• Title/Summary/Keyword: $\alpha$-Glucosidase inhibitory activity

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Inhibitory Effects of Steppogenin and Oxyresveratrol from Morus alba L. against Yeast ${\alpha}$-Glucosidase (뽕나무에서 분리한 Steppogenin과 Oxyresveratrol의 효모 ${\alpha}$-Glucosidase의 억제효과)

  • Chin, Hwi-Seung;NamKung, Woo
    • YAKHAK HOEJI
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    • v.54 no.5
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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.

Anti-Oxidative and Anti-Diabetic Effects of Methanol Extracts from Medicinal Plants (약용식물 메탄올 추출물의 항산화 및 항당뇨 활성)

  • Lee, Youn Ri;Yoon, Nara
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.44 no.5
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    • pp.681-686
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    • 2015
  • The purpose of this study was to measure total phenolic compounds as a measure of antioxidant activity as well as ${\alpha}$-amylase inhibitory and ${\alpha}$-glucosidase inhibitory activities as a measure of anti-diabetic efficacy in methanol extracts from 23 kinds of medicinal plants. Extracts of three medicinal plant species showing high total polyphenol contents were selected (Euonymus alatus stem, Taxus cuspidata fruit, and Eucommia ulmoides leaf). Extracts of six medicinal plant species showing over 60% DPPH radical scavenging activity were also selected [Eucommia ulmoides barks (80.10%), Lycium chinense roots (64.25%), Euonymus alatus stem (73.59%), Lespedeza cuneata (78.20%), Taxus cuspidata fruits (70.52%), and Tilia taquetii leaf and stem (67.81%)]. Regarding ${\alpha}$-glucosidase and ${\alpha}$-amylase inhibitory activities acarbose showing approximately 80% inhibitory activity was selected as a control group, and six species (Eucommia ulmoides heartwood, Eucommia ulmoides bark, Euonymus alatus stem, Dioscorea batatas, Coix lachryma-jobi, and Phaseolus radiatus) showed greater than 80% ${\alpha}$-glucosidase inhibitory activity. Extracts of nine medicinal plant. species showing over 80% ${\alpha}$-amylase inhibitory activity (Pueraria thunbergiana root, Eucommia ulmoides bark, Eucommia ulmoides leaf, Lycium chinense fruits, Euonymus alatus leaf and stem, Euonymus alatus stem, Sasa borealis whole, Dioscorea batatas leaf and stem, and Tilia taquetii leaf and stem). Based on these results, medicinal plants showing high antioxidant and antidiabetic activities can be used as fundamental products in developing new medicines, as well as functional foods to prevent adult disease.

Screening of α-Amylase, α-Glucosidase and Lipase Inhibitory Activity with Gangwon-do Wild Plants Extracts (강원도 자생 산채 추출물의 α-Amylase, α-Glucosidase, Lipase 효소 저해활성 탐색)

  • Kim, Hee-Yeon;Lim, Sang-Hyun;Park, Yu-Hwa;Ham, Hun-Ju;Lee, Kwang-Jae;Park, Dong-Sik;Kim, Kyung-Hee;Kim, Song-Mun
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.40 no.2
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    • pp.308-315
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    • 2011
  • We investigated ${\alpha}$-amylase, ${\alpha}$-glucosidase and lipase inhibitory activity of extracts collected from wild plants in Gangwon-do. 90 wild plants were collected and their water and ethanol extracts were obtained. Results of measuring ${\alpha}$-amylase inhibitory activity indicated more than 80% of activity inhibition in 10 mg/mL concentration for ethanol extracts of three plants and water extracts of two plants. For ${\alpha}$-glucosidase inhibitory activity, ethanol extracts of thirteen plants and water extracts of three plants showed more than 80% of activity inhibition in 10 mg/mL concentration. In the experiment of inhibiting lipase activity, ethanol extracts of seven plants and water extracts of one plants showed above 80% of activity inhibition in 10 mg/mL concentration. These results suggest that the selected extracts could be potentially used as a resource of bioactive materials for health functional foods.

