• Biomolecules & Therapeutics
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• 제26권5호
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• pp.494-502
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• 2018

Breast cancer is currently the most prevalent cancer in women, and its incidence increases every year. Azole antifungal drugs were recently found to have antitumor efficacy in several cancer types. They contain an imidazole (clotrimazole and ketoconazole) or a triazole (fluconazole and itraconazole) ring. Using human breast adenocarcinoma cells (MCF-7 and MDA-MB-231), we evaluated the effects of azole drugs on cell proliferation, apoptosis, cell cycle, migration, and invasion, and investigated the underlying mechanisms. Clotrimazole and ketoconazole inhibited the proliferation of both cell lines while fluconazole and itraconazole did not. In addition, clotrimazole and ketoconazole inhibited the motility of MDA-MB-231 cells and induced $G_1$-phase arrest in MCF-7 and MDA-MB-231 cells, as determined by cell cycle analysis and immunoblot data. Moreover, Transwell invasion and gelatin zymography assays revealed that clotrimazole and ketoconazole suppressed invasiveness through the inhibition of matrix metalloproteinase 9 in MDA-MB-231 cells, although no significant changes in invasiveness were observed in MCF-7 cells. There were no significant changes in any of the observed parameters with fluconazole or itraconazole treatment in either breast cancer cell line. Taken together, imidazole antifungal drugs showed strong antitumor activity in breast cancer cells through induction of apoptosis and $G_1$ arrest in both MCF-7 and MDA-MB-231 cells and suppression of invasiveness via matrix metalloproteinase 9 inhibition in MDA-MB-231 cells. Imidazole drugs have well-established pharmacokinetic profiles and known toxicity, which can make these generic drugs strong candidates for repositioning as antitumor therapies.

• Animal cells and systems
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• 제10권4호
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• pp.203-209
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• 2006

Azoles are widely used antifungal agents, which inhibit the biosynthesis of fungal cell-membrane ergosterol. In this study, using an amphibian follicle culture system, the effects of azoles on follicular steroidogenesis in frogs were examined. Itraconazole (ICZ), clotrimazole (CTZ) and ketoconazole (KCZ) suppressed pregnenolone ($P_5$) production by the follicles ($ED_{50};\;0.04_{\mu}M,\;0.33_{\mu} M,\;and\;0.91_{\mu}M$, respectively) in response to frog pituitary homogenates (FPH). However, fluconazole (FCZ), miconazole (MCZ) and econazole (ECZ) were not effective in the suppression of $P_5$ production. Not all the azoles examined suppressed the conversion of exogenous $P_5$ to progesterone ($P_4$) (by $3{\beta}$- HSD) or $P_4$ to $17{\alpha}$-hydroxyprogesterone ($17{\alpha}$-OHP) (by $17{\alpha}$-hydroxylase), or androstenedione (AD) to testosterone (T) (by $17{\beta}$-HSD). In contrast, CTZ, MCZ and ECZ in medium partially suppressed the conversion of $17{\alpha}$-OHP to AD (by C17-20 lyase) ($ED_{50};\;0.25{\mu} M,\;4.5{\mu}M,\;and\;0.7{mu}M$, respectively) and CTZ, KCZ, ECZ and MCZ strongly suppressed the conversion of exogenous T to estradiol ($E_2$) (by aromatase) ($ED_{50};\;0.02{\mu}M,\;8{\mu}M,\;0.07{\mu}M,\;0.8{\mu}M$, respectively). These results demonstrated that some azole agents strongly suppress amphibian follicular steroidogenesis and particularly, P450scc and aromatase are more sensitive to azoles than other steroidogenic enzymes.

• Journal of the Korean Wood Science and Technology
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• 제36권3호
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• pp.47-54
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• 2008

데크제가 지니고 있는 결점들을 보완하여 보다 효율적인 야외사용 목질재료를 공급하고자, 방부처리합판을 제작하였다. 방부합판은 라디에타소나무 단판을 방부처리하여 사용하였으며, 방부처리는 기존의 방부시설을 사용하고 그 밖의 공정은 (주)선창산업의 합판생산 공정에 따라 제작되었다. 두께 26.8 mm, 90 mm ${\times}$ 180 mm의 방부합판을 제작하였다. 제작된 합판은 합판성능 시험 외에 외장용 데크재로서 사용할 목적에 부합되도록, 방부효력, 치수안정성, 촉진열화시험, 옥외폭로시험을 실시하였다. 방부합판은 방부처리로 인하여 접착력에 대한 영향을 받지 않았다. CUAZ-1호로 처리한 방부합판의 방부효력은 중량감소율이 낮았으며, 치수안정성은 교차 배열한 합판의 특성대로 판재보다 우수하게 나타났다. 촉진열화시험 결과, 표면의 탈색은 진행되었지만 치수의 변화나 표면의 갈라짐 혹은 접착면의 박리와 같은 물리적인 열화는 발생하지 않았다. 옥외에서 17개월 폭로한 시험결과, 휨강도는 다소 감소하였으나 내부접착력은 감소하지 않았다.

