• Title/Summary/Keyword: $5-HT_{1A}$

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Effects of Sophorae Radix on Human Colorectal Adenocarcinoma Cells (고삼의 인체 대장암세포에 미치는 효과)

  • Kim, Min-Chul;Lee, Hee-Jung;Lim, Bo-Ra;Kim, Hyung-Woo;Kim, Byung-Joo
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.26 no.2
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    • pp.155-159
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    • 2012
  • The purpose of this study was to investigate the anti-cancer effects of Sophorae Radix and the effects of 5-Fluorouracil (5-FU) in human colorectal adenocarcinoma cells (HT-29). We used human colorectal adenocarcinoma cell line, HT-29 cells. We examined cell death by MTT assay and caspase 3 assay with Sophorae Radix. To examine the inhibitory effects of Sophorae Radix, cell cycle (sub G1) analysis was done the HT-29 cells after three days with Sophorae Radix. The reversibility of Sophorae Radix was examined on one day to five days treatment with $150{\mu}g$ Sophorae Radix. Sophorae Radix inhibited the growth of HT-29 cells in a dose-dependent fashion. Also we showed that Sophorae Radix induced apoptosis in HT-29 cells by MTT assay, caspase 3 assay and sub-G1 analysis. Sophorae Radix combined with 5-FU markedly inhibited the growth of HT-29 cells compared to Sophorae Radix or 5-FU alone. After 3 days treatment of HT-29 cells with Sophorae Radix, the fraction of cells in sub-G1 phase was much higher than that of the control group. Our findings provide insight into unraveling the effects of Sophorae Radix in human colorectal adenocarcinoma cells and developing therapeutic agents against colorectal cancer.

An Immunohistochemical ana Ultrastructural Studies on the Gut Endocrine Cells in the Hedgehog, Erinaceus koreanus (한국산 고슴도치(Erinaceus koreanus)의 장관 내분비세포에 관한 면역조직화학적 및 전자현미경적 연구)

  • Lee, Jae-Hyun
    • Applied Microscopy
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    • v.18 no.2
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    • pp.59-76
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    • 1988
  • In order to know the distribution, relative frequencies, types and morphology, endocrine cells in the intestinal tract of the hedgehog(Erinaceus koreanus) were studied by light microscopy, immunohistochemistry and electron microscopy. The results obtained are summarized as follows: 1. Two kinds of endocrine cells were demonstrated with two specific staining methods. Argyrophil cells(reactive cells for Grimelius method) were found most frequently in the intestinal region, and were infrequent in the rectum, whereas argentaffin cells (reactive cells for Masson-Hamperl method) were found most frequently in the rectum and in the other legions were infrequent. These reacting cells were mainly found in the intestinal glands, whereas a small number in the mucosa. 2. Twelve kinds of endocrine cells, gastrin(Gas)-, somatostatin (Som)-, serotonin(5-HT)-, glucagon(Glu)-, bovine pancreatic polypeptide(Bpp)-, cholecystokinin(Cck)-, secretin(Sec)-, motilin(Mot)-, glicentin(Gli)-, gastric inhibitor polypeptide(GIp)-, substance P(Sp)-, and neurotensin(Neu)-immunoreactive cells, were identified by immunohistochemical method. Gas-, Som-, 5-HT-, Glu-, Cck-, Sec-, Mot-, Gli-, Sp-, and Neu-reactive cells were observed in the duodenum, and among these Gas- and 5-HT-reactive cells were moderately found while the others were infrequent. In the jejunoileum Gas-, Som-, 5-HT-, Glu-, Cck-, Mot-, Gli-, GIp-, SP-, and Neu-reactive cells were found, and among these 5-HT- and GIp-reactive cells were moderately found while the others were infrequent. In the colon Sec-reactive cell was not detected. 5-HT-reactive cells were found most frequently and the others were infrequent in this region. 5-HT-, Bpp-, GIi- and Neu-reactive cells were found in the rectum. Among these 5-HT-reactive cells were found most frequently. 3. Electron microscopically, five types of endocrine cells, EC, ECL, D, G, A-like cell, were identified in the intestinal region. EC and ECL cells in the duodenum, EC, D and G cells in the jejuno-ileum, EC and A-like cells in the colon and EC cell in the rectum were observed respectively.

