• 약학회지
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• 제54권5호
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• pp.398-402
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• 2010

[ ${\alpha}$ ]Glucosidase inhibitor is a target in the treatment of type II diabetes through the mainly inhibition of glucose levels after meals. In this study, we purified steppogenin and oxyresveratrol from the stem of Morus alba L. and examined their inhibitory activity against yeast ${\alpha}$-glucosidase. Steppogenin and oxyresveratrol were inhibited yeast ${\alpha}$-glucosidase in a dose dependent manner. The $IC_{50}$ activities (50% inhibition) were 34.4 and 9.3 ${\mu}M$, respectively. The kinetic inhibition of steppogenin showed noncompetitive inhibition ($K_m:1.1{\times}10^{-3}M$; $K_i:1{\times}10^{-5}M$), meanwhile oxyresveratrol showed competitive inhibition ($K_m:4.3{\times}10^{-3}M$; $K_i:3.4{\times}10^{-6}M$) against yeast ${\alpha}$-glucosidase. These results indicate that steppogenin and oxyresveratrol are noncompetitive and competitive inhibitors, respectively, against yeast ${\alpha}$-glucosidase.

• 대한환경공학회지
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• 제22권11호
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• pp.2037-2046
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• 2000

산성 혹은 염기성 pH가 활성슬러지 공정에 미치는 저해 작용은 비경쟁적 저해 동력학(noncompetitive inhibition kinetics)을 따르는 것으로 알려져 있으나, pH를 저해 물질의 농도항으로 정량화하기 어렵기 때문에 실질적으로 비경쟁적 저해 동력학식(noncompetitive inhibition kinetic equation)으로 해석하기 어렵다. 따라서 pH에 의한 저해 작용을 기술하는 경험식들이 여러 연구자들에 의해 개발되어 왔는데, 이들은 주로 산성 조건에 대해서만 적용 가능한 것들이다. 본 연구에서는 의사독성농도(pseudo toxic concentration, $C_{PT}$) 개념을 이용하여 pH가 활성슬러지 공정에 미치는 저해 영향을 정량화하는 기법을 개발하였고, 기존에 알려진 모델들과 비교하였다. 그 결과 $C_{PT}$ 개념을 이용한 모델은 넓은 범위의 pH에 대해 최대비성장속도(${\mu}_{max}$)의 감소를 비교적 정확하게 예측할 수 있었고, 같은 동력학식을 이용하여 산성 조건뿐만 아니라 염기성 조건에 대해서도 적용 가능한 것으로 나타났다. 또한 저해계수(inhibition coefficient. $K_I$)의 추정이 간단하다는 장점이 있다.

• BMB Reports
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• 제32권4호
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• pp.385-392
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• 1999

The $NAD^+$-specific activity of a dual coenzyme-specific isocitrate dehydrogenase (IDH; EC 1.1.1.41) from the primitive fungus Pythium ultimum was investigated to elucidate the regulatory factors that may influence the intracellular distribution of carbon and the availability of intermediates, e.g. citrate, for fatty acid synthesis. Inhibition of $NAD^+$-IDH activity by diphospho- and triphosphonucleotides (ATP, ADP, and GTP) reflected the sensitivity of this enzyme to cellular energy charge even though monophosphonucleotides (AMP and GMP) had little effect on activity. NADPH, but not NADH, substantially inhibited $NAD^+$-IDH activity, showing noncompetitive inhibition with isocitrate. Oxalacetate and ${\alpha}$-ketoglutarate showed competitive inhibition with isocitrate, while citrate and cis-aconitate showed mixed-noncompetitive inhibition with isocitrate. Inhibition by these substances ranged from 29 to 46% at 10 mM. The inhibitory effect of oxalacetate was increased synergistically by glyoxylate, which alone caused 31% uncompetitive inhibition at 10 mM, and a mixture of the two substances at 1 mM each showed 98% inhibition of $NAD^+$-IDH activity. The regulation of $NAD^+$-IDH in Pythium ultimum seems to be a complex process involving mitochondrial metabolites. The addition of glyoxylate (3 mM) and oxalacetate (3 mM) to the culture medium resulted in the production of 49% more lipid by P. ultimum.

