• 제목/요약/키워드: ${\alpha}$-Glucosidase inhibitory

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생약재 추출물로부터 분리한 ${\alpha}$-Glucosidase 저해활성물질 탐색 (${\alpha}$-Glucosidase Inhibitory Substances Exploration Isolated from the Herb Extract)

  • 최길용;한갑조;하상철
    • 한국식품저장유통학회지
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    • 제18권4호
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    • pp.620-625
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    • 2011
  • 당뇨병에 효과가 있는 식품소재의 탐색과 그 소재를 이용한 기능성 빵제품 개발에 관한 연구의 일환으로 당뇨병에 효과가 있다고 알려진 소장흡수 저해효소인 ${\alpha}$-glucosidase를 target로 시중에 유통되는 다양한 생약재를 대상으로 탐색을 하였다. ${\alpha}$-Glucosidase 저해활성을 조사하고자 생약재 200여종을 대상으로 물층과 메탄올 층으로 구분하여 탐색한 결과 물층에서는 황기(70.9%)가, MeOH층에서는 구인(72.9%)이 70%이상의 강력한 저해효과를 나타났으며 60%이상으로는 물층에서는 육두구(69%), 상백피(66.9%), 오미자(65%), 삼칠(63.9%), 전호(62.9%), 천문동(62.1%), 정공등(60.9%), 호장근(60.7%), 창출(60.2%), 소자(60.2%)등 이었으며, MeOH층으로는 만삼(67.8%), 도인(67.6%), 방기(63.5%), 동규자(61.6%) 순으로 활성효과를 나타내었으며 50%이상의 저해효과를 보인 것으로는 물층에서는 황정(59.8%), 신곡(59.7%), 택사(59.5%), 의인(59.2%), 세신(59.0%), 시호(53.0%)를 포함한 31여종, MeOH층에서는 사군자(58.8%), 구기자(58.3%), 과루인(58.0%), 백자인(55.9%), 백강잠(55.6%), 계내금(55.4%), 독활(55.3%), 구척(52.7%), 대극(52.7%), 백편두(52.5%) 10종이 저해효과를 나타내었다. 따라서 당뇨병 환자의 기능성 소재로 개발하는데 기초 자료가 될 것으로 기대된다.

Isolation and Characterization of $\alpha$-Glucosidase Inhibitor from the Fungus Ganoderma lucidum

  • Kim, Shin-Duk;Nho, Hong Joon
    • Journal of Microbiology
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    • 제42권3호
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    • pp.223-227
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    • 2004
  • An ${\alpha}$-glucosidase inhibitor, SKG-3, was isolated from the fruiting bodies of Ganoderma lucidum and its physico-chemical properties were characterized. It was a highly specific and effective reversible inhibitor of ${\alpha}$-glucosidase. It showed very potent inhibitory activity against a-glucosidase with an IC$\sub$50/ value of 4.6$\mu\textrm{g}$/$m\ell$, but no activity for any other glycosidases tested. Enzyme activity could be recovered upon dialysis, thus providing evidence for the reversibility of the inhibition. A Lineweaver-Burk plot indicated that the SKG-3 inhibition of ${\alpha}$-glucosidase was competitive.

