• Title/Summary/Keyword: benzimidazole

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Complexation and Properties of Omeprazole with Hydroxypropyl-$\beta$-cyclodextrin (오메프라졸과 Hydroxypropyl-$\beta$-cyclodextrin의 포접화합물의 형성과 특성)

  • 이계주;황성주;이기명
    • YAKHAK HOEJI
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    • v.37 no.4
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    • pp.331-340
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    • 1993
  • Inclusion complex of omeprazole(OMZ) with hydroxypropyl-$\beta$-cyclodextrin(HP-$\beta$-CD) was prepared by freeze-drying method. The complexation was confirmed by means of UV, CD, IR, DSC, XRD and $^{1}$H-NMR spectra. The benzimidazole moiety of OMZ might be found to be included into the cavity of HP-$\beta$-CD and the inclusion complex appeared to be $A_{L}$ type. The stoichiometric ratio of OMZ : HP-$\beta$-CD was found to be 1:1, and the stability constants of the inclusion complex by solubility and UV method were about 34 and 45 M$^{-1}$, respectively. The dissolution of OMZ was significantly enhanced from powder and. yablet of OMZ-HP-$\beta$-CD complex when compared to those of OMZ alone, and oil-to-water partition coefficient of OMZ-HP-$\beta$-CD complex was significantly higher than that of OMZ alone. Therefore, it was expected that the bioavailability of OMZ could be improved markedly by inclusion complexation of OMZ with HP-$\beta$-CD.

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A Study on the Pharmaceutical Characteristics and Analysis of Natural Ginger Extract (천연 생강 추출물의 약리학적 특성 및 분석 연구)

  • Sung, Ki-Chun
    • Journal of the Korean Applied Science and Technology
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    • v.27 no.3
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    • pp.266-272
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    • 2010
  • Natural Ginger extract was extracted from Ginger component using ethanol as a solvent, and we tested various pharmaceutical characteristics in this extract. Characteristics experiment to use natural Ginger extract tested antimicrobial experiment using microbe, and analyzed organic and inorganic component with analysis instrument. From the result of characteristics experiment, some conclusions are obtained as follow. In this experiment, natural Ginger extract was obtained about 22.50 g-Ginger extract(extraction ratio : 1.80%) as liquid state of some viscous yellow-brown color. The result of antimicrobial experiment with staphylococcus aureus and aspergillus niger in microbe decreased more and more according to passage of reaction time. This phenomenon could know that Ginger extract has influenced to antimicrobial effect. In the result of instrumental analysis, aromatic organic components of benzimidazole(1.283), propyl isothiocyanate or isothiocyanic acid(1.477) etcs from Ginger extract were detected with GC/MS and inorganic component of Ca(27.6 ppm), K(24.08 ppm), Mg(6.03 ppm), Na(1.02 ppm), Zn(1.02 ppm), Sb(0.711 ppm) and Li(0.079 ppm) etcs from Ginger extract were detected with ICP/OES.

Dioxygen Binding to the Singly Alkoxo-Bridged Diferrous Complex: Properties of [$Fe^{Ⅱ}_2$(N-Et-HPTB)$Cl_2$]$BPh_4$

  • 김은석;이강봉;Jang, Ho G.
    • Bulletin of the Korean Chemical Society
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    • v.17 no.12
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    • pp.1127-1131
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    • 1996
  • [FeⅡ2(N-Et-HPTB)Cl2]BPh4(1), where N-Et-HPTB is the anion of N,N,N',N'-tetrakis(N-ethyl-2-benzimidazolylmethyl)-2-hydroxy-l,3-diaminopropane, has been synthesized to model dioxygen binding to the diferrous centers of proteins. 1 has a singly bridged structure with a μ-alkoxo of N-Et-HPTB and contains two five-coordinate iron(Ⅱ) centers with two chloride ligands as exogenous ligands. 1 exhibits an electronic spectrum with a λmax at 336 nm in acetone. 1 in acetone exhibits no EPR signal at 4 K, indicating diiron(Ⅱ) centers are antiferromagnetically coupled. Exposure of acetone solution of 1 to O2 at -90 ℃ affords an intense blue color intermediate showing a broad band at 586 nm. This absorption maximum of the dioxygen adduct(1/O2) was found in the same region of μ-l,2-peroxo diiron(Ⅲ) intermediates in the related complexes with pendant pyridine or benzimidazole ligand systems. However, this blue intermediate exhibits EPR signals at g = 1.93, 1.76, and 1.59 at 4 K. These g values are characteristic of S = 1/2 system derived from an antiferromagnetically coupled high-spin Fe(Ⅱ)Fe(Ⅲ) units. 1 is the unique example of a (μ-alkoxo)diferrous complex which can bind dioxygen and form a metastable mixed-valence intermediate. At ambient temperature, most of 1/O2 intermediate decays to form a diamagnetic species. It suggests that the dacay reaction of the intermediate might be bimolecular, implying the formation of mixed-valence tetranuclear species in transition state.