• KSBB Journal
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• 제8권4호
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• pp.341-350
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• 1993

본 연구에서는 sMMO를 갖는 메탄 자화균인 M. triclwsporium OB3b를 이용하여 메탄올 생산을 위한 기초실험을 수행하였다. 중요한 결과를 요약하면 다음과 같다(Table 2). 1. 세포 내 NADH의 재생을 위해 개미산을 첨가 할 때 whole-cell의 sMMO 활성은 pH 7.0 및 $30^{\circ}C$ 에서 최대값을 보이며 propylene을 기질로 할 경우 약 130nmol/mg cell min 정도이다. 2. 인산은 MMO와 MDH 활성을 모두 저해하나 M MDH에 대한 저해 정도가 훨씬 크므로 메탄올 합성 에 사용이 가능하다. Noncompetitive mode를 가정 할 때 저해상수는 각각 185mM(MMO) 및 42mM ( (MDH)이었다. 3. 메탄올은 MMO 활성을 저해하며 noncompeti­t tive mode를 가정할 때 propylene기질의 경우 2 21mM 이었다. 4. 균체 내 sMMO 활성은 성장이 멈춰진 상태에 셔 비교적 때}른 속도로 감소하며 고농도 인산용액에 서 그 속도가 더 빨라진다. 5. 인산농도 91mM에서 메탄은 메탄올로 산화되 어 축적되며 4.5시간 동안 에탄올의 생성속도는 평 균 79nmol/mg min이었다.

• 한국응용약물학회:학술대회논문집
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• 한국응용약물학회 1996년도 춘계학술대회
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• pp.247-247
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• 1996

Previous work in our laboratory has shown that noncompetitive N-methyl-D-aspartate (NMDA) receptor antagonists, MK-801, ketamine, dextrorphan and dextromethorphan cause a pronounced inhibition of apomorphine-induced cage climbing behavior in intact mice, suggesting the involvement of NMDA receptors in the glutamatergic modulation of dopaminergic function at the postsynaptic dopamine (DA) receptors: Therefore, in order to definitively establish the involvement of NMDA receptor in the apomorphine-induced dopaminergic response at the postsynaptic DA receptor, it is necessary to investigate whether or not the noncompetitive NMDA receptor antagonists would inhibit these phenomena not only in intact mice but also in the mice that are devoid of any involvement of indirect dopaminergic function. To minimize the risk of any indirect involvement of NMDA antagonists with DA neurons, vesicular DA stores were first depleted with reserpine.

• Journal of Applied Biological Chemistry
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• 제62권1호
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• pp.81-86
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• 2019

A yellow resin (gamboge) from Garcinia hanburyi has been widely used as folk medicine due to its antibacterial and antitumor activities. We isolated four ${\alpha}$-glucosidase inhibitory compounds from the methanol extract of gamboge. The compounds (1-4) were identified as gambogoic acid (1), moreollic acid (2), gambogic acid (3), and 10-methoxygambogenic acid (4), respectively through spectroscopic data including 2D-NMR and HREIMS. All compounds were examined in the enzyme inhibition assay against ${\alpha}$-glucosidase to identify their inhibitory potencies and kinetic behavior. All compounds (1-4) showed enzyme inhibition against ${\alpha}$-glucosidase, but the activity was significantly affected by the methoxy group on C-10 of ring A and pentenyl pyran moiety of ring D. For example, compound 1 ($IC_{50}=41.4{\mu}M$) bearing pyran ring eight times effective that 4 ($IC_{50}=350.6{\mu}M$) having geranyl group itself. Most active compound was found out to be gambogoic acid (1) which was analyzed most abundant metabolite in gamboge by LC-ESI-MS/MS. In kinetic study, compounds 1 and 2 were proved as noncompetitive inhibitors.

