Clotrimazole is a broad-spectrum antifungal belonging to the imidazole subclass of azole compounds, which interfere with the biosynthesis of ergosterol, a major membrane component of the fungal cytoplasmic membrane. Clotrimazole was discovered in 1969 and was developed by Schering Plough. It inhibits Ca2+-activated potassium channels. The compound has promising anti-cancer effects. Clotrimazole is a reversible inhibitor of cytochrome P450 (CYP450). In vitro-based CYP450 enzyme inhibition screening has been used to evaluate compound interactions.
Clotrimazole is freely soluble in water.
|Application||Clotrimazole is a reversible inhibitor of cytochrome P450 (CYP450). In vitro-based CYP450 enzyme inhibition screening has been used to evaluate compound interactions (Yan et al, 2002).|
|Mechanism of Action||Clotrimazole increases fungal cell permeability by inhibiting ergosterol synthesis, a major cell membrane component found exclusively in fungi, resulting in fungistatic properties. Specifically, it inhibits the microsomal cytochrome P450-dependent 14α-demethylase, which is critical to ergosterol biosynthesis.|
|Spectrum||Clotrimazole is broad-spectrum, targeting a broad range of fungi including Candida and Aspergillus species.|
|Eukaryotic Cell Culture Applications||Clotrimazole can be used to inhibit CYP450 in cell cultures.|
|Cancer Applications||Clotrimazole has promising anti-cancer properties, interfering with glycolytic enzymes, specifically their cellular distribution and activity. Clotrimazole induced a dose-dependent decrease in glucose uptake in three cell lines from human breast cancer cell lines (MCF10A, MCF-7 and MDA-MB-231), affecting the metabolism, growth, and migration. The compound was non-toxic to non-tumor human breast cell lines (Furtado et al, 2012).|
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