5-Lipoxygenase inhibition by antifungal azole derivatives: new tools for immunosuppression?
The effect of novel azole derivatives (itraconazole and fluconazole) on 5-lipoxygenase activity was examined using human polymorphonuclear leukocytes (PMNL) as the enzyme source. The novel imidazole derivative itraconazole proved to be a potent inhibitor (IC50 2 X 10(-6) M) of 5-lipoxygenase activity. In contrast, fluconazole, an antifungal agent with bistriazole structure, had no effect on the Ca2+ ionophore A 23187-induced formation of 5-lipoxygenase metabolites in PMNL.
Jaschonek
K
K
Medizinische Klinik, Universität Tübingen, Federal Republic of Germany.
Steinhilber
D
D
Einsele
H
H
Ehninger
G
G
Roth
H J
HJ
D000935:Antifungal Agents / Q000494:pharmacology; D001091:Arachidonate Lipoxygenases / Q000037:antagonists & inhibitors*; D015725:Fluconazole / Q000494:pharmacology*; D006801:Humans; D007166:Immunosuppressive Agents; D066298:In Vitro Techniques; D017964:Itraconazole; D007654:Ketoconazole / Q000031:analogs & derivatives* / Q000494:pharmacology; D016859:Lipoxygenase Inhibitors; D009504:Neutrophils / Q000187:drug effects / Q000201:enzymology / Q000276:immunology
D000935:Antifungal Agents; D007166:Immunosuppressive Agents; D016859:Lipoxygenase Inhibitors; D017964:Itraconazole; D015725:Fluconazole; D001091:Arachidonate Lipoxygenases; D007654:Ketoconazole