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Synthesis and Characterization of Thiophene-Based Copolymers Containing Urethane and Alkyl Functional Side Chains for Hybrid Bulk Heterojunction Photovoltaic Cell Applications

  • Im, Min-Joung;Kim, Chul-Hyun;Song, Myung-Kwan;Park, Jin-Su;Lee, Jae-Wook;Gal, Yeong-Soon;Lee, Jun-Hee;Jin, Sung-Ho
    • Bulletin of the Korean Chemical Society
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    • v.32 no.2
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    • pp.559-565
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    • 2011
  • The following noble series of statistical copolymers, poly[(2-(3-thienyl)ethanol n-butoxycarbonylmethylurethane)-co-3-hexylthiophene] (PURET-co-P3HT), were synthesized by the chemical dehydrogenation method using anhydrous $FeCl_3$. The structure and electro-optical properties of these copolymers were characterized using $^1H$-NMR, UV-visible spectroscopy, elemental analysis, GPC, DSC, TGA, photoluminescence (PL), and cyclic voltammetry (CV). The statistical copolymers, PURET-co-P3HT (1:0, 2:1, 1:1, 1:2, 1:3), were soluble in common organic solvents and easily spin coated onto indium-tin oxide (ITO) coated glass substrates. Hybrid bulk heterojunction photovoltaic cells with an ITO/G-PEDOT/PURET-co-P3HT:PCBM:Ag nanowires/$TiO_x$/Al configuration were fabricated, and the photovoltaic cells using PURET-co-P3HT (1:2) showed the best photovoltaic performance compared with those using PURET-co-P3HT (1:0, 2:1, 1:1, 1:3). The optimal hybrid bulk heterojunction photovoltaic cell exhibits a power conversion efficiency (PCE) of 1.58% ($V_{oc}$ = 0.82 V, $J_{sc}$ = 5.58, FF = 0.35) with PURET-co-P3HT (1:2) measured by using an AM 1.5 G irradiation (100 mW/$cm^2$) on an Oriel Xenon solar simulator (Oriel 300 W).

Novel 99mTc(CO)3 Complexes with WAY-100635 Moiety for the Development of 5-HT1A Receptor lmaging Agent

  • Choi, Kang-Hyuk;Pyun, Mi-Sun;Hong, Young-Don;Choi, Sun-ju
    • 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.

The Effect of Glucose Deprivation on the Oxygen Deprivation-induced Changes of [[$^3H$]-5-hydroxytryptamine Release in Rat Hippocampal Slices (흰쥐 해마 절편에서 산소고갈에 의한 [$^3H$-5-hydroxytryptamine 유리변동에 미치는 포도당고갈의 영향)

