• Title/Summary/Keyword: a-glucosidase inhibitor

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Effect of Medicinal Plant Water Extracts on Glucose-regulating Enzyme Activities in Goto-Kakizaki Rat Liver Cytosol (약용식물 물 추출물이 Goto-Kakizaki 흰쥐의 간 세포액에서 당대사 관련효소 활성에 미치는 영향)

  • Kim, Dae-Jung;Chung, Mi-Ja;You, Jin-Kyoun;Seo, Dong-Joo;Kim, Jeong-Mi;Choe, Myeon
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.38 no.10
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    • pp.1331-1335
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    • 2009
  • We have studied the anti-diabetic effects of medicinal plant water extracts on hepatic glucose-regulating enzymes such as glucokinase (GK) and acetyl-CoA carboxylase (ACC). $\alpha$-Glucosidase inhibitor is usually used to prevent and treat type II diabetes; thus, anti-$\alpha$-glucosidase activity of medicinal plant water extracts was assayed. The hepatic cytosol faction of a type II diabetic animal (Goto-Kakizaki rat) was used in GK and ACC activity assays. The medicinal plants were Lycium chinense (JGP), Discorea japonica Thunb. (SY), Pyrus pyrifolia (YSB), Cornus officinalis (SSY), Paeonia suffruticosa ANDR. (MDP), Cordyceps militaris (DCH), and Acanthopanax senticosus (GSO). JGP, SY, YSB, and SSY water extracts increased the hepatic GK activity and all medicinal plant water extracts led to an increase in hepatic ACC activity. YSB, SSY, MDP, and GSO water extracts showed significantly higher anti-$\alpha$-glucosidase activity than control samples. The highest anti-$\alpha$-glucosidase activity was observed in GSO water extract and the anti-$\alpha$-glucoside activity was higher than that of Acarbose (reference $\alpha$-glucosidase inhibitor). We suggest that JGP, SY, YSB, and SSY water extracts may exert an anti-diabetic effect by enhancing the glucose metabolism and that YSB, MDP and GSO may be used as natural $\alpha$-glucosidase inhibitors in type II diabetic conditions. Increased ACC activity by plant water extracts may provide additional anti-diabetic effect.

Attenuation of insulin resistance using steamed Polygonatum odoratum var pluriflorum extract in rat skeletal muscle cells L6 myoblast (렛 근육세포 L6에서 둥굴레 추출물의 인슐린저항성 개선)

  • Choi, Mi-Ae
    • The Korea Journal of Herbology
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    • v.31 no.1
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    • pp.1-5
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    • 2016
  • Objectives : The purpose of this study was to investigate inhibitory effects of steamed Polygonatum odoratum extract (POE) on insulin resistance in rat skeletal muscle cells, L6 cells.Methods : Polygonatum odoratum (P. odoratum) extract was extracted with ethyl acetate. Activity of α-glucosidase in POE was measured for blood glucose regulation. MTT assay was examined for cell toxicity. Western blot analysis for measurement of adiponectine, peroxisome proliferator-activated receptorγ (PPARγ), insulin receptor substrate (IRS), glucose transporter 4 (Glut-4) and phosphorylation of serine/threonine-specific protein kinase (Akt) expressions were performed. Akt signaling pathway were analyzed with LY294002, which is a specific PI3K/Akt inhibitor.Results : The results revealed that POE inhibited α-glucosidase activity. Treatment of POE in L6 cells inhibited the differentiation of L6 cells compared to those of vehicl control. Additionally, protein expressions of adiponectine, PPARγ, IRS and Glut-4 were significantly regulated compared to those of vehicle control (p < 0.05), respectively. Futhermore, phosphorylation of Akt was increased in L6 cells treated with POE compared to that of vehicle control (p < 0.05). pAkt expression was significantly accentuated with Akt inhibitor (LY294002).Conclusions : These results suggest that POE may have potential as a natural agent for prevention/improvement of diabetes, especially, regulation of blood glucose. Therefore, further additional study should be conducted to elucidate in depth the pharmaceutical efficacy of these.

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.

Purification and Characterization of Beta-Glucosidase from Weissella cibaria 37

  • Lee, Kang Wook;Han, Nam Soo;Kim, Jeong Hwan
    • Journal of Microbiology and Biotechnology
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    • v.22 no.12
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    • pp.1705-1713
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    • 2012
  • A gene encoding ${\beta}$-glucosidase was cloned from Weissella cibaria 37, an isolate from human feces. Sequence analysis showed that the gene could encode a protein of 415 amino acids in length, and the translated amino acid sequence showed homology (34-31%) with glycosyl hydrolase family 1 ${\beta}$-glucosidases. The gene was overexpressed in E. coli BL21(DE3) using pET26b(+) and a 50 kDa protein was overproduced, which matched well with the calculated size of the enzyme, 49,950.87 Da. Recombinant ${\beta}$-glucosidase was purified by using a his-tag affinity column. The purified ${\beta}$-glucosidase had an optimum pH and a temperature of 5.5 and $45^{\circ}C$, respectively. Among the metal ions (5mM concentration), $Ca^{2+}$ slightly increased the activity (108.2%) whereas $Cu^{2+}$ (46.1%) and $Zn^{2+}$ (56.7%) reduced the activity. Among the enzyme inhibitors (1 mM concentration), SDS was the strongest inhibitor (16.9%), followed by pepstatin A (45.2%). The $K_m$ and $V_{max}$ values of purified enzyme were 4.04 mM and 0.92 ${\mu}mol/min$, respectively, when assayed using pNPG (p-nitrophenyl-${\beta}$-D-glucopyranoside) as the substrate. The enzyme liberated reducing sugars from carboxymethyl cellulose (CMC).

