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为提高甘草次酸(Ib)的抗氧化活性,对其化学结构进行修饰,制备11-羟基甘草萜醇类衍生物。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。微粒体中的自由基由探针物DCFH-DA的氧化程度进行检测。维生素E作为阳性对照物。通过还原反应获得甘草萜醇类两种光学异构体———11α-羟基物(2)和11β-羟基物(3)。这两种化合物显示出较强的抗氧化活性,以1.0 mg/mL浓度,分别抑制自由基浓度为50%和51%。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。以上结果显示,对先导物Ib的C11位羰基和C30位羧基进行还原修饰,可显著提高其抗氧化活性,这种修饰将能增强先导物对自由基损伤有关病理性病变(如AS)的防治潜能。
In order to improve the anti-oxidation activity of glycyrrhetinic acid (Ib), its chemical structure was modified to prepare 11-hydroxyglycylic alcohol derivatives. The antioxidant activity of each compound was determined by an in vitro antioxidant assay model using the cytochrome P450/NADPH oxidation system in liver microsomes. Free radicals in microsomes are detected by the degree of oxidation of the probe DCFH-DA. Vitamin E as a positive control. Two optical isomers of glycyrrhizin were obtained by the reduction reaction—11α-hydroxy (2) and 11β-hydroxy (3). The two compounds showed strong antioxidant activity, with a concentration of 1.0 mg/mL, which inhibited the free radical concentration by 50% and 51%, respectively. Under the same conditions, lead Ib and vitamin E inhibited free radical activity by 31% and 32%, respectively. The above results show that the reduction and modification of the C11 carbonyl group and C30 carboxyl group of lead Ib can significantly increase its antioxidative activity. This modification will enhance the prevention and treatment of lead compounds in pathological lesions (such as AS) related to free radical damage. Potential.