• Title/Summary/Keyword: methyl ester

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Effect of Inhibitor of Nitric Oxide Synthesis on the Ischemic Reconditioning in Isolated Heart of Rat. (NO 억제제가 허혈전처치의 심장 보호효과에 미치는 영향)

  • 유호진;조은용
    • Journal of Chest Surgery
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    • v.29 no.8
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    • pp.807-815
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    • 1996
  • The protective effect of'ischemic preconditioning'on ischemid-reperfusion injury of heart has been reported in various animal species. but without known mechAnism in detail, In An attempt to investigate the cardioprotective mechanism of ischemic preconditioning, we examined the effects of nitric oxide(UO) synthesis in preconditioned heart of rat The isolated hearts perfused by Langendorfr's method were ex- posed to 30min global ischemia followed by 30min reperfusion with oxygenated Krebs-Henseleit(K-H) sol- ution. Ischemic preconditioning was performed with three episodes of Sm n ischemia and Smin repeyfusion before the induction of prolong ischemia(30min)-reperfusion(30min). Ischemic preconditioning prevented the depression of cardiac function(left ventricular pressure .K heart rate) observed in the ischemia- reperfusion hearts and reduced the release of lactate dehydrogenase during the reperfusion period. On electromicroscopic pictures, myocardial ultrastructures wore relatively well preserved in isthemic preconditioned hearts. N6_nitro-L-arginine methyl ester(L-NAME) an inhibitor of L-arginine citric oxide pathway, was infused at a rate O.Smllmin In a dose of 10mg kg-1 before the initial ischemic preconditioning. neither the protection of cardiac function nor the reduction of LDH releAse in ischemic preconditioning hearts was altered in the presence of added L-NAME On ultrastructural finding, the preservation of morphology in ischemic preconditioning heart was not change by the pretreatment of L-UAME. The failure of the WO synthesis inhibitor to reduce t e effect of ischemic preconditioning may be related to be species specific in that NO may allot be the trigger for ischemic preconditioning in rats.

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MLCK and PKC Involvements via Gi and Rho A Protein in Contraction by the Electrical Field Stimulation in Feline Esophageal Smooth Muscle

  • Park, Sun-Young;Shim, Jae-Ho;Kim, Mi-Na;Sun, Yih Hsiu;Kwak, Hyun-Soo;Yan, Xiangmei;Choi, Byung-Chul;Im, Chae-Uk;Sim, Sang-Soo;Jeong, Ji-Hoon;Kim, In-Kyeom;Min, Young-Sil;Sohn, Uy-Dong
    • The Korean Journal of Physiology and Pharmacology
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    • v.14 no.1
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    • pp.29-35
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    • 2010
  • We have shown that myosin light chain kinase (MLCK) was required for the off-contraction in response to the electrical field stimulation (EFS) of feline esophageal smooth muscle. In this study, we investigated whether protein kinase C (PKC) may require the on-contraction in response to EFS using feline esophageal smooth muscle. The contractions were recorded using an isometric force transducer. On-contraction occurred in the presence of $N^G$-nitro-L-arginine methyl ester (L-NAME), suggesting that nitric oxide acts as an inhibitory mediator in smooth muscle. The excitatory composition of both contractions was cholinergic dependent which was blocked by tetrodotoxin or atropine. The on-contraction was abolished in $Ca^{2+}$-free buffer but reappeared in normal $Ca^{2+}$-containing buffer indicating that the contraction was $Ca^{2+}$ dependent. 4-aminopyridine (4-AP), voltage-dependent $K^+$ channel blocker, significantly enhanced on-contraction. Aluminum fluoride (a G-protein activator) increased on-contraction. Pertussis toxin (a $G_i$ inactivator) and C3 exoenzyme (a rhoA inactivator) significantly decreased on-contraction suggesting that Gi or rhoA protein may be related with $Ca^{2+}$ and $K^+$ channel. ML-9, a MLCK inhibitor, significantly inhibited on-contraction, and chelerythrine (PKC inhibitor) affected on the contraction. These results suggest that endogenous cholinergic contractions activated directly by low-frequency EFS may be mediated by $Ca^{2+}$, and G proteins, such as Gi and rhoA, which resulted in the activation of MLCK, and PKC to produce the contraction in feline distal esophageal smooth muscle.

