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)

Glycosidases play a pivotal role in processing of various glycoproteins and glycolipids. It is well known that glycosidases are also involved in a variety of degenerative metabolic disorders such as cancer and AIDS. In order to develop potent alpha-glucosidase inhibitors, we first screened 2,2-diphenyl-1-picrylhydrazyl hydrate as a candidate. 2,2-Diphenyl-1-picrylhydrazyl hydrate was found to inhibit alpha- and beta-glucosidases as well as alpha- and beta-mannosidases. It was also shown to be a non-competitive inhibitor of yeast alpha-glucosidase with a Ki value of 1.1 x 10(-6) M. Taken together, we anticipate that 2,2-diphenyl-1-picrylhydrazyl hydrate may be a potent inhibitor for some incurable metabolic disorders including AIDS.
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PMID:2,2-Diphenyl-1-picrylhydrazyl hydrate, a stable free radical, is an alpha-glucosidase inhibitor. 1141 71

Hydnocarpus wightiana is advocated in traditional Indian medicine to possess strong antidiabetic activity. In the course of identifying bioactive fractions from Indian medicinal plants we observed that acetone extract of the seed hulls of H. wightiana possess strong free radicals (DPPH and ABTS) scavenging, alpha-glucosidase and moderate N-acetyl-beta-D-glucosaminidase inhibitory activities. Further fractionation of the extract led to the isolation of hydnocarpin, luteolin and isohydnocarpin in substantial yields. All the compounds showed strong ABTS scavenging property. However, only luteolin could display strong DPPH scavenging activity. Furthermore, all the three compounds also showed varying degrees of alpha-glucosidase and N-acetyl-beta-D-glucosaminidase inhibitory activity, luteolin being the superior. The kinetics of alpha-glucosidase inhibition by these compounds showed that acetone extract inhibits the enzyme in competitive manner however, luteolin and isohydnocarpin showed mixed-type inhibition. This is the first report assigning hydnocarpin and isohydnocarpin free radical scavenging, alpha-glucosidase and N-acetyl-beta-D-glucosaminidase inhibitory properties and luteolin as N-acetyl-beta-D-glucosaminidase inhibitor. This study suggests that presence of amphiphilic antioxidant molecules along with enzyme inhibitory activities in the acetone extract of H. wightiana seed hulls may be responsible for the antidiabetic properties as advocated in traditional medicine.
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PMID:Free radical scavenging, enzyme inhibitory constituents from antidiabetic Ayurvedic medicinal plant Hydnocarpus wightiana Blume. 1604 66

A series of 2,4-diaryl-2,3,4,5-tetrahydro- (36-40) and 2,4-diaryl-2,3-dihydro-1,5-benzothiazepines (25-35) have been synthesized from the corresponding chalcones 1-24. Both the benzothiazepines and chalcones were evaluated as DPPH free-radical scavengers and as inhibitors of cholinesterases, urease, and alpha-glucosidase. Compounds 2, 5, 6, 7, 10, 13, 18, 21, 36a, 37a, 37b, and 39a showed significant cholinesterase inhibiting activities. Among the 15 dihydro-1,5-benzothiazepines, 26, 32, and 35 exhibited significant radical-scavenging activities; and six tetrahydro-1,5-benzothiazepines (35, 36a, 36b, 37a, 37b, and 39a) were found to be inhibitors of AChE and BChE. Compounds 22, 25, 26, 33, 35, 36a, 37b, and 39a inhibited urease, and 25 and 27-31 were found to be potent inhibitors of alpha-glucosidase.
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PMID:Syntheses and biological activities of chalcone and 1,5-benzothiazepine derivatives: promising new free-radical scavengers, and esterase, urease, and alpha-glucosidase inhibitors. 1719 97

