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Antioxydant activity of beta-carboline derivatives in the LDL oxidation model

  作者 Hadjaz, F; Besret, S; Martin-Nizard, F; Yous, S; Dilly, S; Lebegue, N; Chavatte, P; Duriez, P; Berthelot, P; Carato, P  
  选自 期刊  European Journal of Medicinal Chemistry;  卷期  2011年46-6;  页码  2575-2585  
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[摘要]A series of beta-carboline compounds were synthesized, starting from compound GWC22, their antioxidant activity was determined by inhibition of lipid peroxidation. The oxidation of LDL was induced in the presence of CuSO(4) or 2,2'-azobis(2-amidinopropane) dihydrochloride (AAPH). The protective actions of these compounds against the cytotoxicity were evaluated with lactate dehydrogenase (LDH) activity in bovine aortic endothelial cells (BAECs) and cellular vitality by measuring mitochondrial activity in the presence of MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide). Most of compounds showed an higher antioxidant activity than GWC22 derivative (R = 1.6 for 5 mu M CuSO(4)). The best antioxidant activities are phenolic and benzyloxy derivatives with ratio R = 1.9 to 2.8 for 1 mu M CuSO(4). These substances have protective actions and increase significantly the cell viability. (C) 2011 Elsevier Masson SAS. All rights reserved.

 
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