Differential cytotoxic effects of fenbendazole on mouse lymphoma EL-4 cells and spleen cells

  • Haebeen Jung;You-Jeong Lee;Hong-Gu Joo
    • Korean Journal of Veterinary Research
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    • v.63 no.1
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    • pp.2.1-2.7
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    • 2023
  • Fenbendazole (FBZ) is a benzimidazole anthelmintic widely used to treat parasitic infections. The anticancer effect of FBZ has been recently highlighted leading to its consideration as a potential anticancer agent. Although previous studies have demonstrated the effect of FBZ on cancer cells, there is a paucity of studies on the effect of FBZ on lymphoma cells and normal immune cells. Herein, we investigated the effects of FBZ on a mouse lymphoma cell line, EL-4 cells, and spleen cells, using vincristine as a positive control. The cellular metabolic activity of EL-4 cells was decreased by FBZ, but that of the spleen cells was not decreased. Moreover, FBZ reduced the mitochondrial membrane potential and induced reactive oxygen species production in EL-4 cells, but not in spleen cells. FBZ induced G2/M phase arrest and increased the sub G0/G1 phase ratio, indicating apoptosis. Furthermore, compared to the control cells, the reactivity of spleen cells pretreated with FBZ to lipopolysaccharide was maintained. In summary, FBZ is cytotoxic to EL-4 cells, but not to spleen cells. This study provides experimental evidence that FBZ exerts an anticancer effect, and less cytotoxic effects and functional damage to normal spleen cells.

Effect of Hole-Transporting Layer and Solvent in Solution Processed Highly-Efficient Small Molecule Organic Light-Emitting Diodes

  • Jo, Min-Jun;Hwang, Won-Tae;Chae, Hee-Yeop
    • Proceedings of the Korean Vacuum Society Conference
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    • 2012.08a
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    • pp.250-250
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    • 2012
  • Organic light-emitting diodes (OLED) and polymer light emitting diodes (PLED) have been regarded as the candidate for the next generation light source and flat panel display. Currently, the most common OLED industrial fabrication technology used in producing real products utilizes a fine shadow mask during the thermal evaporation of small molecule materials. However, due to high potential including low cost, easy process and scalability, various researches about solution process are progressed. Since polymer has some disadvantages such as short lifetime and difficulty of purifying, small molecule OLED (SMOLED) can be a good alternative. In this work, we have demonstrated high efficient solution-processed OLED with small molecule. We use CBP (4,4'-N,N'-dicarbazolebiphenyl) as a host doped with green dye (Ir(ppy)3 (fac-tris(2-phenyl pyridine) iridium)). PBD (2-(4-biphenylyl)-5-(4-tert-butylphenyl)-1,3,4-oxadiazole) and TPD (N,N'diphenyl-N,N'-Bis (3-methylphenyl)-[1,1-biphenyl]-4,4'-diamine) are employed as an electron transport material and a hole transport material. And TPBi (2,2',2''-(1,3,5-phenylene) tris (1-phenyl-1H-benzimidazole)) is used as an hole blocking layer for proper hole and electron balance. With adding evaporated TPBi layer, the current efficiency was very improved. Among various parameters, we observed the property of OLED device by changing the thickness of hole transporting layer and solvent which can dissolve organic material. We could make small molecule OLED device with finding proper conditions.

