• Title/Summary/Keyword: p-Dinitrobenzene

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GENERATION OF p-DINITROBENZENE ATMOSPHERE AND METHEMOGLOBIN FORMATION IN RATS

  • Kim, Young-Chul
    • Toxicological Research
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    • v.5 no.2
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    • pp.97-104
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    • 1989
  • A new exposure system was developed to generate p-dinitrobenzene (p-DNB) containing atmosphere. A glass column was filled with small glass beads coated with the chemical. The p-DNB containing medium was heated to a temperature beyond the boiling point of p-DNB. A stream of air flow was forced to pass through the column and let it mixed with fresh air before introducing into an inhalation chamber. The concentration of p-DNB in the chamber air was measured by direct assaying the air directly and by sampling the chemical using a microfilter installed in the chamber.

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Characterization of a Novel Glutathione S-Transferase from Pseudomonas sp. DJ77

  • Jung, U-Hee;Cho, Young-Sik;Seong, Hark-Mo;Kim, Seong-Jae;Kim, Young-Chang;Chung, An-Sik
    • BMB Reports
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    • v.29 no.2
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    • pp.111-115
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    • 1996
  • A novel glutathione S-transferase from Pseudomonas sp. DJ77 was expressed in E. coli and purified by glutathione-affinity chromatography. The enzyme was composed of two identical subunits. The molecular size of the enzyme was 42 kDa by sephadex G-150 gel permeation chromatography and Mr of each subunit was 23 kDa by sodium dodecylsulfate-polyacrylamide gel electrophoresis. pI value of the enzyme was approximately 5.8 by isoelectric focusing. This enzyme showed the highest activity toward 1-chloro-2,4-dinitrobenzene as the electrophilic substrate. The relative activities toward p-nitrobenzyl chloride and 1,2-dichloro-4-nitrobenzene were 3.8% and 1.3% of the activity toward 1-chloro-2,4-dinitrobenzene, respectively. $K_m$ and $V_{max}$ values for 1-chloro-2,4-dinitrobenzene calculated by Lineweaver-Burk plot were 0.76 mM and $14.81\;{\mu}mol/min/mg$, respectively, and those for glutathione were 6.23 mM and $64.93\;{\mu}mol/min/mg$, respectively. The enzyme showed highest glutathione S-transferase activity at pH 8.0 and was stable between pH 6.0 and 9.0. The enzyme retained its activity up to $35^{\circ}C$ for 90 min but was unstable above $45^{\circ}C$.

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PULMONARY XENOBIOTIC CONJUGATION IN THE ISOLATED PURFUSED RABBIT LUNG AND IN VITRO: EFFECT OF ETHANOL

  • Yang, C.Mierha;Carlson, Gary P.
    • Toxicological Research
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    • v.7 no.2
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    • pp.191-208
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    • 1991
  • Pulmonary conjugation pathways may be important for the metabolism of xenobiotics introduced via airways of systemically. The objective of this study was to determine the pulmonary conjugating capacity in both the isolated perfused rabbit lung (IPRL) and in vitro, and the ability of ethanol to alter the above. The IPRL was capable of conjugating glutathione (GSH) with either 1-chloro-2,4-dinitrobenzene (CDNB) of 1,2-epoxy-(p-nitrophenoxy) propane(ENP). The pulmonary GSH conjugation with ENP was inhibited by cibacron blue, indicating the presence of glutathione-S-transferase (GST) u and/or classes, but it was not altered by buthionine sulfoximine, a selective inhibitor of Gamma-glutamylcysteine synthetase.

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Alkali-Metal Ion Catalysis and Inhibition in SNAr Reaction of 1-Halo-2,4-dinitrobenzenes with Alkali-Metal Ethoxides in Anhydrous Ethanol

  • Kim, Min-Young;Ha, Gyu Ho;Um, Ik-Hwan
    • Bulletin of the Korean Chemical Society
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    • v.35 no.8
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    • pp.2438-2442
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    • 2014
  • A kinetic study is reported for $S_NAr$ reaction of 1-fluoro-2,4-dinitrobenzene (5a) and 1-chloro-2,4-dinitrobenzene (5b) with alkali-metal ethoxides (EtOM, M = Li, Na, K and 18-crown-6-ether complexed K) in anhydrous ethanol. The second-order rate constant increases in the order $k_{EtOLi}$ < $k_{EtO^-}$ < $k_{EtONa}$ < $k_{EtOK}$ < $k_{EtOK/18C6}$ for the reaction of 5a and $k_{EtOLi}$ < $k_{EtONa}$ < $k_{EtO^-$ < $k_{EtOK}$ < $k_{EtOK/18C6}$ for that of 5b. This indicates that $M^+$ ion behaves as a catalyst or an inhibitor depending on the size of $M^+$ ion and the nature of the leaving group ($F^-$ vs. $Cl^-$). Substrate 5a is more reactive than 5b, although the $F^-$ in 5a is ca. $10pK_a$ units more basic than the $Cl^-$ in 5b, indicating that the reaction proceeds through a Meisenheimer complex in which expulsion of the leaving group occurs after the rate-determining step (RDS). $M^+$ ion would catalyze the reaction by increasing either the nucleofugality of the leaving group through a four-membered cyclic transition state or the electrophilicity of the reaction center through a ${\pi}$-complex. However, the enhanced nucleofugality would be ineffective for the current reaction, since expulsion of the leaving group occurs after the RDS. Thus, it has been concluded that $M^+$ ion catalyzes the reaction by increasing the electrophilicity of the reaction center through a ${\pi}$-complex between $M^+$ ion and the ${\pi}$-electrons in the benzene ring.

