• Biomolecules & Therapeutics
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• v.19 no.2
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• pp.237-242
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• 2011

This study was designed to investigate the effects of glipizide on the pharmacokinetics of carvedilol after oral or intravenous administration of carvedilol in rats. Clinically carvedilol and glipizide can be prescribed for treatment of cardiovascular diseases as the complications of diabetes, and then, Carvedilol and glipizide are all substrates of CYP2C9 enzymes. Carvedilol was administered orally or intravenously without or with oral administration of glipizide to rats. The effects of glipizide on cytochrome P450(CYP) 2C9 activity and P-gp activity were also evaluated. Glipizide inhibited CYP2C9 activity in a concentration-dependent manner with 50% inhibition concentration ($IC_{50}$) of 18 ${\mu}M$. Compared with the control group, the area under the plasma concentration-time curve (AUC) was significantly increased by 33.0%, and the peak concentration ($C_{max}$) was significantly increased by 50.0% in the presence of glipizide after oral administration of carvedilol. Consequently, the relative bioavailability (R.B.) of carvedilol was increased by 1.13- to 1.33-fold and the absolute bioavailability (A.B.) of carvedilol in the presence of glipizide was increased by 36.8%. After intravenous administration, compared to the control, glipizide could not significantly change the pharmacokinetic parameters of carvedilol. Therefore, the enhanced oral bioavailability of carvedilol may mainly result from inhibition of CYP2C9-mediated metabolism rather than both P-gp-mediated effl ux in the intestinal or in the liver and renal elimination of carvedilol by glipizide.

• Korean Journal of Veterinary Research
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• v.34 no.4
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• pp.867-872
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• 1994

Progesterone catabolizing enzyme, the enzyme $20{\alpha}$-hydroxysteroid dehydrgenase($20{\alpha}$-HSD) is pivotal in the regulation of ovarian function in rodents, which catabolizes progesterone into biologically inactive $20{\alpha}$-hydroxypregn-4-en-3-one($20{\alpha}$-OHP). In this study was carried out the influence of $20{\alpha}$-HSD activity of ovarian function, we investigated changes in ovarian cytosol $20{\alpha}$-HSD activity and serume progesterone concentration during the estrous cycles and pregnancy in rat. During the estrous cycles, the $20{\alpha}$-HSD activities were highest on the progestrous, but serum progesterone concentration was lowest on this phase. During the pregnancy, the $20{\alpha}$-HSD activities were relatively higher early pregnancy(day-1-3 gestation) and late pregnancy(day 21 to parturition), serum progesterone concentration was maintained significantly high to day 19 of gestation. The $20{\alpha}$-HSD activities were lower during the middle pregnancy. From these results, ovarian $20{\alpha}$-HSD activities may possibly act as physiologically very important in the control and maintenance of estrous cycles in rat.

• Journal of Pharmaceutical Investigation
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• v.31 no.1
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• pp.1-5
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• 2001

The aggregation behavior of nystatin (NYS) in the presence of pluronic F127, triblock copolymer of poly (ethylene oxide) (PEO) and poly (propylene oxide) (PPO), was measured and correlated with hemolytic activity. Antifungal activity was also studied using Saccharomyces cerevisiae as a model strain. The critical aggregation concentrations (CAC) of the drug were 50.1, 108.0, 134.2, 154.3, and $217.9\;{\mu}M$ at 0.1%, 0.5%, 1.0%, 1.5%, and 2.0% pluronic F127 solution, respectively. The levels of NYS required to start lysis of erythrocytes were about 80, 100, 125, 150, and $200\;{\mu}M$ at 0.1%, 0.5%, 1.0%, 1.5%, and 2.0% pluronic F127 solution, respectively. It was $50\;{\mu}M$ in the absence of the polymer. Minimal inhibitory concentration (MIC) and minimal fungicidal concentration (MFC) of NYS-pluronic F127 lyophilizate were same at $3\;{\mu}g/ml$, while MIC and MFC of pure NYS are $3\;{\mu}g/ml$ and $12\;{\mu}g/ml$, respectively. By modulating the aggregation behavior of NYS, pluronic F127 was able to reduce the toxicity of the drug without compromising the MIC and MFC.

