• 제목/요약/키워드: Griseofulvin

검색결과 31건 처리시간 0.022초

The Synthesis of 6-(N-Arylamino)-7-Chloro-5,8-Quinolinedione Derivatives for Evaluation of Antifugal Activities

  • Ryu, Chung-Kyu;Kim, Hee-Jeong
    • Archives of Pharmacal Research
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    • 제17권3호
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    • pp.139-144
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    • 1994
  • A series of 6-(N-aylamono)-7-chloro-5, 8-quinolinedione derivatives was newly synthesized for the evaluation of antifugal activities. 5-Amino-8-hydroxy-quinoline (II) was treated with $KCLO_3$ in HCl to give 6,7-dichloro-5,8-quinolinediones (III). 6-(N-Arylamino)-7-chloro5,8-quinolinediones 1-13 were prepared by regioselective nucleophilic substitution of III with arylamines. In the presence of $CeCl_3$, the N-arylamono groups were introduced at the 6-position of 5,8-quinolinedione ring by the regioselective substitution. These derivatives 1-12 were tested for natifungal and also antibacterial activites, in vitro, against Canadida albicans, Aspergillus nier, Tricophyton mentagrophytes, Bacillus subtilis, Pseudomonas aeruginosa, Staphylococcus aureus and Escherichia coil. The MIC values were determined by the two-fold agar/steak dilution method. Newly obtained 6-(N-arylamino)-7-chloro5,8-quinolinedione derivatives showed potent antifungal and antibacterial activities. Among these derivatives, 1,3,5,7,8 and 9 showed more potent antifungal activities than fluconazole and griseofulvin. Also most of derivatives were found to be more active than ampicillin against gram-positive bacteria. 1 and 7 showed the very potent antifungal activities. 1 was the most efective in preventing the growth of Candida albicans, Aspergillus niger, Tricophyton mentagrophytes, Bacillus subtills and Staphylococcus aureus at MIC $1.6\;\mu{g/ml}$.

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서울지역(地域)에서 발생(發生)한 개와 고양이 피부진균증(皮膚眞菌症)에 관(關)한 연구(硏究) (Survey and case study of dermatophytosis of dog and cat occuring in Seoul area)

  • ;허준회;이병천
    • 대한수의학회지
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    • 제32권4호
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    • pp.689-691
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    • 1992
  • 피부진균증 임상소견을 보이거나 Wood램프 검사에서 양성반응을 보인 개와 고양이 66두에 대하여 DTM(dermatophyte test medium)배양을 실시하였다. 배양결과 가장 많이 발생한 진균은 M canis(24회)였으며 이들중 진단시 15증례에서 Wood램프 양성반응을 보였다. 치료제로 초미립자 글리세오풀빈 12.5mg/kg용량으로 1일 2회 투여한 결과 좋은 치료결과를 보였다. 그리고 1일 2회 투여가 같은 용량의 1일 1회 투여보다 효과가 좋은 것으로 나타났다.

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Effect of Micronization on the Extent of Drug Absorption from Suspensions in Humans

  • Oh, Doo-Man;Rane L.Curl;Yong, Chul-Soon;Gordon L.Amidon
    • Archives of Pharmacal Research
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    • 제18권6호
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    • pp.427-433
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    • 1995
  • A microscopic mass balance approach has hsown that the initial saturation (Is), absorption number (An), dose number (Do), and dissolution number (Dn) are four fundamental dimensionless parameters that can be used to estimate the fraction dose absorbed (F)l of suspensions of poorly soluble drugs in humans. The dissolution number of a drug increases with decreasing its particle size. The effect of micronization on F for suspensions was investigated in terms of Dn. About 90% of maximal F can be achieved at $Dn{\approx}2$. Increasing the solubility of a drug results in better oral absorption through increasing Dn and decreasing the solubility of a drug results in better oral absorption through increasing Dn and decreasing Do. The fractions dose absorbed of digoxin, griseofulvin, and benoxaprofen agree with predicted F values sorbed by reducing particle size, while absorption of drugs with high Do and low Dn is limited by solubility and requires higher solubility to enhance the fraction dose absorbed in addition to micronization. Solubility at the physiological pH should be used for the estimation of the fraction dose absorbed.

