• Title/Summary/Keyword: -glucosidase inhibitor

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Effect of 1-deoxynojirimycin on the Replication of Baculoviruses, Bombyx Mori Nucleopolyhedrovirus and Autographa Californica Multiple Nucleopolyhedrovirus

  • Kang, Kyung-Don;Park, Joo-Sung;Cho, Yong-Seok;Park, Young-Shik;Lee, Jae-Yeon;Hwang, Kyo-Yeol;Yuk, Won-Jeong;Kamita, Shizuo George;Suzuki, Koichi;Seong, Su-Il
    • International Journal of Industrial Entomology and Biomaterials
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    • v.23 no.1
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    • pp.123-128
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    • 2011
  • 1-Deoxynojirimycin (DNJ) is an alkaloid that is found at relatively high concentrations in mulberry leaf and tissues of the silkworm, $Bombyx$ $mori$. DNJ is a well known inhibitor of ${\alpha}$-glucosidase, an enzyme that is involved in the early stages of the $N$-linked glycoprotein synthesis pathway. ${\alpha}$-Glucosidase activity in the cell extract from $B.$ $mori$-derived Bm5 cells showed approximately 40-fold less sensitivity to DNJ than ${\alpha}$-glucosidase activity in the cell extract from $Spodoptera$ $frugiperda$-derived Sf9 cells. The replication of $B.$ $mori$ nucleopolyhedrovirus (BmNPV) was not inhibited when it was propagated in BmN cells that were grown in medium containing up to 10 mM DNJ. In contrast, the replication of $Autographa$ $californica$ multiple NPV (AcMNPV) was reduced by 67% when it was propagated in Sf9 cells that were grown in medium containing 10 mM DNJ. The viability of Bm5 and Sf9 cells that were grown in medium containing up to 10 mM DNJ was not affected. Our results suggested that the reduced replication of AcMNPV was the result of the higher sensitivity of ${\alpha}$-glucosidase activity in Sf9 cells to DNJ.

Inhibitory Effect of Aqueous Extracts from the Fruit Body of Lentinus edodes on Rat Intestinal Mucosa $\alpha$-glucosidase Activity and Reducing the Increase of Blood Glucose after Streptozotocin-induced Diabetic Rats

  • Lee, In-Soon;Chae, Heui-Jun;Moon, Hae-Yeon
    • Biomedical Science Letters
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    • v.14 no.1
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    • pp.63-68
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    • 2008
  • The aqueous extract from the fruit body of Lentinus edodes was evaluated for inhibitory activities against $\alpha$-glucosidase isolated from Spargue-Dawley male rats. A aqueous extract of Lentinus edodes exhibited 13.8% inhibitory activity on using 2 mM p-nitrophenyl $\alpha$-D-glucopyranoside as a substrate ($IC_{50}$ 75.3 mg/ml). The aqueous extract of Lentinus edodes inhibition type on $\alpha$-glucosidase was determined to be competitive inhibition. When it was oral administered to increase of blood glucose levels after STZ-induced in a dose dependent dietary. These results suggest that aqueous extract of Lentinus edodes effect a metabolism of intestine, and thereby reducing the increase of blood glucose after STZ-induced.

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[ $\alpha$ ]-Glucosidase Inhibitors from the Roots of Codonopsis lanceolata Trautv

  • Jung, Suk-Whan;Han, Ae-Jin;Hong, Hae-Jin;Choung, Myoung-Gun;Kim, Kwan-Su;Park, Si-Hyung
    • Journal of Applied Biological Chemistry
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    • v.49 no.4
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    • pp.162-164
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    • 2006
  • The roots of Codonopsis lanceolata afforded tangshenoside I(1) and $\beta$-adenosine (2) as $\alpha$-glucosidase inhibitors. Their structures were unambiguously determined by 1D and 2D NMR data including HMQC and HMBC experiments. Compounds 1 and 2 exhibited weak $\alpha$-glucosidase inhibitory activities in vitro with $IC_{50}$ of 1.4 and 9.3 mM, respectively.

