• Title/Summary/Keyword: bromo

Search Result 330, Processing Time 0.025 seconds

Antitumor Effect of an Adenoviral Cytosine Deaminase/Thymidine Kinase Fusion Gene in C6 Glioma Cells (아데노 바이러스 Cytosine Deaminase/Thymidine Kinase 융합 유전자의 항 종양효과)

  • Kim, Young Woo;Choi, Jae Young;Chang, Jin Woo;Park, Yong Gou;Chung, Sang Sup
    • Journal of Korean Neurosurgical Society
    • /
    • v.30 no.sup1
    • /
    • pp.13-19
    • /
    • 2001
  • Objective : We investigated the feasibility of a double suicide gene/prodrug therapy, involving direct introduction of the herpes simplex virus Type 1 thymidine kinase(TK) gene and the Escherichia coli cytosine deaminase(CD) gene, via a recombinant adenoviral vector and ganciclovir(GCV) and/or 5-fluorocytosine(5-FC) treatment, in C6 glioma cells. Methods : Efficient gene transfer and transduction of C6 glioma cells via a recombinant adenovirus were evaluated by infecting cells with adenovirus bearing the ${\beta}$-galactosidase gene and then staining cells with 5-bromo-4-chloro-3-indolyl-13-D-galactoside. CD/TK expression in cells infected with adenovirus bearing the CD/TK gene(ad-CD/TK) was examined by immunoblotting analysis. For in vitro cytotoxicity experiments, the cells were infected with ad-CD/TK or ad-${\Delta}E1$(as a control). After addition of a variety of concentrations of GCV and 5-FU, either separately or in combination, cell viability was determined by staining the cells with crystal violet solution 6 days after infection. Result : C6 glioma cells were efficiently transduced with recombinant adenoviral vector at multiplicities of infection of 200 or more. In vitro cytotoxicity of GCV and/or 5-FC, either alone or in combination, was exclusively observed in the cells transduced with ad-CD/TK. Obvious cytotoxicity(>50% inhibition) was observed in the presence of 5-FC at concentrations greater than 30ug/ml or GCV at concentrations greater than 0.3ug/ml at a multiplicity of infection of 100. Additionally, cytotoxicity in the presence of both GCV and 5-FC was greater than that after sinlge-prodrug treatments, indicating additive effects of the prodrug treatments. Conclusion : The administration of a double-suicide gene/prodrug therapy might have great potential in the treatment of brain tumors.

  • PDF

Studies on the Oxidative Addition Reactions of 1-Bromosilatranes to $SnBr_2$ (1-브로모실라트란의 $SnBr_2$ 에 대한 산화성 첨가반응 연구)

  • Kim, Myeong Un;Eo, Dong Seon;Sin, Ho Cheol;Kim, Jin Gwon;Do, Young Gyu
    • Journal of the Korean Chemical Society
    • /
    • v.38 no.3
    • /
    • pp.241-245
    • /
    • 1994
  • The oxidative addition reaction has been employed to synthesize heteropolynuclear compounds containing Si-M bonding interaction between the silicon atom of silatrane, pentacoordinate silicon derivative with transannular Si-N dative bond, and the main group element. The reaction of $SnBr_2 with 1-bromosilatrane(1a) in acetonitrile gives the mixture of yellow(2a) and white(2b) solids which were isolated and charaterized by ^1H-NMR, ^{29}Si-NMR, ^{119}Sn-NMR and Mass spectroscopy. The yellow compound was characterized as 1-tribromotinsilatrane which had Si-Sn bonding interaction. The reaction of SnBr2 with 1-bromo-3,7,10-trimethylsilatrane(1b) in methanol gives the Sn(Ⅳ) complex, N[CH_2CH(CH_3)O]_3SiSnBr_3(CH_3OH)_2(3),$ which was characterized by various means.

