The Objectives of the Study is to Evaluate the Efficacy and Safety of Acarmet (Metformin HCl 500 mg; Plus Acarbose 50 mg Tablets) Thrice Daily Versus Acarbose 50 mg Thrice Daily Over 16 Weeks in; Subjects With Type 2 Diabetes Mellitus.

... Acarus siro L. is sensitive to the α-amylase inhibitor of bacterial origin acarbose, which reduced the ... a synergism between the effects of the α-amylase inhibitor acarbose and the predatory mite Cheyle...

... In fact, the acarbose ANDA that included a PD study was the first to be filed, by Cobalt Laboratories in January 2005. Third, it ...

Alpha-glucosidase inhibitors (such as acarbose) decrease the absorption of carbohydrates from the digestive tract, thereby lowering the after- ...

Coronary Heart Disease; Acute Coronary Syndrome; Impaired Glucose Tolerance; Diabetes Mellitus, Non-Insulin-Dependent

except glucose. Maltose transport of acarbose-grown cells was inhibited by sucrose and trehalose and, glycerol or maltose. These results suggest that an acarbose-insensitive maltose/sucrose/trehalose that accepts maltose/sucrose/trehalose and is moderately sensitive to acarbose is found in cells grown

Acarbose is an alpha-glucosidase inhibitor which reversibly and competitively inhibits the digestion of oligo- and disaccharides at the brush border of the small intestine. This study evaluates the preventive and therapeutic properties of acarbose in the treatment of obesity. Dose-response experiments were performed during repeated sucrose loads in man in ...

Fifty-gram carbohydrate tolerance tests were performed on healthy volunteers to test the activity and specificity of an alpha-glucoside hydrolase inhibitor, acarbose (BAY g 5421). Two hundred milligrams acarbose reduced the area under the blood glucose response curve by 89% (P less than 0.001) after sucrose by 80% (P less than 0.002) after starch, by 19% ...

Acarbose is an alpha-glucosidase inhibitor acting specifically at the level of postprandial glucose excursion. This compound lowers HbA(1c) by 0.5-1% in patients with Type 2 diabetes, either drug naive or in combination with other antidiabetic drugs. In those with impaired glucose tolerance (IGT), it reduces the incidence of newly diagnosed diabetes by 36.4%. Furthermore, it ...

The prevalence of glucose intolerance is increasing dramatically worldwide. Both impaired glucose tolerance (IGT) and type 2 diabetes are associated with excess mortality from cardiovascular disease. It is now generally accepted that these cardiovascular complications are related to prevailing hyperglycemia, particularly postprandial hyperglycemia. Acarbose specifically ...

The alpha-glucosidase inhibitor acarbose is administered to control blood glucose levels in type 2 diabetic patients and, in several countries, in those with impaired glucose tolerance. The efficacy and safety of the drug has been well established in these patient populations. Acarbose shows no weakening of efficacy in long-term diabetes treatment, reduces ...

... forfeiture of 180-day generic-drug exclusivity for acarbose under Title XI of the MEDICARE PRESCRIPTION DRUG,IMPROVEMENT, AND MODERNIZATION ACT OF 2003 (MMA). ...

to take. Be sure to mention any of the following: acarbose (Prandase, Precose); anticoagulants ('blood thinners') such as warfarin (Coumadin, Jantoven); antifungals such as...

A monocentric, open, randomised, single-dose, six-period crossover trial was carried out in healthy volunteers under fasting conditions to establish the most appropriate study design for a pivotal bioequivalence trial with acarbose (CAS 56180-94-0) regarding a) dosage of the drug, b) type of carbohydrate load, c) type of primary endpoint, and d) sample size. 50 g sucrose or 50 ...

So far little is known about how the antidiabetic drugs acting at the level of gastrointestinal mucosa may affect immune and cellular response to food intake. The following study investigated the association between acarbose treatment and postprandial metabolism, immune- and inflammatory activity in patients with early type 2 diabetes: The Acarbose action ...

... dissolution method should be conducted on 12 tablets each of ... dose tested should be the RLD 1*25mg tablet. ... a baseline for serum glucose in the following manner: ...

... chronic liver disease. Methotrexate and acarbose have been reported to increase liver toxicity in diabetes. A large prospective ...

The absorption, disposition, metabolism, and excretion of acarbose (O-4,6-dideoxy-4-[[(1S, 4R, 5S, 6S)-4,5,6-trihydroxy-3- (hydroxymethyl)-2- cyclohexen-1-yl]amino]-a-D-glucopyranosyl- (1----4)-O-a-D-glucopyranosyl- (1----4) -D-glucopyranose, Bay g 5421) have been studied following a single administration of the 14C-labelled compound to rats and dogs via different routes ...

BackgroundPostprandial hyperglycemia is believed to affect vascular endothelial function. The aim of our study was to compare the effects of acarbose and nateglinide on postprandial endothelial dysfunction.MethodsWe recruited a total of 30 patients with newly diagnosed type 2 diabetes (19 men and 11 women, age 67.8 � 7.3 years). Patients were randomly assigned to 3 groups ...

Contents: Synthesis of pseudo-oligosaccharidic alpha-amylase inhibitors - acarbose and adiposin-2; Development of inductively coupled plasma mass spectrometry with a water-cooled torch; Behavior of d-transition metal carbides in reaction sintering of diam...

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The inhibitory activity on intestinal ?-glucosidase by cyanidin-3-rutinoside was examined in vitro and in vivo. The IC(50) values of cyanidin-3-rutinoside against intestinal maltase, and sucrase were 2,323���14.8 and 250.2���8.1��M, respectively. The kinetic analysis revealed that intestinal sucrase was inhibited by cyanidin-3-rutinoside in a mixed-type manner. The synergistic ...

