• The Korea Journal of Herbology
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• v.32 no.6
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• pp.1-7
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• 2017

Objectives : The heartwood of Sappan Lignum has been used since ancient times as an ingredient in folk medicines against anti-bacterial and anti-anemia purposes. Many bioactive constituents have been derived from this biomass such as chalcones and homoisoflavonoids. In the current investigation, the antioxidant and anti-diabetic properties using DPPH and $ABTS^+$ radicals scavenging, ${\alpha}-glucosidase$, and advanced glycation end products (AGEs) inhibition assays were evaluated by different extraction methods of Sappan Lignum. Methods : In our continuing investigation for bioactive natural ingredients, the antioxidant and ${\alpha}-glucosidase$ inhibitory properties of Sappan Lignum extracts were prepared from different extraction methods and the biological efficacies were investigated in vitro. The antioxidant properties were evaluated employing radical scavenging assays using 1,1-diphenyl-2-picrylhydrazyl (DPPH) and 2,2'-azino-bis (3-ethylbenzothiazoline-6-sulphonic acid) ($ABTS^+$) radicals. In addition, the anti-diabetic effects of Sappan Lignum extracts were tested via ${\alpha}-glucosidase$ and AGEs formation inhibitory assay. The total phenolic contents were determined using a spectrophotometric method. Results : All the tested samples showed dose-dependent radical scavenging and ${\alpha}-glucosidase$ inhibitory activities. Among the tested extracts, the 80% methanolic extract of Sappan Lignum was showed the most potent activity with an $IC_{50}$ value of $82.3{\pm}1.7{\mu}g/m{\ell}$ against DPPH radical scavenging assay. While, $ABTS^+$ radical scavenging activity of 80% methanolic extract was higher than those of other extracts. Also, ${\alpha}-glucosidase$ inhibitory and AGEs formation effects of each extacts and total phenolic contents were evaluated. Conclusions : These results suggested that Sappan Lignum can be considered as a new effective source of natural antioxidant and anti-diabetic materials.

• The Korean Journal of Mycology
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• v.42 no.3
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• pp.207-212
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• 2014

This study was conducted in order to investigate the physiological activities, including antioxidative, fibrinolytic, thrombin inhibitory, and ${\alpha}$-glucosidase inhibitory activities of the water extract and solvent fractions isolated from Pholiota adiposa. The antioxidative activities of the water extract and water fraction were 57.57% and 48.27%, respectively. The fibrinolytic activity was strong only in the ethyl acetate fraction at 0.70 plasmin units/mL. The ethyl acetate fraction showed high thrombin inhibitory activity, and a-glucosidase inhibitory activity at 77.67% and 89.32%, respectively. The ethyl acetate fraction hydrolyzed both $A{\alpha}$ and $B{\beta}$ subunits of human fibrinogen, but did not show reactivity for the ${\gamma}$ form of human fibrinogen. Fibrinolytic activity of the ethyl acetate fraction was not decreased by heating for 10 min at $100^{\circ}C$.

• Korean Journal of Pharmacognosy
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• v.40 no.2
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• pp.150-154
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• 2009

We examined ethanol extracts prepared from the Korean marine algae belonging to the Sargassaceae family for their inhibitory effects on ${\alpha}$-glucosidase activity and free radicals in vitro. Among five marine algae, the extracts of Sargassum yezoense were found to possess strongly ${\alpha}$-glucosidase inhibition and free radicals scavenging activities. Two compounds were isolated via bioactivity guided isolation and tested for their effects on ${\alpha}$-glucosidase, DPPH, $ABTS^{+}$ and $Photochem^{(R)}$ analysis. Their chemical structures were elucidated by spectral analysis and direct comparison with authentic compounds; their structures were identified as sargaquinoic acid (1) and sargahydroquinoic acid (2). The inhibitory effects of compound 1 and 2 ($IC_{50}$ value:14.2 and 12.8 ${\mu}M$, respectively) on ${\alpha}$-glucosidase were more potent that of deoxynojirimycin as a positive control ($IC_{50}$ value:18.0 ${\mu}M$). All compounds displayed antioxidative activity which was measured by DPPH, $ABTS^{+}$ and $Photochem^{(R)}$ apparatus.

• YAKHAK HOEJI
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• v.55 no.6
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• pp.446-450
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• 2011

As an effort to find a new scaffold for ${\alpha}$-glucosidase inhibition, we have prepared total 11 phenylalkylated piperazine derivatives and tested their ${\alpha}$-glucosidase inhibitory activities. Compounds 8 ($IC_{50}=2.73{\pm}0.075mM$) possessing two 3-methoxyphenethyl group on 1,4-position of piperazine showed comparable potency to acarbose used as reference. But other compounds were inactive to ${\alpha}$-glucosidase. The result indicated that proper substituents on the piperazine can engender ${\alpha}$-glucosidase inhibitory activities on the piperazine derivatives.

