• 제목/요약/키워드: metabolite M4

검색결과 204건 처리시간 0.019초

Isolation and Characterization of Aniline-Degrading Bacteria

  • Kahng, Hyung-Yeel;Kim, Seung-Il;Woo, Mi-Jeong;Park, Yong-Keun;Lee, Yung-Nok
    • 미생물학회지
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    • 제30권3호
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    • pp.199-206
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    • 1992
  • Six isolated strains degrading aniline were selected, identified and designated as pseudomonas putida K6, Pseudomonas acidovorans K82, Achromobacter gr. D. V. K24, Achromobacter xylosocidans K4, Moraxella sp. K21 and Moraxella sp. K22. All of them degraded 1000 ppm aniline completely within 30 to 36 hours. Most of these strains are resistant to antibiotics more than one, but Moraxella sp. has not any antibiotic marker tested. Most strains except for P. acidovorans K82 were shown to have resistance to the heavy metal ions such as Ni, Cu, Li, Ba, Co, etc. but not to Hg to which only P. putida K6 was resistant. M. sp. K21 was capable of degrading aniline to a maximum concentration of 2500 ppm without any repression. The incubation of the cell in limited pH ranges (4-8) had no great effect on aniline degradation. The addition of bactopeptone to the minimal media promoted the speed of aniline degradation, but the addition of glucose rather repressed the rate of aniline degradation. Through enzyme assay, A. gr. D. V. K 24 was shown to degrade aniline through artho-pathway and formed .betha.-ketoadipate as intermediate metabolite.

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Protein Binding of Disopyramide -Displacement by Mono-N-Dealkyl-Disopyramide and Variation with Commerial Source of Alpha-1-Acid Glycoprotein-

  • Haughey, David B.;Steinberg, Irving;Lee, Min-Hwa
    • Journal of Pharmaceutical Investigation
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    • 제15권1호
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    • pp.1-7
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    • 1985
  • Previous studies show that the free (unbound) fraction of disopyramide in human serum is drug concentration dependent~ at corresponding serum disopyramide concentrations that are achieved clinically. $^1^{\sim}^3^)\;Moreover$, disopyramide free fraction values vary several fold at any given drug concentration in human serum and tend to decrease as serum cocentrations of alpha-I-acid glycoprotein(AAG) incrase.$^4^)$ A recent $study^5^)$ demonstrates that the free fraction of disopyramide inhuman serum increases almost 2-fold following the addition of $14.4{\mu}M/L$ mono-N-dealkyldisopyramide. These studies and others. $^6^),\;^7^)$ prompted the present investigation to characterize the protein binding of disopyramide in human serum and solutions of AAG in the presence of mono-N-dealkyldisopyramide (a major metabolite of, disopyramide) and to determine the utility of using commercially available alpha-I-acid glycoprotein for drug protein binding displacement studies. Because many basic and acidic compounds are known to bind to alpha-I-acid $glycoprotein^8^)$ the present study. was performed to determine whteher commercially available AAG would provide a convenient protein source for such binding studies.

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Inhibition of Red Ginseng on 5-Hydroxyeicosatetraenoic Acid (5-HETE) Biosynthesis from Arachidonic Acid in Helicobacter Pylori-infected Gastric Cells

  • Park Soo-Jin
    • Nutritional Sciences
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    • 제9권3호
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    • pp.152-158
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    • 2006
  • Helicobacter pylori (H. pylori) infection rapidly stimulated either COX-2 or 5-LOX and released arachidonic acid metabolites that have been considered as pivotal mediators in H. pylori-induced inflammatory responses. To determine whether red ginseng extract (RGE) can suppress the biosynthesis of 5(S)-hydroxyeicosatetraenoic acids (HETE), a precursor metabolite of leukotrienes B4 (LTB4) in H. pylori-provoked inflammatory responses in gastric epithelial cells, the biosynthesis of monohydroxy fatty acids was measured using radioactive arachidonic acid and validated by RP-HPLC using non-radioactive AA as substrate in AGS cells cocultured with H. pylori (ATCC 43504) with or without pretreatment of RGE. Among three known major HETEs, H. pylori infection specifically induced the biosynthesis of $^{14}C-5(S)-HETE$ rather than the complex of $^{14}C-15S-/^{14}C-12(S)-HETE$ from $^{14}C-AA$, concomitantly obtained by HPLC(p<0.01). RGE, 1 to $100{\mu}g/ml$, selectively suppressed H. pylori-stimulated $^{14}C-5(S)-HETE$ production implying the attenuation of 5-lipoxygenase activity, of which was similar to known LOX inhibitor NDGA $(10{\mu}M)$ (p<0.01). However, the amount of 5(S)-HETE was significantly reduced by higher dose of RGE $(100{\mu}g/ml)$ (p<0.05). These results indicated that LOX pathway might be one of principle pathogenic mechanisms of H. pylori and red ginseng could be a nutraceutical against H. pylori infection through inhibiting action of LOX activity.

