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Quercetin Inhibits the 5-Hydroxytryptamine Type 3 Receptor-mediated Ion Current by Interacting with Pre-Transmembrane Domain I

  • Lee, Byung-Hwan;Jung, Sang-Min;Lee, Jun-Ho;Kim, Jong-Hoon;Yoon, In-Soo;Lee, Joon-Hee;Choi, Sun-Hye;Lee, Sang-Mok;Chang, Choon-Gon;Kim, Hyung-Chun;Han, YeSun;Paik, Hyun-Dong;Kim, Yangmee;Nah, Seung-Yeol
    • Molecules and Cells
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    • v.20 no.1
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    • pp.69-73
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    • 2005
  • The flavonoid, quercetin, is a low molecular weight substance found in apple, tomato and other fruit. Besides its antioxidative effect, quercetin, like other flavonoids, has a wide range of neuropharmacological actions including analgesia, and motility, sleep, anticonvulsant, sedative and anxiolytic effects. In the present study, we investigated its effect on mouse 5-hydroxytryptamine type 3 ($5-HT_{3A}$) receptor channel activity, which is involved in pain transmission, analgesia, vomiting, and mood disorders. The $5-HT_{3A}$ receptor was expressed in Xenopus oocytes, and the current was measured with the two-electrode voltage clamp technique. In oocytes injected with $5-HT_{3A}$ receptor cRNA, quercetin inhibited the 5-HT-induced inward peak current ($I_{5-HT}$) with an $IC_{50}$ of $64.7{\pm}2.2{\mu}M$. Inhibition was competitive and voltage-independent. Point mutations of pre-transmembrane domain 1 (pre-TM1) such as R222T and R222A, but not R222D, R222E and R222K, abolished inhibition, indicating that quercetin interacts with the pre-TM1 of the $5-HT_{3A}$ receptor.

Effects of Verapamil on Norepinephrine-, Phenylephrine- and Clonidine-induced Pressor Response in Rabbits and Rats (가토(家兎) 및 Rat에서 Norepinephrine, Phenylephrine 및 Clonidine의 승압반응(昇壓反應)에 대한 Verapamil의 영향(影響))

  • Shin, Dong-ho;Choi, Soo-hyung
    • Korean Journal of Veterinary Research
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    • v.28 no.1
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    • pp.29-36
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    • 1988
  • To examine the selectivity of verapamil, used in the cardiovascular diseases, on alpha-1 and alpha-2 adrenoceptor-induced pressor rsponses, effects of verapamil on alpha-adrenoceptor agonist-induced pressor responses were investigated in urethane-anesthetized rabbits, spinal rabbits, rats and pithed rats. To evaluate the effects of verapamil on each pressor response induced by norepinephrine, phenylephrine and clonidine, these agonists were previously injected into a ear vein, and then same procedures were performed 1~2 min after treatment with intravenous verapamil. The results are summarized as follows: 1. Intravenous verapamil produced dose-dependent depressor response in rabbits and rats. 2. Pressor responses to intravenous norepinephrine($10{\mu}g/kg$) and phenylphrine($30{\mu}g/kg$) were inhibited by pretreatment with intravenous verapamil in rabbits and no difference was noted between the degree of both inhibitions of the pressor response by verapamil. 3. Pressor responses to intravenous norepinephrine($3{\mu}g/kg$), phenylephrine($20{\mu}g/kg$) and clonidine ($300{\mu}g/kg$) were inhibited by pretreatment with intravenous verapamil in spinal rabbits. No difference was noted between the inhibition of norepinephrine-induced pressor response and that of phenylephrine-induced pressor response by verapamil. The inhibition of clonidine-induced pressor response by verapamil was more prominent than that of norepinephrine- or phenylephrine-induced pressor response. 4. Pressor responses to intravenous norepinephrine($3{\mu}g/kg$) and phenylephrine($10{\mu}g/kg$) were inhibited by pretreatment with intravenous verapairlil in rats and no difference was noted between the degree of both inhibitions of the pressor response by verapamil. 5. Pressor responses to intravenous norepinephrine ($3{\mu}g/kg$), phenylephrine($30{\mu}g/kg$) and clonidine($100{\mu}g/kg$) were inhibited by pretreatment with intravenous verapamil in pithed rats. No difference was noted between the inhibition of norepinephrine-induced pressor response and that of phenylephrine-induced pressor response by verapamil. The inhibition of clonidine-induced pressor response by verapamil was more prominent than that of norepinephrine- or phenylephrine-induced pressor response. These results suggest that verapamil significantly inhibits both pressor responses mediated by alpha-1 and alpha-2 adrenoceptors and the inhibition is greater in alpha-2 adrenoceptor-induced response than in alpha-1 adrenoceptor-induced one, and calcium channel takes part in the process of the pressor response mediated by alpha-1 adrenoceptors as well as alpha-2 adrenoceptors.

