This study was designed to investigate the inhibitory effects of Polyopes lancifolia extract (PLE) on α-glucosidase activity, α-amylase activitiy, and postprandial hyperglycemia in streptozotocin (STZ)-induced diabetic mice. The results of this study revealed a marked inhibitory effect of PLE on α-glucosidase and α-amylase activities. The IC50s of PLE against α-glucosidase and α-amylase were 0....

In screening experiments for rat intestinal alpha-glucosidase (sucrase and maltase) inhibitors in 325 plants cultivated in Japan's southern island, of Tanegashima, marked inhibition against both sucrase and maltase was found in the extract of the fruit of Solanum torvum. Enzyme-assay guided fractionation of the extract led to the isolation of methyl caffeate (1) as a rat intestinal sucrase and ...

15-Alkylidene andrographolide derivatives were specific alpha-glucosidase inhibitors. Semi-synthetic studies of these derivatives led to new alpha-glucosidase inhibitors. Their alpha-glucosidase inhibitory activity was evaluated. Bioactivity results indicated that most of the derivatives were excellent alpha-glucosidase inhibitors. Among them, 6c displayed the best alpha-glucosidase inhibitory ...

An epimer of the known glycosidase inhibitor noeurostegine, galacto-noeurostegine, was synthesised in 21 steps from levoglucosan and found to be a potent, competitive and highly selective galactosidase inhibitor of Aspergillus oryzae β-galactosidase. Galacto-noeurostegine was not found to be an inhibitor of green coffee bean α-galactosidase, yeast α-glucosidase and E. coli β-galactosidase, wher...

keywords: Postprandial hyperglycaemia (PPHG), Alpha glucosidase inhibitors (αGI) ABSTRACT Diabetes Mellitus (DM) is a morbid disease worldwide, with increasing incidence as time passes. It has macro-vascular and micro-vascular complications. The main cause of these complications is poorly controlled postprandial hyperglycaemia. Alpha glucosidase inhibitors, namely acarbose, voglibose and miglit...

A novel series of 2-substituted-4,6-diarylpyrimidines 6a-6t has been synthesized, characterized by ¹H-NMR, 13C-NMR and HRMS, and screened for in vitro α-glucosidase inhibitory activity. The majority of the screened compounds possessed significant α-glucosidase inhibitory activity with IC50 values ranging from 19.6 ± 0.21 to 38.9 ± 0.35 μM, which is more potent than the positive control α-glucos...

The conformational analysis of glycosidases affords a route to their specific inhibition through transition-state mimicry. Inspired by the rapid reaction rates of cyclophellitol and cyclophellitol aziridine-both covalent retaining β-glucosidase inhibitors-we postulated that the corresponding carba "cyclopropyl" analogue would be a potent retaining β-glucosidase inhibitor for those enzymes react...

AIMS/INTRODUCTION To assess the efficacy and safety of sitagliptin compared with α-glucosidase inhibitors in Japanese patients with type 2 diabetes inadequately controlled by metformin or pioglitazone alone. MATERIALS AND METHODS In the present multicenter, randomized, open-label, parallel-group, active-controlled, non-inferiority trial, 119 patients aged 20-79 years with type 2 diabetes who ...

KAl(SO4)2.12H2O is found to efficiently and heterogeneously catalyze the one-pot three-component reaction of 2-(nitromethylene)imidazolidine, malononitrile and aldehydes under mild conditions to afford the corresponding tetrahydroimidazo[1,2-a]pyridine in good yields and short reaction times. Docking  study  of  some  compounds  in  the  active  site  of  α-glucosidase demonstrated  that  these...

During studies of the nutritional utilization of pyridoxine 5*-b-D-glucoside, a major form of vitamin B6 in plants, we detected two cytosolic b-glucosidases in jejunal mucosa. As expected, one was broad specificity b-glucosidase that hydrolyzed aryl b-D-glycosides but not pyridoxine b-D-glucoside. We also found a previously unknown enzyme, designated pyridoxine-b-D-glucoside hydrolase, that eff...