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Sample records for acarbose

  1. Acarbose

    Science.gov (United States)

    ... Over time, people who have diabetes and high blood sugar can develop serious or life-threatening complications, including ... diet, exercise, quitting smoking), and regularly checking your blood sugar may help to manage your diabetes and improve ...

  2. Acarbose Bioequivalence: Exploration of New Pharmacodynamic Parameters

    OpenAIRE

    Zhang, Min; Yang, Jin; Tao, Lei; Li, Lingjun; Ma, Pengcheng; Fawcett, John Paul

    2012-01-01

    To investigate bioequivalence (BE) testing of an acarbose formulation in healthy Chinese volunteers through the use of recommended and innovative pharmacodynamic (PD) parameters. Following the Food and Drug Administration (FDA) guidance, a randomized, cross-over study of acarbose test (T) and reference (R) (Glucobay®) formulations was performed with a 1-week wash-out period. Preliminary pilot studies showed that the appropriate dose of acarbose was 2 × 50 mg, and the required number of subjec...

  3. Compound list: acarbose [Open TG-GATEs

    Lifescience Database Archive (English)

    Full Text Available acarbose ACA 00116 ftp://ftp.biosciencedbc.jp/archive/open-tggates/LATEST/Human/in_vitro/acar...bose.Human.in_vitro.Liver.zip ftp://ftp.biosciencedbc.jp/archive/open-tggates/LATEST/Rat/in_vitro/acar...bose.Rat.in_vitro.Liver.zip ftp://ftp.biosciencedbc.jp/archive/open-tggates/LATEST/Rat/in_vivo/Liver/Single/acar...-tggates/LATEST/Rat/in_vivo/Liver/Repeat/acarbose.Rat.in_vivo.Liver.Repeat.zip ...

  4. Acarbose bioequivalence: exploration of new pharmacodynamic parameters.

    Science.gov (United States)

    Zhang, Min; Yang, Jin; Tao, Lei; Li, Lingjun; Ma, Pengcheng; Fawcett, John Paul

    2012-06-01

    To investigate bioequivalence (BE) testing of an acarbose formulation in healthy Chinese volunteers through the use of recommended and innovative pharmacodynamic (PD) parameters. Following the Food and Drug Administration (FDA) guidance, a randomized, cross-over study of acarbose test (T) and reference (R) (Glucobay®) formulations was performed with a 1-week wash-out period. Preliminary pilot studies showed that the appropriate dose of acarbose was 2 × 50 mg, and the required number of subjects was 40. Serum glucose concentrations after sucrose administration (baseline) and co-administration of sucrose/acarbose on the following day were both determined. Three newly defined PD measures of glucose fluctuation (glucose excursion (GE), GE' (glucose excursion without the effect of the homeostatic glucose control), and fAUC (degree of fluctuation of serum glucose based on AUC)), the plateau glucose concentration (C(ss)), and time of maximum reduction in glucose concentration (T (max)) were tested in the evaluation. The adequacy of the two parameters recommended by the FDA, ΔC(SG,max) (maximum reduction in serum glucose concentration) and AUEC((0-4h)) (reduction in the AUC((0-4h)) of glucose between baseline and acarbose formulation) was also evaluated. The T (max) values were comparable, and the 90% confidence intervals of the geometric test/reference ratios (T/R) for ΔC(SG,max), C(ss), GE, and fAUC were all within 80-125%. The parameter GE' was slightly outside the limits, and the parameter AUEC((0-4h)) could not be computed due to the presence of negative values. In acarbose BE evaluation, while the recommended parameter ΔC(SG,max) is valuable, the combination of C(ss) and one of the newly defined glucose fluctuation parameters, GE, GE', and fAUC is preferable than AUEC((0-4h)). The acarbose test formulation can be initially considered to be bioequivalent to Glucobay®. PMID:22419151

  5. Important Aspects of Post-Prandial Antidiabetic Drug, Acarbose.

    Science.gov (United States)

    Singla, Rajeev Kumar; Singh, Radha; Dubey, Ashok Kumar

    2016-01-01

    Acarbose, a well known and efficacious α-amylase and α-glucosidase inhibitor, is a postprandial acting antidiabetic drug. DNS-based α-amylase inhibitory assays showed that use of acarbose at concentrations above 125 µg/ml resulted in release of reducing sugar in the reaction, an unexpected observation. Objective of the present study was to design experimental strategies to address this unusual finding. Acarbose was found to be susceptible to thermo-lysis. Further, besides being an inhibitor, it could also be hydrolyzed by porcine pancreatic α-amylase, but had weaker affinity for α - amylase compared to starch. GRIP docking was done for the mechanistic analysis of the active site in the enzyme for substrate, inhibitor and, inhibitor's metabolite (K2). Interaction between acarbose and α-amylase involved significant hydrogen binding compared to that of starch, producing a stronger enzyme-inhibitor complex. Further, docking analysis led us to predict the site on α-amylase where the inhibitor (acarbose) bound more tightly, which possibly affected the binding and hydrolysis of starch exerting its effective anti-diabetic function. PMID:27086787

  6. Influence of gallic acid on α-amylase and α-glucosidase inhibitory properties of acarbose

    Directory of Open Access Journals (Sweden)

    Ganiyu Oboh

    2016-07-01

    Full Text Available Acarbose is an antidiabetic drug which acts by inhibiting α-amylase and α-glucosidase activities but with deleterious side effects. Gallic acid (GA is a phenolic acid that is widespread in plant foods. We therefore investigated the influence of GA on α-amylase and α-glucosidase inhibitory properties of acarbose (in vitro. Aqueous solutions of acarbose and GA were prepared to a final concentration of 25μM each. Thereafter, mixtures of the samples (50% acarbose + 50% GA; 75% acarbose+25% GA; and 25% acarbose+75% GA were prepared. The results revealed that the combination of 50% acarbose and 50% GA showed the highest α-glucosidase inhibitory effect, while 75% acarbose+25% GA showed the highest α-amylase inhibitory effect. Furthermore, all the samples caused the inhibition of Fe2+-induced lipid peroxidation (in vitro in rat pancreatic tissue homogenate, with the combination of 50% acarbose and 50% GA causing the highest inhibition. All the samples also showed antioxidant properties (reducing property, 2,2'-azino-bis (-3-ethylbenzthiazoline-6-sulphonate [ABTS*] and 1,1-diphenyl-2-picrylhydrazyl [DPPH] free radicals scavenging abilities, and Fe2+ chelating ability. Therefore, combinations of GA with acarbose could be employed as antidiabetic therapy, with a possible reduction of side effects of acarbose; nevertheless, the combination of 50% acarbose and 50% GA seems the best.

  7. Kinetic Determination of Acarbose and Miglitol in Bulk and Pharmaceutical Formulations Using Alkaline Potassium Permanganate

    OpenAIRE

    Ibrahim, F. A.; Ali, F. A.; Ahmed, S. M.; Tolba, M. M.

    2007-01-01

    A simple and sensitive kinetic spectrophotometric method was established for the determination of acarbose and miglitol in bulk and in their pharmaceutical preparations using alkaline potassium permanganate as an oxidizing agent. The method involves determination of acarbose and miglitol by kinetic studies of their oxidation at room temperature for a fixed time of 15 minutes for acarbose and 25 minutes for miglitol. The absorbance of the colored manganate ion was measured at 610 nm. Alternati...

  8. Safety and efficacy of acarbose in the treatment of diabetes in Chinese patients

    Directory of Open Access Journals (Sweden)

    He K

    2014-06-01

    Full Text Available Ke He*, Jun-Cheng Shi*, Xiao-Ming Mao Department of Endocrinology, Nanjing First Hospital Affiliated to Nanjing Medical University, Nanjing, People's Republic of China *These authors contributed equally to this work Abstract: Acarbose is an α-glucosidase inhibitor that is commonly used to control postprandial blood glucose. It functions as a competitive and reversible inhibitor of small intestinal brush border glucosidase, blocks the degradation of starch and sucrose, and delays the absorption of glucose and fructose in the alimentary tract. The starch content of a diet might alter the hypoglycemic effects of acarbose because of its mechanism of action. Chinese individuals consume a typical Eastern diet, which is characterized by a high intake of whole grains, legumes, vegetables, fruits, and fish. These dietary habits allow acarbose to be used extensively in the People's Republic of China. Several Chinese-based studies have demonstrated that the use of acarbose as a monotherapy had similar effects on other anti-diabetes agents in decreasing glycosylated hemoglobin (HbA1c and blood glucose levels, and acarbose in combination with other anti-diabetic drugs could further reduce blood glucose and decrease the mean amplitude of glycemic excursions. Importantly, acarbose is safe and well tolerated, with a low incidence of adverse effects. This article provides a comprehensive review of the safety and efficacy of acarbose for the treatment of diabetes in Chinese patients. Keywords: acarbose, α-glucosidase inhibitor, efficacy, safety

  9. Beneficial metabolic effects of nateglinide versus acarbose in patients with newly-diagnosed type 2 diabetes

    Institute of Scientific and Technical Information of China (English)

    Hong-wei GAO; Chao XIE; Hai-ning WANG; Yu-jing LIN; Tian-pei HONG

    2007-01-01

    Aim: To investigate the acute and chronic effects of nateglinide versus acarbose on plasma asymmetric dimethylarginine (ADMA) levels and lipid profiles in patients with newly-diagnosed type 2 diabetes. Methods: A crossover trial of nateglinide and acarbose was conducted on 16 drug-naive patients with newly-diagnosed type 2 diabetes during a total period of 9 weeks. Plasma glucose, serum insulin, free fatty acids (FFA), lipids and lipoproteins, and plasma ADMA were measured. Results: The efficiencies of a single dose of nateglinide (120 mg) and acarbose (50 mg) for lowering postprandial hyperglycemia were similar. Com-pared to acarbose, nateglinide significantly increased postprandial insulin release after a standard meal test in patients with type 2 diabetes. Nateglinide acutely decreased postprandial 120 min FFA concentrations and 240 min ADMA levels more significantly than acarbose. The fasting high-density lipoprotein choles-terol level increased and the low-density lipoprotein cholesterol level decreased significantly, but the fasting levels of triglycerides, total cholesterol, and ADMA were unchanged after 4 weeks of treatment with nateglinide. Acarbose did not affect fasting lipid profiles or the ADMA levels after 4 weeks of treatment.Conclusion: These results suggest that the reduction of postprandial FFA and ADMA concentrations induced by nateglinide may be associated with the partial restoration of early-phase insulin secretion and may impart a cardiovascular advantage in comparison with acarbose.

  10. An investigation of acarbose effects in PCOS women with postprandial hyperglycemia

    Institute of Scientific and Technical Information of China (English)

    郑建淮; 曹缵孙; 陈晓燕; 毛文军

    2002-01-01

    Objectives: To investigate the effects of insulin resistance on serum androgen level and ovulation of women with polycystic ovary syndrome (PCOS) and observe clinic role of acarbose in the treatment of hyperinsulinemia, postprandial hyperglycemia and anovulation. Methods: 14 women accompanied by postprandial hyperglycemia with PCOS were administrated by acarbose for 12 weeks.14 age-matched individuals who had similar body mass index and normal menstruation were served as controls. Results: Serum T levels declined significantly from 4.09±1.04 nmol/L to 1.71±0.54 nmol/L (P<0.001), after acarbose treatment for 12 weeks. 12 out of 14 cases restored ovulation and menstrual cycles after acarbose treatment, among which 4 got pregnant. Conclusion: Acarbose may play a role on reducing postprandial hyperglycemia and HbAic levels, increase ISI and FSG/FI, indirectly reduce serum androgen levels through reducing plasma insulin level and recover ovarian ovulation in PCOS women with postprandial hyperglycemia.

  11. Kinetic determination of acarbose and miglitol in bulk and pharmaceutical formulations using alkaline potassium permanganate.

    Science.gov (United States)

    Ibrahim, F A; Ali, F A; Ahmed, S M; Tolba, M M

    2007-03-01

    A simple and sensitive kinetic spectrophotometric method was established for the determination of acarbose and miglitol in bulk and in their pharmaceutical preparations using alkaline potassium permanganate as an oxidizing agent. The method involves determination of acarbose and miglitol by kinetic studies of their oxidation at room temperature for a fixed time of 15 minutes for acarbose and 25 minutes for miglitol. The absorbance of the colored manganate ion was measured at 610 nm. Alternatively, the kinetic decrease in the absorbance of permanganate upon addition of the studied drugs at 525 nm was also used. The absorbance concentration plot was rectilinear over the concentration range of 4-20 and 1-10 μg/ml for acarbose and miglitol, respectively. The detection limits were 0.189 and 0.089 μg/ml at 610 nm and 0.081 and 0.179 μg/ml at 525 nm for acarbose and miglitol respectively. The method was successfully applied for the determination of these drugs in their dosage forms. The results obtained were in good agreement with those obtained with the reference methods. PMID:23675017

  12. Effects of acarbose on fecal nutrients, colonic pH, and short-chain fatty acids and rectal proliferative indices.

    Science.gov (United States)

    Holt, P R; Atillasoy, E; Lindenbaum, J; Ho, S B; Lupton, J R; McMahon, D; Moss, S F

    1996-09-01

    Acarbose, an alpha-glycosidase inhibitor, treats diabetes mellitus by delaying the digestion and intestinal absorption of dietary carbohydrates. In effective doses, acarbose induces some passage of carbohydrates into the colon. The effect of such chronic carbohydrate transfer on colonic structure and function is unknown. We studied the effects of 1 year of acarbose administration in diabetes mellitus on fecal energy, protein, and fat, including short-chain fatty acids (SCFA) output, fecal pH, and several metabolizing bacterial species. Changes in colonic histology and epithelial cell proliferation were investigated in rectal biopsies. Fecal macronutrient output was unaffected by acarbose, but pH decreased and total SCFA, butyrate, and acetate output were markedly greater. Breath hydrogen output increased after acarbose, but digoxin-metabolizing bacteria and diacylglycerol (DAG) production were unaltered. Compared with the control, acarbose did not induce hyperplasia or change rectal proliferation. However, total fecal SCFA and butyrate output correlated inversely with proliferation in the rectal upper crypt-a biomarker of risk for colonic neoplasia. In conclusion, long-term acarbose administration does not adversely affect colonic function or fecal nutrient output. If increased fecal SCFA and butyrate reduces upper-crypt proliferation, then acarbose may reduce the risk of colonic neoplasia. PMID:8781308

  13. Acarbose reduces the risk of pre-lunch hypoglycemia in elderly people with diabetes eating rice porridge for breakfast.

    Science.gov (United States)

    Hsieh, Ching Jung

    2010-09-01

    To decrease the risk of postprandial hyperglycemia and late hypoglycemia in elderly people with diabetes who eat rice porridge for breakfast, we administered 50mg acarbose to 30 elderly people with type 2 diabetes. The results demonstrated that acarbose could prevent the fluctuations in post-breakfast blood glucose levels.

  14. Inhibitory effect and mechanism of acarbose combined with gymnemic acidon maltose absorption in rat intestine

    Institute of Scientific and Technical Information of China (English)

    Hong Luo; Le Feng Wang; Toshiaki Imoto; Yasutaka Hiji

    2000-01-01

    AIM The control of diet regimen and nutrient intake, aiming to avoid the evaggerated levels of glucose andanabolic hormone is broadly accepted as basic treatment of diabetes mellitus. Maltose is an importanthydrolysate of starch, main source of nutrition. Acarbose is an alpha-D-glucosidase inhibitor but with a shortinhibitory duration. Gymnemic acid (GA), a group of triterpene glucuronides, inhibits glucose absorptionwith a longer effective duration but it needs a longer time to achieve its maximum effect. To determinewhether nutrient control in diabetic care can be improved by combination of them, we compared thecombinative and individual effect of acarbose and GA on maltose absorption and hydrolysis in smallintestine.METHODS The absorption and hydrolysis of maltose were studied by re-cyclic perfusion of intestinal loopsin situ and motility of the intestine was recorded with the intestinal loop in vitro, of Wistar rat.RESULTS The total inhibitory rate of maltose absorption was improved by the combination of GA (0.1 -1.0 mg/mL) and acarbose (0.1- 2.0 mmol/L) throughout their effective duration (P<0.05, U test ofMann-Whitney), although the improvement only could be seen in the low dosages during the first hour. Withthe combination, inhibitory duration of acarbose on maltose absorption was prolonged to 3 hours and theonset of GA inhibitory effect was fastened to 15 minutes. GAsuppressed the intestinal mobility with a goodcorrelation (r = 0.98) to the inhibitory effect of GA on maltose absorption and the inhibitory effect of2 mmol/L (higher dose) acarbose on maltose hydrolysis was dual modulated by 1 mg/mL GA in vivoindicating that the combined effects involved the functional alteration of intestinal barriers.CONCLUSION There are augmented effects of acarbose and GA, which involve pre-cellular andparacellular barriers. Furthermore, diabetic care can be improved by employing this combination.

  15. Effects of acarbose (Glucobay) in persons with type 1 diabetes : a multicentre study

    NARCIS (Netherlands)

    Sels, J P; Verdonk, H E; Wolffenbuttel, B H

    1998-01-01

    The aim of this multicentre study was to investigate the effect--in everyday life--of long term administration of acarbose on parameters of glycaemic control, daily insulin requirements, lipid parameters and tolerability in ambulant type 1 diabetic subjects insufficiently controlled with diet and in

  16. Improved glycemic control by acarbose therapy in hypertensive diabetic patients: effects on blood pressure and hormonal parameters

    Directory of Open Access Journals (Sweden)

    Rosenbaum P.

    2002-01-01

    Full Text Available A double-blind, randomized, placebo-controlled study was carried out on 44 hypertensive type 2 diabetic subjects previously treated by diet associated or not with sulfonylurea to assess the effects of acarbose-induced glycemic control on blood pressure (BP and hormonal parameters. Before randomization and after a 22-week treatment period (100 to 300 mg/day, the subjects were submitted to a standard meal test and to 24-h ambulatory BP monitoring (ABPM and had plasma glucose, glycosylated hemoglobin, lipid profile, insulin, proinsulin and leptin levels determined. Weight loss was found only in the acarbose-treated group (75.1 ± 11.6 to 73.1 ± 11.6 kg, P<0.01. Glycosylated hemoglobin decreased only in the acarbose group (6.4 ± 1.7 to 5.6 ± 1.9%, P<0.05. Fasting proinsulin decreased only in the acarbose group (23.4 ± 19.3 to 14.3 ± 13.6 pmol/l, P<0.05, while leptin decreased in both (placebo group: 26.3 ± 6.1 to 23.3 ± 9.4 and acarbose group: 25.0 ± 5.5 to 22.7 ± 7.9 ng/ml, P<0.05. When the subset of acarbose-treated patients who improved glycemic control was considered, significant reductions in diurnal systolic, diastolic and mean BP (102.3 ± 6.0 to 99.0 ± 6.6 mmHg, P<0.05 were found. Acarbose monotherapy or combined with sulfonylurea was effective in improving glycemic control in hypertensive diabetic patients. Acarbose-induced improvement in metabolic control may reduce BP in these patients. Our data did not suggest a direct action of acarbose on insulin resistance or leptin levels.

  17. Efficacy and safety of acarbose in the treatment of elderly patients with postprandial hypotension

    Institute of Scientific and Technical Information of China (English)

    JIAN Zai-jin; ZHOU Bai-yu

    2008-01-01

    Background Postprandial hypotension (PPH) occurs frequently in elderly people and may lead to syncope, falls, dizziness, weakness, angina pectoris, and stroke. Some studies suggest that the magnitude of the postprandial fall in blood pressure (BP) is influenced by the rate at which glucose enters the small intestine. We hypothesized that acarbose (a-glucosidase inhibitor), a hypoglycemic agent that decreases the rate of glucose absorption in the small intestine, would attenuate PPH in the elderly, and would be safe in the treatment.Methods Forty-three elderly in-patients with PPH were recruited. All of them were in relatively stable conditions. They had semi-liquid standard meals without and with acarbose for the two following days: screening day and intervention day. Blood pressure and heart rate (HR) were recorded at baseline and every 15 minutes for 120 minutes using a non-invasive ambulatory blood pressure monitoring system during the study, and ejection fraction (EF) and fractional shortening (FS) were measured by two dimensional echocardiography.Results Compared with the screening day, the falls in systolic, diastolic and mean arterial blood pressure (SBP, DBP, MAP) (all P<0.05) were significantly attenuated after taking acarbose during breakfast, so were MAP (P<0.05) during lunch, DBP (P<0.05) and MAP (P<0.05) during supper. The change of HR was not statistically significant after taking acarbose in three meals. EF and FS were positively correlated with the relief rate. The effective power was 63%, and the incidence of adverse drug reaction (ADR) was 9%. Conclusion Acarbose is effective and safe in the treatment of elderly patients with PPH.

  18. STUDY ON EFFICACY OF ACARBOSE (WITH AND WITHOUT CORNSTARCH DIET IN COMPARISON WITH ROSIGLITAZONE IN DIABETIC RATS

    Directory of Open Access Journals (Sweden)

    Khatoon Humera

    2013-02-01

    Full Text Available The aim of this study is to compare metabolic effects of acarbose and rosiglitazone, especially in controlling hyperglycemia and hypercholesterolemia. We have selected acarbose and rosiglitazone for the present study among various currently approved oral hypoglycemics. As diet is also an important component in diabetic therapy, effects of resistant starch diets (e.g. cooked cornstarch on carbohydrate and lipid metabolism were also studied.The metabolic effects of the drugs were investigated and significant changes with respect to blood glucose levels, HbA1c along with lipids profile of drug-treated animals were compared with untreated animal after 7, 15 and 30 days. The experimental result showed excellent glycemic control when acarbose was administered alone. Acarbose along with cooked cornstarch diet produced a more favorable lipid profile, but with significant increased level (p<0.001 of triglycerides. These findings suggest that acarbose and acarbose along with cooked cornstarch are more effective in controlling hyperglycemia with more favorable lipid profile when compared with rosiglitazone.

  19. INFLUENCE OF ACARBOSE ON POSTPRANDIAL DYSMETABOLISM: RESULTS OF AN OPEN-LABEL RANDOMIZED STUDY

    OpenAIRE

    A. Ya. Cherniak; I. M. Petrov; I V Medvedeva

    2015-01-01

    Aim. To evaluate postprandial changes of lipid and glucose profiles, inflammation markers levels and flow-mediated vasodilatation in patients with metabolic syndrome (MS) and to estimate acarbose course treatment efficacy in glucose intolerant patients.Material and methods. A total of 114 MS patients (83 men, 31 women) were examined, MS was associated with impaired glucose tolerance (IGT) in 55 cases. At the first stage postpran- dial dynamics of flow-mediated dilation (FMD), lipid profile pa...

  20. Acarbose, lente carbohydrate, and prebiotics promote metabolic health and longevity by stimulating intestinal production of GLP-1.

    Science.gov (United States)

    McCarty, Mark F; DiNicolantonio, James J

    2015-01-01

    The α-glucosidase inhibitor acarbose, which slows carbohydrate digestion and blunts postprandial rises in plasma glucose, has long been used to treat patients with type 2 diabetes or glucose intolerance. Like metformin, acarbose tends to aid weight control, postpone onset of diabetes and decrease risk for cardiovascular events. Acarbose treatment can favourably affect blood pressure, serum lipids, platelet aggregation, progression of carotid intima-media thickness and postprandial endothelial dysfunction. In mice, lifetime acarbose feeding can increase median and maximal lifespan-an effect associated with increased plasma levels of fibroblast growth factor 21 (FGF21) and decreased levels of insulin-like growth factor-I (IGF-I). There is growing reason to suspect that an upregulation of fasting and postprandial production of glucagon-like peptide-1 (GLP-1)-stemming from increased delivery of carbohydrate to L cells in the distal intestinal tract-is largely responsible for the versatile health protection conferred by acarbose. Indeed, GLP-1 exerts protective effects on vascular endothelium, the liver, the heart, pancreatic β cells, and the brain which can rationalise many of the benefits reported with acarbose. And GLP-1 may act on the liver to modulate its production of FGF21 and IGF-I, thereby promoting longevity. The benefits of acarbose are likely mimicked by diets featuring slowly-digested 'lente' carbohydrate, and by certain nutraceuticals which can slow carbohydrate absorption. Prebiotics that promote colonic generation of short-chain fatty acids represent an alternative strategy for boosting intestinal GLP-1 production. The health benefits of all these measures presumably would be potentiated by concurrent use of dipeptidyl peptidase 4 inhibitors, which slow the proteolysis of GLP-1 in the blood. PMID:25685364

  1. Comparison of Acarbose and Metformin on Albumin Excretion in Patients With Newly Diagnosed Type 2 Diabetes: A Randomized Controlled Trial.

    Science.gov (United States)

    Pan, Qingrong; Xu, Yuan; Yang, Ning; Gao, Xia; Liu, Jia; Yang, Wenying; Wang, Guang

    2016-04-01

    Increased urinary albumin excretion in diabetes not only signals nephropathy but also serves as a risk marker for cardiovascular disease. The data of MARCH (Metformin and AcaRbose in Chinese as the initial Hypoglycaemic treatment) trial demonstrated that acarbose and metformin were similarly efficacious at lowering blood glucose and blood pressure, as well as improving insulin sensitivity in Chinese patients newly diagnosed with type 2 diabetes mellitus. The purpose of this study was to identify the effects of acarbose and metformin therapy on albumin excretion in MARCH study.Baseline urine albumin/creatinine ratio (ACR) of 762 newly diagnosed, drug-naïve patients with type 2 diabetes mellitus was measured. Included patients were randomized to receive either acarbose or metformin and followed for 48 weeks. In addition to change in ACR, the estimated glomerular filtration rates (eGFR) and frequency of metabolic syndrome (MetS) were also assessed.Elevated ACR levels (≥30 mg/g) were present at baseline in 21.9% of all participants. A significant decline in urine ACR was observed in both the acarbose and metformin groups at week 24 and 48 (all P metformin (P = 0.01). Both acarbose and metformin significantly decreased the frequency of MetS at week 24 and 48 (both P metformin decreased urine ACR levels and reduced the frequency of elevated ACR and MetS in Chinese patients with newly diagnosed type 2 diabetes mellitus without affecting eGFR. After 48 weeks' intervention, acarbose therapy resulted in a greater reduction in urine ACR compared with metformin.

  2. Acute effects of acarbose on post-prandial glucose and triglycerides in type 2 diabetics following intake of different Malaysian foods.

    Science.gov (United States)

    Nawawi, H M; Yazid, T N; Ismail, F; Khalid, B A

    2000-03-01

    Acarbose inhibits intestinal alpha-glucosidases resulting in diminished and delayed postprandial hyperglycaemia (PPH). Studies on effects of acarbose on postprandial lipaemia (PPL) have been inconclusive. Little is known about the effects of acarbose on PPH and PPL following intake of a polysaccharide diet. We studied 30 type 2 diabetic patients on dietary and/or oral hypoglycaemic agent(s). Thirty patients were recruited for food A (nasi lemak), 28 for food B (mee goreng) and 28 for food C (roti telur), which represent the typical diets of the three main races in Malaysia. Serial blood samples were taken at 15 min before and up to 240 min after each food intake, without acarbose. Subsequently, three doses of 50 mg acarbose were given orally and the same procedure was repeated the following day. There were significantly lower mean increments in plasma glucose levels after compared to before acarbose treatment 30, 45 and 60 min for food A and at 30, 45, 60, 120, 180 and 240 min for food C, but no significant difference was noted for food B. There was a significantly lower mean fasting glucose level after compared with before acarbose treatment following intake of food A and C but not food B. Short-term treatment with acarbose caused significant diminished and delayed PPH response with food A and C but not with food B. Acarbose was more effective in reducing PPH response in polysaccharide foods with a higher and earlier postprandial glucose peak than in those with a lower and lagged peak. There were no significant differences in the mean fasting or postprandial triglyceride levels before and after acarbose treatment, following intake of all three foods for up to 4 hours. Depending on the food absorption pattern, overnight low dose treatment with acarbose leads to diminished fasting and peak plasma glucose levels, and delayed PPH but insignificant reduction in postprandial lipaemia in poorly controlled type 2 diabetics following intake of racially different Malaysian

  3. Acute effects of acarbose on post-prandial glucose and triglycerides in type 2 diabetics following intake of different Malaysian foods.

    Science.gov (United States)

    Nawawi, H M; Yazid, T N; Ismail, F; Khalid, B A

    2000-03-01

    Acarbose inhibits intestinal alpha-glucosidases resulting in diminished and delayed postprandial hyperglycaemia (PPH). Studies on effects of acarbose on postprandial lipaemia (PPL) have been inconclusive. Little is known about the effects of acarbose on PPH and PPL following intake of a polysaccharide diet. We studied 30 type 2 diabetic patients on dietary and/or oral hypoglycaemic agent(s). Thirty patients were recruited for food A (nasi lemak), 28 for food B (mee goreng) and 28 for food C (roti telur), which represent the typical diets of the three main races in Malaysia. Serial blood samples were taken at 15 min before and up to 240 min after each food intake, without acarbose. Subsequently, three doses of 50 mg acarbose were given orally and the same procedure was repeated the following day. There were significantly lower mean increments in plasma glucose levels after compared to before acarbose treatment 30, 45 and 60 min for food A and at 30, 45, 60, 120, 180 and 240 min for food C, but no significant difference was noted for food B. There was a significantly lower mean fasting glucose level after compared with before acarbose treatment following intake of food A and C but not food B. Short-term treatment with acarbose caused significant diminished and delayed PPH response with food A and C but not with food B. Acarbose was more effective in reducing PPH response in polysaccharide foods with a higher and earlier postprandial glucose peak than in those with a lower and lagged peak. There were no significant differences in the mean fasting or postprandial triglyceride levels before and after acarbose treatment, following intake of all three foods for up to 4 hours. Depending on the food absorption pattern, overnight low dose treatment with acarbose leads to diminished fasting and peak plasma glucose levels, and delayed PPH but insignificant reduction in postprandial lipaemia in poorly controlled type 2 diabetics following intake of racially different Malaysian

  4. Effect of Acarbose on Long-Term Prognosis in Acute Coronary Syndromes Patients with Newly Diagnosed Impaired Glucose Tolerance

    Directory of Open Access Journals (Sweden)

    Peng Yun

    2016-01-01

    Full Text Available Objective. To investigate the effect of acarbose therapy on the long-term prognosis of patients with acute coronary syndromes (ACS complicating newly diagnosed impaired glucose tolerance (IGT. Methodology. 135 patients hospitalized for ACS who had been newly diagnosed with IGT were randomly assigned to acarbose group (150 mg/day, n=67 or control group (no acarbose, n=68. All cases in each group were given the same elementary treatment. Mean follow-up was 2.3 years. The incidence of major adverse cardiovascular event (MACE and carotid intima-middle thickness (CIMT were statistically analyzed. Results. During the mean follow-up of 2.3 years, the risk of recurrent MACE in acarbose group was decreased significantly compared with that in control group (26.67% versus 46.88%, P<0.05; at the same time, thickening of the CIMT was significantly slower than the control group ((1.28 ± 0.42 mm versus (1.51 ± 0.64 mm, P<0.05. Conclusions. Acarbose can effectively reduce the risk of MACE in ACS patients with newly diagnosed IGT, simultaneously retarding the progression of carotid intima-media thickness.

  5. Acarbose Treatment and the Risk of Cardiovascular Disease in Type 2 Diabetic Patients: A Nationwide Seven-Year Follow-Up Study

    Directory of Open Access Journals (Sweden)

    Jui-Ming Chen

    2014-01-01

    Full Text Available Objective. To investigate the potential benefits of acarbose treatment on cardiovascular disease (CVD in patients with type 2 diabetes by using nationwide insurance claim dataset. Research Design and Methods. Among 644,792 newly diagnosed type 2 diabetic patients without preexisting CVD in a nationwide cohort study, 109,139 (16.9% who had received acarbose treatment were analyzed for CVD risk. Those with CVD followed by acarbose therapy were also subjected to analysis. Result. During 7 years of follow-up, 5,081 patients (4.7% developed CVD. The crude hazard ratio (HR and adjusted HR were 0.66 and 0.99, respectively. The adjusted HR of CVD was 1.19, 0.70, and 0.38 when the duration of acarbose use was 24 months, respectively. Adjusted HR was 1.14, 0.64, and 0.41 with acarbose cumulative doses 109,500 mg, respectively. Conclusion. In patients with type 2 diabetes without preexisting CVD, treatment with acarbose showed a transient increase in incidence of CVD in the initial 12 months followed by significant reductions of CVD in prolonged acarbose users. After the first CVD events, continuous use of acarbose revealed neutral effect within the first 12 months. The underlying mechanisms require further investigations.

  6. Kinetic analysis of inhibition of glucoamylase and active site mutants via chemoselective oxime immobilization of acarbose on SPR chip surfaces

    DEFF Research Database (Denmark)

    Sauer, Jørgen; Abou Hachem, Maher; Svensson, Birte;

    2013-01-01

    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 104M−1s−1 and 103s−1, respectively, and that the conformational change to a tight enzyme–inhibitor complex affects the dissociation rate constant by a factor of 102s−1. Additionally...

  7. INFLUENCE OF ACARBOSE ON POSTPRANDIAL DYSMETABOLISM: RESULTS OF AN OPEN-LABEL RANDOMIZED STUDY

    Directory of Open Access Journals (Sweden)

    A. Ya. Cherniak

    2015-09-01

    Full Text Available Aim. To evaluate postprandial changes of lipid and glucose profiles, inflammation markers levels and flow-mediated vasodilatation in patients with metabolic syndrome (MS and to estimate acarbose course treatment efficacy in glucose intolerant patients.Material and methods. A total of 114 MS patients (83 men, 31 women were examined, MS was associated with impaired glucose tolerance (IGT in 55 cases. At the first stage postpran- dial dynamics of flow-mediated dilation (FMD, lipid profile parameters, inflammation markers and insulin levels were estimated. At the second stage patients with MS and IGT (n=55 were randomly assigned to the two groups of treatment. Patients of the first group (n=28 had non-drug treatment. Patients of the second group (n=27 received acarbose 300 mg/day for 3 months in addition to recommendations for lifestyle change. 3 months later postprandial values of lipid and glucose profiles parameters, inflammation markers levels and FMD were reassessed. Results. MS patients with IGT revealed maximal disorders in metabolic parameters during postprandial period: increase in the plasma levels of total cholesterol by 6.1%, high density lipoproteins – by 1.7%, and triglycerides – by 27.87%, increase in atherogenic index by 4.8%, and plasma concentrations of glucose – by 54.7%, insulin – by 30.2%, HOMA index – by 73.3%, as well as concentrations of C-reactive protein (CRP – by 49.7%, tumor necrose factor alpha – by 20.8%, and interleukin-6 (IL-6 – by 51.9%. FMD decreased by 34.3%.After 12 weeks of the acarbose treatment we had revealed positive dynamics of studied indices in postprandial period as compared to an only non-drug management: levels of glucose in- creased by 24.1% vs 44.4%, insulin – by 14.4% vs 24.4%, CRP – by 19.9% vs 36.6%, IL-6 – by 25.1% vs 41.7%; postprandial FMD decreased by 18.9% vs 31.1%.Conclusion. Prescription of acarbose 300 mg/day for 12 weeks in glucose intolerant patients is characterized

  8. Effect of basal insulin combined with acarbose on blood glucose level and complications in patients with newly diagnosed elderly diabetes

    Institute of Scientific and Technical Information of China (English)

    Yu-Qing Guo; Chen-Ru Zhang; Ai-Ge Yang; Fan Liu; Shan-Shan Dong; Yan Kang

    2016-01-01

    Objective:To analyze the effect of basal insulin combined with acarbose on blood glucose level and complications in patients with newly diagnosed elderly diabetes.Methods:A total of 135 cases of patients with newly diagnosed elderly diabetes who were treated in our hospital from July 2012 to January 2015 were enrolled as research subjects and divided into observation group 66 cases and control group 69 cases according to different treatment methods. Control group received acarbose therapy alone, observation group received basal insulin combined with acarbose therapy, and then differences in blood glucose level, oxidative stress indicators, nerve conduction velocity, vascular injury and inflammatory factor levels of two groups were compared.Results:FPG, 2hPG and HbA1C levels of observation group after treatment were lower than those of control group; AGE-P, MDA and NADPH levels were lower than those of control group, and SOD level was higher than that of control group; median MNCV, ulnar MNCV, tibial MNCV, median SNCV and sural SNCV levels were higher than those of control group; sVCAM-1, hs-CRP and IL-6 levels were lower than those of control group. Conclusion:Basal insulin combined with acarbose therapy for patients with newly diagnosed elderly diabetes can effectively optimize the levels of blood glucose and complication-related factors, and it has active clinical significance.

  9. Structure of Bacillus halmapalus alpha-amylase crystallized with and without the substrate analogue acarbose and maltose

    DEFF Research Database (Denmark)

    Lyhne-Iversen, Louise; Hobley, Timothy John; Kaasgaard, Svend G.;

    2006-01-01

    Recombinant Bacillus halmapalus alpha-amylase (BHA) was studied in two different crystal forms. The first crystal form was obtained by crystallisation of BHA at room temperature in the presence of acarbose and maltose - data was collected at cryogenic temperatures to a resolution of 1.9 Å...

  10. Acarbose improves glycemic control and reduces body weight: Subanalysis data of South Asia region

    Directory of Open Access Journals (Sweden)

    S Kalra

    2013-01-01

    Full Text Available Alpha-glucosidase inhibitors (AGIs are widely used especially in Asian countries as a treatment option for type 2 diabetes patients with high postprandial glycaemia. However, data from South Asia region is very limited. In order to examine the effect of AGI in real-life setting, 10 PMS/NIS from all over the world from the launch of acarbose to date were pooled in one database and exploratory analysis was performed for glycemic parameters and weight. In total 62,905 patients were pooled from 21 countries and regions. Mean follow up (± SD was 12.2 ± 4.8 weeks (range 0.1-108.9. From South Asia region (India and Pakistan, 8,738 Asian patients were enrolled. Mean PPG decreased from 240.0 and 261.1 mg/dl at baseline by 70.26 ± 65.10 and 82.96 ± 56.59 mg/dl at the last visit in total and South Asian populations, respectively (n = 53,883; n = 7,991, P < 0.0001 for both. Mean FPG decreased from 171.6 and 176.5 mg/dl at baseline by 38.48 ± 47.83 and 49.59 ± 41.41 mg/dl at the last visit in total and South Asian populations, respectively (n = 56,672; n = 7,837, P < 0.0001 for both. Mean HbA1c decreased from 8.4 and 8.4% at baseline by 1.11 ± 1.31% and 0.91 ± 0.93% at the last visit in total and South Asian populations, respectively (n = 38,843; n = 2,343, P < 0.0001 for both. Mean relative reduction of body weight (BW was 1.40 ± 3.28% and 1.10 ± 3.39% at the last visit for mean baseline BW 73.6 and 74.2 kg in total and South Asian populations, respectively (n = 54,760; n = 7,718, P < 0.0001 for both. Consistent with RCT meta-analyses, post-hoc analysis of real-life data showed acarbose treatment improved glycaemic control and reduced the BW. Acarbose treatment in real life setting showed significant reductions in all glycemic parameters and BW in Asian patients from South Asia region.

  11. An observational study of acarbose treatment in patients with type 2 diabetes from the Middle East and Morocco

    Directory of Open Access Journals (Sweden)

    Shihabi AR

    2013-04-01

    Full Text Available Abdul R Shihabi,1 Essam M Moussa,2 Hania Sobierajska,3 Birgit Schmidt4 1Al Ain Centre, Dubai, United Arab Emirates; 2New Jeddah Hospital, Jeddah, Saudi Arabia; 3Etihad Airways Medical Centre, Abu Dhabi, United Arab Emirates; 4Bayer Schering Pharma AG, Leverkusen, Germany Background: The prevalence of type 2 diabetes is increasing dramatically in the Middle East and North Africa region. However, there are few trials that have determined the effect of antidiabetic treatment in an observational setting in these countries. Methods: This was a noninterventional study performed in Morocco in 2006–2007 and in the Middle East in 2005–2006 to observe the efficacy and safety of acarbose in patients with pretreated or untreated type 2 diabetes. Glycemic parameters (fasting blood glucose, one-hour postprandial blood glucose, and HbA1c were recorded within a 3-month period. The observation period included an initial visit at the start of acarbose therapy and up to three follow-ups. Results: Acarbose was effective in reducing glycemic parameters in patients from Morocco (n = 1082 and the Middle East (n = 1737. The mean one-hour postprandial blood glucose decreased by 35.5% to 165.4 ± 47.9 mg/dL in the Middle East and by 35.5% to 179.0 ± 49.9 mg/dL in Morocco. Mean fasting blood glucose decreased by 30.8% to 126.6 ± 34.2 mg/dL (Middle East and by 34.5% to 150.6 ± 47.1 mg/dL (Morocco. The absolute reduction in HbA1c was 1.3% in the Middle East (final value 7.4% and 1.0% in Morocco (final value 7.5%. Overall, 107 patients (Middle East and 26 patients (Morocco experienced minor drug-related adverse events, which were mainly gastrointestinal. The tolerability of acarbose was rated as very good/good by 80.8% in the Middle East and by 68.6% in Morocco. Conclusion: This study illustrates the efficacy and safety of acarbose in the treatment of type 2 diabetic patients in an observational setting. Keywords: type 2 diabetes, acarbose, Glucobay®, Glucor

  12. Evaluation of effect of acarbose consumption on weight losing in non-diabetic overweight or obese patients in Kerman

    Directory of Open Access Journals (Sweden)

    Akram Nakhaee

    2013-01-01

    Full Text Available Background: High prevalence of obesity and the importance of this issue as a risk factor for chronic diseases such as severe cardiovascular diseases, diabetes, and cancer necessitate the need for treatment. The aim of this study was the evaluation of acarbose effect on the weight loss in non diabetic overweight or obese patients in Kerman. Materials and Methods: A double blind randomized controlled clinical trial was performed on 66 patients with the body mass index (BMI between 25 and 35 kg/m2. Patients were divided in treatment and control groups using the randomization. The treatment group took 100 mg acarbose 3 times a day for 20 weeks in combination with the low calorie diet and exercise. Control group was given placebo, low calorie diet, and exercise. BMI was measured after 20 weeks. The analyses were carried out using t test and repeated measured ANOVA. Results: Patients in acarbose and placebo group had a non significant difference in BMI at baseline. Reducing in weight was considered in every month in both groups, but this reduction was higher in the treatment group. At the 5th month, the difference of BMI in the treatment group was significantly lower than the placebo group (2.31 ± 0.6 vs. 0.76 ± 0.6 kg/m2, P < 0.001. Conclusion: Acarbose, especially in combination with the low calorie diet and exercise, seems to lose weight effectively in obese and overweight patients in communities that have a high carbohydrate intake (like Persian diet.

  13. Utility of an oxidation reaction for the spectrophotometric determination of acarbose in controlled release tablets at various simulated gastrointestinal media.

    Science.gov (United States)

    Sinha, Vivek Ranjan; Kumar, Ruchita V

    2012-01-01

    A sensitive kinetic method for spectrophotometric determination of acarbose is developed and validated for the determination of the drug in bulk and pharmaceutical formulations. The drug was estimated in simulated gastrointestinal media i.e., 0.1 M HCl (pH 1.2) and phosphate buffer (pH 6.8). The method involves the oxidation of acarbose by treating it with a strong oxidizing agent (potassium permanganate (1 x 10(-2) M)) in alkaline media. The reaction kinetics was determined for 20 min at room temperature. The reaction followed first order kinetics and the absorbance of the corresponding manganate ions produced was determined at 610 nm. The absorbance-concentration plot was found to be rectilinear over the concentration range of 2-20 microg/mL. The proposed method was used for estimation of the drug in a novel controlled release dosage form. Thus, the method developed was simple, reproducible and can be successfully applied for the determination of the drug in simulated gastrointestinal fluid. PMID:22574503

  14. Transglycosylation reactions of Bacillus stearothermophilus maltogenic amylase with acarbose and various acceptors

    International Nuclear Information System (INIS)

    It was observed that Bacillus stearothermophilus maltogenic amylase cleaved the first glycosidic bond of acarbose to produce glucose and a pseudotrisaccharide (PTS) that was transferred to C-6 of the glucose to give an α-(1-6) glycosidic linkage and the formation of isoacarbose. The addition of a number of different carbohydrates to the digest gave transfer products in which PTS was primarily attached α-(1-6) to d-glucose, d-mannose, d-galactose, and methyl α-d-glucopyranoside. With d-fructopyranose and d-xylopyranose, PTS was linked α-(1-5) and α-(1-4), respectively. PTS was primarily transferred to C-6 of the nonreducing residue of maltose, cellobiose, lactose, and gentiobiose. Lesser amounts of α-(1-3) and/or α-(1-4) transfer products were also observed for these carbohydrate acceptors. The major transfer product to sucrose gave PTS linked α-(1-4) to the glucose residue. α,α-Trehalose gave two major products with PTS linked α-(1-6) and α-(1-4). Maltitol gave two major products with PTS linked α-(1-6) and α-(1-4) to the glucopyranose residue. Raffinose gave two major products with PTS linked α-(1-6) and α-(1-4) to the d-galactopyranose residue. Maltotriose gave two major products with PTS linked α-(1-6) and α-(1-4) to the nonreducing end glucopyranose residue. Xylitol gave PTS linked α-(1-5) as the major product and d-glucitol gave PTS linked α-(1-6) as the only product. The structures of the transfer products were determined using thin layer-chromatography, high-performance ion chromatography, enzyme hydrolysis, methylation analysis and 13C NMR spectroscopy. The best acceptor was gentiobiose, followed closely by maltose and cellobiose, and the weakest acceptor was d-glucitol. (Copyright (c) 1998 Elsevier Science B.V., Amsterdam. All rights reserved.)