  • 이경은
    • Toxicological Research
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    • v.14 no.4
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    • pp.483-488
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    • 1998
  • During cerebral ischemia two important factors such as hypoxia and reduction of glucose can act as modulating stressor affecting the release of amine neurotransmitters including 5-hydroxytryptamine (5-HT). This study was performed to investigate the effect of glucose deprivation on the oxygen deprivation-induced changes of [3H]-5-HT release in the rat hippocampal slices. Experimental groups were divided into 4 groups for this study: normoxic/normoglycemic group, oxygen-deprived group, glucose-deprived group, and oxygen/glucose-deprived group. The hippocampus of rat brain was sliced by 400 $\mu\textrm{m}$ thickness with manual chopper. After 30 minutes preincubation in the normal buffer, the slices were incubated for 20 min in buffer containing [3H]-5-HT (0.1 M, 74 $\mu\textrm$Ci) for uptake. To measure the release of [3H]-5-HT into the buffer, the incubation medium was drained of and refilled with fresh buffer every ten minutes through a sequence of 14 tubes. Oxygen deprivation by gassing with 95% $N_2$/5% $CO_2$ and/or glucose deprivation was done in the 6th and 7th tube. The radioactivities in each buffer and the tissue were counted using scintillation counter. The results were expressed as fractional release. When slices were exposed to oxygen-deprived media for 20 min, the diminution followed by the rebound release of [3H]-5-HT was observed during the post-oxygen deprived period. However, glucose deprivation or oxygen/glucose deprivation markedly increased the release of [3H]-5-HT. which was opposite to the pattern observed in oxygen-deprived group. These results suggested that oxygen deprivation itself inhibits [3H]-5-HT release in rat hippocampal slices during oxygen-deprived period, but additional glucose deprivation convert the inhibitory response to increase of [3H]-5-HT release.

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Effect of Acute and Chronic Treatment with Risperidone on the Serotonin and Dopamine Receptors in the Rat Brain (Risperidone의 급성 및 만성 투여가 흰쥐 뇌의 Serotonin과 Dopamine 수용체에 미치는 영향)

  • Choi, Yun-Young;Son, Hye-Kyung;Kim, Chang-Yoon;Lee, Chul;Lee, Hee-Kyung;Moon, Dae-Hyuk
    • The Korean Journal of Nuclear Medicine
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    • v.31 no.1
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    • pp.9-18
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    • 1997
  • The therapeutic efficacy of antipsychotic drugs is generally attributed to their ability to block dopamine $D_2$ receptors. Classical $D_2$ antagonists are not effective to treat negative symptoms and produce extrapyramidal side effects On the other hand, atypical antipsychotic agents ameliorate negative symptoms without producing extra-pyramidal side effects, and it is reported to be associated with blockade of serotonin $5-HT_2$ receptors. The purpose of this study was to evaluate the effect of risperidone on neuroreceptors in the rat brain by Quantitative autoradiography method. In acute treatment group, risperidone was injected into Peritoneal cavity of male Wistar rats with dose of 0, 0.1, 0.25, 0.5, 1.0 and 2.0mg/kg in each group(5/group), and they were decapitated after 2 hours. In chronic treatment group, risperidone was injected with dose of 0, 0.1, and 1mg/kg(I.P.) for 21 days and decapitated after 24 hours following last treatment. The effect of risperodone on the binding of [$^3H$]spiperone to $5-HT_2$ and $D_2$ receptors were analysed in 4 discrete regions of the striatum, nucleus accumbens, and frontal cortex by quantitative autoradiography Acute treatment with risperidone reduced cortical $5-HT_2$ specific [$^3H$]spiperone binding to 32% of vehicle-treated control. Subcortical $5-HT_2$ specific [$^3H$]spiperone binding was not affected at all dose groups whereas a significant reduction (57%) in $D_2$ specific [$^3H$]spiperone binding was observed in risperidone treated group at doses of 1-2mg/kg. Chronic treatment with risperidone produced a decrease in the maximal number of cortical $5-HT_2$ receptors to 51% and 46% of control in 0.1mg/kg & 1mg/kg treated group respectively. In conclusion, risperidone is a cortical serotonin receptor antagonist with relatively weak antagonistic action on dopamine receptors. These effects oil neuroreceptors may explain the therapeutic effect of risperidone as a atypical antipsychotic agents.

