Radiosynthesis and <i>in vitro</i> evaluation of 1‐(tetrahydro‐5‐hydroxy‐6‐(hydroxymethyl)‐2H‐pyran‐3‐yl)‐5‐[¹²⁵I]iodouracil: A new potential agent for HSV1‐tk

Jo, Nam Hyun,Kim, Jung Young,El‐,Gamal, Mohammed I.,Choi, Won‐,Kyoung,Park, Jin‐,Hun,Kim, Eun Jung,Cho, Jung‐,Hyuck,Ha, Hyun‐,Joon,Choi, Tae Hyun,Oh, Chang‐,Hyun John Wiley Sons, Ltd. 2011 Journal of labelled compounds & radiopharmaceutica Vol.54 No.2

<P><B>Abstract</B></P><P>Synthesis, radiolabelling, and <I>in vitro</I> evaluation of a new <SUP>125</SUP>I‐labelled iodouracil hexitol nucleoside analogue are reported. The target compound was successfully synthesized by an iodination–destannylation method and then purified by reverse phase HPLC. The radiochemical purity of the product was >99% with decay‐corrected yields of 48±3%. <I>In vitro</I> cellular uptake testing was carried out using MCA and MCA‐tk cell lines for comparison of compound 1 with [<SUP>18</SUP>F]FHBG. The newly synthesized compound 1 showed higher accumulation in herpex simplex virus type 1 thymidine kinase (HSV1‐tk) gene expression cell line (MCA‐tk cell line) than in the wild type MCA cell line compared with [<SUP>18</SUP>F]FHBG. The MCA‐tk to MCA cellular uptake ratio for compound 1 was higher than that of [<SUP>18</SUP>F]FHBG from 2 h after incubation. The radioiodine‐labelled compound 1 (I‐125, <I>t</I><SUB>1/2</SUB>=59.37 days) has a longer physical half‐life than F‐18‐(<I>t</I><SUB>1/2</SUB>=110 min) labelled FHBG. Radioiodine‐labelled compound 1 could be used for monitoring gene expression for a long time. The selectivity for MCA‐tk cell line makes compound 1 a promising imaging agent for HSV1‐tk expression. Copyright © 2010 John Wiley & Sons, Ltd.</P>

5,7-dihydroxy-3,4,6-trimethoxyflavone inhibits the inflammatory effects induced by <i>Bacteroides fragilis</i> enterotoxin via dissociating the complex of heat shock protein 90 and I&kgr;B&agr; and I&kgr;B kinase-&ggr; in intestinal epithelial cell cultu

Kim, J. M.,Lee, D. H.,Kim, J. S.,Lee, J. Y.,Park, H.-G.,Kim, Y.-J.,Oh, Y.-K.,Jung, H. C.,Kim, S. I. Blackwell Publishing Ltd 2009 Clinical and experimental immunology Vol.155 No.3

<P>Summary</P><P>Enterotoxin produced by enterotoxigenic <I>Bacteroides fragilis</I> (BFT) has been associated with mucosal inflammation and diarrhoeal diseases. In this study, the anti-inflammatory molecular mechanism of 5,7-dihydroxy-3,4,6-trimethoxyflavone (eupatilin) was characterized in an HT-29 intestinal epithelial cell line stimulated with BFT. Pre-treatment of HT-29 cells with eupatilin decreased the production significantly of both interleukin (IL)-8 and prostaglandin E<SUB>2</SUB> induced by BFT in a dose-dependent manner. BFT-activated nuclear factor-kappaB (NF-&kgr;B) signals in HT-29 cells and pretreatment with eupatilin suppressed NF-&kgr;B activation that resulted in the significant inhibition of IL-8 and cyclo-oxygenase-2 expression. BFT-induced phosphorylation of both I&kgr;B&agr; and I&kgr;B kinase (IKK) signals was prevented in eupatilin-pretreated HT-29 cells. Transfection of siRNA for IKK-&agr; and IKK-&bgr; decreased the production of IL-8 and prostaglandin E<SUB>2</SUB>; however, the transfection of IKK-&bgr; siRNA showed a more significant reduction of BFT-induced I&kgr;B&agr; phosphorylation compared with that of IKK-&agr; siRNA. In addition, herbimycin A, a specific inhibitor of heat shock protein 90 (Hsp90), decreased the BFT-induced activation of IKK and NF-&kgr;B, suggesting that Hsp90 is associated with a pathway of IKK-NF-&kgr;B-IL-8/cyclo-oxygenase-2 gene signalling. Furthermore, eupatilin dissociated the complex between Hsp90 and IKK-&ggr; in BFT-stimulated HT-29 cells. These results suggest that eupatilin can suppress the NF-&kgr;B signalling pathway by targeting the Hsp90-IKK-&ggr; complex in intestinal epithelial cells and may attenuate BFT-induced inflammatory responses.</P>

