Chen Jichao, Duan Wenli, Bai Renren, Yao Hequan, Shang Jing, Xu Jinyi
State Key Laboratory of Natural Medicines, China Pharmaceutical University, 24 Tong Jia Xiang, Nanjing 210009, PR China; Department of Medicinal Chemistry, China Pharmaceutical University, 24 Tong Jia Xiang, Nanjing 210009, PR China.
State Key Laboratory of Natural Medicines, China Pharmaceutical University, 24 Tong Jia Xiang, Nanjing 210009, PR China; Center for Drug Screening, China Pharmaceutical University, 24 Tong Jia Xiang, Nanjing 210009, PR China.
Bioorg Med Chem Lett. 2014 Aug 1;24(15):3407-11. doi: 10.1016/j.bmcl.2014.05.078. Epub 2014 Jun 2.
Forty β-elemene derivatives were prepared and their antioxidant activity in H2O2-treated human umbilical vein endothelial cells (HUVECs) was first investigated. Among which, the dimer compounds 5r and 5s exhibited the most potent antioxidant activity against reactive oxygen species production. Meanwhile, 5r and 5s led to a significant increase in superoxide dismutase and nitric oxide levels and decrease in malonyldialdehyde and lactate dehydrogenase contents. Furthermore, MTT assay showed that 5r and 5s did not produce obvious cytotoxicity and had significantly cytoprotective effects against oxidative damage on HUVECs.
制备了40种β-榄香烯衍生物，并首次研究了它们在H2O2处理的人脐静脉内皮细胞（HUVECs）中的抗氧化活性。其中，二聚体化合物5r和5s对活性氧的产生表现出最有效的抗氧化活性。同时，5r和5s导致超氧化物歧化酶和一氧化氮水平显著增加，丙二醛和乳酸脱氢酶含量降低。此外，MTT试验表明，5r和5s不会产生明显的细胞毒性，并且对HUVECs的氧化损伤具有显著的细胞保护作用。
