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Sample records for acarbose

  1. Acarbose

    Science.gov (United States)

    ... helps keep blood glucose from rising very high after meals.Over time, people who have diabetes and high blood sugar can develop serious or life-threatening complications, including heart disease, stroke, kidney problems, nerve damage, and eye problems. Taking medication(s), making lifestyle changes ( ...

  2. 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/acarb...ose.Human.in_vitro.Liver.zip ftp://ftp.biosciencedbc.jp/archive/open-tggates/LATEST/Rat/in_vitro/acarb...ose.Rat.in_vitro.Liver.zip ftp://ftp.biosciencedbc.jp/archive/open-tggates/LATEST/Rat/in_vivo/Liver/Single/acarb...-tggates/LATEST/Rat/in_vivo/Liver/Repeat/acarbose.Rat.in_vivo.Liver.Repeat.zip ...

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

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    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.

  4. Acarbose Accelerates Wound Healing via Akt/eNOS Signaling in db/db Mice

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    Xue Han

    2017-01-01

    Full Text Available Refractory wound is a dreaded complication of diabetes and is highly correlated with EPC dysfunction caused by hyperglycemia. Acarbose is a widely used oral glucose-lowering drug exclusively for T2DM. Previous studies have suggested the beneficial effect of acarbose on improving endothelial dysfunction in patients with T2DM. However, no data have been reported on the beneficial efficacy of acarbose in wound healing impairment caused by diabetes. We herein investigated whether acarbose could improve wound healing in T2DM db/db mice and the possible mechanisms involved. Acarbose hastened wound healing and enhanced angiogenesis, accompanied by increased circulating EPC number in db/db mice. In vitro, a reversed BM-EPC dysfunction was observed after the administration of acarbose in db/db mice, as reflected by tube formation assay. In addition, a significantly increased NO production was also witnessed in BM-EPCs from acarbose treated db/db mice, with decreased O2 levels. Akt inhibitor could abolish the beneficial effect of acarbose on high glucose induced EPC dysfunction in vitro, accompanied by reduced eNOS activation. Acarbose displayed potential effect in promoting wound healing and improving angiogenesis in T2DM mice, which was possibly related to the Akt/eNOS signaling pathway.

  5. Low-dose acarbose does not delay digestion of starch but reduces its bioavailability

    NARCIS (Netherlands)

    Wachters-Hagedoorn, R. E.; Priebe, M. G.; Heimweg, J. A. J.; Heiner, A. M.; Elzinga, H.; Stellaard, F.; Vonk, R. J.

    2007-01-01

    Aims Slowly digestible starch is associated with beneficial health effects. The glucose-lowering drug acarbose has the potential to retard starch digestion since it inhibits alpha-amylase and alpha-glucosidases. We tested the hypothesis that a low dose of acarbose delays the rate of digestion of rap

  6. 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

  7. Safety and efficacy of high-dose acarbose treatment for dumping syndrome.

    Science.gov (United States)

    De Cunto, Angela; Barbi, Egidio; Minen, Federico; Ventura, Alessandro

    2011-07-01

    Dumping syndrome (DS) is a complication of Nissen fundoplication. Dietary strategies can ameliorate symptoms, but this approach is not always foolproof. Limited evidence reports the efficacy of acarbose for children who are unresponsive to feeding manipulations. We report 8 patients with DS aged between 7 and 24 months. In 4 of 8 nutritional strategies failed, and acarbose treatment was started. The initial dose was 25 mg for meals, and increased until postprandial glucose was stable. In 3 of 4 children the final dose was higher than previously reported, without adverse effects. Acarbose is useful to treat DS in cases of failure of dietary strategies.

  8. Acarbose Isolation with Gel Type Strong Acid Cation Exchange Resin:Equilibrium, Kinetic and Thermodynamic Studies

    Institute of Scientific and Technical Information of China (English)

    王亚军; 于蕾; 郑裕国; 王远山; 沈寅初

    2013-01-01

    Acarbose, a potentα-glucosidase inhibitor, is widely used as an oral anti-diabetic drug for the treatment of the type 2, non-insulin-dependent diabetes. In this work, a gel type strong acid cation exchange resin 001×4 was applied to isolate acarbose from fermentation broth. It was demonstrated that cation exchanger 001×4 displayed a large adsorption capacity and quick exchange rate for acarbose. The static adsorption equilibrium data were well fitted to the Langmuir equation. Column adsorption experiments demonstrated that high dynamic adsorption capacity was reached at bed height of 104.4 mm, feed flow rate of 1.0 ml·min-1 and acarbose concentration of 4.0 mg·ml-1. Under the optimized conditions, the column chromatography packed with cation exchanger 001×4 recovered 74.3%(by mass) of acarbose from Actinoplanes utahensis ZJB-08196 fermentation broth with purity of 80.1%(by mass), demonstrating great potential in the practical applications in acarbose separation.

  9. Effects of acarbose on starch hydrolysis. Study in healthy subjects, ileostomy patients, and in vitro.

    Science.gov (United States)

    Hiele, M; Ghoos, Y; Rutgeerts, P; Vantrappen, G

    1992-07-01

    The effect of acarbose on hydrolysis of a pure starch meal was investigated in normal subjects and ileostomy patients by means of 13CO2 breath tests and blood glucose levels as parameters of absorption, and of H2 breath tests, serum acetate levels, and ileal loss of carbohydrate as parameters of malabsorption. Additional information on the effect of acarbose on alpha-amylase activity was obtained by in vitro experiments. Acarbose (200 and 400 mg) significantly delayed starch absorption. Serum acetate was found to be a less sensitive marker of malabsorption than breath H2 excretion. After intake of 50 g starch plus 400 mg acarbose, 23-71% of the starch load was lost in the ileostomy effluent, for a large part as starch. This suggests that acarbose considerably inhibits alpha-amylase, and not only brush-border enzymes. In vitro experiments confirm that an inhibition of two thirds of alpha-amylase activity can be expected from pharmacologically used doses of acarbose.

  10. Effects of acarbose treatment on markers of insulin sensitivity and systemic inflammation.

    Science.gov (United States)

    Rudovich, Natalia N; Weickert, Martin O; Pivovarova, Olga; Bernigau, Wolfgang; Pfeiffer, Andreas F H

    2011-06-01

    This study assessed the effect of postprandial glucose reduction by acarbose on insulin sensitivity and biomarkers of systemic inflammation. This was a single-center, double-blind, randomized, placebo-controlled, crossover study <40 weeks in duration, involving 66 subjects with varying degrees of glucose tolerance. Eligible patients completed a 3-week run-in period and were randomized to receive either 100 mg of acarbose three times daily followed by placebo, or vice versa, lasting 12 weeks each with a 12-week washout between interventions. Liquid meal challenges and hyperinsulinemic-euglycemic glucose clamp were performed at weeks 0, 12, 24, and 36. Fasting proinsulin levels and proinsulin-to-adiponectin ratios but not fasting adiponectin levels were significantly lower during acarbose versus placebo treatment. Clamp-derived insulin sensitivity index and body weight were unchanged by the intervention. Levels of fasting insulin, fasting glucose, monocyte chemoattractant protein-1, interleukin-6, and interleukin-1β were comparable between treatments. In the liquid meal challenge tests, postprandial glucose and insulin responses were significantly lower during acarbose versus placebo treatment. The effects of acarbose on the reduction of fasting proinsulin was most pronounced in subjects with impaired fasting glucose/impaired glucose tolerance (n = 24). Reduction of the glycemic load by acarbose decreased fasting levels of proinsulin but had no effect on adiponectin and whole-body insulin sensitivity as well as biomarkers reflecting inflammation. The preventive effects of acarbose on type 2 diabetes mellitus and cardiovascular risk need further investigation and cannot be explained by changes of insulin resistance and inflammatory biomarkers.

  11. 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.

  12. Treatment with acarbose in severe hypoglycaemia due to late dumping syndrome.

    Science.gov (United States)

    Wang, Congcong; Pang, Shuguang; Jiang, Qiang; Duan, Guanglan; Sun, Yongmei; Li, Mei

    2013-12-01

    Dumping syndrome is a serious complication that may occur after gastric surgery in approximately 10% of patients in the 1990s. With the increasing number of patients undergoing bariatric surgery, the incidence of dumping syndrome is likely to increase in recent years. It is necessary for clinicians to recognize the syndrome and master its management. We present a case of recurrent loss of consciousness, which was finally accurately diagnosed as late dumping syndrome twelve years after subtotal gastrectomy and successfully treated with acarbose. A 66-year old lean male was found unconscious repeatedly within one year, oral glucose tolerance tests performed before and after acarbose treatment verified the diagnosis of late dumping syndrome. Hypoglycaemia can damage the body in acute and chronic form. Acarbose can be used as a successful treatment modality for reactive hypoglycaemia due to late dumping syndrome by influencing the release of hormone.

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

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    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. Dietary Flavonoids and Acarbose Synergistically Inhibit alpha-Glucosidase and Lower Postprandial Blood Glucose.

    Science.gov (United States)

    Zhang, Bowei; Li, Xia; Sun, Wenlong; Xing, Yan; Xiu, Zhilong; Zhuang, Chunlin; Dong, Yuesheng

    2017-09-06

    The inhibition of porcine pancreatic α-amylase and mammalian α-glucosidase by sixteen individual flavonoids was determined. The IC50 values for baicalein, (+)-catechin, quercetin, and luteolin were 74.1 ± 5.6, 175.1 ± 9.1, 281.2 ± 19.2, and 339.4 ± 16.3 μM, respectively, against α-glucosidase. The IC50 values for apigenin and baicalein were 146.8 ± 7.1 and 446.4 ± 23.9 μM, respectively, against α-amylase. The combination of baicalein, quercetin or luteolin with acarbose showed synergistic inhibition, and the combination of (+)-catechin with acarbose showed antagonistic inhibition of α-glucosidase. The combination of baicalein or apigenin with acarbose showed additive inhibition of α-amylase at lower concentrations and antagonistic inhibition at a higher concentration. Kinetic studies of α-glucosidase activity revealed that baicalein alone, acarbose alone, and the combination showed non-competitive, competitive, and mixed-type inhibition, respectively. Molecular modeling revealed that baicalein had higher affinity to the non-competitive binding site of maltase, glucoamylase, and isomaltase subunits of α-glucosidase, with glide scores of -7.64, -6.98, and -6.88, respectively. (+)-Catechin had higher affinity to the active sites of maltase and glucoamylase and to the non-competitive site of isomaltase. After sucrose loading, baicalein dose-dependently reduced the postprandial blood glucose (PBG) level in mice. The combination of 80 mg/kg baicalein and 1 mg/kg acarbose synergistically lowered the level of PBG, and the hypoglycemic effect was comparable to 8 mg/kg acarbose. The results indicated that baicalein could be used as a supplemental drug or dietary supplement in dietary therapy for diabetes mellitus.

  16. Acarbose improves hypoglycaemia following gastric bypass surgery without increasing glucagon-like peptide 1 levels.

    Science.gov (United States)

    Valderas, Juan Patricio; Ahuad, Jessica; Rubio, Lorena; Escalona, Manuel; Pollak, Felipe; Maiz, Alberto

    2012-04-01

    Postprandial hypoglycaemia is a severe complication of Roux-en-Y gastric bypass (RYGBP). Acarbose, an α-glucosidase inhibitor (AGI), is employed in its treatment. Several studies have shown that AGIs increase the postprandial levels of glucagon-like peptide 1 (GLP-1). However, an excessive level of GLP-1 is one of the factors involved in the physiopathology of this condition. We analysed the effect of acarbose oral administration in eight RYBGP patients with clinically significant hypoglycaemia or dumping syndrome. Glucose, insulin and GLP-1 plasma levels in fasting and after ingestion of a standard meal (Ensure Plus®; 13 g protein, 50 g carbohydrate, 11 g fat) were measured. The test was repeated the following week with the oral administration of 100 mg of acarbose 15 min prior to the meal. Five patients developed asymptomatic hypoglycaemia during the test (glucose level <50 mg/dl) with inappropriately high insulin levels and exaggerated GLP-1 response. Acarbose ingestion avoided hypoglycaemia in all of the patients and increased the lowest plasma glucose level (46.4 ± 4.8 vs. 59.0 ± 2.6 mg/dl, p < 0.01). Acarbose ingestion decreased the area under the curve for serum insulin and GLP-1 levels at 15 min after the meal. Acarbose avoided postprandial hypoglycaemia following RYGBP by decreasing the hyperinsulinemic response. This was associated with a decrease in early GLP-1 secretion, in contrast to that observed in non-surgical subjects. This finding could be explained by the reduction of glucose load in the jejunum produced by the α-glucosidase inhibition, which is the main stimulus for GLP-1 secretion.

  17. 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

  18. Modulation of circulating vasoactive peptides and extracellular matrix proteins are two novel mechanisms in the cardioprotective action of acarbose.

    Science.gov (United States)

    Rudovich, Natalia; Pivovarova, Olga; Bernigau, Wolfgang; Sparwasser, Andrea; Tacke, Christopher; Murahovshi, Veronica; Mertes, Gabriele; Birkenfeld, Andreas L; Bergmann, Andreas; Weickert, Martin O; Pfeiffer, Andreas F

    2016-12-01

    Acarbose, an alpha-glucosidase inhibitor, unexpectedly reduced the incidence of hypertension and cardiovascular endpoints in the STOP-NIDDM study. Based on the growing evidence of a link between vasoregulatory peptides and metabolic traits, we hypothesized that changes of the Glycemic Index by acarbose may modulate vasoregulatory peptide levels via regulation of postprandial metabolism. Subjects with type 2 diabetes and with metabolic syndrome were treated with acarbose (12 weeks, 300mg/d) in a double-blind, placebo-controlled, cross-over intervention. Changes in fasting and postprandial levels of midregional pro-atrial natriuretic peptide (MR-proANP), C-terminal pro-endothelin-1 (CT-proET-1) and midregional pro-adrenomedullin (MR-proADM), WNT1 Inducible Signaling Pathway Protein 1 (WISP1) as well as fasting and postprandial glucose/insulin levels in the liquid meal test were assessed. Acarbose strongly decreased postprandial insulin concentrations in subjects with metabolic syndrome (P=0.004), and postprandial glucose excursions in both groups. Postprandial MR-proANP and CT-proET-1 levels increased after acarbose treatment (P<0.01 and P<0.05, respectively) in subjects with metabolic syndrome only. No effect of acarbose treatment on MR-prADM was observed in both groups. All three peptides were correlated with each over, but neither with insulin sensitivity in euglycemic clamps, nor with adiponectin levels. WISP1 decreased after acarbose treatment in subjects with metabolic syndrome. Plasma MR- proANP and CT-proET-1 concentrations, but not MR-prADM concentrations, were affected by treatment with acarbose over 12 weeks. Our findings provide new possible mechanisms of acarbose action in diabetes and metabolic syndrome.

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

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    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.

  20. Effect of Acarbose on Control of Metabolic Parameters in Patients with Diabetes Type 1

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    A. Ziaee

    2012-07-01

    Full Text Available Introduction & Objective: Acarbose is an intestinal alpha-glucosidase inhibitor that delays absorption of carbohydrates. Findings of some studies show that it has been effective in better control of blood glucose in patients with diabetes type 1. The goal of this study is to investigate the effect of administration of acarbose on glycemic & lipid parameters and daily insulin requirements and tolerability in type 1 diabetic patient.Materials & Methods: This was a clinical trial randomized double blind placebo controlled study. Performed on patients with history of at least 1 year diabetes type 1 and had HbA1c≥7.5%. Patients with Cr≥2, partial GI obstruction or IBD were excluded from the study. 45 patients were randomized to be administered acarbose or placebo for 12 weeks. Initial dose of acarbose was 25 mg T.D.S for 2 weeks, and then it was increased to 50 mg T.D.S for 10 weeks. BMI, FBS, 2hpp, HbA1c, Total cholesterol, HDL, LDL, TG and Insulin dosage were investigated monthly.Results: The values of BMI, FBS, 2hpp, HbA1c, Total cholesterol, and TG & Insulin requirements decreased significantly in the case group compared to the controls (P=0.003, P=0.005, P<0.001, P=0.001, P=0.003, P<0.001, P<0.001, respectively; but no significant changes were observed in HDL &LDL levels. Conclusion: Administration of acarbose together with insulin to type 1 diabetic patient can be valuable in improving metabolic control (BMI, FBS, 2hpp, HbA1c, Total cholesterol and TG.(Sci J Hamadan Univ Med Sci 2012;19(2:5-10

  1. 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.

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

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    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.

  3. Effect of acarbose on biochemical responses and clinical symptoms in dumping syndrome.

    Science.gov (United States)

    Lyons, T J; McLoughlin, J C; Shaw, C; Buchanan, K D

    1985-01-01

    A dose of 50 mg of acarbose was administered with a standard breakfast to 13 subjects with dumping syndrome. Significant attenuation of hyperglycaemia (p less than 0.01) was observed, and rises in plasma gastric inhibitory polypeptide, insulin and enteroglycagon were reduced (p less than 0.05). Plasma levels of neurotensin, vasoactive intestinal polypeptide and somatostatin were not affected. Dumping score was reduced, but this did not achieve statistical significance. In a longer-term study, 9 patients took acarbose, 50 mg t.i.d., for 1 month. No significant reduction in the number or severity of dumping attacks was observed, but a majority expressed a preference for the drug and some individuals experienced a marked improvement of symptoms.

  4. Actinoplanes utahensis ZJB-08196 fed-batch fermentation at elevated osmolality for enhancing acarbose production.

    Science.gov (United States)

    Wang, Ya-Jun; Liu, Li-Ling; Wang, Yuan-Shan; Xue, Ya-Ping; Zheng, Yu-Guo; Shen, Yin-Chu

    2012-01-01

    Acarbose, a potent α-glucosidase inhibitor, is as an oral anti-diabetic drug for treatment of the type two, noninsulin-dependent diabetes. Actinoplanes utahensis ZJB-08196, an osmosis-resistant actinomycete, had a broad osmolality optimum between 309 mOsm kg(-1) and 719 mOsm kg(-1). Utilizing this unique feature, an fed-batch culture process under preferential osmolality was constructed through intermittently feeding broths with feed medium consisting of 14.0 g l(-1) maltose, 6.0 g l(-1) glucose and 9.0 g l(-1) soybean meal, at 48 h, 72 h, 96 h and 120 h. This intermittent fed-batch culture produced a peak acarbose titer of 4878 mg l(-1), increased by 15.9% over the batch culture.

  5. Design and development of bilayer tablet for immediate and extended release of acarbose and metformin HCl

    OpenAIRE

    Meenakshi Joshi; Ruchi Tiwari; Gaurav Tiwari

    2014-01-01

    The present investigation studied a novel Bilayer tablet having extended release (ER) system of metformin HCl (M.HCl) with Eudragit RS 100 and RL 100 and immediate release (IR) system of Acarbose with PVP K30 and PEG 6000 in different ratios using solvent evaporation technique. Solid dispersions (SDs) were characterized by Fourier Transform-Infra Red spectroscopy, Diffrential Scanning Calorimetry, X-Ray Diffractometry and Scanning Electron Microscopy. Selected SD system was subjected to Bilay...

  6. Inhibitory mechanism of acarbose and 1-deoxynojirimycin derivatives on carbohydrases in rat small intestine.

    Science.gov (United States)

    Samulitis, B K; Goda, T; Lee, S M; Koldovský, O

    1987-01-01

    The inhibitory action and mechanism of inhibition of two types of alpha-glucosidase inhibitors, acarbose (Bay-g-5421) and 1-deoxynojirimycin derivatives (Bay-m-1099 and Bay-o-1248), on small intestinal carbohydrases (sucrase, isomaltase, glucoamylase, trehalase and lactase) and pancreatic alpha-amylase were compared in vitro using small intestinal brush border membranes and pancreatic homogenates from adult Sprague-Dawley rats. Acarbose at a low (4 microM) concentration strongly inhibited the activities of glucoamylase, alpha-amylase and sucrase (98, 68, and 63%, respectively). At a high (200 microM) concentration, isomaltase activity was also inhibited (28%); effects on trehalase and lactase activities were negligible. Both the 1-deoxynojirimycin derivatives were even more potent inhibitors of sucrase (Ki = 8.6 x 10(-8) M for Bay-m-1099;Ki = 5.0 X 10(-8) M for Bay-o-1248) than acarbose (Ki = 9.9 x 10(-7) M). Whereas glucoamylase activity was strongly inhibited by the 1-deoxynojirimycin derivatives, alpha-amylase activity was not. In contrast to acarbose, the 1-deoxynojirimycin derivatives at high concentrations (20-200 microM) inhibited considerably trehalase and lactase (a beta-galactosidase) activities. The inhibition of lactase activity was stronger by Bay-m-1099 (Ki = 4.9 X 10(-6) M) than by Bay-o-1248 (Ki = 6.7 X 10(-5) M). Where inhibition was seen, kinetic analysis showed fully competitive inhibition of sucrase, isomaltase, trehalase, glucoamylase and lactase by all three inhibitors.

  7. The complete genome sequence of the acarbose producer Actinoplanes sp. SE50/110

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    Schwientek Patrick

    2012-03-01

    Full Text Available Abstract Background Actinoplanes sp. SE50/110 is known as the wild type producer of the alpha-glucosidase inhibitor acarbose, a potent drug used worldwide in the treatment of type-2 diabetes mellitus. As the incidence of diabetes is rapidly rising worldwide, an ever increasing demand for diabetes drugs, such as acarbose, needs to be anticipated. Consequently, derived Actinoplanes strains with increased acarbose yields are being used in large scale industrial batch fermentation since 1990 and were continuously optimized by conventional mutagenesis and screening experiments. This strategy reached its limits and is generally superseded by modern genetic engineering approaches. As a prerequisite for targeted genetic modifications, the complete genome sequence of the organism has to be known. Results Here, we present the complete genome sequence of Actinoplanes sp. SE50/110 [GenBank:CP003170], the first publicly available genome of the genus Actinoplanes, comprising various producers of pharmaceutically and economically important secondary metabolites. The genome features a high mean G + C content of 71.32% and consists of one circular chromosome with a size of 9,239,851 bp hosting 8,270 predicted protein coding sequences. Phylogenetic analysis of the core genome revealed a rather distant relation to other sequenced species of the family Micromonosporaceae whereas Actinoplanes utahensis was found to be the closest species based on 16S rRNA gene sequence comparison. Besides the already published acarbose biosynthetic gene cluster sequence, several new non-ribosomal peptide synthetase-, polyketide synthase- and hybrid-clusters were identified on the Actinoplanes genome. Another key feature of the genome represents the discovery of a functional actinomycete integrative and conjugative element. Conclusions The complete genome sequence of Actinoplanes sp. SE50/110 marks an important step towards the rational genetic optimization of the acarbose production

  8. 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.

  9. 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

  10. Coefficient of beta-cell failure in patients with type 2 diabetes treated with pioglitazone or acarbose.

    Science.gov (United States)

    Göke, B; Lübben, G; Bates, P C

    2004-02-01

    A new method of assessing the coefficient of failure of pancreatic beta-cells from any index of glycaemia has been proposed. This method of analysis has been used to assess data on HbA1c and fasting glucose concentrations from a randomised study comparing pioglitazone with acarbose. Patients were treated for 26 weeks with either pioglitazone 45 mg once daily or acarbose 300 mg/day as 3 equal doses. Plasma HbA1c concentration was measured every two months and fasting glucose was measured monthly. The coefficient of failure was determined for each patient from the slope of the least squares regression line over time. The coefficient of failure from HbA1c was - 2.65 +/- 2.13 %/year with pioglitazone and - 1.25 +/- 3.11 %/year with acarbose, indicating improved beta-cell function in each case. The coefficient of failure was improved to a significantly greater extent with pioglitazone ( P Coefficient of failure from fasting blood glucose also showed a greater improvement with pioglitazone (- 53.1 +/- 95.0 mg/dl/year) than with acarbose (- 29.9 +/- 142.5 mg/dl/year; p = 0.049). The coefficient of failure showed a significantly greater improvement of beta-cell function with pioglitazone than with acarbose during 26 weeks of treatment.

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

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    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.

  12. 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...... 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...

  13. Design and development of bilayer tablet for immediate and extended release of acarbose and metformin HCl

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    Meenakshi Joshi

    2014-01-01

    Full Text Available The present investigation studied a novel Bilayer tablet having extended release (ER system of metformin HCl (M.HCl with Eudragit RS 100 and RL 100 and immediate release (IR system of Acarbose with PVP K30 and PEG 6000 in different ratios using solvent evaporation technique. Solid dispersions (SDs were characterized by Fourier Transform-Infra Red spectroscopy, Diffrential Scanning Calorimetry, X-Ray Diffractometry and Scanning Electron Microscopy. Selected SD system was subjected to Bilayer tablet preparation by direct compression. Compressed tablets were evaluated for physical parameters, drug release and stability. SEM studies suggested the homogenous dispersion of the drug in polymers. FT-IR studies confirmed the formation of hydrogen bonding between the drug and polymer. XRD and DSC suggested the amorphous nature of the drug in SDs. All tablet formulations showed compliance with pharmacopoeial standards. In-vitro dissolution kinetics followed the Higuchi model via a non-fickian diffusion controlled release mechanism after the initial burst release. Stability studies conducted for optimized formulation did not show any change in the physical properties, drug content and drug release. Bilayer tablets showed an IR effect to provide the loading dose of the drug, followed by ER effect for 12 h, indicating a promising potential of the M.HCl and Acarbose Bilayer tablet as an alternative to the conventional dosage form.

  14. X-ray Structure of Cyclodextrin Glycosyltransferase Complexed with Acarbose. Implications for the Catalytic Mechanism of Glycosidases

    NARCIS (Netherlands)

    STROKOPYTOV, B; PENNINGA, D; ROZEBOOM, HJ; KALK, KH; DIJKHUIZEN, L; DIJKSTRA, BW

    1995-01-01

    Crystals of cyclodextrin glycosyltransferase (CGTase) from Bacillus circulans strain 251 were soaked in buffer solutions containing the pseudotetrasaccharide acarbose, a strong amylase- and CGTase inhibitor. The X-ray structure of the complex was elucidated at 2.5-Angstrom resolution with a final

  15. Efficacy of acarbose in different geographical regions of the world: analysis of a real-life database.

    Science.gov (United States)

    Weng, Jianping; Soegondo, Sidartawan; Schnell, Oliver; Sheu, Wayne H-H; Grzeszczak, Wladyslaw; Watada, Hirotaka; Yamamoto, Noriyuki; Kalra, Sanjay

    2015-02-01

    Alpha-glucosidase inhibitors are recommended in some international guidelines as first-line, second-line and third-line treatment options but are not used worldwide due to perceived greater effectiveness in Asians than Caucasians. Data from ten post-marketing non-interventional studies using acarbose, the most widely used alpha-glucosidase inhibitor, from 21 countries, provinces and country groups were pooled. Effects on glycated hemoglobin (HbA1c ) were analysed for four major ethnicity/region groups (European Caucasians and Asians from East, Southeast and South Asia) to identify differences in the response to acarbose. The safety and efficacy populations included 67 682 and 62 905 patients, respectively. Mean HbA1c in the total population decreased by 1.12 ± 1.31% at the 3-month visit from 8.4% at baseline (p multivariable analyses of covariance. After adjustment for relevant baseline confounding factors, Southeast and East Asians had slightly better responses to acarbose than South Asians and European Caucasians; however, the differences were small. Acarbose was effective in both European Caucasians and Asians; however, after adjustment for baseline confounding factors, significant small differences in response favoured Southeast and East Asians. © 2014 The Authors. Diabetes/Metabolism Research and Reviews published by John Wiley & Sons, Ltd.

  16. Synergistic effects of acarbose and an Oroxylum indicum seed extract in streptozotocin and high-fat-diet induced prediabetic mice.

    Science.gov (United States)

    Sun, Wenlong; Sang, Yuanbin; Zhang, Bowei; Yu, Xiaoxia; Xu, Qinmin; Xiu, Zhilong; Dong, Yuesheng

    2017-03-01

    Prediabetes is defined as blood glucose levels above normal but below diabetes thresholds, and up to 70% of individuals with prediabetes will eventually develop diabetes if left untreated. Acarbose, the first FDA approved anti-prediabetes agent, has some disadvantages, such as reducing the risk of diabetes by only 36%, side effects and limited effects on complications. The aim of this study is to develop a new agent to treat prediabetes and to investigate the anti-prediabetes effects and mechanisms of acarbose and an Oroxylum indicum seed extract (OISE) in prediabetic mice. The combined drugs can reduce the dose of acarbose by 80% and reduce the risk of diabetes by 75%, which is one fold higher than acarbose monotherapy. The combined drugs showed synergistic anti-prediabetes effects and could be effective in preventing the complications of prediabetes. The combined drugs could improve glucose tolerance, improve lipid metabolism and reduce oxidative stress and tissue damage. For the mechanisms, the combined drugs can reduce synergistically postprandial hyperglycaemia by inhibiting α-glucosidase. Furthermore, baicalein in OISE was demonstrated to be a major component in reducing oxidative stress and chrysin was the primary compound that activated PPARγ.