The inhibitory activity on intestinal ?-glucosidase by cyanidin-3-rutinoside was examined in vitro and in vivo. The IC₅₀ values of cyanidin-3-rutinoside against intestinal maltase, and sucrase were 2,323���14.8 and 250.2���8.1��M, respectively. The kinetic analysis revealed that intestinal sucrase was inhibited by cyanidin-3-rutinoside in a mixed-type manner. ...

vision If high blood sugar is not treated, a serious, life-threatening condition called diabetic ketoacidosis could develop. Call your doctor immediately if you have any of the...

Postprandial hypotension (PPH) is defined as a decrease of systolic blood pressure by more than 20 mmHg after meals. Severe PPH is a troublesome diabetic complication, which has no established means of treatment. We encountered a patient who had diabetes mellitus complicated by severe PPH and attempted to treat this problem using several medications (octreotide, midodrine hydrochloride, and ...

An extracellular enzyme activity in the culture supernatant of the acarbose producer Actinoplanes sp. strain SE50 catalyzes the transfer of the acarviosyl moiety of acarbose to malto-oligosaccharides. This acarviosyl transferase (ATase) is encoded by a gene, acbD, in the putative biosynthetic gene cluster for the ?-glucosidase inhibitor ...

This study was performed to observe the effects of acarbose and Rumex patientia on morphological change of pancreatic B cells in streptozotocin (STZ)-induced diabetic (type 2) rats. Two-day-old Wistar albino rats were intraperitoneally injected with 100mg/kg of STZ or vehicle alone for control. Vehicle and STZ given rats were divided into six groups (1st, 2nd and the 3rd ...

The objective of this study was to investigate the hypoglycemic effects of quercetin (QE) in animal models of diabetes mellitus (DM). A starch solution (1 g/kg) with and without QE (100 mg/kg) or acarbose (40 mg/kg) was orally administered to streptozotocin (STZ)-induced diabetic rats after an overnight fast. Postprandial plasma glucose levels were measured and incremental ...

The objective of this study was to investigate the hypoglycemic effects of quercetin (QE) in animal models of diabetes mellitus (DM). A starch solution (1 g/kg) with and without QE (100 mg/kg) or acarbose (40 mg/kg) was orally administered to streptozotocin (STZ)-induced diabetic rats after an overnight fast. Postprandial plasma glucose levels were measured and incremental ...

A maltogenic amylase gene was cloned in Escherichia coli from a gram-negative thermophilic bacterium, Thermus strain IM6501. The gene encoded an enzyme (ThMA) with a molecular mass of 68 kDa which was expressed by the expression vector p6xHis119. The optimal temperature of ThMA was 60�C, which was higher than those of other maltogenic amylases reported so far. Thermal inactivation kinetic ...

The X-ray structures of complexes of Thermoactinomyces vulgaris R-47 alpha-amylase 1 (TVAI) with an inhibitor acarbose and an inactive mutant TVAI with malto-hexaose and malto-tridecaose have been determined at 2.6, 2.0 and 1.8A resolution, and the structures have been refined to R-factors of 0.185 (R(free)=0.225), 0.184 (0.217) and 0.164 (0.200), respectively, with good ...

A simple and rapid CZE method was established for the simultaneous determination of valienamine, acarbose and validamycin A, using a 20-kV CZE with the detection wavelength of 193 nm and 50 mM phosphoric acid-20 mM Tris (pH 5.3) as a running buffer. The calibration curves of valienamine, acarbose, and validamycin A showed a good linear relationship at a ...

Polyphenol-rich extracts from a range of berries inhibited ?-amylase in vitro, but the most effective were from raspberry and rowanberry (IC50 values of 21.0 and 4.5 ?g/mL, respectively). The inhibitory components were examined by different approaches. Extracts from yellow and red raspberries were equally able to inhibit ?-amylase. Because the yellow raspberry extracts effectively lacked ...

A high-throughput method for rapid determination of starch hydrolase inhibition was developed using a 96-well microplate UV-vis reader to monitor the turbidity decrease over time. The area under the curve of turbidity measured over time was used to quantify the inhibitory effect of polyphenolic compounds on porcine pancreatic amylase, rat intestine ?-glucosidase, and fungal amyloglucosidase. ...

Phosphorylase kinase (PhK), an (alphabetagammadelta)(4) complex, stimulates energy production from glycogen in the cascade activation of glycogenolysis. Its large homologous alpha and beta subunits regulate the activity of the catalytic gamma subunit and account for 81% of PhK's mass. Both subunits are thought to be multidomain structures, and recent predictions based on their sequences suggest ...

The influence of metronidazole on the breath hydrogen response and symptoms of sucrose malabsorption was investigated in a double-blind, randomized and controlled study. Carbohydrate malabsorption was induced by the competitive alpha-glucosidase inhibitor, acarbose. Metronidazole reduced flatulence and the breath hydrogen response during sucrose malabsorption without a change ...

of terminally modified maltodextrins and cyclodextrins (Figure 1A). The sequence of the five-domain R observed activities on cyclodex- trins, terminally modified linear maltodextrins, and amylose, certainly

The aim of this study was to investigate the effects of acarbose and Rumex patientia on liver ultrastructure in streptozotocin (STZ)-induced diabetic (type II) rats. Forty-two-day-old, neonatal Wistar albino rats were used. They were divided into six groups. STZ was injected into groups 4, 5 and 6 on postnatal day 2. Groups 1 and 5 received water, groups 2 and 6 received 2% ...