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Chemical Composition and Antimicrobial Activity of Cone Volatile oil of Cupressus macrocarpa Hartwig from Nilgiris, India

  • Manimaran, S.;Themozhil, S.;Nanjan, M.J.;Suresh, B.
    • Natural Product Sciences
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    • 제13권4호
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    • pp.279-282
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    • 2007
  • The aim of the present study was to investigate the various chemical components present in the cone volatile oil of Cupressus macrocarpa and also determine its antimicrobial activity. Totally 13 compounds were identified with 99.99% by GC-MS analysis. The major compounds identified were terpinene-4-ol (19.42%), dinopol (15.63%), ${\alpha}$-pinene (13.58%), and ${\beta}$-pinene (12.16%). The antimicrobial activity was carried out for the oil and a 2% cream formulation using cup plate method by measuring the zone of inhibition. The gram positive organisms used were Bacillus subtilis, Staphylococcus aureus, Bacillus megaterium, and Bacillus cogulans. The gram negative organisms used were Escherichia coli, Kleibseilla pneumonia, Pseudomonas aeruginosa and Salmonella typhi. In vitro antifungal studies were also carried out by using organisms, Candida albicans, Aspergillus flavus, Trichoderma lignorum and Cryptococcus neoformans. The standard drugs used were penicillin ($100{\mu}g/mL$), gentamycin ($100{\mu}g/mL$) and griseofulvin ($100{\mu}g/mL$) for gram positive bacteria, gram negative bacteria and fungi respectively. Both oil and cream formulation showed good activity against fungi than bacteria. This study is being reported for the first time on cone volatile oil of this plant.

Xylaroisopimaranin A, a New Isopimarane Derivative from an Endophytic Fungus Xylaralyce sp.

  • Bao, Shang-Song;Liu, Hui-Hui;Zhang, Xue-Qing;Liu, Cheng-Xiong;Li, Xiao-Cong;Guo, Zhi-Yong
    • Natural Product Sciences
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    • 제25권3호
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    • pp.228-232
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    • 2019
  • Five secondary metabolites, including a new isopimarane derivative xylaroisopimaranin A (1), were isolated from the endophytic fungus Xylaralyce sp. (HM-1), and their structures were elucidated by 1D, 2D NMR, MS and CD spectra. Their bioactivities were performed to antibacterial, Hep G2 cells cytotoxicity and brine shrimp inhibition. The biological evaluation results showed that the xylaroisopimaranin A (1), xylabisboein B (2), griseofulvin (3), 5-methylmellein (4) and mellein-5-carboxlic acid (5) displayed no significant Hep G2 cells cytotoxicity and antibacterial acitivity, but they inhibited the brine shrimp with $IC_{50}$ from 0.5 to $25{\mu}mol/mL$.

Microsporum canis에 대한 5가지 항진균제와 맥반석 가루의 항진균 효과 (Antifungal Activity of 5 Antifungal Agents and Granitic Powder on Microsporum canis)

  • 강태형;이정치;원영호;오석일;이정길;이채용
    • 한국임상수의학회지
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    • 제22권4호
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    • pp.371-376
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    • 2005
  • The aim of this study was to determine tile inhibitory effect of granitic powder against Microsporum canis. Fourteen strains of M. canis isolated from dgs and cats with fungal dermatitis and two strains isolated from humans were used in this study. The in vitro antifungal activities of granitic powder and 5 commercialized antifungal agents (terbinafine, itraconazole, ketoconazole, griseofulvin and fluconazole) were compared. The antifungal effect was measured by the broth microdilution method and was expressed as the minimal inhibitory concentration (MIC). The MIC value of the granitic powder was ranged from 31.3 to 250mg/ml. Terbinafine showed the lowest MIC value among the 5 commercial antifungal agents $(0.0078-0.125{\mu}g/ml)$, while fluconazole showed the highest MIC values $(125-1,000{\mu}g/ml)$. The MIC range of itraconazole, griseofuvin and ketoconazole were $0.125-0.5{\mu}g/ml\;0.625-5{\mu}g/ml$ and $10-40{\mu}g/ml$ respectively. The Geometric mean(GM) MIC values of terbinafine and ketoconazole against M. canis isolated from human were $0.0078{\mu}g/ml\;and\;10{\mu}g/ml$, respectively, while the GM MIC values of these agents against M. canis isolated from animals were $0.063{\mu}g/ml\;and\;31.4{\mu}g/ml$, respectively. Other antifungal agents did not show any significant differences in antifungal activity against M. canis of animal or human origin. Although granitic powder was shown to have antifungal activity, it was much lower than that of the 5 commercialized antifungal agents.

