• 한국미생물·생명공학회지
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• 제47권4호
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• pp.651-661
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• 2019

Targeting the pathogen viability using drugs is associated with development of drug resistance due to selective pressure. Hence, there is an increased interest in developing agents that target bacterial virulence. In this study, the inhibitory effect of ciclopirox, an antifungal agent with iron chelation potential, on the microbial virulence factors was evaluated in 26 clinical MDR Pseudomonas aeruginosa isolates collected from Alexandria Main University Hospital, a tertiary hospital in Egypt. Treatment with 9 ㎍/ml ciclopirox inhibited the hemolytic activity in 70% isolates, reduced pyocyanin production, decreased protease secretion in 46% isolates, lowered twitching and swarming motility, and decreased biofilm formation by 1.5- to 4.5-fold. The quantitative real-time PCR analysis revealed that treatment with ciclopirox downregulated the expression levels of alkaline protease (aprA) and pyocyanin (phzA1). Ciclopirox is used to treat hematological malignancies and the systemic administration of ciclopirox is reported to have adequate oral absorption with a satisfactory drug safety profile. It is important to calculate the appropriate clinical dose and therapeutic index to reposition ciclopirox from a topical antifungal agent to a promising virulence-modifying agent agent against P. aeruginosa, a problematic Gram-negative pathogen.

• 한국생물정보학회:학술대회논문집
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• 한국생물정보시스템생물학회 2005년도 BIOINFO 2005
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• pp.139-143
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• 2005

Cytochrome P450 14${\alpha}$-sterol demethylase enzyme (CYP51) is the target a of azole type antifungals. The azole blocks the ergosterol synthesis and thereby inhibits fungal growth. A three-dimensional (3D) homology model of CYP51 from Candida albicans was constructed based on the X-ray crystal structure of CYP51 from Mycobacterium tuberculosis. Using this model, the binding modes for the substrate (24-methylene-24, 25-dihydrolanosterol) and the known inhibitors (fluconazole, voriconazole, oxiconazole, miconazole) were predicted from docking. Virtual screening was performed employing Structure Based Focusing (SBF). In this procedure, the pharmacophore models for database search were generated from the protein-ligands interactions each other. The initial structure-based virtual screening selected 15 compounds from a commercial available 3D database of approximately 50,000 molecule library, Being evaluated by a cell-based assay, 5 compounds were further identified as the potent inhibitors of Candida albicans CYP51 (CACYP51) with low minimal inhibitory concentration (MIC) range. BMD-09-01${\sim}$BMD-09-04 MIC range was 0.5 ${\mu}$g/ml and BMD-09-05 was 1 ${\mu}$g/ml. These new inhibitors provide a basis for some non-azole antifungal rational design of new, and more efficacious antifungal agents.

• 대한수의학회지
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• 제22권2호
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• pp.139-147
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• 1982

A total of 133 isolates of yeast-like fungi was tested for sensitivity to seven different antifungal agents. The yeast-like fungi tested were isolated from the milk from normal or mastitic bovine quaters or from bovine feces. They were 5 Candida albicans (C. albicans) isolates, 63 C. krusei, 27 C. tropicalis, 5 C. parapsilosis, 10 Torulopsis glabrata, 6 Rhodotorula sp., 6 Hansenula sp. and 1 Pichia sp. isolate. The antifungal agents tested were nystatin, griseofulvin, cycloheximide, 5-fluorocytosine, miconazol, clotrimazole and tolnaftate. In general, clotrimazole, miconazol and 5-fluorocytosine were more effective in antifungal activity in vitro against the test organisms than the rest of the agents tested. However, some of the isolates showed higher resistance to certain antifungal agents compared to the other isolates of the some species. They were: 1 C. albicans isolate to 5-fluorocytosine; 1 C. albicans to 5-fluorocytosine, miconazol and clotrimazole; 1 C. krusei to 5-fluorocytosine and cycloheximide; and 11 C. tropicalis isolates to cycloheximide. The minimum inhibitory concentrations(MIC) of clotrimazole were $12.5{\mu}g/ml$ or lower for all isolates tested except one C. albicans isolate, for which MIC of the drug was $100{\mu}g/ml$. On the other hand, the MIC's of cycloheximide were $6.5{\mu}g/ml$ or lower for all isolates except the following; all isolates of C. albicans ($100{\mu}g/ml$), C. pseudotropicalis ($200{\mu}g/ml$) and Rhodotorula sp. ($25-50{\mu}g/ml$), 11 C. tropicalis isolates ($100{\mu}g/ml$) and 1 C. krusei isolate ($200{\mu}g/ml$).

