• Title/Summary/Keyword: ${\alpha}-glucosidase$ inhibition activity

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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.

Screening of $\alpha$-amylase and $\alpha$-glucosidase Inhibitors from Brazilian Plant Extracts for Treatment of Rumen Acidosis (100종 브라질 식물 추출물로부터 반추동물 산독증 예방치료를 위한 $\alpha$-amylase 및 $\alpha$-glucosidase 저해제의 선별)

  • Kim, Mi-Sun;An, Seon-Mi;Jung, In-Chang;Kwon, Gi-Seok;Sohn, Ho-Yong
    • Food Science and Preservation
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    • v.17 no.2
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    • pp.290-296
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    • 2010
  • To develop anti-acidosis and anti-diabetes agentsfrom natural products, the inhibitory activities of Brazilian plant extracts against microbial $\alpha$-amylase and $\alpha$-glucosidase were evaluated. Among 100 different ethanol extracts tested, those of Acacia jurema Mart., Anacardium humile A. St.-Hil., Cedrela odorata L., and Guazuma ulmifolia Lam showed good inhibitoryactivities toward both enzymes. In addition, an extract of Plumeria drastica Mart. showed specific inhibition of $\alpha$-amylase, whereas that of Eugenia uniflora L. demonstrated strong inhibition of the enzyme. IC50 values of $\alpha$-amylase inhibition suggested that the extract of A. humile A. St.-Hil., which has been used as an anti-diabetes medicine in Brazil, had potent inhibitory activity. The IC50 for the A. humile A. St.-Hil. extract ($91.2{\mu}g/mL$) was similar to that of acarbose ($50.5{\mu}g/mL$). This activity of A. humile A. St.-Hil. was not reduced by heat or acid treatment. Moreover, treatment with HCl (0.01 M) for 1 h increased the inhibitory activity from 57.5% to 81.2%. Also, the extract did not cause hemolysis of human red blood cells at levels up to 1 mg/mL. The results indicate that the extract of A. humile A. St.-Hil. is potentially useful as an anti-acidosis and anti-diabetes agent.

In vitro antioxidant property and α-glucosidase and pancreatic lipase inhibiting activities of Jeju camellia mistletoe (Korthalsella japonica (Thunb.) Engl.) extracts (제주 동백나무 겨우살이(Korthalsella japonica (Thunb.) Engl.)의 항산화 및 α-glucosidase와 pancreatic lipase 저해 활성)

  • Park, Eun Mi;Kim, Min Young
    • Journal of Applied Biological Chemistry
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    • v.60 no.3
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    • pp.241-244
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    • 2017
  • The antioxidant activity of various solvent extracts from Jeju camellia mistletoe (Korthalsella japonica (Thunb.) Engl.) was investigated using various in vitro assays as the 1,1-diphenyl-2-picrylhydrazyl radical scavenging, ferrous ion chelating and reducing power assays. Methanol and ethanol extracts showed the most potent antioxidant activity in all assays tested followed by water extract. The inhibitory effect of the Jeju camellia mistletoe extracts on pancreatic lipase and $\acute{a}$-glucosidase was also evaluated and the results showed that methanol and ethanol extracts markedly reduced both enzyme activities. Therefore, the methanol and ethanol extracts of Jeju camellia mistletoe is definitely worthy of further investigation for these beneficial effects on nutraceutical medicine.

Hypoglycemic Effect of the Methanol Extract of Soybean Sprout in Streptozotocin-Induced Diabetic Rats (Streptozotocin 유발 당뇨쥐에 있어서 콩나물 메탄올 추출물의 헐당강하효과)

