Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: EC:3.2.1.20 (alpha-glucosidase)
 4,237 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Acarbose is known to inhibit glucoamylase, maltase and sucrase. Our aim was to test whether it would also inhibit glucosyltransferase (GTF), to determine the type of inhibition and to compare the inhibitor potency of acarbose with that of nojirimycin and deoxynojirimycin, two other glucosidase inhibitors. Enzyme inhibition was measured either by chemical assay or by incorporation of radioactivity into product. Acarbose effectively inhibited the synthesis of polysaccharide by GTF from strains of Streptococcus mutans and Streptococcus sanguis, but not by fructosyltransferase from Streptococcus salivarius. Acarbose and 1-deoxynojirimycin were more potent inhibitors of GTF than maltose, nojirimycin or various amino sugars. The mechanism of action of these compounds is consistent with competitive inhibition.
 ...
PMID:Inhibition by acarbose, nojirimycin and 1-deoxynojirimycin of glucosyltransferase produced by oral streptococci. 622 60

The syntheses of two ammonium salts of 1,4-dideoxy-1,4-imino-d-galactitol containing erythritol sulfate side chains are described. The parent compound is a known inhibitor of the enzyme UDP-galactopyranose mutase (UDP-galactopyranose furanomutase, E.C. 5.4.99.9), which is responsible for the conversion of UDP-galactopyranose into UDP-galactofuranose and is presumably protonated in its active form. The side chain was chosen because it is present in a known sulfonium ion alpha-glucosidase inhibitor, salacinol. The syntheses of the selenonium analogues derived from 1,4-dideoxy-1,4-seleno-d-galactitol are also described. The synthetic strategy in the syntheses of all four salts involved the nucleophilic attack of a protected derivative of the alditol at the least hindered carbon of 2,4-O-benzylidene d- or l-erythritol-1,3-cyclic sulfate to give adducts that were subsequently deprotected. The importance of different protecting groups used in the various syntheses is also highlighted. Enzyme inhibition assays carried out on these compounds, and the corresponding sulfonium ions synthesized previously, show that they are poor inhibitors of UDP-galactopyranose mutase.
 ...
PMID:Synthesis of novel ammonium and selenonium ions and their evaluation as inhibitors of UDP-galactopyranose mutase. 1533 48

A novel-immobilized enzyme strategy created by magnetic nanospheres for monitoring enzyme activity and screening inhibitors followed by high performance liquid chromatography (HPLC) has been demonstrated. Through the reaction of the aldehyde groups with amine groups, alpha-glycosidase was simply and stably immobilized onto magnetic nanospheres by the cross-linking agent glutaraldehyde. In order to profiling the activity of the immobilized alpha-glucosidase, the natural substrate was hydrolyzed by it and the yield of product was determined by HPLC. Compared with traditional bioassay approach, the prepared immobilized alpha-glucosidase displays a high activity and stability which allows it to be easily reused for 10 times. Enzyme inhibition assays by known inhibitor glucobay and three candidate traditional Chinese medicines (TCMs) were then investigated using a similar methodology. This assay was able to readily detect the change of the immobilized enzyme activity based on measuring a decrease of product formation using HPLC. The approach is general and offers many attractive advantages including easy product isolation, inexpensive cost, and high efficiency in terms of reagent consumption.
 ...
PMID:Development of high performance liquid chromatography with immobilized enzyme onto magnetic nanospheres for screening enzyme inhibitor. 1860 77

MeOH extracts of 37 herbs were tested in screening experiments for rat intestinal alpha-glucosidase. The MeOH extract of the aerial parts of Scutellaria lateriflora L. (Lamiaceae) significantly inhibited sucrase and maltase activities, using sucrose and maltase as the substrates. Enzyme inhibition guided-fractionation of the MeOH extract of S. lateriflora resulted in the isolation of a new diterpene glucoside, deacetylajugarin-IV 18-O-beta-D-glucopyranoside (1), along with 20 known phenolics (2-21). The structures of 1-21 were elucidated on the basis of MS and NMR data analyses. Baicalein (4) and baicalin (10), a glycoside of 4, showed moderate sucrase inhibitory activities at IC50 values of 14.9 and 36.3 microM, respectively, whereas luteolin (3), acteoside (16), leucosceptoside A (18), and isoacteoside (20) showed weak inhibitory activities at IC50 values of 811, 522, 727, and 443 microM, respectively. This is the first report on mammalian alpha-glucosidase inhibitory activities of S. lateriflora extract and identification of the constituents responsible for the activities. Apigenin (2), luteolin (3), 6-methoxyluteolin 4'-methyl ether (6), isoscutellarin 8-O-beta-D-glucuronide (7), luteolin 7-O-beta-D-glucuronide (9), wogonin 7-O-beta-D-glucuronide methyl ester (12), eriodictyol (13), naringenin (14), naringenin 7-O-beta-D-glucuronide (15), jionoside D (17), leucosceptoside A (18), and (+)-syringaresinol 4'-O-beta-D-glucopyranoside (21) were isolated from this plant for the first time. The inhibitory properties of S. lateriflora extract against alpha-glucosidase provide a prospect for its antidiabetic usage.
 ...
PMID:Chemical constituents of the aerial parts of Scutellaria lateriflora and their alpha-glucosidase inhibitory activities. 2257 44