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

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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.

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.

Isolation of $\alpha$-Glucosidase Inhibitor Producing Soil Microorganism and Inhibitory Effects of Microbial Metabolites on ${\alpha}$-Glucosidase

  • Lee, Jin-Woo;Park, Sung-Sook;Kang, Byoung-Yong;Kim, Kyoung-Je;Ha, Nam-Joo
    • Proceedings of the PSK Conference
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    • 2002.10a
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    • pp.335.3-336
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    • 2002
  • To find ${\alpha}$-Glucosidase Inhibitors produced by Actinomycetes, 20 soil samples were tested and 53 Actimycetes were isolated. One of 53 Actinomycetes (strain PM718) showed very potent inhibitory activity in vitro. The morphological and physiological characteristics of strain PM 718 were investigated. The spore morphology. spore chain morphology and spore surface were observed by scanning electron microscope. The inhibitory activity of strain PM718 in vivo has been studied in mice made hyperglycemia by Streptozotocin treatment. The strain PM718 showed signficant reduction of blood glucose level(more than 30%) in mice loaded with maltose.

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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.

Acute Toxicity and Antimicrobial Activity of 1-Deoxynojirimycin (1-Deoxynojirimycin의 급성독성 및 항균효과)

  • 백남수;김영만
    • The Korean Journal of Food And Nutrition
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    • v.11 no.6
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    • pp.629-634
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    • 1998
  • 1-Deoxynojirimycin which is a potent intestinal ${\alpha}$-glucosidase inhibitor was purified from the culture broth by ion exchange chromatography, Sephadex LH20 column chromatography, TSK gel chromatography and HPLC respectively. Acute toxicity of 1-deoxynojirimycin, which was loaded through the oral as dose of 200mg/kg, was investigated in IRC mouse. None of the tested IRC mice were not dead and increase of body weight showed also the same results in comparison with control mice. The antimicrobial susceptibility of 20 pathogenic strains against 3 antidiabetic compounds (1-deoxynojirimycin, AO-128, acarbose) were obtained by agar dilution method. All of the three antidiabetic compounds has very weak antimicrobial activity (MIC>100$\mu\textrm{g}$/ml).

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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.

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

  • Yuk, Heung Joo;Noh, Geon Min;Choe, Jeong Sook;Kwon, Oh Kyung;Hong, Su Young;Kang, Sang Soo;Cho, Kye Man;Park, Dong Sik
    • Korean Journal of Environmental Agriculture
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    • v.34 no.1
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    • pp.57-63
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    • 2015
  • BACKGROUND: Momordica charantia (MC) have been used in various parts of the world to treat diabetes. Despite the highest effects of phytochemicals than any other part of the plant, the main components of seed of MC grown in Korea and their properties have not been studied extensively. METHODS AND RESULTS: The seeds of MC were extracted into five different polarity solvents: 30%, 50%, 70%, 95% ethanol and distilled water. The 95% ethanol extract showed the most potent inhibition ($IC_{50}=88.7{\mu}g/mL$) against ${\alpha}$-glucosidase. To investigate the compounds responsible for this effect, activity guided fractionation of MC seeds by chromatography yielded two phytochemicals which were confirmed as vicine (1) and ${\alpha}$-eleostearic acid (2) based on their NMR and ESI-MS spectroscopic data. Among them, ${\alpha}$-eleostearic acid (2) possessed potent ${\alpha}$-glucosidase inhibitory activities with $IC_{50}$ values from $32.4{\mu}g/mL$. CONCLUSION: Collectively, the results from this present study strongly suggest that both extract and ${\alpha}$-eleostearic acid (2) have potent ${\alpha}$-glucosidase inhibitory activity. Furthermore, ${\alpha}$-eleostearic acid (2) as the most active ${\alpha}$-glucosidase inhibitor was proven to be present in high quantities in the MC seeds by a HPLC chromatogram.

Linoleic Acid from Bamboo (Phyllostachys Bambusoides) Displaying Potent α- Glucosidase Inhibition (대나무로부터 분리한 linoleic acid의 α-glucosidase 저해활성 연구)

  • Jung, Sun-In;Kang, Su-Tae;Choi, Cheol-Yong;Oh, Kyeong-Yeol;Cho, Jung-Keun;Rengasamy, Rajesh;Park, Ki-Hun
    • Journal of Life Science
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    • v.19 no.5
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    • pp.680-683
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    • 2009
  • Glycosidase inhibitors are major targets in the treatment of type II diabetes, cancer and viral infections. This study was carried out to investigate the glycosidase inhibitory substances from bamboo (Phyllostachys bambusoides). Bamboo was extracted with methanol and then further fractionated with n-hexane, chloroform, n-BuOH and aqueous to get an active fraction. All extracts were evaluated for ${\alpha}$-glucosidase inhibitory activities to identify the n-hexane fraction with 33.5 ${\mu}$g/ml of IC50 value. Active compound 1 in the n-hexane fraction was identified as linoleic acid, which exhibited inhibitory activity with 12.4 ${\mu}$M of IC50 value. Mechanistic analysis showed that linoleic acid exhibited noncompective inhibition. This is the first study in which bamboo is reported to show ${\alpha}$-glucosidase inhibitory activity.

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

  • 송주경;정성현
    • Biomolecules & Therapeutics
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    • v.6 no.4
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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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Inhibitory Effects of Crude Drugs on $\alpha$-Glucosidase

  • Choi, Hyuck-Jai;Kim, Nam-Jae;Kim, Dong-Hyun
    • Archives of Pharmacal Research
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    • v.23 no.3
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    • pp.261-266
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    • 2000
  • The inhibitory activity of several crude drugs on $\alpha$-glucosidases, which are the key enzymes for carbohydrate digestion and the prevention of diabetic complications, was investigated. Several crude drugs including Terminaliae Fructus, Mori Cortex Radicis, Caesalpiniae Lignum and Cyrophora esculenta potently inhibited maltase and sucrase isolated from rat intestine, while Arecae Semen and Corni Fructus remarkably inhibited $\alpha$-amylase. Caesalpiniae Lignum and Gyrophora esculenta exhibited significant reductions of blood glucose elevation in mice loaded with maltose and sucrose.

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