  15. Randomized, Double-Blinded, Double-Dummy, Active-Controlled, and Multiple-Dose Clinical Study Comparing the Efficacy and Safety of Mulberry Twig (Ramulus Mori, Sangzhi) Alkaloid Tablet and Acarbose in Individuals with Type 2 Diabetes Mellitus

    Science.gov (United States)

    Chen, Yao

    2016-01-01

    Aims. To evaluate the efficacy and safety of mulberry twig alkaloid (SZ-A) tablet compared with acarbose in patients with type 2 diabetes. Methods. This clinical trial enrolled 38 patients who were randomized into two groups (SZ-A: 23; acarbose: 15) and were treated for 24 weeks. Patients and clinical trial staffs were masked to treatment assignment throughout the study. The primary outcome measures were glycated hemoglobin (HbA1c) and 1-hour and 2-hour postprandial and fasting plasma glucose levels from baseline to the end of treatment. Analysis included all patients who completed this study. Results. By the end of this study, HbA1c level in SZ-A group was decreased from baseline significantly (P < 0.001). No significant difference was found when compared with acarbose group (P = 0.652). Similarly, 1-hour and 2-hour postprandial plasma glucose levels in SZ-A group were decreased from baseline statistically (P < 0.05), without any significant differences compared with acarbose group (P = 0.748 and 0.558, resp.). The fasting plasma glucose levels were not significantly changed in both groups. One of 23 patients in SZ-A group (4.76%) and 5 of 15 patients in acarbose group (33.33%) suffered from gastrointestinal adverse events. Conclusions. Compared with acarbose, SZ-A tablet was effective and safe in glycemic control in patients with type 2 diabetes. PMID:27547230

  16. Alpha-glucosidase inhibitor, acarbose, improves glycamic control and reduces body weight in type 2 diabetes: Findings on indian patients from the pooled data analysis

    Directory of Open Access Journals (Sweden)

    Sanjay Kalra

    2013-01-01

    Full Text Available Alpha-glucosidase inhibitors are widely used especially in Asian countries as a treatment option for type 2 diabetes patients with high postprandial glycemia (PPG. The higher carbohydrate in the Indian diets lead to greater prandial glycemic excursion, increased glucosidase, and incretin activity in the gut and may need special therapeutic strategies to tackle these glucose peaks. This is the subgroup analysis of Indian subjects who participated in the GlucoVIP study that investigated the effectiveness and tolerability of acarbose as add-on or monotherapy in a range of patients with type 2 diabetes mellitus. A total of 1996 Indian patients were included in the effectiveness analysis. After 12.5 weeks (mean, the mean change in 2-hour PPG from baseline was −74.4 mg/dl, mean HbA1c decreased by -1.0%, and mean fasting blood glucose decreased by -37.9 mg/dl. The efficacy of acarbose was rated "very good" or "good" in 91.1% of patients, and tolerability as "very good" or "good" in 88.0% of patients. The results of this observational study suggest that acarbose was effective and well tolerated in the Indian patients with T2DM.

  17. alpha-Glucosidase inhibition (acarbose) fails to enhance secretion of glucagon-like peptide 1 (7-36 amide) and to delay gastric emptying in Type 2 diabetic patients

    DEFF Research Database (Denmark)

    Hücking, K; Kostic, Z; Pox, C;

    2005-01-01

    AIM: Acarbose is able to enhance GLP-1 release and delay gastric emptying in normal subjects. The effect of alpha-glucosidase inhibition on GLP-1 has been less evident in Type 2 diabetic patients. The aim of this study was to investigate the possible influence of acarbose on GLP-1 release...... and gastric emptying in Type 2 diabetic patients after a mixed test meal. PATIENTS AND METHODS: Ten Type 2 diabetic patients were tested with 100 mg acarbose or placebo served with a mixed meal that was labelled with 100 mg 13C-octanoic acid. Plasma concentrations of glucose, insulin, C-peptide, glucagon, GLP......-1 and GIP were determined over 6 h. Gastric emptying was measured by determining breath 13CO2 using infrared absorptiometry. Statistics repeated-measures anova. RESULTS: Gastric emptying rates (t1/2: 162 +/- 45 vs. 163 +/- 62 min, P = 0.65) and plasma concentrations (increasing from approximately 12...

  18. Untersuchungen zum Einbau des Stickstoffes in der Acarviose-Einheit der Acarbose bei [Actinoplanes] sp. 50/110: die Aminotransferase Acb

    OpenAIRE

    Diaz-Guardamino Uribe, Paz Marta

    2001-01-01

    Diese Arbeit befasste sich mit dem Stickstoffstoffwechsel bei Actinoplanes sp. unter besonderer Berücksichtigung der Frage, wie der Stickstoff in den alpha-Glucosidaseinhibitor Acarbose während der Biogenese eingeführt wird. Zu klären galt es welches der postulierten Intermediate der Biosynthese transaminiert und durch welches Enzym diese Reaktion katalysiert wird. Heterologe PCR führte zur Identifizierung der Glutaminsynthetasen kodierenden Gene glnA und glnII auf dem Genom von Actinopla...

  19. Characterization of two coleopteran α-amylases and molecular insights into their differential inhibition by synthetic α-amylase inhibitor, acarbose.

    Science.gov (United States)

    Channale, Sonal M; Bhide, Amey J; Yadav, Yashpal; Kashyap, Garima; Pawar, Pankaj K; Maheshwari, V L; Ramasamy, Sureshkumar; Giri, Ashok P

    2016-07-01

    Post-harvest insect infestation of stored grains makes them unfit for human consumption and leads to severe economic loss. Here, we report functional and structural characterization of two coleopteran α-amylases viz. Callosobruchus chinensis α-amylase (CcAmy) and Tribolium castaneum α-amylase (TcAmy) along with their interactions with proteinaceous and non-proteinaceous α-amylase inhibitors. Secondary structural alignment of CcAmy and TcAmy with other coleopteran α-amylases revealed conserved motifs, active sites, di-sulfide bonds and two point mutations at spatially conserved substrate or inhibitor-binding sites. Homology modeling and molecular docking showed structural differences between these two enzymes. Both the enzymes had similar optimum pH values but differed in their optimum temperature. Overall, pattern of enzyme stabilities were similar under various temperature and pH conditions. Further, CcAmy and TcAmy differed in their substrate affinity and catalytic efficiency towards starch and amylopectin. HPLC analysis detected common amylolytic products like maltose and malto-triose while glucose and malto-tetrose were unique in CcAmy and TcAmy catalyzed reactions respectively. At very low concentrations, wheat α-amylase inhibitor was found to be superior over the acarbose as far as complete inhibition of amylolytic activities of CcAmy and TcAmy was concerned. Mechanism underlying differential amylolytic reaction inhibition by acarbose was discussed. PMID:27132147

  20. Glycemic variability in insulin treated type 2 diabetes with well-controlled hemoglobin A1c and its response to further treatment with acarbose

    Institute of Scientific and Technical Information of China (English)

    SU Jian-bin; WANG Xue-qin; CHEN Jin-feng; WU Gang; JIN Yan

    2011-01-01

    Background Glycemic variability, an HbA1c-independent risk factor, has more deleterious effects than sustained hyperglycemia in the development of diabetic complications. This study analyzed the characteristics of glycemic variability in type 2 diabetes mellitus (T2DM) with HbA1c<6.5% in duration of twice daily premixed insulin treatment and the effect of further treatment with acarbose.Methods Eighty-six T2DM patients who used premixed insulin analogue (insulin aspart 30) twice daily and had HbA1c <6.5% and 20 controlled subjects with normal glucose regulation (NGR) were monitored using the continuous glucose monitoring (CGM) system. The mean amplitude of glycemic excursions (MAGE), mean of daily differences (MODD) were used for assessing intra-day, inter-day glycemic variability. Hypoglycemia was defined as glucose level <3.9 mmol/L for at least 15 minutes in CGM. According to reference values of MAGE, T2DM patients were classified into two groups:Iow-MAGE group with MAGE <3.4 mmol/L (L-MAGE) and high-MAGE group with MAGE >3.4 mmol/L (H-MAGE). H-MAGE group received further treatment with acarbose for 2 weeks and was monitored a second time with CGM system.Results After first CGM, L-MAGE group had 41 cases, and H-MAGE group had 45 cases. The MAGE and MODD of T2DM group were all higher than those of subjects with NGR (P<0.01). Twenty-four percent (n=11) in H-MAGE group had a total of 13 hypoglycemic events, 10 of the 13 events occurred at night, meanwhile 5%(n=2) in L-MAGE group had a total of 2 hypoglycemic events, which also occurred at night(hypoglycemic events: 24% vs. 5%, x2=6.40, P<0.01).MAGE value was correlated with hypoglycemia value and 2-hour postprandial plasma glucose value (r=0.32 and 0.26,respectively, P<0.05). After further acarbose therapy and secondly CGM, MAGE and MODD values in H-MAGE group were all significantly decreased (40%, P<0.01, and 15%, P<0.05, respectively), but remained higher than in the subjects with NGR (P<0

  1. 玉液汤联合阿卡波糖治疗糖耐量减低(IGT)患者临床观察%Yuye Tang Joint Acarbose Treatment of IGT in Patients with Clinical Observation

    Institute of Scientific and Technical Information of China (English)

    张王孝

    2012-01-01

    目的:观察玉液汤联合阿卡波糖治疗IGT患者的临床疗效.方法:将120例符合标准的IGT患者随机分为两组,每组60例,两组患者无显著差异,具有可比性.两组都给予饮食和运动干预,在此基础上,对照组给予阿卡波糖,治疗组给予玉液汤联合阿卡波糖进行治疗.治疗16周,观察治疗前后两组患者的2h OGTT、FPG、FINS、HbA1c,以及脱离IGT状态的达标率.结果:治疗组和对照组患者的2h OGTT、FPG、HbA1c和FINS都显著降低,而治疗组FINS的降低更显著;治疗组患者脱离IGT状态的达标率显著高于对照组.结论:玉液汤联合阿卡波糖治疗IGT患者的疗效优于单纯使用阿卡波糖治疗.%Objective : Observe the clinical efficacy of Yuye Tang joint acarbose treatment of IGT patients. Method: 120 patients met the criteria of IGT patients were randomly divided into two groups, each group of 60 cases, patients were no significant differences were comparable. The two groups were given diet and exercise intervention on this basis, the control group were given acarbose treatment group received Yuye soup joint acarbose treatment. 16 weeks of treatment, observation and treatment of two groups of patients before and after 2h of OGTT, FPG and FINS and HbA lc, as well as from the IGT state compliance rate. Result: Treatment group and control group of patients with 2h of OGTT, FPG and HbAlc and FINS are significantly reduced, FINS of the treatment group reduced more significantly, treatment group compliance rate was significantly higher from the IGT state. Conclusion: Yuye Tang acarbose treatment of IGT patients more effective than simply the use of acarbose treatment.

  2. 格列美脲与阿卡波糖治疗2型糖尿病60例观察%To observe glimepiride and acarbose treatment on 60 cases with type 2 diabetes mellitus

    Institute of Scientific and Technical Information of China (English)

    2013-01-01

      目的观察格列美脲与阿卡波糖治疗2型糖尿病(T2DM)的临床疗效。方法选取T2DM患者60例,予以格列美脲与阿卡波糖口服12周。结果治疗后TG(甘油三酯)、TC(总胆固醇)、LDL-C(低密度脂蛋白)、FPG(空腹血糖)、2hPG(餐后2h血糖)、HbA1c(糖化血红蛋白)均下降(P <0.05),HDL-C(高密度脂蛋白)升高(P <0.05),HOMA-IR(胰岛素抵抗指数)改善(P <0.05)。结论格列美脲联合阿卡波糖治疗T2DM,血糖控制满意,血脂、HOMA-IR改善。%Objective To observe glimepiride and acarbose treatment on 60 cases with type 2 diabetes mellitus(T2DM). Method Glimepiride and acarbose were used 12 weeks in 60 patients with T2DM. Results TG,TC, LDL-C, FBG, 2hPG and HbA1c decreased while HDL-C incressed after treatment(P <0.05); HOMA-IR was improved more significantly(P <0.05). Conclusion Glimepiride and acarbose to treat T2DM have satisfactory effects in glucose, blood lipids and HOMA-IR.

  3. Effect of acarbose addition on acute and subacute rumen acidosis in an in vitro fermentation study%酸中毒条件下添加阿卡波糖对瘤胃微生物发酵的影响

    Institute of Scientific and Technical Information of China (English)

    毛胜勇; 何文波; 朱伟云

    2012-01-01

    The effect of acarbose addition on ruminant fermentation was investigated in three experiments. In the first and second experiments, the effects of acarbose addition on subacute rumen acidosis was studied. The final concentration of acarbose in the media was 0, 0. 1, 0. 2 or 0. 4 mg/mL. In the first study, the substrate consisted of 0. 8 g cracked corn and 0. 2 g Chinese dry grass. As compared with the control, the acarbose addition increased the pH value and the ratio of acetate to propionate, and decreased acetate, propionate, butyrate, isobutyrate, total volatile fatty acid and lactic acid concentrations. In the second experiment, the substrates consisted of cracked sorghum, corn, barley and wheat. The acarbose supplement increased pH, NH3-N, lac-tate concentration and the ratio of the acetate to propionate, and decreased acetate, propionate, butyrate and TVFA concentration. In the third experiment, the effect of acarbose addition on acute rumen acidosis was investigated, the pH, acetate, propionate, acetate, propionate, valerate, isovalerate and TVFA concentrations were reduced by acarbose addition, while the pH value was improved. There were no significant changes in the isobutyrate, butyrate, and isovalerate concentrations. In general, these results indicated that acarbose addition increased the pH value and reduced lactic acid concentration, and it has the potential to prevent rumen acidosis.%利用体外培养技术,评估了急性与亚急性酸中毒条件下添加阿卡波糖对瘤胃微生物发酵的影响.设3个实验,实验1和实验2体外摸拟了亚急性酸中毒(5.0<pH<5.6)、实验3模拟了急性酸中毒条件(pH<5.0),各实验中阿卡波糖添加量均为0,0.1,0.2和0.4 mg/mL.实验1中底物组成为0.8g玉米和0.2g粉碎羊草,实验2以高梁、玉米、小麦和大麦为底物,实验3发酵底物为0.75g玉米、0.25g纤维二糖、0.25g甘露糖和0.25g木糖;各实验组均设4个重复,体外培养24h.结果表明,实验1

  4. A comparison of efficacy and tolerance of nateglinide and acarbose monotherapy in type 2 diabetes mellitns%那格列奈与阿卡波糖有效性及耐受性比较研究

    Institute of Scientific and Technical Information of China (English)

    潘长玉; 高妍; 李光伟; 朱禧星; 高鑫; 刘昕

    2009-01-01

    目的 比较那格列奈与阿卡波糖在2型糖尿病(T2DM)患者中的有效性及耐受性.方法 随机、双盲、双模拟、平行组、多中心临床研究.237例单纯饮食治疗血糖控制不佳[糖化血红蛋白(HbA1c)6.5%~11.0%]的T2DM患者,随机给予那格列奈(120 mg,3次/d,119例)或阿卡波糖(100 mg,3次/d,118例)治疗12周.结果 与基线相比,治疗后两组患者HbA1c、空腹血糖(FPG)、餐后2 h血糖(PG2h)及体重均显著降低(P0.05);FPG与基线相比的变化,两组差异亦无统计学意义(P>0.05),PG2h与基线相比的变化,那格列条组与阿卡波糖组分别为(-1.45±2.74)mmol/L、(-2.20±2.21)mmol/L(P=0.0017),体重与基线相比,那格列奈组与阿卡波糖组分别为(-0.66±1.79)kg、(-2.06±2.00)kg,P=0.0000.两组可能与研究药物相关的不良反应例数及比例差异无统计学意义.结论 那格列奈(120 mg,3次/d)在单纯饮食治疗血糖控制不佳的T2DM患者中疗效肯定,与阿卡波糖(100 mg,3次/d)降低HbA1c疗效相当,且耐受性良好.%Objective To compare the efficacy and tolerability of nateglinide with those of acarbose in Chinese type 2 diabetes mellitus (T2DM) patients.Methods This multi-center,randomized,double-blind,parallel-arm study compared the efficacy and tolerability of nateglinide( 120 mg,3/d,n = 119) and those of acarbose( 100 mg,3/d,n = 118) during a 12-week treatment in T2DM patients uncontrolled by diet with glycosylated haemoglobin (HbA1c) 6.5% - 11.0% .Results Monotherapy with nateglinide (120 mg,3/d)or acarbose (100 mg,3/d)decreased HbA1c to a similar extent during 12-week treatment.The mean change from baseline to end-point in HbAlc was ( -0.90±0.98)% and ( -0.83±0.81 )% in patients receiving nateglinide and acarbose,respectively,with no significant difference between the two groups (P>0.05).The decrease in fasting plasma glucose (FPG)was similar between nateglinide and acarbose (P > 0.05).The mean change in 2-hour postprandial plasma glucose ( PG

  5. 格列美脲联合阿卡波糖治疗2型糖尿病临床观察%Clinical observation of glimepiride combined with acarbose in the treatment of type 2 diabetes

    Institute of Scientific and Technical Information of China (English)

    雷建军; 王成尧; 徐胜; 冯雪峰

    2015-01-01

    Objective:To explore the clinical effect of glimepiride combined with acarbose in the treatment of type 2 diabetes. Methods:60 patients with type 2 diabetes were randomly divided into the control group and the observation group with 30 cases in each.The control group was given glimepiride tablet treatment.The observation group was given acarbose tablet treatment on the basis of the control group.Results:The posttreatment FBG、2hPG and HbA1c of two groups were significantly lower than before treatment(P<0.05).After treatment,HbA1c,2hPG and FBG of the observation group were better than those of the control group(P<0.05).Conclusion:Glimepiride combined with acarbose in the treatment of type 2 diabetes can effectively control the fasting and postprandial blood glucose,the effect is satisfied.%目的:探讨格列美脲联合阿卡波糖治疗2型糖尿病的临床效果。方法:将60例2型糖尿病患者随机分为对照组和观察组各30例。对照组给予格列美脲片治疗;观察组在对照组的基础上给予阿卡波糖片治疗。结果:两组治疗后 FBG、2hPG 及 HbA1c 明显低于治疗前(P<0.05)。治疗后,观察组 FBG、2hPG 及 HbA1c 优于对照组(P<0.05)。结论:格列美脲联合阿卡波糖治疗2型糖尿病可有效控制空腹及餐后血糖,效果满意。

  6. 地特胰岛素联合阿卡波糖治疗2型糖尿病临床观察%Cinical observation of insulin detemir combined with acarbose in curing type 2 diabetic patients

    Institute of Scientific and Technical Information of China (English)

    劳丹华; 黄剑娴

    2012-01-01

    Objective To observe the effect of insulin detemir combined with acarbose in treatment of patients with type 2 diabetes (T2DM).Methods 32 T2DM patients whose blood glucose control was poor receiving twice daily isophane protamine biosynthetic human insulin( Novolin 30R) combined or not combined with oral hypoglycemic drugs,were switched to receive insulin detemir injection once daily and oral acarbose three times daily for 12 weeks.By self-contrasted method,observed blood glucose before and after three meals,before sleeping,glycated hemoglobin ( HbA1c),change of body mass index( BMI),incidence of hypoglycemia,compliance and satisfaction of patients (by questionnaire) before and after treatment.Results After treatment,the blood glucose before and after three meals,before sleeping and HbA1 c declined sigmifieatly ( t =11.212,14.997,10.863,17.950,11.108,14.034,12.422,22.764,all P <0.01 )compared to state before treatment.The rate of hypoglycemia in the day was 3.1%,without nocturnal symptoms of hypoglycemia.BMI had certain declining,but there was no statistical significance (P > 0.05).The compliance and satisfaction of patients were in a higher rate (x2 =10.255,9.143,all P < 0.01 ).Conclusion Insulin detemir combined with acarbose could effectively control the blood glucose,incidence of hypoglycemia,without increasing body mass,achieve good compliance and satisfaction of patients.%目的 观察地特胰岛素联合阿卡波糖治疗2型糖尿病的临床疗效.方法 对32例经预混精蛋白生物合成人胰岛素治疗血糖控制不佳的2型糖尿病患者,采用地特胰岛素每天1次注射,联合阿卡波糖,每天3次口服,治疗12周,采用自身对照,观察治疗前后三餐前、三餐后、睡前血糖、糖化血红蛋白(HbA1c)水平、体质量指数(BMI)变化及低血糖发生情况、患者治疗依从性和满意率.结果 治疗后三餐前、三餐后及睡前血糖、HbA1c均比治疗前明显下降(t=11.212、14.997、10.863、17

  7. Clinical Observation of Insulin Detemir Combined Acarbose in Type 2 Diabetic Patients after Intensive Treatment%强化治疗后的2型糖尿病患者转地特胰岛素联合阿卡波糖治疗的临床观察

    Institute of Scientific and Technical Information of China (English)

    祝恩梅

    2011-01-01

    目的 观察经持续皮下注射胰岛素(CSII)强化治疗的2型糖尿病(T2DM)患者改用地特胰岛素加阿卡波糖治疗的有效性、安全性及患者依从性.方法 将52例经CSII强化治疗达标的T2DM患者随机分为每日1次地特胰岛素+三餐口服阿卡波糖组和每日2次混合精蛋白锌重组人胰岛素组(优泌林70/30),各26例.12周后比较两组患者糖化血红蛋白(HbA1c),三餐前、三餐后及睡前血糖水平,患者依从性和满意率通过问卷调查来统计.结果 两组间HbA1c比较差异无统计学意义(P>0.05);地特胰岛素+阿卡波糖组中餐前与中餐后2 h血糖均低于精蛋白锌重组人胰岛素组,其差异有统计学意义(P<0.05),两组低血糖发生率相似,无统计学差异(P>0.05);地特胰岛素组患者的依从性和满意率明显高于精蛋白锌重组人胰岛素组.结论 CSII强化治疗后的T2DM患者改用地特胰岛素加阿卡波糖治疗有较好的疗效和安全性,患者依从性、满意率高.%Objective To observe the effectiveness, safety and patient compliance of type 2 diabetes ( T2DM )patients with continuous subcutaneous insulin infusion( CSⅡ )intensive treatment switching to detemir insulin therapy combined acarbose.Methods After intensive treatment by CSⅡ,52 patients with type 2 diabetes mellitus were randomly divided into two groups:detemir combined acarbose group and recombinant human hybrid protamine zinc insulin group.Detemir was given once daily and acarbose were orally given with three meals.Recombinant human hybrid protamine zinc insulin( Humulin 70/30 )were given twice daily.After 12 weeks treatment, we measured glycated hemoglobin( HbAlc )and blood glucose including before meals, after meals and before sleep.Patient compliance and satisfaction were estimated through questionnaires.Results HbA1 c between the two groups had no significant difference( P > 0.05 ).Blood glucose before meals and blood glucose 2 h after meals in detemir

  8. Coste-efectividad de la adición de acarbosa al tratamiento de pacientes con diabetes tipo 2 en España Cost-effectiveness of the addition of acarbose to the treatment of patients with type-2 diabetes in Spain

    Directory of Open Access Journals (Sweden)

    Carme Piñol

    2007-04-01

    Full Text Available Objetivos: Evaluar el coste-efectividad de la adición de acarbosa al tratamiento de pacientes con diabetes mellitus tipo 2 (DM2 en España. Métodos: Se utilizó el CORE Diabetes Model (modelo de simulación informática publicado y validado para proyectar a largo plazo los resultados clínicos y de costes de la DM2. Las probabilidades de transición y los riesgos se obtuvieron de distintas publicaciones. Los efectos del tratamiento y las características basales de la cohorte se obtuvieron de un metaanálisis. Los costes directos se extrajeron de diversas publicaciones y se proyectaron a lo largo de la vida de los pacientes bajo la perspectiva del Sistema Nacional de Salud de España. Los costes y beneficios fueron descontados en un 3% anual. Se realizaron análisis de sensibilidad. Resultados: El tratamiento con acarbosa se asoció con mejoras en la esperanza de vida (0,23 años y en los años de vida ajustados por calidad (AVAC (0,21 años. Los costes directos fueron en promedio, por paciente, de 468 € más caros con acarbosa que con placebo. La razón de coste-efectividad incremental fue de 2.002 €/año de vida ganado y de 2.199 €/AVAC ganado. La curva de aceptabilidad mostró que con una disponibilidad a pagar de 20.000 €, generalmente aceptada como muy buen valor monetario, el tratamiento con acarbosa se asoció con una probabilidad del 93,5% de ser coste-efectiva. Conclusiones: Este estudio económico a largo plazo mostró que la adición de acarbosa al tratamiento de pacientes con DM2 produjo mejoras en la esperanza de vida y en los AVAC de estos pacientes.Objectives: To assess the cost-effectiveness of the addition of acarbose to existing treatment in patients with type 2 diabetes mellitus (DM2 in Spain. Methods: The CORE Diabetes Model (a published and validated computer simulation model was used to project long-term clinical and cost outcomes in DM2. Transition probabilities and risk adjustments were derived from published

  9. 基础胰岛素联合阿卡波糖对初诊老年糖尿病患者血糖水平及并发症的影响%Effect of basal insul in combined with acarbose on blood glucose level and compl ications in patients with newly diagnosed elderly diabetes

    Institute of Scientific and Technical Information of China (English)

    郭玉卿; 张趁茹; 杨爱格; 刘璠; 董闪闪; 康岩; 王丽娜

    2016-01-01

    Objective:To analyze the effect of basal insulin combined with acarbose on blood glucose level and complica-tions in patients with newly diagnosed elderly diabetes.Methods:A total of 135 cases with newly diagnosed elderly diabetes who were treated in our hospital from July 2012 to January 201 5 were enrolled as research subjects and divided into observation group (66 cases)and control group (69 cases)according to different treatment methods.Control group received acarbose thera-py alone,observation group received basal insulin combined with acarbose therapy,and then differences in blood glucose level, oxidative stress indicators,nerve conduction velocity,vascular injury and inflammatory factor levels of two groups were com-pared.Results:FPG,2hPG and HbA1C levels of observation group after treatment were lower than those of control group (P<0.05);AGE-P,MDA and NADPH levels were lower than those of control group,and SOD level was higher than that of control group (P <0.05 );median MNCV,ulnar MNCV,tibial MNCV,median SNCV and sural SNCV levels were higher than those of control group (P <0.05);sVCAM-1,hs-CRP and IL-6 levels were lower than those of control group (P <0.05). Conclusion:Basal insulin combined with acarbose therapy for patients with newly diagnosed elderly diabetes can effectively opti-mize the levels of blood glucose and complication-related factors,and it has active clinical significance.%目的::分析基础胰岛素联合阿卡波糖对初诊老年糖尿病患者血糖水平及并发症情况的影响.方法:2012年7月~2015年1月间河北医科大学第一医院收治的初诊老年糖尿病患者135例作为研究对象,按照治疗方式不同分为观察组66例,对照组69例.对照组患者接受单纯阿卡波糖治疗,观察组患者接受基础胰岛素联合阿卡波糖治疗,对比两组患者的血糖水平、氧化应激指标、神经传导速度、血管损伤及炎症因子水平等差异.结果:治疗后观察组患者的 FPG

  10. Análisis de la relación coste-efectividad de la acarbosa en el tratamiento de pacientes con intolerancia a la glucosa Cost-effectiveness analysis of acarbose in the treatment of patients with impaired glucose tolerance

    Directory of Open Access Journals (Sweden)

    Ramón Sabés

    2004-12-01

    comparado y el horizonte temporal del estudio y utilizar alguna medida de resultados en salud que tenga en cuenta los efectos del tratamiento.Objective: To perform a cost-effectiveness analysis of treatment with acarbose in patients with impaired glucose tolerance (IGT in comparison with conventional treatment (based on medical counseling on diet and health and without drug treatment from the perspective of the public payer. Material and method: A cost-effectiveness analysis was performed using data on efficacy, the incidence of diabetes mellitus type 2 (DM2 and cardiovascular events from the STOP-NIDDM clinical trial of acarbose treatment vs. placebo. The study used a decision tree analysis to estimate the health and economic impact of the two alternative treatments in a population of 1,000 patients over a period of 40 months. Resource use and cost data refer to the Spanish health care system. Results: 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. Conclusions: Acarbose treatment in patients diagnosed with IGT appeared to be the dominant alternative compared with conventional treatment. The cost per avoided progression to DM2 and per additional individual free of a cardiovascular event was moderately low in some of the scenarios included in the sensitivity analysis. For a more comprehensive evaluation of the possible treatment of patients with IGT, the alternatives under comparison and the time horizon of the study would need to be increased and more refined health outcome measures, comprising

  11. Intervention effect of individualized diet nursing combined with acarbose on blood glucose and intestinal flora of pa-tients with type 2 diabetes%个体化饮食护理联合阿卡波糖治疗对2型糖尿病病人血糖和肠道菌群的干预作用

    Institute of Scientific and Technical Information of China (English)

    沈婷; 陶琼; 王婧; 陈红; 李玲; 何旭梅; 胡波

    2016-01-01

    Objective:To probe into the change situation of blood glucose and intestinal flora of T2DM patients who received the treatment of individualized diet nursing combined with acarbose.Methods:A total of 296 T2DM patients who received and cured from December 2013 to December 2015 were selected as the study sub-jects and randomly divided into two groups.The patients in control group were given the conventional treatment and nursing,while the patients in research group received the treatment of individualized diet nursing combined with acarbose on the basis of conventional treatment and nursing for 3 months,then to compare the change situ-ation of the fasting blood glucose (FBG),postprandial 2 h blood glucose (2 hBG),glycosylated hemoglobin (HbA1c)and intestinal bifidobacterium,milk acid coli,Enterococcus,Escherichia coli between the two groups before and after treatment.Results:After the treatment for 3 months,the FBG,2 hBG,HbA1c and intestinal En-terococcus,Escherichia coli in two groups were lower than those before treatment(P 0.05 ).After the treatment,the FBG,2 hBG,HbA1c and intestinal Enterococcus,Escherichia coli in research group were lower than those in control group(P 0.05)。治疗后研究组 FBG、2 hBG、HbA1c 及肠道肠球菌、大肠埃希氏菌均低于对照组(P <0.05),肠道双歧杆菌高于对照组(P <0.05)。[结论]在常规治疗基础上给予 T2DM 病人个体化饮食护理联合阿卡波糖治疗可以有效降低 T2DM 病人血糖水平,改善病人肠道菌群紊乱状态。

  12. Clinical curative effect and safety analysis of insulin glargine and acarbose treatment in elderly diabetes patients%甘精胰岛素联用阿卡波糖治疗老年糖尿病患者的临床疗效及安全性评价

    Institute of Scientific and Technical Information of China (English)

    王筱景; 阮凌燕; 周小爱

    2014-01-01

    目的:评价甘精胰岛素联用阿卡波糖治疗老年糖尿病患者的临床疗效及安全性。方法老年糖尿病患者120例随机分为治疗组和对照组,各60例。治疗组用甘精胰岛素联合阿卡波糖,对照组用精蛋白生物合成人胰岛素注射液联合阿卡波糖,胰岛素始剂量为0.15 U・ kg-1,根据血糖水平调整胰岛素用量及口服药物用量,随访观察3个月。监测患者血糖水平,并记录不良事件;随访记录2组患者的血糖达标时间和每日胰岛素总量,计算日平均血糖,检测患者治疗后的糖化血红蛋白水平和空腹 C 肽值。结果治疗3个月后,患者的糖化血红蛋白、空腹血糖及日平均血糖水平较治疗前均降低(P <0.05),其中,治疗组的日平均血糖水平显著低于对照组(P <0.05)。治疗组的血糖达标时间和胰岛素日用量均少于对照组(P 均<0.05),治疗后空腹 C 肽含量明显高于对照组(P <0.05)。治疗组的不良反应发生率低于对照组(P <0.05)。结论甘精胰岛素联用阿卡波糖治疗老年糖尿病患者具有良好疗效,能快速、安全、有效地控制患者血糖。%Objective To study the clinical curative effect and safety analysis of insulin glargine with acarbose treatment in elderly patients with diabetes.Methods A total of 120 cases of elderly patients with diabetes were randomly divided into two groups.The 60 patients of treat-ment group were treated with insulin glargine and acarbose combination , and the 60 patients of the control group were treated with isophane prota -mine biosynthetic human insulin injection and acarbose combination .The patient monitored blood glucose levels and recorded adverse events .The therapeutic time and the daily amount of insulin were recorded of two groups of patients.The average daily blood sugar were calculated and the HbA1c and fasting c -peptide values were detected at 3 months

  13. The Effect of Diet Therapy Combined with Acarbose Treatment for Postprandial Blood Glucose Ele-vation of Patients with Mild Diabetes%饮食疗法联合阿卡波糖对轻型糖尿病患者餐后血糖升高的治疗效果

    Institute of Scientific and Technical Information of China (English)

    孙学丽; 周素宏

    2016-01-01

    Objective To explore the effect of diet therapy combined with acarbose treatment for post-prandial blood glucose elevation of patients with mild diabetes.Methods From Jul.2013 to Aug.2015,132 patients with mild diabetes in Baodi District People′s Hospital were included in the study and divided into an observation group and a control group according to draw method,66 cases each.The control group was given acarbose 50 mg/time 1 time/day orally,and the observation group was given individualized dietary guidance program according to the body mass,blood lipids,blood glucose,nutrition and other indicators of the patients, combined with acarbose for treatment.The fasting blood glucose (FBG),2-hour postprandial blood glucose (2 h-PBG),glycated hemoglobin (HbA1c),alanine aminotransferase (ALT),serum creatinine (Cr),blood urea nitrogen ( BUN ) , total cholesterol ( TC ) , low density lipoprotein cholesterol ( LDL-C ) , triglycerides ( TG) ,high density lipoprotein cholesterol ( HDL-C) and other index were detected before and after 2 weeks of treatment.Results The FBG,2 h-PBG,ALT,serum Cr,BUN,TC,LDL-C,TG,drug maintenance dose, sugar recovery time of the observation group were significantly lower than the control group [ ( 5.9 ± 0.5) mmol/L vs (6.1 ±0.5) mmol/L,(7.2 ±0.6) mmol/L vs (7.5 ±0.7) mmol/L,(43 ±8) U/L vs (48 ±8) U/L,(98 ±14) μmoI/L vs (105 ±17)μmoI/L,(6.9 ±0.9) mmol/L vs (7.3 ±0.5) mmol/L, (4.68 ±0.67) mmol/L vs (5.03 ±0.65) mmol/L,(2.54 ±0.65) mmol/L vs (2.96 ±0.73) mmol/L, (1.35 ±0.41) mmol/L vs (1.62 ±0.48) mmol/L,(69 ±14) mg/d vs(77 ±19) mg/d,(6.8 ±1.5) d vs (7.5 ±2.1) d,P <0.05].The HDL-C of the observation group was significantly higher than the control group[(1.56 ±0.47) mmol/L vs (1.03 ±0.29) mmol/L,P<0.05];the HbA1c of the observation group was significantly lower than the control group after 12 weeks of treatment [ ( 5.36 ±1.17 )% vs ( 6.15 ± 1.02)%,P <0.05];the total effective of the observation group was significantly higher

  14. The therapeutic effect of insulin glargine versu NPH insulin as add-on therapy to previous acarbose or metformin in senile obese type 2 diabetics%加用甘精胰岛素对老年肥胖2型糖尿病口服降糖药控制不佳患者的疗效

    Institute of Scientific and Technical Information of China (English)

    王宾; 胡桂荣; 何丽; 孟红旗; 党静; 谢淑薏

    2012-01-01

    Objective To study the effectiveness and safety of insulin glargine versus isophane insulin as add-on therapy to previous OHA in senile obese type 2 diabetic patients who failed to control their blood glucose with oral hypoglycemic agents (OHA). Methods Sixty-one patients who failed to control their blood glucose with OHA were randomized into insulin glargine group and isophane insulin group. They were administered previous acarbose and/or metformin tablet and insulin glargine or isophand insulin as add-on therapy. The observation lasted for 12 weeks. Result (1) Both groups showed significant difference in HbAic FPG, and 2 hPG compared with before treatment, and in HbA1c and 2 hPG between the two groups (all P0. 05). (2) The BMI of the insulin glargine group was reduced by 2. 7 kg/m2 compared with before treatment) while that of the isophand insulin group was basically unchanged compared with before treatment (3) The 45. 2% of patients with insulin glargine treatment and the 73. 3% of patients with isophand insulin treatment had symptomatic hypoglycemia, and the difference was statistically significant (P<0. 05). (4) At the end of treatment, the dosa of insulin glargine group and isophand insulin group was (18. 7±3. 5) U/d and (26. 0±3. 7) U/d respectively, and the difference was statistically significant (P<0. 05). Conclusion The combination of insulin glargine with acarbose and/or metfonnin is effective in controlling the blood glucose, decreasing the incidence of hypoglycemia,and controlling the body weight of senile obese type 2 diabetic patients.%目的 研究口服降糖药控制不佳的老年肥胖T2DM患者加用甘精胰岛素或中效胰岛素联合应用治疗的有效性和安全性. 方法 将口服降糖药控制不佳的老年肥胖T2DM患者61例随机分为甘精胰岛素组和中效胰岛素组,治疗期内阿卡波糖和(或)二甲双胍剂量不变,分别加用甘精胰岛素或中效胰岛素每晚睡前注射1次联合治疗,进行12

  15. 君力达盐酸二甲双胍肠溶胶囊联合阿卡波糖对糖尿病患者空腹及餐后2h血糖、糖化血红蛋白以及甘油三酯水平的影响%Junlida Metformin Hydrochloride Enteric Capsules Connect Acarbose Dia-betes Fasting and Postprandial 2 h Blood Glucose, Glycosylated Hemoglobin and Triglyceride Levels of Influence

    Institute of Scientific and Technical Information of China (English)

    罗云霞; 庞建立

    2016-01-01

    目的:探讨君力达盐酸二甲双胍肠溶胶囊联合阿卡波糖对糖尿病患者空腹及餐后2h血糖、糖化血红蛋白以及甘油三酯水平的影响。方法选取在该科住院治疗的糖尿病患者52例,按照数字随机方式将患者分为对照组和观察组,各组为26例,分别对两组患者进行严格饮食控制及加强锻炼,对照组在此基础上实施君力达盐酸二甲双胍肠溶胶囊予以口服治疗,0.5 g/次,3次/d;观察组患者在上述药物基础上给予联合阿卡波糖50 mg予以治疗,嚼碎吞服,3次/d,持续12周。结果两组患者治疗前,就空腹血糖(FPG)及餐后2 h血糖(2 hPG)、糖化血红蛋白(Hb A1c)以及甘油三酯(TG)水平组间比较无明显差异(P<0.05)。两组患者治疗12周后,其空腹血糖(FPG)及餐后2 h血糖(2 hPG)、糖化血红蛋白(Hb A1c)以及甘油三酯(TG)水平均呈现出明显降低状况,观察组患者治疗后与对照组相比,降低幅度明显高于后者且差异显著(P<0.05);观察组后总有效率(96.15%)与对照组(76.92%)相比,明显高于后者且差异明显(P<0.05);观察组治疗12周后,其血糖控制的疗效与对照组相比,明显高于后者(P<0.05)。结论针对糖尿病患者,在对其进行严格的控制饮食及加强锻炼的基础上,采取君力达盐酸二甲双胍肠溶胶囊联合阿卡波糖进行治疗,其疗效更为确切,能够对患者的血糖水平具有很好的改善效果,有效降低低血糖相应发生率,在临床当中具有很好的应用和推广价值。%Objective To investigate the jun eed metformin hydrochloride enteric capsules joint acarbose fasting and post-prandial 2 h blood glucose in patients with diabetes, the influence of glycosylated hemoglobin and triglyceride levels. Methods Selecting the university hospital treatment of 52 patients with diabetes, according to the number of random, pa-tients can be divided into control group and observation group, each group of 26 cases

  16. 门冬胰岛素30联和阿卡波糖与胰岛素4次皮下注射治疗2型糖尿病临床疗效观察%Clinical efficacy observation between insulin aspart 30 injection combined with acarbose and four-times-insulin subcu-taneous injection in patients with poorly-cntronlled type 2 diaetes

    Institute of Scientific and Technical Information of China (English)

    胡艺琼; 陈晓文

    2014-01-01

    目的:比较单用门冬胰岛素(诺和锐)30血糖控制差的2型糖尿病患者加用阿卡波糖后和其改用四次胰岛素皮下注射方案的有效性、安全性。方法将医院60例单用诺和锐30血糖控制差的2型糖尿病患者随机分为2组,对照组30例采用诺和锐303次皮下注射同时3餐嚼服阿卡波糖;研究组30例采用4次胰岛素皮下注射(生物合成人胰岛素 R +地特胰岛素)。根据血糖调整胰岛素剂量,连续治疗12周后比较2组空腹血糖、餐后血糖、糖化血红蛋白(HbA1c)、胰岛素使用剂量及低血糖发生情况。结果2组空腹血糖,餐后血糖,HbA1c 都较前明显下降(P 0.05);对照组胰岛素用量明显减少,且低血糖发生率低,差异均有统计学意义(P 0. 05);The control group significantly reduced the amount of insulin,with lower incidence of hy-poglycemia,the differences were statistical significance(P < 0. 05). Conclusion NovoMix 30 combined with acarbose re-duces the amount of insulin when the blood glucose control is at target,and has less incidence of hypoglycemia comparing with four-subcutaneous-insulin injections.

  17. Drug: D00216 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available n hsa04973(279+280+8972) Carbohydrate digestion and absorption map07051 Antidiabetics Therapeutic category o...0BF01 Acarbose D00216 Acarbose (JAN/USAN/INN) USP drug classification [BR:br08302] Blood Glucose Regulators Antidiabetic...ting metabolism 396 Antidiabetic agents 3969 Others D00216 Acarbose (JAN/USAN/INN) Anatomical Therapeutic Ch...f drugs in Japan [BR:br08301] 3 Agents affecting metabolism 39 Other agents affec

  18. 瑞格列奈联合阿卡波糖治疗老年性2型糖尿病临床观察%Clinical Observation of Combined Treatment of Repaglinide and Acarbose in Aged Patients with Diabetes Type 2

    Institute of Scientific and Technical Information of China (English)

    蔡正华

    2009-01-01

    目的:观察瑞格列奈、阿卡波糖联合治疗老年性2型糖尿病患者的临床疗效及安全性.方法:观察58例2型糖尿病患者服用瑞格列奈及阿卡波糖,疗程12周,监测治疗前后空腹及餐后2 h血糖(FBG、PBG)、糖化血红蛋白(HbAlc)、肝功、肾功.结果:FBG、PBG及HbAlc较治疗前显著下降(P<0.05),尤其是餐后血糖更为明显(P<0.01).无一例肝肾功能损害,也无严重低血糖及其它严重不良反应发生.结论:瑞格列奈联合阿卡波糖治疗2型糖尿病降糖作用确切,而且安全性、耐受性良好.

  19. 甘精胰岛素联合阿卡波糖与预混胰岛素治疗2型糖尿病的效果比较%Study on the effects of glargined with acarbose and isophane protamine biosynthetcic human insulin in patients with type 2 diabetic

    Institute of Scientific and Technical Information of China (English)

    李艳萍; 李红梅

    2009-01-01

    目的 比较甘精胰岛素(Glargine)联合阿卡波糖与预混胰岛素(精蛋白生物合成人胰岛素30R)治疗2型糖尿病的疗效及对血糖波动的影响.方法 将65例2型糖尿病随机分为A组采用甘精胰岛素联合阿卡波糖治疗,B组采用预混胰岛素每日2次皮下注射.以空腹血糖(mFBG)<7mmol/L为目标,并监测早餐后2h血糖(mFPIG),午餐后2h血糖(mFP2G)和晚餐后2h血糖(mFP3G)计算1d 4次血糖样本的标准差(SD),以及最高和最低血糖之差(△).观察两组的血糖波动、胰岛素日用量、低血糖发生率.结果 A组胰岛素日用量、低血糖发生率均低于B组(P<0.05),血糖波动小.结论 甘精胰岛素联合阿卡波糖治疗2型糖尿病比预混胰岛素更利于血糖的平稳,低血糖的发生率低,波动影响更小,患者依从性好.

  20. alpha-Glycosidase inhibitory activity of hexagalloylglucose from the galls of Quercus infectoria.

    Science.gov (United States)

    Hwang, J K; Kong, T W; Baek, N I; Pyun, Y R

    2000-04-01

    Hexagalloylglucose (3-O-digalloyl-1,2,4,6-tetra-O-galloyl-beta-D- glucose), which was isolated from the methanol extract of the galls of Quercus infectoria, significantly inhibited alpha-glycosidases such as sucrase, maltase and isomaltase. Its inhibitory activity was comparable to acarbose being used as a hypoglycemic agent, while the inhibitory activity on alpha-amylase was approximately 10 times lower than that of acarbose. The results indicate that, when compared to acarbose, hexagalloylglucose might reduce the side effects by reducing inhibition of alpha-amylase. PMID:10821056

  1. Abdominal bloating

    Science.gov (United States)

    ... acarbose, and medicines or foods containing lactulose or sorbitol, may cause bloating. More serious disorders that may ... from foods with high levels of fructose or sorbitol Avoid foods that can produce gas, such as ...

  2. Prolonged successful therapy for hyperinsulinaemic hypoglycaemia after gastric bypass

    DEFF Research Database (Denmark)

    Myint, K S; Greenfield, J R; Farooqi, I S;

    2012-01-01

    Spontaneous hyperinsulinaemic hypoglycaemia following gastric bypass surgery (GBS) is increasingly recognised. However, its pathophysiology remains unclear. Some patients require pancreatectomy. Medical therapy with calcium channel blockers, acarbose and diazoxide has been reported to be beneficial...

  3. Medical management of metabolic dysfunction in PCOS

    OpenAIRE

    Duleba, Antoni J.

    2011-01-01

    Polycystic ovary syndrome (PCOS) is associated with metabolic derangements including insulin resistance, dyslipidemia, systemic inflammation and endothelial dysfunction. There is a growing need to develop pharmacologic interventions to improve metabolic function in women with PCOS. Medications that have been tested in patients with PCOS include metformin, thiazolidinediones, acarbose, naltrexone, orlistat, vitamin D and statins.

  4. Miglitol, a new alpha-glucosidase inhibitor

    NARCIS (Netherlands)

    Sels, J P; Huijberts, M S; Wolffenbuttel, B H

    1999-01-01

    Miglitol (Bay m 1099, Bayer) is a second generation alpha-glucosidase inhibitor. It is a derivative of 1-desoxynojirimycin, and binds reversibly to the brushborder alpha-glucosidase enzymes. In contrast to its parent drug (acarbose, Bay g 5421, Bayer), miglitol is almost completely absorbed in the s

  5. 2003~2005年我院口服降糖药物利用分析%Drug utilization analysis of oral hypoglycemic agents in our hospital during the period of 2003 ~ 2005

    Institute of Scientific and Technical Information of China (English)

    辛海莉; 蔡雯雯; 郭蔚

    2007-01-01

    To assess the drug utilization and tendency of progress of oral hypoglycemic agents in our hospital and to provide references for rational administration clinically. Methods: DDDs, sales quantities, sales expenses and the ratio of sales expenses sequencing to that of DDDs in our hospital during the period of 2003 ~ 2005 were analyzed statistically with the method of DDDs analysis. Results:The top two antidiabetic drugs according to DDDs were melbine ( dimethyl diguanide) and gliclazide three successive years. The DDDs of acarbose increased dramatically. Which blood glucose regulatsry drugs ranked lower, the ratio of sales expenses sequencing to that of DDDs of glipizide and gliclazide controlled release pellets was equal or about, whereas that of rosiglitazone, acarbose(glucobay) and glimepiride was less than 1. Conclusion:The study shows that the drug utilization of oral hypoglycemic agents in our hospital is basically rational and is in accordance with the trend of advancement and drug therapeutic strategies of diabetes mellitus.