  • PDF

Effect of Acupuncture on Depression and Cell Proliferation in Hippocampal Gyrus Dentatus of Maternal-separated Rat Pups (침술 치료가 모성분리 새끼 쥐의 우울증과 해마의 치상회 세포증식에 미치는 영향)

  • Park, Jung-Sik;Lim, Hyung-Ho
    • Journal of Korean Medicine Rehabilitation
    • /
    • v.29 no.2
    • /
    • pp.91-99
    • /
    • 2019
  • Objectives The loss of maternal care during early postnatal period may increase development of mood-related disorders, such as depression, anxiety, and personality disorders. In this study, the effect of acupuncture on depression in relation with cell proliferation in the hippocampal gyrus dentatus was investigated using maternal-separated rat pups. Methods On the postnatal 14th day, rat pups from six dams were grouped into following groups: maternal care group, maternal separation group, maternal separation and non-acupoint-acupunctured group, maternal separation and Zusanli-acupunctured group, and maternal separation and fluoxetine-treated group. Acupuncture was performed from postnatal 28th day to postnatal 37th day. The rat pups that belong in the maternal separation and fluoxetine-treated group were injected subcutaneously with 5 mg/kg fluoxetine hydrochloride once a day for the same period of time. To evaluate activity of the rat pups, open field test was performed. Immunohistochemistry for serotonin (5-hydroxytryptamine, 5-HT) and tryptophan hydroxylase (TPH) in the dorsal raphe and for 5-bromo-2'-deoxyuridine (BrdU) in the hippocampal gyrus dentatus was conducted. Results The present results reveal that the activity was decreased by maternal separation. In contrast, acupuncture at Zusanli overcame maternal separation-induced hypoactivity. Maternal separation suppressed TPH expression and 5-HT synthesis in the dorsal raphe and decreased cell proliferation in the hippocampal gyrus dentatus of rat pups. In contrast, acupuncture at Zusanli alleviated maternal separation-induced decrease of 5-HT synthesisand TPH expression. Conclusions The present results demonstrate that acupuncture at Zusanli ameliorated depressive state through increasing cell proliferation and enhancing 5-HT synthesis.

Anti-osteoarthritic effects of a combination of pomegranate concentrate powder, Eucommiae cortex and Achyranthis radix in rats

  • Choi, Beom-Rak;Ku, Sae-Kwang;Kang, Su-Jin;Park, Hye-Rim;Sung, Mi-Sun;Lee, Young-Joon;Park, Ki-Moon
    • The Journal of Korean Medicine
    • /
    • v.39 no.4
    • /
    • pp.86-113
    • /
    • 2018
  • Objectives: We examined the effects of a mixed formula consisting of dried pomegranate concentrate powder (PCP) and the aqueous extracts of Eucommiae cortex (EC) and Achyranthis radix (AR) in rats with surgically induced osteoarthritis (OA). Methods: Two weeks after OA-inducing surgery, a PCP:EC:AR 5:4:1 (g/g) combination or single formula was orally administered. Changes in body weight, knee thickness, maximum knee extension angle, bone mineral density of the knee joints, femoral and tibial articular surfaces, and compressive strength of the femoral and tibial articular cartilage (AC) were assessed, along with the prostaglandin E2 level, 5-lipoxygenase, matrix metalloproteinase (MMP)-2 and MMP-9 activity, and chondrogenic gene mRNA expression in the femoral and tibial AC with the synovial membrane (SM). In addition, the number of cleaved poly(ADP-ribose) polymerase, cyclooxygenase and tumor necrosis factor-${\alpha}$-immunoreactive cells in the femoral and tibial AC with SM were monitored, and the rate of cell proliferation was determined with a 5-bromo-2'-deoxyuridine uptake assay. Results : The signs of surgically induced OA in rats were significantly inhibited by both PCP, EC and AR combined and single formulas. In particular, the combination formula-treated OA model rats showed dose-dependent, significantly increased inhibitory activity against all tested criteria compared with single formula-treated rats. Conclusions: Taken together, our results suggest that the combination formula synergistically increased the anti-OA effects of its components through anti-inflammatory and chondrogenic activity in rats with surgically induced OA. In addition, 200, 100 and 50 mg/kg combination formula treatments showed dose-dependent inhibitory activity against all of the tested criteria.

