• Journal of Microbiology and Biotechnology
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• v.32 no.4
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• pp.504-513
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• 2022

Chitin deacetylase (CDA) inhibitors were developed as novel antifungal agents because CDA participates in critical fungal physiological and metabolic processes and increases virulence in soil-borne fungal pathogens. However, few CDA inhibitors have been reported. In this study, 150 candidate CDA inhibitors were selected from the commercial Chemdiv compound library through structure-based virtual screening. The top-ranked 25 compounds were further evaluated for biological activity. The compound J075-4187 had an IC50 of 4.24 ± 0.16 µM for AnCDA. Molecular docking calculations predicted that compound J075-4187 binds to the amino acid residues, including active sites (H101, D48). Furthermore, compound J075-4187 inhibited food spoilage fungi and plant pathogenic fungi, with minimum inhibitory concentration (MIC) at 260 ㎍/ml and minimum fungicidal concentration (MFC) at 520 ㎍/ml. Therefore, compound J075-4187 is a good candidate for use in developing antifungal agents for fungi control.

• Korean Journal of Microbiology
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• v.50 no.3
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• pp.201-209
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• 2014

This study was carried out in order to develop a biological control of anthracnose of red pepper caused by fungal pathogens. In particular, this study focuses on the Colletotrichum species, which includes important fungal pathogens causing a great deal of damage to red pepper. Antagonistic bacteria were isolated from the soil of pepper fields, which were then tested for biocontrol activity against the Colletotrichum gloeosporioides anthracnose pathogen of pepper. Based on the 16S rRNA sequence analysis, the isolated bacterial strain CS-52 was identical to Bacillus sp. The culture broth of Bacillus sp. CS-52 had antifungal activity toward the hyphae and spores of C. gloeosporioides. Moreover, the substances with antifungal activity were optimized when Bacillus sp. CS-52 was grown aerobically in a medium composed of 0.5% glucose, 0.7% $K_2HPO_4$, 0.2% $KH_2PO_4$, 0.3% $NH_4NO_3$, 0.01% $MnSO_4{\cdot}7H_2O$, and 0.15% yeast extract at $30^{\circ}C$. The inhibition of spore formation resulting from cellulase, siderophores, and indole-3-acetic acid (IAA), were produced at 24 h, 48 h, and 72 h, respectively. Bacillus sp. CS-52 also exhibited its potent fungicidal activity against anthracnose in an in vivo test, at a level of 70% when compared to chemical fungicides. These results identified substances with antifungal activity produced by Bacillus sp. CS-52 for the biological control of major plant pathogens in red pepper. Further studies will investigate the synergistic effect promoting better growth and antifungal activity by the formulation of substances with antifungal activity.

• The Korean Journal of Pesticide Science
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• v.4 no.1
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• pp.32-37
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• 2000

A series of transition metal complexes of 3,6-bis(6'-methyl-2'-pyridyl)pyridazine ($L^{1}$) and 3,6-bis(2'-pyridyl)pyridazine ($L^{2}$) as artificial nuclease, $1{\sim}8$ were synthesized. After determining of X-ray crystal structure, hydrolysis rate constants of phosphates, as DNA model compound and biological activities were confirmed. $L^{2}$-Zn(II) complex, 8 was shown the best hydrolysis rate constant. The $L^{2}$-Ni(II) complex, 5 and $L^{2}$-Co(II) complex, 6 showed the highest herbicidal activity against SCP (Scriptus Juncoids) with excellent tolerance to rice, ORY (Oryzae sativa L.). And the $L^{1}$-Co(II) complex, 2, $L^{1}$-Zn(II) complex, 4 and ligand ($L^{1}$ amp; $L^{2}$) displayed above 90% fungicidal activity against MAG (Magnaporthe grisea).

• The Korean Journal of Pesticide Science
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• v.16 no.3
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• pp.209-216
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• 2012

In the continued research on natural fungicides for control of plant diseases by using plant-derived products, we found that Spatholobus suberectus Dunn had a strong fungicidal activity against several plant pathogens. S. suberectus (1 kg) was extracted with 80% aqueous MeOH and then the concentrated extract was partitioned with n-hexane, EtOAc, n-BuOH and $H_2O$ successively. The four layers were tested their disease contron efficacies against 6 plant diseases such as rice blast (RCB), rice sheath blight (RSB), tomato grey mold (TGM), tomato late blight (TLB), wheat leaf rust (WLR), and barley powdery mildew (BPM). The EtOAc fraction was highly active showing over 80% control against RCB, TGM, TLB, and BPM. By using silica gel chromatography, preparative TLC and HPLC, six compounds that were expected to have antifungal activity were separated. Their chemical structures were identified as ethanone, hydroxytyrosol, epicatechin, procyanidin B2, dimethoxy daizein and formononetin by ESI-MS, $^1H$-NMR, $^{13}C$-NMR, and 2D-NMR spectroscopic analyses. The chemicals except epicatechin were first reported in S. suberectus. Study on in vitro and in vivo antifungal activities of the isolated compounds is in progress.

