• Title/Summary/Keyword: $NO_2$ inhibition

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General Pharmacological Properties of Recombinant Human Parathyroid Hormone (재조합 부갑상선 흘몬의 일반약리작용)

  • 이은방;장혜옥;이향주;천선아
    • Biomolecules & Therapeutics
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    • v.6 no.2
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    • pp.159-164
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    • 1998
  • General pharmacological properties of recombinant human parathyroid hormone (hPTH) were examined. The administration of hPTH (7, 35 and 175 lU/kg sc) in mice had no effects in general behavior and central nervous system, and no influences on normal body temperature, writhing syndromes induced by 0.7% acetic acid solution and chemoshock produced by strychnine and pentetrazol solution. hPTH (9 and 44 lU/kg, sc) given to anesthetized rabbits showed no effect on blood pressure of carotid artery and respiration, and it did not influence the responses produced by injection of acetylcholine or epinephrine. It showed no direct effect at 4.4$\times$10$_{-2}$IU/ml in isolated stomach fundus and uterus of rats and ileum of guinea-pig, and it also showed no inhibition of contraction produced by acetylcholine, oxytocin, serotonin and histamine in the above-mentioned preparations. It did not influence intestinal propulsion at the doses of 7,35 and 175 lU/kg sc in mice. This drug exhibited no effect on urinary excretion at the doses of 7 and 35 lU/kg sc in rats. However, at a dose of 175 lU/kg sc, it showed a decreased urination along with decreased excretion of potassium, sodium and chloride ion. These results indicate that hPTH does not exert any of serious pharmacological effects except the inhibition of urination at a highest dose used.

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Characterization of the Galvanizing Behavior Depending on Annealing Dew Point and Chemical Composition in Dual-Phase Steels

  • Shin, K.S.;Park, S.H.;Jeon, S.H.;Bae, D.C.;Choi, Y.M.
    • Corrosion Science and Technology
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    • v.9 no.6
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    • pp.247-253
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    • 2010
  • The characteristics of selective oxidation prior to hot-dip galvanizing with the annealing atmosphere dew point and chemical composition in dual-phase steels and their effect on the inhibition layer formation relevant to coating adhesion have been studied using a combination of electron microscopic and surface analytical techniques. The annealed and also galvanized samples of 3 kinds of Si/Mn ratios with varied amounts of Si addition were prepared by galvanizing simulator. The dew point was controlled at soaking temperature $800^{\circ}C$ in 15%$H_2$ -85%$N_2$ atmosphere. It was shown that good adhesion factors were mainly uniformity of oxide particle distribution of low number density and low Si/Mn ratio prior to hot-dip galvanizing. Their effect was the greatly reduced coating bare spots and the formation of uniform inhibition layer leading to good adhesion of Zn overlay. The mechanism of good adhesion is suggested by two processes: the formation of inhibition layer on the oxide free surface uncovered with no $SiO_2$-containing particles in particular, and the inhibition layer bridging of oxide particles. The growth of inhibition layer was enhanced markedly by the delayed reaction of Fe and Al with the increase of Si/Mn ratio.

Vasorelaxing Effect of Isoflavonoids Via Rho-kinase Inhibition in Agonist-Induced Vasoconstriction (Isoflavonoids에 의한 혈관이완효과에 있어 Rho-kinase의 역할)

  • Je, Hyun-Dong
    • YAKHAK HOEJI
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    • v.50 no.4
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    • pp.293-299
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    • 2006
  • The aim of present study was to investigate the possible influence of Rho-kinase inhibition on the plant-derived estrogen-like compounds-induced arterial relaxation. Agonist- or depolarization-induced vascular smooth muscle contractions involve the activation of Rho-kinase pathway. However there are no reports addressing the question whether this pathway is involved in genistein-or daidzein-induced vascular relaxation in rat aortae precontracted with phenylephrine or thromboxane $A_2$ mimetic U-46619. We hypothesized that Rho-kinase inhibition plays a role in vascular relaxation evoked by genistein or daidzein in rat aortae. Endothelium-intact and denuded arterial rings from male Sprague-Dawley rats were used and isometric contractions were recorded using a computerized data acquisition system. Genistein concentration-dependently inhibited phenylephrine or thromboxane $A_2-induced$ contraction regardless of endothelial function. Surprisingly, in the agonists-induced contraction, similar results were also observed in aortae treated with daidzein, the inactive congener for protein tyrosine kinase inhibition, suggesting that Rho-kinase might act upstream of tyrosine kinases in phenylephrine-induced contraction. In conclusion, in the agonists-precontracted rat aortae, genistein and daidzein showed similar relaxant response regardless of tyrosine kinase inhibition or endothelial function.

