Antioxidant activity of benzoxazolinonic and benzothiazolinonic derivatives in the LDL oxidation model.
A series of benzazolone compounds were synthesized utilizing benzoxazolinonic and benzothiazolinonic heterocycles as the building unit. The antioxidant activity of these compounds 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 action of these compounds against the cytotoxicity was 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). The best antioxidant activities were observed for phenolic compounds 13 and 14b with ratio R=2.5, 3.2 (5microM). Both of these test substances increased the cell viability significantly as indicated by MTT assay and LDH release assay.
Yekini
Ismaël
I
Faculté de Pharmacie, Université Lille Nord de France, Laboratoire de Chimie Thérapeutique (EA 1043)3, Rue du Professeur Laguesse, BP 83, 59006 LILLE Cedex, France.
Hammoudi
Fatma
F
Martin-Nizard
Françoise
F
Yous
Saïd
S
Lebegue
Nicolas
N
Berthelot
Pascal
P
Carato
Pascal
P
D000818:Animals; D000975:Antioxidants / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D001011:Aorta / Q000166:cytology / Q000378:metabolism / Q000473:pathology; D001583:Benzoxazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D001681:Biological Assay; D002417:Cattle; D002470:Cell Survival / Q000187:drug effects / Q000502:physiology; D042783:Endothelial Cells / Q000187:drug effects / Q000378:metabolism; D007770:L-Lactate Dehydrogenase / Q000378:metabolism; D008077:Lipoproteins, LDL / Q000378:metabolism*; D010084:Oxidation-Reduction / Q000187:drug effects; D013844:Thiazoles / Q000138:chemical synthesis / Q000378:metabolism / Q000494:pharmacology*
D000975:Antioxidants; D001583:Benzoxazoles; D008077:Lipoproteins, LDL; D013844:Thiazoles; C017057:benzoxazolone; D007770:L-Lactate Dehydrogenase