• Mycobiology
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• v.47 no.2
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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.

• Bulletin of the Korean Chemical Society
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• v.33 no.8
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• pp.2627-2634
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• 2012

Strobilurins are one of the most important classes of agricultural fungicides. To discover new strobilurin derivatives with high activity against resistant pathogens, a series of novel ${\beta}$-methoxyacrylate analogues were designed and synthesized by integrating substituted pyrimidine with a strobilurin pharmacophore. The compounds were confirmed and characterized by infrared, $^1H$ nuclear magnetic resonance, elemental analysis and mass spectroscopy. The bioassays indicated that most of the compounds (1a-1h) exhibited potent antifungal activities against Colletotrichum orbiculare, Botrytis cinerea Pers and Phytophthora capsici Leonian at the concentration of 50 ${\mu}g/mL$. Exhilaratingly, compound 1d (R=3-trifluoromethylphenyl) showed better antifungal activity against all the tested fungi than the commercial strobilurin fungicide azoxystrobin.

• Journal of Microbiology and Biotechnology
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• v.28 no.7
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• pp.1086-1093
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• 2018

Honokiol, a bioactive compound isolated from the cone and bark of Magnolia officinalis, has been shown to have various activities including inhibition of the growth of Candida albicans. We investigated the roles of the Hsp90-calcineurin pathway in the antifungal activity of honokiol. The pharmacologic tool was employed to evaluate the effects of Hsp90 and calcineurin in the antifungal activity of honokiol. We also evaluated the protective effects of the calcineurin inhibitor cyclosporin A (CsA) on honokiol-induced mitochondrial dysfunction by the fluorescence staining method. The Hsp90 inhibitor potentiated the antifungal activity of honokiol. A C. albicans strain with the calcineurin gene deleted displayed enhanced sensitivity to honokiol. However, co-treatment with calcineurin inhibitor CsA attenuated the cytotoxic activity of honokiol due to the protective effect on mitochondria. Our results provide insight into the action mechanism of honokiol.

• Korean Journal of Pharmacognosy
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• v.32 no.2 s.125
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• pp.140-144
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• 2001

The composition of essential oils in the leaves of three cultivars (Ban-Chung-Gat, Chung-Gat and Dolsan-Gat) of Brassica juncea L. were analyzed and their antifungal activity were investigated in this study. Allyl isothiocyanate, 2-phenyl ethyl isothiocyanate, 4-isothiocyanato-1-butene, 5-methyl isothiazole, benzene acetaldehyde, benzene propane nitrile and beta-ionone have been identified in all of the experimented oils. The main component of the oils from Ban-Chung-Gat and Chung-Gat was 2-phenyl ethyl isothiocyanate while allyl isothiocyanate was the representing compound in the oil of Dolsan-Gat. The antifungal activities of the oils were tested by micro broth dilution method and disc diffusion method. As the result the oils exhibited significant inhibiting activities against Aspergillus niger, A. flavus, Trichoderma viride, Candida albicans, C. utilis, C. tropicalis, Cryptococcus neoformans, Trichosporon mucoides, Trichophyton tonsurans and Geotrichum capitatum.

• Microbiology and Biotechnology Letters
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• v.21 no.6
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• pp.564-569
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• 1993

AF-001A is a novel antifungal cyclic glyco-peptise isolated from Pseudomonas cepacia AF6008. AF-001A is a mixture of AF-011A1 and AF-001A2. Each compound contains glycine(1), serine(2), asparagine(1), 2,4-diaminobutyric acid(1), beta-hydroxytyrosine(1), xylose(1) and a methylene chain amino acid(1). Additionally, A1 contains one beta-hydroxyasparagine that is replaced with as asparagine in A2. AF-011A showed high in vitro antifungal activity against various animal and plant pathogenic fungi and caused no irritation on the skin of rabbits.

• YAKHAK HOEJI
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• v.57 no.6
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• pp.383-387
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• 2013

In the present study, we determined the antifungal effect of obacunone isolated from Phellodendri Cortex against Candida ablicans, a pathogenic fungus. The antifungal effect was analyzed by an in-vitro susceptibility test and in a murine model of disseminated candidiasis. Possible mechanism of the antifungal activity was also examined. Analyses of data resulting from the susceptibility test revealed that the compound inhibited C. albicans growth. At 25 ${\mu}g$ obacunone/ml, there was app. 45% reduction of CFUs (colony forming units) as compared to obacunone-untreated C. albicans yeast cells (P<0.01). In the murine model of disseminated candidiasis due to C. albicans, obacunone enhanced resistance of mice against disseminated candidiasis. During an entire period of 30-day observation, control animals all died within 14 days, whereas 60% of obacunone-treated mice survived (P<0.05). In addition, obacunone inhibited the hyphal production, a major virulence factor of C. albicans, from the blastoconidial form. Thus, obacunone appears to have antifungal activity for C. albicans infection. This may possibly be mediated by the blockage of hyphal production.

