The effects of theα-glucosidase inhibitor BAY g 5421 (Acarbose) on postprandial blood glucose, serum insulin, and triglyceride levels: Dose-time-response relationships in man

1979 ◽  
Vol 175 (1) ◽  
pp. 87-94 ◽  
Author(s):  
I. Hillebrand ◽  
K. Boehme ◽  
G. Frank ◽  
H. Fink ◽  
P. Berchtold
Molecules ◽  
2021 ◽  
Vol 26 (15) ◽  
pp. 4638
Author(s):  
Tao Tian ◽  
Guo-Ying Chen ◽  
Hao Zhang ◽  
Feng-Qing Yang

As a key enzyme regulating postprandial blood glucose, α-Glucosidase is considered to be an effective target for the treatment of diabetes mellitus. In this study, a simple, rapid, and effective method for enzyme inhibitors screening assay was established based on α-glucosidase catalyzes reactions in a personal glucose meter (PGM). α-glucosidase catalyzes the hydrolysis of maltose to produce glucose, which triggers the reduction of ferricyanide (K3[Fe(CN)6]) to ferrocyanide (K4[Fe(CN)6]) and generates the PGM detectable signals. When the α-glucosidase inhibitor (such as acarbose) is added, the yield of glucose and the readout of PGM decreased accordingly. This method can achieve the direct determination of α-glucosidase activity by the PGM as simple as the blood glucose tests. Under the optimal experimental conditions, the developed method was applied to evaluate the inhibitory activity of thirty-four small-molecule compounds and eighteen medicinal plants extracts on α-glucosidase. The results exhibit that lithospermic acid (52.5 ± 3.0%) and protocatechualdehyde (36.8 ± 2.8%) have higher inhibitory activity than that of positive control acarbose (31.5 ± 2.5%) at the same final concentration of 5.0 mM. Besides, the lemon extract has a good inhibitory effect on α-glucosidase with a percentage of inhibition of 43.3 ± 3.5%. Finally, the binding sites and modes of four active small-molecule compounds to α-glucosidase were investigated by molecular docking analysis. These results indicate that the PGM method is feasible to screening inhibitors from natural products with simple and rapid operations.


2018 ◽  
Vol 76 (6) ◽  
pp. 156-162
Author(s):  
Satoko Noguchi ◽  
Kohei Suruga ◽  
Kumiko Nakai ◽  
Akihiro Murashima ◽  
Yoshihiro Koshino-Kimura ◽  
...  

Nutrients ◽  
2020 ◽  
Vol 12 (4) ◽  
pp. 1115 ◽  
Author(s):  
Mariana O. C. Coelho ◽  
Alistair J. Monteyne ◽  
Ishara D. Kamalanathan ◽  
Vesna Najdanovic-Visak ◽  
Tim J. A. Finnigan ◽  
...  

Circulating uric acid concentrations have been linked to various metabolic diseases. Consumption of large boluses of nucleotides increases serum uric acid concentrations. We investigated the effect of a nucleotide-rich mixed meal on postprandial circulating uric acid, glucose, and insulin responses. Ten healthy adults participated in a randomised, controlled, double-blind, crossover trial in which they consumed a mixed-meal containing either nucleotide-depleted mycoprotein (L-NU) or high-nucleotide mycoprotein (H-NU) on two separate visits. Blood samples were collected in the postabsorptive state and throughout a 24 h postprandial period, and were used to determine circulating uric acid, glucose, and insulin concentrations. Mixed meal ingestion had divergent effects on serum uric acid concentrations across conditions (time x condition interaction; P < 0.001), with L-NU decreasing transiently (from 45 to 240 min postprandially) by ~7% (from 279 ± 16 to 257 ± 14 µmol·L−1) and H-NU resulting in a ~12% increase (from 284 ± 13 to 319 ± 12 µmol·L−1 after 210 min), remaining elevated for 12 h and returning to baseline concentrations after 24 h. There were no differences between conditions in blood glucose or serum insulin responses, nor in indices of insulin sensitivity. The ingestion of a nucleotide-rich mixed-meal increases serum uric acid concentrations for ~12 h, but does not influence postprandial blood glucose or serum insulin concentrations.