  • 김정인;강민정;배세연
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.32 no.6
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    • pp.921-925
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    • 2003
  • To control blood glucose level as close to normal is the major goal of treatment of diabetes mellitus. $\alpha$-glucosidase is the enzyme to digest dietary carbohydrate and inhibition of $\alpha$-glucosidase could suppress postprandial hyperglycemia. The methanol extract of soybean sprout was tested for the inhibitory activities against $\alpha$-glucosidase in vitro. Soybean sprout extract inhibited yeast $\alpha$-glucosidase activity by 24.5% at the concentration of 5 mg/mL. The methanol extract of soybean sprout was subsequently subjected to sequential fractionation with hexane, ethyl acetate, butanol and water. Among the fractions tested ethyl acetate-soluble fraction showed relatively strong inhibition against $\alpha$-glucosidase by 36.3% at the concentration of 5 mg/mL. Acarbose, standard $\alpha$-glucosidase inhibitor, inhibited $\alpha$-glucosidase activity by 40.1%. The ability of soybean sprout extract to lower postprandial glucose was studied in streptozotocin-induced diabetic rats. Starch solution (1 g/kg) with and without the methanol extract of soybean sprout (500 mg/kg) was administered to diabetic rats after an overnight-fast by gastric intubation. A single oral dose of soybean sprout extract inhibited the increase in blood glucose levels significantly at 60, 90, 120, 180 min (p<0.05) and decreased incremental response areas under the glycemic response curve significantly (p<0.05). These results suggest that soybean sprout might exert hypoglycemic effect by inhibiting $\alpha$-glucosidase activity.

Bio-assay Guided Isolation and Identification of α-Glucosidase Inhibitors from the Leaves of Diospyros lotus (고욤나무 잎으로부터 활성유도 분획법에 의한 α-Glucosidase 저해물질 분리 및 확인)

  • Kim, Sang Jun;Kim, Ji-Ae;Kim, Da Hye;Kwak, Seol Hwa;Yu, Kang-Yeol;Jang, Seon Il;Kim, Seon-Yeong;Jeong, Seung-Il
    • Korean Journal of Pharmacognosy
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    • v.46 no.2
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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.

α-Glucosidase inhibitory caged xanthones from the resin of Garcinia hanburyi

  • Jin, Young Min;Kim, Jeong Yoon;Lee, Soo Min;Tan, Xue Fei;Park, Ki Hun
    • Journal of Applied Biological Chemistry
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    • v.62 no.1
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    • pp.81-86
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    • 2019
  • A yellow resin (gamboge) from Garcinia hanburyi has been widely used as folk medicine due to its antibacterial and antitumor activities. We isolated four ${\alpha}$-glucosidase inhibitory compounds from the methanol extract of gamboge. The compounds (1-4) were identified as gambogoic acid (1), moreollic acid (2), gambogic acid (3), and 10-methoxygambogenic acid (4), respectively through spectroscopic data including 2D-NMR and HREIMS. All compounds were examined in the enzyme inhibition assay against ${\alpha}$-glucosidase to identify their inhibitory potencies and kinetic behavior. All compounds (1-4) showed enzyme inhibition against ${\alpha}$-glucosidase, but the activity was significantly affected by the methoxy group on C-10 of ring A and pentenyl pyran moiety of ring D. For example, compound 1 ($IC_{50}=41.4{\mu}M$) bearing pyran ring eight times effective that 4 ($IC_{50}=350.6{\mu}M$) having geranyl group itself. Most active compound was found out to be gambogoic acid (1) which was analyzed most abundant metabolite in gamboge by LC-ESI-MS/MS. In kinetic study, compounds 1 and 2 were proved as noncompetitive inhibitors.

Antioxidant and Biological Activity in the Leaves of Adzuki Bean (Vigna angularis L.)

