• Biomedical Science Letters
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• v.11 no.4
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• pp.473-479
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• 2005

Possible mechanism of decreased catechol-O-methyltransferase (COMT) activity in cholestatic rat liver was studied. Hepatic and serum COMT activities were determined from the experimental rats with common bile duct ligation (CBDL). The Michaelis-Menten constants in this hepatic enzyme were also measured. The activities of cytosolic, mitochondrial and mircosomal COMT as well as their Vmax values were found to be decreased significantly in CBDL plus taurocholic acid (TCA) injected group than in the control group, such as CBDL alone groups. However, their Km values in the experimental groups did not vary. Serum COMT activity increased slightly in the CBDL plus TCA injected group than in the control group. The above results suggest that TCA represses biosynthesis of the COMT in the liver. The elevated activity of the serum COMT is believed to be caused by the increment of membrane permeability of hepatocytes upon TCA mediated liver cell necrosis.

• Biomedical Science Letters
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• v.11 no.4
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• pp.503-508
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• 2005

Possible mechanisms of increased serum aryl sulfotransferase (AST) isozyme activities in cholestatic rats were studied. Serum AST-I, II and -III, IV isozymes activities were determined from the experimental rats with common bile duct ligation (CBDL) or choledocho-caval shunt (CCS). The activities of serum AST-I, II and -III, IV isozymes were found to be increased significantly in both the CCS plus taurocholic acid (TCA) injected group, and the CBDL plus TCA group than those in each control group, such as CCS or CBDL alone groups. The above results suggest that the elevated serum AST most likely due to increased hepatocyte membrane permeability caused by TCA mediated liver cell necrosis.

• Biomedical Science Letters
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• v.11 no.1
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• pp.37-43
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• 2005

The possible mechanisms of increased aryl sulfotransferase (AST) isozymes activities in cholestatic rat liver were studied. Hepatic AST-I, II and -III, IV activities were determined from the experimental rats with common bile duct ligation (CBDL). The Michaelis-Menten constants in these hepatic enzymes were also measured. The activities of mitochondrial AST-I, II and -III, IV, and microsomal AST-III, IV as well as their Vmax values were found to be increased significantly in CBDL plus taurocholic acid (TCA) injected group than in the control group, such as CBDL alone groups. However, their Km values in the experimental groups did not vary. The results suggest that TCA stimulates biosynthesis of the AST in the liver.

• Biomedical Science Letters
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• v.10 no.4
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• pp.421-427
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• 2004

The possible mechanisms of decreased monoamine oxidase (MAO) A and B activities in cholestatic rat liver were studied. Hepatic and serum MAG activities were determined from the experimental rats with common bile duct ligation (CBDL). The Michaelis-Menten constants in these hepatic enzymes were also measured. The activities of mitochondrial MAO A and B, and mircosomal MAO B as well as their Vmax values were found to be decreased significantly in CBDL plus taurocholic acid (TCA) injected group than in the control group, such as CBDL alone groups. However, their Km values in the experimental groups did not vary. Serum MAO activity increased significantly in the CBDL plus TCA injected group than in the control group. The above results suggest that TCA represses biosynthesis of the MAO in the liver. The elevated activity of the serum MAO is believed to be caused by the increment of membrane permeability ofhepatocytes upon TCA mediated liver cell necrosis.

• Biomolecules & Therapeutics
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• v.4 no.3
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• pp.257-264
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• 1996

The protective effect of human urinary trypsin inhibitor (UTI) on acute pancreatitis was studied in beagle model. After pancreatitis was experimentally induced in beagle dogs by infusing trypsin and sodium taurocholate into the accessory pancreatic ducts under laprotomy, effects of UTI were compared to those of aprotinin. Routine physical examination, hematology and blood chemistry values were used as parameters and checked on a periodical basis during the experiment. At the end of experiment, surviving animals were sacrificed and liver, kidney, and pancreas were histologically examined. The results of this study warrant the development of UTI as new therapeutics for acute pancreatitis.

• 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 .

