Improved method for estimation of azole antifungal inhibitory concentrations against<i>Candida</i>species, based on azole/antibiotic interactions

Odds, Frank C.; Abbott, A.B.; Pye, G.; Troke, Peter F.

doi:10.1080/02681218680000461

Cited by 47 publications

(25 citation statements)

References 8 publications

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“…Since econazole appears to be bound strongly by serum proteins, it is unsuitable for systemic therapy. The in vitro antifungal activity of econazole is comparable to that of miconazole; broad-spectrum activity against dermatophytes, Candida species, other pathogenic yeasts, filamentous fungi, and some gram-positive bacteria (26,202,255,303).…”

Section: Econazolementioning

confidence: 80%

“…In an assay to test for the suppression of intracellular ATP synthesis, terconazole had no effect. Other tested triazoles also had no effect in this assay (202).…”

Section: Antifungal Imidazoles Under Developmentmentioning

confidence: 96%

“…In in vitro studies, tioconazole was fourfold more active than miconazole against Candida species and was more potent than miconazole against isolates of Cryptococcus neoformans, Torulopsis glabrata, and several species of dermatophytes; tiocona-zole was comparable to miconazole against Aspergillus species (145). In vitro studies by Odds and co-workers (201,202) and Lefler and Stevens (174) also demonstrated the broad-spectrum activity of tioconazole in comparison to other azole derivative antifungal drugs.…”

Section: Tioconazolementioning

confidence: 97%

“…To the contrary, Preusser and Rostek (230) found no mitochondrial damage in their ultrastructural studies of the effect of econazole on Trichophyton rubrum and C. albicans. Biochemically, inhibition of enzyme-catalyzed release of spheroplasts of young cells of C. albicans has been shown (13), as well as suppression of ATP concentrations in the fungus (202). Others have demonstrated complete release of ['4C]aminoisobutyric acid from cells of C. albicans, suggesting direct membrane damage to the yeast (103).…”

Section: Econazolementioning

confidence: 99%

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Overview of medically important antifungal azole derivatives

1988

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Fungal infections are a major burden to the health and welfare of modern humans. They range from simply cosmetic, non-life-threatening skin infections to severe, systemic infections that may lead to significant debilitation or death. The selection of chemotherapeutic agents useful for the treatment of fungal infections is small. In this overview, a major chemical group with antifungal activity, the azole derivatives, is examined. Included are historical and state of the art information on the in vitro activity, experimental in vivo activity, mode of action, pharmacokinetics, clinical studies, and uses and adverse reactions of imidazoles currently marketed (clotrimazole, miconazole, econazole, ketoconazole, bifonazole, butoconazole, croconazole, fenticonazole, isoconazole, oxiconazole, sulconazole, and tioconazole) and under development (aliconazole and omoconazole), as well as triazoles currently marketed (terconazole) and under development (fluconazole, itraconazole, vibunazole, alteconazole, and ICI 195,739).

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Section: Econazolementioning

confidence: 80%

“…In an assay to test for the suppression of intracellular ATP synthesis, terconazole had no effect. Other tested triazoles also had no effect in this assay (202).…”

Section: Antifungal Imidazoles Under Developmentmentioning

confidence: 96%

Section: Tioconazolementioning

confidence: 97%

Section: Econazolementioning

confidence: 99%

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Overview of medically important antifungal azole derivatives

1988

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“…In the 1970s and 1980s, synergy between TET and AMB was observed clinically and in animal models with wildtype strains of C. albicans, Aspergillus species and Cryptococcus species (Graybill & Mitchell, 1980;Kwan et al, 1972;Odds et al, 1986;Raab & Hogl, 1980;Rubin et al, 1983). However, no molecular mechanism was elucidated at the time for any of these species and it is important to revisit this phenomenon as the use of TETregulatable promoters in these species has become increasingly common and as standardized methods of determining MIC have been defined.…”

Section: Introductionmentioning

confidence: 99%

Tetracycline alters drug susceptibility in Candida albicans and other pathogenic fungi

et al. 2008

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The tetracycline (TET) promoter has been used in several systems as an inducible regulator of gene expression. In control analyses, the standard Candida albicans laboratory strain SC5314 was found to have altered susceptibility to a variety of antifungal drugs in the presence of relatively high concentrations (50-200 mg ml "1 ) of TET. Altered susceptibility was most notable with exposure to amphotericin B (AMB), with a 32-fold increase in susceptibility, and terbinafine (TRB), with a 32-fold decrease in susceptibility. The TET/AMB synergy was observed in several clinical isolates of C. albicans and in the distantly related species Aspergillus fumigatus and Cryptococcus neoformans. The TET/AMB synergy is not related to efflux pump activity, as determined by FACS analyses and by analysis of a strain containing efflux pump deletions. Gene expression analyses by luciferase and by quantitative real-time reverse transcriptase PCR failed to identify significant alterations in expression of any genes associated with resistance. C. albicans grown with TET for 48 h does show a reduction in total cellular ergosterol. Analysis of growth curves suggests that the TET effect is associated with lack of a diauxic shift, which is related to a loss of mitochondrial function. MitoTracker fluorescent dye was used to demonstrate that TET has a direct effect on mitochondrial function. These results demonstrate the need for careful analysis of TET effects when using a TET-inducible promoter, especially in studies that involve antifungal drugs. This study defines some limits to the use of the TET-inducible promoter, and identifies effects on cells that are the result of TET exposure alone, not the result of expression of a targeted gene.

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