• Korean Journal of Pharmacognosy
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• v.25 no.3
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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.

• Journal of Microbiology and Biotechnology
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• v.15 no.3
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• pp.652-655
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• 2005

This paper describes the development of an enzymatic assay system for the identification of inhibitors of isocitrate lyase (ICL), one of the key enzymes of the glyoxylate cycle that is considered as a new target for antifungal drugs. A 1.6 kb DNA fragment encoding the isocitrate lyase from Candida albicans ATCC10231 was amplified by PCR, cloned into a vector providing His-Patch-thioredoxin-tag at the N-terminus, expressed in Escherichia coli, and purified by metal chelate affinity chromatography. The molecular mass of the purified ICL was approximately 62 kDa, as determined by SDS-PAGE, and the enzyme activity was directly proportional to incubation time and enzyme concentration. The effects of itaconate-related compounds on ICL activity were also investigated. Among them, itaconic acid, 3-nitropropionate, and oxalate had strong inhibitory activities with $IC_{50}$ values of 5.8, 5.4 and $8.6\;{mu}g/ml$, respectively. These inhibitors also exhibited antifungal activity on YPD agar media containing acetate as a sole carbon source, albeit at high concentration. The results indicate that the C. albicans ICL may be a regulatory enzyme playing a crucial role in fungal growth and is a prime target for antifungal agents.

• The Plant Pathology Journal
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• v.40 no.2
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• pp.218-224
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• 2024

Plants are treasure trove of novel compounds that have potential for antifungal chemicals and drugs. In our previous study, we had screened plant extracts obtained from more than eight hundred plant materials collected in Korea, and found that butanol fraction of the Actinostemma lobatum were most potent in suppressing growth of diverse fungal pathogens of plants. Here in this study, we describe further analysis of the butanol fraction, and summarize the results of subsequent antifungal activity test for the sub-fractions against a selected set of plant pathogenic fungi. This line of analyses allowed us to identify the sub-fractions that could account for a significant proportion of observed antifungal activity of initial butanol fraction from A. lobatum. Further analysis of these sub-fractions and determination of structure would provide the shortlist for novel compounds that can be a lead to new agrochemicals.

• Bulletin of the Korean Chemical Society
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• v.31 no.12
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• pp.3684-3692
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• 2010

A series of azole-containing piperazine derivatives have been designed and synthesized. The obtained compounds were investigated in vitro for their antibacterial, antifungal and cytotoxic activities. The preliminary results showed that most compounds exhibited moderate to significant antibacterial and antifungal activities in vitro. 1-(4-((4-chlorophenyl) (phenyl)methyl)piperazin-1-yl)-2-(1H-imidazol-1-yl)ethanone and 1-(4-((4-Chlorophenyl)(phenyl)methyl)piperazin-1-yl)-2-(2-phenyl-1H-imidazol-1-yl)ethanone gave remarkable and broad-spectrum antimicrobial efficacy against all tested strains with MIC values ranging from 3.1 to $25\;{\mu}g/mL$, and exhibited comparable activities to the standard drugs chloramphenicol and fluconazole in clinic. Moreover, 2-((4-((4-chlorophenyl)(phenyl)methyl)piperazin-1-yl)methyl)-1H-benzo[d]imidazole was found to be the most effective in vitro against the PC-3 cell line, reaching growth inhibition values (36.4, 60.1 and 76.5%) for each tested concentration: $25\;{\mu}g/mL$, $50\;{\mu}g/mL$ and $100\;{\mu}g/mL$ in dose-dependent manner. The results also showed that the azole ring had noticeable effect on their antimicrobial and cytotoxic activities, and imidazole and benzimidazole moiety were much more favourable to biological activity than 1,2,4-triazole.

• Microbiology and Biotechnology Letters
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• v.38 no.1
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• pp.13-18
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• 2010

Past decade systemic mycoses caused by opportunistic human fungal pathogens, including Candida, Aspergillus, and Cryptococcus, have been a growing problem for both immunocompromised and immunocompetent individuals. Particularly, Cryptococcus neoformans has recently emerged as a major fungal pathogen, which can cause fungal pneumonia and meningitis that are lethal if not timely medicated. However, treatment for cryptococcosis has been difficult due to a lack of proper anti-cryptococcal drugs with fungicidal activity and less toxicity. In this review we introduced novel therapeutic methods for treating cryptococcosis by exploring pathogenomic signa1ing networks of C. neoformans with genome-wide transcriptome approaches as well as diverse molecular/genetic tools.

• Journal of Microbiology and Biotechnology
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• v.24 no.9
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• pp.1216-1225
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• 2014

Biofilm-related infections of Candida albicans are a frequent cause of morbidity and mortality in hospitalized patients, especially those with immunocompromised status. Options of the antifungal drugs available for successful treatment of drug-resistant biofilms are very few, and as such, new strategies need to be explored against them. The aim of this study was to evaluate the efficacy of phenylpropanoids of plant origin against planktonic cells, important virulence factors, and biofilm forms of C. albicans. Standard susceptibility testing protocol was used to evaluate the activities of 13 phenylpropanoids against planktonic growth. Their effects on adhesion and yeast-to-hyphae morphogenesis were studied in microplate-based methodologies. An in vitro biofilm model analyzed the phenylpropanoid-mediated prevention of biofilm development and mature biofilms using XTT-metabolic assay, crystal violet assay, and light microscopy. Six molecules exhibited fungistatic activity at ${\leq}0.5mg/ml$, of which four were fungicidal at low concentrations. Seven phenylpropanoids inhibited yeast-to-hyphae transition at low concentrations (0.031-0.5 mg/ml), whereas adhesion to the solid substrate was prevented in the range of 0.5-2 mg/ml. Treatment with ${\leq}0.5mg/ml$ concentrations of at least six small molecules resulted in significant (p < 0.05) inhibition of biofilm formation by C. albicans. Mature biofilms that are highly resistant to antifungal drugs were susceptible to low concentrations of 4 of the 13 molecules. This study revealed phenylpropanoids of plant origin as promising candidates to devise preventive strategies against drug-resistant biofilms of C. albicans.

