• 제목/요약/키워드: metabolite M2

검색결과 284건 처리시간 0.023초

홍국균 발효 메밀에서의 rutin과 monacolin K의 함량 변화 (Content of Rutin and Monacolin K in the Red Buckwheat Fermented with Monascus ruber)

  • 강동주;엄주방;이성구;이종훈
    • 한국식품과학회지
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    • 제35권2호
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    • pp.242-245
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    • 2003
  • 좋은 아미노산 조성의 단백질과 높은 식이섬유 함량을 비롯한 좋은 영양조성을 가지고 있어 건강기능식품의 재료로 주목을 받고 있는 메밀에는 항산화효과, 혈압강하작용 등에 효과가 있는 것으로 알려진 rutin이라는 flavonol 배당체가 많이 함유되어 있다. 홍국의 제조에 쓰이는 Monascus속 곰팡이는 cholesterol 생합성 저해효과를 나타내는 monacolin K라는 대사산물을 생산하는 것으로 보고되었다. 본 연구에서는 두가지 성분을 모두 함유한 건강기능식품의 제조를 위해 도정메밀과 발아시킨 도정메밀을 이용한 홍국을 제조하여 두가지 성분의 변화를 검토하였다. 도정메밀의 발아에 따른 rutin 함량은 초기에 약간 감소하였으나 싹의 길이에 비례하여 증가했고, 홍국균의 증식이 메밀에 함유된 rutin 함량에는 영양을 미치지 않는 것으로 나타났다. 발아시킨 도정메밀로 제조한 홍국의 monacolin K 함량은 발아시키지 않은 도정메밀에서 보다 낮게 나타났으며, 메밀 싹 길이의 증가에 따라 monacolin K 함량은 점차 감소하는 것으로 나타났다. 발아시킨 메밀을 이용한 홍국의 제조에서는 발아에서 오는 탄소원 및 영양분 감소가 홍국균의 증식에 영향을 주어 monacolin K의 함량을 떨어뜨리는 것으로 추정된다.

신장 세포에서 Levamisole의 세포내 Alkaline Phosphatase 활성 증가 (Increase of Cellular Alkaline Phosphatase Activity by Levamisole in Kidney Cells)

  • 황준일;김종환;김주일;이경태;권창호
    • Journal of Pharmaceutical Investigation
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    • 제26권4호
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    • pp.309-314
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    • 1996
  • The purpose of this study is to explain the relationship between the pharmacological mechanism of levamisole and the cellular activity of cellular alkaline phosphatase (ALPase) in kidney cells. The results of our investigation were as follows. 1. Cellular ALPase activity in Macacus rhesus monkey kidney cells (MA 104 cells) and primary cultured rabbit kidney proximal tubular cells treated with levamisole was increased about two or three times than control. However, 50% of ALPase activity in cultured medium was inhibited by levamisole itself. 2. The proliferation of MA 104 and cultured rabbit kidney proximal tubular cells was linearly decreased in paralleled with increase of levamisole concentration $(50\;and\;500\;{mu}M)$ with MTT test. 3. In the heat stability tests, the inhibition of ALPase activity with and without levamisole at $56^{\circ}C$ in MA 104 cells showed different $IC_{50}$ values. 4. HPLC analysis of levamisole metabolites produced by cultured MA 104 cells suggested that the formation of a metabolite, that may be associated with its increase of cellular ALPase activity. Based on these results, we assumed that the increase of cellular ALPase activity by levamisole was evoked by modification of the ALPase catalytic sites.

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Light/Dark Responsiveness of Kinetin-Inducible Secondary Metabolites and Stress Proteins in Rice Leaf

  • Cho, Kyoung-Won;Kim, Dea-Wook;Jung, Young-Ho;Shibato, Junko;Tamogami, Shigeru;Yonekura, Masami;Jwa, Nam-Soo;Kubo, Akihiro;Agrawal, Ganesh Kumar;Rakwal, Randeep
    • Journal of Crop Science and Biotechnology
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    • 제10권2호
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    • pp.112-116
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    • 2007
  • Kinetin(KN) is an inducer of rice(Oryza sativa L.) defense/stress responses, as evidenced by the induction of inducible secondary metabolite and defense/stress protein markers in leaf. We show a novel light-dependent effect of KN-triggered defense stress responses in rice leaf. Leaf segments treated with KN(100 ${\mu}M$) show hypersensitive-like necrotic lesion formation only under continuous light illumination. Potent accumulation of two phytoalexins, sakuranetin and momilactone A(MoA) by KN that peaks at 48 h after treatment under continuous light is completely suppressed by incubation under continuous dark. Using two-dimensional gel electrophoresis we identified KN-induced changes in ribulose-1, 5-bisphosphate carboxylase/oxygenase, energy- and pathogenesis-related proteins(OsPR class 5 and 10 members) by N-terminal amino acid sequencing and mass spectrometry. These changes were light-inducible and could not be observed in the dark(and control). Present results provide a new dimension(light modulation/regulation) to our finding that KN has a potential role in the rice plant self-defense mechanism.