¹³¹I-labeled chitosan hydrogels for radioembolization: A preclinical study in small animals

Hwang, H.,Kim, K.I.,Kwon, J.,Kim, B.S.,Jeong, H.S.,Jang, S.J.,Oh, P.S.,Park, H.S.,Lim, S.T.,Sohn, M.H.,Jeong, H.J. Pergamon Press 2017 Nuclear medicine and biology Vol.52 No.-

<P>Advances in knowledge: Transarterial embolization is a conceivable treatment option for patients with inoperable liver cancer to mitigate the disease progression. Recently, we have developed chitosan-based hydrogel microparticles. In the present study, the hydrogel microparticles were radiolabeled with I-131 for treatment of liver cancer. Our results demonstrated that a hepatic arterial injection of I-125 -labeled Chi resulted in substantial liver accumulation, which was accompanied by virtually no extrahepatic deposition. The results of the present study also showed that administration of I-131 Chi markedly suppressed tumor growth, compared to controls and to animals receiving unlabeled Chi. I-131 -labeled chitosan hydrogel microparticles represent a new therapeutic approach for treatment of liver cancer. (C) 2017 Elsevier Inc. All rights reserved.</P>

Two NF-κB inhibitor-alpha (IκBα) genes from rock bream (Oplegnathus fasciatus): Molecular characterization, genomic organization and mRNA expression analysis after immune stimulation

Lee, Y.,Umasuthan, N.,Whang, I.,Revathy, K.S.,Lee, S.,De Zoysa, M.,Oh, C.,Kang, D.H.,Noh, J.K.,Lee, J. Academic Press 2014 FISH AND SHELLFISH IMMUNOLOGY Vol.41 No.2

IκBα is a member of IκB family, which sequesters NF-κB in an inactivate form in the cytoplasm and blocks the translocation of NF-κB to nucleus. The IκBα paralogs of rock bream (OfIκBα-A and OfIκBα-B) encoded IκBα proteins with typical features including, highly conserved IκB degradation motif, six ankyrin repeats and a PEST sequence. However, their amino acid identity and similarity were only 55.6 and 69.7%, respectively suggesting that these two genes could be the two different isoforms of IκBα. The number and size of the exons of OfIκBα-A and OfIκBα-B were conserved well with all the compared vertebrate species, although they have significantly different genomic sizes. Phylogenetic analysis revealed that OfIκBα-A and OfIκBα-B proteins cluster with IκBα family members; however, they were grouped with different subclades in IκBα family. Tissue specific expression of OfIκBα mRNA was constitutively detected in all the tested tissues, and they showed the higher transcription level in heart, liver, gill and peripheral blood cells, respectively. The injection of flagellin stimulated the mRNA expression of OfIκBα paralogs in head kidney and intestine. Moreover, the OfIκBα mRNA expression in gill and liver was significantly up-regulated by LPS, poly I:C and Edwardsiella tarda challenges. The transcription of OfIκBα was up-regulated in early-phase of injection and then rapidly restored. These results suggest that the OfIκBα paralogs might be involved in rapid immune responsive reactions in rock bream against bacterial and viral pathogens.

정적 연소기내 혼합기 농도변화에 따른 OH분포 측정

최동석(D.S.Choi),김덕줄(D.J.Kim),오승묵(S.M.Oh),황의상(E.S.Hwang),정용일(Y.I.Jeong) 한국자동차공학회 1996 한국자동차공학회 춘 추계 학술대회 논문집 Vol.1996 No.6_2

The OH molecule is a highly reactive combustion intermediate and relatively abundant in combustion systems. It also has the availability of convenient UV -laser systems to excite the A²Σ-X²?? electronic transition. The spectroscopic parameters describing this transition are well known. In this research, the OH molecule was measured in the laminar flame burner and constant volume combustion chamber(CVCC) in order to use it as the fundamental data for studying combustion phenomena. The LIF images of the OH molecule in the laminar 리ame burner were caught by using KrF excimer laser and ICCD camera. The natural fluorescence<br/> of OH was also measured by the interference filter(310 nm) and spectrometer in the CVCC at different equivalence ratios.

