• Archives of Pharmacal Research
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• 제14권2호
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• pp.130-136
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• 1991

Nicotine (100 .mu. M) was incubated with microsomes (1 mg/ml) prepared from New Zealand White rabbits. On the basis of microsomal weight, the rate of nicotine oxidation were calculated on the basis of cytochrome P-450 concentration, the specific activity of the metabolic oxidation catalyzed by lung was approximately 4 times greater than liver (6.4 vs 1, 65 nmoles nicotine oxidized. nmole cytochrome $P-450^{-1}\;min{-1})$. These studies employed several methods of altering activities of specific isozymes present in pulmonary microsomes, including the use of the isozyme2 and 6 specific inhibitor $\alpha$-methylbenzyl ABT, metabolite inhibitors, norbenzphetamine and N-hydroxyamphetamine. TCDD induction and Arochlor 1260 pretreatment. These results support the conclusion that nicotine metabolism by rabbit lung microsomes is mediated primarily by cytochrome P-450 isozyme 2.

• Journal of Microbiology and Biotechnology
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• 제19권4호
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• pp.368-371
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• 2009

In the course of screening for the melanogenesis inhibitors, aspochalasin I was isolated from solid-state culture of Aspergillus sp. Fb020460. Its structure was determined by spectroscopic analysis including mass spectroscopy and NMR analysis. Aspochalasin I potently inhibited melanogenesis in Mel-Ab cells with an $IC_{50}$ value of $22.4{\mu}M$ without cytotoxicity.

• Journal of Microbiology and Biotechnology
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• 제17권10호
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• pp.1717-1720
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• 2007

In the course of screening for nitric oxide inhibitors in activated microglial BV-2 cells, cyclo(dehydrohistidyl-L-tryptophyl) was isolated from solid-state fermentation cultures of an unidentified fungal strain, Fb956. Its structure was determined by spectroscopic methods including 2D NMR and chiral TLC analyses. Cyclo(dehydrohistidyl-L-tryptophyl) was found to have an inhibitory activity on nitric oxide production with an $IC_{50}$ of $6.5\;{\mu}M$ in activated BV-2 cells. The structure determination and biological activity of cyclo(dehydrohistidyl-L-tryptophyl) was reported for the first time in this study.

• Journal of Microbiology and Biotechnology
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• 제17권3호
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• pp.543-545
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• 2007

4-Hydroxy-3-(3'-methyl-2'-butenyl)-benzoic acid (HMBA) was previously isolated from Curvularia sp. KF119 as a cell-cycle inhibitor. However, the present study used a novel and practical synthetic method to prepare a large quantity of HMBA. The synthetic HMBA was found to inhibit the cell-cycle progression of HeLa cells with a comparable potency to the natural fungal metabolite. The inhibition of the cell-cycle progression by the synthetic HMBA involved both the activation of $p21^{WAF1}$ and the inhibition of cyclin D1 expression in the cells. Consequently, this new synthetic procedure provides an easy and convenient way to produce or manipulate the original fungal metabolite.

• Journal of Microbiology and Biotechnology
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• 제18권6호
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• pp.1115-1120
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• 2008

A novel cathepsin B inhibitor-producing bacterium was isolated from marine sediments and identified based on its 16S rDNA sequence as Pseudomonas sp. strain PB01 (Accession No. EU126129). The growth and enzyme inhibitor production were investigated under various culture conditions. A mixture of organic nitrogen source was required for the optimal production, whereas both glucose and maltose proved to be the effective carbon sources for cathepsin B inhibitor production. Other optimal culture conditions included temperature range between 25 and $28^{\circ}C$, initial medium pH of 6.6, and shaking speed of 200 rpm. Under these optimal conditions, the maximum inhibitory activity from culture broth was approximately 50% after 30 h of cultivation. Additionally, kinetic study revealed that inhibitor production paralleled with cell growth, which suggested that the inhibitor may be a primary metabolite of that bacterium.

• 생약학회지
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• 제15권1호
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• pp.15-23
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• 1984

To find antimicrobial strains of the soil microorganisms in Korea, they were isolated from the soil samples of different locations and screened for antibiotic activity against several standard microbes. An isolate among them had an antibacterial activity against gram-positive bacteria. The examination of its morphological and biochemical characteristics according to the International Streptomyces Project methods showed that it belongs to the genus Streptomyces. The strain was named DMC-72. The strain appears to be a new strain when it was compared with the species within the genus which have been so far reported. The antibiotic metabolite of the strain was produced in submerged culture method. It was found to be a quinone compound and was named soulomycin. This strain was also found to produce an ${\alpha}-amylase$ inhibitor in the submerged culture.