  6. In Vitro Screening of Medicinal Plants Used in Mexico as Antidiabetics with Glucosidase and Lipase Inhibitory Activities

    OpenAIRE

    Guillermo Ramírez; Miguel Zavala; Julia Pérez; Alejandro Zamilpa

    2012-01-01

    This work shows the inhibitory effect on glucosidase and lipase enzymes of 23 medicinal plants described as traditional treatments for diabetes in several Mexican sources. Hydroalcoholic extracts of selected plants were evaluated at 1 mg/mL for glucosidase and 0.25 mg/mL for lipase inhibitory activities, respectively. Camellia sinensis, acarbose, and orlistat were used as positive controls. Dose-response curves were done with the most active species. Sixty percent of all tested extracts inhib...

  7. In vitro hypoglycemic effects of selected dietary fiber sources

    OpenAIRE

    Ahmed, Faiyaz; Sairam, Sudha; Urooj, Asna

    2010-01-01

    The physiological functions of dietary fiber and its role in health promotion and risk reduction of some chronic diseases has been well documented. In the present investigation, the effect of three dietary fiber sources, oats (OA), barley (BA) and psyllium husk (PH) on glucose adsorption, diffusion and starch hydrolysis were studied using in vitro techniques by simulating gastrointestinal conditions and compared with the commercial dietary fiber sources wheat bran (WB), acarbose (ACB) and gua...

  8. A high-throughput assay for quantification of starch hydrolase inhibition based on turbidity measurement.

    Science.gov (United States)

    Liu, Tingting; Song, Lixia; Wang, Hongyu; Huang, Dejian

    2011-09-28

    A high-throughput method for rapid determination of starch hydrolase inhibition was developed using a 96-well microplate UV-vis reader to monitor the turbidity decrease over time. The area under the curve of turbidity measured over time was used to quantify the inhibitory effect of polyphenolic compounds on porcine pancreatic amylase, rat intestine α-glucosidase, and fungal amyloglucosidase. Acarbose equivalence (AE) was introduced for the first time and defined as IC50 of acarbose divided by the IC50 of the sample measured under the same 96-well plate. This way, the run-to-run variations are canceled out. Among the plant extracts tested, grape seed extracts (1,440 μmolAE/g) and cinnamon bark extracts (1600 μmolAE/g) are the most active in inhibiting rat intestine α-glucosidase. For porcine α-amylase inhibition, grape seed extracts (5710 μmol AE/g) are close to four times more active (equal weight basis) than acarbose (1550 μmolAE/g).

  9. Glucose lowering effect of montbretin A in Zucker Diabetic Fatty rats.

    Science.gov (United States)

    Yuen, Violet G; Coleman, John; Withers, Steven G; Andersen, Raymond J; Brayer, Gary D; Mustafa, Sally; McNeill, John H

    2016-01-01

    Diabetes is an increasingly prevalent disease state with a global impact. It is important that effective and cost-efficient methods be developed to treat this disease state. Zucker diabetic fatty rats, an animal model of type 2 diabetes, were treated with montbretin A (MbA), a selective human pancreatic α-amylase inhibitor, isolated from the corms of the Crocosmia crocosmiiflora plant that may have potential as a glucose-lowering agent. The study purpose was to determine if MbA was an orally effective treatment for diabetes. The effect of MbA was compared to a current clinical treatment modality, acarbose that is associated with gastrointestinal side effects known to affect patient compliance. MbA and acarbose were administered daily in the drinking water. Body weight and fluid intake were measured daily to calculate dose consumption. Plasma glucose levels were determined twice weekly in both the fed and fasted state. At termination samples were collected to assess increased risk of secondary complications related to diabetes and oxidative stress. There was no effect of either MbA or acarbose treatment on insulin levels. Plasma glucose levels were significantly lower following MbA treatment in the ZT group which persisted throughout the study period (day 49: 12.1 ± 1.2 mM). However, while there was an initial decrease in plasma glucose levels in the acarbose-treated fatty group, this effect was not sustained (day 49: 20.6 ± 1.3 mM) through to termination. MbA improved the oxidative status of the fatty diabetic animals as well as attenuated markers for increased risk of cardiovascular complications associated with diabetes. This study demonstrated that, at a lower dose as compared to acarbose (10 mg/kg/day), chronic oral administration of MbA (7.5 mg/kg/day) was an effective glucose-lowering agent in the treatment of type 2 diabetes. PMID:26547551

  10. Resultados preliminares do uso de anti-hiperglicemiantes orais no diabete melito gestacional Preliminary results of the use of oral hypoglycemic drugs on gestational diabetes mellitus

    Directory of Open Access Journals (Sweden)

    Jean Carl Silva

    2005-08-01

    Full Text Available OBJETIVO: comparar a eficácia da glibenclamida e da acarbose com insulina no tratamento do diabete melito gestacional (DMG em relação ao controle glicêmico materno, peso do recém-nascido (RN e hipoglicemia neonatal. MÉTODOS: trata-se de ensaio clínico randomizado, prospectivo e aberto. Foram incluídas 57 pacientes com diagnóstico de DMG, que necessitaram de terapêutica complementar à dietoterapia e à atividade física. As gestantes foram aleatoriamente alocadas em um de três grupos com terapêuticas diferentes: um grupo controle conduzido com insulinoterapia, outro com glibenclamida e outro com acarbose. O período do estudo foi de sete meses (1º de outubro de 2003 a 1º de maio de 2004. Os desfechos primários avaliados foram o nível glicêmico materno após o inicio do tratamento, a necessidade de troca de terapêutica para controle glicêmico, peso do RN e presença de hipoglicemia neonatal. A análise estatística foi realizada pelo teste estatístico ANOVA, com nível de significância de 5%. RESULTADOS: as características maternas foram semelhantes nos três grupos estudados. O controle glicêmico não foi obtido em três pacientes que utilizaram glibenclamida (15% e em sete das usuárias de acarbose (38,8%. Não houve diferença quanto à glicemia em jejum e pós-prandial e no peso médio do RN entre os três grupos. A incidência de fetos grandes para a idade gestacional foi de 5,2, 31,5 e 11,1% nos grupos tratados com insulina, glibenclamida e acarbose, respectivamente. A hipoglicemia neonatal ocorreu em seis RN, sendo quatro deles do grupo glibenclamida (21,0%. CONCLUSÕES: a glibenclamida foi mais eficiente para o controle glicêmico que a acarbose, mas ambos foram menos eficientes que a insulina. Os RN de pacientes alocadas no grupo glibenclamida apresentaram maior incidência de macrossomia e de hipoglicemia neonatal quando comparados com os RN cujas mães receberam outros tratamentos.PURPOSE: to compare the

  11. Dipeptidyl Peptidase-4 Inhibitor Use Is Not Associated With Acute Pancreatitis in High-Risk Type 2 Diabetic Patients: A Nationwide Cohort Study.

    Science.gov (United States)

    Chang, Chia-Hsuin; Lin, Jou-Wei; Chen, Shu-Ting; Lai, Mei-Shu; Chuang, Lee-Ming; Chang, Yi-Cheng

    2016-02-01

    To analyze the association between use of DPP-4 inhibitors and acute pancreatitis in high-risk type 2 diabetic patients. A retrospective nationwide cohort study was conducted using the Taiwan National Health Insurance claim database. The risk associated with sitagliptin was compared to that with acarbose, a second-line antidiabetic drug prescribed for patients with similar diabetes severity and with a known neutral effect on pancreatitis. Between January 1, 2009 and December 31, 2010, a total of 8526 sitagliptin initiators and 8055 acarbose initiators who had hypertriglyceridemia or prior hospitalization history for acute pancreatitis were analyzed for the risk of hospitalization due to acute pancreatitis stratified for baseline propensity score. In the crude analysis, sitagliptin was associated with a decreased risk of acute pancreatitis (hazard ratio [HR] 0.74; 95% confidence interval [CI]: 0.62-0.88) compared to acarbose in diabetic patients with prior history of hospitalization for pancreatitis or hypertriglyceridemia. The association was abolished after stratification for propensity score quintiles (adjusted HR 0.95; 95% CI: 0.79-1.16). Similar results were found separately in both patients' histories of prior hospitalization of acute pancreatitis (adjusted HR 0.97; 95% CI: 0.76-1.24) and those with hypertriglyceridemia (adjusted HR 0.86; 95% CI: 0.65-1.13). No significant association was found for different durations or accumulative doses of sitagliptin. In the stratified analysis, no significant effect modification was found in relation to patients' characteristics. Use of sitagliptin was not associated with an increased risk of acute pancreatitis in high-risk diabetic patients with hypertriglyceridemia or with history of acute pancreatitis.

  12. Genetic engineering in Actinoplanes sp. SE50/110 - development of an intergeneric conjugation system for the introduction of actinophage-based integrative vectors.

    Science.gov (United States)

    Gren, Tetiana; Ortseifen, Vera; Wibberg, Daniel; Schneiker-Bekel, Susanne; Bednarz, Hanna; Niehaus, Karsten; Zemke, Till; Persicke, Marcus; Pühler, Alfred; Kalinowski, Jörn

    2016-08-20

    The α-glucosidase inhibitor acarbose is used for treatment of diabetes mellitus type II, and is manufactured industrially with overproducing derivatives of Actinoplanes sp. SE50/110, reportedly obtained by conventional mutagenesis. Despite of high industrial significance, only limited information exists regarding acarbose metabolism, function and regulation of these processes, due to the absence of proper genetic engineering methods and tools developed for this strain. Here, a basic toolkit for genetic engineering of Actinoplanes sp. SE50/110 was developed, comprising a standardized protocol for a DNA transfer through Escherichia coli-Actinoplanes intergeneric conjugation and applied for the transfer of ϕC31, ϕBT1 and VWB actinophage-based integrative vectors. Integration sites, occurring once per genome for all vectors, were sequenced and characterized for the first time in Actinoplanes sp. SE50/110. Notably, in case of ϕC31 based vector pSET152, the integration site is highly conserved, while for ϕBT1 and the VWB based vectors pRT801 and pSOK804, respectively, no sequence similarities to those in other bacteria were detected. The studied plasmids were proven to be stable and neutral with respect to strain morphology and acarbose production, enabling future use for genetic manipulations of Actinoplanes sp. SE50/110. To further broaden the spectrum of available tools, a GUS reporter system, based on the pSET152 derived vector, was also established in Actinoplanes sp. SE50/110. PMID:27181842

  13. Traditionally used plants in diabetes therapy: phytotherapeutics as inhibitors of alpha-amylase activity Plantas tradicionalmente utilizadas na terapia da diabetes: fitomedicamentos como inibidores da atividade alfa-amilase

    Directory of Open Access Journals (Sweden)

    Ingrid Funke

    2006-03-01

    Full Text Available Diabetes mellitus is a metabolic disorder characterized by chronic hyperglycaemia. There are many and diverse therapeutic strategies in the management of Type 2 diabetes. The inhibition of alpha-amylase activity is only one possibility to lower postprandial blood glucose levels. In our in-vitro studies we could demonstrate that different plants, mostly traditionally used in common diabetic therapy in Africa or Europe, are able to inhibit alpha-amylase, which is responsible for the breakdown of oligosaccharides into monosaccharides which are absorbed. An inhibition of alpha-amylase activity of 90% was seen with the extract of the leaves of Tamarindus indica. To quantify inhibtion rates, acarbose was used (IC50: 23.2 µM. Highest inhibition level of acarbose in our testmodel was about 85%. Additionally tests with pure polyphenolic compounds might explain the biological activity of the selected plants.Diabetes mellitus é uma desordem metabólica caracterizada pela hiperglicemia crônica. Existem diversas estratégias terapêuticas no tratamento da diabetes Tipo 2. A inibição da atividade da a-amilase é apenas uma possibilidade de reduzir os níveis de glicose posprandiais. Nos nossos estudos in vitro pudemos demonstrar que diferentes plantas, especialmente as tradicionalmente usadas em terapia comum de diabetes na África ou Europa, são capazes de inibir a a-amilase, a qual é responsável pela quebra dos oligossacarídeos em monossacarídeos, os quais são absorvidos. Uma inibição da atividade da a-amilase da ordem de 90% foi observada com o extrato das folhas de Tamarindus indica. Para quantificar os graus de inibição, acarbose foi usada (IC50: 23,2 mM. O maior grau de inibição de acarbose no nosso modelo de teste foi de cerca de 85%. Adicionalmente testes com compostos polifenólicos puros poderão explicar a atividade biológica das plantas selecionadas.

  14. Antidiabetic potential and secondary metabolites screening of mangrove gastropod Cerithidea obtusa

    Institute of Scientific and Technical Information of China (English)

    Reni Tri Cahyani; Sri Purwaningsih; Azrifitria

    2015-01-01

    Objective: To study the possible effects of Cerithidea obtusa extract as antidiabetic and to screen the secondary metabolites presence. Methods: Antidiabetic activity of Cerithidea obtusa extract was measured in vitro usingα-glucosidase inhibition method. Whereas, secondary metabolites screening was measured qualitatively. Results: The methanol extract had antidiabetic activity (IC50 = 36.40 mg/mL). However, the control drug acarbose had significantly higher antidiabetic activity (IC50 = 0.32 mg/mL). Secondary metabolites screening showed the presence of alkaloids, flavonoids, triterpenoids and saponins. Conclusions: The methanol extract had antidiabetic activity and the presence of alkaloids, flavonoids and triterpenoids might contribute to the activity.

  15. In silico approach for alpha-amylase inhibitory activity of diosmetin and galangin

    OpenAIRE

    Arumugam Madeswaran; Kuppusamy Asokkumar; Muthuswamy Umamaheswari; Thirumalaisamy Sivashanmugam; Varadharajan Subhadradevi

    2014-01-01

    Objective: The objective of the current study is to evaluate the α-amylase inhibitory activity of diosmetin and galangin using in silico docking studies.Methods: In this perspective, diosmetin and galangin were prepared for the docking evaluation. Acarbose, a known α-amylase inhibitor was used as the standard. In silico docking studies were carried out using recent version of AutoDock 4.2, which has the basic principle of Lamarckian genetic algorithm.Results: The results showed that the selec...

  16. Identification of Highly Potent and Selective α-Glucosidase Inhibitors with Antiglycation Potential, Isolated from Rhododendron arboreum

    OpenAIRE

    Rabia Raza; Zaitoon Ilyas; Sajid Ali; Muhammad Nisar; Muhammad Younas Khokhar; Jamshed Iqbal

    2015-01-01

    This study explored antidiabetic potential of eight known pure compounds, isolated from the bark of Rhododendron arboreum. Invitro studies of these compounds against α and β-glucosidases revealed them as very potent and selective inhibitors of α-glucosidase. Compound 7 (3-O-acetylursolic acid) was found to be the most potent inhibitor of α-glucosidase with 3.3±0.1µM IC 50 value which was many folds higher than standard inhibitor acarbose. Antiglycation studies of compounds showed that all com...

  17. α-Glucosidase inhibitory activities of isoflavanones, isoflavones, and pterocarpans from Mucuna pruriens.

    Science.gov (United States)

    Dendup, Tshewang; Prachyawarakorn, Vilailak; Pansanit, Acharavadee; Mahidol, Chulabhorn; Ruchirawat, Somsak; Kittakoop, Prasat

    2014-05-01

    Three new isoflavanones (1-3) and thirteen known compounds (4-16) were isolated from the roots of Mucuna pruriens. The absolute configurations of isoflavanones 1-3 and parvisoflavanone (4), lespedeol C (5), and uncinanone C (6) were addressed by a circular dichroism technique. Isoflavanones, isoflavones, and pterocarpans of M. pruriens were found to be α-glucosidase inhibitors. Medicarpin (7) and parvisoflavone B (9) were potent α-glucosidase inhibitors (twofold less active than the standard drug acarbose). The production of bioactive metabolites in M. pruriens seems to be season-dependent. PMID:24782227

  18. Synthesis, characterization and in vitro anti-diabetic activity of catechin grafted inulin.

    Science.gov (United States)

    Liu, Jun; Lu, Jian-feng; Kan, Juan; Wen, Xiao-yuan; Jin, Chang-hai

    2014-03-01

    In this study, a novel biological macromolecule with strong in vitro anti-diabetic activity was developed by grafting catechin onto inulin via a free radical mediated method. The characterization, α-glucosidase and α-amylase inhibitory activities of catechin grafted inulin (catechin-g-inulin) were investigated. Results showed that the grafting ratio of catechin-g-inulin was 124.8 mg CAE/g. UV-vis spectrum of catechin-g-inulin exhibited a new band at 280 nm, attributing to B ring of catechin moiety. FT-IR spectrum of catechin-g-inulin showed new absorption bands between 1540 and 1418 cm(-1), attributing to CC stretching vibration of catechin moiety. (1)H NMR spectrum of catechin-g-inulin preserved all the characteristic proton signals of inulin and partial signals of catechin. These all confirmed the successful grafting copolymerization. Conjugation probably occurred between OH of inulin (C-6) and H-6/H-8 of catechin (A ring). Catechin-g-inulin also exhibited increased thermal stability and crystallinity as compared to inulin. Moreover, in vitro anti-diabetic assays showed the α-glucosidase inhibitory activity decreased in the order of catechin-g-inulin>catechin>acarbose>inulin, and α-amylase inhibitory activity decreased in the order of catechin-g-inulin>acarbose>catechin>inulin. These indicated the potential of catechin-g-inulin in the development of a novel effective anti-diabetic agent.

  19. Triterpenes as uncompetitive inhibitors of α-glucosidase from flowers of Punica granatum L.

    Science.gov (United States)

    Salah El Dine, Riham; Ma, Qiong; Kandil, Zeinab A; El-Halawany, Ali M

    2014-01-01

    The α-glucosidase and maltase inhibitory effects of Punica granatum L. flowers (PGF) were investigated. The methanol extract (PGFMe), n-hexane extract (PGFH), chloroform extract (PGFC) and the remaining water fraction (PGFW) were assayed for their α-glucosidase and maltase inhibitory effects. PGFW showed potent α-glucosidase inhibition with IC₅₀ of 0.8 μg/mL followed by PGFMe (IC₅₀ of 4.0 μg/mL) then PGFC (IC₅₀ of 5.21 μg/mL) in comparison to acarbose (0.9 μM). Due to its selectivity towards α-glucosidase, PGFC was subjected to bioactivity-guided isolation of its main active constituents. Five known compounds (1-5) were identified as β-sitosterol (1), oleanolic acid (2), ursolic acid (3), p-coumaric acid (4) and apigenin (5). Ursolic and oleanolic acids showed potent α-glucosidase inhibition (IC₅₀ of 39.0 and 35.0 μM, respectively), while they did not show significant maltase inhibition. Kinetic study using the double Lineweaver-Burk plot revealed that ursolic acid uncompetitively inhibited α-glucosidase in comparison with acarbose as a competitive inhibitor. PMID:24956202

  20. Inhibition of recombinant human maltase glucoamylase by salacinol and derivatives.

    Science.gov (United States)

    Rossi, Elena J; Sim, Lyann; Kuntz, Douglas A; Hahn, Dagmar; Johnston, Blair D; Ghavami, Ahmad; Szczepina, Monica G; Kumar, Nag S; Sterchi, Erwin E; Nichols, Buford L; Pinto, B M; Rose, David R

    2006-06-01

    Inhibitors targeting pancreatic alpha-amylase and intestinal alpha-glucosidases delay glucose production following digestion and are currently used in the treatment of Type II diabetes. Maltase-glucoamylase (MGA), a family 31 glycoside hydrolase, is an alpha-glucosidase anchored in the membrane of small intestinal epithelial cells responsible for the final step of mammalian starch digestion leading to the release of glucose. This paper reports the production and purification of active human recombinant MGA amino terminal catalytic domain (MGAnt) from two different eukaryotic cell culture systems. MGAnt overexpressed in Drosophila cells was of quality and quantity suitable for kinetic and inhibition studies as well as future structural studies. Inhibition of MGAnt was tested with a group of prospective alpha-glucosidase inhibitors modeled after salacinol, a naturally occurring alpha-glucosidase inhibitor, and acarbose, a currently prescribed antidiabetic agent. Four synthetic inhibitors that bind and inhibit MGAnt activity better than acarbose, and at comparable levels to salacinol, were found. The inhibitors are derivatives of salacinol that contain either a selenium atom in place of sulfur in the five-membered ring, or a longer polyhydroxylated, sulfated chain than salacinol. Six-membered ring derivatives of salacinol and compounds modeled after miglitol were much less effective as MGAnt inhibitors. These results provide information on the inhibitory profile of MGAnt that will guide the development of new compounds having antidiabetic activity.

  1. Alpha-glucosidase inhibitory activity of Syzygium cumini (Linn.) Skeels seed kernel in vitro and in Goto-Kakizaki (GK) rats.

    Science.gov (United States)

    Shinde, Jayantrao; Taldone, Tony; Barletta, Michael; Kunaparaju, Naveen; Hu, Bo; Kumar, Sunil; Placido, Jessica; Zito, S William

    2008-05-19

    Syzygium cumini seed kernel extracts were evaluated for the inhibition of alpha-glucosidase from mammalian (rat intestine), bacterial (Bacillus stearothermophilus), and yeast (Saccharomyces cerevisiae, baker's yeast). In vitro studies using the mammalian alpha-glucosidase from rat intestine showed the extracts to be more effective in inhibiting maltase when compared to the acarbose control. Since acarbose is inactive against both the bacterial and the yeast enzymes, the extracts were compared to 1-deoxynojirimycin. We found all extracts to be more potent against alpha-glucosidase derived from B. stearothermophilus than that against the enzymes from either baker's yeast or rat intestine. In an in vivo study using Goto-Kakizaki (GK) rats, the acetone extract was found to be a potent inhibitor of alpha-glucosidase hydrolysis of maltose when compared to untreated control animals. Therefore, these results point to the inhibition of alpha-glucosidase as a possible mechanism by which this herb acts as an anti-diabetic agent. PMID:18374320

  2. Traditional Medicinal Herbs and Food Plants Have the Potential to Inhibit Key Carbohydrate Hydrolyzing Enzymes In Vitro and Reduce Postprandial Blood Glucose Peaks In Vivo

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    M. Fawzi Mahomoodally

    2012-01-01

    Full Text Available We hypothesized that some medicinal herbs and food plants commonly used in the management of diabetes can reduce glucose peaks by inhibiting key carbohydrate hydrolyzing enzymes. To this effect, extracts of Antidesma madagascariense (AM, Erythroxylum macrocarpum (EM, Pittosporum senacia (PS, and Faujasiopsis flexuosa (FF, Momordica charantia (MC, and Ocimum tenuiflorum (OT were evaluated for α-amylase and α-glucosidase inhibitory effects based on starch-iodine colour changes and PNP-G as substrate, respectively. Only FF and AM extracts/fractions were found to inhibit α-amylase activity significantly (P<0.05 and coparable to the drug acarbose. Amylase bioassay on isolated mouse plasma confirmed the inhibitory potential of AM and FF extracts with the ethyl acetate fraction of FF being more potent (P<0.05 than acarbose. Extracts/fractions of AM and MC were found to inhibit significantly (P<0.05 α-glucosidase activity, with IC50 comparable to the drug 1-deoxynojirimycin. In vivo studies on glycogen-loaded mice showed significant (P<0.05 depressive effect on elevation of postprandial blood glucose following ingestion of AM and MC extracts. Our findings tend to provide a possible explanation for the hypoglycemic action of MC fruits and AM leaf extracts as alternative nutritional therapy in the management of diabetes.

  3. Inhibition of α-glucosidase activity by ethanolic extract of Melia azedarach L. leaves

    Science.gov (United States)

    Sulistiyani; Safithri, Mega; Puspita Sari, Yoana

    2016-01-01

    Development of α-glucosidase inhibitor derived from natural products is an opportunity for a more economic management of diabetes prevention. The objective of this study was to test the activity of α-glucosidase with or without potential inhibitor compounds. By in vitro method, α-glucosidase hydrolizes p-nitrophenyl-α-D-glucopiranoside to glucose and the yellow of p-nitrophenol which can be determined with spectrophotometry at 400 nm. The ability of ethanolic leaf extract of Melia azedarach L. as a-glucosidase inhibitor was compared with that of commercial acarbose (Glucobay®). Acarbose showed strong inhibitory activity against a-glucosidase with IC50 values of 2.154 µg/mL. The crude ethanolic leaf extract of M. azedarach, however, showed less inhibitory activity with IC50 value of 3, 444.114 µg/mL. Total phenolics of M. azedarach leaves EtOH extract showed 17.94 µg GAE/mg extract and flavonoids total compound of 9.55 µg QE/mg extract. Based on the published wide range of IC50 values of extracts reported as a-glucosidase inhibitor which were between 10, 000 ppm-0.66 ppm, our result suggests that extract of M.azedarach leaves is potential candidate for development of anti-hyperglycemic formulation.

  4. Inhibition of α-Amylase and α-Glucosidase Activity by Tea and Grape Seed Extracts and their Constituent Catechins

    Science.gov (United States)

    Yilmazer-Musa, Meltem; Griffith, Anneke M.; Michels, Alexander J.; Schneider, Erik; Frei, Balz

    2015-01-01

    We evaluated the inhibitory effects of plant-based extracts (grape seed, green tea, and white tea) on α-amylase and α-glucosidase activity, glucosidases required for starch digestion. The abundant flavan-3-ol monomers (catechins) in these extracts were also tested for their inhibitory potential and evaluated against the pharmacological glucosidase inhibitor, acarbose. To evaluate relative potency of these extracts and catechins, the concentrations required for 50 and 90% inhibition of enzyme activity were determined. Maximum enzyme inhibition was used to assess an inhibitor’s relative efficacy. Results showed that grape seed extract strongly inhibited both α-amylase and α-glucosidase activity, with equal and much higher potency, respectively, than acarbose. While tea extracts and individual catechin 3-gallates were less effective inhibitors of α-amylase, they were potent inhibitors of α-glucosidase. Our data show that plant extracts containing catechin 3-gallates are potent inhibitors of α-glucosidase, and suggest that procyanidins found in grape seed extract strongly inhibit α-amylase activity. PMID:22697360

  5. Aqueous Extract of Nypa fruticans Wurmb. Vinegar Alleviates Postprandial Hyperglycemia in Normoglycemic Rats

    Directory of Open Access Journals (Sweden)

    Nor Adlin Yusoff

    2015-08-01

    Full Text Available Nypa fruticans Wurmb. vinegar, commonly known as nipa palm vinegar (NPV has been used as a folklore medicine among the Malay community to treat diabetes. Early work has shown that aqueous extract (AE of NPV exerts a potent antihyperglycemic effect. Thus, this study is conducted to evaluate the effect of AE on postprandial hyperglycemia in an attempt to understand its mechanism of antidiabetic action. AE were tested via in vitro intestinal glucose absorption, in vivo carbohydrate tolerance tests and spectrophotometric enzyme inhibition assays. One mg/mL of AE showed a comparable outcome to the use of phloridzin (1 mM in vitro as it delayed glucose absorption through isolated rat jejunum more effectively than acarbose (1 mg/mL. Further in vivo confirmatory tests showed AE (500 mg/kg to cause a significant suppression in postprandial hyperglycemia 30 min following respective glucose (2 g/kg, sucrose (4 g/kg and starch (3 g/kg loadings in normal rats, compared to the control group. Conversely, in spectrophotometric enzymatic assays, AE showed rather a weak inhibitory activity against both α-glucosidase and α-amylase when compared with acarbose. The findings suggested that NPV exerts its anti-diabetic effect by delaying carbohydrate absorption from the small intestine through selective inhibition of intestinal glucose transporters, therefore suppressing postprandial hyperglycemia.

  6. 2011~2012我院门诊患者口服降血糖药物应用分析%2011-2012 in Our Hospital Outpatients Oral Fall Blood Sugar Medicine Application Analysis

    Institute of Scientific and Technical Information of China (English)

    胡廷雪

    2013-01-01

    目的了解我院门诊患者口服降糖药应用情况,指导临床合适用药。方法统计2011年~2012年2年内门诊患者口服降糖药物的应用情况,统计内容包括口服降糖药物的名称、规格、销售数量、销售金额、限定日剂量、用药频度以及日用药金额等。结果口服降糖药中的阿卡波糖、二甲双胍以及瑞格列奈药物的销售额连续2年均位居前3位,二甲双胍、阿卡波糖和格列吡嗪药物使用频度较高,连续2年均保持着前3位,从DDDc来看,阿卡波糖和瑞格列奈最高,而吡格列酮和二甲双胍最低,销售金额序号与DDDs序号的比值在0.33~2.00之间。结论我院口服降糖药的应用基本科学、合理、有效,符合用药的基本原则。%Objective To understand the application of oral hypoglycemic drugs in our hospital outpatient patients, guiding clinical proper medication. Methods Statistics from 2011 to 2012,2 years outpatient oral hypoglycemic drugs, statistics includes name, oral antidiabetic drug specifications, sales volume, sales amount, defined daily dose, DDDs and daily cost.Results The oral hypoglycemic drugs acarbose, metformin and repaglinide drug sales for 2 consecutive years ranked the top 3, the higher frequency of metformin, acarbose and glipizide drug use, for 2 consecutive years maintained the top 3, from DDDc, acarbose, repaglinide column Nai the highest and lowest, pioglitazone and metformin, sales the amount of numbers and the DDDs numbers of the ratio between 0.33 and 2.Conclusion Oral hypoglycemic drugs in our hospital in basic science, application of reasonable, effective, consistent with the fundamental principles of drug.

  7. Cost-effectiveness study of oral hypoglycemic agents in the treatment of outpatients with type 2 diabetes attending a public primary care clinic in Mexico City

    Science.gov (United States)

    de León-Castañeda, Christian Díaz; Altagracia-Martínez, Marina; Kravzov-Jinich, Jaime; Cárdenas-Elizalde, Ma del Rosario; Moreno-Bonett, Consuelo; Martínez-Núñez, Juan Manuel

    2012-01-01

    Introduction Worldwide, diabetes mellitus presents a high burden for individuals and society. In Latin America, many people with diabetes have limited access to health care, which means that indirect costs may exceed direct health care cost. Diabetes is Mexico’s leading cause of death. Purpose To evaluate the cost-effectiveness ratios of the most used oral hypoglycemic agents (OHA) in the treatment of outpatients with type 2 diabetes attending a public primary care clinic in Mexico City. Design A cross-sectional and analytic study was conducted in Mexico City. Methodology Twenty-seven adult outpatients with type 2 diabetes who were treated either with metformin or glibenclamide were included. Acarbose was used as an alternative strategy. The study was carried out from the perspective of Mexican society. Direct medical and nonmedical costs as well as indirect costs were evaluated using a structured questionnaire. Efficacies of all drug treatments were evaluated retrospectively. A systematic search was conducted to select published randomized clinical trials based on predetermined inclusion criteria, and treatment success was defined as glycosylated hemoglobin factor ≤ 7%. Efficacy data of each drug and/or combination were analyzed using meta-analysis. The Monte Carlo Markov model was used. Quality-adjusted life-years (QALY) were used as the unit of effectiveness; incremental and sensitive analyses were performed and a 5% discount rate was calculated. A hypothetical cohort of 10,000 patients was modeled. Results The odds ratios of the success of each drug treatment were obtained from the meta-analyses, and were the following: 5.82 (glibenclamide), 3.86 (metformin), 3.5 (acarbose), and 6.76 (metformin–glibenclamide). The cost-effectiveness ratios found were US$272.63/QALY (glibenclamide), US$296.48/QALY (metformin), and US$409.86/QALY (acarbose). Sensitivity analysis did not show changes for the most cost-effective therapy when the effectiveness probabilities or

  8. Cost-effectiveness study of oral hypoglycemic agents in the treatment of outpatients with type 2 diabetes attending a public primary care clinic in Mexico City

    Directory of Open Access Journals (Sweden)

    Cárdenas-Elizalde MR

    2012-03-01

    Full Text Available Christian Díaz de León-Castañeda, Marina Altagracia-Martínez, Jaime Kravzov-Jinich, Ma del Rosario Cárdenas-Elizalde, Consuelo Moreno-Bonett, Juan Manuel Martínez-NúñezDepartment of Biological Systems and Health Care, Biological and Health Sciences Division, Universidad Autónoma Metropolitana-Xochimilco, Mexico DF, MexicoIntroduction: Worldwide, diabetes mellitus presents a high burden for individuals and society. In Latin America, many people with diabetes have limited access to health care, which means that indirect costs may exceed direct health care cost. Diabetes is Mexico's leading cause of death.Purpose: To evaluate the cost-effectiveness ratios of the most used oral hypoglycemic agents (OHA in the treatment of outpatients with type 2 diabetes attending a public primary care clinic in Mexico City.Design: A cross-sectional and analytic study was conducted in Mexico City.Methodology: Twenty-seven adult outpatients with type 2 diabetes who were treated either with metformin or glibenclamide were included. Acarbose was used as an alternative strategy. The study was carried out from the perspective of Mexican society. Direct medical and nonmedical costs as well as indirect costs were evaluated using a structured questionnaire. Efficacies of all drug treatments were evaluated retrospectively. A systematic search was conducted to select published randomized clinical trials based on predetermined inclusion criteria, and treatment success was defined as glycosylated hemoglobin factor ≤ 7%. Efficacy data of each drug and/or combination were analyzed using meta-analysis. The Monte Carlo Markov model was used. Quality-adjusted life-years (QALY were used as the unit of effectiveness; incremental and sensitive analyses were performed and a 5% discount rate was calculated. A hypothetical cohort of 10,000 patients was modeled.Results: The odds ratios of the success of each drug treatment were obtained from the meta-analyses, and were the

  9. Marrubiin: a potent α-glucosidase inhibitor from Marrubium alysson.

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    M. Abd El-Mohsen

    2014-02-01

    Full Text Available Summary. α-Glucosidase is an important target to discover new agents for treatment of diabetes-II and in slimming. The objective of this study is to investigate the effect of marrubiin, a major constituent of many medicinal plants including Marrubium alysson, as α-Glucosidase inhibitor. Bioassay-guided screening, isolation and purification of bioactive compounds of methanol extract of M. alysson was carried out followed by identification using 1H and 13C NMR analysis, and comparing isolated compounds with the published data. Inhibition of α-glucosidase activity bioassay at different concentrations of enzyme (0.3, 0.6, 1.5, 3 and 6 U/ml and substrate (sucrose: 7.5, 15, 30, 60 and 120 mM, and at different pretreatment times. Alpha-acarbose used as positive control in comparison to isolated compounds. Molecular docking was done to find out the interaction between compounds and the α-glucosidase receptor using MOE (molecular modeling environment. Bioassay-guided isolation led to the identification of three known labdane diterpenes; from which marrubiin (1 showed strong inhibition with IC50 of 16.62 μM. Docking studies of compound (1 against the α-glucosidase enzyme gave comparable scores and hydrogen bond interaction (-12.474 kcal/mol but different binding mode to the alpha-acarbose (-12.335 kcal/mol. These data suggest that marrubiin has an inhibitory effect on α-glucosidase activity and these findings provide insight into the traditional uses of Marrubium species for treatment of diabetes. Industrial relevance. Natural products isolated from plants are rich source to new drugs for medicinal use. Docking studies of marrubiin diterpenes against the α-glucosidase enzyme gave comparable scores and hydrogen bond interaction but different binding mode to the positive standard alpha-acarbose. These data suggest that marrubiin has an inhibitory effect on α-glucosidase activity and these findings provide insight into the traditional uses of

  10. Terpenoids with alpha-glucosidase inhibitory activity from the submerged culture of Inonotus obliquus.

    Science.gov (United States)

    Ying, You-Min; Zhang, Lin-Yan; Zhang, Xia; Bai, Hai-Bo; Liang, Dong-E; Ma, Lie-Feng; Shan, Wei-Guang; Zhan, Zha-Jun

    2014-12-01

    Lanostane-type triterpenoids, inotolactones A and B, a drimane-type sesquiterpenoid, inotolactone C, and five known terpenoids 6β-hydroxy-trans-dihydroconfertifolin, inotodiol, 3β,22-dihydroxyanosta-7,9(11),24-triene, 3β-hydroxycinnamolide, and 17-hydroxy-ent-atisan-19-oic acid, were isolated from the submerged culture of chaga mushroom, Inonotus obliquus. Their structures were characterized by spectroscopic methods, including MS and NMR (1D and 2D) spectroscopic techniques. Inotolactones A and B, examples of lanostane-type triterpenoids bearing α,β-dimethyl, α,β-unsaturated δ-lactone side chains, exhibited more potent alpha-glucosidase inhibitory activities than the positive control acarbose. This finding might be related to the anti-hyperglycemic properties of the fungus and to its popular role as a diabetes treatment. In addition, a drimane-type sesquiterpenoid and an atisane-type diterpenoid were isolated from I. obliquus. PMID:25446238

  11. Turmeric (Curcuma longa L.) volatile oil inhibits key enzymes linked to type 2 diabetes.

    Science.gov (United States)

    Lekshmi, P C; Arimboor, Ranjith; Indulekha, P S; Menon, A Nirmala

    2012-11-01

    Anti-diabetic capacity of Curcuma longa volatile oil in terms of its ability to inhibit glucosidase activities was evaluated. Turmeric volatile oils inhibited glucosidase enzymes more effectively than the reference standard drug acarbose. Drying of rhizomes was found to enhance α-glucosidase (IC₅₀ = 1.32-0.38 μg/ml) and α-amylase (IC₅₀ = 64.7-34.3 μg/ml) inhibitory capacities of volatile oils. Ar-Turmerone, the major volatile component in the rhizome also showed potent α-glucosidase (IC₅₀ = 0.28 μg) and α-amylase (IC₅₀ = 24.5 μg) inhibition.

  12. Nutritional Composition, α-Glucosidase Inhibitory and Antioxidant Activities of Ophiopogon japonicus Tubers

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    Yancui Wang

    2015-01-01

    Full Text Available Ophiopogon japonicus tubers have been widely used as food and traditional Chinese medicine in China. However, their nutritional composition has not been fully reported yet. This study aimed to analyze the nutritional composition of O. japonicus tubers. The α-glucosidase inhibitory and antioxidant activities of the extracts obtained from O. japonicus tubers were also evaluated by in vitro assays. The results indicated that O. japonicus tubers are rich in carbohydrates, proteins, minerals, and amino acids. Among four extracts, the n-butanol fraction (nBF and chloroform/methanol extract (CME of O. japonicus tubers had high amounts of total phenolic and flavonoid contents and exhibited good α-glucosidase inhibitory and antioxidant activities. The α-glucosidase inhibition of nBF was higher than acarbose. Overall, O. japonicus tubers are full of nutritional compounds and have good α-glucosidase inhibitory and antioxidant activities.

  13. New C₂₀-gibberellin diterpene from the leaves of Schefflera sessiliflora De P. V.

    Science.gov (United States)

    Nguyen, Tan Phat; Tran, Thi Thao Vy; Mai, Dinh Tri; Le, Tien Dung; Phan, Nhat Minh; Bui, Trong Dat

    2015-01-01

    From the leaves of Schefflera sessiliflora De P. V., one new C20-gibberellin diterpene 2β,12β-dihydroxygibberellin (12β-hydroxy-GA110 or 2β-hydroxy-GA112) (1), together with three known compounds, trans-tiliroside (2), kaempferol 3-O-β-D-glucuronopyranoside (3), 5-p-trans-coumaroylquinic acid (4), was isolated for the first time from the genus Schefflera by various chromatography methods. Their structures were elucidated by IR, UV, HR-ESI-MS, NMR 1D and 2D experiments and comparison with previous reported data. The α-glucosidase inhibitory activity of all compounds was measured. The isolates (2, 3) showed better α-glucosidase inhibitory activity (IC50 = 134.60, 147.10 μM, respectively) than the standard drug acarbose (IC50 = 214.50 μM).

  14. α-GLUCOSIDASE AND α -AMYLASE INHIBITORY ACTIVITIES OF RAPHANUS SATIVUS LINN.

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    R. Vadivelan et al

    2012-09-01

    Full Text Available Herbal medicine has been used for many years by different cultures around the world for the treatment of diabetes. There has been an enormous interest in the development of alternative medicines for type 2 diabetes, specifically screening for phytochemicals with the ability to delay or prevent glucose absorption. The goal of the present study is to evaluate the invitro antidiabetic activity of Raphanus sativus ethanolic extract and fractions by α-glucosidase and α -amylase inhibitory activity. Raphanus sativus ethanolic extract and fractions showed dose dependent inhibition of α-glucosidase and α -amylase enzyme and exhibited lower inhibitory activity than acarbose. The study revealed the antidiabetic potential and could be helpful to develop medicinal preparations and nutraceuticals and function foods for diabetes.

  15. PENGHAMBAT α AMILASE: JENIS, SUMBER, DAN POTENSI PEMANFAATANNYA DALAM KESEHATAN [α Amylase Inhibitors: Types, Sources, and Their Potential Utilization for Health Purposes

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    Budiasih Wahyuntari

    2011-12-01

    Full Text Available SUMMARYAlpha amylase inhibitors affect carbohydrate metabolism in digestive system. The inhibitors induce carbohydrate tolerance, fullness and prolonging gastric emptying that might be used to aid in diabetic and obesity treatment. There are two types of α- amylase inhibitors, proteinaceous and non-proteinaceous ones. Proteinaceous inhibitor is classified into seven classes including legumes, lectin, knottin, cereal, Kunitz, -thionin and thaumatin types. Plant proteinaceous inhibitors are present in cereals and legumes. Some non-proteinaceous inhibitors include flavonid, polyphenols, organic acid that might be produced by microbes or extracted from plants such as acarbose, saponin dan cardiac glycoside, gallic acid, proto-catechuic acid, caffeic acid, ellagic acid, ferulic acid, quercetin hibiscus acid and α-, β- and γ-cyclodextrin.

  16. Identification of Highly Potent and Selective α-Glucosidase Inhibitors with Antiglycation Potential, Isolated from Rhododendron arboreum

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    Rabia Raza

    2015-01-01

    Full Text Available This study explored antidiabetic potential of eight known pure compounds, isolated from the bark of Rhododendron arboreum. Invitro studies of these compounds against α and β-glucosidases revealed them as very potent and selective inhibitors of α-glucosidase. Compound 7 (3-O-acetylursolic acid was found to be the most potent inhibitor of α-glucosidase with 3.3±0.1µM IC 50 value which was many folds higher than standard inhibitor acarbose. Antiglycation studies of compounds showed that all compounds were also very active antiglycation agents. The studied biological properties of these compounds suggest that they are therapeutically interesting and important tools for treatment of diabetes.

  17. Chemical genetics and cereal starch metabolism: structural basis of the non-covalent and covalent inhibition of barley β-amylase.

    Science.gov (United States)

    Rejzek, Martin; Stevenson, Clare E; Southard, Andrew M; Stanley, Duncan; Denyer, Kay; Smith, Alison M; Naldrett, Mike J; Lawson, David M; Field, Robert A

    2011-03-01

    There are major issues regarding the proposed pathway for starch degradation in germinating cereal grain. Given the commercial importance but genetic intractability of the problem, we have embarked on a program of chemical genetics studies to identify and dissect the pathway and regulation of starch degradation in germinating barley grains. As a precursor to in vivo studies, here we report systematic analysis of the reversible and irreversible inhibition of the major β-amylase of the grain endosperm (BMY1). The molecular basis of inhibitor action was defined through high resolution X-ray crystallography studies of unliganded barley β-amylase, as well as its complexes with glycone site binder disaccharide iminosugar G1M, irreversible inhibitors α-epoxypropyl and α-epoxybutyl glucosides, which target the enzyme's catalytic residues, and the aglycone site binders acarbose and α-cyclodextrin.

  18. Report: screening of selected medicinal plants for their enzyme inhibitory potential - a validation of their ethnopharmacological uses.

    Science.gov (United States)

    Khuda, Fazli; Iqbal, Zafar; Khan, Ayub; Zakiullah; Shah, Yasar; Khan, Abad

    2014-05-01

    In present study four medicinal plants namely Valeriana wallichii, Xanthium strumarium, Achyranthes aspera and Duchesnea indica belonging to different families were collected in Khyber Pakhtunkhwa province and crude extract and subsequent fractions were analyzed for their inhibitory potential against acetylcholinesterase, butyrylcholinesterase and α-glucosidase enzymes. Valeriana wallichii, Xanthium strumarium and Achyranthes aspera were significantly active against cholinesterases. Chloroform and ethylacetate fractions of Valeriana wallichii exhibited significant activity against acetylcholinesterase (IC50: 61μg/ml) and butyrylcholinesterase enzymes (IC50: 58μg/ml), respectively. Similarly ethylacetate fraction of Achyranthes aspera showed significant activity against acetylcholinesterase (IC50: 61 μg/ml) and butyrylcholinesterase enzymes (IC50: 61 μg/ml), respectively. In case of α-glucosidase enzyme, the chloroform fraction of Xanthium strumarium exhibited significant inhibitory activity (IC50: 72 μg/ml) as compared to the standard compound acarbose (IC50: 483 μg/ml). Duchesnea indica showed no such activities. PMID:24811822

  19. Syntheses of new 3-thiazolyl coumarin derivatives, in vitro α-glucosidase inhibitory activity, and molecular modeling studies.

    Science.gov (United States)

    Salar, Uzma; Taha, Muhammad; Khan, Khalid Mohammed; Ismail, Nor Hadiani; Imran, Syahrul; Perveen, Shahnaz; Gul, Sahib; Wadood, Abdul

    2016-10-21

    3-Thiazolylcoumarin derivatives 1-14 were synthesized via one-pot two step reactions, and screened for in vitro α-glucosidase inhibitory activity. All compounds showed inhibitory activity in the range of IC50 = 0.12 ± 0.01-16.20 ± 0.23 μM as compared to standard acarbose (IC50 = 38.25 ± 0.12 μM), and also found to be nontoxic. Molecular docking study was carried out in order to establish the structure-activity relationship (SAR) which demonstrated that electron rich centers at one and electron withdrawing centers at the other end of the molecules showed strong inhibitory activity. All the synthesized compounds were characterized by spectroscopic techniques such as EI-MS, HREI-MS, (1)H NMR and (13)C NMR. CHN analysis was also performed.