유우유방염(乳牛乳房炎)에 관여(關與)하는 효모양진균(酵母樣眞菌)에 관한 연구(硏究) 2. 효모양진균(酵母樣眞菌)의 항진균성물질(抗眞菌性物質)에 대한 감수성(感受性) (Studies on the Yeast-Like Fungi Associated with Bovine Mastitis 2. Sensitivity of Yeast-Like Fungi to Antifungal Agents)

  • 여상건;최원필
    • 대한수의학회지
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    • 제22권2호
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    • pp.139-147
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    • 1982
  • A total of 133 isolates of yeast-like fungi was tested for sensitivity to seven different antifungal agents. The yeast-like fungi tested were isolated from the milk from normal or mastitic bovine quaters or from bovine feces. They were 5 Candida albicans (C. albicans) isolates, 63 C. krusei, 27 C. tropicalis, 5 C. parapsilosis, 10 Torulopsis glabrata, 6 Rhodotorula sp., 6 Hansenula sp. and 1 Pichia sp. isolate. The antifungal agents tested were nystatin, griseofulvin, cycloheximide, 5-fluorocytosine, miconazol, clotrimazole and tolnaftate. In general, clotrimazole, miconazol and 5-fluorocytosine were more effective in antifungal activity in vitro against the test organisms than the rest of the agents tested. However, some of the isolates showed higher resistance to certain antifungal agents compared to the other isolates of the some species. They were: 1 C. albicans isolate to 5-fluorocytosine; 1 C. albicans to 5-fluorocytosine, miconazol and clotrimazole; 1 C. krusei to 5-fluorocytosine and cycloheximide; and 11 C. tropicalis isolates to cycloheximide. The minimum inhibitory concentrations(MIC) of clotrimazole were $12.5{\mu}g/ml$ or lower for all isolates tested except one C. albicans isolate, for which MIC of the drug was $100{\mu}g/ml$. On the other hand, the MIC's of cycloheximide were $6.5{\mu}g/ml$ or lower for all isolates except the following; all isolates of C. albicans ($100{\mu}g/ml$), C. pseudotropicalis ($200{\mu}g/ml$) and Rhodotorula sp. ($25-50{\mu}g/ml$), 11 C. tropicalis isolates ($100{\mu}g/ml$) and 1 C. krusei isolate ($200{\mu}g/ml$).

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개 피부병 유래의 Microsporum canis의 항진균제 감수성 (Antifungal Susceptibility of Microsporum canis isolated from canine dermatophytosis)

  • 한기옥;최원필
    • 대한수의학회지
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    • 제41권2호
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    • pp.173-176
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    • 2001
  • 개 피부병 유래 Microsporum canis 57주와 표준균주 1주 등 58주를 broth microdilution test로 계통이 다른 7가지 항진균제에 대한 감수성을 조사하고 고찰하였다. M canis의 항진균주에 대한 MIC(기하평균) 측정에서 terbinafine은 $MIC{\leq}0.004{\sim}0.031(0.007){\mu}g/ml$, itraconazole은 $MIC{\leq}0.004{\sim}0.125(0.029){\mu}g/ml$, ketoconazole은 MIC $0.015{\sim}0.5(0.097){\mu}g/ml$, tolnaftage은 MIC $0.031{\sim}1(0.155){\mu}g/ml$순으로 감수성이 높았고, griseofulvine은 MIC $0.063{\sim}2(0.285){\mu}g/ml$, amphotericin B는 MIC $0.125{\sim}2(0.540){\mu}g/ml$, flucytosine(5-Fe)은 MIC $4{\sim}64(26.430){\mu}g/ml$으로 감수성이 낮았다.

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개 외이도에서 분리한 세균 및 M pachydermatis의 약제감수성에 대하여 (Drug susceptibility of bacteria and M pachydermatis isolated from canine external ear canals)

  • 김기향;최원필;여상건
    • 대한수의학회지
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    • 제39권3호
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    • pp.560-565
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    • 1999
  • The present work was conducted to investigate the drug susceptibility of microorganisms isolated from canine external ear canals. Antifungal susceptibility test of M pachydermatis (17 strains) was perfomed by agar dilution method, using 11 antifungal drugs including amphotericin B(A), nystatin(N), pimaricin(P), griseofulvin(G), bifonazole(B), clotrimazole(C), miconazole(M), econazole(E), ketoconazole(K), tolnaftate(T), 5-fluorocytosine(F). All isolates were highly sensitive to K, M, T(geometric mean MIC ; GM $MIC{\leq}0.16{\mu}g/ml$) but they weren't sensitive to P, F and G(GM $MIC{\geq}92.37{\mu}g/ml{\sim}{\geq}128{\mu}g/ml$). Antibacterial susceptibility test against 119 isolates of bacteria was performed by agar dilution method, using 9 antibacterial drugs including erythromycin(ET), chloramphenicol(CP), gentamycin(G), vancomycin(V), ampicillin(AP), amoxacillin(AX), chlortetracycline(CT), ciprofloxacin(CF), enrofloxacin(EF). All isolates of Staphylococcus spp(101 strains) were highly sensitive to EF, CF, G(GM MIC $0.33{\sim}1.47{\mu}g/ml$). In other gram positive cocci(4 strains), they were highly sensitive to EF, CF, V(GM MIC $1{\sim}4.76{\mu}g/ml$) and CT(GM MIC 1 UFL unit/ml). In gram positive rods(13 strains), they were highly sensitive to EF, CF, G(GM $MIC{\leq}0.19{\sim}1{\mu}g/ml$). In Pseudomonas aeruginosa(1 strain), it was highly sensitive to AX, EF, ET, CF(GM MIC $0.06{\sim}1{\mu}g/ml$) and CT(GM MIC 1 UFL unit/ml). All isolates weren't sensitive to AP(GM MIC 16~>$32{\mu}g/ml$).

