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Volume 36 Issue 2
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Article Navigation >  Journal of Pharmaceutical Practice and Service  > 2018  >  36(2): 112-115,135

WANG Pengru, LI Wei, PENG Xuemi, ZHENG Wei, GUO Liangjun, JIN Yongsheng. Synthesis and anti-oxidation activity of schisandrone derivatives[J]. Journal of Pharmaceutical Practice and Service, 2018, 36(2): 112-115,135. doi: 10.3969/j.issn.1006-0111.2018.02.004
Citation: WANG Pengru, LI Wei, PENG Xuemi, ZHENG Wei, GUO Liangjun, JIN Yongsheng. Synthesis and anti-oxidation activity of schisandrone derivatives[J]. Journal of Pharmaceutical Practice and Service, 2018, 36(2): 112-115,135. doi: 10.3969/j.issn.1006-0111.2018.02.004
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Synthesis and anti-oxidation activity of schisandrone derivatives

doi: 10.3969/j.issn.1006-0111.2018.02.004
  • 1.

    Student Brigade, Second Military Medical University, Shanghai 200433, China;Department of Organic Chemistry, School of Pharmacy, Second Military Medical University, Shanghai 200433, China

  • 2.

    Department of Pharmacy, No. 98 Hospital of PLA, Huzhou 313000, China

  • 3.

    Department of Organic Chemistry, School of Pharmacy, Second Military Medical University, Shanghai 200433, China

  • Received Date: 2017-09-29
  • Rev Recd Date: 2017-10-19
  • 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.
  • [1] Williams SC.Alzheimer's disease:Mapping the brain's decline[J].Nature,2013,502(7473):S84-S85.
    [2] Hane F T,Robinson M,Lee B Y,et al.Recent progress in Alzheimer's disease research,Part 3:diagnosis and treatment.[J].J Alzheimers Dis,2017,57(3):645-665.
    [3] 黄诒森,何燕,张均.五味子三种成分的抗氧化作用[J].中国药理学与毒理学杂志,1990,4(4):275-277.
    [4] 贾丽艳,拓西平,朱嘉琦,等.华中五味子酮对阿尔茨海默病样大鼠海马内IL-1β及iNOS表达的影响[J].第二军医大学学报,2005,26(2):161-163.
    [5] Van der Mey M,Hatzelmann A,Van der Laan IJ,et al.Novel selective PDE4 inhibitors.1.Synthesis,structure-activity relationships,and molecular modeling of 4-(3,4-dimethoxyphenyl) -2h-phthalazin-1-ones and analogues[J].J Med Chem,2001,44(16):2511-2522.
    [6] 陈志卫,胡永洲.四种天然槲皮素-3-糖苷的合成[J].有机化学,2006,26(6):813-816.
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Synthesis and anti-oxidation activity of schisandrone derivatives

doi: 10.3969/j.issn.1006-0111.2018.02.004
  • 1. Student Brigade, Second Military Medical University, Shanghai 200433, China;Department of Organic Chemistry, School of Pharmacy, Second Military Medical University, Shanghai 200433, China
  • 2. Department of Pharmacy, No. 98 Hospital of PLA, Huzhou 313000, China
  • 3. Department of Organic Chemistry, School of Pharmacy, Second Military Medical University, Shanghai 200433, China
  • Received Date: 2017-09-29
  • Rev Recd Date: 2017-10-19

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.

WANG Pengru, LI Wei, PENG Xuemi, ZHENG Wei, GUO Liangjun, JIN Yongsheng. Synthesis and anti-oxidation activity of schisandrone derivatives[J]. Journal of Pharmaceutical Practice and Service, 2018, 36(2): 112-115,135. doi: 10.3969/j.issn.1006-0111.2018.02.004
Citation: WANG Pengru, LI Wei, PENG Xuemi, ZHENG Wei, GUO Liangjun, JIN Yongsheng. Synthesis and anti-oxidation activity of schisandrone derivatives[J]. Journal of Pharmaceutical Practice and Service, 2018, 36(2): 112-115,135. doi: 10.3969/j.issn.1006-0111.2018.02.004
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