• Mycobiology
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• 제47권2호
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• pp.242-249
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• 2019

Betaine derivatives are considered major ingredients of shampoos and are commonly used as antistatic and viscosity-increasing agents. Several studies have also suggested that betaine derivatives can be used as antimicrobial agents. However, the antifungal activity and mechanism of action of betaine derivatives have not yet been fully understood. In this study, we investigated the antifungal activity of six betaine derivatives against Malassezia restricta, which is the most frequently isolated fungus from the human skin and is implicated in the development of dandruff. We found that, among the six betaine derivatives, lauryl betaine showed the most potent antifungal activity. The mechanism of action of lauryl betaine was studied mainly using another phylogenetically close model fungal organism, Cryptococcus neoformans, because of a lack of available genetic manipulation and functional genomics tools for M. restricta. Our genome-wide reverse genetic screening method using the C. neoformans gene deletion mutant library showed that the mutants with mutations in genes for cell membrane synthesis and integrity, particularly ergosterol synthesis, are highly sensitive to lauryl betaine. Furthermore, transcriptome changes in both C. neoformans and M. restricta cells grown in the presence of lauryl betaine were analyzed and the results indicated that the compound mainly affected cell membrane synthesis, particularly ergosterol synthesis. Overall, our data demonstrated that lauryl betaine influences ergosterol synthesis in C. neoformans and that the compound exerts a similar mechanism of action on M. restricta.

• 생약학회지
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• 제25권3호
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• pp.293-304
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• 1994

In order to estimate accurate originality of the important crude drugs, Gastrodia, Dendrobium, Bletilla and Cremastra spp. were investigated comparing their morphological, anatomical and physicochemical characteristics and antibacterial, antifungal activities. The results of the studies as follows: 1. In morphological and anatomical studies, Korean Gastrodia contained more mucilage duct and symbiotic fungi than imported Gastrodia. Korean Dendrobium contained starch grains but without starch grains in the imported Dendrobium from China enclosed with thicken silicified wall. The corm of Cremasta appendiculata contained raphides of bundles with mucilage while the bulbs of Tulipa edulis contained several various starch grains form. 2. In physiological and TLC analysis, crude drugs in Orchidaceae contained common constituents with fluorescence and much mucilage. 3. The EtOH extracts of Gastrodia, Dendrobium, Bletilla, Cremastra showed antibacterial activities against B. subtilis and E. coli (Dendrobium>Gastrodia>Bletilla>Cremastra). But, no antifungal activities against C. albicans, A. niger were observed.

• Archives of Pharmacal Research
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• 제27권3호
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• pp.295-299
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• 2004

The antifungal activities of the essential oil from Agastache rugosa and its main component, estragole, combined with ketoconazole, one of the azole antibiotics commonly used to treat infections caused by Trichophyton species, were evaluated in this study. The combined effects were measured by the checkerboard microtiter and the disk diffusion tests, against T. erinacei, T. mentagrophytes, T. rubrum, T. schoenleinii and T. soudanense. Susceptibility of the five Trichophyton species to the oil alone, or ketoconazole alone, differed distinctly. The fractional inhibitory concentration indices (FICI) of ketoconazole combined with estragole or A. rugosa essential oil, against the tested Trichophyton species, were between 0.05 and 0.27, indicating synergistic effects. These drug combinations exhibited the most significant synergism against T. mentagrophytes, with FICIs of 0.05 and 0.09 for estragole and the essential oil fraction from A. rugosa, respectively. Isobolograms based on the data from checkerboard titer tests also indicated significant synergism between ketoconazole and the Agastache oil fraction or estragole, against the Trichophyton species evaluated. Trichophyton susceptibility to ketoconazole was significantly improved by combination with the Agastache rugosa oil fraction or its main component, estragole.

