Synthesis and anti-oxidation activity of schisandrone derivatives
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摘要: 目的 设计合成五味子酮衍生物,并测试其体内抗氧化活性。 方法 采用酰化等方法合成了10个五味子酮衍生物,其中7个为首次报道,同时测试合成的化合物对小鼠血清中超氧化物歧化酶(SOD)的影响,分析构效关系。 结果 化合物 2、3、5 和 8 可明显提高SOD的活力,其中化合物 2、3、5 的作用明显优于五味子酮。 结论 五味子酮衍生物具有良好的抗氧化活性。构效关系表明,五味子酮结构中1位的羰基和2位,3位的甲基不影响五味子酮的抗氧化活性。Abstract: Objective To design and synthesize schisandrone derivatives for the therapy of disease like AD,and to measure their anti-oxidation activity. Methods Ten compounds were synthesized,and seven of them were first reported.The influence all the compounds on SOD from the mouse serum were measured to evaluate anti-oxidation activity.Structure-activity relationship (SARs) were also discussed. Results Compounds 2, 3, 5 and 8 could increase the activity of SOD in mouse serum.Furthermore,Compounds 2, 3 and 5 showed better activities than schisandrone. Conclusion Synthesized schisandrone derivatives showed anti-oxidation activity.The SARs demonstrated the carbonyl of C-1 position and the methyls of C-2 and 3 had no influences to the anti-oxidant activity.
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Key words:
- schisandrone /
- synthesis /
- anti-oxidation
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