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The Development of a Continuing Nursing Care Program for Cancer Patients after Discharge (암환자의 퇴원후 계속 간호 프로그램 개발)

  • Kwon, In-Soo;Eun, Young
    • Journal of Korean Academy of Nursing
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    • v.31 no.1
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    • pp.81-93
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    • 2001
  • The purpose of this study was to develop a continuing nursing care program for cancer patients and the caregivers staying at their home and to test its effects on patients' symptom distress, caregiver burden, and satisfaction of life. The continuing nursing care program was based on the homecare needs of cancer patients, and was provided by three clinical nurses who took care of the patients while they were hospitalized. The program consisted of discharge education about selfcare using education materials(book and handout) and provisions of direct care. These were counselling and education during which visiting patients' home one week after discharge and telephone counseling two weeks after discharge. Counseling by telephone was always available during the research period. A quasi-experimental research design was used to test the effects of the program. Subjects for this study were 53 cancer patients discharged from the hospital and caregivers. These subjects were assigned to an experimental group (n=23) receiving continuous nursing care, or to a control group (n=30) not receiving continuous nursing care. Data from control group was collected first to protect from contamination. Data collection was done from October of 1998 to February of 2000. The collected data was analysed using mean, t-test, and chi-square test computed by SPSS software. The summary of results was as follows: 1) The symptom distress was a little decreased at posttest, but there were no significant differences between the experimental and the control group in symptom distress. 2) The score of caregiver burden was significantly decreased in experimental group at posttest, but no differences in control group. 3) There were no significant differences between the experimental and control group in the satisfaction of life. 4) The score of satisfaction of continuing nursing care program in experimental group at posttest was 2.321 of 3. In conclusion, even though this study did not obtain evidence of effectiveness of continuing nursing care program on patients, such as. It is still expected to be effective by a more improved program. Therefore we want to give some suggestions for further studies. 1) It is needed to make a communication channel with the patient's doctor to response promptly and appropriately to patient's conditions. 2) The research is necessary on patients in terminal stage or early stage of cancer diagnosis who have many nursing needs. 3) It is needed to readjust the roles and job assignment of clinical nurse to implement effectively as a program provider.

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A Research on the Navigation of Northern Sea Route According to Safety of Vessel and Crews (선박 및 선원의 인명 안전을 고려한 북극해 항로 운항 연구)

