• Korean Journal of Pharmacognosy
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• v.35 no.4 s.139
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• pp.271-275
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• 2004

Distylium racemosum Sieb. Et Zucc contains some compounds inhibit -amylase activity in experimental conditions. The inhibitory test showed that 50% acetone extracts from the bark and leaves of the plant strongly inhibited salivary -amylase activity. Proanthocyanidin(PA) which has strong inhibitory activity was extracted from the leaves by chromatography on Sephadex LH-20. The inhibitory activities and the inhibition kinetics of the PA were studied against three kinds of enzymes: human salivary ${\alpha}-Amylase$ (SAA), pork pancreatin ${\alpha}-Amylase$ (PAA) and yeast ${\alpha}-Glucosidase$ (AG). Then the activities of PA against SAA, PAA and AG were compared with those of acarbose, a commercial agent. The inhibitory activities of PA were stronger than those of acarbose. Inhibition kinetics of the PA showed competitive inhibition for SAA and PAA, and non competitive inhibition for GA.

• Applied Biological Chemistry
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• v.48 no.1
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• pp.103-108
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• 2005

${\alpha}-Amylase$ inhibitor is used to control blood glucose level by inhibiting starch digestion in the small intestine and delaying the absorption of glucose. In this study, we investigated the effect of the ethanol extracts from more than 1400 species of plants against ${\alpha}-amylase$ with the aim of developing a new ${\alpha}-amylase$ inhibitor. In the results, Cornus walteri extracts showed the highest inhibition activity. The inhibitory effect of Cornus walteri extract on the carbohydrate hydrolysis enzymes has different sensitivities against ${\alpha}-amylase$ from salivary and pancreatin and against ${\alpha}-glucosidase$ from yeast and porcine small intestine. In the study of inhibition kinetics of ${\alpha}-amylase$ and ${\alpha}-glucosidase$, Cornus walteri extract showed competitive inhibition against salivary and pancreatin while showing the combination of uncompetitive and noncompetitive inhibition against ${\alpha}-glucosidase$. The Cornus walteri extract was stable at acidic and thermal conditions. As for the blood glucose and body weight levels of Cornus walteri extract, we confirmed anti-hyperglycemic and anti-obesity effects. Also, in the investigation of the mRNA lever, Cornus walteri extract upregulated the level of GLUT4 mRNA in the quadriceps muscle.

• BMB Reports
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• v.40 no.4
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• pp.494-500
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• 2007

The endophytic bruchid pest Callosobruchus maculatus causes severe damage to storage cowpea seeds, leading to economical losses. For this reason the use of $\alpha$-amylase inhibitors to interfere with the pest digestion process has been an interesting alternative to control bruchids. With this aim, $\alpha$-amylase inhibitors from baru seeds (Dipteryx alata) were isolated by affinity chromatographic procedures, causing enhanced inhibition of C. maculatus and Anthonomus grandis $\alpha$-amylases. To attempt further purification, this fraction was applied onto a reversed-phase HPLC column, generating four peaks with remarkable inhibition toward C. maculatus $\alpha$-amylases. SDS-PAGE and MALDI-ToF analysis identified major proteins of approximately 5.0, 11.0, 20.0 and 55 kDa that showed $\alpha$-amylase inhibition. Results of in vivo bioassays using artificial seeds containing 1.0% (w/w) of baru crude extract revealed 40% cowpea weevil larvae mortality. These results provide evidence that several $\alpha$-amylase inhibitors classes, with biotechnological potential, can be isolated from a single plant species.

• 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.

