Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts: Gene/Protein Disease Symptom Drug Enzyme Compound   Target Concepts: Gene/Protein Disease Symptom Drug Enzyme Compound

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Query: EC:3.2.1.20 (alpha-glucosidase)
4,237 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Several glycosides of calystegines B1 and B2 were synthesized by use of rice alpha-glucosidase and the whole cells of Rhodotorula lactosa, and their glycosidase inhibitory activities were investigated. Incubation of mixture of calystegine B1 and maltose with rice alpha-glucosidase gave 3-O-alpha-D-glucopyranosylcalystegine B1 (2, 11.3%). An enzymatic beta-transglucosylation reaction of calystegines B1 or B2 with cellobiose using the whole cells of R. lactosa gave 3-O-beta-D-glucopyranosylcalystegine B1 (1) (0.9%) or 4-O-beta-D-glucopyranosylcalystegine B2 (3, 11.2%), respectively, while similar beta-transgalactosylation of calystegine B2 from lactose gave 4-O-beta-D-galactopyranosylcalystegine B2 (4, 10.1%). The glycosylation of calystegines B1 and B2 markedly decreased or abolished their inhibition against beta-glucosidase, alpha- or beta-galactosidase. Compound 4 however retained more or less the potency of calystegine B2 against trehalase. Interestingly, compound 1 was a noncompetitive inhibitor of rice alpha-glucosidase, with a Ki value of 0.9 +/- 0.1 microM.
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PMID:Enzymatic synthesis of the glycosides of calystegines B1 and B2 and their glycosidase inhibitory activities. 944 68

Intestinal absorption of beta-disaccharide (cellobiose, maltose and lactose) conjugates of p-nitrophenol (p-nitrophenyl beta-disaccharide) were examined in terms of the hydrolysis of disaccharide conjugate to monosaccharide conjugate and the transport of monosaccharide conjugate by Na+/glucose transport carrier (SGLT1). beta-Cellobioside, beta-maltoside and beta-lactoside of p-nitrophenol (p-NP) were hydrolyzed to p-nitrophenyl beta-glucoside (p-NPbeta glc) on the mucosal side, and p-NPbeta glc appeared on the serosal side. Although p-NP beta-disaccharide, p-NP and p-NP glucuronide also appeared on the serosal side, their amounts were much lower than that of p-NPbeta glc. The amount of p-NPbeta glc transported to the serosal side was decreased in the presence of phloridzin (transport inhibitor of SGLT1) and in the absence of Na+ (a cosubstrate of SGLT1), indicating that p-NPbeta glc was formed from p-NP beta-disaccharide on the mucosal side and transported to the serosal side by SGLT1. Furthermore, the absorption clearance of p-NPbeta glc, which was formed from p-NP beta-cellobioside and p-NP beta-lactoside by lactase-phloridzin hydrolase (LPH), was much higher than that of p-NPbeta glc itself, although the absorption clearance of p-NPbeta glc, which was formed from p-NP beta-maltoside by maltase was similar to that of p-NPbeta glc itself. These results indicated that p-NPbeta glc was transported by the vectorial cooperation of SGLT1 with LPH from mucosal p-NP beta-cellobioside or p-NP beta-lactoside.
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PMID:Intestinal Na+/glucose cotransporter-mediated transport of glucose conjugate formed from disaccharide conjugate. 946 25

The hypoglycemic effect and the alpha-glucosidase activity inhibition of acarbose (AC:alpha-glucosidase inhibitor) were investigated in normal and KK-Ay mice, an animal model of noninsulin-dependent diabetes mellitus (NIDDM). AC improved hyperglycemia after an oral administration of maltose or sucrose, dose dependently in normal mice (1, 10, and 50mg/kg body weight) and in KK-Ay mice (50mg/kg). Furthermore, AC (50mg/kg) significantly inhibited maltase and sucrase activities in the small intestines of normal and KK-Ay mice (inhibitory efficacy: sucrase > maltase). The enzymatic inhibition in KK-Ay mice is stronger than in normal mice. However, AC (50 mg/kg) did not suppress the blood glucose in oral lactose tolerance and did not inhibit the lactase activity in either normal or KK-Ay mice. These findings indicate that the AC effect on the inhibition of alpha-glucosidase activity is selective for sucrase and maltase in normal and NIDDM mice.
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PMID:Effect of acarbose (alpha-glucosidase inhibitor) on disaccharase activity in small intestine in KK-Ay and ddY mice. 974 58

