• Title/Summary/Keyword: 카테콜

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Action Mechanism of LB10522, a New Catechol-Substituted Cephalosporin (카테콜 치환체를 가진 세파로스포린계 항생제 LB10522의 작용기전)

  • Kim, Mu-Yong;Oh, Jeong-In;Paek, Kyoung-Sook;Kim, In-Chull;Kwak, Jin-Hwan
    • YAKHAK HOEJI
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    • v.40 no.1
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    • pp.102-111
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    • 1996
  • LB10522 is a new parenteral broad spectrum cephalosporin with a catechol moiety at C-7 position of beta-lactam ring. This compound can utilize tonB-dependent iron transp ort system in addition to porin proteins to enter bacterial periplasmic space and access to penicillin-binding proteins (PBPs) which are the lethal targets of ${\beta}$-lactam antibiotics. The chelating activity of LB10522 to metal iron was measured by spectrophotometrically scanning the absorbance from 200 to 900nm. When $FeCl_3$ was added, optical density was increased between 450 and 800nm. LB10522 was more active against gram-negative strains in iron-depleted media than in iron-replete media. This is due to the increased expression of iron transport channels in iron-depleted condition. LB10522 showed a similar activity against E. coli DC2 (permeability mutant) and E. coli DCO (wild type strain) in both iron-depleted and iron-replete media, indicating a minimal permeaility barrier for LB10522 uptake. LB10522 had high affinities to PBP 3 and PBP 1A, 1B of E. coli. By blocking these proteins, LB10522 caused inhibition of cell division and the eventual death of cells. This result was correlated well with the morphological changes in E. coli exposed to LB10522. Although the in vitro MIC of LB10522 against P. aeruginosa 1912E mutant (tonB) was 8-times higher than that of the P. aeruginosa 1912E parent strain, LB10522 showed a similar in vivo protection efficacy against both strains in the mouse systemic infection model. This result suggested that tonB mutant, which requires a high level of iron for normal growth, might have a difficulty in surviving in their host with an iron-limited environment.

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Inhibition of Enzymatic Browning of Crown Daisy by Maillard Reaction Products (마이얄반응생성물(Maillard reaction product)에 의한 쑥갓의 효소적갈면 억제)

  • Kim, Ji-Hae;Song, Hyeon-Seung;Park, Inshik
    • Journal of Life Science
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    • v.22 no.11
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    • pp.1451-1455
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    • 2012
  • The study was conducted to investigate the effect of Maillard reaction products (MRPs) on enzymatic browning of crown daisy (Chrysanthmum coronarium var. spatiosum). The MRPs prepared by heating various amino acid and sugar at $90^{\circ}C$ caused a strong inhibitory effect on crown daisy polyphenol oxidase (PPO, ${\sigma}$-diphenol oxygen oxidoreductase, EC 1.10.3.1). As the reaction time of the solution containing glycine and glucose increased at $90^{\circ}C$, the production of MRPs was increased, whereas the amounts of glycine and glucose were decreased. Accordingly, the inhibitory effect of crown daisy PPO activity by MRPs was increased as the amounts of synthesized MRPs were increased. The MRPs synthesized from the various amino acids and sugars significantly reduced the PPO activity, particularly MRPs prepared by glutamine and xylose. The Michealis-Menten constant value ($K_m$) of crown daisy PPO with catechol as a substrate was 22.0 mM, and MRPs were a noncompetitive inhibitor against crown daisy PPO.

Application of Stress Hormones in Saliva in Research of Orofacial Pain Related with Stress (스트레스와 관련된 구강안면통증의 연구에 있어서 타액내의 스트레스호르몬의 활용)

  • Ryu, Ji-Won;Yoon, Chang-Lyuk;Ahn, Jong-Mo
    • Journal of Oral Medicine and Pain
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    • v.32 no.2
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    • pp.201-210
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    • 2007
  • Many diseases occur by stress or effect of stress. The basis for using hormones in research of stress is the observation that most systems in the body show changes during stress and that hormonal markers in these changes are related with stress. Conceptually, the central role of sympathetic nervous system(SNS) and hypothalamus-pituitary-adrenal(HPA) axis activity in stress provides copious justification for measuring hormonal changes. Catecholamines like epinephrine and norepinephrine, cortisol, testosterone and growth hormone and so on show sensitive reaction to stress. The major advantage of salivary sample to stress research is that its sampling technique can be performed in non-stressful conditions and without physical restraint and ethical problems. Because hormone levels in saliva is a good reflection of hormone levels in plasma, application of stress hormones in saliva is very useful for research of orofacial pain related with stress.

