• Title/Summary/Keyword: dual action

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Nefopam Reduces Dysesthesia after Percutaneous Endoscopic Lumbar Discectomy

  • Ok, Young Min;Cheon, Ji Hyun;Choi, Eun Ji;Chang, Eun Jung;Lee, Ho Myung;Kim, Kyung Hoon
    • The Korean Journal of Pain
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    • v.29 no.1
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    • pp.40-47
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    • 2016
  • Background: Neuropathic pain, including paresthesia/dysesthesia in the lower extremities, always develops and remains for at least one month, to variable degrees, after percutaneous endoscopic lumbar discectomy (PELD). The recently discovered dual analgesic mechanisms of action, similar to those of antidepressants and anticonvulsants, enable nefopam (NFP) to treat neuropathic pain. This study was performed to determine whether NFP might reduce the neuropathic pain component of postoperative pain. Methods: Eighty patients, who underwent PELD due to herniated nucleus pulposus (HNP) at L4-L5, were randomly divided into two equal groups, one receiving NFP (with a mixture of morphine and ketorolac) and the other normal saline (NS) with the same mixture. The number of bolus infusions and the infused volume for 3 days were compared in both groups. The adverse reactions (ADRs) in both groups were recorded and compared. The neuropathic pain symptom inventory (NPSI) score was compared in both groups on postoperative days 1, 3, 7, 30, 60, and 90. Results: The mean attempted number of bolus infusions, and effective infused bolus volume for 3 days was lower in the NFP group for 3 days. The most commonly reported ADRs were nausea, dizziness, and somnolence, in order of frequency in the NFP group. The median NPSI score, and all 5 median sub-scores in the NFP group, were significantly lower than that of the NS group until postoperative day 30. Conclusions: NFP significantly reduced the neuropathic pain component, including paresthesia/dysesthesia until 1 month after PELD. The common ADRs were nausea, dizziness, somnolence, and ataxia.

The Perception of Teenagers on the Bully - With the subject of primary, middle and high school students - (학교청소년이 지각하는 집단 따돌림에 관한 연구 -초.중.고등학생을 대상으로-)

  • 정혜경;김경희
    • Journal of Korean Academy of Nursing
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    • v.30 no.1
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    • pp.137-147
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    • 2000
  • The purpose of this study was to investigate characteristics of teenagers' perceptions to bullies according to the classification types of Q-methodology. The results of the analysis were classified in 5 types. Type 1, which was the type geared foward solution, showed that they expressed a strong attitude of sympathy and protection towards the victim. However, they had harbored rage and hostile feelings against the assaulter. For example, when they witnessed the bully in action, they positively intervened in the situation. Type 2, which was the observer type, showed that they thought the victims were to blame for their misfortune. Also, when a friend who was left out in the cold by his classmates, they were just watched without showing any special interest. Type 3, which was the type of conflict, indicated that they believed that the both the victim and the assaulter should have responsibility. In contrast to the previous type, they had sympathy for the friend who was left out in the cold by his classmates, they had the dual feeling that intended to use the bully under the situation with his friend. Type 4, which was the type of assenting, indicated that they assumed an indifferent attitude to the situation, while they implied assenting to the situation of the friend who had a bad relationship with them. Type 5, which was the negative type, showed that they had the negative view to the situation of bully itself so that they did not recognize the bully as the method of revenge for whatever reason. The results of the study showed that the bully increased the factor of stress to school life of the victim or assaulter, even in the subjective position. The perception of the bully should change according to the characteristics of the types of people and it is necessary to study how to cope with the situations.

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Pharmacological Action of Panax Ginseng on the Behavioral Toxicities Induced by Psychotropic Agents

  • Kim Hyoung-Chun;Shin Eun-Joo;Jang Choon-Gon;Lee Myung-Koo;Eun Jae-Soon;Hong Jin-Tae;Oh Ki-Wan
    • Archives of Pharmacal Research
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    • v.28 no.9
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    • pp.995-1001
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    • 2005
  • Morphine-induced analgesia has been shown to be antagonized by ginseng total saponins (GTS), which also inhibit the development of analgesic tolerance to and physical dependence on morphine. GTS is involved in both of these processes by inhibiting morphine-6-dehydrogenase, which catalyzes the synthesis of morphinone from morphine, and by increasing the level of hepatic glutathione, which participates in the toxicity response. Thus, the dual actions of ginseng are associated with the detoxification of morphine. In addition, the inhibitory or facilitated effects of GTS on electrically evoked contractions in guinea pig ileum (I-L-receptors) and mouse vas deferens $(\delta-receptors)$ are not mediated through opioid receptors, suggesting the involvement of non-opioid mechanisms. GTS also attenuates hyperactivity, reverse tolerance (behavioral sensitization), and conditioned place preference induced by psychotropic agents, such as methamphetamine, cocaine, and morphine. These effects of GTS may be attributed to complex pharmacological actions between dopamine receptors and a serotonergic/adenosine $A_{2A}1\delta-opioid$ receptor complex. Ginsenosides also attenuate the morphine-induced cAMP signaling pathway. Together, the results suggest that GTS may be useful in the prevention and therapy of the behavioral side effects induced by psychotropic agents.

