• 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.

• 한국식품영양과학회지
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• 제44권5호
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• pp.681-686
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• 2015

약용식물 23종 메탄올 추출물의 폴리페놀 함량을 측정한 후 항산화 활성을 측정하고, 항당뇨 활성으로는 ${\alpha}$-amylase 저해 활성, ${\alpha}$-glucosidase 저해 활성을 검정하여 혈당강하 활성을 나타낼 수 있는 약용식물을 선발하고자 한다. 약용식물의 폴리페놀 함량을 분석한 결과 1.50~15.25 mg GAE/g의 다양한 함량 범위로 나타났으며 가장 높은 함량은 주목열매(15.25 mg GAE/g), 화살나무줄기(15.12 mg GAE/g), 두충잎(14.24 mg GAE/g)으로 3종이 나타났다. 60% 이상 DPPH 라디칼 소거능을 본 약용식물로는 두충 줄기수피(80.10%), 구기자나무 뿌리(64.25%), 화살나무 줄기(73.59%), 비수리(78.20%), 주목열매(70.52%), 뽕잎나무 잎줄기(67.81%) 부위 추출물로 6종이 선발되었다. ${\alpha}$-Glucosidase를 80% 이상 저해한 약용소재로는 두충 줄기심재, 두충 줄기수피, 화살나무 줄기, 마, 율무, 녹두 6종이 선발되었다. ${\alpha}$-Amylase를 80% 이상 저해한 약용식물로는 칡뿌리, 두충 줄기수피, 두충잎, 구기자 열매, 화살나무 잎줄기, 화살나무 줄기, 조릿대 지상부, 마, 뽕잎나무 잎줄기 추출물 등 9종이 선발되었다. 항산화 및 항당뇨 활성이 우수했던 약용식물들은 향후 새로운 의약품 개발 및 성인병 예방의 건강기능식품으로 개발하는 데 있어 좋은 기초자료로 활용될 것으로 기대된다.

• 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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• 제18권3호
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• pp.163-168
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• 2013

In this study, we investigated the inhibitory effects of Baechu kimchi added Ecklonia cava on the activities of ${\alpha}$-glucosidase and ${\alpha}$-amylase and its alleviating effect on the postprandial hyperglycemia in STZ-induced diabetic mice. Baechu kimchi added Ecklonia cava (BKE, 15%) was fermented at $5^{\circ}C$ for 28 days. Optimum ripened BKE was used in this study as it showedthe strongest inhibitory activities on ${\alpha}$-glucosidase and ${\alpha}$-amylaseby fermentation time among the BKEs in our previous study. The BKE was extracted with 80% methanol and the extract solution was concentrated, and then used in this study. The BKE extract showed higher inhibitory activities than Baechu kimchi extract against ${\alpha}$-glucosidase and ${\alpha}$-amylase. The $IC_{50}$ values of the BKE extract against ${\alpha}$-glucosidase and ${\alpha}$-amylase were 0.58 and 0.35 mg/mL, respectively; BKE exhibited a lower ${\alpha}$-glucosidase inhibitory activity but a higher ${\alpha}$-amylase inhibitory activity than those of acarbose. The BKE extract alleviated postprandial hyperglycemia caused by starch loading in normal and streptozotocin- induced diabetic mice. Furthermore, the BKE extract significantly lowered the incremental area under the curve in both normal and diabetic mice (P<0.05). These results indicated that the BKE extract may delay carbohydrate digestion and thus glucose absorption.

• KSBB Journal
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• 제31권3호
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• pp.165-170
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• 2016