  • Kim, Won-Ouk;Youn, Dae-Gwun;Park, Woe-Chul
    • Journal of the Korean Society of Marine Environment & Safety
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    • v.21 no.1
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    • pp.40-46
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    • 2015
  • Arctic Ocean has rapidly melted due to global warming, by this, commercial ship has been operating through the area. Reason to develop the Northern Sea Route(NSR) even in extreme conditions, the distance than the existing route is shortened, which bring economic benefits. For these reason, the International Maritime Organization(IMO) established safety standards of the Arctic navigation(Polar Code) in order to ensure safe operation in the Northern Sea Route. In this study, it has been described ice types and safety standards of Artic vessel what officer needs to know for safe navigation on the Arctic Ocean. And It was verified by simulation the theoretical knowledge for the safe operation of the Arctic vessel. As a result, it was found that ship needs to reduce speed and analyze ice for safe operation before enter into the ice, it is necessary to enter at right angle to break ice safety and efficiently. Also according to the result of the simulation of navigation entering in ice channel(Lead), it was difficult to change course, it is believed that require emergency training for passing Vessel. In the future, It shall be analyzed precisely under various conditions of scenario.

Experimental Study of Performance of PEMFC Operated in Dead-End Mode (수소극 Dead-End 모드 고분자 전해질 연료전지의 실험적 연구)

  • Ji, Sang-Hoon;Hwang, Yong-Sheen;Choi, Jong-Won;Lee, Dae-Young;Park, Joon-Ho;Jang, Jae-Hyuk;Kim, Min-Soo;Cha, Suk-Won
    • Transactions of the Korean Society of Mechanical Engineers B
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    • v.34 no.6
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    • pp.643-648
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    • 2010
  • Portable fuel cells are commonly operated in the dead-end mode because of such as high fuel utilization. However, the performance of such systems deteriorates continuously with an increase in the amount of by-products such as water vapor and nitrogen. In this study, to verify the effect of water vapor on Proton Exchange Membrane Fuel Cells (PEMFCs), constant-load experiments were carried out for a current density of 600 mA/cm2 and a voltage of 0.4 V, respectively. The performance of the cell was more stable under constant voltage conditions than under constant current density conditions. Condensed water accumulated in the anode channel near the cell outlet. The experimental results show how the relative humidity (RH = 0.15, 0.4 and 0.75) of air at the cathode side affect the performance of PEMFCs with dead-end anode. At RH values higher than 0.15, the mean power density increased by up to 51% and the mean purge duration decreased by up to 25% compared to the corresponding initial values.

[$Ca^{2+}$ Sensitization Mechanism in Stretch-induced Myogenic Tone

  • Kim, Jung-Sup;Ryu, Sung-Kyung;Ahn, Duck-Sun;Kang, Bok-Soon;Lee, Young-Ho
    • The Korean Journal of Physiology and Pharmacology
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    • v.6 no.1
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    • pp.33-39
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    • 2002
  • It has been suggested that $Ca^{2+}$ sensitization mechanisms might contribute to myogenic tone, however, specific mechanisms have not yet been fully identified. Therefore, we investigated the role of protein kinase C (PKC)- or RhoA-induced $Ca^{2+}$ sensitization in myogenic tone of the rabbit basilar vessel. Myogenic tone was developed by stretch of rabbit basilar artery. Fura-2 $Ca^{2+}$ signals, contractile responses, PKC immunoblots, translocation of PKC and RhoA, and phosphorylation of myosin light chains were measured. Stretch of the resting vessel evoked a myogenic contraction and an increase in the intracellular $Ca^{2+}$ concentration $([Ca^{2+}]_i)$ only in the presence of extracellular $Ca^{2+}$. Stretch evoked greater contraction than high $K^+$ at a given $[Ca^{2+}]_i.$ The stretch-induced increase in $[Ca^{2+}]_i$ and contractile force were inhibited by treatment of the tissue with nifedipine, a blocker of voltage-dependent $Ca^{2+}$ channel, but not with gadolinium, a blocker of stretch-activated cation channels. The PKC inhibitors, H-7 and calphostin C, and a RhoA-activated protein kinase (ROK) inhibitor, Y-27632, inhibited the stretch-induced myogenic tone without changing $[Ca^{2+}]_i.$ Immunoblotting using isoform-specific antibodies showed the presence of $PKC_{\alpha}$ and $PKC_{\varepsilon}$ in the rabbit basilar artery. $PKC_{\alpha},$ but not $PKC_{\varepsilon},$ and RhoA were translocated from the cytosol to the cell membrane by stretch. Phosphorylation of the myosin light chains was increased by stretch and the increased phosphorylation was blocked by treatment of the tissue with H-7 and Y-27632, respectively. Our results are consistent with important roles for PKC and RhoA in the generation of myogenic tone. Furthermore, enhanced phosphorylation of the myosin light chains by activation of $PKC_{\alpha}$ and/or RhoA may be key mechanisms for the $Ca^{2+}$ sensitization associated with myogenic tone in basilar vessels.