3 Dimensional Mobile Phone Internal Antenna Using the Helix Element (헤릭스를 이용한 3차원 구조의 휴대폰 내장형 안테나)

  • Hong, Min-Gi;Son, Tae-Ho
    • The Journal of Korean Institute of Electromagnetic Engineering and Science
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    • v.19 no.8
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    • pp.906-912
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    • 2008
  • We designed and implemented a 3-dimensional structure internal antenna which has volume less than 1.5 cc for mobile phone to improve efficiency and gain. Multiple bending for the resonance of small internal antenna derives reduction of gain due to cancellation of antenna current. In this study, the current cancelation was reduced by the minimization of antenna bending. And the helix element was applied for the purpose both compensation of short antenna length and action of radiation element. For the verification of this study, a 1.5 cc volume 3D antenna which was fabricated by the press method applied to the dual band mobile phone. Measurement showed that efficiencies and gains under the slide down and up were 27.73 %, 0.29 dBi for the GSM band and 46.84 %, 2.27 dBi for the USPCS band, and had good performance under the small antenna volume. H-plane radiation pattern showed omnidirectional for the both band.

Anti-inflammatory Effect of Ribes fasciculatum in IFN-${\gamma}$/LPS-stimulated Mouse Peritoneal Macrophage

  • Kim, Jin Kyu;Kim, Ha Na;Kang, Chung Sik;Seo, Je Han;Seo, Hyun Won;Im, Jun Sang;Kim, Bong Seok;Cha, Dong Seok;Kwon, Jin;Oh, Chan Ho;Ma, Sang Yong;Nam, Jung Il;Jeon, Hoon
    • Natural Product Sciences
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    • v.20 no.2
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    • pp.113-118
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    • 2014
  • Ribes fasciculatum which belongs to Saxifragaceae has been widely used as a traditional medicine for the treatment of symptoms associated with lacquer poison. However, pharmacological studies on the R. fasciculatum are extremely limited until now. Thus, in this study, we evaluated the possible anti-inflammatory effects of ethyl acetate fraction of R. fasciculatum (ERF) using IFN-${\gamma}$/LPS-stimulated peritoneal macrophage model. We investigated the change in nitrite level in the absence or presence of ERF after LPS stimulation, and we found that ERF effectively attenuates the NO production in a dose dependent manner without notable toxicity. To determine the mechanism of the inhibitory action of ERF on NO production, we performed iNOS enzyme activity assay and Western blotting. Here we showed that both of iNOS enzyme activities and iNOS expressions were significantly down-regulated by ERF, indicating that these dual activities of ERF are responsible for ERF-mediated NO suppression. In addition, ERF inhibitied the expression of cyclooxygenase-2 (COX-2), an another key enzyme in inflammation through suppression of NF-${\kappa}B$ activation. We also tested anti-inflammatory properties of ERF not only in vitro, but in vivo using trypsin-induced paw edema model in mice. Our results revealed that the increased paw volume in response to trypsin injection was recovered by ERF supplement dose dependently.

YH18968, a Novel 1,2,4-Triazolone G-Protein Coupled Receptor 119 Agonist for the Treatment of Type 2 Diabetes Mellitus