1. The aim of the present study was to compare the effects of glipizide controlled-release (CR) tablets monotherapy with that of glipizide CR tablets plus acarbose on glycaemic variability in newly diagnosed Type 2 diabetes (T2DM) patients using a continuous glucose-monitoring system (CGMS). 2. Forty newly diagnosed T2DM patients whose glycated haemoglobin A1c (HbA1c) levels ...

Hepatic encephalopathy (HE) is caused by liver impairment and has a multitude of symptoms in affected patients, including change in level of consciousness, intellectual function, and neuromuscular function. Pharmacologic therapy includes use of nonabsorbable disaccharides (lactulose and lactitol), and antibiotics such as neomycin, paromycin, metronidazole, and rifaximin. Probiotics, ...

The gene valC encoding an enzyme homologous to the 2-epi-5-epi-valiolone kinase (AcbM) of the acarbose biosynthetic pathway was identified in the validamycin A biosynthetic gene cluster. Inactivation of valC resulted in mutants that lack the ability to produce validamycin A. Complementation experiments with a replicating plasmid harboring full-length valC restored the ...

A series of ?-glucosidase inhibitors with the oleanolic acid core and different cinnamic amide ligands were designed and synthesized. Their preliminary structure-activity relationships were analyzed. In general, the compounds with 3,28-disubstituted oleanolic acid exhibited stronger activity than those 28-monosubstituted analogues, and variation of cinnamic amide substitution significantly ...

Non-insulin-dependent diabetes mellitus (NIDDM) is a metabolic disease that is common in the elderly, and is characterised by insulin insufficiency and resistance. Measures such as bodyweight reduction and exercise improve the metabolic defects, but pharmacological therapy is the most frequently used and successful therapy. The sulphonylureas stimulate insulin secretion. Metformin and troglitazone ...

A potent natural alpha-glucosidase inhibitor called kotalanol has been isolated from an antidiabetic traditional Ayurvedic medicine, the roots and stems of Salacia reticulata Wight, through bioassay-guided separation. The structure of kotalanol was elucidated on the basis of chemical and physicochemical evidence to be the inner salt comprised of 1-deoxyheptosyl-3-sulfate anion and ...

Studies were carried out to determine if bile acid absorption is perturbed by the intestinal sucrase inhibitors, Acarbose and BAY m 1099 (1,5-dideoxy-1.5((2-hydroxy-ethyl) imino-)-D-glucitol). The intestinal absorption of taurocholic acid (TA) in male Wistar rats, anesthetized with pentobarbital (50mg/ig, i.p.), was assessed from its excretion rate in bile. In acute studies, ...

We found alpha-glucosidase inhibitory effect of Zn(II) complex with 6-methyl-2-picolinmethylamide (6mpa-ma) which showed the highest blood glucose lowering effect in Zn(II) complexes with picolinamide derivatives in KK-A(y) mice. The Zn(II) complex showed strong alpha-glucosidase inhibitory activity greater by about eighty times (substrate: maltose) and forty times (substrate: sucrose) compared ...

Tight control of blood glucose is the most important strategy for the treatment of diabetes mellitus. Here, we investigated the beneficial effects of Welsh onion on fasting and postprandial hyperglycemia. Inhibitory activities of hot water extracts from the green stalk and white bulb, which are the edible portions of the Welsh onion, and the fibrous root extract against yeast ?-glucosidase were ...

Tight control of blood glucose is the most important strategy for the treatment of diabetes mellitus. Here, we investigated the beneficial effects of Welsh onion on fasting and postprandial hyperglycemia. Inhibitory activities of hot water extracts from the green stalk and white bulb, which are the edible portions of the Welsh onion, and the fibrous root extract against yeast ?-glucosidase were ...

The dumping syndrome consists of early postprandial abdominal and vasomotor symptoms, resulting from osmotic fluid shifts and release of vasoactive neurotransmitters, and late symptoms secondary to reactive hypoglycemia. Effective relief of symptoms of dumping syndrome can be achieved with dietary modifications to minimize ingestion of simple carbohydrates and to exclude fluid intake during ...

The putative biosynthetic gene cluster for the alpha-glucosidase inhibitor acarbose was identified in the producer Actinoplanes sp. 50/110 by cloning a DNA segment containing the conserved gene for dTDP-D-glucose 4,6-dehydratase, acbB. The two flanking genes were acbA (dTDP-D-glucose synthase) and acbC, encoding a protein with significant similarity to 3-dehydroquinate ...

alpha-Amylases are widely occurring, multidomain proteins with a catalytic (beta/alpha)8-barrel. In barley alpha-amylase, insight into the catalytic mechanism is gained from the X-ray crystal structure of its molecular complex with acarbose, a pseudotetrasaccharide that acts like a transition-state analogue and which is shown to bind at two specific regions of the enzyme. The ...

Cyanidin and its glycosides are naturally dietary pigments which have been indicated as promising candidates to have potential benefits to humans, especially in the prevention and treatment of diabetes mellitus. We investigated the structure activity relationships of cyanidin and its glycosides to inhibit intestinal ?-glucosidases and pancreatic ?-amylase in vitro. The results found that cyanidin ...

Inhibition of intestinal alpha glucosidase plays a major role in preventing rise in postprandial glucose level in diabetics. Cymbopogon martinii (CM) (family Poaceae) is used in traditional Indian medicine in treatment of diabetes mellitus. The alpha glucosidase inhibitory action of the plant is studied. The active component was separated using hot water extraction of the whole plant powder, ...