Characterization of Asian dust using steric mode of sedimentation field-flow fractionation (Sd/StFFF) (Steric 모드의 침강장-흐름 분획법을 이용한 황사의 특성분석)

  • Eum, Chul Hun;Kim, Bon Kyung;Kang, Dong Young;Lee, Seungho
    • Analytical Science and Technology
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    • v.25 no.6
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    • pp.476-482
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    • 2012
  • Asian dust particles are known to have sizes ranging from a few nanometers up to about a few micrometers. The environmental and health effects depend on the size of the dust particles. The smaller, the farther they are transported, and the deeper they penetrate into the human respiratory system. Sedimentation field-flow fractionation (SdFFF) provides separation of nano to microparticles using a combination of centrifugal force and parabolic laminar flow in a channel. In this study, the steric mode of SdFFF (Sd/StFFF) was tested for size-based separation and characterization of Asian dust particles. Various SdFFF experimental parameters including flow rate, stop-flow time and field strength of the centrifugal field were optimized for the size analysis of Asian dust. The Sd/StFFF calibration curve showed a good linearity with $R^2$ value of 0.9983, and results showed an excellent capability of Sd/StFFF for a size-based separation of micron-sized particles.The optical microscopy (OM) was also used to study the size and the shape of the dust particles. The size distributions of the samples collected during a thick dust period were shifted towards larger sizes than those of the samples collected during thin dust periods. It was also observed that size distribution of the sample collected during dry period shifts further towards larger sizes than that of the samples collected during raining period, suggesting the sizes of the dust particle decrease during raining periods as the components adsorbed on the surface of the dust particles were removed by the rain water. Results show Sd/StFFFis a useful tool for size characterization of environmental particles such as the Asian dust.

Retrieval of Atmospheric Optical Thickness from Digital Images of the Moon (월면 디지털 영상 분석을 이용한 대기 광학두께 산출)

  • Jeong, Myeong-Jae
    • Korean Journal of Remote Sensing
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    • v.29 no.5
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    • pp.555-568
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    • 2013
  • Atmospheric optical thickness during nighttime was estimated in this study using analysis on the images of the moon taken from commercial digital camera. Basically the Langely Regression method was applied to the observations of the moon for the cloudless and optically stable sky conditions. The spectral response functions for the red(R), green(G), and blue(B) channels were employed to derive effective wavelength centers of each channel for the observations of the moon, and the correspondent Rayleigh optical thickness were also calculated. Aerosol optical thickness (AOT) was calculated by subtracting Rayleigh optical thickness from the atmospheric optical thickness derived from the Langley regression method. As there are only handful of nighttime AOT observations, the AOT from the moon observations was compared with the AOT from sun-photometers and the MODIS satellite sensor, which was taken several hours before the moon observations of this study. As a result, the values of AOT from moon observations agree with those from sun-photometers and MODIS within 0.1 for the R, G, B channels of the digital camera. On the other hand, ${\AA}$ngstr$\ddot{o}$m Exponent seems to be subject to larger errors due to its sensitiveness to the spectral errors of AOT. Nevertheless, the results of this study indicate that the method reported in this study is promising as it can provide nighttime AOT relatively easily with a low cost instrument like digital camera. More observations and analyses are warranted to attain improved nighttime AOT observations in the future.