Glycolysis Mediated Sarcoplasmic Reticulum Ca2+ Signal Regulates Mitochondria Ca2+ during Skeletal Muscle Contraction (근수축시 해당작용에 의한 근형질 세망의 Ca2+ 변화가 미토콘드리아 Ca2+ 증가에 미치는 영향)

  • Park, Dae-Ryoung
    • Exercise Science
    • /
    • v.26 no.3
    • /
    • pp.229-237
    • /
    • 2017
  • PURPOSE: This study was to investigate the Glycolysis mediated sarcoplasmic reticulum (SR) $Ca^{2+}$ signal regulates mitochondria $Ca^{2+}$ during skeletal muscle contraction by using glycolysis inhibitor. METHODS: To examine the effect of Glycolysis inhibitor on SR and mitochondria $Ca^{2+}$ content, we used skeletal muscle fiber from gastrocnemius muscle. 2-deoxy glucose and 3-bromo pyruvate used as glycolysis inhibitor, it applied to electrically stimulated muscle contraction experiment. Intracellular $Ca^{2+}$ content, SR, mitochondria $Ca^{2+}$ level and mitochondria membrane potential (MMP) was detected by confocal microscope. Mitochondrial energy metabolism related enzyme, citric acid synthase activity also examined for mitochondrial function during the muscle contraction. RESULTS: Treatment of 2-DG and 3BP decreased the muscle contraction induced SR $Ca^{2+}$ increase however the mitochondria $Ca^{2+}$ level was increased by treatment of inhibitors and showed and overloading as compared with the control group. Glycolysis inhibitor and thapsigargin treatment showed a significant decrease in MPP of skeletal muscle cells compared to the control group. CS activity significantly decreased after pretreatment of glycolysis inhibitor during skeletal muscle contraction. These results suggest that regulation of mitochondrial $Ca^{2+}$ levels by glycolysis is an important factor in mitochondrial energy production during skeletal muscle contraction CONCLUSIONS: These results suggest that mitochondria $Ca^{2+}$ level can be regulated by SR $Ca^{2+}$ level and glycolytic regulation of intraocular $Ca^{2+}$ signal play pivotal role in regulation of mitochondria energy metabolism during the muscle contraction.

Evaluation of Selective Media Containing Iron Source and Alpha-Glucosidase Substrates for Enterobacter sakazakii (Cronobacter spp.) Detection

  • Chon, Jung-Whan;Seo, Kun-Ho;Yim, Jin-Hyeok;Bae, Dongryeoul;Kim, Binn;Kim, Tae-Jin;Jeong, Dongkwan;Song, Kwang-Young
    • Journal of Dairy Science and Biotechnology
    • /
    • v.39 no.1
    • /
    • pp.9-19
    • /
    • 2021
  • Enterobacter sakazakii (Cronobacter spp.) causes meningitis, necrotizing enterocolitis, sepsis, and bacteremia in neonates and children and has a high mortality rate. For rapid E. sakazakii detection, various differential and selective media containing α-glucosidase substrates, such as 5-bromo-4-chloro-3-indolyl-α-D-glucopyranoside (BCIG) or 4-methylumbelliferyl-α-D-glucoside (α-MUG), have been developed as only E. sakazakii exhibits α-glucosidase activity in the genus Enterobacter. However, Escherichia vulneris (family: Enterobacteriaceae) can also utilize α-glucosidase substrates, thereby resulting in false positives. Various iron sources are known to promote the growth of gram-negative bacteria. This study aimed to develop a selective medium containing α-glucosidase substrates for E. sakazakii detection that would eliminate false positives, such as those of E. vulneris, and to determine the role of iron source in the medium. Three previously developed (TPD) media, i.e., Oxoid, OK, and VRBG, and the medium developed in this study, i.e., NGTE, were evaluated using 58 E. sakazakii and 5 non-E. sakazakii strains. Fifty-four E. sakazakii strains appeared as fluorescent or chromogenic colonies on all four media that were assessed. Two strains showed colonies on NGTE medium and not on TPD media. In contrast, the remaining two strains showed colonies on TPD media and not on NGTE medium. None of the non-E. sakazakii strains showed fluorescent or chromogenic colonies on any of the evaluated media except E. vulneris, which showed colonies on TPD media and not on NGTE medium. This study demonstrated that the newly developed NGTE medium was not only equally efficient in promoting the growth of bacterial colonies when compared with the currently available media but also eliminated false positives, such as E. vulneris.