Inhibition of intestinal alpha glucosidase plays a major role in preventing rise in postprandial glucose level in diabetics. Cymbopogon martinii (CM) (family Poaceae) is used in traditional Indian medicine in treatment of diabetes mellitus. The alpha glucosidase inhibitory action of the plant is studied. The active component was separated using hot water extraction of the whole plant powder, ...

Three flavonoids from tartary buckwheat bran, namely, quercetin (Que), isoquercetin (Iso) and rutin (Rut), have been evaluated as alpha-glucosidase inhibitors by fluorescence spectroscopy and enzymatic kinetics and have also been compared with the market diabetes healer, acarbose. The results indicated that Que, Iso and Rut could bind alpha-glucosidase to form a new complex, ...

Non-insulin-dependent diabetes mellitus is a metabolic disease that is common and is characterized by insulin insufficiency and resistance. Measures such as body weight reduction and exercise improve the metabolic defects, but pharmacological therapy is the most frequently used and successful therapy. The sulphonylureas stimulate insulin secretion. Metformin and troglitazone increase disposal and ...

A rigorous method for the least-squares nonlinear regression analysis of displacement isothermal titration calorimetric data is presented. The method can fit the binding isotherm of a ligand which is competitively inhibited in its binding by another bound ligand to a molecule with n identical and independent binding sites. There are no other assumptions for the method and no approximations. ...

Lupine is a medicinal food plant with potential value in the management of diabetes. In white mice, extracts of seeds of the white lupine [Lupinus albus (L. termis L.)] were associated with increased tolerance to an oral glucose bolus. Antihyperglycemic activity was present in extracts of the whole seed but not extracts of the seed coat, and was not detected when glucose was administered ...

An HPLC-UV method has been developed for the determination of valibose, miglitol, voglibose and acarbose, the four anti-diabetic drugs. The separation was accomplished successfully by using reversed phase chromatography (Prevail carbohydrate column, 250 mm x 4.6 mm, 5 microm) with a gradient acetonitrile-phosphate buffer solution (pH 8.0) at a wavelength of 210 nm. ...

The active fraction extracted from dragon's blood displayed an inhibitory effect on alpha-glucosidase activity with an IC50 of 0.152 microg/mL, which is nearly half of the crude material. Its inhibition on alpha-glucosidase was noncompetitive. In addition, when this fraction was orally administered to mice dosed with Acarbose (20 mg/kg), the active fraction (100, 300, 500 ...

Quercetin, kaempferol and to a lesser extent rutin have been reported to have antidiabetic activities when assessed by various assay models including in vitro alpha-glucosidase inhibition studies. A related structural analogue, kaempferol-3-O-rutinoside (KR) however has not yet been studied for such biological effects. It was found that KR is a potent inhibitor of alpha-glucosidase in vitro with ...

A novel amino-oligosaccharide, named SF638-1, was isolated from the culture filtrate of the Streptomyces strain PW638. Its chemical structure was determined by electrospray ionization tandem mass spectrometry (ESI-MS/MS) and two-dimensional nuclear magnetic resonance spectroscopy. The novel compound was a mixed inhibitor of human pancreatic ?-amylase, with a K(i) value in the same order of ...

Microbial conversion of unsaturated fatty acids often leads to special changes in their product structures and in biological potential. In our continuous effort to screen natural products for their antimicrobial and enzyme inhibitor activities, we found that 10-hydroxy-8(E)-octadecenoic acid (HOD) exhibited strong anti-alpha-glucosidase (EC 3.2.1.20) activity. HOD is an intermediate in the ...

In the course of searching for new classes of ?-glucosidase inhibitors originated from natural resources, 11 kinds of isoflavones, i.e., medicarpin (1), formononetin (2), mucronulatol (3), (3R)-calussequinone (5), (3R)-5'-methoxyvestitol (6), tectorigenin (7), biochanin A (8), tuberosin (9), calycosin (10), daidzein (11), and genistein (12), as well as a flavone, liquritigenin (4), were isolated ...

OBJECTIVE To investigate whether the dipeptidyl peptidase-4 inhibitor vildagliptin improves endothelium-dependent vasodilatation in patients with type 2 diabetes. RESEARCH DESIGN AND METHODS Sixteen subjects with type 2 diabetes (age 59.8 � 6.8 years, BMI 29.1 � 4.8 kg/m(2), HbA(1c) 6.97 � 0.61) on oral blood glucose lowering treatment were included. Participants received vildagliptin 50 mg ...

Human pancreatic ?-amylase (HPA) catalyzes the hydrolysis of ?-d-(1,4) glycosidic linkages in starch and is one of the major therapeutic targets for type II diabetes. Several acarviostatins isolated from Streptomyces coelicoflavus var. nankaiensis previously showed more potent inhibition of HPA than acarbose, which has been successfully used in clinical therapy. However, the ...

A glucodextranase (iGDase) from Arthrobacter globiformis I42 hydrolyzes alpha-1,6-glucosidic linkages of dextran from the non-reducing end to produce beta-D-glucose via an inverting reaction mechanism and classified into the glycoside hydrolase family 15 (GH15). Here we cloned the iGDase gene and determined the crystal structures of iGDase of the unliganded form and the complex with ...

TreX is an archaeal glycogen-debranching enzyme that exists in two oligomeric states in solution, as a dimer and tetramer. Unlike its homologs, TreX from Sulfolobus solfataricus shows dual activities for alpha-1,4-transferase and alpha-1,6-glucosidase. To understand this bifunctional mechanism, we determined the crystal structure of TreX in complex with an acarbose ligand. The ...

