Synthesis of 13-β-elemene ester derivatives and evaluation of their antioxidant activity in human um

来源 :Chinese Journal of Natural Medicines | 被引量 : 0次 | 上传用户:leihaibo880125
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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), 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. 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 was 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 significant cytotoxicity, but increased the viability of HUVECs by H2O2 in a dose-dependent manner. prodrug-like compound, showed improved stability relative to compound 4 in vitro.
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