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프레드니솔론 투여에 의한 조폐포자충(Pneumocystis carinii)성 간질성 폐염에 대한 실험적 연구 (An experimental study on prednisolone-induced interstitial pneumonia caused by Pneumocystis carinii)

  • 신대환;이영하;나영은
    • Parasites, Hosts and Diseases
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    • 제27권2호
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    • pp.101-108
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    • 1989
  • 실험 동물의 면역기능을 인위적으로 억제시킴과 동시에 몇 가지 항생 물질을 투여하여 Pneumocystis carin힐 또는 다른 원인에 의한 폐염을 발현시킨 다음 각 원인별 치사율 및 평균 생 존 기간(mean survival day) 등을 비교함으로써 간질성 폐염의 원인충으로서 흑 carinil히 중요성 을 알아보고자 이 연구를 실시하였다. 실험 동물로 Sprague-Dawley계 흰쥐 90마리를 사용하였고 각각 15마리씩 1개 대조군과 다음 5개 투약군으로 분류하였다. 1군 prednisolone(25mg/kg twice weekly), 2군 prednisolone과 tetracycline (75mg/kg/day) , 3군 prednisolone, tetracycline 및 trimethoprim·sulfamethoBazole (50∼250mg/kg/day), 4군 prednisolone과 trimethoprim-sulfamethozazole, 5군 prednisolone과 griseofulvin(300 mg/kg/day). 상기 약제를 횐쥐가 죽을 때까지 투여하고 각 흰쥐의 생존 기간을 측정하였다. 죽은 흰쥐는 즉시 부검하여 폐장을 적출한 후 접촉 도말 표본과 조직 절편 표본을 만들고 toluidine blue O, Giemsa, Gomori's methenamine-silver, hematoxylin-eosin, Brown & Brenn 염색 등을 하여 관찰하였다. 각 군별 평균 생존 기간은 1군 $19.3{\pm}5.2$일, 2군 $41.1{\pm}14.0$일, 3군 $50.5{\pm}18.4$일, 4군 $43.0{\pm}22.9$일, 5군 $21.8{\pm}5.1$일이었다. 카 군별 생존 기간의 차이를 비교하면 1군과 2군, 1군과 3군 및 1 군과 4군이 각각 유의한 차이(p<0.01)를 보여 세균 감염 방지시 생존 기간이 연장되는 것으로 나타났다. 또 1군과 5군의 생존 기간은 거의 차이가 없었고, 2군과 5군, 3군과 5군 및 4군과 5군은 유의한 차이(p<0.01)를 보여 진균 감염보다는 세균이나 P. carinii 감염이 흰쥐 사인에 직접적인 영향을 주는 것으로 나타났다. P. carinii 폐염에 의한 사망은 실험 17일에 최초로 나타났으며 각 군별 비율은 3군이 92.9%로 가장 높고, 2군 및 5군이 80.0%, 4군이 78.6%, 1군이 33.3%를 보였다. P. carinii 폐염으로 죽은 53마리를 분류한 바 stage 1은 11.3%, stage 2는 28.3%, stage 3은 60.4%이었다. 죽은 흰쥐의 사인을 기간별로 분류했을 때 실험 전기(1일∼28일)는 세균 감염에 의한 사망이 많 고, 실험 중기(29∼56일)는 주로 P. carinii 폐염에 의한 사망이었으며 진균과의 혼합감염이 이 시 기에 나타났다. 실험 후기 (57∼82일)에는 세균, 진균 감염 없이 모두 P. carinii 폐염으로 사망하 였다. 이상의 결과로 볼 때 면역억제제 투여 1개월 이후 흰쥐의 사망 원인으로는 세균이나 진균성 폐염 보다 P. carinii 폐염이 더욱 중요하다는 것을 알 수 있었다.

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