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From the fruit of Pandanus tectorius Parkinson ex Du Roi, one new (1) and six known aldehyde compounds (2-7) were isolated by various chromatography methods. Based on their spectroscopic data, these compounds were identified as (Z)-4-hydroxy-3-(4-hydroxy-3-methylbut-2-en-1-yl) benzaldehyde (1), p-hydroxybenzaldehyde (2), syringaldehyde (3), (E)-ferulaldehyde (4), (E)-sinapinaldehyde (5), vanillin (6) and 5-hydroxymethylfurfual (7). The α-glucosidase inhibitory activity of all compounds was measured. The isolated compounds (1-6) showed better α-glucosidase inhibitory activity (IC50 values ranging from 36.5 to 192.4 μM) than the standard drug acarbose (IC50 = 214.5 μM).
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We investigated 77 patients (mean age 58.7 years, mean BMI 27.3 kg/m2), treated by diet alone for at least 4 weeks. The subjects were randomized into three treatment groups for 16 weeks: 100 mg t.i.d. acarbose (n = 25) or 1 mg t.i.d. glibenclamide (n = 27) or one t.i.d. placebo (n = 25). Before and after therapy, the levels of fasting plasma glucose, glycosylated haemoglobin, fasting insulin, plasma glucose and insulin 1 h after a standardized breakfast were measured and insulin sensitivity determined by euglycaemic hyperinsulinaemic clamp test.
We here report a quantitative study on the binding kinetics of inhibition of the enzyme glucoamylase and how individual active site amino acid mutations influence kinetics. To address this challenge, we have developed a fast and efficient method for anchoring native acarbose to gold chip surfaces for surface plasmon resonance studies employing wild type glucoamylase and active site mutants, Y175F, E180Q, and R54L, as analytes. The key method was the chemoselective and protecting group-free oxime functionalization of the pseudo-tetrasaccharide-based inhibitor acarbose. By using this technique we have shown that at pH 7.0 the association and dissociation rate constants for the acarbose-glucoamylase interaction are 10(4)M(-1)s(-1) and 10(3)s(-1), respectively, and that the conformational change to a tight enzyme-inhibitor complex affects the dissociation rate constant by a factor of 10(2)s(-1). Additionally, the acarbose-presenting SPR surfaces could be used as a glucoamylase sensor that allowed rapid, label-free affinity screening of small carbohydrate-based inhibitors in solution, which is otherwise difficult with immobilized enzymes or other proteins.
In the base case, acarbose treatment was slightly dominant over conventional treatment since it achieved improved outcomes at an even lower cost. Sensitivity analysis revealed that acarbose treatment lost dominance due to a moderately positive cost-effectiveness ratio for avoided progression to DM2 in some scenarios. The cost-effectiveness ratio was particularly sensitive to the cost of cardiovascular treatments, the risk of progression to DM2, the daily doses of acarbose, and the publicly funded share of the cost of this drug.
The α-glucosidase inhibitory effect of the crude extract was far better than the standard clinically used drug, acarbose (IC₅₀, 107.31 ± 12.31 µg/ml). A subsequent fractionation of the crude extract was made using solvents of ascending polarity (petroleum ether, chloroform, ethyl acetate, n-butanol and water). The ethyl acetate (IC₅₀, 2.95 ± 0.47 µg/ml) and n-butanol (IC₅₀, 25.80 ± 2.01 µg/ml) fractions which contained predominantly kaempferol (56.7 ± 7.7 µM) and kaempferol 3-O-gentiobioside (50.0 ± 8.5 µM), respectively, displayed the highest carbohydrate enzyme inhibitory effect.
We conducted a population-based cohort study involving people aged 66 or more years who were newly dispensed an oral antidiabetes drug. Individuals who had received acarbose or a thiazolidinedione were excluded. The rate of insulin initiation was calculated by use of the Kaplan-Meier method. Factors associated with insulin initiation were identified by multivariable Cox regression analyses.
In the present study, the preparation, characterization, antioxidant and antidiabetic activities of catechin-grafted chitosan (catechin-g-chitosan) were investigated. The graft of catechin onto chitosan was achieved by redox system and confirmed using various instrumental methods. Proton nuclear magnetic resonance spectroscopy indicates that catechin has been successfully grafted onto chitosan. The morphology observation shows that chitosan changes to a softened nature with porous surface after grafting. Catechin-g-chitosan also exhibits reduced thermal stability and enhanced crystallinity compared to chitosan. Moreover, catechin-g-chitosan shows 0.51 of reducing power, 46.81% of hydroxyl radical-scavenging activity and 67.08% of DPPH radical-scavenging activity at 1mg/ml, which are much higher than that of chitosan. The antidiabetic activity in vitro assays shows that the α-glucosidase inhibitory effect decreases in the order of catechin-g-chitosan>catechin>acarbose>chitosan, and the α-amylase inhibitory effect decreases in the order of acarbose>catechin-g-chitosan>catechin>chitosan. The improved antioxidant and antidiabetic activities of catechin-g-chitosan are attributed to the phenolic groups in the catechin residues.
