Design, synthesis and antioxidant activity evaluation of novel β-elemene derivatives

被引：30
作者：
Chen, Jichao [1 ,2 ]
Duan, Wenli [1 ,3 ]
Bai, Renren [1 ,2 ]
Yao, Hequan [1 ,2 ]
Shang, Jing [1 ,3 ]
Xu, Jinyi [1 ,2 ]
机构：
[1] China Pharmaceut Univ, State Key Lab Nat Med, Nanjing 210009, Jiangsu, Peoples R China
[2] China Pharmaceut Univ, Dept Med Chem, Nanjing 210009, Jiangsu, Peoples R China
[3] China Pharmaceut Univ, Ctr Drug Screening, Nanjing 210009, Jiangsu, Peoples R China
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2014年 / 24卷 / 15期
基金：
中国国家自然科学基金;
关键词：
beta-Elemene; Antioxidant activity; Reactive oxygen species; Oxidative stress; Cytoprotective effect; CELL-CYCLE; OXIDATIVE STRESS; ARREST; APOPTOSIS;
D O I：
10.1016/j.bmcl.2014.05.078
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Forty beta-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, KIT assay showed that 5r and 5s did not produce obvious cytotoxicity and had significantly cytoprotective effects against oxidative damage on HUVECs. (C) 2014 Elsevier Ltd. All rights reserved.
引用
收藏
页码：3407 / 3411
页数：5
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