• Title/Summary/Keyword: sodium deoxycholate

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Impact of Micellar Vehicles on in situ Intestinal Absorption Properties of Beta-Lapachone in Rats

  • Jang, Soung Baek;Kim, Dongju;Kim, Seong Yeon;Park, Changhee;Jeong, Ji Hoon;Kuh, Hyo-Jeong;Lee, Jaehwi
    • The Korean Journal of Physiology and Pharmacology
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    • v.17 no.1
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    • pp.9-13
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    • 2013
  • The aim of the present study was to examine the effect of micellar systems on the absorption of beta-lapachone (b-lap) through different intestinal segments using a single-pass rat intestinal perfusion technique. B-lap was solubilized in mixed micelles composed of phosphatidylcholine and sodium deoxycholate, and in sodium lauryl sulfate (SLS)-based conventional micelles. Both mixed micelles and SLS micelles improved the in situ permeability of b-lap in all intestinal segments tested although the mixed micellar formulation was more effective in increasing the intestinal absorption of b-lap. The permeability of b-lap was greatest in the large intestinal segments. Compared with SLS micelles, the effective permeability coefficient values measured with mixed micelles were 5- to 23-fold higher depending on the intestinal segment. Our data suggest that b-lap should be delivered to the large intestine using a mixed micellar system for improved absorption.

Pharmacological Effect of Cholates of Cardiac Function (심운동(心運動)에 대한 담즙산의 영향)

  • Ro, J.Y.;Kim, H.Y.;Hong, S.S.
    • The Korean Journal of Pharmacology
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    • v.14 no.1_2
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    • pp.41-46
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    • 1978
  • The effects of sodium taurocholate(STC) and sodium deoxycholate(SDC) on cardiac function were examined by using isolated atria of rabbit and guinea pig and heart of anesthetized frog. Also the antiarrythmic action of STC and SDC on atrial arrhythmias induced by epinephrine or ouabain was studied. The results were following. The cholates exhibited a slight decrease in rate and contractile amplitude of the isolated rabbit atria. The cholates abolished partially the spontaneous arrhythmic occurring in isolated rabbit and guinea pig atria but no effect on the atrial arrhythmia induced by ouabain and epinephrine was observed. Concomitant administration of cholates with ouabain produced a marked prolongation of atrial arrhythmia in comparison to that of ouabain alone in both isolated rabbit and guinea pig atria. The cholates exhibited a marked prolongation in ventricular arrhythmia and cardiac arrest time in comparison to that of ouabain treatment. However, the combined treatment with cholates and ouabain produced a slight prolongation in comparison to that of ouabain alone in the heart of anesthetized frog. The above results suggest that cholates have a slight antiarrythmic effect on the heart but this effectiveness is different from those of propranolol that is non-selective antiarrhythmic drug.

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Purification and Characterization of an Alkali-Thermostable Lipase from Thermophilic Anoxybacillus flavithermus HBB 134

  • Bakir, Zehra Burcu;Metin, Kubilay
    • Journal of Microbiology and Biotechnology
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    • v.26 no.6
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    • pp.1087-1097
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    • 2016
  • An intracellular lipase from Anoxybacillus flavithermus HBB 134 was purified to 7.4-fold. The molecular mass of the enzyme was found to be about 64 kDa. The maximum activity of the enzyme was at pH 9.0 and 50℃. The enzyme was stable between pH 6.0 and 11.0 at 25℃, 40℃, and 50℃ for 24 h. The Km and Vmax of the enzyme for pNPL substrate were determined as 0.084 mM and 500 U/mg, respectively. Glycerol, sorbitol, and mannitol enhanced the enzyme thermostability. The enzyme was found to be highly stable against acetone, ethyl acetate, and diethyl ether. The presence of PMSF, NBS, DTT and β-mercaptoethanol inhibited the enzyme activity. Hg2+, Fe3+, Pb2+, Al3+, and Zn2+ strongly inhibited the enzyme whereas Li+, Na+, K+, and NH4+ slightly activated it. At least 60% of the enzyme activity and stability were retained against sodium deoxycholate, sodium taurocholate, n-octyl-β-D-glucopyranoside, and CHAPS. The presence of 1% Triton X-100 caused about 34% increase in the enzyme activity. The enzyme is thought to be a true lipase since it has preferred the long-chain triacylglycerols. The lipase of HBB 134 cleaved triolein at the 1- or 3-position.

