• Biomolecules & Therapeutics
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• v.18 no.1
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• pp.65-70
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• 2010

The blood-brain barrier (BBB) transport of acetylcholinesterase (AChE) inhibitors, donepezil and tacrine suggested to be mediated by choline transport system in our previous study. Therefore, in the present study, we investigated the interaction of other AChE inhibitors, rivastigmine and galantamine with choline transporter at the BBB. The effects of rivastigmine and galantamine on the transport of choline by conditionally immortalized rat brain capillary endothelial cell lines (TR-BBB cells) were characterized by cellular uptake study using radiolabeled choline. The uptake of [$^3H$]choline was inhibited by rivastigmine and galantamine, with $IC_{50}$ values (i.e. concentration necessary for 50% inhibition) for 1.13 and 1.15 mM, respectively. Rivastigmine inhibited the uptake of [$^3H$]choline competitively with $K_i$ of 1.01 mM, but galantamine inhibited noncompetitively. In addition, the efflux of [$^3H$]choline was significantly inhibited by rivastigmine and galantamine. Our results indicated that the BBB choline transporter may be involved in a part of the influx and efflux transport of rivastigmine across the BBB. These findings should be therapeutically relevant to the treatment of Alzheimer's disease (AD) with AChE inhibitors, and, more generally, to the BBB transport of CNS-acting cationic drugs via choline transporter.

• Proceedings of the Korean Society of Soil and Groundwater Environment Conference
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• 2002.09a
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• pp.283-286
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• 2002

Solubilization and partitioning of naphthalene was investigated in an aqueous system containing soils and surfactants. The environmental behavior of polycyclic aromatic hydrocarbons(PAHs) was mainly governed by their solubility and partitioning properties on soil media in a subsurface system. In surfactant-enhanced remediation systems, surfactants might be an additional variable. a natural soil ,silica and kaolinite were tested as soil media. two nonionic surfactants, Triton X-100 and Hydropropy1-$\beta$-cyclodextrin (HPCD) were employed for naphthalene solubilization. Naphthalene showed linear on natural soil while non-linear sorption on silica and kaolinite. Soils have higher sorption capacity for Triton X-100 than HPCD indicating Triton X-100 formed ad-micelle on the soil surface. Desorption study showed a hysterysis and reversible desorption. The partitioning coefficient(K$_{D}$) of naphthalene was increased as the concentration of surfactant was increased. (below CMC), however, the coefficient was decreased above CMC. This indicates that naphthalene is partitioned into the micelles and the partition occurs competitively on both ad-micelle and free micelles as surfactant concentration increases. Therefore, the target compounds to be dissolved into aqueous phase in a surfactant enhanced remediation system might be highly partitioned on to the ad-micelle resulting in an adverse effect rather increased solubilization would be achieved.d.

• BMB Reports
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• v.43 no.9
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• pp.622-628
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• 2010

Dimethyl sulfoxide (DMSO) can be reduced to dimethyl sulfide by MsrA, which stereospecifically catalyzes the reduction of methionine-S-sulfoxide to methionine. Our previous study showed that DMSO can competitively inhibit methionine sulfoxide reduction ability of yeast and mammalian MsrA in both in vitro and in vivo, and also act as a non-competitive inhibitor for mammalian MsrB2, specific for the reduction of methionine-R-sulfoxide, with lower inhibition effects. The present study investigated the effects of DMSO on the physiological antioxidant functions of methionine sulfoxide reductases. DMSO elevated hydrogen peroxide-mediated Saccharomyces cerevisiae cell death, whereas it protected human SK-Hep1 cells against oxidative stress. DMSO reduced the protein-carbonyl content in yeast cells in normal conditions, but markedly increased protein-carbonyl accumulation under oxidative stress. Using Msr deletion mutant yeast cells, we demonstrated the DMSO's selective inhibition of the antioxidant function of MsrA in S. cerevisiae, resulting in an increase in oxidative stress-induced cytotoxicity.