An Experimental Study of Effect on ECV 304 Cells, Platelet Rich Plasma and Rats treated with L-NAME by Ondamtang extract (온담탕이 고혈압 백서와 인간유래 혈관내피세포주(ECV 304)에 미치는 영향)

  • Baek Il-Sung;Park Chang-Gook;Lee So-Yeon;Yoon Hyeon-Deok;Sin Wo-Chul;Park Chi-Sang
    • Herbal Formula Science
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    • v.12 no.2
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    • pp.175-202
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    • 2004
  • Nitric oxide(NO) play an important role in normal and pathophysiological cells including as a messenger molecule, neurotransmitter, microbiocidal agent, or dilator of blood vessels and artheriosclerosis, hypertension, myocardial infarction, respectively. To investigate that Ondamtang in the potential contribution of the levels of nitric oxide generated by endothelial nitric oxide synthase (eNOS) and the mechanisms of protection against L-NAME, human ECV304 cells, which normally do not express eNOS, were expressed by L-NAME. L-NAME stimulated rat or cells were found to be resistant to injury and delayed death following the Ondam-tang. Inhibition of nitric oxide synthesis abolished the protective effect against L-NAME, thrombin and collagen exposure. Interestingly, such effects have bee observed during stimulation with agents such as KCl on L-NAME mediate rats, were damaged by the NOS inhibitor NG-nitro-L-arginine methyl ester (L-NAME). Cardiovascular diseases is one of the blood vessels and renin-angiotensin system dynfunction. So we studied on herbal medicine that have a relation of vessels endothelium necrosis. In Oriental Medicine, Ondam-tang has been used for disease in relation to cardiovascular system. We studied on the protection and inhibitory effects of cardiovascular diseases in L-NAME induced rat or ECV304 cell lines through the Cell morphological pattern, Tunel assay, LDH activity, heart rate, blood pressure and immunohistochemistric analysis by Ondam-tang. As the result of this study, In group, the anti-apoptosis and necrosis in the cardiovascular system have a potential capacity for prevented, protected and treating the diseases of cardiovascular system, against the necrosis of rat and ECV304 cells with eNOS and calpain expression by L-NAME is promoted.

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Ethanol Extract of Cynanchum wilfordii Produces Endothelium-Dependent Relaxation in Rat Aorta and Anti-inflammatory Activity in Human Aortic Smooth Muscle Cells

  • Choi, Deok-Ho;Lee, Yun-Jung;Kim, Eun-Joo;Li, Xiang;Kim, Hye-Yoom;Hwang, Sun-Mi;Yoon, Jung-Joo;Lee, So-Min;Min, Eun-Kyeong;Kang, Dae-Gill;Lee, Ho-Sub
    • The Journal of Korean Medicine
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    • v.31 no.6
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    • pp.47-57
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    • 2010
  • Objective: The present study investigated the effect of ethanol extract of Cynanchum wilfordii (ECW) on vascular relaxation and vascular inflammation in rat artery isolated from rats and anti-inflammatory activity in human aortic smooth muscle cells (HASMC). Methods: Vascular tone and guanosine 3',5'-cyclic monophosphate (cGMP) production were examined in rat artery isolated from Sprague Dawley rats, in the presence of ECW. HASMC were incubated with tumor necrosis factor-alpha (TNF-${\alpha}$) or Angiotensin II for 24 h. Matrix metalloproteinase (MMP)-2 and anti-oxidant activity of ECW was investigated by pretreatment with ECW in HASMC. Results: Cumulative treatment of ECW relaxed aortic smooth muscles of rats in a dose-dependent manner. ECW-induced vasorelaxation was significantly decreased by pretreatment of L-arginine methyl ester (L-NAME) or oxadiazolo-quinoxalinone (ODQ). Furthermore, ECW treatment of thoracic aorta significantly increased cGMP production. Incubation of ECW with ODQ or L-NAME markedly decreased ECW-induced cGMP production. ECW treatment dose-dependently suppressed TNF-${\alpha}$- or Angiotensin II-induced increase in matrix metalloproteinase-2 expression in HASMC. Also, ECW exhibited 2,2-diphenyl-1-picrylhydrazyl radical scavenging activity in vitro and reduced TNF-${\alpha}$-induced increase in reactive oxygen species production in a dose-dependent manner. Conclusions: Taken together, the results suggest that ECW exerts vascular relaxation via NO/cGMP signaling pathway and decreases MMP-2 expression via anti-oxidant activity.

