• Biomolecules & Therapeutics
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• v.22 no.5
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• pp.400-405
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• 2014

G-protein coupled receptor 119 (GPR119) has emerged as a novel target for the treatment of type 2 diabetes mellitus. GPR119 is involved in glucose-stimulated insulin secretion (GSIS) from the pancreatic b-cells and intestinal cells. In this study, we identified a novel small-molecule GPR119 agonist, HD047703, which raises intracellular cAMP concentrations in pancreatic ${\beta}$-cells and can be expected to potentiate glucose-stimulated insulin secretion from human GPR119 receptor stably expressing cells (CHO cells). We evaluated the acute efficacy of HD047703 by the oral glucose tolerance test (OGTT) in normal C57BL/6J mice. Then, chronic administrations of HD047703 were performed to determine its efficacy in various diabetic rodent models. Single administration of HD047703 caused improved glycemic control during OGTT in a dose-dependent manner in normal mice, and the plasma GLP-1 level was also increased. With respect to chronic efficacy, we observed a decline in blood glucose levels in db/db, ob/ob and DIO mice. These results suggest that HD047703 may be a potentially promising anti-diabetic agent.

• Proceedings of the Korean Society of Plant Biotechnology Conference
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• 2005.11a
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• pp.27-39
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• 2005

a-Ketol linolenic acid [KODA, 9,10-ketol-octadecadienoic acid, or 9-hydroxy-10 -oxo-12(Z), 15(Z)-octadecadienoic acid] was found as a stress-induced factor in Lemna paucicostata. KODA reacts with catecholamines to generate many products that strongly induce flowering in L. paucicostata, although KODA itself was inactive. KODA contains an asymmetric carbon at the 9-position in the molecule; the 9-hydroxyl group is predominantly 9R, with an enantiomeric excess of 40% (70% 9R and 30% 9S). We analyzed two major products of the reaction between KODA and norepinephrine, named FN1 and FN2. FN1 was identified as a tricyclic a-ketol fatty acid, 9(R)-11-{(2'R,8’R,10'S,11'S)-2',8'-dihydroxy-7'-oxo-11'-[(Z)-2-pentenyl]-9'-oxa-4'-azatricyclo[6.3.1.01.5]dodec-5'en-10'-yl}-9-hydroxy-10-oxoundecanoic acid. FN2 was the C-9 epimer of FN1. FN1 was derived from 9R-type KODA and FN2 from 9S-type. FN1 showed strong flower-inducing activity, but FN2 was inactive. Pharbitis nil (violet) is a typical short-day plant; flowering can be induced by exposing a seedling cultivated under continuous light to a single 16-h dark period. We analyzed endogenous KODA levels and showed that they were closely related to flower induction: KODA sharply increased in the later part of a 16-h dark period, on the other hand, it failed to increase in the night-break experiment. In addition to it, KODA increased transiently in immature flower buds in all the plants we examined, including P. nil. No such increase of KODA was seen in foliar buds of P. nil. When KODA was sprayed on seedlings of Pharbitis, flower induction was promoted only by the (R)-form of KODA. We also found that KODA enhances flowering in garden plants such as carnations and impatienses. These phenomena indicate that KODA may be involved in flowering formationg of plants and it is potentially useful for a regulating agent for commercial plant flowering.

• Korean Journal of Fisheries and Aquatic Sciences
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• v.25 no.6
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• pp.474-484
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• 1992

The stock identification of small yellow croaker. Pseudosciaena Polyactis from Mokpo area was carried out using molecular biological methods such as mt-DNA restriction fragment length polymorphism(RFLP) and the N-terminal fragment polymorphism of muscle actin obtained after protease digestion. The entire mt-DNA genomic size from the small yellow croaker at Mokpo area was estimated to be about $16\pm0.2$ Kb. Furthermore, fourteen restriction endonucleases revealed a total of 37 restriction sites to the mt-DNA molecule, however, eight of the fourteen enzymes showed a significant restriction site variation. Six of the enzymes examined produced a single restriction profile for all individuals surveyed, indicating that they don't react on the same mt-DNA obtained from small yellow croaker. The Staphylococcus aureus $V_8$ protease is able to cleave the muscle actin of small yellow croaker and to yield a N-terminal peptide of 26 and 16 KDa, respectively.