Autophagy Inhibition Promotes Gambogic Acid-induced Suppression of Growth and Apoptosis in Glioblastoma Cells

  • Luo, Guo-Xuan;Cai, Jun;Lin, Jing-Zhi;Luo, Wei-Shi;Luo, Heng-Shan;Jiang, Yu-Yang;Zhang, Yong
    • Asian Pacific Journal of Cancer Prevention
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    • v.13 no.12
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    • pp.6211-6216
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    • 2012
  • Objective: To investigate the effects of gambogic acid (GA) on the growth of human malignant glioma cells. Methods: U251MG and U87MG human glioma cell lines were treated with GA and growth and proliferation were investigated by MTT and colony formation assays. Cell apoptosis was analyzed by annexin V FITC/PI flow cytometry, mitochondrial membrane potential assays and DAPI nuclear staining. Monodansylcadaverine (MDC) staining and GFP-LC3 localisation were used to detect autophagy. Western blotting was used to investigate the molecular changes that occurred in the course of GA treatment. Results: GA treatment significantly suppressed cell proliferation and colony formation, induced apoptosis in U251 and U87MG glioblastoma cells in a time- and dose-dependent manner. GA treatment also lead to the accumulation of monodansylcadaverine (MDC) in autophagic vacuoles, upregulated expressions of Atg5, Beclin 1 and LC3-II, and the increase of punctate fluorescent signals in glioblastoma cells pre-transfected with GFP-tagged LC3 plasmid. After the combination treatment of autophagy inhitors and GA, GA mediated growth inhibition and apoptotic cell death was further potentiated. Conclusion: Our results suggested that autophagic responses play roles as a self-protective mechanism in GA-treated glioblastoma cells, and autophagy inhibition could be a novel adjunctive strategy for enhancing chemotherapeutic effect of GA as an anti-malignant glioma agent.

The Anti-Adipogenic Activity of a New Cultivar, Pleurotus eryngii var. ferulae 'Beesan No. 2', through Down-Regulation of PPAR γ and C/EBP α in 3T3-L1 Cells

  • Kang, Min-Jae;Kim, Keun Ki;Son, Byoung Yil;Nam, Soo-Wan;Shin, Pyung-Gyun;Kim, Gun-Do
    • Journal of Microbiology and Biotechnology
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    • v.26 no.11
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    • pp.1836-1844
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    • 2016
  • Adipogenesis is one of the cellular processes and a highly controlled program. Nowadays, inhibition of adipogenesis has received attention as an effective way to regulate obesity. In the current study, we investigated the inhibition effect of a chloroform extract of Pleurotus eryngii var. ferulae 'Beesan No. 2' (CEBT) on adipogenesis in 3T3-L1 murine preadipocytes. Pleurotus eryngii var. ferulae is one of many varieties of King oyster mushroom and has been reported to have various biological activities, including antitumor and anti-inflammation effects. Biological activities of 'Beesan No. 2', a new cultivar of Pleurotus eryngii var. ferulae, have not yet been reported. In this study, we found that CEBT suppressed adipogenesis in 3T3-L1 cells through inhibition of key adipogenic transcription factors, such as peroxisome proliferatoractivated receptor ${\gamma}$ and CCAAT/enhancer binding protein ${\alpha}$. Additionally, CEBT reduced the expression of the IRS/PI3K/Akt signaling pathway and its downstream factors, including mammalian target of rapamycin and p70S6 kinase, which stimulate adipogenesis. Furthermore, ${\beta}-catenin$, a suppressor of adipogenesis, was increased in CEBT-treated cells. These results indicate that Pleurotus eryngii var. ferulae 'Beesan No. 2' effectively inhibited adipogenesis, so this mushroom has potential as an anti-obesity food and drug.