  20. Polyketides from the Mangrove-Derived Endophytic Fungus Nectria sp. HN001 and Their α-Glucosidase Inhibitory Activity

    Science.gov (United States)

    Cui, Hui; Liu, Yayue; Nie, Yang; Liu, Zhaoming; Chen, Senhua; Zhang, Zhengrui; Lu, Yongjun; He, Lei; Huang, Xishan; She, Zhigang

    2016-01-01

    Four new polyketides: nectriacids A–C (1–3) and 12-epicitreoisocoumarinol (4), together with three known compounds: citreoisocoumarinol (5), citreoisocoumarin (6), and macrocarpon C (7) were isolated from the culture of the endophytic fungus Nectria sp. HN001, which was isolated from a fresh branch of the mangrove plant Sonneratia ovata collected from the South China Sea. Their structures were determined by the detailed analysis of NMR and mass spectroscopic data. The absolute configuration of the stereogenic carbons for compound 4 was further assigned by Mosher’s ester method. All of the isolated compounds were tested for their α-glucosidase inhibitory activity by UV absorbance at 405 nm, and new compounds 2 and 3 exhibited potent inhibitory activity with IC50 values of 23.5 and 42.3 μM, respectively, which were more potent than positive control (acarbose, IC50, 815.3 μM). PMID:27136568

  1. From carbohydrates to drug-like fragments: Rational development of novel α-amylase inhibitors.

    Science.gov (United States)

    Al-Asri, Jamil; Fazekas, Erika; Lehoczki, Gábor; Perdih, Andrej; Görick, Cornelia; Melzig, Matthias F; Gyémánt, Gyöngyi; Wolber, Gerhard; Mortier, Jérémie

    2015-10-15

    Starch catabolism leading to high glucose level in blood is highly problematic in chronic metabolic diseases, such as type II diabetes and obesity. α-Amylase catalyzes the hydrolysis of starch, increasing blood sugar concentration. Its inhibition represents a promising therapeutic approach to control hyperglycaemia. However, only few drug-like molecule inhibitors without sugar moieties have been discovered so far, and little information on the enzymatic mechanism is available. This work aims at the discovery of novel small α-amylase binders using a systematic in silico methodology. 3D-pharmacophore-based high throughput virtual screening of small compounds libraries was performed to identify compounds with high α-amylase affinity. Twenty-seven compounds were selected and biologically tested, revealing IC50 values in the micromolar range and ligand efficiency higher than the one of the bound form of acarbose, which is used as a reference for α-amylase inhibition.

  2. In Vitro Antioxidant and Enzymes Inhibitory activity of Chloroform Fraction of Hydroalcoholic extract obtained from Argemone mexicana

    Directory of Open Access Journals (Sweden)

    Nayak P

    2013-03-01

    Full Text Available In the present investigation antioxidant and alphaamylase inhibitory activity of chloroform fraction of Argemone mexicana were evaluated. The antioxidant activity of chloroform fraction of A. mexicana was evaluated by DPPH, Super oxide radical Scavenging activity, ABTS radical cation scavenging activity and Nitric oxide radical scavenging activity. Alpha-amylase inhibitory activity of chloroform fraction was evaluated by DNS method respectively. The observed resultant antioxidant activity of chloroform fraction in all studied models was moderate as compared with reference standard Ascorbic acid. The chloroform fraction exhibited appreciable α-amylase inhibitory activity with an IC50 value 48.92μg/ml respectively, when compared with acarbose (IC50 value 83.33μg/ml.In conclusion, from the results of present study it is confirmed that antioxidant and alpha-amylase inhibitory activity of chloroform fraction of A. mexicana may contribute in its earlier observed antidiabetic potential.

  3. Effect of 'antidiabetis' herbal preparation on serum glucose and fructosamine in NOD mice.

    Science.gov (United States)

    Petlevski, R; Hadzija, M; Slijepcevic, M; Juretic, D

    2001-05-01

    The antihyperglycemic effect of the Antidiabetis herbal preparation ((Myrtilli folium (Vaccinium myrtillus L.), Taraxaci radix (Taraxacum officinale Web.), Cichorii radix (Cichorium intybus L.), Juniperi fructus (Juniperus communis L.), Centaurii herba (Centaurium umbellatum Gilib.), Phaseoli pericarpium (Phaseolus vulgaris), Millefollii herba (Achillea millefolium L.), Morii folium (Morus nigra L.), Valeriane radix (Valleriana officinalis L.), Urticae herba et radix (Urtica dioica L.)), patent No. P-9801091 Zagreb, Croatia was investigated. Two extracts were prepared: ethanol extract (extract 1), and ethanol extract from which ethanol was evaporated on a rotatory evaporator at a temperature of 45 degrees C (extract 2). Extract 1 and extract 2 were administered (in experiment 1) to alloxan-induced non-obese diabetic (NOD) mice in the same dose of 20 mg/kg. Blood glucose was determined before, and 10, 30, 60 and 120 min after the preparation administration. Extract 1 and extract 2 decreased the level of blood glucose by 10 and 20%, respectively, of the initial value (at 0 min, mean = 22.6 +/- 8.3 mmol/l). Serum levels of glucose and fructosamine were determined in NOD mice, NOD mice administered extract 2 in a dose of 20 mg/kg of extract 2, and NOD mice administered acarbose in a dose of 25 mg/100 g chow, in order to verify the hypoglycemic action of extract 2 (in experiment 2). Extract 2 and acarbose were admixed to the chow. The duration of treatment was 7 days. Significantly lower glucose (P < 0.05) and fructosamine (P < 0.001) levels were recorded in extract 2 treated NOD mice as compared with NOD mice. Study results showed extract 2 to significantly decrease the level of glucose and fructosamine in alloxan induced NOD mice. Our future studies will be focused on the search of active principles of the extracts. PMID:11297848

  4. Development of an antidiabetic formulation (ADJ6) and its inhibitory activity against α-amylase and α-glucosidase.

    Science.gov (United States)

    Duraiswamy, Anand; Shanmugasundaram, Devanand; Sasikumar, Changam Sheela; Cherian, Sanjay M; Cherian, Kotturathu Mammen

    2016-07-01

    There has recently been much advancement in the diagnosis, treatment, and research of metabolic disorders, especially diabetes. Current research around the world is focused on finding an alternative source of treatment from natural resources for diabetic management, apart from the available synthetic medicines. The present study is a preliminary study of a polyherbal formulation using edible natural resources and an assessment of its antidiabetic activity. The formulation was screened for its phytochemical constituents, total phenols, flavonoids, and vitamin C content. It was also analyzed for its inhibitory effect against the digestive enzymes α-amylase and α-glucosidase, compared with the standard drug acarbose. The formulation showed the presence of major constituents such as steroids, cardiac glycosides, phenols, flavonoids, and saponins. It also had a high level of phenols (340 ± 2.5 mg/g), flavonoids (235.4 ± 8.3 mg/g), and vitamin C (470.8 ± 16.6 mg/g), and showed a half-maximal inhibitory concentration (IC50) value of 0.41 ± 0.03 mg/mL and 0.51 ± 0.01 mg/mL for amylase and glucosidase, respectively. The results showed that ADJ6 had a significant inhibitory activity on α-amylase and α-glucosidase; however, its inhibitory activity was less than that of acarbose. The plants that are formulated in ADJ6 possess potent antidiabetic activity. Thus, we found that ADJ6 is a potent lead for effective diabetic management; however, an evaluation of the formulation must be illustrated using an in vivo model. PMID:27419082

  5. Comparison of Antioxidant Potential and Rat intestinal a-Glucosidases inhibitory Activities of Quercetin, Rutin, and Isoquercetin

    Directory of Open Access Journals (Sweden)

    S-H Jo

    2009-12-01

    Full Text Available Summary: Inhibition of α-amylase and α-glucosidases involved in the digestion and absorption of carbohydrates can decrease the postprandial increase  of blood glucose level after a mixed carbohydrate diet. Therefore, the inhibitory activity of quercetin and its glycoside derivatives such as rutin and isoquercetin against rat intestinal α-glucosidases (sucrase, maltase, glucoamylase, and isomaltase and porcine pancreatic α-amylase were compared in vitro. Among the tested three flavonols, quercetin had the highest maltase, glucoamylase, and isomaltase inhibitory activities. The isomaltase and α-amylase inhibitory activities of the above three flavonols were also compared to a known type 2 diabetes drug (Acarbose, strong  α-amylase inhibitor. Compared  to acarbose, quercetin and its derivatives showed a significant inhibition of isomaltase but did not show high inhibitory activity against porcine pancreatic  α-amylase. Furthermore, the oxygen radical absorbance capacity (ORAC of these flavonols was evaluated. Quercetin had the highest peroxyl radical absorbing activity, followed by rutin and isoquercetin. These results suggest that the selected flavonols which have high ORAC value with α-glucosidase inhibitory activity and low α-amylase activity could be physiologically useful for treatment of diabetes, although in vivo experiments are needed. Industrial relevance: The α-glucosidase inhibitory activity and antioxidant activity in quercetin would be helpful to manage glucose uptake and the glucose-induced increased levels of mitochondrial reactive oxygen species (ROS linked to hyperglycemia. This in vitro study therefore provides the biochemical rationale for the benefit of quercetin-based dietary supplement and enzymatic conversion from rutin or isoquercetin to quercetin for enhancing bioactive food components using high rutin-contained grain such as buckwheat.  

  6. Alpha-Glucosidase Inhibition and Hypoglycemic Activities of Sweitenia mahagoni Seed Extract

    Directory of Open Access Journals (Sweden)

    Tutik Wresdiyat

    2015-04-01

    Full Text Available Inhibition of α-glucosidase and hypoglycemic activity are two effects commonly used to identify bioactive compounds with potential to treat diabetes. The objectives of this study were to analyse and compare the bioactive compounds and α-glucosidase inhibitory effect of four different types of Swietenia mahagoni seed extract, and to analyse the hypoglycemic activity of the greatest inhibition of α-glucosidase-extract in rats. The extracts were obtained using two different solvents (aqueous and ethanol and two different methods: maceration and reflux methods. This resulted in four types of extract varying by solvent and extraction method. Testing of these extracts for α-glucosidase inhibitory effect was carried out in vitro using spectrophotometer. Testing for hypoglycemic activity was carried out in vivo using rats. A total of 40 male Sprague-Dawley rats were divided into eight groups: (1 the negative control group, received an oral dose of aquadest only, (2 the positive control group, was given 90% sucrose orally without S. mahagoni seed extract, and five treated groups (3-7, were given 90% sucrose followed by the best extract-ethanolic S. mahagoni seed extract in doses of 100, 200, 300, 400, and 500 mg/kgBW, and (8 the acarbose group, was given 90% sucrose orally followed by acarbose. Glucose levels in each animal were measured at 0, 30, 60, 90, and 120 min after treatment. The results showed the greatest inhibition of α-glucosidase in ethanolic extract, using maceration methods. This ethanolic-maceration S. mahagoni seed extract also showed hypoglycemic effects in hyperglycemic rats at dose from 100 to 500 mg/kgBW. Ethanolic extract of S. mahagoni seed, using maceration method, can be proposed as potential antidiabetic agent.

  7. Effect of Sitagliptin on Markers of Risk Factors and Risk Factors Correlated with Cardiovascular Complications of Type 2 Diabetes%西格列汀对2型糖尿病心血管并发症相关危险因素及标志物的影响

    Institute of Scientific and Technical Information of China (English)

    张坤; 任巧华; 吴韬; 杜俊文

    2016-01-01

    into Sitagliptin group (30 cases) and Acarbose group (30 cases).The two groups were respectively given a daily dose of 100 mil-ligram of Sitagliptin and a daily dose of 150 milligram of Acarbose in addition to routine treatment for 24 weeks.The body mass index (BMI), glucose level, blood pressure, carotid intimae media thickness (CIMT) and the markers of cardiovascular risk factor of the two groups pretherapy and 24 weeks after treatment were observed and compared .The adverse reaction of two groups during therapy was also observed .Results Compared with that of pretherapy , the levels of BMI , level of fasting plas-ma glucose, 2-hour postprandial blood glucose and glycosylated hemoglobin were decreased after 24 weeks of treatment in both groups.After 24 weeks of treatment , the Sitagliptin group had a greater decrease in BMI , compared with the Acarbose group ( P<0.05 ) .Compared with that of pretherapy , the CIMT was decreased in Sitagliptin group after 24 weeks of treatment .Af-ter 24 weeks of treatment , compared with Acarbose group , the CIMT in Sitagliptin group was obviously reduced ( P<0.05 ) . Compared with that of pretherapy , the levels of homocysteine , C-reactive protein , mannose binding lectin , plasminogen activa-tor inhibitor-1, mat-rix metalloproteinase-9 declined significantly in the Sitagliptin group after 24 weeks of treatment .After 24 weeks of treatment , compared with those of Acarbose group , the markers of Sitagliplin group were lower ( P<0.05 ) .Conclu-sion Sitagliptin has similar effect in reducing blood glucose level as Acarbose , but Sitagliptin can reduce body weight effec-tively and has some protective effect on cardiovascular complications through inhibition of theses markers .

  8. Chemical Constituents of Malaysian U. cordata var. ferruginea and Their in Vitro α-Glucosidase Inhibitory Activities.

    Science.gov (United States)

    Abdullah, Nur Hakimah; Salim, Fatimah; Ahmad, Rohaya

    2016-01-01

    Continuing our interest in the Uncaria genus, the phytochemistry and the in-vitro α-glucosidase inhibitory activities of Malaysian Uncaria cordata var. ferruginea were investigated. The phytochemical study of this plant, which employed various chromatographic techniques including recycling preparative HPLC, led to the isolation of ten compounds with diverse structures comprising three phenolic acids, two coumarins, three flavonoids, a terpene and an iridoid glycoside. These constituents were identified as 2-hydroxybenzoic acid or salicylic acid (1), 2,4-dihydroxybenzoic acid (2), 3,4-dihydroxybenzoic acid (3), scopoletin or 7-hydroxy-6-methoxy-coumarin (4), 3,4-dihydroxy-7-methoxycoumarin (5), quercetin (6), kaempferol (7), taxifolin (8), loganin (9) and β-sitosterol (10). Structure elucidation of the compounds was accomplished with the aid of 1D and 2D Nuclear Magnetic Resonance (NMR) spectral data and Ultraviolet-Visible (UV-Vis), Fourier Transform Infrared (FTIR) spectroscopy and mass spectrometry (MS). In the α-glucosidase inhibitory assay, the crude methanolic extract of the stems of the plant and its acetone fraction exhibited strong α-glucosidase inhibition activity of 87.7% and 89.2%, respectively, while its DCM fraction exhibited only moderate inhibition (75.3%) at a concentration of 1 mg/mL. The IC50 values of both fractions were found to be significantly lower than the standard acarbose suggesting the presence of potential α-glucosidase inhibitors. Selected compounds isolated from the active fractions were then subjected to α-glucosidase assay in which 2,4-dihydroxybenzoic acid and quercetin showed strong inhibitory effects against the enzyme with IC50 values of 549 and 556 μg/mL compared to acarbose (IC50 580 μg/mL) while loganin and scopoletin only showed weak α-glucosidase inhibition of 44.9% and 34.5%, respectively. This is the first report of the isolation of 2-hydroxybenzoic acid, 2,4-dihydroxybenzoic acid and loganin from the genus and

  9. 2007~2009年某院降糖药应用分析%Use of hypoglycemic drugs in a hospital: 2007-2009

    Institute of Scientific and Technical Information of China (English)

    汪铁山; 陈莉婧; 张生潭; 林敬明

    2011-01-01

    Objective To investigate the characteristics and use of hypoglycemic drugs in a hospital of Guangzhou and to provide references for clinical rational use of drugs.Methods The use of hypoglycemic drugs from 2007 to 2009 was statistically analyzed, including the amount of drugs, consumption sum, DDDs, DDC and order ratio.Results The consumption sum of hypoglycemic drugs increased year by year with annual increase rates of 43.37% and 41.54 %, respectively.Of all the oral hypoglycemic drugs used, the consumption sum of acarbose tablets, metformin hydrochloride tablets and gliclazide modified release tablets remained top 3 over the 3 years, and acarbose tablets steadily ranked first in DDDs.Of all the insulin injections used, Humulin 70/30 took the lead in consumption quantity and consumption sum over the 3 years.Conclusion The use of hypoglycemic drugs is basically stable and reasonable in spite of their rapid increase in both consumption sum and quantity.%目的 了解广州市某医院降糖药应用特点和发展趋势,为临床合理用药提供参考.方法 对该院2007~2009年降糖药主要品种、销售金额、用药频度(DDDs)、日均费用(DDC)和排序比进行统计和分析.结果 3年来降糖药销售金额逐年增长,增长率分别为43.37%和41.54%.其中,口服降糖药销售金额排序中,阿卡波糖片、盐酸二甲双胍片和格列齐特缓释片连续3年均排在前3位,阿卡波糖片DDDs排序3年均为最大;注射用胰岛素类药物中,优泌灵70/30混合型使用数量及销售金额连续3年均位居榜首.结论 该院降糖药销售金额和使用数量增长较快,但其应用基本稳定、较为合理.

  10. Inhibition of Qiaojing Bushen Capsule on Intestinal Glucose Absorption in vitro%荞精补肾胶囊对小肠葡萄糖吸收的体外抑制作用

    Institute of Scientific and Technical Information of China (English)

    高秀娟; 马会霞; 姚荣妹; 孙娜; 江春花; 喇孝瑾

    2012-01-01

    Objective- To observe inhibition of Qiaojing Bushen capsules (QJBS) in vitro on glucose absorptionin small intestinal. Method; SD rats were fasted and gave water for 24 hours, then sacrificed to prepare small intestine in vitro everted model. Rats were divided into the blank control group, and acarbose tablets group 0. 25 g · L-1 and QJBS group: QJBS 1-QJBS 5 (2. 5, 5.0, 10. 0, 20. 0, 40. 0 g · L-1). The sugar substrate and tested drugs were added into gut sac, which were incubated for 120 min at 37 t to determin glucose concentrations, and the inhibition rate was calculated. Result; Each group of QJBS can inhibit small intestinal absorption of glucose, when the drug concentration was 20 g · L-1 , inhibitory effect was the most obvious. The inhibition rat was (67. 7 ± 10.5)%, which was equal to acarbose. Conclusion: QJBS can inhibit intestinal glucose absorption, the effect may be related to inhibition of intestinal a-glucosidase.%目的:观察荞精补肾胶囊(QJBS)体外抑制小肠葡萄糖吸收的作用.方法:SD大鼠禁食不禁水24 h,处死,制备小肠离体外翻模型,随机分为空白对照组、阿卡波糖对照组(0.25 g·L-1)和QJBS 1 ~ QJBS 5 (2.5,5.0,10.0,20.0,40.0 g·L-1).将肠囊分别放人等量的营养液中,加入麦芽糖及受试药物,在37℃水浴箱中孵育120 min,测定葡萄糖浓度并计算抑制率.结果:QJBS各组对离体小肠葡萄糖的吸收具有抑制作用,当药物质量浓度为20.0 g·L-1,抑制作用最明显,抑制率为(67.7±10.5)%,与阿卡波糖抑制作用相当.结论:QJBS能够抑制小肠对葡萄糖的吸收,其作用可能与抑制肠道α-糖苷酶类有关.

  11. Optimization of enzymatic production of anti-diabetic peptides from black bean (Phaseolus vulgaris L.) proteins, their characterization and biological potential.

    Science.gov (United States)

    Mojica, Luis; de Mejía, Elvira González

    2016-02-01

    The aim was to optimize the production of bioactive peptides from black bean (Phaseolus vulgaris L.) protein isolate and to determine their biological potential using biochemical and in silico approaches. Protein fractions were generated using eight commercially available proteases after 2, 3 and 4 h and 1:20, 1:30 and 1:50 enzyme/substrate (E/S) ratios. The best combination of conditions to generate anti-diabetic peptides was with alcalase for 2 h and E/S of 1:20; with inhibition values for dipeptidyl peptidase IV (DPP-IV, 96.7%), α-amylase (53.4%) and α-glucosidase (66.1%). Generated peptides were characterized using LC-ESI-MS/MS. Molecular docking analysis was performed to predict individual peptide biological potential using DockingServer®. Peptides EGLELLLLLLAG, AKSPLF and FEELN inhibited DPP-IV more efficiently in silico through free energy interactions of -9.8, -9.6 and -9.5 kcal mol(-1), respectively, than the control sitagliptin (-8.67 kcal mol(-1)). The peptide TTGGKGGK (-8.97 kcal mol(-1)) had higher inhibitory potential on α-glucosidase compared to the control acarbose (-8.79 kcal mol(-1)). Peptides AKSPLF (-10.2 kcal mol(-1)) and WEVM (-10.1 kcal mol(-1)) generated a lower free energy interaction with the catalytic site of α-amylase in comparison with acarbose (-9.71 kcal mol(-1)). Bean peptides inhibited the tested enzymes through hydrogen bonds, polar and hydrophobic interactions. The main bindings on the catalytic site were with ASP192, GLU192 and ARG 253 on DPP-IV; TYR151, HIS201 and ILE235 on α-amylase; and ASP34, THR83 and ASN32 on α-glucosidase. For the first time, a systematic evaluation and characterization of the anti-diabetic peptides from black bean protein isolate is presented with the potential for inhibiting important molecular markers related to diabetes. PMID:26824775

  12. Chemical Constituents of Malaysian U. cordata var. ferruginea and Their in Vitro α-Glucosidase Inhibitory Activities

    Directory of Open Access Journals (Sweden)

    Nur Hakimah Abdullah

    2016-04-01

    Full Text Available Continuing our interest in the Uncaria genus, the phytochemistry and the in-vitro α-glucosidase inhibitory activities of Malaysian Uncaria cordata var. ferruginea were investigated. The phytochemical study of this plant, which employed various chromatographic techniques including recycling preparative HPLC, led to the isolation of ten compounds with diverse structures comprising three phenolic acids, two coumarins, three flavonoids, a terpene and an iridoid glycoside. These constituents were identified as 2-hydroxybenzoic acid or salicylic acid (1, 2,4-dihydroxybenzoic acid (2, 3,4-dihydroxybenzoic acid (3, scopoletin or 7-hydroxy-6-methoxy-coumarin (4, 3,4-dihydroxy-7-methoxycoumarin (5, quercetin (6, kaempferol (7, taxifolin (8, loganin (9 and β-sitosterol (10. Structure elucidation of the compounds was accomplished with the aid of 1D and 2D Nuclear Magnetic Resonance (NMR spectral data and Ultraviolet-Visible (UV-Vis, Fourier Transform Infrared (FTIR spectroscopy and mass spectrometry (MS. In the α-glucosidase inhibitory assay, the crude methanolic extract of the stems of the plant and its acetone fraction exhibited strong α-glucosidase inhibition activity of 87.7% and 89.2%, respectively, while its DCM fraction exhibited only moderate inhibition (75.3% at a concentration of 1 mg/mL. The IC50 values of both fractions were found to be significantly lower than the standard acarbose suggesting the presence of potential α-glucosidase inhibitors. Selected compounds isolated from the active fractions were then subjected to α-glucosidase assay in which 2,4-dihydroxybenzoic acid and quercetin showed strong inhibitory effects against the enzyme with IC50 values of 549 and 556 μg/mL compared to acarbose (IC50 580 μg/mL while loganin and scopoletin only showed weak α-glucosidase inhibition of 44.9% and 34.5%, respectively. This is the first report of the isolation of 2-hydroxybenzoic acid, 2,4-dihydroxybenzoic acid and loganin from the genus

  13. Study on Inhibition Effect of Syzygium cumini Extracts on the Activity of α-glucosidase%乌墨根部提取物对α-葡萄糖苷酶抑制活性的研究

    Institute of Scientific and Technical Information of China (English)

    张富东; 李玲; 牛艳芬; 高丽辉; 林华; 刘旭

    2014-01-01

    目的:探讨乌墨根部提取物对α-葡萄糖苷酶的抑制活性。方法:通过建立体外α-葡萄糖苷酶抑制模型,对乌墨根部提取物进行活性筛选,并对化合物浓度与抑制活性关系进行研究。结果:粗提物12,17,21在体外对α-葡萄糖苷酶均有一定的抑制活性,其中粗提物21的抑制活性(IC50=94.89μg/mL),远高于阳性对照阿卡波糖的抑制活性(IC50=1095.65μg/mL)。结论:乌墨根部提取物对α-葡萄糖苷酶有抑制活性,具有一定的潜在开发价值。%Objective:To investigate the inhibition effect of the extracts from the root ofSyzygiumcuminion the activity ofα- glucosidase.Methods:By establishingα- glucosidase screen inhibitory model,the activity of ex-tracts from the root ofSyzygiumcuminiwas screened. The relationship between the inhibitory ratio and the extract concentration was also studied.Results:Compounds 12,17,21 showed a good inhibitory effect on the activity ofα- glucosidase,and the inhibitory effect of compound 21(IC50 = 94.89μg/mL)was much higher than that of the pos-itive control of acarbose(IC50 = 1 095.65μg/mL).Conclusion:The extracts from the root ofSyzygiumcumini have inhibition effects on the activity ofα- glucosidase,and presented a certain potential value in the development and utilization.

  14. 2012-2014年南京地区34家医院常用口服降糖药利用分析%Utilization of Oral Hypoglycemic Drugs in 34 Hospitals in Nanjingfrom 2012 to 2014

    Institute of Scientific and Technical Information of China (English)

    王璐璐; 刘慧; 陶祥

    2016-01-01

    目的:了解南京地区口服降糖药的最新应用近况和发展趋势,为临床合理使用口服降糖药提供参考。方法:根据长江流域医药情报研究所提供的南京地区2012-2014年口服降糖药的销售数据,采用限定日剂量分析法,对该地区34家医院近三年口服降糖药的销售金额、用药频度(DDDs)和限定日费用(DDC)等进行回顾性统计与分析。结果:销售金额排名前三位的药物是阿卡波糖、格列美脲、二甲双胍,DDDs排名前三位的药物是格列美脲、二甲双胍、阿卡波糖,总销售金额和总DDDs均呈逐年增长趋势,销售金额与DDDs的序号比值在0.3~2.3之间。结论:2012-2014年南京地区口服降糖药需求量逐年增加,药物使用符合安全、有效、经济的用药原则。%Objective:To evaluate the utilization and trend of oral hypoglycemic drugs in Nanjing area, and provideclinical references for the rational use of drugs.Methods:According to the sales data of oral hypoglycemic drugs in 34 hospitals in Nanjing area from 2012 to 2014,its utilization was analyzed retrospectively in aspects of consumption sum,DDDs and DDC bymeans of defined daily dose.Results:The top 3 oral hypoglycemic drugs in the list of consumption sum were acarbose, glimepiride and metformin. In terms of DDDs, glimepiride, metformin and acarbose ranked top 3. The consumption sum and DDDs of oral hypoglycemic drugs increased year by year in Nanjing area. The ratio of serial number of consumption sum and DDDs was from 0.3 to 2.3.Conclusion:Thedemand of oral hypoglycemic drugs increased year by year from 2012 to 2014, and its utilization conformed to safe,effective and economic principles.

  15. Analysis on Use of Hypoglycemic Drugs in Our Hospital during 2008-2010%2008-2010年我院降血糖药物用药分析

    Institute of Scientific and Technical Information of China (English)

    林国强; 沈斌

    2012-01-01

    Objective To investigate the current situation and the development trend of the hypoglycemic drugs used in our hospital to provide reference for the clinical application of antidiabetic drugs and its management. Methods The data of hypoglycemic drugs in the medical supply store were collected based on the used amount, defined daily dosages (DDDs) and the sums of money for statistical analysis during 2008 - 2010. Results The average annual increasing rate of the consumption amount of antidiabetic drugs was 40% during these three years. Acarbose occupied the first place in the list of the sum of consumption money and DDDs. Sulfonylureas and biguanides were most commonly used hypoglycemic drugs in clinic during successive 3 years, accounting for 32% of the total value of DDDs in whole antidiabetic drugs. The first line of antidiabetic drugs included metformin, gliclazide, acarbose, glipizide and insulin. Conclusion The used amounts of hypoglycemic drugs are gradually increased with the increase of diabetic patients year by year. Therefore, more attention should be paid to the curative effects and safety in medication.%目的 为降血糖药物的临床应用和管理提供参考.方法 对2008年至2010年医院药库出库的降血糖药物使用金额、用药频度(DDDs)、用药金额、各年度DDDs前10位药物等进行统计分析.结果 3年间降血糖药物销售金额年平均增长率为40%.销售金额及DDDs居首位的是阿卡渡糖,磺酰脲类和双胍类连续3年为临床主要使用的降血糖药物,占所有降血糖药物DDDs总值的32%;二甲双胍、格列齐特、阿卡波糖、格列美脲、胰岛素等为临床一线用药.结论 降血糖药物的用量随着糖尿病患者的增加逐年增长,因此临床用药应注意药物疗效及安全性.

  16. Product-Specific Regulatory Pathways to Approve Generic Drugs: The Need for Follow-up Studies to Ensure Safety and Effectiveness.

    Science.gov (United States)

    Kesselheim, Aaron S; Gagne, Joshua J

    2015-10-01

    Generic drugs possessing the same active ingredients, dosage form, strength, route of administration, and labeling can be approved by the US Food and Drug Administration (FDA) as interchangeable with a brand-name drug without needing to repeat the formal Phase I, II, and III clinical trials conducted by the original manufacturers. In recent years, the FDA has approved several generic drugs using product-specific testing to determine therapeutic equivalence in accordance with the unique features of the particular drug. These have been used in two primary situations: (1) cases for which certain bioequivalence studies were not relevant; and (2) cases of complex molecules that may require specially tailored pharmaceutical equivalence studies. Examples include venlafaxine extended release, acarbose, vancomycin capsules, sodium ferric gluconate, salmon calcitonin nasal spray, and enoxaparin. Product-specific approaches to demonstrating therapeutic equivalence are essential to avoid delays in low-cost generic drug availability but can have important clinical implications; yet, currently, there is no formal process in place to monitor the safety and effectiveness of generic drugs approved using modified regulatory pathways. Several strategies can be used to monitor the safety and effectiveness of generic drugs approved via product-specific determinations of therapeutic equivalence.

  17. The role of lipid and carbohydrate digestive enzyme inhibitors in the management of obesity: a review of current and emerging therapeutic agents.

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    Tucci, Sonia A; Boyland, Emma J; Halford, Jason Cg

    2010-01-01

    Obesity is a global epidemic associated with significant morbidity and mortality in adults and ill health in children. A proven successful approach in weight management has been the disruption of nutrient digestion, with orlistat having been used to treat obesity for the last 10 years. Although orlistat-induced weight loss remains modest, it produces meaningful reductions in risk factors for obesity-related conditions such as diabetes and cardiovascular disease. Moreover, this lipase inhibitor is free of the serious side effects that have dogged appetite-suppressing drugs. This success had driven investigation into new generation nutraceuticals, supplements and pharmaceutical agents that inhibit the breakdown of complex carbohydrates and fats within the gut. This review focuses on agents purported to inhibit intestinal enzymes responsible for macronutrient digestion. Except for some synthetic products, the majority of agents reviewed are either botanical extracts or bacterial products. Currently, carbohydrate digestion inhibitors are under development to improve glycemic control and these may also induce some weight loss. However, colonic fermentation induced side effects, such as excess gas production, remain an issue for these compounds. The α-glucosidase inhibitor acarbose, and the α-amylase inhibitor phaseolamine, have been used in humans with some promising results relating to weight loss. Nonetheless, few of these agents have made it into clinical studies and without any clinical proof of concept or proven efficacy it is unlikely any will enter the market soon. PMID:21437083

  18. Gynura procumbens Extract Alleviates Postprandial Hyperglycemia in Diabetic Mice

    Science.gov (United States)

    Choi, Sung-In; Park, Mi Hwa; Han, Ji-Sook

    2016-01-01

    This study was designed to investigate the inhibitory effect of Gynura procumbens extract against carbohydrate digesting enzymes and its ability to ameliorate postprandial hyperglycemia in streptozotocin (STZ)-induced diabetic mice. G. procumbens extract showed prominent α-glucosidase and α-amylase inhibitory effects. The half-maximal inhibitory concentration (IC50) of G. procumbens extract against α-glucosidase and α-amylase was 0.092±0.018 and 0.084±0.027 mg/mL, respectively, suggesting that the α-amylase inhibition activity of the G. procumbens extract was more effective than that of the positive control, acarbose (IC50=0.164 mg/mL). The increase in postprandial blood glucose levels was more significantly alleviated in the G. procumbens extract group than in the control group of STZ-induced diabetic mice. Moreover, the area under the curve significantly decreased with G. procumbens extract administration in STZ-induced diabetic mice. These results suggest that G. procumbens extract may help alleviate postprandial hyperglycemia by inhibiting carbohydrate digesting enzymes. PMID:27752493

  19. Inhibition of key enzymes related to diabetes and hypertension by Eugenol in vitro and in alloxan-induced diabetic rats.

    Science.gov (United States)

    Mnafgui, Kais; Kaanich, Fatima; Derbali, Amal; Hamden, Khaled; Derbali, Fatma; Slama, Sadok; Allouche, Noureddine; Elfeki, Abdelfattah

    2013-12-01

    The present study investigated the effect of treating diabetic rats with eugenol (EG). In vitro enzyme activity was measured in the presence of eugenol, and it was found to inhibit pancreatic α-amylase (IC(50) = 62.53 µg/mL) and lipase (IC(50) = 72.34 µg/mL) as well as angiotensin converting enzyme (ACE) activity (IC50 = 130.67 µg/mL). In vivo, EG reduced the activity of amylase in serum, pancreas and intestine also the peak level of glucose by 60% compared to diabetic rats. Furthermore, eugenol similar to acarbose reduced serum glycosylated hemoglobin (HbA1c), lipase and ACE levels. In addition, treatments with EG showed notable decrease in serum total-cholesterol, triglycerides and low density lipoprotein-cholesterol levels with an increase of high density lipoprotein-cholesterol. Overall, EG significantly reverted back to near normal the values of the biochemical biomarkers such as transaminases (AST&ALT), alkaline phosphatase (ALP), creatine phosphokinase (CPK) and gamma-glutamyl transpeptidase (GGT) activities, total-bilirubin, creatinine, urea and uric acid rates.

  20. In Vitro Screening of Medicinal Plants Used in Mexico as Antidiabetics with Glucosidase and Lipase Inhibitory Activities

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    Guillermo Ramírez

    2012-01-01

    Full Text Available This work shows the inhibitory effect on glucosidase and lipase enzymes of 23 medicinal plants described as traditional treatments for diabetes in several Mexican sources. Hydroalcoholic extracts of selected plants were evaluated at 1 mg/mL for glucosidase and 0.25 mg/mL for lipase inhibitory activities, respectively. Camellia sinensis, acarbose, and orlistat were used as positive controls. Dose-response curves were done with the most active species. Sixty percent of all tested extracts inhibited more than 25% of α-glucosidase activity. C. sinensis displayed an inhibition of 85% (IC50 = 299 μg/mL, while Ludwigia octovalvis and Iostephane heterophylla showed the highest inhibition (82.7 %, IC50 = 202 μg/mL and 60.6%, CI50 = 509 μg/mL, resp.. With respect to lipase activity, L. octovalvis and Tecoma stans were the most inhibiting treatments (31.4%, IC50 = 288 μg/mL; 27.2%, IC50 = 320 μg/mL, while C. sinensis displayed 45% inhibition (IC50 = 310 μg/mL. These results indicate that a high proportion of plants used in Mexico as treatment for diabetes displays significant inhibition of these digestive enzymes.

  1. Synthesis, In vitro and Docking Studies of New Flavone Ethers as α-Glucosidase Inhibitors.

    Science.gov (United States)

    Imran, Syahrul; Taha, Muhammad; Ismail, Nor Hadiani; Kashif, Syed Muhammad; Rahim, Fazal; Jamil, Waqas; Wahab, Habibah; Khan, Khalid Mohammed

    2016-03-01

    We report herein the synthesis, α-glucosidase inhibition and docking studies for a series of 3-15 new flavones. A simple nucleophilic substitution reaction takes place between 3'hydroxyflavone (2) with halides to afford the new flavones. Chalcone (1), 3'hydroxyflavone (2) and the newly synthesized flavones (3-15) were being evaluated for their ability to inhibit activity of α-glucosidase. Compounds 2, 3, 5, 7-10 and 13 showed good inhibitory activity with IC50 values ranging between 1.26 and 36.44 μM as compared to acarbose (IC50 = 38.25 ± 0.12 μM). Compounds 5 (5.45 ± 0.08 μM), 7 (1.26 ± 0.01 μM) and 8 (8.66 ± 0.08 μM) showed excellent inhibitory activity, and this may be due to trifluoromethyl substitution that is common for these compounds. Compound 7, a 2,5-trifluoromethyl-substituted compound, recorded the highest inhibition activity, and it is thirty times better than the standard drug. Docking studies for compound 7 suggest that both trifluoromethyl substituents are well positioned in a binding pocket surrounded by Phe300, Phe177, Phe157, Ala278, Asp68, Tyr71 and Asp214. The ability of compound 7 to interact with Tyr71 and Phe177 is extremely significant as they are found to be important for substrates recognition by α-glucosidase. PMID:26362113

  2. New Gallotannin and other Phytochemicals from Sycamore Maple (Acer pseudoplatanus) Leaves.

    Science.gov (United States)

    Zhang, Lu; Tu, Zong-cai; Yuan, Tao; Ma, Hang; Niesen, Daniel B; Wang, Hui; Seeram, Navindra P

    2015-11-01

    The maple (Acer) genus is a reported source of bioactive (poly)phenols, including gallotannins, but several of its members, such as the sycamore maple (A. pseudoplatanus), remain uninvestigated. Herein, thirty-nine compounds, including a new gallotannin, 1,2,3-tri-O-galloyl-6-O-(p-hydroxybenzoyl)-β-D- glucopyranoside (1), and thirty-eight (2-39) known compounds, consisting of four gallotannins, one ellagitannin, thirteen flavonoids, eight hydroxycinnamic acids, ten benzoic acid derivatives, and two sesquiterpenoids, were isolated from sycamore maple leaves. Their structures were determined based on NMR and mass spectral analyses. The isolates were evaluated for α-glucosidase inhibitory and antioxidant activities. Among the isolates, the gallotannins were the most potent α-glucosidase inhibitors with thirteen-fold more potent activity compared with the clinical drug, acarbose (IC50 = 16-31 vs. 218 µM). Similarly, the gallotannins showed the highest antioxidant activities, followed by the other phenolic sub-classes, while the sesquiterpenoids were inactive.

  3. Inhibition of α-Glucosidase by Thiosulfinate as a Target for Glucose Modulation in Diabetic Rats

    Directory of Open Access Journals (Sweden)

    Abdulrahman L. Al-Malki

    2016-01-01

    Full Text Available Postprandial hyperglycemia is a predisposing factor for vascular dysfunction and organ damage. α-glucosidase is a hydrolytic enzyme that increases the glucose absorption rate and subsequently elevates blood glucose levels. Garlic (Allium sativum L. is a rich source of several phytonutrients, including thiosulfinate (THIO. The aim of this study was to evaluate the ability of THIO, a potent inhibitor of intestinal α-glucosidase, to reduce postprandial blood glucose. Male albino rats were randomly assigned to five different groups (n=10/group. Group 1 served as the control group. Groups 2–5 were injected intraperitoneally with a single dose of streptozotocin (STZ to induce diabetes. Group 2 comprised untreated diabetic rats. Groups 3 and 4 contained diabetic rats that were given THIO orally (20 mg/kg body weight/day and 40 mg/kg body weight/day, resp.. Group 5 was the positive control having diabetic rats treated orally with acarbose (10 mg/kg body weight/day; positive control. Diabetic rats treated with THIO displayed a significant blood glucose reduction (p<0.001 and < 0.01 by analysis of variance, resp. and a significant elevation in insulin compared with that of untreated rats. THIO is an effective noncompetitive intestinal α-glucosidase inhibitor that promotes hypoglycemic action (p<0.001 in STZ-injected rats. THIO is a promising agent for the management of postprandial hyperglycemia.

  4. Inhibition of α-Glucosidase by Thiosulfinate as a Target for Glucose Modulation in Diabetic Rats.

    Science.gov (United States)

    Al-Malki, Abdulrahman L

    2016-01-01

    Postprandial hyperglycemia is a predisposing factor for vascular dysfunction and organ damage. α-glucosidase is a hydrolytic enzyme that increases the glucose absorption rate and subsequently elevates blood glucose levels. Garlic (Allium sativum L.) is a rich source of several phytonutrients, including thiosulfinate (THIO). The aim of this study was to evaluate the ability of THIO, a potent inhibitor of intestinal α-glucosidase, to reduce postprandial blood glucose. Male albino rats were randomly assigned to five different groups (n = 10/group). Group 1 served as the control group. Groups 2-5 were injected intraperitoneally with a single dose of streptozotocin (STZ) to induce diabetes. Group 2 comprised untreated diabetic rats. Groups 3 and 4 contained diabetic rats that were given THIO orally (20 mg/kg body weight/day and 40 mg/kg body weight/day, resp.). Group 5 was the positive control having diabetic rats treated orally with acarbose (10 mg/kg body weight/day; positive control). Diabetic rats treated with THIO displayed a significant blood glucose reduction (p < 0.001 and < 0.01 by analysis of variance, resp.) and a significant elevation in insulin compared with that of untreated rats. THIO is an effective noncompetitive intestinal α-glucosidase inhibitor that promotes hypoglycemic action (p < 0.001) in STZ-injected rats. THIO is a promising agent for the management of postprandial hyperglycemia. PMID:27051452

  5. Pharmacotherapy of polycystic ovary syndrome--an update.

    Science.gov (United States)

    Saha, Lekha; Kaur, Sharonjeet; Saha, Pradip Kumar

    2012-02-01

    Polycystic ovary syndrome (PCOS) is a persisting challenge to clinical and basic research scientists as none of the presently available medications have been fully able to combat these consequences. The aim of the present review is to summarize the different lines of treatment available for the different symptomologies that women with PCOS presents. In this comprehensive review, search was made for various treatment options available for PCOS by using Cochrane library, Pubmed, Medline, in addition to the relevant printed medical journals and periodicals. The search results revealed that oral contraceptives containing oestrogen and progesterone regularize the menstruation, antiandrogens like spironolactone and drosperinone have proven to be effective in hirsutism and acne, clomiphene is the gold standard for ovulation induction, but multiple pregnancies and clomiphene failure add to its limitation. Hence, aromatase inhibitors like letrozole, low-dose gondotropins, and ovarian drilling procedure have shown to be beneficial effect in clomiphene-resistant cases. Insulin sensitizers such as metformin, thiazolidinediones, and d-chiro-inositol increase insulin sensitivity and improve ovulation rate. Recently, melatonin, N-acetyl cysteine, acarbose, and statins have shown positive results in different symptomologies of PCOS. The results show that PCOS treatment constitutes varied line of treatment depending upon the clinical features with which a woman is presenting. Still, unfortunately, none of the treatments are fully able to combat the PCOS. PMID:21210850

  6. Comparative evaluation of polysaccharides isolated from Astragalus, oyster mushroom, and yacon as inhibitors of α-glucosidase.

    Science.gov (United States)

    Zhu, Zhen-Yuan; Zhang, Jing-Yi; Chen, Li-Jing; Liu, Xiao-Cui; Liu, Yang; Wang, Wan-Xiao; Zhang, Yong-Min

    2014-04-01

    The incidence of diabetes has increased considerably, and become the third serious chronic disease following cancer and cardiovascular diseases. Though acarbose, metformin, and 1-deoxynojirimycin have good efficacy for clinical application as hypoglycemic drugs, their expensive costs and some degree of side effects have limited their clinical application. Recently, increasing attention has concentrated on the polysaccharides from natural plant and animal sources for diabetes. In order to illustrate the pharmaceutical activity of polysaccharides as natural hypoglycemic agents, polysaccharides isolated from Astragalus, oyster mushroom, and Yacon were evaluated for their inhibitory effects on α-glucosidase. Polysaccharides were extracted and purified from Astragalus, Oyster mushroom, and Yacon with hot water at 90 °C for 3 h, respectively. The total sugar content of the polysaccharide was determined by the phenol-sulfuric acid method. The α-glucosidase inhibitory activity was measured by the glucose oxidase method. The results exhibited that the inhibitory effects on α-glucosidase were in decreasing order, Astragalus > oyster mushroom > Yacon. The α-glucosidase inhibition percentage of Astragalus polysaccharide and oyster mushroom polysaccharide were over 40% at the polysaccharide concentration of 0.4 mg·mL(-1). The IC50 of Astragalus polysaccharide and oyster mushroom polysaccharide were 0.28 and 0.424 mg·mL(-1), respectively. The information obtained from this work is beneficial for the use polysaccharides as a dietary supplement for health foods and therapeutics for diabetes. PMID:24863354

  7. Sucrose induces vesicle accumulation and autophagy.

    Science.gov (United States)

    Higuchi, Takahiro; Nishikawa, Jun; Inoue, Hiroko

    2015-04-01

    It has been shown that the treatment of mammalian cells with sucrose leads to vacuole accumulation associated with lysosomes and upregulation of lysosomal enzyme expression and activity. Autophagy is an evolutionarily conserved homeostatic process by which cells deliver cytoplasmic material for degradation into lysosomes, thus it is probable that sucrose affects the autophagic activity. The role of sucrose in autophagy is unknown; however, another disaccharide, trehalose has been shown to induce autophagy. In the current study, we used mouse embryonic fibroblasts to investigate whether sucrose induces autophagy and whether vesicle formation is associated with autophagy. The results showed that sucrose induces autophagy while being accumulated within the endosomes/lysosomes. These vesicles were swollen and packed within the cytoplasm. Furthermore, trehalose and the trisaccharide raffinose, which are not hydrolyzed in mammalian cells, increased the rate of vesicles accumulation and LC3-II level (a protein marker of autophagy). However, fructose and maltose did not show the same effects. The correlation between the two processes, vesicle accumulation and autophagy induction, was confirmed by treatment of cells with sucrose plus invertase, or maltose plus acarbose-the α-glucosidase inhibitor-and by sucrose deprivation. Results also showed that vesicle accumulation was not affected by autophagy inhibition. Therefore, the data suggest that sucrose-induced autophagy through accumulation of sucrose-containing vesicles is caused by the absence of hydrolysis enzymes.

  8. In vitro and in vivo comparison of the biological activities of two traditionally and widely used Arum species from Jordan: Arum dioscoridis Sibth & Sm. and Arum palaestinum Boiss.

    Science.gov (United States)

    Afifi, Fatma U; Kasabri, Violet; Litescu, Simona C; Abaza, Ismail M

    2016-08-01

    Arum dioscoridis and A. palaestinum (Araceae) are indigenous plant species in Jordan. HPLC-MS analysis of A. dioscoridis revealed the presence of apigenin, luteolin, quercetin, quercetin-3-O-β-glucoside, vitexin, isoorientin, esculin, and caffeic and ferulic acids. Both Arum spp., influenced gastrointestinal carbohydrate and lipid digestion and absorption. Orlistat inhibited dose dependently and highly substantially pancreatic lipase (PL) in vitro. Similar to orlistat, Arum species aqueous extracts (AEs), apigenin, caffeic acid and esculin exhibited a concentration related PL inhibition. Comparable to acarbose, dual inhibition of α-amylase/α-glucosidase was observed for both Arum species. Like guar gum, A. dioscoridis AE minimised substantially area under 24 h glucose curve. Acute starch-induced postprandial hyperglycaemia in overnight fasting rats was highly significantly (p < 0.001) decreased by A. dioscoridis AE. A. palaestinum could not perform effectively in either starch- or glucose-fed fasting rats. No antiproliferative effects against colorectal cancer cell lines HT29, HCT116 and SW620 were detected for tested Arum spp.