Alleviation of Atopic Dermatitis through Probiotic and Mixed-probiotic Treatments in an Atopic Dermatitis Model

  • Seo, Jae-Gu;Chung, Myung-Jun;Lee, Hyun-Gi
    • Food Science of Animal Resources
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    • v.31 no.3
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    • pp.420-427
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    • 2011
  • The use of lactic-acid bacteria (LAB) is effective for preventing and curing immune disorders by activating the immune system in the digestive tract and the consequent immune response in the blood. In this study, LAB and mixed LABs were used in an atopic dermatitis (AD) mouse model. Alleviation of AD was observed based on the change in cytokine level and immunohistochemical staining. An ex vivo test showed that immunoglobulin-E and interleukin (IL)-4 levels were significantly lower in all groups treated with LAB than in the group treated with only 1-chloro-2,4-dinitrobenzene. Results of an in vivo test based on the ex vivo results showed that the scratch score decreased in all groups treated with the LAB and particularly decreased in the group treated with mixed LABs. Additionally, the T helper (Th) 1 cytokines interferon-gamma and IL-12p40 were upregulated by the LAB and mixed-LABs, whereas levels of the Th2 cytokine IL-4 were downregulated in a mouse model of AD-like skin lesions. Furthermore, hematoxylin & eosin and immunohistochemical staining of the dorsal area of the mice in each group showed that AD improved in the LAB-treated groups. These results suggest that LAB and mixed LABs inhibit the development of AD in NC/Nga mice by suppressing the Th2 cell response and increasing the Th1 cell response. Our results indicate that mixed LABs are better than LAB for treating AD-like skin lesions.

Immunomodulatory Effects of Eurya emarginata on NC/Nga Mice as Models for Atopic Dermatitis (아토피 피부염의 동물 모델인 NC/Nga Mice에서의 우묵사스레피의 면역조절 효과)

  • Lee, Seungheon
    • Journal of Life Science
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    • v.24 no.4
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    • pp.447-453
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    • 2014
  • In this study, a test for the immunity control effect by ethanolic extract of Eurya emarginata (EE-70E) on NC/Nga mice as the models for atopic dermatitis was conducted with the following results. Atopic dermatitis in NC/Nga mice was induced by repeated application of 1-chloro-2,4-dinitrobenzene (DNCB) for 5 weeks. Mice were orally administered EE-70E or terfenadine, positive control for 3 weeks. Scratching behavior, clinical skin severity, and the levels of IL-4, L-13, IL-17, total serum IgG1, and total serum IgE were measured. The oral administration with EE-70E doses of 200 or 400 mg/kg significantly decreased scratching behavior scores and clinical skin severity score in a dose-dependent manner (p<0.05). The administration of EE-70E at 400 mg/kg significantly decreased cytokines within the blood serum, that is, IL-4, L-13, and IL-17 compared to the control group (p<0.05). The level of blood histamine was statistically significantly decreased. Administration of EE-70E at 400 mg/kg significantly decreased the levels of total serum IgE (p<0.05). The above results indicated that EE-70E was effective in improving the symptoms of atopic dermatitis through various immunity control mechanisms.

p38 MAPK Inhibitor NJK14047 Suppresses CDNB-Induced Atopic Dermatitis-Like Symptoms in BALB/c Mice

  • Lee, Ju-Hyun;Son, Seung-Hwan;Kim, Nam-Jung;Im, Dong-Soon
    • Biomolecules & Therapeutics
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    • v.30 no.6
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    • pp.501-509
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    • 2022
  • Atopic dermatitis (AD) is a chronic inflammatory skin disorder. Suppression of MAPKs and NF-κB is implicated as a vital mechanism of action of several traditional Chinese medicines for AD therapy. Although overexpression of MAPK mRNA in the skin tissue has been shown in the AD model, the roles of each MAPK in AD pathogenesis have rarely been studied. This study examined the effect of NJK14047, an inhibitor of p38 MAPKs, on AD-like skin lesions induced in BALB/c mice by sensitization and challenges with 1-chloro-2,4-dinitrobenzene (CDNB) on dorsal skin and ears, respectively. After induction of AD, NJK14047 (2.5 mg/kg) or dexamethasone (10 mg/kg) was administrated for 3 weeks via intraperitoneal injection. Following its administration, NJK14047 suppressed CDNB-induced AD-like symptoms such as skin hypertrophy and suppressed mast cell infiltration into the skin lesions. It also reduced CDNB-induced increase in TH2 cytokine (IL-13) and TH1 cytokines (interferon-γ and IL-12A) levels but did not decrease serum IgE level. Furthermore, NJK14047 blocked CDNB-induced lymph node enlargement. These results suggest that NJK14047, a p38 MAPK inhibitor, might be an optimal therapeutic option with unique modes of action for AD treatment.

