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

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Sargassum yezoense Extract Inhibits Carbohydrate Digestive Enzymes In Vitro and Alleviates Postprandial Hyperglycemia in Diabetic Mice.

  • Park, Jae-Eun;Lee, Ji-Hee;Han, Ji-Sook
    • Preventive Nutrition and Food Science
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    • v.22 no.3
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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.

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.

Physiological Functionalities of Hot Water Extract of Codonopsis lanceolata and Some Medicinal Materials, and Their Mixtures (더덕과 일부 한약재 열수추출물의 혼합 비율에 따른 생리활성)

  • Oh, Hae-Sook;Kim, Jun-Ho
    • The Korean Journal of Community Living Science
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    • v.18 no.3
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    • pp.407-415
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    • 2007
  • The aim of this study was to investigate the physiological functionalities of Codonopsis lanceolata, Glycyrrhiza uralensis, Chaenomeles sinensis, Crataegus pinnafida, and their mixtures. We also determined their antioxidative, fibrinolytic, and ${\alpha}-glucosidase$ inhibitory activities. The antioxidative activities of Codonopsis lanceolata, Glycyrrhiza uralensis, Chaenomeles sinensis, and Crataegus pinnafida were 79%, 88.3%, 89.9%, and 89.3% respectively. Their fibrinolytic activities were 0.80plasmin unit/mi, 0.57 plasmin unit/mi, 0.52 plasmin unit/mi, and 0.53 plasmin unit/mi respectively. The ${\alpha}-glucosidase$ inhibitory activity of Codonopsis lanceolata was 25%. The 10-fold diluents of Glycyrrhiza uralensis, Chaenomeles sinensis, and Crataegus pinnafida showed ${\alpha}-glucosidase$ inhibitory activities of 93.6%, 65.3%, and 61.3% respectively. In antioxidative activity tests of the medicinal plants mixtures at various ratios, the mixtures of Glycyrrhiza uralensis, Chaenomeles sinensis, and Crataegus pinnafida with Codonopsis lanceolata showed antioxidative activities of approximately 90%. In fibrinolytic activity tests mixtures(1:1) of Codonopsis lanceolata with Chaenomeles sinensis and Crataegus pinnafida exhibited increases of 23% and 24% in activity respectively. In ${\alpha}-glucosidase$ inhibitory activity tests, a mixture (4:1) of Codonopsis lanceolata and 10-fold diluted Glycyrrhiza uralensis showed an inhibitory activity of 98%, a mixture (3:1) of Codonopsis lanceolata and 10-fold diluted Chaenomeles sinensis showed an inhibitory activity of 69.6%, and a mixture (1:1) of Codonopsis lanceolata and 10-fold diluted Crataegus pinnafida showed an inhibitory activity of 50.2%. In conclusion, the mixtures of Glycyrrhiza uralensis, Chaenomeles sinensis, and Crataegus pinnafida with Codonopsis lanceolata will be used as a material for the development of biofunctional foods.

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Biological activities of Solvent Fractions Isolated from Areca catechu L

  • Kim, Jun-Ho;Oh, Hae-Sook
    • Biomedical Science Letters
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    • v.16 no.4
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    • pp.271-277
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    • 2010
  • This study was conducted to investigate the biological activities of Areca catechu L. The antioxidative, fibrinolytic, thrombin inhibitory, and ${\alpha}$-glucosidase inhibitory activities of Areca catechu L extracted with hexane, $CHCl_3$, ethyl acetate, butanol, and water were measured. The water fraction showed the highest extraction yield at 3.65% (w/w). The butanol, $CHCl_3$, water, and ethyl acetate fractions showed strong antioxidative activities at 81.6%, 87.1%, 88.0%, and 89.5%, respectively. The fibrinolytic activity was strong only in the ethyl acetate fraction at 0.84 plasmin units/ml. The 100-fold dilution of the water fraction had the strongest thrombin inhibitory activity at 59.2%. The 100-fold dilution of butanol fraction displayed the strongest ${\alpha}$-glucosidase inhibitory activity at 88.6%. In conclusion, the extracts of Areca catechu L hold promise for use in the development of biofunctional foods to prevent cardiovascular diseases.

Effect of Medicinal Herb Prepared through Traditional Antidiabetic Prescription on α-Glucosidase Activity and Evaluation Method for Anti-Melanogenesis Agents Using α-Glucosidase Activity (당뇨 처방에 근거한 생약재의 α-Glucosidase 활성 저해 효과 및 이를 활용한 미백 소재 평가법)

  • Kim, Mi Jin;Im, Kyung Ran;Yoon, Kyung-Sup
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.44 no.7
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    • pp.993-999
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    • 2015
  • For the purpose of investigating the in vitro antidiabetic activity of a medicinal herb and herb mixture extracts prepared through traditional antidiabetic prescription, this study examined ${\alpha}$-glucosidase inhibitory activity. Tyrosinase, a type I membrane glycoprotein, is synthesized and glycosylated in the endoplasmic reticulum (ER) and Golgi. The enzyme is subsequently transported to melanosomes, where it participates in melanogenesis. Previous studies showed that disruption of early ER N-glycan processing by an ${\alpha}$-glucosidase inhibitor suppresses tyrosinase enzymatic activity and melanogenesis. According to the results, most oriental medicinal herbal extracts were stronger than acarbose and N-butyldeoxynojirimycin, known as an ${\alpha}$-glucosidase inhibitor. Interestingly, ethyl acetate layer of enzyme hydrolyzed Cheongsimyeonjaeum had an inhibitory effect on melanin synthesis in B16F1 cells, although it did not inhibit tyrosinase activity directly. Together, ${\alpha}$-glucosidase inhibition activity could be used to evaluate anti-melanogenesis, although cross-checking with melanin inhibitory assay is recommended.