Actions of acetylcholine, norepinephrine, histamine and prostaglandin F2α on motility of pig oviductal isthmic smooth muscle (돼지 난관협부 평활근의 운동성에 대한 acetylcholine, norepinephrine, histamine 및 prostaglandin F2α의 작용)

  • Rho, Gyu-jin;Park, Sang-eun;Shim, Cheol-soo;Kim, Joo-heon;Choe, Sang-young
    • Korean Journal of Veterinary Research
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    • v.34 no.3
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    • pp.493-500
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    • 1994
  • The purpose of this study was to investigate the effects of neurotransmitters and the source of $Ca^{2+}$ in the effects of neurotransmitters on the motility of pig oviductal isthmic smooth muscle. The motility of the isolated smooth muscle was recorded by using physiological recording system. The results were summarized as follows; Acetylcholine, norepinephrine, histamine and prostaglandin $F_{2{\alpha}}(PGF_{2{\alpha}})$ caused the contraction and the contractile responses were increased in a dose-dependent manner from the concentration of $10^{-7}$ to $10^{-4}M$. The maximum contractility of acetylcholine, norepinephrine, histamine and $PGF_{2{\alpha}}$ was 65.99, 28.66, 83.99 and 47.33% of 100 mM K contraction, respectively. The contractile response induced by acetylcholine$(10^{-6}M)$ was completely blocked by the pretreatment with cholinergic receptor blocker, atropine$(10^{-6}M)$, the contractile response induced by norepinephrine$(10^{-5}M)$ was blocked by the pretreatment with ${\alpha}$-adrenergic receptor blocker, phentolamine$(10^{-6}M)$ but was not blocked and rather increased by the pretreatment with ${\beta}$-adrenergic receptor blocker. propranolol$(10^{-6}M)$, the contractile response induced by histamine$(10^{-6}M)$ was completely blocked by the pretreatment with $H_1$-histaminergic receptor blocker, pyrilamine$(10^{-6}M)$ but was increased by the pretreatment with $H_2$-histaminergic receptor blocker, cimetidine$(10^{-6}M)$. The contractile response induced by acetylcholine$(10^{-6}M)$, norepinephrine$(10^{-5}M)$ and histamine$(10^{-6}M)$ was weakly contracted response in $Ca^{2+}$-free medium, but the contractile response induced by $PGF_{2{\alpha}}(10^{-6}M)$ was disappeared. The contractile response induced by acetylcholine$(10^{-6}M)$, norepinephrine$(10^{-5}M)$ and histamine$(10^{-6}M)$ was powerfully depressed by the pretreatment with $Ca^{2+}$-channel blocker, verapamil$(10^{-5}M)$ but the contractile response induced by $PGF_{2{\alpha}}(10^{-6}M)$ was completely inhibited.

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Multiscale Modeling and Simulation of Direct Methanol Fuel Cell (직접메탄올 연료전지의 Multiscale 모델링 및 전산모사)

  • Kim, Min-Su;Lee, Young-Hee;Kim, Jung-Hwan;Kim, Hong-Sung;Lim, Tae-Hoon;Moon, Il
    • Membrane Journal
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    • v.20 no.1
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    • pp.29-39
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    • 2010
  • This study focuses on the modeling of DMFC to predict the characteristics and to improve its performance. This modeling requires deep understanding of the design and operating parameters that influence on the cell potential. Furthermore, the knowledge with reference to electrochemistry, transport phenomena and fluid dynamics should be employed for the duration of mathematical description of the given process. Considering the fact that MEA is the nucleus of DMFC, special attention was made to the development of mathematical model of MEA. Multiscale modeling is comprised of process modeling as well as a computational fluid dynamics (CFD) modeling. The CFD packages and process simulation tools are used in simulating the steady-state process. The process simulation tool calculates theelectrochemical kinetics as well as the change of fractions, and at the same time, CFD calculates various balance equations. The integrated simulation with multiscal modeling explains experimental observations of transparent DMFC.