Fluconazole (UK-49,858) treatment of candidiasis in normal and diabetic rats

Fisher, Melanie; Lee, P G; Tarry, William F.

doi:10.1128/aac.33.7.1042

Cited by 11 publications

(9 citation statements)

References 17 publications

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“…One of these antifungal agents is the triazole fluconazole (Flu) (4,10,14,33,34,41). In vivo experimental studies suggested that Flu is active against disseminated candidiasis (8,9,29,31,32,35,37). Recently, the antifungal efficacy of Flu was demonstrated in persistently granulocytopenic rabbits when it was used for prevention or early treatment (39,40).…”

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confidence: 99%

Effects of amphotericin B and fluconazole on the extracellular and intracellular growth of Candida albicans

Etten

Rhee

Kampen

et al. 1991

Antimicrob Agents Chemother

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The effects of amphotericin B and fluconazole on the extracellular and intracellular growth of Candida albicans were studied. With respect to the extracellular growth of C. albicans, antifungal activity was measured in terms of MICs and minimal fungicidal concentrations as well as by determination of the concentration that effectively killed (>99.9%) C. albicans in the absence or presence (amphotericin B only) of serum. Amphotericin B was highly active in terms of killing, even at an increased inoculum size. In the presence of serum, amphotericin B activity was substantially reduced. For fluconazole, activity was restricted to inhibition of fungal growth, even after the inoculum size was reduced. With respect to the intracellular growth of C. albicans, antifungal activity was measured by using monolayers of murine peritoneal macrophages infected with C. albicans and was measured in terms of inhibition of germ tube formation as well'as effective killing (>99%) of C. albicans. Amphotericin B was highly active against C. albicans. At an increased ratio of infection, amphotericin B activity was slightly reduced. Fluconazole had no antifungal activity. Neither a reduction in the ratio of infection nor exposure of C. albicans to fluconaz'ole prior to macrophage ingestion resulted in activity against intracellular C. albicans by fluconazole. Previous exposure of C. albicans to amphotericin B resulted in increased intracellular activity of amphotericin B. The. intracellular antifungal activity of the combination of fluconazole with amphotericin B was les than that of amphotericin B alone. Amphotericin B showed fungicidal activity against C. albicans growing both extracellularly and intracellularly, whereas fluconazole inhibited growth only of extracellular C. albicans. A slight antagonistic effect between fluconazole and aiflphotericin B was found with respect to intracellular as well as extracellular C. albicans.Deep-seated candidal infections are an important cause of morbidity and mortality in immunocompromised patients (15,21,22). The current drug of choice for most systemic mycoses is still amphotericin B (AmB), but its use is restricted by a variety of toxic side effects (6,13,15,21,22). Consequently, there is a need for effective and less toxic drugs for the treatment of patients with these infections. One of these antifungal agents is the triazole fluconazole (Flu) (4,10,14,33,34,41). In vivo experimental studies suggested that Flu is active against disseminated candidiasis (8,9,29,31,32,35,37). Recently, the antifungal efficacy of Flu was demonstrated in persistently granulocytopenic rabbits when it was used for prevention or early treatment (39,40). Little is still known, however, on the role of Flu in the treatment of systemic candidiasis in immunocompromised patients. Since the host defense mechanisms in these patients are severely impaired, the intrinsic antifungal activity of the antifungal agent is of great importance for effective treatment. Unfortunately, standardized in vitro methods for assessment of ...

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confidence: 99%

Effects of amphotericin B and fluconazole on the extracellular and intracellular growth of Candida albicans

Etten

Rhee

Kampen

et al. 1991

Antimicrob Agents Chemother

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“…It was reported by Stojanovska et al, that administration of HFD and dexamethasone resulted in higher insulin resistance in rats compared to those treated with dexamethasone alone [22]. This finding could be correlated to the role of HFD in the stimulating of the expression of several proinflammatory cytokines and inflammatory responsive proteins in hypothalamus and this leads to impairment of the insulin-signaling pathway as described by Prada et al, [23].…”

Section: Discussionmentioning

confidence: 64%

“…Metformin (MET) was selected as a reference drug used to treat IR; it was administered orally in a dose of 400mg/kg/day [22]. Doses of fluconazole (20,40mg/kg/day) (FLU 20, 40) were selected and administered orally in accordance with Fisher et al, [23].…”

Section: Rat Aminotransferase (Ast) Colorimetric Kit Was Obtained From Biodiagnostic Comentioning

confidence: 99%

Fluconazole, a Fungal Cytochrome P450 Enzyme Inhibitor: The Potential Role in Augmenting Hepatotoxicity and Hyperinsulinemia Induced by Dexamethasone in Rats

et al. 2019

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“…Fifteen days after DM induction, rats in groups 3–8 were inoculated intraperitoneally with 0.2 mL of a suspension containing 10 5 colony forming units (CFU)/mL obtained from a clinical C. albicans strain (Fisher et al. 1989 ).…”

Section: Methodsmentioning

confidence: 99%

Nanoparticle formulation increases Syzygium cumini antioxidant activity in Candida albicans -infected diabetic rats

Bitencourt

Cargnelutti

Stein

et al. 2017

Pharmaceutical Biology

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Context:Syzygium cumini (L.) Skeels (Myrtaceae) is a medicinal plant widely used in folk medicine for the treatment of diabetes mellitus (DM). However, studies on the use of this plant and of nanoparticle formulations against DM-related fungal infections are scarce.Objective: To evaluate the effect of the treatments with aqueous seed extract of S. cumini (ASc) and ASc-loaded polymeric nanoparticles (NPASc) on biochemical parameters in Candida albicans-infected diabetic rats.Materials and methods: Male Wistar rats were divided into eight groups: Control, DM, C. albicans, C. albicans + ASc, C. albicans + NPASc, DM + C. albicans, DM + C. albicans + ASc and DM + C. albicans + NPASc. Rats were daily treated with ASc or NPASc (100 mg/kg) for 21 days. Biochemical parameters in serum and urine, advanced oxidation protein product (AOPP) and TBARS levels in the serum, kidney, liver and pancreas and N-acetyl-β-d-glucosaminidase (NAG) activities in kidney and urine were evaluated.Results: Biochemical and oxidative stress parameters increased in rats with DM and/or candidiasis. NPASc was more effective than ASc in decreasing glucose (56%), cholesterol (33%) and creatinine (51%) levels; serum (16%) and pancreatic (46%) AOPP and renal (48%) TBARS levels when compared with DM + C. albicans group. In C. albicans group, both treatments decreased NAG activity but did not decrease creatinine levels.Conclusions: These data suggest that the use of nanotechnology is able to improve plant extract properties such as antioxidant activity that may be useful in diabetes-related complications.

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Fluconazole (UK-49,858) treatment of candidiasis in normal and diabetic rats

Cited by 11 publications

References 17 publications

Effects of amphotericin B and fluconazole on the extracellular and intracellular growth of Candida albicans

Effects of amphotericin B and fluconazole on the extracellular and intracellular growth of Candida albicans

Fluconazole, a Fungal Cytochrome P450 Enzyme Inhibitor: The Potential Role in Augmenting Hepatotoxicity and Hyperinsulinemia Induced by Dexamethasone in Rats

Nanoparticle formulation increases Syzygium cumini antioxidant activity in Candida albicans -infected diabetic rats

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