  9. Turmerin, the antioxidant protein from turmeric (Curcuma longa) exhibits antihyperglycaemic effects.

    Science.gov (United States)

    Lekshmi, P C; Arimboor, Ranjith; Raghu, K G; Menon, A Nirmala

    2012-01-01

    A wide range of proteinaceous inhibitors are present in plants to protect themselves from hydrolytic enzymes. In this study, turmerin, a water-soluble peptide in turmeric rhizomes, was evaluated for its inhibitory potential against glucosidase and its antioxidant (AO) capacity. Turmerin inhibited α-amylase and α-glucosidase activities with IC₅₀ values 31 and 192 µg mL⁻¹, respectively. Under the experimental conditions, those values for a standard glucosidase inhibitor, acarbose, were 81 and 296 µg mL⁻¹, respectively. The AO capacity of turmerin was evaluated using in vitro assay systems. Turmerin showed good DPPH (IC₅₀ = 29 µg mL⁻¹) and superoxide (IC₅₀ = 48 µg mL⁻¹) and moderate ABTS (IC₅₀ = 83 µg mL⁻¹) radical scavenging and Fe(II) chelation (IC₅₀ = 101 µg mL⁻¹) capacities. The inhibitory potential showed by turmerin against enzymes linked to type 2 diabetes, as well as its moderate AO capacity, could rationalise the traditional usage of turmeric rhizome preparations against diabetes.

  10. In vitro antidiabetic and inhibitory potential of turmeric (Curcuma longa L) rhizome against cellular and LDL oxidation and angiotensin converting enzyme.

    Science.gov (United States)

    Lekshmi, P C; Arimboor, Ranjith; Nisha, V M; Menon, A Nirmala; Raghu, K G

    2014-12-01

    Turmeric (Curcuma longa L) rhizome extracts were evaluated for their antidiabetic, antihypertensive and antioxidant potentials. α-Glucosidase (0.4 μg/mL) and α-amylase (0.4 μg/mL) inhibitory potential of turmeric ethyl acetate extract was significantly higher than those of the reference drug acarbose (17.1 μg/mL and 290.6 μg/mL respectively). Protein glycation inhibitory potential of ethyl acetate extract was 800 times higher than that of ascorbic acid. High potential of ethyl acetate extract to scavenge free radicals and to reduce LDL oxidation and cellular oxidative stress was also revealed. The positive correlation obtained between the free radical scavenging capacity of the extracts and their antiglycation potential further confirmed the role of antioxidants in controlling glycation reactions. Ethyl acetate extract was also found as effective in reducing hypertension by inhibiting angiotensin converting enzyme (ACE). Antidiabetic, ACE inhibitory and antioxidant capacities of the extracts were in the order of their curcumin contents.

  11. In silico approach for alpha-amylase inhibitory activity of diosmetin and galangin

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    Arumugam Madeswaran

    2014-10-01

    Full Text Available Objective: The objective of the current study is to evaluate the α-amylase inhibitory activity of diosmetin and galangin using in silico docking studies.Methods: In this perspective, diosmetin and galangin were prepared for the docking evaluation. Acarbose, a known α-amylase inhibitor was used as the standard. In silico docking studies were carried out using recent version of AutoDock 4.2, which has the basic principle of Lamarckian genetic algorithm.Results: The results showed that the selected flavonoids showed binding energy ranging between -6.84 kcal/mol to  -5.96 kcal/mol when compared with that of the standard (-1.97 kcal/mol. Inhibition constant (9.73 µM to 42.76 µM and intermolecular energy (-8.33 kcal/mol to -7.15 kcal/mol of the ligands also coincide with the binding energy.Conclusion: Diosmetin and galangin contributed excellent α-amylase inhibitory activity than the standard because of its structural parameters. These molecular docking analyses of the selected compounds could lead to the further development to find the potent α-amylase inhibitors for the treatment of diabetes.  

  12. In Vitro and in Vivo Anti-Hyperglycemic Effects of Omija (Schizandra chinensis Fruit

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    Young-In Kwon

    2011-02-01

    Full Text Available The entrocytes of the small intestine can only absorb monosaccharides such as glucose and fructose from our diet. The intestinal absorption of dietary carbohydrates such as maltose and sucrose is carried out by a group of a-glucosidases. Inhibition of these enzymes can significantly decrease the postprandial increase of blood glucose level after a mixed carbohydrate diet. Therefore, the inhibitory activity of Omija (Schizandra chinensis extract against rat intestinal a-glucosidase and porcine pancreatic a-amylase were investigated in vitro and in vivo. The in vitro inhibitory activities of water extract of Omija pulp/skin (OPE on a-glucosidase and a-amylase were potent when compared to Omija seeds extract (OSE. The postprandial blood glucose lowering effect of Omija extracts was compared to a known type 2 diabetes drug (Acarbose, a strong a-glucosidase inhibitor in the Sprague-Dawley (SD rat model. In rats fed on sucrose, OPE significantly reduced the blood glucose increase after sucrose loading. Furthermore, the oxygen radical absorbance capacity (ORAC of OSE and OPE was evaluated. OPE had higher peroxyl radical absorbing activity than OSE. These results suggest that Omija, which has high ORAC value with a-glucosidase inhibitory activity and blood glucose lowering effect, could be physiologically useful for treatment of diabetes, although clinical trials are needed.

  13. Phlorotannins from Alaskan Seaweed Inhibit Carbolytic Enzyme Activity

    Science.gov (United States)

    Kellogg, Joshua; Grace, Mary H.; Lila, Mary Ann

    2014-01-01

    Global incidence of type 2 diabetes has escalated over the past few decades, necessitating a continued search for natural sources of enzyme inhibitors to offset postprandial hyperglycemia. The objective of this study was to evaluate coastal Alaskan seaweed inhibition of α-glucosidase and α-amylase, two carbolytic enzymes involved in serum glucose regulation. Of the six species initially screened, the brown seaweeds Fucus distichus and Alaria marginata possessed the strongest inhibitory effects. F. distichus fractions were potent mixed-mode inhibitors of α-glucosidase and α-amylase, with IC50 values of 0.89 and 13.9 μg/mL, respectively; significantly more efficacious than the pharmaceutical acarbose (IC50 of 112.0 and 137.8 μg/mL, respectively). The activity of F. distichus fractions was associated with phlorotannin oligomers. Normal-phase liquid chromatography-mass spectrometry (NPLC-MS) was employed to characterize individual oligomers. Accurate masses and fragmentation patterns confirmed the presence of fucophloroethol structures with degrees of polymerization from 3 to 18 monomer units. These findings suggest that coastal Alaskan seaweeds are sources of α-glucosidase and α-amylase inhibitory phlorotannins, and thus have potential to limit the release of sugar from carbohydrates and thus alleviate postprandial hyperglycemia. PMID:25341030

  14. Triterpene saponins with α-glucosidase inhibition and cytotoxic activity from the leaves of Schefflera sessiliflora.

    Science.gov (United States)

    Nguyen, Tan Phat; Le, Tien Dung; Phan, Nhat Minh; Bui, Trong Dat; Mai, Dinh Tri

    2016-06-01

    From the leaves of Schefflera sessiliflora De P. V., two new triterpene saponins including one oleanane-type saponin, named scheffleraside C (1) and one lupane-type saponin scheffleraside D (2), together with six known triterpene saponins (3-8), were isolated by various chromatography methods. Among them, 3 was found for the first time from natural sources, while 6-8 were isolated for the first time from the genus Schefflera. Their structures were elucidated by IR, UV, HR-ESI-MS, NMR 1D and 2D experiments, and comparison of their NMR data with previously reported data. Their α-glucosidase inhibition and cytotoxic activity against MCF-7 human breast cancer cell lines were evaluated. The isolates (1, 3-5, 8) showed stronger α-glucosidase inhibitory activity (IC50 = 5.99-76.58 μM) than the standard drug acarbose (IC50 = 214.50 μM). At the concentration of 100 μg/ml, the isolates (1, 2) showed appreciable cytotoxic activity (67.92, 63.83%, respectively). PMID:26690849

  15. In vitro screening of medicinal plants used in Mexico as antidiabetics with glucosidase and lipase inhibitory activities.

    Science.gov (United States)

    Ramírez, Guillermo; Zavala, Miguel; Pérez, Julia; Zamilpa, Alejandro

    2012-01-01

    This work shows the inhibitory effect on glucosidase and lipase enzymes of 23 medicinal plants described as traditional treatments for diabetes in several Mexican sources. Hydroalcoholic extracts of selected plants were evaluated at 1 mg/mL for glucosidase and 0.25 mg/mL for lipase inhibitory activities, respectively. Camellia sinensis, acarbose, and orlistat were used as positive controls. Dose-response curves were done with the most active species. Sixty percent of all tested extracts inhibited more than 25% of α-glucosidase activity. C. sinensis displayed an inhibition of 85% (IC(50) = 299 μg/mL), while Ludwigia octovalvis and Iostephane heterophylla showed the highest inhibition (82.7 %, IC(50) = 202 μg/mL and 60.6%, CI(50) = 509 μg/mL, resp.). With respect to lipase activity, L. octovalvis and Tecoma stans were the most inhibiting treatments (31.4%, IC(50) = 288 μg/mL; 27.2%, IC(50) = 320 μg/mL), while C. sinensis displayed 45% inhibition (IC(50) = 310 μg/mL). These results indicate that a high proportion of plants used in Mexico as treatment for diabetes displays significant inhibition of these digestive enzymes. PMID:23082084

  16. In-vitro α-amylase and α-glucosidase inhibitory activity of Adiantum caudatum Linn. and Celosia argentea Linn. extracts and fractions

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    Madhusudhan Telagari

    2015-01-01

    Materials and Methods: The plant extracts were prepared, first with cold maceration (70% v/v ethanol and then by Soxhlation techniques (95% v/v ethanol. Subsequently, the combined extracts were subjected for fractionation. Different concentrations (0.1, 0.2, 0.3, 0.4, and 0.5 mg/ml of extract and fractions were subjected to α-amylase and α-glucosidase inhibitory assay. The absorbance was measured at 540 and 405 nm using multiplate reader and the percentage of α- amylase and α- glucosidase inhibitory activity and IC 50 values of extract and fractions were calculated. Results: Fraction 2 of A. caudatum and fraction 4 of C. argentea has shown highest α-amylase and α-glucosidase inhibitory potential with IC 50 values of 0.241, 0.211 and 0.294, 0.249 mg/ml, respectively, which was comparable with acarbose (0.125 and 0.93 mg/ml. Whereas, extracts and remaining fractions of both the plants have shown lesser activity. Conclusion: The results of the present study indicate that, fraction 2 of A. caudatum, rich in triterpenoids and phenolics and fraction 4 of C. argentea, rich in flavonoids, are effective α- amylase and α- glucosidase inhibitors, which may be helpful to reduce the postprandial glucose levels. Hence, further studies may throw light on the antidiabetic potential of A. caudatum and C. argentea, especially in the management of type 2 diabetes.

  17. Effect of Long-Term Dietary Arginyl-Fructose (AF on Hyperglycemia and HbA1c in Diabetic db/db Mice

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    Kwang-Hyoung Lee

    2014-05-01

    Full Text Available We have previously reported that Amadori compounds exert anti-diabetic effects by lowering sucrose-induced hyperglycemia in normal Sprague-Dawley rats. In the present study we extended our recent findings to evaluate whether α-glucosidase inhibitor arginyl-fructose (AF lowers blood glucose level in diabetic db/db mice, a genetic model for type 2 diabetes. The db/db mice were randomly assigned to high-carbohydrate diets (66.1% corn starch with and without AF (4% in the diet for 6 weeks. Changes in body weight, blood glucose level, and food intake were measured daily for 42 days. Dietary supplementation of AF resulted in a significant decrease of blood glucose level (p < 0.001 and body weight (p < 0.001. The level of HbA1c, a better indicator of plasma glucose concentration over prolonged periods of time, was also significantly decreased for 6-week period (p < 0.001. Dietary treatment of acarbose® (0.04% in diet, a positive control, also significantly alleviated the level of blood glucose, HbA1c, and body weight. These results indicate that AF Maillard reaction product improves postprandial hyperglycemia by suppressing glucose absorption as well as decreasing HbA1c level.

  18. Synthesis of water soluble glycosides of pentacyclic dihydroxytriterpene carboxylic acids as inhibitors of α-glucosidase.

    Science.gov (United States)

    Xu, Jiancong; Nie, Xuliang; Hong, Yanping; Jiang, Yan; Wu, Guoqiang; Yin, Xiaoli; Wang, Chunrong; Wang, Xiaoqiang

    2016-04-01

    A series of compounds were synthesized by glycosylation of maslinic acid (MA) and corosolic acid (CA) with monosaccharides and disaccharides, and the structures of the derivatives were elucidated by standard spectroscopic methods including (1)H NMR, (13)C NMR and HRMS. The α-glucosidase inhibitory activities of all the novel compounds were evaluated in vitro. The solubility and inhibitory activity of α-glucosidase assays showed that the bis-disaccharide glycosides of triterpene acids possessed higher water solubility and α-glucosidase inhibitory activities than the bis-monosaccharide glycosides. Among these compounds, maslinic acid bis-lactoside (8e, IC50 = 684 µM) and corosolic acid bis-lactoside (9e, IC50 = 428 µM) had the best water solubility, and 9e exhibited a better inhibitory activity than acarbose (IC50 = 478 µM). However, most of glycosylated derivatives possessed lower inhibitory activities than the parent compounds, although their water solubility was enhanced obviously. Moreover, the kinetic inhibition studies indicated that 9e was a non-competitive inhibitor, and structure-activity relationships of the derivatives are also discussed. PMID:26974355

  19. Purification of Flavonoids from Chinese Bayberry (Morella rubra Sieb. et Zucc.) Fruit Extracts and α-Glucosidase Inhibitory Activities of Different Fractionations.

    Science.gov (United States)

    Yan, Shuxia; Zhang, Xianan; Wen, Xin; Lv, Qiang; Xu, Changjie; Sun, Chongde; Li, Xian

    2016-01-01

    Chinese bayberry (Morella rubra Sieb. et Zucc.) fruit have a diverse flavonoid composition responsible for the various medicinal activities, including anti-diabetes. In the present study, efficient simultaneous purification of four flavonoid glycosides, i.e., cyanidin-3-O-glucoside (1), myricetin-3-O-rhamnoside (2), quercetin-3-O-galactoside (3), quercetin-3-O-rhamnoside (4), from Chinese bayberry pulp was established by the combination of solid phase extract (SPE) by C18 Sep-Pak(®) cartridge column chromatography and semi-preparative HPLC (Prep-HPLC), which was followed by HPLC and LC-MS identification. The purified flavonoid glycosides, as well as different fractions of fruit extracts of six bayberry cultivars, were investigated for α-glucosidase inhibitory activities. The flavonol extracts (50% methanol elution fraction) of six cultivars showed strong α-glucosidase inhibitory activities (IC50 = 15.4-69.5 μg/mL), which were higher than that of positive control acarbose (IC50 = 383.2 μg/mL). Four purified compounds 1-4 exerted α-glucosidase inhibitory activities, with IC50 values of 1444.3 μg/mL, 418.8 μg/mL, 556.4 μg/mL, and 491.8 μg/mL, respectively. Such results may provide important evidence for the potential anti-diabetic activity of different cultivars of Chinese bayberry fruit and the possible bioactive compounds involved. PMID:27589714

  20. Anti-α-glucosidase and Anti-dipeptidyl Peptidase-IV Activities of Extracts and Purified Compounds from Vitis thunbergii var. taiwaniana.

    Science.gov (United States)

    Lin, Yin-Shiou; Chen, Chiy-Rong; Wu, Wei-Hau; Wen, Chi-Luan; Chang, Chi-I; Hou, Wen-Chi

    2015-07-22

    Ethanol extracts (Et) from the stem (S) and leaf (L) of Vitis thunbergii var. taiwaniana (VTT) were used to investigate yeast α-glucosidase and porcine kidney dipeptidyl peptidase-IV (DPP-IV) inhibitory activities. Both VTT-Et showed complete α-glucosidase inhibition at 0.1 mg/mL; VTT-S-Et and VTT-L-Et showed 26 and 11% DPP-IV inhibition, respectively, at 0.5 mg/mL. The VTT-Et interventions (20 and 50 mg/kg) resulted in improvements in impaired glucose tolerance of diet-induced obese rats. (+)-Hopeaphenol, (+)-vitisin A, and (-)-vitisin B were isolated from the ethyl acetate fractions of S-Et and showed yeast α-glucosidase inhibition (IC50 = 18.30, 1.22, and 1.02 μM) and porcine kidney DPP-IV inhibition (IC50 = 401, 90.75, and 15.3 μM) compared to acarbose (6.39 mM) and sitagliptin (47.35 nM), respectively. Both (+)-vitisin A and (-)-vitisin B showed mixed noncompetitive inhibition against yeast α-glucosidase and porcine kidney DPP-IV, respectively. These results proposed that VTT extracts might through inhibitions against α-glucosidase and DPP-IV improve the impaired glucose tolerance in diet-induced obese rats.

  1. Pilot study on the additive effects of berberine and oral type 2 diabetes agents for patients with suboptimal glycemic control

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    Di Pierro, Francesco; Villanova, Nicola; Agostini, Federica; Marzocchi, Rebecca; Soverini, Valentina; Marchesini, Giulio

    2012-01-01

    Background Suboptimal glycemic control is a common situation in diabetes, regardless of the wide range of drugs available to reach glycemic targets. Basic research in diabetes is endeavoring to identify new actives working as insulin savers, use of which could delay the introduction of injectable insulin or reduce the insulin dose needed. Commonly available as a nutraceutical, berberine is a potential candidate. Methods and results Because its low oral bioavailability can be overcome by P-glycoprotein inhibitors like herbal polyphenols, we have tested the nutraceutical combination of Berberis aristata extract and Silybum marianum extract (Berberol®) in type 2 diabetes in terms of its additive effect when combined with a conventional oral regimen for patients with suboptimal glycemic control. After 90 days of treatment, the nutraceutical association had a positive effect on glycemic and lipid parameters, significantly reducing glycosylated hemoglobin, basal insulin, homeostatic model assessment of insulin resistance, total and low-density lipoprotein cholesterol, and triglycerides. A relevant effect was also observed in terms of liver function by measuring aspartate transaminase and alanine transaminase. The product had a good safety profile, with distinctive gastrointestinal side effects likely due to its acarbose-like action. Conclusion Although further studies should be carried out to confirm our data, Berberol could be considered a good candidate as an adjunctive treatment option in diabetes, especially in patients with suboptimal glycemic control. PMID:22924000

  2. Zinc oxide nanoparticles as novel alpha-amylase inhibitors

    Science.gov (United States)

    Dhobale, Sandip; Thite, Trupti; Laware, S. L.; Rode, C. V.; Koppikar, Soumya J.; Ghanekar, Ruchika-Kaul; Kale, S. N.

    2008-11-01

    Amylase inhibitors, also known as starch blockers, contain substances that prevent dietary starches from being absorbed by the body via inhibiting breakdown of complex sugars to simpler ones. In this sense, these materials are projected as having potential applications in diabetes control. In this context, we report on zinc oxide nanoparticles as possible alpha-amylase inhibitors. Zinc oxide nanoparticles have been synthesized using soft-chemistry approach and 1-thioglycerol was used as a surfactant to yield polycrystalline nanoparticles of size ˜18 nm, stabilized in wurtzite structure. Conjugation study and structural characterization have been done using x-ray diffraction technique, Fourier transform infrared spectroscopy, UV-visible spectroscopy, and transmission electron microscopy. Cytotoxicity studies on human fibrosarcoma (HT-1080) and skin carcinoma (A-431) cell lines as well as mouse primary fibroblast cells demonstrate that up to a dose of 20 μg/ml, ZnO nanoparticles are nontoxic to the cells. We report for the first time the alpha-amylase inhibitory activity of ZnO nanoparticles wherein an optimum dose of 20 μg/ml was sufficient to exhibit 49% glucose inhibition at neutral pH and 35 °C temperature. This inhibitory activity was similar to that obtained with acarbose (a standard alpha-amylase inhibitor), thereby projecting ZnO nanoparticles as novel alpha-amylase inhibitors.

  3. Physicochemical and biofunctional properties of crab chitosan nanoparticles.

    Science.gov (United States)

    Nguyen, The Han; Kwak, Hae Soo; Kim, Sang Moo

    2013-08-01

    The physicochemical and biofunctional properties of crab chitosan nanoparticles of two different sizes (Nano A and B) manufactured by dry milling method were evaluated for commercialization. The deacetylation degrees (DD) of Nano A, B and the control chitosan were 90.9, 93.0, and 92.7% respectively whereas their molecular weights (M(w)) were 43.9, 44.7 and 208.8 kDa. The average sizes of the dispersed Nano A, B and the control chitosan in cetyltrimethylammonium chloride were 735.9, 849.4 and 2,382.4 nm, respectively, which were lower than 1441.7, 2935.6 and 6832.9 nm of the intact chitosans. Chitosan nanoparticles had mild tyrosinase, antioxidant and angiotensin I converting enzyme (ACE), but weak collagenase, elastase and beta-glucuronidase inhibitory activity. However, Nano A had strong alpha-glucosidase inhibitory activity, which was comparable to that of acarbose, a commercial alpha-glucosidase inhibitor. In addition, the minimum inhibitory concentrations (MICs) of chitosan and its nanoparticles ranged from 30 to > 200 microg/mL against each four gram-positive and gram-negative bacteria. Therefore, crab chitosan nanoparticles could be used as a nutraceutical, cosmeceutical or pharmaceutical product.

  4. Grape skin phenolics as inhibitors of mammalian α-glucosidase and α-amylase--effect of food matrix and processing on efficacy.

    Science.gov (United States)

    Lavelli, V; Sri Harsha, P S C; Ferranti, P; Scarafoni, A; Iametti, S

    2016-03-01

    Type-2 diabetes is continuously increasing worldwide. Hence, there is a need to develop functional foods that efficiently alleviate damage due to hyperglycaemia complications while meeting the criteria for a sustainable food processing technology. Inhibition of mammalian α-amylase and α-glucosidase was studied for white grape skin samples recovered from wineries and found to be higher than that of the drug acarbose. In white grape skins, quercetin and kaempferol derivatives, analysed by UPLC-DAD-MS, and the oligomeric series of catechin/epicatechin units and their gallic acid ester derivatives up to nonamers, analysed by MALDI-TOF-MS were identified. White grape skin was then used for enrichment of a tomato puree (3%) and a flat bread (10%). White grape skin phenolics were found in the extract obtained from the enriched foods, except for the higher mass proanthocyanidin oligomers, mainly due to their binding to the matrix and to a lesser extent to heat degradation. Proanthocyanidin solubility was lower in bread, most probably due to formation of binary proanthocyanin/protein complexes, than in tomato puree where possible formation of ternary proanthocyanidin/protein/pectin complexes can enhance solubility. Enzyme inhibition by the enriched foods was significantly higher than for unfortified foods. Hence, this in vitro approach provided a platform to study potential dietary agents to alleviate hyperglycaemia damage and suggested that grape skin phenolics could be effective even if the higher mass proanthocyanidins are bound to the food matrix. PMID:26943361

  5. Alpha-amylase inhibitory activity and sterol composition of the marine algae, Sargassum glaucescens

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    Nasrin Payghami

    2015-01-01

    Full Text Available Background: Sargassum species (phaeophyceae are economically important brown algae in southern parts of Iran. Sargassum is mainly harvested as a row material in alginate production industries and is a source of plant foods or plant bio-stimulants even a component of animal foods. Objective: In this study, Sargassum glaucescens, collected from the seashore of Chabahar, was employed for phytochemical and biological evaluations. Materials and Methods: For that purpose, the dried algae was extracted by methanol and subjected to different chromatographic separation methods. Results: Six sterols, fucosterol (1, 24(S-hydroxy-24-vinylcholesterol (2, 24(R-hydroxy-24-vinylcholesterol (3, stigmasterol (4, β-sitosterol (5 and cholesterol (6 were identified by spectroscopic methods including 1 H-NMR, 13 C-NMR and mass spectroscopy. In vitro alpha-amylase inhibitory test was performed on the methanolic extract and the results revealed a potent inhibition (IC 50 = 8.9 ± 2.4 mg/mL of the enzyme compared to acarbose as a positive control. Conclusion: Various biological activities and distribution of sterols in Sargassum genus have been critically reviewed here. The results concluded that these algae are a good candidate for further anti-diabetic investigations in animals and human.

  6. Fucoidan - An α-amylase inhibitor from Sargassum wightii with relevance to NIDDM.

    Science.gov (United States)

    Lakshmana Senthil, S; Vinoth Kumar, T; Geetharamani, D; Suja, G; Yesudas, Rincy; Chacko, Amrutha

    2015-11-01

    The present experiment was conducted to screen the α-amylase inhibitory activity of fucoidan extracted from Sargassum wightii collected at the coastal area of Mandapam, Tamil Nadu, India. Fucoidan was extracted from the sporophyll of S. Wightii by ethanol and CaCl2 precipitation method. The average yield was 1.8±0.16% and the extracted fucoidan was found to contain 53±0.52% of fucose and 36±0.60% of sulphate. Structural elucidation (FT-IR and NMR) and in vitro α-amylase activity of purified fucoidon were performed. Fucoidan at the concentration of 62.5, 125 and 250μg exhibited 24.81, 62.50 and 99.24% inhibition against α-amylase, respectively, in a dose dependent manner. Fucoidan from S. wightii also inhibits α-glucosidase which clearly indicates dual inhibitory activity of the compound. The IC50 value against α-amylase of fucoidan is found to be 103.83μg which is more effective than that of acarbose (16mg). PMID:26325676

  7. α-Glucosidase Inhibitors from Fruits of Rosa canina L.

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    Behvar Asghari

    2015-04-01

    Full Text Available As part of ongoing project on screening plants used in Iranian folk medicine to treatment of diabetes, α-glucosidase inhibition activities of Rosa canina extracts have been tested. The acetone extract of the plant exhibited significant inhibition with IC 50 value of 0.3 µg/ml. The enzyme based assay guided fractionation of the acetone extract led to the isolation of daucosterol (1 and D-glucono-1,4-lactone (2, as highly active α-glucosidase inhibitors. Their structures were determined by 1H- and 13C-NMR spectroscopic evidences. The IC 50 values of daucosterol and D-glucono-1,4-lactone on yeast α-glucosidase were 13.3 and 6.5 µM, respectively, while IC 50 of acarbose was 16.1 µM, as a positive control. The Lineweaver-Burk plots analysis elucidated that both of the compounds inhibited the enzyme competitively. The study suggests that isolated compounds can be good candidates as α-glucosidase inhibitors and provide strong rationale for more in vivo studies.

  8. Bauhinia forficata Link authenticity using flavonoids profile: relation with their biological properties.

    Science.gov (United States)

    Ferreres, Federico; Gil-Izquierdo, Angel; Vinholes, Juliana; Silva, Sara T; Valentão, Patrícia; Andrade, Paula B

    2012-09-15

    HPLC-DAD-ESI/MS(n) was used to ascertain the authenticity of two certified and two commercial Bauhinia forficata Link samples. Different flavonoids profiles were obtained, involving 39 compounds. Just kaempferol-3-O-(2-rhamnosyl)rutinoside was found in all analysed samples. Five compounds were common to the certified samples of B. forficata Link and B. forficata Link subsp. pruinosa (Vogel) Fortunato & Wunderlin, being kaempferol derivatives the most representative ones. The phenolic composition of B. forficata Link subsp. pruinosa (Vogel) Fortunato & Wunderlin is described herein for the first time, accounting for eight compounds, while 10 new compounds were identified in B. forficata Link. Commercial B. forficata Link showed higher contents of quercetin derivatives, in addition to the presence of myricetin derivatives and flavonoids-(galloyl)glycosides, for which the MS fragmentation pattern is reported for the first time. B. forficata Link and the two commercial samples were able to inhibit α-glucosidase, with EC(50) values lower than that found for acarbose. Mild effects on cholinesterases were observed with the certified samples, while commercial ones were more effective. The same behaviour was observed concerning the scavenging of DPPH, nitric oxide and superoxide radicals. The presence of high contents of quercetin derivatives in commercial samples seems to directly influence their biological properties. The differences between phenolic profiles and their relation with the authenticity of commercial samples are discussed.

  9. Bioactive Natural Products from Piper betle L. Leaves and their α -Glucosidase Inhibitory Potential

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    Andreia P. Oliveira

    2016-05-01

    Full Text Available Piper betle L. can be a valuable proposal for the prevention and treatment of several disorders. In fact, i ts leaves are largely consumed as mouth freshener and masticator, being known for their biological properties. This material possesses several kinds of bioactive natural products. Considering that diabetes is a worldwide disease with strong impact on human health, this work intended to explore the in vitro α-glucosidase inhibitory capacity of P. betle leaves, as well as to improve the knowledge on their metabolic pattern. Thus, a targeted metabolite analysis of the aqueous and ethanolic extract was performed by GC-MS, a similar qualitative profile of both extracts being observed. Fourteen metabolites were determined in P. betle leaves, five of them for the first time. Alanine and β-sitosterol were the main amino acid and sterol, respectively. Stearic and palmitic acids were the predominant fatty acids. A strong capacity to inhibit α-glucosidase was noticed, ethanol extract being more active than the positive control (acarbose tested under the same conditions. Taking into account the results obtained, this work further extends the potential application of this herbal medicine, suggesting that its consumption may have a positive impact in the prevention and treatment of diabetes disease.

  10. Antidiabetic Indian plants: a good source of potent amylase inhibitors.

    Science.gov (United States)

    Bhat, Menakshi; Zinjarde, Smita S; Bhargava, Shobha Y; Kumar, Ameeta Ravi; Joshi, Bimba N

    2011-01-01

    Diabetes is known as a multifactorial disease. The treatment of diabetes (Type II) is complicated due to the inherent patho-physiological factors related to this disease. One of the complications of diabetes is post-prandial hyperglycemia (PPHG). Glucosidase inhibitors, particularly α-amylase inhibitors are a class of compounds that helps in managing PPHG. Six ethno-botanically known plants having antidiabetic property namely, Azadirachta indica Adr. Juss.; Murraya koenigii (L.) Sprengel; Ocimum tenuflorum (L.) (syn: Sanctum); Syzygium cumini (L.) Skeels (syn: Eugenia jambolana); Linum usitatissimum (L.) and Bougainvillea spectabilis were tested for their ability to inhibit glucosidase activity. The chloroform, methanol and aqueous extracts were prepared sequentially from either leaves or seeds of these plants. It was observed that the chloroform extract of O. tenuflorum; B. spectabilis; M. koenigii and S. cumini have significant α-amylase inhibitory property. Plants extracts were further tested against murine pancreatic, liver and small intestinal crude enzyme preparations for glucosidase inhibitory activity. The three extracts of O. tenuflorum and chloroform extract of M. koenigi showed good inhibition of murine pancreatic and intestinal glucosidases as compared with acarbose, a known glucosidase inhibitor. PMID:18955350

  11. Evaluation of alpha- amylase inhibition by Urtica dioica and Juglans regia extracts

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    Mahsa Rahimzadeh

    2014-06-01

    Full Text Available Objective(s:One strategy for the treatment of diabetes is inhibition of pancreatic α- amylase. Plants contains different chemical constituents with potential for inhibition of α-amylase and hence maybe used as therapeutic. Materials and Methods: Urtica dioica and Juglans regia Linn were tested for α-amylase inhibition. Different concentrations of leaf aqueous extracts were incubated with enzyme substrate solution and the activity of enzyme was measured. For determination of the type of inhibition, Dixon plot was depicted. Acarbose was used as the standard inhibitor. Results: Both plant extracts showed time and concentration dependent inhibition of α-amylase. 60% inhibition was seen with 2 mg/ml of U. dioica and0.4 mg/ml of J. regia aqueous extract. Dixon plots revealed the type of α-amylase inhibition by these two extracts as competitive inhibition. Conclusion: Determination of the type of α-amylase inhibition by these plant extracts could provide by successful use of plant chemicals as drug targets.

  12. Phenylethanoid glycosides and phenolic glycosides from stem bark of Magnolia officinalis.

    Science.gov (United States)

    Xue, Zhenzhen; Yan, Renyi; Yang, Bin

    2016-07-01

    An investigation of the hydrophilic constituents of the stem bark of Magnolia officinalis was performed and which led to isolation and identification of twenty-one previously unreported glycosides. These included eleven phenylethanoid glycosides, magnolosides F-P, and ten phenolic glycosides, magnolosides Q-Z, along with eight known compounds. Their structures were elucidated on the basis of extensive spectroscopic analyses and chemical hydrolysis methods, as well as by comparison with literature data. Most of the phenylethanoid glycosides contained an allopyranose moiety, which is rare in the plant kingdom. Magnolosides I and K as well as 2-(3,4-dihydroxyphenyl) ethanol 1-O-[4-O-caffeoyl-2-O-α-l-rhamnopyranosyl-3-O-α-l-rhamnopyranosyl-6-O-β-d-glucopyranosyl]-β-d-glucopyranoside showed more potent α-glucosidase inhibitory effects (IC50 values of 0.13, 0.27, and 0.29mM, respectively) than the positive control, acarbose (IC50 value of 1.09mM) in vitro. Magnolosides H, E and D also showed moderate cytotoxicity against MGC-803 and HepG2 cells with IC50 values of 13.59-17.16μM and 29.53-32.46μM, respectively. PMID:27086163

  13. Structural characterization and inhibition on α-d-glucosidase activity of non-starch polysaccharides from Fagopyrum tartaricum.

    Science.gov (United States)

    Wang, Xiao-Ting; Zhu, Zhen-Yuan; Zhao, Liang; Sun, Hui-Qing; Meng, Meng; Zhang, Jin-Yu; Zhang, Yong-Min

    2016-11-20

    In the present study, the crude polysaccharide was extracted from Fagopyrum tartaricum and purified by Sephadex G-25 and G-75 column to produce a polysaccharide fraction termed TBP-II. Its average molecular weight was 26kDa. The structural characterization of TBP-II was investigated by gas chromatography, periodate oxidation-Smith degradation, Methylation and NMR. Congo red was applied to explore its advanced structures. The results revealed that chemical composition and structural characteristic of TBP-II was mainly consisted of galactose, arabinose, xylose and glucose with a molar ratio of 0.7:1:6.3:74.2. The backbone of TBP-II was composed of (1→4)-linked α-d-glucopyranosyl (Glcp), while the branches comprised of (1→3)-linked α-d-glucopyranosyl (Glcp), (1→6)-linked α-d-galactopyranosyl (Galp) and (1→2,4)-linked α-d-rhamnopyranosyl (Rhap). The structure of TBP-II was 1,3 and 1,6-branched-galactorhamnoglucan that had a linear backbone of (1→4)-linked α-d-glucopyranose (Glcp). Using Congo red assay showed that it was absent of triple helix structure. The α-d-glucosidase inhibitory activity of TBP-II was determined using acarbose as positive control. The result showed that the inhibition rate depended on the concentration of polysaccharides. PMID:27561539

  14. Pyridine sulfonamide as a small key organic molecule for the potential treatment of type-II diabetes mellitus and Alzheimer's disease: In vitro studies against yeast α-glucosidase, acetylcholinesterase and butyrylcholinesterase.

    Science.gov (United States)

    Riaz, Sadaf; Khan, Islam Ullah; Bajda, Marek; Ashraf, Muhammad; Qurat-Ul-Ain; Shaukat, Ayesha; Rehman, Tanzeel Ur; Mutahir, Sadaf; Hussain, Sajjad; Mustafa, Ghulam; Yar, Muhammad

    2015-12-01

    This paper presents the efficient high yield synthesis of novel pyridine 2,4,6-tricarbohydrazide derivatives (4a-4i) along with their α-glucosidase, acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibition activities. The enzymes inhibition results showed the potential of synthesized compounds in controlling both type-II diabetes mellitus and Alzheimer's disease. In vitro biological investigations revealed that most of compounds were more active against yeast α-glucosidase than the reference compound acarbose (IC50 38.25±0.12μM). Among the tested series the compound 4c bearing 4-flouro benzyl group was noted to be the most active (IC50 25.6±0.2μM) against α-glucosidase, and it displayed weak inhibition activities against AChE and BChE. Compound 4a exhibited the most desired results against all three enzymes, as it was significantly active against all the three enzymes; α-glucosidase (IC50 32.2±0.3μM), AChE (IC50 50.2±0.8μM) and BChE (IC50 43.8±0.8μM). Due to the most favorable activity of 4a against the tested enzymes, for molecular modeling studies this compound was selected to investigate its pattern of interaction with α-glucosidase and AChE targets.

  15. Antidiabetic Indian Plants: A Good Source of Potent Amylase Inhibitors

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    Menakshi Bhat

    2011-01-01

    Full Text Available Diabetes is known as a multifactorial disease. The treatment of diabetes (Type II is complicated due to the inherent patho-physiological factors related to this disease. One of the complications of diabetes is post-prandial hyperglycemia (PPHG. Glucosidase inhibitors, particularly α-amylase inhibitors are a class of compounds that helps in managing PPHG. Six ethno-botanically known plants having antidiabetic property namely, Azadirachta indica Adr. Juss.; Murraya koenigii (L. Sprengel; Ocimum tenuflorum (L. (syn: Sanctum; Syzygium cumini (L. Skeels (syn: Eugenia jambolana; Linum usitatissimum (L. and Bougainvillea spectabilis were tested for their ability to inhibit glucosidase activity. The chloroform, methanol and aqueous extracts were prepared sequentially from either leaves or seeds of these plants. It was observed that the chloroform extract of O. tenuflorum; B. spectabilis; M. koenigii and S. cumini have significant α-amylase inhibitory property. Plants extracts were further tested against murine pancreatic, liver and small intestinal crude enzyme preparations for glucosidase inhibitory activity. The three extracts of O. tenuflorum and chloroform extract of M. koenigi showed good inhibition of murine pancreatic and intestinal glucosidases as compared with acarbose, a known glucosidase inhibitor.

  16. Xanthium strumarium as an Inhibitor of α-Glucosidase, Protein Tyrosine Phosphatase 1β, Protein Glycation and ABTS⁺ for Diabetic and Its Complication.

    Science.gov (United States)

    Hwang, Seung Hwan; Wang, Zhiqiang; Yoon, Ha Na; Lim, Soon Sung

    2016-01-01

    Phytochemical investigation of the natural products from Xanthium strumarium led to the isolation of fourteen compounds including seven caffeoylquinic acid (CQA) derivatives. The individual compounds were screened for inhibition of α-glucosidase, protein tyrosine phosphatase 1β (PTP1β), advanced glycation end products (AGEs), and ABTS⁺ radical scavenging activity using in vitro assays. Among the isolated compounds, methyl-3,5-di-caffeoyquinic acid exhibited significant inhibitory activity against α-glucosidase (18.42 μM), PTP1β (1.88 μM), AGEs (82.79 μM), and ABTS⁺ (6.03 μM). This effect was marked compared to that of the positive controls (acarbose 584.79 μM, sumarin 5.51 μM, aminoguanidine 1410.00 μM, and trolox 29.72 μM respectively). In addition, 3,5-di-O-CQA (88.14 μM) and protocatechuic acid (32.93 μM) had a considerable inhibitory effect against α-glucosidase and ABTS⁺. Based on these findings, methyl-3,5-di-caffeoyquinic acid was assumed to be potentially responsible for the anti-diabetic actions of X. strumarium. PMID:27649132

  17. Determination of a-glucosidase inhibitory activity from selected Fabaceae plants.

    Science.gov (United States)

    Dej-Adisai, Sukanya; Pitakbut, Thanet

    2015-09-01

    Nineteen plants from Fabaceae family, which were used in Thai traditional medicine for treatment of diabetes, were determined of α-glucosidase inhibitory activity via enzymatic reaction. In this reaction, α-glucosidase was used as enzyme, which, reacted with the substrate, p-nitrophenol-D-glucopyranoside (pNPG). After that the product, p-nitro phenol (pNP) will be occurred and observed the yellow colour at 405 nm. In this study, acarbose was used as positive standard which, inhibited this enzyme with IC₅₀ as 331 ± 4.73 μg/ml. Caesalpinia pulcherrima leaves showed the highest activity with IC₅₀ as 436.97 ± 9.44 μg/ml. Furthermore, Bauhinia malabarica leaves presented moderately activity with IC₅₀ as 745.08 ± 11.15 μg/ml. However, the other plants showed mild to none activity of α-glucosidase inhibition. Accordingly, this study can support anti-diabetes of these plants in traditional medicine and it will be the database of the biological activity of Fabaceae plant. PMID:26408887

  18. Antioxidant and antidiabetic activities of 11 herbal plants from Hyrcania region, Iran

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    Hossein Dehghan

    2016-01-01

    Full Text Available In the present study, 2,2-diphenyl-1-picrylhydrazyl radical scavenging, α-amylase and α-glucosidase inhibition activities, and total phenolic contents of n-hexane, ethyl acetate, and methanol extracts of various parts of Allium paradoxum, Buxus hyrcana, Convolvulus persicus, Eryngium caucasicum, Heracleum persicum, Pimpinella affinis, Parrotia persica, Primula heterochroma, Pyrus boissieriana, Ruscus hyrcanus, and Smilax excelsa were investigated. These plants, which mostly serve as food flavoring, were collected from Hyrcania region, Sari, Iran. Some extracts of H. persicum, S. excels, P. boissieriana, P. persica, and P. heterochroma exhibited significant antidiabetic activities in α-amylase and α-glucosidase assays, more effective than acarbose (concentrations that cause 50% inhibition = 75.7 μg/mL and 6.1 μg/mL against α-amylase and α-glucosidase, respectively. Also, C. persicus, P. boissieriana, and P. heterochroma showed strong antioxidant activities, compared with butylated hydroxytoluene (concentration that causes 50% inhibition = 16.7 μg/mL. In conclusion, this study can recommend these plants as good candidates for further investigations to find potent antidiabetic natural products or probable lead compounds. Statistical analysis showed significant correlation between the 2,2-diphenyl-1-picrylhydrazyl scavenging activity and total phenolic contents (r = 0.711, p < 0.001.

  19. Evaluation of α-amylase inhibitory potential of three medicinally important traditional wild food plants of India

    Directory of Open Access Journals (Sweden)

    K.S.N Jyothi

    2011-01-01

    Full Text Available Naturally available α-amylase inhibitors from medicinally important plants are shown to be effective in managing postprandial hyperglycemia (PPHG which is of major concern in Type -2 diabetes. Three wild food plants namely Oxalis corniculata, Basella rubra , and Cocculus hirsutus with known traditional medicinal values were tested for α-amylase inhibition in order to evaluate their inhibitory potential on porcine pancreatic α-amylase. A total of 15 extracts obtained from three plants by aqueous and solvent extraction have been tested for their inhibitory potential against porcine pancreatic α-amylase. Of the fifteen extracts, five extracts showed concentration-dependent potent inhibition of >75% with IC50 (half maximal inhibitory concentration values much less than that of standard anti-diabetic drug acarbose namely aqueous extract of Oxalis corniculata 89.87% (100 μg/ml, IC 50 -68.08 0.06, chloroform, acetone and methanol extracts of Cocculus hirsutus exhibited 83.33% (60 μg/ml, IC 50 -70.48 18.39, 79.10% (100 μg/ml, IC 50 -80.77 0.63, 77.2% (100 μg/ml, IC 50 -80.11 2.23 respectively. The other extracts of the plants showed inhibition, but not statistically significant. Thus, these extracts showing potent inhibition might prove to be efficient sources for the extraction of natural α-amylase inhibitors.

  20. Oral versus postingestive origin of polysaccharide appetite in the rat.

    Science.gov (United States)

    Sclafani, A; Nissenbaum, J W

    1987-01-01

    Previous studies have revealed that rats consume substantial amounts of polysaccharide solutions, even if the solutions are made bitter with the addition of sucrose octa acetate (SOA). The present experiment used the gastric sham-feeding preparation to determine if it is the orosensory or postingestive properties of polysaccharides that motivate rats to consume polysaccharide (Polycose) solutions. In Experiment 1, food deprived rats sham fed less of a 0.05% SOA + 32% Polycose solution than they did of a 32% glucose solution, but their SOA-Polycose intake was still considerable (44 ml/hr). The same rats refused to sham feed SOA-gum and SOA-sugar solutions that were similar to the SOA-Polycose solution in bitter taste, viscosity and free sugar content. In Experiment 2, rats sham fed as much of a 32% Polycose solution as they did of a 32% sucrose solution. Despite the gastric fistula, some of the ingested Polycose was absorbed as evidenced by an increase in the rats' blood glucose levels. The addition of acarbose, a drug that inhibits polysaccharide digestion, to the Polycose solution blocked the increase in blood glucose, but did not reduce the rats' sham feeding of the solution. These findings indicate that it is the orosensory (presumably taste) properties of polysaccharide solutions, not their postingestive effects, that initially attract rats to the solutions. The results question the assumption that polysaccharides are "tasteless" to animals.

  1. Is gastric sham feeding really sham feeding?

    Science.gov (United States)

    Sclafani, A; Nissenbaum, J W

    1985-03-01

    Rats were fitted with gastric cannulas, food deprived, and allowed to drink a sugar solution that drained out of the opened cannula; i.e., the rats sham-fed. Although this procedure is thought to prevent absorption of ingested food, it was found that the sham feeding of a 32% glucose or sucrose solution significantly elevated blood glucose levels. The addition of acarbose, a drug that inhibits the digestion of sucrose, to the 32% sucrose solution blocked the blood glucose rise, as did closing the pylorus with an inflatable pyloric cuff. Neither the drug nor the cuff, however, reduced the amount of sucrose solution consumed. These findings indicate that gastric sham feeding does not necessarily prevent the digestion and absorption of food, although absorption is not essential for the appearance of a vigorous sham-feeding response. Nevertheless the possibility that neural or hormonal feedback from the stomach contributes to the sham-feeding response cannot be excluded, and until this issue is resolved the results of gastric sham-feeding studies should be interpreted with caution.

  2. On the role of the mouth and gut in the control of saccharin and sugar intake: a reexamination of the sham-feeding preparation.