To determine effects of acarbose on baseline and postprandial serum glucose and insulin concentrations in healthy dogs, if effects of acarbose were dosage related, and if acarbose caused any short-term adverse effects.
Two new sulfonylureas being investigated are repaglinide, which has a rapid onset of action, rapid reversal, and potential usefulness as a preprandial treatment of NIDDM, and glimepiride, the most potent sulfonylurea on a weight basis with an efficacy similar to that for glyburide. Metformin, an orally administered biguanide hypoglycemic agent, decreases blood glucose levels by 50 to 100 mg/dL and consistently improves triglyceride levels. Another agent for NIDDM therapy is acarbose, an a-glucosidase inhibitor. This agent avidly binds to intestinal disaccharidases and limits the postprandial increase in blood glucose. Troglitazone, a member of the thiazolidinedione class of insulin sensitizers, enhances insulin action and lowers blood glucose and blood pressure levels. In overweight patients with diabetes, fenfluramine has been the most effective centrally acting weight reduction agent.
This manuscript provides a comprehensive review of the epidemiologic evidence linking type 2 diabetes (T2D) and its precursor conditions, elevated adiposity and hyperinsulinemia, to dementia. The mechanisms relating these conditions to dementia may be vascular and non-vascular. Elevated adiposity in middle age is related to a higher risk of dementia but the data on this association in old age is conflicting. Several studies have shown that hyperinsulinemia, a consequence of higher adiposity and insulin resistance, is also related to a higher risk of dementia, including late onset Alzheimer's disease (LOAD). Studies have consistently shown a relation of T2D with higher dementia risk, but the associations are stronger for vascular dementia compared to LOAD. A large proportion of the world population may be at increased risk of dementia given the trends for increasing prevalence of overweight, obesity, hyperinsulinemia, and T2D. However, these associations may present a unique opportunity for prevention and treatment of dementia. There are several known modalities that are effective in the prevention and T2D and the reduction of hyperinsulinemia including lifestyle interventions, metformin, thiazolideniodones, and acarbose. Several studies in the prevention and treatment of T2D are currently measuring cognitive outcomes and will provide information on whether T2D treatment and prevention can prevent cognitive decline and dementia.
The inhibitory activity of Cuminum cyminum seed-isolated component was evaluated against lens aldose reductase and alpha-glucosidase isolated from Sprague-Dawley male rats and compared to that of 11 commercially available components derived from C. cyminum seed oil, as well as quercitrin as an aldose reductase inhibitor and acarbose as an alpha-glucosidase inhibitor. The biologically active constituent of C. cyminum seed oil was characterized as cuminaldehyde by various spectral analyses. The IC(50) value of cuminaldehyde is 0.00085 mg/mL against aldose reductase and 0.5 mg/mL against alpha-glucosidase, respectively. Cuminaldehyde was about 1.8 and 1.6 times less in inhibitory activity than acarbose and quercitin, respectively. Nonetheless, cuminaldehyde may be useful as a lead compound and a new agent for antidiabetic therapeutics.
Pistacia integerrima Stewart in traditionally used as folk remedy for various pathological conditions including diabetes. In order to identify the bioactive compound responsible for its folk use in diabetes, a phytochemical and biological study was conducted. Pistagremic acid (PA) was isolated from the dried galls extract of P. integerrima. Strong α-glucosidase inhibitory potential of PA was predicted using its molecular docking simulations against yeast α-glucosidase as a therapeutic target. Significant experimental α-glucosidase inhibitory activity of PA confirmed the computational predictions. PA showed potent enzyme inhibitory activity both against yeast (IC(50): 89.12±0.12μM) and rat intestinal (IC(50): 62.47±0.09μM) α-glucosidases. Interestingly, acarbose was found to be more than 12 times more potent an inhibitor against mammalian (rat intestinal) enzyme (having IC(50) value 62.47±0.09μM), as compared to the microbial (yeast) enzyme (with IC(50) value 780.21μM). Molecular binding mode was explored via molecular docking simulations, which revealed hydrogen bonding interactions between PA and important amino acid residues (Asp60, Arg69 and Asp 70 (3.11Å)), surrounding the catalytic site of the α-glucosidase. These interactions could be mainly responsible for their role in potent inhibitory activity of PA. PA has a strong potential to be further investigated as a new lead compound for better management of diabetes.
Orally taken alpha-glucosidase inhibitors are used for the management of diabetes mellitus. These drugs can prevent the postprandial rise of the blood glucose level by inhibiting the enzymatic digestion of carbohydrates in the intestinal lumen. Non-absorbable inhibitors such as acarbose are expected to function exclusively in the intestine, but absorbable inhibitors such as miglitol may exert an inhibitory effect on non-intestinal alpha-glucosidases present in the various cell types of the body. The potential side-effects of absorbable inhibitors are evaluated in this literature review. It is concluded that there is little risk of inducing unwanted side-effects when miglitol is taken in an oral dose of approximately 1 mg kg-1 body weight. The use of absorbable inhibitors is, however, not advised in case of kidney dysfunction.
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Our preliminary data show add-on OHAs to PR might achieve better early viral kinetics and SVR. However, further larger studies are needed to confirm these findings.
