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Alpha-glucosidase Inhibitor

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1. Alpha-glucosidase inhibitors for prevention or delay of type 2 diabetes mellitus and its associated complications in people at increased risk of developing type 2 diabetes mellitus. (PubMed)

Alpha-glucosidase inhibitors for prevention or delay of type 2 diabetes mellitus and its associated complications in people at increased risk of developing type 2 diabetes mellitus. Alpha-glucosidase inhibitors (AGI) reduce blood glucose levels and may thus prevent or delay type 2 diabetes mellitus (T2DM) and its associated complications in people at risk of developing of T2DM.To assess the effects of AGI in people with impaired glucose tolerance (IGT), impaired fasting blood glucose (IFG

2018 Cochrane

2. The effect of luseogliflozin and alpha-glucosidase inhibitor on heart failure with preserved ejection fraction in diabetic patients: rationale and design of the MUSCAT-HF randomised controlled trial. (PubMed)

The effect of luseogliflozin and alpha-glucosidase inhibitor on heart failure with preserved ejection fraction in diabetic patients: rationale and design of the MUSCAT-HF randomised controlled trial. Type 2 diabetes mellitus (T2DM) is a strong risk factor for coronary artery disease and heart failure, particularly heart failure with preserved ejection fraction (HFpEF). The aim of the ongoing MUSCAT-HF (It stands for Prospective Comparison of Luseogliflozin and Alpha-glucosidase (...) on the Management of Diabetic Patients with Chronic Heart Failure and Preserved Ejection Fraction) trial is to evaluate the efficacy of luseogliflozin, a sodium-glucose cotransporter 2 (SGLT2) inhibitor, versus voglibose, an alpha-glucosidase inhibitor, using brain natriuretic peptide (BNP) as the index of therapeutic effect in T2DM patients with HFpEF.A total of 190 patients with T2DM and HFpEF (ejection fraction >45%) who are drug-naïve or taking any anti-diabetic agents will be randomised (1:1) to receive

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2019 BMJ open

3. Efficacy and safety of combination therapy with an alpha-glucosidase inhibitor and a dipeptidyl peptidase-4 inhibitor in patients with type 2 diabetes mellitus: A systematic review with meta-analysis. (PubMed)

Efficacy and safety of combination therapy with an alpha-glucosidase inhibitor and a dipeptidyl peptidase-4 inhibitor in patients with type 2 diabetes mellitus: A systematic review with meta-analysis. The combination of dipeptidyl peptidase-4 (DPP4) inhibitors and α-glucosidase inhibitors (AGIs) might provide an additive or synergistic glucose-lowering effect, as they have a complementary mode of action. In the present study, we examined the efficacy and safety of the addition of a DPP4 (...) inhibitor to patients with type 2 diabetes inadequately controlled with an AGI.We carried out an electronic search of MEDLINE, EMBASE, the Cochrane Library and Clinicaltrials.gov through October 2016. Randomized controlled trials written in English that compared DPP4 inhibitors plus AGI (DPP4i/AGI) and placebo plus AGI (PCB/AGI) in patients with type 2 diabetes were selected. Data on the study characteristics, efficacy and safety outcomes were extracted, and the risk of potential biases was assessed

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2017 Journal of Diabetes Investigation

4. Glitazones and alpha-glucosidase inhibitors as the second-line oral anti-diabetic agents added to metformin reduce cardiovascular risk in Type 2 diabetes patients: a nationwide cohort observational study (PubMed)

Glitazones and alpha-glucosidase inhibitors as the second-line oral anti-diabetic agents added to metformin reduce cardiovascular risk in Type 2 diabetes patients: a nationwide cohort observational study Metformin is the standard first-line drug for patients with Type 2 diabetes (T2DM). However, the optimal second-line oral anti-diabetic agent (ADA) remains unclear. We investigated the cardiovascular risk of various ADAs used as add-on medication to metformin in T2DM patients from a nationwide (...) cohort.T2DM patients using different add-on oral ADAs after an initial metformin therapy of > 90 days were identified from the Taiwan National Health Insurance Database. Five classes of ADAs, including sulphonylureas (SU), glinides, thiazolidinediones (TZD), alpha-glucosidase inhibitors (AGI), and dipeptidyl peptidase-4 inhibitors (DPP-4I) were selected for analysis. The reference group was the SU added to metformin. Patients were excluded if aged < 20 years, had a history of stroke or acute coronary