Isolation and Identification of α-Glucosidase Inhibitory Compounds, Hyperoside, and Isoquercetin from Eleutherococcus senticosus Leaves (가시오갈피(Eleutherococcus senticosus) 잎으로부터 α-Glucosidase의 저해 활성 물질, Hyperoside와 Isoquercetin의 분리 및 구조·동정)

  • Lee, Ki Yeon;Hong, Soo Young;Jeong, Hye Jeong;Lee, Jae Hyoung;Lim, Sang Hyun;Heo, Nam-Kee;Kim, Songmun;Kim, Hee-Yeon
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.43 no.12
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    • pp.1858-1864
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    • 2014
  • In the present investigation, the anti-diabetic potential of 80% ethanol extract of Eleutherococcus senticosus leaves (EEES) was examined based on ${\alpha}$-glucosidase inhibitory activities. EEES was sequentially fractionated with n-hexane, chloroform, ethyl acetate (EtAOc), n-butanol, and $H_2O$. Of the various fractions, EtAOc fraction effectively inhibited ${\alpha}$-glucosidase activity by 68.05%. Therefore, EtAOc fraction was selected for further isolation and identification studies. EtAOc fraction was separated by medium pressure liquid chromatography with silica and ODS gel to yield eight fractions (EAA~EAH). Based on the results of ${\alpha}$-glucosidase inhibitory activity, EAH fraction was re-chromatographed to yielded four more fractions (EAHA~EAHD). Of these, EAHC fraction showed higher ${\alpha}$-glucosidase inhibitory activity of 93.60%. EAHC fraction was re-chromatographed and yielded EAHCA and EAHCB fractions. Further, identification and chemical structures of these two fractions were analyzed using $^1H$-NMR, $^{13}C$-NMR, and mass spectra data. Based on the results of the spectral data, the isolated compounds were identified as hyperoside and isoquercetin. Results of the present study indicate that the isolated compounds, hyperoside, and isoquercetin from leaves of E. senticosus could be used for the development of new anti-diabetic drugs.

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.

Hypoglycemic Effect of Padina arborescens Extract in Streptozotocin-induced Diabetic Mice

  • Park, Mi Hwa;Han, Ji Sook
    • Preventive Nutrition and Food Science
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    • v.17 no.4
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    • pp.239-244
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    • 2012
  • This study investigated the hypoglycemic effect of the Padina arborescens extract in STZ-induced diabetic mice. Freeze-dried Padina arborescens were extracted with 80% methanol and concentrated for use in this study. The hypoglycemic effect was determined by inhibitory activities against ${\alpha}$-glucosidase and ${\alpha}$-amylase as well as the alleviation of postprandial blood glucose level. Padina arborescens extracts showed higher inhibitory activities than acarbose, a positive control against ${\alpha}$-glucosidase and ${\alpha}$-amylase. The $IC_{50}$ values of Padina arborescens extracts against ${\alpha}$-glucosidase and ${\alpha}$-amylase were 0.26 and 0.23 mg/mL, respectively, which evidenced as more effective than observed with acarbose. The increase of postprandial blood glucose levels were significantly suppressed in the Padina arborescens extract administered group than the control group in the streptozotocin induced diabetic mice. Furthermore, the area under the curve (AUC) was significantly lowered via Padina arborescens extract administration in diabetic mice (p 0.05). These results indicated that the Padina arborescens extract might be used as an inhibitor of ${\alpha}$-glucosidase and ${\alpha}$-amylase and delay absorption of dietary carbohydrates.

The activity of ${\alpha}$-amylase and ${\alpha}$-glucosidase as anti-diabetic function

  • Kim, Misook;Kim, Eunji;Kwak, Han Sub;Jeong, Yoonhwa
    • Nutrition Research and Practice
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    • v.8 no.5
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    • pp.602-606
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    • 2014
  • BACKGROUND/OBJECTIVES: We investigated total 26 ingredients of Saengshik which will be commercially produced as an anti-diabetic dietary supplement. SUBJECTS/METHODS: Thirteen vegetables, nine cereals, three legumes and one seed were extracted with aqueous ethanol for 2 h at $60^{\circ}C$, and evaluated for their inhibitory effects against ${\alpha}$-amylase and ${\alpha}$-glucosidase and for total phenolic and flavonoid contents. RESULTS: All ingredients inhibited ${\alpha}$-amylase activity except cabbage. Strong inhibitory activity of ${\alpha}$-amylase was observed in leek, black rice, angelica and barley compared with acarbose as a positive control. Stronger inhibition of ${\alpha}$-glucosidase activity was found in small water dropwort, radish leaves, sorghum and cabbage than acarbose. All Saengshik ingredients suppressed ${\alpha}$-glucosidase activity in the range of 0.3-60.5%. Most ingredients contained total phenols which were in the range of 1.2-229.4 mg gallic acid equivalent/g dried extract. But, total phenolic contents were not observed in carrot, pumpkin and radish. All ingredients contained flavonoid in the range of 11.6-380.7 mg catechin equivalent/g dried extract. CONCLUSIONS: Our results demonstrate that Saengshik containing these ingredients would be an effective dietary supplement for diabetes.