Diarrhoea is a relatively frequent adverse event, accounting for about 7% of all drug adverse effects. More than 700 drugs have been implicated in causing diarrhoea; those most frequently involved are antimicrobials, laxatives, magnesium-containing antacids, lactose- or sorbitol-containing products, nonsteroidal anti-inflammatory drugs, prostaglandins, colchicine, antineoplastics, antiarrhythmic drugs and cholinergic agents. Certain new drugs are likely to induce diarrhoea because of their pharmacodynamic properties; examples include anthraquinone-related agents, alpha-glucosidase inhibitors, lipase inhibitors and cholinesterase inhibitors. Antimicrobials are responsible for 25% of drug-induced diarrhoea. The disease spectrum of antimicrobial-associated diarrhoea ranges from benign diarrhoea to pseudomembranous colitis. Several pathophysiological mechanisms are involved in drug-induced diarrhoea: osmotic diarrhoea, secretory diarrhoea, shortened transit time, exudative diarrhoea and protein-losing enteropathy, and malabsorption or maldigestion of fat and carbohydrates. Often 2 or more mechanisms are present simultaneously. In clinical practice, 2 major types of diarrhoea are seen: acute diarrhoea, which usually appears during the first few days of treatment, and chronic diarrhoea, lasting more than 3 or 4 weeks and which can appear a long time after the start of drug therapy. Both can be severe and poorly tolerated. In a patient presenting with diarrhoea, the medical history is very important, especially the drug history, as it can suggest a diagnosis of drug-induced diarrhoea and thereby avoid multiple diagnostic tests. The clinical examination should cover severity criteria such as fever, rectal emission of blood and mucus, dehydration and bodyweight loss. Establishing a relationship between drug consumption and diarrhoea or colitis can be difficult when the time elapsed between the start of the drug and the onset of symptoms is long, sometimes up to several months or years.
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PMID:Drug-induced diarrhoea. 1064 76

The potential of Lactobacillus rhamnosus R for producing exopolysaccharide (EPS) when grown on basal minimum medium supplemented with glucose or lactose was investigated. EPS production by L. rhamnosus R is partially growth associated and about 500 mg of EPS per liter was synthesized with both sugars. The product yield coefficient (Y(EPS/S)) was 3.15 (0.0315 g of EPS [g of lactose](-1)) and 2.88 (0.0288 g of EPS [g of glucose](-1)). It was clearly shown that the amount of EPS produced declined upon prolonged fermentation. Degradation of EPS in fermentation processes was also assessed by measuring its molecular weights and viscosities. As these reductions might have a negative effect on the yield and viscosifying properties of EPS, it was essential to examine possible causes related to this breakdown. The decrease in viscosities and molecular weights of EPS withdrawn at different cultivation times permitted us to suspect the presence of a depolymerizing enzyme in the fermentation medium. Our study on enzymatic production profiles showed a large spectrum of glycohydrolases (alpha-D-glucosidase, beta-D-glucosidase, alpha-D-galactosidase, beta-D-galactosidase, beta-D-glucuronidase, and some traces of alpha-L-rhamnosidase). These enzymes were localized, two of them (alpha-D-glucosidase and beta-D-glucuronidase) were partially purified and characterized. When incubated with EPS, these enzymes were capable of lowering the viscosity of the polymer as well as liberating some reducing sugars. Upon prolonged incubation (27 h), the loss of viscosity was increased up to 33%.
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PMID:Production of exopolysaccharide by Lactobacillus rhamnosus R and analysis of its enzymatic degradation during prolonged fermentation. 1083 3

