• Parasites, Hosts and Diseases
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• 제54권2호
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• pp.139-145
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• 2016

Toxoplasmosis is a serious disease caused by Toxoplasma gondii, one of the most widespread parasites in the world. Lipid metabolism is important in the intracellular stage of T. gondii. Stearoyl-CoA desaturase (SCD), a key enzyme for the synthesis of unsaturated fatty acid is predicted to exist in T. gondii. Sterculic acid has been shown to specifically inhibit SCD activity. Here, we examined whether sterculic acid and its methyl ester analogues exhibit anti-T. gondii effects in vitro. T. gondii-infected Vero cells were disintegrated at 36 hr because of the propagation and egress of intracellular tachyzoites. All test compounds inhibited tachyzoite propagation and egress, reducing the number of ruptured Vero cells by the parasites. Sterculic acid and the methyl esters also inhibited replication of intracellular tachyzoites in HFF cells. Among the test compounds, sterculic acid showed the most potent activity against T. gondii, with an $EC_{50}$ value of $36.2{\mu}M$, compared with $EC_{50}$ values of $248-428{\mu}M$ for the methyl esters. Our study demonstrated that sterculic acid and its analogues are effective in inhibition of T. gondii growth in vitro, suggesting that these compounds or analogues targeting SCD could be effective agents for the treatment of toxoplasmosis.

• Asian-Australasian Journal of Animal Sciences
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• 제31권5호
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• pp.712-720
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• 2018

Objective: The aim of this experiment was to evaluate the effect of dietary supplementation with the docosahexaenoic acid (DHA)-rich microalgae, Aurantiochytrium limacinum (AURA) on pig performance, carcass traits, and the fatty acid composition of pork Longissimus lumborum (LL) and backfat. Methods: A total of 144 Pig Improvement Company (PIC)${\times}$Goland finishing pigs (72 females and 72 castrated males) of mean weight 117.1 (${\pm}13.1$) kg were blocked by sex and body weight and provided with 0% or 1% AURA in isonutritive and isocaloric diets. A total of 24 pens provided 12 replicates per treatment. Animals were weighed on day 0 and 28 with feed and water intake recorded per pen. After 31 days supplementation (28 days of study and 3 days until the slaughtering date) three animals per pen (n = 72) were slaughtered and the LL and backfat thickness, lean meat content and dressing percentage were recorded for the carcasses. The fatty acid (FA) profile of the LL and backfat was established by direct FA methyl ester synthesis. Results: No differences were observed for any performance parameters or carcass traits. Supplementation with AURA resulted in significant changes to the FA profiles of both the LL and backfat with male and female pigs responding differently to supplementation in terms of particular FAs. Overall, pork LL samples had significantly higher eicosapentaenoic acid (p<0.001) and DHA concentrations (p<0.001), and higher omega-3 (n-3) FAs (p<0.001), as well as an increased omega3:omega6 (n-3:n-6) ratio (p = 0.001). For backfat, supplementation resulted in significantly higher amounts of DHA (p<0.001) and n-3 FAs (p<0.001). Conclusion: These results indicate that dietary supplementation with 1% AURA over a 31 day period can increase the FA composition of pork LL and backfat, specifically the DHA, with no major impact on growth performance and carcass traits.

• Bulletin of the Korean Chemical Society
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• 제35권5호
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• pp.1485-1490
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• 2014

