• 한국미생물·생명공학회지
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• 제44권2호
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• pp.124-129
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• 2016

식용버섯인 노랑느타리버섯으로부터 α-glucosidase 저해제의 추출과 정제에 대하여 연구하였다. α-glucosidase 저해제는 노랑느타리버섯 자실체를 증류수로 30℃에서 12시간 처리하였을 때 가장 많이 추출되었다. α-glucosidase 저해제를 sephadex G-100 여과 크로마토그래피와 펩신 가수분해, sephadex G-50 여과 크로마토그래피, 역상 HPLC로 정제한 결과 수율과 α-glucosidase 저해활성은 각각 12.2%와 IC₅₀ 9.10 mg/ml이었다. 정제한 α-glucosidase 저해제는 Thr-Ile-Ala-Phe-Ile-Asp (A)과 Tyr-Tyr-Ala-Ile-Gly-Asp (B)의 서열을 갖고 있는 두개의 헥사펩타이드를 함유하였고 이들의 분자량은 각각 (A)가 678.79 Da, (B)가 643.7 Da이었다. 정제한 α-glucosidase 저해제는 α-glucosidase에 대하여 혼합형 저해양상을 보였고 streptozotocin으로 유도된 당뇨 쥐모델에서 50 mg/kg과 300 mg/kg 투여시 혈당함량을 낮추어 주는, 농도 의존적 혈당상승억제 효과를 보였다.

• Journal of Microbiology and Biotechnology
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• 제25권2호
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• pp.174-177
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• 2015

A potent α-glucosidase inhibitor (compound I) was isolated from coffee brews by activity-based fractionation and identified as a β-carboline alkaloid norharman (9H-pyrido[3.4-b]indole) on the basis of mass spectroscopy and nuclear magnetic resonance spectra (¹H NMR, ¹³C NMR, and COSY). The norharman showed potent inhibition against α-glucosidase enzyme in a concentration-dependent manner, with an IC₅₀ value of 0.27 mM for maltase and 0.41 mM for sucrase. A Lineweaver-Burk plot revealed that norharman inhibited α-glucosidase enzyme uncompetitively, with a K_i value of 0.13 mM.

• 미생물학회지
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• 제50권4호
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• pp.381-383
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• 2014

미생물 기원의 ${\alpha}$-glucosidase 저해제를 탐색하는 과정에서 토양에서 분리한 균주인 Bacillus sp. SKU31-1 배양액에서 강력한 저해제 compound K을 일련의 크로마토그래피 방법에 의해 분리 정제하였고 $^1H$ NMR, $^{13}C$ NMR, $^1H-^1H$ COSY spectra 분석과 문헌조사를 통해 5-amino-1-hydroxymethyl-1,2,3,4-cyclohexanetetrol로 동정되었다. Compound K의 ${\alpha}$-glucosidase 저해 활성은 $IC_{50}$값이 maltose 기질에서는 $1.9{\mu}M$이고, sucrose 기질 사용시 4.9 mM이었다. Lineweaver Burk plot에 의해 $K_i$값이 0.15 mM 로 강력한 경쟁적 저해제 임이 밝혀졌다.

• International Journal of Industrial Entomology and Biomaterials
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• 제33권1호
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• pp.24-30
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• 2016

1-Deoxynojirimycin (DNJ) have been extensively investigated for their α-glucosidase inhibitor on postprandial hyperglycemia, and applied in nutraceuticals and medicine for preventing or delaying progression of type 2 diabetes. However, the amount of DNJ in mulberry leaves is low (about 0.1%), therefore, more effective extraction method is needed. This study was performed to develop microbial DNJ for biological methods of DNJ as an alternative to the chemical methods. In this study, we obtained evidence for Bacillus subtilis that produce DNJ in large quantities by high performance liquid chromatography. Inhibition of α-glucosidase activity was determined to DNJ production or non-production. Investigation of the effect of mulberry leaves powder concentration (1~5%), using the DNJ high-production bacteria, provided evidence for microbial mass production of DNJ. When the 4% mulberry leaf powder for 9 days was used, the α-glucosidase inhibitory activity was over the 85%. Also, the results presented in this study confirm DNJ yield's increasement in microbes using the various of nutrients and provide insight of ways to improve DNJ yields in microorganisms.

• 한국식품영양과학회지
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• 제40권2호
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• pp.308-315
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• 2011

연구는 강원도 자생 산채류의 다양한 약리 기능 중 ${\alpha}$-glucosidase, ${\alpha}$-amylase, lipase 효소 저해활성이 우수한 식물소재를 탐색하는데 있다. 강원도 양구, 평창, 태백에서 자생하고 있는 산채 90종을 채집하여 물과 에탄올로 각각 추출하였다. 항비만 활성 탐색은 ${\alpha}$-amylase, ${\alpha}$-glucosidase, lipase 저해활성을 검정하였다. 그 결과 산채 90종 중 ${\alpha}$-amylase 활성 저해능이 높은 식물로 에탄올 추출물 3종, 물추출물 2종, ${\alpha}$-glucosidase 활성 저해능이 높은 식물로 에탄올 추출물 13종, 물 추출물 3종, lipase 활성 저해능이 높은 식물로 에탄올 추출물 7종, 물 추출물 1종이 선발되었다. 향후 본 연구결과는 비만과 당뇨 등 대사성 질환에 대해 예방 혹은 치료 효과가 있는 기능성식품으로 개발하는데 있어 좋은 기초자료로 활용될 것으로 기대된다.