• The Korean Journal of Mycology
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• v.39 no.2
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• pp.91-98
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• 2011

Oudemansiella mucida, an edible and medicinal mushrooms belonging to Tricholomataceae of Basidiomycota, has been known to produce antifungal substances to inhibit the mycelial growth and spore germination of the plant pathogenic fungi. To produce good amount of antifungal substances from culture media, the optimal culture conditions of O. mucida were investigated. The most favorable conditions for the mycelial growth were $25^{\circ}C$ and pH 5 in potato dextrose agar. The most favorable carbon and nitrogen sources promoting mycelial growth were maltose and calcium nitrate, respectively. The optimum C/N ratio was about 20 : 1 in case that 3% glucose was supplemented to the basal medium as a carbon source. The optimal mycelial growth of O. mucida was found in the Hennerberg medium. The crude extract from submerged culture of potato dextrose broth exhibited inhibition of mycelial growth of Colletotrichum acutatum, Botrytis cinerea and Pyricularia oryzae but, fungicidal activity is not good enough to compared with commercially available fungicides tested. Therefore, the antifungal substances extracted from submerged culture of O. mucida might have a potential to be used for biocontrol agent of fungal diseases of plants.

• Restorative Dentistry and Endodontics
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• v.41 no.2
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• pp.91-97
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• 2016

Objectives: The purpose of this ex vivo study was to compare the antifungal activity of a synthetic peptide consisting of 15 amino acids at the C-terminus of human ${\beta}$-defensin 3 (HBD3-C15) with calcium hydroxide (CH) and Nystatin (Nys) against Candida albicans (C. albicans) biofilm. Materials and Methods: C. albicans were grown on cover glass bottom dishes or human dentin disks for 48 hr, and then treated with HBD3-C15 (0, 12.5, 25, 50, 100, 150, 200, and $300{\mu}g/mL$), CH ($100{\mu}g/mL$), and Nys ($20{\mu}g/mL$) for 7 days at $37^{\circ}C$. On cover glass, live and dead cells in the biomass were measured by the FilmTracer Biofilm viability assay, and observed by confocal laser scanning microscopy (CLSM). On dentin, normal, diminished and ruptured cells were observed by field-emission scanning electron microscopy (FE-SEM). The results were subjected to a two-tailed t-test, a one way analysis variance and a post hoc test at a significance level of p = 0.05. Results: C. albicans survival on dentin was inhibited by HBD3-C15 in a dose-dependent manner. There were fewer aggregations of C. albicans in the groups of Nys and HBD3-C15 (${\geq}100{\mu}g/mL$). CLSM showed C. albicans survival was reduced by HBD3-C15 in a dose dependent manner. Nys and HBD3-C15 (${\geq}100{\mu}g/mL$) showed significant fungicidal activity compared to CH group (p < 0.05). Conclusions: Synthetic HBD3-C15 peptide (${\geq}100{\mu}g/mL$) and Nys exhibited significantly higher antifungal activity than CH against C. albicans by inhibiting cell survival and biofilm.

• Applied Biological Chemistry
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• v.44 no.3
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• pp.191-196
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• 2001

${\alpha},{\beta}$-Unsaturated carboxanilides 5 with trifluromethylated dihydro-1,4-oxathiins were synthesized for the development of new agrochemical fungicide. Chlorination of trifluoromethylated ${\beta}-keto$ ester 6 followed by the reaction with 1,2-mercaptoethanol gave intermediate 1,4-oxathiane 11. Without purification of 11, substitution of hydroxy group by chlorine, followed by dehydrochlorination of 10 in the presence of triethylamine afforded trifluoromethylated dihydro-1,4-oxathiin ethyl ester 9. Acylation of the hydroxy group of the carboxylic acid 12 followed by treatment of various amines gave the corresponding trifluoromethylated dihydro-1,4-oxathiin carboxamides 5. Antifungal screening (in vivo) of the synthesized compounds against typical plant diseases, which include rice blast, rice sheath blight, cucumber gray mold, tomato late blight, wheat leaf rust, and barley powdery mildew, was carried out. Where meta position of the phenyl group was substituted with isopropoxy or isopropyl group, excellent antifungal activities against rice sheath blight and wheat leaf rust were detected.