We have designed and developed a new ladder type tetrafused ${\pi}$-conjugated building block such as dihydroindolo[3,2-b]indole (DINI) and investigated its role as an electron rich unit. The photovoltaic properties of a new semiconducting ${\pi}$-conjugated polymer, poly[[5,10-bisoctyl-5,10-dihydroindolo[3,2-b]indole-[5,6- bis(octyloxy)-4,7-di(thiophen-2-yl)benzo[c][1,2,5]thiadiazole]], represented by PDINI-OBTC8 are described. The new polymer PDINI-OBTC8 was synthesized in donor-acceptor (D-A) fashion, where fused ${\pi}$-conjugated tetracyclic DINI, and 5,6-bis(octyloxy)-4,7-di(thiophen-2-yl) benzo[c][1,2,5]thiadiazole (OBTC8) were employed as electron rich (donor) and electron deficient (acceptor) moieties, respectively. The conventional bulk heterojunction (BHJ) device structure ITO/PEDOT:PSS/PDINI-OBTC8:PCB71M/LiF/Al was utilized to fabricate polymer solar cells (PSCs), which comprises the blend of PDINI-OBTC8 and [6,6]-phenyl-$C_{71}$-butyric acid methyl ester ($PC_{71}BM$) in BHJ network. A BHJ PSC that contain PDINI-OBTC8 delivered power conversion efficiency (PCE) value of 1.68% with 1 vol% of 1,8-diidooctane (DIO) under the illumination of A.M 1.5G 100 $mW/cm^2$.

• Bulletin of the Korean Chemical Society
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• 제28권10호
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• pp.1781-1786
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• 2007

Two copper(II) complexes, [CuL3](ClO4)2 bearing one N-CH2CH2CONH2 group as well as one N-CH2CH2CN group and [CuL4](ClO4)2 bearing two N-CH2CH2CONH2 groups, have been prepared by the selective hydrolysis of [CuL2](ClO4)2 (L2 = C-meso-1,8-bis(cyanoethyl)-5,5,7,12,12,14-hexamethyl-1,4,8,11-tetraazacyclotetradecane). The complex [CuL5](ClO4)2 bearing one N-CH2CH2C(=NH)OCH3 and one N-CH2CH2CN groups has been prepared as the major product from the reaction of [CuL2](ClO4)2 with methanol in the presence of triethylamine. In acidic aqueous solution, the N-CH2CH2C(=NH)OCH3 group of [CuL5](ClO4)2 undergoes hydrolysis to yield [CuL6](ClO4)2 bearing both N-CH2CH2COOCH3 and N-CH2CH2CN groups. The crystal structure of [CuL5](ClO4)2 shows that the complex has a slightly distorted square-pyramidal coordination polyhedron with an apical Cu-N (N-CH2CH2C(=NH)OCH3 group) bond. The apical Cu-N bond distance (2.269(3) A) is ca. 0.06 A longer than the apical Cu-O (N-CH2CH2CONH2 group) bond of [CuL4](ClO4)2. The pendant amide group of [CuL3](ClO4)2 is involved in coordination. The carboxylic ester group of [CuL6](ClO4)2 is also coordinated to the metal ion in various solvents but is removed from the coordination sphere in the solid state.

• The Korean Journal of Physiology and Pharmacology
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• 제1권6호
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• pp.809-816
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• 1997

The present study was designed to investigate whether endogenous nitric oxide(EDNO) is involved in submandibular vasodilation and salivation induced by parasympathetic nerve stimulation. Effects of $N^w$-nitro-L-arginine-methyl ester (L-NAME) which blocks the synthesis of EDNO from L-arginine on the submandibular vasodilation and salivation induced by chords stimulation or administration of various vasodilators were examined in anesthetized cats. Effect of L-NAME on $K^+$ efflux induced by carbachol was also examined using the excised submandibular slice in vitro. In the submandibular slices, acetylcholine$(10^{-5}\;mol/L)$ or vasoactive intestinal polypeptide$(VIP,\;10^{-5}\;mol/L)$ increased $NO_2$ contents, which was Prevented by pretreatment with L-NAME. Salivary secretion in response to the chords stimulation$(3\;V,\;1\;msec,\;10{\sim}20\;Hz)$ was completely blocked by treatment with atropine(1 mg/kg). Increased blood flow response to the low frequency(1, 2, 5 Hz) stimulation was significantly reduced, whereas the blood flow induced by the higher frequency(10,20 Hz) stimulation was not affected. Lingual-arterial infusion of L-NAME(100 mg/kg) significantly diminished the vasodilatory and salivary responses to the chorda stimulation at all stimuli frequencies used. Intra-arterial infusion of L-NAME(100 mg/kg markedly diminished the vasodilatory responses to acetylcholine$(5\;{\mu}g/kg)$, VIP$(5\;{\mu}g/kg)$ or bradykinin$(5\;{\mu}g/kg)$. In the excised submandibular slice, $K^+$ efflux in response to carbachol$(10^{-5}\;mol/L)$ was significantly decrease by pretreatment with L-NAME$(10^{-5}\;mol/L)$. In the isolated submandibular artery precontracted with phenylephrine$(10^{-5}\;mol/L)$, the vasorelaxation induced by ACh$(10^{-7}\;mol/L)$ was reversed into a contraction by methylene blue$(10^{-4}\;mol/L)$. These results suggest that EDNO may play an important role in vasodilation and secretion of the submandibular gland.