Cloning and expression of glutathione S-transferase (GST) cDNA from Gossypium hirsutum L.

  • Kang, Won-Hee;Kim, Myong-Jo;Lim, Jung-Dae;Yun, Song-Joong;Chung, Ill-Min;Yu, Chang-Yeon
    • Korean Journal of Medicinal Crop Science
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    • v.10 no.4
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    • pp.294-297
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    • 2002
  • A gene coding for the GST of cotton (Gh-5) was cloned into Escherichia coli and experssed. The enzyme remained within the cytoplasm of E. coli. An 696 bp open reading frame was in the 988 base pair fragment of the recombinant plasmid pET-30b(+). The deduced protein sequence consists of 232 amino acids and has a molecular mass of 30235.58 Da. The cloned enzyme conjugated reduced glutathione and 1-chloro-2,4-dinitrobenzene (CDNB). Plant GST cDNA was expressed in microbe and produced polypeptide had function as an enzyme.

Studies on the Antifungal Action of Leather in Korea (Part. 2) (한국에서의 피혁방미에 관한 연구 2)

  • 김종협;장건형;최춘언
    • Korean Journal of Microbiology
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    • v.3 no.1
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    • pp.18-23
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    • 1965
  • It seems like that the characteristics and drug-resistances of fungi are respectively different in various circumstances. Scores of chemicals were applicated to the leather-fungi in this study. M-dinitrobenzene, 2, 4-dinitrochlorobenzene and phenyl mercuric acetate inhibited the growth of Aspergilli which were isolated from Korean-leather. The minimum fungicidal limits of p-nitrophenol, 8-hydroxyquinoline and sodium-pentachlorophenolate against the Korean-originated strains are different from that of other country. In the mass-screening of fungicides, artificial "Leather-extracts media" have been designed and used, and the media contributed to screening-tests. Fat and oils which are the materials of fat-liquoring in leather manufacture affects the drugresistance of the leather-fungi. It is found that the accelerating-method on malt-agar plate is effective to determinate the fungicidal action of chemicals in short time.hort time.

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Effect of Glucose-diethyldithiocarbamate on Drug Metabolizing Enzymes in Rats (Glucose-diethyldithiocarbamate가 흰쥐의 약물 대사 효소에 미치는 영향 연구)

  • 최병기;신혜주
    • Biomolecules & Therapeutics
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    • v.8 no.4
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    • pp.299-304
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    • 2000
  • The modulation of cytochrome P450(P450) activities and glutathione S-transferase (GST) was investigated after i.p. administration of glucose-diethyldithiocarbamate (Glu-DDTC) to rats. P450 1 A2 and 2El activities were inhibited by 60% 4 hr after the administration of 200 mg Glu-DDTC/kg and those activities were recovered to original levels 24 hr after dosing. In contrast, GST activities were enhanced up to 24 hr after dosing. These results seem to be due to the bifunctional activity of Glu-DDTC. Glu-DDTC acts as an inhibitor of P450 enzymes as well as inducer of GST enzyme. Glu-DDTC inhibited PNP hydroxylation (P450 2El) and ethoxycoumarin O-deethylation (P450 1A2) in a dose-dependent manner up to 200 mg/kg wherease it did not affect testosterone 6$\beta$-hydroxylation (P450 3A) and pentoxyresorufin O-dealkylation (P450 2B) activities. Induction of GST activity toward 1-chloro-2,4-dinitrobenzene (CDNB) and 1,2-dichloro-4-nitrobenzenen (DCNB) was dependent on the dose of Glu-DDTC and no species difference in the GST induction was seen between rat and mouse. Amoung GST subunits, Ya, Yb1 and partially Yb2 were induced by Glu-DDTC as conjugated by western blotting. The levels Yp, Yk and Yc subunits were not affected by Glu-DDTC treatment. Therefore the enhanced activity of GST toward CDNB and DCNB might be due to the induction of Ya, Ybl and partially Yb2 subunits. In conclusion, Glu-DDTC selectively inhibited P45O 1A2 and P450 2El activities whereas it enhanced Ya, Ybl subunits and partially Yb2 subunits of GST and the antimutagenic activity of this compound might be attributed from the modulation of these enzyme activities in animals.

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