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2018 Cardiovascular diabetology

5. Therapeutic monitoring of TNF-alpha inhibitors in rheumatoid arthritis

Therapeutic monitoring of TNF-alpha inhibitors in rheumatoid arthritis Ther Therapeutic monitoring of TNF-alpha apeutic monitoring of TNF-alpha inhibitors in rheumatoid arthritis inhibitors in rheumatoid arthritis Diagnostics guidance Published: 10 July 2019 www.nice.org.uk/guidance/dg36 © NICE 2019. All rights reserved. Subject to Notice of rights (https://www.nice.org.uk/terms-and-conditions#notice-of- rights).Y Y our responsibility our responsibility This guidance represents the view of NICE (...) possible. Therapeutic monitoring of TNF-alpha inhibitors in rheumatoid arthritis (DG36) © NICE 2019. All rights reserved. Subject to Notice of rights (https://www.nice.org.uk/terms-and- conditions#notice-of-rights). Page 2 of 36Contents Contents 1 Recommendations 4 2 Clinical need and practice 5 The problem addressed 5 The condition 6 The care pathways 6 3 The diagnostic tests 8 The interventions 8 The comparator 9 4 Evidence 11 Clinical effectiveness 11 Cost effectiveness 17 5 Committee discussion 25

2019 National Institute for Health and Clinical Excellence - Diagnostics Guidance

6. Sitagliptin but not alpha glucosidase inhibitor reduced the serum soluble CD163, a marker for activated macrophage, in individuals with type 2 diabetes mellitus. (PubMed)

Sitagliptin but not alpha glucosidase inhibitor reduced the serum soluble CD163, a marker for activated macrophage, in individuals with type 2 diabetes mellitus. Dipeptidyl peptidase-4 inhibitor (DPP-4i) is commonly used worldwide for the treatment of type 2 diabetes mellitus. In addition to its hypoglycemic activity, DPP-4i might have anti-inflammatory effects. In this study we examined the effects of DPP-4i on the serum levels of soluble CD163 (sCD163), a marker for activated macrophages (...) , in individuals with type 2 diabetes mellitus. We compared these anti-inflammatory effects with those of α glucosidase inhibitor (αGI).Japanese patients with type 2 diabetes mellitus who were stably maintained on ≤2mg/day glimepiride alone were recruited and randomly assigned to receive additional sitagliptin (n=37) or αGI (n=37). Levels of sCD163 were measured before the addition and after a 24-week treatment period.Addition of sitagliptin significantly reduced the serum sCD163 (632 vs. 575ng/mL, p<0.05

2017 Diabetes research and clinical practice

7. Alpha-glucosidase inhibitors and risk of cancer in patients with diabetes mellitus: a systematic review and meta-analysis. (PubMed)

Alpha-glucosidase inhibitors and risk of cancer in patients with diabetes mellitus: a systematic review and meta-analysis. Several studies have shown that anti-diabetic medications may modify the risk of cancer. We performed a systematic review and meta-analysis to evaluate the effect of alpha-glucosidase inhibitors (AGIs) on the risk of cancer in patients with diabetes mellitus. We conducted a systematic search of Medline, EMBASE, and Web of Science databases, up to September 30, 2016. Random

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2017 Oncotarget

8. Meta-analysis and critical review on the efficacy and safety of alpha glucosidase inhibitors in Asian and non-Asian populations. (PubMed)

Meta-analysis and critical review on the efficacy and safety of alpha glucosidase inhibitors in Asian and non-Asian populations. To evaluate the efficacy and safety of alpha-glucosidase inhibitors (AGI) in Asian and non-Asian type 2 diabetes patients.Studies were identified through a literature search of MEDLINE, EMBASE and other databases until December 2016. All statistical analyses were carried out in Review Manager statistical software by computing the weighted mean difference or odds ratio (...) in HbA1c compared with dipeptidyl peptidase-4 inhibitors and sulfonylurea. In non-Asian patients, AGI treatment showed a lower reduction in HbA1c compared with thiazolidinedione. No significant difference was observed in HbA1c change and bodyweight change when comparing AGI with other oral hypoglycemic agents between Asian and non-Asian patients.The effects of AGI treatment on glycemic control and bodyweight reduction were superior to the placebo without an increased incidence of hypoglycemia