• Journal of Microbiology and Biotechnology
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• v.19 no.11
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• pp.1393-1400
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• 2009

A bacteriocin-producing strain PI80 was isolated from the gut of Penaeus indicus (Indian white shrimp) and identified as Streptococcus phocae PI80. The bacteriocin was purified from a culture supernatant to homogeneity as confirmed by Tricine SDS-PAGE. Reverse-phase HPLC analysis revealed a single active fraction eluted at 12.94 min, and MALDI-TOF mass spectrometry analysis showed the molecular mass to be 9.244 kDa. This molecular mass does not correspond to previously described streptococcal bacteriocins. The purified bacteriocin was named phocaecin PI80 from its producer strain, as this is the first report of bacteriocin production by Streptococcus phocae. The bacteriocin exhibited a broad spectrum of activity and inhibited important pathogens: Listeria monocytogenes, Vibrio parahaemolyticus, and V. fischeri. The antibacterial substance was also sensitive to proteolytic enzymes: trypsin, protease, pepsin, and chymotrypsin, yet insensitive to catalase, peroxidase, and diastase, confirming that the inhibition was due to a proteinaceous molecule (i.e., the bacteriocin), and not due to hydrogen peroxide or diacetyl. Phocaecin PI80 moderately tolerated heat treatment (up to $70^{\circ}C$ for 10 min) and resisted certain solvents (acetone, ethanol, and butanol). A massive leakage of $K^+$ ions from E. coli $DH5\alpha$, L. monocytogenes, and V. parahaemolyticus was induced by phocaecin PI80, as measured by Inductively Coupled Plasma Optical Emission Spectrometry (ICPOES). Therefore, the results of this study show that phocaecin PI80 may be a useful tool for inhibiting L. monocytogenes in seafood products that do not usually undergo adequate heat treatment, whereas the cells of Streptococcus phocae PI80 could be used to control vibriosis in shrimp farming.

• Korean Journal of Environmental Biology
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• v.30 no.2
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• pp.77-89
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• 2012

With the advent of the genomics era powered by DNA sequencing technologies, life science is being transformed significantly and biological research and development have been accelerated. Environmental biology concerns the relationships among living organisms and their natural environment, which constitute the global biogeochemical cycle. As sustainability of the ecosystems depends on biodiversity, examining the structure and dynamics of the biotic constituents and fully grasping their genetic and metabolic capabilities are pivotal. The high-speed high-throughput next-generation sequencing can be applied to barcoding organisms either thriving or endangered and to decoding the whole genome information. Furthermore, diversity and the full gene complement of a microbial community can be elucidated and monitored through metagenomic approaches. With regard to human welfare, microbiomes of various human habitats such as gut, skin, mouth, stomach, and vagina, have been and are being scrutinized. To keep pace with the rapid increase of the sequencing capacity, various bioinformatic algorithms and software tools that even utilize supercomputers and cloud computing are being developed for processing and storage of massive data sets. Environmental genomics will be the major force in understanding the structure and function of ecosystems in nature as well as preserving, remediating, and bioprospecting them.

• Biomolecules & Therapeutics
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• v.22 no.3
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• pp.260-266
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• 2014

This study evaluated the pharmacokinetic profile and therapeutic efficacy of piroxicam (PX), a long acting non-steroidal anti-inflammatory drug for the treatment of arthritis, following intra-articular (IA) injection in comparison to the pharmacokinetic profile and therapeutic efficacy of PX after intramuscular (IM) injection. In the pharmacokinetic study in rats, systemic exposure and pharmacokinetic parameters of PX after a single IA dose were compared with systemic exposure and pharmacokinetic parameters of PX after administration of the same dose IM (0.6 mg/kg). The anti-inflammatory and analgesic effects of IA PX were evaluated simultaneously in a monoiodoacetate-induced osteoarthritis rat model. The plasma PX concentration rapidly rose following IA injection, and it was comparable to the plasma PX concentration following IM injection, suggesting the rapid efflux of the drug molecule from the joint cavity. However, in the efficacy study, the IA PX administration significantly reduced the knee swelling by reducing the level of prostaglandin $E_2$ in the joint, compared to that following administration of IA vehicle and after administration of the IM PX dose. In addition, we found that the anti-inflammatory and anti-nociceptive efficacies of IA PX were synergistically increased upon co-treatment with hyaluronic acid (HA), a potent agent for the treatment of osteoarthritis, at the weight ratio of 1:1 or 1:2, and these effects were more pronounced than those following administration of HA or PX alone. In conclusion, this study demonstrated the efficacy of the IA use of PX alone and/or in combination with HA in osteoarthritis.