  17. 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.

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

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    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.

  19. A novel osmolality-shift fermentation strategy for improving acarbose production and concurrently reducing byproduct component C formation by Actinoplanes sp. A56.

    Science.gov (United States)

    Cheng, Xin; Peng, Wei-Fu; Huang, Lin; Zhang, Bao; Li, Kun-Tai

    2014-12-01

    Component C (Acarviosy-1,4-Glc-1,1-Glc) was a highly structural acarbose analog, which could be largely formed during acarbose fermentation process, resulting in acarbose purification being highly difficult. By choosing osmolality level as the key fermentation parameter of acarbose-producing Actinoplanes sp. A56, this paper successfully established an effective and simplified osmolality-shift strategy to improve acarbose production and concurrently reduce component C formation. Firstly, the effects of various osmolality levels on acarbose fermentation were firstly investigated in a 50-l fermenter. It was found that 400-500 mOsm/kg of osmolality was favorable for acarbose biosynthesis, but would exert a negative influence on the metabolic activity of Actinoplanes sp. A56, resulting in an obviously negative increase of acarbose and a sharp formation of component C during the later stages of fermentation (144-168 h). Based on this fact, an osmolality-shift fermentation strategy (0-48 h: 250-300 mOsm/kg; 49-120 h: 450-500 mOsm/kg; 121-168 h: 250-300 mOsm/kg) was further carried out. Compared with the osmolality-stat (450-500 mOsm/kg) fermentation process, the final accumulation amount of component C was decreased from 498.2 ± 27.1 to 307.2 ± 9.5 mg/l, and the maximum acarbose yield was increased from 3,431.9 ± 107.7 to 4,132.8 ± 111.4 mg/l.

  20. Structure of a Bacillus halmapalus family 13 ά-amylase, BHA, in complex with an acarbose-derived nonasaccharide at 2.1 A resolution

    Energy Technology Data Exchange (ETDEWEB)

    Davies,G.; Brzozowski, A.; Dauter, Z.; Rasmussen, M.; Borchert, T.; Wilson, K.

    2005-01-01

    The enzymatic digestion of starch by {alpha}-amylases is one of the key biotechnological reactions of recent times. In the search for industrial biocatalysts, the family GH13 {alpha}-amylase BHA from Bacillus halmapalus has been cloned and expressed. The three-dimensional structure at 2.1 Angstrom resolution has been determined in complex with the (pseudo)tetrasaccharide inhibitor acarbose. Acarbose is found bound as a nonasaccharide transglycosylation product spanning the -6 to +3 subsites. Careful inspection of electron density suggests that the bound ligand could not have been formed through successive transglycosylations of acarbose and must also have featured maltose or maltooligosaccharides as an acceptor.

  1. Pneumatosis cystoides intestinalis of the ascending colon related to acarbose treatment: a case report

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    Vogel Yilin

    2009-09-01

    Full Text Available Abstract Introduction Pneumatosis cystoides intestinalis is characterized by the presence of multiple gas-filled cysts in the intestinal wall, the submucosa and/or subserosa of the intestine. The term pneumatosis cystoides coli is synonymous with pneumatosis cystoides intestinalis when the disorder is limited to the colon. It is a secondary finding caused by a wide variety of underlying gastrointestinal or extragastrointestinal diseases but rarely occurs in the course of treatment with an α-glucosidase inhibitor. This is the first report of pneumatosis cystoides intestinalis after 12 years of treatment with the α-glucosidase inhibitor acarbose. Case presentation A 65-year-old Caucasian German woman was referred to our hospital for hemicolectomy. She had been treated for type 2 diabetes mellitus with an α-glucosidase inhibitor (acarbose, 150 mg daily for 12 years. Three months before referral, she had complained of left abdominal pain. 'Polyposis coli' in the ascending colon and diverticulosis were diagnosed. Colonoscopy and computed tomography scans of the abdomen were repeated and revealed pneumatosis cystoides coli located in the ascending colon, whereas diverticulosis of the sigmoid colon was confirmed. Histological examination of a biopsy specimen only showed colon mucosa. After discontinuing administration of the α-glucosidase inhibitor for 3 months and on repeated colonoscopy, the polypoid lesions had completely disappeared. Conclusion This case illustrates that pneumatosis cystoides coli can be a source of diagnostic confusion. Pneumatosis cystoides coli must be considered in the initial differential diagnosis of patients especially in the presence of multiple colonic polypoid lesions. It is important to take pneumatosis cystoides intestinalis into consideration when prescribing α-glucosidase inhibitors to patients with diabetes who have diabetic autonomic neuropathy with decreased intestinal motility, or to patients taking steroids.

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

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    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

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

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    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.

  4. Bilayer Tablet Formulation of Metformin HCl and Acarbose: A Novel Approach To Control Diabetes.

    Science.gov (United States)

    Tiwari, Ruchi; Gupta, Ankita; Joshi, Meenakshi; Tiwari, Gaurav

    2014-01-01

    The present investigation studied a novel bilayer tablet having an extended release system of metformin HCl with Eudragit RS 100 and RL 100 and an immediate release system of acarbose with polyvinylpyrrolidone K30 (PVP K30) and polyethylene glycol 6000 (PEG 6000) in different ratios using solvent evaporation and cogrinding techniques. Solid dispersions (SDs) were characterized by Fourier transform infrared spectroscopy (FT-IR), differential scanning calorimetry (DSC), powder x-ray diffractometry (XRD), scanning electron microscopy (SEM), as well as by content uniformity, in vitro dissolution studies, and release kinetics. The selected SD system was subjected to bilayer tablet preparation by direct compression. Compressed tablets were evaluated for drug content, weight variation, friability, hardness, and thickness, and they underwent in vitro dissolution studies. The progressive disappearance of IR, x-ray, and thermotropic drug signals in SDs and physical mixtures were related to increasing amount of polymer. SEM studies suggested the homogenous dispersion of drug in polymers. FT-IR studies confirmed the formation of hydrogen bonding between drug and polymer. All tablet formulations showed compliance with pharmacopoeial standards. The formulations gave an initial burst effect to provide the loading dose of the drug followed by extended release for 12 h (Higuchi model via a non-Fickian diffusion controlled release mechanism). Stability studies conducted for the optimized formulation did not show any change in physical properties, drug content, or in vitro drug release. The goal of diabetes therapy today is to achieve and maintain as near normal glycemia as possible to prevent the long-term microvascular and macrovascular complications of elevated blood glucose levels. Oral therapeutic options for the treatment of type 2 diabetes mellitus, until recently, have been severely limited. Metformin, a biguanide, targets additional mechanisms of hyperglycemia by inhibiting

  5. Comparative assessment of the efficacy and safety of acarbose and metformin combined with premixed insulin in patients with type 2 diabetes mellitus.

    Science.gov (United States)

    Wu, Honghua; Liu, Jie; Lou, Qingqing; Liu, Jing; Shen, Li; Zhang, Mingxia; Lv, Xiaofeng; Gu, Mingjun; Guo, Xiaohui

    2017-09-01

    This study, a subgroup analysis of the data from the Organization Program of DiabEtes INsulIN ManaGement study, aimed to compare the efficacy and safety profiles of acarbose and metformin used in combination with premixed insulin.This analysis included 80 and 192 patients taking only 1 oral antidiabetic drug, classified into acarbose (treated with acarbose + insulin) and metformin groups (treated with metformin + insulin), respectively. The efficacy and safety data were analyzed for within- and between-group differences. The clinical trial registry number was NCT01338376.The percentage of patients who achieved target hemoglobin A1c (HbA1c) <7% in the acarbose and metformin groups were 38.75% and 30.73%, respectively, after a 16-week treatment. The average HbA1c levels in the acarbose and metformin groups were comparable at baseline and decreased significantly in both groups at the end of the study. All 7 blood glucose decreased significantly in both groups at endpoint compared with that at baseline. Insulin consumption was higher in the metformin group in terms of total daily amount and units/kg body weight. Incidences of hypoglycemia were similar in both groups. Body weight changed significantly in both groups from baseline to endpoint, but with no significant difference between the groups. Mean scores of Morisky Medication Adherence Scale improved in both groups at endpoint.Combination of insulin with acarbose or metformin could improve glycemic control in patients with type 2 diabetes mellitus. Acarbose and metformin were found to be comparable in terms of efficacy, weight gain, and incidence of hypoglycemia.

  6. Acarbose reduces blood glucose by activating miR-10a-5p and miR-664 in diabetic rats.

    Directory of Open Access Journals (Sweden)

    Qian Zhang

    Full Text Available MicroRNAs (miRNAs are non-coding RNA molecules involved in the post-transcriptional regulation of a large number of genes, including those involved in glucose metabolism. Acarbose is an α-glucosidase inhibitor that improves glycemic control by decreasing the intestinal absorption of glucose, thereby decreasing the elevation of postprandial blood glucose. However, acarbose is poorly absorbed into the blood stream from the gut. Therefore, the exact mechanisms by which acarbose affects glucose metabolism are unclear. This study investigated the effect of acarbose on glucose metabolism in diabetic rats and tested the hypothesis that acarbose acts directly through miRNA-regulated expression in the intestinal epithelium. Rats were divided into four groups: a control group, a diabetic group (DM, a low dose of acarbose group (AcarL and a high dose of acarbose group (AcarH. Ileum samples were analyzed using miRCURY LNA™ microRNA Array, qPCR and immunohistochemistry. We found that 8-week treatment with acarbose significantly decreased fasting blood glucose. Oral glucose tolerance tests (OGTT showed that blood glucose was significantly reduced in the AcarL and AcarH groups at 30 min, 60 min and 120 min after oral glucose administration. We found that miR-151*, miR-10a-5p, miR-205, miR-17-5p, miR-145 and miR-664 were up-regulated in the AcarH group, while miR-541 and miR-135b were down-regulated. Through target gene analysis, real time PCR and immunohistochemistry verification, we found that these miRNAs suppressed the expression of proinflammatory cytokines [IL6 (interleukin 6 and TNF (tumor necrosis factor] and mitogen activated protein kinase 1 (MAPK1. Our data suggest that acarbose can improve blood glucose in diabetic rats through the MAPK pathway and can down-regulate proinflammatory factors by activating miR-10a-5p and miR-664 in the ileum.

  7. Hydrogen gas production is associated with reduced interleukin-1β mRNA in peripheral blood after a single dose of acarbose in Japanese type 2 diabetic patients.

    Science.gov (United States)

    Tamasawa, Atsuko; Mochizuki, Kazuki; Hariya, Natsuyo; Saito, Miyoko; Ishida, Hidenori; Doguchi, Satako; Yanagiya, Syoko; Osonoi, Takeshi

    2015-09-05

    Acarbose, an α-glucosidase inhibitor, leads to the production of hydrogen gas, which reduces oxidative stress. In this study, we examined the effects of a single dose of acarbose immediately before a test meal on postprandial hydrogen gas in breath and peripheral blood interleukin (IL)-1β mRNA expression in Japanese type 2 diabetic patients. Sixteen Japanese patients (14 men, 2 women) participated in this study. The mean±standard deviation age, hemoglobin A1c and body mass index were 52.1±15.4 years, 10.2±2.0%, and 27.7±8.0kg/m(2), respectively. The patients were admitted into our hospital for 2 days and underwent test meals at breakfast without (day 1) or with acarbose (day 2). We performed continuous glucose monitoring and measured hydrogen gas levels in breath, and peripheral blood IL-1β mRNA levels before (0min) and after the test meal (hydrogen gas: 60, 120, 180, and 300min; IL-1β: 180min). The induction of hydrogen gas production and the reduction in peripheral blood IL-1β mRNA after the test meal were not significant between days 1 (without acarbose) and 2 (with acarbose). However, the changes in total hydrogen gas production from day 1 to day 2 were closely and inversely associated with the changes in peripheral blood IL-1β mRNA levels. Our results suggest that an increase in hydrogen gas production is inversely associated with a reduction of the peripheral blood IL-1β mRNA level after a single dose of acarbose in Japanese type 2 diabetic patients. Copyright © 2015 Elsevier B.V. All rights reserved.

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

    Energy Technology Data Exchange (ETDEWEB)

    Hwa Park, K.; Jeong Kim, M.; Seob Lee, H.; Kim, D. [Department of Food Science and Technology and Research Center for New Bio-Materials in Agriculture, Seoul National University, Suwon (Korea, Republic of); Soo Han, N.; Robyt, J.F. [Laboratory for Carbohydrate Chemistry and Enzymology, Department of Biochemistry and Biophysics, Iowa State University, Ames, IA (United States)

    1998-12-15

    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 {alpha}-(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 {alpha}-(1-6) to d-glucose, d-mannose, d-galactose, and methyl {alpha}-d-glucopyranoside. With d-fructopyranose and d-xylopyranose, PTS was linked {alpha}-(1-5) and {alpha}-(1-4), respectively. PTS was primarily transferred to C-6 of the nonreducing residue of maltose, cellobiose, lactose, and gentiobiose. Lesser amounts of {alpha}-(1-3) and/or {alpha}-(1-4) transfer products were also observed for these carbohydrate acceptors. The major transfer product to sucrose gave PTS linked {alpha}-(1-4) to the glucose residue. {alpha},{alpha}-Trehalose gave two major products with PTS linked {alpha}-(1-6) and {alpha}-(1-4). Maltitol gave two major products with PTS linked {alpha}-(1-6) and {alpha}-(1-4) to the glucopyranose residue. Raffinose gave two major products with PTS linked {alpha}-(1-6) and {alpha}-(1-4) to the d-galactopyranose residue. Maltotriose gave two major products with PTS linked {alpha}-(1-6) and {alpha}-(1-4) to the nonreducing end glucopyranose residue. Xylitol gave PTS linked {alpha}-(1-5) as the major product and d-glucitol gave PTS linked {alpha}-(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 {sup 13}C 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.)

  9. Effect of acarbose on milk yield and composition in early-lactation dairy cattle fed a ration to induce subacute ruminal acidosis.

    Science.gov (United States)

    McLaughlin, C L; Thompson, A; Greenwood, K; Sherington, J; Bruce, C

    2009-09-01

    Subacute ruminal acidosis reduces lactation performance in dairy cattle and most often occurs in animals fed a high concentrate:forage ration with large amounts of readily fermentable starch, which results in increased production of volatile fatty acids and lactic acid and a reduction in ruminal pH. Acarbose is commercially available (Glucobay, Bayer, Wuppertal, Germany) and indicated for the control of blood glucose in diabetic patients. In cattle, acarbose acts as an alpha-amylase and glucosidase inhibitor that slows the rate of degradation of starch to glucose, thereby reducing the rate of volatile fatty acid production and maintaining rumen pH at higher levels. The ability of acarbose to reverse the reduced feed intake and milk fat percentage and yield associated with a high concentrate:forage ration with a high risk of inducing subacute ruminal acidosis was evaluated in 2 experiments with lactating dairy cattle. In 2 preliminary experiments, the effects of a 70:30 concentrate:forage ration on ruminal pH and lactation were evaluated. Ruminal pH was monitored in 5 Holstein steers with ruminal cannulas every 10 min for 5 d. Ruminal pH was dairy cows, the 70:30 concentrate:forage ration decreased feed intake 5%, milk fat percentage 7%, and milk fat yield 8% compared with a 50:50 concentrate:forage ration but did not affect milk yield. Early lactating dairy cattle were offered the 70:30 concentrate:forage ration with 0 or 0.75 g/d of acarbose added in a crossover design in 2 experiments. In the first experiment, acarbose increased dry matter feed intake (23.1 vs. 21.6 kg/d) and 3.5% fat-corrected milk yield (33.7 vs. 31.7 kg/d) because of an increase in percentage milk fat (3.33 vs. 3.04%) compared with control cows. In the second experiment, cows were fasted for 3 h before the morning feeding to induce consumption of a large meal to mimic conditions that might be associated with unplanned delayed feeding. In this experiment, acarbose also increased feed intake (22

  10. 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......H-induced crystallisation of BHA in a MES-HEPES-Boric acid-buffer (MHB-buffer) at 30oC - the solubility of BHA in MHB has a retrograde temperature dependency, and crystallisation of BHA was only possible by raising the temperature to at least 25oC. Data was collected at cryogenic temperatures to a resolution of 2.0 Å...

  11. 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

    Directory of Open Access Journals (Sweden)

    Mengyi Li

    2016-01-01

    Full Text Available 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.

  12. Modes of Action of Acarbose Hydrolysis and Transglycosylation Catalyzed by a Thermostable Maltogenic Amylase, the Gene for Which Was Cloned from a Thermus Strain

    Science.gov (United States)

    Kim, Tae-Jip; Kim, Myo-Jeong; Kim, Byung-Cheon; Kim, Jae-Cherl; Cheong, Tae-Kyou; Kim, Jung-Wan; Park, Kwan-Hwa

    1999-01-01

    A maltogenic amylase gene was cloned in Escherichia coli from a gram-negative thermophilic bacterium, Thermus strain IM6501. The gene encoded an enzyme (ThMA) with a molecular mass of 68 kDa which was expressed by the expression vector p6xHis119. The optimal temperature of ThMA was 60°C, which was higher than those of other maltogenic amylases reported so far. Thermal inactivation kinetic analysis of ThMA indicated that it was stabilized in the presence of 10 mM EDTA. ThMA harbored both hydrolysis and transglycosylation activities. It hydrolyzed β-cyclodextrin and starch mainly to maltose and pullulan to panose. ThMA not only hydrolyzed acarbose, an amylase inhibitor, to glucose and pseudotrisaccharide (PTS) but also transferred PTS to 17 sugar acceptors, including glucose, fructose, maltose, cellobiose, etc. Structural analysis of acarbose transfer products by using methylation, thin-layer chromatography, high-performance ion chromatography, and nuclear magnetic resonance indicated that PTS was transferred primarily to the C-6 of the acceptors and at lower degrees to the C-3 and/or C-4. The transglycosylation of sugar to methyl-α-d-glucopyranoside by forming an α-(1,3)-glycosidic linkage was demonstrated for the first time by using acarbose and ThMA. Kinetic analysis of the acarbose transfer products showed that the C-4 transfer product formed most rapidly but readily hydrolyzed, while the C-6 transfer product was stable and accumulated in the reaction mixture as the main product. PMID:10103262

  13. 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.

  14. Comparison of the Effects of Acarbose and TZQ-F, a New Kind of Traditional Chinese Medicine to Treat Diabetes, Chinese Healthy Volunteers

    Directory of Open Access Journals (Sweden)

    Huang Yuhong

    2014-01-01

    Full Text Available Ethnopharmacological Relevance. TZQ-F has been traditionally used in Traditional Chinese Medicine as a formula for the treatment of diabetes. Aim of the Study. This study aims to compare the pharmacologic effects and gastrointestinal adverse events between TZQ-F and acarbose. Methods. The double-blind randomized placebo-controlled fivefold crossover study was performed in 20 healthy male volunteers. Plasma glucose, plasma IRI, and plasma C-peptide were measured to assess the pharmacologic effects. Flatus and bowel activity were measured to assess the adverse event of gastrointestinal effect. Results. 3 and 4 tablets of TZQ decreased the Cmax of plasma glucose compared with that of the previous day and with placebo. 3 tablets also decreased Cmax of plasma C-peptide compared with placebo. 4 tablets increased Cmax of plasma insulin after breakfast and the AUC of plasma C-peptide after breakfast and dinner. 2 tablets did not decrease plasma glucose and elevated the Cmax and AUC of C-peptide after breakfast and dinner, respectively. Acarbose 50 mg decreased the Cmax of plasma insulin and C-peptide after breakfast and the Cmax of plasma glucose and C-peptide after dinner. The subjects who received TZQ did not report any abdominal adverse events. Conclusions. 3 tablets of TZQ have the same effects as the acarbose.

  15. 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

  16. Structure of the complex of a yeast glucoamylase with acarbose reveals the presence of a raw starch binding site on the catalytic domain.

    Science.gov (United States)

    Sevcík, Jozef; Hostinová, Eva; Solovicová, Adriana; Gasperík, Juraj; Dauter, Zbigniew; Wilson, Keith S

    2006-05-01

    Most glucoamylases (alpha-1,4-D-glucan glucohydrolase, EC 3.2.1.3) have structures consisting of both a catalytic and a starch binding domain. The structure of a glucoamylase from Saccharomycopsis fibuligera HUT 7212 (Glu), determined a few years ago, consists of a single catalytic domain. The structure of this enzyme with the resolution extended to 1.1 A and that of the enzyme-acarbose complex at 1.6 A resolution are presented here. The structure at atomic resolution, besides its high accuracy, shows clearly the influence of cryo-cooling, which is manifested in shrinkage of the molecule and lowering the volume of the unit cell. In the structure of the complex, two acarbose molecules are bound, one at the active site and the second at a site remote from the active site, curved around Tyr464 which resembles the inhibitor molecule in the 'sugar tongs' surface binding site in the structure of barley alpha-amylase isozyme 1 complexed with a thiomalto-oligosaccharide. Based on the close similarity in sequence of glucoamylase Glu, which does not degrade raw starch, to that of glucoamylase (Glm) from S. fibuligera IFO 0111, a raw starch-degrading enzyme, it is reasonable to expect the presence of the remote starch binding site at structurally equivalent positions in both enzymes. We propose the role of this site is to fix the enzyme onto the surface of a starch granule while the active site degrades the polysaccharide. This hypothesis is verified here by the preparation of mutants of glucoamylases Glu and Glm.

  17. 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.

  18. Inhibition of Human and Rat Sucrase and Maltase Activities To Assess Antiglycemic Potential: Optimization of the Assay Using Acarbose and Polyphenols.

    Science.gov (United States)

    Pyner, Alison; Nyambe-Silavwe, Hilda; Williamson, Gary

    2017-10-04

    We optimized the assays used to measure inhibition of rat and human α-glucosidases (sucrase and maltase activities), intestinal enzymes which catalyze the final steps of carbohydrate digestion. Cell-free extracts from fully differentiated intestinal Caco-2/TC7 monolayers were shown to be a suitable source of sucrase-isomaltase, with the same sequence as human small intestine, and were compared to a rat intestinal extract. The kinetic conditions of the assay were optimized, including comparison of enzymatic and chromatographic methods to detect the monosaccharide products. Human sucrase activity was more susceptible than the rat enzyme to inhibition by acarbose (IC50 (concentration required for 50% inhibition) = 2.5 ± 0.5 and 12.3 ± 0.6 μM, respectively), by a polyphenol-rich green tea extract, and by pure (-)-epigallocatechin gallate (EGCG) (IC50 = 657 ± 150 and 950 ± 86 μM respectively). In contrast, the reverse was observed when assessing maltase activity (e.g. IC50 = 677 ± 241 and 14.0 ± 2.0 μM for human and rat maltase, respectively). 5-Caffeoylquinic acid did not significantly inhibit maltase and was only a very weak inhibitor of sucrase. The data show that for sucrase and maltase activities, inhibition patterns of rat and human enzymes are generally qualitatively similar but can be quantitatively different.

  19. Determination of Acarbose Tablets by Hydrophilic-interaction Chromatography%阿卡波糖片的亲水色谱法测定

    Institute of Scientific and Technical Information of China (English)

    谢赞; 杜旭召; 何丽娟; 陈玉洁; 史颖

    2011-01-01

    建立了亲水色谱法测定阿卡波糖片的含量及其有关物质.采用Phenomenex氨基柱,以6 mmol/L磷酸二氢钾缓冲液(pH 6.8)-乙腈(28:72)为流动相,检测波长210nm.阿卡波糖在4~20mg/ml浓度范围内线性关系良好.平均回收率为99.2%,RSD为0.7%.%A hydrophilic-ineraction chromatography method was established for the determination of acarbose tablets and its related substances.A Phenomenex NH2 colum was used with the mobile phase of 6 mmol/L potassium dihydrogen phosphate buffer (pH 6.8) -acetonitrile (28∶ 72), at the detection wavelength of 210 nm.The calibration curve was linear in the concentration range of 4 - 20 mg/ml.The average recovery was 99.2 % with RSD of 0.7 %.

  20. 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

  1. Acarbose insulin glargine combined on treatment of elderly diabetic%甘精胰岛素联合阿卡波糖治疗老年糖尿病的疗效观察

    Institute of Scientific and Technical Information of China (English)

    王明岗

    2010-01-01

    目的 探讨甘精胰岛素联合阿卡波糖治疗老年糖尿病的临床疗效.方法 2008年1月至2010年1月门诊或住院诊治的老年2型糖尿病患者246例,随机分为治疗组126例,对照组120例,治疗组采用甘精胰岛素联合阿卡波糖治疗,对照组采用精蛋白锌重组人胰岛素混合注射液治疗;观察两组临床效果及B细胞功能变化.结果 两组血糖达标时间比较,P<0.05有显著差异性;两组胰岛素日用量、低血糖发生率比较,P<0.01有显著差异性;治疗前、后C肽+胰岛素释放试验检测比较P<0.05有显著差异性.结论 甘精胰岛素联合阿卡波糖能达到良好控制血糖,又能减少胰岛素用量,降低低血糖发生率,有效的改善β细胞功能.而且用药依从性良好的治疗老年2型糖尿病方案.%Objective To investigate insulin glargine combined acarbose treatment of senile diabetes therapy. Methods 246 cases type 2 diabetes were treated in out - patient or in hospital from January 2008 to January 2010 who were randomly divided into treatment group( 126 ) and control group (120). Treatment group patients treated with insulin glargine combined acarbose treatment, and control group were treated by Protamine zinc mixed recombinant human insulin injection treatment;To observe clinical effects and β -cell function. Results Comparison of two groups of blood glucose time, P < 0. 05; Two groups of insulin daily dose, the incidence of hypoglycemia,P < 0. 01 ;Treatment before and after the C peptide + insulin release test comparison, P < 0. 05; Conclusion Insulin glargine combined acarbose can achieve good control of blood glucose and reducing insulin dosage, reducing the incidence of low blood sugar, which an improvement of β cell function. It is a good drug compliance and treatment program in elderly type 2 diabetes.

  2. 阿卡波糖治疗高血压伴糖尿病的疗效分析%The analysis of clinical effect of treating hypertension associated with diabetes melitus with acarbose

    Institute of Scientific and Technical Information of China (English)

    胡云

    2012-01-01

      Objective: To discuss the clinical effect of treating hypertension associated with diabetes melitus with acarbose. Methods: Choosed 80 patients of hypertension associated with diabetes melitusfrom May. 2009 to May. 2011 to divide into study group and controled group. These two groups were treated wtih insulinum combined valsartan or nifedipine, and study group were treated with acarbose added. Compared the effect rate and SBP, DBP of these two groups. Results: The effect rate in study group was higher than controled group. The results of SBP and DPB after treating 6 weeks and 12 weekes, there was significant difference between thses two groups. Conclusion: Acarbose combining hypotensive drugs could treat hypertension better to extend in clinical.%  目的探讨阿卡波糖治疗原发性高血压伴2型糖尿病患者的疗效和分析.方法选取并回顾性分析2009-05至2011-05原发性高血压伴2型糖尿病患者80例.其中30例采用胰岛素配合缬沙坦、硝苯地平治疗,其余50例在此基础上联合阿卡波糖治疗.对比两组患者治疗有效率以及收缩压(SBP)、舒张压(DBP).结果研究组显效以及有效率明显高于对照组,两组差异有统计学意义(P<0.05).治疗6周、12周后研究组SBP、DBP明显小于对照组,两组差异有统计学意义(P<0.05).结论阿卡波糖配合降压药物治疗高血压伴糖尿病患者效果好于普通降压药物,值得临床推广.

  3. 阿卡波糖治疗2型糖尿病的药物经济学分析%Pharmacoeconomic Analysis of Acarbose Treatment of Type 2 diabetes

    Institute of Scientific and Technical Information of China (English)

    郭华春

    2015-01-01

    Objective To evaluate the effect of acarbose in treatment of type 2 diabetes melitus(T2DM)economic benefit.Methods Colect the data of 88 cases of T2DM patients,the patients were randomly divided into two groups, 44 cases in each.A group of patients with acarbose in the treatment of patients in the B group,metformin treatment, compared two groups of patients with curative effect cost(C)/(E)ratio.Results The two groups after the treatment of FPG and 2 hPG were significantly lower than those before treatment(P0.05),but the 2 hPG A group was significantly lower than that in B group;FPG as indicators of efficacy,the difference between the two groups had no statistical signifi- cance(P>0.05); with 2 hPG as the standard of curative effect,the total effective rate of group A was significantly higher than that of B group(P0.05).Conclusion the therapeutic effect of acarbose and metformin control FPG quite, but the control effect of 2 hPG is better than that from the perspective of economics analysis of curative effect of metformin, acarbose and metformin, below the clinical medication,should be a reasonable choice according to the specific condition of patients.%目的评价阿卡波糖治疗2型糖尿病(T2DM)的经济学效益.方法收集T2DM 88例患者资料,将患者采用随机数字表法分为两组,各44例.A组患者应用阿卡波糖治疗,B组患者应用二甲双胍治疗,比较两组患者的成本(C)/疗效(E)比.结果两组患者治疗后FPG及2 hPG均较治疗前明显降低(P0.05),但A组的2 hPG明显低于B组;以FPG为疗效指标,两组比较差异无统计学意义(P>0.05);以2 hPG为疗效标准,A组总有效率明显高于B组(P0.05).结论 阿卡波糖控制FPG的疗效与二甲双胍相当,但控制2 hPG疗效优于二甲双胍,从疗效经济学角度分析,阿卡波糖低于二甲双胍,临床应根据患者的具体情况合理选择用药.