The Actions of Diphenylhydantoin sodium and Quinidine on the Adenosine triphosphatase Activity in Mitochondrial Fraction of Rabbit Heart (가토심근(家兎心筋) Mitochondria 분획내(分劃內) Adenosine triphosphatase 활성도(活性度)에 대(對)한 Diphenylhydantoin sodium 및 Quinidine의 작용(作用))

  • Hong, Ki-Whan
    • The Korean Journal of Pharmacology
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    • v.8 no.1
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    • pp.31-40
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    • 1972
  • The author studied the actions of ouabain and diphenylhydantoin sodium on the ATPase activity in mitochondrial fraction isolated from rabbit heart and compared with that of quinidine. The results obtained are as follows: 1) In studying the $(Na^++K^+)-activated$ ATPase activity, the rabbit heart isolated was immediately frozen for 7-9 days (ageing of preparation) and thereafter the mitochondria1 fraction obtained by differential centrifugation technic was treated with solution A containing 0.15% deoxycholate for 24-48 hours at $-10^{\circ}C$ before using in experiment. These methods increased the activity ratio to 0.87-0.98. 2) The $(Na^++K^+)-activated$ ATPase activity in mitochondrial fraction of rabbit heart was not completely but markedly inhibited by ouabain. This inhibitory action of ouabain was moderately antagonised by $K^+$ concentration at constant Na concentration. 3) Diphenylhydantoin sodium in concentration of $5{\times}10^{-4}{\sim}10^{-3}M$ stimulated markedly not only $Mg^{++}-dependent$ ATPase activity but also $(Na^++K^+)$-activated ATPase activity and in concentration lower than $10^{-6}M$ had little effect. However, this effect of diphenylhydantoin was markedly increased in the presence of $Na^+$ alone rather than $K^+$ alone, but lesser than that effect in the presence of both $Na^+$ and $K^+$, together. The stimulating effect of diphenylhydantoin was specifically antagonized by ouabaion. 4) When the rabbits were intravenously injected with ouabain and diphenylhydantion respectively, $(Na^++K^+)-activated$ ATPase activity of rabbit heart of ouabain-treated group was much decreased and both $(Na^++K^+)-activated$ ATPase and $Mg^{++}-activated$ ATPase activity were moderately increased in diphenylhydantoin-treated rabbit group. 5) The $(Na^++K^+)-activated$ ATPase activity in mitochondrial fraction of rabbit heart was slightly inhibited by quinidine in high concentration of $10^{-4}M$, but nearly little effect was observed below the concentration of $5{\times}10^{-5}M$. 6) It might be possible to conclude that diphenylhydantoin specifically antagonised the action of ouabain on the membrane ATPase, which is different from the action of quinidine.

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Effect of Ginseng Alcohol Extract on the Oxygen Consumption of Rat Liver Mitochondria (인삼알콜추출물이 쥐간 mitochondria의 산소 소모율에 미치는 영향)

  • Lee, Joong-Woo;Kim, In-Kyo;Kang, Doo-Hee
    • The Korean Journal of Physiology
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    • v.13 no.1_2
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    • pp.23-28
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    • 1979
  • The following results were drawn from the experiment conducted to see the effect of ginseng alcohol extract on the mitochondrial oxidation of the rat liver. 1) Mitochondrial oxygen consumption increased in the low concentration and decreased in the high concentration of ginseng alcohol extract. 2) When the mitochondria was destroyed mechanically or was swollen by low concentration of $AgNO_3$, mitochondrial oxygen consumption was inhibited in all concentration of ginseng alcohol extract. 3) Oxygen consumption of intact mitochondria increased in the low concentration but decreased in the high concentration of sodium deoxycholate. 4) Ginseng alcohol extract inhibited cytochrome oxidase activities of liver mitochondria. These results suggest that low concentration of ginseng alcohol extract activates the oxygen consumption of liver mitochondria by increasing the permeability of the mitochondrial membrane and high concentration of the extract inhibit the oxygen consumption by inhibiting the enzyme activity related to respiration.

