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CHEN Ji-Chao, DUAN Wen-Li, BAI Ren-Ren, YAO He-Quan, WU Xiao-Ming, SHANG Jing, XU Jin-Yi. Synthesis of 13-β-elemene ester derivatives and evaluation of their antioxidant activity in human umbilical vein endothelial cells[J]. 中国天然药物, 2015, 13(8): 618-627.
引用本文: CHEN Ji-Chao, DUAN Wen-Li, BAI Ren-Ren, YAO He-Quan, WU Xiao-Ming, SHANG Jing, XU Jin-Yi. Synthesis of 13-β-elemene ester derivatives and evaluation of their antioxidant activity in human umbilical vein endothelial cells[J]. 中国天然药物, 2015, 13(8): 618-627.
CHEN Ji-Chao, DUAN Wen-Li, BAI Ren-Ren, YAO He-Quan, WU Xiao-Ming, SHANG Jing, XU Jin-Yi. Synthesis of 13-β-elemene ester derivatives and evaluation of their antioxidant activity in human umbilical vein endothelial cells[J]. Chinese Journal of Natural Medicines, 2015, 13(8): 618-627.
Citation: CHEN Ji-Chao, DUAN Wen-Li, BAI Ren-Ren, YAO He-Quan, WU Xiao-Ming, SHANG Jing, XU Jin-Yi. Synthesis of 13-β-elemene ester derivatives and evaluation of their antioxidant activity in human umbilical vein endothelial cells[J]. Chinese Journal of Natural Medicines, 2015, 13(8): 618-627.

Synthesis of 13-β-elemene ester derivatives and evaluation of their antioxidant activity in human umbilical vein endothelial cells

Synthesis of 13-β-elemene ester derivatives and evaluation of their antioxidant activity in human umbilical vein endothelial cells

  • 摘要: In the present study, a series of 13--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), malonyldialdehyde (MDA), nitric oxide (NO), and lactic dehydrogenase (LDH), which were superior to that of the positive control vitamin E. Furthermore, they did not produce any obvious cytotoxicity, but increased the viability of HUVECs injured by H2O2 in a dose-dependent manner. Additionally, compound 5w, designed as a prodrug-like compound, showed improved stability relative to compound 4 in vitro.

     

    Abstract: In the present study, a series of 13--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), malonyldialdehyde (MDA), nitric oxide (NO), and lactic dehydrogenase (LDH), which were superior to that of the positive control vitamin E. Furthermore, they did not produce any obvious cytotoxicity, but increased the viability of HUVECs injured by H2O2 in a dose-dependent manner. Additionally, compound 5w, designed as a prodrug-like compound, showed improved stability relative to compound 4 in vitro.

     

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