  • Han, Taedong;Lee, Byoung Moon;Park, Yoo Hoi;Lee, Dong Hoon;Choi, Hyun Ho;Lee, Taehoon;Kim, Hakwon
    • Biomolecules & Therapeutics
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    • v.26 no.2
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    • pp.201-209
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    • 2018
  • G protein-coupled receptor 119 (GPR119) is expressed in the pancreas and gastrointestinal tract, and its activation promotes insulin secretion in the beta cells of the pancreatic islets as well as the secretion of glucagon-like peptide-1 (GLP-1) in intestinal L cells, consequently improving glucose-stimulated insulin secretion. Due to this dual mechanism of action, the development of small-molecule GPR119 agonists has received significant interest for the treatment of type 2 diabetes. We newly synthesized 1,2,4-triazolone derivatives of GPR119 agonists, which demonstrated excellent outcomes in a cyclic adenosine monophosphate (cAMP) assay. Among the synthesized derivatives, YH18968 showed cAMP=2.8 nM; in GLUTag cell, GLP-1secretion=2.3 fold; in the HIT-T15 cell, and insulin secretion=1.9 fold. Single oral administration of YH18968 improved glucose tolerance and combined treatment with a dipeptidyl peptidase 4 (DPP-4) inhibitor augmented the glucose lowering effect as well as the plasma level of active GLP-1 in normal mice. Single oral administration of YH18968 improved glucose tolerance in a diet induced obese mice model. This effect was maintained after repeated dosing for 4 weeks. The results indicate that YH18968 combined with a DPP-4 inhibitor may be an effective therapeutic candidate for the treatment of type 2 diabetes.

An Experiment on the Culture of Laver, Porphgra tenera, on the 'Sae-ol-bal' (triple-knotted blind) Laver Bed (세올발에 의한 김 양식시험)

  • KOH Nam-Pyo;PARK Chong Hong
    • Korean Journal of Fisheries and Aquatic Sciences
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    • v.1 no.1
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    • pp.19-30
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    • 1968
  • An experiment on the culture of laver, Porphyra tenera, was carried out from September 26, 1965 to February 12, 1966 at a laver farm on the coast of Gae-do, Hwacheong-myeon, Yeocheon-gun, Jeonranam-do, using 'Sae-ol-bal' (triple-knotted blind) laver bed, resulting in the following data: 1. 'Sae-ol-bal' laver, bed was less destroyed compared to ordinary (dual knotted blind) laver bed, the destruction rate being $9.8\%$ in 'Sae-ol-bal' laver bed, while $35.3\%$ in ordinary laver bed (Table 5). 2. The quantity of laver yield is the greatest on the edge-part, the next on the basal part, and the smallest on the middle part of the 'Sae-ol-bal' laver bed (Table 6, Figs. $7\~8$). 3. The ordinary laver bed may yield better harvest on the calm farm but 'Sae-ol-bal' laver bed yields better harvest at a farm where the destruction of bed is remarkable by wind and wave action.

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Preparation and Characterization of Self-assembled Glycol Chitosan Hydrogels Containing Palmityl-acylated Exendin-4 for Extended Hypoglycemic Action

  • Lee, Ju-Ho;Lee, Chang-Kyu;Bae, Sung-Ho;Yoon, Jeong-Hyun;Choi, Eun-Joo;Oh, Kyung-Taek;Lee, Eun-Seong;Lee, Kang-Choon;Youn, Yu-Seok
    • Journal of Pharmaceutical Investigation
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    • v.41 no.3
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    • pp.173-178
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    • 2011
  • Injectable chitosan hydrogels have attracted great potential due to sustained-release property and safety. Here, palmityl-acylated glycol chitosan (Pal-GC) was used to generate physically cross-linked hydrogels by virtue of hydrophobic attraction of linear fatty carbons. Glycol chitosan was chemically modified with N-hydroxysuccinimide-activated palmitic acid in dimethylsulfoxide (DMSO) containing dimethylaminopyridine. Through a series of preparation steps of (i) dialysis with DMSO, (ii) addition of palmityl-acylated exendin-4 (Ex4-C16), and (iii) dialysis with water, Pal-GC was self-assembled to form physically cross-linked hydrogels entrapped with Ex4-C16. The Pal-GC derivative was analyzed by using 1H NMR, and the surface morphology of Pal-GC hydrogels formed was examined by scanning electron microscopy. Also, the hypoglycemic effect induced by Pal-GC hydrogels containing Ex4-C16 (250 nmol/kg) was evaluated in non-fasted type 2 diabetic db/db mice and compared with GC hydrogels containing native Ex4 at the same dose. Results showed that palmityl group was successfully conjugated with the amines of glycol chitosan, and that Pal-GC efficiently generated the hydrogels formation. Moreover, Pal-GC hydrogels containing Ex4-C16 was found to greatly prolong the hypoglycemia duration (~ 4 days). This was due to the dual-functions of the palmityl groups present in both GC and exendin-4 such as hydrophobic attraction and plasma albumin-binding. We consider this new type of self-assembled GC hydrogels loaded with Ex4-C16 would be a promising long-acting sustained-release system with anti-diabetic property.

