[en] A series of b-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 CuSO4 or 2,20-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 mM CuSO4). The best antioxidant activities are phenolic and benzyloxy derivatives with ratio R = 1.9 to 2.8 for 1 mM CuSO4. These substances have protective actions and increase significantly the cell viability.
Research Center/Unit :
Laboratoire de Chimie Thérapeutique, Faculté de Pharmacie, Université Lille Nord de France Département de Pharmacologie Médicale, Faculté de Pharmacie, Université Lille Nord de France Institut Pasteur de Lille, Faculté de Pharmacie, Université Lille Nord de France
Disciplines :
Pharmacy, pharmacology & toxicology
Author, co-author :
Hadjaz, Fariza; Université Lille Nord de France > Faculté de Pharmacie > Laboratoire de Chimie Thérapeutique
Besret, Soizic; Université Lille Nord de France > Faculté de Pharmacie > Laboratoire de Chimie Thérapeutique
Martin-Nizard, Françoise; Université Lille Nord de France > Institut Pasteur de Lille, Faculté de Pharmacie
Yous, Said; Université Lille Nord de France > Faculté de Pharmacie > Laboratoire de Chimie Thérapeutique
Dilly, Sébastien ; Université de Liège - ULiège > Giga Neurosciences - CIRM > Laboratoire de pharmacologie - Laboratoire de Chimie Pharmaceutique
Lebegue, Nicolas; Université Lille Nord de France > Faculté de Pharmacie > Laboratoire de Chimie Thérapeutique
Chavatte, Philippe; Université Lille Nord de France > Faculté de Pharmacie > Laboratoire de Chimie Thérapeutique
Duriez, Patrick; Université Lille Nord de France > Faculté de Pharmacie > Département de Pharmacologie Médicale
Berthelot, Pascal; Université Lille Nord de France > Faculté de Pharmacie > Laboratoire de Chimie Thérapeutique
Carato, Pascal; Université Lille Nord de France > Faculté de Pharmacie > Laboratoire de Chimie Thérapeutique
Language :
English
Title :
Antioxydant activity of β-carboline derivatives in the LDL oxidation model