Tetrahydrobiopterin Inhibits PDGF-stimulated Migration and Proliferation in Rat Aortic Smooth Muscle Cells via the Nitric Oxide Synthase-independent Pathway

  • Jiang, Xiaowen;Kim, Bo-Kyung;Lin, Haiyue;Lee, Chang-Kwon;Kim, Jung-Hwan;Kang, Hyun;Lee, Pil-Young;Jung, Seung-Hyo;Lee, Hwan-Myung;Won, Kyung-Jong
    • The Korean Journal of Physiology and Pharmacology
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    • v.14 no.3
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    • pp.177-183
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    • 2010
  • Tetrahydrobiopterin (BH4), an essential cofactor for nitric oxide synthase (NOS) activity, is known to play important roles in modulating both NO and superoxide production during vascular diseases such as atherosclerosis. However, the role of BH4 in functions of vascular smooth muscle cells is not fully known. In this study, we tested the effects of BH4 and dihydrobiopterin (BH2), a BH4 precursor, on migration and proliferation in response to platelet-derived growth factor-BB (PDGF-BB) in rat aortic smooth muscle cells (RASMCs). Cell migration and proliferation were measured using a Boyden chamber and a 5-bromo-2'-deoxyuridine incorporation assay, respectively, and these results were confirmed with an ex vivo aortic sprout assay. Cell viability was examined by 2,3-bis [2-methoxy-4-nitro-5-sulfophenyl]-2H-tetrazolium-5-carboxanilide assays. BH4 and BH2 decreased PDGF-BBinduced cell migration and proliferation in a dose-dependent manner. The inhibition of cell migration and proliferation by BH4 and BH2 was not affected by pretreatment with $N^G$-nitro-L-arginine methyl ester, a NOS inhibitor. Moreover, the sprout outgrowth formation of aortic rings induced by PDGF-BB was inhibited by BH4 and BH2. Cell viability was not inhibited by BH4 and BH2 treatment. The present results suggest that BH4 and BH2 may inhibit PDGF-stimulated RASMC migration and proliferation via the NOS-independent pathway. Therefore, BH4 and its derivative could be useful for the development of a candidate molecule with an NO-independent anti-atherosclerotic function.

