• 대한약학회:학술대회논문집
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• 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2-2
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• pp.185.3-185.3
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• 2003

Juglone and naphthazarine derivatives were newly systhesized for the evaluation of antifungal activities. These derivatives were prepared by methylation of juglone and 2, 3-dichloro-5, 8-dihydroxy-l, 4-naphthoquinone, and by regioselective nucleophilic subsitution with arylthiols. All compounds were tested in vitro for their growth inhibitory activities against pathogenic fungi by the standard method. The MIC values were determined by comparison to flucytosine as a standard agent. (omitted)

• Bulletin of the Korean Chemical Society
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• 제14권2호
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• pp.262-265
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• 1993

Conformational free energy calculations using an empirical potential function and a hydration shell model (program CONBIO) were carried out on antifungal agent fluconazole in the unhydrated and hydrated states. The initial geometry of fluconazole was obtained from two minimized fragments of it using a molecular mechanics MMPMI and followed by minimizing with a semiempirical AM1 method. In both states, the feasible conformations were obtained from the calculations of conformational energy, conformational entropy, and hydration free energy by varying all the torsion angles of the molecule. The intramolecular hydrogen bonds of isopropyl hydroxyl hydrogen and triazole nitrogens and the structural flexibility are of significant importance in stabilizing the conformations of fluconazole in both states. Hydration is proved to be one of the essential factors in stabilizing the overall conformation in aqueous solution. Two F atoms of phenyl ring are not identified as an essential key in determining the stable conformations and may be responsible for the interaction with the receptor of fluconazole.

• Mycobiology
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• 제40권1호
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• pp.53-58
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• 2012

This research is concerned with the fungicidal properties of nano-size silver colloidal solution used as an agent for antifungal treatment of various plant pathogens. We used WA-CV-WA13B, WA-AT-WB13R, and WA-PR-WB13R silver nanoparticles (AgNPs) at concentrations of 10, 25, 50, and 100 ppm. Eighteen different plant pathogenic fungi were treated with these AgNPs on potato dextrose agar (PDA), malt extract agar, and corn meal agar plates. We calculated fungal inhibition in order to evaluate the antifungal efficacy of silver nanoparticles against pathogens. The results indicated that AgNPs possess antifungal properties against these plant pathogens at various levels. Treatment with WA-CV-WB13R AgNPs resulted in maximum inhibition of most fungi. Results also showed that the most significant inhibition of plant pathogenic fungi was observed on PDA and 100 ppm of AgNPs.

• 한국균학회지
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• 제25권4호통권83호
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• pp.348-353
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• 1997

계피의 항진균활성을 검색한 결과 에테르 추출물이 우수한 활성을 나타내는 것으로 평가되어 계피 에테르의 추출물로부터 항진균물질 AF-001을 분리 정제하였으며 이를 동정한 결과 trans-cinnamaldehyde로 확인되었다. AF-001은 피부진균증의 원인 균주인 Tricophyton mentagrophytes, Microsporium gypseum, Epidermophyton floccosum, Cryptococcus neofomans, Aspergillus niger, Candida albicans와 Penicillium avellaneum에 대해 $38{\sim}79\;{\mu}g/ml$의 최소저지농도를 보였으며 imidazole계의 대표적인 항진균제인 Ketoconazole보다 광범위한 항균 스펙트럼을 보였다.

• KSBB Journal
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• 제30권3호
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• pp.132-139
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• 2015

In order to use the symbiotic bacteria from ethomophatogenic nematodes as a biological control agent for agriculture, the cultural condition for maintaining phase I and antifungal activity was investigated. Symbiotic bacteria (SB) 1 stain from nematodes were selected from the three strains isolated from entomopathogenic nematodes. The growth of the SB 1 strain in NB, TSB, TY and YS medium was higher than that of the SB 2 and SB 3 strain. The packed cell volume of the SB 1 strain was reduced in NB medium which showed radical pH change. Phase I of the SB 1 strain was maintained in TSB medium after being stored for 2 weeks at $4^{\circ}C$. Culture broth with the SB 1 strain in TSB medium for 6 days and 7 days showed antifungal activities against Rhizoctonia solani KACC 40142, Botrytis cinerea Pers. KACC 40854, and Botrytis cinerea Pers. KACC 41008. Culture broth with the SB 1 strain in TSB medium containing 100 mM L-proline for 5 days showed antifungal activities against Rhizoctonia solani KACC 40142, and Botrytis cinerea Pers. KACC 40854.

• 생명과학회지
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• 제14권5호
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• pp.859-862
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• 2004

본 연구에서는 두 균주, Bacillus sp. LP03, TBM40-3의 biosurfactan에 대한 생육 시 적절한 온도와 유화활성에 대한 실험을 행한 후 가장 적절한 조건에서 배양하였고, 이미 항진균성과 유화활성에 대해 실험실 수준에서 검증된 TBM40-3뿐 아니라 분리되어 보관되어 있는 균주, LP03 또한 실험실 수준에서 항진균성 및 유화활성이 확인되었고 이후에 시행한 부추에 생기는 병인 B. cinerea에 대한 항진균성 및 생육조사를 시행한 결과 이미 항진균성과 유화활성이 확인되어있던 TBM40-3에 비해 그 효과가 우수할 뿐 아니라 생육 촉진효과를 확인할 수 있었다.

