Miglitol: Assessment of its Role in the Treatment of Patients with Diabetes Mellitus

Campbell, Lance K.; Baker, Danial E.; Campbell, R. Keith

doi:10.1345/aph.19269

Cited by 96 publications

(45 citation statements)

References 33 publications

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“…Voglibose has not been subject to a literature review. It is difficult to value the results of these reviews because all have methodological weaknesses: no description of search strategy and inclusion criteria (5)(6)(7), no report of search results (5)(6)(7)(8)(9), and they either lack or have an unclear quality assessment of the included studies (5)(6)(7)(8)(9). In general, all reviews reported beneficial effects on glycemic control.…”

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confidence: 99%

α-Glucosidase Inhibitors for Patients With Type 2 Diabetes

et al. 2005

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OBJECTIVE -To review the effects of monotherapy with ␣-glucosidase inhibitors (AGIs) for patients with type 2 diabetes, with respect to mortality, morbidity, glycemic control, insulin levels, plasma lipids, body weight, and side effects. RESEARCH DESIGN AND METHODS -We systematically searched the CochraneCentral register of Controlled Trials, MEDLINE, EMBASE, Current Contents, LILACS, databases of ongoing trials, and reference lists, and we contacted experts and manufacturers. Inclusion criteria were randomized controlled trials of at least 12 weeks' duration, AGI monotherapy compared with any intervention, and one of the following outcome measures: mortality, morbidity, GHb, blood glucose, lipids, insulin levels, body weight, or side effects. Two independent reviewers assessed all abstracts, extracted all data, and assessed quality. We contacted all authors for data clarification. Continuous data were expressed as weighted mean differences and analyzed with a random-effects model. Possible influences of study characteristics and quality were assessed in sensitivity and meta-regression analyses.RESULTS -Forty-one studies were included in the review (30 acarbose, 7 miglitol, 1 voglibose, and 3 combined), and heterogeneity was limited. We found no evidence for an effect on mortality or morbidity. Compared with placebo, AGIs had a beneficial effect on GHb (acarbose Ϫ0.77%; miglitol Ϫ0.68%), fasting and postload blood glucose and postload insulin. With acarbose dosages higher than 50 mg t.i.d., the effect on GHb was the same, but the occurrence of side effects increased. Acarbose decreased the BMI by 0.17 kg/m 2 (95% CI 0.08 -0.26). None of the AGIs had an effect on plasma lipids. Compared with sulfonylurea, AGIs seemed inferior with respect to glycemic control, but they reduced fasting and postload insulin levels. For comparisons with other agents, little data were available.CONCLUSIONS -We found no evidence for an effect on mortality or morbidity. AGIs have clear beneficial effects on glycemic control and postload insulin levels but not on plasma lipids. There is no need for dosages higher than 50 mg acarbose t.i.d. Diabetes Care 28:166 -175, 2005A lpha-glucosidase inhibitors (AGIs; acarbose, miglitol, voglibose) are widely used in the treatment of patients with type 2 diabetes. AGIs delay the absorption of carbohydrates from the small intestine and thus have a lowering effect on postprandial blood glucose and insulin levels.In modern medicine, the efficacy of an intervention should be investigated in well-designed randomized trials. Results from the trials should be collected in a high-quality systematic review, if possible with a meta-analysis. And finally, the evidence should have its repercussions on practice guidelines.How does this apply for AGIs? Recommendations on when to use AGIs and the evidence used for these recommendations appear to be different in various guidelines. For example, the guideline by the European Diabetes Policy Group (1) and a consensus statement by the American Diabetes Association (2)...

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confidence: 99%

α-Glucosidase Inhibitors for Patients With Type 2 Diabetes

et al. 2005

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“…Miglitol was used as a standard inhibitor molecule for the comparison as it was alone capable of satisfying all the five rules of Lipinski in comparison to acarbose, metformin, and voglibose standards [33,34]. The ligand molecules along with the standard miglitol were docked into the binding pockets of α-amylase and α-glucosidase to find out their binding interactions.…”

Section: Molecular Docking Analysismentioning

confidence: 99%

INHIBITION OF Α-Amylase AND Α-Glucosidase BY (6rs)-22-Hydroxy-23,24,25,26,27-Pentanor-Vitamin-D3-6,19-Sulfur DIOXIDE-ADDUCT, MANOALIDE AND 5β-Cholestane-3α,7α,12α,24,25,26-Hexol ISOLATED FROM ACETONE EXTRACT OF HELIANTHUS ANNUUS L. SEEDS

Sonkamble

Wagh

Kamble

2018

Int J Pharm Pharm Sci

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Objective: This investigation includes characterization of phytochemicals from acetone extract of Helianthus annuus L. seeds responsible for α-amylase and α-glucosidase inhibition revealed from in vitro and in silico approaches. Methods:Seed extract was qualitatively and quantitatively analysed for the presence of bioactive molecules. In vitro α-amylase and α-glucosidase inhibition assays and kinetics studies for α-glucosidase were done. Thin layer chromatography (TLC) autography of extract was done to screen potent inhibitors and characterized by high-resolution liquid chromatography-mass spectrometry (HR LC-MS). Characterized molecules were further used for in silico studies.Results: Qualitative investigation reveals the presence of flavonoids, glycosides, alkaloids, terpenoids, and steroids. Quantitative analysis for total phenolic content and total flavonoid content of the extract was 0.1±0.005 mg/ml GAE and 0.025±0.003 mg/ml QE respectively. Percent inhibition of α-amylase and α-glucosidase ascertained in presence of extract was 60.42±0.6 and 83.22±0.18 at 0.01 mg while 36.24±0.81 and 37.67±0.15 at 0.005 mg of extracts for both enzymes respectively. Kinetics studies of α-glucosidase inhibition illustrated the non-competitive type of inhibition. TLC autography inhibition patterns were characterized by HR LC-MS. Characterized molecules on docking revealed (6RS)- 22-hydroxy-23,24,25,26,27-pentanor-vitamin-D3-6,19-sulfurdioxide-adduct, manoalide and 5β-cholestane-3α,7α,12α,24,25,26-hexol as the best docked molecules with lowest binding energies of-12.5,-11 and-10.2 kcal/mol for α-amylase and-14.2,-11 and-11.2 kcal/mol for α-glucosidase respectively. Conclusion:Results clearly suggested that (6RS)-22-hydroxy-23,24,25,26,27-pentanor-vitamin-D3-6,19-sulfurdioxide-adduct, manoalide and 5β-cholestane-3α,7α,12α,24,25,26-hexol could be considered as lead molecules for the discovery of potent antidiabetic agents.

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“…Two different AGIs were used: acarbose (Bayer, West Haven, CT), which is not absorbed by the small intestine, and deoxynojirimycin (1-deoxynojirimycin hydrochloride, Sigma-Aldrich), which, like its closely related analog miglitol, is absorbed [14][15][16] by active transport [17]. Both compounds have a very high affinity for intestinal glucosidases [18].…”

Section: A-glucosidase Inhibitorsmentioning

confidence: 99%