  • Lee, Kyung Jun;Lee, Jung-Ro;Shin, Myoung-Jae;Cho, Gyu-Taek;Lee, Ho-Sun;Ma, Kyung-Ho;Lee, Gi-An;Chung, Jong-Wook
    • Korean Journal of Plant Resources
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    • v.31 no.3
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    • pp.237-253
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    • 2018
  • The adzuki bean (Vigna angularis L.) is a red-grained legume that has a number of essential nutrients and is used in traditional dishes in Asia. Adzuki bean industrial by-products are also a potential low-cost source of some unique bioactive polyphenols. Hence, here, the authors aimed to perform a comparative study of the phytochemical profiles of the leaves and seeds of the adzuki bean and compare their antioxidant, ${\alpha}$-glucosidase inhibition, and tyrosinase inhibition activity. The authors assessed antioxidant activity by DPPH, ABTS, FRAP, PR, TPC, and SOD assays, which showed wide variation, respectively. From the relative antioxidant capacity index results, 10 adzuki bean landraces were selected to compare for phytochemicals and bioactivity using leaf and seed extracts. Antioxidant, ${\alpha}$-glucosidase inhibition, and tyrosinase inhibition activity in the leaf extracts were higher than in the seed extracts, and there were more flavonols and isoflavones in the leaf extracts than in the seed extracts. This study demonstrated that adzuki bean leaf extracts could be a new natural antioxidant or antidiabetic agent and a skin whitener and can also be used in industrial applications.

Inhibitory Effect of Extracts from Paeoniae radix on Postprandial Hyperglycemia (작약(Paeoniae radix) 추출물의 식후 과혈당 억제작용)

  • 지승택;이성진;이강은;손용태;정요경
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.31 no.1
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    • pp.131-135
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    • 2002
  • This study was carried out to investigate the inhibitory effect of extracts from Paeoniae radix on postprandial hyperglycemia. Organic solvent (hexane, ethyl acetate, butanol, water) extracts from Paeoniae radix were fractionated by high performance liquid chromatography. These fractions were used to screen $\alpha$-glucosidase (EC 3.2.1.20) inhibitors by microplate colorimetric assay. The fractions 11, 12, 18, 19 of ethyl acetate extract from Paeoniae radix showed inhibitory activity by 85%, 84%, 77%, 77% at concentration of 20 $\mu\textrm{g}$/mL, respectively. The selected fractions (no. 10~no. 19) significantly reduced by 22% the blood glucose elevation in comparison with positive control in mice loaded with maltose. The fractions of Paeoniae radix were determined in vitro inhibitory activity on $\alpha$-glucosidase and in vivo inhibition effect on blood glucose elevation in mice. Therefore, these results suggest that the extract of Paeoniae radix can be used as a new nutraceutial for inhibition on postprandial hyperglycemia as well as resource pool for lead compounds as a $\alpha$-glucosidase inhibitor.

Effects of Radix Sophora Flavescentis Extract on Insulin Secretion in RIN-m5F Cells and $\alpha$-glucosidase Inhibition (고삼(苦蔘)이 RIN-m5F세포의 인슐린 분비와 $\alpha$-glucosidase 활성 억제에 미치는 영향)

  • An, So-Hyun;Cho, Chung-Sik;Kim, Cheol-Jung
    • The Journal of Internal Korean Medicine
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    • v.30 no.3
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    • pp.481-494
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    • 2009
  • Background : Radix Sophora Flavescentis (SF) is used for the treatment of diabetes mellitus in Traditional Korean Medicine. However, little is known about the effects of Radix Sophora Flavescentis extract (SFE) on the hypoglycemic mechanism. Objective : We performed a series of experiments to verify the effects of SFE on the proliferation of RIN-m5F, the secretion and synthetic processes of insulin with glucose stimulation and inhibition of $\alpha$-glucosidase. Methods : Various amounts of SFE were added to the RIN-m5F cell culture to identify the effects on the cell proliferation, total amounts of insulin secretion, and related gene expression at the molecular level. Also to identify the inhibitory effect on the $\alpha$-glucosidase activities, ${\rho}NPG$ assay was done with various SFE concentrations followed by comparison with control. Results : SFE did not show considerable effects on RIN-m5F cells proliferation, insulin secretion or insulin mRNA expression, whichever phenomena did not depend on the glucose concentration. However, SFE significantly inhibited $\alpha$-glucosidase activity in a dose dependent manner compared to control. Conclusions : This study showed that SFE has potent $\alpha$-glucosidase inhibitory activity. Thus, SF may by used for the improvement of overall glycemic control. Further mechanism studies on the lipid toxicity and oxidation stress of SF seem to be necessary.

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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.