• The Korean Journal of Pesticide Science
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• v.12 no.1
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• pp.88-96
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• 2008

To obtain protoplasts of Colletotrichum acutatum JC24, conidia were inoculated onto cellophane membrane placed on PDA and incubated at $25^{\circ}C$ for 20 hrs under the dark condition. Cellophane membranes, where mycelia were incubated, were soaked into 2% lysing enzyme solution prepared with 0.02 M phosphate buffer (pH 7.0) including 1.2 M sorbitiol. After treatment in 2% enzyme solution for 2 - 3 hrs, it could be possible to harvest $2-3\;{\times}\;10^6$ protoplasts/mL. The effect of several fungicides on reversion ratio was determined by using the protoplasts obtained from C. acutatum JC24. Any protoplasts could not be reversed to mycelia on reversion PDA amended with $10\;{\mu}\;g\;mL^{-1}$ of propineb. With tebuconazole, inhibition ratio of protoplast reversion was 100 and 0.9% at 0.5 and $0.1\;{\mu}\;g\;mL^{-1}$, respectively, while inhibitory effect on mycelial growth was 85.1 and 75.7%. The inhibitory tendency of carbendazim on protoplast reversion was as same as mycelial growth. In the case of strobilurins, trifloxystrobin and kresoxim-methyl, they only could inhibit protoplast reversion of C. acutatum JC24, when salicylhydroxamic acid (SHAM) was amended into reversion PDA with strobilurins.

• The Plant Pathology Journal
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• v.36 no.4
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• pp.335-345
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• 2020

Tomato grey mould has been one of the destructive fungal diseases during tomato production. Ten mM of menadione sodium bisulfite (MSB) was applied to tomato plants for eco-friendly control of the grey mould. MSB-reduced tomato grey mould in the 3rd true leaves was prolonged at least 7 days prior to the fungal inoculation of two inoculum densities (2 × 10⁴ and 2 × 10⁵ conidia/ml) of Botrytis cinerea. Protection efficacy was significantly higher in the leaves inoculated with the lower disease pressure of conidial suspension compared to the higher one. MSB-pretreatment was not effective to arrest oxalic acid-triggered necrosis on tomato leaves. Plant cell death and hydrogen peroxide accumulation were restricted in necrotic lesions of the B. cinereainoculated leaves by the MSB-pretreatment. Decreased conidia number and germ-tube elongation of B. cinerea were found at 10 h, and mycelial growth was also impeded at 24 h on the MSB-pretreated leaves. MSB-mediated disease suppressions were found in cotyledons and different positions (1st to 5th) of true leaves inoculated with the lower conidial suspension, but only 1st to 3rd true leaves showed decreases in lesion sizes by the higher inoculum density. Increasing MSB-pretreatment times more efficiently decreased the lesion size by the higher disease pressure. MSB led to inducible expressions of defence-related genes SlPR1a, SlPR1b, SlPIN2, SlACO1, SlChi3, and SlChi9 in tomato leaves prior to B. cinerea infection. These results suggest that MSB pretreatment can be a promising alternative to chemical fungicides for environment-friendly management of tomato grey mould.

• Journal of Life Science
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• v.20 no.3
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• pp.403-410
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• 2010

In order to produce high-quality fermenting composts, a microorganism was isolated from the natural world. The bacterium has not only in high enzyme activities but also had good antimicrobial activities against phytopathogenic microorganisms. Its cultivating characteristics were then investigated. Bacterium KJ-9, which contains high CMCase, protease and chitinase activities and excellent antimicrobial activities against phytopathogenic microorganisms, was separated from leaf mold and identified as Bacillus licheniformis by two methods: Bergey's Manual of Systematic Bacteriology and API 50 CHL Carbohydrate Test Kit (Bio Merieux, France) using an ATB (Automated Identification) computer system (Bio Merieux, France). Optimal medium for cultivation of B. licheniformis was 2% soluble starch as a carbon source, 0.5% yeast extract as a nitrogen source and 0.05% $MgSO_4{\cdot}7H_2O$. Optimal growth conditions of pH, temperature and shake speed were pH 7.0, $50^{\circ}C$ and 180 rpm, respectively. Culture broth of B. licheniformis KJ-9 cultured for 36~60 hr was effective in fungicidal activities against plant pathogens including Botrytis cinerea, Corynespora cassicola, Fusarium oxysporum, and Rhizoctonia solani.