• Mycobiology
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• 제48권1호
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• pp.44-50
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• 2020

Calonectria pseudonaviculata and C. henricotiae are two closely related fungal species responsible for boxwood blight disease of ornamental shrubs (Buxus spp.) in the U.S. and Europe. A previous study has shown isolates of the latter species, which is restricted to Europe, to be less sensitive to tetraconazole, an azole fungicide. In this study, we have analyzed the CYP51 paralogs for polymorphism in 26 genomes, representing geographically disparate populations of C. pseudonaviculata (n = 19) and C. henricotiae (n = 7), from the U.S., Europe, Asia, and New Zealand. The presence of a CYP51A pseudogene and lack of a functional CYP51A paralog in all C. pseudonaviculata genomes examined is a novel discovery for fungi and could have implications for the evolution of resistance to antifungal chemicals.

• Mycobiology
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• 제38권3호
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• pp.215-218
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• 2010

Azoles are currently the most widely used class of antifungal drugs clinically, and are effective for treating fungal infections. Target site of azoles is ergosterol biosynthesis in fungal cell membrane, which is absent in the mammalian host. However, the development of resistance to azole treatments in the fungal pathogen has become a significant challenge. Here, we report the identification and functional characterization of a UPC2 homolog in the human pathogen Cryptococcus neoformans. UPC2 plays roles in ergosterol biosynthesis, which is also affected by the availability of iron in Saccharomyces cerevisiae and Candida albicans. C. neoformans mutants lacking UPC2 were constructed, and a number of phenotypic characteristics, including antifungal susceptibility and iron utilization, were analyzed. No differences were found between the mutant phenotypes and wild type, suggesting that the role of C. neoformans UPC2 homolog may be different from those in S. cerevisiae and C. albicans, and that the gene may have a yet unknown function.

• Archives of Pharmacal Research
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• 제27권3호
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• pp.295-299
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• 2004

The antifungal activities of the essential oil from Agastache rugosa and its main component, estragole, combined with ketoconazole, one of the azole antibiotics commonly used to treat infections caused by Trichophyton species, were evaluated in this study. The combined effects were measured by the checkerboard microtiter and the disk diffusion tests, against T. erinacei, T. mentagrophytes, T. rubrum, T. schoenleinii and T. soudanense. Susceptibility of the five Trichophyton species to the oil alone, or ketoconazole alone, differed distinctly. The fractional inhibitory concentration indices (FICI) of ketoconazole combined with estragole or A. rugosa essential oil, against the tested Trichophyton species, were between 0.05 and 0.27, indicating synergistic effects. These drug combinations exhibited the most significant synergism against T. mentagrophytes, with FICIs of 0.05 and 0.09 for estragole and the essential oil fraction from A. rugosa, respectively. Isobolograms based on the data from checkerboard titer tests also indicated significant synergism between ketoconazole and the Agastache oil fraction or estragole, against the Trichophyton species evaluated. Trichophyton susceptibility to ketoconazole was significantly improved by combination with the Agastache rugosa oil fraction or its main component, estragole.

• 한국임상수의학회지
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• 제20권1호
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• pp.86-90
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• 2003

Little is known to data about the in vitro activity of antimicrobial agents aganist Brucella cams (B cams) isolated from Korea. Our study aimed at determining the in vitro activities of 15 antimicrobial agents against 3 isolates and 52 isolates of B cams from dogs in 1994 and 2002, respectively. In minimal inhibitory concentration (MIC) study, minocycline and doxycycline showed the lowest MICs ( < 0.06-0.5 ug/ml). Gentamicin, streptomycin, ciprofloxacin, norfloxacin and rifampin showed MICs in the range of less than 1 ug/ml. Lincomycin and sulfisox azole showed the highest MICs ( > 32 ug/ml). Interestingly, MICs of macrolides (erythromycin, spiramycin, tylosin) against 52 isolates in 2002 were 16-64 times higher than that of 3 isolates in 1994. In minimal bactericidal concentration (MBC) study, gentamicin, streptomycin, ciprofloxacin and norfloxacin showed the lowest MBCs [0.12-1 ug/ml (1-2 times higher than MIC)], but minocycline and doxycycline showed the highest MBCs [8-32 ug/ml (128 times higher than MIC)]. Rifampin showed the MBCs in the range from 2 to 4 ug/ml (2-4 times higher than MIC).

