Subcellular distribution and antifungal effects of fluconazole in human phagocytic cells. Demonstration of the antifungal agent in neutrophil polymorphonuclear leucocytes and monocytes by autoradiography and electron micrography.
Electron microscopic autoradiography was used to demonstrate the presence of [3H] fluconazole (CAS 86386-73-4) in neutrophils and monocytes isolated from volunteers. Quantitative analysis of the autoradiographs showed significant accumulation of fluconazole in both phagocytic cells. The distribution of fluconazole was equal in the different intracellular compartments such as cytoplasm and nucleus. Fluconazole (20 micrograms/ml) induced ultrastructural changes in Candida albicans cells which had been phagocytized by neutrophils or monocytes (macrophages) in vitro. Particularly, changes in the plasma membrane and in the cytoplasmic structure of the intraphagocytic yeast cells were observed electron microscopically.
Wildfeur
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Department of Anatomy and Cellular Biology, University of Ulm, Fed. Rep. Germany.
Reisert
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I
Laufen
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H
D000935:Antifungal Agents / Q000378:metabolism / Q000494:pharmacology*; D001345:Autoradiography; D002176:Candida albicans / Q000187:drug effects; D015725:Fluconazole / Q000378:metabolism / Q000494:pharmacology*; D006801:Humans; D066298:In Vitro Techniques; D008854:Microscopy, Electron; D009000:Monocytes / Q000187:drug effects / Q000378:metabolism* / Q000648:ultrastructure; D009504:Neutrophils / Q000187:drug effects / Q000378:metabolism* / Q000648:ultrastructure; D009940:Organoids / Q000378:metabolism
D000935:Antifungal Agents; D015725:Fluconazole