• Proceedings of the Korean Vacuum Society Conference
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• 2011.08a
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• pp.198-198
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• 2011

Organocatalysis is a relatively new and popular area within the field of chiral molecule synthesis. It is one of the main branches of enantioselective synthesis with enzymatic and organometallic catalysis. In recent years, immense high quality studies on catalysis by chiral secondary amines were reported. These progresses instantly led to different organocatalytic activation concepts, so thousands of researchers from academia and the chemical industry are currently involved in this field and new ideas, new approaches, and creative thinking have been rapidly emerged. Organocatalysts, some of which are natural products, appear to solve the problems of metal catalysts. Compared to metal-based catalysis, they have many advantages including savings in cost, time, and energy, easier experimental procedure, and reduction of chemical waste. These benefits originate from the following factors. First, organocatalysts are generally stable in oxygen and water in the atmosphere, there is no need for special equipments or experimental techniques to operate under anhydrous or anaerobic conditions. Second, organic reagents are naturally available from biological materials as single enantiomers that they are easy and cheap to prepare which makes them suitable for small-scale to industrial-scale reactions. Third, in terms of safety related catalysis, small organic molecules are non-toxic and environmentally friendly. Therefore, the purpose of this research is to develop novel synthetic methods and design for various organocatalyst. Furthermore, it is expected that these organocatalysts can be applied to a variety of asymmetric reactions and study the transition state of these reactions using a metal sulface. Here, we report the synthesis of unprecedented organocatalysts, proline and pyrrolidine derivatives with quaternary carbon center.

• Korean Chemical Engineering Research
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• v.53 no.2
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• pp.243-246
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• 2015

Colorimetric sensors were usually used to detect specific metal ions using selective color change of solutions. While almost organic dye in colorimetric sensors detected single molecule, dithizone (DTZ) solution could be separately detected above 5 kinds of heavy metal ions by the change of clear color. Namely, DTZ could be used as multi-colorimetric sensors. However, DTZ was generally used as aqueous type and paper/pellet-type DTZ was not reported yet. Therefore, in this work, polystyrene (PS) was prepared to composite with DTZ and then DTZ/PS pellet was obtained, which was used to selectively detect 10 kinds of heavy metal ions. When 10 ppm of Hg and Co ions was exposed in DTZ/PS pellets, clear color change was revealed. It is noted that DTZ/PS pellet could be used in detecting of heavy metal ion as dry type.

• Journal of the Korean Chemical Society
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• v.24 no.3
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• pp.193-200
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• 1980

The crystal structure of N-acetyl-L-cysteine, $C_5H_9NO_3S,$ has been determined from three dimensional photographic intensity data $(CuK{\alpha}$ radiation) by single crystal X-ray diffraction analysis. There is one formula unit in the triclinic unit cell with a = 7.04(3), b = 5.14(2), c = 8.25(3) ${\AA}$, ${\alpha}$ = 106(2), ${\beta}$ = 51(1), ${\gamma}$ = 124(2)$^{\circ}$ and space group P$_1$, The structure was solved by the direct method and refined by the full matrix least-squares method. The final R value is 12.3% for 629 observed reflections. The C-carboxyl group and the N-acetyl group are very neary planar. The molecule appears to form with neighboring molecules a hydrogen bond, $O-H{\cdot}{\cdot}{\cdot}O(3)$ of length 2.59${\AA}$.

• The Korean Journal of Physiology
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• v.17 no.1
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• pp.1-11
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• 1983

1) The two microelectrode method was used to voltage clamp small preparations of rabbit sinoatrial node. The kinetics of hyperpolarization activated inward current, $i_f$ were analysed. 2) The hrperpolarization pulses activated $i_f$ current in the presence of $10^{-7}g/ml$ TTX and 2 mM $Mn^{2+}$. The activation range was in between -45 mV to -75 mV. The current magnitude was increased and time course was faster by strong hyperpolarization pulses. 3) Standard envelope tests indicated that this current is exponentially controlled by single gate. 4) Semilogarithmic plot of $i_f$ activation versus time was found to be linear in the activation range. The decrease in current magnitude and the shifts in activation curve and rate constants curve to the hyperpolarizing direction were obtained with $Ba^{2+}$, indicating that $Ba^{2+}$ shifts the voltage dependence of the gating kinetics, were partially reversed by 24 mM $K^+$.