• Title/Summary/Keyword: ${\beta}$-Cyclodextrin

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Quantitative Estimation of Binding Site Polarities of Water-Soluble Polyparacyclophanes in Aqueous Solution by Spectrofluorometry (형광광도법에 의한 수용액중 수용성 폴리파라시클로판류의 결합부위의 극성 측정)

  • Chun, In-Koo
    • Journal of Pharmaceutical Investigation
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    • v.21 no.3
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    • pp.133-141
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    • 1991
  • The fluorescence characteristics of l-anilinonaphthalene-8-sulfonate (ANS) and 2-p-toluidinylnaphthalene-6-sulfonate (TNS) made the dyes useful probes for the determination of the polarity at the binding sites of several water-soluble polyparacyclophanes. Polyparacyclophanes used were 1,6,20,25-tetraaza[ 6.1.6.1]paracyclophane (CPM 44), 1,7,21,27 -tetraaza[7.1.7.1]paracyclophane (CPM 55). 1,7,21,27 -tetraaza-14,34-dioxa[7.1.7.1]paracyclophane (CPE 55) and 1,8,22,29-tetraaza-15,36-dioxa[8.1.8.1] paracyclophane (CPE 66). The fluorescence quantum yield, emission maximum, and half bandwidth of ANS or TNS obtained in a variety of solvent systems were plotted as a function of four kinds of empirical solvent polarity scales such as dielectric constant (D), (D-l)/(2D+1). Y and Z values. It was found that the Z-value-emission maximum $(\overline}V_F,\;cm^{-1})$ profile showed the most reliable linearity. ANS and TNS interacted with CPM 44, CPM 55, CPE 55. CPE 66. ${\alpha}-cyclodextrin$ (CyD) and ${\beta}-CyD$ in the aqueous solution, and from the emission maxima the polarities (Z-value) of their binding sites were calculated to be 92.65, 87.50, 93.35, 84.52, 94.36, and 90.48 for ANS, respectively. and 91.07, 89.68, 85.44, 86.74 and 87.6 for TNS except for ${\alpha}-CyD$, respectively.

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Chemical Washing of PAH-Contaminated Soil with Cyclodextrins as a Main Surfactant: A Labscale Study (사이클로덱스트린을 이용한 PAH오염토양의 화학적 세정)

  • Sung Hyun Kwon;Daechul Cho
    • Journal of the Korea Academia-Industrial cooperation Society
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    • v.3 no.4
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    • pp.295-302
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    • 2002
  • PAHs (polycyclic aromatic hydrocarbons) deposited in soil are one of serious problems against sustainable land use. In this paper, chemical soil flushing in a packed sandy soil matrix using a natural surfactant, $\beta$-cyclodextrin (CD) was studied via a fluorescence spectroscopy and a dye labelling. The contaminants are lipophilic ring compounds- phenanthrene and naphthalene. Sand type and flushing intensity (rate and concentration) are chosen as important investigation variables. The removal efficiencies were proportional to flow rate, concentration, temperature of the flushing solution and voidity of the sand column. Initial sorption of the surfactant onto the soil matrix was found to be a key step while flow shear was more crucial in the latter steps. The residual portion of the surfactant, which was most likely to be due to the initial sorption, would not be so influential on this type of soil washing for long times. These results will be useful in future for pilot scale in situ washing and for establishing better soil washing strategy.

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Novel Pathogenetic Mechanism in a Clinical Isolate of Yersinia enterocolitica KU14

  • Sato Yoshinori;Kaneko Kenichi;Sasahara Takeshi;Inoue Matsuhisa
    • Journal of Microbiology
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    • v.44 no.1
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    • pp.98-105
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    • 2006
  • Yersinia enterocolitica induces a broad range of gastrointestinal syndromes, including acute enteritis. We previously reported that the clinical isolate, Y. enterocolitica KU14, which lacks pYV, was still capable of causing clinical infection. The present study demonstrated that KU14 did not trigger the death of macrophages in vitro, unlike WA-314 (ATCC51871, which harbors the pYV virulence plasmid). However, the intracellular growth of KU14 in the macrophages was greater than that of WA-C (ATCC51872, a non-plasmid harboring the derivative pYV plasmid). Treatment with a cholesterol-binding drug $(\beta-cyclodextrin)$ that affected lipid rafts resulted in a dramatic reduction in the inracellular growth of KU14. These data clearly indicate that the enhanced inracellular growth of KU14 is related to lipid raft-mediated infection.

Dissolution Characteristics of Biphenyl Dimethyl Dicarboxylate from Solid Dispersions with Copolyvidone

  • Moon, Jee-Hyun;Chun, In-Koo
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 1997.04a
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    • pp.118-118
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    • 1997
  • Solid dispersions were used to increase the dissolution rate of biphenyl dimethyl dicarboxylate (DDB) in water, with the ultimate goal of optimizing its bioavailability when incoporated into pharmaceuticals. Carriers used were Kollidon 30, Kollidon VA 64, 2-hydroxypropyl-${\beta}$-cyclodextrin (HPCD), sodium salicylate or sodium benzoate. DDB solid dispersions were prepared at drug to carrier proportions ranging from 1 : 5 to 1 : 20 (w/w) by solvent evaporation method. DDB tablets (7.5 mg) were prepared by compressing the powder mixture composed of solid dispersions, lactose, corn starch, crospovidone and magnesium stearate using a single-punch press. DDB capsules (7.5 mg) were prepared by filing the mixture into empty hard gelatin capsules (size #1). Dissolution studies of DDB from powdered solid dispersions, tablets and capsules were performed in 900 $m\ell$ of water at 100 rpm and 37$^{\circ}C$ by the paddle method. The dissolved amount was assayed by HPLC and expressed as the mean(%)of three determinations.