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Induction of Colonial Growth of the Cellulolytic Fungus, Genus Trichoderma (섬유소분해균인 Trichoderma의 群體生長의 유도에 관하여)

  • Park, Hee-Moon;Hong, Soon-Woo;Hah, Yung-Chil
    • Korean Journal of Microbiology
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    • v.22 no.3
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    • pp.143-150
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    • 1984
  • The effect of growth inhibitors on colonial growth of cellulolytic fungus, genus Trichoderma, was investigated to develop a method for the effective screening of various auxotrophs and hypercellulolytic strains. As the results, it was revealed that non-ionic detergents such as Sodium deoxycholate and Triton X-100 were the better ones as a growth inhibitor than Oxgall which has been used to restrict the colony size in genus Trichoderma. Each individual colony remained distinct on minimal plate supplemented with 0.05% Triton X-100 for as long as two or more weeks. The screening of 150 to 200 colonies simultaneous on a single plate was possible in the presence of Triton X-100. The effect of Triton X-100 on simultaneous screening was higher than that of Oxgall by a factor of two.

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Effect of Triol Fraction of Ginseng Saponin on Filamentous Formation through Reduction in C-AMP Concentration in Bacillus subtizis. (Botcillus subtilis에서 인삼 saponin의 triol fraction에 의한 C-AMP농도 감소가 filament생성에 미치는 효과)

  • 조영동;최수영
    • Journal of Ginseng Research
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    • v.7 no.1
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    • pp.63-67
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    • 1983
  • Bacillus subtilis grown on medium containing 0.1% trios fraction, 0.005% sodium deoxycholate, and 0.05% taurocholate respectively was shown to grow as filamentous form and contain 2.3 x 10-5M, 1 x 10-5M, and 2.3${\times}$10-5M of intracellular C-AMP, respectively. The concentration was 3 or 4 times lower than that of the control. But concentrations of extracellula: C-AMP were similar to that of the control. Such decrease in C-AMP concentration was shown to parallel with decrease in autolysin activity indicating 40% and 20% lower activity of Bacillus subtilis grown on medium containing 0.05% and 0. l% triol fraction respectively than that of the control, The activity was also shown to be in inverse proportion with the formation of filament .

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The Properties of Cement Paste Mixed with Carbon Nanotubes Dispersion Solution (탄소나노튜브 분산용액을 혼입한 시멘트 페이스트의 특성 변화)

  • Park, Sung-Hwan;Kim, Ji-Hyun;Chung, Chul-Woo
    • Proceedings of the Korean Institute of Building Construction Conference
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    • 2021.05a
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    • pp.201-202
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    • 2021
  • Currently, the domestic construction industry is trying to expand the range of building materials due to overload of growth. In particular, several studies are being conducted to make up for the weakness of building materials by solving problems such as reduction of tensile strength and brittle behavior of concrete. Among them, efforts to maximize the use of carbon nanotubes (CNT) that has excellent mechanical and electrical conductivity properties are continuing. However, CNT is hydrophobic and have a strong Van der Waals force between particles, making it difficult to obtain an effective dispersion state. Therefore, in this study, various kinds of surfactants like DOC (Sodium Deoxycholate), PVP (Polyvinylpyrrolidone), and PCE (Polycarboxylate ester) were added to improve the dispersibility of CNT, and analyzed the changes in the properties of the cement paste mixed with them.

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Graphene Oxide/Polyimide Nanocomposites for Gas Barrier Applications (산화그래핀이 함유된 폴리이미드 나노복합막의 기체차단성 평가 및 활용)