• The Korean Journal of Physiology
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• 제28권2호
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• pp.197-202
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• 1994

The present study was aimed to determine if endogenous L-arginine-nitric oxide (NO) pathway has central, rather than peripheral, mechanisms in blood pressure regulation. Arterial blood pressure and heart rate responses to acute inhibition of the t-arginine-NO pathway were examined in rats anesthetized with thiopental (50 mg/kg, IP). An intracerebroventricular (ICV) cannula was placed in the left lateral ventricle. The right femoral artery was cannulated to measure arterial blood pressure and the vein to serve as an infusion route. $N^G-nitro-L-arginine$ methyl ester (L-NAME) was infused either intracerebroventricularly or intravenously. ICV infusion $(1.25\;{\mu}L/min)$ of L-NAME $(20\;or\;100\;{\mu}g/kg)$ per minute for 60 min) increased the mean arterial pressure and heart rate. Plasma renin concentrations(PRC) were significantly lower in L-NAME-infused group than in the control. L-Arginine $(60\;{\mu}g/min,\;ICV)$ prevented the pressor response to ICV L-NAME. The pressor response was not affected by simultaneous intravenous infusion of saralasin, but was abolished by hexamethonium treatment. Intravenous infusion $(40\;{\mu}L/min,\;10{\sim}100\;{\mu}g/kg\;per\;minute\;for\;60\;min)$ also increased blood pressure, while it decreased heart rate. These results indicate that endogenous L-arginine-NO pathway has separate central and peripheral mechanisms in regulating the cardiovascular function. The central effect may not be mediated via activation of renin-angiotensin system, but via, at least in part, activation of the sympathetic outflow.

• 한국산학기술학회논문지
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• 제11권12호
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• pp.4854-4862
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• 2010

본 연구에서 thyme oil의 주성분인 thymol (1)과 유사한 구조를 갖는 4-isopropyl-3-methylphenol (2), 5-isopropyl-3-methylphenol (3), 4-isopropylphenol (4)과 2-isopropylphenol (5)을 출발 물질로 하여 sulfonyl ester 계열 유도체 25종을 합성하였다. IR, $^1H$-NMR과 GC/MS를 이용하여 이들 유도체들이 합성되었음을 확인하였다. 이들 유도체들에 대한 식물병원균의 생장 억제실험은 벼도열병균(Pyrcularia grisea), 벼잎집무늬마름병균(Rhizoctonia solani), 토마토잎마름역병균(Phytophthora infestans), 오이탄저병균(Colletotrichum orbiculare)과 오이흰가루병균(Sphaerotheca fusca)에 대하여 실시하였다. 그 결과, 2-isopropyl-5-methylphenyl o-toluenesulfonate (1a), 2-isopropylphenyl 2,4,5-trich lorobenzenesulfonate (5b)와 2-isopropylphenyl 2-methyl-5-nitrobenzenesulfonate (5e)는 각각 in vivo에서 벼도열병균(Pyrcularia grisea), 토마토잎마름역병균(Phytophthora infestans)과 오이흰가루병균(Sphaerotheca fusca)에 대하여 우수한 항균활성을 나타내었다.