NF-kB and AP-1-regulatory Mechanism of Buthus Martensi Karsch Herbal Acupuncture Solution on Inflammatory Cytokine-induced Human Chondrocytes Dysfunction

  • Cho, Jae-Yong;Kim, Kyung-Ho;Cho, Hyun-Seok;Lim, Dae-Jung;Hwang, Ji-Hye;Kim, Kap-Sung
    • Journal of Acupuncture Research
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    • v.23 no.2
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    • pp.61-72
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    • 2006
  • Objectives : Human chondrocytes co-treated with Buthus martensi Karsch herbal acupuncture solution(BMK-HAS) extract produced significantly less NO compared with chondrocytes stimulated with $IL-1{\beta}$ alone Methods : Activation and translocation of and NF-kB DNA binding activity were determined by Western blotting and specific enzyme-linked immunosorbent assay. Results : The inhibition of NO production correlated with the suppression of induction and expression of nuclear factor-kB (NF-kB) and activation protein-1 (AP-1)-dependent gene. BMK-HAS inhibited the activation and translocation of NF-kB to the nucleus, indicating that BMK-HAS inhibits the $IL-1{\beta}-induced$ production of NO in human chondrocytes by interfering with the activation of NF-kB through a novel mechanism. In addition, BMK-HAS reduced prostaglandin E2 (PGE2)production in mouse peritoneal macrophages stimulated with lipopolysaccharide, whereas no influence on the activity of inducible NO synthase (iNOS), cyclooxygenase-2 (COX-2) or cyclooxygenase-1 (COX-1) was observed. My data, therefore, suggest that BMK-HAS may be a therapeutically effective inhibitor of $IL-1{\beta}-induced$ inflammatory effects that are dependent on NF-kB activation in human OA chondrocytes. Conclusion : The results indicate that BMK-HAS exerts anti-inflammatory effects related to the inhibition of neutrophil functions and of NO and PGE2 production, which could be due to a decreased expression of iNOS and COX-2 through the transcription factors NF-kB and AP-1.

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Immune-Enhancing Activity of Staphylea bumalda Leave (고추나무 잎의 면역증진 활성)

  • Jin Boo Jeong
    • Proceedings of the Plant Resources Society of Korea Conference
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    • 2020.08a
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    • pp.86-86
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    • 2020
  • The leaves of Staphylea bumalda (S. bumalda) as a deciduous tree distributed in Korea, China and Japan are used to treat respiratory diseases or inflammation. However, there is no scientific research on the immune-enhancing activity of S. bumalda leaves. Thus, in this study, we investigated the effect of water extracts from S. bumalda leaves (SBL) on the macrophage activity using mouse macrophage cells, RAW264.7. SBL increased production of immunomodulators such as NO, iNOS, IL-1β, IL-6, TNF-α and MCP-1 in RAW264.7 cells and activated phagocytic activity of RAW264.7 cells. Inhibition of TLR2 and TLR4 blocked SBL-mediated production of immunomodulators in RAW264.7 cells. In addition, SBL-mediated production of immunomodulators was attenuated by JNK inhibition in RAW264.7 cells. SBL increased JNK phosphorylation, while Inhibition of TLR2 and TLR4 blocked SBL-mediated JNK phosphorylation in RAW264.7 cells. These results are thought to be evidence that SBL activates JNK through stimulation of TLR2 and TLR4 in macrophage to induce the production of immunomodulators. In LPS-stimulated RAW264.7 cells, SBL inhibited over-production of immunomodulators. Summarizing the results, SBL showed immunostimulatory activity under normal conditions and immunosuppressive activity under LPS-induced excessive immune response conditions.

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Characterization of Aspartate Aminotransferase Isoenzymes from Leaves of Lupinus albus L. cv Estoril