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Layer-specific serotonergic induction of long-term depression in the prefrontal cortex of rats

  • Shin, Dongchul;Cho, Kwang-Hyun;Joo, Kayoung;Rhie, Duck-Joo
    • The Korean Journal of Physiology and Pharmacology
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    • v.24 no.6
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    • pp.517-527
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    • 2020
  • Layer 2/3 pyramidal neurons (L2/3 PyNs) of the cortex extend their basal dendrites near the soma and as apical dendritic tufts in layer 1, which mainly receive feedforward and feedback inputs, respectively. It is suggested that neuromodulators such as serotonin and acetylcholine may regulate the information flow between brain structures depending on the brain state. However, little is known about the dendritic compartment-specific induction of synaptic transmission in single PyNs. Here, we studied layer-specific serotonergic and cholinergic induction of long-term synaptic plasticity in L2/3 PyNs of the agranular insular cortex, a lateral component of the orbitofrontal cortex. Using FM1-43 dye unloading, we verified that local electrical stimulation to layers 1 (L1) and 3 (L3) activated axon terminals mostly located in L1 and perisomatic area (L2/3). Independent and AMPA receptor-mediated excitatory postsynaptic potential was evoked by local electrical stimulation of either L1 or L3. Application of serotonin (5-HT, 10 μM) induced activity-dependent longterm depression (LTD) in L2/3 but not in L1 inputs. LTD induced by 5-HT was blocked by the 5-HT2 receptor antagonist ketanserin, an NMDA receptor antagonist and by intracellular Ca2+ chelation. The 5-HT2 receptor agonist α-me-5-HT mimicked the LTD induced by 5-HT. However, the application of carbachol induced muscarinic receptor-dependent LTD in both inputs. The differential layer-specific induction of LTD by neuromodulators might play an important role in information processing mechanism of the prefrontal cortex.

Antiproliferative Effect of Opuntia humifusa Ethanol Extract on Human Carcinoma HT-29 Cells (천년초 선인장 줄기 에탄올 추출물의 HT-29 대장암 세포증식 저해효과)

  • Park, Soo Young;Kim, Young A;Ly, Sun Yung
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.43 no.12
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    • pp.1827-1834
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    • 2014
  • Colon cancer is the third highest cause of death in Korea. Known dietary causes of colon cancer include a diet rich in fat and red meat as well as inadequate intake of dietary fiber, fruits, and vegetables. Therefore, recent research has focused on the anticancer effects of natural products. Opuntia humifusa is a type of prickly pear that is known to contain biologically active compounds that can be used in the treatment of diabetes mellitus, arteriosclerosis, and hyperglycemia. The aim of this study was to determine whether or not O. humifusa extract affects proliferation, cell death, and DNA fragmentation in human carcinoma HT-29 cells. O. humifusa is rich in carbohydrates, minerals (Mg, K, and Ca), and total phenolics. HT-29 cells were treated with extracts of O. humifusa at concentrations of 0, 0.25, 0.5, 1, and 2 mg/mL for 24 or 48 hours. O. humifusa extracts inhibited HT-29 cell growth in a dose-dependent manner. Hoechst 33342/PI double staining and Comet assay were performed to observe changes in nuclei of cancer cells undergoing cell death. The results of both tests showed that O. humifusa extract induced cell shrinkage, DNA fragmentation, and chromatin condensation dose-dependently in HT-29 cells. The results of this study suggest that O. humifusa extract inhibits the growth of HT-29 via induction of DNA fragmentation and chromatin condensation.

Effects of Resveratrol and trans-3,5,4'-Trimethoxystilbene on Glutamate-Induced Cytotoxicity, Heme Oxygenase-1, and Sirtuin 1 in HT22 Neuronal Cells