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Glipizide is a second generation sulphonylurea agent that is available in a Gastrointestinal Therapeutic System (GITS) extended-release formulation. Glipizide GITS provides more stable plasma drug concentrations than the immediate-release formulation and the once-daily regimen may optimise patient compliance. In patients with type 2 diabetes mellitus, glipizide GITS is at least as effective as the immediate-release formulation of glipizide in providing glycaemic control, and may have a greater effect on fasting plasma glucose levels. Any therapeutic advantage over other antidiabetic agents remains to be established, but in a preliminary report (n = 40) glipizide GITS provided better glycaemic control and produced less fasting insulinaemia than glibenclamide (glyburide). The incidence of hypoglycaemic symptoms with glipizide GITS is low (< or = 3%). Quality of life was improved compared with baseline after 12 weeks' treatment with glipizide GITS 5 to 20 mg/day plus diet in a US double-blind, placebo-controlled trial in 569 patients with type 2 diabetes mellitus. Hyperglycaemic symptom-related distress decreased with glipizide GITS treatment, while hypoglycaemic symptom-related distress was not significantly increased compared with placebo plus diet. Quality of life during glipizide GITS treatment has not been compared with that during treatment with other antidiabetic agents. Monthly productivity losses related to absenteeism were $US91 (1995 values) per patient lower in the glipizide GITS group compared with the placebo group in the latter prospective study. Productivity parameters improved slightly or did not change significantly in the glipizide GITS group, but deteriorated in the placebo group. Differences in direct healthcare costs between groups were small and not comprehensively reported. Glipizide GITS was the least costly strategy for first-line therapy in a US cost-of-treatment model of the first 3 years after diagnosis of type 2 diabetes mellitus. The total per-patient cost was $US4867 with glipizide GITS, $US5196 with metformin and $US5249 with acarbose (1996/1997 values). Monthly drug acquisition costs were lower, and glycosylated haemoglobin levels and patient compliance were improved, after formulary conversion from the immediate-release to the GITS formulation of glipizide in a US single-hospital retrospective analysis.
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To determine the pharmacokinetics, safety, and tolerability of a novel, controlled-release oral formulation of alpha-lipoic acid (LA) and to investigate whether sustaining the concentration of LA in plasma would have a beneficial effect on glycemic control in patients with type 2 diabetes.
Midgut infusions of sucrose and other disaccharides were compared with monosaccharides for their effects on intestinal mucosal growth in rats otherwise maintained on total parenteral nutrition for 7 days. Mucosal mass progressively increased in a proportional relationship to the concentration of infused sucrose. At equal concentrations by weight, disaccharide infusions stimulated mucosal growth more than monosaccharides. Disaccharide-induced mucosal adaptation was abolished when there was no hydrolysis of the disaccharide. The results suggest that the functional work load of absorbing epithelium, including the "work of hydrolysis," plays an important role in the stimulus for intestinal adaptation.
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The starch-degrading yeast Candida tsukubaensis CBS 6389 secreted amylase at high activity when grown in a medium containing soluble starch. The extracellular alpha-amylase activity was very low. The major amylase component was purified by DEAE-Sephadex A-50 chromatography and Ultrogel AcA 44 gel filtration and characterized as a glucoamylase. The enzyme proved to be a glycoprotein with a molecular weight of 56 000. The glucoamylase had a temperature optimum at 55 degrees C and displayed highest activity in a pH range of 2.4-4.8. Acarbose strongly inhibited the purified glucoamylase. Debranching activity was present as demonstrated by the release of glucose from pullulan.
Fasted subjects received iv insulin infusion to reach plasma glucose 4.4-5.6 mmol/liter. Subjects received iv exenatide (DM2) or saline (DM2 and healthy volunteers), followed by iv glucose challenge.
Slowly Progressive Type 1 Diabetes (SPT1D) is characterized by the absence of insulin dependence at the onset of diabetes and persistent detection of islet cell autoantibodies. These patients with high titers of glutamic acid decarboxylase autoantibodies (GADA) are known to progress to insulin dependence within several years. Low-dose insulin injections have been reported to prevent or delay the decline of insulin secretion in SPT1D patients. We experienced the case of an SPT1D patient with preserved endogenous insulin secretion and good glycemic control achieved with α-glucosidase inhibitor (α-GI) treatment alone for 10 years despite having continuously elevated GADA titers. The details of this case suggest that α-GI treatment might have preventive effects on SPT1D progression.
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To compare the effect of addition of pioglitazone and acarbose to sulphonylureas and metformin therapy on metabolic parameters and on markers of endothelial dysfunction and vascular inflammation in type 2 diabetic patients.
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Lean and obese Zucker rats received a diet containing 10% sucrose for 7 days. A part of the rats was treated with acarbose (15 mg/kg/day in chow). Blood glucose, plasma insulin, lipid peroxides, and as a more specific marker of oxidative stress, 8-isoprostanes, were analyzed. As cellular markers of oxidative stress we determined the activities of mitochondrial aconitase and NADPH-oxidase in aorta, heart, and kidney. In addition, poly(ADP-ribose) polymerase activity (PARP) was measured in aorta.