• Journal of the Korean Wood Science and Technology
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• v.29 no.2
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• pp.140-145
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• 2001

Antimicrobial and antioxidative activities on heartwood extractives of domestic species were investigated to develop a natural fungicide or preservative. Six flavanones including pinostrobin, eriodictyol, naringenin, pinocembrin, taxifolin and verecundin were isolated from Prunus sargentii which has been selected due to its high antimicrobial and antioxidative activities among the tested species. According to the results of antifungal test, pinocembrin was evaluated as the highest antifungal compound among the test compounds, which showed 80% of hyphal growth inhibition rate. Antifungal activity of pinocembrin was similar to hinokitiol(${\beta}$-thujaplicin), strong antimicrobial compound isolated from Thujopsis dolabrata. Naringenin followed pinocembrin in its antifungal activity. However, verecundin did not show any antifungal activity. No compound was effective in antibacterial activities. As a result of the measurement of free radical scavenging activity, antioxidative activities of taxifolin and eriodictyol were 2 times that of ${\alpha}$-tocopherol, and antioxidative index of these compounds were even superior to that of ${\alpha}$-tocopherol. In this regard, it could inferred that high antifungal and antioxidative activities of extractives of P. sargentii were derived from pinocembrin, taxifolin and eriodictyol, respectively.

• Journal of Life Science
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• v.15 no.6 s.73
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• pp.1005-1012
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• 2005

Endophytic Bacillus sp. CY22 was previously isolated from the interior of balloon flower root and showed strong antifungal activity against phytopathogenic fungi such as Rhizoctonia solnni, Fusarium oxysporum, and Phythium ultimum. Many Bacillus strains produce antifungal compound such as iturin, fengycin, and mycosubtilin. We isolated and identified antifungal compound from cell supernatant of the endophytic strain. By the MALDI-TOF mass result, the antifungal compound was similar to the known antifungal lipopeptide iturin. It was found that the purified iturin had three isoforms with protonated masses of m/z 1,043.39, 1,057.42, and 1,071.42 and different structures in combination with $Na^{+}$ ion using MALDI-TOF MS. The ita22 gene, which transacylase gene is associated with production of antifungal iturin, had an open reading frame (ORF) of 1,200 bp encoding 400 amino acids. Results of deduced amino acids sequence homology search, Ita22 was homologous with FenF (BAB69697) of Bacillus subtilis 168.

• Journal of Microbiology and Biotechnology
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• v.25 no.9
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• pp.1429-1432
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• 2015

To identify plant-derived cell signaling inhibitors with antifungal properties, a twocomponent screening system using both wild-type Cryptococcus neoformans and a calcineurin mutant was employed owing to their counter-regulatory actions on the Hog1 mitogenactivated protein kinase and calcineurin pathways. Of the 2,000 plant extracts evaluated, a single bioactive compound from M. obovata Thunb. was found to act specifically on the calcineurin pathway of C. neoformans. This compound was identified as magnoloside A, and had potent antifungal activities against various Cryptococcus strains with minimum inhibitory concentration values ranging from 1.0 to 4.0 μg/ml.

• Mycobiology
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• v.37 no.1
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• pp.31-36
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• 2009

A phytochemical study on the flower of Calotropis gigantea (Linn.) using silica gel column chromatography and preparative thin layer chromatography, led to the first time isolation of Di-(2-ethylhexyl) phthalate (compound 1) and anhydrosophoradiol-3-acetate (compound 2). The structures of these compounds were confirmed by spectroscopic analyses (IR, HRTOFMS and NMR). The antibacterial and antifungal activities of ethyl acetate extract, compound 1 and compound 2 were measured using the disc diffusion method. Ethyl acetate extract and compound 1 presented better results than compound 2. The minimum inhibitory concentrations (MICs) of the extract and compounds were found to be in the range of $16{\sim}128{\mu}g/ml$. The cytotoxicity ($LC_{50}$) against brine shrimp nauplii (Artemia salina) were also evaluated and found to be 14.61 ${\mu}g/ml$ for ethyl acetate, 9.19 ${\mu}g/ml$ for compound 1 and 15.55 ${\mu}g/ml$ for compound 2.