We have studied the uptake of maltose in the thermoacidophilic gram-positive bacterium Alicyclobacillus acidocaldarius, which grows best at 57 degrees C and pH 3.5. Under these conditions, accumulation of [(14)C]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. Uptake of radiolabeled maltose was inhibited by maltotetraose, acarbose, and cyclodextrins but not by lactose, sucrose, or trehalose. The kinetic parameters (K(m) of 0.91 +/- 0.06 microM and V(max) ranging from 0.6 to 3.7 nmol/min/mg of protein) are consistent with a binding protein-dependent ATP binding cassette (ABC) transporter. A corresponding binding protein (MalE) that interacts with maltose with high affinity (K(d) of 1.5 microM) was purified from the culture supernatant of maltose-grown cells. Immunoelectron microscopy revealed distribution of the protein throughout the cell wall. The malE gene was cloned and sequenced. Five additional open reading frames, encoding components of a maltose transport system (MalF and MalG), a putative transcriptional regulator (MalR), a cyclodextrinase (CdaA), and an alpha-glucosidase (GlcA), were identified downstream of malE. The malE gene lacking the DNA sequence that encodes the signal sequence was expressed in Escherichia coli. The purified wild-type and recombinant proteins bind maltose with high affinity over a wide pH range (2.5 to 7) and up to 80 degrees C. Recombinant MalE cross-reacted with an antiserum raised against the wild-type protein, thereby indicating that the latter is the product of the malE gene. The MalE protein might be well suited as a model to study tolerance of proteins to low pH.
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PMID:Maltose and maltodextrin transport in the thermoacidophilic gram-positive bacterium Alicyclobacillus acidocaldarius is mediated by a high-affinity transport system that includes a maltose binding protein tolerant to low pH. 1105 72

A microfiltration (MF) membrane bioreactor was developed for an efficient production of a recombinant thermostable alpha-glucosidase (rSsGA) from Sulfolobus solfataricus MT-4. The aim of the membrane bioreactor was to improve the control of the concentration of key components in the growth of genetic engineered microorganisms, such as Escherichia coli. The influence of medium composition was studied in relation to cell growth and alpha-glucosidase production. The addition of components such as yeast extract and tryptone resulted in a higher enzyme production. High cell density cultivation of E. coli BL21(DE3) on semidefined medium, exploiting a microfiltration bioreactor, was studied in order to optimize rSsGA production. In addition to medium composition, the inducer employed (either isopropyl beta-D-thiogalactopyranoside or lactose), the induction duration, and the cultivation mode influenced both the final biomass and the enzyme yield. The MF bioreactor allowed a cell concentration of 50 g/L dry weight and a corresponding alpha-glucosidase production of 11,500 U/L. The improvement obtained in the enzyme production combining genetic engineering and the microfiltration strategy was estimated to be 2,000-fold the wild-type strain.
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PMID:Effective production of a thermostable alpha-glucosidase from Sulfolobus solfataricus in Escherichia coli exploiting a microfiltration bioreactor. 1106 36

Acarbose analogues, containing cellobiose and lactose structures, were prepared by reaction of the two disaccharides with acarbose and Bacillus stearothermophilus maltogenic amylase. The kinetics for the inhibition by the two analogues was studied for beta-glucosidase, beta-galactosidase, cyclomaltodextrin glucanosyltransferase (CGTase), and alpha-glucosidase. Both analogues were potent competitive inhibitors for beta-glucosidase, with K(I) values in the range of 0.04-2.44 microM, and the lactose analogues were good uncompetitive inhibitors for beta-galactosidase, with K(I) values in the range of 159-415 microM, while acarbose was not an inhibitor for either enzyme at 10 and 5 mM, respectively. Both analogues were also potent mixed inhibitors for CGTase, with K(I) values in the range of 0.1-9.3 microM. The lactose analogue was a 6.4-fold better competitive inhibitor for alpha-glucosidase than was acarbose.
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PMID:Inhibition of beta-glycosidases by acarbose analogues containing cellobiose and lactose structures. 1128 1