Nitroxergic Nerve Relaxes Rat Gastric Smooth Muscle by NO-cGMP Pathway

  • Yoon, Yoong-Sam;Choi, Hyoung-Chul;Jung, Young-Sook;Kim, Jong-Ho;Lee, Kwang-Youn;Sohn, Uy-Dong;Ha, Jeoung-Hee;Kim, Won-Joon
    • The Korean Journal of Physiology and Pharmacology
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    • v.4 no.5
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    • pp.369-378
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    • 2000
  • This study was undertaken to investigate an involvement of nitroxergic innervation in gastric smooth muscle of rat. Isometric tension study, the measurement of single cell length, NADPH diaphorase stain of smooth muscle layers and neuronal nitric oxide synthase (nNOS) western blotting were performed. Sodium nitroprusside (SNP), a nitric oxide donor, relaxed the muscle strips precontracted by acetylcholine (ACh) in a concentration-dependent manner. Pretreatment of L-arginine decreased the contraction induced by electric field stimulation (EFS). Pretreatment of $N^G-nitro-L-arginine$ methyl ester (L-NAME), a NOS inhibitor, increased the EFS-induced contractions. LY 83583, a guanylate cyclase (GC) inhibitor, reversed the inhibitory actions of L-arginine on the muscle contractions. The effects of L-Arginine, L-NAME and LY 83583 on ACh-induced contractions were not significant. L-arginine reduced the EFS-induced contraction in circular muscle, whereas L-NAME enhanced the EFS-induced contraction in longitudinal strips. By EFS, the phasic contractions appeared approximately $20{\sim}25$ seconds later. L-NAME significantly shortened the delay time to about $2{\sim}3$ seconds. In single cell study, ACh contracted gastric smooth muscle cells, SNP relaxed the cells, and the latter also inhibited the ACh-induced contraction. LY 83583 enhanced the ACh-induced contraction and antagonized SNP-induced relaxation. NADPH diaphorase activity was assessed by a histochemistry, nitroblue tetrazolium (NTB) staining. Positive staining was observed in both circular and longitudinal muscle layers. L-arginine increased the staining, while L-NAME decreased the staining. Western blotting for nNOS proved the presence of nNOS in rat gastric smooth muscle. EFS and additional $Ca^{2+}$ increased nNOS protein expression. These results suggest that in rat stomach, both circular and longitudinal muscle layers are innervated with nitroxergic nerves which relax the gastric smooth muscle via NO-cGMP pathway.

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Syntheses of Pyrrolo[2,1-b]thiazole Carboxanilides and Their Selective Antifungal Activities against Rice Blast and Wheat Leaf Rust (Pyrrolo[2,1-b]thiazole 카르복스아닐라이드 유도체의 합성 및 그들의 벼 도열병균과 밀 붉은녹병균에 대한 선택적인 항균활성)

  • Hahn, Hoh-Gyu;Nam, Kee-Dal;Yang, Bum-Seung;Choe, Gyeong-Ja;Cho, Kwang-Yun;Lee, Seon-Woo
    • The Korean Journal of Pesticide Science
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    • v.9 no.2
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    • pp.122-131
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    • 2005
  • For development of new agrochemical fungicide, syntheses of pyrrolo[2,1-b]thiazole carboxanilide derivatives 9 and antifungal screening against 6 kinds of plant pathogens were carried out. Functionalization of carboxylic acid on C-2 into carboxanilide in the pyrrolo[2,1-b]thiazole resulted in new 20 candidates, in which are ${\alpha},{\beta}$-unsaturated carboxanilide and methyl groups that are in cis relationship. Treatment of acetoxy-1,4-thiazin with magnesium in refluxing methanol gave pyrrolo[2,1-b]thiazole ethyl ester 4 in higher yield than that of the previous report. Hydrolysis of this compound afforded the corresponding acid 5, which reacted with aniline derivatives in the presence of coupling reagent, DIC to give pyrrolo[2,1-b]thiazole carboxanilides 9. As the result of in vivo antifungal assay of 9 against rice blast, rice sheath blight, cucumber gray mold, tomato late blight, wheat leaf rust, and barley powdery mildew, some compounds showed selectively antifungal activities against the rice blast and wheat leaf rust.

Flavor Components in the Bellflower Roots (Platycodon glaucum Nakai) (도라지 뿌리의 향기성분에 관하여)

  • Chung, Tae-Yung;Kim, Jeong-Lim;Hayase, Fumitaka;Kato, Hiromichi
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.16 no.2
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    • pp.136-146
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    • 1987
  • Flavor components were trapped by stimultaneous steam distillation-extraction method for investigating it in the bellflower roots and fractionated into four groups such as a neutral, a basic, a phenolic and an acidic fraction. An acidic fraction methylated with diazomethane solution and three others were analysed by GC and GC-MS equipping a fused silica capillary column, and S-containing compounds in these were detected with a flame photometric detector (FPD). The total of one hundred and three compounds from the bellflower roots were identified: they were 6 aliphatic hydrocarbons, 10 aromatic hydrocarbons, 2 terpene hydrocarbons, 12 alcohols, 8 terpene alcohols, 17 aldehydes, 3 terpene aldehydes, 5 ketones, 5 esters, 3 furans, 2 thiazoles, 2 lactones, 2 sulfides, 9 phenols, l2 carboxylic acids and 5 others. The greater part of the others except carboxylic acids were identified from a neutral fraction of which was assumed to be indispensable for the reproduction of bellflower root odor in a sensory evaluation. As a result of a sensory evaluation, 1-hexanal, trans-2-hexenal, 1-hexanol, cis-3-hexenol, trans-2-hexenol, 1-octen-3-ol and so forth identified in a neutral fraction were considered to be the key compounds of grass-like odor in the bellflower roots.