• Korean Journal of Community Nutrition
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• v.15 no.5
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• pp.670-678
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• 2010

Recognition thresholds for NaCl, sucrose, citric acid, and caffeine, as well as the pleasant concentration of NaCl were assessed in 176 males and 312 females aged 50-88 years. Furthermore, relationships among taste sensitivities, taste preferences, and lifestyles were examined. The taste solutions were presented one after the other in ascending order using the sip-and-spit method. For the recognition thresholds of the 4 basic tastes, women perceived significantly lower concentrations than the men. However, the pleasant concentration of NaCl did not show a gender difference. Sensitivities for the 4 basic tastes did not decrease with age in the men, but they did significantly decrease with age for the women, especially for those above 70 years. For men, regular exercise was positively correlated with sensitivities for sour taste and bitter taste, and physical activity was negatively correlated with the pleasant concentrations of NaCl. For women, who had more physical activity, sensitivities for sweet taste and sour taste were lower compared to the others. This study indicates that the sensitivities for 4 basic tastes in water diminished with age, but pleasant salt concentration did not change with age. Further research on pleasant NaCl concentration is required to determine factors affecting salt preference, in order to decrease salt intake in the elderly.

• Environmental Analysis Health and Toxicology
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• v.10 no.1_2
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• pp.47-54
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• 1995

To investigate and evaluated the scavenging and antioxidative effects of various flavonoids on paraquat induced toxicity, in vivo and vitro tests of eight flavonoids (catechin, epocatechin, flavone, chrysin, apigenin, quercetin, morin and biochanin A) were carried out. The generation of reactive oxygen substances(ROS) in PMS-NADH system $H_2O_2$ induced hemolysis and lipidperoxidation to blood, NADPH dependent lipidperoxidation to liver and lung microsome by paraquat were studied.The results are summerized as follows; 1) In the concentration ranges from 3.3 to 9.8$\mu$M of catechin,epicatechin, quercetin and biochanin A removed the 50% of DPPH radical scavenging effects. 2) In the concentration ranges from 0.60 to 1.86 mM of catechin, epicatechin, quercetin and biochanin A showed the inhibitory and antioxidative activity on superoxide anion which gernerated in PMA-NADH system. 3) In the concentration ranges from 0.12 to 0.49mM of catechin, epicatechin, quercetin and biochanin A showed the inhibitory and antioxidative activity on H202 which generated in PMA-NADH system. 4) In the concentration ranges from 0.6 x10$^{-5}$ to 6.3 x 10$^{-5}$mM of catechin, epicatechin, flavone, chrysin, quercetin and morin showed the inhibitory and antioxidative activity on $H_2O_2$ induced hemolysis to blood 5) All flavonoids tested exhibited inhibitory and antioxidative effects on paraquat induced liver and tung microsomal lipidperoxidation. Therefore, all flavonoids evaluated showed the useful compounds for scavenger and antioxidant on paraquat induced toxicity.

• Journal of Microbiology and Biotechnology
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• v.19 no.6
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• pp.582-587
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• 2009

Immobilized cells of Arthrohacter nitroguajacolicus ZJUTB06-99 capable of producing nitrilase were used for biotransformation of acrylonitrile to acrylic acid. Six different entrapment matrixes were chosen to search for a suitable support in terms of nitrilase activity. Ca-alginate proved to be more advantageous over other counterparts in improvement of the biocatalyst activity and bead mechanical strength. The effects of sodium alginate concentration, $CaCl_2$ concentration, bead diameter, and ratio by weight of cells to alginate, on biosynthesis of acrylic acid by immobilized cells were investigated. Maximum activity was obtained under the conditions of 1.5% sodium alginate concentration, 3.0% $CaCl_2$ concentration, and 2-mm bead size. The beads coated with 0.10% polyethylenimine (PEI) and 0.75% glutaraldehyde (GA) could tolerate more phosphate and decrease leakage amounts of cells from the gel. The beads treated with PEI/GA could be reused up to 20 batches without obvious decrease in activities, which increased about 100% compared with the untreated beads with a longevity of 11 batches.