Antidiabetic Activity and Enzymatic Activity of Commercial Doenjang Certified for Traditional Foods (전통식품 품질인증 일부 시판 된장의 효소활성 및 항당뇨 활성)

  • Lee, So-Young;Kim, In-Sun;Park, So-Lim;Lim, Seong-Il;Choi, Hye-Sun;Choi, Shin-Yang
    • KSBB Journal
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    • v.27 no.6
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    • pp.361-366
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    • 2012
  • We investigated the anti-diabetic activity and enzymatic activity of 24 commercial doenjang samples certified for traditional foods. Twenty four doenjang samples showed the wide ranges in enzymatic activities (protease activities 0-50.45 unit/g, ${\alpha}$-amylase activities 0-675.9 unit/g, ${\beta}$-amylase 13.6-308.6 unit/g), and there were no difference in enzymatic activity by the producing region. To evaluate the potential anti-diabetic activity of 24 doenjang samples, we examined the effect of doenjang methanol extract (DME) on 2-[n-(7-nitrobenz-2-oxa-1, 3-diazol-4-yl) amyno]-2-deoxy-d-glucose (2-NBDG) uptake. Ten samples among 24 samples significantly stimulated the uptake of 2-NBDG. When the cells were treated with DME at 400 ug/mL, No. 17 and 23 specially stimulated 2-NBDG uptake by 1.23-fold and 1.25-fold, respectively, compared with untreated control cell. And there were no cytotoxicity in the C2C12 cells treated with DME at concentration of 500 ug/mL. Among 24 samples, No. 6, 7, 12, 21 and 24 showed the ${\alpha}$-glucosidase inhibitor activity at concentration of 10 mg/mL; however, they were less effective than acarbose which is a commercial ${\alpha}$-glucosidase inhibitor.

Inhibitory Effect of Bacillus subtilis Y3-7 Culture Broth on $\alpha$-Glucosidase Activity (Bacillus subtilis Y3-7 배양액의 $\alpha$-glucosidase 활성 억제 효과)

  • Myoung, Kil-Sun;Heo, Gun;Yoon, Suck-Yong;Shim, Jae-Jung;Lee, Jung-Hee;Lim, Kwang-Sei;Huh, Chul-Sung
    • Korean Journal of Food Science and Technology
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    • v.40 no.5
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    • pp.558-561
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    • 2008
  • Culture broth of Bacillus subtilis Y3-7 in tryptic soy broth (TSB) isolated from Korean traditional fermented food was evaluated for the inhibition of $\alpha$-glucosidase. The results of in vitro studies using the yeast $\alpha$-glucosidase demonstrated that the culture broth exerted inhibitory effects on $\alpha$-glucosidase with $IC_{50}$ value of 1.62 mg/mL, and functioned as a competitive inhibitor. Furthermore, the culture broth of B. subtilis Y3-7 significantly improved glucose tolerance in normal and streptozotocin-induced diabetic mice. The blood glucose levels in the mice receiving sucrose supplementation in the culture broth (1 g/kg, 2 g/kg) were measured at 48.7%, which corresponded to 22.2% of the levels measured in the control mice. These results indicated that the culture broth of B. subtilis Y3-7 in TSB might be considered as a useful compound for the preparation of functional foods for diabetic patients.

Synthesis and Conformational Study of Ser and Cys Derivatives of N-Hydroxy Diketopiperazine

  • You, Sang-Woo;Park, Won-Choul;Lee, Hyoung-Tae;Ueom, Jeong-Hoon;Jang, Soon-Min;Lee, Kyung-Hee;Lim, Dong-Yeol
    • Bulletin of the Korean Chemical Society
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    • v.28 no.12
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    • pp.2414-2418
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    • 2007
  • N-Hydroxy diketopiperazine derivatives from L- and D-forms of Ser and Cys were synthesized for the first time and the ring conformation of both analogues in water was determined to be close to flat via NMR and ab initio calculations. However, the side chain of the Ser analogue was oriented toward a pseudo-equatorial position while that of the Cys analogue was slightly oriented toward a pseudo-axial direction, with a slightly distorted boat-shaped ring conformation. Among them, the D-Cys analogue was found to be a weak inhibitor of α- glucosidase.