• 한국잡초학회지
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• 제17권1호
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• pp.66-70
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• 1997

(주)LG화학에서 개발중엔 LGC-40863은 벼에 대해 높은 안전성을 보이며 피 등 여러 잡초를 방제하는 신규제초제이다. LGC-40863은 관련 제초제나 식물에서의 효과 발현 증상으로 부터 acetolactate synthase(ALS)를 저해하는 것으로 추정된다. 본 연구에서는 LGC-40863의 ALS에 대한 영향을 알아보기 위하여 벼와 피로부터 추출한 ALS를 사용하여 $I_{50}$값과 효소반응속도를 조사하였다. LGC-40863의 $I_{50}$값은 14(벼), 16mM(피)였고, 대조약제로 사용한 imazapyr와 chlorsulfuron의 $I_{50}$값은 각각 12-15mM, 0.03-0.04mM였으므로 LGC-40863의 $I_{50}$값은 imazapyr와 유사하고 chlorsulfuron에 비해서는 약 400배 정도 높았다. 그리고 세 가지 약재 모두 벼와 피 간의 감수성 차이는 크지 않았다. 효소반응속도 면에서 살펴보면, LGC-40863은 벼와 피 모두 pyruvate에 대해 noncompetitive inhibition을 나타내었으며, chlorsulfuron과 imazapyr는 벼에서 각각 noncompetitive와 uncompetitive inhibition을 하는 것으로 나타났으므로 LGC-40863은 chlorsulfuron과 저해유형이 비슷하였다.

• Journal of Microbiology and Biotechnology
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• 제8권3호
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• pp.287-290
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• 1998

Acarbose effectively inhibited the synthesis of dextran, and the inhibition pattern was a noncompetitive type with a $K_i$ value of 1.35 mM. It also inhibited the disproportionation reaction of dextransucrase with isomaltotriose and decreased the efficiency of the maltose acceptor reaction. Increased concentration of dextransucrase or maltose in reaction digests, however, decreased the degree of inhibition by acarbose.

• Journal of Applied Biological Chemistry
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• 제66권
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• pp.1-6
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• 2023

Dendranthema zawadskii is a one of the popular plants as native in South Korea. In this study, linarin was isolated and purified using silica-gel, Diaion, and Sephadex LH-20 from the aerial parts of D. zawadskii. The chemical structure was completely identified through spectroscopic data including 1D, 2D nucleic magnetic resonance, and HRFABMS. Furthermore, linarin inhibited the bacterial neuraminidase (BNA) activity with 13.5 μM of IC₅₀ dose-dependently. Through the enzyme kinetic experiments, linarin as BNA inhibitor exhibited a typical noncompetitive inhibition mode which K_m was contestant and V_max decreased as the concentration of the inhibitor increased. It was further identified that the inhibition constant was 16.0 μM. Linarin was the most abundance metabolite in the aerial part of D. zawadskii extract by UHPLC-TOF/MS analysis. Therefore, D. zawadskii and its main component are expected that it can be effectively used for the infection and inflammation caused by bacteria.

• Journal of Microbiology and Biotechnology
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• 제18권7호
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• pp.1298-1307
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• 2008

In this study, we investigated the inhibition effects of single and mixed heavy metal ions ($Zn^{2+},\;Ni^{2+},\;Cu^{2+},\;and\;Cd^{2+}$) on iron oxidation by Acidithiobacillus ferrooxidans. Effects of metals on the iron oxidation activity of A. ferrooxidans are categorized into four types of patterns according to its oxidation behavior. The results indicated that the inhibition effects of the metals on the iron oxidation activity were noncompetitive inhibitions. We proposed a reduced inhibition model, along with the reduced inhibition constant ($\alpha_i$), which was derived from the inhibition constant ($K_I$) of individual metals and represented the tolerance of a given inhibitor relative to that of a reference inhibitor. This model was used to evaluate the toxicity effect (inhibition effect) of metals on the iron oxidation activity of A. ferrooxidans. The model revealed that the iron oxidation behavior of the metals, regardless of metal systems (single, binary, ternary, or quaternary), is closely matched to that of any reference inhibitor at the same reduced inhibition concentration, $[I]_{reduced}$, which defines the ratio of the inhibitor concentration to the reduced inhibition constant. The model demonstrated that single metal systems and mixed metal systems with the same reduced inhibitor concentrations have similar toxic effects on microbial activity.