• Preventive Nutrition and Food Science
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• 제19권1호
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• pp.5-9
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• 2014

This study was designed to investigate the inhibitory effects of Polyopes lancifolia extract (PLE) on ${\alpha}$-glucosidase activity, ${\alpha}$-amylase activitiy, and postprandial hyperglycemia in streptozotocin (STZ)-induced diabetic mice. The results of this study revealed a marked inhibitory effect of PLE on ${\alpha}$-glucosidase and ${\alpha}$-amylase activities. The $IC_{50}s$ of PLE against ${\alpha}$-glucosidase and ${\alpha}$-amylase were 0.20 mg/mL and 0.35 mg/mL, respectively. PLE was a more effective inhibitor of ${\alpha}$-glucosidase and ${\alpha}$-amylase activities than acarbose, the positive control. The postprandial blood glucose levels of STZ-induced diabetic mice were significantly lower in the PLE treated group than in the control group. Moreover, PLE administration was associated with a decreased area under the curve for the glucose response in diabetic mice. These results indicate that PLE may be a potent inhibitor of ${\alpha}$-glucosidase and ${\alpha}$-amylase activities and may suppress postprandial hyperglycemia.

• 한국미생물·생명공학회지
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• 제49권4호
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• pp.566-575
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• 2021

Galactose and soybean meal were selected as the best carbon and nitrogen sources, repectively, for the efficient production of α-glucosidase inhibitor (AGI) and 1-deoxynojirimycin (DNJ) by a newly isolated Bacillus subtilis MORI. The optimal concentrations of the galactose and soybean meal for the production of AGI and DNJ were investigated by response surface methodology. For the production of AGI, the optimal galactose and soybean meal concentrations were 4.3% (w/v) and 3.2% (w/v), respectively, and for DNJ, 4.5% (w/v) and 3.0% (w/v), respectively. The nearly identical optimal concentrations of galactose and soybean meal for the production of both AGI and DNJ indicated a close correlation between the production of AGI and DNJ. The maximum production of AGI (50,880 GIU/ml) and DNJ (824 ㎍/ml) obtained from the statistically optimized medium in a jar fermenter was 2.33 and 2.38-fold, respectively, higher than those (21,798 GIU/ml and 346 ㎍/ml, respectively) of the pre-optimized medium. The production of both AGI and DNJ was greatly increased by jar fermentation (AGI of 38,524 GIU/ml and DNJ of 491 ㎍/ml) compared with flask fermentation.

• 한국균학회지
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• 제44권1호
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• pp.57-60
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• 2016

식용버섯 자실체를 이용하여 새로운 식후 혈당상승억제물질을 개발하기 위하여 노랑느타리버섯 자실체에 함유되어있는 ${\alpha}$-glucosidase 저해물질을 증류수로 추출하여 식후 혈당 상승억제효과를 조사하였다. ${\alpha}$-Glucosidase 저해물질을 함유한 노랑느타리버섯 물추출물은 streptozotocin으로 당뇨를 유발시킨 당뇨 쥐에서 장기 30 mg/kg, 150 mg/kg 경구투여(2일)와 단기 500 mg/kg, 1,000 mg/kg 경구투여(120분)시 모두, 농도 의존적으로 식후 혈당상승억제 효과를 보였다.

• 생약학회지
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• 제46권2호
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• pp.105-108
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• 2015

To establish the anti-diabetic(α-glucosidase inhibitory) activity of D. lotus leaf extract, isolate and identify the constituents responsible for the activity. The methanolic extract of leaves was partitioned between water, n-butanol and ethyl acetate. Bio-assay guided fractionation, based on inhibition of ;${\alpha}$-glucosidase, allowed isolation and identification of the active components. Liquid chromatography/mass spectrometry(LC/MS), ¹ H-NMR and ¹³ C-NMR spectra analyses demonstrated that the active compound was myricetin-3-O-;${\alpha}$-L-rhamnoside(1). Compound 1 demonstrated a strong inhibition on the α-glucosidase, in vitro and ;${\alpha}$-glucosidase inhibitory value was calculated as 98.08%, when that of a reference drug, acarbose was estimated as 83.03%. The present study indicates compound 1 could be considered as an ;${\alpha}$-glucosidase inhibitor and developed as an important antidiabetes agent for type II diabetes therapy.

• Bulletin of the Korean Chemical Society
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• 제29권5호
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• pp.921-927
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• 2008

Discovery of $\alpha$-glucosidase inhibitors has been actively pursued with the aim to develop therapeutics for the treatment of diabetes and the other carbohydrate mediated diseases. As a method for the discovery of new novel inhibitors of $\alpha$-glucosidase, we have addressed the performance of the computer-aided drug design protocol involving the homology modeling of $\alpha$-glucosidase and the structure-based virtual screening with the two docking tools: FlexX and the automated and improved AutoDock implementing the effects of ligand solvation in the scoring function. The homology modeling of $\alpha$-glucosidase from baker’s yeast provides a high-quality 3-D structure enabling the structure-based inhibitor design. Of the two docking programs under consideration, AutoDock is found to be more accurate than FlexX in terms of scoring putative ligands to the extent of 5-fold enhancement of hit rate in database screening when 1% of database coverage is used as a cutoff. A detailed binding mode analysis of the known inhibitors shows that they can be stabilized in the active site of $\alpha$- glucosidase through the simultaneous establishment of the multiple hydrogen bond and hydrophobic interactions. The present study demonstrates the usefulness of the automated AutoDock program with the improved scoring function as a docking tool for virtual screening of new $\alpha$-glucosidase inhibitors as well as for binding mode analysis to elucidate the activities of known inhibitors.