  4. 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

  5. Therapeutic effect of glargine insulin combined with acarbose in elderly diabetic patients%甘精胰岛素联合阿卡波糖在老年糖尿病患者中的应用

    Institute of Scientific and Technical Information of China (English)

    罗小勇

    2013-01-01

    Objective To investigate the clinical efficacy and safety of glargine insulin combined with protamine zinc recombinant lispro insulin in elderly diabetic patients.Methods 96 cases of elderly diabetic were divided into the observation group (52 cases) and control group (44 cases),the control group was given protamine zinc recombinant insulin lispro treatment,and therapeutic effect was observed.Results After treatment FEG,2PBG and HbAlc were significantly lower than those before treatment (P<0.05); after treatment,glycemic index showed no significant difference between the two groups (P>0.05); the observation group' s hypoglycemia was 3.64%,significantly lower than 15.91% of the control group (P<0.05).Conclusion The combined therapy of the glargine insulin and acarbose treatment for senile diabetes is secure,effective,and patients are easier to accept.%目的 探讨甘精胰岛素联合阿卡波糖治疗老年糖尿病的临床疗效及安全性.方法 将96例老年糖尿病患者分为观察组52例和对照组44例,观察组给予甘精胰岛素联合阿卡波糖治疗,对照组给予精蛋白锌重组赖脯胰岛素治疗,观察两组患者治疗效果.结果 两组患者治疗后FEG、2PBG及HbAlc均明显低于治疗前(P<0.05);两组患者治疗后各血糖指标比较差异无统计学意义(P>0.05).观察组低血糖发生率为3.64%,明显低于对照组的15.91% (P<0.05).结论 甘精胰岛素联合阿卡波糖治疗老年糖尿病安全、有效,更易被患者接受.

  6. 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

  7. 阿卡波糖或吡格列酮+二甲双胍对单用二甲双胍控制不佳的2型糖尿病合并精神分裂症患者的疗效分析%Curative effect analysis of acarbose or pioglitazone + metformin in the treatment of type 2 diabetes mellitus complicated with schizophrenia under poor metformin monotherapy control

    Institute of Scientific and Technical Information of China (English)

    周艳兰; 陈新河; 刘艳萍; 陈钊; 严玲

    2015-01-01

    Objective To compare the curative effect and safety of acarbose or pioglitazone in the treatment of type 2 diabetes mellitus complicated with schizophrenia under poor metformin monotherapy control. Methods A total of 103 patients of type 2 diabetes mellitus complicated with schizophrenia under poor metformin monotherapy control were randomly divided into acarbose group with 52 cases and pioglitazone group with 51 cases. The acarbose group received metformin+acarbose for treatment, and the pioglitazone group received metformin+pioglitazone. Treatment lasted for 24 weeks. Blood glucose and blood lipid were detected before and after treatment in the two groups, and their body mass and blood pressure were recorded. Adverse reactions as hypoglycemia were recorded for comparison.Results After treatment, both groups had lower fasting plasma glucose (FPG) and glycosylated hemoglobin (HbA1c) than those before treatment (P0.05).Conclusion Implement of acarbose or pioglitazone can effectively control blood glucose with high safety in the treatment of type 2 diabetes mellitus complicated with schizophrenia under poor metformin monotherapy control. Acarbose provides better effect in reducing 2 h PG than pioglitazone, while pioglitazone’s effect in reducing FPG is better than acarbose.%目的:比较2型糖尿病合并精神分裂症患者单用二甲双胍血糖控制不佳时加用阿卡波糖或吡格列酮的疗效和安全性。方法103例单用二甲双胍血糖控制不佳的2型糖尿病合并精神分裂症患者随机分为阿卡波糖组52例和吡格列酮组51例。阿卡波糖组采用二甲双胍+阿卡波糖治疗,吡格列酮组采用二甲双胍+吡格列酮治疗,疗程均为24周。两组治疗前后检测血糖、血脂指标,测量体质量和血压,记录低血糖等不良反应情况并进行对比。结果疗程结束后,两组空腹血糖(FPG)、糖化血红蛋白(HbA1c)均低于治疗前(P0.05)。结论单用二

  8. Study on curative effect comparison of sitagliptin and acarbose for primordial type 2 diabetes mellitus and influence to relevant gastrointestinal hormones%西格列汀与阿卡波糖对初发2型糖尿病的疗效比较和胃肠道相关激素的影响研究

    Institute of Scientific and Technical Information of China (English)

    张安英; 于世斌; 李晨芳; 张晓晴; 王颜刚

    2016-01-01

    目的:对比分别用西格列汀与阿卡波糖治疗初发2型糖尿病的疗效,并分析两者对患者胃肠道相关激素的影响。方法选取在我院收治的初发2型糖尿病患者80例,随机分为实验组与对照组,实验组患者给予西格列汀片治疗,对照组给予阿卡波糖片治疗。6个月后观察两组患者的体重指数、空腹血糖、餐后两小时血糖、糖化血红蛋白、胃饥饿素及胃泌素的变化情况。结果治疗后两组患者的体重指数、糖化血红蛋白、空腹血糖及餐后两小时血糖均明显下降(P0.05);实验组患者经西格列汀干预后,血压明显下降,胃饥饿素分泌减少,与治疗前相比,差异具有统计学意义(P 0.05). after sitagliptin intervention, blood pressure of experimental group decreased significantly, ghrelin’s secretion decreased, difference showed statistical significance compared with that before treatment(P<0.05). after acarbose intervention, serum total cholesterol (tc) of control group decreased, and gastrin’s secretion increased, difference showed statistical significance compared with that before treatment(P<0.05).Conclusion sitagliptin and acarbose has good therapeutic effect for primordial type 2 diabetes, and sitagliptin can adjust blood pressure and ghrelin of patients, acarbose has intervention effect on blood lipid and gastrin of patients.

  9. Analysis of the clinical curative effect of lantus plus acarbose applied for the treatment of elderly diabetes patients%甘精胰岛素联合阿卡波糖治疗老年人糖尿病疗效分析

    Institute of Scientific and Technical Information of China (English)

    车树林; 暴树芝

    2011-01-01

    目的 探讨甘精胰岛素联合阿卡波糖在老年糖尿病患者治疗中的临床意义。方法 将84例老年糖尿病患者随机分为观察组和对照组,观察组应用甘精胰岛素联合阿卡波糖治疗,对照组使用普通胰岛素联合阿卡波糖治疗,观察两组患者治疗效果。结果 两组患者在治疗后的空腹血糖、餐后2h血糖、糖化血红蛋白的浓度及治疗后不良反应发生情况差异均有统计学意义(均P <0.05)。结论 甘精胰岛素联合阿卡波糖治疗老年糖尿病是一种有效的治疗方法,可以获得理想的血糖控制及较少的并发症。%Objective To explore the clinical significance of lantus plus acarbose applied for the treatment of elderly diabetes patieats.Methods 84 old diabetes patients treated in our hospital were randomly divided into experimental group and control group. The patients of experimental group were treated with lantus plus acarbose, the control group used normal insulin. To observe the therapeutic effect of two groups. Results The levels of fasting plasma glucose,2 hours postprandial glucose,glycosylated hemoglobin A1C and the occurrence of adverse reactions after the treatment were statistically significant ( P < 0. 05 ). Conclusion Lantus plus acarbose was an effective treatment for elderly diabetes patients, and could obtain the ideal blood sugar and less complications, and clinical effect of the therapy was ideal, and it was worth used widely.

  10. 甘精胰岛素联合阿卡波糖治疗老年糖尿病30例及护理分析%Clinical Effect of Insulin Glargine Combined with Acarbose in Treating Senile Diabetes and Nursing Analysis in 30 Cases

    Institute of Scientific and Technical Information of China (English)

    胡明伟; 毛柳

    2015-01-01

    目的:观察甘精胰岛素联合阿卡波糖治疗老年糖尿病的临床疗效。方法选取老年2型糖尿病患者60例,随机均分为治疗组和对照组。治疗前护理人员对所有患者的基本情况进行评估,在整个过程中对其进行健康教育、饮食护理、运动护理、预防低血糖等。治疗组采用甘精胰岛素联合阿卡波糖治疗,甘精胰岛素皮下注射、1次/日,阿卡波糖片口服、3次/日;对照组采用门冬胰岛素30皮下注射,早晚餐前各1次。16周后评价两组疗效。结果治疗组餐后2 h血糖明显高于对照组( P 0.05);治疗组低密度脂蛋白胆固醇低于治疗前水平( P0.05)。结论甘精胰岛素联合阿卡波糖治疗老年糖尿病,能较好控制患者血糖,且低血糖发生率低,依从性好,值得临床推广。%Objective To observe the clinical effect of insulin glargine combined with acarbose in treating senile diabetes and to analyze its nursing. Methods 60 elderly patients with type 2 diabetes mellitus ( T2DM ) were selected and divided into the treatment group and the control group randomly and equally. The nursing staff conducted the evaluation on the basic situation of all patients before treatment and performed the health education, dietary nursing, exercise nursing, hypoglycemia prevention, etc. The treatment group was treated by in-sulin glargine combined with acarbose, insulin glargine by subcutaneous injection once daily, oral acarbose tablets 3 times daily;the con-trol group adopted the Insulin Aspart 30 Injection by subcutaneous injection, once before breakfast and again before dinner. The fasting and postprandial blood glucose level, glycated hemoglobin and incidence of hypoglycemia after 16 weeks were observed and compared between the two groups. The blood pressure and blood lipids in the treatment group were compared between before and after treat-ment. Results The postprandial 2 h blood glucose level in the

  11. 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

  12. Comparison of Insulin Aspart 30 Combined with Metformin or Acarbose on Glycemic Variability and Compliance Status in Patients with Type 2 Diabetes%门冬胰岛素30联合二甲双胍或阿卡波糖对2型糖尿病患者血糖变异的影响及达标状况的比较

    Institute of Scientific and Technical Information of China (English)

    徐芬娟; 沈飞霞; 张青森; 宣少平; 朱娟飞

    2013-01-01

    目的 观察门冬胰岛素30单用或联合二甲双胍、阿卡波糖对2型糖尿病患者血糖变异的影响及达标状况.方法 患者随机分为3组,分别接受门冬胰岛素30、门冬胰岛素30+二甲双胍(简称二甲双胍组)、门冬胰岛素30+阿卡波糖(简称阿卡波糖组)治疗,保持三餐前和睡前血糖平衡,观察血糖波动指标、达标时间、低血糖事件、胰岛素量及费用.结果 门冬胰岛素30组在晚餐后及2:00血糖高于二甲双胍组及阿卡波糖组;其余时间点血糖差异无统计学意义.治疗后8个时间点血糖标准差、最大血糖波动幅度二甲双胍组及阿卡波糖组<门冬胰岛素30组.餐后血糖波动幅度则阿卡波糖组<门冬胰岛素30组.从治疗开始到达标时间门冬胰岛素30组较二甲双胍组和阿卡波糖组长,低血糖发生率3组无显著性差异,每日2次胰岛素比例二甲双胍组>阿卡波糖组>门冬胰岛素30组,达标后胰岛素日用量门冬胰岛素30组、阿卡波糖组均>二甲双胍组(P<0.05),日费用阿卡波糖组>二甲双胍组和门冬胰岛素30组.结论 单用门冬胰岛素30治疗血糖波动幅度较大,从治疗到达标所需要的时间相对较长;联合二甲双胍或阿卡波糖可以降低血糖波动幅度,减少胰岛素注射次数;联合二甲双胍可以减少胰岛素日用量.%OBJECTIVE To investigate the effect of Insulin aspart 30 alone or combined with metformin or acarbose on the glucose variability and the reach of standard conditions in patients with type 2 diabetes.METHODS The patients diagnosed type 2 diabetes were randomly divided into three groups:the Insulin aspart 30 group,the metformin group and the acarbose group,which received the treatment of Insulin aspart 30,Insulin Aspart 30+metformin and Insulin Aspart 30+aearbose respectively.The blood glucose homeostasis were maintained before meals and at bedtime,and then the blood glucose fluctuation index,the standard time

  13. Study on the reduction of postprandial blood glucose with acarbose promoted by four-combination probiotics in diabetic mice%益生菌促进阿卡波糖降低糖尿病小鼠餐后血糖的研究

    Institute of Scientific and Technical Information of China (English)

    钟丹; 殷瑜; 戈梅; 钱秀萍

    2016-01-01

    目的:研究四联益生菌对阿卡波糖降低糖尿病小鼠餐后血糖作用的影响。方法高脂饲料喂养4周的小鼠腹腔注射链脲佐菌素(STZ)造模,随机血糖大于16.7 mmol/L 即视为糖尿病造模成功。造模成功的小鼠灌胃四联益生菌(嗜酸乳杆菌、鼠李糖乳杆菌、长双歧杆菌及地衣芽孢杆菌)各109 cfu/d,3周后,考察益生菌是否具有促进阿卡波糖降低糖尿病小鼠餐后血糖的作用。并通过检测小鼠血清胆固醇、甘油三酯、胰岛素及胰高血糖素样肽-1(GLP-1)水平,研究益生菌对小鼠糖尿病的改善作用。结果单独给以低剂量阿卡波糖30 mg/kg 或四联益生菌均无明显降低餐后血糖的作用,但两者联合给药组小鼠餐后1~2 h 血糖值明显低于的糖尿病组及单独给以阿卡波糖或益生菌组。四联益生菌组小鼠血清 TG 水平明显低于糖尿病组,而 GLP-1水平则明显高于糖尿病组,两组间血清胆固醇及胰岛素无显著性差异。结论四联益生菌具有促进阿卡波糖降低糖尿病小鼠餐后血糖的作用,这种促进作用可能跟益生菌改善甘油三酯及GLP-1的水平有关。%Objective To evaluate the effect of four-combination probiotics on reducing postprandial blood glucose of acarbose in diabetic mice. Methods The mice were fed with diet enriched with high glucose and high fat, and after 4 weeks streptozotocin (STZ) was injected intraperitoneally. The criteria for the successful modelling was random blood sugar (RBS) aboved the cutoff value (16.7 mmol/L). The probiotics group mice were given orally four-combination probiotics (Lactobacillus acidophilus, L. rhamnosus, Bifidobacterium longum, Bacillus icheniformis), after 3 weeks their promotion on hypoglycemic activities to acarbose in diabetic mice were assayed. At the end of the experimental period, triglyceride, total cholesterol, insulin and GLP-1 in the plasma were determined

  14. 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。

  15. Efficacy of liraglutitude on obsese type 2diabetes patients with poor response to treatment acarbose joint premixed insulin%利拉鲁肽治疗阿卡波糖联合预混胰岛素疗效不佳的肥胖2型糖尿病患者疗效观察

    Institute of Scientific and Technical Information of China (English)

    赵艳艳; 郭丽艳

    2015-01-01

    Objective To observe the liraglutitude peptide on the application of combined premixed insulin treatment efficacy of acarbose poor clinical efficacy and safety of obese patients with type 2 diabetes.Method Selection for the application of combined premixed acarbose poor insulin treatment the curative effect of 30 cases of obese patients with type 2 diabetes in the application on the basis of acarbose and premixed insulin plus with the lalu peptide treatment for 12 weeks.Observation comparison before and after treatment of fasting blood glucose (FBG), 2 h postprandial blood glucose (2 HPBG), glycosylated hemoglobin (HbA1C), body mass index (BMI), blood lipid, adiponectin, steady state model of insulin resistance index (HOMA IR), the steady-state model islet beta cells secrete index (H0MA- beta), fasting insulin (Fins), insulin use and adverse reactions such as index.Results With the lalu peptide after 12 weeks of treatment in patients with FBG, 2 HPBG, HbA1C, TG, BMI, insulin dosage, Fins, HOMA IR were significantly lower, the difference was statistically significant (P < 0.05), adiponectin, H0MA - beta levels was significantly elevated, the difference was statistically significant (P < 0.05).The main adverse reaction of gastrointestinal reaction and low blood sugar, but both mild and short-lived.Conclusion Of acarbose and premixed insulin after combined treatment of poor blood sugar control still obese patients with type 2 diabetes, combined with the liraglutitude peptide can effectively control the blood sugar, improve blood fat, reduce weight.%目的:观察利拉鲁肽对应用阿卡波糖联合预混胰岛素治疗疗效不佳的肥胖2型糖尿病患者的临床疗效和安全性。方法:选择对应用阿卡波糖联合预混胰岛素治疗疗效不佳的肥胖2型糖尿病患者30例,在应用阿卡波糖和预混胰岛素的基础上加用利拉鲁肽治疗12周。观察比较治疗前后的空腹血糖(FBG)、餐后2h血糖(2hPBG)

  16. Systematic Review of Efficacy and Safety and Pharmacoeconomics Analysis of Acarbose versus Metformin in the Treatment of Type 2 Diabetes%阿卡波糖对比二甲双胍治疗2型糖尿病疗效与安全性的系统评价及药物经济学分析

    Institute of Scientific and Technical Information of China (English)

    2015-01-01

    OBJECTIVE:To systematically review the efficacy,safety and economy of acarbose versus metformin in the treat-ment of type 2 diabetes,and provide evidence-based reference for the clinical treatment. METHODS:Retrieved from PubMed, Medline,CJFD,Wanfang database,VIP database,randomized controlled trails (RCT) about acarbose (test group) versus metfor-min(control group)in the treatment of type 2 diabetes were collected. Meta-analysis was performed by using Rev Man 5.2 statis-tics software,and the decision tree model was used to do the cost-effectiveness analysis by using TreeAge Pro 2011.1.0.12.1 soft-ware. RESULTS:A total of 8 RCT,involving 418 patients. Results of Meta-analysis showed 2 h postprandial blood glucose (2 h PG)in test group [MD=-2.21,95%CI(-2.92,-1.51),P<0.001] was lower than that of control group,there was no signifi-cant diffcrencc in the glycated hemoglobin levels[MD=0.02,95%CI(-0.38,0.34),P=0.91],fasting blood glucose level[MD=0.05,95%CI(0.91,1.01),P=0.92] and incidence of adverse reactions [OR=1.84,95%CI(0.80,4.24),P=0.92] between 2 groups. Results of decision tree analysis showed the cost-effectiveness ratio in test group and control group was 847.15 and 272.53,respec-tively;and incremental cost-effectiveness ratio was 13 776. CONCLUSIONS:Acarbose shows an obvious advantage on decreasing the 2 h PG of type 2 diabetes,however,pharmacoeconomics shows metformin has higher economic effects. Due to the limit of methodological quality,large-scale and high quality RCT are required for further validation of the conclusions.%目的:系统评价阿卡波糖对比二甲双胍治疗2型糖尿病的有效性、安全性和经济性,以为临床治疗提供循证参考。方法:计算机检索PubMed、Medline、中国期刊全文数据库、万方数据库、中文科技期刊数据库,收集阿卡波糖(试验组)对比二甲双胍(对照组)治疗2型糖尿病的随机对照试验(RCT),提取资料并进行质量评价后,采用Rev Man 5

  17. Observation of the effect of acarbose tablets combined with insulin in the treatment of elderly patients with type 2 diabetes%阿卡波糖联合胰岛素治疗老年人2型糖尿病疗效观察

    Institute of Scientific and Technical Information of China (English)

    章卫健; 孙晓娟

    2014-01-01

    Objective To evaluate the efficacy and safety of acarbose tablets combined with protamine zinc recombinant lai pulp mixing insulin injection in the treatment of elderly patients with type 2 diabetes.Methods 170 elderly patients with type 2 diabetes were randomly divided into the observation group and the control group.85 cases in the observation group were given acarbose tablets combined with protamine zinc recombinant lai pulp mixing insulin injection,85 cases in the control group received aspart 30.The patients were followed up for 12 weeks,the blood glu cose levels,blood glucose fluctuation,glycosylated hemoglobin (HbAlc),the incidence of hypoglycemia and insulin dosage were observed.Results' The level of fasting plasma glucose (FPG) (t =9.92,P < 0.05),2h postprandial blood glucose(2hPG) (t =18.18,P <0.05),the mean blood glucose within 4h(t =13.62,P <0.05),days of average blood glucose fluctuations (t =14.56,P < 0.05) of observation group dropped significantly compared with that before treatment;HbAlc achieved rate(6.5%)of the observation group and control group were 35.29%,28.23%,re spectively,HbAlc achieved rate (7.0%) of observation group and control group were 57.64%,52.94%,the differences were not statistically significant(all P > 0.05).The dose of insulin was significantly lower in the observation group(20.11 ±3.36) u/d than(35.78 ±4.68) u/d in the control group(t =25.08,P <0.01).There were 2 cases of hypoglycemic events and 3 cases in the control group.Conclusion Protamine zinc recombinant insulin lispro injection combined with acarbose has reliable clinical efficacy and safety.%目的 评价阿卡波糖联合精蛋白锌重组赖脯胰岛素混合注射液治疗口服药失效的老年人2型糖尿病的临床疗效和安全性.方法 老年2型糖尿病患者170例,按住院号随机分为观察组(85例)和对照组(85例),观察组给予阿卡波糖联合精蛋白锌重组赖脯胰岛素混合注射液,

  18. Effect of Domestic Acarbose Combined with Glipizide on Blood Lipid and Coagulation Indicators Improvement in Type 2 Diabetic Patients%国产阿卡波糖联合格列吡嗪对2型糖尿病患者血脂、凝血指标的改善作用

    Institute of Scientific and Technical Information of China (English)

    侯保俊; 吴海燕

    2016-01-01

    异无统计学意义(P>0.05)。结论国产阿卡波糖联合格列吡嗪治疗2型糖尿病的临床疗效良好,能明显降低患者的血糖水平,控制血脂及凝血指标。%Objective To study effect of domestic acarbose combined with glipizide on blood lipid and coagulation indicators improvement in diabetic patients .Methods Total of 68 patients with type 2 diabetes in Wuhan Thirteenth Hospital from Aug.2013 to Feb.2015 were divided into an observation group and a control group according to the random number table method,34 patients in each group.The control group was treated with glipizide 5-10 mg/time,3 times a day, half an hour before meal per oral.The observation group was added with domestic acarbose on the basis of the control group′s regimen,25-50 mg each time,3 times a day,per chewing oral.After 6 months of treatment,the clinical curative effect,the blood sugar, blood fat, blood coagulation index changes from before treatment to after 3 months and 6 months of treatment,and the adverse reactions after the treatment were compared.Results After treatment,the total effective rate of the observation group was higher than the control group [91.2% (31/34) vs 70.6%(24/34)],the difference was statistically significant (P0.05).Conclusion Domestic acarbose combined with glipizide treatment on diabetic patients can significantly lower blood sugar levels and control blood lipids and coagulation indexes.

  19. 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

  20. 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

  1. Evolution toward small molecule inhibitor resistance affects native enzyme function and stability, generating acarbose-insensitive cyclodextrin glucanotransferase variants

    NARCIS (Netherlands)

    Kelly, Ronan M.; Leemhuis, Hans; Gatjen, Linda; Dijkhuizen, Lubbert; Gätjen, Linda

    2008-01-01

    Small molecule inhibitors play an essential role in the selective inhibition of enzymes associated with human infection and metabolic disorders. Targeted enzymes may evolve toward inhibitor resistance through selective incorporation of mutations. Acquisition of insensitivity may, however, result in

  2. Evolution toward small molecule inhibitor resistance affects native enzyme function and stability, generating acarbose-insensitive cyclodextrin glucanotransferase variants

    NARCIS (Netherlands)

    Kelly, Ronan M.; Leemhuis, Hans; Gatjen, Linda; Dijkhuizen, Lubbert; Gätjen, Linda

    2008-01-01

    Small molecule inhibitors play an essential role in the selective inhibition of enzymes associated with human infection and metabolic disorders. Targeted enzymes may evolve toward inhibitor resistance through selective incorporation of mutations. Acquisition of insensitivity may, however, result in

  3. 阿卡波糖与二甲双胍治疗2型糖尿病的成本-疗效分析%Cost-effectiveness analysis of acarbose and metformin for the treatment of type 2 diabetes mellitus

    Institute of Scientific and Technical Information of China (English)

    吴赛君; 吴皖

    2014-01-01

    目的 比较阿卡波糖与二甲双胍治疗2型糖尿病的成本-疗效,选择符合药物经济学的药物.方法 147例门诊2型糖尿病患者按治疗方法分为阿卡波糖组(n=69)与二甲双胍组(n=78),分别接受阿卡波糖片(50mg/次,3次/d)和二甲双胍片(0.5g/次,3次/d)口服治疗12周.药物经济学评价以成本(C)/疗效(E)比值表示.结果 2组治疗后的空腹血糖(FPG)和餐后2h血糖(2hPG)均明显下降,与治疗前比较差异均有统计学意义(P<0.05),但治疗前及治疗后2组间FPG和2hPG比较差异无统计学意义(P>0.05).以FPG作为评价指标,二甲双胍组和阿卡波糖组总有效率分别为87.18%和84.06%,差异无统计学意义(P>0.05),C/E比值分别为5.06元和7.59元.以2hPG作为评价指标,二甲双胍组和阿卡波糖组总有效率分别为88.46%和82.61%,差异无统计学意义(P>0.05),C/E比值分别为4.99元和7.73元.结论 二甲双胍治疗2型糖尿病比阿卡波糖更经济,符合药物经济学原则.

  4. 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

  5. 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.

  6. Inhibitory effect of rhubarb on intestinal α-glucosidase activity in type ...

    African Journals Online (AJOL)

    Keywords: Type 1 diabetes, α-Glucosidase activity, Acarbose®, Rhubarb, Postprandial glucose level ... intestinal absorption of carbohydrates [3]. Type 1 diabetes, which is caused by insulin deficiency ... novel drugs with high activity and low.

  7. 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 ...

  8. 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...

  9. Effects of alpha-glucosidase inhibitors on mouth to caecum transit time in humans.

    OpenAIRE

    Ladas, S D; Frydas, A; Papadopoulos, A.; S. A. Raptis

    1992-01-01

    The alpha-glucosidase inhibitors acarbose and miglitol have been successfully used to control postprandial hyperglycaemia in diabetics. They probably work by slowing carbohydrate digestion and absorption, but their effect on mouth to caecum transit time has not been studied. The effect acarbose (100 mg), miglitol (100 mg), and placebo on mouth to caecum transit time (380 kcal breakfast with 20 g of lactulose) was investigated in 18 normal volunteers using breath hydrogen analysis. Both miglit...

  10. Enzyme analysis for Pompe disease in leukocytes; superior results with natural substrate compared with artificial substrates.

    Science.gov (United States)

    van Diggelen, O P; Oemardien, L F; van der Beek, N A M E; Kroos, M A; Wind, H K; Voznyi, Y V; Burke, D; Jackson, M; Winchester, B G; Reuser, A J J

    2009-06-01

    Enzyme analysis for Pompe disease in leukocytes has been greatly improved by the introduction of acarbose, a powerful inhibitor of interfering alpha-glucosidases, which are present in granulocytes but not in lymphocytes. Here we show that the application of acarbose in the enzymatic assay employing the artificial substrate 4-methylumbelliferyl-alpha-D: -glucoside (MU-alphaGlc) is insufficient to clearly distinguish patients from healthy individuals in all cases. Also, the ratios of the activities without/with acarbose only marginally discriminated Pompe patients and healthy individuals. By contrast, when the natural substrate glycogen is used, the activity in leukocytes from patients (n = 82) with Pompe disease is at most 17% of the lowest control value. The use of artificial substrate in an assay with isolated lymphocytes instead of total leukocytes is a poor alternative as blood samples older than one day invariably yield lymphocyte preparations that are contaminated with granulocytes. To diagnose Pompe disease in leukocytes we recommend the use of glycogen as substrate in the presence of acarbose. This assay unequivocally excludes Pompe disease. To also exclude pseudo-deficiency of acid alpha-glucosidase caused by the sequence change c.271G>A (p.D91N or GAA2; homozygosity in approximately 1:1000 caucasians), a second assay employing MU-alphaGlc substrate plus acarbose or DNA analysis is required.