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Liquid Chromatography-Tandem Mass Spectrometric Analysis of Nannozinone A and Its Application to Pharmacokinetic Study in Mice

  • Lee, Chul Haeng;Kim, Soobin;Lee, Jaehyeok;Jeon, Ji-Hyeon;Song, Im-Sook;Han, Young Taek;Choi, Min-Koo
    • Mass Spectrometry Letters
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    • 제12권1호
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    • pp.21-25
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    • 2021
  • We aimed to develop and validate a sensitive analytical method of nannozinone A, active metabolite of Nannochelins A extracted from the Myxobacterium Nannocytis pusilla, in mouse plasma using a liquid chromatography-tandem mass spectrometry (LC-MS/MS). Mouse plasma samples containing nannozinone A and 13C-caffeine (internal standard) were extracted using a liquid-liquid extraction (LLE) method with methyl tert-butyl ether. Standard calibration curves were linear in the concentration range of 1 - 1000 ng/mL (r2 > 0.998) with the inter- and intra-day accuracy and precision results less than 15%. LLE method gave results in the high and reproducible extraction recovery in the range of 78.00-81.08% with limited matrix effect in the range of 70.56-96.49%. The pharmacokinetics of nannozinone A after intravenous injection (5 mg/kg) and oral administration (30 mg/kg) of nannozinone A were investigated using the validated LC-MS/MS analysis of nannozinone A. The absolute oral bioavailability of nannozinone A was 8.82%. Plasma concentration of nannozinone A after the intravenous injection sharply decreased for 4 h but plasma concentration of orally administered nannozinone A showed fast distribution and slow elimination for 24 h. In conclusion, we successfully applied this newly developed sensitive LC-MS/MS analytical method of nannozinone A to the pharmacokinetic evaluation of this compound. This method can be useful for further studies on the pharmacokinetic optimization and evaluating the druggability of nannozinone A including its efficacy and toxicity.

Clinical Factors Affecting the Serum Retention of a Teratogenic Etretinate after the Acitretin Administration

  • Jeong, Jong Heon;Hyun, Gyu Hwan;Park, Yu Jeong;Kwon, Sung Won;Lee, Ai-Young
    • Biomolecules & Therapeutics
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    • 제30권6호
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    • pp.562-569
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    • 2022
  • Etretinate, an acitretin metabolite, has a long retention duration in adipose tissues with a teratogenic potential. FDA advises a contraceptive period of at least three years after discontinuing acitretin. However, the effect of accumulated etretinate in adipose tissues on fetus is unknown. Although the teratogenic threshold for serum concentration of etretinate has been presented as higher than 2 ng/mL, that of acitretin is unknown. To examine factors affecting body retention of acitretin and etretinate, effects of acitretin dosage, acitretin-taking duration, elapsed time after stopping acitretin, age, sex, concomitant alcohol consumption, and foods and supplements rich in vitamin A intake on serum concentrations of acitretin and etretinate were analyzed in 14 acitretin-taken patients and 58 controls without taking acitretin or etretinate. Serum concentrations of acitretin, but not etretinate, tended to be inversely related to the discontinuation duration. They were also related to old age. Different from a published result that alcohol consumption could promote the metabolism of acitretin into etretinate, alcohol intake did not affect serum concentrations of etretinate. Unexpectedly, more frequent intake of vitamin A or provitamin A-rich food and supplements was associated with higher serum acitretin, whereas less frequent intake of vitamin A or provitamin A-rich food and supplements was associated with higher serum levels of etretinate in acitretin-taken patients. Despite preliminary data, inter-individual variations in serum retention of etretinate suggest the necessity of further research before applying the same guidelines to everyone to minimize unnecessary contraception.

Production and Identification of Secondary Metabolite Gliotoxin-Like Substance Using Clinical Isolates of Candida spp.