Next generation pyrosequencing of high G+C content genomes still poses problems to automated sequencing and assembly processes which necessitates cost and time intensive manual work in order to finish such genomes completely. The sequencing of the high G+C actinomycete Actinoplanes sp. SE50/110 was performed with standard pyrosequencing technology (454 Life Sciences) and revealed a high number of ...

The extracellular amylolytic system of Filobasidium capsuligenum consisted of an ?-amylase (1,4-?-d-glucan glucanhydrolase, EC 3.2.1.1) and two forms of glucoamylase (1,4-?-d-glucan glucohydrolase, EC 3.2.1.3). The enzymes were purified by ammonium sulfate fractionation, repeated ion-exchange chromatography (DEAE-Sephadex A-50), and gel filtration (Sephadex G-25, Sephadex G-100 sf). ?-Amylase had ...

Inhibition of ?-glucosidase and pancreatic ?-amylase is one of the therapeutic approaches for delaying carbohydrate digestion, resulting in reduced postprandial glucose. The aim of this study was to evaluate the phytochemical analysis and the inhibitory effect of various cinnamon bark species against intestinal ?-glucosidase and pancreatic ?-amylase. The results showed that the content of total ...

The antihyperglycemic effect of the Antidiabetis herbal preparation ((Myrtilli folium (Vaccinium myrtillus L.), Taraxaci radix (Taraxacum officinale Web.), Cichorii radix (Cichorium intybus L.), Juniperi fructus (Juniperus communis L.), Centaurii herba (Centaurium umbellatum Gilib.), Phaseoli pericarpium (Phaseolus vulgaris), Millefollii herba (Achillea millefolium L.), Morii folium (Morus nigra ...

Solute receptors (binding proteins) are indispensable components of canonical ATP-binding cassette importers in prokaryotes. Here, we report on the characterization and crystal structures in the closed and open conformations of AcbH, the solute receptor of the putative carbohydrate transporter AcbFG which is encoded in the acarbose (acarviosyl-1,4-maltose) biosynthetic gene ...

Thermoactinomyces vulgaris R-47 alpha-amylase 2 (TVAII) has the unique ability to hydrolyze cyclodextrins (CDs), with various sized cavities, as well as starch. To understand the relationship between structure and substrate specificity, x-ray structures of a TVAII-acarbose complex and inactive mutant TVAII (D325N/D421N)/alpha-, beta- and gamma-CDs complexes were determined at ...

Metabolic syndrome is characterized by a group of risk factors (obesity, glucose metabolism disorders, dyslipidemia and hypertension) which appear to be caused by obesity related mechanisms of cellular metabolism and the systemic energy balance. A fibre poor diet rich in fat combined with lack of physical activity are important causative factors. A suitable change in diet combined with regular ...

SUMMARYType 2 diabetes mellitus (T2DM) affects more than 7% of adults in the US and leads to substantial personal and economic burden. In prediabetic states insulin secretion and action�potential targets of preventive interventions�are impaired. In trials lifestyle modification (i.e. weight loss and exercise) has proven effective in preventing incident T2DM in high-risk groups, although weight ...

The manumycin group of antibiotics, represented by manumycin (1), asukamycin (2), colabomycin, U-62,162, and U-56,407, contains as a central structural element a multifunctional m-C/sub 7/N unit. This moiety, consisting of a six-membered ring carrying one carbon and one nitrogen atom in a meta disposition, is ubiquitous in nature in a variety of forms. The m-C/sub 7/N unit is most commonly ...

In the present study, we report the study by a combination of electrophoretically mediated microanalysis method with a partial technique for screening alpha-glucosidase inhibitors from 21 traditional Chinese drugs. In the setup, substrates and enzymes were introduced into the capillary as distinct plugs, the electrophoretic conditions for enzyme reaction and separation of substrates and products ...

Mulberry (Morus alba L.) leaf extract (MLE) was investigated as a potent plant-derived ?-glucosidase inhibitor with low ?-amylase inhibitory activity. MLE was prepared by heating in an autoclave at 121 �C for 15 minutes, and its in vitro and in vivo antihyperglycemic activities were investigated. The adverse side effects of MLE were analyzed by measuring the weight and volume of the cecum, stool ...

Inhibition of intestinal ?-glucosidases and pancreatic ?-amylases is an approach to controlling blood glucose and serum insulin levels in individuals with Type II diabetes. The two human intestinal glucosidases are maltase-glucoamylase and sucrase-isomaltase. Each incorporates two family 31 glycoside hydrolases responsible for the final step of starch hydrolysis. Here we compare the inhibition ...

The entrocytes of the small intestine can only absorb monosaccharides such as glucose and fructose from our diet. The intestinal absorption of dietary carbohydrates such as maltose and sucrose is carried out by a group of ?-glucosidases. Inhibition of these enzymes can significantly decrease the postprandial increase of blood glucose level after a mixed carbohydrate diet. Therefore, the inhibitory ...

?-Glucosidase inhibitor has considerable potential as a diabetes mellitus type 2 drug because it prevents the digestion of carbohydrates. The search for the constituents reducing ?-glucosidase activity led to the finding of active compounds in the fruiting body of Ganoderma lucidum. The CHCl(3) extract of the fruiting body of G. lucidum was found to show inhibitory activity on ?-glucosidase in ...

Glycosylation often mediates important biological processes through the interaction of carbohydrates with complementary proteins. Most chemical tools for the functional analysis of glycans are highly dependent upon various linkage chemistries that involve the reducing terminus of carbohydrates. However, because of ring opening, the structural integrity of the reducing sugar ring (pyranose or ...

