• 한국생물공학회:학술대회논문집
• /
• 한국생물공학회 2005년도 생물공학의 동향(XVI)
• /
• pp.458-459
• /
• 2005

• 농약과학회지
• /
• 제6권3호
• /
• pp.209-217
• /
• 2002

Metalaxyl 살균제 저항성(RPC)과 감수성(SPC) 고추역병균주(Phytaphthora capsici)들에 대한 2-N-benzyl-5-phenoxy-3-isothiazolone 유도체들의 살균활성을 비교분자 유사성 지수분석(CoMSIA)과 홀로그램 구조-활성 관계(HQSAR) 방법으로 분석하였다. 두 균주의 살균활성에 대한 PLS 계산결과, 교차 확인값($q^2$)과 Pearson 상관계수($r^2$) (CoMSIA: RPC; $q^2=0.675,\;r^2=0.942$, SPC; $q^2=0.350,\;r^2=0.876$ 및 HQSAR: RPC; $q^2=0.519,\;r^2=0.869$, SPC; $q^2=0.483,\;r^2=0.990$)를 비교한 바, 두 방법 모두 양호한 분석 결과를 나타내었다. 그리고 CoMSIA 등고도로부터 특히, RPC에 대한 선택적인 살균활성 요소는 phenoxy-기의 meta, para(C1-C6) 위치에 소수성이 작고 입체적으로 크지 않은 H-결합 받게가 치환 될 경우이었으며 CoMSIA 보다는 HQSAR 방법이 높은 예측성을 나타내었다.

• 미생물학회지
• /
• 제33권3호
• /
• pp.170-174
• /
• 1997

강한 항진균 활성을 나타내며, 낮은 적혈구 용혈활성을 갖는 새로운 합성 펩티드를 얻기 위하여 cecropin A(1-8)-magainin 2(1-12) 및 이들의 유사체들을 설계하고 이들을 고상법에 의하여 합성하였다. 합성 펩티드의 항진균 활성은 Trichosporon beigelii에 대한 성장억제능에 의하여 측정하였으며, 세포독성은 인간의 적혈구 세포에 대한 용혈활성에 의하여 측정하였다. 펩티드의 양쪽 친매성의 증가는 항진균활성보다는 적혈구 용혈황성에 큰 영향을 미쳤다. Cecropin A(1-8)-magainin 2(1-12)의 12번 아미노산이 Lys을 Ala으로 치환시킨 유사체 펩티드(A2)는 가장 강한 항진균활성(minimum inhibitory concentration : 2.5.$\mu$g/ml)을 나타내며 비교적 낮은 적혈구 용혈활성(200.$\mu$g/ml의 펩티드 농도에서 0.5% hemolysis를 나타냄)을 나타내었다. 따라서 A2의 펩티드는 세포독성을 갖지 않으며 강한 항진균 활성을 가지는 모델로서 유용하게 사용될 것이다.

• Journal of the Korean Wood Science and Technology
• /
• 제48권1호
• /
• pp.107-116
• /
• 2020

Termiticidal and fungicidal activities of wood vinegar from Cinnamomum parthenoxylon (CP) stem wood have been evaluated against Coptotermes curvignathus and wood rotting fungi (Schizophyllum commune and Fomitopsis palustris). The utilized CP wood vinegar was produced in the operating temperature range 250-300℃ pyrolysis. A no-choice test was applied for evaluating termiticidal activity with 33 active termites and antifungal activity using the agar media assay. The result showed that an increase in the concentrations of CP wood vinegar significantly raised the mortality of termite. CP wood vinegar showed high termiticidal activity, organic acids (acetic acid 42.91%, 3-butenoic acid 6.89%, butanoic acid, 2-propenyl ester 2.26%), and ketones (1-hydroxy-2-propanone 5.14%, 3-methylcyclopentane-1,2-dione 2.34%) might be largely contributed to termiticidal activity in addition to other minor components. Furthermore, CP wood vinegar exhibited significant inhibition of fungal growth. These data showed that CP wood vinegar was more toxic to white-rot fungi (S. commune) than brown-rot (F. palustris). The results suggested that phenolic compounds from lignin degradation were responsible for good antifungal activity.

• Bulletin of the Korean Chemical Society
• /
• 제31권11호
• /
• pp.3341-3347
• /
• 2010

A series of oxazolidinone-based strobilurin analogues were efficiently synthesized by the reaction of 3-(2-bromomethylphenyl) oxazolidin-2-one with 1-substituted phenyl-2H-pyrazolin-3-one. Their structures were confirmed and characterized by $^1H$-NMR, $^{13}C$-NMR, elemental analysis, and mass spectroscopy. In addition, the crystal structure of the target compound 3-(2-((1-phenyl-2H-pyrazol-3-yloxy)methyl)phenyl) oxazolidin-2-one was determined by single crystal X-ray diffraction. The bioassay results of these compounds indicated that some of the oxazolidin-2-one derivatives containing N-substituted phenyl 2H-pyrazol ring exhibited potential in vivo fungicidal activities against M. grisea at the dosage of $1\;g\;L^{-1}$.