  • Noorulhuda Ojaimi Mahdi, Al-Dahlaki;Safaa Al-Deen Ahmed Shanter, Al-Qaysi
    • 한국미생물·생명공학회지
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    • 제50권4호
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    • pp.488-500
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    • 2022
  • Most fungal infections by opportunistic yeast pathogens such as Candida spp. are the major causes of morbidity and mortality in patients with lowered immune. Previous studies have reported that some strains of Candida secret secondary metabolites play an important role in the decreasing of immunity in the infected patient. In this study, 110 Candida spp. were isolated from different clinical specimens from Baghdad hospitals. Candida isolates were identified by conventional methods, they were processed for Candida speciation on CHROMagar. The results of identification were confirmed by internal transcribed spacer (ITS) sequencing. Phylogenetic trees were analyzed with reference strains deposited in GenBank. Antifungal susceptibility testing was evaluated by the disc diffusion method and performed as recommended by the Clinical and Laboratory Standard Institute (CLSI) M44-A document. Candida isolates investigated produce secondary metabolites gliotoxin with HPLC technique and quantification. Out of 110 Candida isolates, C. albicans (66.36%) was the most frequent isolate, followed by the isolates of C. tropicalis (10.9%) and C. glabrata (6.36%) respectively. Concerning the antifungal susceptibility test, Candida isolates showed a high level of susceptibility to Miconazole (70.9%), Itraconazole (68.2%), and Nystatine (64.5%). The ability of obtained isolates of Candida spp. to produce gliotoxin on RPMI medium was investigated, only 28 isolates had the ability to secret this toxin in culture filtrates. The highest concentrations were detected in C. albicans (1.048 ㎍/ml). Gliotoxin productivity of other Candida species was significantly lower. The retention time for gliotoxin was approximately 5.08 min.

LC-MS/MS를 이용한 농산물 중 Isoxaflutole과 대사산물(Diketonitrile)의 동시시험법 개발 (Development of Simultaneous Analytical Method for Determination of Isoxaflutole and its Metabolite (Diketonitrile) residues in Agricultural Commodities Using LC-MS/MS)

  • 고아영;김희정;도정아;장진;이은향;주윤지;김지영;장문익;이규식
    • 농약과학회지
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    • 제20권2호
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    • pp.93-103
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    • 2016
  • Isoxaflutole은 isoxazole계 화합물로 광엽잡초의 체내로 흡수되어 plastoquinone의 합성에 관여하는 4-hydroxy-phenylpyruvate dioxygenase (HPPD)를 저해하거나 carotenoid의 생합성을 억제하는 이행성 제초제이다. 본 연구에서는 국내 신규농약 isoxaflutole에 대한 안전관리를 위해 농산물 중 isoxaflutole 및 diketonitrile의 잔류시험법을 개발하였다. 농산물 시료(감귤, 감자, 고추, 현미, 대두) 중 isoxaflutole 및 diketonitrile을 0.1% acetic acid in water/acetonitrile (2/8, v/v)으로 추출한 뒤 dichloromethane을 이용해 분배한 후, LC-MS/MS로 분석하였다. 시험법의 직선성은 농도 대비 피크면적과의 결정계수($r^2$)가 0.997 이상으로 우수하였으며, 검출한계 및 정량한계는 각각 0.003, 0.01 mg/kg으로 높은 감도를 나타냈다. 농산물 시료 중 모든 처리구에서 평균 회수율은 72.9%-107.3% (RSD 9% 이내)였고, 타실험실과의 실험실간 검증 결과에서도 72.4-111.0%를 나타내어 검증 결과는 모두 CODEX 가이드라인(CAC/GL 40, 2003)의 기준이내를 만족하는 값으로 확인되었다. 따라서 개발된 시험법의 낮은 검출한계 및 정량한계, 우수한 직선성, 회수율 시험을 통한 양호한 정밀성 및 재현성 등이 입증되어 농산물 중 isoxaflutole 및 diketonitrile을 분석하기 위한 식품공전 공정시험법으로 활용하고자 한다.

rvH1N1 Neuraminidase Inhibitory Activities of Phenolics from Perilla frutescens (L.) and Their Contents in Cultivars and Germplasm

