title: Antioxydant activity of β-carboline derivatives in the LDL oxidation model.
abstract: A series of β-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 2,2'-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 μM CuSO4). The best antioxidant activities are phenolic and benzyloxy derivatives with ratio R=1.9 to 2.8 for 1 μM CuSO4. These substances have protective actions and increase significantly the cell viability.
authors.affiliation: Université Lille Nord de France, Faculté de Pharmacie, Laboratoire de Chimie Thérapeutique (EA 4481) 3, Département de Pharmacologie Médicale, rue du Professeur Laguesse, BP 83, 59006 Lille, France.
authors.forename: Fariza
authors.initials: F
authors.lastname: Hadjaz
authors.forename: Soizic
authors.initials: S
authors.lastname: Besret
authors.forename: Françoise
authors.initials: F
authors.lastname: Martin-Nizard
authors.forename: Saïd
authors.initials: S
authors.lastname: Yous
authors.forename: Sébastien
authors.initials: S
authors.lastname: Dilly
authors.forename: Nicolas
authors.initials: N
authors.lastname: Lebegue
authors.forename: Philippe
authors.initials: P
authors.lastname: Chavatte
authors.forename: Patrick
authors.initials: P
authors.lastname: Duriez
authors.forename: Pascal
authors.initials: P
authors.lastname: Berthelot
authors.forename: Pascal
authors.initials: P
authors.lastname: Carato
mesh_terms: D000818:Animals; D000975:Antioxidants / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D001011:Aorta / Q000166:cytology / Q000187:drug effects / Q000201:enzymology; D002243:Carbolines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D002417:Cattle; D002470:Cell Survival / Q000187:drug effects; D008078:Cholesterol, LDL / Q000737:chemistry / Q000187:drug effects / Q000378:metabolism*; D004305:Dose-Response Relationship, Drug; D004353:Drug Evaluation, Preclinical; D042783:Endothelial Cells / Q000187:drug effects / Q000378:metabolism; D007770:L-Lactate Dehydrogenase / Q000378:metabolism; D015227:Lipid Peroxidation / Q000187:drug effects*; D008928:Mitochondria / Q000187:drug effects / Q000378:metabolism; D008954:Models, Biological; D015394:Molecular Structure; D010084:Oxidation-Reduction; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
chemical_list: D000975:Antioxidants; D002243:Carbolines; D008078:Cholesterol, LDL; D007770:L-Lactate Dehydrogenase