Dual inhibition of cyclooxygenase and lipoxygenase by 2-acetylthiophene 2-thiazolylhydrazone (CBS-1108) and effect on leukocyte migration in vivo.
CBS-1108, 2- acetylthiophene 2- thiazolyhydrazone , inhibits 5-lipoxygenase activity in polymorphonuclear leukocytes (PMNs) (IC50 = 2 X 10(-6) M), 12-lipoxygenase (IC50 = 9 X 10(-6) M) and cyclooxygenase (IC50 = 2 X 10(-6) M) in platelets. Inhibition of the two pathways of arachidonic acid cascade could lead to additional beneficial anti-inflammatory activity by comparison with classical aspirin-like drugs. In fact, only inhibitors of both cyclooxygenase and lipoxygenase such as NDGA and CBS-1108 inhibit leukocyte migration in an animal model of acute inflammatory response.
D000818:Animals; D001091:Arachidonate Lipoxygenases; D001241:Aspirin / Q000494:pharmacology; D001792:Blood Platelets / Q000201:enzymology; D002266:Carboxymethylcellulose Sodium / Q000494:pharmacology; D002634:Chemotaxis, Leukocyte / Q000187:drug effects*; D016861:Cyclooxygenase Inhibitors; D006801:Humans; D007249:Inflammation / Q000097:blood; D016859:Lipoxygenase Inhibitors; D008297:Male; D009504:Neutrophils / Q000201:enzymology; D011817:Rabbits; D051381:Rats; D011919:Rats, Inbred Strains; D013844:Thiazoles / Q000494:pharmacology*
D016861:Cyclooxygenase Inhibitors; D016859:Lipoxygenase Inhibitors; D013844:Thiazoles; C041430:2-acetylthiophene-2-thiazolylhydrazone; D001091:Arachidonate Lipoxygenases; D002266:Carboxymethylcellulose Sodium; D001241:Aspirin