• Journal of Ginseng Research
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• v.29 no.1
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• pp.37-43
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• 2005

We performed in vitro and in vivo studies to know whether the inhibitory effects of ginsenosides on $5-HT_{3A}$ receptor channel acctivity are coupled to anti-nausea and anti-vomiting action. In vitro study, we investigated the effect of compound K (CK) and M4, which are ginsenoside metabolites, on human $5-HT_{3A}$ receptor channel activity expressed in Xenopus oocytes using two-electrode voltage clamp technique. Treatment of CK or M4 themselves had no effect in both oocytes injected with $H_2O\;and\;5-HT_{3A}$ receptor cRNA. In oocytes injected with $5- HT_{3A}$ receptor cRNA, M4 treatment inhibited more potently 5-HT-induced inward peak current $(I_{5-HT})$ than CK with dose-dependent and reversible manner. The half-inhibitory concentrations $(IC_{50})$ of CK and M4 were $36.9\;\pm\;10.1\;and\;7.3\;\pm\;2.2\;{\mu}M$, respectively. The inhibition of $I_{5-HT}$ by M4 was non-competitive and voltage-independent. These results indicate that M4 might regulate $5-HT_{3A}$ receptors. In vivo experiments, injection of cisplatin (7.5 mg/kg, i.v.) induced both nausea and vomiting with 1 h latency. These episodes reached to peak after 2 h and persisted for 4 h. Pre-treatment of GTS (500 mg/kg, p.o.) significantly reduced cisplatin-induced nausea and vomiting by $51\;\pm\;8.4\;and\;48.8\;\pm\;6.4\%$ during 4 h compared to GIS­untreated group, respectively. These results show the possibility that in vitro inhibition of $5-HT_{3A}$ receptor channel activity by ginsenosides might be coupled to in vivo anti-emetic activity.

• Journal of the Korean Society of Fisheries and Ocean Technology
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• v.46 no.1
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• pp.10-19
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• 2010

As a series of studies about improvement of yellow croaker drift gill net fishing gear and development of the labor saving fishing system, this study analyzed the behavior characteristics of fishing gear, which does use three types of different sinker materials in the field tests. The result of maritime performance test indicated that the fishing gear which used the lead reached the maximum depth and bio ceramics hauled to the surface of water the fastest. The correlation between the sinking time (St) and depth (Dsl, Dsc, Dsb) of maritime performance test can be shown such experimental equations as Dsl=2.70St - 0.75, Dsc = 2.38St - 1.15, Dsb = 1.77St - 4.00. The correlation between the hauling time (Ht) and depth (Dhl, Dhc, Dhb) of maritime performance test can be shown such experimental equations as and Dhl = 7.88Ht + 35.48, Dhc = 7.80Ht + 40.01, Dhb = 7.95Ht + 36.44.

• Proceeding of EDISON Challenge
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• 2017.03a
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• pp.46-53
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• 2017

알츠하이머병은 치매를 유발하는 가장 주된 원인 질환으로 환자들은 인지장애를 겪게 된다. 현재 치료약으로 사용되는 약으로는 acetylcholinesterase 저해재가 있지만 이 약들의 효과는 미비하다. 그래서 인지기능에 영향을 미친다고 알려진 신경전달물질인 GABA, Glutamate, acetylcholine의 수치를 조절 할 수 있는 $5-HT_6$ receptor antagonist가 현재 개발되고 있다. 현재 여러 antagonist들이 임상실험 되었고, 인지 능력향상에 효과를 보이고 있다. 그러나, $5-HT_6$ receptor의 구조가 밝혀지지 않아 아직 원자적 수준의 결합 분석이 이루어지지 않았으므로 이 부분에 대한 연구가 필요하다. 따라서 본 연구에서는 Homology modeling을 통해 receptor의 구조를 예측하고, 현재 임상실험 중인 antagonist들 중 7개를 docking을 통해 단백질과 리간드의 결합을 예측하였다. Edison에서 Galaxy TBM과 Galaxy Refine을 사용하여 Homology modeling 한 결과 GPCR의 전형적인 모델에 특징적으로 긴 cterminal을 가졌다는 것을 확인 할 수 있었다. 생성된 구조를 가지고 Edison의 Dock 프로그램으로 7개의 antagonist가 어떠한 결합을 하는지 분석하였다. 그 결과, binding pose에 공통적으로 Trp102, Asp106, Val107, Pro177, Phe188, Val189, Ala192, Phe284, Phe285, Asn288, Thr306, Tyr310이 관여하는 것을 docking을 통해 알 수 있었다. 특히, Phe285는 7개의 antagonist 중에 4개와의 interaction을 하고 있는 것을 관찰하였다. 이 연구를 통하여 $5-HT_6$에 효과적으로 결합하여 치료효과를 낼 수 있는 신약을 개발할 수 있다.