Characterization and Culture Optimization of an Glucosidase Inhibitor-producing Bacteria, Gluconobactor oxydans CK-2165 (α-Glucosidase 저해제 생산 균주, Gluconobacter oxydans CK-2165의 특성 및 배양 최적화)

  • Kim, Byoung-Kook;Suh, Min-Jung;Park, Ji-Su;Park, Jang-Woo;Suh, Jung-Woo;Kim, Jin-Yong;Lee, Sun-Young;Choi, Jongkeun;Suh, Joo-Won;Lee, In-Ae
    • Journal of the Korea Academia-Industrial cooperation Society
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    • v.13 no.11
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    • pp.5179-5186
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    • 2012
  • Miglitol, a well-known therapeutic intervention agents for diabetes, exhibits competitive inhibitory activity against ${\alpha}$-glucosidase and it is usually produced through three sequential steps including chemical and bioconversion processes. Gluconobactor oxydans (G. oxydans) belonging to acetic acid bacteria biologically, converts 1-deoxy-1-(2-hydroxyethylamino)-D-glucitol (P1) into a key intermidiate, 6-(2-hydroxyetyl) amino-6-deoxy-${\alpha}$-L-sorbofuranose (P2) by incomplete oxidation. In this study, we identified and optimized fermentation conditions of CK-2165, that was selected in soil samples by comparing the bioconversion yield. CK-2165 strain was found to be closely related to G. oxydans based on the result of phylogenetic analysis using 16S rDNA sequence. Utilization of API 20 kits revealed that this strain could use glucose, mannose, inositol, sorbitol, rhamnose, sucrose, melibiose, amygdalin and arabinose as carbon sources. The culture conditions were optimized for industrial production and several important factors affecting bioconversion rate were also tested using mycelial cake. Cell harvested at the late-stationary phase showed the highest bioconversion yield and $MgSO_4$ was critically required for the catalytic activity.

Oxya Chinensis Sinuosa Mishchenko Extract: Potent Glycosidase Inhibitor Alleviates Postprandial Hyperglycemia in Diabetic Mice (당뇨 모델을 이용한 벼메뚜기(O. Mistshenk) 추출물의 식후 고혈당 완화 효과)

  • Park, Jae Eun;Han, Ji Sook
    • Journal of Life Science
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    • v.30 no.12
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    • pp.1054-1062
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    • 2020
  • This study was designed to investigate whether extracts from Oxya chinensis sinuosa Mistshenk (an edible insect considered a grasshopper) could inhibit the activity of carbohydrate digestive enzymes and alleviate postprandial hyperglycemia in diabetic mice. Oxya chinensis sinuosa Mistshenk was extracted with 80% ethanol (OEE) or water (OWE) and then concentrated. The carbohydrate digestive enzyme-inhibiting activity of the resulting extracts was evaluated by examining α-glucosidase and α-amylase. The IC50 values of OEE against α-glucosidase and α-amylase were 0.229 mg/ml and 0.106 mg/ml, respectively. This result indicated that OEE has stronger inhibitory effects than OWE and positive control. The blood glucose levels of the diabetic control mice increased after one meal. However, when OEE (300 mg/kg) was added to starch, this increase in postprandial blood glucose levels was significantly suppressed. The area under the curve also significantly decreased following the administration of OEE, which exhibited no cytotoxicity. These results indicate that OEE is more efficacious than OWE and may be used as a carbohydrate digestive enzyme inhibitor, delay carbohydrate digestion and glucose absorption, and thus alleviate postprandial hyperglycemia caused by dietary carbohydrates.

Anti-diabetic Effects of Mixed Extracts from Lycium chinense, Cordyceps militaris, and Acanthopanax senticosus (지골피, 동충하초, 가시오가피 혼합 추출물의 항당뇨 작용)

  • Kim, Dae-Jung;Kim, Jeong-Mi;Kim, Tae-Hyuck;Baek, Jong-Mi;Kim, Hyun-Sook;Choe, Myeon
    • Korean Journal of Plant Resources
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    • v.23 no.5
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    • pp.423-429
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    • 2010
  • In this study, we examined the anti-diabetic activity in vitro by the mixed Korean herb water extracts(JDG) composed of Lycium chinense, Cordyceps militaris, and Acanthopanax senticosus on hepatic glucose-regulating enzyme activities such as glucokinase(GK), acetyl-CoA carboxylase(ACC), and inhibition activity of $\alpha$-glucosidase. The hepatic cytosol fraction of a type II diabetic animal(Goto-Kakizaki rat) was used in GK and ACC activity assays. JDG mixed water extracts significantly increased the hepatic GK and ACC activity. The highest anti-$\alpha$-glucosidase activity was observed in JDG 5 water extract when compared to the acarbose control, inhibitor of $\alpha$-glucosidase. We suggest that Lycium chinense, Cordyceps militaris, and Acanthopanax senticosus mixed water extracts may exert an anti-diabetic activity by enhancing the glucose metabolism and may be used as natural $\alpha$-glucosidase inhibitors in type 2 diabetic conditions.