• Biomedical Science Letters
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• v.3 no.1
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• pp.49-54
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• 1997

Meanwhile Pityrosporum species as well as Candida species in yeast phase are not pathogenic, Pityrosporum in mycelial phase is pathogenic. Pityrosporum species can be isolated not only from tinea versicolor patients but also from ninety (90) percent of healthy persons. Minimal inhibitory concentration (MIC) of ketoconazole against Pityrosporum spp. was 0.05~0.8$\mu\textrm{g}$ ml$^{-1}$and the MIC of ketoconazole was the lowest. Of itraconazole, selenium sulfide, sodium thiosulfate and ketoconazole had the lowest MIC against P. orbiculare. The P. orbiculare strains isolated from healthy persons were inhibited by lower MIC than those isolated from tinea versicolor patients. P. ovale strains were inhibited by lower MIC at MIC$_{50}$ and MIC$_{90}$ of oral and topical antifungal agents than p. orbiculare.

• Journal of Oral Medicine and Pain
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• v.46 no.2
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• pp.33-40
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• 2021

Purpose: Oral candidiasis is the most common fungal infection in the oral cavity which is usually diagnosed from clinical findings. A retrospective study was conducted to identify risk factors for oral candidiasis and to characterize the demographic and clinical features of affected patients. Methods: From January 1, 2019 to December 31, 2019, it consisted of 90 oral candidiasis patients diagnosed based on clinical finding and treated with antifungal drugs. As a retrospective study of those people, surveys were conducted on sex, age, systemic disease, a use of dentures, complaints of dry mouth, smoking and alcohol consumption, culture on potato dextrose agar (PDA) medium, culture on chromogenic agar (CA) medium and a duration of antifungal treatment. Results: Among 90 selected patients, the male and female ratio was 41:49. Overall, female had a higher infection rate than male in all age groups. In this study, oral candidiasis was not clearly susceptible to dry mouth, smoking or drinking, wearing dentures and association with systemic disease. Among 90 patients with oral candidiasis, 83 had colonies formed on PDA medium and 53 had colonies formed on CA medium. The duration of antifungal treatment was highest between 5 and 8 weeks. In addition, there was statistical significance between the culture results in CA medium and the duration of antifungal treatment. Conclusions: Generally, old age or infants, dry mouth, smoking, a use of dentures and endocrine abnormalities are risk factors to increase oral candidiasis; however, in this study, it was mainly found in the elderly aged 60 or older regardless of sex and the incidence of oral candidiasis was not obviously related with patients with dry mouth, smoking or drinking, denture wearers and endocrine abnormalities. Interestingly, when the fungi were cultured in CA medium, the duration of antifungal treatment was increased.

• Korean Journal of Clinical Pharmacy
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• v.34 no.1
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• pp.71-78
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• 2024

Background: Oral cancer drugs, particularly tyrosine kinase inhibitors (TKIs), are increasingly popular due to their convenience. However, they pose challenges like drug interactions, especially with medications like azole antifungals. While the FDA provides some guidance, more detailed information is needed to manage these interactions effectively. A meta-analysis was conducted to understand the impact of interactions between TKIs and azole antifungals on adverse events during clinical studies. Methods: A meta-analysis followed PRISMA guidelines. Data from PubMed, EMBASE, and references were searched until November 30, 2021. Inclusion criteria encompassed studies on TKI-antifungal interactions in English. Study selection and quality assessment were conducted by two independent investigators. Results: Out of 158 articles, 11 were selected for analysis. Combination therapy showed a slight increase in adverse events but was not statistically significant (OR 1.02, 95% CI 0.49-2.13, p=0.95). AUC and Cmax fold changes did not significantly impact adverse event development. Both itraconazole and ketoconazole showed no significant difference in adverse event development compared to TKI alone. Conclusions: Study finds TKI-DDI not significantly linked to AE increase; azole antifungal types not related to AE. Future DDI research crucial for drug development.

• Journal of Food Hygiene and Safety
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• v.8 no.3
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• pp.141-145
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• 1993

Thirty nine kinds of Korean herb drugs have screened for antimicrobial activity of some pathogenic microorganisms. It was revealed that some of hot water extracts from herb drugs showed antimicrobial activity in one or more strain of pathogenic microorganisms. Phellodendron amurense and Coptis chinensis inhibited growth of Staphylococcus aureus. Rubus coreanus showed antibacterial activity in Staphylococcus aureus and Pseudomonas aeruginosa. Citrus unshill inhibited growth of Escherichia coli and Cornus officinalis showed antibacterial activity in E. coli and Pseudomonas aeruginosa. Dioscorea battltas and Cinnamomum cassia showed antibacterial activity in Pseodomonas aeruginosa. And also, ScutelJa baicaJerrsis inhibited growth of Candida albicanus. Achyranthes japonica and Glycyrrhiza uralensis showed antifungal activity in Aspergillus niger. It was noteworthy that Glycrrhiza uranensis inhibited growth of Staphylococcus aureus, E. coli, Pseudomonas aeruginosa and Aspergillus niger.