Simultaneous Determination of Catecholamines, Serotonin and Their Metabolites in the Biological Sample Using HPLC/ECD (생체 시료 중 카테콜 아민류, 세로토닌 및 대사물질들의 HPLC/ECD 동시 정량분석)

  • Min, Ji-Hyun;Hahn, Young-Hee
    • YAKHAK HOEJI
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    • v.55 no.4
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    • pp.277-283
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    • 2011
  • Simultaneous monitoring of catecholamines and serotonin with their appropriate extraction from the biological samples is required in order to understand thoroughly the regulation of the central and peripheral nervous system. In the present research the segmented gradient elution with the solid phase extraction using a C18 cartridge rather than the previous isocratic elution with alumina extraction is successfully employed to determine norepinephrine (NE), epinephrine (E), dopamine (DA), serotonin (5HT), 3,4-dihydroxyphenylacetic acid (DOPAC) and 5-hydroxyindoleacetic acid (5HIAA) simultaneously within 20 minutes using 3,4-dihydroxyhydrocinnamic aicd as the internal standard (IS). Linearities were obtained in the concentration range between $5{\times}10^{-6}M$ and $1{\times}10^{-4}M$ for all 7 compounds with detection limits of 0.6~1.9 ${\mu}M$. The present HPLC/ECD method yielded reasonable accuracy (relative error; -1.4~1.1%) and precision (relative standard deviation; 0.4~1.9%) for 9 measurements of the standard solution consisting of NE, E, DA, 5HT, DOPAC and 5HIAA compounds. Recoveries of catecholamines, serotonin and their metabolites from human serum were in the range of 57%~86%. While the concentrations of NE and 5HT in the serum of normal Sprague-Dawley rat were found as $1.4{\times}10^{-6}M$ and $2.6{\times}10^{-6}M$, respectively, the contents of NE and 5HT in the serum of the stressed rat were increased 5.6 times and 1.4 times more, respectively.

Recent progress on polydopamine surface chemistry (폴리도파민 표면화학: 발명 10 년의 이야기)

  • Eom, Soomin;Park, Hong Key;Park, Jihyo;Hong, Seonki;Lee, Haeshin
    • Journal of Adhesion and Interface
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    • v.19 no.1
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    • pp.19-29
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    • 2018
  • Polydopamine coating is one of the most straightforward and widely used method for surface modification inspired by adhesiveness of mussel foot protein contributed by co-existence of catechol and amine. This technique has been utilized not only in surface modification but other numerous fields of study as well. For the past decade, the subject of polydopamine has been thoroughly studied since the initial polydopamine research published in 2007, including its chemical structure, coating conditions, and material characteristics. In this study, we report the current trends and progress of polydopamine coating methods, the newly developing areas of polydopamine related research such as using dopamine derivatives and polyphenolic compounds, improvement of various functionalization and application of polydopamine coating, and explain the state of current attempts to discover the chemical mechanism, structure, and properties of polydopamine.

Riboflavin Status Influences the Biosynthesis of Flavin Peptides and Related Enzyme Activities in Rat Liver Mitochondria (리보플라빈 결핍이 쥐간의 미토콘드리아의 플라빈 펩티드와 관련된 효소 활성에 미치는 영향)

  • Shin, Sook;Kim, Jae-Young;Park, In-Kook
    • The Korean Journal of Zoology
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    • v.38 no.4
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    • pp.498-504
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    • 1995
  • The effeds of riboflavin defidency on the biosynthesis of flavin pepddes and levels of flavoenzymes and catecholamines have been investigated. The percentage of 14C. riboflavin radioactivity formed in mitochondria appeared to increase up to 2 weeks but started to decline at 3 weeks. A significant increase of radioactivity incorporation into mitochondria and into trypsin-digestable plus trypsin-non-digestibie flavin peptides was detected in riboflavin-deficient animals. More than 35% of incorporation was observed at the end of the first week and 160% higher incorporation was observed in fiavin peptide after the second week. Activities of MAO and succinate dehydrogenase were affected markedly by riboflavin status whereas those of acetyichoilnesterase were not affected. Riboflavin defidency also brought about marked reductions in levels of epineplrrine and norepinephrine. it is concluded that the levels of flavin peptides, MAO and succinate dehydrogenase, and catecholamines were affected significanily by the availability of riboflavin and in particular the duration of its depiction.

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Effects of Catecholamine on the Fusion of Chick Embryo Myoblasts in vitro (鷄胚筋原細胞의 融合에 미치는 카테콜아민의 影響)

  • Kang, Man-Sik;Ha, Doo-Bong;Lee, Chung-Choo;Park, Yung-Chul;Hyockman Kwon
    • The Korean Journal of Zoology
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    • v.27 no.2
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    • pp.73-84
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    • 1984
  • In order to investigate the effect of neurotransmitter on myoblast differentiation in vitro, the effects of dopamine and epinephrine on myoblast fusion and on the intracellular cAMP level in cultured myoblasts were examined. Dopamine $(3\\times10^{-5}M)$ and epinephrine $(3\\times10^{-5}M)$, when added at 34 hr after cell plating, markedly inhibited myoblast fusion, and dopamine was more potent than epinephrine. Both dopamine and epinephrine had no effect on intracellular cAMP level. At the same time, exogeneous dbcAMP, $PGE_1$, and aspirin were used to examine whether cAMP is involved in myoblast differentiation. dbcAMP $(1\\times10^{-4}M)$ inhibited myoblast fusion, whereas $PGE_1 (3\\times10^{-6}M)$ had no inhibitory effect, rather enhancing myoblast fusion. Aspirin, an inhibitor of PG synthetase, was shown to inhibit myoblast fusion. Possible mechanism by which dopamine or epinephrine at a specific concentration used inhibits myoblast fusion is discussed.