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A Kinetic Study on the Esterification of Oleic Acid with Methanol in the Presence of Amberlyst-15 (Amberlyst-15 촉매의 존재 하에서 올레산과 메탄올의 에스테르화 반응 속도식 연구)

  • Kim, Young-Joo;Kim, Deog-Keun;Rhee, Young Woo;Park, Soon-Chul;Lee, Jin-Suk
    • Korean Chemical Engineering Research
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    • v.43 no.5
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    • pp.621-626
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    • 2005
  • The esterification reaction of free fatty acid with methanol was investigated in the presence of catalyst, Amberlyst-15, producing fatty acid methyl ester, namely, biodiesel. In this paper, the effects of the reaction parameters such as reaction temperature, mole ratio of alcohol to oleic acid and mass of catalyst on the catalytic activity have been examined. The results showed that the reaction rate increased about twice as the temperature increased every $20^{\circ}C$ in the reaction temperature range from 333 K to 373 K. The equilibrium conversion rate of oleic acid increased with the feed mole ratio of alcohol to acid ranging from 6:1 to 44:1. When the feed mole ratio was higher than 44:1, all the results were similar to that of 44:1. As for the influence of the mass of catalyst, the initial reaction rate increased from 1.2 to 1.3 times as the mass of catalyst doubles in the range of the catalyst weight from 5 to 20 wt%. The experiment data obtained were well described by the second reaction rate using a pseudo-homogeneous model.

The Post Annealing Effect of Organic Thin Film Solar Cells with P3HT:PCBM Active Layer (P3HT:PCBM 활성층을 갖는 유기 박막태양전지의 후속 열처리 효과)

  • Jang, Seong-Kyu;Gong, Su-Cheol;Chang, Ho-Jung
    • Journal of the Microelectronics and Packaging Society
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    • v.17 no.2
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    • pp.63-67
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    • 2010
  • The organic solar cells with Glass/ITO/PEDOT:PSS/P3HT:PCBM/Al structure were fabricated using regioregular poly (3-hexylthiophene) (P3HT) polymer:(6,6)- phenyl $C_{61}$-butyric acid methyl ester (PCBM) fullerene polymer as the bulk hetero-junction layer. The P3HT and PCBM as the electron donor and acceptor materials were spin casted on the indium tin oxide (ITO) coated glass substrates. The optimum mixing concentration ratio of photovoltaic layer was found to be P3HT:PCBM = 4:4 in wt%, indicating that the short circuit current density ($J_{SC}$), open circuit voltage ($V_{OC}$), fill factor (FF) and power conversion efficiency (PCE) values were about 4.7 $mA/cm^2$, 0.48 V, 43.1% and 0.97%, respectively. To investigate the effects of the post annealing treatment, as prepared organic solar cells were post annealed at the treatment time range from 5min to 20min at $150^{\circ}C$. $J_{SC}$ and $V_{OC}$ increased with increasing the post annealing time from 5min to 15min, which may be originated from the improvement of the light absorption coefficient of P3HT and improved ohmic contact between photo voltaic layer and Al electrode. The maximum $J_{SC},\;V_{OC}$, FF and PCE values of organic solar cell, which was post annealed for 15min at $150^{\circ}C$, were found to be about 7.8 $mA/cm^2$, 0.55 V, 47% and 2.0%, respectively.