  • Yoo, Byung Min;Lee, Min Yong;Park, Ho Bum
    • Membrane Journal
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    • v.27 no.2
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    • pp.154-166
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    • 2017
  • Polymeric films for gas barrier applications such as food packaging and electronic devices have attracted great interest due to their cheap, light and easy processability among gas barrier materials. Especially in electronic devices, extremely low gas permeance is necessary for maintaining the device performance. However, current polymeric barrier films still suffer from relatively high gas permeance than other materials. Therefore, there have been strong needs to enhance the gas barrier performance of polymeric barrier films while keep their own advantages. Recently, graphene is highlighted as a 2D-layered material for gas barrier applications. However, owing to the poor workability and difficulty to produce in engineering scale, graphene oxide (GO) is on the rise. GO consists of oxygen-containing functional groups on surface with intrinsic 2D-layered structure and high aspect ratio, and it can be well-dispersed in aqueous polar solvents like water, resulting in scalable mass production. Here, we prepared GO incorporated polyimide (PI) nanocomposites. PI is widely used barrier polymer with high mechanical strength and thermal and chemical stability. We demonstrated that PI/GO nanocomposites could perform as a gas barrier. Furthermore, surfactants (Triton X-100 (TX) and Sodium deoxycholate (SDC)) are introduced to enhance the gas barrier performance by improving the degree of dispersion of GO in PI matrix. As a result, TX enhanced the gas barrier performance of PI/GO nanocomposites which is similar to predicted value. This finding will provide new insight to polymer nanocomposites for gas barrier applications.

Dissolution and Duodenal Permeation Characteristics of Lovastatin from Bile Salt Solid Dispersions (담즙산염과의 고체분산체로부터 로바스타틴의 용출 및 십이지장 점막 투과 특성)

  • Chun, In-Koo
    • Journal of Pharmaceutical Investigation
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    • v.39 no.2
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    • pp.97-106
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    • 2009
  • Although lovastatin (LS) is widely used in the treatment of hypercholesterolemia, its bioavailability is known to be around 5%. This study was aimed to increase the solubility and dissolution-permeation rates of LS using solid dispersions (SDs) with bile salts. The solubilities of LS in water, aqueous bile salt solutions and non-aqueous vehicles were determined, and effects of bile salts on the cellulose or duodenal permeation of LS from SDs were evaluated using a horizontal permeation system. SDs were prepared at various ratios of LS to carriers, such as sodium deoxycholate (SDC), sodium glycocholate (SGC) and/or 2-hydroxypropyl-$\beta$-cyclodextrin (HPCD). The addition of bile salts (25 mM) in water increased markedly the solubility of LS by the micellar solubilization. Some non-aqueous vehicles were effective in solubilizing LS. From differential scanning calorimetric studies, it was found that the crystallinity of LS in SDs disappeared, indicating a formation of amorphous state. The SDs showed markedly enhanced dissolution compared with those of their physical mixtures (PMs) and drug alone. In the dissolution-permeation studies using a cellulose membrane, the donor and receptor solutions were maintained as a sink condition using pH 7.0 phosphate buffer containing 0.05% sodium lauryl sulfate (SLS). The flux of LS alone was nearly same as that of LS-SDC-HPCD (1:3:6) PM. However, the flux of LS-SDC-HPCD (1:3:6) SD slightly increased compared with drug alone and PM, suggesting that entrapment of LS in micelles does not significantly hinder the permeation across cellulose membrane. In the dissolution-duodenal permeation studies using a LS-HPCD-SDC (1:3:6) SD, the addition of various bile salts in donor solutions (25 mM) enhanced the permeation of LS markedly, and the fluxes were found to be $0.69{\pm}0.41$, $0.87{\pm}0.51$, $0.84{\pm}0.46$, $0.47{\pm}0.17$ and $0.68{\pm}0.32{\mu}g/cm^2/hr$ for sodium cholate (SC), SDC, SGC, sodium taurodeoxycholate (STDC) and sodium taurocholate (STC), respectively. The stepwise increase of donor SGC concentration increased the flux dose-dependently. From the relationship of donor SGC concentration and flux, the concentration of SGC initiating the permeation across the duodenal mucosa was calculated to be 11.1 mM, which is nearly same as the critical micelle concentration (CMC, 11.6 mM) of SGC. However, with no addition of bile salts and below CMC, the permeation was very limited and irratic, indicating that LS itself is very poor permeable. Higher protions of bile salt in SD such as LS-SDC or LS-SGC (1 : 49 and 1 : 69) showed highly promoted fluxes. In conclusion, SD systems with bile salts, which may form their micelles in intestinal fluids, might be a promising means for providing enhanced dissolution and intestinal permeation of practically insoluble and non-absorbable LS.