• Journal of the Korean Society of Food Science and Nutrition
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• v.41 no.1
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• pp.73-78
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• 2012

Excessive intake of trans fats is known to be a risk factor for cardiovascular diseases. Previously, we have shown that green tea extract (GTE) lowers the intestinal absorption of lipids and lipid-soluble compounds in rats. This study was conducted to investigate a possible role of GTE on the lymphatic absorption of elaidic acid, a major trans fat in the diet. Adult male Sprague-Dawley rats with lymph duct cannula were infused via an intraduodenal catheter at 3.0 mL/hr for 8 hr with a lipid emulsion containing $180.0{\mu}mol$ elaidic acid, $400.0{\mu}mol$ triolein, $20.7{\mu}mol$ cholesterol, $3.1{\mu}mol$ ${\alpha}$-tocopherol, and $396.0{\mu}mol$ sodium-taurocholate with or without (control) GTE in a 24 mL PBS buffer (pH, 6.4). Simultaneously, lymph was collected hourly for 8 hr via the lymph duct cannula. There was a significant difference in lymph flow by GTE. Also, the lymphatic absorption of elaidic acid for 8 hr was significantly lower in rats infused with GTE than in those not infused with GTE. Similarly, GTE infusion decreased the lymphatic outputs of cholesterol, oleic acid, and phospholipids, compared with the controls. These findings provide clear evidence that GTE has an inhibitory effect on the intestinal absorption of elaidic acid and other lipids. Our work here provides the foundation for further studies to examine and evaluate dietary strategies to ameliorate dietary trans fats from the diet.

• YAKHAK HOEJI
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• v.56 no.3
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• pp.164-172
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• 2012

This study was aimed to increase the solubility, dissolution and permeation rates of atorvastatin calcium (ATC) using bile salt and/or 2-hydroxypropyl-${\beta}$-cyclodextrin ($HP{\beta}CD$). From solubility studies, sodium deoxycholate (SDC) among bile salts studied was found to have the highest solubilizing effect on ATC ($4.4{\pm}0.4$ mg/ml), and the order of increasing solubility was SDC>sod. cholate>sod. glycocholate>sod. taurodeoxycholate>sod. taurocholate>conjugated bile acid. ATC solid dispersions were prepared at various ratios of drug to SDC and/or $HP{\beta}CD$, and evaluated by differential scanning calorimetry (DSC), dissolution studies and dissolution-permeation studies. DSC curves showed amorphous state of ATC in the physical mixture and solid dispersion. Dissolution rates of ATC-SDC solid dispersions and physical mixture were markedly increased at pH 6.8, but decreased at pH 1.2 with greater proportions of SDC due to the precipitation of SDC, compared with that of drug alone. On the other hand, dissolution rates of ATC-$HP{\beta}CD$ solid dispersion and physical mixture at pH 1.2 were varied with the ratio of drug to carriers. From duodenal permeation studies, it was found that fluxes of ATC (donor dose: 0.5 mg/3.5 ml) in the presence of 25 mM sodium glycocholate, SDC, sod. cholate and sod. taurocholate $(5.7{\pm}0.9$, $5.6{\pm}0.9$, $4.8{\pm}0.7$ and $4.6{\pm}0.9\;{\mu}g/cm^2/hr$, respectively) were enhanced, compared with drug alone ($3.4{\pm}0.9\;{\mu}g/cm^2/hr$). In the dissolution-permeation studies, 1 : 9 : 10 (w/w) ATC-SDC-$HP{\beta}CD$ solid dispersion increased the flux 2.2 times, compared with 1 : 5 : 4 (w/w) ATC-lactose-corn starch mixture as control. In conclusion, solid dispersions with bile salt and $HP{\beta}CD$ were found to be an effective means for increasing the dissolution and permeation rates of ATC.

• Journal of Pharmaceutical Investigation
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• v.33 no.3
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• pp.187-193
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• 2003

This study was aimed to formulate various phospholipid nanoparticles composed of different surfactants and to evaluate the deformability of the phospholipid vesicles as candidates of useful ultradeformable nanoparticles. In vitro deformability of the phospholipid nanoparticles was studied using an extruder under a certain pressure. The sizes of phospholipid nanoparticles, passed volumes, and concentrations of the phospholipids in suspensions before and after extrusion were measured. The deformability indexes were estimated by using passed volumes, sizes of phospholipid nanoparticles and concentrations of phospholipids. Conventional liposomes, placed under a certain pressure of an extruder, showed no passed volume indicating little deformability. Similar to conventional liposomes, phospholipid nanoparticles containing surfactants such as sodium taurocholate, Myrj 45, or Myrj 53 showed little deformability. In contrast, phospholipid nanoparticles composed of Tween 20, Triton X-100, or sodium deoxycholate showed higher deformability indexes than others. Taken together, the deformability of phospholpid nanoparticles could be significantly affected by the type of surfactants. Moreover, these results suggest that the deformability of phospholipid nanoparticles could be modulated by surfactants.

• 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.