  11. Role of metabolic control on diabetic nephropathy

    Directory of Open Access Journals (Sweden)

    Macedo Célia Sperandéo

    2002-01-01

    Full Text Available OBJECTIVE: The aim of this investigation was studying the influence of glucose metabolic control on diabetic nephropathy. The authors observed the effect of acarbose, insulin, and both drugs on the metabolic control and development of mesangial enlargement of kidney glomeruli in alloxan-diabetic rats. METHODS: Five groups of Wistar rats were used: normal rats (N, non-treated alloxan-diabetic rats (D, alloxan-diabetic rats treated with acarbose (AD, alloxan-diabetic rats treated with insulin (ID, and alloxan-diabetic rats treated with insulin plus acarbose (IAD. The following parameters were evaluated: body weight; water and food intake; diuresis; blood and urine glucose levels; and the kidney lesions: mesangial enlargement and tubule cell vacuolization. Renal lesions were analysed using a semi-quantitative score 1, 3, 6, 9, and 12 months after diabetes induction. RESULTS: Diabetic rats showed a marked increase of glycemia, urinary glucose levels, diuresis, water and food intake, and weight loss, while the treated diabetic rats showed significant decreased levels of these parameters. The most satisfactory metabolic control was that of diabetic rats treated with acarbose + insulin. There was a significant mesangial enlargement in diabetic rats compared to normal rats from the third up to the 12th month after diabetes induction, with a significant difference between the animals treated with acarbose + insulin and non-treated diabetic rats. A difference between the animals treated with acarbose or insulin alone and non-treated diabetics rats was not seen. CONCLUSIONS: The authors discuss the results stressing the role of diabetic metabolic control in the prevention of diabetic nephropathy.

  12. A new diagnostic assay for glycogen storage disease type II in mixed leukocytes.

    Science.gov (United States)

    Okumiya, Toshika; Keulemans, Joke L M; Kroos, Marian A; Van der Beek, Nadine M E; Boer, Marijke A; Takeuchi, Hiroaki; Van Diggelen, Otto P; Reuser, Arnold J J

    2006-05-01

    We have established a new method for the enzymatic diagnosis of glycogen storage disease type II (Pompe disease or acid maltase deficiency) using mixed leukocytes. The method employs glycogen and 4-methylumbelliferyl-alpha-D-glucopyranoside (4MU-alphaGlc) as substrates for measuring the lysosomal acid alpha-glucosidase (acid alphaGlu) activity, and incorporates acarbose to eliminate the interference of unrelated alpha-glucosidases (predominantly maltase-glucoamylase). It is shown that 3.0 micromol/L acarbose completely inhibits the maltase-glucoamylase activity at pH 4.0, but the lysosomal acid alphaGlu activity by less than 5%. With this method, we determined the acid alphaGlu activity in mixed leukocytes from 25 patients with glycogen storage disease type II (2 infantile and 23 late-onset cases), one GAA2/GAA2 homozygote and 30 healthy subjects. In the assay with glycogen as substrate, the addition of acarbose created a clear separation between the patient and the control ranges. In the assay with 4MU-alphaGlc as substrate, the two ranges were fully separated but remained very close despite the use of acarbose. The separation of the patient and normal ranges was improved considerably by taking the ratio of acarbose-inhibited over uninhibited activity. A GAA2/GAA2 homozygote was correctly diagnosed with 4MU-alphaGlc but misdiagnosed as patient when glycogen was used as substrate. We conclude that the inclusion of 3.0 micromol/L acarbose in the assays with glycogen and 4MU-alphaGlc substrates at pH 4.0 allows for the specific measurement of lysosomal acid alphaGlu activity in mixed leukocytes, thus enabling a reliable diagnosis of glycogen storage disease type II in this specimen.

  13. The influence of hypoglycemic drugs on exercise-mediated hypoglycemic effects in elderly type 2 diabetic patients

    Science.gov (United States)

    Xu, Qin; Wang, Fengdi; Wu, Yuemei; Li, Feng

    2015-01-01

    Background: To evaluate the impact of different hypoglycemic drugs on exercise-mediated blood glucose (BG) reduction. Methods: One-hundred and five retirees who were diagnosed with type 2 diabetes mellitus (T2DM) within a two-year period were included in this study. The participants were instructed to walk for 20 to 30 minutes at a moderate-speed (4.0 to 4.5 km/h) after breakfast. Blood pressure and fingertip BG were measured before and after walking. Results: The rate of BG reduction was significantly higher in all exercise groups when compared to that of non-exercised patients. Among all groups, BG declined the most in the un-medicated group, while the lowest BG reduction was observed in the acarbose group. Surprisingly, the BG reduction in acarbose group was significantly lower when compared with non-acarbose groups (P<0.0001). Interestingly, after further correcting for sex, age, BMI, diabetes history, walking time, walking speed and walking distance, only age was found to be an influencing factor (t=-3.304, P=0.001). Pearson correlation of age and BG reduction showed that correlation coefficient of age was only 0.183 and revealed no statistical significance. Conclusions: Walking at a moderate speed for 20 to30 minutes after breakfast provided a beneficial BG reduction effect in elderly T2DM patients. Among the medicated groups, the smallest BG reduction rate was observed in patients taking acarbose. We suggest that acarbose might influence hypoglycemic effects of exercise. The results of this study will be helpful for determining the best clinical usage of hypoglycemic medications in elderly T2DM patients. PMID:26550367

  14. 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.

  15. Cuminaldehyde: Aldose Reductase and alpha-Glucosidase Inhibitor Derived from Cuminum cyminum L. Seeds.

    Science.gov (United States)

    Lee, Hoi-Seon

    2005-04-06

    The inhibitory activity of Cuminum cyminum seed-isolated component was evaluated against lens aldose reductase and alpha-glucosidase isolated from Sprague-Dawley male rats and compared to that of 11 commercially available components derived from C. cyminum seed oil, as well as quercitrin as an aldose reductase inhibitor and acarbose as an alpha-glucosidase inhibitor. The biologically active constituent of C. cyminum seed oil was characterized as cuminaldehyde by various spectral analyses. The IC(50) value of cuminaldehyde is 0.00085 mg/mL against aldose reductase and 0.5 mg/mL against alpha-glucosidase, respectively. Cuminaldehyde was about 1.8 and 1.6 times less in inhibitory activity than acarbose and quercitin, respectively. Nonetheless, cuminaldehyde may be useful as a lead compound and a new agent for antidiabetic therapeutics.

  16. Segmental pneumatosis cystoides coli: computed tomography-facilitated diagnosis

    Directory of Open Access Journals (Sweden)

    Dorota Ksiadzyna

    Full Text Available Background: Intestinal pneumatosis is a rare entity of unclear etiopathogenesis characterized by the presence of gaseous cystic or linear collections within the intestinal wall. Intestinal pneumatosis may be primary and idiopathic in origin or, more frequently, it accompanies various clinical conditions. Rarely, the development of intestinal pneumatosis is attributed to the pharmacotherapy with different drugs. Case report: This is a case report of cystic pneumatosis limited to the large intestine with predominant clinical presentation of chronic watery diarrhea in a 64-year-old man suffering from diabetes mellitus treated with metformin and acarbose. The patient had been referred to the outpatient gastroenterology clinic for further investigation of numerous polyp-like lesions found on colonoscopy. There was no history of cigarette smoking, drug abuse or extraintestinal complaints. The patient was in a good general condition and his laboratory tests were normal. No relevant abnormalities were found on chest X-ray, esophagogastroduodenoscopy or abdominal ultrasound, but computed tomography showed intramural gas-filled bubbles in the cecum and splenic flexure without signs of perforation or any other significant pathology in the abdominal cavity. The final diagnosis of pneumatosis cystoides coli (PCC, possibly related to treatment with acarbose, was established. On a follow-up visit after discontinuation of acarbose the patient reported no complaints and remained asymptomatic for the next 12 months. Discussion: To conclude, drug-related PCC should be considered in a differential diagnosis of gastrointestinal symptoms and/or polyp-like lesions disclosed on colonoscopy in diabetic patients treated with acarbose.

  17. Liver alpha-amylase gene expression as an early obesity biomarker.

    Science.gov (United States)

    Mojbafan, Marzieh; Afsartala, Zohreh; Amoli, Mahsa M; Mahmoudi, Mahdi; Yaghmaei, Parichehreh; Larijani, Bagher; Ebrahim-Habibi, Azadeh

    2017-04-01

    Obesity is a major health problem worldwide, for which preventive and therapeutic means are still needed. Alpha-amylase is a digestive enzyme whose inhibition has been targeted as a potential anti-obesity strategy. However, alpha-amylase gene expression has not been particularly attended to, and in contrast with pancreatic and salivary amylases, fewer studies have focused on liver alpha-amylase. The present study aimed at investigating the expression of alpha-amylase gene in obese and normal mice at RNA and protein level as well as acarbose effect on this gene expression in hepatocyte cell culture. Control and case groups were fed by normal mouse pellet and high-fat diet respectively, during 8 weeks. After this period, serum biochemical parameters including glucose, cholesterol, triglycerides, AST, ALT and alpha-amylase were assayed. Liver alpha-amylase gene was analyzed by real time PCR, and liver enzyme was assayed with Bernfeld and ELISA methods Hepatocyte cell culture derived from both group were also treated by acarbose and alpha-amylase activity and gene expression was analyzed by above mentioned methods. All biochemical factors showed an increase in obese mice, but the increase in ALT and AST were not statistically significant. Alpha-amylase levels were also increased in obese mice, both at RNA and protein level, while a decrease was seen in obese mice derived hepatocytes after acarbose treatment. Elevated liver alpha-amylase levels may be indicative of initial stages of obesity and the use of acarbose could be considered as a treatment of obesity which could be potentially effective at multiple levels. Copyright © 2016. Published by Elsevier Urban & Partner Sp. z o.o.

  18. 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).

  19. Inhibitory Effect of Heracleum persicum and Ziziphus jujuba on Activity of Alpha-Amylase

    Directory of Open Access Journals (Sweden)

    Reza Afrisham

    2015-01-01

    Full Text Available Postprandial hyperglycemia plays an important role in the development of type 2 diabetes. Inhibition of alpha-amylase was led to a delay in breaks down of starch and glycogen and prevented a rapid rise in blood sugar. Alpha-amylase was isolated by gel filtration chromatography Sephadex G-75 from bovine pancreas. Then, total methanolic extracts of plants were prepared and IC50 values of extracts on alpha-amylase were obtained and compared with acarbose IC50. The polyphenolic content of extracts and antioxidant capacity were determined by Folin-Ciocalteu test and DPPH test, respectively. The specific activity of alpha-amylase was 48.2 U/mg. For inhibition of alpha-amylase, IC50 values of H. persicum, Z. jujuba, and acarbose were 307, 827, and 113 μg/ml, respectively. For inhibition of DPPH radical, IC50 values of extracts were 235 and 701 μg/ml. Total phenolic contents of methanol extracts were 73.8±3.2 and 44.2±1.8 μg tannic acid equivalent/mg extract. Acarbose causes gastrointestinal symptoms and liver toxicity, but H. persicum and Z. jujuba decrease these side effects and prevent gastrointestinal disorders. Due to the high polyphenolic content and antioxidant capacity of these plants and significant inhibitory effect of the plants on alpha-amylase, these plants can be proposed for treatment of diabetic patients.

  20. Effects of alpha-glucosidase inhibitors on mouth to caecum transit time in humans.

    Science.gov (United States)

    Ladas, S D; Frydas, A; Papadopoulos, A; Raptis, S A

    1992-09-01

    The alpha-glucosidase inhibitors acarbose and miglitol have been successfully used to control postprandial hyperglycaemia in diabetics. They probably work by slowing carbohydrate digestion and absorption, but their effect on mouth to caecum transit time has not been studied. The effect acarbose (100 mg), miglitol (100 mg), and placebo on mouth to caecum transit time (380 kcal breakfast with 20 g of lactulose) was investigated in 18 normal volunteers using breath hydrogen analysis. Both miglitol and acarbose significantly increased breath hydrogen excretion (F2,34 = 6.31, p = 0.005) and shortened the mouth to caecum transit time (F2,34 = 3.49, p = 0.04) after breakfast compared with placebo. There was a significant negative correlation between breath hydrogen excretion and mouth to caecum transit time suggesting that with shorter transit times significantly more carbohydrates were spilled into the colon. These results indicate that alpha-glucosidase inhibitors accelerate mouth to caecum transit time by inducing carbohydrate malabsorption.

  1. Effective Control of Postprandial Glucose Level through Inhibition of Intestinal Alpha Glucosidase by Cymbopogon martinii (Roxb.

    Directory of Open Access Journals (Sweden)

    Varsha Ghadyale

    2012-01-01

    Full Text Available Inhibition of intestinal alpha glucosidase plays a major role in preventing rise in postprandial glucose level in diabetics. Cymbopogon martinii (CM (family Poaceae is used in traditional Indian medicine in treatment of diabetes mellitus. The alpha glucosidase inhibitory action of the plant is studied. The active component was separated using hot water extraction of the whole plant powder, differential solvent extraction, and silica gel column chromatography. The 30 : 70 toluene : ethyl acetate fraction showed optimum activity. The silica gel chromatography fraction demonstrated 98, 98, and 68% inhibition for starch, maltose, and sucrose, respectively, at 5 mg/kg body weight of rats. Intestinal absorption studies using noneverted intestinal sacs, as well as in vivo studies in streptozotocin-induced diabetic rats using oral glucose tolerance with maltose and sucrose load, revealed better inhibition of alpha glucosidase as compared to acarbose. Kinetic studies using Lineweaver Burk plot showed mixed to noncompetitive type of inhibition by CM. In vivo studies with maltose load of 2 mg and 3 mg/gm body weight showed a noncompetitive pattern of inhibition at 5 mg/kg body weight of CM as against 60 mg/kg body weight of acarbose. Thus CM is more effective alpha glucosidase inhibitor and at lower concentration than acarbose.

  2. Inhibition of Porcine Pancreatic Amylase Activity by Sulfamethoxazole: Structural and Functional Aspect.

    Science.gov (United States)

    Maity, Sujan; Mukherjee, Koel; Banerjee, Amrita; Mukherjee, Suman; Dasgupta, Dipak; Gupta, Suvroma

    2016-06-01

    Combating Type-2 diabetes mellitus is a pivotal challenge in front of the present world. Several lines of therapy are in practice for resisting this deadly disease which often culminates with cardiovascular complexities, neuropathy and retinopathy. Among various therapies, administration of alpha glucosidase inhibitors is common and widely practiced. Sulfonylurea category of anti diabetic drug often suffers from cross reactivity with sulfamethoxazole (SMX), a common drug in use to treat a handful of microbial infections. However the specific cellular target generating postprandial hypoglycemia on SMX administration is till date unraveled. The present work has been initiated to elucidate the effects of a group of sulfonamide drugs inclusive of SMX for their amylase inhibitory role. SMX inhibits porcine pancreatic amylase (PPA) in a noncompetitive mode with an average IC50 value 0.94 mM respectively. Interaction of SMX with PPA is manifested with gradual quenching of tryptophan fluorescence with concomitant shift in lambda max value (λmax). Binding is governed by entropy driven factor (24.8 cal mol(-1) K(-1)) with unfavorable contribution from enthalpy change. SMX interferes with the activity of acarbose in a synergistic mode to reduce the effective dose of acarbose as evident from the in vitro PPA inhibition study. In summary, loss of PPA activity in presence of SMX is indicative of structural changes of PPA which is further augmented in the presence of acarbose as explained in the schematic model and docking study.

  3. 两种治疗2型糖尿病联合用药方案的费用-效果分析%Analysis on treatment cost-effect of type 2 diabetes in two combination schemes

    Institute of Scientific and Technical Information of China (English)

    樊玉霞

    2011-01-01

    目的:探讨两种常用的联合用药方案对2型糖尿病的治疗效果和经济效果.方法:选择2型糖尿病患者100例,随机分为A、B两组,每组50例,分别运用混人胰岛素联合阿卡波糖和阿卡波糖联合二甲双胍进行治疗,并对其进行费用-效果分析.结果:A组的总有效率为86%,B组的有效率为92%,两种治疗方案具有相似的临床疗效,但阿卡波糖联合二甲双胍治疗方案的费用为235.48元,明显低于应用混人胰岛素联合阿卡波糖治疗方案的费用(389.10元),差异具有统计学意义(P<0.05),更具有经济学价值.结论:从药物经济学考虑,两种方案中阿卡波糖联合二甲双胍治疗方案在社区治疗2型糖尿病中更为理想,值得推广.%Objective: To discuss the treatment effect -economic effect by using two combination schemes for type 2 diabetes. Methods: 100 patients with type 2 diabetes were selected and randomly divided into group A and group B, each group had 50 cases. Two groups were respectively used mixed human insulin jointed with Acarbose and Acarbose jointed with Metformin to treat type 2 diabetes. Treatment cost-effect were analysed. Results: The total effective rate of group A was 86%, total effective rate of group B was 92%, two treatment programs had similar clinical efficacy, the cost of Acarbose jointed with Metformin was 235.48 yuan, which was significantly lower than the cost of mixed human insulin jointed with Acarbose (389.10 yuan). There was a statistically significant difference (P<0.05), and had more economic value. Conclusion: Acarbose jointed with Metformin to treat type 2 diabetes is worthy to application in the community with its ideal effect from consideration of the drug economics.

  4. 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.

  5. Characterization of a Digestive α-Amylase in the Midgut of Pieris brassicae L. (Lepidoptera: Pieridae)

    Science.gov (United States)

    Sharifloo, Ali; Zibaee, Arash; Sendi, Jalal J.; Jahroumi, Khalil Talebi

    2016-01-01

    The current study deals with a digestive α-amylase in the larvae of Pieris brassicae L. through purification, enzymatic characterization, gene expression, and in vivo effect of a specific inhibitor, Acarbose. Although α-amylase activity was the highest in the whole gut homogenate of larvae but compartmentalization of amylolytic activity showed an equal activity in posterior midgut (PM) and anterior midgut (AM). A three step purification using ammonium sulfate, Sepharyl G-100 and DEAE-Cellulose Fast flow revealed an enzyme with a specific activity of 5.18 U/mg, recovery of 13.20, purification fold of 19.25 and molecular weight of 88 kDa. The purified α-amylase had the highest activity at optimal pH and temperature of 8 and 35°C. Also, the enzyme had Vmax values of 4.64 and 3.02 U/mg protein and Km values of 1.37 and 1.74% using starch and glycogen as substrates, respectively. Different concentrations of acarbose, ethylenediamine tetraacetic acid, and ethylene glycol-bis (β-aminoethylether) N, N, N′, N′-tetraacetic acid significantly decreased activity of the purified α-amylase. The 4th instar larvae of P. brassicae were fed on the treated leaves of Raphanus sativus L. with 0.22 mM of Acarbose to find in vivo effects on nutritional indices, α-amylase activity, and gene expression. The significant differences were only found in conversion efficiency of digested food, relative growth rate, and metabolic cost of control and fed larvae on Acarbose. Also, amylolytic activity significantly decreased in the treated larvae by both biochemical and native-PAGE experiments. Results of RT-PCR revealed a gene with 621 bp length responsible for α-amylase expression that had 75% identity with Papilio xuthus and P. polytes. Finally, qRT-PCR revealed higher expression of α-amylase in control larvae compared to acarbose-fed ones. PMID:27014094

  6. 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

  7. 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.

  8. In vitro α-glucosidase and α-amylase inhibition by aqueous, hydroalcoholic, and alcoholic extract of Euphorbia hirta L.

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    Manjur Ali Sheliya

    2016-01-01

    Full Text Available Background: Euphorbia hirta L. (Euphorbiaceae, commonly known as Dudhani, is distributed in the warm region of India and China. Traditionally, it is used in respiratory and gastrointestinal disorders. In addition, the antidiabetic property of the plant was also reported in the literature. This study was designed to evaluate the effect of aqueous, hydroalcoholic, and methanolic extracts (MEHs of E. hirta on α-glucosidase and α-amylase in vitro. Materials and Methods: Aqueous, hydroalcoholic, and MEHs of E. hirta were prepared as per application program interface. In α-glucosidase activity, α-glucosidase (0.1 μ/mL and substrate, 2.5 mM p-nitrophenyl-α-D-glucopyranoside was used; absorbance was recorded at 405 nm. In α-amylase activity, α-amylase solution (1.0 μ/mL and substrate, 0.25% starch were used, and absorbance was measured at 540 nm. The IC50values were calculated by linear regression. Results: All the extracts showed α-glucosidase inhibitory activity comparable to acarbose with MEH having highest inhibitory activity among tested extracts. The observed IC50values were 213.63, 146.9, 78.88, and 8.07 μg/mL for aqueous, hydroalcoholic, MEH, and acarbose, respectively. All the extracts have shown mild α-amylase inhibitory activity compared to acarbose. Lineweaver–Burk plot has shown that the MEH is a mixed noncompetitive inhibitor for α-glucosidase enzyme. Conclusion: The results from this in vitro study clearly indicated that MEH of E. hirta had strong inhibitory activity against α-glucosidase and mild inhibitory activity against α-amylase. It can be used for management of postprandial hyperglycemia with lesser side effects, and provide a strong rationale for further animal and clinical studies.

  9. Hypoglycemic Effects of Three Medicinal Plants in Experimental Diabetes: Inhibition of Rat Intestinal α-glucosidase and Enhanced Pancreatic Insulin and Cardiac Glut-4 mRNAs Expression.

    Science.gov (United States)

    Moradabadi, Leila; Montasser Kouhsari, Shideh; Fehresti Sani, Mohammad

    2013-01-01

    Garlic (Allium sativum L., Alliaceae), Persian shallot (Allium ascalonicum L., Alliaceae ) and Sage (Salvia officinalis L., Lamiaceae) are believed to have hypoglycemic properties and have been used traditionally as antidiabetic herbal medicines in Iran. In this study, diabetes was induced by subcutaneous injection of alloxan monohydrate (100 mg kg(-1)) to male Wistar rats. Antidiabetic effects of methanolic extracts of the above mentioned three plants on alloxan-diabetic rats was investigated in comparison with the effects of antidiabetic drugs such as acarbose, glibenclamide and metformin by measuring postprandial blood glucose (PBG), oral glucose tolerance test (OGTT), inhibition of rat intestinal α-glucosidase enzymes activities and pancreatic Insulin and cardiac Glut-4 mRNAs expression. In short term period, hypoglycemic effects of A. sativum and A. ascalonicum showed significant reduction of PBG similar to glibenclamide (5 mg kg(-1) bw) while S. officinalis significantly reduced PBG similar to acarbose (20 mg kg(-1) bw). After 3 weeks of treatment by methanolic plant extracts, significant chronic decrease in the PBG was observed similar to metformin (100 mg kg(-1) bw). For OGTT, S. officinalis reduced PBG in a similar way as acarbose (20 mg kg(-1) bw). Intestinal sucrase and maltase activities were inhibited significantly by A. sativum, A. ascalonicum and S. officinalis. In addition, we observed increased expression of Insulin and Glut-4 genes in diabetic rats treated with these plants extracts. Up regulation of Insulin and Glut-4 genes expression and inhibition of α-glucosidaseactivities are the two mechanisms that play a considerable role in hypoglycemic action of garlic, shallot and sage.

  10. 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.

  11. Development and validation of HPLC-UV-MS method for the control of four anti-diabetic drugs in suspected counterfeit products.

    Science.gov (United States)

    Dai, Xiu-mei; An, Ning; Wu, Jian-min; Li, Hui-yi; Zhang, Qi-ming

    2010-03-01

    An HPLC-UV method has been developed for the determination of valibose, miglitol, voglibose and acarbose, the four anti-diabetic drugs. The separation was accomplished successfully by using reversed phase chromatography (Prevail carbohydrate column, 250 mm x 4.6 mm, 5 microm) with a gradient acetonitrile-phosphate buffer solution (pH 8.0) at a wavelength of 210 nm. Furthermore, the method of a high-performance liquid chromatography coupled with ESI-MS in positive ionization mode has been established. These two methods were successfully applied to the assay and qualitative detection of four alpha-glucosidase inhibitors in the potential counterfeit anti-diabetic drugs.

  12. 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.

  13. [Development of alpha-glucosidase inhibitor from medicinal herbs].

    Science.gov (United States)

    Ji, Fang; Xiao, Guochun; Dong, Li; Ma, Zijiao; Ni, Jingman

    2010-06-01

    Alpha-glucosidase inhibitor can reduce the postprandial hyperglycemia and have good effect on preventing and treating the diabetes and diabetic complication. Along with the application of acarbose which is a kind of alpha-glucosidase inhibitor, many research groups pay attention to the crude alpha-glucosidase inhibitor screened from the medicinal herbs in order to find new, safe, and effective medicine. The development of alpha-glucosidase inhibitor screened from the medicinal herbs and its evaluation in vivo and vitro as well as the varieties of the medicinal herbs that contain alpha-glucosidase inhibitor in recent 30 years were summarized in this paper.

  14. 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...

  15. 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.

  16. Inhibitory Properties of Aqueous Ethanol Extracts of Propolis on Alpha-Glucosidase

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    Hongcheng Zhang

    2015-01-01

    Full Text Available The objective of the present study was to evaluate the inhibitory properties of various extracts of propolis on alpha-glucosidase from baker’s yeast and mammalian intestine. Inhibitory activities of aqueous ethanol extracts of propolis were determined by using 4-nitrophenyl-D-glucopyranoside, sucrose and maltose as substrates, and acarbose as a positive reference. All extracts were significantly effective in inhibiting α-glucosidase from baker’s yeast and rat intestinal sucrase in comparison with acarbose (P<0.05. The 75% ethanol extracts of propolis (75% EEP showed the highest inhibitory effect on α-glucosidase and sucrase and were a noncompetitive inhibition mode. 50% EEP, 95%, EEP and 100% EEP exhibited a mixed inhibition mode, while water extracts of propolis (WEP and 25% EEP demonstrated a competitive inhibition mode. Furthermore, WEP presented the highest inhibitory activity against maltase. These results suggest that aqueous ethanol extracts of propolis may be used as nutraceuticals for the regulation of postprandial hyperglycemia.

  17. Evaluation of anti-diabetic and alpha glucosidase inhibitory action of anthraquinones from Rheum emodi.

    Science.gov (United States)

    Arvindekar, Aditya; More, Tanaji; Payghan, Pavan V; Laddha, Kirti; Ghoshal, Nanda; Arvindekar, Akalpita

    2015-08-01

    Rheum emodi is used as a culinary plant across the world and finds an eminent role in the Ayurvedic and traditional Chinese systems of medicine. The plant is known to principally contain 1,8-dihydroxyanthraquinones (DHAQs) like rhein, aloe emodin, emodin, chrysophanol and physcion that possess diverse pharmacological and therapeutic actions. The present work deals with developing a platform technology for isolation of these DHAQs and evaluating their anti-diabetic potential. Herein, we report the anti-hyperglycemic activity and alpha glucosidase (AG) inhibitory actions of five isolated DHAQs from R. emodi. All the five isolated DHAQs showed good anti-hyperglycemic activity with aloe emodin exhibiting maximum lowering of blood glucose in an oral glucose tolerance test. However, on evaluation of the AG inhibitory potential of the DHAQs only emodin exhibited potent intestinal AG inhibition (93 ± 2.16%) with an IC50 notably lower than acarbose. Subsequent kinetic studies indicated a mixed type of inhibition for emodin. In vivo studies using oral maltose load showed almost total inhibition for emodin when compared to acarbose. Molecular docking studies revealed the presence of an allosteric topographically distinct 'quinone binding site' and showed that interaction with Ser 74 occurs exclusively with emodin, which is vital for AG inhibition. The net benefit from the glucose lowering effect and mixed type inhibition by emodin would enable the administration of a small dosage that is safe and non-toxic in the case of prolonged use in treating diabetes.

  18. 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.

  19. Physicochemical Characterisation of Polysaccharides from the Seeds and Leaves of Miracle Fruit (Synsepalum dulcificum and Their Antioxidant and α-Glucosidase Inhibitory Activities In Vitro

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    Huajun Jian

    2017-01-01

    Full Text Available Miracle fruit (Synsepalum dulcificum has been well known and studied for its unique taste-modifying ability. In this study, the monosaccharide composition, molecular weight (Mw, and in vitro bioactivities (antioxidant, α-glucosidase inhibition of polysaccharides from the seeds (MFP-S and leaves (MFP-L of miracle fruit were investigated. The results showed that MFP-S was a homogeneous polysaccharide (Mw 2804 Da with glucose. MFP-L displayed three fractions (92093, 1496, and 237 Da consisting of rhamnose, arabinose, galactose, glucose, and xylose. Moreover, the antioxidant and α-glucosidase inhibition of MFP-L were significantly greater than those of MFP-S. The α-glucosidase inhibition of MFP-L was remarkably better than the positive control, acarbose (an antidiabetes drug. More specifically, the 50% inhibitory concentration (IC50 values of α-glucosidase activities for MFP-S, MFP-L, and acarbose were 33, 0.01, and 1 mg mL−1, separately. Therefore, MFP-L can be developed as a functional factor with both antioxidant and antidiabetes activities in food applications.