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Enzymatic Synthesis of Vanillin-a -Glucoside and Ethyl Vanillin-a -Glucoside (효소적 방법에 의한 Vanillin-$\alpha$ -Glucoside 및 Ethyl Vanillin-$\alpha$ -Glucoside의 합성)

  • 김삼곤;김근수;나도영;김영회
    • Journal of the Korean Society of Tobacco Science
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    • v.25 no.2
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    • pp.120-127
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    • 2003
  • Cyclodextrin glucanotransferase (CGTase) from Bacillus stearothermophilus synthesized vanillin and ethyl vanillin monoglucoside, with a series of its maltooligoglucosides by transglycosylation with dextrin as a donor, and vanillin or ethyl vanillin as an acceptor. The monoglucoside formed from reaction mixture of vanillin or ethyl vanillin by the successive actions of CGTase and Rhizopus glucoamylase was isolated by extraction with n-butanol saturated with water and silica gel column chromatography. The structure of the isolated monoglucoside was identified as vanillin- $\alpha$ -D-glucoside and ethyl vanillin- $\alpha$ -D-glucoside, respectively, by FAB-MS, UV, IR, 1H-NMR, 13C-NMR spectra and products by hydrolysis with acid, $\alpha$ - and $\beta$ -glucosidases.

Isolation of Alkalophilic Bacillus sp. KJ-133 Producing Cyclomaltodextrinase and Its Enzyme Production (Cyclomaltodextrinase를 생산하는 Alkalophilic Bacillus sp. KJ-133의 분리와 효소생산 조건)

  • 정혜진;권호정
    • Microbiology and Biotechnology Letters
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    • v.28 no.4
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    • pp.219-222
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    • 2000
  • To produce and utilize microbial cyclomaltodextrinase being industrially useful, we isolated an alkalophilic Bacillus strain from soil which was capable of degrading cyclodextrins. The newly isolated strain was aerobic, gram-positive, spore-forming, motile, rod shape(0.2~0.4$\times$1.4~4.4 $\mu\textrm{m}$), and 35.8 mol% of DNA base composition. Based on its morphological, phisiological, and biochemical properties, it was identified as alkalophilic Bacillus sp. KJ-133 and cultivated well in the ranges of $30~40^{\circ}C$ and pH 8.0~9.0 . The cyclomaltodextrinase of the strain showed maximal production after 48h of cultivation at $37^{\circ}C$, and the activity was inhibited by Ag2+, Hg2+, Cu2+, and p-chloromercuribenzoate.

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Amylolytic Enzymes Produced from Hyperthermophilic Archaebactorium Thermococcus profundus (고도 호열성 Archaebacterium Thermococcus profundus가 생산하는 Amylolytic Enzymes)

  • Jeong, Yeong-Cheol;Kim, Gyeong-Suk;No, Seung-Hwan
    • The Korean Journal of Food And Nutrition
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    • v.7 no.4
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    • pp.259-266
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    • 1994
  • The hyperthermophilic archaebacterium Thermococcus profundus Isolated from a deep-sea hydrothermal vent system, produced several amylolytic enzymes such as extracellular amylase and pullulanase, intracellular a-1,4-91ucosidase in respone to the presence of complex carbohydrates In the growth medium. This strain showed high activities on 0.5% maltose than on complex carbohydrates One of the amylases was partially purified by ammonium sulfate precipitation, DEAE-Toyopearl chromatography. The amylase exhibited maximal activity at pH 5.5 and 80$^{\circ}C$, and was stable in the range of pH 5.5 to 9.5 and up to 80$^{\circ}C$ for 30 min. The enzyme activity was no dependence on Ca2+ and not inhibited by detergents. The amylase hydrolyzed soluble starch, amylose, amylopectin and glycogen to produce maltose and maltotriose with trace amounts of glucose, but not pullulan and ${\alpha}$-, ${\beta}$-, ${\gamma}$-cyclodextrin. Malto-oligosaccharides ranging from maltotetraose to maltoheptaose were hydrolyzed in an endo fashion.

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Separation of racemic enantiomer carvedilol and its metabolites using capillary electrophoresis (Capillary Electrophoresis에 의한 carvedilol 및 그 대사체의 거울상이성질체 분리)

  • Jo, Cheon-Ho;Koo, So-Hyun;Myung, Seung-Woon
    • Analytical Science and Technology
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    • v.19 no.4
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    • pp.275-279
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    • 2006
  • A capillary electrophoresis method for the separation of carvedilol and its metabolites enantiomers using cyclodextrins as the chiral selectors was developed. The effect of several types of cyclodextrins, concentration and capillary temperature for enantiomer resolution were investigated. Best results were obtained by 15 mM carboxymethyl-${\beta}$-cyclodextrin in the run buffer. Also the effect of capillary temperature on efficiency was assessed. The optimized method was applied for separation of chiral carvedilol and its three metabolites.