  • Martins, Maria Luisa Louro;De Freitas Barbosa, Miguel Pedro;De Varennes E Mendonca, Amarilis Paula Alberti
    • BMB Reports
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    • v.35 no.2
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    • pp.220-227
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    • 2002
  • Two aspartate aminoransferase (EC 2.6.1.1) isoenzymes (AAT-1 and AAT-2) from Lupinus albus L. cv Estoril were separated, purified, and characterized. The molecular weight, pI value, optimum pH, optimum temperature, and thermodynamic parameters for thermal inactivation of both isoenzymes were obtained. Studies of the kinetic mechanism, and the kinetics of product inhibition and high substrate concentration inhibition, were performed. The effect of some divalent ions and irreversible inhibitors on both AAT isoenzymes was also studied. Native PAGE showed a higher molecular weight for AAT-2 compared with AAT-1. AAT-1 appears to be more anionic than AAT-2, which was suggested by the anion exchange chromatography. SDS-PAGE showed a similar sub-unit molecular weight for both isoenzymes. The optimum pH (between 8,0 and 9.0) and temperature ($60-65^{\circ}C$) were similar for both isoenzymes. In the temperature range of $45-65^{\circ}C$, AAT-2 has higher thermostability than AAT-1. Both isoenzymes showed a high affinity for keto-acid substrates, as well as a higher affinity to aspartate than glutamate. Manganese ions induced an increase in both AAT isoenzymes activities, but no cooperative effect was detected. Among the inhibitors tested, hydroxylamine affected both isoenzymes activity by an irreversible inhibition mechanism.

Evaluation of Biological Activities of Invasive Alien Plants for Development of Functional Biomaterials

  • So Jin Kim;Su Hyeong Heo;Min Gun Kim;Kyung Hwan Boo;Chang Sook Kim
    • Proceedings of the Plant Resources Society of Korea Conference
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    • 2022.09a
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    • pp.112-112
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    • 2022
  • This study aims to confirm the possibility of using the invasive alien plants in Jeju as a functional biomaterial. To achieve this purpose, 70% ethanol extract and solvent fractions were prepared for five invasive alien plants (Hypochaeris radicata, Rumex acetosella, Humulus japonicus Siebold & Zucc., Solanum viarum, Lactuca scariolar) and their antioxidant, antibacterial anti-inflammatory and anti-obesity effects were investigated. The DPPH radical scavenging activity of ethanol extract from invasive alien plants was shown in the order of Rumex acetosella > Hypochaeris radicata > Humulus japonicus. Antimicrobial activity of ethanol extract against food poisoning bacteria (4 species) and oral cavity-induced microorganisms (6 species) was measured. As a result, the extract of Humulus japonicus showed high antibacterial effects against food poisoning bacteria (E. coli, V. parahaemolyticus) and oral microbes (L. casei, S. epidermidis, E. faecalis). In LPS-induced RAW 264.7 cells, the anti-inflammatory effect of ethanol extract from invasive alien plants was investigated. As a result, the NO production inhibition activity was highest in the Rumex acetosella and the Humulus japonicus Siebold & Zucc. ethanol extract, and the NO production inhibition activity was concentration-dependent. In addition, the Rumex acetosella and the Humulus japonicus Siebold & Zucc. ethanol extract showed a concentration-dependent inhibitory effect on cytokine (IL-6) production. These extracts also showed inhibitory activity of COX-2, an inflammatory protein. This suggests that NO production inhibition activity by the extract of invasive alien plants is the result of inhibition of iNOS and COX-2 expression. Currently, organic solvent fractions of crude extract are manufactured and the investigation of active ingredients is continuing along with evaluation of biological activity such as anti-inflammatory. These results are expected to be a major data for the study on the separation and utilization of active ingredients with antioxidant, antibacterial and anti-inflammatory effects using foreign plant crude extract and solvent fractions, and are highly likely to be applied to the development of functional food and cosmetics materials.

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A STUDY ON THE ANTIMICROBIAL EFFECT OF FLUORIDE-RELEASING REMOVABLE ORTHODONTIC APPLIANCES (불소유리 가철성 교정장치의 항균효과에 관한 연구)

  • Jang, Ki-Taeg
    • Journal of the korean academy of Pediatric Dentistry
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    • v.26 no.1
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    • pp.133-138
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    • 1999
  • To study the antimicrobial effect of fluoride-releasing removable orthodontic appliances, 0 wt%(Group 1), 5 wt%(Group 2) and 10 wt%(Group 3) of $CaF_2$ were added to orthodontic resin. The specimens were then put in media in which S. mutans and Lactobacillus, known cariogenic bacteria, were cultured. Inhibiting zones were measured 24, 48 and 72 hours later. The following conclusions were reached: 1 In the Lactobacillus media, no zone of inhibition was observed regardless of the time passed. 2. In the S. mutans media, zones of inhibition were observed after 48 hours. 3. S. mutans showed greater inhibition in Group 3 compared to Group 2, after 72 hours rather than 48 hours(p<0.01).

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