The synthesis, spectroscopic, enzyme-inhibition, and free-radical-scavenging properties of a series of vanadium(IV) complexes, compounds 1-10, were investigated. These complexes exhibit a dimeric structure with hydrazide ligands coordinated in a bidentate fashion. All complexes are stable in the solid state, but exhibit varying degrees of stability in solution. In coordinating solvent such as DMSO, stepwise binding of two solvent molecules at the 6th positions trans to the V double bond O bond of the dimeric unit is observed. The dimeric compounds are converted to monomeric species in which both solvent molecules and the hydrazide ligands are coordinated to the V(IV) center. The free hydrazide ligands 11-20 were inactive against alpha-glucosidase, but the V(IV) complexes showed varying degrees of inhibition, depending on the type of ligand. The DPPH-radical-scavenging activities of 1-20 were determined, which indicated that steric and/or electronic effects responsible for changes in geometry play important roles in terms of antioxidant potential.
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PMID:Synthesis, spectroscopy, and biological properties of vanadium(IV)-hydrazide complexes. 1820 28

Four alkaloids named piperumbellactams A-D (1-4) were isolated from branches of Piper umbellatum together with known N-hydroxyaristolam II (5), N-p-coumaroyl tyramine (6), 4-nerolidylcatechol (7), N-trans-feruloyltyramine, E-3-(3,4-dihydroxyphenyl)-N-2-[4-hydroxyphenylethyl]-2-propenamide, beta-amyrin, friedelin, apigenin 8-C-neohesperidoside, acacetin 6-C-beta-d-glucopyranoside, beta-sitosterol, its 3-O-beta-d-glucopyranoside and its 3-O-beta-d-[6'-dodecanoyl]-glucopyranoside. Glycosidase inhibition, antioxidant and antifungal activities of these compounds were evaluated. Compounds 1-3 showed moderate alpha-glucosidase enzyme inhibition with IC50 values 98.07+/-0.44, 43.80+/-0.56 and 29.64+/-0.46, respectively. In DPPH radical scavenging assay, compounds 2, 3 and 6 showed potent inhibitory activity while compounds 4, 5 and 7 showed potent antifungal activity.
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PMID:Bioactive aristolactams from Piper umbellatum. 1840 Feb 39

Fruits of seven fully ripened strawberry cultivars grown in Brazil (Dover, Camp Dover, Camarosa, Sweet Charlie, Toyonoka, Oso Grande, and Piedade) were evaluated for total phenolics, antioxidant activity based on DPPH radical scavenging assay, and functionality such as inhibition of alpha-amylase, alpha-glucosidase, and angiotensin I-converting enzyme (ACE) relevant for potentially managing hyperglycemia and hypertension. The total phenolics content ranged from 966 to 1571 microg of gallic acid/g of fruit fresh weight for Toyonoka and Dover, respectively. No correlation was found between total phenolics and antioxidant activity. The major phenolic compounds in aqueous extracts of strawberries were ellagic acid, quercetin, and chlorogenic acid. Strawberries had high alpha-glucosidase inhibitory activity. However, alpha-amylase inhibitory activity was very low in all cultivars. This suggested that strawberries could be considered as a potential dietary source with anti-hyperglycemic potential. The evaluated cultivars had no significant ACE inhibitory activity, reflecting low anti-hypertensive potential.
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PMID:Functionality of bioactive compounds in Brazilian strawberry (Fragaria x ananassa Duch.) cultivars: evaluation of hyperglycemia and hypertension potential using in vitro models. 1852 4

Lipids extracted from tsao-ko were separated into three fractions with silica gel column chromatography and fed to mice (3 mo old) for 90 d to clarify their inhibitory activity on digestive enzyme activity. The diets contained the following: control--no tsao-ko, 0.05% total lipid of tsao-ko (TL), 0.0109% chloroform fraction (CF), 0.0245% acetone fraction (AF), or 0.00365% methanol fraction (MeF). Although CF and AF slightly inhibited the activities of alpha-glucosidase, alpha-amylase, and lipase, intakes of these fractions had little influence on plasma and liver lipid concentrations when compared with the control diet. MeF did not inhibit alpha-glucosidase but had DPPH radical scavenging activity and the mice fed this fraction had the most marked reduction in plasma glucose and TBARS concentrations compared with the other diet groups. These results suggest that the fat-soluble polar components of tsao-ko contain an active component that might be associated with decreased plasma glucose and TBARS concentrations in mice.
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PMID:Effect of lipid extracted from tsao-ko (Amomum tsao-ko Crevost et Lemaire) on digestive enzyme activity, antioxidant activity, plasma and liver lipids, and blood glucose levels of mice. 1900 69