2014 ◽  
Vol 307 (12) ◽  
pp. G1191-G1197 ◽  
Author(s):  
Sony S. Thazhath ◽  
Tongzhi Wu ◽  
Michelle J. Bound ◽  
Helen L. Checklin ◽  
Karen L. Jones ◽  
...  

Endothelial function, measured by flow-mediated dilatation (FMD), predicts cardiovascular events and is impaired postprandially. The objective of this study was to evaluate the effects of changes in composition or duration of ingestion of a meal, which slows gastric emptying and/or small intestinal nutrient exposure, on postprandial endothelial function. Twelve healthy subjects (6 male, 6 female; 33 ± 6 yr) were each studied on three occasions, in a randomized crossover design. After an overnight fast, subjects consumed a [13C]octanoic acid-labeled mashed potato meal (“ meal 1”), or meal 1 mixed with 9 g guar (“ meal 2”) within 10 min, or meal 1 divided into 12 equal portions over 60 min (“ meal 3”). Brachial artery FMD was measured every 30 min for 120 min. Blood glucose, serum insulin, and gastric emptying (breath test) were evaluated for 240 min. Data are means ± SE. Compared with meal 1, meal 2 was associated with slower gastric emptying (half-emptying time 285 ± 27 vs. 208 ± 15 min, P < 0.05), lower postprandial blood glucose and insulin ( P < 0.001 for both), and a delayed, but more sustained, suppression of FMD ( P < 0.001). After meal 3, both glycemic increment and reduction in FMD were less than after meal 2 ( P < 0.05 for both). The decrement in FMD was directly related to the increment in blood glucose ( r = 0.46, P = 0.02). We conclude that, in health, postprandial FMD is influenced by perturbation of gastric emptying and the duration of meal consumption, which also impact on glycemia.


1996 ◽  
Vol 24 (5) ◽  
pp. 438-447 ◽  
Author(s):  
S Okada ◽  
K Ishii ◽  
H Hamada ◽  
S Tanokuchi ◽  
K Ichiki ◽  
...  

Studies were carried out to assess various ways of improving glycaemic control and lipid profiles of patients with non-insulin-dependent diabetes mellitus (NIDDM) in whom glucose metabolism was poor. Part or all of the dose of the sulphonylurea that had been used to treat patients in Group 1 ( n = 8) was replaced by an α-glucosidase inhibitor. Symptoms related to hypoglycaemia disappeared and the postprandial blood glucose level was significantly increased ( P < 0.043) but serum lipid levels were not significantly altered and the mean glycosylated haemoglobin level was unchanged. In Group 2 ( n = 10) patients, a large part of the insulin dose was replaced by an α-glucosidase inhibitor. Hypoglycaemia-related symptoms disappeared but there were no significant changes in lipid profiles, postprandial blood glucose or glycosylated haemoglobin levels. The third group of patients ( n = 9) had been treated with insulin alone and were given additional α-glucosidase inhibitor without changing their insulin dose. This did not significantly change their lipid profiles, postprandial blood glucose or glycosylated haemoglobin levels. In Group 4 ( n = 9) the addition of an α-glucosidase inhibitor to the initial sulphonylurea did not produce any significant changes in mean postprandial blood glucose or glycosylated haemoglobin levels. The results for individual patients indicated that the glycosylated haemoglobin levels had improved after the change of treatment only in those patients whose connective peptide immunoreactivity was > 6.0 ng/ml.


2017 ◽  
Vol 12 (S 01) ◽  
pp. S1-S84
Author(s):  
G Andersen ◽  
G Meiffren ◽  
B Alluis ◽  
A Ranson ◽  
R Soula ◽  
...  

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