Screening of $\alpha$-Amylase and $\alpha$-Glucosidase Inhibitor from Nepalese Plant Extracts (100종 네팔 식물 추출물로부터 $\alpha$-Amylase 및 $\alpha$-Glucosidase저해제의 선별)

  • Kim, Mi-Sun;Ahn, Seon-Mi;Jung, In-Chang;Kwon, Gi-Seok;Sohn, Ho-Yong
    • Microbiology and Biotechnology Letters
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    • v.38 no.2
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    • pp.183-189
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    • 2010
  • In the course of screening for anti-acidosis and anti-diabetes agent from natural products, the inhibitory activities of Nepales plant extracts against microbial $\alpha$-amylase and $\alpha$-glucosidase were evaluated. Among the 100 different kinds of ethanol extracts, Cedrus deodara (Roxb.) G. Don and Myrica nagi Thunb showed strong inhibition activities against $\alpha$-amylase. The $IC_{50}$ values of C. deodara (Roxb.) G. Don, M. nagi Thunb and acarose, a commercial available anti-diabetes agent, were 44.5, 47.5 and $50.5\;{\mu}g/mL$, respectively. Considering the crude extract of C. deodara (Roxb.) G. Don, and M. nagi Thunb, these extracts have strong potentials as anti-acidosis or anti-diabates agent. In a while, Cleistocalyx operculatus (Roxb.) extract showed a good inhibition activity to $\alpha$-amylase and $\alpha$-glucosidase, even it was recently reported. The selected three extracts did not show any hemolysis activity against human red blood cell up to 1 mg/mL, and the inhibition activities were maintained by heat or acid treatment. Moreover, treatment of HCl (0.01N) for 1 h into C. operculatus (Roxb.) and M. nagi Thunb increased the inhibition activity from 50% to 70%. Our results suggest that C. deodara (Roxb.) G. Don, M. nagi Thunb, and C. operculatus (Roxb.) are potential as anti-acidosis and anti-diabetes agents.

α-Glucosidase Inhibition Activity of Methanol Extracts and Fractions Obtained from Three Dryopteridaceae Species (면마과 3종 메탄올 추출물 및 분획물의 α-Glucosidase 억제 활성)

  • Kim, Na Rae;Chi, Lai Won;Lee, Cheol Hee
    • Korean Journal of Medicinal Crop Science
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    • v.21 no.4
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    • pp.301-305
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    • 2013
  • This study was performed to select adequate plant materials for developing a natural ${\alpha}$-glucosidase inhibitor by analyzing ${\alpha}$-glucosidase inhibition activity in fronds and rhizomes of three Dryopteridaceae species: Cyrtomium fortunei, Polystichum polyblepharum, and P. lepidocaulon. The highest ${\alpha}$-glucosidase inhibitor obtained from frond of P. lepidocaulon ($4.16{\mu}g{\cdot}mL^{-1}$), and rhizome of C. fortunei ($1.84{\mu}g{\cdot}mL^{-1}$), showed much higher inhibition activity than acarbose ($1413.70{\mu}g{\cdot}mL^{-1}$). The biomass required to inhibit ${\alpha}$-glucosidase by 50% was 0.04 ~ 0.35mg for frond and 0.03 ~ 0.10mg for rhizome, and P. lepidocaulon required the least amount of fronds and P. lepidocaulon the least rhizomes. In frond, ${\alpha}$-glucosidase inhibition activity was the highest in water fraction of C. fortunei ($20.2{\mu}g{\cdot}mL^{-1}$), and n-butanol fraction of P. lepidocaulon ($9.33{\mu}g{\cdot}mL^{-1}$) and P. polyblepharum ($5.10{\mu}g{\cdot}mL^{-1}$). In rhizome, it was the highest in n-butanol fractions of C. fortunei ($19.76{\mu}g{\cdot}mL^{-1}$) and P. polyblepharum ($4.47{\mu}g{\cdot}mL^{-1}$), and ethylacetate fraction of P. lepidocaulon ($5.46{\mu}g{\cdot}mL^{-1}$). The frond biomass required for 50% ${\alpha}$-glucosidase inhibition was the lowest in the water fraction of C. fortunei (1.43mg), and n-butanol fractions of P. lepidocaulon (1.10mg) and P. polyblepharum (0.66mg). The required biomass of rhizome was the lowest in the water fraction of C. fortunei (1.59mg), and n-hexane fractions of P. lepidocaulon (0.04mg) and P. polyblepharum (0.15mg). The result of this study suggested that the three Dryopteridaceae species had high ${\alpha}$-glucosidase inhibition activity with small biomass, which might have high value as materials for economical anti-diabetic medication.