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

  • 김미선;안선미;정인창;권기석;손호용
    • 한국식품저장유통학회지
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    • 제17권2호
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    • pp.290-296
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    • 2010
  • 반추동물의 급성 산독증의 예방 및 치료제 개발을 위해 100종의 브라질 식물 추출물을 이용하여 미생물 유래의 $\alpha$-amylase 및 $\alpha$-glucosidase 저해 활성을 평가하였다. 그 결과 Acacia jurema Mart., Anacardium humile A. St.-Hil., Cedrela odorata L., 및 Guazuma ulmifolia Lam 추출물에서 우수한 $\alpha$-amylase 및 $\alpha$-glucosidase 저해 활성을 확인하였으며, Plumeria drastica Mart.에서는 우수한 $\alpha$-amylase 특이적 저해활성을, Eugenia uniflora L.에서는 강력한 $\alpha$-glucosidase 특이적 저해 활성을 확인하였다. 6종의 추출물을 대상으로 $\alpha$-amylase에 대한 $IC_{50}$ 평가 결과, 현지에서 항당뇨제로 사용되는 A. humile A. St.-Hil., 추출물($IC_{50}$: $91.2{\mu}g/ml$)이 가장 강력한 저해를 나타내었으며, 항당뇨제로 이용되고 있는 acarbose ($IC_{50}$:$50.5{\mu}g/mL$)의 저해활성에 필적하였다. A. humile A. St.-Hil., 추출물은 $80^{\circ}C$, 또는 0.01N HCl 조건에서 60분간 처리에 활성의 변화가 나타나지 않았으며, 산 처리시에는 오히려 활성의 증가가 나타났다. 또한 A. humile A. St.-Hil., 추출물은 인간 적혈구에 대한 용혈활성을 나타내지 않아 반추동물의 급성 산독증 및 인간 당뇨병 치료에도 이용 가능하리라 판단된다.

여주씨에서 분리한 Vicine과 α-Eleostearic Acid의 α-glucosidase 저해효과 (α-Glucosidase Inhibitory Effect of Vicine and α-Eleostearic Acid from the Seeds of Momordica charantia)

  • 육흥주;노건민;최정숙;권오경;홍수영;강상수;조계만;박동식
    • 한국환경농학회지
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    • 제34권1호
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    • pp.57-63
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    • 2015
  • 최근 들어 여주의 혈당개선의 약리학적 효능이 보고됨에 따라 기능성 채소로 각광받고 있다. 주로 여주 과실만이 식용으로 쓰이지만 여주씨 또한 다양한 가공과정을 거칠 경우(건여주 혹은 건조분말, 환, 엑기스 등) 필연적으로 함께 섭취되기도 한다. 본 연구에서는 과실이외의 특히, 연구결과가 미비한 여주씨에 대해 생리활성물질의 구명 및 혈당개선의 효과에 대한 연구를 수행하였다. 다양한 추출물 및 단일 활성성분의 혈당개선 in vitro검증법인 ${\alpha}$-glucosidase에 대한 저해효과를 측정하였고, 활성을 나타내는 추출물 또는 활성성분과의 상관관계를 구명하였다. 구체적으로는 95% 에탄올 추출물 및 비극성 용매 등에 다량 추출되는 생리활성물질인 ${\alpha}$-eleostearic acid는 우수한 저해효과를 나타내었다($IC_{50}=43.4{\mu}g/mL$). 또한 효소저해제의 함량을 HPLC를 통한 정량분석을 수행함으로써 여주씨에 함유된 기능성성분의 혈당개선 식 의약 소재로의 응용가능성을 연구하였다.

잠뇨로부터 질소함유 당물질 분리 및 glycosidase에 대한 저해활성 (Isolation of N-Containing Sugars from Silkworm Urine and Their Glycosidase Inhibitory Activities)

  • 송주경;정성현
    • Biomolecules & Therapeutics
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    • 제6권4호
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    • pp.364-370
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    • 1998
  • Glycosidase inhibitors from urine of Bombyx mori were isolated and their inhibitory activities on glycosidases were evaluated. Six compounds were isolated by using several ion exchange columns, and their chemical structures were identified by the physicochemical and spectral data. Compound IV, V and Ⅵ were identified as 1-deoxynojirimycin, fagomine and 1,4-dideoxy-1,4-imino-D-arabinitol, respectively. Among six compounds isolated,1-deoxynojirimycin(IV) was the most potent inhibitor on $\alpha$-glucosidase and $\beta$-galactosidase of rat intestine, and its inhibitory activities for trehalase and almond $\beta$-glucosidase were relatively weak. Compound V and Ⅵl retained a little inhibitory potency toward $\alpha$-glucosidase and $\beta$-galactosidase. Compound II and III, however, have been found to have no effect on all glycosidases tested in this study.

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

  • 김상준;김지애;김다혜;곽설화;유강열;장선일;김선영;정승일
    • 생약학회지
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    • 제46권2호
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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.