• Bulletin of the Korean Chemical Society
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• v.30 no.5
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• pp.1107-1112
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• 2009

The aim of this study is to develop and synthesize $5-HT_{1A}$ receptor imaging agents with WAY-100635 moiety and $^{99m}Tc(CO)_3$ core. WAY-100635 is commonly known as $5-HT_{1A}$ antagonist and its labeled compound ([$^{11}C$] WAY-100635) has been used as effective radioligand for imaging brain $5-HT_{1A}$ receptors with PET(Positron Emission Tomography). However, there are several restrictions in using a radioisotope of C-11 and requires for more effective radioisotopes and ligands. In order to produce a structure most similar to WAY-100635, WAY-100635 derivatives containing a cysteine chelator were designed and confirmed by using in silico (Hyperchem). The novel compounds (7a, 7b, 7c) were prepared in five or 7 steps with yields of 16%, 36% and 42%, respectively and radiolabeled with $[^{99m}Tc(CO)_3(H_2O)_3]^{+}$. The labeling yield was 99% for all the newly synthesized compounds. [$^{99m}Tc(CO)_3$]- WAY-100635 derivatives show a neutral charge which were confirmed by paper electrophoresis.

• Proceedings of the Korean Institute of Electrical and Electronic Material Engineers Conference
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• 2003.11a
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• pp.486-489
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• 2003

Red organic electroluminescent(EL) devices based on poly(N-vinylcarbazole)(PVK) and tris(8-hydroxyquinorine aluminum)($Alq_3$) doped with red emissive material, 4-(dicyanomethylene)-2-t-butyl-6-(1,1,7,7-tetramethyljulolidyl-9-enyl)4H-pyran(DCJTB), poly(3-hexylthiophene)(P3HT), Rubrene and 4-dicyanomethylene-2-methyl-6[2-(2,3,6,7-tetrahydro-1H,5H-benzo-[i.j])quinolizin-8yl)vinyl-4H-pyran(DCM2) were fabricated. We examine the energy transfer from $Alq_3$ to DCJTB, P3HT, Rubrene and DCM2 by comparing between the PL and EL spectrum. The maximum peak PL intensities were achieved when the doping concentration of DCJTB, DCM2, P3HT and Rubrene has 5, 1, 0.5, 2wt%, respectively. The maximum luminance of device using DCJTB showed $594\;cd/m^2$ at 15V.

• The Korean Journal of Physiology and Pharmacology
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• v.7 no.6
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• pp.295-301
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• 2003

Striatum plays a crucial role in the movement control and habitual learning. It receives an information from wide area of cerebral cortex as well as an extensive serotonergic (5-hydroxytryptamine, 5-HT) input from raphe nuclei. In the present study, the effects of 5-HT to modulate synaptic transmission were studied in the rat corticostriatal brain slice using in vitro extracellular recording technique. Synaptic responses were evoked by stimulation of cortical glutamatergic inputs on the corpus callosum and recorded in the dorsal striatum. 5-HT reversibly inhibited coticostriatal glutamatergic synaptic transmission in a dose-dependent fashion (5, 10, 50, and $10{\mu}M$), maximally reducing in the corticostriatal population spike (PS) amplitude to $40.1{\pm}5.0$% at a concentration of $50{\mu}M$ 5-HT. PSs mediated by non-NMDA glutamate receptors, which were isolated by bath application of the NMDA receptor antagonist, d,l-2-amino-5-phospohonovaleric acid (AP-V), were decreased by application of $50{\mu}M$ 5-HT. However, PSs mediated by NMDA receptors, that were activated by application of zero $Mg^{2+}$ aCSF, were not significantly affected by $50{\mu}M$ 5-HT. To test whether the corticostriatal synaptic inhibitions by 5-HT might involve a change in the probability of neurotransmitter release from presynaptic nerve terminals, we measured the paired-pulse ratio (PPR) evoked by 2 identical pulses (50 ms interpulse interval), and found that PPR was increased ($33.4{\pm}5.2$%) by 5-HT, reflecting decreased neurotransmitter releasing probability. These results suggest that 5-HT may decrease neurotransmitter release probability of glutamatergic corticostriatal synapse and may be able to selectively decrease non-NMDA glutamate receptor-mediated synaptic transmission.