Feeding manufactured liquid diets to early-weaned pigs improves growth performance and reduces days to market weight compared with pigs receiving pelleted dry feed. Few alternative dietary ingredients are utilized in manufactured liquid diets other than byproducts of the dairy industry, especially for sources of carbohydrates. This experiment was designed to evaluate the efficacy of starch from partially hydrolyzed corn syrup solids (CSS), at two different levels of hydrolyzation, as a replacement for lactose in manufactured liquid diets. Forty-eight pigs were removed from sows at 1 d of age and randomly assigned to one of three treatments: 1) control with lactose as the carbohydrate source, 2) lactose replaced (gram for gram) with CSS (dextrose equivalent [DE]-20), and 3) lactose replaced with DE-42. In addition, 10 pigs were randomly removed from several litters to provide estimates of initial body composition and small intestinal variables. Twenty-four pigs were removed from the study on d 10 of treatment, and the remaining 24 pigs were removed on d 20 of treatment. Pigs averaged 9,845 +/- 191 g at d 20 of treatment regardless of dietary treatment (P > 0.20). No differences in ADG, ADFI, or feed efficiency were detected between treatment groups from d 0 to 20 (P > 0.19). Whole-body water, protein, lipid, and ash accretion rates were unaffected by dietary treatment from d 0 to 10 or from d 0 to 20 (P > 0.20). The replacement of lactose with CSS did not affect intestinal villi height or width, or crypt depth (P > 0.10). Pigs fed lactose tended to have greater lactase activity on d 10 than pigs fed CSS (P < 0.07). Also, pigs fed lactose tended to have lower oligosaccharidase activity than pigs fed the DE-20 diet on d 20 (P < 0.07). No other differences in lactase, maltase, or long oligosaccharidase specific activity on d 10 or 20 of treatment were detected (P > 0.12). Plasma urea nitrogen concentrations were unaffected by diet on d 10 and 20 of treatment. In addition, dry matter digestibility of the diets averaged approximately 85.6 +/- 0.8% and was unaffected by dietary treatment or day of treatment. These results suggest that partially hydrolyzed CSS can be used as a replacement for lactose in manufactured liquid diets for neonatal pigs.
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PMID:Efficacy of partially hydrolyzed corn syrup solids as a replacement for lactose in manufactured liquid diets for neonatal pigs. 1183 12

The effect of source of carbohydrate on gut histology, digestion efficiency, and growth performance in early-weaned (25 d) rabbits at the starter period (25 to 39 d) was investigated. Six diets were factorially arranged to study the effect of partial substitution of starch (0, 25, or 50%) by lactose at two levels of fiber (30 or 36% NDF). Diets were formulated to meet or exceed essential nutrient requirements of growing rabbits. A feeding trial was conducted to measure the effect of treatments on growth performance in 252 rabbits that were fed the experimental diets in the starter period and thereafter received a common feed until 60 d of age. Fecal apparent digestibility was determined at 35 d of age in nine animals per diet. The four diets with extreme lactose content were used to determine ileal apparent digestibility of starch and lactose (nine replicates per diet), weights of stomach and cecum, stomach pH, cecal fermentation traits, amylase and disaccharidase activities (10 animals per diet), and jejunal morphology (six animals per diet). Weaning increased (P < 0.001) amylase activity by 59% but decreased (P < 0.001) maltase, sucrase, and lactase activities by 30, 48, and 72%, in parallel with a reduction of villus height by 19%. Dietary NDF level did not affect either jejunal morphology or sucrase and lactase activities but increased amylase (P = 0.05) and maltase (P < 0.001) activities by 22 and 92%, respectively. Substitution of starch by lactose had no effect on jejunal morphology or enzymatic activity. Ileal lactose and starch digestibility were not affected by dietary NDF or lactose level and averaged 73.8 and 90.8%, respectively. Substitution of starch by fiber and lactose affected ileal flux of starch plus lactose (by -0.5 and +1.7 g/d) and cecal pH (by +2.1 and -2.8%, respectively). Fecal NDF digestibility was relatively low (23.1% on average) and was not affected by treatments, whereas that of lactose and starch was almost complete. An increase of dietary NDF level led to an impairment of ADG and feed efficiency in the starter (P < 0.002) and in the overall (P < 0.03) fattening period. Substitution of starch by lactose linearly decreased (P < 0.001) feed efficiency in the starter period and linearly increased (P < 0.001) diarrhea incidence in the fattening period. The results indicate that digestive capability of early-weaned rabbits is limited and should be taken into account to establish optimal levels and sources of carbohydrates in the starter diet.
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PMID:Effect of levels of starch, fiber, and lactose on digestion and growth performance of early-weaned rabbits. 1200 9


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