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为优化甘草次酸(Ib)的抗氧化活性,对其化学结构进行修饰,通过还原和脱水反应制备了2个甘草萜醇类共轭烯衍生物。各化合物的抗氧化活性由肝微粒体中的细胞色素P450/NADPH氧化系统做体外抗氧化实验模型进行测定。微粒体中的自由基诱发情况由探针DCFH-DA的氧化程度进行检测,维生素E作为阳性对照物。初步的活性测定结果显示,甘草萜醇类两种同环和异环双烯衍生物——18β-olean-11,13(18)-diene-3β,30-diol(IV)和18β-olean-9(11),12-diene-3β,30-diol(V)显示出较强的抗氧化活性,以1.0 mg.mL-1的浓度,分别抑制自由基活性为45%和41%。相同条件下,先导物Ib和维生素E分别抑制31%和32%的自由基活性。此结果显示,对先导物Ib的C11位羰基的脱去和C30位羧基进行还原修饰,可显著提高其抗氧化活性。
In order to optimize the anti-oxidative activity of glycyrrhetinic acid (Ib), its chemical structure was modified and two glycyrrhizin alcohol conjugate derivatives were prepared by reduction and dehydration reaction. Antioxidant activity of each compound was determined by an in vitro antioxidant model of cytochrome P450 / NADPH oxidation system in liver microsomes. Free radical induction in microsomes was determined by the degree of oxidation of probe DCFH-DA, with vitamin E as a positive control. The preliminary results of the activity assay showed that the two isocyclic and iso-cycloalkene derivatives -18β-olean-11,13 (18) -diene-3β, 30-diol (IV) and18β-olean- 9 (11), 12-diene-3β, 30-diol (V) showed strong anti-oxidative activity, and inhibited free radical activity of 45% and 41% respectively at the concentration of 1.0 mg.mL-1. Under the same conditions, lead Ib and vitamin E inhibited 31% and 32% of free radical activity, respectively. The results showed that the lead C 1 off carbonyl and C30 carboxyl carboxyl reduced modification can significantly improve its antioxidant activity.