Dietary Aloe Improves Insulin Sensitivity via the Suppression of Obesity-induced Inflammation in Obese Mice

  • Shin, Eun-Ju;Shim, Kyu-Suk;Kong, Hyun-Seok;Lee, Sung-Won;Shin, Seul-Mee;Kwon, Jeung-Hak;Jo, Tae-Hyung;Park, Young-In;Lee, Chong-Kil;Kim, Kyung-Jae
    • IMMUNE NETWORK
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    • v.11 no.1
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    • pp.59-67
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    • 2011
  • Background: Insulin resistance is an integral feature of metabolic syndromes, including obesity, hyperglycemia, and hyperlipidemia. In this study, we evaluated whether the aloe component could reduce obesity-induced inflammation and the occurrence of metabolic disorders such as blood glucose and insulin resistance. Methods: Male C57BL/6 obese mice fed a high-fat diet for 54 days received a supplement of aloe formula (PAG, ALS, Aloe QDM, and Aloe QDM complex) or pioglitazone (PGZ) and were compared with unsupplemented controls (high-fat diet; HFD) or mice fed a regular diet (RD). RT-PCR and western blot analysis were used to quantify the expression of obesity-induced inflammation. Results: Aloe QDM lowered fasting blood glucose and plasma insulin compared with HFD. Obesity-induced inflammatory cytokine (IL-$1{\beta}$, -6, -12, TNF-${\alpha}$) and chemokine (CX3CL1, CCL5) mRNA and protein were decreased markedly, as was macrophage infiltration and hepatic triglycerides by Aloe QDM. At the same time, Aloe QDM decreased the mRNA and protein of $PPAR{\gamma}/LXR{\alpha}$ and $11{\beta}$-HSD1 both in the liver and WAT. Conclusion: Dietary aloe formula reduces obesity-induced glucose tolerance not only by suppressing inflammatory responses but also by inducing anti-inflammatory cytokines in the WAT and liver, both of which are important peripheral tissues affecting insulin resistance. The effect of Aloe QDM complex in the WAT and liver are related to its dual action on $PPAR{\gamma}$ and $11{\beta}$-HSD1 ression and its use as a nutritional intervention against T2D and obesity-related inflammation is suggested.

Physicochemical Properties, Stabilities and Pharmacokinetics of Cephalosporin 3'-Quinolone Dithiocarbamate (세팔로스포린 3'-퀴놀론의 물리화학적 성질, 안정성 및 체내약물동태)

  • 나성범;공재양;김완주;지웅길
    • YAKHAK HOEJI
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    • v.37 no.6
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    • pp.638-646
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    • 1993
  • A cepfialosporin with an aminothiazoiylmethoxyimino-type side chain at the 7 position and bicyclic quinolone dithicarbamate at the 3' position was synthesized. It has broad and potent antivacterial activity in vitro. The antibacterial spectrum reflects contributions of both the cephalosporin moiety and the quinolone moiety. Thus, this compound was named DACD implying a dualaction cephalosporin derivative. In this paper, the physicochemical proper-ties (lipid-water partition, pKa), stability and pharmacokinetics of DACD were determined and compared with cefotaxime 3'-norfloxacin dithiocarbamate (CENO). Stability tests were studied in pH 1.20, 6.80 and 8.00 buffers and in the presence of AB type human plasma, rat liver homogenate and its .betha.-lactamase. The pharmacokinetic parameters of DACD were evaluated in mice after a single intravenous dose of 40 mg/kg. The results are as follows. The lipid-water partition coefficient of DACD was higher than that of CENO. The calculated pKa values of CENO and DACD, were 6.82$\pm$0.03, 7.53$\pm$0.21, respectively. In the hydrolysis test, half-lives (t$^{1/2}$) of CENO and DACD was 66.0 hr and 80.0 hr in pH 6.80 buffer, 190 hr and 91.4 hr in pH 8.00 buffer. CENO and DACD were rapidly hydrolyzed in human plasma and in rat liver hornogenate. Half-lives (t$_{1/2}$ of CENO and DACD were 1.29 hr and 1.15 hr in hyman plasma, 0.62 hr and 0.71 hr rat liver homogenate. In $\beta$-lactamase stability test, CENO and DACD were very stable to the .betha.-lactamases obtained from three different strains. Half-life (t$_{1/2}$) and areas under the curve (AUC) in mice were 2.33 hr and 15.97 (mg.h/1), respectively.

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