    Science.gov (United States)

    Sclafani, A; Nissenbaum, J W

    1985-06-01

    Adult female rats, each fitted with a gastric fistula, were tested for their "normal-feeding" (fistula closed) and "sham-feeding" (fistula open) response to saccharin and sugar solutions under a variety of conditions. When hungry, rats consumed no more of a 0.2% saccharin solution with their fistula open than they did with their fistula closed. Increasing or decreasing the saccharin concentration did not increase the amount of solution sham fed, but adding a small amount of glucose (3%) to the saccharin solution did increase the amount sham fed. Thirsty rats, unlike hungry, significantly increased their 0.2% saccharin solution intake when tested with an open fistula. When tested with a 32% glucose solution, hungry rats consumed up to six times more solution with their fistula open than with their fistula closed. The hungry rats also sham fed significantly more of the 32% glucose solution than of the 0.2% saccharin solution or 0.2% saccharin + 3% glucose solution. Sham-feeding of a 32% sucrose solution significantly elevated blood glucose levels, but blocking this effect by adding acarbose, a drug that inhibits sucrose digestion, did not reduce the amount of solution sham fed. Several possible explanations for the differential sham-feeding response to saccharin and sugar solutions are discussed.

  3. Purification, enzymatic characterization, and nucleotide sequence of a high-isoelectric-point alpha-glucosidase from barley malt

    DEFF Research Database (Denmark)

    Frandsen, T P; Lok, F; Mirgorodskaya, E;

    2000-01-01

    .5, and catalyzed the hydrolysis by a retaining mechanism, as shown by nuclear magnetic resonance. Acarbose was a strong inhibitor (K(i) = 1.5 microM). Molecular recognition revealed that all OH-groups in the non-reducing ring and OH-3 in the reducing ring of maltose formed important hydrogen bonds to the...... enzyme in the transition state complex. Mass spectrometry of tryptic fragments assigned the 92-kD protein to a barley cDNA (GenBank accession no. U22450) that appears to encode an alpha-glucosidase. A corresponding sequence (HvAgl97; GenBank accession no. AF118226) was isolated from a genomic phage...... library using a cDNA fragment from a barley cDNA library. HvAgl97 encodes a putative 96.6-kD protein of 879 amino acids with 93.8% identity to the protein deduced from U22450. The sequence contains two active site motifs of glycoside hydrolase family 31. Three introns of 86 to 4,286 bp interrupt the...

  4. Synthesis and biological evaluation of novel 1,2,4-triazine derivatives bearing carbazole moiety as potent α-glucosidase inhibitors.

    Science.gov (United States)

    Wang, Guangcheng; Wang, Jing; He, Dianxiong; Li, Xin; Li, Juan; Peng, Zhiyun

    2016-06-15

    A new series of 1,2,4-triazine derivatives bearing carbazole moiety 7a-7p were designed, synthesized, and evaluated for their α-glucosidase inhibitory activity. The majority of the screened compounds displayed potent α-glucosidase inhibitory activity, with IC50 values in the range of 4.27±0.07-47.75±0.25μM as compared to the standard drug acarbose. Among the series, compound 7k represented the most potent α-glucosidase inhibitory activity with IC50 values of 4.27±0.07μM. Kinetic analysis revealed that compound 7k is a non-competitive inhibitor with a Ki of 4.43μM. Furthermore, the binding interactions of compound 7k with α-glucosidase was confirmed through molecular docking. This study showed these 1,2,4-triazine derivatives bearing carbazole moiety as a new class of α-glucosidase inhibitors. PMID:27177827

  5. Assay-guided fractionation study of alpha-amylase inhibitors from Garcinia mangostana pericarp.

    Science.gov (United States)

    Loo, Alvin Eng Kiat; Huang, Dejian

    2007-11-28

    Alpha-amylase inhibitor (alpha-AI) activity of Garcinia mangostana, commonly known as mangosteen, pericarp extracts was studied by assay guided fractionations from lipophilic to hydrophilic using combined solvent extraction and Amberlite XAD2 adsorption chromatography. Neither the lipophilic, xanthone containing fraction, nor the highly polar fraction, which has no affinity on Amberlite XAD2, showed any alpha-AI. The fraction that shows very high inhibitory activity contains primarily polyphenols and can be adsorbed on Amberlite XAD2. The IC50 of 5.4 microg/mL of this fraction is comparable to that of acarbose, a prescribed alpha-AI used in the control of type II diabetes, at 5.2 microg/mL. Total phenolic content (TPC) of each fraction was measured and the TPC has no correlation with the alpha-AI activity. The lipophilic fraction contains mainly xanthones as revealed by HPLC-MS analysis. Colorimetric analysis coupled with UV-vis and IR spectroscopic analysis demonstrated that the fractions with high alpha-AI activity are primarily oligomeric proanthocyanidins (OPCs) with little gallate moiety. There is also evidence to show that the alpha-AI by these OPCs is not purely by nonspecific protein complexation. Both tannic acid and G. mangostana OPCs precipitate BSA equally well but G. mangostana OPCs are 56 times more effective in inhibiting alpha-amylase.

  6. Norsesquiterpenoids and triterpenoids from strawberry cv. Falandi.

    Science.gov (United States)

    Yang, Dan; Liang, Jian; Xie, Haihui; Wei, Xiaoyi

    2016-07-15

    Falandi is a common strawberry (Fragaria × ananassa Duch.) cultivar in southern China. Further study of the chemical constituents in Falandi fruit led to the isolation of nine norsesquiterpenoids and three triterpenoids. Falandioside D (1) and falandins A (2) and B (3) were new norsesquiterpenoids, and the others excluding tormentic acid (11) were found in strawberry for the first time. Compounds 1 and 11 exhibited potent α-glucosidase inhibitory activity with the half maximal inhibitory concentration (IC50) values of 565.0 and 27.4 μM in comparison to acarbose (619.9 μM). Compounds 3, 7 (blumenol C glucoside), and 11 showed cytotoxicity against human nasopharyngeal carcinoma cell line CNE1 with the IC50 values of 57.6, 56.4, and 36.0 μM, respectively. Among new compounds, 1 showed 2,2'-azinobis(3-ethylbenzthiazoline-6-sulfonic acid) (ABTS) radical cation scavenging capacity (IC50=36.2 μM). These results suggested that non-phenolic constituents were also involved in the antidiabetic, antitumour, and antioxidant effects of strawberry fruit. PMID:26948590

  7. 2-(2-Phenylethyl)chromone derivatives in artificial agarwood from Aquilaria sinensis.

    Science.gov (United States)

    Liao, Ge; Mei, Wen-Li; Dong, Wen-Hua; Li, Wei; Wang, Pei; Kong, Fan-Dong; Gai, Cui-Juan; Song, Xi-Qiang; Dai, Hao-Fu

    2016-04-01

    Seven new 2-(2-phenylethyl)chromone derivatives (1-7) including a chlorinated one (4), together with eight known ones (8-15), were isolated from the EtOAc extract of artificial agarwood originating from Aquilaria sinensis (Lour.) Gilg. All structures including the absolute configurations were unambiguously elucidated by spectroscopic (NMR, UV, IR, MS) methods, Mosher's method, and comparison with reported data in the literatures. Among those, compounds 8, 12, and 14 exhibited significant inhibition against α-glucosidase in vitro with IC50 values of 0.15, 0.05, and 0.09 mM, respectively (with acarbose as the positive control; IC50: 0.98 mM). In addition, compounds 3, 9, 11, and 14 showed weak inhibitory activity against AChE; and compounds 12 and 13 displayed weak cytotoxicity against human gastric cell line (SGC-7901) among three types of tested human cancer cell lines (BEL-7402, K562, and SGC-7901). PMID:26784520

  8. In vitro and in vivo comparison of the biological activities of two traditionally and widely used Arum species from Jordan: Arum dioscoridis Sibth & Sm. and Arum palaestinum Boiss.

    Science.gov (United States)

    Afifi, Fatma U; Kasabri, Violet; Litescu, Simona C; Abaza, Ismail M

    2016-08-01

    Arum dioscoridis and A. palaestinum (Araceae) are indigenous plant species in Jordan. HPLC-MS analysis of A. dioscoridis revealed the presence of apigenin, luteolin, quercetin, quercetin-3-O-β-glucoside, vitexin, isoorientin, esculin, and caffeic and ferulic acids. Both Arum spp., influenced gastrointestinal carbohydrate and lipid digestion and absorption. Orlistat inhibited dose dependently and highly substantially pancreatic lipase (PL) in vitro. Similar to orlistat, Arum species aqueous extracts (AEs), apigenin, caffeic acid and esculin exhibited a concentration related PL inhibition. Comparable to acarbose, dual inhibition of α-amylase/α-glucosidase was observed for both Arum species. Like guar gum, A. dioscoridis AE minimised substantially area under 24 h glucose curve. Acute starch-induced postprandial hyperglycaemia in overnight fasting rats was highly significantly (p < 0.001) decreased by A. dioscoridis AE. A. palaestinum could not perform effectively in either starch- or glucose-fed fasting rats. No antiproliferative effects against colorectal cancer cell lines HT29, HCT116 and SW620 were detected for tested Arum spp. PMID:26284613

  9. Design, synthesis and biological evaluation of novel coumarin thiazole derivatives as α-glucosidase inhibitors.

    Science.gov (United States)

    Wang, Guangcheng; He, Dianxiong; Li, Xin; Li, Juan; Peng, Zhiyun

    2016-04-01

    A new series of coumarin thiazole derivatives 7a-7t were synthesized, characterized by (1)H NMR, (13)C NMR and element analysis, evaluated for their α-glucosidase inhibitory activity. The majority of the screened compounds displayed potent inhibitory activities with IC50 values in the range of 6.24±0.07-81.69±0.39μM, when compared to the standard acarbose (IC50=43.26±0.19μM). Structure-activity relationship (SAR) studies suggest that the pattern of substitution in the phenyl ring is closely related to the biological activity of this class of compounds. Among all the tested molecules, compound 7e (IC50=6.24±0.07μM) was found to be the most active compound in the library of coumarin thiazole derivatives. Enzyme kinetic studies showed that compound 7e is a non-competitive inhibitor with a Ki of 6.86μM. Furthermore, the binding interactions of compound 7e with the active site of α-glucosidase were confirmed through molecular docking. This study has identified a new class of potent α-glucosidase inhibitors for further investigation.

  10. Rapid identification of α-glucosidase inhibitors from Phlomis tuberosa by Sepbox chromatography and thin-layer chromatography bioautography.

    Directory of Open Access Journals (Sweden)

    Yingbo Yang

    Full Text Available Alpha-glucosidase inhibitors currently form an important basis for developing novel drugs for diabetes treatment. In our preliminary tests, the ethyl acetate fraction of Phlomis tuberosa extracts showed significant α-glucosidase inhibitory activity (IC₅₀ = 100 μg/mL. In the present study, a combined method using Sepbox chromatography and thin-layer chromatography (TLC bioautography was developed to probe α-glucosidase inhibitors further. The ethyl acetate fraction of P. tuberosa extracts was separated into 150 individual subfractions within 20 h using Sepbox chromatography. Then, under the guidance of TLC bioautography, 20 compounds were successfully isolated from these fractions, including four new diterpenoids [14-hydroxyabieta-8,11,13-triene-11-carbaldehyde-18-oic-12-carboxy-13-(1-hydroxy-1-methylethyl-lactone (1, 14-hydroxyabieta-8,11,13-triene-17-oic-12-carboxy-13-(1-hydroxy-1-methylethyl-lactone (2, 14,16-dihydroxyabieta-8,11,13-triene-15,17-dioic acid (3, and phlomisol (15,16-eposy-8,13(16,14-labdatrien-19-ol (4], and 16 known compounds. Activity estimation indicated that 15 compounds showed more potent α-glucosidase inhibitory effects (with IC50 values in the range 0.067-1.203 mM than the positive control, acarbose (IC50 = 3.72 ± 0.113 mM. This is the first report of separation of α-glucosidase inhibitors from P. tuberosa.

  11. Isolation and Characterization of an α-Glucosidase Inhibitor from Musa spp. (Baxijiao Flowers

    Directory of Open Access Journals (Sweden)

    Zhanwu Sheng

    2014-07-01

    Full Text Available The use of α-glucosidase inhibitors is considered to be an effective strategy in the treatment of diabetes. Using a bioassay-guided fractionation technique, five Bacillus stearothermophilus α-glucosidase inhibitors were isolated from the flowers of Musa spp. (Baxijiao. Using NMR spectroscopy analysis they were identified as vanillic acid (1, ferulic acid (2, β-sitosterol (3, daucosterol (4 and 9-(4′-hydroxyphenyl-2-methoxyphenalen-1-one (5. The half maximal inhibitory concentration (IC50 values of compounds 1–5 were 2004.58, 1258.35, 283.67, 247.35 and 3.86 mg/L, respectively. Compared to a known α-glucosidase inhibitor (acarbose, IC50 = 999.31 mg/L, compounds 3, 4 and 5 showed a strong α-glucosidase inhibitory effect. A Lineweaver-Burk plot indicated that compound 5 is a mixed-competitive inhibitor, while compounds 3 and 4 are competitive inhibitors. The inhibition constants (Ki of compounds 3, 4 and 5 were 20.09, 2.34 and 4.40 mg/L, respectively. Taken together, these data show that the compounds 3, 4 and 5 are potent α-glucosidase inhibitors.

  12. Pregnancy Following Bariatric Surgery-Medical Complications and Management.

    Science.gov (United States)

    Narayanan, Ram Prakash; Syed, Akheel A

    2016-10-01

    Bariatric surgery is most commonly carried out in women of childbearing age. Whilst fertility rates are improved, pregnancy following bariatric surgery poses several challenges. Whilst rates of many adverse maternal and foetal outcomes in obese women are reduced after bariatric surgery, pregnancy is best avoided for 12-24 months to reduce the potential risk of intrauterine growth retardation. Dumping syndromes are common after bariatric surgery and can present diagnostic and therapeutic challenges in pregnancy. Early dumping occurs due to osmotic fluid shifts resulting from rapid gastrointestinal food transit, whilst late dumping is characterized by a hyperinsulinemic response to rapid absorption of simple carbohydrates. Dietary measures are the mainstay of management of dumping syndromes but pharmacotherapy may sometimes become necessary. Acarbose is the least hazardous pharmacological option for the management of postprandial hypoglycemia in pregnancy. Nutrient deficiencies may vary depending on the type of surgery; it is important to optimize the nutritional status of women prior to and during pregnancy. Dietary management should include adequate protein and calorie intake and supplementation of vitamins and micronutrients. A high clinical index of suspicion is required for early diagnosis of surgical complications of prior weight loss procedures during pregnancy, including small bowel obstruction, internal hernias, gastric band erosion or migration and cholelithiasis. PMID:27488114

  13. Biologic Propensities and Phytochemical Profile of Vangueria madagascariensis J. F. Gmelin (Rubiaceae: An Underutilized Native Medicinal Food Plant from Africa

    Directory of Open Access Journals (Sweden)

    Nelvana Ramalingum

    2014-01-01

    Full Text Available Vangueria madagascariensis (VM, consumed for its sweet-sour fruits, is used as a biomedicine for the management of diabetes and bacterial infections in Africa. The study aims to assess the potential of VM on α-amylase, α-glucosidase, glucose movement, and antimicrobial activity. The antioxidant properties were determined by measuring the FRAP, iron chelating activity, and abilities to scavenge DPPH, HOCl, ∙OH, and NO radicals. Leaf decoction, leaf methanol, and unripe fruit methanol extracts were observed to significantly inhibit α-amylase. Active extracts against α-glucosidase were unripe fruit methanol, unripe fruit decoction, leaf decoction, and ripe fruit methanol, which were significantly lower than acarbose. Kinetic studies revealed a mixed noncompetitive type of inhibition. Leaf methanolic extract was active against S. aureus and E. coli. Total phenolic content showed a strong significant positive correlation (r=0.88 with FRAP. Methanolic leaf extract showed a more efficient NO scavenging potential and was significantly lower than ascorbic acid. Concerning ∙OH-mediated DNA degradation, only the methanol extracts of leaf, unripe fruit, and ripe fruit had IC50 values which were significantly lower than α-tocopherol. Given the dearth of information on the biologic propensities of VM, this study has established valuable primary information which has opened new perspectives for further pharmacological research.

  14. Bioactive diterpenoids and flavonoids from the aerial parts of Scoparia dulcis.

    Science.gov (United States)

    Liu, Qing; Yang, Qi-Ming; Hu, Hai-Jun; Yang, Li; Yang, Ying-Bo; Chou, Gui-Xin; Wang, Zheng-Tao

    2014-07-25

    Six new diterpenoids, 4-epi-7α-O-acetylscoparic acid A (1), 7α-hydroxyscopadiol (2), 7α-O-acetyl-8,17β-epoxyscoparic acid A (3), neo-dulcinol (4), dulcinodal-13-one (5), and 4-epi-7α-hydroxydulcinodal-13-one (6), and a new flavonoid, dillenetin 3-O-(6″-O-p-coumaroyl)-β-D-glucopyranoside (10), along with 12 known compounds, were isolated from the aerial parts of Scoparia dulcis. The 7S absolute configuration of the new diterpenoids 1-4 and 6 was deduced by comparing their NOESY spectra with that of a known compound, (7S)-4-epi-7-hydroxyscoparic acid A (7), which was determined by the modified Mosher's method. The flavonoids scutellarein (11), hispidulin (12), apigenin (15), and luteolin (16) and the terpenoids 4-epi-scopadulcic acid B (9) and betulinic acid (19) showed more potent α-glucosidase inhibitory effects (with IC50 values in the range 13.7-132.5 μM) than the positive control, acarbose. In addition, compounds 1, 11, 12, 15, 16, and acerosin (17) exhibited peroxisome proliferator-activated receptor gamma (PPAR-γ) agonistic activity, with EC50 values ranging from 0.9 to 24.9 μM. PMID:24955889

  15. Influence of variety, storage, and simulated gastrointestinal digestion on chemical composition and bioactivity of polysaccharides from sweet cherry and apple tree fruits

    Directory of Open Access Journals (Sweden)

    Kelly A. Ross

    2015-12-01

    Full Text Available This work examined the effect of extraction regime (hot water vs. simulated in vitro gastrointestinal digestion and postharvest storage on the chemical composition, molecular weight, and bioactive properties of polysaccharides obtained from sweet cherries (Lapins and Staccato varieties and apples (Gala and Fuji varieties. The yields of the polysaccharides isolated from cherries and apples ranged from 0.2 to 2.4% on a dry weight fruit basis. All of the isolated polysaccharides contained protein, phenolic compounds, and uronic acid. All polysaccharides contained the sugar monomers: rhamnose, arabinose, xylose, mannose, galactose, and glucose. Also, all of the polysaccharides obtained using the different extraction regimes were shown to possess antioxidant activity as determined with the ferric reducing antioxidant power and the 2,2-azinobis (3-ethyl-benzothiazoline-6-sulfonic acid (ABTS radical scavenging assays. Only the polysaccharides isolated from the cherry and apples after simulated in vitro gastrointestinal digestion showed appreciable α-glucosidase inhibition activity, with polysaccharides obtained from Staccato cherries showing nearly 90% of the inhibition of α-glucosidase as achieved with the positive control acarbose. This work shows that bioactive polysaccharides are available and/or can be isolated during digestion which supports the concept that fruit polysaccharides play a role in enhancing human health.

  16. 我院2012年~2014年降血糖药物的使用分析%Application of antidiabetic drugs in hospital in 2012~2014

    Institute of Scientific and Technical Information of China (English)

    蒋丽

    2016-01-01

    Objective To investigate the application of antidiabetic drugs in hospital.Methods The use of antidiabetic drugs in hospitalin 2012~2014 was analyzed retrospectively in respect of consumption sum、DDDs、drugs daily cost(DDC) etc.Results The top 5 antidiabetic drugs in respect of DDDs were acarbose, voglibose, glimepiride, glimepiride,metformin.Conclusion The antidiabetic drugs used in our hospital is rational.%目的:了解某院降糖药的应用特点与趋势。方法对某院2012年~2014年降糖药的销售金额、用药频度(DDDs)、日均费用(DDC)等进行回顾性分析。结果降糖药DDDs排序列前5位的是阿卡波糖、伏格列波糖、格列美脲、吡格列酮、二甲双胍。结论降糖药的应用情况基本合理。

  17. Sucrose induces vesicle accumulation and autophagy.

    Science.gov (United States)

    Higuchi, Takahiro; Nishikawa, Jun; Inoue, Hiroko

    2015-04-01

    It has been shown that the treatment of mammalian cells with sucrose leads to vacuole accumulation associated with lysosomes and upregulation of lysosomal enzyme expression and activity. Autophagy is an evolutionarily conserved homeostatic process by which cells deliver cytoplasmic material for degradation into lysosomes, thus it is probable that sucrose affects the autophagic activity. The role of sucrose in autophagy is unknown; however, another disaccharide, trehalose has been shown to induce autophagy. In the current study, we used mouse embryonic fibroblasts to investigate whether sucrose induces autophagy and whether vesicle formation is associated with autophagy. The results showed that sucrose induces autophagy while being accumulated within the endosomes/lysosomes. These vesicles were swollen and packed within the cytoplasm. Furthermore, trehalose and the trisaccharide raffinose, which are not hydrolyzed in mammalian cells, increased the rate of vesicles accumulation and LC3-II level (a protein marker of autophagy). However, fructose and maltose did not show the same effects. The correlation between the two processes, vesicle accumulation and autophagy induction, was confirmed by treatment of cells with sucrose plus invertase, or maltose plus acarbose-the α-glucosidase inhibitor-and by sucrose deprivation. Results also showed that vesicle accumulation was not affected by autophagy inhibition. Therefore, the data suggest that sucrose-induced autophagy through accumulation of sucrose-containing vesicles is caused by the absence of hydrolysis enzymes. PMID:25389129

  18. Report from the 1st Cardiovascular Outcome Trial (CVOT) Summit of the Diabetes & Cardiovascular Disease (D&CVD) EASD Study Group.

    Science.gov (United States)

    Schnell, Oliver; Standl, Eberhard; Catrinoiu, Doina; Genovese, Stefano; Lalic, Nebojsa; Skra, Jan; Valensi, Paul; Ceriello, Antonio

    2016-01-01

    The 1st Cardiovascular Outcome Trial (CVOT) Summit of the Diabetes & Cardiovascular Disease (D&CVD) EASD Study Group was held during the annual meeting on 30 October 2015 in Munich. This summit was organized in light of recently published and numerous ongoing CVOTs on diabetes, which have emerged in response to the FDA and the EMA Guidelines. The CVOT Summit stands as a novel conference setup, with the aim of serving as a reference meeting for all topics related to CVOTs in diabetes. Members of the steering committee of the D&CVD EASD Study Group constitute the backbone of the summit. It included presentations of key results on DPP-4 inhibitors, GLP-1-Analogues, SGLT-2 inhibitors, acarbose and insulins. Diabetologists' and cardiologists' perspective on the potential need of new study designs were also highlighted. Furthermore, panel discussions on the design of CVOTs on diabetes were included in the program. The D&CVD EASD Study Group will continue its activity. In-depth discussions and presentations of new CVOTs like LEADER, will be resumed at the 2nd CVOT on diabetes of the D&CVD EASD Study Group, which will be held from 20-22 October 2016 in Munich ( http://www.dcvd.org). PMID:26892706

  19. In vitro hypoglycemic effects of selected dietary fiber sources.

    Science.gov (United States)

    Ahmed, Faiyaz; Sairam, Sudha; Urooj, Asna

    2011-06-01

    The physiological functions of dietary fiber and its role in health promotion and risk reduction of some chronic diseases has been well documented. In the present investigation, the effect of three dietary fiber sources, oats (OA), barley (BA) and psyllium husk (PH) on glucose adsorption, diffusion and starch hydrolysis were studied using in vitro techniques by simulating gastrointestinal conditions and compared with the commercial dietary fiber sources wheat bran (WB), acarbose (ACB) and guar gum (GG). The glucose binding capacity of all the samples was higher than WB and ACB at 5 mM concentration. In all the samples, the diffusion of glucose was directly proportional to the time and diffusion rate was significantly lower (p ≤ 0.01) in the system containing various samples compared to control. Glucose dialysis retardation index (GDRI) was 100 for OA, BA and PH at 60 min, at 120 min the maximal GDRI was in PH. Whereas; WB and ACB exhibited maximal GDRI at 180 and 240 min. All of these mechanisms might create a concerted function in lowering the rate of glucose absorption and as a result, decrease the postprandial hyperglycemia. PMID:23572748

  20. In vitro α-amylase inhibitory activity and in vivo hypoglycemic effect of ethyl acetate extract of Mallotus repandus (Willd.) Muell. stem in rat model

    Institute of Scientific and Technical Information of China (English)

    Md. Rakib Hasan; Nizam Uddin; Md. Monir Hossain; Md. Mahadi Hasan; Md. Emtiaz Yousuf; Swagata Sarker Lopa; Tasmina Rahman

    2014-01-01

    Objective: To investigate the therapeutic effects of ethyl acetate extract of Mallotus repandus stem in α-amylase inhibitory activity (in vitro) and hypoglycemic activity in normal and glucose induced hyperglycemic rats (in vivo). Methods: Ethyl acetate extract of Mallotus repandus stem was tested for the presence of phytochemical constituents, α-amylase inhibitory activity and hypoglycemic effect in normal rats and glucose induced hyperglycemic rats.Results:Presence of different types of phytochemicals was identified in the extract. The extract has moderate α-amylase inhibitory activity [IC50=(2.038±0.033) mg/mL] as compared to acarbose. The does 1000 mg/kg significantly reduced (P<0.0100) fasting blood glucose level in normal rats. In oral glucose tolerance test, both 1000 and 2000 mg/kg doses showed good hypoglycemic activity (P<0.0001) like glibenclamide in each specific hour after administration. Overall time effect in oral glucose tolerance test was found extremely significant (P<0.0001) with F (3, 48) value=202.4.Conclusions:These findings suggest that this plant may be a potential source for the development of new oral hypoglycemic agent.

  1. Inhibitory Potential of Five Traditionally Used Native Antidiabetic Medicinal Plants on α-Amylase, α-Glucosidase, Glucose Entrapment, and Amylolysis Kinetics In Vitro

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    Carene M. N. Picot

    2014-01-01

    Full Text Available Five traditionally used antidiabetic native medicinal plants of Mauritius, namely, Stillingia lineata (SL, Faujasiopsis flexuosa (FF, Erythroxylum laurifolium (EL, Elaeodendron orientale (EO, and Antidesma madagascariensis (AM, were studied for possible α-amylase and α-glucosidase inhibitory property, glucose entrapment, and amylolysis kinetics in vitro. Only methanolic extracts of EL, EO, and AM (7472.92±5.99, 1745.58±31.66, and 2222.96±13.69 μg/mL, resp. were found to significantly (P<0.05 inhibit α-amylase and were comparable to acarbose. EL, EO, AM, and SL extracts (5000 μg/mL were found to significantly (P<0.05 inhibit α-glucosidase (between 87.41±3.31 and 96.87±1.37% inhibition. Enzyme kinetic studies showed an uncompetitive and mixed type of inhibition. Extracts showed significant (P<0.05 glucose entrapment capacities (8 to 29% glucose diffusion retardation index (GDRI, with SL being more active (29% GDRI and showing concentration-dependent activity (29, 26, 21, 14, and 5%, resp.. Amylolysis kinetic studies showed that methanolic extracts were more potent inhibitors of α-amylase compared to aqueous extracts and possessed glucose entrapment properties. Our findings tend to provide justification for the hypoglycaemic action of these medicinal plants which has opened novel avenues for the development of new phytopharmaceuticals geared towards diabetes management.

  2. Polyketides with α-Glucosidase Inhibitory Activity from a Mangrove Endophytic Fungus, Penicillium sp. HN29-3B1.

    Science.gov (United States)

    Liu, Yayue; Yang, Qin; Xia, Guoping; Huang, Hongbo; Li, Hanxiang; Ma, Lin; Lu, Yongjun; He, Lei; Xia, Xuekui; She, Zhigang

    2015-08-28

    Five new compounds, pinazaphilones A and B (1, 2), two phenolic compounds (4, 5), and penicidone D (6), together with the known Sch 1385568 (3), (±)-penifupyrone (7), 3-O-methylfunicone (8), 5-methylbenzene-1,3-diol (9), and 2,4-dihydroxy-6-methylbenzoic acid (10) were obtained from the culture of the endophytic fungus Penicillium sp. HN29-3B1, which was isolated from a fresh branch of the mangrove plant Cerbera manghas collected from the South China Sea. Their structures were determined by analysis of 1D and 2D NMR and mass spectroscopic data. Structures of compounds 4 and 7 were further confirmed by a single-crystal X-ray diffraction experiment using Cu Kα radiation. The absolute configurations of compounds 1-3 were assigned by quantum chemical calculations of the electronic circular dichroic spectra. Compounds 2, 3, 5, and 7 inhibited α-glucosidase with IC50 values of 28.0, 16.6, 2.2, and 14.4 μM, respectively, and are thus more potent than the positive control, acarbose. PMID:26230970

  3. Targeted genome editing in the rare actinomycete Actinoplanes sp. SE50/110 by using the CRISPR/Cas9 System.

    Science.gov (United States)

    Wolf, Timo; Gren, Tetiana; Thieme, Eric; Wibberg, Daniel; Zemke, Till; Pühler, Alfred; Kalinowski, Jörn

    2016-08-10

    The application of genome editing technologies, like CRISPR/Cas9 for industrially relevant microorganisms, is becoming increasingly important. Compared to other methods of genetic engineering the decisive factor is that CRISPR/Cas9 is relatively easy to apply and thus time and effort can be significantly reduced in organisms, which are otherwise genetically difficult to access. Because of its many advantages and opportunities, we adopted the CRISPR/Cas9 technology for Actinoplanes sp. SE50/110, the producer of the diabetes type II drug acarbose. The functionality of genome editing was successfully shown by the scarless and antibiotic marker-free deletion of the gene encoding the tyrosinase MelC, which catalyzes the formation of the dark pigment eumelanin in the wild type strain. The generated ΔmelC2 mutant of Actinoplanes sp. SE50/110 no longer produces this pigment and therefore the supernatant does not darken. Furthermore, it was shown that the plasmid containing the gene for the Cas9 protein was removed by increasing the temperature due to its temperature-sensitive replication. The precision of the intended mutation was proven and possible off-target effects caused by the genome editing system were ruled out by genome sequencing of several mutants. PMID:27262504

  4. KAPASITAS ANTIOKSIDAN DAN INHIBITOR ALFA GLUKOSIDASE EKSTRAK UMBI BAWANG DAYAK [Antioxidant and Alpha-Glucosidase Inhibitory Properties of Bawang Dayak Bulb Extracts

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    Andi Early Febrinda*

    2013-12-01

    Full Text Available Bawang dayak (Eleutherine palmifolia is an indigenous plant in Borneo traditionally used by Dayak tribes to treat any kind of degenerative deseases including diabetes mellitus. The purpose of this research was to measure antioxidant and antidiabetic capacities of water and ethanolic extracts of bawang dayak bulb. Parameters evaluated in this research were phytochemical screening, total phenolics, flavonoid content, DPPH free-radical scavenging activity, and alpha glucosidase inhibiting (AGI activity. The result showed that the total phenolics and flavonoid content in bawang dayak ethanolic extract (217.71 mg GAE/g and 65.35 mg QE/g were higher than that of the water extract (139.93 mg GAE/g and 16.95 mg QE/g. The ethanolic extract also had higher antioxidant and AGI activities (IC50 112 and 241 ppm than that of the water extract (IC50 526 and 505 ppm. In addition, the IC50 values for AGI in bawang dayak ethanolic extract was lower than acarbose which is known as a commercial antidiabetic agent.

  5. Clinical Observation of 105 Cases with Insulin Glargine Plus Oral Hypoglycemic Drugs for Treating Type 2 Diabetes%甘精胰岛素加口服降糖药治疗2型糖尿病105例临床观察

    Institute of Scientific and Technical Information of China (English)

    刘红丽; 王叶菊

    2011-01-01

    Objective To observe the therapeutic efficacy and safety of insulin glargine plus acarbose on patients with type 2 diabetes with poor efficacy of premixed human insulin in converted. Methods To se-lect105 patients with type 2 diabetic in Hanzhong Central Hospital from 2008 June to 2010 June inpatient, previous use of premixed human insulin 30R, poor glycemic control or hypoglycemia has emerged frequently, conversion of insulin glargine plus acarbose treatment. After 12 weeks,fasting blood glucose( FBG ),2-hour plasma glucose( 2hPG ),hemoglobin A1C( HbAlC )and recorded the incidence rate of hypoglycemia, changes in body mass and insulin dose were observed. Results In98 cases,fasting blood glucose,2-hour plasma glucose, hemoglobin A1C compliance rate was respectively 92% ,87% ,83% ,the incidence of hypoglycemia significantly decreased, insulin dose was reduced, the body mass was not significant changes. Conclusion For patients with poor effect of premixed human insulin in treatment of poor patients," 2 back 1" treatment strategy to provide better glycemic control, and reduce the rate of hypoglycemia.%目的 观察预混人胰岛素疗效不佳的2型糖尿病患者转换甘精胰岛素加阿卡波糖治疗后的疗效及安全性.方法 选取汉中市中心医院2008年6月至2010年6月住院的2型糖尿病患者105例,既往使用预混人胰岛素30R,血糖控制不佳或频繁出现低血糖者,转换甘精胰岛素加阿卡波糖治疗.12周后观察空腹血糖、餐后2 h血糖、糖化血红蛋白,并记录低血糖发生次数、体质量变化及胰岛素剂量.结果 98例患者空腹、餐后2 h血糖、糖化血红蛋白达标率分别是92%、87%、83%,低血糖发生率明显降低,胰岛素剂量较前减少,体质量无明显变化.结论 对于预混人胰岛素治疗欠佳的患者,"2退1"的治疗策略能提供更佳的血糖控制,并减少低血糖的发生率.

  6. Pilot study on the additive effects of berberine and oral type 2 diabetes agents for patients with suboptimal glycemic control

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    Di Pierro F

    2012-07-01

    Full Text Available Francesco Di Pierro,1 Nicola Villanova,2 Federica Agostini,2 Rebecca Marzocchi,2 Valentina Soverini,2 Giulio Marchesini21Scientific Department, Velleja Research, Milano, 2Diseases of Metabolism, S Orsola Malpighi Hospital, Bologna, ItalyBackground: Suboptimal glycemic control is a common situation in diabetes, regardless of the wide range of drugs available to reach glycemic targets. Basic research in diabetes is endeavoring to identify new actives working as insulin savers, use of which could delay the introduction of injectable insulin or reduce the insulin dose needed. Commonly available as a nutraceutical, berberine is a potential candidate.Methods and results: Because its low oral bioavailability can be overcome by P-glycoprotein inhibitors like herbal polyphenols, we have tested the nutraceutical combination of Berberis aristata extract and Silybum marianum extract (Berberol® in type 2 diabetes in terms of its additive effect when combined with a conventional oral regimen for patients with suboptimal glycemic control. After 90 days of treatment, the nutraceutical association had a positive effect on glycemic and lipid parameters, significantly reducing glycosylated hemoglobin, basal insulin, homeostatic model assessment of insulin resistance, total and low-density lipoprotein cholesterol, and triglycerides. A relevant effect was also observed in terms of liver function by measuring aspartate transaminase and alanine transaminase. The product had a good safety profile, with distinctive gastrointestinal side effects likely due to its acarbose-like action.Conclusion: Although further studies should be carried out to confirm our data, Berberol could be considered a good candidate as an adjunctive treatment option in diabetes, especially in patients with suboptimal glycemic control.Keywords: berberine, silymarin, glycosylated hemoglobin, diabetes

  7. Bioactive 30-Noroleanane Triterpenes from the Pericarps of Akebia trifoliata

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    Jing Wang

    2014-04-01

    Full Text Available Two new 30-noroleanane triterpenes, 2α,3β,20α-trihydroxy-30-norolean-12-en-28-oic acid (1, 2α,3β-dihydroxy-23-oxo-30-norolean-12,20(29-dien-28-oic acid (2, were isolated from the pericarps of Akebia trifoliata, together with four known ones, 3β-akebonoic acid (3, 2α,3β-dihydroxy-30-noroleana-12,20(29-dien-28-oic acid (4, 3α-akebonoic acid (5 and quinatic acid (6. Their structures were established on the basis of detailed spectroscopic analysis, and they were all isolated from the pericarps of A. trifoliata for the first time. Compounds 3−6 showed in vitro bacteriostatic activity against four assayed Gram-positive bacterial strains. In particular 3 showed antibacterial activity toward MRSA with a MIC value 25 μg/mL, which was more potent than kanamycin (MIC 125 μg/mL. No compounds showed antibacterial activity toward the three Gram-negative bacteria tested. Compounds 4 and 5 showed interesting in vitro growth inhibitory activity against human tumor A549 and HeLa cell lines, with IC50 values ranging from 8.8 and 5.6 μM, respectively. Compounds 1, 2, 5 and 6 were further revealed to show significant in vitro α-glucosidase inhibitory activity with IC50 values from 0.035 to 0.367 mM, which were more potent than the reference compound acarbose (IC50 0.409 mM.

  8. Synthesis and structure investigation of novel pyrimidine-2,4,6-trione derivatives of highly potential biological activity as anti-diabetic agent

    Science.gov (United States)

    Barakat, Assem; Soliman, Saied M.; Al-Majid, Abdullah Mohammed; Lotfy, Gehad; Ghabbour, Hazem A.; Fun, Hoong-Kun; Yousuf, Sammer; Choudhary, M. Iqbal; Wadood, Abdul

    2015-10-01

    Synthesis of (±)-1,3-dimethyl-5-(1-(3-nitrophenyl)-3-oxo-3-phenylpropyl)pyrimidine-2,4,6(1H,3H,5H)-trione (3) is reported. The structure of compound 3 was deduced by using spectroscopic methods, X-ray crystallography, and DFT calculations. The calculated geometric parameters were found to be in good agreement with the experimental data obtained from the X-ray structure. The NBO calculations were performed to predict the natural atomic charges at the different atomic sites and to study the different intramolecular charge transfer (ICT) interactions. The high LP(3)O6 →z BD*(2)O5-N3 ICT interaction energy (165.36 kcal/mol) indicated very strong n → π* electron delocalization while the small LP(2)O → BD*(1)C-H ICT interaction energies indicated that the C-H … O intramolecular interactions are weak. The 1H and 13C NMR chemical shifts calculated using GIAO method showed good agreement with the experimental data. The calculated electronic spectra of the studied compound using TD-DFT method showed intense electronic transition band at 243.9 nm (f = 0.2319) and a shoulder at 260.2 nm (f = 0.1483) which were due to H-4/H-2/H-1/H → L+2 and H-5 → L electronic excitations, respectively. Compound 3 (IC50 = 305 ± 3.8 μM) was identified as a potent inhibitor of α-glucosidase in vitro and showed several fold more inhibition than the standard drug acarbose (IC50 = 841 ± 1.73 μM). Molecular docking of the synthesized compound was discussed.

  9. In vitro potential of Ascophyllum nodosum phenolic antioxidant-mediated alpha-glucosidase and alpha-amylase inhibition.

    Science.gov (United States)

    Apostolidis, E; Lee, C M

    2010-04-01

    Ascophyllum nodosum is a brown seaweed that grows abundantly in the Northeast coastal region. In this study, the potential of A. nodosum for type 2 diabetes management through antioxidant-mediated alpha-glucosidase and alpha-amylase inhibition was investigated. After the initial screening of 4 locally harvested seaweeds, A. nodosum was chosen for its highest phenolic content and was subjected to water extraction. Among extraction ratios of 50 g to 100 to 1000 mL at room temperature, 50 g/400 mL yielded the highest phenolic content of 4.5 mg/g wet weight. For evaluation of extraction temperature ranging from 20 to 80 degrees C, 50 g/400 mL was chosen as a minimum amount of extractant. Among temperatures studied, extraction at 80 degrees C resulted in the highest total phenolic contents (4.2 mg/g wet weight). All extracts had similar levels of antioxidant activity in the range of 60% to 70% in terms of 1, 1-diphenyl-2-picrylhydrazyl (DPPH) free radical scavenging activity. The 80 degrees C extract had the highest alpha-glucosidase and alpha-amylase inhibitory activity with IC(50) of 0.24 and 1.34 microg phenolics, respectively, compared to the IC(50) of acarbose, reference inhibitor, being 0.37 and 0.68 microg. The results show that fresh A. nodosum has strong alpha-glucosidase and mild alpha-amylase inhibitory activities that correlated with phenolic contents. This study suggests a nutraceutical potential of A. nodosum based on phytochemical antioxidant and antihyperglycemia activities. PMID:20492300

  10. Novel benzoxazine-based aglycones block glucose uptake in vivo by inhibiting glycosidases.

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    Hanumantharayappa Bharathkumar

    Full Text Available Glycoside hydrolases catalyze the selective hydrolysis of glycosidic bonds in oligosaccharides, polysaccharides, and their conjugates. β-glucosidases occur in all domains of living organisms and constitute a major group among glycoside hydrolases. On the other hand, the benzoxazinoids occur in living systems and act as stable β-glucosides, such as 2-(2,4-dihydroxy-7-methoxy-2H-1,4-benzoxazin-3(4H-one-β-D-gluco-pyranose, which hydrolyse to an aglycone DIMBOA. Here, we synthesized the library of novel 1,3-benzoxazine scaffold based aglycones by using 2-aminobenzyl alcohols and aldehydes from one-pot reaction in a chloroacetic acid catalytic system via aerobic oxidative synthesis. Among the synthesized benzoxazines, 4-(7-chloro-2,4-dihydro-1H-benzo[d][1,3]oxazin-2-ylphenol (compound 7 exhibit significant inhibition towards glucosidase compared to acarbose, with a IC50 value of 11.5 µM. Based upon results generated by in silico target prediction algorithms (Naïve Bayesian classifier, these aglycones potentially target the additional sodium/glucose cotransporter 1 (where a log likelihood score of 2.70 was observed. Furthermore, the in vitro glucosidase activity was correlated with the in silico docking results, with a high docking score for the aglycones towards the substrate binding site of glycosidase. Evidently, the in vitro and in vivo experiments clearly suggest an anti-hyperglycemic effect via glucose uptake inhibition by 4-(7-chloro-2,4-dihydro-1H-benzo[d][1,3]oxazin-2-ylphenol in the starved rat model. These synthetic aglycones could constitute a novel pharmacological approach for the treatment, or re-enforcement of existing treatments, of type 2 diabetes and associated secondary complications.

  11. Alpha-Glucosidase Enzyme Biosensor for the Electrochemical Measurement of Antidiabetic Potential of Medicinal Plants.

    Science.gov (United States)

    Mohiuddin, M; Arbain, D; Islam, A K M Shafiqul; Ahmad, M S; Ahmad, M N

    2016-12-01

    A biosensor for measuring the antidiabetic potential of medicinal plants was developed by covalent immobilization of α-glucosidase (AG) enzyme onto amine-functionalized multi-walled carbon nanotubes (MWCNTs-NH2). The immobilized enzyme was entrapped in freeze-thawed polyvinyl alcohol (PVA) together with p-nitrophenyl-α-D-glucopyranoside (PNPG) on the screen-printed carbon electrode at low pH to prevent the premature reaction between PNPG and AG enzyme. The enzymatic reaction within the biosensor is inhibited by bioactive compounds in the medicinal plant extracts. The capability of medicinal plants to inhibit the AG enzyme on the electrode correlates to the potential of the medicinal plants to inhibit the production of glucose from the carbohydrate in the human body. Thus, the inhibition indicates the antidiabetic potential of the medicinal plants. The performance of the biosensor was evaluated to measure the antidiabetic potential of three medicinal plants such as Tebengau (Ehretis laevis), Cemumar (Micromelum pubescens), and Kedondong (Spondias dulcis) and acarbose (commercial antidiabetic drug) via cyclic voltammetry, amperometry, and spectrophotometry. The cyclic voltammetry (CV) response for the inhibition of the AG enzyme activity by Tebengau plant extracts showed a linear relation in the range from 0.423-8.29 μA, and the inhibition detection limit was 0.253 μA. The biosensor exhibited good sensitivity (0.422 μA/mg Tebengau plant extracts) and rapid response (22 s). The biosensor retains approximately 82.16 % of its initial activity even after 30 days of storage at 4 °C. PMID:26887579

  12. Longer lifespan in male mice treated with a weakly estrogenic agonist, an antioxidant, an α-glucosidase inhibitor or a Nrf2-inducer.

    Science.gov (United States)

    Strong, Randy; Miller, Richard A; Antebi, Adam; Astle, Clinton M; Bogue, Molly; Denzel, Martin S; Fernandez, Elizabeth; Flurkey, Kevin; Hamilton, Karyn L; Lamming, Dudley W; Javors, Martin A; de Magalhães, João Pedro; Martinez, Paul Anthony; McCord, Joe M; Miller, Benjamin F; Müller, Michael; Nelson, James F; Ndukum, Juliet; Rainger, G Ed; Richardson, Arlan; Sabatini, David M; Salmon, Adam B; Simpkins, James W; Steegenga, Wilma T; Nadon, Nancy L; Harrison, David E

    2016-10-01

    The National Institute on Aging Interventions Testing Program (ITP) evaluates agents hypothesized to increase healthy lifespan in genetically heterogeneous mice. Each compound is tested in parallel at three sites, and all results are published. We report the effects of lifelong treatment of mice with four agents not previously tested: Protandim, fish oil, ursodeoxycholic acid (UDCA) and metformin - the latter with and without rapamycin, and two drugs previously examined: 17-α-estradiol and nordihydroguaiaretic acid (NDGA), at doses greater and less than used previously. 17-α-estradiol at a threefold higher dose robustly extended both median and maximal lifespan, but still only in males. The male-specific extension of median lifespan by NDGA was replicated at the original dose, and using doses threefold lower and higher. The effects of NDGA were dose dependent and male specific but without an effect on maximal lifespan. Protandim, a mixture of botanical extracts that activate Nrf2, extended median lifespan in males only. Metformin alone, at a dose of 0.1% in the diet, did not significantly extend lifespan. Metformin (0.1%) combined with rapamycin (14 ppm) robustly extended lifespan, suggestive of an added benefit, based on historical comparison with earlier studies of rapamycin given alone. The α-glucosidase inhibitor, acarbose, at a concentration previously tested (1000 ppm), significantly increased median longevity in males and 90th percentile lifespan in both sexes, even when treatment was started at 16 months. Neither fish oil nor UDCA extended lifespan. These results underscore the reproducibility of ITP longevity studies and illustrate the importance of identifying optimal doses in lifespan studies. PMID:27312235

  13. Composition and Biological Activity of Volatile Oil from Salviajudaica and S. multicaulis from Jordan.

    Science.gov (United States)

    Afifi, Fatma U; Kasabri, Violet; Al-Jaber, Hala I; Abu-Irmaileh, Barakat E; Al-Qudah, Mahmoud A; Abazaa, Ismail F

    2016-04-01

    The aim of this work was to determine the composition of the hydro-distilled essential oil of Salvia judaica Boiss. and S. multicaulis Vahl. (Lamiaceae) from Jordan by GC and GC-MS and to report the actual composition of their fresh leaves and flowers using SPME (Solid Phase Micro-Extraction).Their dual alpha-amylase/alpha glucosidase and pancreatic lipase inhibitory activities as well as their anti-proliferative potential were screened. The aroma profile of the leaves, flowers, and flowers at pre-flowering stages of S. judaica, obtained through SPME was composed of sesquiterpene hydrocarbons (87.7 %, 71.8 %, and 86.2 %, respectively) while the hydro-distilled oil of the dry leaves was rich in oxygenated sesquiterpenes (50.8%). Fresh leaves of S. multicaulis were rich in oxygenated monoterpenes (58.1%), while monoterpene hydrocarbons dominated the blooming flowers (57.2%) and the flowers at the pre-flowering stage (64.7%). The hydro-distilled oil of the dry leaves was rich in oxygenated monoterpenes (77.6%). With doxorubicin as a positive control, no anti-proliferative activity was observed against colorectal cancer cell lines HT29, HCT116, and SW620 using SRB assay for either Salvia spp. In vitro enzymatic starch digestion was evaluated with Acarbose (IC50: 0.2 ± 0.0 µg /mL) as the reference drug. The respective IC50 (mg/mL) values of S. judaica and S. multicaulis aqueous extracts were 4.9 ± 0.4 and 10.3 ± 0.9. Modulation of pancreatic lipase activity (PL) was determined by colorimetry and compared with Orlistat (IC50 : 0.11 ± 0.0 µg/mL). PL-IC50 values (µg/mL) obtained for S. judaica and S. multicaulis were 108.5±6.4 and 31.8 ± 0.8, respectively.

