Journal
CHEMICAL BIOLOGY & DRUG DESIGN
Volume 72, Issue 3, Pages 225-228Publisher
WILEY
DOI: 10.1111/j.1747-0285.2008.00694.x
Keywords
anti-inflammatory activity; fluconazole; imidazole antimycotics; itraconazole; ketoconazole; leukotriene B-4; molecular structure; neutrophils; platelet-activating factor; voriconazole
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The objective of this study was to compare the anti-inflammatory potencies of the imidazole antimycotics, fluconazole, itraconazole, ketoconazole and voriconazole (0.5 and 5 mu M) in relation to their molecular structures. Anti-inflammatory activity was determined according to the magnitude of inhibition of production of leukotriene B-4 and influx of Ca2+ following activation of the cells with the chemo-attractant platelet-activating factor (200 nM), using enzyme-linked immunosorbent assay and spectrofluorometric procedures, respectively. Treatment of platelet-activating factor-activated neutrophils with the imidazole antimycotics resulted in inhibition of production of leukotriene B-4 and attenuation of Ca2+ influx, the order of potency being itraconazole > ketoconazole > fluconazole = voriconazole. These observations demonstrate the requirement for both the diazole/triazole moiety (all four agents), and the substituted phenylpiperazinyl ether side chain (itraconazole and ketoconazole only) for maximal anti-inflammatory activity of this class of pharmacological agents.
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