• 한국미생물·생명공학회지
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• 제42권3호
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• pp.219-224
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• 2014

본 연구에서는 우리나라 전통발효식품에서 분리한 효모들을 이용하여 새로운 항당뇨성 ${\alpha}$-glucosidase 저해물질을 개발하기 위하여, 먼저 48종의 효모들의 ${\alpha}$-glucosidase 저해활성을 측정한 결과, Pichia burtonii Y257-7의 무세포 추출물이 가장 높은 저해활성을 보여 시험균주로 최종 선발하였다. ${\alpha}$-glucosidase 저해제 최적 생산 조건을 검토한 결과, Pichia burtonii Y257-7를 $28^{\circ}C$에서 24시간 LB 배지(pH 6.0)에 배양하여 얻은 무세포 추출물에서 가장 높은 ${\alpha}$-glucosidase 저해활성을 보였다. 최적 생산조건에서 얻은 ${\alpha}$-glucosidase 저해물질을 $0.45{\mu}m$와 $0.2{\mu}m$ syringe filter unit로 여과한 후 Sephadex G-50 column chromatography와 연속 용매 추출을 실시하여 부분정제한 후 일반 쥐와 당뇨유발 쥐를 이용하여 항당뇨 효과를 조사하였다. 정상 쥐와 streptozotocin으로 당뇨를 유발시킨 당뇨유발 쥐에 Pichia burtonii Y257-7이 생산하는 ${\alpha}$-glucosidase 저해제의 부분정제물을 전분과 함께 500 mg/kg, 1000 mg/kg 농도로 경구 투여한 결과, 시판 혈당강하제인 acarbose보다는 효과가 낮았지만 농도 의존적으로 정상 쥐와 당뇨유발 쥐 모두에서 혈당 상승 억제 효과를 확인할 수 있었다.

• Mycobiology
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• 제41권3호
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• pp.149-154
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• 2013

An ${\alpha}$-glucosidase inhibitor was developed from Aspergillus oryzae N159-1, which was screened from traditional fermented Korean foods. The intracellular concentration of the inhibitor reached its highest level when the fungus was cultured in tryptic soy broth medium at $27^{\circ}C$ for five days. The inhibitor was purified using a series of purification steps involving ultrafiltration, Sephadex G-25 gel permeation chromatography, strong cation exchange solid phase extraction, reverse-phase high performance liquid chromatography, and size exclusion chromatography. The final yield of the purification was 1.9%. Results of the liquid chromatography-tandem mass spectrometry (LC-MS/MS) analysis indicated that the purified ${\alpha}$-glucosidase inhibitor was a tri-peptide, Pro-Phe-Pro, with the molecular weight of 360.1 Da. The IC50 value of the peptide against ${\alpha}$-glucosidase activity was 3.1 mg/mL. Using Lineweaver-Burk plot analysis, the inhibition pattern indicated that the inhibitor acts as a mixed type inhibitor.

• 미생물학회지
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• 제38권2호
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• pp.139-143
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• 2002

탄수화물분해 효소인 $\alpha$-glucosidase의 활성을 저해하는 물질을 생성하는 미생물을 검색하기 위하여 토양시료로 부터 수종의 미생물을 검색하였다. 토양 시료에서 강력한 $\alpha$-glucosidase 저해제를 생성하는 방선균PM718을 분리하였고 그 저해제의 활성을 기지물질인 acarbose와 비교 측정한 결과 우수한 활성을 나타냄을 확인하였다. 또한 그 활성은 pH 변화에도 안정된 활성을 유지하는 것을 확인하였다.

• Natural Product Sciences
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• 제10권5호
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• pp.223-227
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• 2004

This study was carried out to investigate inhibitory effect of extracts from the root of Paeonia lactiflora on postprandial hyperglycemia. Organic solvent (hexane, ethyl acetate, butanol, aqueous) extracts from the crude drug were fractionated by high performance liquid chromatography. These fractions were examined to evaluate ${\alpha}-glucosidase$ (EC 3. 2. 1. 20) inhibition by microplate colorimetric assay. Among the fractions examined, the ethyl acetate fraction from the roots of Paeonia lactiflora showed potent inhibitory effects on ${\alpha}-glucosidase$. Therefore, further fractionation of the fraction was carried out to isolate the active principles. Finally, we isolated and Purified 1,2,3,4,6-penta-O-galloyl-beta-D-glucose (PGG) as a active principle by activity-guided fractionation. These results suggest that the extract from the root of Paeonia lactiflora can be used as a new nutraceutial for inhibition on postprandial hyperglycemia and PGG might be a candidate for developing an ${\alpha}-glucosidase$ inhibitor.

• 한국미생물·생명공학회지
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• 제17권3호
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• pp.207-212
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• 1989

토양으로부터 분리 한 균주 YS-221-B로부터 $\alpha$-D-Glucosidase Inhibitor 생산조건을 검토한 결과는 다음과 같다. 최적 pH와 온도는 8.0, 3$0^{\circ}C$였으며, 탄소원으로는 mannitol, 1-Inositol, erythritol과 같은 당알코올이 양호하였으며, 질소원으로는 asparagine, beef extract가 양호하였다. Riboflavin, folic acid, thiamine과 같은 vitamin의 첨가에 의해서 저해물질 생산이 10~20% 증가되었으며, 금속이온 중에 $Zn^{++}$, $Mg^{++}$은 약 20% 정도 물질생산을 촉진시켰으나 Li$^+$, Co$^{++}$ $Ca^{++}$, Fe$^{++}$ 등은 감소시켰다. 그리고 pH8.0, 3$0^{\circ}C$에서 8~9일간 배양함으로써 저해물질 생산이 최고에 달하였다.