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Study on analytical method of residual benzimidazole anthelmintics in meat by LC/MS (LC/MS를 이용한 식육중 잔류 벤지미다졸계 구충제 분석법 연구)

  • Choi Eun-Young;Seo Heyng-Seok;Baek Kui-Jeong;Hur Boo-Hong;Seo Lee-Won;Joung Dong-Suk
    • Korean Journal of Veterinary Service
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    • v.28 no.1
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    • pp.81-89
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    • 2005
  • Recently, mass spectrometry coupled with liquid chromatography (LC/MS) has been a preferred technique for determination of organic compounds in complex matrixes. LC/MS provides a high degree sensitivity and specificity of the compounds of interest. The purpose of this study was to confirm analytical method of residual 6 benzimidazoles (thiabendazole, oxfendazole, mebendazole, albendazole, flubendazole and fenbendazole) in meat by LC/MS. Benzimidazoles were analyzed by LC/MS on XTerra $C_{18}$ column with 0.01% trifluoroacetic acid-acetonitrile (TFA) in a gradient mode as mobile phase, and that were identified by electrospray ionization with selected ion recording mode at 150-350 amu mass range. Residual benzimidazoles were extracted from tissue with ethylacetate, and elute benzimidazoles with $50\%$ acetonitrile. In the LC/MS analysis of benzimidazoles, signal to noise ratio was showed relatively high in the positive mode and special ion in the quality analysis was determined via $[M+H]^+$ and Fragment ions. A spectrum of benzimidazoles was showed from all 6 benzimidazoles

Chemical Resistance and Control of Dollar Spot Caused by Sclerotinia homoeocarpa on Turfgrass of Golf Courses in Korea (한국 골프장 잔디에서의 Sclerotinia homoeocarpa의 약제 저항성 및 방제)

  • Kim, Jeong-Ho;Choi, Hee-Youl;Shim, Gyu-Yul;Kim, Young-Ho
    • Asian Journal of Turfgrass Science
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    • v.24 no.2
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    • pp.170-175
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    • 2010
  • A total of 24 isolates of S. homoeocarpa were isolated from 16 golf courses in Korea. Chemical resistance of 24 isolates was determined by in vitro fungal growth on fungicide-amended media with thiophanatemethyl (Benzimidazole fungicide family), tebuconazole (demethylation inhibitor fungicide family: DMI), and iprodione (dicarboximide fungicide family). Results indicated that 83.3% of 24 isolates were resistant to iprodione, 62.5% resistant to thiophanate-methyl and 0% resistant to tebuconazale. The dual resistance of iprodione and thiophanate-methyl was 58.3.%. Occurrence rate of fungicide resistance of thiophanate-methyl and iprodione had no relation to turfgrass varieties and isolated locations of pathogen. In the filed test, procymidone, boscalid, and fluquinconazole+pyrimethanil effectively controlled the dollar spot of creeping bentgrass.

Stability Improvement of Esomeprazole Magnesium Dihydrate Enteric-Coated Tablet by Adding Alkalizing Agents (에스오메프라졸 마그네슘 이수화물을 함유하는 장용성 제제의 안정성 개선)

  • Cho, Young Ho;Jeon, Hyo Bin;Lee, Jong-Hwa;Lee, Gye Won
    • KSBB Journal
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    • v.32 no.2
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    • pp.108-116
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    • 2017
  • Omeprazole, a benzimidazole derivative, suppresses gastric acid secretion by inhibiting $H^+/K^+$ ATPase in gastric parietals cells, and by reducing $H^+$ concentration. To improve stability of esomeprazole magnesium dihydrate (ESMD), enteric-coated preperation was composed of core tablet, subcoating and enteric coating layer. We were evaluated in vitro dissolution characteristics between test and reference ESMD preparation and stability. We could prepare enteric-coated formulation of ESMD by controlling disintegrating agent and coating ratio which could rapidly dissolved in neutral or alkali medium. The formulation D5 with crospovidone of 1.25% and coating ratio of 16.25% had a similar dissolution behavior compare to reference preparation. Difference factor ($f_1$) and similarity factor ($f_2$) were 0~15 and 50~100 and there was no significant difference in bioequivalence between formulations. The content and dissolution rate of formulation D5 were $96.54{\pm}0.21$ and $78.56{\pm}0.87%$ without change of color in accelerated condition ($40^{\circ}C$, RH 75%, high density polyethylene (HDPE) container) for 6 months. This study concluded that our enteric coated preparation of ESMD could be an useful method to improve stability of unstable drug without direct contact with coating material.