• Journal of Power Electronics
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• v.16 no.5
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• pp.1629-1638
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• 2016

Differential power processing (DPP) systems are among the most effective architectures for photovoltaic (PV) power systems because they are highly efficient as a result of their distributed local maximum power point tracking ability, which allows the fractional processing of the total generated power. However, DPP systems require a high-efficiency, high step-up/down bidirectional converter with broad operating ranges and galvanic isolation. This study proposes a single, magnetic, high-efficiency, high step-up/down bidirectional DC-DC converter. The proposed converter is composed of a bidirectional flyback and a bidirectional isolated switched-capacitor cell, which are competitively cheap. The output terminals of the flyback converter and switched-capacitor cell are connected in series to obtain the voltage step-up. In the reverse power flow, the converter reciprocally operates with high efficiency across a broad operating range because it uses hard switching instead of soft switching. The proposed topology achieves a genuine on-off interleaved energy transfer at the transformer core and windings, thus providing an excellent utilization ratio. The dynamic characteristics of the converter are analyzed for the controller design. Finally, a 240 W hardware prototype is constructed to demonstrate the operation of the bidirectional converter under a current feedback control loop. To improve the efficiency of a PV system, the maximum power point tracking method is applied to the proposed converter.

• Microbiology and Biotechnology Letters
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• v.24 no.2
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• pp.197-205
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• 1996

The $\beta$-xylosidase was purified 99- fold from the culture supernatant of Pseudo onas sp. CB-33 by ammonium sulfate precipitation, PEI precipita- tion, DEAE-Sephadex column chromatography, Sephadex G-75 gel filtration chromatography and preparative disc gel electrophoresis. Molecular weight of the enzyme was estimated to be 44,000 by SDS polyacrylamide gel electrophoresis. The enzyme has a pH optimum for activity at 7.0 and is stable over pH 6.5-9.0. The optimal temperature of the enzyme was 45$\circ$C, and its enzymatic activity was completely inactivated at 55$\circ$C for 30 min. Km value of the enzyme for p-nitrophenyl-$\beta$-D-xylopyranoside was calculated to be 4.6 mM. The effect of various reagents on the $\beta$-xylosidase activity was investigated. The enzyme activity was completely inhibited by Hg$^{2+}$, Cu$^{2+}$ and Zn$^{2+}$. The $\beta$-xylosidase was inactivated by tryptophan-specific reagent, N-bromosuccinimide and tyrosine-specific reagent, iodine. The enzyme could degrade xylo-oligosaccharides to xylose and the enzyme was competitively inhibited by xylose. The $\beta$-xylosidase and endoxylanase from Psedomonas sp. CB-33 hydrolized xylan synergically. The purified enzyme also showed $\alpha$-L-arabinofuranosidase activity.

• Proceedings of the Korean Society of Soil and Groundwater Environment Conference
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• 2000.11a
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• pp.182-195
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• 2000

Indigenous bacteria from poplar roots (Populus mnadensis var. eugenei, 'Imperial Carolina') and Southern Californian shrub rhizospheres as well as two tree-colonizing Rhizobium strains (ATCC 10320 and 35645) were genetically engineered to express constitutively and stably toluene o-monooxygenase (TOM) from Burkholderia cepacia G4 by integrating the torn locus into the chromosome. The poplar and Rhizobium recombinants degraded trichloroethylene (TCE) at 0.8-2.1 nmol/min.mg protein (initial TCE concentration, 10u M) and competitive against the unengineered hosts in wheat and barley rhizospheres for one month (colonization at 1-23 $\times$ 10$^{5}$ CFU/cm root). In addition, six of these recombinants colonized poplar roots stably and competitively with populations as high as 79 $\pm$ 12% of all rhizosphere bacteria after 28 days (0.2-31 $\times$ 10$^{5}$ CFU/cm root). Furthermore, five of the most-competitive poplar recombinants (e.g., Pb3-1 and Pb5-1 which were identified as Pseudomonas PsK) retained the ability to express TOM for 29 days as 100 $\pm$ 0% of the recombinants detected in the poplar rhizosphere had constitutive expression of TOM.