  • Ha, Tae Joung;Lee, Myoung-Hee;Park, Chang-Hwan;Kim, Jung-In;Oh, Eunyoung;Pae, Suk-Bok;Park, Jae Eun;Kim, Sung-Up;Kwak, Do-Yeon
    • Plant Breeding and Biotechnology
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    • 제6권4호
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    • pp.404-412
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    • 2018
  • The influenza neuraminidase (NA, E.C. 3.2.1.18), an antiviral, has been the target of high pharmaceutical companies due to its essential role in viral replication cycle. Perilla frutescens (P. frutescens) is used in traditional Chinese medicine for various diseases, such as cold due to wind-cold, headache and cough. In this context, four major polyphenolic compounds including rosmarinic acid-3-O-glucoside (1), rosmarinic acid (2), luteolin (3), and apigenin (4) isolated from P. frutescens were evaluated for their inhibitory effect on recombinant virus H1N1 neuraminidase (rvH1N1 NA). Among the test compounds, rosmarinic acid and luteolin inhibited the rvH1N1 NA with an $IC_{50}$ of 46.7 and $8.4{\mu}M$, respectively. The inhibition kinetics analyzed by the Dixon plots indicated that rosmarinic acid and luteolin were noncompetitive inhibitors and that the inhibition constant, $K_I$, was established as 43.9 and $14.3{\mu}M$, respectively. In addition, 578 genetically diverse accessions and 39 cultivars of P. frutescens were analyzed using HPLC to characterize the diversity of polyphenolic composition and concentration. The individual and total compositions exhibited significant difference (P < 0.05), especially rosmarinic acid which was detected as the predominant metabolite in all accessions (58.8%) and cultivars (62.8%). Yeupsil and Sangback cultivars exhibited the highest rosmarinic acid ($3,393.5{\mu}g/g$) and luteolin ($383.3{\mu}g/g$) content respectively. YCPL177-2 with the high concentration ($889.8{\mu}g/g$) of luteolin may be used as a genetic resource for breeding elite cultivars.

경엽 및 관주처리에 따른 배추 중 Trifloxystrobin의 안전성 평가 (Risk Assessment of Trifloxystrobin in Chinese Cabbage by Foliar Application and Drenching)

  • 안설화;이상복;안문호;김재덕
    • 농약과학회지
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    • 제11권1호
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    • pp.27-31
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    • 2007
  • HPLC에 의한 배추 중 trifloxystrobin의 회수율은 $84.6{\sim}95.3%$이었고 대사산물인 CGA321113의 회수율은 $86.4{\sim}87.3%$이었으며, 검출한계는 모두 0.04 mg $kg^{-1}$이었다. 경엽처리시 배추 중 trifloxystrobin 잔류량은 수확 5일과 6일전 2회 처리, 수확 3일과 7일전 3회 처리에서 모두 농약잔류허용기준(temporary MRL, 0.5 mg $kg^{-1}$)을 초과하였다. 관주처리 배추에서의 trifloxystrobin 잔류량은 기준량(1500배 희석액 주당 150 mL) 및 배량(1500배 희석액 주당 300 mL)처리에서 각각 0.16, 0.31 mg $kg^{-1}$으로 MRL 미만이었다. 따라서 살균제 trifloxystrobin(22% 액상수화제)를 사용하여 배추 재배시 농약잔류허용기준에 의하여 토양처리가 안전할 것으로 사료되며 경엽처리시 안전사용기준으로 부적합하다고 판단된다.

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

  • 서미정;김여운;신윤용
    • 한국환경성돌연변이발암원학회지
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    • 제24권4호
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    • pp.198-205
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    • 2004
  • Cytochrome P4501B1(CYP1B1) is known to be inducible by xenobiotic compounds 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 Hepa-I and MCF-7 cells, 5' flanking DNA of human CYP1B1 was cloned into pGL3 basic vector containing luciferase gene, and then transfected into these cells. After treatment of chemicals, the luciferase activity was measured. CYP1B1 enzyme metabolize PAHs and estradiol. CYP1B1 metabolize estradiol to 4-hydrozyestradiol that is considered as carcinogenic metabolite. Recent industrialized industrialized society, human has been widely been exposed to widespread environmental contaminants such as PAHs(polycyclic aromatic hydrocarbon) that are originated from the imcomplete 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 biomarker for PAHs. Therefore we have studied the effect of PAHs in the human breast cancer cells MCF-7 to evaluate bioactivity of PAHs. We have used the United State of America EPA selected 13 different PAHs, PAHs mixtures and extracts from environmental samples to evaluate the bioassay system. We examined effects of PAHs on the CYP1B1-luciferase reporter gene and CYP1B1 mRNA level. Benzo(k)fluoranthene and dibenzo(a, h)anthracene showed strong response to CYP1B1 promoter activity stimulation, and also CYP1B1 mRNAs increase in MCF-7 cells in a concentration-dependent manner. RT-PCR analysis indicated that PAHs significantly up-regulate the level of CYP1B1 mRNA. Some flavonoids such as genistein, daidzein, chrysin, naringenin and morin were also investigeted. These flavonoids decreased B(k)F infuced luciferase activity at low concentration. But, these flavonoids exhibited stimulatory effect at high concentration.

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