Neurogenic effect of exercise via the thioredoxin-1/ extracellular regulated kinase/β-catenin signaling pathway mediated by β2-adrenergic receptors in chronically stressed dentate gyrus

  • Kim, Mun-Hee;Leem, Yea-Hyun
    • Korean Journal of Exercise Nutrition
    • /
    • v.23 no.3
    • /
    • pp.13-21
    • /
    • 2019
  • [Purpose] Chronic stress is a precipitating factor for depression, whereas exercise is beneficial for both the mood and cognitive process. The current study demonstrates the anti-depressive effects of regular exercise and the mechanisms linked to hippocampal neurogenesis. [Methods] Mice were subjected to 14 consecutive days of restraint, followed by 3 weeks of treadmill running, and were then subjected to behavioral tests that included the forced swimming and Y-maze tests. Protein levels were assessed using western blot analysis and newborn cells were detected using 5-bromo-2'-deoxyuridine (BrdU). [Results] Three weeks of treadmill running ameliorated the behavioral depression caused by 14 days of continuous restraint stress. The exercise regimen enhanced BrdU-labeled cells and class III β-tubulin levels in the hippocampal dentate gyrus, as well as those of thioredoxin-1 (TRX-1) and synaptosomal β2-adrenergic receptors (β2-AR) under stress. In vitro experiments involving treatment with recombinant human TRX-1 (rhTRX-1) augmented the levels of phospho-extracellular signal-regulated kinases 1 and 2 (ERK1/2), nuclear β-catenin, and proliferating cell nuclear antigens, which were previously inhibited by U0216 and FH535 (inhibitors of ERK1/2 and β-catenin/T cell factor-mediated transcription, respectively). The hippocampal neurogenesis elicited by a 7-day exercise regimen was abolished by a selective inhibitor of β2-AR, butoxamine. [Conclusion] These results suggest that TRX-1-mediated hippocampal neurogenesis by β2-AR function is a potential mechanism underlying the psychotropic effect of exercise.

Treadmill exercise ameliorates post-traumatic stress disorder-induced memory impairment in Sprague-Dawley rats

  • Kim, Tae-Woon;Seo, Jin-Hee;Jung, Sun-Young;Kim, Dae-Young;Kim, Chang-Ju;Lee, Sam-Jun
    • Korean Journal of Exercise Nutrition
    • /
    • v.15 no.4
    • /
    • pp.173-182
    • /
    • 2011
  • Post-traumatic stress disorder (PTSD) is a stress-related mental disorder induced by severe external stressors such as assault, disaster or severe accident. We investigated the effects of treadmill exercise on short-term memory in relation to apoptosis and cell proliferation in the hippocampus following PTSD. Stress to the pregnant rats was induced by exposure of maternal rats to the hunting dog in an enclosed room. Exposure time was 10 min, repeated three times per day, with 1 hour interval. Exposure of maternal rats to the hunting dog was continued 7 days after pregnancy until delivery. The pregnant rats in the exercise groups were forced to run on a treadmill for 30 min once a day for the same duration of stress exposure. Step-down avoidance task for short-term memory, western blot for Bcl-2, Bax, and immunohistochemistry for caspase-3, 5-bromo-2'-deoxyuridine (BrdU), and Ki-67 were conducted. Maternal rats exposed to stress during pregnancy showed short-term memory impairment. Expressions of Bax, Bcl-2, ratio of Bax to Bcl-2, and caspase-3 in the hippocampus were increased in the PTSD rats. Cell proliferation in the hippocampal dentate gyrus was decreased in the PTSD rats. Treadmill exercise alleviated short-term memory impairment and suppressed expressions of Bax, the ratio of Bax to Bcl-2, and caspase-3. Treadmill exercise also increased cell proliferation. The present results indicate that treadmill exercise alleviated PTSD-induced short-term memory impairment by suppressing apoptotic cell death and enhancing cell proliferation in the hippocampus.

