| 五味子酮衍生物的合成与抗氧化活性研究 |
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| 引用本文： | 王鹏儒,李伟,彭雪米,郑巍,郭良君,金永生.五味子酮衍生物的合成与抗氧化活性研究[J].药学实践杂志,2018,36(2):112-115,135. |
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| 作者姓名： | 王鹏儒 李伟 彭雪米 郑巍 郭良君 金永生 |
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| 作者单位： | 第二军医大学学员旅, 上海 200433;第二军医大学药学院有机化学教研室, 上海 200433,第二军医大学学员旅, 上海 200433;第二军医大学药学院有机化学教研室, 上海 200433,第二军医大学学员旅, 上海 200433;第二军医大学药学院有机化学教研室, 上海 200433,解放军98医院药剂科, 浙江 湖州 313000,解放军98医院药剂科, 浙江 湖州 313000,第二军医大学药学院有机化学教研室, 上海 200433 |
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| 基金项目： | 国家自然科学基金资助项目（20502034）；原南京军区医学创新课题重大项目（14ZD02） |
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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。
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| 关 键 词： | 五味子酮 合成 抗氧化作用 |
| 收稿时间： | 2017/9/29 0:00:00 |
| 修稿时间： | 2017/10/19 0:00:00 |
Synthesis and anti-oxidation activity of schisandrone derivatives |
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| WANG Pengru,LI Wei,PENG Xuemi,ZHENG Wei,GUO Liangjun and JIN Yongsheng.Synthesis and anti-oxidation activity of schisandrone derivatives[J].The Journal of Pharmaceutical Practice,2018,36(2):112-115,135. |
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| Authors: | WANG Pengru LI Wei PENG Xuemi ZHENG Wei GUO Liangjun and JIN Yongsheng |
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| Institution: | Student Brigade, Second Military Medical University, Shanghai 200433, China;Department of Organic Chemistry, School of Pharmacy, Second Military Medical University, Shanghai 200433, China,Student Brigade, Second Military Medical University, Shanghai 200433, China;Department of Organic Chemistry, School of Pharmacy, Second Military Medical University, Shanghai 200433, China,Student Brigade, Second Military Medical University, Shanghai 200433, China;Department of Organic Chemistry, School of Pharmacy, Second Military Medical University, Shanghai 200433, China,Department of Pharmacy, No. 98 Hospital of PLA, Huzhou 313000, China,Department of Pharmacy, No. 98 Hospital of PLA, Huzhou 313000, China and Department of Organic Chemistry, School of Pharmacy, Second Military Medical University, Shanghai 200433, China |
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| 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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| Keywords: | schisandrone synthesis anti-oxidation |
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