  20. Inhibitory potential of fatty acids on key enzymes related to type 2 diabetes.

    Science.gov (United States)

    Su, Chun-Han; Hsu, Chun-Hua; Ng, Lean-Teik

    2013-01-01

    This study aimed to examine the inhibitory mechanisms of fatty acids on key enzymes related to type 2 diabetes, and their effects on starch digestion rate. Among the 10 fatty acids analyzed, oleic acid showed the strongest anti-α-glucosidase activity, followed by linoleic acid, and their activities were more potent than acarbose, but they possessed a weaker anti-α-amylase activity. Kinetic assays demonstrated that oleic acid and linoleic acid were competitive inhibitors, and their interactions with α-glucosidase exhibited a character of static quenching, which indicates that they would bind to α-glucosidase to form a complex. However, they had little effects on the secondary structures of α-glucosidase. In vitro study showed that oleic acid and linoleic acid were more potent than acarbose in inhibiting starch digestion. Taken together, these results conclude that oleic acid and linoleic acid possess potent inhibitory effects on α-glucosidase activity. Copyright © 2013 International Union of Biochemistry and Molecular Biology, Inc.

  1. 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

    Science.gov (United States)

    Mahomoodally, M. Fawzi; Subratty, A. Hussein; Gurib-Fakim, A.; Choudhary, M. Iqbal; Nahar Khan, S.

    2012-01-01

    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. PMID:22654584

  2. Isatin based Schiff bases as inhibitors of α-glucosidase: Synthesis, characterization, in vitro evaluation and molecular docking studies.

    Science.gov (United States)

    Rahim, Fazal; Malik, Fazal; Ullah, Hayat; Wadood, Abdul; Khan, Fahad; Javid, Muhammad Tariq; Taha, Muhammad; Rehman, Wajid; Ur Rehman, Ashfaq; Khan, Khalid Mohammed

    2015-06-01

    Isatin base Schiff bases (1-20) were synthesized, characterized by (1)H NMR and EI/MS and evaluated for α-glucosidase inhibitory potential. Out of these twenty (20) compounds only six analogs showed potent α-glucosidase inhibitory potential with IC50 value ranging in between 2.2±0.25 and 83.5±1.0μM when compared with the standard acarbose (IC50=840±1.73μM). Among the series compound 2 having IC50 value (18.3±0.56μM), 9 (83.5±1.0μM), 11 (3.3±0.25μM), 12 (2.2±0.25μM), 14 (11.8±0.15μM), and 20 (3.0±0.15μM) showed excellent inhibitory potential many fold better than the standard acarbose. The binding interactions of these active analogs were confirmed through molecular docking.

  3. Oligomeric procyanidins of French maritime pine bark extract (Pycnogenol) effectively inhibit alpha-glucosidase.

    Science.gov (United States)

    Schäfer, Angelika; Högger, Petra

    2007-07-01

    The standardized maritime pine bark extract (Pycnogenol) was reported to exert clinical anti-diabetic effects after peroral intake. However, an increased insulin secretion was not observed after administration of the extract to patients. Our aim was to elucidate whether the described clinical effects of Pycnogenol are related to inhibition of alpha-glucosidase. Therefore, we analyzed the inhibitory activity of Pycnogenol, green tea extract and acarbose towards alpha-glucosidase. Furthermore, we explored different fractions of Pycnogenol containing compounds of diverse molecular masses from polyphenolic monomers, dimers and higher oligomers to uncover which components exhibited the most pronounced inhibitory activity. We found that Pycnogenol exhibited the most potent inhibition (IC(50) about 5 microg/mL) on alpha-glucosidase compared to green tea extract (IC(50) about 20 microg/mL) and acarbose (IC(50) about 1mg/mL). The inhibitory action of Pycnogenol was stronger in extract fractions containing higher procyanidin oligomers. The results obtained assign a novel, local effect to oligomeric procyanidins and contribute to the explanation of glucose-lowering effects of Pycnogenol observed in clinical trials with diabetic patients.

  4. Grape seed and tea extracts and catechin 3-gallates are potent inhibitors of α-amylase and α-glucosidase activity.

    Science.gov (United States)

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

    2012-09-12

    This study evaluated the inhibitory effects of plant-based extracts (grape seed, green tea, and white tea) and their constituent flavan-3-ol monomers (catechins) on α-amylase and α-glucosidase activity, two key glucosidases required for starch digestion in humans. To evaluate the relative potency of extracts and catechins, their concentrations required for 50 and 90% inhibition of enzyme activity were determined and compared to the widely used pharmacological glucosidase inhibitor, acarbose. Maximum enzyme inhibition was used to assess relative inhibitory 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. Whereas tea extracts and catechin 3-gallates were less effective inhibitors of α-amylase, they were potent inhibitors of α-glucosidase. Nongallated catechins were ineffective. The data show that plant extracts containing catechin 3-gallates, in particular epigallocatechin gallate, are potent inhibitors of α-glucosidase activity and suggest that procyanidins in grape seed extract strongly inhibit α-amylase activity.

  5. 山胡椒抑制体内外α-糖苷酶活性研究%α-Glucosidase Inhibitory Activity in vitro and vivo of Lindera Glauca(Sieblet Zucc) Blume

    Institute of Scientific and Technical Information of China (English)

    曹乃锋; 武小红; 康文艺

    2010-01-01

    对山胡椒抑制酵母α-葡萄糖苷酶和大鼠小肠α-葡萄糖苷酶活性进行了研究.利用96微孔板法检测其α-葡萄糖苷酶抑制活性.结果表明,抑制酵母α-葡萄糖苷酶实验中,山胡椒石油醚部位(IC50=229.70 μg/mL)、乙酸乙酯部位(IC50=259.10 μg/mL)和正丁醇部位(IC50=165.80 μg/mL)活性低于阳性对照Acarbose(IC50=1081.27 μg/mL);抑制大鼠小肠α-葡萄糖苷酶实验中,仅有乙酸乙酯部位(IC50=418.17 μg/mL)具有活性,阳性对照Acarbose 未检测出其IC50.实验证明,山胡椒各提取部位具有较好抑制酵母α-葡萄糖苷酶活性,但只有乙酸乙酯部位具有良好的大鼠小肠α-葡萄糖苷酶抑制活性.

  6. 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.

  7. 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

    Directory of Open Access Journals (Sweden)

    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.

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

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    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.

  9. 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.

  10. 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

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    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

  11. 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

  12. 针刺降糖穴治疗糖尿病的临床疗效及机理探讨

    Institute of Scientific and Technical Information of China (English)

    周巨伦

    2013-01-01

      目的:探讨降糖穴治疗糖尿病的临床疗效及作用机理。方法:本研究共搜集50例餐后血糖偏高的Ⅱ型糖尿病患者,共分为 A、B 两组,A 组为对31例餐后血糖偏高的Ⅱ型糖尿病患者采用针刺降糖穴结合口服阿卡波糖片治疗;B 组另对27例餐后血糖偏高的Ⅱ型糖尿病患者采用口服阿卡波糖片治疗作为对照组,观察两组患者治疗前后餐后2h 血糖的变化情况。结果:针刺降糖穴结合口服阿卡波糖片组的降血糖作用效果明显优于单纯口服药物组,总有效率达100%。结论:针刺降糖穴具有起效快,降血糖作用强,无副作用等优点,是一种较好治疗糖尿病的方法。%Objective: To investigate the clinical efficacy and mechanism of treatment of diabetes melitus by acupuncturing the hypoglycemic acupoint. Methods: This study has colected 50 cases of high blood sugar after meals in patients with type Ⅱ diabetes melitus, divided into A, B groups, A group of 31 cases of high postprandial blood sugar in patients with type Ⅱ diabetes glucose point accept acupuncturing the hypoglycemic point combined with oral acarbose tablets; B group of the other 27 cases of high postprandial blood glucose in patients with type Ⅱ diabetes melitus treated with oral acarbose tablets as a control group,the blood sugar changement of patients were observed before and after postprandial 2h. Results:Effect of group with acupuncturing the hypoglycemic acupoints combined with oral hypoglycemic acarbose tablets was better than oral medication group, the total effective rate was 100%. Conclusion: Acupuncturing the hypoglycemic acupoint has the advantages of quik and strong effect of hypoglycemic,and no side effects,etc.,and is a better way to treat diabetes.

  13. 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

  14. α-Glucosidase Inhibitory Activitives of S.xanthoxylon Bunge ,N.tangutorum Bobr and N.sibirica Pall, grown in Neimenggu from Zygophyllaceae%内蒙古产白刺、小果白刺和霸王α-葡萄糖苷酶抑制活性

    Institute of Scientific and Technical Information of China (English)

    常星; 康文艺

    2012-01-01

    首次利用体外α-葡萄糖苷酶抑制模型对内蒙古产3种蒺藜科植物的9个提取物进行活性评价,并与阳性对照Acarbose比较,发现3种植物均有抑制α-葡萄糖苷酶活性.其中白刺石油醚提取物对α-葡萄糖苷酶的抑制活性(IC50 =81.80 mg/L)最高,其余依次为小果白刺乙酸乙酯提取物(IC50=610.29 mg/L),霸王石油醚(IC50=627.22mg/L)和乙酸乙酯提取物(IC50 =838.40 mg/L),它们的抑制活性远大于阳性对照Acarbose( IC50=1103.01 mg/L).结果发现,不同植物不同溶剂提取物的α-葡萄糖苷酶抑制活性不同.同一植物不同溶剂提取物相比较,甲醇提取物的α-葡萄糖苷酶抑制活性不及乙酸乙酯和石油醚提取物.%The a-glucosidase inhibitory activities of nine extracts from three species of Zygophyllaceae in Neimenggu were evaluated in vitro by 96-microplate-based method for the first time. All these three species showed a-glucosidase inhibitory activities compared with the positive control " acarbose ". Among these nine extracts, petroleum ether extract of Nitraria tangutorum Bobr. Had the highest inhibitory activity (IC50 =81.80 mg/L) .followed by the ethyl acetate extract of N. Sibirica Pall( IC50 = 610.29 mg/L) ,the petroleum ether extract (IC50, = 627. 22 mg/L) and ethyl acetate extract (IC50 =838.40 mg/L) of Sarcozygium xanthoxylon Bunge,all of which are much higher than that of acarbose (IC50= 1103.01 mg/mL). Different extracts of different plants showed different inhibitory activies, while the inhibitory activity of different extracts from the same plant varied a lot. The methanolic extract had lower inhibitory activity than that of ethyl acetate extract and petroleum ether extract.

  15. 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.

  16. Effects of extracts of lupine seed on blood glucose levels in glucose resistant mice: antihyperglycemic effects of Lupinus albus (white lupine, Egypt) and Lupinus caudatus (tailcup lupine, Mesa Verde National Park).

    Science.gov (United States)

    Knecht, Kathryn T; Nguyen, Hoa; Auker, Adrienne D; Kinder, David H

    2006-01-01

    Lupine is a medicinal food plant with potential value in the management of diabetes. In white mice, extracts of seeds of the white lupine [Lupinus albus (L. termis L.)] were associated with increased tolerance to an oral glucose bolus. Antihyperglycemic activity was present in extracts of the whole seed but not extracts of the seed coat, and was not detected when glucose was administered intraperitoneally rather than orally. However, in contrast to results seen with the prescription drug, acarbose, lupine extract did not appear to increase the bulk or carbohydrate content of the feces. Antihyperglycemic activity was also seen in extracts of the tailcup lupine (L. caudatus) found in the Four Corners Region of the United States.

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

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    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.

  18. Influence of ursolic acid on glucooligosaccharides synthesized by dextransucrase from Leuconostoc mesenteroides Lm 28

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    TONKA VASILEVA

    2015-08-01

    Full Text Available A study of modulation of the reactions catalyzed by dextransucrase from Leuconostoc mesenteroides Lm 28 strain in the presence of triterpenoid ursolic acid was carried out. This compound showed concentration dependent inhibition of the studied dextransucrase and Ki = 1.9 mM, which is about 5 times higher than Ki value of the known glucansucrase inhibitor acarbose. Ursolic acid affected significantly the acceptor reactions catalyzed by Lm 28 dextransucrase in the presence of maltose and sucrose to maltose ratio 2. Increasing concentrations of ursolic acid shifted concentration and degree of polymerization (DP distribution of the synthesized glucooligosaccharides (GOS to acceptor products with DP ≤ 5. The oligosaccharide synthesis scheme applied in this study is a promising approach for production of GOS with controlled length of the chain.

  19. 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).

  20. a -Glucosidase Inhibitors from Dendrobium tortile

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    Rachawadee Limpanit

    2016-03-01

    Full Text Available From the whole plant of Dendrobium tortile, a new compound, namely 4-(2-hydroxypropyl-2(5H-furanone, was isolated, together with six known compounds, which included trans-tetracosylferulate (2, cis-docosylferulate (3, p-hydroxybenzaldehyde (4, 3,4-dihydroxy-3,4 ¢ -dimethoxybibenzyl (5, (2S-eriodictyol (6 and dendrofalconerol A (7. The structures of these compounds were determined through analysis of 1-D and 2-D NMR and HR-ESI-MS data. All of the isolates were evaluated for their a -glucosidase inhibitory activity. Compound 7 showed strong a -glucosidase inhibitory activity when compared with the positive control acarbose, whereas compounds 5 and 6 exhibited appreciable effects. An enzyme kinetic study revealed that compound 7 is a non-competitive inhibitor of a -glucosidase. This is the first report of the chemical constituents with biological activity from D. tortile.

  1. Sensitive fluorimetric assays for α-glucosidase activity and inhibitor screening based on β-cyclodextrin-coated quantum dots.

    Science.gov (United States)

    Liu, Si-Yao; Wang, Huan; He, Tian; Qi, Liang; Zhang, Zhi-Qi

    2016-02-01

    A fluorescence method was established for a α-glucosidase activity assay and inhibitor screening based on β-cyclodextrin-coated quantum dots. p-Nitrophenol, the hydrolysis product of the α-glucosidase reaction, could quench the fluorescence of β-cyclodextrin-coated quantum dots via an electron transfer process, leading to fluorescence turn-off, whereas the fluorescence of the system turned on in the presence of α-glucosidase inhibitors. Taking advantage of the excellent properties of quantum dots, this method provided a very simple, rapid and sensitive screening method for α-glucosidase inhibitors. Two α-glucosidase inhibitors, 2,4,6-tribromophenol and acarbose, were used to evaluate the feasibility of this screening model, and IC50 values of 24 μM and 0.55 mM were obtained respectively, which were lower than those previously reported. The method may have potential application in screening α-glucosidase inhibitors.

  2. New Phragmalin-Type Limonoids from Chukrasia tabularis and Their α-Glucosidase Inhibitory Activity

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    Jun-Lin Peng

    2016-01-01

    Full Text Available Phytochemical investigation on the stems of C. tabularis led to the isolation of five new phragmalin-type limonoids and six known ones. The structures of the new compounds 1–5, named chukbularisins A–E, were elucidated by spectroscopic techniques (IR, HRESIMS, 1D and 2D NMR and comparisons with published data. All the compounds were evaluated for in vitro α-glucosidase inhibitory activity. Compounds 2, 3, 4, 5, and 8 exhibited inhibitory activity against α-glucosidase with IC50 values of 0.06 ± 0.008, 0.04 ± 0.002, 0.52 ± 0.039, 1.09 ± 0.040, and 0.20 ± 0.057 mM, respectively (using acarbose as positive control, IC50 0.95 ± 0.092 mM.

  3. Antidiabetic effect of an active fraction extracted from dragon's blood (Dracaena Cochinchinensis).

    Science.gov (United States)

    Gu, Hui-Juan; Lv, Jing-Ci; Yong, Ke-Lan; Chen, Xu; Liu, Pei-Pei; Zhang, Xia-Bing

    2009-02-01

    The active fraction extracted from dragon's blood displayed an inhibitory effect on alpha-glucosidase activity with an IC50 of 0.152 microg/mL, which is nearly half of the crude material. Its inhibition on alpha-glucosidase was noncompetitive. In addition, when this fraction was orally administered to mice dosed with Acarbose (20 mg/kg), the active fraction (100, 300, 500 mg/kg) significantly suppressed increase of blood glucose levels after sucrose loading in a dose-dependent manner. These results suggest that this extract from dragon's blood exerts an anti-diabetic effect by suppressing intestinal carbohydrate absorption and thereby reducing the postprandial increase of blood glucose.

  4. Oligosaccharide binding to barley alpha-amylase 1

    DEFF Research Database (Denmark)

    Robert, X.; Haser, R.; Mori, H.;

    2005-01-01

    Enzymatic subsite mapping earlier predicted 10 binding subsites in the active site substrate binding cleft of barley alpha-amylase isozymes. The three-dimensional structures of the oligosaccharide complexes with barley alpha-amylase isozyme 1 (AMY1) described here give for the first time a thorough...... insight into the substrate binding by describing residues defining 9 subsites, namely -7 through +2. These structures support that the pseudotetrasaccharide inhibitor acarbose is hydrolyzed by the active enzymes. Moreover, sugar binding was observed to the starch granule-binding site previously determined...... in barley alpha-amylase isozyme 2 (AMY2), and the sugar binding modes are compared between the two isozymes. The "sugar tongs" surface binding site discovered in the AMY1-thio-DP4 complex is confirmed in the present work. A site that putatively serves as an entrance for the substrate to the active site...

  5. Effect of Phenolic Compounds from Elderflowers on Glucose- and Fatty Acid Uptake in Human Myotubes and HepG2-Cells

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    Giang Thanh Thi Ho

    2017-01-01

    Full Text Available Type 2 diabetes (T2D is manifested by progressive metabolic impairments in tissues such as skeletal muscle and liver, and these tissues become less responsive to insulin, leading to hyperglycemia. In the present study, stimulation of glucose and oleic acid uptake by elderflower extracts, constituents and metabolites were tested in vitro using the HepG2 hepatocellular liver carcinoma cell line and human skeletal muscle cells. Among the crude extracts, the 96% EtOH extract showed the highest increase in glucose and oleic acid uptake in human skeletal muscle cells and HepG2-cells. The flavonoids and phenolic acids contained therein were potent stimulators of glucose and fatty acid uptake in a dose-dependent manner. Most of the phenolic constituents and several of the metabolites showed high antioxidant activity and showed considerably higher α-amylase and α-glucosidase inhibition than acarbose. Elderflower might therefore be valuable as a functional food against diabetes.

  6. 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.

  7. 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.

  8. 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.

  9. 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.

  10. 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.

  11. Bergamotane Sesquiterpenes with Alpha-Glucosidase Inhibitory Activity from the Plant Pathogenic Fungus Penicillium expansum.

    Science.gov (United States)

    Ying, You-Min; Fang, Cheng-An; Yao, Feng-Qi; Yu, Yuan; Shen, Ying; Hou, Zhuo-Ni; Wang, Zhen; Zhang, Wei; Shan, Wei-Guang; Zhan, Zha-Jun

    2017-01-01

    Two new bergamotane sesquiterpene lactones, named expansolides C and D (1 and 2), together with two known compounds expansolides A and B (3 and 4), were isolated from the plant pathogenic fungus Penicillium expansum ACCC37275. The structures of the new compounds were established by detailed analyses of the spectroscopic data, especially 1D-, 2D-NMR, and HR-ESI-MS. In an in vitro bioassay, the epimeric mixture of expansolides C and D (1 and 2) (in a ratio of 2:1 at the temprature of the bioassay) exhibited more potent α-glucosidase inhibitory activity (IC50 =0.50 ± 0.02 mm) as compared with the positive control acarbose (IC50 = 1.90 ± 0.05 mm). To the best of our knowledge, it was the first report on the α-glucosidase inhibitory activity of bergamotane sesquiterpenes.

  12. Antioxidants and α-glucosidase inhibitors from "Liucha" (young leaves and shoots of Sibiraea laevigata).

    Science.gov (United States)

    Zhao, Jian-Qiang; Wang, Yan-Ming; Yang, Yan-Long; Zeng, Ying; Mei, Li-Juan; Shi, Yan-Ping; Tao, Yan-Duo

    2017-09-01

    The young leaves and shoots of Sibiraea laevigata, known as "Liucha", are used as tea by Tibetans to improve digestion after meals. Long-term consumption of "Liucha" will cause weight loss. In present work, we reported on the isolation and NMR and chemical analysis-based elucidation of seven new sorbitol O-caffeic acid ester derivatives named sorbitol esters A-G (1-7) and eighteen known phenolic compounds from S. laevigata. All of the isolates were evaluated for their antioxidant and α-glucosidase inhibitory activities. Among them sorbitol ester A (1), sorbitol ester D (4), sorbitol ester F (6), sorbitol ester G (7), isoferulic acid (15), methyl caffeate (18), trans-p-hydroxycinnamic acid (19), and kaempferol 3-O-β-d-(6″-E-p-coumaroyl)-glucopyranoside (25) showed more potent α-glucosidase inhibitory activity than the clinical drug acarbose. Copyright © 2017 Elsevier Ltd. All rights reserved.

  13. 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.

  14. Increased glucose metabolism and alpha-glucosidase inhibition in Cordyceps militaris water extract-treated HepG2 cells.

    Science.gov (United States)

    Kim, Dae Jung; Kang, Yun Hwan; Kim, Kyoung Kon; Kim, Tae Woo; Park, Jae Bong; Choe, Myeon

    2017-06-01

    Recent living condition improvements, changes in dietary habits, and reductions in physical activity are contributing to an increase in metabolic syndrome symptoms including diabetes and obesity. Through such societal developments, humankind is continuously exposed to metabolic diseases such as diabetes, and the number of the victims is increasing. This study investigated Cordyceps militaris water extract (CMW)-induced glucose uptake in HepG2 cells and the effect of CMW treatment on glucose metabolism. Colorimetric assay kits were used to determine the glucokinase (GK) and pyruvate dehydrogenase (PDH) activities, glucose uptake, and glycogen content. Either RT-PCR or western blot analysis was performed for quantitation of glucose transporter 2 (GLUT2), hepatocyte nuclear factor 1 alpha (HNF-1α), phosphatidylinositol 3-kinase (PI3k), protein kinase B (Akt), phosphorylated AMP-activated protein kinase (pAMPK), phosphoenolpyruvate carboxykinase, GK, PDH, and glycogen synthase kinase 3 beta (GSK-3β) expression levels. The α-glucosidase inhibitory activities of acarbose and CMW were evaluated by absorbance measurement. CMW induced glucose uptake in HepG2 cells by increasing GLUT2 through HNF-1α expression stimulation. Glucose in the cells increased the CMW-induced phosphorylation of AMPK. In turn, glycolysis was stimulated, and glyconeogenesis was inhibited. Furthermore, by studying the mechanism of action of PI3k, Akt, and GSK-3β, and measuring glycogen content, the study confirmed that the glucose was stored in the liver as glycogen. Finally, CMW resulted in a higher level of α-glucosidase inhibitory activity than that from acarbose. CMW induced the uptake of glucose into HepG2 cells, as well, it induced metabolism of the absorbed glucose. It is concluded that CMW is a candidate or potential use in diabetes prevention and treatment.

  15. Screening alpha-glucosidase and alpha-amylase inhibitors from natural compounds by molecular docking in silico.

    Science.gov (United States)

    Jhong, Chien-Hung; Riyaphan, Jirawat; Lin, Shih-Hung; Chia, Yi-Chen; Weng, Ching-Feng

    2015-01-01

    The alpha-glucosidase inhibitor is a common oral anti-diabetic drug used for controlling carbohydrates normally converted into simple sugars and absorbed by the intestines. However, some adverse clinical effects have been observed. The present study seeks an alternative drug that can regulate the hyperglycemia by down-regulating alpha-glucosidase and alpha-amylase activity by molecular docking approach to screen the hyperglycemia antagonist against alpha-glucosidase and alpha-amylase activities from the 47 natural compounds. The docking data showed that Curcumin, 16-hydroxy-cleroda-3,13-dine-16,15-olide (16-H), Docosanol, Tetracosanol, Antroquinonol, Berberine, Catechin, Quercetin, Actinodaphnine, and Rutin from 47 natural compounds had binding ability towards alpha-amylase and alpha-glucosidase as well. Curcumin had a better biding ability of alpha-amylase than the other natural compounds. Analyzed alpha-glucosidase activity reveals natural compound inhibitors (below 0.5 mM) are Curcumin, Actinodaphnine, 16-H, Quercetin, Berberine, and Catechin when compared to the commercial drug Acarbose (3 mM). A natural compound with alpha-amylase inhibitors (below 0.5 mM) includes Curcumin, Berberine, Docosanol, 16-H, Actinodaphnine/Tetracosanol, Catechin, and Quercetin when compared to Acarbose (1 mM). When taken together, the implication is that molecular docking is a fast and effective way to screen alpha-glucosidase and alpha-amylase inhibitors as lead compounds of natural sources isolated from medicinal plants. © 2015 International Union of Biochemistry and Molecular Biology.

  16. 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.

  17. Inhibitory Effect of Capparis spinosa Extract on Pancreatic Alpha-Amylase Activity

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    Mostafa Selfayan

    2016-04-01

    Full Text Available Background Diabetes mellitus is a metabolic disorder characterized by high blood glucose level caused due to deficiency of insulin secretion or insulin function. The inhibition of carbohydrate hydrolyzing enzymes such as α-amylase can be an important strategy for decrease postprandial blood glucose level in patients with type II diabetes. Plants contains different chemical constituents with potential for inhibition of α-amylase and hence maybe used as therapeutic. Objectives The aim of the present study is to investigate the effect of the ethanolic extract of Capparis spinosa on pancreatic α-amylase activities to find out the relevance of the plant in controlling blood sugar. Materials and Methods In this experimental study, root and leaves of C. spinosa were tested for α-amylase inhibition. Different concentrations (1.56, 3.12, 6.25, 12.5 and 25 mg/mL of extracts were incubated with enzyme substrate solution and the spectrometric method used for measure enzyme activity. Also acarbose was used as the standard inhibitor. Results Both root and leaves extracts showed inhibition of α-amylase (root = 97.31% and leaves = 98.92%. The root and leaves extracts of C. spinosa exhibited appreciable α-amylase inhibitory activity with an IC50 values 5.93 mg/mL and 3.89 mg/mL respectively, when compared with acarbose (IC50 value 0.038 mg/mL. Conclusions This study supports that root and leaves extracts of C. spinosa exhibit considerable α-amylase inhibitory activities. These results could be useful for developing functional foods by combination of plant-based foods for treatment of diabetes mellitus.

  18. Ashanti pepper (Piper guineense Schumach et Thonn) attenuates carbohydrate hydrolyzing, blood pressure regulating and cholinergic enzymes in experimental type 2 diabetes rat model.

    Science.gov (United States)

    Adefegha, Stephen Adeniyi; Oboh, Ganiyu; Adefegha, Omowunmi Monisola

    2017-01-01

    Ashanti pepper (Piper guineense Schumach et Thonn) seed is well known in folkloric medicine in the management of type 2 diabetes (T2DM) with little or no scientific documentation for its action. This study investigated the effect of Ashanti pepper seed on some enzymes relevant to carbohydrate hydrolysis, blood regulation and the cholinergic system, as well as the blood glucose level, lipid profile, antioxidant parameters, and hepatic and renal function markers in T2DM rats. T2DM was induced by feeding rats with high-fat diet (HFD) for 14 days followed by a single intraperitoneal dose of 35 mg/kg body weight of streptozotocin (STZ). Three days after STZ induction, diabetic rats were placed on a dietary regimen containing 2%-4% Ashanti pepper. Reduced blood glucose level with decreased α-amylase, α-glucosidase and angiotensin I converting enzyme (ACE) activities were observed in Ashanti pepper seed and acarbose-treated rat groups when compared to that of the diabetic control rat group. Furthermore, the results revealed that inclusion of 2%-4% Ashanti pepper seed in diabetic rat fed group diets may ameliorate the lipid profile, antioxidant status, and hepatic and renal function in T2DM rats as much as in the acarbose-treated groups. In addition, a chromatographic profile of the seed revealed the presence of quercitrin (116.51 mg/g), capsaicin (113.94 mg/g), dihydrocapsaicin (88.29 mg/g) and isoquercitrin (74.89 mg/g). The results from this study clearly suggest that Ashanti pepper could serve as a promising source of phenolic compounds with great alternative therapeutic potentials in the management of T2DM.

