linoleic acid catalyzed by soybean 15-lipoxygenase. Anthrone (IC50 62 +/- 2 mumol/l), dithranol (IC50 72 +/- 1 mumol/l) and rhein anthrone (IC50 76 +/- 6 mumol/l) were the most effective radical scavengers of the diphenylpicrylhydrazyl radical. The antioxidant activities in hepatocytes and the radical scavenging activities were correlated, whereas the inhibition of enzymatic lipid peroxidation showed no correlation with the two other effects.
研究了7种蒽醌和4种蒽酮在体外对非酶促和酶促脂质过氧化的活性及其清除自由基的能力。在叔丁基过氧化氢诱导的大鼠肝细胞非酶促过氧化反应中,地蒽酚和蒽酮是最强的抗氧化剂,IC50值分别为8±1和24±5μmol/L。大黄酸(IC50 64±2μmol/L)和芦荟大黄素(IC50 65±3μmol/L)对大豆15-脂氧合酶催化的亚油酸过氧化表现出最高的抑制活性。蒽酮(IC50 62±2μmol/L)、地蒽酚(IC50 72±1μmol/L)和大黄酸蒽酮(IC50 76±6μmol/L)是最有效的二苯苦味酰基自由基清除剂。肝细胞中的抗氧化活性与自由基清除活性相关,而酶促脂质过氧化的抑制与其他两种效应无关。