• 한국미생물·생명공학회지
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• 제34권4호
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• pp.368-372
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• 2006

Quercetin은 flavonoid 계통의 물질로서 자연계에서 채소나 과일에 매우 흔하다. 또한 인체에서는 radical scavenger로서 신체항상성 뿐만 아니라 직장암의 예방에도 중요한 역할을 한다. Glucosidase를 포함한 glycosidase는 많은 종류의 대사성 질환에 관련이 있다. 유용한 $\alpha$-glucosidase 저해제를 스크리닝 하던 중 chemical library로부터 quercetin을 선별하였다. Quercetin은 $\alpha$-glucosidase에 가역적으로, 느리게 결합하며, 비경쟁적인 저해제인데, $6.3\times10^{-8}$ M의 Ki값을 가진다. 이러한 결과는 비록 기전 연구가 더 필요하지만, quercetin이 당뇨병과 같은 퇴행성 질환을 치료할 수 있다는 잠재성을 보여주는 것이다.

• Preventive Nutrition and Food Science
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• 제22권3호
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• pp.166-171
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• 2017

In this study, we investigated whether Sargassum yezoense extract (SYE) could inhibit ${\alpha}-glucosidase$ and ${\alpha}-amylase$ activities, and alleviate postprandial hyperglycemia in streptozotocin (STZ)-induced diabetic mice. Freeze-dried S. yezoense was extracted with 80% ethanol and concentrated for use in this study. The hypoglycemic effect was determined by evaluating the inhibitory activities of SYE against ${\alpha}-glucosidase$ and ${\alpha}-amylase$ as well as its ability to decrease postprandial blood glucose levels. The half-maximal inhibitory concentrations of SYE against ${\alpha}-glucosidase$ and ${\alpha}-amylase$ were $0.078{\pm}0.004$ and $0.212{\pm}0.064mg/mL$, respectively. SYE was a more effective inhibitor of ${\alpha}-glucosidase$ and ${\alpha}-amylase$ activities than the positive control, acarbose. The increase in postprandial blood glucose levels was significantly alleviated in the SYE group compared with that in the control group of STZ-induced diabetic mice. Furthermore, the area under the curves significantly decreased with SYE administration in STZ-induced diabetic mice. These results suggest that SYE is a potent inhibitor of ${\alpha}-glucosidase$ and ${\alpha}-amylase$ activities and alleviates postprandial hyperglycemia caused by dietary carbohydrates.

• International Journal of Industrial Entomology and Biomaterials
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• 제15권2호
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• pp.161-164
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• 2007

While searching for ${\alpha}$-glucosidase inhibitors, the active compound was found in a methanol extract of Burthus martensi Kirsch. The separation of the active compound was performed using various chromatography methods and the physico-chemical properties of the purified compound were characterized. The compound showed very potent inhibitory activity against ${\alpha}-glucosidase$ with an $IC_{50}$ value of $5.3\;{\mu}g/ml$. Lineweaver-Burk plot indicated that its inhibition of ${\alpha}-glucosidase$ was competitive.

• 한국응용약물학회:학술대회논문집
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• 한국응용약물학회 1998년도 Proceedings of UNESCO-internetwork Cooperative Regional Seminar and Workshop on Bioassay Guided Isolation of Bioactive Substances from Natural Products and Microbial Products
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• pp.134-134
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• 1998

The modulation of glycosidase activity by inhibitors is of great interest. Such compounds have been shown to be important tools in mechanistic studies on glycohydrolase as well as having promising therapeutic application. An ${\alpha}$-glucosidase inhibitor was isolated from culture filterates of Penicillium sp. The inhibitor was active against ${\alpha}$-glucosidase isolated from yeast and porcine small intestine. However, it showed no inhibition to Aspergillus ${\alpha}$-galactosidase, Escherichia coli ${\beta}$-galactosidase, and jack bean ${\alpha}$-mannosidase. The inhibitor was highly soluble in ether, methanol and chloroform. The inhibitor was purified using silica gel, Sephadex LH-20 column chromatography and reverse-phase HPLC. The inhibitory compound designated PA-7(IC$\sub$50/=35$\mu\textrm{g}$) was obtained as white powder. The structure of PA-7 was determined with spectroscopic data of EI-MS, FAB-MS, $^1$H, and $\^$13/C NMR. The inhibitor has a diketopiperazine moiety.

• Journal of Microbiology and Biotechnology
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• 제21권3호
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• pp.263-266
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• 2011

Methylelaiophylin isolated from Streptomyces melanosporofaciens was selected as an ${\alpha}$-glucosidase inhibitor with an $IC_{50}$ value of 10 ${\mu}M$. It showed mixed-type inhibition of ${\alpha}$-glucosidase with a $K_i$ value of 5.94 ${\mu}M$. In addition, methylelaiophylin inhibited the intracellular trafficking of hemagglutinin-neuramidase (HN), a glycoprotein of Newcastle disease virus (NDV), in baby hamster kidney (BHK) cells. Methylelaiophylin inhibited the cell surface expression of NDV-HN glycoprotein without significantly affecting HN glycoprotein synthesis in NDV-infected BHK cells.