• 대한화학회지
• /
• 제47권3호
• /
• pp.241-249
• /
• 2003

3-(1-Ethoxycarbonyl)ethyl-1,2-dihydro-2-oxoquinoxaline(8)을 hydrazine hydrate와 반응시켜 3-(1-hydrazinocarbonyl)ethyl-2-hydroxyquinoxaline(9)을 합성하였고, 화합물 9를 치환 벤즈알데하이드류 또는 heteroaryl aldehyde류와 반응시켜 2-hydroxyquinoxaline류(10-12)를 합성하였다. 또한 화합물 9를 alkyl (ethoxymethylene)- cyanoacetate류 또는 ethoxymethylenemalononitrile과 반응시켜 분자내 고리화반응에 의하여 5-amino-1-[2-(3-hydroxyquinoxalin-2-yl)propanoyl]-pyrazole류(13)를 합성하였다. 얻어진 화합물 10-13은 dimethyl sulfoxide 용액에서 lactam형과 lactime형 사이에 토토머화 현상을 나타내었는데, 이들의 토토머 비를 $^1H$ NMR로서 측정하였다. 그리고 합성한 화합물들에 대한 제초력과 살균력도 조사하였다.

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

• 한국미생물·생명공학회지
• /
• 제27권5호
• /
• pp.354-358
• /
• 1999

In order to know the antifungal characteristics of saturated fatty acids having 6 to 12 carbons, their minimum inhibitory concentrations (MICs) and minimum fungicidal concentrations (MFCs) were estimated against Saccharomyces cerevisiae. Fatty acids from C6 to C11 exhibited increasing activity with chain length, but C12 fatty acid did not show activity at all. In relation to antifungal modes of actions, fatty acids investigated showed on inhibitory activity toward the plasma membrane H+-ATPase of Saccharomyces cerevisiae. Their inhibitions to the glucose-induced acidification and ATP hydrolysis caused by the proton pump were found to be in common wiht antifungal activities. At the test concentration of 1mM, hexanoic acid (C6) showed the lowest inhibition of about 30%, while undecanoic acid(C11) showed the strongest inhibition of over 90%. In addition, as seen with antifungal activity, the inhibitory activity of dodecanoic acid (C12) was suddenly reduced to less than 50%.

• Applied Biological Chemistry
• /
• 제37권4호
• /
• pp.287-294
• /
• 1994

새로운 3-(4-치환-phenyl)-1-(2-furyl)propenone, 1과 3-(4-치환-phenyl)-1-(2-furyl)-3-thiophenylpropanones, 2 유도체를 합성하여 in vitro에서 잿빛 곰팡이균(Botrytis cineria, BC), 사과 부란병균(Valsa ceratosperma, VC), 마늘 균핵병균(Sclerotium cepivorum, SC) 및 고추 역병균(Phytophthora capsici, PC) 등의 곰팡이 균류에 대한 구조-항균활성 관계(SAR)를 알아보았다. 그 결과, 2보다 1이 비교적 큰 항균활성을 나타내었으며 특히, E(Syn)형의 4-chloro group 치환체, 1d나 비 치환체, 1a가 4가지 균중의 BC균에 대하여 가장 강력한 항균활성$(EC_{50}=10{\sim}11\;ppm)$을 보였다. 1의 가수분해 반응속도상수(logk)와 ${\sigma}$상수사이에 좋은 상관성 $(r^2=0.90)$으로부터 치환기 (X)의 음하전과 ${\beta}$탄소원자의 양하전에 의존적인 항균활성을 나타낼 것으로 예상되었다.

• Biomolecules & Therapeutics
• /
• 제8권3호
• /
• pp.223-227
• /
• 2000

Propolis, a natural resinous compound collected from honey bees, contains many biochemical constituents and has been used for traditional medicines as early as 300 B .C. Recently, it has been reported to possess many biological activities such as antibacterial, antiviral, fungicidal, local anaesthetic, immunostimulating, antiinflammatory and free radical scavenging properties. To investigate activities of chrysin, one of propolis effective compounds for blood coagulation system was injected endotoxin (4000 EU/kg, i.v.) in rats at 1 hr after administered chrysin (20 mg/kg, p.o.). This study was resulted that chrysin has antiplatelet aggregation activity in vitro, delay of blood clotting time and prothrombin time, and reduction of fibrinogen and FDP in vivo. Chrysin has increased SOD activity, GSH content and GST activity, and decreased MDA content in liver. The result suggests that the antithrombosis effect of chrysin is suppressive activity for a blood coagulation system and antioxidative activity.