Alleviating Effects of Baechu Kimchi Added Ecklonia cava on Postprandial Hyperglycemia in Diabetic Mice

  • Lee, Hyun-Ah;Song, Yeong-Ok;Jang, Mi-Soon;Han, Ji-Sook
    • Preventive Nutrition and Food Science
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    • v.18 no.3
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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.

ACE and α-glucosidase Inhibitory Activity of the Glucosinolates in Dolsan Leaf Mustard Pickle during Storage (저장기간 중 돌산갓피클에서 Glucosinolates의 ACE 및 α-glucosidase 저해활성)

  • Son, Hae-Reon;Oh, Sun-Kyung;Tsukamoto, Chigen;Choi, Myeong-Rak
    • KSBB Journal
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    • v.31 no.3
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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.

Inhibitory Activity of Aralia elata Leaves on Protein Tyrosine Phosphatase 1B and α-Glucosidase (참두릅 잎의 Protein Tyrosine Phosphatase 1B와 α-Glucosidase 저해 활성)

  • Cho, Yoon Sook;Seong, Su Hui;Bhakta, Himanshu Kumar;Jung, Hee Jin;Moon, Kyung Ho;Choi, Jae Sue
    • Korean Journal of Pharmacognosy
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    • v.47 no.1
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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.

Enhancement of the Anti-hyperglycemic and Antioxidant Activities of Five Selected Beans by the Germination Process (발아에 따른 콩류의 식후 혈당 상승 억제효능과 항산화 활성)

  • Cho, Cha-Young;Choi, Hwang-Yong;Jo, Sung-Hoon;Ha, Kyoung-Soo;Chung, Ji-Sang;Jang, Hae-Dong;Kwon, Young-In
    • The Korean Journal of Food And Nutrition
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    • v.25 no.2
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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.

Physiological Functionalities of Solvent Fractions Isolated from Crataegi Fructus

  • Oh, Hae-Sook;Kim, Jun-Ho
    • Biomedical Science Letters
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    • v.14 no.4
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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.

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Evaluation of Cytotoxicity, Carbohydrate, and Lipid Inhibitory Activity of Codonopsis lanceolata using Different Solvent Fractions

  • Boo, Hee-Ock;Park, Jeong-Hun;Kim, Seung-Mi;Woo, Sun-Hee;Park, Hyeon-Yong
    • KOREAN JOURNAL OF CROP SCIENCE
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    • v.60 no.4
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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.

Physiological activities of natural color powders and their mixtures (천연소재로부터 분리한 색소분말과 혼합물의 생리활성)

  • Kang, Jae-Ran;Kang, Min-Jung;Sim, Hye-Jin;Choi, Myeong-Hyo;Shin, Jung-Hye
    • Food Science and Preservation
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    • v.23 no.1
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    • pp.80-88
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    • 2016
  • Seven kinds (acacia, cochineal, catechu, grape peel, persimmon, gallnut and clove) of color powders obtained from natural resources and their mixtures were evaluated for their biological activities, such as antioxidant (ABTS and DPPH radicals scavenging), cholesterol absorption, and COX-2 inhibitory activities. Catechu, gallnut and clove were selected for the further studies due to its the best activities. The cholesterol absorption, COX-2 inhibitory, ${\alpha}$-amylase inhibitory and ${\alpha}$-glucosidase inhibitory activities were measured using the mixtures of catechu, gallnut and clove. The ABTS radical scavenging activity of the seven types of natural color powders were higher than the DPPH radical scavenging activity. The cholesterol absorption activity was significantly higher in cloves. The COX-2 inhibitory activity was significantly lower in acacia. The ${\alpha}$-amylase inhibitory activity was higher in catechu and gallnut, indicating that there were no significant difference between two mixtures. The ${\alpha}$-glucosidase inhibitory activity was the highest in catechu, which was higher than that of the catechu-containing mixtures. From all these results, a synergistic effect could be obtained when utilizing a mixture of powders rather than using only individual type. Since the activity of each powder was different, further studies will be required for clarifying the interactions between mixtures.