Polymorphisms in the neurokinin-2 receptor gene are associated with angiotensin-converting enzyme inhibitor-induced cough

Kim, T.-B.,Oh, S.-Y.,Park, H.-K.,Jeon, S.-G.,Chang, Y.-S.,Lee, K.-Y.,Cho, Y. S.,Chae, I.-H.,Kim, Y.-K.,Cho, S.-H.,Moon, H.-B.,Min, K.-U.,Kim, Y.-Y. Blackwell Publishing Ltd 2009 Journal of clinical pharmacy and therapeutics Vol.34 No.4

<P>Summary</P><P>Background and objective: </P><P>Treatment with angiotensin-converting enzyme (ACE) inhibitors can induce chronic cough in many patients. Genetic variations in the neurokinin 2 receptor gene (NK2R) are significantly associated with cough sensitivity to capsaicin.</P><P>Methods: </P><P>This study assessed the relationship between genetic polymorphisms in the NK2R gene and chronic cough in 91 patients taking ACE inhibitors. Patients included in the study did not have chest abnormalities, postnasal drip, gastroesophageal reflux or a recent history of upper respiratory infection.</P><P>Results: </P><P>We detected two single nucleotide polymorphisms in the NK2R gene (i.e., Gly231Glu and Arg375His). The allelic frequencies at amino acid 231 were 36·3% for Gly/Gly, 49·5% for Gly/Glu and 14·3% for Glu/Glu. The allelic frequencies at amino acid 375 were 74·7% for Arg/Arg, 24·2% for Arg/His and 1·1% for His/His. The prevalence of chronic cough in patients with the amino acid 231 genotype was 33·3% in Gly/Gly homozygotes, 24·4% in Gly/Glu heterozygotes and 0% in Glu/Glu homozygotes. There was a statistically significant association between chronic cough and the Glu/Glu allele (<I>P</I> = 0·028) when the data were analyzed with a recessive model. In addition, there was a significant inverse linear association between the number of Glu231 alleles and ACE inhibitor-related cough (<I>P </I>=<I> </I>0·026). The prevalence of chronic cough in patients with the amino acid 375 genotype was 22·1% in Arg/Arg homozygotes, 31·8% in Arg/His heterozygotes and 0% in His/His homozygotes, although none of these association were statistically significant.</P><P>Conclusion: </P><P>Our findings indicate that the Gly231Glu polymorphism is associated with a lower prevalence of ACE inhibitor-related cough.</P>

Effects of dextrorotatory morphinans on brain Na⁺ channels expressed in Xenopus oocytes

Lee, J.H.,Shin, E.J.,Jeong, S.M.,Lee, B.H.,Yoon, I.S.,Lee, J.H.,Choi, S.H.,Kim, Y.H.,Pyo, M.K.,Lee, S.M.,Chae, J.S.,Rhim, H.,Oh, J.W.,Kim, H.C.,Nah, S.Y. North-Holland ; Elsevier Science Ltd 2007 european journal of pharmacology Vol.564 No.1

We previously demonstrated that dextromethorphan (DM; 3-methoxy-17-methylmorphinan) analogs have neuroprotective effects. Here, we investigated the effects of DM, three of its analogs (DF, 3-methyl-17-methylmorphinan; AM, 3-allyloxy-17-methoxymorphian; and CM, 3-cyclopropyl-17-methoxymorphinan) and one of its metabolites (HM; 3-methoxymorphinan), on Na<SUP>+</SUP> channel activity. We used the two-microelectrode voltage-clamp technique to test the effects of DM, DF, AM, CM and HM on Na<SUP>+</SUP> currents (I<SUB>Na</SUB>) in Xenopus oocytes expressing cRNAs encoding rat brain Nav1.2 α and β1 or β2 subunits. In oocytes expressing Na<SUP>+</SUP> channels, DM, DF, AM and CM, but not HM, induced tonic and use-dependent inhibitions of peak I<SUB>Na</SUB> following low- and high-frequency stimulations. The order of potency for the inhibition of peak I<SUB>Na</SUB> was AM-CM > DM=DF. The DM, DF, AM and CM-induced tonic inhibitions of peak I<SUB>Na</SUB> were voltage-dependent, dose-dependent and reversible. The IC<SUB>50</SUB> values for DM, DF, AM and CM were 116.7+/-14.9, 175.8+/-16.9, 38.6+/-15.5, and 42.5+/-8.5 μM, respectively. DM and its analogs did not affect the steady-state activation and inactivation voltages. AM and CM, but not DM and DF, inhibited the plateau I<SUB>Na</SUB> more effectively than the peak I<SUB>Na</SUB> in oocytes expressing inactivation-deficient I1485Q-F1486Q-M1487Q (IFMQ3) mutant channels; the IC<SUB>50</SUB> values for AM and CM in this system were 8.4+/-1.3 and 8.7+/-1.3 μM, respectively, for the plateau I<SUB>Na</SUB> and 43.7+/-5.9 and 32.6+/-7.8 μM, respectively, for the peak I<SUB>Na</SUB>. These results collectively indicate that DM and its analogs could be novel Na<SUP>+</SUP> channel blockers acting on the resting and open states of brain Na<SUP>+</SUP> channels.

