• Mycobiology
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• v.31 no.2
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• pp.95-98
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• 2003

Aantifungal agents were tested against 30 clinical isolates of Cryptococcus neoformans var. neoformans using the NCCLS method(M27-A2). Posaconazole, itraconazole and amphotericin B had lower MIC than the remaining four antifungal agents. The MIC result for posaconazole was over 220-fold lower active than fluconazole. Fluconazole MICs for most isolates fell within the dose-dependant range. The overall MIC ranges and $MIC_{50}s$ were amphotericin B(0.03-0.25; 0.25), fluconazole(0.5-64; 16), itraconazole(0.015-1; 0.125), terbinafine(0.06->2; 1), caspofungin(8-32; 32), voriconazole(0.015-0.5; 0.25), and posaconazole(0.015-0.25; 0.06 ${\mu}g/ml$), respectively. In conclusion, the $MIC_{50}s$ of these drugs did not exhibit any sign of an upward shift with the exception of fluconazole and tendency cross-resistance between the seven drugs was not observed. We conclude that in vitro resistance to antifungal agents has not significantly changed despite the recent wide-spread use of triazoles for long-term treatment of Cryptococcal meningitis.

• Proceedings of the Korean Society of Applied Pharmacology
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• 1996.04a
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• pp.167-167
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• 1996

A series of 6-[(N-Halophenyl)amino] -7-Bromo-5,8-quinolinediones (BQs) newly synthesized were tested for antifungal activities, in vitro, against Candida sp., Aspergillus niger and Trichophyton mentagrophytes. The MIC values were determined by the twofold dilution method. Among these derivatives, BQ4 and 7 showed more potent antifungal activities than fluconazole and ketoconazole. BQ 4 and 7 were compared with fluconazole in the treatment of established systemic infections with Candida albicans in normal rats. Intraperitoneally administered BQs for 7 days and 14 days reduced Candida albicans colony count in kidneys and livers as well as fluconazole. The therapeutic potential of BQs has been assessed by evaluating their activities (survival rate) against systemic infections in normal mice with Candida albicans. These compounds, particularly showed activities comparable with fluconazole. BQ4 and 7 had about EO$\_$50/, 0.05, 0.06mg/kg but fluconazole had ED$\_$50/, 6.0mg/kg respectively.

• Proceedings of the PSK Conference
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• 2003.04a
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• pp.311.2-312
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• 2003

The purposes of this study were to evaluate bioequivalence (BE) using In-transformed pharmacokinetic parameters obtained from two fluconazole products and to develop the analytical methods for the quantitative determination of fluconazole in human serum. In addition, the in vitro dissolution profiles of the two fluconazole products at dissolution media: 0.1 M hydrochloride (KP Ⅶ Apparatus II method) were assessed. (omitted)

• Journal of Oral Medicine and Pain
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• v.33 no.1
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• pp.27-33
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• 2008

Candidiasis, an opportunistic infectious condition caused by the genus Candida, is the most common oral fungal infection in humans. The diagnosis of oral candidiasis can often be made based on recognition of its clinical pattern, but at times there is difficulty in making a clinical diagnosis because of its various manifestations. Several antifungal medications have been developed for managing fungal infections. Despite the availability of several effective antimycotics for the treatment of oral candidiasis, failure of therapy is not uncommon due to the unique environment of the oral cavity, where the flushing effect of saliva and the cleaning action of the oral musculature tend to reduce the drug concentration to sub-therapeutic levels. In this case report, we present two patients diagnosed with chronic hyperplastic candidiasis and median rhomboid glossitis, which are known as rare forms of candidiasis. In both cases, there was a significant reduction of clinical signs and symptoms when fluconazole was prescribed after the failure of initial nystatin therapy.

• Korean Journal of Clinical Laboratory Science
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• v.54 no.2
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• pp.133-141
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• 2022

Candida is one of the most common causes of bloodstream infections and a leading cause of morbidity and mortality among hospitalized patients. The purpose of this study was to provide important information for formulating empirical treatment plans for candidemia by investigating the antifungal resistance rate of Candida. Among the Candida strains (973 cases) isolated from blood culture tests at the S hospital in 2009~2018, 4.7% (N=44) comprising the Candida spp. (932 strains) showed resistance to fluconazole. The resistant strains included C. albicans, C. parapsilosis, C. tropicalis, and C. glabrata. In addition Candida spp. (947 strains) showed resistance to amphotericin B (N=6, 0.6%), flucytosine (N=23, 2.4%) and voriconazole (N=24, 3.1%). C. albicans was resistant to fluconazole (N=23, 6.9%) and voriconazole (N=21, 6.0%), The statistical analysis showed that C. albicans and non-albicans Candida species were resistant to fluconazole (P=0.039) and voriconazole (P<0.001). A monitoring system to understand the rate of candidiasis infections in a hospital setting is required. It is also important to make the right choice of the antifungal agent based on drug susceptibility patterns. Therefore, an infection surveillance policy that tracks Candida resistance through regular antifungal susceptibility tests is necessary.

