• The Korean Journal of Physiology and Pharmacology
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• v.20 no.2
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• pp.193-200
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• 2016

Sertraline, a selective serotonin reuptake inhibitor (SSRI), has been reported to lead to cardiac toxicity even at therapeutic doses including sudden cardiac death and ventricular arrhythmia. And in a SSRI-independent manner, sertraline has been known to inhibit various voltage-dependent channels, which play an important role in regulation of cardiovascular system. In the present study, we investigated the action of sertraline on Kv1.5, which is one of cardiac ion channels. The effect of sertraline on the cloned neuronal rat Kv1.5 channels stably expressed in Chinese hamster ovary cells was investigated using the whole-cell patch-clamp technique. Sertraline reduced Kv1.5 whole-cell currents in a reversible concentration-dependent manner, with an $IC_{50}$ value and a Hill coefficient of $0.71{\mu}M$ and 1.29, respectively. Sertraline accelerated the decay rate of inactivation of Kv1.5 currents without modifying the kinetics of current activation. The inhibition increased steeply between -20 and 0 mV, which corresponded with the voltage range for channel opening. In the voltage range positive to +10 mV, inhibition displayed a weak voltage dependence, consistent with an electrical distance ${\delta}$ of 0.16. Sertraline slowed the deactivation time course, resulting in a tail crossover phenomenon when the tail currents, recorded in the presence and absence of sertraline, were superimposed. Inhibition of Kv1.5 by sertraline was use-dependent. The present results suggest that sertraline acts on Kv1.5 currents as an open-channel blocker.

• Journal of Environmental Science International
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• v.24 no.11
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• pp.1393-1404
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• 2015

Ten empirical disinfection models for the plasma process were used to find an optimum model. The variation of model parameters in each model according to the operating conditions (first voltage, second voltage, air flow rate, pH, incubation water concentration) were investigated in order to explain the disinfection model. In this experiment, the DBD (dielectric barrier discharge) plasma reactor was used to inactivate Phytophthora capsici which cause wilt in tomato plantation. Optimum disinfection models were chosen among ten models by the application of statistical SSE (sum of squared error), RMSE (root mean sum of squared error), $r^2$ values on the experimental data using the GInaFiT software in Microsoft Excel. The optimum models were shown as Log-linear+Tail model, Double Weibull model and Biphasic model. Three models were applied to the experimental data according to the variation of the operating conditions. In Log-linear+Tail model, $Log_{10}(N_o)$, $Log_{10}(N_{res})$ and $k_{max}$ values were examined. In Double Weibull model, $Log_{10}(N_o)$, $Log_{10}(N_{res})$, ${\alpha}$, ${\delta}_1$, ${\delta}_2$, p values were calculated and examined. In Biphasic model, $Log_{10}(N_o)$, f, $k_{max1}$ and $k_{max2}$ values were used. The appropriate model parameters for the calculation of optimum operating conditions were $k_{max}$, ${\alpha}$, $k_{max1}$ at each model, respectively.

• Microbiology and Biotechnology Letters
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• v.16 no.6
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• pp.484-488
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• 1988

Two forms of extracellular endo-inulinase, designated as PIand P II were resolved from a species of Pseudomonas isolated from soil. Both enzymes were glycoproteins with their carbohydrate content of 15% for PIand 2.4% for P II inulinase. Tryptophan residue was proved to be an essential amino acid for their catalytic activity. The molecular weights of PIand P II were estimated to be 210, 000 and 170, 000, respectively. The activity of the two enzymes was strongly inhibited by p-chloromercuribenzoate but the inhibition was nearly completely offset by the addition of the reducing agents such as cysteine or dithiothreitol. On the other hand, the two enzymes were activated about 50-60% of their activities by the presence of Co$^{+2}$ ion, and quite stable at pH values ranging from pH 4.0 to 1.5. They also appeared to be relatively thermostable, and no appreciable inactivation was observed after incubation at 55$^{\circ}C$ for 2 hours. About 70 % hydrolysis rate with PIand 56 % with P II were achieved when inulin was hydrolyzed at 5$0^{\circ}C$ for 12 hours with 60 units of the enzymes in 2 % inulin solution.