• Microbiology and Biotechnology Letters
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• v.38 no.2
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• pp.183-189
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• 2010

In the course of screening for anti-acidosis and anti-diabetes agent from natural products, the inhibitory activities of Nepales plant extracts against microbial $\alpha$-amylase and $\alpha$-glucosidase were evaluated. Among the 100 different kinds of ethanol extracts, Cedrus deodara (Roxb.) G. Don and Myrica nagi Thunb showed strong inhibition activities against $\alpha$-amylase. The $IC_{50}$ values of C. deodara (Roxb.) G. Don, M. nagi Thunb and acarose, a commercial available anti-diabetes agent, were 44.5, 47.5 and $50.5\;{\mu}g/mL$, respectively. Considering the crude extract of C. deodara (Roxb.) G. Don, and M. nagi Thunb, these extracts have strong potentials as anti-acidosis or anti-diabates agent. In a while, Cleistocalyx operculatus (Roxb.) extract showed a good inhibition activity to $\alpha$-amylase and $\alpha$-glucosidase, even it was recently reported. The selected three extracts did not show any hemolysis activity against human red blood cell up to 1 mg/mL, and the inhibition activities were maintained by heat or acid treatment. Moreover, treatment of HCl (0.01N) for 1 h into C. operculatus (Roxb.) and M. nagi Thunb increased the inhibition activity from 50% to 70%. Our results suggest that C. deodara (Roxb.) G. Don, M. nagi Thunb, and C. operculatus (Roxb.) are potential as anti-acidosis and anti-diabetes agents.

• Food Science and Preservation
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• v.17 no.2
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• pp.290-296
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• 2010

To develop anti-acidosis and anti-diabetes agentsfrom natural products, the inhibitory activities of Brazilian plant extracts against microbial $\alpha$-amylase and $\alpha$-glucosidase were evaluated. Among 100 different ethanol extracts tested, those of Acacia jurema Mart., Anacardium humile A. St.-Hil., Cedrela odorata L., and Guazuma ulmifolia Lam showed good inhibitoryactivities toward both enzymes. In addition, an extract of Plumeria drastica Mart. showed specific inhibition of $\alpha$-amylase, whereas that of Eugenia uniflora L. demonstrated strong inhibition of the enzyme. IC50 values of $\alpha$-amylase inhibition suggested that the extract of A. humile A. St.-Hil., which has been used as an anti-diabetes medicine in Brazil, had potent inhibitory activity. The IC50 for the A. humile A. St.-Hil. extract ($91.2{\mu}g/mL$) was similar to that of acarbose ($50.5{\mu}g/mL$). This activity of A. humile A. St.-Hil. was not reduced by heat or acid treatment. Moreover, treatment with HCl (0.01 M) for 1 h increased the inhibitory activity from 57.5% to 81.2%. Also, the extract did not cause hemolysis of human red blood cells at levels up to 1 mg/mL. The results indicate that the extract of A. humile A. St.-Hil. is potentially useful as an anti-acidosis and anti-diabetes agent.

• Food Science and Preservation
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• v.21 no.2
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• pp.254-263
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• 2014

This study was carried out to analyze the effects of water and 70% ethanol extract on the antioxidative and antidiabetic activities of Smilax china L., a vine shrub belonging to the lily family. The activities of the extracts were measured based on the total phenolic and flavonoid contents and through on the results of the antioxidant tests, such as the electron-donating ability, ABTs radical scavenging activities, SOD-like activity, xanthine oxidase inhibition effect, antioxidant protection factor (PF), TBARs content and ACE inhibition activity, and ${\alpha}$-glucosidase, and ${\alpha}$-amylase inhibition activity. The resulting total phenolic and flavonoid contents of the 70% ethanol extract from S. china L. were greater than those of the water extract from S. china L. With regard to the results of the antioxidant tests, such as the electron-donating ability, ABTs radical scavenging activity, SOD-like activity, xanthine oxidase inhibition effect, antioxidant protection factor (PF), and TBARs content, those from the 70% ethanol extract from S. china L. were greater than those from the water extract from S. china L. Also, with regard to the ACE inhibition effect and ${\alpha}$-glucosidase and ${\alpha}$-amylase inhibition, those from the 70% ethanol extract from S. china L. were greater than those from the water extract from S. china L. All these findings show that the 70% ethanol extract from S. china L. has greater antioxidative and antidiabetic effects and can be used as a preventive agent for oxidation and diabetes.