  14. Composition and Biological Activity of Volatile Oil from Salviajudaica and S. multicaulis from Jordan.

    Science.gov (United States)

    Afifi, Fatma U; Kasabri, Violet; Al-Jaber, Hala I; Abu-Irmaileh, Barakat E; Al-Qudah, Mahmoud A; Abazaa, Ismail F

    2016-04-01

    The aim of this work was to determine the composition of the hydro-distilled essential oil of Salvia judaica Boiss. and S. multicaulis Vahl. (Lamiaceae) from Jordan by GC and GC-MS and to report the actual composition of their fresh leaves and flowers using SPME (Solid Phase Micro-Extraction).Their dual alpha-amylase/alpha glucosidase and pancreatic lipase inhibitory activities as well as their anti-proliferative potential were screened. The aroma profile of the leaves, flowers, and flowers at pre-flowering stages of S. judaica, obtained through SPME was composed of sesquiterpene hydrocarbons (87.7 %, 71.8 %, and 86.2 %, respectively) while the hydro-distilled oil of the dry leaves was rich in oxygenated sesquiterpenes (50.8%). Fresh leaves of S. multicaulis were rich in oxygenated monoterpenes (58.1%), while monoterpene hydrocarbons dominated the blooming flowers (57.2%) and the flowers at the pre-flowering stage (64.7%). The hydro-distilled oil of the dry leaves was rich in oxygenated monoterpenes (77.6%). With doxorubicin as a positive control, no anti-proliferative activity was observed against colorectal cancer cell lines HT29, HCT116, and SW620 using SRB assay for either Salvia spp. In vitro enzymatic starch digestion was evaluated with Acarbose (IC50: 0.2 ± 0.0 µg /mL) as the reference drug. The respective IC50 (mg/mL) values of S. judaica and S. multicaulis aqueous extracts were 4.9 ± 0.4 and 10.3 ± 0.9. Modulation of pancreatic lipase activity (PL) was determined by colorimetry and compared with Orlistat (IC50 : 0.11 ± 0.0 µg/mL). PL-IC50 values (µg/mL) obtained for S. judaica and S. multicaulis were 108.5±6.4 and 31.8 ± 0.8, respectively. PMID:27396212

  15. Production of a highly potent epoxide through the microbial metabolism of 3β-acetoxyurs-11-en-13β,28-olide by Aspergillus niger culture.

    Science.gov (United States)

    Ali, Sajid; Nisar, Muhammad; Gulab, Hussain

    2016-09-01

    Context 3β-Acetoxyurs-11-en-13β,28-olide (I), a triterpenoid, is found in most plant species. Pharmacologically triterpenes are very effective compounds with potent anticancer, anti-HIV and antimicrobial activities. Objectives Microbial transformation of 3β-acetoxyurs-11-en-13β,28-olide (I) was performed in order to obtain derivatives with improved pharmacological potential. Materials and methods Compound (I, 100 mg) was incubated with Aspergillus niger culture for 12 d. The metabolite formed was purified through column chromatography. Structure elucidation was performed through extensive spectroscopy (IR, MS and NMR). In vitro α- and β-glucosidase inhibitory, and antiglycation potentials of both substrate and metabolite were evaluated. Results Structure of metabolite II was characterized as 3β-acetoxyurs-11,12-epoxy-13β,28-olide (II). Metabolite II was found to be an oxidized product of compound I. In vitro α- and β-glucosidases revealed that metabolite II was a potent and selective inhibitor of α-glucosidase (IC50 value = 3.56 ± 0.38 μM), showing that the inhibitory effect of metabolite II was far better than compound I (IC50 value = 14.7 ± 1.3 μM) as well as acarbose (IC50 value = 545 ± 7.9 μM). Antiglycation potential of compound II was also high with 82.51 ± 1.2% inhibition. Thus, through oxidation, the biological potential of the substrate molecule can be enhanced. Conclusion Biotransformation can be used as a potential tool for the production of biologically potent molecules.

  16. A comparative study of alpha amylase inhibitory activities of common anti-diabetic plants at Kharagpur 1 block

    Directory of Open Access Journals (Sweden)

    Dineshkumar B

    2010-01-01

    Full Text Available In India, the prevalence of diabetes mellitus is on the increase and needs to be addressed appropriately. In this study area, herbal remedies are considered convenient for management of Type 2 diabetes with postprandial hyperglycemia due to their traditional acceptability and availability, low costs, lesser side effects. Comparative evaluation of alpha amylase inhibitory activities of selected plants extracts. Kharagpur is situated in the Midnapur West district of West Bengal in India. In this district, diabetes prevalence is comparatively high. Ten common plants in IIT Kharagpur 1 Block namely, Acalypha indica, Allium cepa, Allium sativum, Azadirachta indica, Musa sapientum, Mangifera indica, Murraya, Ocimum sanctum, Phyllanthus amarus and Tinospora cordifolia were tested for their alpha amylase inhibitory activities to establish anti-diabetic potentials. The plant extracts were prepared sequentially with petroleum ether, hexane, chloroform, ethanol and aqueous. The extracts obtained were subjected to in vitro alpha amylase inhibitory assay using starch azure as a substrate and porcine pancreatic amylase as the enzyme. Statistical difference and linear regression analysis were performed by using Graphpad prism 5 statistical software. Ethanol extracts of Mangifera indica, Azadirachta indica and petroleum ether extract of Murraya koenigii (at a concentrations 10-100μg/ml showed maximum percentage inhibition on alpha amylase activity with an IC 50 value of 37.86 ± 0.32μg/ml, 62.99 ± 1.20μg/ml and 59.0 ± 0.51μg/ml respectively when compared with acarbose (IC 50 value 83.33 ± 0.75μg/ml. The results showing that Mangifera indica, Azadirachta indica and Murraya koenigii might be effective in lowering post prandial hyperglycemia.

  17. New treatments for patients with type 2 diabetes mellitus.

    Science.gov (United States)

    Wolffenbuttel, B H; Graal, M B

    1996-11-01

    In subjects with type 2 diabetes, both defects of insulin secretion and insulin resistance contribute to the development of hyperglycaemia. The major goals of treatment are to optimise blood glucose control, and normalise the associated lipid disturbances and elevated blood pressure. Pharmacologic treatment is often necessary. This paper discusses new forms of oral treatment for subjects with type 2 diabetes. These include a new sulphonylurea compound glimepiride (Amaryl), which binds to a different protein of the putative sulphonylurea receptor than glibenclamide, and seems to have a lower risk of hypoglycaemia. A new class of drugs with insulin secretory capacity, of which repaglinide (NovoNorm) is the leading compound, is now in phase III clinical trials. Alpha-glucosidase inhibitors reversibly inhibit alpha-glucosidase enzymes in the small intestine, which delays cleavage of oligo- and disaccharides to monosaccharides. This leads to a delayed and reduced blood glucose rise after a meal. Two compounds are in development or have been marketed, ie, miglitol and acarbose (Glucobay). Another new class of drugs is the thiazolidine-diones, which seem to work by enhancing insulin action. The 'insulin sensitising' effects of the leading compounds, troglitazone and BRL 49653C, do not involve any effect on insulin secretion. These drugs also seem to beneficially influence serum cholesterol and triglyceride levels. Oral antihyperglycaemic agents can be used only during a limited period of time in most patients, after which the diabetic state 'worsens' and insulin therapy has to be started. In this light, two new forms of treatment which require subcutaneous injections are also discussed: the synthetic human amylin analogue AC137 (pramlintide) and glucagon-like peptide-1 (7-36)-amide, a strong glucose-dependent stimulator of insulin secretion. It remains to be seen whether these compounds can be developed further for clinical use in patients with diabetes.

  18. Synthesis of novel flavone hydrazones: in-vitro evaluation of α-glucosidase inhibition, QSAR analysis and docking studies.

    Science.gov (United States)

    Imran, Syahrul; Taha, Muhammad; Ismail, Nor Hadiani; Kashif, Syed Muhammad; Rahim, Fazal; Jamil, Waqas; Hariono, Maywan; Yusuf, Muhammad; Wahab, Habibah

    2015-11-13

    Thirty derivatives of flavone hydrazone (5-34) had been synthesized through a five-step reaction and screened for their α-glucosidase inhibition activity. Chalcone 1 was synthesized through aldol condensation then subjected through oxidative cyclization, esterification, and condensation reaction to afford the final products. The result for baker's yeast α-glucosidase (EC 3.2.1.20) inhibition assay showed that all compounds are active with reference to the IC50 value of the acarbose (standard drug) except for compound 3. Increase in activity observed for compounds 2 to 34 clearly highlights the importance of flavone, hydrazide and hydrazone linkage in suppressing the activity of α-glucosidase. Additional functional group on N-benzylidene moiety further enhances the activity significantly. Compound 5 (15.4 ± 0.22 μM), a 2,4,6-trihydroxy substituted compound, is the most active compound in the series. Other compounds which were found to be active are those having chlorine, fluorine, and nitro substituents. Compounds with methoxy, pyridine, and methyl substituents are weakly active. Further studies showed that they are not active in inhibiting histone deacetylase activity and do not possess any cytotoxic properties. QSAR model was being developed to further identify the structural requirements contributing to the activity. Using Discovery Studio (DS) 2.5, various 2D descriptors were being used to develop the model. The QSAR model is able to predict the pIC50 and could be used as a prediction tool for compounds having the same skeletal framework. Molecular docking was done for all compounds using homology model of α-glucosidase to identify important binding modes responsible for inhibition activity. PMID:26491979

  19. Heart Failure Considerations of Antihyperglycemic Medications for Type 2 Diabetes.

    Science.gov (United States)

    Standl, Eberhard; Schnell, Oliver; McGuire, Darren K

    2016-05-27

    Prevalent and incident heart failure (HF) is increased in people with type 2 diabetes mellitus, with risk directly associated with the severity of hyperglycemia. Furthermore, in patients with type 2 diabetes mellitus, mortality is increased ≈10-fold in patients with versus without HF. Reducing HF with antihyperglycemic therapies, however, has been unsuccessful until recently. In fact, HF as an important outcome in patients with type 2 diabetes mellitus seems to be heterogeneously modulated by antihyperglycemic medications, as evidenced by results from cardiovascular outcome trials (CVOTs) and large observational cohort studies. Appropriately powered and executed CVOTs are necessary to truly evaluate cardiovascular safety and efficacy of new antihyperglycemic medications, as reflected by the guidance of the US Food and Drug Administration and other regulatory agencies since 2008. In light of the best available evidence at present, metformin and the sodium-glucose-co-transporter 2-inhibitor empagliflozin seem to be especially advantageous with regard to HF effects, with their use associated with reduced HF events and improved mortality. Acarbose, the dipeptidyl-peptidase 4-inhibitor sitagliptin, the glucagon-like peptide 1-receptor agonist lixisenatide based on presently available CVOT results comprise reasonable additional options, as significant harm in terms of HF has been excluded for those drugs. Additions to this list are anticipated pending results of ongoing CVOTs. Although no HF harm was seen in CVOTs for insulin or sulfonylureas, they should be used only with caution in patients with HF, given their established high risk for hypoglycemia and some uncertainties on their safety in patients with HF derived from epidemiological observations. Pioglitazone is contraindicated in patients with HF>New York Heart Association I, despite some benefits suggested by CVOT subanalyses. PMID:27230644

  20. Effects of carbohydrase-inhibiting compounds on in vitro rumen fermentation

    Directory of Open Access Journals (Sweden)

    Giorgio Marchesini

    2014-08-01

    Full Text Available Batch culture fermentations with ruminal content were conducted to determine the effects of plant-derived [bilberry extract (BBE, phaseolamin, white mulberry (WMB, common flax] carbohydrase-inhibiting compounds on microbial fermentation. The cultures with these compounds, at two different doses (15 and 150 mg, were compared with both acarbose (ACB and batch cultures without the addition of any enzyme-inhibiting compounds (Control. Incubations were conducted in triplicate and replicated. The pH, volatile fatty acids, ammonia N, apparent dry matter (DMD and starch disappearance were measured after 5 and 24 h of incubation. Treatment with ACB, after 5 h, significantly reduced maize meal fermentation, resulting in the highest pH levels (P<0.01, the lowest total VFA concentration (P=0.01 and the lowest DMD (P<0.01. On the opposite, BBE and WMB caused the highest drop in pH, due to the rapid fermentation of their sugar content. Treatment with BBE resulted in an increase in propionate and in an apparently low ammonia N concentration, whilst ACB (150 mg led to the highest values of acetate (P<0.05 and to a relative high concentration of ammonia N. After 24 h the differences in the fermentation pattern among supplements remained similar to those found after 5 h. In addition, BBE showed an activity against starch degradation, although this effect was concealed by the fermentation of sugars present in that supplement. These results show that some compounds modify the fermentation pattern of the substrate, but further studies are needed to clarify their impact on the complex rumen microbial community.

  1. In Vitro Antioxidant, Anti-Diabetes, Anti-Dementia, and Inflammation Inhibitory Effect of Trametes pubescens Fruiting Body Extracts

    Directory of Open Access Journals (Sweden)

    Kyung Hoan Im

    2016-05-01

    Full Text Available Trametes pubescens, white rot fungus, has been used for folk medicine in Asian countries to treat ailments such as cancer and gastrointestinal diseases. This study was initiated to evaluate the in vitro antioxidant, anti-diabetes, anti-dementia, and anti-inflammatory activities of T. pubescens fruiting bodies. The 1,1-diphenyl-2-picryl-hydrazyl (DPPH free radical scavenging activities of T. pubescens methanol (ME and hot water (HWE extracts (2.0 mg/mL were comparable to butylated hydroxytoluene (BHT, the positive control. However, the chelating effects of ME and HWE were significantly higher than that of BHT. The HWE (6 mg/mL also showed comparable reducing power to BHT. Eleven phenol compounds were detected by high performance liquid chromatography (HPLC analysis. The α-amylase and α-glucosidase inhibitory activities of the ME and HWE of the mushroom were lower than Acarbose, the standard reference; however, the inhibitory effects of the mushroom extracts at 2.0 mg/mL were moderate. The acetylcholinesterase (AChE and butyrylcholinesterase (BChE inhibitory effects of ME and HWE were moderate and comparable with galanthamine, the standard drug to treat early stages of Alzheimer’s disease (AD. The ME had a neuroprotective effect against glutamate-induced PC-12 cell cytotoxicity at the concentration range of 2–40 μg/mL. The mushroom extracts also showed inflammation inhibitory activities such as production of nitric oxide (NO and expression of inducible nitric oxide synthase (iNOS in lipopolysaccharide (LPS-induced murine macrophage-like cell lines (RAW 264.7 and significantly suppressed the carrageenan-induced rat paw-edema. Therefore, fruiting body extracts of T. pubescens demonstrated antioxidant related anti-diabetes, anti-dementia and anti-inflammatory activities.

  2. Synthesis, X-Ray Crystal Structures, Biological Evaluation, and Molecular Docking Studies of a Series of Barbiturate Derivatives

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    Assem Barakat

    2016-01-01

    Full Text Available A series of barbiturates derivatives synthesized and screened for different set of bioassays are described. The molecular structures of compounds 5a, 5d, and 5f were solved by single-crystal X-ray diffraction techniques. The results of bioassay show that compounds 4a, 4b, 4c, 4d, 4e, 4f, and 4g are potent antioxidants in comparison to the tested standards, butylated hydroxytoluene (BHT, and N-acetylcysteine. Compounds 4a–4e (IC50=101.8±0.8–124.4±4.4 μM and 4g (IC50=104.1±1.9 μM were more potent antioxidants than the standard (BHT, IC50=128.8±2.1 μM. The enzyme inhibition potential of these compounds was also evaluated, in vitro, against thymidine phosphorylase, α-glucosidase, and β-glucuronidase enzymes. Compounds 4c, 4h, 4o, 4p, 4q, 5f, and 5m were found to be potent α-glucosidase inhibitors and showed more activity than the standard drug acarbose, whereas compounds 4v, and 5h were found to be potent thymidine phosphorylase inhibitors, more active than the standard drug, 7-deazaxanthine. All barbiturates derivatives (4a–4x, 4z, and 5a–5m were found to be noncytotoxic against human prostate (PC-3, Henrietta Lacks cervical (HeLa and Michigan Cancer Foundation-7 breast (MCF-7 cancer cell lines, and 3T3 normal fibroblast cell line, except 4y which was cytotoxic against all the cell lines.

  3. In Vitro Antioxidant, Anti-Diabetes, Anti-Dementia, and Inflammation Inhibitory Effect of Trametes pubescens Fruiting Body Extracts.

    Science.gov (United States)

    Im, Kyung Hoan; Nguyen, Trung Kien; Choi, Jaehyuk; Lee, Tae Soo

    2016-01-01

    Trametes pubescens, white rot fungus, has been used for folk medicine in Asian countries to treat ailments such as cancer and gastrointestinal diseases. This study was initiated to evaluate the in vitro antioxidant, anti-diabetes, anti-dementia, and anti-inflammatory activities of T. pubescens fruiting bodies. The 1,1-diphenyl-2-picryl-hydrazyl (DPPH) free radical scavenging activities of T. pubescens methanol (ME) and hot water (HWE) extracts (2.0 mg/mL) were comparable to butylated hydroxytoluene (BHT), the positive control. However, the chelating effects of ME and HWE were significantly higher than that of BHT. The HWE (6 mg/mL) also showed comparable reducing power to BHT. Eleven phenol compounds were detected by high performance liquid chromatography (HPLC) analysis. The α-amylase and α-glucosidase inhibitory activities of the ME and HWE of the mushroom were lower than Acarbose, the standard reference; however, the inhibitory effects of the mushroom extracts at 2.0 mg/mL were moderate. The acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory effects of ME and HWE were moderate and comparable with galanthamine, the standard drug to treat early stages of Alzheimer's disease (AD). The ME had a neuroprotective effect against glutamate-induced PC-12 cell cytotoxicity at the concentration range of 2-40 μg/mL. The mushroom extracts also showed inflammation inhibitory activities such as production of nitric oxide (NO) and expression of inducible nitric oxide synthase (iNOS) in lipopolysaccharide (LPS)-induced murine macrophage-like cell lines (RAW 264.7) and significantly suppressed the carrageenan-induced rat paw-edema. Therefore, fruiting body extracts of T. pubescens demonstrated antioxidant related anti-diabetes, anti-dementia and anti-inflammatory activities. PMID:27196881

  4. Diabetes mellitus in dogs and cats: diagnosis and therapy

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    Mot, T.,

    2008-12-01

    Full Text Available Diabetes mellitus (DM is a disease of humans and animals, which causes increased levels of blood sugar (glucose. Normally,glucose is brought into the cells by a hormone - insulin.The cells then metabolize glucose to make energy used for all functions of the body. Animals suffering from DM either lack insulin, or the cells cannotuse the insulin that is there. As a result, blood glucose levels increase, and the cells have to use other substances for energy. When blood glucose levels become too high, glucose is found in the urine, causing increased frequency of urination and increased drinking. When blood glucose remains elevated over a period of time, other metabolic changes can occur, such as weight loss, acidosis, seizures, coma, blindness, cataracts, and nerve damage. Animals that are eating normally and not showing signs of illness may only require a blood or urine test to diagnose DM. Concurrent diseases (such as infection, Cushing’s disease, hyperthyroidism, pancreatitis, gastroenteritis, inflammatory bowel disease, hepatic lipidosis, or kidney disease make diabetes more difficult to diagnose and manage. A complete blood screen and other specific tests may be recommended to obtain the diagnosis and baseline values for treatment and future monitoring. The treatment for diabetes in dogs is similar to the treatment for diabetes in humans, through diet and insulin therapy. Dogs and cats with DM are usually treated with insulin. Insulin is a protein and, as such, not suitable for oral administration. Thus, it is administered once or several times daily by the subcutaneous route. Adjustment of the blood glucose concentration demands long hospital care, and subsequently the owner constantly has to keep a strict schedule at home. In veterinary practice the main groups of oral antidiabetic (used in human medicine either are: carbohydrate absorption inhibitors (e.g. acarbose; insulin sensitisers (biguanides such as metformin, thiazolidinedions

  5. Drug Promiscuity in PDB: Protein Binding Site Similarity Is Key.

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    V Joachim Haupt

    Full Text Available Drug repositioning applies established drugs to new disease indications with increasing success. A pre-requisite for drug repurposing is drug promiscuity (polypharmacology - a drug's ability to bind to several targets. There is a long standing debate on the reasons for drug promiscuity. Based on large compound screens, hydrophobicity and molecular weight have been suggested as key reasons. However, the results are sometimes contradictory and leave space for further analysis. Protein structures offer a structural dimension to explain promiscuity: Can a drug bind multiple targets because the drug is flexible or because the targets are structurally similar or even share similar binding sites? We present a systematic study of drug promiscuity based on structural data of PDB target proteins with a set of 164 promiscuous drugs. We show that there is no correlation between the degree of promiscuity and ligand properties such as hydrophobicity or molecular weight but a weak correlation to conformational flexibility. However, we do find a correlation between promiscuity and structural similarity as well as binding site similarity of protein targets. In particular, 71% of the drugs have at least two targets with similar binding sites. In order to overcome issues in detection of remotely similar binding sites, we employed a score for binding site similarity: LigandRMSD measures the similarity of the aligned ligands and uncovers remote local similarities in proteins. It can be applied to arbitrary structural binding site alignments. Three representative examples, namely the anti-cancer drug methotrexate, the natural product quercetin and the anti-diabetic drug acarbose are discussed in detail. Our findings suggest that global structural and binding site similarity play a more important role to explain the observed drug promiscuity in the PDB than physicochemical drug properties like hydrophobicity or molecular weight. Additionally, we find ligand

  6. Alpha-Glucosidase Enzyme Biosensor for the Electrochemical Measurement of Antidiabetic Potential of Medicinal Plants

    Science.gov (United States)

    Mohiuddin, M.; Arbain, D.; Islam, A. K. M. Shafiqul; Ahmad, M. S.; Ahmad, M. N.

    2016-02-01

    A biosensor for measuring the antidiabetic potential of medicinal plants was developed by covalent immobilization of α-glucosidase (AG) enzyme onto amine-functionalized multi-walled carbon nanotubes (MWCNTs-NH2). The immobilized enzyme was entrapped in freeze-thawed polyvinyl alcohol (PVA) together with p-nitrophenyl-α- d-glucopyranoside (PNPG) on the screen-printed carbon electrode at low pH to prevent the premature reaction between PNPG and AG enzyme. The enzymatic reaction within the biosensor is inhibited by bioactive compounds in the medicinal plant extracts. The capability of medicinal plants to inhibit the AG enzyme on the electrode correlates to the potential of the medicinal plants to inhibit the production of glucose from the carbohydrate in the human body. Thus, the inhibition indicates the antidiabetic potential of the medicinal plants. The performance of the biosensor was evaluated to measure the antidiabetic potential of three medicinal plants such as Tebengau ( Ehretis laevis), Cemumar ( Micromelum pubescens), and Kedondong ( Spondias dulcis) and acarbose (commercial antidiabetic drug) via cyclic voltammetry, amperometry, and spectrophotometry. The cyclic voltammetry (CV) response for the inhibition of the AG enzyme activity by Tebengau plant extracts showed a linear relation in the range from 0.423-8.29 μA, and the inhibition detection limit was 0.253 μA. The biosensor exhibited good sensitivity (0.422 μA/mg Tebengau plant extracts) and rapid response (22 s). The biosensor retains approximately 82.16 % of its initial activity even after 30 days of storage at 4 °C.

  7. The role of lipid and carbohydrate digestive enzyme inhibitors in the management of obesity: a review of current and emerging therapeutic agents

    Directory of Open Access Journals (Sweden)

    Sonia A Tucci

    2010-05-01

    Full Text Available Sonia A Tucci, Emma J Boyland, Jason CG HalfordKissileff Laboratory for the Study of Human Ingestive Behaviour, School of Psychology, University of Liverpool, Liverpool, UKAbstract: Obesity is a global epidemic associated with significant morbidity and mortality in adults and ill health in children. A proven successful approach in weight management has been the disruption of nutrient digestion, with orlistat having been used to treat obesity for the last 10 years. Although orlistat-induced weight loss remains modest, it produces meaningful reductions in risk factors for obesity-related conditions such as diabetes and cardiovascular disease. Moreover, this lipase inhibitor is free of the serious side effects that have dogged appetite-suppressing drugs. This success had driven investigation into new generation nutraceuticals, supplements and pharmaceutical agents that inhibit the breakdown of complex carbohydrates and fats within the gut. This review focuses on agents purported to inhibit intestinal enzymes responsible for macronutrient digestion. Except for some synthetic products, the majority of agents reviewed are either botanical extracts or bacterial products. Currently, carbohydrate digestion inhibitors are under development to improve glycemic control and these may also induce some weight loss. However, colonic fermentation induced side effects, such as excess gas production, remain an issue for these compounds. The α-glucosidase inhibitor acarbose, and the α-amylase inhibitor phaseolamine, have been used in humans with some promising results relating to weight loss. Nonetheless, few of these agents have made it into clinical studies and without any clinical proof of concept or proven efficacy it is unlikely any will enter the market soon.Keywords: lipase, amylase, saccharidases, overweight, orlistat, Alli®, digestion, body weight

  8. Influence of Total Anthocyanins from Bitter Melon (Momordica charantia Linn.) as Antidiabetic and Radical Scavenging Agents.

    Science.gov (United States)

    Güdr, Aytaç

    2016-01-01

    The majority of the antioxidant and antidiabetic activities of fruits are anthocyanins; a group of polyphenolics that are responsible for the color of many fruits, vegetables and flowers. The harvesting time, storage conditions, maturity, extraction steps etc. are very important for the biological activities based on the alteration of chemical composition. The free radical scavenging and antidiabetic activities of total anthocyanins from bitter melon (Momordica charantia Linn) fruit (TAMC) were evaluated by considering four harvesting times. The free radical scavenging activities of the TAMC samples were assessed using DPPH(•), DMPD(•+) and ABTS(•+) assays against BHA, rutin and trolox standards. September as a harvesting period (TAMC-S) had effective DPPH(•) (SC50 2.55 ± 0.08 μg/mL), DMPD(•+) (SC50 2.68 ± 0.09 μg/mL) and ABTS(•+) (SC50 8.19 ± 0.09 μg/mL) scavenging activities compared with other samples and standards. In addition, August (TAMC-A) as a harvesting period showed very influential inhibitory activity against α-amylase (IC50 56.86 ± 1.12 μg/mL) and moderate inhibitory activity against α-glucosidase (IC50 88.19 ± 0.74 μg/mL). In comparison, pharmaceutical active ingredients such as acarbose exhibited anti-amylase and anti-glucosidase activities with IC50 values of 93.07 ± 1.49 μg/mL and 77.25 ± 1.20 μg/mL respectively. These results suggest that the correct selection of harvest period can significantly increase anthocyanin quantity because of the pharmaceutic properties of TAMC. Consequently, TAMC may be interesting for incorporation in pharmaceutical preparations for human health, since it can suppress hyperglycaemia that can be also used as food additives due to its antiradical activity. PMID:27610171

  9. Analysis of Sitagliptin Combined With Glimepiride in Treatment of Type 2 Diabetes Effect%西格列汀联合格列美脲治疗2型糖尿病的效果分析

    Institute of Scientific and Technical Information of China (English)

    王守丽

    2015-01-01

    目的:分析格列美脲联合西格列汀治疗2型糖尿病的临床疗效。方法选取60例2型糖尿病患者,30例(试验组)应用格列美脲联合西格列汀治疗,30例(对照组)应用格列美脲联合阿卡波糖治疗,对比两组治疗效果。结果治疗12周后,试验组和对照组的FBG、2 hPG和HbA1c水平均明显降低(P<0.05),但试验组FBG、2 hPG和HbA1c的水平均显著低于对照组(P<0.05)。结论格列美脲和西格列汀联合治疗2型糖尿病的临床效果好。%Objective Analysis of joint Sitagliptin Glimepiride clinical curative effect for the treatment of type 2 diabetes. Methods 60 cases of patients with type 2 diabetes were chosed, 30 cases (treatment group) application of combined Sitagliptin Glimepiride treatment, 30 cases (control group) application of combined acarbose Glimepiride treatment, compared two groups of therapeutic effect. Results After 12 weeks of treatment group and control group of FBG, 2 HPG and HbA1c levels were significantly lower (P<0.05), but the experimental group FBG, 2 HPG and HbA1c levels were significantly lower than control group (P<0.05). Conclusion Glimepiride and west Glenn dean combination therapy for type 2 diabetes clinical effect is good, is worth popularizing in clinic.

  10. Influence of sitgliptin and metformin treatment on glucose fluctuation and serum inflammatory factors in preliminary diagnosed type 2 diabetes mellitus

    Institute of Scientific and Technical Information of China (English)

    Qin Xiang; Xun Wu

    2016-01-01

    Objective:To investigate the influence of stigliptin and metformin treatment on glucose fluctuation and serum inflammatory factors in preliminary diagnosed Type 2 diabetes mellitus. Methods: From January 2014 to December 2015, 168 cases of patients with newly diagnosed Type 2 diabetes mellitus were recruited and divided randomly into observation group and control group. The observation group was given sitgliptin (Januvia, 100 mg per d), while the control group was given metformin (Glucophage tablet, initial dose 0.5 g bid, twice per d), and the dosage of drugs was adjusted every 2 weeks according to glucose level. If the glucose level still wasn’t controlled to reach the normal standard by maximum dosage of drugs, 0.5 g bid of acarbose (Glucobay) was applied for the treatment 3 times one day till the glucose level reached the normal standard and the observation was kept for 6 months. The HbA1c, BMI, fluctuation indexes, and serum inflammatory factors of two groups were compared. Results: After the treatment of control group and observation group, the differences of PPGE (t=8.425,P=0.012), MAGE (t=7.348,P=0.014) and MODD (t=9.327,P=0.010) between two groups were significant (P<0.05). The differences of IL-6 (t=6.337,P=0.010) and TNF-α(t=6.521,P=0.011) level of observation group and control group after treatment were statistical significant (P<0.05).Conclusions:The sitgliptin could not only achieve glycemic control goal as metformin, but also induce glucose fluctuation and inhibit serum inflammation better.

  11. 抗糖尿病药物的临床用药分析%Analysis of the usage of anti-diabetes drugs

    Institute of Scientific and Technical Information of China (English)

    李旭; 何晶; 韩莹旻; 邹明

    2011-01-01

    Objective To analyze the clinical application status of anti-diabetes agent used in our hospital, and to provide reference for clinical application. Methods The anti-diabetes drugs variety, amount and the frequency of drug usage and other data from 2007 to 2009, were statistically analyzed using internet methods. Results The sales revenue of the anti-diabetes drugs increased from year to year, and its sales proportion among all drugs in the hospital was gradually increasing at the same time. The sales revenue of the insulin-type drugs was the largest and increased every year. Acarbose, metformin and glimepiride were the main oral anti-diabetes drugs in our hospital. Conclusions Anti-diabetes drugs have big market potential. The drugs that are safe, effective with good compliance and moderate prices are the majority of diabetes-treating drugs.%目的 分析医院抗糖尿病药物的使用情况,为临床合理用药提供依据.方法 运用医院药库计算机网络系统对我院2007-2009年所用的抗糖尿病药物品种、金额和用药频度等数据进行统计学分析.结果 抗糖尿病药物的销售金额呈逐年上升趋势,在我院药物总销售金额所占比例逐渐增加.其中胰岛素类药物在所有抗糖尿病药物的销售中占有率最大,3年的销售金额分别为30.21万元、126.93和246.58万元.阿卡波糖、二甲双胍和格列美脲是我院使用的主要口服抗糖尿病药物.结论 糖尿病的致病因素很多,主要和胰岛素分泌或生成异常有关.抗糖尿病药物市场潜力大,安全、有效、依从性好、价格适中的药物是糖尿病治疗药物的必然发展趋势.

  12. 医院2012-2014年口服降糖药物利用分析%Use analysis of oral hypoglycemic drugs in hospital from 2012 to 2014

    Institute of Scientific and Technical Information of China (English)

    王燕平; 张琳

    2015-01-01

    目的 评价北京军区总医院口服降糖药的应用情况.方法 采用限定日剂量(DDD)分析方法,对北京军区总医院2012-2014年口服降糖药的用药频度、销售金额等数据进行统计、分析.结果 口服降糖药的用药频度逐年增长(2012-2014年依次为:1 874 755、1 913 100、2 233 570),销售金额呈增长趋势(2012-2014年依次为:1 073.42、1 027.66、1 324.25万元).用药频度和销售金额排序前3位的药品为阿卡波糖、二甲双胍、格列美脲;销售金额排序与用药频度排序的比值均为1.00.结论 本院门诊患者口服降糖药的使用基本合理.%Objective To analyze the use of oral hypoglycemic drugs in Beijing Military Region General Hospital of Chinese People' s Liberation Army.Methods The data of frequency of drug use (DDDs),sale account of oral hypoglycemic drugs in Beijing Military Region General Hospital of Chinese People's Liberation Army from 2012 to 2014 were retrospectively analyzed.Results The DDDs of oral hypoglycemic drugs increased year by year (2012:1 874 755,2013:1 913 100,2014:2 233 570),the sale account were keep increasing (2012:10.734 2 million yuan,2013:10.276 6 million yuan,2014:13.242 5 million yuan).Acarbose,metformin and glimepiride ranked top 3 for both DDDs and sale account,their rank ratio of DDDs/sale account were all 1.00.Conclusion The use of hypoglycemic drugs in our hospital is rational on the whole.

  13. Selected tea and tea pomace extracts inhibit intestinal α-glucosidase activity in vitro and postprandial hyperglycemia in vivo.

    Science.gov (United States)

    Oh, Jungbae; Jo, Sung-Hoon; Kim, Justin S; Ha, Kyoung-Soo; Lee, Jung-Yun; Choi, Hwang-Yong; Yu, Seok-Yeong; Kwon, Young-In; Kim, Young-Cheul

    2015-01-01

    Type 2 diabetes mellitus (T2DM) is a metabolic disorder characterized by postprandial hyperglycemia, which is an early defect of T2DM and thus a primary target for anti-diabetic drugs. A therapeutic approach is to inhibit intestinal α-glucosidase, the key enzyme for dietary carbohydrate digestion, resulting in delayed rate of glucose absorption. Although tea extracts have been reported to have anti-diabetic effects, the potential bioactivity of tea pomace, the main bio waste of tea beverage processing, is largely unknown. We evaluated the anti-diabetic effects of three selected tea water extracts (TWE) and tea pomace extracts (TPE) by determining the relative potency of extracts on rat intestinal α-glucosidase activity in vitro as well as hypoglycemic effects in vivo. Green, oolong, and black tea bags were extracted in hot water and the remaining tea pomace were dried and further extracted in 70% ethanol. The extracts were determined for intestinal rat α-glucosidases activity, radical scavenging activity, and total phenolic content. The postprandial glucose-lowering effects of TWE and TPE of green and black tea were assessed in male Sprague-Dawley (SD) rats and compared to acarbose, a known pharmacological α-glucosidase inhibitor. The IC50 values of all three tea extracts against mammalian α-glucosidase were lower or similar in TPE groups than those of TWE groups. TWE and TPE of green tea exhibited the highest inhibitory effects against α-glucosidase activity with the IC50 of 2.04 ± 0.31 and 1.95 ± 0.37 mg/mL respectively. Among the specific enzymes tested, the IC50 values for TWE (0.16 ± 0.01 mg/mL) and TPE (0.13 ± 0.01 mg/mL) of green tea against sucrase activity were the lowest compared to those on maltase and glucoamylase activities. In the animal study, the blood glucose level at 30 min after oral intake (0.5 g/kg body wt) of TPE and TWE of both green and black tea was significantly reduced compared to the control in sucrose-loaded SD rats. The TPE

  14. Dimerization mediates thermo-adaptation, substrate affinity and transglycosylation in a highly thermostable maltogenic amylase of Geobacillus thermoleovorans.

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    Deepika Mehta

    5 and acarbose, while the truncated form does not because of the lack of extra sugar-binding space formed due to dimerization. CONCLUSION/SIGNIFICANCE: N-terminal domain controls enthalpy-driven thermostabilization, substrate-binding affinity and transglycosylation activity of Gt-Mamy by homodimer formation.

  15. Diabetes: insulin resistance and derangements in lipid metabolism. Cure through intervention in fat transport and storage.

    Science.gov (United States)

    Raz, Itamar; Eldor, Roi; Cernea, Simona; Shafrir, Eleazar

    2005-01-01

    of the compliant application of drastic lifestyle change comprising both diet and exercise and pharmacotherapy that reduces mesenteric fat mass and activity. The first step should be an attempt to effectively induce a lifestyle change. Next comes pharmacotherapy including acarbose, metformin, PPARgamma, or PPARgammaalpha agonists, statins and orlistat, estrogens in postmenopausal women or testosterone in men. Among surgical procedures, gastric bypass has been proven to produce beneficial results in advance of other surgical techniques, the evidence basis of which still needs strengthening. PMID:15386813

  16. Selected Tea and Tea Pomace Extracts Inhibit Intestinal α-Glucosidase Activity in Vitro and Postprandial Hyperglycemia in Vivo

    Directory of Open Access Journals (Sweden)

    Jungbae Oh

    2015-04-01

    Full Text Available Type 2 diabetes mellitus (T2DM is a metabolic disorder characterized by postprandial hyperglycemia, which is an early defect of T2DM and thus a primary target for anti-diabetic drugs. A therapeutic approach is to inhibit intestinal α-glucosidase, the key enzyme for dietary carbohydrate digestion, resulting in delayed rate of glucose absorption. Although tea extracts have been reported to have anti-diabetic effects, the potential bioactivity of tea pomace, the main bio waste of tea beverage processing, is largely unknown. We evaluated the anti-diabetic effects of three selected tea water extracts (TWE and tea pomace extracts (TPE by determining the relative potency of extracts on rat intestinal α-glucosidase activity in vitro as well as hypoglycemic effects in vivo. Green, oolong, and black tea bags were extracted in hot water and the remaining tea pomace were dried and further extracted in 70% ethanol. The extracts were determined for intestinal rat α-glucosidases activity, radical scavenging activity, and total phenolic content. The postprandial glucose-lowering effects of TWE and TPE of green and black tea were assessed in male Sprague-Dawley (SD rats and compared to acarbose, a known pharmacological α-glucosidase inhibitor. The IC50 values of all three tea extracts against mammalian α-glucosidase were lower or similar in TPE groups than those of TWE groups. TWE and TPE of green tea exhibited the highest inhibitory effects against α-glucosidase activity with the IC50 of 2.04 ± 0.31 and 1.95 ± 0.37 mg/mL respectively. Among the specific enzymes tested, the IC50 values for TWE (0.16 ± 0.01 mg/mL and TPE (0.13 ± 0.01 mg/mL of green tea against sucrase activity were the lowest compared to those on maltase and glucoamylase activities. In the animal study, the blood glucose level at 30 min after oral intake (0.5 g/kg body wt of TPE and TWE of both green and black tea was significantly reduced compared to the control in sucrose-loaded SD

  17. Radicamine B体外抑制小肠葡萄糖的吸收作用%Radicamine B Inhibits Glucose Absorption in Rat Intestines in vitro

    Institute of Scientific and Technical Information of China (English)

    孟爱国; 刘春艳; 马红翠

    2011-01-01

    目的:探讨radicamine B对大鼠体外小肠葡萄糖吸收的影响.方法:采用α-葡萄糖苷酶抑制实验及酶抑制动力学实验和离体大鼠小肠葡萄糖吸收模型来研究radicamine B的抑制作用.结果:radicamine B对α-葡萄糖昔酶和大鼠体外小肠葡萄糖的吸收均呈剂量依赖性抑制作用,其IC(50)分别为2.19,0.094 g·L(-1),与拜糖平相比较无显著性差异.而且radicamine B对α-葡萄糖苷酶活性属于竞争性抑制,Ki=6.3×10(-7)mol·L(-1).结论:radicamine B能显著抑制小肠葡萄糖的吸收,有望成为一种治疗糖尿病的药物.%Objective: To investigate the inhibitory effect of radicamine B on glucose absorption in rat intestines in vitro. Method: The inhibitory effect of radicamine B was evaluated by α-glucosidase inhibitory test, inhibitory kinetics assay and assay of glucose absorption in rat intestines in vitro. Result: Radicamine B showed an inhibitory effect on both α-glucosidase and glucose' s absorption in the small intestine in a dose-dependent manner and the IC50 value were 2. 19 g· L-1 and 0. 094 g·L-1, respectively. No significant difference was found between acarbose and radicamine B in the inhibitory effect on intestinal glucose absorption. In addition, the inhibitory pattern of radicamine B was competitive enzyme inhibition with its Ki of 6.3 × 10-7 mol · L-1. Conclusion: Radicamine B significantly inhibites glucose absorption in the small intestine. It indecates that radicamine B might be a novel therapeutic drug for diabetes.

  18. Potent α-amylase inhibitory activity of Indian Ayurvedic medicinal plants

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    Bhargava Shobha Y

    2011-01-01

    Full Text Available Abstract Background Indian medicinal plants used in the Ayurvedic traditional system to treat diabetes are a valuable source of novel anti-diabetic agents. Pancreatic α-amylase inhibitors offer an effective strategy to lower the levels of post-prandial hyperglycemia via control of starch breakdown. In this study, seventeen Indian medicinal plants with known hypoglycemic properties were subjected to sequential solvent extraction and tested for α-amylase inhibition, in order to assess and evaluate their inhibitory potential on PPA (porcine pancreatic α-amylase. Preliminary phytochemical analysis of the lead extracts was performed in order to determine the probable constituents. Methods Analysis of the 126 extracts, obtained from 17 plants (Aloe vera (L. Burm.f., Adansonia digitata L., Allium sativum L., Casia fistula L., Catharanthus roseus (L. G. Don., Cinnamomum verum Persl., Coccinia grandis (L. Voigt., Linum usitatisumum L., Mangifera indica L., Morus alba L., Nerium oleander L., Ocimum tenuiflorum L., Piper nigrum L., Terminalia chebula Retz., Tinospora cordifolia (Willd. Miers., Trigonella foenum-graceum L., Zingiber officinale Rosc. for PPA inhibition was initially performed qualitatively by starch-iodine colour assay. The lead extracts were further quantified with respect to PPA inhibition using the chromogenic DNSA (3, 5-dinitrosalicylic acid method. Phytochemical constituents of the extracts exhibiting≥ 50% inhibition were analysed qualitatively as well as by GC-MS (Gas chromatography-Mass spectrometry. Results Of the 126 extracts obtained from 17 plants, 17 extracts exhibited PPA inhibitory potential to varying degrees (10%-60.5% while 4 extracts showed low inhibition ( 50% was obtained with 3 isopropanol extracts. All these 3 extracts exhibited concentration dependent inhibition with IC50 values, viz., seeds of Linum usitatisumum (540 μgml-1, leaves of Morus alba (1440 μgml-1 and Ocimum tenuiflorum (8.9 μgml-1. Acarbose as the

  19. Antimicrobial and selected in vitro enzyme inhibitory effects of leaf extracts, flavonols and indole alkaloids isolated from Croton menyharthii.