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2017 Journal of Diabetes Investigation

9. Alpha-glucosidase inhibitor use is associated with decreased colorectal neoplasia risk in patients with type 2 diabetes mellitus receiving colonoscopy: a retrospective study (PubMed)

Alpha-glucosidase inhibitor use is associated with decreased colorectal neoplasia risk in patients with type 2 diabetes mellitus receiving colonoscopy: a retrospective study The purpose of this study was to clarify the factors that influence the incidence of colorectal neoplasia in patients with type 2 diabetes mellitus (DM).Among a total of 1176 patients who underwent total colonoscopy at our hospital, we retrospectively analyzed 168 patients with type 2 DM. Univariate and multivariate (...) logistic regression analyses were then performed to identify the risk factors associated with colorectal neoplasia.A multivariate analysis of these patients demonstrated that male gender (odds ratio [OR] = 4.04, 95% confidence interval [CI] = 1.67-10.37, p = 0.002), taking statins (OR = 4.59, 95% CI = 1.69-13.43, p = 0.003), taking alpha glucosidase inhibitor (α-GI) (OR = 0.35, 95% CI = 0.13-0.87, p = 0.023) and taking low-dose aspirin (LDA) (OR = 0.32, 95% CI = 0.10-0.95, p = 0.040) were independent

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2017 Oncotarget

10. Alpha-glucosidase inhibitors and hepatotoxicity in type 2 diabetes: a systematic review and meta-analysis. (PubMed)

Alpha-glucosidase inhibitors and hepatotoxicity in type 2 diabetes: a systematic review and meta-analysis. Alpha-glucosidase inhibitors (AGIs) was reported to be associated with several rare adverse hepatic events, but with inconsistent results. We aimed to investigate the risk of hepatotoxicity associated with the use of AGIs in patients with type 2 diabetes mellitus (T2DM), and performed a systematic review and meta-analysis. Fourteen studies (n = 2881) were eligible, all of which were RCTs

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2016 Scientific reports

11. Alpha-glucosidase Inhibitor

Alpha-glucosidase Inhibitor Alpha-glucosidase Inhibitor Toggle navigation Brain Head & Neck Chest Endocrine Abdomen Musculoskeletal Skin Infectious Disease Hematology & Oncology Cohorts Diagnostics Emergency Findings Procedures Prevention & Management Pharmacy Resuscitation Trauma Emergency Procedures Ultrasound Cardiovascular Emergencies Lung Emergencies Infectious Disease Pediatrics Neurologic Emergencies Skin Exposure Miscellaneous Abuse Cancer Administration 4 Alpha-glucosidase Inhibitor (...) Alpha-glucosidase Inhibitor Aka: Alpha-glucosidase Inhibitor , Acarbose , Precose , Miglitol , Glyset From Related Chapters II. Indications Close to target ( <8% as monotherapy) III. Contraindications (DKA) Intestinal disorder Colonic ulceration Partial IV. Mechanism Structurally similar to Reversible inhibitor of alpha glucosidase Present in brush border of Interferes with hydrolysis of carbohydrates Complex carbohydrates Dietary disaccharides Delays absorption of and other monosaccharides V

2018 FP Notebook

12. Antioxidants and α-glucosidase inhibitors from Neptunia oleracea fractions using <sup>1</sup>H NMR-based metabolomics approach and UHPLC-MS/MS analysis. (PubMed)

Antioxidants and α-glucosidase inhibitors from Neptunia oleracea fractions using 1H NMR-based metabolomics approach and UHPLC-MS/MS analysis. Neptunia oleracea is a plant cultivated as vegetable in Southeast Asia. Previous works have revealed the potential of this plant as a source of natural antioxidants and α-glucosidase inhibitors. Continuing our interest on this plant, the present work is focused in identification of the bioactive compounds from different polarity fractions of N (...) . The UHPLC-MS/MS profiling of EF and MF had tentatively identified the phenolics present. Together with some non-phenolic metabolites, a total of 37 metabolites were tentatively assigned.The findings of this work supported that N. oleracea is a rich source of phenolics that can be potential antioxidants and α-glucosidase inhibitors for the management of diabetes. To our knowledge, this study is the first report on the metabolite-bioactivity correlation and UHPLC-MS/MS analysis of N. oleracea fractions.