  19. Cyanobacterial pigments as natural anti-hyperglycemic agents: An in vitro study

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    Tonmoy Ghosh

    2016-08-01

    Full Text Available Traditional medicines for controlling postprandial hyperglycemia includes herbs and plant extracts as well as synthetic drugs like acarbose. Synthetic drug molecules frequently have side effects such as flatulence and diarrhea. Cyanobacterial pigments have excellent anti-oxidant and free radical scavenging properties. Thus, α-amylase and α-glucosidase inhibiting activities of purified pigments and crude extracts from three cyanobacterial species, Lyngbya, Microcoleus and Synechocystis sp., were investigated. Lyngbya extract had the highest total anti-oxidant activity (TAC before digestion (48.26 ± 0.04 µg AAE ml-1 while purified lycopene had the highest TAC after digestion (154.16 ± 0.96 µg AAE ml-1. The Microcoleus extract had the highest ABTS scavenging activity before digestion (98.23 ± 0.25 % while purified C-phycocyanin (C-PC had the highest ABTS scavenging after digestion (99.69 ±0.04 %. None of the digested or undigested extracts performed better than acarbose in inhibiting α-amylase but the digested Microcoleus extract was able to inhibit its activity by ~35 %. The purified pigments gave inhibitory activities ranging from ~ 8 – 16 %. The Lyngbya extract had the highest inhibitory activity against α-glucosidase both before and after digestion (62.22 ± 0.02 and 97.82 ± 0.03 % respectively. Purified C-phycoerythrin (C-PE, C-PC, lycopene and myxoxanthophyll could inhibit α-glucosidase in a range of ~83 – 96 %. Considering the potent inhibitory activities of purified pigments against both α-amylase and α-glucosidase, cyanobacterial pigments could be used as food additives for their dual advantage of anti-oxidant and anti-hyperglycemic activities.

  20. Alfa-glucosidase-inhibiting activity of some Mexican plants used in the treatment of type 2 diabetes.

    Science.gov (United States)

    Andrade-Cetto, Adolfo; Becerra-Jiménez, Jaime; Cárdenas-Vázquez, René

    2008-02-28

    Type 2 diabetes is an endocrine disease, which accounts for 9% of deaths worldwide. The aim of oral therapy is to reach normoglycemia to prevent later complications. Among glucose-lowering medications, alpha-glucosidase inhibitors delay the absorption of ingested carbohydrates, reducing the postprandial glucose and insulin peaks. In the present study, we tested the butanolic extracts of four Mexican plants with respect to their alpha-glucosidase inhibition activity, without excluding other possible mechanisms of action. The plants Cecropia obtusifolia Bertol., Equisetum myriochaetum Schlecht & Cham, Acosmium panamense (Benth.) Yacolev and Malmea depressa (Baill) R.E. Fries are used in traditional medicine to treat type 2 diabetes. In previous studies, we have demonstrated these plants' hypoglycemic activity and determined the phytochemical composition of their extracts. Our results in n-STZ diabetic rats loaded with maltose showed that Malmea and Acosmium extracts decreased plasma glucose significantly from 30 min on resembling the effect of acarbose. Cecropia extract produced the highest reduction of plasma glucose, and at 90 min, the glucose level was lower than the fasting level, which suggests another mechanism of action. Equisetum did not exert any effect. In vitro assays of alpha-glucosidase activity showed an IC(50) of 14 microg/ml for Cecropia, 21 microg/ml for Malmea, and 109 microg/ml for Acosmium, which were lower than that of acarbose (128 microg/ml). Equisetum did not show any significant effect on this assay, either. These results contribute to understand the mechanism of action of these plants on glucose metabolism.

  1. In vitro and in vivo α-amylase and α-glucosidase inhibiting activities of the protein extracts from two varieties of bitter gourd (Momordica charantia L.).

    Science.gov (United States)

    Poovitha, Sundar; Parani, Madasamy

    2016-07-18

    α-amylase and α-glucosidase digest the carbohydrates and increase the postprandial glucose level in diabetic patients. Inhibiting the activity of these two enzymes can control postprandial hyperglycemia, and reduce the risk of developing diabetes. Bitter gourd or balsam pear is one of the important medicinal plants used for controlling postprandial hyperglycemia in diabetes patients. However, there is limited information available on the presence of α-amylase and α-glucosidase inhibiting compounds. In the current study, the protein extracts from the fruits of M. charantia var. charantia (MCC) and M. charantia var. muricata (MCM) were tested for α-amylase and α-glucosidase inhibiting activities in vitro, and glucose lowering activity after oral administration in vivo. The protein extract from both MCC and MCM inhibited the activity of α-amylase and α-glucosidase through competitive inhibition, which was on par with Acarbose as indicated by in vitro percentage of inhibition (66 to 69 %) and IC50 (0.26 to 0.29 mg/ml). Both the protein extracts significantly reduced peak blood glucose and area under the curve in Streptozotocin-induced diabetic rats, which were orally challenged with starch and sucrose. Protein extracts from the fruits of the two varieties of bitter gourd inhibited α-amylase and α-glucosidase in vitro and lowered the blood glucose level in vivo on par with Acarbose when orally administrated to Streptozotocin-induced diabetic rats. Further studies on mechanism of action and methods of safe and biologically active delivery will help to develop an anti-diabetic oral protein drug from these plants.

  2. 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 .

  3. Estudios de intervención dirigidos a disminuir el riesgo de padecer diabetes mellitus tipo 2 Intervention studies aimed at lowering the risk of type 2 diabetes mellitus

    Directory of Open Access Journals (Sweden)

    José Luis Valenciaga Rodríguez

    2003-12-01

    Full Text Available Los estudios de intervención en población de riesgo, dirigidos a disminuir la frecuencia de la aparición de la diabetes mellitus tipo 2 (DM 2, son considerados orientadores para el enfoque del trabajo con esos pacientes. El objetivo del presente estudio es revisar los resultados de investigaciones dirigidas a disminuir el riesgo de padecer DM 2. Los sujetos estudiados presentaban alguna de las siguientes condiciones: glucosa alterada en ayunas (GAA o tolerancia a la glucosa alterada (TGA, antecedente personal de diabetes gestacional y síndrome metabólico. Se citan, entre otros, DPP (diabetes prevention program, DPS (diabetes prevention study, STOP-NIDDM (study to prevent non-insulin-dependent diabetes mellitus, Hiperglucemia en ayunas, DAISI (dutch acarbose intervention trial, Da Quing (estudio chino, TRIPOD (troglitazone In the prevention of diabetes, intervención, XENDOS (xenical in the prevention of diabetes in obese subjects, WOSCOPS (west of scotland coronary prevention study, EDIT (early diabetes intervención trial, NAVIGATOR (nateglinide and valsartan in impaired glucose tolerance outcomes research, DREAM (diabetes reduction assessment with ramipril and rosiglitazone medication. Estos consistían en cambios de estilo de vida (fundamentalmente ejercicios físicos sistemáticos y orientaciones nutricionales y/o intervenciones terapéuticas. Se concluye que en personas con 25 o más años de edad de ambos sexos, con riesgo de padecer DM 2, la adopción de un estilo de vida saludable logra disminuir el riesgo de padecer el síndrome diabético. En sujetos con alto riesgo de DM 2, los fármacos que reportan mejores y más consistentes resultados son el metformin y la acarbosa. Otros como la nateglidina, rosiglitazona, ramipril y valsartan, se están investigando actualmente.Intervention studies on population at risk aimed at lowering the frequency of occurrence of type 2 diabetes mellitus(DM2 are considered as guiding lines for the work

  4. 内蒙古产柽柳和多枝柽柳α-葡萄糖苷酶抑制活性%α-Glucosidase Inhibitory Activity of Tamarix chinensis Lout.and Tamarix ramosissima Ledeb.in Nei Meng-gu

    Institute of Scientific and Technical Information of China (English)

    常星; 崔维恒; 张俊柯; 吴雨虹; 康文艺

    2011-01-01

    首次利用体外α-葡萄糖苷酶抑制模型以96微孔板法,对内蒙古产2种柽柳属植物不同溶剂提取物进行活性评价,并与阳性对照Acarbose比较,发现6种提取物均有较好的α-葡萄糖苷酶抑制作用,远远强于阳性对照Acarbose(IC50=1103.01 μg·mL-1)的抑制活性.结果显示,同一植物不同溶剂提取物相比较,两者石油醚提取物α-葡萄糖苷酶抑制活性不及乙酸乙酯和正丁醇提取物;不同植物同一溶剂的提取物抑制活性也不同,6种提取物中,多枝柽柳的正丁醇和柽柳的乙酸乙酯提取物抑制活性最高(IC50=13.36和17.35μg·mL-1).所有提取物对α-葡萄糖苷酶活性的抑制效果均很好,且多枝柽柳抑制活性整体上较柽柳好,具有良好的潜在开发价值.%The α-glucosidase inhibitory activities of different extracts from two species Tamarix in Nei Meng-gu were screened and compared with acarbose as positive control in vitro by the 96-microplate-based method for the first time.The results showed that six extracts from two species Tamarix showed good inhibitory activity, and they were all greatly higher than that of acarbose ( IC50 = 1103.0l μg · mL- 1 ) as positive control.Petroleum ether extract had lower inhibitory activity than that of ethyl acetate extract and methanolic extract in the same plant.Extracts from different plant of same polar solvent had different inhibitory activity.In six extracts,the l-butanol extract of T.ramosissima and ethyl acerate extract of T.chinensis had the highest inhibitor activity of α-glucosidase (IC50 = 13.36 和 17.35 μg · mL-1 ).The all extracts of two species Tamarix in Nei Meng-gu had good inhibitory activity of α-glucosidase, and inhibitory activity of T.ranosissima was higher than that of T.chinensis.Two plants could be exploited the diabetes drugs as α-glucosidases inhibitors in future.

  5. Compound Danshen Dripping Pill Adjunctive Therapy for Type 2 Diabetes in 65 Cases%复方丹参滴丸辅助治疗2型糖尿病65例

    Institute of Scientific and Technical Information of China (English)

    江霞; 徐文军; 高厚明; 郭彬

    2011-01-01

    目的 观察复方丹参滴丸辅助治疗2型糖尿病的临床效果.方法 选择2型糖尿病患者130例,随机均分为对照组和治疗组各65例,对照组口服格列齐特缓释片(80 mg,每日2次)、阿卡波糖片(100 mg,每日3次).治疗组在对照组基础上加服复方丹参滴丸(10丸,每日3次),疗程10周.结果 对照组总有效率为60.00%,治疗组总有效率为81.54%,两组总有效率比较有显著性差异(x2=5.46,P<0.05);两组治疗10周后空腹血糖、餐后2 h血糖、糖化血红蛋白、血清总胆固醇和甘油三酯均显著下降,且治疗组改善更明显.结论 复方丹参滴丸辅助治疗2型糖尿病疗效较好,值得临床推广.%Objective To study the clinical curative effect of Fufang Danshen Dripping Pill as an adjunctive therapy for type 2 diabetes. Methods A hundred and thirty patients with type 2 diabetes were randomly evenly assigned to control and treatment groups. The control group( n = 65) receive Gliclazide Sustained Release Tablets plus Acarbose Tablets for 10 weeks. and the treatment group( n =65) received Gliclazide Sustained Release Tablets+Acarbose Tablets in combination with Compound Danshen Dripping Pill for 10 weeks. Results The effective rate was 60. 00% in the control group and 81. 54% in the treatment group. There was significant difference in the total effective rate between the two groups (χ2 = 5. 46, P < 0. 05) . After 10 - week treatment. FBG, P2hBG, HbA1c, TC and TCJ were decreased significantly ( P < 0. 05), but the treatment group showing better improvement than control group. Conclusion Compound Danshen Dripping Pill as an adjunctive therapy for type 2 diabetes achieved satisfactory curative effect,whice deserves to be popularized in clinic.

  6. Lactucaxanthin - a potential anti-diabetic carotenoid from lettuce (Lactuca sativa) inhibits α-amylase and α-glucosidase activity in vitro and in diabetic rats.

    Science.gov (United States)

    Gopal, Sowmya Shree; Lakshmi, Magisetty Jhansi; Sharavana, Gurunathan; Sathaiah, Gunaseelan; Sreerama, Yadahally N; Baskaran, Vallikannan

    2017-03-22

    Intestinal and pancreatic α-amylase and α-glucosidase inhibitors offer an approach to lower the levels of post-prandial hyperglycemia through the control of dietary starch breakdown in digestion. This study hypothesized that lactucaxanthin (Lxn) in lettuce (Lactuca sativa) inhibits the activity of α-amylase and α-glucosidase. In this study, the interaction of Lxn with α-amylase and α-glucosidase in silico and its inhibitory effect on these enzymes were studied using in vitro and STZ-induced diabetic rat models. Lxn was isolated from lettuce with 96% purity confirmed by HPLC and LCMS. The in silico analysis showed that Lxn has a lower binding energy (-6.05 and -6.34 kcal mol(-1)) with α-amylase and α-glucosidase compared to their synthetic inhibitors, acarbose (-0.21 kcal mol(-1)) and miglitol (-2.78 kcal mol(-1)), respectively. In vitro α-amylase and α-glucosidase inhibition assays revealed that Lxn had IC50 values of 435.5 μg mL(-1) and 1.84 mg mL(-1), but acarbose has values of 2.5 and 16.19 μg mL(-1). The in vivo results showed an increased activity for α-amylase and α-glucosidase in the intestine (4.7 and 1.30 fold, p < 0.05) and pancreas (1.3 and 1.48 fold, p < 0.05) of STZ induced diabetic rats compared to normal rats. Whereas the activity decreased (p < 0.05) in the Lxn fed diabetic rats, except for the intestinal α-glucosidase activity (1.69 ± 0.12 PNP per min per mg protein). This was confirmed by the low blood glucose level (239.4 ± 18.2 mg dL(-1)) in diabetic rats fed Lxn compared to the diabetic group (572.2 ± 30.5 mg dL(-1), p < 0.05). Lxn significantly inhibited (p < 0.05) the activity of α-amylase and α-glucosidase and could be of medical and nutritional relevance in the treatment of diabetes.

  7. 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

  8. Antihyperglycemic Activity of the Leaves from Annona cherimola Miller and Rutin on Alloxan-induced Diabetic Rats

    Science.gov (United States)

    Calzada, Fernando; Solares-Pascasio, Jesús Iván; Ordoñez-Razo, R. M.; Velazquez, Claudia; Barbosa, Elizabeth; García-Hernández, Normand; Mendez-Luna, David; Correa-Basurto, José

    2017-01-01

    Background: Annona cherimola, known as “chirimoya” has been reported in Mexican traditional medicine for the treatment of diabetes. Objective: The aims of the present study were to validate and assess the traditional use of A. cherimola as an antidiabetic agent. Materials and Methods: The ethanol extract from A. cherimola (300 mg/kg, EEAc), subsequent fractions (100 mg/kg), and rutin (30 mg/kg) were studied on alloxan-induced type 2 diabetic (AITD) and normoglycemic rats. In addition, oral glucose tolerance test (OGTT) and oral sucrose tolerance test (OSTT) were performed in normoglycemic rats. Molecular docking technique was used to conduct the computational study. Results: Bioassay-guided fractionation of EEAc afforded as major antihyperglycemic compound, rutin. EEAc attenuated postprandial hyperglycemia in acute test using AITD rats (331.5 mg/dL) carrying the glycemic levels to 149.2 mg/dL. Rutin after 2 h, attenuated postprandial hyperglycemia in an acute assay using AITD rats such as EEAc, with maximum effect (150.0 mg/dL) being seen at 4 h. The antihyperglycemic activities of EEAc and rutin were comparable with acarbose (151.3 mg/dL). In the subchronic assay on AITD rats, the EEAc and rutin showed a reduction of the blood glucose levels since the 1st week of treatment, reaching levels similar to normoglycemic state (116.9 mg/kg) that stayed constant for the rest of the assay. OGTT and OSTT showed that EEAc and rutin significantly lowered blood glucose levels in normoglycemic rats at 2 h after a glucose or sucrose load such as acarbose. Computational molecular docking showed that rutin interacted with four amino acids residues in the enzyme α-glucosidase. Conclusion: The results suggest that rutin an α-glucosidase inhibitor was responsible in part of the antihyperglycemic activity of A. cherimola. Its in vivo antihyperglycemic activity is in good agreement with the traditional use of A. cherimola for the treatment of diabetes. SUMMARY The ethanol extract

  9. Application of oral hypoglycemic agent in Our Hospital in 2013%我院2013年门诊口服降糖药临床应用分析

    Institute of Scientific and Technical Information of China (English)

    余彬; 王述蓉

    2014-01-01

    Objective:To make out the current situation and trend of oral hypoglycemic agent used in hospital and to make objective evaluation. Methods:The use of oral hypoglycemic agent in our hospital in 2013 was analyzed retrospectively in respect of consumption sum, DDDs .RESULTS:The top 3 oral hypoglycemic agent of consumption sum were Repaglinide, Acarbose and Glipizide.The top 3 oral hypoglycemic agent in respect of DDDs were Glipizide, Gliclazide Sustained-release Tablets and Glibenclamide. DDDc of Glibenclamide Glipizide and Gliclazide Sustained-release Tablets were the top 3.Conclusion:The use of oral hypoglycemic agent used in our hospital is rational on the whole, Acarbose of Glycosidase inhibitors and Gliclazide of Sulfonylureas are the most common because their good effects and few adverse reactions.%目的:对我院2013年门诊口服降糖药临床应用情况及趋势作出客观评价。方法:统计我院2013年门诊口服降糖药的销售金额、用药频度(DDDs)等,进行回顾性分析。结果:我院2013年口服降糖药销售金额排序前3位的是瑞格列奈片、阿卡波糖、格列吡嗪;DDDs排序前3位是格列吡嗪、格列齐特缓释片、格列苯脲片;日均费用前3位为格列苯脲片、格列吡嗪片、格列齐特缓释片。结论:我院口服降糖药使用较合理,糖苷酶抑制剂阿卡波糖、磺脲类药物的格列齐特因其疗效好、不良反应较少等居主导地位。

  10. Modified Regulatory Pathways to Approve Generic Drugs in the US and a Systematic Review of Their Outcomes.

    Science.gov (United States)

    Kesselheim, Aaron S; Polinski, Jennifer M; Fulchino, Lisa A; Isaman, Danielle L; Gagne, Joshua J

    2015-04-01

    Generic drugs are approved on the basis of pharmaceutical equivalence and bioequivalence. Some drug products have unique structural or functional attributes, necessitating modified approaches to bioequivalence determinations. The aim of this systematic review was to identify studies that evaluated laboratory or clinical outcomes of six drugs approved via modified bioequivalence approaches. We conducted a systematic review of articles published through February 2014 in MEDLINE, EMBASE, and International Pharmaceutical Abstracts related to six recent drugs subject to modified regulatory approaches: venlafaxine extended release tablet (Effexor XR), acarbose (Precose), enoxaparin (Lovenox), vancomycin capsules (Vancocin), sodium ferric gluconate (Ferrlecit), and calcitonin salmon nasal spray (Miacalcin NS). We included all empirical evaluations (whether in vivo or in vitro) and excluded case studies, qualitative analyses, and pharmacoeconomic evaluations. Studies were summarized and evaluated on their methodological quality and assessed for bias using the Cochrane Risk of Bias Assessment Tool. Articles were divided into studies of US FDA-approved generics and non-FDA-approved generics available in non-US locations. We extracted drug(s) studied, study design, setting, sample size, population characteristics, study endpoints and results, and source of funding. After retrieving 1408 articles and searching through the full text of 106 articles, we found 26 articles that met our inclusion criteria-8 examining FDA-approved versions and 18 examining non-FDA-approved versions. Among FDA-approved generics, five studies of enoxaparin showed minor variations in biologic activities of unclear clinical importance, and no publications involved acarbose, venlafaxine ER, or vancomycin capsules. Among non-FDA-approved generics, nine studies of enoxaparin supported generic bioequivalence, despite three showing minor variations in drug activity. Four of six studies of venlafaxine ER

  11. 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.

  12. 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.

  13. 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.

  14. Modeling of cooked starch digestion process using recombinant human pancreatic α-amylase and maltase-glucoamylase for in vitro evaluation of α-glucosidase inhibitors.

    Science.gov (United States)

    Cao, Xiaofang; Zhang, Chen; Dong, Yangyang; Geng, Peng; Bai, Fang; Bai, Gang

    2015-09-23

    In human, digestion of cooked starch mainly involves breaking down of α-amylase to α-limit dextrins and small linear malto-oligosaccharides, which are in turn hydrolyzed to glucose by the gut mucosal maltase-glucoamylase (MGAM). Human pancreatic α-amylase (HPA), amino- and carboxyl-terminal portions of MGAM (ntMGAM and ctMGAM) catalyze the hydrolysis of α-D-(1,4) glycosidic linkages in starch, playing a crucial role in the production of glucose in the human lumen. Accordingly, these enzymes are effective drug targets for the treatments of type 2 diabetes and obesity. In this study, a Plackett-Burman based statistical screening procedure was adopted to determine the most critical factors affecting cooked starch digestion by the combination of HPA, ctMGAM and ntMGAM. Six factors were tested and experimental results showed that pH and temperature were the major influencing factors, with optimal pH and temperature at 6.0 and 50 °C, respectively. Surprisingly, ntMGAM had no significant contribution to the glucose production from starch digestion compared to the HPA and ctMGAM. The optimal proportion of HPA and ctMGAM in a starch digestion system was further determined by response surface methodology. Results showed a maximum starch digestion (88.05%) within 0.5 h when used HPA:ctMGAM=1:9 (U). The inhibitory effects of various inhibitors on the cooked starch digestion by HPA1/ctMGAM9 were evaluated by determining their half maximal inhibitory concentration (IC50) values. Acarviostatin II03 showed the highest inhibitory activity, with 67 times higher potency than acarbose. Moreover, acarviostatin II03 could significantly depress postprandial blood glucose levels in mice, better than that by acarbose. These findings suggest that our in vitro enzymatic system can simulate in vivo starch digestion process, and thus can be used to screen and evaluate α-glucosidase inhibitors.

  15. Different Proportions of Huangqi (Radix Astragali Mongolici and Honghua (Flos Carthami Injection on α-Glucosidase and α-Amylase Activities

    Directory of Open Access Journals (Sweden)

    Hui Liao

    2015-01-01

    Full Text Available Objective. To study the effect of different proportions of Huangqi (Radix Astragali Mongolici and Honghua (Flos Carthami injection on α-glucosidase and α-amylase activity simultaneously. Methods. The injections were prepared according to the standards of the China Food and Drug Administration. The assay for potential α-glucosidase inhibitors was based on the hydrolysis of 4-methylumbelliferyl-α-D-glucopyranoside (4-MUG. The α-amylase EnzChek assay kit was used to determine potential α-amylase inhibitors. Acarbose was the positive control. Results. The half maximal (50% inhibitory concentration (IC50 of acarbose against α-glucosidase and α-amylase was (1.8±0.4 μg/mL and (227±32 μg/mL, respectively. Honghua showed significant inhibition of α-glucosidase activity compared with Huangqi (P<0.01. Honghua inhibited α-amylase activity, but Huangqi did not. IC50s for α-glucosidase inhibition by mixtures at 10 : 1, 5 : 1, and 2 : 1 were significantly lower than those at the 20 : 1 mixture (P<0.01. α-Amylase inhibition by the 2 : 1 mixture was significantly higher than that by the 20 : 1, 10 : 1, and 5 : 1 mixtures at 500 μg/mL and 1000 μg/mL (P<0.01, with 5 : 1 significantly higher than 20 : 1 and 10 : 1 at 1000 μg/mL (P<0.01. Conclusion. Honghua significantly inhibited α-glucosidase activity compared with Huangqi (P<0.01. For simultaneous inhibition of α-glucosidase and α-amylase activities, the mixtures at 2 : 1 and 5 : 1 exhibited significant effects compared with those at 20 : 1 (P<0.01.

  16. α-Glucosidase Inhibitory Activity of Salvia honania L.H.Bailey in vivo and vitro%河南鼠尾草抑制体内外α-糖苷酶活性研究

    Institute of Scientific and Technical Information of China (English)

    闫文义; 曹乃峰; 张倩; 康文艺

    2012-01-01

    The yeast and rat intestinal a-glucosidase inhibitory activity of Saltia. honania was assayed by the method of 96-microplates for the first time. Yeast a-glucosidase inhibitory activity of ethyl acetate extracts (IC50= 28.73 μg/mL) and n-butanol extracts of S. honania (IC50=73.90 μg/mL) were higher than that of Acaibose (IC50 =1081.27 μg/ mL) as positive control. Only ethyl acetate extracts (IC50 =366.79 μg/mL) showed inhibitory activity on rat intestinal a-glucosidase, and the IC50 value of Acarbose was not detected. The results indicated that both ethyl acetate extracts and n-butanol extracts of S. honania showed a better yeast a-glucosidase inhibitory activity, but only ethyl acetate extracts showed a better rat intestinal a-glucosidase inhibitory activity.%本文采用96微孔板法,首次对河南鼠尾草抑制酵母和大鼠小肠α-葡萄糖苷酶活性进行研究.河南鼠尾草乙酸乙酯提取物(IC50=28.73μg/mL)和正丁醇提取物(IC50 =73.90 μg/mL)抑制酵母α-葡萄糖苷酶活性远高于阳性对照Acarbose(IC50=1081.27 μg/mL),但只有乙酸乙酯提取物(IC50=366.79μ/mL)具有抑制大鼠小肠α-葡萄糖苷酶活性,阳性对照Acarbose未检测出其IC50.结果表明,河南鼠尾草乙酸乙酯提取物和正丁醇提取物均具有较好的酵母α-葡萄糖苷酶抑制活性,但只有乙酸乙酯提取物具有良好的大鼠小肠α-葡萄糖苷酶抑制活性.

  17. Thyroid Cancer Risk Is Not Increased in Diabetic Patients

    Science.gov (United States)

    Tseng, Chin-Hsiao

    2012-01-01

    Objective This study evaluated thyroid cancer risk with regards to diabetes status and diabetes duration, and with the use of anti-diabetic drugs including sulfonylurea, metformin, insulin, acarbose, pioglitazone and rosiglitazone, by using a population-based reimbursement database in Taiwan. Methods A random sample of 1,000,000 subjects covered by the National Health Insurance was recruited. After excluding patients with type 1 diabetes, 999730 subjects (495673 men and 504057 women) were recruited into the analyses. Logistic regression estimated the odds ratios (OR) and their 95% confidence intervals (CI) for independent variables including age, sex, diabetes status/duration, anti-diabetic drugs, other medications, comorbidities, living regions, occupation and examinations that might potentially lead to the diagnosis of thyroid cancer in various models. Results The diabetic patients had a significantly higher probability of receiving potential detection examinations (6.38% vs. 5.83%, Pdiabetes status was 0.816 (0.652–1.021); and for diabetes duration diabetes was 0.071 (0.010–0.507), 0.450 (0.250–0.813), 0.374 (0.203–0.689) and 1.159 (0.914–1.470), respectively. Among the anti-diabetic agents, only sulfonylurea was significantly associated with thyroid cancer, OR (95% CI): 1.882 (1.202–2.947). The OR (95% CI) for insulin, metformin, acarbose, pioglitazone and rosiglitazone was 1.701 (0.860–3.364), 0.696 (0.419–1.155), 0.581 (0.202–1.674), 0.522 (0.069–3.926) and 0.669 (0.230–1.948), respectively. Furthermore, patients with benign thyroid disease or other cancer, living in Kao-Ping/Eastern regions, or receiving potential detection examinations might have a significantly higher risk; and male sex, hypertension, dyslipidemia, chronic obstructive pulmonary disease, vascular complications or use of statin, aspirin or non-steroidal anti-inflammatory drugs might be associated with a significantly lower risk. Conclusions There is a lack of an overall

  18. 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.

  19. 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

    2016-04-27

    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

  20. Thyroid cancer risk is not increased in diabetic patients.

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    Chin-Hsiao Tseng

    Full Text Available OBJECTIVE: This study evaluated thyroid cancer risk with regards to diabetes status and diabetes duration, and with the use of anti-diabetic drugs including sulfonylurea, metformin, insulin, acarbose, pioglitazone and rosiglitazone, by using a population-based reimbursement database in Taiwan. METHODS: A random sample of 1,000,000 subjects covered by the National Health Insurance was recruited. After excluding patients with type 1 diabetes, 999730 subjects (495673 men and 504057 women were recruited into the analyses. Logistic regression estimated the odds ratios (OR and their 95% confidence intervals (CI for independent variables including age, sex, diabetes status/duration, anti-diabetic drugs, other medications, comorbidities, living regions, occupation and examinations that might potentially lead to the diagnosis of thyroid cancer in various models. RESULTS: The diabetic patients had a significantly higher probability of receiving potential detection examinations (6.38% vs. 5.83%, P<0.0001. After multivariable-adjustment, the OR (95% CI for diabetes status was 0.816 (0.652-1.021; and for diabetes duration <1 year, 1-3 years, 3-5 years and ≥ 5 years vs. non-diabetes was 0.071 (0.010-0.507, 0.450 (0.250-0.813, 0.374 (0.203-0.689 and 1.159 (0.914-1.470, respectively. Among the anti-diabetic agents, only sulfonylurea was significantly associated with thyroid cancer, OR (95% CI: 1.882 (1.202-2.947. The OR (95% CI for insulin, metformin, acarbose, pioglitazone and rosiglitazone was 1.701 (0.860-3.364, 0.696 (0.419-1.155, 0.581 (0.202-1.674, 0.522 (0.069-3.926 and 0.669 (0.230-1.948, respectively. Furthermore, patients with benign thyroid disease or other cancer, living in Kao-Ping/Eastern regions, or receiving potential detection examinations might have a significantly higher risk; and male sex, hypertension, dyslipidemia, chronic obstructive pulmonary disease, vascular complications or use of statin, aspirin or non-steroidal anti

  1. 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.