Genomic analysis of the hyperthermophilic archaeon Pyrococcus furiosus revealed the presence of an open reading frame (ORF PF1939) similar to the enzymes in glycoside hydrolase family 13. This amylolytic enzyme, designated PFTA (Pyrococcus furiosus thermostable amylase), was cloned and expressed in Escherichia coli. The recombinant PFTA was extremely thermostable, with an optimum temperature of ...

In this article we discuss the available data on the effects of combined therapy of ezetimibe with agents affecting lipid metabolism other than statins. We consider studies evaluating the effects of combined therapy of ezetimibe with bile acid sequestrants, fenofibrate, niacin, n-3 fatty acids, plant sterols, orlistat, metformin, acarbose and glitazones. Combination of ...

Polygonum sachalinensis is a widespread invasive plant in Europe. Chemical profiles of its different organs were studied by HPLC-UV-ESI/MS. Seven major constituents quercetin-3-O-beta-D-galactopyranoside, quercetin-3-O-arabinopyranoside, lapathoside D, N-trans-feruloyltyramine, lapathoside C, hydropiperoside, and vanicoside B were isolated and identified. The free radical-scavenging, ...

Diabetes is known as a multifactorial disease. The treatment of diabetes (Type II) is complicated due to the inherent patho-physiological factors related to this disease. One of the complications of diabetes is post-prandial hyperglycemia (PPHG). Glucosidase inhibitors, particularly alpha-amylase inhibitors are a class of compounds that helps in managing PPHG. Six ethno-botanically known plants ...

Diabetes is known as a multifactorial disease. The treatment of diabetes (Type II) is complicated due to the inherent patho-physiological factors related to this disease. One of the complications of diabetes is post-prandial hyperglycemia (PPHG). Glucosidase inhibitors, particularly ?-amylase inhibitors are a class of compounds that helps in managing PPHG. Six ethno-botanically known plants having ...

Amylomaltases are 4-?-glucanotransferases (EC 2.4.1.25) of glycoside hydrolase family 77 that transfer ?-1,4-linked glucans to another acceptor, which can be the 4-OH group of an ?-1,4-linked glucan or glucose. The amylomaltase-encoding gene (PAE1209) from the hyperthermophilic archaeon Pyrobaculum aerophilum IM2 was cloned and expressed in Escherichia coli, and the gene product (PyAMase) was ...

SUMMARYHuman salivary ?-amylase (HSAmy) has three distinct functions relevant to oral health: 1) hydrolysis of starch; 2) binding to hydroxyapatite; and 3) binding to bacteria (e.g. viridans streptococci). Although the active site of HSAmy for starch hydrolysis is well characterized, the regions responsible for the bacterial binding are yet to be defined. Since HSAmy possesses several secondary ...

Amylase inhibitors, also known as starch blockers, contain substances that prevent dietary starches from being absorbed by the body via inhibiting breakdown of complex sugars to simpler ones. In this sense, these materials are projected as having potential applications in diabetes control. In this context, we report on zinc oxide nanoparticles as possible alpha-amylase inhibitors. Zinc oxide ...

Management of severe insulin resistance (IR) is a major clinical challenge in many patients with obesity or lipodystrophy, and also in rarer patients with proven or suspected genetic defects in the insulin receptor or downstream signalling. The latter group can present at any time between birth and early adult life, with a variable clinical course broadly correlated with the severity of IR. ...

Context:The close link between type 2 diabetes and excess body weight highlights the need to consider the weight effects of different treatment regimens. We examine the impact of "weight-friendly" type 2 diabetes pharmacotherapies and suggest treatment strategies that mitigate weight gain.Evidence Acquisition:Evidence was identified via PubMed search by class and agent and in bibliographies of ...

Obesity is a global epidemic associated with significant morbidity and mortality in adults and ill health in children. A proven successful approach in weight management has been the disruption of nutrient digestion, with orlistat having been used to treat obesity for the last 10 years. Although orlistat-induced weight loss remains modest, it produces meaningful reductions in risk factors for ...

Type 2 diabetes mellitus is a public health problem of epidemic proportions and its prevalence is on the rise. The typical American born today has a one in three chance of developing type 2 diabetes. This diagnosis is associated with an adverse cardiovascular prognosis and is considered the risk equivalent of established coronary disease. Many risk factors, including the metabolic syndrome, have ...

Clostridium thermohydrosulfuricum mutant Z 21-109 produced intracellular thermostable pullulanase and glucoamylase activities. The glucoamylase activity was inactivated by treating C. thermohydrosulfuricum cells with 10% (v/v) propan-1-ol at 85 degrees C in the presence of 5 mM-CaCl2. Pullulanase activity was selectively solubilized from cells by treatment with detergent and lipase. The ...

Context: The Centers for Disease Control and Prevention estimates that there are approximately 79,000,000 individuals in the United States with prediabetes [impaired glucose tolerance (IGT) and/or impaired fasting glucose] and that approximately 40-50% will progress to type 2 diabetes mellitus (T2DM) during their lifetime. Therefore, treatment of high-risk IGT individuals to prevent T2DM has ...

Glycaemic control in Type 1 diabetes has been proven efficient in preventing microvascular and neurological complications. The assumption that good control of hyperglycaemia may also have significant impact on alleviation of complications in Type 2 diabetes has gained growing support in recent years. Measures such as body weight reduction and exercise improve the metabolic defects, but ...

Previous studies have revealed that rats consume substantial amounts of polysaccharide solutions, even if the solutions are made bitter with the addition of sucrose octa acetate (SOA). The present experiment used the gastric sham-feeding preparation to determine if it is the orosensory or postingestive properties of polysaccharides that motivate rats to consume polysaccharide (Polycose) solutions. ...