Alpha-glucosidase Inhibition Activity of Methanol Extracts Obtained from Nine Pteridophyte Species Native to Korea (자생 양치식물 9종의 성엽 및 근경 추출물의 α-glucosidase 억제 활성)

  • Kim, Na Rae;Chi, Lai Won;Lee, Cheol Hee
    • Korean Journal of Plant Resources
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    • v.26 no.4
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    • pp.411-416
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    • 2013
  • This study was conducted not only to analyze ${\alpha}$-glucosidase inhibition activity with fronds and rhizomes of nine Pteridophyte species, but also to select the plant materials suitable for natural ${\alpha}$-glucosidase inhibitor. Harvested rhizomes and fronds were washed, freeze-dried and grinded. After conducting ultrasonification extraction for 30 minutes in ultrasonic water tank with 100% methanol solvent, and vacuum filtration, ${\alpha}$-glucosidase inhibition activity was measured. Acarbose was used as the positive control. After mixing $100{\mu}L$ of 0.7 unit ${\alpha}$-glucosidase enzyme solution into $50{\mu}L$ of extract and reacting them at $37^{\circ}C$ for 10 minutes, $50{\mu}L$ of 1.5 mM ${\rho}$-NPG solution was taken and reacted at $37^{\circ}C$ for 20 minutes. The reaction was stopped with 1 mL of 1 M $Na_2CO_3$ and absorbance was measured in 405 nm. With the regression analysis, the content of solubility solids (the value of $IC_{50}$) which can inhibit 50% of 0.7 unit ${\alpha}$-glucosidase solution's activity was investigated. The frond ($IC_{50}=14.00{\sim}913.33{\mu}g{\cdot}mL^{-1}$) and rhizome extracts ($IC_{50}=12.93{\sim}205.84{\mu}g{\cdot}mL^{-1}$) of nine Pteridophyte species showed higher ${\alpha}$-glucosidase inhibition activity in comparison with acarbose ($IC_{50}=1413.70{\mu}g{\cdot}mL^{-1}$). The extracts of fronds and rhizomes showed higher value than acarbose by 1.55~100.98 and 6.87~109.33 times each. Especially, ${\alpha}$-glucosidase inhibition activities of Pyrrosia lingua in fronds and Osmunda cinnamomea var. fokiensis in rhizomes were the highest. The necessary biomass of fronds and rhizomes for inhibiting 50% of ${\alpha}$-glucosidase activity showed the lowest value, 0.35, 0.27 mg each, in O. cinnamomea var. fokiensis. $IC_{50}$ value of P. lingua was the highest among fronds of nine Pteridophyte species, but content of soluble solids was 2.4 times less than O. cinnamomea var. fokiensis. So frond of O. cinnamomea var. fokiensis is more economic in comparison with P. lingua. As the result of this study, O. cinnamomea var. fokiensis showed high ${\alpha}$-glucosidase inhibition activity even with small biomass. Therefore it was considered to be high-valued economic material as natural ${\alpha}$-glucosidase inhibitor.

Acute Toxicity and Antimicrobial Activity of 1-Deoxynojirimycin (1-Deoxynojirimycin의 급성독성 및 항균효과)

  • 백남수;김영만
    • The Korean Journal of Food And Nutrition
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    • v.11 no.6
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    • pp.629-634
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    • 1998
  • 1-Deoxynojirimycin which is a potent intestinal ${\alpha}$-glucosidase inhibitor was purified from the culture broth by ion exchange chromatography, Sephadex LH20 column chromatography, TSK gel chromatography and HPLC respectively. Acute toxicity of 1-deoxynojirimycin, which was loaded through the oral as dose of 200mg/kg, was investigated in IRC mouse. None of the tested IRC mice were not dead and increase of body weight showed also the same results in comparison with control mice. The antimicrobial susceptibility of 20 pathogenic strains against 3 antidiabetic compounds (1-deoxynojirimycin, AO-128, acarbose) were obtained by agar dilution method. All of the three antidiabetic compounds has very weak antimicrobial activity (MIC>100$\mu\textrm{g}$/ml).