Simultaneous Electroanalysis of Nitric Oxide and Nitrite

  • Oritani, Tadato;Okajima, Takeyoshi;Kitamura, Fusao;Ohsaka, Takeo
    • 전기화학회지
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    • 제5권4호
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    • pp.209-211
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    • 2002
  • The simultaneous sensing of nitric oxide (NO) and its metabolite, nitrite $(NO_2^-)$ has been studied by Osteryoung square-wave voltarnmetery (OSWV) in physiological pH solution (0.1 M phosphate buffer solution, pH 7.2). Using an electrochemically pretreated glassy carbon (GC) electrode, OSWV was successfully applied to observe the well-separated oxidation peaks at ca. 0.58 and 0.80V vs. Ag/AgCI for NO and $(NO_2^-)$, respectively. This clear separation between the NO and $(NO_2^-)$ oxidation peaks may be due to the formation of surface oxides (e.g., quinone (C=O) or carboxylic $(COO^-)$ group) and surface defects introduced by the electrochemical pretreatment of GC electrodes.

Pharmacokinetic Changes in Drugs during Protein-Calorie Malnutrition: Correlation between Drug Metabolism and Hepatic Microsomal Cytochrome P450 Isozymes

  • Lee, Joo-Hyun;Suh, Ok-Kyung;Lee, Myung-Gull
    • Archives of Pharmacal Research
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    • 제27권7호
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    • pp.693-712
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    • 2004
  • The rats with protein-calorie malnutrition (PCM, 5% casein diet for a period of 4-week) were reported to exhibit 60 and 80% suppression in the hepatic microsomal cytochrome P450 (CYP) 1 A2 and CYP2C11 levels, respectively, and 40-50% decreases in CYP2E1 and CYP3A 1/2 levels compared to control (23% casein diet for a period of 4-week) based on Western blot analysis. In addition, Northern blot analysis showed that CYP1 A2, CYP2E1, CYP2C11, and CYP3A1/2 mRNAs decreased in the state of PCM as well. Hence, pharmacokinetic changes of the drugs in rats with PCM [especially the area under the plasma concentration-time curve from time zero to time infinity (AUC) changes of metabolite(s)] reported from literatures were tried to explain in terms of CYP isozyme changes in the rats. Otherwise, the time-averaged nonrenal clearance ($CL_{NR}$) of parent drug was compared. Pharmacokinetic changes of the drugs in other types of malnutritional state, such as kwashiorkor and marasmus, in both human and animal models were also compared. The drugs reviewed are as follows: diuretics, antibiotics, anticancer agents, antiepileptics, antiarrythmics, analgesics, xanthines, antimalarials, and miscellaneous.

Cometabolism of $\omega$-Phenylalkanoic Acids with Butyric Acid for Efficient Production of Aromatic Polyesters in Pseudomonas putida BM01