Fitness cost is usually associated with insecticide resistance and may be mitigated by increased energy accumulation and mobilization. Preliminary evidence in the maize weevil (Coleoptera: Curculionidae) suggested possible involvement of amylases in such phenomenon. Therefore, alpha-amylases were purified from an insecticide-susceptible and two insecticide-resistant strains (one with fitness cost ...

The metabolic syndrome (MetS) is strongly associated with insulin resistance and consists of a constellation of factors that raise the risk for cardiovascular diseases and diabetes mellitus. Therefore, the primary goals of treating MetS are prevention of type 2 diabetes and cardiovascular events. Three levels of intervention may be considered for individuals with MetS : 1) management of underlying ...

The midgut of the tobacco hornworm, Manduca sexta, actively secretes potassium ions. This can be measured as short-circuit current (I(sc)) with the midgut mounted in an Ussing chamber and superfused with a high-K(+) saline containing as its major osmolyte 166 mM sucrose. Iso-osmotic substitution of sucrose by non-metabolisable compounds (mannitol, urea, NaCl and the polyethylene glycols 200, 400 ...

We investigated the effects of divalent alkaline earth and first-row transition metal and zinc ions on ?-glucosidase activity in vitro and in vivo. CuSO? and ZnSO? exhibited a high ?-glucosidase inhibitory effect in vitro. The IC(50) values of CuSO? were 0.77 � 0.01 (substrate; maltose) and 0.78 � 0.01 (substrate; sucrose), and those of ZnSO? were 5.49 � 0.14 (substrate; maltose) and 4.70 ...

Inhibition of alpha-glucosidase is a therapeutic approach for diabetes. In this study, a method based on online liquid chromatography-diode array detection-tandem mass spectrometry and biochemical detection (LC-DAD-MS/MS-BCD) was developed to screen and identify alpha-glucosidase inhibitors from selected beverage extracts, including pu-erh tea ( Camellia sinensis var. assamica), eagle tea ( Litsea ...

Three mutations, Ser54?Pro, Thr314?Ala, and His415?Tyr, were identified in Aspergillus awamori glucoamylase gene expressed by Saccharomyces cerevisiae. The mutant glucoamylase (GA) was substantially more thermostable than a wild-type GA at 70��C, with a 3.0�KJ�mol(-1) increase in the free energy of thermo-inactivation. The effect of starch from different botanical sources on the production ...

Type I diabetes mellitus is a metabolic disease caused by chronic immune attack against the insulin-producing cells of the pancreas. It has recently been shown that the clinical course of this disease can be interrupted by immune ablation and PBSCT. In this report, we describe our experience with this treatment modality in a series of eight cases. Patients with newly diagnosed type I diabetes were ...

Objective:The objective of this study was to evaluate the ?-amylase inhibitory activity of different extracts of Phyllanthus amarus against porcine pancreatic amylase in vitro.Materials and Methods:The plant extracts were prepared sequentially with ethanol, chloroform, and hexane. Each extract was evaporated using rotary evaporator, under reduced pressure. Different concentrations (10, 20, 40, 60, ...

Ascophyllum nodosum is a brown seaweed that grows abundantly in the Northeast coastal region. In this study, the potential of A. nodosum for type 2 diabetes management through antioxidant-mediated alpha-glucosidase and alpha-amylase inhibition was investigated. After the initial screening of 4 locally harvested seaweeds, A. nodosum was chosen for its highest phenolic content and was subjected to ...

Postprandial hypoglycaemia is increasingly recognised as a complication of gastric bypass surgery. While post-bypass hypoglycaemia is often responsive to dietary modification, a subset of individuals develop life-threatening neuroglycopenia, with loss of consciousness, seizures and motor vehicle accidents. Such patients require complex nutritional and medical management strategies to reduce ...

A gene cluster responsible for the biosynthesis of validamycin, an aminocyclitol antibiotic widely used as a control agent for sheath blight disease of rice plants, was identified from Streptomyces hygroscopicus subsp. jinggangensis 5008 using heterologous probe acbC, a gene involved in the cyclization of D-sedoheptulose 7-phosphate to 2-epi-5-epi-valiolone of the acarbose ...

A gene cluster responsible for the biosynthesis of validamycin, an aminocyclitol antibiotic widely used as a control agent for sheath blight disease of rice plants, was identified from Streptomyces hygroscopicus subsp. jinggangensis 5008 using heterologous probe acbC, a gene involved in the cyclization of d-sedoheptulose 7-phosphate to 2-epi-5-epi-valiolone of the acarbose ...

Non-insulin-dependent diabetes mellitus (NIDDM, type 2 diabetes) is a heterogeneous disease resulting from a dynamic interaction between defects in insulin secretion and insulin action. There are various pharmacological approaches to improving glucose homeostasis, but those currently used in clinical practice either do not succeed in restoring normoglycaemia in most patients or fail after a ...

The berry fruits of highbush blueberry (Vaccinium corymbosum) contain bioactive compounds with potential health benefits. The objective was to evaluate blueberries grown in southern Illinois as well as the effect of fermentation, at two different temperatures, on chemical and physical parameters. Fruits from fifteen blueberry cultivars were analyzed. Fruit diameter ranged from 12.8 mm to 18.7 mm, ...

Glucansucrase (GSase) from Streptococcus mutans is an essential agent in dental caries pathogenesis. Here, we report the crystal structure of S. mutans glycosyltransferase (GTF-SI), which synthesizes soluble and insoluble glucans and is a glycoside hydrolase (GH) family 70 GSase in the free enzyme form and in complex with acarbose and maltose. Resolution of the GTF-SI ...