• Korean Journal of Medicinal Crop Science
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• v.26 no.5
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• pp.382-390
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• 2018

Background: The plant Aster koraiensis has long been used as an ingredient in folk medicine. It has been reported that Aster koraiensis extract (AKE) prevents the progression of diabetes-induced retinopathy and nephropathy. However, although these beneficial effects of AKE on diabetes complications have been identified, the antidiabetic effects of AKE have not yet been completely investigated and quantified. In the present study, the glucose-lowering and antioxidant effects of aqueous and ethanolic AKEs were evaluated. Methods and Results: The glucose-lowering effects of aqueous and ethanolic (30%-, 50%-, and 80%-ethanol) AKEs were investigated via ${\alpha}$-glucosidase inhibitory assays. The mode of inhibition by AKEs on ${\alpha}$-glucosidase was identified through kinetic analysis. The total antioxidant capacity of each of the 4 AKEs was evaluated by assessing their conversion rate of $Cu^{2+}$ to $Cu^+$. The content of chlorogenic acid and 3,5-di-O-caffeoylquinic acid, the bioactive compounds in AKE, in each extract were analyzed by high performance liquid chromatography (HPLC). The AKEs showed potent ${\alpha}$-glucosidase inhibitory activity with mixed inhibition mode, and significant antioxidant capacity. Conclusions: These results of this study suggested that the AKEs tested had ${\alpha}$-glucosidase inhibitory and antioxidant effects. Among the extracts, the 80% ethanol extract showed the most significant ${\alpha}$-glucosidase inhibitory activity, with a half maximal inhibitory concentration ($IC_{50}$ value) of $1.65{\pm}0.36mg/m{\ell}$ and a half maximal effective concentration ($EC_{50}$ value) for its antioxidant activity of $0.42{\pm}0.10mg/m{\ell}$. It can therefore be used as a source of therapeutic agents to treat diabetes patients.

• Korean Journal of Microbiology
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• v.38 no.2
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• pp.139-143
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• 2002

To find $\alpha$-glucosidase inhibitors produced by Actinomycetes, bacteria belonging to Actinomycetes were isolated from soil sample using Bennett's medium. The inhibitory activity induced by these bacteria on $\alpha$-glucosidase, which is the key enzymes far carbohydrates digestion and the prevention of diabetic complications, was investigated. A strain of these bacteria, PM718 potently inhibited $\alpha$-glucosidase activity in vitro.

• Korean Journal of Medicinal Crop Science
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• v.15 no.2
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• pp.128-131
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• 2007

This study was carried out to investigate inhibitory effect of extracts from Artemisia capillaris Thumb. on maltase, sucrase, ${\alpha}-amylase$, nonspecific ${\alpha}-glucosidase$, and postprandial hyperglycemia. Methanol extract and organic solvent (n-hexane, ethyl acetate, butanol, aqueous) fractions from the medicinal herb were determined for the inhibitory activities against maltase, sucrase and ${\alpha}-amylase$. The methanol extract from A. capillaris strongly inhibited maltase (57%) and ${\alpha}-glucosidase$ (72%) at the concentration of 100 ${\mu}g/m{\ell}$. Among the four fractions (n-hexane, ethyl acetate, butanol, aqueous) examined, the butanol fraction from A. capillaris showed potent inhibitory effects on maltase (73%), sucrase (33%), and ${\alpha}-amylase$ (75%) at the concentration of 100 ${\mu}g/m{\ell}$. The butanol fraction from Artemisia capillaris also exhibited significant reductions (20%) of blood glucose elevation in mice loaded with maltose. These results suggest that the extract from Artemisia capillaris can be used as a new nutraceutical for inhibition on postprandial hyperglycemia

• 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.

• 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.

• Horticultural Science & Technology
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• v.28 no.5
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• pp.857-863
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• 2010

This study was conducted to evaluate the antioxidant activity, Angiotensin I Converting Enzyme (ACE) inhibitory activity, ${\alpha}$-glucosidase inhibitory activity, nitrate synthesis inhibitory activity, and antiproliferation inhibitory effect on ethanol extract and its solvent fractions of $Coreopsis$ $tinctoria$ Nutt. Ethyl acetate fraction was the strongest at 1,1-diphenyl-2-picryl hydrazyl (DPPH) ($IC_{50}=0.100mg{\cdot}mL^{-1}$) and 2,2'-Azino-bis-(3-ethylbenozothiazoline-6-sulfonic acid) (ABTS) (15.785 mg AA $eq{\cdot}10mg^{-1}$) radical scavenging activity, ACE (40.96% at $1mg{\cdot}mL^{-1}$), and ${\alpha}$-glucosidase ($IC_{50}=0.125mg{\cdot}mL^{-1}$) inhibitory effect among the solvent fractions. Nitrate synthesis inhibitory activity of ethanol extract, chloroform fraction, and ethyl acetate fraction effectively inhibited NO formation in a dose-dependent manner without the cytotoxic effect. Ethanol extract and its solvent fractions inhibited growth of HCT-116 colon cancer cells in a dose-dependent manner. n-Hexane fraction showed the highest antiproliferation inhibitory effect of $0.041mg{\cdot}mL^{-1}$ among fractions.