A new phenylpropanoid glycoside, dolichandroside-A, together with seven known compounds alpha-lapachone, lapachol, aloesaponarin II, 8-hydroxydehydroiso-alpha-lapachone, beta-sitosterol, 3,8-dihydroxydehydroiso-alpha-lapachone and verbascoside were isolated from the active ethyl acetate soluble extract of heartwood of Dolichandrone falcata. All except for dolichandroside-A are known compounds, but have been isolated for the first time from this plant. The structure of all these compounds was determined on the basis of 1D- and 2D-NMR spectral data. All the isolates were tested for alpha-glucosidase inhibitory and DPPH radical scavenging activity. This is the first report identifying DPPH scavenging activity and alpha-glucosidase inhibitory activity in D. falcata. Furthermore, along with a new compound, dolichandroside-A, this study also assigns for the first time alpha-glucosidase inhibitory activity to verbascoside and aloe saponarin-II.
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PMID:Dolichandroside A, a new alpha-glucosidase inhibitor and DPPH free-radical scavenger from Dolichandrone falcata seem. 1911 32

A bioassay-guided fractionation and chemical examination of antihyperglycemic root extract of Derris indica resulted in isolation and characterization of two new furanoflavanoids (1, 2) along with thirteen known compounds (3-15). Their structures were determined on the basis of extensive spectroscopic (IR, MS, 1D and 2D NMR) data analysis and by comparison with the literature data. All the compounds were tested in vitro for intestinal alpha-glucosidase inhibitory and DPPH radical activity. New compounds (1, 2) displayed moderate intestinal alpha-glucosidase inhibitory as well as free radical scavenging activity. Other compounds also displayed varying degrees of moderate intestinal alpha-glucosidase inhibitory activity. Pongamol (6) displayed potent intestinal alpha-glucosidase inhibition.
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PMID:New furanoflavanoids, intestinal alpha-glucosidase inhibitory and free-radical (DPPH) scavenging, activity from antihyperglycemic root extract of Derris indica (Lam.). 1951 70

Spices are extensively used to enhance the taste and flavor of foods and are known to possess several medicinal properties. Myristica fragrans, Parmelia perlata, Illicium verum, Trachyspermum copticum and Myristica malabarica, the commonly used spices in India were assessed for antidiabetic activity in streptozotocin induced diabetic rats. In the in vitro insulin secretion studies on isolated islets of Langerhans, M. fragrans, T. copticum and M. malabarica showed dose dependent insulin secretion. At 1 mg/ml, P. perlata showed significant in vitro alpha-glucosidase inhibitory activity with IC(50) value of 0.14 mg/ml followed by M. malabarica (0.64 mg/ml), I. verum (0.67 mg/ml), M. fragrans (0.85 mg/ml) and T. copticum (0.92 mg/ml). The DPPH free radical scavenging activity of the extracts at a concentration of 1 mg/ml was as M. malabarica (90.45%), M. fragrans (89.89%), I. verum (87.22%), P. perlata (76.70%) and T. copticum (38.14%). P. perlata showed the highest phenolic content (i.e., 118.5 mg gallic acid equivalents/g) followed by M. malabarica (84.13 mg gallic acid equivalents/g). M. malabarica showed the highest flavonoid content (i.e., 38.35 mg quercetin equivalents/g). Regular use of these spices may prevent postprandial rise in glucose levels through inhibition of intestinal alpha-glucosidase and may maintain blood glucose level through insulin secretagogue action.
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PMID:Insulin secretagogue, alpha-glucosidase and antioxidant activity of some selected spices in streptozotocin-induced diabetic rats. 2143 56


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