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

    Science.gov (United States)

    Ramalingum, Nelvana; Mahomoodally, M. Fawzi

    2014-01-01

    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. PMID:24812627

  3. Inhibitory effects of pomegranate extracts on recombinant human maltase-glucoamylase.

    Science.gov (United States)

    Kawakami, Kayoko; Li, Peng; Uraji, Misugi; Hatanaka, Tadashi; Ito, Hideyuki

    2014-09-01

    α-Glucosidase inhibitors are currently used in the treatment of type 2 diabetes. In this study, we investigated the inhibitory activities of aril and pericarp extracts from pomegranates obtained various regions against recombinant human maltase-glucoamylase (MGAM). The inhibitory activities of the aril extracts tended to be stronger than those of the pericarp extracts. The Iranian aril extract was the most effective inhibitor. We investigated the polyphenol content of the pomegranate extracts using the Folin-Ciocalteu method. Among the aril extracts, the Iranian aril extract showed the highest polyphenol content. We further evaluated inhibitory activity against α-glucosidase from the rat small intestine. Pomegranate extract used in this study showed slightly different inhibitory activities according to α-glucosidase origin. Iranian aril extract was the most effective inhibitor of α-glucosidases, especially recombinant human MGAM. Bioassay-guided fractionation of the pomegranate arils led to identification of punicalagin and oenothein B as potent inhibitors of α-glucosidase. Oenothein B showed inhibitory activity with a half-maximal inhibitory concentration (IC(50)) value of 174 μM. Its potency was comparable to that of the α-glucosidase inhibitor acarbose with an IC(50) value of 170 μM. Dixon plot kinetic analysis of oenothein B showed a noncompetitive inhibition with a K(i) value of 102 μM. These results suggest that pomegranate arils would be useful for suppressing postprandial hyperglycemia.

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

    Directory of Open Access Journals (Sweden)

    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.

  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. 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.

  7. Complications of bariatric surgery: dumping syndrome, reflux and vitamin deficiencies.

    Science.gov (United States)

    Tack, Jan; Deloose, Eveline

    2014-08-01

    Bariatric surgical procedure are increasingly and successfully applied in the treatment of morbid obesity. Nevertheless, these procedures are not devoid of potential long-term complications. Dumping syndrome may occur after procedures involving at least partial gastric resection or bypass, including Roux-en-Y gastric bypass (RYGB) and sleeve gastrectomy. Diagnosis is based on clinical alertness and glucose tolerance testing. Treatment may involve dietary measures, acarbose and somatostatin analogues, or surgical reintervention for refractory cases. Gastro-esophageal reflux disease (GERD) can be aggravated by vertical banded gastroplasty and sleeve gastrectomy procedures, but pre-existing GERD may improve after RYGB and with adjustable gastric banding. Nutrient deficiencies constitute the most important long-term complications of bariatric interventions, as they may lead to haematological, metabolic and especially neurological disorders which are not always reversible. Malabsorptive procedures, poor postoperative nutrient intake, recurrent vomiting and poor compliance with vitamin supplement intake and regular follow-up are important risk factors. Preoperative nutritional assessment and rigourous postoperative follow-up plan with administration of multi-vitamin supplements and assessment of serum levels is recommended in all patients.

  8. 2型糖尿病患者红细胞胞浆钙调素活性变化的研究%A study of calmodulin activities of erythrocytes and its influencing factors in type 2 diabetic patients

    Institute of Scientific and Technical Information of China (English)

    赵铁耘; 李秀钧; 吴兆锋; 张翔迅; 左凤琼

    2000-01-01

    ObjectiveTo evaluate the calmodulin (CaM) activities of erythrocytes and the possible causes toinfluence the changes of CaM levels in type 2 diabetic (DM2) patients.Methods 70 patients with DM2 were studied.Of the 70 patients, 46 were treated with only oral hypoglycemic agents (OHA) (32 treated with sulfonylureas, 20treated with biguanides, 4 treated with Acarbose).24 were on insulin or insulin+OHA for more than three weeks.Themeasurement of soluble CaM of erythrocytes was performed by the methods of Wallace RW.Results ①)The activities ofsoluble CaM of erythrocytes in DM2 were significantly lower than that in normal subjects ( P 0.05);而OHA组CaM活性较正常组显著降低(P<0.05)。③多因素分析显示2型糖尿病患者红细胞胞浆中CaM活性与年龄、体重指数(BMI)呈负相关,与空腹Ins水平呈正相关。结论2型糖尿病患者红细胞胞浆中可溶性CaM活性明显降低,而Ins治疗可使其红细胞胞浆中可溶性CaM活性有所恢复。

  9. 2008年至2010年我院口服降血糖药使用情况分析%Analysis on Use Status of Oral Hypoglycemic Agents in Our Hospital during 2008-2010

    Institute of Scientific and Technical Information of China (English)

    向光芳; 郑姣妮; 姜宁

    2012-01-01

    Objective To provide fundamental basis for rational use of medicines in clinic, we investigated the application of oral hypo-glycemic agents at our hospital. Methods The statistic analysis was carried out to study the use of oral hypoglycemic agents in our hospital during 2008 - 2010 using order of consumption sum and frequency degree analysis methods. Results Thiazolidinediones, a - glucosidase inhibitor and biguanides ranked the top three among all the oral hypoglycemic agents in consumption sum. The highest DDDs is rosiglita-zone, followed by glimepiride and acarbose. Conclusion The use of oral hypoglycemic agents in our hospital is basically reasonable.%目的 了解医院口服降血糖药的使用情况,为临床合理用药提供参考.方法 采用金额排序和频度分析法,对医院2008年至2010年口服降血糖药进行统计分析.结果 口服降糖药用药金额排前3位的分别是噻唑烷二酮类、a-糖苷酶抑制剂和双胍类;用药频度最高的是罗格列酮,其次是格列美脲和阿卡波糖.结论 医院口服降血糖药的使用基本合理.

  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. Monoalkylated barbiturate derivatives: X-ray crystal structure, theoretical studies, and biological activities

    Science.gov (United States)

    Barakat, Assem; Al-Majid, Abdullah Mohammed; Soliman, Saied M.; Islam, Mohammad Shahidul; Ghawas, Hussain Mansur; Yousuf, Sammer; Choudhary, M. Iqbal; Wadood, Abdul

    2017-08-01

    Barbiturate derivatives are privileged structures with a broad range of pharmaceutical applications. We prepared a series of 5-monoalkylated barbiturate derivatives (3a-l) and evaluated, in vitro, their antioxidant (DPPH assay), and α-glucosidase inhibitory activities. Compounds 3a-l were synthesized via Michael addition. The structure of compound 3k was determined using X-ray single-crystal diffraction, and geometric parameters were calculated using density functional theory at the B3LYP/6-311G(d,p) level of theory. Further, the structural analysis of 3k were also investigated. Biological studies revealed that compounds 3b (IC50 = 133.1 ± 3.2 μM), 3d (IC50 = 305 ± 7.7 μM), and 3e (IC50 = 184 ± 2.3 μM) have potent α-glucosidase enzyme inhibitors and showed greater activity than the standard drug acarbose (IC50 = 841 ± 1.73 μM). Compounds 3a-3i were found to show weak antioxidant activity against 1,1-diphenyl-2-picryl-hydrazyl (DPPH) radicals (IC50 = 91 ± 0.75 to 122 ± 1.0 μM) when tested against a standard antioxidant, gallic acid (IC50 = 23 ± 0.43 μM).

  12. In Vitro and In Vivo Effects of Norathyriol and Mangiferin on α-Glucosidase.

    Science.gov (United States)

    Shi, Zhi-Long; Liu, Yi-Dan; Yuan, Yun-Yun; Song, Da; Qi, Mei-Feng; Yang, Xu-Juan; Wang, Ping; Li, Xiao-Ying; Shang, Jian-Hua; Yang, Zhao-Xiang

    2017-01-01

    Norathyriol is a metabolite of mangiferin. Mangiferin has been reported to inhibit α-glucosidase. To the best of our knowledge, no study has been conducted to determine or compare those two compounds on inhibiting α-glucosidase in vitro and in vivo by far. In this study, we determined the inhibitory activity of norathyriol and mangiferin on α-glucosidase in vitro and evaluated their antidiabetic effect in diabetic mice. The results showed that norathyriol inhibited α-glucosidase in a noncompetitive manner with an IC50 value of 3.12 μM, which is more potent than mangiferin (IC50 = 358.54 μM) and positive drug acarbose (IC50 = 479.2 μM) in the zymological experiment. Both of norathyriol and mangiferin caused significant (p < 0.05) reduction in fasting blood glucose and the blood glucose levels at two hours after carbohydrate loading and it was interesting that mangiferin and norathyriol can make the decline of the blood glucose earlier than other groups ever including normal group in the starch tolerance test. However, norathyriol and mangiferin did not significantly influence carbohydrate absorption in the glucose tolerance test. Therefore, the antidiabetic effects of norathyriol and mangiferin might be associated with α-glucosidase, and norathyriol was more potent than mangiferin.

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

    Directory of Open Access Journals (Sweden)

    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.

  14. Potential of lignin from Canna edulis ker residue in the inhibition of α-d-glucosidase: Kinetics and interaction mechanism merging with docking simulation.

    Science.gov (United States)

    Xie, Fan; Gong, Shengxiang; Zhang, Wei; Wu, Jinhong; Wang, Zhengwu

    2017-02-01

    In this study, we extracted lignin from Canna edulis ker residue. Its chemical structure, inhibitory activity on α-d-glucosidase, and kinetics as well as interaction mechanism were investigated by using spectrum analysis and docking simulation. The isolated lignin was composed by guaiacyl and syringal units, and exhibited stronger inhibition on α-d-glucosidase than acarbose with the half maximal inhibitory concentration at 5.3±0.3μM. It was a non-competitive inhibitior with Km and Ki values of 0.53±0.02mM and 0.92±0.12μM, respectively. It could quench the intrinsic fluorescence of α-d-glucosidase through a static quenching mode. The calculated values of enthalpy and entropy change were 20.8±2.5kJmol(-1) and 172.7±0.8Jmol(-1)K(-1), respectively. There was a single binding site on α-d-glucosidase for lignin, and the binding distance was 3.2nm. The molecular docking analysis exhibited that the hydrogen bonds, hydropholic interaction, and van der Waals forces were the main forces for lignin bind to α-d-glucosidase. This work provides a new insight into the interaction between the lignin and α-d-glucosidase, which might be beneficial to type 2 diabetes with the application of lignin in functional food and pharmacy fields.

  15. 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.

  16. Fucoidan--a α-D-glucosidase inhibitor from Sargassum wightii with relevance to type 2 diabetes mellitus therapy.

    Science.gov (United States)

    Vinoth Kumar, T; Lakshmanasenthil, S; Geetharamani, D; Marudhupandi, T; Suja, G; Suganya, P

    2015-01-01

    The present study was conducted to screen the α-d-glucosidase inhibitory activity of fucoidan extracted from Sargassum wightii collected at Mandapam coastal area, Tamil Nadu, India. Fucoidan was extracted from the sporophyll of S. wightii using ethanol, acetone and CaCl2 precipitation. 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. FT-IR, NMR and in vitro α-d-glucosidase activity of purified fucoidan were performed. Fucoidan at the concentration of 31.25, 62.5, 125 and 250 μg exhibited 19, 31, 38 and 71% inhibition against α-d-glucosidase respectively in a dose dependent manner. The IC50 value against α-D-glucosidase of fucoidan is found to be 132.9 μg which is more effective than that of acarbose (1mg). The diverse biological activities of Fucoidan include anticancer, anti inflammatory and antimicrobial but the α-d-glucosidase inhibitory activity of native fucoidan from S. wightii for type 2 diabetes therapy is first of its kind.

  17. 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).

  18. Isolation and screening of glucosidase inhibitors from Chinese medicines

    Institute of Scientific and Technical Information of China (English)

    黄哲; 马骏; 原爱红; 夏佳慧; 孔宪涛

    2004-01-01

    Objective: To search for glucosidase inhibitors from Chinese medicines. Methods: Six kinds of widelyused Chinese medicines with the activity of decreasing blood glucose were prepared by the process of boiling, condensing,precipitating, exchanging with resins and rinsing. In vitro glucosidase inhibitory activities were examined by photometric bioassay derived from rats, yeast and almond of all the Chinese medicine extracts. Diabetic ICR mice models were established by intraperitoneal injection of STZ (200 mg/kg). To investigate the in vivo effect of lowering blood glucose, the mouse blood glucose level was assayed at 30 min after being given 2.5 g/kg starch and acarbose or varied concentrations of different constituents of some Chinese medicines by stomach tube. Results: The constituents of Sangye, Sangzhi, Sangbaipi, Dihuang and Yuzhu showed potent inhibitory activities against glucosidase. Furthermore, the first kind of constituents was proved to be beneficial in reducing blood glucose by in vivo glucose tolerance experiments. Conclusion: The constituents of Chinese medicines with reducing blood glucose effect have been discovered, thus providing a clue to novel drugs.

  19. 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.

  20. 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.

  1. Oral Fusobacterium nucleatum subsp. polymorphum binds to human salivary α-amylase.

    Science.gov (United States)

    Zulfiqar, M; Yamaguchi, T; Sato, S; Oho, T

    2013-12-01

    Fusobacterium nucleatum acts as an intermediate between early and late colonizers in the oral cavity. In this study, we showed that F. nucleatum subsp. polymorphum can bind to a salivary component with a molecular weight of approximately 110 kDa and identified the protein and another major factor of 55 kDa, as salivary α-amylase by time-of-flight mass spectrometry and immuno-reactions. Salivary α-amylase is present in both monomeric and dimeric forms and we found that formation of the dimer depends on copper ions. The F. nucleatum adhered to both monomeric and dimeric salivary α-amylases, but the numbers of bacteria bound to the dimeric form were more than those bound to the monomeric form. The degree of adherence of F. nucleatum to four α-amylases from different sources was almost the same, however its binding to β-amylase was considerably decreased. Among four α-amylase inhibitors tested, acarbose and type 1 and 3 inhibitors derived from wheat flour showed significant activity against the adhesion of F.nucleatum to monomeric and dimeric amylases, however voglibose had little effect. Moreover F. nucleatum cells inhibited the enzymatic activity of salivary α-amylase in a dose-dependent manner. These results suggest that F. nucleatum plays more important and positive role as an early colonizer for maturation of oral microbial colonization.

  2. Screening of α-Glucosidase Inhibitory Activity from Some Plants of Apocynaceae, Clusiaceae, Euphorbiaceae, and Rubiaceae

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    Berna Elya

    2012-01-01

    Full Text Available Diabetes mellitus (DM is recognized as a serious global health problem that is characterized by high blood sugar levels. Type 2 DM is more common in diabetic populations. In this type of DM, inhibition of α-glucosidase is a useful treatment to delay the absorption of glucose after meals. As a megabiodiversity country, Indonesia still has a lot of potential unexploited forests to be developed as a medicine source, including as the α-glucosidase inhibitor. In this study, we determine the α-glucosidase inhibitory activity of 80% ethanol extracts of leaves and twigs of some plants from the Apocynaceae, Clusiaceae, Euphorbiaceae, and Rubiaceae. Inhibitory activity test of the α-glucosidase was performed in vitro using spectrophotometric methods. Compared with the control acarbose (IC50 117.20 μg/mL, thirty-seven samples of forty-five were shown to be more potent α-glucosidase inhibitors with IC50 values in the range 2.33–112.02 μg/mL.

  3. Screening of α-glucosidase inhibitory activity from some plants of Apocynaceae, Clusiaceae, Euphorbiaceae, and Rubiaceae.

    Science.gov (United States)

    Elya, Berna; Basah, Katrin; Mun'im, Abdul; Yuliastuti, Wulan; Bangun, Anastasia; Septiana, Eva Kurnia

    2012-01-01

    Diabetes mellitus (DM) is recognized as a serious global health problem that is characterized by high blood sugar levels. Type 2 DM is more common in diabetic populations. In this type of DM, inhibition of α-glucosidase is a useful treatment to delay the absorption of glucose after meals. As a megabiodiversity country, Indonesia still has a lot of potential unexploited forests to be developed as a medicine source, including as the α-glucosidase inhibitor. In this study, we determine the α-glucosidase inhibitory activity of 80% ethanol extracts of leaves and twigs of some plants from the Apocynaceae, Clusiaceae, Euphorbiaceae, and Rubiaceae. Inhibitory activity test of the α-glucosidase was performed in vitro using spectrophotometric methods. Compared with the control acarbose (IC(50) 117.20 μg/mL), thirty-seven samples of forty-five were shown to be more potent α-glucosidase inhibitors with IC(50) values in the range 2.33-112.02 μg/mL.

  4. Comparative hypoglycemic activity of different fractions of Thymus serpyllum L. in alloxan induced diabetic rabbits.

    Science.gov (United States)

    Alamgeer, -; Mushtaq, Muhammad Naveed; Bashir, Sajid; Ullah, Ikram; Karim, Sabeha; Rashid, Muhammad; Malik, Muhammad Nasir Hayat; Rashid, Haroonur

    2016-09-01

    The aim of present study was to evaluate and compare the hypoglycemic activity of different solvents extracts of Thymus serpyllum in rabbits. Diabetes was induced with single intravenous injection of alloxan monohydrate (150mg/kg). Glibenclamide and acarbose were used as standard drugs. The crude powder of Thymus serpyllum (500 mg/kg b.w) significantly reduced blood glucose level in both normal and diabetic rabbits. Various extracts of Thymus serpyllum were compared for their hypoglycemic activity in diabetic rabbits. Ether and aqueous extracts significantly reduced the blood glucose level with maximum effect (p<0.001) produced by aqueous extract, which was selected for further study. Aqueous extract significantly inhibited the rise in glucose level in oral glucose tolerance test. The extract showed synergistic effect with different doses of insulin; however serum insulin level of the diabetic rabbits was not significantly increased by the extract. HbA1c level was significantly (p<0.05) reduced whereas hemoglobin level was significantly increased in three months study. Phytochemical screening of the aqueous extract showed the presence of alkaloids, flavonoids, tannins, terpinoids, reducing sugar and cardiac glycosides. It is concluded that the aqueous extract might be used alone or in combination with insulin to manage diabetes and its associated complications.

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

    Science.gov (United States)

    Payghami, Nasrin; Jamili, Shahla; Rustaiyan, Abdolhossein; Saeidnia, Soodabeh; Nikan, Marjan; Gohari, Ahmad Reza

    2014-01-01

    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. In this study, Sargassum glaucescens, collected from the seashore of Chabahar, was employed for phytochemical and biological evaluations. For that purpose, the dried algae was extracted by methanol and subjected to different chromatographic separation methods. 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 (IC50 = 8.9 ± 2.4 mg/mL) of the enzyme compared to acarbose as a positive control. 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. 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.

  7. Biology-oriented drug synthesis (BIODS) of 2-(2-methyl-5-nitro-1H-imidazol-1-yl)ethyl aryl ether derivatives, in vitro α-amylase inhibitory activity and in silico studies.

    Science.gov (United States)

    Taha, Muhammad; Imran, Syahrul; Ismail, Nor Hadiani; Selvaraj, Manikandan; Rahim, Fazal; Chigurupati, Sridevi; Ullah, Hayat; Khan, Fahad; Salar, Uzma; Javid, Muhammad Tariq; Vijayabalan, Shantini; Zaman, Khalid; Khan, Khalid Mohammed

    2017-10-01

    A new library of 2-(2-methyl-5-nitro-1H-imidazol-1-yl)ethyl aryl ether derivatives (1-23) were synthesized and characterized by EI-MS and (1)H NMR, and screened for their α-amylase inhibitory activity. Out of twenty-three derivatives, two molecules 19 (IC50=0.38±0.82µM) and 23 (IC50=1.66±0.14µM), showed excellent activity whereas the remaining compounds, except 10 and 17, showed good to moderate inhibition in the range of IC50=1.77-2.98µM when compared with the standard acarbose (IC50=1.66±0.1µM). A plausible structure-activity relationship has also been presented. In addition, in silico studies was carried out in order to rationalize the binding interaction of compounds with the active site of enzyme. Copyright © 2017 Elsevier Inc. All rights reserved.

  8. Computational drug design of potential α-amylase inhibitors using some commercially available flavonoids

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    Arumugam Madeswaran

    2014-03-01

    Full Text Available The primary objective of this study was to investigate the α-amylase inhibitory activity of flavonoids using in silico docking studies. In this perspective, flavonoids like biochanin, chrysin, hesperitin, morin, tricin and vitexycarpin were selected. Acarbose, a known α-amylase inhibitor was used as the stan-dard. In silico docking studies were carried out using AutoDock 4.2, based on the Lamarckian genetic algorithm principle. The results showed that all the selected flavonoids showed binding energy ranging between -7.20 kcal/mol to -6.21 kcal/mol when compared with that of the standard (-2.94 kcal/mol. Inhibition constant (5.31 µM to 27.89 µM and intermolecular energy (-8.99 kcal/mol to -7.41 kcal/mol of the flavonoids also coincide with the binding energy. The α-amylase inhibitory activity of the selected flavonoids was in order of tricin > hesperitin > vitexycarpin > chrysin > morin > biochanin. These molecular docking analyses could lead to the further development of potent α-amylase inhibitors for the treatment of diabetes.

  9. Aqueous Extract of Annona macroprophyllata: A Potential α-Glucosidase Inhibitor

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    F. Brindis

    2013-01-01

    Full Text Available Annona genus contains plants used in folk medicine for the treatment of diabetes. In the present study, an aqueous extract prepared from Annona macroprophyllata (Annonaceae, also known as A. diversifolia leaves was evaluated on both the activity of yeast α-glucosidase (an in vitro assay and sucrose tolerance in Wistar rats. The results have shown that the aqueous extract from A. macroprophyllata inhibits the yeast α-glucosidase with an IC50 = 1.18 mg/mL, in a competitive manner with a Ki = 0.97 mg/mL, a similar value to that of acarbose (Ki = 0.79 mg/mL. The inhibitory activity of A. macroprophyllata was reinforced by its antihyperglycemic effect, at doses of 100, 300, and 500 mg/kg in rats. Chromatographic analysis identified the flavonoids rutin and isoquercitrin in the most polar fractions of A. macroprophyllata crude extract, suggesting that these flavonoids are part of the active constituents in the plant. Our results support the use of A. macroprophyllata in Mexican folk medicine to control postprandial glycemia in people with diabetes mellitus, involving active constituents of flavonoid nature.

  10. Rosiglitazone.

    Science.gov (United States)

    Balfour, J A; Plosker, G L

    1999-06-01

    Rosiglitazone, a thiazolidinedione antidiabetic agent, improves insulin resistance, a key underlying metabolic abnormality in most patients with type 2 (non-insulin-dependent) diabetes mellitus. In animal models of insulin resistance, rosiglitazone decreased plasma glucose, insulin and triglyceride levels and also attenuated or prevented diabetic nephropathy and pancreatic islet cell degeneration. In contrast with troglitazone, rosiglitazone does not induce cytochrome P4503A4 metabolism. It does not interact significantly with nifedipine, oral contraceptives, metformin, digoxin, ranitidine or acarbose. In clinical trials in patients with type 2 diabetes mellitus, rosiglitazone 2 to 12 mg/day (as a single daily dose or 2 divided daily doses) improved glycaemic control, as shown by decreases in fasting plasma glucose and glycosylated haemoglobin (HbA1c). Addition of rosiglitazone 2 to 8 mg/day to existing sulphonylurea, metformin or insulin therapy achieved further reductions in fasting plasma glucose and HbA1c. Oral combinations improved insulin sensitivity and beta-cell function according to a homeostasis model assessment. Consistent with its mechanism of action, rosiglitazone appears to be associated with a low risk of hypoglycaemia (<2% of patients receiving monotherapy). There is no evidence to date that rosiglitazone shares the hepatotoxicity of troglitazone.

  11. Crystal structures of human pancreatic alpha-amylase in complex with carbohydrate and proteinaceous inhibitors.

    Science.gov (United States)

    Nahoum, V; Roux, G; Anton, V; Rougé, P; Puigserver, A; Bischoff, H; Henrissat, B; Payan, F

    2000-01-01

    Crystal structures of human pancreatic alpha-amylase (HPA) in complex with naturally occurring inhibitors have been solved. The tetrasaccharide acarbose and a pseudo-pentasaccharide of the trestatin family produced identical continuous electron densities corresponding to a pentasaccharide species, spanning the -3 to +2 subsites of the enzyme, presumably resulting from transglycosylation. Binding of the acarviosine core linked to a glucose residue at subsites -1 to +2 appears to be a critical part of the interaction process between alpha-amylases and trestatin-derived inhibitors. Two crystal forms, obtained at different values of pH, for the complex of HPA with the protein inhibitor from Phaseolus vulgaris (alpha-amylase inhibitor) have been solved. The flexible loop typical of the mammalian alpha-amylases was shown to exist in two different conformations, suggesting that loop closure is pH-sensitive. Structural information is provided for the important inhibitor residue, Arg-74, which has not been observed previously in structural analyses. PMID:10657258

  12. 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.

  13. Pathophysiology, diagnosis and management of postoperative dumping syndrome.

    Science.gov (United States)

    Tack, Jan; Arts, Joris; Caenepeel, Philip; De Wulf, Dominiek; Bisschops, Raf

    2009-10-01

    Dumping syndrome is a frequent complication of esophageal, gastric or bariatric surgery. Rapid gastric emptying, with the delivery to the small intestine of a significant proportion of solid food as large particles that are difficult to digest, is a key event in the pathogenesis of this syndrome. This occurrence causes a shift of fluid from the intravascular component to the intestinal lumen, which results in cardiovascular symptoms, release of several gastrointestinal and pancreatic hormones and late postprandial hypoglycemia. Early dumping symptoms comprise both gastrointestinal and vasomotor symptoms. Late dumping symptoms are the result of reactive hypoglycemia. Besides the assessment of clinical alertness and endoscopic or radiological imaging, a modified oral glucose tolerance test might help to establish a diagnosis. The first step in treating dumping syndrome is the introduction of dietary measures. Acarbose can be added to these measures for patients with hypoglycemia, whereas several studies advocate guar gum or pectin to slow gastric emptying. Somatostatin analogs are the most effective medical therapy for dumping syndrome, and a slow-release preparation is the treatment of choice. In patients with treatment-refractory dumping syndrome, surgical reintervention or continuous enteral feeding can be considered, but the outcomes of such approaches are variable.

  14. Octreotide improves early dumping syndrome potentially through incretins: a case report.

    Science.gov (United States)

    Sato, Daisuke; Morino, Katsutaro; Ohashi, Natsuko; Ueda, Emi; Ikeda, Kazuhiro; Yamamoto, Hideka; Ugi, Satoshi; Yamamoto, Hiroshi; Araki, Shinichi; Maegawa, Hiroshi

    2013-01-01

    Dumping syndrome, or rapid gastric emptying, is a frequent complication after gastric surgery. In this case, the patient was a 47-year-old woman who 10 years previously had undergone distal gastrectomy with Billroth I reconstruction for early-stage gastric cancer. She presented with symptoms of weakness, headache, palpitation, sweating, dizziness and significant fatigue between one and two hours after a meal. Because a 75 g oral glucose tolerance test (75 g-OGTT) induced both acute postprandial tachycardia (within 1 hour) and postprandial hypoglycemia, we diagnosed this patient with early and late dumping syndrome. Dietary measures and acarbose improved symptoms of late dumping syndrome but did not prevent the symptoms of early dumping syndrome such as postprandial tachycardia, weakness, headache, palpitation, and dizziness. We therefore used the somatostatin analogue octreotide, which has been reported as an effective therapy for early dumping syndrome. Octreotide prevented the symptoms of early dumping syndrome, especially postprandial tachycardia, but caused postprandial hyperglycemia. Glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP) were completely suppressed during the 75 g-OGTT following subcutaneous injection of octreotide. No change was observed in vasoactive intestinal polypeptide (VIP), which is the gastrointestinal peptide hormone generally responsible for early dumping syndrome, suggesting possible contribution of incretins in early dumping syndrome of this patient.