This study was carried out for investigate that physiological activity, quantification and qualitative were sinigrin of Dolsan leaf mustard pickle (DLMP) during storage. sinigrin contains high amounts of nutritional and medicinal compounds, which are important for maintaining optimum health. ACE inhibitory activity was ranged between 43.2 and 79.4%. DLMP methanol extracts demonstrated highest ACE inhibitory activity at 79.4% on day 14, whereas DLMP ethanol extracts demonstrated highest Angiotensin I-converting Enzyme (ACE) inhibitory activity of 43.2% at day 0. The ${\alpha}-glucosidase$ inhibitory activity of positive control 0.02% (v/v) acarbose was 78%. The DLMP methanol extracts had the highest ${\alpha}-glucosidase$ inhibitory activity at 64.0% on day 14, whereas DLMP ethanol extracts had the lowest ${\alpha}-glucosidase$ inhibitory activity of 42.8% at day 28. Sinigrin was high in DLMP methanol extracts at $49.55{\mu}g/ml$ on day 14 of storage. Sinigrin standard was eluted at 2.73 min and MS analysis was m/z 283.03 along with fragment ions at m/z 204 and 149.06. These data show that sinigrin formed desulfo-glucosinolates $[M-SO_3-2H_2O+K+2H]^+$. Sinigrin concentration increased until day 14 and then decreased after that. DLMP methanol extracts had consistently higher sinigrin concentration than DLMP acetonitrile extracts during 28 days of storage.

• 생약학회지
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• 제47권1호
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• pp.29-37
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• 2016

Anti-diabetic potential of the leaves of A. elata through the inhibitory activity on PTP1B and ${\alpha}$-glucosidase has not been reported. In this study, the EtOAc fraction of methanolic extract from the leaves of A. elata showed potent inhibitory activity against the PTP1B and ${\alpha}$-glucosidase with $IC_{50}$ value of $96.29{\pm}0.3$ and $264.71{\pm}14.87{\mu}g/mL$, respectively. Three known triterpenoids, oleanolic acid, oleanolic acid-28-O-${\beta}$-D-glucopyranoside and oleanolic acid-3-O-${\beta}$-D-glucopyranoside were isolated from the most active EtOAc fraction. We determined the chemical structure of these triterpenoids through comparisons of published nuclear magnetic resonance (NMR) spectroscopic data. Furthermore, we screened these triterpenoids for their ability to inhibit PTP1B and ${\alpha}$-glucosidase over a range of concentrations ($12.5-50{\mu}M$). All three terpenoids significantly inhibited PTP1B in a concentration dependent manner and oleanolic acid effectively inhibited ${\alpha}$-glucosidase. In addition, these compounds revealed potent inhibitory activity with negative binding energies toward PTP1B, showing high affinity and tight binding capacity in the molecular docking studies. Therefore, the results of the present study clearly demonstrate that A. elata leaves and its triterpenoid constituents might be beneficial in the prevention or treatment of diabetic disease.

• 한국식품영양학회지
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• 제25권2호
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• pp.246-252
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• 2012

After a mixed carbohydrate diet, inhibition of ${\alpha}$-amylase and ${\alpha}$-glucosidase involved in the digestion and absorption of carbohydrates can significantly decrease the postprandial increase of blood glucose level. In the course of screening these useful enzyme inhibitors, we selected five kinds of bean, using an in-vitro enzyme inhibition assay method. To evaluate the effect of germination process on the functionality of the bean, we investigated the inhibitory activities of the water extracts of non-germinated bean and germinated bean against ${\alpha}$-amylase and ${\alpha}$-glucosidase, relevant to postprandial hyperglycemia. We also investigated the oxygen radical absorbance capacity(ORAC), total phenolics content, and postprandial blood glucose lowering effect in rats(Sprague-Dawley rat model). Most germinated beans showed significantly higher ${\alpha}$-glucosidase inhibitory activity, compared with non-germinated beans. Among germinated beans, Glycine max had the highest ${\alpha}$-glucosidase inhibitory activity(53.3%). The water extract of germinated Phaseolus vulgaris L. had the highest ${\alpha}$-amylase inhibitory activity(95.1%), followed by Glycine max(58.7%), and Glycine max L. Merr(54.1%). Furthermore, the five germinated beans also showed high antioxidant activities in ORAC assay. Results suggested that the germination process may improve and enhance the anti-hyperglycemia potential and antioxidant activity of the bean.