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2019 BMC Complementary and Alternative Medicine

13. An α-glucosidase inhibitor could reduce T-wave alternans in type 2 diabetes patients. (PubMed)

An α-glucosidase inhibitor could reduce T-wave alternans in type 2 diabetes patients. We tested the hypothesis that an alpha-glucosidase inhibitor (α-GI), miglitol, is effective in protecting the cardiovascular system in type 2 diabetes mellitus (T2DM).We studied 19 hospitalized heart disease patients with T2DM in whom we performed continuous glucose monitoring, Holter electrocardiogram, and ambulatory blood pressure (BP) monitoring simultaneously for 48h. The α-GI miglitol was administered

2019 Journal of electrocardiology

14. COMBODART (dutasteride + tamsulosin), 5-? reductase inhibitor + alpha-blocker

COMBODART (dutasteride + tamsulosin), 5-? reductase inhibitor + alpha-blocker Haute Autorité de Santé - COMBODART (dutastéride + tamsulosine), inhibiteur de la 5-α réductase + alpha-bloquant Développer la qualité dans le champ sanitaire, social et médico-social Recherche Évaluation & Recommandation La HAS Accréditation & Certification Outils, Guides & Méthodes Agenda Avis sur les Médicaments COMBODART (dutastéride + tamsulosine), inhibiteur de la 5-α réductase + alpha-bloquant Substance active

2017 Haute Autorite de sante

15. Gluco-1H-imidazole: A New Class of Azole-Type β-Glucosidase Inhibitor (PubMed)

Gluco-1H-imidazole: A New Class of Azole-Type β-Glucosidase Inhibitor Gluco-azoles competitively inhibit glucosidases by transition-state mimicry and their ability to interact with catalytic acid residues in glucosidase active sites. We noted that no azole-type inhibitors described, to date, possess a protic nitrogen characteristic for 1 H-imidazoles. Here, we present gluco-1 H-imidazole, a gluco-azole bearing a 1 H-imidazole fused to a glucopyranose-configured cyclitol core, and three close (...) analogues as new glucosidase inhibitors. All compounds inhibit human retaining β-glucosidase, GBA1, with the most potent ones inhibiting this enzyme (deficient in Gaucher disease) on a par with glucoimidazole. None inhibit glucosylceramide synthase, cytosolic β-glucosidase GBA2 or α-glucosidase GAA. Structural, physical and computational studies provide first insights into the binding mode of this conceptually new class of retaining β-glucosidase inhibitors.

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2018 Journal of the American Chemical Society

16. N-glycan Remodeling Using Mannosidase Inhibitors to Increase High-mannose Glycans on Acid α-Glucosidase in Transgenic Rice Cell Cultures (PubMed)

N-glycan Remodeling Using Mannosidase Inhibitors to Increase High-mannose Glycans on Acid α-Glucosidase in Transgenic Rice Cell Cultures Glycoengineering of plant expression systems is a prerequisite for the production of biopharmaceuticals that are compatible with animal-derived glycoproteins. Large amounts of high-mannose glycans such as Man7GlcNAc2, Man8GlcNAc2, and Man9GlcNAc2 (Man7/8/9), which can be favorably modified by chemical conjugation of mannose-6-phosphate, are desirable (...) for lysosomal enzyme targeting. This study proposed a rice cell-based glycoengineering strategy using two different mannosidase inhibitors, kifunensine (KIF) and swainsonine (SWA), to increase Man7/8/9 glycoforms of recombinant human acid α-glucosidase (rhGAA), which is a therapeutic enzyme for Pompe disease. Response surface methodology was used to investigate the effects of the mannosidase inhibitors and to evaluate the synergistic effect of glycoengineering on rhGAA. Both inhibitors suppressed formation

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2018 Scientific reports

17. UHPLC/MS Identifying Potent α-glucosidase Inhibitors of Grape Pomace via Enzyme Immobilized Method (PubMed)

UHPLC/MS Identifying Potent α-glucosidase Inhibitors of Grape Pomace via Enzyme Immobilized Method α-Glucosidases have been a major target in controlling and managing postprandial blood glucose and therefore diabetes treatment. This study aims to further identify and purify active compounds from the most active ethyl acetate fraction collected previously in Tinta Cão grape pomace extract (TCEE) using a newly developed and highly effective immobilization method, including obtaining compounds (...) previously shown to inhibit the enzyme. Purification used crosslinked chitosan beads with α-glucosidases bound to polymer, which acted as immobilized enzyme vehicle to collect inhibitors. Compounds absorbed into the beads were eluded using methanol, where collected fraction was subjected to UHPLC-MS analysis to identify active compounds. Results presented 5 major compounds: viniferifuran (amurensin H), p-coumaroyl-6-O-D-glucopyranoside, p-coumaroyl-6-O-hexoside, (epi)catechin-hexoside, 10-carboxyl