• Bulletin of the Korean Chemical Society
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• v.34 no.12
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• pp.3867-3870
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• 2013

• YAKHAK HOEJI
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• v.39 no.4
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• pp.417-426
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• 1995

6-[(N-4-Chlorophenyl)amino]-7-chloro-5,8-quinolinedione (RCK20) was tested for antifungal activities, in vivo, against Candida albicans. RCK20 was compared vath ketoconazole and fluconazole in the treatment of systemic infection with Candida albicans in normal rats. The therapeutic potential of RCK20 had been assessed by evaluating their activities (survival rate) against systemic infections with in normal mice with Candida albicans. RCK20 improved survival rates as well as ketokonazole. RCK20 had ED$_{50}$. 0.25$\pm$0.18 mg/kg but ketoeonazole and fluconazole had ED$_{50}$, 8.00$\pm$0.73, 10$\pm$0.43 mg/kg respectively. Activities of RCK20 showed superior to that of ketoconazole and fluconazole. Intraperitoneauy administered RCK20 at the ED$_{50}$, 0.25 mg/kg for 7days and 14days reduced Candida albicans colony count in the kidneys and livers as well as ketoconazole and fluconazole at these ED$_{50}$, 8.00 and 10 mg/kg. Acute oral toxicity studies of RCK20 were carried out in ICR mice of both sexes. These acute oral toxicities of RCK20 were low and LD$_{50}$ values were over 2.850 mg/kg in ICR mice. The Genotoxicities of RCK20 had been evaluated. RCK20 was negative in Ames test with Salmonella typhimurium (TA98 and TA100). The clastogenicity was tested on the RCK20 with in vivo mouse micronucleus assay. RCK20 did not show any clastogenic effect in mouse peripheral blood and was negative in mouse micronucleus assay. These results indicate that RCK20 has no genotoxic potential under these experimental condition.

• YAKHAK HOEJI
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• v.59 no.6
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• pp.259-265
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• 2015

In recent, there are increasing reports about pharmacological activities of Crataegi Fructus which has been used for many centuries as medicinal and food sources in East Asia. However, its antifungal efficacy needs to be investigated. Thus, in the current study, we determined synergistic antifungal activity of the Crataegi Fructus extract (CFE) when combined with fluconazole (FLC) against disseminated candidiasis due to Candida albicans. This fungus is one of the most problematic fungal pathogens. Data resulting from a microdilution susceptibility test showed that CFE had a dose-dependent antifungal activity. When the extract was combined with FLC, the activity was synergistic. For example, the antifungal activity by the combination of CFE at $20{\mu}g/ml$ plus FLC at $0.1{\mu}g/ml$ was 4 times more effective than antifungal activity by FLC alone at the same concentration (P<0.05). In the murine model of disseminated candidiasis, the combination therapy potentiated resistance of mice, resulting in 80% of C. albicans-infected animals surviving the entire period of 40 days observation, whereas mice given CFE alone or FLC alone all died with 17 and 23 days, respectively, although they survived longer than the untreated control animals (P<0.05). The CFE's antifungal activity seemed to be related to the blockage of hyphal production of C. albicans yeast cells. In summary, CFE has a synergistic antifungal activity, which can be produced by combining CFE with FLC. Thus, our data strongly indicate that CFE may be a potential candidate as an antifungal agent for combination therapy.

• Journal of Veterinary Clinics
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• v.30 no.6
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• pp.473-477
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• 2013

A 7-year-old castrated male Maltese developed anemia, ascites with peritonitis, and vomiting after urethrostomy. A microbial culture test of the peritoneal fluid indicated Candida albicans. Antifungal therapy was administered with intravenous fluconazole combined with antibacterial therapy. The patient recovered completely 37 days after referral admission.

• Journal of Microbiology and Biotechnology
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• v.14 no.4
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• pp.693-697
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• 2004

YH-1715R, (2R,3R)-2-(2,4-difluorophenyl)-3-(3-methoxy-1,2,4-isothiazol-3-yl-thio)-1-( 1H-1,2,4-triazol-l-yl)-2-butanol, a new triazole derivative obtained by the structural modification of fluconazole, was found to exhibit potent anti-Candida activity against a wide variety of Candida albicans (C. albicans) (MIC: 0.4-12.5 mg/l). To investigate the mode of action of YH-1715R, its effect on ergosterol biosynthesis in cell-free extracts and whole cells of C. albicans was examined. The inhibitory activity of YH-1715R was approximately ten-fold higher than that of fluconazole. To determine the primary action mechanism of YH-1715R, its inhibitory activity against lanosterol $14\alpha$-demethylase (14$\alpha$-DM), a major target for azole, was measured using gas-liquid chromatography. YH-1715R and fluconazole were found to inhibit 14a-DM with an $IC_{50}$ of 0.015 $\mu$M and 0.01$8\mu$M, respectively, plus the mode of inhibition of YH-1715R and fluconozole was noncompetitive with a $K_i$ of 0.0533$\mu$M and 0.0975$\mu$M.