• Proceedings of the Korean Society of Life Science Conference
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• 2003.05a
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• pp.23-37
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• 2003

A novel inhibitor against maltose-producing a-amylase was prepared via stepwise degradation of a high molecular weight acarbose (HMWA) using Thermus maltogenic amylase (ThMA). The structure of the purified inhibitor was determined to be ${\alpha}$-D-glucopyranosyl-${\alpha}$-acarviosinyl-D-glucopyranose (GlcAcvGlc). Progress curves of p-nitrophenyl-${\alpha}$-D-maltoside (PNPG2) hydrolysis by various amylolytic enzymes, including maltogenase (MGase), ThMA, and cyclodextrinase(CDase) I-5, in the presence of acarbose or GlcAcvGlc indicated a slow-binding mode of inhibition. The inhibition potency of GlcAcvGlc for MGase, ThMA, and CDase I-5 was 3 orders of magnitude higher than that of acarbose.

• Journal of the Korean Society of Food Science and Nutrition
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• v.40 no.2
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• pp.308-315
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• 2011

We investigated ${\alpha}$-amylase, ${\alpha}$-glucosidase and lipase inhibitory activity of extracts collected from wild plants in Gangwon-do. 90 wild plants were collected and their water and ethanol extracts were obtained. Results of measuring ${\alpha}$-amylase inhibitory activity indicated more than 80% of activity inhibition in 10 mg/mL concentration for ethanol extracts of three plants and water extracts of two plants. For ${\alpha}$-glucosidase inhibitory activity, ethanol extracts of thirteen plants and water extracts of three plants showed more than 80% of activity inhibition in 10 mg/mL concentration. In the experiment of inhibiting lipase activity, ethanol extracts of seven plants and water extracts of one plants showed above 80% of activity inhibition in 10 mg/mL concentration. These results suggest that the selected extracts could be potentially used as a resource of bioactive materials for health functional foods.

• Journal of Pharmacopuncture
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• v.22 no.2
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• pp.115-121
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• 2019

Objectives: The objective of this study was to evaluate antidiabetic activity of Chaturmukha rasa based on streptozotocin induced diabetes model, alpha amylase inhibitory activity, alpha Glucosidase inhibitory activity and inhibition of sucrase. Methods: Chaturmukha rasa was prepared as per Ayurvedic formulary. Antidiabetic activity was measured in experimentally streptozotocin induced rats. The dose was taken as 45 mg/kg, i.p. The antidiabetic activity of Chaturmukha rasa was compared Triphala Kwatha, a marketed formulation. Further In vitro $\acute{\alpha}$- Amylase Inhibitory Assay, In vitro salivary amylase Inhibitory Assay, In vitro ${\alpha}-Glucosidase$ Inhibitory Assay and In vitro Sucrase Inhibitory Assay was performed with respect to Chaturmukha rasa. The IC50 value was calculated for all the above activity. Results: Streptozotocin with Acarbose showed significant decrease in blood glucose level whereas streptozotocin with Triphala kwatha showed more decrease in blood glucose level than Streptozotocin with Acarbose. The combination of Streptozotocin + Triphala kwatha + Chaturmukha rasa showed a significant decrease in blood glucose level on 21st day. In vitro $\acute{\alpha}$- Amylase Inhibitory Assay the Chaturmukha rasa showed IC50 value $495.94{\mu}l$ when compared with Acarbose $427.33{\mu}l$, respectively. In the ${\alpha}-Glucosidase$ Inhibitory Assay Chaturmukha rasa showed IC50 value $70.93{\mu}l$ when compared with Acarbose $102.28{\mu}l$, respectively. In vitro Sucrase Inhibitory Assay Chaturmukha rasa showed IC50 value $415.4{\mu}l$ when compared with Acarbose $371.43{\mu}l$, respectively. Conclusion: This study supports that Chaturmukha rasa may inhibit diabetes by inhibition of salivary amylase or alpha Glucosidase or sucrase. This may be the mechanism by which Chaturmukha rasa inhibits diabetes. Further this study supports the usage of Chaturmukha rasa for the management of diabetes.