To clarify a postprandial glucose suppression effect of diacylated anthocyanin with alpha-glucosidase (AGH) inhibitory activity, a single oral administration study of it in male 8-week-old Sprague-Dawley rats was performed. The diacylated anthocyanin used in this study was peonidin 3-O-[2-O-(6-O-E-feruloyl-beta-D-glucopyranosyl)-6-O-E-caffeoyl-beta-D-glucopyranoside]-5-O-beta-D-glucopyranoside ...

A screening of 5 plants used for making drinks in Vietnam revealed a Cleistocalyx operculatus (Roxb.) Merr and Perry flower bud extract to have the highest inhibitory activity against the alpha-glucosidase enzyme. The anti-hyperglycemic effects of an aqueous extract from flower buds of Cleistocalyx operculatus (CO), a commonly used material for drink preparation in Vietnam, were therefore ...

The inhibitory activity from the isolated component of the fruiting body Phellinus merrillii (PM) was evaluated against ?-glucosidase and lens aldose reductase from Sprague-Dawley male rats and compared to the quercetin as an aldose reductase inhibitor and acarbose as an ?-glucosidase inhibitor. The ethanol extracts of PM (EPM) showed the strong ?-glucosidase and aldose ...

The increasing interest in click chemistry and its use to stabilize turn structures led us to compare the propensity for ?-turn stabilization of different analogs designed as mimics of the ?-turn structure found in tendamistat. The ?-turn conformation of linear ?-amino acid-containing peptides and triazole-cyclized analogs were compared to 'conventional' lactam- and disulfide-bridged hexapeptide ...

An extract from the roots of Ligusticum porteri, orally administered to groups of normal and diabetic mice, showed significant hypoglycemic and antihyperglycemic effects. Experimental type-II DM was achieved by treating mice with streptozotocin 15 min after an injection of ?-nicotinamide adenine dinucleotide. (Z)-6,6',7,3'?-diligustilide (1), (Z)-ligustilide (2), 3-(Z)-butylidenephthalide (3), ...

The prevalence of diabetes is increasing in epidemic proportion worldwide. Because of the morbidity and mortality associated with the disease, it is becoming a major burden for the health care system. With a better understanding of the pathogenesis of type 2 diabetes, the concept of primary prevention has emerged. A number of studies demonstrated that both lifestyle modification program and ...

We have studied the uptake of maltose in the thermoacidophilic gram-positive bacterium Alicyclobacillus acidocaldarius, which grows best at 57�C and pH 3.5. Under these conditions, accumulation of [¹⁴C]maltose was observed in cells grown with maltose but not in those grown with glucose. At lower temperatures or higher pH values, the transport rates substantially decreased. ...

Aims: To investigate the safety, tolerability, pharmacokinetics, and pharmacodynamics of LY2189265 (LY), a novel, long-acting GLP-1 analog, administered once-weekly to subjects with type 2 diabetes. Materials and Methods: This was a placebo-controlled, parallel-group, subject- and investigator-blind study of LY in subjects (N=43) with type-2 diabetes mellitus controlled with diet and exercise ...

BackgroundIndian medicinal plants used in the Ayurvedic traditional system to treat diabetes are a valuable source of novel anti-diabetic agents. Pancreatic ?-amylase inhibitors offer an effective strategy to lower the levels of post-prandial hyperglycemia via control of starch breakdown. In this study, seventeen Indian medicinal plants with known hypoglycemic properties were subjected to ...

Hepatic encephalopathy (HE) is a challenging clinical complication of liver dysfunction with a wide spectrum of neuropsychiatric abnormalities that range from mild disturbances in cognitive function and consciousness to coma and death. The pathogenesis of HE in cirrhosis is complex and multifactorial, but a key role is thought to be played by circulating gut-derived toxins of the nitrogenous ...

Diets high in calories and sweetened foods with disaccharides frequently lead to exaggerated postprandial spikes in blood glucose. This state induces immediate oxidant stress and free radicals which trigger oxidative stress-linked diabetic complications. One of the therapeutic approaches for decreasing postprandial hyperglycemia is to retard absorption of glucose by the inhibition of carbohydrate ...

Diets high in calories and sweetened foods with disaccharides frequently lead to exaggerated postprandial spikes in blood glucose. This state induces immediate oxidant stress and free radicals which trigger oxidative stress-linked diabetic complications. One of the therapeutic approaches for decreasing postprandial hyperglycemia is to retard absorption of glucose by the inhibition of carbohydrate ...

The debates continue over the validity of the metabolic syndrome concept. The continuous increment of the obesity pandemic is almost worldwide paralleled by rising rates of metabolic syndrome prevalence. Then, it seems obvious that these debates drove the need for further investigations as well as a deeper cooperation between relevant national and international organizations regarding the issue. ...

The debates continue over the validity of the metabolic syndrome concept. The continuous increment of the obesity pandemic is almost worldwide paralleled by rising rates of metabolic syndrome prevalence. Then, it seems obvious that these debates drove the need for further investigations as well as a deeper cooperation between relevant national and international organizations regarding the issue. ...

The development and progress of antidiabetic drugs (e.g., insulin preparations and hypoglycemic drugs) are retrospectively investigated in Japan. Their influences on the treatment of diabetes mellitus (DM) and its epidemiological aspects are also discussed. 1) Insulin preparations: Insulin was introduced for DM therapy in 1925, two or three years after its discovery in Canada. The preparations ...