• 구강회복응용과학지
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• 제38권2호
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• pp.120-126
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• 2022

심한 의치성 구내염의 경우, 항진균제의 처방이 효과적이지 않은 경우가 있다. 이번 증례는 5개월간 fluconazole을 처방받았으나, 증상의 개선이 없었던 72세의 환자에 증례이다. 본원의 재진단을 거쳐 약물치료를 시행하였고, 임시의치를 제작하여, 구강회복을 기하고자 하였다. 그러나 계속되는 약물치료에도 구강상태가 호전되지 않는 증례에서 미생물학적인 분석 및 보조요법이 도움이 될 수 있음을 본 증례를 통해 살펴보고자 한다.

• 약학회지
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• 제56권3호
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• pp.204-209
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• 2012

The purpose of this study was to construct database for a drug safety information website to serve as an access point of up-to-date resources for a wide variety of drug-safety information helping patients and healthcare professionals make well-informed decisions about medication use. All the contents developed were confirmed by the council of advisors who were the experts in drug safety. The detailed contents of database on frequently prescribed drug including 9 NSAIDs, 19 antibiotics, 24 cardiovascular, 21 metabolic, 14 respiratory, 20 digestive, 22 hormonal, 10 genitourinary, 10 anti-allergic, 27 antifungal/antiviral, and 71 neuropsychiatric agents were developed based on the approved drug labeling of the Korean FDA. A separately searchable database of drug-specific safety information for patients and health professionals was constructed for users in need of different depth of knowledge on using medications safely. The safety information on highly prevalent chronic diseases and drug classes was also developed. Finally the most recent global drug safety news was provided. The consumer directed information was developed in layman's terms as means of proving user-friendly information. The creation of this type of website is part of the Korean FDA's ongoing initiative to address and promote the safe use of medications for the public.

• 대한수의학회지
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• 제41권2호
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• pp.173-176
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• 2001

개 피부병 유래 Microsporum canis 57주와 표준균주 1주 등 58주를 broth microdilution test로 계통이 다른 7가지 항진균제에 대한 감수성을 조사하고 고찰하였다. M canis의 항진균주에 대한 MIC(기하평균) 측정에서 terbinafine은 $MIC{\leq}0.004{\sim}0.031(0.007){\mu}g/ml$, itraconazole은 $MIC{\leq}0.004{\sim}0.125(0.029){\mu}g/ml$, ketoconazole은 MIC $0.015{\sim}0.5(0.097){\mu}g/ml$, tolnaftage은 MIC $0.031{\sim}1(0.155){\mu}g/ml$순으로 감수성이 높았고, griseofulvine은 MIC $0.063{\sim}2(0.285){\mu}g/ml$, amphotericin B는 MIC $0.125{\sim}2(0.540){\mu}g/ml$, flucytosine(5-Fe)은 MIC $4{\sim}64(26.430){\mu}g/ml$으로 감수성이 낮았다.

• 한국자원식물학회:학술대회논문집
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• 한국자원식물학회 2019년도 추계학술대회
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• pp.103-103
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• 2019

Glycyrrhizae radix, commonly known as licorice, is a perennial herb belonging to Leguminosae and also includes various components such as, glycyrrhizin, liquiritin, liquiritigenin and isoliquiritigenin etc. Licorice has been widely used in East Asia as a medicine having pharmacological effects like antioxidants, anti-bacterial, anti-inflammatory, anti-cancer and immune modulatory activities. Among various licorice, Glycyrrhiza (G.) uralensis G. glabra and G. inflata are used for pharmaceutical purposes in Korea. However, cultivation of licorice has some problems such as low quality, low productivity, and early leaf drop. Korea Rural Development Administration developed new cultivars Wongam and Sinwongam, which are improved in cultivation and quality. To register the newly developed cultivar (s) on Ministry of Food and Drug Safety in Korea as a medicine, it is necessary to prove the similarity and difference through the comparative studies between already-registered species and new cultivars. Some fungi and bacteria usually in the human oral cavity and intestines exist as harmless state in human body. Also, the skin and genital infections by fungi can lead to toxic systemic infections and are accompanied by flushing, rashes, burning or painful sensation. The influences of licorice varieties on fungi and bacteria might be an evidence to prove the outstanding effect of newly developed licorice variety. In this study, the antifungal and antibacterial activity was investigated using newly developed licorice varieties Wongam, and Sinwongam against various fungi and bacteria. These results means newly developed licorice could be used as a replacement of already-registered species in terms of antifungal and antibacterial application.