• Toxicological Research
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• v.13 no.4
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• pp.359-365
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• 1997

Many factors are known to be responsible for cerebral ischemic injury, such as excitatory neurotransmitters, increased intraneuronal calcium, or disturbance of cellular energy metabolism. Recently, oxygen free radicals, formed during ischemia/reperfusion, have been proposed as one of the main causes of ischemia/reperfusion injury. Therefore, to investigate the role of oxygen free radical during ischemia/reperfusion, in the present study the effect of endogenous oxygen free radical scavenger, superoxide dismutase / catalase(SOD / catalase) on the release of [$^3$H]-5-hydroxytryptamine([$^3$H]-5-HT) during hypoxia/reoxygenation in rat hippocampal slices was measured. The hippocampus was obtained from the rat brain and sliced 400 gm thickness with manual chopper. After 30 min's preincubation in the normal buffer, the slices were incubated for 20 min in a buffer containing [$^3$H]-5-HT(0.1 $\mu$M, 74 $\mu$Ci) for uptake, and washed. To measure the release of [$^3$H]-5-HT into the buffer, the incubation medium was drained off and refilled every ten minutes through a sequence of 14 tubes. Induction of hypoxia for 20 min (gassing it with 95% N$_2$/5% CO$_2$) was done in the 6th and 7th tube, and oxygen free radical scavenger, SOD / catalase was added 10 minutes prior to induction of hypoxia. The radioactivity in each buffer and the tissue were counted using liquid scintillation counter and the results were expressed as a percentage of the total activity. When slices were exposed to hypoxia for 20 min, [$^3$H]-5-HT release was markedly decreased and a rebound release of [$^3$H]-5-HT was observed on the post-hypoxic reoxygenation period. SOD / catalase did not changed the release of [$^3$H]-5-HT in control group, but inhibited the decrease of [$^3$H]-5-HT release in hypoxic period and rebound increase of [$^3$H]-5-HT in reoxygenation period. This result suggest that superoxide anion may play a role in the hypoxic-, and reoxygenation-induced change of [$^3$H]-5-HT release in rat hippocampal slices.

• The Journal of Korean Medicine
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• v.24 no.4
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• pp.82-86
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• 2003

Objective : To examine the inhibition of 5-Hydroxytryptamine(5-HT) induced vasocontraction of the water extract of Acanthopanax senticosus Harms roots (ASR) on rat thoracic Aorta and mesenteric artery with and without endothelium. Methods : Segments of thoracic aorta and mesenteric artery obtained from rats immediately after delivery were mounted in organ baths superfused on a polygraph. Results : We found that the thoracic aorta segments responded to the water extract of ASR with a dose-dependent and concentration-dependent vasorelaxation. 5-HT produced a concentration-dependent contraction of the thoracic aorta and mesenteric artery. At high concentrations of ASR, the inhibition responses were 93.7% (Jang-su), 93.5% (Heok-ryong-kang-sung), 92.8% (Mt. Back-doo), and 83.5% (Yeon-byun) of the maximum 5-HT induced contraction. At high concentrations of ASR, the relaxational response at thoracic aorta and mesenteric artery wi1h endothelium were 95.2% and 94.6%; without endothelium were 93.5% and 92.5% of 1he maximum 5-HT induced contraction. Conclusions : In conclusion, the effect of water extract of ASR had potent inhibition at 5-HT and the effect of ASR in isolated thoracic aorta and mesenteric artery showed dose-dependent inhibition but endothelium-independent response.

• Asian-Australasian Journal of Animal Sciences
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• v.25 no.7
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• pp.913-920
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• 2012

In this study, we investigated the relationship between unsaturated fatty acids influencing beef flavor and four types of SNPs (c.280A>G, c.388G>A, c.408G>C and c.456A>G) located at exon 2, 3 and 4 of the FABP4 gene, which is a fatty acid binding protein 4 in Korean cattle (n = 513). When analyzing the relationship between single genotype, fatty acids and carcass trait, individuals of GG, GG, CC and GG genotypes that are homozygotes, had a higher content of unsaturated fatty acids and marbling scores than other genotypes (p<0.05). Then, haplotype block showed strong significant relationships not only with unsaturated fatty acids (54.73%), but also with marbling scores (5.82) in $ht1{\times}ht1$ group (p<0.05). This $ht1{\times}ht1$ group showed significant differences with unsaturated fatty acids and marbling scores that affected beef flavor in Korean cattle. Therefore, it can be inferred that the $ht1{\times}ht1$ types might be valuable new markers for use in the improvement of Korean cattle.

• Proceedings of the Korean Institute of Electrical and Electronic Material Engineers Conference
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• 2000.07a
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• pp.308-311
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• 2000

The organic electroluminescene (EL) device has gathered much interested because of its potential in materials and simple device fabrication. We fabricated EL device which have a mixed single emitting layer containing N,N'-diphenyl-N,N'-(3-methylphenyl)-1,1'-biphenyl-4,4'-diamine [TPD] and poly(3-hexylthiophene) [P3HT]. The molar ratio between P3HT and TPD chaged with 1:1, 3:1, 5:1, 3:2 and 5:2. EL intensity of ITO/P3HT+TPD/Mg:In devices is enhanced by addition of TPD into P3HT. This can be explained that the energy transfer occurs from TPD to P3HT. Recombination probability increases in emitting layer because that TPD as hole transport material plays a role more injection hole and Mg:In (3.7eV) electrode has low work function make easily electron injection. ITO/P3HT+TPD(5:2)/Mg:In devices emit orange-red light at 28V.