Anti-inflammatory activity of a dual inhibitor of cyclooxygenase and lipoxygenase pathways, CBS-1108 (2-acetylthiophene-2-thiazolylhydrazone).
Anti-inflammatory therapy is actually devolved to glucocorticoids which prevent the release of arachidonic acid from phospholipids and consequently its subsequent transformation into prostaglandins and leukotrienes. This activity explains in part why steroids are better anti-inflammatory agents than acetylsalicylic acid (ASA)-like drugs which only reduce prostaglandin production. Despite their superior therapeutic actions, there are many side effects associated with corticosteroids. Therefore in recent years, research of non-steroid dual inhibitors of prostaglandin and leukotriene production has been developed. The present paper investigates the pharmacological activity of such a new compound, CBS-1108 (2-acetylthiophene-2-thiazolylhydrazone), in comparison with dexamethasone, cyclooxygenase inhibitors (ASA and indomethacin) and reference dual inhibitors (nordihydroguaiaretic acid (NDGA) and 3-amino-1-(m-trifluoromethylphenyl)-2-pyrazoline (BW-755 C]. The two-pathway inhibitors and ASA-like drugs are similarly effective on paracentesis-induced disruption of the blood-aqueous barrier and on croton oil-induced ear edema. On the contrary in an animal model of leukocyte migration and on mast cell degranulation, NDGA and CBS-1108 are very active when the other tested compounds are inefficient.
D000818:Animals; D000893:Anti-Inflammatory Agents; D001082:Aqueous Humor / Q000378:metabolism; D002465:Cell Movement / Q000187:drug effects; D003436:Croton Oil; D016861:Cyclooxygenase Inhibitors; D004487:Edema / Q000517:prevention & control; D005136:Eye Proteins / Q000378:metabolism; D007962:Leukocytes / Q000187:drug effects; D016859:Lipoxygenase Inhibitors; D008297:Male; D008407:Mast Cells / Q000378:metabolism; D011817:Rabbits; D012701:Serotonin / Q000378:metabolism; D013844:Thiazoles / Q000494:pharmacology*
D000893:Anti-Inflammatory Agents; D016861:Cyclooxygenase Inhibitors; D005136:Eye Proteins; D016859:Lipoxygenase Inhibitors; D013844:Thiazoles; D012701:Serotonin; D003436:Croton Oil; C041430:2-acetylthiophene-2-thiazolylhydrazone