• The Korean Journal of Physiology and Pharmacology
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• 제1권2호
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• pp.185-193
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• 1997

The characteristics of $Na^+$-dependent cycloleucine uptake was investigated in OK cells with regard to substrate specificity and regulation by protein kinase C (PKC). Inhibition studies with different synthetic and natural amino acids showed a broad spectrum affinity to neutral amino acids regardless of their different side chains including branched or aromatic, indicating that the $Na^+$-dependent cycloleucine uptake in OK cells is mediated by System $B^o$ or System $B^o$-like transporter rather than the classical System A or ASC. Phorbol 12-myristate 13-acetate (PMA) and phorbol 12,13-dibutyrate, but not $4{\alpha}-PMA$ elicited a time-dependent biphasic stimulation of $Na^+$-dependent cycloleucine uptake, which produced early transient peak at 30 min and late sustained peak at 180min. Both the early and late stimulations by PMA were due to an increase in Vmax and not due to a change in Km. PKC inhibitors blocked both the early and late stimulation by PMA, while protein synthesis inhibitors blocked the late stimulation only. These results suggest the existence and regulation by PKC of System $B^o$ or System $B^o$-like broad spectrum transport system for neutral amino acids in OK cells.

• 약학회지
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• 제49권4호
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• pp.347-354
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• 2005

Lipopolysaccharide (LPS) induces synthesis of several inflammatory cytokines and nitric oxide (NO). NO in brain is involved not only in the regulation of important metabolic pathways via intracellular cyclic GMP-dependent path­ways, but also in neurotoxic damage by reacting with superoxide ion leading to form peroxynitrite radical. Oxidative stress has suggested to be related to the inhibition of NO synthase/cyclic GMP pathway. OQ21 is a new fluorinated quinone compound that is recently known to have inhibitory effects on both NO synthase (NOS) and guanylyl cyclase (GC). In this study, we examined effects of OQ21, other known NOS or GC inhibitors, or an antioxidant, melatonin, on the oxidative stress produced by LPS in rat brain. Oxidative stress was observed by using the 2',7'-dichlorofluorescin diacetate to measure intra-cellular reactive oxygen species (ROS) production and by measuring the formation of thiobarbituric acid reactive substances to measure lipid peroxidation. LPS induced significant increase in both ROS produdction and lipid peroxidation in all brain regions tested (striatum, hippocampus and cortex), which were dissected 6hr after intraperitoneal administration of LPS to rats. Direct striatal injection of two NOS inhibitors, N-nitro-L-arginine methyl ester and diphenyleneiodonium, or a GC inhibitor, IH-[1,2,4]oxadiazolo[4,3-a]quinoxaline-l-one, produced no significant ROS increase. However, OQ21 enhanced ROS formation in striatal tissues from LPS-treated rats. Melatonin decreased LPS-induced ROS formation and decreased ROS formation increased by OQ21 in striatum of LPS-treated rats.

• 대한화학회지
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• 제26권3호
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• pp.188-193
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• 1982

새로운 혼성 폴리에스테르 4가지를 합성하여 액정성을 DSC 및 편광 현미경을 사용하여 조사, 연구하였다. 세가지 혼성 폴리에스테르는 같은 메소젠 단위를 갖고 있으나 폴리메틸렌 유연 격자중 메틸렌기 수가 기수-우수, 기수-기수 및 우수-우수의 조합으로 되어 있는점이 다르며, 또 하나의 혼성 폴리에스테르는 양단에 p-옥시벤조일기가 결합하고 있는 메틸-및 브로모히드로 퀴논 단위가 데카메틸렌 격자에 결합하고 있는 구조를 갖고 있다. 이들 폴리에스테르는 모두 녹는점 및 그 이상의 온도에서 네마틱 액정상을 형성함을 알았으며 네마틱${\to}$등방성 액체간의 상변환이 가역적으로 일어남을 DSC 및 현미경으로 관찰할 수 있었다. 액정${\to}$등방성액체의 상변환에 수반되는 열역학적 성질을 중합체의 구조와 관련시켜 고찰하였다.