Alaternin and emodin with hydroxyl radical inhibitory and/or scavenging activities and hepatoprotective activity on tacrine-induced cytotoxicity in HepG2 cells
Alaternin and emodin with hydroxyl radical inhibitory and/or scavenging activities and hepatoprotective activity on tacrine-induced cytotoxicity in HepG2 cells
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DOI：
10.1007/bf02975849
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发表时间：
2004-09-01
影响因子：
6.7
通讯作者：
Choi, JS
中科院分区：
文献类型：
--
作者：
Jung, HA;Chung, HY;Choi, JS
分别评估了两种蒽醌、阿拉特宁（2-羟基大黄素）和大黄素的抗氧化和保肝潜力，以清除和/或抑制芬顿反应产生的羟基自由基，并保护他克林诱导的人肝来源 HepG2 细胞的细胞毒性。使用强荧光探针 2',7'-二氯荧光素，通过荧光分光光度计研究了对无细胞化学体系 (FeSO4/H2O2) 中产生的羟基自由基的抑制活性。使用5,5-二甲基-1-吡咯啉-N-氧化物作为羟基自由基捕获剂，通过电子自旋共振光谱测定羟基自由基清除活性。他克林诱导的 HepG2 细胞毒性通过 3[4,5-二甲基噻唑-2基]-2,5-二苯基四唑溴化物测定来测定。虽然阿拉特宁对羟自由基的清除活性与大黄素相似，且具有剂量依赖性，但前者对羟自由基产生的抑制活性强于后者，IC50值分别为3.05+/-0.26μM和13.29+/-3.20μM。此外，两种蒽醌类化合物阿拉丁宁和大黄素对他克林诱导的细胞毒性表现出保肝活性，EC50值分别为4.02 μM和2.37 μM。用作阳性对照的抗肝毒性剂水飞蓟素表现出2.00μM的EC50值。这些结果表明，阿拉特宁和大黄素同时具有抗氧化和保肝活性。
The antioxidative and hepatoprotective potentials of two anthraquinones, alaternin (2-hydroxyemodin) and emodin, to scavenge and/or inhibit hydroxyl radicals generated by the Fenton reaction and to protect tacrine-induced cytotoxicity in human liver derived HepG2 cells were evaluated, respectively. The inhibitory activity on hydroxyl radical generated in a cell-free chemical system (FeSO4/H2O2) was investigated by a fluorescence spectrophotometer using a highly fluorescent probe, 2',7'-dichlorofluorescein. The hydroxyl radical scavenging activity was determined by electron spin resonance spectroscopy using 5,5-dimethy-1-pyrroline-N-oxide as hydroxyl radicals trapping agents. Tacrine-induced HepG2 cell toxicity was determined by a 3[4,5-dimethylthiazole-2yl]-2,5-diphenyltertrazolium bromide assay. Although the scavenging activity of alaternin on hydroxyl radical was similar to that of emodin in dose-dependent patterns, the inhibitory activity exhibited by the former on hydroxyl radical generation was stronger than that of the latter, with IC50 values of 3.05 +/- 0.26 muM and 13.29 +/- 3.20 muM, respectively. In addition, the two anthraquinones, alaternin and emodin showed their hepatoprotective activities on tacrine-induced cytotoxicity, and the EC50 values were 4.02 muM and 2.37 muM, respectively. Silymarin, an antihepatotoxic agent used as a positive control exhibited the EC50 value of 2.00 muM. These results demonstrated that both alaternin and emodin had the simultaneous antioxidant and hepatoprotective activities.