Oxidant effect of La(NO₃)₃.6H₂O solution on the crystalline characteristics of nanocrystalline ZrO₂ films grown by atomic layer deposition

Oh, N.K.,Kim, J.T.,Kang, G.,An, J.K.,Nam, M.,Kim, S.Y.,Park, I.S.,Yun, J.Y. New York] ; North-Holland 2017 APPLIED SURFACE SCIENCE - Vol.394 No.-

Nanocrystalline ZrO<SUB>2</SUB> films were synthesized by atomic layer deposition method using CpZr[N(CH<SUB>3</SUB>)<SUB>2</SUB>]<SUB>3</SUB> (Cp=C<SUB>5</SUB>H<SUB>5</SUB>) as the metal precursor and La(NO<SUB>3</SUB>)<SUB>3</SUB>.6H<SUB>2</SUB>O solution as the oxygen source. La element in the deposited ZrO<SUB>2</SUB> films could not be detected as its content was below the resolution limit of the X-ray photoelectron spectroscopy. The alternative introduction of La(NO<SUB>3</SUB>)<SUB>3</SUB>.6H<SUB>2</SUB>O solution to conventionally used H<SUB>2</SUB>O as the oxidant effectively altered the crystalline structure, grain size, and surface roughness of the grown ZrO<SUB>2</SUB> films. Specifically, the crystalline structure of the ZrO<SUB>2</SUB> film changed from a mixture of tetragonal and monoclinic phases to monoclinic phase. The average grain size also increased, and the resulting film surface became rougher. The average grain sizes of the ZrO<SUB>2</SUB> films prepared from La(NO<SUB>3</SUB>)<SUB>3</SUB>.6H<SUB>2</SUB>O solution at concentrations of 10, 20, 30, and 40% were 280, 256, 208, and 200nm, respectively, whereas that prepared using H<SUB>2</SUB>O oxidant was 142nm. However, the concentration of La(NO<SUB>3</SUB>)<SUB>3</SUB>.6H<SUB>2</SUB>O solution minimally influenced the crystalline characteristics of the nanocrystalline ZrO<SUB>2</SUB> films i.e., the crystalline structure, grain size, and surface roughness except for crystallite size.

Docetaxel (Taxotere), cisplatin, UFT, and leucovorin combination chemotherapy in advanced gastric cancer

Oh, S C,Park, K H,Choi, I K,Yoon, S Y,Kim, S J,Seo, J H,Choi, C W,Kim, B S,Shin, S W,Kim, J S,Kim, Y H Nature Publishing Group 2005 The British journal of cancer Vol.92 No.5

<P>We conducted this study to ascertain the efficacy and toxicity of docetaxel and cisplatin combined with oral UFT and leucovorin as a first-line treatment for patients with advanced gastric cancer. In all, 52 patients received courses of docetaxel 60 mg m<SUP>−2</SUP> intravenously (i.v.) for 1 h and then cisplatin 75 mg m<SUP>−2</SUP> i.v. for 2 h on day 1. Oral UFT at 400–600 mg day<SUP>−1</SUP>, as determined by body surface area, and leucovorin at 75 mg day<SUP>−1</SUP> were administered for 21 consecutive days from day 1, and this was followed by a 7-day drug-free interval. A total of 225 courses were administered, and the median number of courses per patient was four. Four complete responses (7.7%) and 22 partial responses (42.3%) were achieved, giving an overall response rate of 50% (95% Confidence Interval: 36.4–63.6%). The major toxicity was neutropenia, which reached grade 3/4 in 36 patients (69.3%). Grade 3/4 nausea and vomiting was observed in 12 patients (23.1%). Median time to progression was 22 weeks (4 to 156+ weeks), median survival duration was 48 weeks (4 to 156+ weeks), and median response duration was 24 weeks (6–152 weeks). We conclude that docetaxel, cisplatin, oral UFT, and leucovorin combination chemotherapy is effective and tolerable for the treatment of advanced gastric cancer.</P>

Evaluation of potential-induced degradation in crystalline Si solar cells using Na fault injection

Oh, W.,Kim, J.,Kang, B.,Bae, S.,Lee, K.D.,Lee, H.S.,Kim, D.,Chan, S.I. Pergamon Press 2016 Microelectronics reliability Vol.64 No.-

<P>Photovoltaic (PV) modules are exposed to high-voltage stress between grounded module frames and solar cells, a configuration called potential-induced degradation (PID). Since PID mainly depends on the solar cells used for module packaging, several steps for PID tests can be omitted. We carried out PID tests on the cell level with Na fault injection in accordance with IEC 62804 and examined the extent of PID with saturation current density (J(02)) extracted from I-V measurements in the dark. Na-fault injection is a reasonable means for performing PID tests on the cell level without module packaging. (C) 2016 Elsevier Ltd. All rights reserved.</P>