• Journal of Microbiology and Biotechnology
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• 제19권10호
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• pp.1169-1175
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• 2009

An antifungal chitinase, ChiCW, produced by Bacillus cereus 28-9 is effective against conidial germination of Botrytis elliptica, the causal agent of lily leaf blight. ChiCW as a modular enzyme consists of a signal peptide, a catalytic domain, a fibronectin type-III-like domain, and a chitin-binding domain. When two C-terminal domains of ChiCW were truncated, $ChiCW{\Delta}FC$ (lacking the chitin-binding domain and fibronectin type III-like domain) lost its antifungal activity. Since $ChiCW{\Delta}C$ (lacking the chitin-binding domain) could not be expressed in Escherichia coli as $ChiCW{\Delta}FC$ did, a different strategy based on protein engineering technology was designed to investigate the involvement of the chitin-binding domain of ChiCW ($ChBD_{ChiCW}$) in antifungal activity in this study. Because ChiA1 of Bacillus circulans WL-12 is a modular enzyme with a higher hydrolytic activity than ChiCW but not inhibitory to conidial germination of Bo. elliptica and the similar domain composition of ChiA1 and ChiCW, the C-terminal truncated derivatives of ChiA1 were generated and used to construct chimeric chitinases with $ChBD_{ChiCW}$. When the chitin-binding domain of ChiA1 was replaced with $ChBD_{ChiCW}$, the chimeric chitinase named ChiAAAW exhibited both high enzyme activity and antifungal activity. The results indicate that $ChBD_{ChiCW}$ may play an important role in the antifungal activity of ChiCW.

• 공업화학
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• 제17권6호
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• pp.633-637
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• 2006

본 연구에서는 triazole계 항진균제인 이트라코나졸의 대량합성을 위한 효과적인 합성법을 제시하였다. Janssen Pharmaceutica에 의해 발표된 기존의 의약화학적 합성경로는 2,4-dichloroacetophenone을 출발물질로 하는 직렬(linear) 합성의 14 단계로서 전체수율이 1.4%에 불과하였고 대량합성에 부적합한 위험물질로서 methanesulfonyl chloride ($CH_{3}SO_{2}Cl$)와 수소기체 및 sodium hydride (NaH)를 사용하고 있다. 또한 고가의 1-acetyl-4-(4-hydroxyphenyl)piperazine 및 팔라듐을 사용함으로써 생산 단가가 높은 문제점이 있었다. 이를 개선하기 위해서 병렬(convergent) 합성 전략을 수립하였는데, 이트라코나졸의 대략 반에 해당하는 중간체 II와 III을 각각 합성한 다음 두 부분을 결합시키는 12단계의 합성공정을 개발하였고 전체 수율은 12.0%로서 합성효율이 크게 개선되었다. 이 과정에서 공정을 간략화하고 위험물질 및 고가의 반응물의 사용을 배제함으로써 생산 원가를 크게 절감시킬 수 있었다.

• KSBB Journal
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• 제13권6호
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• pp.669-674
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• 1998

This study was carried out particularly focusing on he antitumor effect in combination with 5-fluorocytosine(5-FC), antifungal agent, and extracellular cytosine deaminase from Chromobacterium violaceum YK 391 against U-937, K-562 and SNU-C4 cells. While the addition of 10$\mu\textrm{g}$/100 ${\mu}\ell$ of anticancer agent, 5-fluorouracil(5-FU), to U-937, K-562 and SNU-C4 caused the decrease of proliferation 90%, 75% and 93% respectively, the addition of 20 $\mu\textrm{g}$/100 ${\mu}\ell$ of the extracellular cytosine deaminase and 10 $\mu\textrm{g}$/100 ${\mu}\ell$ of antifungal agent 5-FC caused the decrease of proliferation 80%, 70% and 90%, respectively. These results, therefore, reveal that this enzyme has the similar clinical effect for considering of adjuvant antitumor effect. From the above results, the treatment of 5-FC and the cytosine deaminase was very effective and showed the possibility to remove side effects which easily occur by the treatment of 5-FU only. An extracellular cytosine deaminase.

• Journal of Microbiology and Biotechnology
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• 제20권10호
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• pp.1397-1402
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• 2010

Papyriflavonol A (PapA), a prenylated flavonoid [5,7,3',4'-tetrahydroxy-6,5'-di-(${\gamma},{\gamma}$-dimethylallyl)-flavonol], was isolated from the root barks of Broussonetia papyrifera. Our previous study showed that PapA has a broad-spectrum antimicrobial activity against pathogenic bacteria and fungi. In this study, the mode of action of PapA against Candida albicans was investigated to evaluate PapA as an antifungal agent. The minimal inhibitory concentration (MIC) values were 10~25 ${\mu}g/ml$ for C. albicans and Saccharomyces cerevisiae, Gram-negative bacteria (Escherichia coli and Salmonella typhimurium), and Gram-positive bacteria (Staphylococcus epidermidis and Staphylococcus aureus). The kinetics of cell growth inhibition, scanning electron microscopy, and measurement of plasma membrane florescence anisotrophy revealed that the antifungal activity of PapA against C. albicans and S. cerevisiae is mediated by its ability to disrupt the cell membrane integrity. Compared with amphotericin B, a cell-membrane-disrupting polyene antibiotic, the hemolytic toxicity of PapA was negligible. At 10~25 ${\mu}g/ml$ of MIC levels for the tested strains, the hemolysis ratio of human erythrocytes was less than 5%. Our results suggest that PapA could be a therapeutic fungicidal agent having potential as a broad spectrum antimicrobial agent.