4.5 Article

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

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 24, Issue 15, Pages 3407-3411

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2014.05.078

Keywords

beta-Elemene; Antioxidant activity; Reactive oxygen species; Oxidative stress; Cytoprotective effect

Funding

  1. National Natural Science Foundation of China [81373280, 30873156, 30672524]
  2. New Century Excellent Talents in University [NCET-07-0851]
  3. Mega-project of Science Research for the 12th Five-Year Plan of China [2011ZX09401-007]
  4. National Science and Technology Infrastructure Program [2012BAI30B001]
  5. Project Program of State Key Laboratory of Natural Medicines, China Pharmaceutical University [SKLNMZZCX201404]

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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.

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