Synthesis and antifungal activities of 4-[5-(2-cyclopropylaminopyrimidin-4-yl)-4-arylthiazol-5-yl]piperidine derivatives on Phytophthora capsici (4-[5-(2-cyclopropylaminopyrimidin-4-yl)-4-arylthiazol-5-yl] piperidine 유도체들의 합성과 고추역병균에 대한 살균활성)

  • Nam, Seok-Woo;Lee, Gyung-Rak;Kim, Tae-Joon;Chung, Bong-Jin;Choi, Won-Sik
    • The Korean Journal of Pesticide Science
    • /
    • v.16 no.1
    • /
    • pp.1-10
    • /
    • 2012
  • Fungicidal activities against phytopathogenic fungi of diarylthiazole compound of 4-[5-(2-cyclopropylaminopyrimidin-4-yl)-4-(4-fluorophenyl)thiazol-5-yl]-1-methylpiperidine (I) have been determined to be excellent and compound I was used as the leading compounds in this study. Furthermore, the compound was synthesized by reacting them with five functional groups, 4-fluoro-3-methylphenyl, 4-fluoro-3-chlorophenyl, 4-chloro-2-fluorophenyl, 4-bromo-3-methylphenyl and 2,4-dichlorophenyl groups instead of 4-fluorophenyl group. Also, 2-amino-, 2-(N-ethoxycarbonyl)piperidin-4-yl-, and 2-piperidin-4-yl-thiazole were introduced as the leads instead of 2-N-methylpiperidine-4-yl-thiazol of compound I. VIII-1~VIII-5 and XIII-1~XV-5 compounds were newly synthesized and their structures were confirmed by $^1H$-NMR-spectrum. The fungicidal activities of all the synthesized compounds against Phytophthora capsici were examined using the whole plant method. Among the VIII-1~VIII-5 and XIII-1~XV-5 chemicals, XIV-3 showed the most potent antifungal activity in vivo. While the $EC_{50}$ and $EC_{90}$ values of the commercial fungicide dimethomorph and I were $4.26{\pm}0.02$, $14.72{\pm}0.05$ and $1.01{\pm}0.11$, $6.31{\pm}0.09mM$, those of 4-[5-(2-cyclopropylaminopyrimidin-4-yl)-4-(4-chloro-2-fluorophenyl)thiazol-5-yl]-1-methylpiperidine (XIV-3) was $0.98{\pm}0.21$ and $5.85{\pm}0.05mM$. Therefore, XIV-3 can be considered as a viable candidate for the control of plant diseases caused by P. capsici, and further studies will be conducted on the mode of action XIV-3.

Effects of Non-Steroidal Anti-Inflammatory Drugs on the FMLP-Induced Migration of Neutrophil (비스테로이드성 항염증제가 FMLP에 의한 사람 중성구의 이동에 미치는 영향)

  • Kim, Woo-Mi;Kang, Koo-Il
    • The Korean Journal of Pharmacology
    • /
    • v.30 no.1
    • /
    • pp.137-143
    • /
    • 1994
  • Enhancement or diminution of leukocyte migration to the specific site might be important factors for the development of inflammatory diseases. To investigate the effects of non-steroidal anti-inflammatory drugs (NSAIDs) on chemotaxis of neutrophil, we obtained neutrophils by Hypaque-Ficoll step gradient centrifugation and tested the effects of seven drugs on the n-formyl-leucyl-phenylalanine (FMLP)-induced migration of neutrophil using a 48-well micro chemotaxis assembly. Oxyphenbutazone, phenylbutazone, sulindac, zomepirac, and ibuprofen suppressed the migration of neutrophil at the therapeutic concentrations, however, indomethacin showed stimulation effect. IC50s for inhibition of neutrophil migration by these drugs are less than 100uM. When drugs were preincubated with FMLP, no inhibition on migration of neutrophil was observed. These results indicated that inhibitory effects of these drugs on migration of neutrophil might be related to the receptor sites of neutrophil rather than molecular inactivation of chemoattractant (FMLP). In conclusion, we suggested that the property of inhibition effects on neutrophil migration of several NSAIDs might be another mode of pharmacological action for anti-iflammatory effect, which showed significant effects at concentrations below therapeutic levels, in addition to cyclooxygenase inhibition.

  • PDF