• Journal of Microbiology and Biotechnology
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• v.23 no.6
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• pp.771-778
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• 2013

Essential oils are increasingly of interest for use as novel drugs acting as antimicrobial and antiviral agents. In the present study, we report the in vitro antiviral activities of 29 essential oils, extracted from Chinese indigenous aromatic plants, against the tobacco mosaic virus (TMV). Of these essential oils, those oils from ginger, lemon, tea tree, tangerine peel, artemisia, and lemongrass effected a more than 50% inhibition of TMV at 100 ${\mu}g/ml$. In addition, the mode of antiviral action of the active essential oils was also determined. Essential oils isolated from artemisia and lemongrass possessed potent inactivation and curative effects in vivo and had a directly passivating effect on TMV infection in a dose-dependent manner. However, all other active essential oils exhibited a moderate protective effect in vivo. The chemical constitutions of the essential oils from ginger, lemon, tea tree, tangerine peel, artemisia, and lemongrass were identified by gas chromatography and gas chromatography-mass spectrometry. The major components of these essential oils were ${\alpha}$-zingiberene (35.21%), limonene (76.25%), terpinen-4-ol (41.20%), limonene (80.95%), 1,8-cineole (27.45%), and terpinolene (10.67%). The curative effects of 10 individual compounds from the active essential oils on TMV infection were also examined in vivo. The compounds from citronellal, limonene, 1,8-cineole, and ${\alpha}$-zingiberene effected a more than 40% inhibition rate for TMV infection, and the other compounds demonstrated moderate activities at 320 ${\mu}g/ml$ in vivo. There results indicate that the essential oils isolated from artemisia and lemongrass, and the individual compound citronellal, have the potential to be used as an effective alternative for the treatment of tobacco plants infected with TMV under greenhouse conditions.

• Journal of Microbiology and Biotechnology
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• v.9 no.3
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• pp.235-242
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• 1999

We investigated the growth-inhibitory mechanism of Helicobacter pylori by omeprazole (OMP) and its activated sulfenamide (OAS). Using dithiothreitol (DTT) and 5,5'-dithio-bis[2-nitrobenzoic acid] (DTNB; Ellman's reagent), we first determined the relationship between the binding capacity of these compounds to H. pylori membrane and its significance to membrane P-type ATPase activity. After incubation of the intact H. pylori cells with either OMP or OAS, the residual quantity of free SH-groups on the cell membrane was measured, and, the resulting values were plotted as a function of time. From this experiment, we found that there was a considerable difference in the membrane-binding rates between OMP and OAS. At neutral pH, the disulfide bond formation on H. pylori membrane was completed within 2 min of incubation of the intact cells with OAS. By OMP, however, it was gradually formed, exceeding 10 min of incubation for completion, whereby, the extent of P-type ATPase inhibition appeared to be proportional to the disulfide forming rate. From this data, it was suggested that the disulfide formation might directly affect enzyme activity. Since OMP per se cannot yield a disulfide bond with cysteine, it is predicted that the enzyme inactivation must be caused by the OAS form. Accordingly, we postulated that, under the neutral pH, OMP could be converted to OAS in the course of transport. By extrapolating the inhibitory slopes, we could evaluate K₁ values, relating to their minimal inhibitory concentrations (MICs) for H. pylori growth. In these MIC ranges, H. pylori uptake or vesicular export of nutrients such as peptides were totally prohibited, but their effect in Escherichia coli were negligible. From these observations, we strongly suggest that the P-type ATPase activity is essential for the survival of H. pylori cells in particular.

• Food Science and Biotechnology
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• v.18 no.5
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• pp.1132-1137
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• 2009

Successive application of Saccharomyces cerevisiae DSM 70424 and Saccharomyces rouxii DSM 2535 or DSM 2531 in the production of non-alcoholic beer was investigated. The aim of the study was to consider the impact of the 2 mentioned strains of S. rouxii on the reduction of alcohol content in wort fermented at 12 or $24^{\circ}C$ for 96 hr, applying periodic aeration. The 2 S. rouxii strains were added at the $48^{th}$ hr of fermentation after thermal inactivation of S. cerevisiae cells. The greatest alcohol decrease rate was observed for the treatment containing S. rouxii DSM 2535-fermented at $24^{\circ}C$ (from 1.56 to 0.36%). The concentration of acetaldehyde, diacetyl, and 2,3-pentandione, that have a key role in appearance of 'wort' and 'buttery' off flavors, were significantly lower in S. rouxii-containing treatments fermented at $24^{\circ}C$. S. rouxii-containing treatment fermented at $24^{\circ}C$ showed slightly lower overall flavor acceptability compared to S. cerevisiae-containing treatment fermented at the same temperature. Such score was improved for the products obtained at $12^{\circ}C$.

• Journal of Life Science
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• v.11 no.2
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• pp.103-107
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• 2001