• Biomolecules & Therapeutics
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• v.3 no.3
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• pp.192-198
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• 1995

The affinity of mequitazine, a non-sedating antihistamine, for muscarinic receptors was evaluated in the guinea-pig ventricle and ileum by in vitro binding techniques and functional studies. In binding studies, [$^3$H]quinuclidinyl benzilate (QNB) identified a single class of muscarinic receptors with similar apparent $K_{D}$ value of about 100 pM in two tissues. Mequitazine inhibited [$^3$H]QNB binding to muscarinic receptors competitively. Analysis of the mequitazine inhibition curve of [$^3$H]QNB binding to ventricular microsome and ileal homogenate indicated the presence of a single homogeneous binding site with Ki value of 25 nM and 18 nM, respectively. In functional studies, mequitazine caused parallel rightward shifts of concentration-response curves for carbachol and histamine in the isolated guinea-pig ileum. The slope values obtained from Schild plot analysis for the antagonistic action of mequitazine on muscarinic and histamine $H_1$-receptors were not significantly different from unity. The p $A_2$values of mequitazine for muscarinic and histamine $H_1$-receptors were about 7.6 ( $K_{M}$= 25.1 nM) and 8.88 ( $K_{H}$= 1.32 nM), respectively. These results indicate that the muscarinic receptor blocking action of mequitazine is 15 times less potent than the $H_1$receptor blocking action, but high concentration of this drug may cause the peripheral muscarinic receptor blocking effect.t.t.t.

• Journal of Life Science
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• v.16 no.5
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• pp.866-869
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• 2006

The inhibitory effect of pine needle (Pinus densiflora S.) on potato polyphenol oxidase (PPO) was investigated. The addition of the pine needle extract exhibited a higher inhibitory effect on the potato polyphenol oxidase activity than that of the citric acid or potassium sorbate. The enzyme activity was strongly inhibited in a pH range of 7.0-8.0. When the incubation time of reaction mixture was increased, the potato polyphenol oxidase activity was markedly inhibited. The pine needle extract inhibited the potato polyphenol oxidase non-competitively. And also the pine needle extract subjected to a heat treatment at $100^{\circ}C$ for 10 min or to an acid treatment at pH 2.0, 3.0, and 4.0 for 3 hours still retained inhibitory effect on potato polyphenol oxidase.

• Natural Product Sciences
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• v.17 no.2
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• pp.113-116
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• 2011

Arginase competitively inhibits nitric oxide synthase (NOS) via use of the common substrate L-arginine. Arginase II has recently reported as a novel therapeutic target for the treatment of cardiovascular diseases such as atherosclerosis. In our experiment, the EtOH extracts of four-hundreds extracts drugs were investigated for the arginase inhibitory activity. Among them, four extracts exhibited over 50% inhibition of arginase II activity compared to control at a concentration of 150${\mu}g/ml$. In particular, the seed of Arctium lappa, gum-resin of Boswellia carterii, aerial part of Artemisia apiacea and rhizome of Cyperus rotundus inhibited arginase II activity, with $IC_{50}$ values of 118.4, 135.4, 123.9 and 86.7${\mu}g/ml$, respectively. In addition, four plant extracts showed less than 20% inhibition of arginase I activity at 150${\mu}g/ml$. These plants might be the potential candidate materials in the development of the novel atherosclerosis drug.

• Korean Journal of Veterinary Research
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• v.27 no.1
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• pp.35-40
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• 1987

Higenamine, a benzyltetrahydroisopuinoline analog isolated from aconite tuber, has potent isotropic action. Recent studies suggest it may have beta receptor agonistic property in that its inotropic action is blocked by propranolol in isolated rabbit heart. However, no study has been carried out on other organs than heart. Higenamine is expected to have pharmacological actions on smooth muscle on the ground that it has catecholamine moiety and tetrahydrosioquinoline nucleus in its chemical structure, both of which are well known to have smooth muscle relaxation effects. Therefore present study was aimed at determining whether higenamine has bronchodilating effect in isolated guinea pig trachea smooth muscle rich in adrenergic beta receptor and if any, it has agonistic effect on beta receptor. The results were summarized as follows : 1. Higenamine had remarkable bronchodilating effect in guinea pig tracheal smooth muscle in a dose-dependent manner. 2. Bronchodilator effect of higenamine in isolated guinea pig tracheal smooth muscle was blocked competitively by propranolol. The $pD_2$ value of higenamine in isolated guinea pig tracheal smooth muscle was 5.65 and the $pA_2$ value of propranolol against higenamine in the same preparation was 7.97.