Inhibition of Carbohydrate-Digesting Enzymes and Amelioration of Glucose Tolerance by Korean Medicinal Herbs

  • Kim, Sung-Hee;Kwon, Chong-Suk;Lee, Jung-Soon;Son, Kun-Ho;Lim, Jin-Kyu;Kim, Jong-Sang
    • Preventive Nutrition and Food Science
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    • 제7권1호
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    • pp.62-66
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    • 2002
  • As inhibitors of carbohydrate-digesting enzymes can prevent hyperglycemia that is known to cause many macrovascular complications, they may prove a useful adjunct to hypocaloric diets in patients with type 2 diabetes and obesity. Inhibitory activities of two hundred and fifteen kinds of medicinal herb extracts against $\alpha$-glucosidase (EC 3.2.1.20) and $\alpha$-amylase (EC 3.2.1.1) have been investigated in vitro. Adenophora triphylla, Aneilema keisak, and Morus bombysis significantly suppressed rat intestinal $\alpha$-glucosidase activity iu vitro. Porcine pancreatic amylase was efficiently inhibited by methanol extracts of Epimedium koreanum, Campsis grandiflora and Salvia plebeia. Methanol extract of Epimedium koreanum among the medicinal herbs tested showed the strongest inhibitory activity against porcine pancreatic $\alpha$-amylase with 0.1 mg/ML of $IC_{50}$/. The herb extract also improved glucose tolerance in ICR mice when loaded with 0.9 g soluble starch per kg body weight. Taken together, Epimedium koreanum merits further evaluation as a therapeutic measure.

Hypoglycemic Activity of the Hexane Extract of Oriental Melon (Cucumis melo L. var. makuwa Makino) Seeds and Its Active Compounds

  • Chen, Lei;Kim, Hye Suk;Choi, Bo-Ram;Yang, Shaonan;Xu, Enning;Suh, Jun Kyu;Kang, Young-Hwa
    • 한국자원식물학회지
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    • 제27권6호
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    • pp.622-628
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    • 2014
  • The aim of this work is to evaluate the potential of oriental melon (Cucumis melo L. var. makuwa Makino) seeds for the management of type 2 diabetes by controlling glucose absorption. The ${\alpha}$-glucosidase and ${\alpha}$-amylase inhibitory effects of the hexane extracts from oriental melon seeds were investigated. A bioassay-guided fractionation technique was used to elucidate the principal active components. The results show that the hexane extract from oriental melon seeds exhibited high inhibitory activities against ${\alpha}$-glucosidase and ${\alpha}$-amylase. The hexane extract was further fractionated into four sub-fractions. Among them, the sub-fraction F-1 exhibited the most potent anti-diabetic effect. The active components were isolated and identified by gas chromatography/mass spectroscopy (GC-MS). Free fatty acids showed significant hypoglycemic activity (p < 0.001) and fatty acid composition influenced enzyme inhibitory activities. These results suggest that oriental melon seeds could be used to prevent type 2 diabetes.

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

  • 안소현;조충식;김철중
    • 대한한방내과학회지
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    • 제30권3호
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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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연잎(Nelumbo nucifera) 추출물의 in vitro 생리활성 (In vitro biological activities of lotus (Nelumbo nucifera) leaves extract)

  • 박은정;조혜원;박유진;인만진;김동청
    • Journal of Applied Biological Chemistry
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    • 제64권2호
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    • pp.121-125
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    • 2021
  • 연잎(Nelumbo nucifera)의 60% (v/v) 에탄올 수용액 추출물의 항산화, 혈장 항응고 및 α-glucosidase 저해 효과를 in vitro에서 확인하였다. 연잎 추출물의 수율은 35.3±1.1%이었고, 폴리페놀 화합물 함량은 186.2±5.2 ㎍ gallic acid equivalents/mg으로 나타났다. 연잎 추출물은 농도에 비례하여 유리라디칼, 양이온라디칼 및 아질산염을 효과적으로 소거하였고 뛰어난 환원력을 보유하고 있었다. 또한 연잎 추출물은 농도 의존적으로 우수한 혈장 항응고 및 α-glucosidase 저해 활성을 나타내었다.