• Toxicological Research
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• 제14권3호
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• pp.349-356
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• 1998

We identified S9940, a novel microbial metabolite from Streptomyces spp., to inhibit the release of neurotransmitter from PC12 cells. S9940 is an inhibitor of trifiated norepinephrine ([$^{3}H$]-NE) release in high $K^+$ buffer solution containing ionomycin, indicating that S9940 inhibits neurotransmitter release after the influx of $Ca^{2+}$ ions. We also examined the effect of S9940 on $\beta-glucuronidase$ release from guinea pig neurophils and the effect on the neurite extension of PC12 cells and rat hippocampal neurons. As a result, S9940 inhibited $\beta-glucuronidase$ release: when treated with $5{\mu}g/ml$ of S9940, which prevented [$^{3}H$]-NE release, the inhibition of neurite extension for both PC12 cells and rat hippocampal neurons was observed.

• 한국전자통신학회논문지
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• 제11권10호
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• pp.969-982
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• 2016

최근 천연물로부터 신약 후보물질을 개발하려는 연구가 활발히 이루어지고 있다. 인체 내에서 천연물은 주로 효소에 의해 대사된다. 본 연구는 화합물의 인체내 대사반응과 주로 관련된 효소에 의한 대사반응의 특징을 연관규칙마이닝을 활용하여 분석한다. 화합물이 인체 내에서 효소 대사반응과 관련된 데이터를 BRENDA(: BRaunschweig ENzyme DAtabase)로부터 수집하였다. 수집된 데이터를 효소대사반응의 기본 틀에 근거하여, 대사물들을 기질대사물, 생성대사물, 억제대사물, 그리고 활성대사물들로 구분한다. 이러한 대사물들로 이루어진 기질대사물 트랜잭션, 생성대사물 트랜잭션, 그리고 모든 대사물들을 포함한 효소반응트랜잭션들을 구성하였다. 또한 종 정보를 반영한 6개의 트랜잭션들로 구성하였다. 연관규칙 마이닝을 활용하여 6개의 트랜잭션에서 빈발대사물 및 패턴을 분석하였다. 또한 대사물들 사이의 관련성을 분석하였다. 그 결과 효소대사반응에 참여하는 대사물들의 분포와 패턴을 식별할 수 있었다. 더욱이 기질에만 속하는 순수 기질대사물들을 식별하였고 이들 대부분이 아주 낮은 지지도임을 확인할 수 있었다. 연구결과는 순수 기질대사물은 효과적인 대사변환 예측 모델 개발에 활용될 수 있다.

• Food Science and Biotechnology
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• 제15권4호
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• pp.647-649
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• 2006

Mevinolin, a fungal metabolite, is a potent inhibitor of 3-hydroxy-methyl-3-glutaryl-coenzyme A (HMG-CoA) reductase, the rate-controlling enzyme in cholesterol biosynthesis. In this investigation, the optimum factors for mevinolin production by Monascus pilosus IFO 480 in soymeal fermentation were studied. The highest yield of mevinolin, 2.82 mg mevinolin per g dry weight, without citrinin (a toxic fungal secondary metabolite) was obtained after 21 days of fermentation at $30^{\circ}C$ at 65% moisture content, particle size 0.6-0.9 mm, and initial substrate pH of 6.0. Mevinolin was present in the fermentation substrate predominantly in the hydroxycarboxylate form (open lactone, 92.1-97.3%), which is currently being used as a hypocholesterolemic agent.

• 대한약학회:학술대회논문집
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• 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.1
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• pp.310.1-310.1
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• 2003

SD-2007 ia an apicidin analogue, possessing a potent histone deacetylase inhibiting activity. A rapid and senstive LC/MS method was developed for the determination of SD-2007 and its major active metabolite. apicidin. in rat serum. SD-2007 and apicidin was extracted by liquid-liquid extraction using methyl t-butyl ether. SD-2007 and apicidin were monitored in a SIM mode at m/z of 679 and 622, respectively. (omitted)