Solubilization of IH-901, a Novel Intestinal Metabolite of Ginseng Saponin, in Aqueous Solution (인삼사포닌의 소장내 최종대사물인 IH-901의 수용액중 가용화)

  • Kwon, Oh-Seung;Chung, Youn-Bok
    • Journal of Pharmaceutical Investigation
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    • v.34 no.5
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    • pp.385-391
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    • 2004
  • The purpose of the present study was to formulate the aqueous solution of $20-O-{\beta}-D-glucopyranosyl-20(S)-protopanaxadiol\;(IH-901)$, an intestinal bacterial metabolic derivative from Ginseng protopanaxadiol saponin. For this purpose, the effects of various solubilization agents such as cosolvents [ethanol, propylene glycol (PG), polyethylene glycol 300 (PEG 300), polyethylene glycol 400 (PEG 400), glycerin], surfactants $(Tween\;80,\;Cremophor^{\circledR}\;RH40,\;Cremophor^{\circledR}\;EL,\;Poloxamer\;407,\;Poloxamer\;188)$ and a complexation agent $[hydroxypropyl-{\beta}-cyclodextrin\;(HPBCD)]$, on the solubility of IH-90l in aqueous solution were evaluated. The solubility of IH-901 in water was under $1\;{\mu}g/ml\;at\;20^{\circ}C$. Cosolvents such as ethanol, PG, PEG 300, PEG 400 and glycerin did not enhance the solubility of IH-901 at the 0 - 40% concentration range. The solubility of IH-901 was significantly elevated by the addition of cosolvents over the 80% concentration range. On the other hand, tween 80, $Cremophor^{\circledR}\;EL,\;Cremophor^{\circledR}\;RH40$ and HPBCD showed enhanced effects on the solubility of IH-901. The enhanced effects of Poloxamer 407 or Poloxamer 188 on the IH-901 solubility were less pronounced compared with $Cremophor^{\circledR}\;EL\;or\;Cremophor^{\circledR}\;RH40$. As a results, $Cremophor^{\circledR}$ aqueous solution was selected as an optimum solvent system. The aqueous solutions containing 10% $Cremophor^{\circledR}\;EL$ and 7% $Cremophor^{\circledR}\;RH40$ were formulated as dosing solutions containing 5.0 mg/ml of IH-901 for its intravenous and oral administration, respectively. The formular showed physical stability after stored for 7 days at $4^{\circ}C$.

Transmucosal Delivery of Luteinizing Hormone Releasing Hormone(LHRH): Evaluation of Membrane Permeability Enhancement of $[D-Ala^6]$ LHRH in Rabbit Mucosa and Ovulation Inducing Effect in Vaginal Administration of Rat by the Addition of Several Absorption Enhancers (황체호르몬 유리호르몬의 경점막 수송: 수종의 흡수촉진제를 사용한 $[D-Ala^6]$ LHRH의 점막투과촉진 및 흰쥐에 있어서의 배란유도효과 향상)

  • Han, Kun;Jeong, Nam-Joo;Park, Jeong-Sook;Park, Hee-Beom;Chung, Youn-Bok;Moon, Dong-Cheul
    • YAKHAK HOEJI
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    • v.38 no.4
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    • pp.440-450
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    • 1994
  • Due to the limited bioavailability of $[D-Ala^6]$LHRH from nonparenteral transmucosal sites of administration, enhancement of mucosal permeability by coadministration of several protease inhibitors and/or penetration enhancers were studied in rabbit mucosa. As a reliable bioassay method for $[D-Ala^6]$LHRH, ovulation-inducing effect were measured after vaginal administration in the rat. The permeation of $[D-Ala^6]$LHRH through the mucosal membrane of rabbit mounted on George-Grass diffusion cells were examined in the presence of polyoxyethylene 9-lauryl ether (POE), ${\beta}$-cyclodextrin$({\beta}-CyD)$ or ethylene diamine tetra acetate disodium salt(EDTA). The vaginal membrane showed higher permeability of $[D-Ala^6]$LHRH than the rectal and nasal membrane. POE and ${\beta}-CyD$ showed a small promoting effect on the membrane permeation of $[D-Ala^6]$LHRH, but EDTA showed significant enhancement. Ovaluation was enhanced by the coadministration of sodium laurate(0.5%), a protease inhibitor but was not enhanced by EDTA, a penetration enhancer. On the other hands, coadministration of sodium tauro 24,25 dihydrofusidate(1%) and EDTA(2%) enhanced the ovulation inducing-effect 2.8 times. These results suggest that the vaginal administration of $[D-Ala^6]$LHRH with STDHF or sodium laurate as a protease inhibitor, and EDTA as a penetration enhancer, may become an elective method for transmucosal delivery of $[D-Ala^6]$ LHRH.

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