• Journal of the Korean Wood Science and Technology
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• 제36권6호
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• pp.77-87
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• 2008

국내산 주요 침엽수 소경목의 활용 방안으로 리기다소나무를 이용한 목재 모형 사방댐을 제작하여 강도 성능을 평가하였다. 목재 모형 사방댐은 직경 90 mm의 CUAZ-2 (Copper Azole) 처리한 리기다소나무 방부 원주목을 사용하여 3 Type으로 접합부를 달리하여 제작하였다. 각 Type별 사방댐은 횡목 5층 종목 4층 총 9층의 높이 790 mm로 제작 하였으며 수평 재하 시험과 충격 시험을 통한 강도 성능 평가와 화상처리를 통한 구조물의 변형을 검토 하였다. 직경 90 mm의 원주목을 사용한 목재 모형 사방댐의 수평 재하 시험 결과 직결나사를 사용한 경우 쇄석의 유무는 강도에 큰 영향을 미치지 않았지만 변형은 23% 감소하였다. 전선볼트를 사용한 일체형 사방댐의 경우 쇄석을 채운 경우 1.5배 강도가 증가하고 변형은 감소하였다. 직결나사에 고리가 달린 전선볼트로 보강한 경우 4.8배 강도가 증가하였다. 직경 90 mm 목재 모형 사방댐의 충격 시험 결과 쇄석을 채우지 않은 직결나사 사방댐은 1회 충격에 구조물 전체가 파괴되었으며 전선볼트를 사용한 사방댐은 1회 충격시 779 kgf의 충격이 직접적으로 가해지는 횡목에서 파괴되었다. 2회 충격시 기초부가 파괴되며 545 kgf로 반력이 감소하였고 3회 충격시 기초부 전체가 파괴되며 263 kgf로 반력이 감소하였다.

• Journal of the Korean Wood Science and Technology
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• 제37권3호
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• pp.245-254
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• 2009

최근 환경오염 및 인체 유해성으로 사용이 제한 받고 있는 목재방부제인 chromated copper arsenate (CCA) 그리고 CCA의 대체방부제로 사용되고 있는 고가의 Copper Azole (CuAz)과 alkaline Copper quaternary (ACQ)를 대체하기 위하여 유기폐기물인 두부비지, $CuSO_4$ 그리고/또는 Borax를 이용하여 조제하였다. 이렇게 조제된 두부비지 목재방부제의 사용 가능성을 확인하기 위하여 갈색부후균에 대한 방부효능을 조사하고, 그 방부제가 처리된 목재시편을 FE-SEM과 EDS를 이용하여 현미경적 분석을 수행하였다. 두부비지 방부제로 처리한 목재시편은 Postia placenta와 Gloeophyllum trabeum에 대해 우수한 방부효능을 보였으며, 비지의 가수분해를 위해 사용된 산농도 및 온도의 증가, 그리고 Borax의 첨가는 방부효능을 향상시켰다. 두부비지 방부제로 처리된 시편의 현미경적 관찰을 통하여 비지 가수분해물과 구리의 반응을 통해 용탈과정 중에 용출에 대한 내성을 향상시킨다는 것을 확인할 수 있었다. 상기 결과를 토대로 두부비지 방부제가 경제성과 환경적 측면에서 목재방부제로 사용될 수 있다고 생각한다.

• Corrosion Science and Technology
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• 제4권5호
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• pp.191-200
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• 2005

Two azole compounds viz., Imidazole (IM) and 2-Methylimidazole (2-MIM) were studied to investigate their inhibiting action on corrosion of mild steel in phosphoric acid ($H_3PO_4$) solution by mass loss and polarization techniques at 302K-333K. It has been found that the inhibition efficiency of the all inhibitors increased with increase in inhibitor concentration and decreases with increasing temperature and also with increase in acid concentrations. The inhibition efficiency of these compounds showed very good inhibition efficiency. At 0.5% of IM and 2-MIM in 1N and 5N phosphoric acid solution at 302K to 333K for 5 hours immersion period, the inhibition efficiency of 2-Methylimidazole found to be higher than Imidazole. The adsorption of these compounds on the mild steel surface from the acids has been found to obey Tempkin's adsorption isotherm. The values of activation energy ($E{\alpha}$) and free energy of adsorption (${\Delta}G{\alpha}ds$) were also calculated. The plots of log $W_f$ against time (days) at 302K give straight line which suggested that it obeys first order kinetics and also calculate the rate constant k and half life time $t_{1/2}$. Surface was analyzed by SEM and FITR spectroscopy.