The equine chorionic gonadotropin (eCG) subunits $\alpha$ and ${\beta}$ are transcribed from different genes and associate noncovalently to form the bioactive eCG heterodimer. Dimerization is rate limiting for eCG secretion, and dissociation leads to hormone inactivation. The correct conformation of the heterodimer is alto important for efficient secretion, hormone-specific post-translational modifications, receptor binding and signal transduction. To determine whether ${\alpha}$ and ${\beta}$ subunits can be synthesized as a single polypeptide chain (tethered-eCG) and also display biological activity, the tethered-eCG molecule by fusing the carboxyl terminus of the eCG ${\beta}$-subunit to the amino terminus of the af-subunit was construe-ted and transfected into chinese hamster ovary (CHO-Kl) cells. LH- and FSH-like activities were assayed in terms of testosterone production and aromatase activity in primary cultured rat Leydig cells and granulosa cells, respectively. The tethered-eCG was efficiently secreted and showed similar LH-like activity to the dimeric eCG ${\alpha}$/${\beta}$ and native eCG. FSH-like activity of the tethered-eCG was also shown similarly in comparison with the native and wild type eCG ${\alpha}$/${\beta}$. Our data for the first time suggest that the tethered-eCG can be expressed efficiently and the produced product by the CHO-K1 cells is fully LH- and FSH-like activities in rat in vitro bioassay system. Our results also suggest that this molecular can imply particular models of FSH-like activity not LH-like activity in the eCG. Taken together, these data indicate that the constructs of tethered molecule will be useful in the study of mutants that affect subunit association and/or secretion.

• Journal of the Korean Association of Oral and Maxillofacial Surgeons
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• v.38 no.2
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• pp.101-109
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• 2012

Objectives: The inactivation of the tumor suppressor gene $p16^{INK4a}$ plays an important role in the development of malignant tumors, including oral squamous cell carcinoma. The p16 gene is involved in the p16/cyclin-dependent kinase/retinoblastoma (Rb) gene pathway of cell cycle control. The p16 protein is considered a negative regulator of this pathway. The p16 gene encodes an inhibitor of cyclin-dependent kinases 4 and 6 which regulate the phosphorylation of the retinoblastoma gene and G1 to S phase transition in the cell cycle. However, the p16 gene can lose its functionality through point mutations, loss of heterozygosity or methylation of its promoter region. Materials and Methods: In this study, the authors analyzed the correlation between various clinicopathological findings- patient age, gender and smoking, disease recurrence, tumor size, stage, and differentiation- and p16 protein expression or p16 promoter hypermethylation in 59 cases of head and neck squamous cell carcinoma. Results: The results revealed p16 protein expression and p16 promoter hypermethylation in 28 cases (47.5%) and 21 cases (35.6%), respectively, of head and neck squamous cell carcinoma. However, neither p16 protein expression nor p16 promoter hypermethylation had any statistical influence on clinicopathological findings or survival rate. Conclusion: This data, and a review of the literature, suggest that p16 promoter hypermethylation cannot yet be used as an independent prognostic factor influencing carcinogenesis, but must be considered as an important factor along with other genetic alterations affecting the pRb pathway.

• Archives of Pharmacal Research
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• v.3 no.1
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• pp.7-12
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• 1980

Ampliciline was synthesized from 6-amino-pencillanic acid (6-APA) and D-.alpha. phenylglycine methyl ester by using amplicilin synthesizing enzyme from Peudomonas melanogenum (IAM 1655). The whole cell enzyme was immobilized by entrapping it in the polyacrylamide gel lattices. The polymer used in the enzyme entrapment was made from 150 mg per ml of acrylamide monomer and 8 mg per ml of N, N'-methylenebisacrylamide. About 200 mg/whole cell enzyme was mixed in the polymer for entrapment. The maximal activity retention after immobilization was 56%. The optimal pH values for the whole cell enzyme and the immobilized whole cell enzyme were 6.0 and 5.9, respectively. The optimal temperature for the enzyme activity were the same for both type of preparations. The enzyme stabilities against pH and heat increased for immobilized whole cell enzyme. Immobilized cell was more stable especially in the acidic condition while both type were found to be very suceptible to thermal inactivation at a temperature above 4.deg.C. The kinetic constants obtained from Lineweaver-Burk plot based on two substate reaction mechanism showed somewhat higher value for immobilized whole cell enzyme as compared to the whole cell enzyme : the Km value for 6-APA were 7.0 mM and 12.5 mM while Km values for phenylglycine methyl ester were 4.5 mM and 8.2 mM, respectively. Using the immobilized whole cell enzyme packed in a column reactor, the productivity of ampiciline was studied by varying the flow rate of substrate solution. At the space velocity, SV, 0.14 hr$^{-1}$ the conversion was 45%. Operational stability found in terms of half life was 30 hr at SV = 0.2 hr.

• KIPS Transactions on Computer and Communication Systems
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• v.6 no.5
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• pp.231-238
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• 2017

A Class B device in LoRaWAN periodically receives a Beacon message from a gateway for synchronization, and it also periodically activates a ping slot to receive data from the server. In this paper, we save energy consumption by controlling the beacon-less operation which is immediately started on the packet loss. In addition, we propose a method that the server inactivates the ping slots of a device according to the amount of messages, which have to be received from the server, to save energy consumption resulting from activated but unused empty slots. The experiment with the 20% of packet loss rate showed that the reduced beacon-less operation and the inactivation of the ping slot decrease the energy consumption by 96.7% and 60% as compared to the existing method.