  • Kim, Dae-Won;Kim, Young-Mi;Kang, Sung-Don;Han, Young-Min;Pae, Hyun-Ock
    • Biomolecules & Therapeutics
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    • v.20 no.3
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    • pp.306-312
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    • 2012
  • Resveratrol (trans-3,5,4'-trihydroxystilbene) has received considerable attention recently for the potential neuroprotective effects in neurodegenerative disorders where heme oxygenase-1 (HO-1) and sirtuin 1 (SIRT1) represent promising therapeutic targets. Resveratrol has been known to increase HO-1 expression and SIRT1 activity. In this study, the effects of resveratrol and trans-3,5,4'-trimethoxystilbene (TMS), a resveratrol derivative, on cytotoxicity caused by glutamate-induced oxidative stress, HO-1 expression, and SIRT1 activation have been investigated by using murine hippocampal HT22 cells, which have been widely used as an in vitro model for investigating glutamate-induced neurotoxicity. Resveratrol protected HT22 neuronal cells from glutamate-induced cytotoxicity and increased HO-1 expression as well as SIRT1 activity in a concentration-dependent manner. Cytoprotection afforded by resveratrol was partially reversed by the specific inhibition of HO-1 expression by HO-1 small interfering RNA and the nonspecific blockage of HO-1 activity by tin protoporphyrin IX, but not by SIRT1 inhibitors. Surprisingly, TMS, a resveratrol derivative with methoxyl groups in lieu of the hydroxyl groups, and trans-stilbene, a non-hydroxylated analog, failed to protect HT22 cells from glutamate-induced cytotoxicity and to increase HO-1 expression and SIRT1 activity. Taken together, our findings suggest that the cytoprotective effect of resveratrol was at least in part associated with HO-1 expression but not with SIRT1 activation and, importantly, that the presence of hydroxyl groups on the benzene rings of resveratrol appears to be necessary for cytoprotection against glutamate-induced oxidative stress, HO-1 expression, and SIRT1 activation in HT22 neuronal cells.

Antinociceptive Effect and the Mechanism of Bee Venom Pharmacopuncture on Inflammatory Pain in the Rat Model of Collagen-induced Arthritis: Mediation by 5HT-3 & Muscarinic Cholinergic Receptors (Collagen-induced Arthritis Rat Model에서 염증성 통증에 대한 봉독약침의 진통효과 및 기전연구: 5HT-3 & Muscarinic Cholinergic Mechanisms에 대한 연구)

  • Seo, Byung-Kwan;Park, Dong-Suk;Baek, Yong-Hyeon
    • Journal of Acupuncture Research
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    • v.28 no.1
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    • pp.37-44
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    • 2011
  • 배경 및 목적 : 봉독약침요법(bee venom pharmacopuncture, BVP)은 rheumatoid arthritis(RA)의 치료에 활용되고 있으나, RA로 인한 염증성 통증에 대한 봉독약침의 진통효과와 specific mechanism은 아직까지 명확하게 밝혀지지 않았다. 이에 본 연구에서는 RA animal model로서 collagen-induced arthritis(CIA) rat model에서 봉독약침의 a1-adrenergic, 5HT-3 그리고 muscarinic cholinergic mechanism을 확인하고자 한다. 방법 : CIA를 유도하기 위하여 male Sprague-Dawley rat에 freund's incomplete adjuvant에 유화(乳化)시킨 bovine type II collagen을 주입하고 14일 후 booster injection 시행하였다. 진통효과는 tail flick latency (TFL)로 평가하였다. 결과 : 관절염의 유도 이후 염증성 통증 역치는 시간이 지나면서 낮아지며, 5주 이후로는 통증 역치에 큰 변화가 없이 유지되었다. 첫 번째 immunization으로부터 5주 경과 후 족삼리($ST_{36}$)에 봉독약침처치(0.25 mg/ kg)를 시행하여 유의한 진통효과를 관찰하였다. 또한 봉독약침의 진통효과는 ondansetron(5HT-3 receptor antagonist, 0.5mg/kg, i.p.), atropine(muscarinic cholinergic receptor antagonist, 1mg/kg, i.p.)의 전처치에 의하여 억제되었으나, prazosin(a1-adrenergic receptor antagonist, 1mg/kg, i.p.)의 전처치에 의해서는 억제되지 않았다. 결론 : 봉독약침은 CIA로 인한 염증성 통증에 유의한 진통효과를 나타내며 그 analgesic mechanism은 5HT-3와 muscarinic cholinergic receptor에 의하여 매개되며 a1-adrenergic receptor에 의하여 매개되지는 않았다.