    Science.gov (United States)

    Aderogba, Mutalib A; Ndhlala, Ashwell R; Rengasamy, Kannan R R; Van Staden, Johannes

    2013-01-01

    Croton species are used in folk medicine in the management of infections, inflammation and oxidative stress-related diseases. In order to isolate, characterize and evaluate the bioactive constituents of Croton menyharthii Pax leaf extracts, repeated column fractionation of the ethyl acetate fraction from a 20% aqueous methanol crude extract afforded three flavonols identified by NMR (1D and 2D) spectroscopic methods as myricetrin-3-O-rhamnoside (myricetrin, 1), quercetin-3-O-rhamnoside (2) and quercetin (3) along with an indole alkaloid, (E)-N-(4-hydroxycinnamoyl)-5-hydroxytryptamine, [trans-N-(p-coumaroyl) serotonin, 4]. All the compounds are reported from the leaf extract of this plant for the first time. The crude extracts, four solvent fractions (hexane, DCM, ethyl acetate and butanol) and isolated compounds obtained from the leaves were evaluated for their inhibitory effects on selected bacteria, a fungus (Candida albicans), cyclooxygenase (COX-2), α-glucosidase and acetylcholinesterase (AChE). Amongst the compounds, quercetin (3) was the most active against Bacillus subtilis and Candida albicans while myricetrin-3-O-rhamnoside (1) and trans-N-(p-coumaroyl) serotonin (4) were the most active compounds against Escherichia coli, Klebsiella pneumonia and Staphylococcus aureus. The inhibitory activity of myricetrin-3-O-rhamnoside (1) against COX-2 was insignificant while that of the other three compounds 2-4 was low. The AChE inhibitory activity of the alkaloid, trans-N-(p-coumaroyl) serotonin was high, with a percentage inhibitory activity of 72.6% and an IC50 value of 15.0 µg/mL. The rest of the compounds only had moderate activity. Croton menyharthii leaf extracts and isolated compounds inhibit α-glucosidase at very low IC50 values compared to the synthetic drug acarbose. Structure activity relationship of the isolated flavonols 1-3 is briefly outlined. Compounds 1-4 and the leaf extracts exhibited a broad spectrum of activities. This validates the

  20. Antimicrobial and Selected In Vitro Enzyme Inhibitory Effects of Leaf Extracts, Flavonols and Indole Alkaloids Isolated from Croton menyharthii

    Directory of Open Access Journals (Sweden)

    Johannes Van Staden

    2013-10-01

    Full Text Available Croton species are used in folk medicine in the management of infections, inflammation and oxidative stress-related diseases. In order to isolate, characterize and evaluate the bioactive constituents of Croton menyharthii Pax leaf extracts, repeated column fractionation of the ethyl acetate fraction from a 20% aqueous methanol crude extract afforded three flavonols identified by NMR (1D and 2D spectroscopic methods as myricetrin-3-O-rhamnoside (myricetrin, 1, quercetin-3-O-rhamnoside (2 and quercetin (3 along with an indole alkaloid, (E-N-(4-hydroxycinnamoyl-5-hydroxytryptamine, [trans-N-(p-coumaroyl serotonin, 4]. All the compounds are reported from the leaf extract of this plant for the first time. The crude extracts, four solvent fractions (hexane, DCM, ethyl acetate and butanol and isolated compounds obtained from the leaves were evaluated for their inhibitory effects on selected bacteria, a fungus (Candida albicans, cyclooxygenase (COX-2, α-glucosidase and acetylcholinesterase (AChE. Amongst the compounds, quercetin (3 was the most active against Bacillus subtilis and Candida albicans while myricetrin-3-O-rhamnoside (1 and trans-N-(p-coumaroyl serotonin (4 were the most active compounds against Escherichia coli, Klebsiella pneumonia and Staphylococcus aureus. The inhibitory activity of myricetrin-3-O-rhamnoside (1 against COX-2 was insignificant while that of the other three compounds 2–4 was low. The AChE inhibitory activity of the alkaloid, trans-N-(p-coumaroyl serotonin was high, with a percentage inhibitory activity of 72.6% and an IC50 value of 15.0 µg/mL. The rest of the compounds only had moderate activity. Croton menyharthii leaf extracts and isolated compounds inhibit α-glucosidase at very low IC50 values compared to the synthetic drug acarbose. Structure activity relationship of the isolated flavonols 1–3 is briefly outlined. Compounds 1–4 and the leaf extracts exhibited a broad spectrum of activities. This validates the

  1. Antimicrobial and selected in vitro enzyme inhibitory effects of leaf extracts, flavonols and indole alkaloids isolated from Croton menyharthii.

    Science.gov (United States)

    Aderogba, Mutalib A; Ndhlala, Ashwell R; Rengasamy, Kannan R R; Van Staden, Johannes

    2013-01-01

    Croton species are used in folk medicine in the management of infections, inflammation and oxidative stress-related diseases. In order to isolate, characterize and evaluate the bioactive constituents of Croton menyharthii Pax leaf extracts, repeated column fractionation of the ethyl acetate fraction from a 20% aqueous methanol crude extract afforded three flavonols identified by NMR (1D and 2D) spectroscopic methods as myricetrin-3-O-rhamnoside (myricetrin, 1), quercetin-3-O-rhamnoside (2) and quercetin (3) along with an indole alkaloid, (E)-N-(4-hydroxycinnamoyl)-5-hydroxytryptamine, [trans-N-(p-coumaroyl) serotonin, 4]. All the compounds are reported from the leaf extract of this plant for the first time. The crude extracts, four solvent fractions (hexane, DCM, ethyl acetate and butanol) and isolated compounds obtained from the leaves were evaluated for their inhibitory effects on selected bacteria, a fungus (Candida albicans), cyclooxygenase (COX-2), α-glucosidase and acetylcholinesterase (AChE). Amongst the compounds, quercetin (3) was the most active against Bacillus subtilis and Candida albicans while myricetrin-3-O-rhamnoside (1) and trans-N-(p-coumaroyl) serotonin (4) were the most active compounds against Escherichia coli, Klebsiella pneumonia and Staphylococcus aureus. The inhibitory activity of myricetrin-3-O-rhamnoside (1) against COX-2 was insignificant while that of the other three compounds 2-4 was low. The AChE inhibitory activity of the alkaloid, trans-N-(p-coumaroyl) serotonin was high, with a percentage inhibitory activity of 72.6% and an IC50 value of 15.0 µg/mL. The rest of the compounds only had moderate activity. Croton menyharthii leaf extracts and isolated compounds inhibit α-glucosidase at very low IC50 values compared to the synthetic drug acarbose. Structure activity relationship of the isolated flavonols 1-3 is briefly outlined. Compounds 1-4 and the leaf extracts exhibited a broad spectrum of activities. This validates the

  2. 茜草抑制α-葡萄糖苷酶活性成分研究%α-Glucosidase inhibitors from Rubia cordifolia

    Institute of Scientific and Technical Information of China (English)

    康文艺; 张丽; 宋艳丽

    2009-01-01

    目的:寻找茜草中抑制α-葡萄糖苷酶活性的成分.方法:利用体外抑制α-葡萄糖苷酶活性模型进行追踪,采用各种色谱法分离,运用多种谱学技术鉴定结构,并对活性化合物进行酶抑制动力学研究.结果:茜草三氯甲烷提取物具有很高的活性,从中分离出3个具抑制α-葡萄糖苷酶活性的蒽醌类化合物,分别鉴定为:1,3-二羟基-2-甲基蒽醌(1),1-羟基-2一甲基葸醌(2)和1,2-二羟基蒽醌(3),其中化合物3(IC_(50)=7.97 mg·L~(-1))活性最好,与1(IC_(50)=35.96 mg·L~(-1))和2(IC_(50)=15.98 mg·L~(-1))的活性都明显高于阳性对照阿卡波糖(IC_(50)=1 081.27 mg·L~(-1)).化合物1和2为竞争性抑制类型.结论:化合物1-3为首次报道对α-葡萄糖苷酶抑制活性.%Objective: To search α-glucosidase inhibitors from Rubia cordifolia. Methed: The α-glucosidase inhibitors were isolated by the column chromatographic techniques and the bioassay-guided method in vitro. A combination of MS and NMR spectrosco-py was used to identify the chemical structures. The inhibitory kinetics of the inhibitors were also investigated. Result: The chloroform extract showed high inhibitory activity,and three active compounds were isolated and identified as 1,3-dihydroxy-2-methylanthraquinone (1), 1-hydroxy-2-methylanthraquinone (2) and 1,2-dihydroxyanthraquinone (3). The IC_(50) values of compound 1-3 were all lower than that of acarbose. Compound 1 and 2 shown competitive type manner on α-glucosidase, whereas compound 3 shown noncompetitive type model. Conclusion: Compounds 1-3 as strong inhibitors of α-glucosidase were reported for the first time.

  3. 滇丁香中抑制α-葡萄糖苷酶活性成分研究%α-Glucosidase inhibitors' from Luculia pinciana

    Institute of Scientific and Technical Information of China (English)

    康文艺; 张丽; 宋艳丽

    2009-01-01

    Objective: To search α-glucosidase inhibitors from Luculia pinciana. Method: The α-glucosidase inhibitor was isolated by the column chromatographic techniques and the bioassay-guided method in vitro. A combination of MS and NMR spectroscopy was used to identify the chemical structures. The inhibitory kinetic of the isolations was also investigated. Result: The ethyl acetate extract showed strongest inhibitory activity, and five active compounds were isolated and identified as scopletin (1), 5-methoxy-8-hydroxycoumarin (2), 1α,3β,24-trihydroxyursolic acid (3), ursolic acid (4) and oleanolic acid (5). The IC_(50) values of all compounds were lower than that of acarbose. Four of them shown noncompetitive type manner on a-glucosidase inhibition except that compound 3 is competitive type manner. Conclusion: Compounds 1-4 as the inhibitors of a-glucosidase were reported for the first time.%目的:寻找滇丁香中具有抑制α-葡萄糖苷酶活性的成分.方法:利用体外抑制α-葡萄糖苷酶活性模型进行追踪,采用各种色谱法分离,运用多种谱学技术鉴定结构,并对活性较强的几个单体化合物进行酶抑制动力学研究.结果:滇丁香的醋酸乙酯部分具有较高的活性,从中分离出5个抑制α-葡萄糖苷酶活性的化合物,分别鉴定为:莨菪内酯(1),5-甲氧基-8-羟基香豆素(2),1α,3β,24-三羟基熊果酸(3),熊果酸(4)和齐墩果酸(5),其中化合物4(IC_(50) 3-3 mg·L~(-1)),5(IC_(50)2.88 mg·L~(-1))的活性最好,明显高于阳性对照阿卡波糖(IC_(50) 1081.27 mg·L~(-1)).化合物3为竞争性抑制.结论:化合物1~4为首次报道对α-葡萄糖苷酶有抑制活性.

  4. Effects of Onion (Allium cepa L. Extract Administration on Intestinal α-Glucosidases Activities and Spikes in Postprandial Blood Glucose Levels in SD Rats Model

    Directory of Open Access Journals (Sweden)

    Sun-Ho Kim

    2011-06-01

    Full Text Available Diets high in calories and sweetened foods with disaccharides frequently lead to exaggerated postprandial spikes in blood glucose. This state induces immediate oxidant stress and free radicals which trigger oxidative stress-linked diabetic complications. One of the therapeutic approaches for decreasing postprandial hyperglycemia is to retard absorption of glucose by the inhibition of carbohydrate hydrolyzing enzymes,α-amylase and α-glucosidases, in the digestive organs. Therefore, the inhibitory activity of Korean onion (Allium cepa L. extract against rat intestinal α-glucosidases, such as sucrase, maltase, and porcine pancreatic α-amylase were investigated in vitro and in vivo. The content of quercetin in ethyl alcohol extract of onion skin (EOS was 6.04 g/100 g dried weight of onion skin. The in vitro half-maximal inhibitory concentrations (IC50 of EOS and quercetin, a major phenolic in onion, on rat intestinal sucrase were 0.40 and 0.11 mg/mL, respectively. The postprandial blood glucose lowering effects of EOS and quercetin were compared to a known type 2 diabetes drug (Acarbose, a strong α-glucosidase inhibitor in the Sprague-Dawley (SD rat model. In rats fed on sucrose, EOS significantly reduced the blood glucose spike after sucrose loading. The area under the blood glucose-time curve (AUClast in EOS-treated SD rats (0.5 g-EOS/kg was significantly lower than in untreated SD rats (259.6 ± 5.1 vs. 283.1 ± 19.2 h·mg/dL. The AUClast in quercetin-treated SD rats (0.5 g-quercetin/kg was similar to in EOS-treated group (256.1 ± 3.2 vs. 259.6 ± 5.1 h·mg/dL. Results from this study indicates that although quercetin does have blood glucose lowering potential via α-glucosidase inhibition, there are other bioactive compounds present in onion skin. Furthermore, the effects of two weeks administration of EOS in a high carbohydrate-dietary mixture (Pico 5053 on sucrase and maltase activities in intestine were evaluated in SD rat model

  5. Ultrasonic extraction of polysaccharides from Laminaria japonica and their antioxidative and glycosidase inhibitory activities

    Science.gov (United States)

    Wan, Peng; Yang, Xiaoman; Cai, Bingna; Chen, Hua; Sun, Huili; Chen, Deke; Pan, Jianyu

    2015-08-01

    In the present study, ultrasonic extraction technique (UET) is used to improve the yield of polysaccharides from Laminaria japonica (LJPs). And their antioxidative as well as glycosidase inhibitory activities are investigated. Box-Behnken design (BBD) combined with response surface methodology (RSM) is applied to optimize ultrasonic extraction for polysaccharides. The optimized conditions are obtained as extraction time at 54 min, ultrasonic power at 1050 W, extraction temperature at 80°C and ratio of material to solvent at 1:50 (g mL-1). Under these optimal ultrasonic extraction conditions, an actual experimental yield (5.75% ± 0.3%) is close to the predicted result (5.67%) with no significant difference ( P > 0.05). Vitro antioxidative and glycosidase inhibitory activities tests indicate that the crude polysaccharides (LJP) and two major ethanol precipitated fractions (LJP1 and LJP2) are in a concentration-dependent manner. LJP2 (30%-60% ethanol precipitated polysaccharides) possesses the strongest α-glucosidase inhibitory activity and moderate scavenging activity against hydroxyl radicals (66.09% ± 2.19%, 3.0 mg mL-1). Also, the inhibitory activity against α-glucosidase (59.08% ± 3.79%, 5.0 mg mL-1) is close to that of acarbose (63.99% ± 3.27%, 5.0 mg mL-1). LJP1 (30% ethanol precipitated polysaccharides) exhibits the strongest scavenging activity against hydroxyl radicals (99.80% ± 0.00%, 3.0 mg mL-1) and moderate α-glucosidase inhibitory activity (47.76% ± 1.92%, 5.0 mg mL-1). LJP shows the most remarkable DPPH scavenging activity (66.20% ± 0.11%, 5.0 mg mL-1) but weakest α-glucosidase inhibitory activity (37.77% ± 1.30%, 5.0 mg mL-1). However, all these LJPs exert weak inhibitory effects against α-amylase. These results show that UET is an effective method for extracting bioactive polysaccharides from seaweed materials. LJP1 and LJP2 can be developed as a potential ingredient in hypoglycemic agents or functional food for the management of

  6. 新诊断2型糖尿病患者采取沙格列汀联合二甲双胍治疗的疗效及安全性分析%EFFICACY AND SAFETY OF SHAH GLENN DEAN COMBINED WITH METFORMIN IN THE TREAT- MENT OF THE PATIENTS WITH NEWLY DIAGNOSED TYPE 2 DIABETES

    Institute of Scientific and Technical Information of China (English)

    钱冬

    2015-01-01

    's hos‐pital from February 2012 to January 2014 in type 2 diabetic patients ,using random number table method for grouping ,they were divided into study group and control group ,47 cases in each group .The control group received acarbose and metformin treatment ,the research group were treated by Shah Glenn Dean combined with metformin treatment .Fasting blood glucose (FBG) ,2h postprandial blood glucose (2hPG) , glycosylated hemoglobin (HbA1c) ,fasting insulin ,insulin resistance index (HOMA - IR) ,body weight and body mass index of two groups were recorded before and after treatment ,and medication compliance and adverse reaction rate were compared between the two groups .Results Before treatment ,FBG ,2hPG and HbA1 c values had no significant difference (P>0 .05) between the two groups ,and the fasting insulin level and HOMA -IR value also had no significant difference (P> 0 .05) .After treatment ,FBG ,2hPG and HbA1c in study group were lower than that in the control group ,but the fasting insulin levels were higher and the HOMA -IR value was lower ,the difference was statistically significant (P0 .05);HbA1 c stand‐ard rate was higher in the research group than that in the control group ,the difference was statistically sig‐nificant (P0 .05) .The medication mistakes and wrong of research group wear rate were lower than the control group ,the difference was statistically significant (P< 0 .05) .Conclusion Clinical curative effect of metformin and Shah Glenn Dean therapy in patients with type 2 diabetes is better than metformin and acarbose schemes ,and the security is good ,worthy of further promotion in clinic .

  7. Reduction of podocytes number in late diabetic alloxan nephropathy: prevention by glycemic control Redução do número de podócitos na fase tardia da nefropatia diabética aloxânica: prevenção pelo controle glicêmico

    Directory of Open Access Journals (Sweden)

    Célia Sperandéo Macedo

    2007-10-01

    Full Text Available PURPOSE: To determine podocyte number and GBM thickness in diabetic rats either under glycemic control or without glycemic control at 6 and 12 months after diabetes induction. METHODS: 100 wistar rats weighing 200-300g were divided into 6 groups: Normal group (N6 and N12- 25 rats; Diabetic group (D6 and D12- 25 rats, diabetic treated group ( DT 6 and DT 12- 25 rats on insulin 1,8- 3,0 IU/Kg associated with acarbose (50mg to 100g of food daily mixed in chow. Alloxan was injected intravenously in a dose of 42 mg/Kg of weight. Body weight, waterintake, 24-h diuresis, glycemia and glucosuria were determined before induction, 7 and 14 days after induction and monthly thereafter. Treatment started at day 14. Three groups were sacrificed at 6 months (N6,D6, DT6 and 3 groups at 12 months (N12, D12, DT12 with the renal tissue being prepared for electron microscopy. RESULTS: Glycemia in DT6¨and in DT12 was significantly different from that in D6 and D12 rats and similar to that in N6 and N12 animals. The number of podocytes in DT6 was not different from that in N6 and D6 (median = 11; the number of podocytes in DT12 (median = 11 differed from that in D12 (median = 8, but not from that in N12 (median = 11. GBM thickness in D6 (0.18 micrometers was lower than in D12 (0.29 micrometers; while in DT6 (0.16 micrometers it was lower than in D6 (0.18 micrometers. In DT12 (0.26 micrometers, it was lower than in D12 (0.29 micrometers. CONCLUSION: The control of hyperglycemia prevented GBM thickening in early and late (12 mo alloxan diabetic nephropathy and podocyte number reduction.OBJETIVO: Avaliar o número de podócitos e espessamento da membrana basal glomerular (MBG em ratos diabéticos com e sem controle glicêmico com 6 e 12 meses da indução. MÉTODOS: 100 ratos Wistar com 200-300g compuseram 6 grupos: Normal (N6, N12 - 25 animais Diabético (D6,D12 - 25 animais e diabético tratado com insulina 1,8 a 3,0 U/Kg e acarbose misturada a ração (50g para cada

  8. Study on α-glucosidase inhibitory activity of extracts from six varieties of Cucurbita moschata Duch.%6种栽培品种南瓜提取物的α-葡萄糖苷酶抑制活性的研究

    Institute of Scientific and Technical Information of China (English)

    李昌勤; 卢引; 顾雪竹; 顾海鹏; 康文艺

    2012-01-01

    Objective: To study the α-glucosidase inhibitory activity of extracts from six varieties of Cucurbita moschata Duch. (Jingou, Tianmian, Riben, Chaotianmiben, Miben and Liaoningxinminjingou ) . Methods. By established α-glucosidase inhibitory model in vitro,the activity of extracts from C.moschata was screened.The relationship of inhibitory ratio and the extract concentration were also studied. Results: Different extracts from six varieties of C.moschata all had inhibitory activity of a-glucosidase, among which petroleum ether extract of C.moschata(Jingou) had the highest inhibitor activity of α-glucosidase (IC50 = 143.91μg/mL), which was lower than that of Acarbose( IC50 = 1103.0μg/mL).Among different extracts inhibitor activity of petroleum ether extract was higher than that of ethyl acetate extract and methanol extract.Conclusion:The extracts from six varieties of C. moschata all had inhibitory activity of α-glucosidase, but different varieties of the inhibition rate had certain difference.%目的:对6种不同栽培品种南瓜(金钩、甜面、日本、辽宁新民金钩、超甜蜜本、蜜本)提取物α-葡萄糖苷酶抑制活性进行研究。方法:通过建立体外α-葡萄糖苷酶抑制模型,对南瓜提取物进行活性筛选,并对提取物浓度与抑制活性关系进行研究。结果:6种栽培品种南瓜不同溶剂提取物均有一定的α-葡萄糖苷酶抑制活性,其中,金钩南瓜石油醚提取物的抑制活性最好(IC50=143.91μg/mL),活性远大于阳性对照阿卡波糖(IC50=1103.01μg/mL)。不同溶剂提取物显示石油醚提取物抑制活性均高于乙酸乙酯提取物和甲醇提取物。结论:6种栽培品种南瓜提取物均有一定的α-葡萄糖苷酶抑制活性,但不同品种其抑制活性具有一定的差别。

  9. 我院2006-2010年抗糖尿病药物应用分析%Utilization analysis of anti-diabetic drugs in our hospital during 2006-2010

    Institute of Scientific and Technical Information of China (English)

    刘朋; 纪立伟; 梁晓丽

    2013-01-01

      目的:分析北京医院抗糖尿病药的应用情况,为临床合理用药提供参考。方法:对卫生部北京医院2006–2010年抗糖尿病药物的种类、用量、销售金额、用药频度、日均费用等进行分析。结果:我院口服抗糖尿病药的销售金额占抗糖尿病药总金额的70%,其中,以α-葡萄糖苷酶抑制剂所占比例最高,胰岛素类约占30%;阿卡波糖、二甲双胍、诺和灵30R的DDDs较高,临床较为常用;二甲双胍、格列美脲、格列喹酮的DDC较低;噻唑烷二酮类药物的销售金额和DDDs逐年下降,其他药品的销售金额和DDDs均呈上升趋势,DDC逐年下降。瑞格列奈、那格列奈、甘精胰岛素的排序比值较低。结论:我院2006–2010年抗糖尿病药物的使用品种相对稳定,基本满足临床安全、经济、有效用药的需求。%Objective:To analyze the application situation of antidiabetic drugs in our hospital to provide reference for clinical rational drug use. Methods:The variety, amount, consumption sum, DDDs and average daily cost of antidiabetic drugs used in our hospital during 2006–2010 were analyzed retrospectively. Results:Sales amount of oral antidiabetic drugs accounted for 70%of the total amount of antidiabetic drugs. The sales amount ofα-glucosidase inhibitor was the largest and the sales amount of insulin accounted for about 30%of the total amount of antidiabetic drugs. The values of DDDs of acarbose, metformin and Novolin 30R were higher than that of other antidiabetic drugs due to more common use in clinic. The values of DDC of metformin, glimepiride, gliquidone were lower. Exception for the decrease in the sales amount and DDDs of thiazolidinediones, the sales amount and DDDs of other antidiabetic drugs showed an upward trend. The ratios of consumption sum sequence to DDDs sequence of repaglinide, nateglinide and the insulin glargine were smaller. Conclusion:The oral antidiabetic drugs used in our

  10. Pharmacotherapy for hepatic encephalopathy.

    Science.gov (United States)

    Phongsamran, Paula V; Kim, Jiwon W; Cupo Abbott, Jennifer; Rosenblatt, Angela

    2010-06-18

    associated with neurotoxicity in patients with cirrhosis, including dose-dependent peripheral neuropathy. Vancomycin may be a safer option for HE in patients with chronic liver disease; however, limited experience, possible bacterial overgrowth and risk for enteric bacteria resistance preclude the routine use of vancomycin for HE. Rifaximin is a novel antimicrobial agent with a wide spectrum of activity that has shown promise as an alternative antimicrobial treatment option for HE. Several clinical trials have compared rifaximin to the disaccharides, lactulose and lactitol, and the antimicrobial neomycin. Rifaximin appears to be at least as effective as conventional drug therapy and has been associated with fewer adverse effects due to its limited systemic absorption. The available clinical data appear to support a favourable benefit-risk ratio for rifaximin, which has shown efficacy with an improved tolerability profile. Future studies are needed in order to truly characterize its cost effectiveness in today's healthcare environment. Other less frequently utilized alternative treatment options include administration of benzodiazepine receptor antagonists, branched-chain amino acids, ornithine aspartate, zinc supplementation, sodium benzoate, dopamine receptor agonists, acarbose and probiotics. Presently, there is relatively limited clinical data supporting their routine use in HE. PMID:20518580

  11. "The metabolic syndrome... is dead": These reports are an exaggeration

    Directory of Open Access Journals (Sweden)

    Tenenbaum Alexander

    2011-01-01

    identifies additional important residual vascular risk mainly associated with insulin resistance and atherogenic dyslipidemia (low high density lipoprotein-cholesterol (HDL-C, high triglycerides, small, dense LDL-C. Therefore, the metabolic syndrome could be a useful additional contributor in estimation of global cardiovascular risk beyond age, high LDL-C or other standard risk factors. The components of the metabolic syndrome have partially overlapping mechanisms of pathogenic actions mediated through common metabolic pathways. Therefore their total combined effect could be less than the summed of the individual effects. The concept that the metabolic syndrome is a consequence of obesity and insulin resistance, provides a useful "life-style changes" approach for prevention and treatment: caloric restriction, weight-loss and increased physical activity. The next step could theoretically be pharmacological interventions such as metformin, acarbose, fibrates, weight-loss drugs (currently only orlistat is practically available and perhaps glucagon-like peptide-1 agonists. A third step should probably be kept for bariatric surgery.

  12. Study on Vitro Bioactivity of Guava Leaves Flavonoids%番石榴叶总黄酮提取物的体外生物学活性研究

    Institute of Scientific and Technical Information of China (English)

    李丹如; 卢颖; 田冰洁; 吴晓英

    2015-01-01

    Compared the vitro bioactivity of guava leaves flavonoids crude extract by the optimal extraction conditions (sample A) and guava leaf flavonoids fine extract purified by AB-8 macroporous resin (sample B). Studied on antioxidation of samples by the DPPH radical scavenging , hydroxyl radical scavenging , reducing power andα-glucosidase inhibitory to comapre the vitro bioactivity between sample A and sample B. Flavonoids content of the sample A and sample B were 7.8%and 13.28%, with DPPH free radical scavenging rates of 87.61%and 97.22%, with hydroxyl radical scavenging rate of 62.32%and 80.45%and withα-glucosidase inhibitory rates of 99.17%and 99.81%,which are much larger than acarbose. And restoring force of sample B is much larger than the sample A. Sample A and sample B has a certain amount of antioxidant activity and α-glucosidase inhibitory effect, which may have a certain relationship with flavonoids, as a whole, sample B slightly higher than the sample.%比较经优化条件提取的番石榴叶总黄酮粗提物(样品A)和经AB-8大孔树脂纯化的番石榴叶总黄酮精提物(样品B)的体外生物学活性.通过清除DPPH自由基、羟自由基、还原力检测样品的抗氧化能力及研究对α-葡萄糖苷酶的抑制作用来比较样品A、B的体外生物学活性. 样品A和样品B的黄酮含量分别为7.8%、13.28%, 对DPPH自由基的清除率分别为87.61%、97.22%,对羟自由基的清除率分别为62.32%、80.45%,样品B的还原力远大于样品A;样品A和样品B对α-葡萄糖苷酶的抑制率分别为99.17%、99.81%,远大于阿卡波糖.样品A和样品B都有一定的抗氧化能力和对α-葡萄糖苷酶有一定的抑制作用,总体上样品B高于样品A,可能与其中的总黄酮含量有关.

  13. Application Analysis of Oral Hypoglycemic Drugs in 34 Hospitals of Nanjing during 2011-2013%南京地区34家医院2011~2013年常用口服降糖药用药分析

    Institute of Scientific and Technical Information of China (English)

    王璐璐; 刘慧

    2014-01-01

    Objective:To evaluate the utilization of oral hypoglycemic drugs in 34 hospitals of Nanjing to provide clinical reference for the drug rational use. Methods: According to the sales data of oral hypoglycemic drugs in 34 hospitals of Nanjing from 2011 to 2013,the utilization of oral hypoglycemic drugs was analyzed retrospectively in respect of consumption sum,DDDs and defined daily cost ( DDC) by daily dose limit analysis method. Results: The top 3 oral hypoglycemic drugs in the list of consumption sum were acarbose,glimepiride and metformin. In terms of DDDs,glimepiride, metformin and gliclazide ranked the top 3. The consumption sum and DDDs of oral hypoglycemic drugs were increased year by year in Nanjing. The ratio of serial number of consumption sum and DDDs was from 0. 3 to 2. 0. Conclusion: The demanded quantity of oral hypoglycemic drugs is increased year by year from 2011 to 2013. The application conforms to the safe, effective and economic principle. The drugs should be chosen according to the drug characteristics in order to improve the abnormal glucose metabolism and prevent and treat the complications.%目的::了解南京地区口服降糖药的应用近况和发展趋势,为临床合理使用口服降糖药提供参考。方法:根据长江流域医药情报研究所提供的南京地区2011~2013年口服降糖药的销售数据,采用限定日剂量分析法,对该地区34家医院近三年口服降糖药的销售金额、用药频度( DDDs)和限定日费用( DDC)等进行统计分析。结果:销售金额排名前三位的药物是阿卡波糖、格列美脲、二甲双胍,DDDs排名前三位的药物是格列美脲、二甲双胍、格列齐特,总销售金额和总DDDs均呈逐年增长趋势,销售金额与DDDs的序号比值在0.3~2.0之间。结论:2011~2013年南京地区口服降糖药需求量逐年增加,口服降糖药使用符合安全、有效、经济的用药原则,建议治疗时根据药物的特点进行选择,

  14. 1例胰岛素过敏老年2型糖尿病患者降糖药物的选择与药学监护%Pharmaceutical care for an insulin allergy elderly patient with type 2 diabetes

    Institute of Scientific and Technical Information of China (English)

    史天陆; 李明

    2012-01-01

    目的 通过参与胰岛素过敏伴心功能不全老年2型糖尿病患者降糖的药物治疗实践,探讨临床药师参与临床药物治疗和开展药学监护的方法 .方法 临床药师参与临床治疗团队,根据患者具体病情变化,提供合理性意见,与临床医师共同制定个体化治疗方案,并开展有效药学监护.结果 患者对多种胰岛素存在过敏现象,且无法耐受胰岛素脱敏治疗,综合考虑患者年龄、生理状况以及药物作用特点等因素,药师建议给予联合口服作用温和或半衰期短的胰岛素促分泌剂格列吡嗪控释片和α-糖苷酶抑制剂类阿卡波糖片进行降糖治疗,并在治疗过程中对药物剂量适时进行有效调整,治疗方案维持7 d后,患者血糖控制较平稳,出院回家.结论 临床药师深入临床直接面向患者提供药学服务,参与制定患者个体化治疗方案,开展药学监护,可避免延误患者的有效药物治疗,切实提高药物治疗水平和医疗质量.%Objective To seek the methods of providing individualized medications and pharmaceutical care for an insulin allergy elderly patient with type 2 diabetes when clinical pharmacists worked in clinical departments. Methods Clinical pharmacists participated in the drug therapy for an insulin allergy elderly patient with type 2 diabetes, provided reasonable opinions for individualized medications and offered special pharmaceutical cares for the main drugs. Results Because the insulin allergy elderly patient with type 2 diabetes couldn' t tolerate insulin desensitization therapy, clinical pharmacist suggested combination use of glipizide controlled-release tablets and acarbose tablets after comprehensive consideration of the patient age, physical condition as well as the characteristics of drugs and other factors, and adjusted drug dose timely during the course of treatment. The patient recovered and was discharged from hospital after blood sugar control treatment for 7

  15. 干血滤纸片和白细胞酸性α-葡萄糖苷酶活性测定平台的建立及临床应用%Establishment and clinical application of dried blood spots and mixed leukocytes for determination of acid α-glucosidase activity

    Institute of Scientific and Technical Information of China (English)

    邱文娟; 王霞; 王瑜; 叶军; 韩连书; 张惠文; 顾学范

    2010-01-01

    目的 建立干血滤纸片和门细胞酸性α-葡萄糖苷酶(GAA)活性测定方法 及正常参考值,用于糖原累积病Ⅱ型(GSD Ⅱ)患者的酶学诊断.方法 利用GAA特异性水解荧光底物4-MUG的原理,采用阿卡波糖抑制其同工酶,建立干血滤纸片(DBS)和白细胞测定GAA活性方法 .取700例DBS样本和100例白细胞样本作为正常对照建立DBS和白细胞测定GAA活性正常参考值,并对临床疑诊4例患者及其父母进行GAA活性测定.结果 DBS法具有良好的精密度,室温或低于室温保存至少4周时DBS GAA活性无明显影响.正常新生儿和儿童-成人DBS的GAA参考范围分别为8.92~60.03 pmol/(punch·h)和8.00~37.43 pmol/(punch·h);正常人白细胞GAA参考范围:12.56~50.26 nmol/(mg蛋白·h),共检出4例GSD Ⅱ型患者.结论 DBS法测定GAA活性具有敏感、快速、高通量等特点,适于GSD Ⅱ型高危人群筛查和诊断;白细胞法测定GAA活性也具有快速、特异性高等特点,适于患者的确诊.%Objective Glycogen storage disease type Ⅱ(GSD Ⅱ,Pompe disease)is caused by the deficiency of acid α-glucosidase(GAA)that leads to lysosomal glycogen accumulation.Early diagnosis and treatment of GSD Ⅱ are considered to be critical for maximum efficacy of the enzyme replacement therapy.The aim of this study was to introduce two reliable methods and to generate the reference range of GAA activitv.Method The assay of GAA activity was performed in dried blood spots(DBS)and mixed leukocytes with acarbose to eliminate isoenzyme interference and to generate the reference range.GAA activitv was assayed in 700 specimens for DBS from normal subjects and 100 specimens for mixed leukocytes from normal subjects to set up reference range.GAA activity in the samples of 4 patients who were clinically suspected of GSD Ⅱ and their parents were also assayed.Result The intra-run and inter-run precision of the DBS method wag less than 10%.GAA activity tested by DBS was

  16. Study on the Current Use Situation of National Essential Medicine and Its Related Factors of Priority Use Based on Our Hospital and Parts of the Country%基于我院和国内部分地区的国家基本药物使用现状及其优先使用相关因素研究Δ

    Institute of Scientific and Technical Information of China (English)

    赵程程; 闫素英

    2015-01-01

    OBJECTIVE:To understand the status of the use of national essential medicines,and provides reference for further implementing the national essential medicine system and promoting the priority use of national essential medicines. METHODS:Ac-cording to the statistics analysis of the use of national essential medicines(for example the antihypertensives and oral hypoglycemic agents)in Beijing,Shanghai and Guangzhou areas,the related influential factors about priority use of national essential medicines were explored. RESULTS:The proportions of use amount of national essential medicines in our hospital in 2012-2013 to the total amount of medicines were 21.20% and 18.75%,respectively,with a downtrend;the proportion of antihypertension drugs to total amount was only 14.05%and 13.70%,respectively;compared with the same generic drugs with individual pricing,the GMP prod-ucts of Valsartan capsule,Bisoprilol tablet and Amlodipine tablet had no advantages in DDDs,or even lower. DDDs of individual pricing drugs of Acarbose tablet in medical institutions in Beijing area and tertiary hospitals in Shanghai and Guangzhou area in 2011-2012 were much higher than the generic GMP products with the same generic drugs. CONCLUSIONS:The clinical use of na-tional essential medicines in our hospital and parts of the country still remains to be further improved,the influential factors includ-ed reimbursement mechanism,awareness rate of related knowledge,physicians’habit to drug use and pursuing economic benefits. The propaganda and training should be strengthened,awareness rate of medical staff and publics to national essential medicines, the availability of national essential medicines and national essential medicine system and medicare reimbursement payment policy should be improved,and the priority use of national essential medicines should be promoted by more measures combination use.%目的:了解国家基本药物的使用现状,为进一步贯彻落实国家基本药物制度、

  17. Study on the Optimum Proportion of Radix Astragalus with Flos Carthami on alpha - Glucosidase and Antioxidant Activities%黄芪与红花抑制α-葡萄糖苷酶及抗氧化活性的最佳配比研究

    Institute of Scientific and Technical Information of China (English)

    廖晖; 王孝敏

    2015-01-01

    oligomer to deter-mine the impacts of the samples to yeast alpha glycosidase enzyme activity,in which,acarbose was taken as the positive control. Oxygen radial absorbance capacity(ORAC)was adopted to determine the antioxidant ac-tivity of samples,in which,vitamin C was taken as the positive control. Results The astragaloside 0. 127 mg contained in each 1 ml radix astragalus extraction and the general flavone 0. 57 mg in each 1 ml flos carthami extraction. All of them met the content requirement of CFDA - relevant activity component. IC50 of the inhibi-tion of flos carthami for alpha - glucosidase activity was(32. 8 ± 5. 7)μg/ ml,significantly lower than that of radix astragalus[(1686 ± 810)μg/ ml,P < 0. 01]. IC50 was lower significantly at the ratios of radix astragalus and flos carthami as 10: 1,5: 1 and 2: 1 as compared with that at the ratio of 20: 1(P <0. 01)separately. ORAC value of flos carthami was(1090 ± 161)μmol TE/ g,higher significantly than that of radix astragalus[(205 ± 32)μmol TE/ g,P <0. 01]. When the ratios of the crude herbal materials were 5: 1 and 2: 1,ORAC value was higher significantly than that at 20: 1 and 10: 1 respectively(P <0. 01). Conclusion Both radix astragalus and flos carthami act on the inhibition of yeast alpha - glucosidase activity and has a certain of antioxidant activity. While improving the above indexes,the actions of the crude herbal materials are significant at the ratio of 5:1 and 2: 1 as compared with those at 20: 1(P < 0. 01).

  18. The effects of walking exercise on glycometabolism, dynamic blood pressure and the quality of life of patients with hypertension and type 2 diabetes%步行运动对高血压合并糖尿病患者糖代谢、动态血压及生活质量的影响

    Institute of Scientific and Technical Information of China (English)

    王正斌; 邱春光; 黄振文; 韩战营; 孙国举; 孙寒

    2014-01-01

    Objective To explore the effects of walking exercise on glycometabolism,dynamic blood pressure and the quality of life of patients with both hypertension and type 2 diabetes on the basis of conventional drug treatment.Methods Sixty-two patients with both hypertension and diabetes who could support taking walking exercise of more than 5,000 steps/d were randomly divided into a walking exercise group (32 cases) and a control group (30 cases).Both groups were given conventional drug treatment (including valsartan,acarbose and metformin).Those in the walking exercise group took more than 10,000 steps/d of aerobic exercise while the patients in the control group were just given normal community care.This continued for a period of 3 months.Fasting plasma glucose (FPG),glycated hemoglobin-A1C (HbA1c),fasting insulin (FINS),the homeostasis model of assessment for insulin resistence index (HOMA-IR),the homeostasis model of assessment for insulin sensitivity (HOMA-IS),dynamic blood pressure parameters and quality of life were observed.Results In the walking exercise group,the FPG,HbA1c,FINS,HOMA-IR,HOMA-IS,dynamic blood pressure and quality of life indicators were all significantly different after 3 months of daily walking exercise compared with either baseline or the control group.Conclusion Accompanied by conventional drug therapy,10,000 steps/d of walking exercise can improve the glucose metabolism,dynamic blood pressure and quality of life of patients suffering from mild hypertension and type 2 diabetes.%目的 观察在常规药物治疗基础上辅以步行运动对高血压合并2型糖尿病患者糖代谢、动态血压及生活质量的影响.方法 应用计步器筛选出62例在我科门诊或住院治疗且步行运动量<5000步/d的高血压合并2型糖尿病患者,采用随机数字表法将其分为运动组(32例)及对照组(30例).2组患者均给予常规药物(包括缬沙坦、二甲双胍、阿卡波糖)治疗,运动组患

  19. 甘精胰岛素联合阿卡波糖对2型糖尿病患者血糖达标率及胰岛β细胞功能的影响%The effect of insulin glargine combined with carbose on blood glucose attaining standardand pancreatic β cell function of type 2 diabetic patients

    Institute of Scientific and Technical Information of China (English)

    包灵敏; 刘存安

    2013-01-01

    Objective To explore the effect of insulin glargine combined with carbose onblood glucose attaining standard and pancreatic β cell function of type 2 diabetic patients.Methods 70 type 2 diabetic patients were divided into observation group and control group.All the patients got fundamental treatment as diet control and physical exercise.Patients of observing group got extra treatment as using insulin glargine combined with carbose,while patients of control group got extra treatment as using premixed insulin 30R(isophane protamine biosynthetic human insulin),all the treatment lasted for 8 weeks.Results 8 weeks after treatment,the rate of reaching standard of FBG and 2h postprandial plasma glucose and glycosylated hemoglobin (95.0%,85.0% and 77.5%) of observing group were significantly higher than those of control group (77.5%,62.5% and 55.0%) (x2 =5.16,5.23 and 4.53,all P <0.05).The levels of FCP and PCP increased significantly in both groups than that of before treatment (t =2.43,2.32,2.28,2.19,all P < 0.05),and the change of observation group was more obviously than that of control group (t =2.17,2.13,all P < 0.05).The occurrence rate of hypoglycemia of observation group was significantly lower than that of control group(x2 =4.11,P <0.05).Conclusion Treating diabetic patient by insulin glargine combined with acarbose has high safety,and helps to reach the standard of FBG and glycosylated hemoglobin,reduce the incurrence rate of hypoglycemia,protect and improve the function of pancreatic 3 cell,and postpone the beginning and progress of complication.%目的 探讨甘精胰岛素联合阿卡波糖对2型糖尿病患者血糖达标率及胰岛β细胞功能的影响.方法 选择2型糖尿病患者70例,按就诊病历号顺序随机分为观察组与对照组.两组患者均予以饮食控制和体育锻炼等基础治疗.观察组在此基础上予以甘精胰岛素联合阿卡波糖治疗,对照组在此基础上予以精蛋白生物合成人

  20. [A 50-year history of new drugs in Japan-the development and progress of anti-diabetic drugs and the epidemiological aspects of diabetes mellitus].

    Science.gov (United States)

    Ozawa, Hikaru; Murai, Yuriko; Ozawa, Terutaka

    2003-01-01

    recombinant products prevailed throughout the 1990s. Human insulin analogues (i.e., Insulin lispro and Insulin aspart) appeared in 2001. These are applied for after-meal glycosmia owing to their ultrarapid onset of activity. Self-injection by DM patients was legalized in 1981. To make the infection technique sure and easy, cartridge (pen-type) and disposable kit-type needles were devised in the 1990s. 2) Oral hypoglycemic drugs: Instead of the exclusive parenteral usage of insulins, there was also demand for oral dosage forms. The first of the sulfonyrlurea (SU) group, BZ-55, was used for DM clinically in 1955 in Germany. But it was soon withdrawn because of its antibacterial action. This led to the development of various SU groups. Tolbutamide (1956), chlorpropamide (1959), acetohexamide (1964) and tolazamide (1961) were introduced to Japan as first-generation SUs. Then glyclopyramide (Kyorin, 1965), glybenclamide (1971), gliclazide (1984) and glimepiride (1999) appeared as the second-generation SUs. These were used orally for Type 2 diabetes. Biguanide (BG) group, phenformin HC1 (1959), metformin HC1 (1961) and buformin HC1 (1961) had also been in use by oral treatment of Type 2 diabetes. SU appears to act by increasing the sensitivity of b-cells, which secrete insulin. BG probably exerts by increasing glucose transport across the membranes of target organs. 3) New types of antidiabetic drugs: a-Glucosidase inhibitors (i.e., acarbose: Bayer, 1993; and voglibose: Takeda, 1994) act on hyperglycemia after meals by decreasing glucose absorption. Thiazolidinedione compounds, such as troglitazone (Sankyo, 1995) and pioglitazone HC1 (Takeda, 1994) act by increasing the insulin sensitivity of the target tissues. These are useful for Type 2 DM patients when SUs are ineffective. Nevertheless, troglitazone was discontinued in 2000 due to severe liver damage. Nateglinide (Ajinomoto Co., 1999), which is a D-phenylalanine derivative acting similar to SUs, is useful orally for after

  1. Effect of Siraitiae Fructus Extracts from Different Growth Period Fruit on Postprandial Blood Glucose in Mice%不同生长期罗汉果提取物对小鼠餐后血糖生成的影响

    Institute of Scientific and Technical Information of China (English)

    夏星; 钟振国; 刘慧娟; 何伟平; 朱晓韵

    2012-01-01

    α-glucosidasc enzyme activity. Method; Kuenming mice were divided into starch load (6 g·kg-1 ) and glucose load (2 g o kg -1 ) group, each group consists of 9 subgroups: normal control, starch load or glucose load control, positive control (acarbose 0. 01 g ·kg-1 ) , 90 days Siraitiae Fructus extracts high, medium and low dose (1, 0. 5 , 0. 25 g o kg-1 ) , 60 days Siraitiae Fructus extracts high, medium and low dose ( 1 , 0.5, 0. 25 g o kg ~' ) . The postprandial blood glucose induced by starch and glucose were observed after 7 days Siraitiae Fructus extracts administration, and the postprandial insulin levels were determined via ELISA method. Moreover, the inhibition effect of Siraitiae Fructus extracts on α-glucosidase activity was determined in vitro. Result; All dosage of 90 days and 60 days Siraitiae Fructus extracts inhibited peak value of postprandial blood glucose; all dosage of 90 days Siraitiae Fructus extracts reduced glycemic index induced by starch ( P < 0. 05 ) , and the glycemic index induced by glucose was reduced at 0. 25 g ·kg-1 (P<0. 05) ; moreover, 0. 5 g·kg-1 of 60 days Siraitiae Fructus extracts significantly reduced glycemic index induced by starch ( P < 0. 01 ) , but all dose of 60 days Siraitiae Fructus extracts only demonstrated a trend to reduce the glycemic index induced by glucose. All dose of 90 days Siraitiae Fructus extracts significantly increased postprandial insulin ( P < 0. 001 ) , and 60 days Siraitiae Fructus extracts increased postprandial insulin dose dependently. The IC50 value of 90 and 60 days Siraitiae Fructus extracts was 11.51 g·L-1 and 2. 40 g ·L-1 , respectively. Conclusion; Mangosteen extract is effectual in the inhibition of the rapid increase of postprandial blood glucose, which are primarily mediated by increasing postprandial insulin levels andet-glucosidase inhibition, there is a difference in hypoglycemic mechanism between Siraitiae Fructus extracts from different growth period fruit.

  2. Community intervention in patients with abnormal glucose tolerance%糖耐量异常患者的社区干预

    Institute of Scientific and Technical Information of China (English)

    高发海

    2015-01-01

    目的:研究社区干预对糖耐量异常患者的重要意义.方法:2012年5月-2013年5月收治糖耐量异常患者112例,所有患者都口服葡萄糖耐量测试,将其随机分成干预组和对照组,各56名.社区卫生服务人员对对照组的所有患者叮嘱其半年进行 1 次血糖、尿糖检测,并作好记录.而干预组则除了定期做检测外,还指导发放糖尿病知识手册,邀其参加相关知识讲座,给予定量的阿卡波糖片口服,而且对其每日三餐饮食进行规定和指导,并要求其每天早上0.5 h和晚上0.5 h的运动锻炼.经过1年以后,比较两组患者的糖尿病发病率、并发症发生率、空腹和餐后2 h的血糖水平.结果:干预组和对照组糖尿病发病例数分别是8例和21例,发病率分别是14.2%和37.5%;两组并发症发生例数分别是4例和14例,发病率分别是7.14%和25.0%;空腹和餐后2 h血糖水平,干预组明显低于对照组,差异有统计学意义(P<0.05).结论:社区干预对于糖耐量异常患者意义重大,具有必要性和可行性.%Objective:To explore the significance of community intervention for patients with abnormality of sugar tolerance. Methods:112 patients with abnormal glucose tolerance were selected from May 2012 to May 2013.All patients were given oral glucose tolerance test.They were randomly divided into the intervention group and the control group with 56 cases in each.For all the patients in the control group,the community health service personnel told the blood glucose and urine glucose detection every half a year,and made record.In the intervention group,in addition to the regular inspection, patients were given diabetes knowledge handbook,patients were invited to participate in the relevant knowledge lectures,acarbose tablet oral was given quantitatively,and guided the three meals a day diet,patients were asked to exercise for half an hour in every morning and evening.1 year later,we compared the incidence of diabetes