• Journal of Nuclear Fuel Cycle and Waste Technology(JNFCWT)
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• v.19 no.3
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• pp.367-386
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• 2021

The overestimation and underestimation of the radioactivity concentration of difficult-to-measure radionuclides can occur during the implementation of the scaling factor (SF) method because of the uncertainties associated with sampling, radiochemical analysis, and application of SFs. Strict regulations ensure that the SF method as an indirect method does not underestimate the radioactivity of nuclear wastes; however, there are no clear regulatory guidelines regarding the overestimation. This has been leading to the misuse of the SF methodology by stakeholders such as waste disposal licensees and regulatory bodies. Previous studies have reported instances of overestimation in statistical implementation of the SF methodology. The analysis of the two most popular linear models of the SF methodology showed that severe overestimation may occur and radioactivity concentration data must be dealt with care. Since one major source of overestimation is the use of minimum detectable activity (MDA) values as true activity values, a comparative study of instrumental techniques that could reduce the MDAs was also conducted. Thermal ionization mass spectrometry was recommended as a suitable candidate for the trace level analysis of long-lived beta-emitters such as iodine-129. Additionally, the current status of the United States and Korea was reviewed from the perspective of overestimation.

• The Korean Journal of Ecology
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• v.19 no.5
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• pp.385-392
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• 1996

Changes in polyamine titers and enzyme activities during radicle growth of Glycine max were studied in order to investigate the effect of ferulic acid in regulation of polyamine biosynthesis. Among eight compounds used, gallic acid stimulated the radicle growth and ferulic acid inhibited it significantly. During the radicle growth of Glycine max, the content of putrescine was shown the highest level at the second day, while at the fourth day spermidine was the highest and spermine followed. Ornithine decarboxylass (ODC, EC 4.1.1.17) seems to be responsible for biosynthesis of putrescine. As the concentration of ferulic acid (0.001, 0.01, 0.1 mM) treated increased, the content of spermine was gradually enhanced and putrescine was increased at 0.001~0.01 mM, decreased after 0.1 mM concentration but spermidine was not affected. Ferulic acid elevated ODC and S-adenosylmethionine decarboxylass (SAMDC, EC 4.1.1.50) activity. ODC activity was increased more than 120% and SAMDC activity was increased about 50% more than that of the control. Diamine oxidase (DAO EC, 1.4.3.6) activity was enhanced about 20% at low concentration, decreased after then.

• Journal of Pharmacopuncture
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• v.2 no.1 s.2
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• pp.13-25
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• 1999

This study was undertaken to determine whether Juglandis Semen (JAS) extraction exerts protective effect against oxidant-induced inhibition of $Na^+$-pump activity in cerebral cortex. $Na^+$-pump activity was estimated by measuring ouabain-sensitive oxygen consumption. The oxygen consumption significantly inhibited by 1 mM t-butylhydroperoxide (tBHP), which was prevented by addition of 2% JAS extraction. The oxygen consumption was increased by an increase in $Na^+$ concentration from 5 to 100mM, $K^+$ concentration from 0.5 to 10 mM, and $Mg^{++}$ concentration from 0.2 to 5 mM. These changes in ion concentrations did not affect the inhibitory effct of tBHP and protective action of JAS on oxygen consumption. tBHP(1mM) produced a significant increase in lipid peroxidation in cerebral cortex, which was prevented by 2% JAS extraction. These result suggest that JAS exerts protective effect against tBHP-induced inhibition of $Na^+$-pump activity in the cerebral cortex, this effect may be due to by an antioxidant action.

• Biomolecules & Therapeutics
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• v.11 no.2
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• pp.139-144
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• 2003

Ganoderma lucidum is commonly known as medically potent mushroom, which has been widely used in China and other oriental countries for the treatment of various diseases, including cancer. In this report, we investigated the anti-oxidant and protective effect of Ganodema lucidum extract (GLE) against the DNA damage induced by free radical and U.V. In the assay of cell growth inhibition, the inhibitory cell growth rate induced by hydroxyl radical was dose-dependently decreased by GLE. This results support that GLE has a detoxifying activity against cytotoxicity of hydroxyl radical in E. coli cell. GLE also protected ColE1 plasmid DNA damage in the concentration of 200$\mu\textrm{g}$ per reaction on the DNA fragmentation assay. The nuclear tailing by hydrogen peroxide in single cell gel electrophoresis(SCGE) was decreased by GLE in the concentration of 50$\mu\textrm{g}$/ml. These data indicate that Ganoderma lucidum has an anti-oxidative activity to hydrogen peroxide. The mutation rate after irradiation of U.V. was reduced by 50$\mu\textrm{g}$/ml GLE and total number of Rif (Rifampicin) resistant mutants was decreased in a concentration dependent manner when added the GLE exogenously in a culture media. According to the results, it is likely that GLE has not only an anti-oxidative activity to hydroxyl radical but also an anti-mutagenic activity to U.V. mutagenesis.