• 대한의생명과학회지
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• 제14권4호
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• pp.249-255
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• 2008

In this study we investigated the biological activities of Crataegi Fructus, including antioxidative, fibrinolytic, $\alpha$-glucosidase inhibitory, and thrombin inhibitory activities. Crataegi Fructus, hot water extract was fractionated into hexane, $CHCLl_3$, ethyl acetate, butanol, and water fractions, and each of these was assayed individually. The water fraction showed the highest extraction yield at 4.08% (w/w). The antioxidative activities of the water, ethyl acetate, and butanol fractions were 31.07%, 45.87%, 50.28%, and 91.74%, respectively. Assays for fibrinolytic activity indicated that only the butanol fraction has significant efficacy at 1.93 plasmin units/ml. Thrombin inhibitory assays indicated that the 10-fold dilutions of the $CHCLl_3$, ethyl acetate, and butanol fractions had inhibitory activities of 34.97%, 41.43%, and 58.10%, respectively. The 10-fold dilutions of the only ethyl acetate fraction demonstrated $\alpha$-glucosidase inhibitory activities of 75.07%. From the above results, we propose that extracts of Crataegi Fructus can be used as a material for the development of biofunctional foods.

• 한국작물학회지
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• 제60권4호
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• pp.498-503
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• 2015

This study was conducted to evaluate the cytotoxicity and ${\alpha}-Amylase$, ${\alpha}-Glucosidase$, pancreatic lipase inhibition in vitro by different solvent fractions from the roots of Codonopsis lanceolata. The values of $IC_{50}$ against Calu-6 cell showed a high effect in n-hexane fraction ($10.13{\mu}g/mL$) whereas DW fraction exhibited the weakest inhibition on cell viability, having an $IC_{50}$ value of over $1,000{\mu}g/mL$. The values of $IC_{50}$ against HCT-116 cell showed the highest activity in n-BuOH fraction ($102.01{\mu}g/mL$), followed by n-hexane fraction ($145.85{\mu}g/mL$), methylene chloride fraction ($332.02{\mu}g/mL$), ethyl acetate fraction ($462.93{\mu}g/mL$) and DW fracion ($>1,000{\mu}g/mL$). ${\alpha}-Amylase$ inhibitory activity in methylene chloride fraction and ethyl acetate fraction was found to have a higher inhibitory effect with 24.5% and 25.6% than the other fractions. The highest ${\alpha}-Glucosidase$ inhibitory activity was observed from the ethyl acetate fraction extract, while the extract of DW fraction showed the lowest level of inhibitory activity at given experiment concentration. The pancreatic lipase inhibitory activity of C. lanceolata was found to have a higher the effect in ethyl acetate fraction. Inhibition of lipase activity of the ethyl acetate fraction and n-hexane fraction showed a relatively high, while the extract of DW fraction showed the lowest level at given experiment concentration. These results suggested that the roots of C. lanceolata may assist in the potential biological activity on carbohydrate, lipid Inhibitory activity and anticancer activity.

• 한국식품저장유통학회지
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• 제23권1호
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• pp.80-88
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• 2016

천연색소 혼합물의 생리활성을 검증하고자 하고자 천연색소 7종에 대하여 ABTS 라디칼 소거활성과 DPPH 라디칼 소거활성, 콜레스테롤 흡착활성 및 COX-2 저해활성을 측정하였으며, 활성이 우수하였던 시료 3종(아선약, 오배자, 정향)을 선별하였다. 선정된 3종 시료의 혼합물 4종(아선약+오배자, 아선약+정향, 오배자+정향, 아선약+오배자+정향)에 대해서는 콜레스테롤 흡착활성, COX-2 저해활성, ${\alpha}$-glucosidase 및 ${\alpha}$-amylase 저해활성을 측정하였다. 천연색소 시료들은 DPPH 라디칼 소거활성에 비해 ABTS 라디칼 소거활성이 더 우수하였으며, 콜레스테롤 흡착활성은 정향이 유의적으로 높았고, COX-2 저해활성은 아카시아 분말이 유의적으로 낮았으며, 여타 시료간에는 유의적인 활성의 차이가 없었다. ${\alpha}$-Amylase 저해활성은 아선약과 오배자에서 높았으나, 혼합물들에서는 서로간에 유의적인 차이가 없었다. ${\alpha}$-Glucosidase 저해활성은 아선약 분말이 가장 높았고, 아선약이 첨가된 혼합물의 활성이 더 높았다. 이상의 결과를 종합하여 볼 때 천연색소의 생리활성은 혼합물로 조성하여 활용할 때 시너지 효과를 얻을 수 있으나, 조합되는 물질간의 상호작용에 따라 활성의 증감 정도는 상이하므로 이에 대해서는 앞으로 더 많은 연구가 필요할 것으로 생각된다.