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호수 생태계의 생화학적 분석

  • 최승익;안태석
    • Korean Journal of Microbiology
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    • v.33 no.1
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    • pp.50-54
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    • 1997
  • 이 글에서는 호수생태계에서 일어나는 변화 중 .betha.-glucosidase 활성도를 중심으로 생화학적인 분석과정을 통하여 유기물질의 분해, 생성, 소비등에 대한 과정을 설명하고자 한다. .betha.-glucosidase효소는 비교적 기질특이성이 넓고, glucose, celluhexose, carboxy-methylcellulose등의 .betha.고리를 가수분해시켜 monomer로 분해시키는 효소로서 수환경에서는 매우 중요하다. 즉 cellobiohydrolase에 의해 분해된 oligomer나 dimer를 세균의 세포막을 통과할 수 있는 크기로 분해시키는 효소이고, 이 효소의 분해 산물인 포도당은 세균에 의하여 바로 이용되고, catabolite inhibitor로 작용하므로, 이 효소 활성도의 높고 낮음은 수중생태계에서 탄소의 흐름과 세균 군집의 성장을 이해하는데 매우 중요하다(3).

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Gelidium amansii Extract, a Potent α-glucosidase and α-amylase Inhibitor, Alleviates Postprandial Hyperglycemia in Diabetic Mice (당뇨 마우스에서 우뭇가사리(Gelidium amansii)의 식후 고혈당 완화 효과)

  • Park, Jae-Eun;Kim, Jung-Min;Han, Ji-Sook
    • Journal of Life Science
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    • v.27 no.9
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    • pp.1052-1058
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    • 2017
  • Gelidium amansii shows antioxidant and anti-obesity effects; however, the effect on postprandial blood glucose levels is not known. The objective of the present study was to investigate the inhibitory effect of Gelidium amansii extract (GAE) on carbohydrate-digesting enzymes and its ability to alleviate postprandial hyperglycemia in streptozotocin (STZ)-induced diabetic mice. Gelidium amansii was extracted with 80% ethanol and concentrated for use in this study. The ${\alpha}-glucosidase$ and ${\alpha}-amylase$ inhibition assays were performed using the colorimetric method. ICR normal and STZ-induced diabetic mice were orally administered GAE (300 mg/kg body weight) or acarbose (100 mg/kg body weight) alone or soluble starch (2 g/kg body weight). Blood samples were taken from the tail vein at 0, 30, 60 and 120 min. Our results indicated that GAE markedly inhibited ${\alpha}-glucosidase$ and ${\alpha}-amylase$ activities with $IC_{50}$ values of $0.099{\pm}0.009mg/ml$ and $0.178{\pm}0.038mg/ml$, respectively, and was a more effective inhibitor than acarbose, the positive control. Further, the postprandial blood glucose levels of STZ-induced diabetic mice in the GAE-administered group were significantly lower than those of control group mice (p<0.05). Moreover, the area under the curves (AUC) significantly decreased with GAE administration in STZ-induced diabetic mice (p<0.05). These results indicate that GAE may be effective in decreasing postprandial blood glucose levels by inhibiting carbohydrate-digesting enzymes such as ${\alpha}-amylase$ and ${\alpha}-glucosidase$. Therefore, GAE could be used as a potential functional food for alleviating postprandial hyperglycemia.

Isolation and Characterization of α-glucosidase Inhibitors from Euonymus alatus (화살나무(Euonymus alatus)로 부터 α-glucosidase 저해 물질의 분리 및 동정)

  • Kim, Shin-Duk
    • Microbiology and Biotechnology Letters
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    • v.45 no.4
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    • pp.311-315
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    • 2017
  • ${\alpha}$-glucosidase inhibitory compounds (1-4) in a 50% methanol extract of Euonymus alatus were isolated by activity-based fractionations and the structures determined on the basis of chemical and spectral characterization techniques such as $^1H$ and $^{13}C$ nuclear magnetic resonance spectroscopy, $^1H-^1H$ correlation spectroscopy (COSY), and heteronuclear multiple bond correlation (HMBC). The compounds 1-4 belong to flavonols and exhibited potent inhibitory activities against ${\alpha}$-glucosidase, with $IC_{50}$ values of 25.3, 17.1, 47.3, and $35.1{\mu}M$, respectively. All the isolated compounds were more potent than the positive control acarbose. This is the first report describing the potential hypoglycemic effect of Euonymus alatus through ${\alpha}$-glucosidase inhibition and identification of its active components.