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2018 Journal of food science

18. α-Glucosidase Inhibitors From the Coral-Associated Fungus Aspergillus terreus (PubMed)

α-Glucosidase Inhibitors From the Coral-Associated Fungus Aspergillus terreus Nine novel butenolide derivatives, including four pairs of enantiomers, named (±)-asperteretones A-D (1a/1b-4a/4b), and a racemate, named asperteretone E (5), were isolated and identified from the coral-associated fungus Aspergillus terreus. All the structures were established based on extensive spectroscopic analyses, including HRESIMS and NMR data. The chiral chromatography analyses allowed the separation (...) revised to (±)-asperteretones B (2a/2b) and D (4), respectively. Additionally, compounds 1a/1b-4a/4b and 5 were evaluated for the α-glucosidase inhibitory activity, and all these compounds exhibited potent inhibitory potency against α-glucosidase, with IC50 values ranging from 15.7 ± 1.1 to 53.1 ± 1.4 μM, which was much lower than that of the positive control acarbose (IC50 = 154.7 ± 8.1 μM), endowing them as promising leading molecules for the discovery of new α-glucosidase inhibitors for type-2

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2018 Frontiers in chemistry

19. Characterization of α-Glucosidase Inhibitors from Clinacanthus nutans Lindau Leaves by Gas Chromatography-Mass Spectrometry-Based Metabolomics and Molecular Docking Simulation (PubMed)

Characterization of α-Glucosidase Inhibitors from Clinacanthus nutans Lindau Leaves by Gas Chromatography-Mass Spectrometry-Based Metabolomics and Molecular Docking Simulation Clinacanthus nutans (C. nutans) is an Acanthaceae herbal shrub traditionally consumed to treat various diseases including diabetes in Malaysia. This study was designed to evaluate the α-glucosidase inhibitory activity of C. nutans leaves extracts, and to identify the metabolites responsible for the bioactivity.Crude (...) , palmitic acid, phytol, hexadecanoic acid (methyl ester), 1-monopalmitin, stigmast-5-ene, pentadecanoic acid, heptadecanoic acid, 1-linolenoylglycerol, glycerol monostearate, alpha-tocospiro B, and stigmasterol. In-silico study via molecular docking was carried out using the crystal structure Saccharomyces cerevisiae isomaltase (PDB code: 3A4A). Interactions between the inhibitors and the protein were predicted involving residues, namely LYS156, THR310, PRO312, LEU313, GLU411, and ASN415 with hydrogen

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2018 Molecules : A Journal of Synthetic Chemistry and Natural Product Chemistry

20. Rapidly screening of α-glucosidase inhibitors from Dioscorea opposita Thunb. peel based on rGO@Fe3O4 nanocomposites microreactor (PubMed)

Rapidly screening of α-glucosidase inhibitors from Dioscorea opposita Thunb. peel based on rGO@Fe3O4 nanocomposites microreactor Present study aimed to immobilise the α-glucosidase on suitable supports to construct enzymatic microreactors and their subsequent applicability in efficient inhibitor screening from the Chinese Yam (Dioscorea opposita Thunb.) peel. A type of lamellar and porous composites (rGO@Fe3O4) were synthesised with a facile one-step solvothermal method and employed (...) as carriers to construct enzymatic microreactors for screening α-glucosidase ligand from the Chinese Yam peel in league with the high performance liquid chromatography and mass spectrometry (HPLC-MS). The immobilisation amount of α-glucosidase on rGO@Fe3O4 under the optimised conditions was about 40 μg α-glucosidase/mg carriers. Furthermore, the binding capacities of screened inhibitors, 2,4-dimethoxy-6,7-dihydroxyphenanthrene and batatasin I, were 35.6 and 68.2%, respectively. Hence, considering

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2018 Journal of enzyme inhibition and medicinal chemistry

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