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Synthesis of 13-β-elemene ester derivatives and evaluation o

發(fā)布時間:2021-09-05 07:45
  In the present study, a series of 13-β-elemene ester derivatives were designed and prepared, and their antioxidant activity was investigated in the H2O2-treated human umbilical vein endothelial cells(HUVECs). Among the test compounds, the dimer compounds 5v and 5w exhibited the most potent antioxidant activity with significant ROS suppression being observed. Both compounds markedly inhibited the H2O2-induced changes in various biochemical substances, such as superoxide dismutase(SOD), malonyldia... 

【文章來源】:Chinese Journal of Natural Medicines. 2015,13(08)SCICSCD

【文章頁數(shù)】:10 頁

【文章目錄】:
Introduction
Material and Methods
    Chemistry General
    Synthesis of the target compounds 5a-w
    Pharmacology Assay for ROS inhibition
    Assay for intracellular levels of superoxide dismutase (SOD),malonyldialdehyde (MDA), nitric oxide (NO), and lactic dehydrogenase (LDH)
    Assay for cell viability of HUVECs injured by H2O2
    Assay for cytotoxicity in normal HUVECs
    Assay for the stability of 5w in vitro
Results
    Chemistry General procedure for the preparation of 13-chloro-β-elemene 2 [18]
    Generalprocedureforthepreparationof13-acetoxy-β-elemene 3[19]
    General procedure for the preparation of 13-β-elemenol 4[19]
    General procedure for the preparation of 13-β-elemene derivative 5
    Pharmacological evaluation ROS inhibitory activity
    Restoration of the antioxidant capacity by 5v and 5w
    Improvement of the viability of H2O2-injured HUVECs by 5v and 5w
    Cytotoxicity for 5v and 5w in normal HUVECs
    Stability of compound 5w
Discussion
Conclusion


【參考文獻(xiàn)】:
期刊論文
[1]β-欖香烯抗氧化損傷作用的實(shí)驗(yàn)研究[J]. 毛利飛,霍偉敏,柳軍,尚靖.  中國臨床藥理學(xué)與治療學(xué). 2012(07)
[2]系列β-欖香烯糖苷衍生物的合成[J]. 楊蘭義,張殊佳,鄭學(xué)仿,尹紅星.  有機(jī)化學(xué). 2008(10)
[3]大鼠膽汁中β-欖香烯代謝產(chǎn)物的研究[J]. 李志,王堃,陳玉仁,吳秀英,蘇成業(yè).  藥學(xué)學(xué)報. 2000(11)



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