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Targeting Catecholamines to Develop New Drugs for Attention Deficit Hyperactivity Disorder (주의력결핍 과잉행동장애 치료제 개발을 위한 카테콜아민계 표적화)

  • Sung-Cherl Jung;Chang-Hwan Cho;Hye-Ji Kim;Eun-A Ko;Min-Woo Ha;Oh-Bin Kwon
    • Journal of Medicine and Life Science
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    • v.18 no.3
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    • pp.41-48
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    • 2021
  • The prevalence of attention deficit hyperactivity disorder (ADHD), a developmental neuropsychiatric disorder, is high among children and adolescents. The pathogenesis of ADHD is mediated with genetic, biological, and environmental factors. Most therapeutic drugs for ADHD have so far targeted biological causes, primarily by regulating catecholaminergic neurotransmitters. However, ADHD drugs that are clinically treated have various problems in their addictiveness and drug stability; thus, it is recommended that efficacy and safety should be secured through simultaneous prescription of multiple drugs rather than a single drug treatment. Accordingly, it is necessary to develop drugs that newly target pathogenic mechanisms of ADHD. In this study, we attempt to confirm the possibility of developing new drugs by reviewing dopamine-related developmental mechanisms of neurons and their correlation with ADHD. Histone deacetylase inhibitors (HDACi) can regulate the concentration of intracellular dopamine in neurons by expressing vesicular monoamine transporter 2 and inducing the exocytosis of neurotransmitters to the synaptic cleft, thereby promoting the development of neurons and signal transmission. This cellular modulation of HDACi is expected to treat ADHD by regulating endogenous catecholamines such as dopamine. Although studies are still in the preclinical stage, HDAC inhibitors clearly have potential as a therapeutic agent with low addictiveness and high efficacy for ADHD treatment.

Inhibition of Adrenergic Agonists-induced Metastatic Ability of Liver Cancer Cells by Ethanol Extract of Premature Citrus Unshiu Peel (청피 에탄올 추출물이 스트레스성 카테콜아민으로 유도한 간암세포의 전이를 억제하는 효과 및 기전 연구)

  • Shin-Hyung Park
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.38 no.1
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    • pp.10-15
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    • 2024
  • Previous studies have highlighted the pivotal role of the β-adrenergic receptor (β-AR) signaling pathway in stimulating cancer metastasis induced by chronic stress. According to the theory of traditional Korean medicine, chronic stress can induce Qi stagnation. Based on the traditional role of premature citrus unshiu peel in moving Qi, we hypothesized that an ethanol extract of premature citrus unshiu peel (EPCU) can attenuate chronic stress-induced cancer progression. In this study, we investigated the potential role of EPCU on modulating the adrenergic agonists-induced metastatic properties of liver cancer cells. Our findings revealed that adrenergic agonists, including norepinephrine (NE), epinephrine (E), and isoproterenol (ISO), augmented the migratory capacity of Hep3B human hepatocellular carcinoma cells, which was completely abrogated by EPCU treatment in a concentration-dependent manner. Consistently, EPCU inhibited the E-induced invasive property of Hep3B cells in a dose-dependent manner. These results suggest that EPCU efficiently attenuates adrenergic agonists-induced metastatic abilities of liver cancer cells. As a molecular mechanism, EPF suppressed the phosphorylation of major components of β-AR signaling pathway, including Src, signal transducer and activator of transcription 3 (STAT3) and ERK, induced by E treatment. Taken together, our results demonstrate that EPCU impedes the adrenergic agonists-driven metastatic potential of cancer cells by inhibiting β-AR signaling pathway. This study provides basic evidence supporting the probable use of premature citrus unshiu peel to prevent metastasis in liver cancer patients under chronic stress.

Adhesive Polyethylene Glycol Coatings for Low Biofouling Copper-Zinc Alloy Substrates (황동 표면의 생물 부착 억제를 위한 접착성 폴리에틸렌글라이콜 코팅)

  • Sang-woo Lee;Hyun Ho Shin;Seokjun Kwon;Ji Hyun Ryu
    • Journal of Adhesion and Interface
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    • v.24 no.3
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    • pp.105-111
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    • 2023
  • Recently, there has been a growing interest in low biofouling coatings for various industrial applications including precious metal and jewelry applications. Contaminations including cells and bacteria of the metallic substrates (i.e., accessories, earring, and piercings) may irritate the contacted tissue surfaces or induce an abnormal reaction. In this study, catechol-conjugated polyethylene glycol (PEG-C) was synthesized as low bio-fouling coating materials inspired by mussel-adhesion. PEG-C-coated copper-zinc alloy surfaces showed excellent cell viability and significant inhibitions of protein and cell adhesions to metal surfaces. Thus, PEG-C coating methods and PEG-C-coated metallic substrates can be usefully exploited for versatile industrial applications, particularly for precious metal and jewelry industries.