Population Dynamics and Fitness Comparison of Sensitive and Resistant Phenotypes of Botrytis cinerea to Benzimidazole, Dicarboximide, and N-phenylar-bamate Fungicides

  • Kim, Byung-Sup;Park, Eun-Woo;Cho, Kwang-Yun
    • The Plant Pathology Journal
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    • v.17 no.3
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    • pp.149-153
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    • 2001
  • A total of 2109 isolates of Botrytis cinerea were collected from infected plants fo strawberry, tomato, and cucumber in Korea from 1994 to 1996. Based on in virtotests for mycelial growth on potato-dextrose agar containing fungicides, the esolates were classified into six phenotypic groups : SSR, SRR, RSS, RRS, RSR, and RRR, representing sensitivity (S) or resistance (R) to carbendazim, procymidone, and diethofencarb. In that order the isolation frequencies of the SSR, SRR, RSS, RRS, RSR, and RRR phenotypes were 28.7, 1.1, 28.8, 39.4, 1.0, and 0.9%, respectively. Three isolates from each SSR, SRR, RSS, RRS, and RSR and an isolate of RRR phenotype were selected and evaluated for their fitness-related characteristics such as pathogenic aggressiveness, mycelial growth rate, sporulation, and sclerotial formation. Competitive abilities of the SSR, SRR, RSS, RRS, and RSR phenotypes were also compared by inculating mixtures of conidial suspensions of two phenotypes to cucumber plant, and then determining re-isolation frequencies from lesions. In general, significant differences in fitness-related characteristics, except pathogenic aggressiveness, were found not only between but also within phenotype groups. In the competitiveness tests, carbendazim-sinsitive phenotypes (SSR and SRR) were found to be more competitive than the resistant ones (RSS and RSR), whereas, the procymidone-resistant phenotypes (SRR and RRS) appeared to be more competitive than the sensitive ones (SSR, RSS, and RSR). There was no consistent dominance in competitiveness between the diethofencarb-resistant and sensitive phenotypes. The RSR phenotype was the least competitive among the five phenotypes.

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Estimation of uncertainty for the determination of residual flubendazole in pork (돼지고기 중 플루벤다졸 잔류분석의 불확도 추정)

  • Kim, MeeKyung;Park, Su-Jeong;Lim, Chae-Mi;Cho, Byung-Hoon;Kwon, Hyun-Jeong;Kim, Dong-Gyu;Chung, Gab-Soo
    • Korean Journal of Veterinary Research
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    • v.47 no.2
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    • pp.139-145
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    • 2007
  • Measurement uncertainty could play an important role in the assessment of test results in laboratories and industries. We investigated measurement uncertainties possibly included in determination of flubendazole, a benzimidazole anthelmintic, in pork by HPLC. The concentration of flubendazole was 62.69 ng/g in a sample of pork. Uncertainty was estimated in the analytical procedure of flubendazole. A model equation was made for determination of flubendazole in pork. The four uncertainty components such as weight of sample, volume of sample, calibration curve, and recovery were selected to estimate measurement uncertainties. Standard uncertainty was calculated for each component and all the standard uncertainties were combined. The combined standard uncertainty was expanded to a sample population as an expanded uncertainty. The expanded uncertainty was calculated using k value on Student's t-table and effective degrees of freedom from Welch-Satterthwaite formula. The expanded uncertainty was calculated as 3.45 with the combined standard uncertainty, 1.584 6 and the k value, 2.18. The final expression can be ($62.69{\pm}3.45$) ng/g (confidence level 95%, k = 2.18). The uncertainty value might be estimated differently depending on the selection of the uncertainty components. It is difficult to estimate all the uncertainty factors. Therefore, it is better to take several big effecting components instead of many small effecting components.