  • Song, Jae-Jun;Choi, Mun-Hwan;Yoon, Sung-Chul;Huh, Nam-Eung
    • Journal of Microbiology and Biotechnology
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    • 제11권3호
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    • pp.435-442
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    • 2001
  • Poly(3-hydroxy-5-phenylvalerate) [P(3HPV)] was efficiently accumulated from 5-phenylvalerate (5PV) in Pseudomonas putida BM01 in a mineral salts medium containing butyric acid (BA) as the cosubstrate. A nove aromatic copolyester, poly(5 mol% 3-hydroxy-4-phenylbutyrate-co- 95 mol% 3-hydroxy-6-phenylhexanoate) [P(3HPB-co-3HPC)] was also synthesized from 6-phenylhexanoate (6PC) plus Ba. The two aromatic polymers, P(3HPV) and P(3HPB-co-3HPC), were found to be amorphous and showed different glass-transition temperatures at $15^{\circ}C$ and $10^{\circ}C$, respectively. When the bacterium was grown ina medium containing 20 mM 5PV as the sole carbon source for 140 h, 0.4 g/l of dry cells was obtained in a flask cultivation and 20 wt% of P(3HPV) homopolymer was accumulated in the cells. However, when it was grown with a mixture of 2 mM 5PV and 50 mM BA for 40 h, the yield of dry biomass was increased up to 2.5 g/l and the content of P(3HPV) in the dry cells was optimally 56 wt%. This efficient production of P(3HPV) homopolymer from the mixed substrate was feasible because BA only supported cell growth and did not induce any aliphatic PHA accumulation. The metabolites released into the PHA synthesis medium were analyzed using GC or GC/MS. Two $\beta$-oxidation derivatives, 3-phenylpropionic acid and trans-cinnamic acid, were found in the 5V-grown cell medium and these comprised 55-88 mol% of the 5PV consumed. In the 6PC-grown medium containing Ba, seven ${\beta}$-oxidation and related intermediates were found, which included phenylacetic acid, 4-phenylbutyric acid, cis-4-phenyl-2-butenoic acid, trans-4-phenyl-3-butenoic acid, trans-4-phenyl-2-butenoic acid, 3-hydroxy-4-phenylbutyric acid, and 3-hydroxy-6-phenylhexanoic acid. Accordingly, based on the metabolite analysis, PHA synthesis pathways from the two aromatic carbon sources are suggested.

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Characterization of Norepinephrine Release in Rat Posterior Hypothalamus Using in vivo Brain Microdialysis

  • Sung, Ki-Wug;Kim, Seong-Yun;Kim, Ok-Nyu;Lee, Sang-Bok
    • The Korean Journal of Physiology and Pharmacology
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    • 제6권1호
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    • pp.9-14
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    • 2002
  • In the present study, we used the microdialysis technique combined with high performance liquid chromatography (HPLC) and electrochemical detection to measure the extracellular levels of norepinephrine (NE) in the posterior hypothalamus in vivo, and to examine the effects of various drugs, affecting central noradrenergic transmission, on the extracellular concentration of NE in the posterior hypothalamus. Microdialysis probes were implanted stereotaxically into the posterior hypothalamus (coordinates: posterior 4.3 mm, lateral 0.5 mm, ventral 8 mm, relative to bregma and the brain surface, respectively) of rats, and dialysate collection began 2 hr after the implantation. The baseline level of monoamines in the dialysates were determined to be: NE $0.17{\pm}0.01,$ 3,4-dihydroxyphenylacetic acid (DOPAC) $0.94{\pm}0.07,$ homovanillic acid (HVA) $0.57{\pm}0.05$ pmol/sample (n=8). When the posterior hypothalamus was perfused with 90 mM potassium, maximum 555% increase of NE output was observed. Concomitantly, this treatment significantly decreased the output of DOPAC and HVA by 35% and 28%, respectively. Local application of imipramine $(50\;{\mu}M)$ enhanced the level of NE in the posterior hypothalamus (maximum 200%) compared to preperfusion control values. But, DOPAC and HVA outputs remained unchanged. Pargyline, an irreversible monoamine oxidase inhibitor, i.p. administered at a dose of 75 mg/kg, increased NE output (maximum 165%), while decreased DOPAC and HVA outputs (maximum 13 and 12%, respectively). These results indicate that NE in dialysate from the rat posterior hypothalamus were neuronal origin, and that manipulations which profoundly affected the levels of extracellular neurotransmitter had also effects on metabolite levels.

GC/MS를 이용한 carteolol의 대사 및 배설연구 (Study on Metabolism and Excretion of Carteolol in Human Urine using GC/MS)

  • 민혜기;김명수;조현우;김택제;김동현;명승운
    • 분석과학
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    • 제15권5호
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    • pp.482-487
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    • 2002
  • Carteolol은 국제올림픽위원회 (IOC)에서 금지약물로 규정하고 있는 ${\beta}$-차단제 중의 하나이다. 본 실험에서는 GC/MS를 사용하여 사람의 소변으로부터 carteolol의 복용여부를 확인하기 위한 검출방법 및 대사와 배설에 대해서 고찰하였다. 이를 위하여 효소 가수분해방법과 산 가수분해방법을 비교하여 보았는데 효소가수분해방법이 더 좋은 결과를 얻을 수 있었다. 효소 가수분해방법을 이용하여 실험한 결과 RSD 10%내외의 정밀도와 $0.05{\mu}g/m{\ell}$를 제외하고는 오차 5%이내의 좋은 정확도를 보여주었으며 회수율은 78.5%로 나타났다. Carteolol은 소변에서 대부분이 free carteolol과 conjugated carteolol로 존재하며 소량의 p-OH-carteolol로 대사됨을 알 수 있었으며 모 약물로 배출되는 양 중 conjugated form이 59.4%로 나타났다. 소변으로 배출된 carteolol의 양을 측정한 결과 복용양의 49%가 복용 후 72시간까지 모 약물로 배출됨을 알 수 있었다.

Genistein이 Benzo(k)fluoranthene에 의한 CYP1B1 유전자조절 작용에 미치는 영향 (Effect of Genistein on the Benzo(k)fluoranthene Regulated CYP1B1 Gene Expression)

  • 서미정;신윤용
    • 한국환경성돌연변이발암원학회지
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    • 제24권4호
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    • pp.163-170
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    • 2004
  • CYP1B1 enzyme metabolize PAHs and estradiol. CYP1B1 metabolize estradiol to 4-hydroxyestradiol that is considered as carcinogenic metabolite. Luciferase activity was induced about 20 folds over that control by 1 nM TCDD (2,3,7,8-tetrchlorodibenzo-p-dioxin) and these inductions were dose-dependent. Recent industrialized society, human hasbeen widely been exposed to widespread environmental contaminants such as PAHs (polycyclic aromatic hydrocarbon) that are originated from the incomplete combustion of hydrocarbons. PAHs are known to be ligands of the AhR (aryl hydrocarbon receptor). Induction of cytochrome P4501B1(CYP1B1) in cell culture is widely used as a biomarket for PAHs. Therefore we have studied the effect of PAHs in the human breast cancer cells MCF-7 to evaluate bioactivity of PAHs. Cytochrome P4501B1(CYP1B1) is known to be inducible by xenobiotic compounda such as policyclic aromatic hydrocarbon (PAH) and dioxins such as 2,3,7,8-tetrachloro-dibenzo-p-dioxin(TCDD). And these induction of CYP1B1 is also regulated by many categories of chemicals. In order to investigate the effects of several chemicals on CYP1B1 gene expression in luciferase gene, and then transfected into these cells. After treatment of chemicals, the luciferase activity was measured. We examined effects of PAHs on the CYP1B1-lucifrease reporter gene and CYP1B1 mRNA level. Benzo(k)fluoranthene showed strong response to CYP1B1 promoter activity stimulation, and also CYP1B1 mRNAs increase in MCF-7 cells in a concentration-dependent manner. flvonoids such as genistein decreased B(k)F induced luciferase activity at low concentration. it exhibited stimulatory effect at high concentration.

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인축의 뇨 중 aflatoxin $M_1$의 오염분석 및 위해성 평가 (Detection of Aflatoxin $M_1$ in Human and Porcine Urine and Its Risk Assessment)

  • 김현정;곽보연;손동화
    • 한국식품과학회지
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    • 제41권2호
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    • pp.215-219
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    • 2009
  • $AFB_1$의 대사산물 중 하나인 $AFM_1$을 사람과 돼지의 뇨에서 cdELISA를 통해 분석함으로써 간접적으로 $AFB_1$의 위해성 평가를 수행하고자 하였다. 항 $AFM_1$ 항체와 ${AFB_1}-HRP$를 이용한 cdELISA에서 $AFM_1$의 검출한계는 10 pg/mL로 나타났다. 사람의 요에 $AFM_1$을 3-100 pg/mL 농도가 되게 첨가한 후 cdELISA로 분석하였을 때 그 회수율은 117-167%(평균 139${\pm}$19.1)의 범위로 나타났다. 사람의 뇨 중 $AFM_1$의 오염량을 cdELISA로 분석한 결과 전체 172개의 시료 중 165개의 시료에서 평균 2.74${\pm}$1.89 pg/mL 농도로 검출되었다. 뇨 중 $AFM_1$의 일일배출량은 평균 3.97 ng/day으로 나타났고, $AFB_1$의 섭취량은 체내전환율 5%로 가정하였을 때, 79.4 ng/day로 추정되었다. 따라서 사람의 일일섭취추정량 (PDI)은 1.28 ng/kg bw/day로 나타났으며 돼지의 PDI는 9.2 ng/kg bw/day로 나타났다. 한편 $AFB_1$ 섭취의 위해성 평가에서 사람의 PDI는, 일일섭취감내량(TDI, 0.15 ng/kg bw/day)보다 8.5배나 높은 값을 보였지만 외국의 연구결과와 비교하였을 때 대체로 비슷하게 나타났다.