  15. A Rare Case of Noninsulinoma Pancreatogenous Hypoglycemia Syndrome

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    Jeffrey Nadelson

    2012-01-01

    Full Text Available As the obesity pandemic continues to worsen and medical interventions remain only moderately effective, bariatric surgery remains an important option for patients. In certain instances, patients who have undergone the procedure experience postprandial symptoms of neuroglycopenia caused by noninsulinoma pancreatogenous hypoglycemia syndrome (NIPHS. NIPHS is a recently described syndrome and is also very rare, and therapeutic approaches are still under debate. We report the case of a 51-year-old female who underwent Roux-en-Y gastric bypass and presented with episodic postprandial hypoglycemia 2 years after surgery. An insulinoma was absent from all abdominal imaging. Fasting C-peptide, insulin, and glucose were normal. Due to the possibility of NIPHS, clinical treatment was commenced with acarbose, leading to a significant reduction of hypoglycemic episodes. NIPHS occurs in approximately 0.5% to 7% of patients with hyperinsulinemic hypoglycemia. Sporadic hypoglycemia postgastric bypass is an important entity that should be understood by all surgeons and internists who are involved in postgastric bypass care.

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

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    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.

  17. Phlorotannins from Alaskan Seaweed Inhibit Carbolytic Enzyme Activity

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    Joshua Kellogg

    2014-10-01

    Full Text Available 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.

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

    Science.gov (United States)

    Yang, Yingbo; Gu, Lihua; Xiao, Ying; Liu, Qing; Hu, Haijun; Wang, Zhengtao; Chen, Kaixian

    2015-01-01

    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.

  19. Antioxidant and α-Amylase Inhibitory Property of Phyllanthus virgatus L.: An In Vitro and Molecular Interaction Study

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    Arshya Hashim

    2013-01-01

    Full Text Available The present study on Phyllanthus virgatus, known traditionally for its remedial potential, for the first time provides descriptions of the antioxidant and inhibition of α-amylase enzyme activity first by in vitro analyses, followed by a confirmatory in silico study to create a stronger biochemical rationale. Our results illustrated that P. virgatus methanol extract exhibited strong antioxidant and oxidative DNA damage protective activity than other extracts, which was well correlated with its total phenolic content. In addition, P. virgatus methanol extract strongly inhibited the α-amylase activity (IC50 33.20 ± 0.556 μg/mL, in a noncompetitive manner, than acarbose (IC50 76.88 ± 0.277 μg/mL, which showed competitive inhibition. Moreover, this extract stimulated the glucose uptake activity in 3T3-L1 cells and also showed a good correlation between antioxidant and α-amylase activities. The molecular docking studies of the major bioactive compounds (9,12-octadecadienoic acid, asarone, 11-octadecenoic acid, and acrylic acid revealed via GC-MS analysis from this extract mechanistically suggested that the inhibitory property may be due to the synergistic effect of these bioactive compounds. These results provide substantial basis for the future use of P. virgatus methanol extract and its bioactive compound in in vivo system for the treatment and management of diabetes as well as in the related condition of oxidative stress.

  20. Patient with pontine warning syndrome and bilateral posterior internuclear ophthalmoplegia: case report

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    Su Li

    2010-06-01

    Full Text Available Abstract Background Capsular warning syndrome was first described in 1993, featured with repetitive episodes of motor and/or sensory dysfunction without cortical signs. Recently, it has been demonstrated that clinically typical capsular warning syndrome can be associated with pontine infarct and the term “pontine warning syndrome� was coined. Case Presentation A 54-year-old woman with a history of hypertension was seen with profound left-sided hemiplegia. She had had 3 episodes of left-sided weakness before complete hemiplegia. Her speech was slurred. Left central facial palsy and hemiglossoplegia were presented. Her left plantar response was extensor and bilateral posterior internuclear ophthalmoplegia was seen on neurologic examination. Biochemical tests revealed hyperglycemia and dyslipidemia on the next day. MRI demonstrated an acute right paramedian pontine infarct. The patient was commenced on oral clopidogrel, atorvastatin and acarbose. After 23 days of hospitalization, she was discharged with severe left hemiplegia. Conclusions 1 Pontine warning syndrome may be underestimated and understudied. 2 Posterior internuclear ophthalmoplegia is a rare clinical sign in cerebrovascular diseases, while it can help to locate a brainstem lesion rather than an internal capsular one. 3 Blood pressure lowing administration may be improper for patients with pontine warning syndrome.

  1. 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.

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

    Science.gov (United States)

    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

  3. Enzymatic and molecular strategies to diagnose Pompe disease.

    Science.gov (United States)

    Reuser, Ajj; Verheijen, Fw; Kroos, Ma; Okumiya, T; Van Diggelen, Op; Van der Ploeg, At; Halley, Djj

    2010-01-01

    Enzyme replacement therapy for Pompe disease, a neuromuscular disorder characterized by lysosomal glycogen storage due to acid α-glucosidase deficiency, has entered the clinic. There is more than ever a need for early and reliable diagnosis. The objective of this review is to present a critical review of the recent literature on laboratory procedures to diagnose Pompe disease by enzymatic assay and DNA analysis. The methods we used were Compilation and expert interpretation of recent and relevant publications. The introduction of new and the updating of existing laboratory procedures have facilitated the diagnosis of Pompe disease (glycogen storage disease type II; acid maltase deficiency; OMIM 232300). With regard to enzymatic analysis, the application of acarbose as inhibitor of maltase-glucoamylase has enabled the use of mixed leukocyte preparations as diagnostic material. The use of glycogen as a natural substrate in the reaction mixture adds to the selectivity of this procedure. Newborn screening is envisaged and facilitated by the introduction of high-throughput procedures. DNA analysis has become an integral part of the diagnostic procedure for confirmation and completion, for carrier detection, and for genetic counseling.

  4. Zinc oxide nanoparticles as novel alpha-amylase inhibitors

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    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.

  5. In Vitro and In Vivo Effects of Norathyriol and Mangiferin on α-Glucosidase

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    Zhi-Long Shi

    2017-01-01

    Full Text Available Norathyriol is a metabolite of mangiferin. Mangiferin has been reported to inhibit α-glucosidase. To the best of our knowledge, no study has been conducted to determine or compare those two compounds on inhibiting α-glucosidase in vitro and in vivo by far. In this study, we determined the inhibitory activity of norathyriol and mangiferin on α-glucosidase in vitro and evaluated their antidiabetic effect in diabetic mice. The results showed that norathyriol inhibited α-glucosidase in a noncompetitive manner with an IC50 value of 3.12 μM, which is more potent than mangiferin (IC50 = 358.54 μM and positive drug acarbose (IC50 = 479.2 μM in the zymological experiment. Both of norathyriol and mangiferin caused significant (p<0.05 reduction in fasting blood glucose and the blood glucose levels at two hours after carbohydrate loading and it was interesting that mangiferin and norathyriol can make the decline of the blood glucose earlier than other groups ever including normal group in the starch tolerance test. However, norathyriol and mangiferin did not significantly influence carbohydrate absorption in the glucose tolerance test. Therefore, the antidiabetic effects of norathyriol and mangiferin might be associated with α-glucosidase, and norathyriol was more potent than mangiferin.

  6. Synthesis, biological evaluation and molecular docking studies of chromone hydrazone derivatives as α-glucosidase inhibitors.

    Science.gov (United States)

    Wang, Guangcheng; Chen, Ming; Wang, Jing; Peng, Yaping; Li, Luyao; Xie, ZhenZhen; Deng, Bing; Chen, Shan; Li, Wenbiao

    2017-07-01

    A series of chromone hydrazone derivatives 4a-4p have been synthesized, characterized by (1)H NMR and (13)C NMR and evaluated for theirinvitro α-glucosidase inhibitory activity. Out of these tested compounds, six (4a, 4b, 4d, 4j, 4o and 4p) displayed potent α-glucosidase inhibitory activity with IC50 values in the range of 20.1±0.19μM to 45.7±0.23μM, as compared to the standard drug acarbose (IC50=817.38±6.27μM). Among this series, compound 4d (IC50=20.1±0.19μM) with 4-sulfonamide substitution at phenyl part of hydrazide was found to be the most active compound. Lineweaver-Burk plot analysis indicated that compound 4d is a non-competitive inhibitor of α-glucosidase. The binding interactions of the most active analogs were confirmed through molecular docking studies. Docking studies showed 4d are interacting with the residues Glu-276, Asp-214, Asp-349 and Arg-439 through hydrogen bonds, arene-anion and arene-cation interactions. In summary, our studies shown that these chromone hydrazone derivatives are a new class of α-glucosidase inhibitors. Copyright © 2017 Elsevier Ltd. All rights reserved.

  7. Antioxidant, α-glucosidase and xanthine oxidase inhibitory activity of bioactive compounds from maize (Zea mays L.).

    Science.gov (United States)

    Nile, Shivraj H; Park, Se W

    2014-01-01

    Chemical investigations into maize (Zea mays L.) kernels yielded phenolic compounds, which were structurally established using chromatographic and spectroscopic methods. The isolated phenolic compounds from maize kernel were examined in vitro for their antioxidant abilities by DPPH (2,2-diphenyl-1-picryl hydrazine) radical, OH radical scavenging activity, and reducing ability, along with α-glucosidase and xanthine oxidase (XO) inhibition. The isolated maize phenolics revealed significant xanthine oxidase and α-glucosidase inhibitory activity to that of allopurinol and acarbose in vitro and in vivo, respectively. The kinetics study with xanthine oxidase revealed competitive type of inhibition by isolated maize vanillic acid (M2), ferulic acid (M5), 3'-methoxyhirsutrin (M7), and peonidin-3-glucoside (M10) as compared to control allopurinol. Overall, with few exceptions, all the phenolic compounds from maize kernel revealed significant biological activities with all parameters examined. Also, the phenolic compounds from maize were found to be more reactive toward DPPH radical and had considerable reducing ability and OH radical scavenging activity. These findings suggest that maize kernel phenolic compounds can be considered as potential antioxidant, α-glucosidase, and XO inhibitory agents those might be further explored for the design of lead antioxidant, antidiabetic and antigout drug candidates using in vivo trials.

  8. 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.

  9. 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.

  10. [Alpha-glucosidase inhibitory activity of Aeschynanthus maculatus].

    Science.gov (United States)

    Tian, Pu-yu; Kang, Wen-yi

    2012-10-01

    To study the inhibitory activity of Aeschynanthus maculatus on alpha-glucosidase. The inhibilitory model of in vitro alpha-glucosidase was established. Active extracts of A. maculatus were isolated and identified bymultiple chromatographic methods, and their molecular structures were identifiied by spectral techniques. Seven coumpounts were isolated from A. maculatus and isolated as lupeol(1), stigmasterol(2), ursolic acid(3), stigmast-5,22(E)-diene-3beta-ol(4), beta-daucosterol(5), 3-hydroxy-12-taraxasten-28-oic-acid(6) and oleanic acid(7). Compounds 1 (IC50 25.41 mg x L(-1)),3(IC0 4.42 mg L(-1)),4(IC50 11.50 mg x L(-1)),6(IC50 14.17 mg x L(-1)) and 7(IC50 2.88 mg x L(-1)) had higher inhibitory activities than that of acarbose (IC50 1103.01 mg x L(-1)) as the positive control drug. Compound 1-7 were isolated from this plant for the first time. Compound 6 was isolated from Gesneriaceae family for the first time. Compound 7 was isolated from Aeschynanthus genus for the first time.

  11. 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.

  12. 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.

  13. α-Glucosidass inhibitory activity of Sonchus oleraceus Linn%苦苣菜α-葡萄糖苷酶的抑制活性

    Institute of Scientific and Technical Information of China (English)

    江正样

    2010-01-01

    采用索氏提取法提取苦苣策全草,以96微孔板法测定苦苣菜不同极性提取物体外α-葡萄苷糖苷酶掏作用,并与阳性对照Acarbose进行比较,发现苦苣菜石油醚和乙酸乙酯提取物均有较好的α-葡萄糖苷酶抑制作用.苦苣菜的石油醚提取物的抑制效果最好(IC50=33.25μg·mL-1).其次为乙酸乙酯提取物(IC50=1909.14,1μg·mL-1).石油醚提取物远远大于阳性对照Acarbose(IC50=1103.01μg·mL-1)的抑制活性.不同溶剂的提取物比较,苦苣莱石油醚提取物对时α-葡萄糖苷酶活性的抑制效果很好,具有良好的潜在开发价值.

  14. Screening of minor bioactive compounds from herbal medicines by in silico docking and the trace peak exposure methods.

    Science.gov (United States)

    Wu, Bin; Song, Hui-Peng; Zhou, Xu; Liu, Xin-Guang; Gao, Wen; Dong, Xin; Li, Hui-Jun; Li, Ping; Yang, Hua

    2016-03-04

    Screening of high potent enzyme inhibitors from herbal medicines is always lacking of efficiency due to the complexity of chemicals. The constituents responsible for the holistic effect may be trace-level chemicals, but these chemicals were covered by highly abundant compositions. To challenge this bottleneck, a strategy for screening minor bioactive compounds was proposed. It generally included four steps, (1) preliminarily find the enzyme binders by ultrafiltration; (2) optimise and predict the potential inhibitors by docking analysis; (3) selectively identify and prepare trace compounds by segment and exposure approach; (4) validate the activity and summarize the structure-activity relationship. As a case study, α-glucosidase (AGH) and Ginkgo biloba extract were used as the experimental materials. By comprehensive screening, 11 trace flavones were screened out and identified as strong AGH inhibitors. Among them, AGH inhibitory activities of syringetin and sciadopitysin were reported for the first time. Their IC50 values were 36.80 and 8.29μM, respectively, which were lower than that of a positive control acarbose. In addition, the AGH inhibitory activities of the flavonoids could be ranked, based on a decreased order, as biflavone, flavone, flavone glycoside, flavone biglycoside. The strategy is expected to be practical and useful for screening bioactive molecules from herbal medicines, especially for the minor compounds, which will definitely accelerate the discovery of new drug candidates.

  15. 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.

  16. Structural enzymology of Cellvibrio japonicus Agd31B protein reveals α-transglucosylase activity in glycoside hydrolase family 31.

    Science.gov (United States)

    Larsbrink, Johan; Izumi, Atsushi; Hemsworth, Glyn R; Davies, Gideon J; Brumer, Harry

    2012-12-21

    The metabolism of the storage polysaccharides glycogen and starch is of vital importance to organisms from all domains of life. In bacteria, utilization of these α-glucans requires the concerted action of a variety of enzymes, including glycoside hydrolases, glycoside phosphorylases, and transglycosylases. In particular, transglycosylases from glycoside hydrolase family 13 (GH13) and GH77 play well established roles in α-glucan side chain (de)branching, regulation of oligo- and polysaccharide chain length, and formation of cyclic dextrans. Here, we present the biochemical and tertiary structural characterization of a new type of bacterial 1,4-α-glucan 4-α-glucosyltransferase from GH31. Distinct from 1,4-α-glucan 6-α-glucosyltransferases (EC 2.4.1.24) and 4-α-glucanotransferases (EC 2.4.1.25), this enzyme strictly transferred one glucosyl residue from α(1→4)-glucans in disproportionation reactions. Substrate hydrolysis was undetectable for a series of malto-oligosaccharides except maltose for which transglycosylation nonetheless dominated across a range of substrate concentrations. Crystallographic analysis of the enzyme in free, acarbose-complexed, and trapped 5-fluoro-β-glucosyl-enzyme intermediate forms revealed extended substrate interactions across one negative and up to three positive subsites, thus providing structural rationalization for the unique, single monosaccharide transferase activity of the enzyme.

  17. Natural Prenylchalconaringenins and Prenylnaringenins as Antidiabetic Agents: α-Glucosidase and α-Amylase Inhibition and in Vivo Antihyperglycemic and Antihyperlipidemic Effects.

    Science.gov (United States)

    Sun, Hua; Wang, Dong; Song, Xiaotong; Zhang, Yazhou; Ding, Weina; Peng, Xiaolin; Zhang, Xiaoting; Li, Yashan; Ma, Ying; Wang, Runling; Yu, Peng

    2017-03-01

    Inhibition of α-glucosidase and α-amylase decreases postprandial blood glucose levels and delays glucose absorption, making it a treatment strategy for type 2 diabetes. This study examined in vivo and in vitro antidiabetic activities of natural prenylchalconaringenins 1 and 2 and prenylnaringenins 3 and 4, found in hops and beer. 3'-Geranylchalconaringenin (2) competitively and irreversibly inhibited α-glucosidase (IC50 = 1.08 μM) with activity 50-fold higher than that of acarbose (IC50 = 51.30 μM) and showed moderate inhibitory activity against α-amylase (IC50 = 20.46 μM). Docking analysis substantiated these findings. In addition, compound 2 suppressed the increase in postprandial blood glucose levels and serum levels of total cholesterol and triglycerides in streptozotocin-induced diabetic mice. Taken together, these results suggest that 2 has dual inhibitory activity against α-glucosidase and α-amylase and alleviates diabetic hyperglycemia and hyperlipidemia, making it a potential functional food ingredient and drug candidate for management of type 2 diabetes.

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

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    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.

  19. 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.

  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. Induction of Diverse Bioactive Secondary Metabolites from the Mangrove Endophytic Fungus Trichoderma sp. (Strain 307 by Co-Cultivation with Acinetobacter johnsonii (Strain B2

    Directory of Open Access Journals (Sweden)

    Liuhong Zhang

    2017-02-01

    Full Text Available Two new sesquiterpenes, microsphaeropsisin B (1 and C (2, and two new de-O-methyllasiodiplodins, (3R, 7R-7-hydroxy-de-O-methyllasiodiplodin (4 and (3R-5-oxo-de-O-methyllasiodiplodin (5, together with one new natural product (6 and twelve known compounds (3, 7–17, were isolated from the co-cultivation of mangrove endophytic fungus Trichoderma sp. 307 and aquatic pathogenic bacterium Acinetobacter johnsonii B2. Their structures, including absolute configurations, were elucidated by extensive analysis of spectroscopic data, electronic circular dichroism, Mo2(AcO4-induced circular dichroism, and comparison with reported data. All of the isolated compounds were tested for their α-glucosidase inhibitory activity and cytotoxicity. New compounds 4 and 5 exhibited potent α-glucosidase inhibitory activity with IC50 values of 25.8 and 54.6 µM, respectively, which were more potent than the positive control (acarbose, IC50 = 703.8 µM. The good results of the tested bioactivity allowed us to explore α-glucosidase inhibitors in lasiodiplodins.

  4. Synthesis of novel inhibitors of α-glucosidase based on the benzothiazole skeleton containing benzohydrazide moiety and their molecular docking studies.

    Science.gov (United States)

    Taha, Muhammad; Ismail, Nor Hadiani; Lalani, Salima; Fatmi, Muhammad Qaiser; Atia-Tul-Wahab; Siddiqui, Salman; Khan, Khalid Mohammed; Imran, Syahrul; Choudhary, Muhammad Iqbal

    2015-03-06

    In an effort to design and synthesize a new class of α-glucosidase inhibitor, we synthesized benzothiazole hybrid having benzohydrazide moiety (5). Compound 5 was reacted with various substituted aryl aldehyde to generate a small library of compounds 6-35. Synthesis of compounds was confirmed by the spectral information. These compounds were screened for their α-glucosidase activity. They showed a varying degree of α-glucosidase inhibition with IC50 values ranging between 5.31 and 53.34 μM. Compounds 6, 7, 9-16, 19, 21-30, 32-35 showed superior activity as compared to standard acarbose (IC50 = 906 ± 6.3 μM). This has identified a new class of α-glucosidase inhibitors. The predicted physico-chemical properties indicated the drug appropriateness for most of these compounds, as they obey Lipinski's rule of five (RO5). A hybrid B3LYP density functional theory (DFT) was employed for energy, minimization of 3D structures for all synthetic compounds using 6-311 + G(d,p) basis sets followed by molecular docking to explore their interactions with human intestinal C- and N-terminal domains of α-glucosidase. All compounds bind to the prospective allosteric site of the C- terminal domain, and consequently, may be considered as mixed inhibitors. It was hypothesized that both the dipole moment and H-bond interactions govern the biological activation of these compounds.

  5. Antidiabetic and anticancer activities of Mangifera indica cv. Okrong leaves

    Science.gov (United States)

    Ganogpichayagrai, Aunyachulee; Palanuvej, Chanida; Ruangrungsi, Nijsiri

    2017-01-01

    Diabetes and cancer are a major global public health problem. Plant-derived agents with undesirable side-effects were required. This study aimed to evaluate antidiabetic and anticancer activities of the ethanolic leaf extract of Mangifera indica cv. Okrong and its active phytochemical compound, mangiferin. Antidiabetic activities against yeast α-glucosidase and rat intestinal α-glucosidase were determined using 1 mM of p-nitro phenyl-α-D-glucopyranoside as substrate. Inhibitory activity against porcine pancreatic α-amylase was performed using 1 mM of 2-chloro-4 nitrophenol-α-D-maltotroside-3 as substrate. Nitrophenol product was spectrophotometrically measured at 405 nm. Anticancer activity was evaluated against five human cancer cell lines compared to two human normal cell lines using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay. Mango leaf extract and mangiferin exhibited dose-dependent inhibition against yeast α-glucosidase with the IC50 of 0.0503 and 0.5813 mg/ml, respectively, against rat α-glucosidase with the IC50 of 1.4528 and 0.4333 mg/ml, respectively, compared to acarbose with the IC50 of 11.9285 and 0.4493 mg/ml, respectively. For anticancer activity, mango leaf extract, at ≥200 μg/ml showed cytotoxic potential against all tested cancer cell lines. In conclusion, mango leaf possessed antidiabetic and anticancer potential in vitro. PMID:28217550

  6. Antidiabetic and anticancer activities of Mangifera indica cv. Okrong leaves.

    Science.gov (United States)

    Ganogpichayagrai, Aunyachulee; Palanuvej, Chanida; Ruangrungsi, Nijsiri

    2017-01-01

    Diabetes and cancer are a major global public health problem. Plant-derived agents with undesirable side-effects were required. This study aimed to evaluate antidiabetic and anticancer activities of the ethanolic leaf extract of Mangifera indica cv. Okrong and its active phytochemical compound, mangiferin. Antidiabetic activities against yeast α-glucosidase and rat intestinal α-glucosidase were determined using 1 mM of p-nitro phenyl-α-D-glucopyranoside as substrate. Inhibitory activity against porcine pancreatic α-amylase was performed using 1 mM of 2-chloro-4 nitrophenol-α-D-maltotroside-3 as substrate. Nitrophenol product was spectrophotometrically measured at 405 nm. Anticancer activity was evaluated against five human cancer cell lines compared to two human normal cell lines using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay. Mango leaf extract and mangiferin exhibited dose-dependent inhibition against yeast α-glucosidase with the IC50 of 0.0503 and 0.5813 mg/ml, respectively, against rat α-glucosidase with the IC50 of 1.4528 and 0.4333 mg/ml, respectively, compared to acarbose with the IC50 of 11.9285 and 0.4493 mg/ml, respectively. For anticancer activity, mango leaf extract, at ≥200 μg/ml showed cytotoxic potential against all tested cancer cell lines. In conclusion, mango leaf possessed antidiabetic and anticancer potential in vitro.

  7. Antidiabetic and anticancer activities of Mangifera indica cv. Okrong leaves

    Directory of Open Access Journals (Sweden)

    Aunyachulee Ganogpichayagrai

    2017-01-01

    Full Text Available Diabetes and cancer are a major global public health problem. Plant-derived agents with undesirable side-effects were required. This study aimed to evaluate antidiabetic and anticancer activities of the ethanolic leaf extract of Mangifera indica cv. Okrong and its active phytochemical compound, mangiferin. Antidiabetic activities against yeast α-glucosidase and rat intestinal α-glucosidase were determined using 1 mM of p-nitrophenyl-α-D-glucopyranoside as substrate. Inhibitory activity against porcine pancreatic α-amylase was performed using 1 mM of 2-chloro-4 nitrophenol-α-D-maltotroside-3 as substrate. Nitrophenol product was spectrophotometrically measured at 405 nm. Anticancer activity was evaluated against five human cancer cell lines compared to two human normal cell lines using 3-(4,5-dimethylthiazol-2-yl-2,5-diphenyltetrazolium bromide assay. Mango leaf extract and mangiferin exhibited dose-dependent inhibition against yeast α-glucosidase with the IC 50 of 0.0503 and 0.5813 mg/ml, respectively, against rat α-glucosidase with the IC 50 of 1.4528 and 0.4333 mg/ml, respectively, compared to acarbose with the IC 50 of 11.9285 and 0.4493 mg/ml, respectively. For anticancer activity, mango leaf extract, at ≥200 μg/ml showed cytotoxic potential against all tested cancer cell lines. In conclusion, mango leaf possessed antidiabetic and anticancer potential in vitro.

  8. Diplotaxis simplex suppresses postprandial hyperglycemia in mice by inhibiting key-enzymes linked to type 2 diabetes

    Directory of Open Access Journals (Sweden)

    Hamida Jdir

    2015-04-01

    Full Text Available Abstract Nutritional properties of Diplotaxis simplex Spreng., Brassicaceae, an edible wild cruciferous largely distributed in North Africa, were investigated. Potassium (3690–3780 mg/100 g and calcium (900–1170 mg/100 g were the most concentrated minerals. Linoleinic acid was found to be the main fatty acid (25.4–27.7%, followed by palmitic acid (13.2–15.3%. Moreover, lipidic fraction of leaves was characterized by a relatively high rate of ethyl linoleate (14.4% and phytol (17.6%. Ethyl acetate extract of D. simplex flowers showed concentration-dependent α-amylase (IC50 3.46 mg/ml and α-glucosidase (IC50 0.046 mg/ml inhibitory activities. The positive in vitro enzymes inhibition was confirmed by a maltose tolerance test, which showed that treatment with flowers extract significantly inhibited the rise in blood glucose levels of maltose-loaded mice comparable to the standard antihyperglycemic agent acarbose. From these results, it may be concluded that D. simplex flowers can be used effectively as a safer alternative therapy to control postprandial hyperglycemia.

  9. Preventive pharmacotherapy in type 2 diabetes mellitus.

    Science.gov (United States)

    Choudhary, Neeraj; Kalra, Sanjay; Unnikrishnan, Ambika Gopalkrishnan; Ajish, T P

    2012-01-01

    Over the last few decades certain demographic changes have been observed worldwide, which have led to an increase in the prevalence of chronic non-communicable diseases. Type 2 diabetes mellitus and associated cardiovascular disease are major contributors to this disease burden leading to rising morbidity and mortality. It is worrisome to see that type 2 diabetes with its micro- and macrovascular complications is occurring in younger populations where it was hitherto unseen. Prevention appears to be an important strategy to reduce the burden of disease. Along with inculcating healthy lifestyle habits across populations, it may be suitable to use preventive pharmacotherapy in those with pre-diabetes and / or other risk factors like obesity, hypertension, and on the like. Metformin, alpha glucosidase inhibitors like acarbose, miglitol, and voglibose, and pioglitazone have all been used with success. The issues of compliance and adverse effects during long-term use have tempered the use of these drugs. The best approach would be to motivate the patient for effective lifestyle changes, and pharmacological management if the lifestyle changes are not successful in achieving their goals.

  10. [Adjunctive therapies to glycaemic control of type 1 diabetes mellitus].

    Science.gov (United States)

    Gabbay, Mônica de A Lima

    2008-03-01

    Since Diabetes Control and Complications Trial (DCCT), intensive therapy has been directed at achieving glucose and glycosylated hemoglobin (HbA1c) values as close to normal as possible regarding safety issues. However, hyperglycemia (especially postprandial hyperglycemia) and hypoglicemia continue to be problematic in the management of type 1 diabetes. The objective of associating other drugs to insulin therapy is to achieve better metabolic control lowering postprandial blood glucose levels. Adjunctive therapies can be divided in four categories based on their mechanism of action: enhancement of insulin action (e.g. the biguanides and thiazolidinediones), alteration of gastrointestinal nutrient delivery (e.g. acarbose and amylin) and other targets of action (e.g. pirenzepine, insulin-like growth factor I and glucagon-like peptide-1). Many of these agents have been found to be effective in short-term studies with decreases in HbA1c of 0.5-1%, lowering postprandial blood glucose levels and decreasing daily insulin doses.

  11. 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.

  12. 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

  13. Characterization and Comparison of Protein and Peptide Profiles and their Biological Activities of Improved Common Bean Cultivars (Phaseolus vulgaris L.) from Mexico and Brazil.

    Science.gov (United States)

    Mojica, Luis; de Mejía, Elvira González

    2015-06-01

    Common bean (Phaseolus vulgaris L.) is a good source of protein, vitamins, minerals and complex carbohydrates. The objective was to compare protein profile, including anti-nutrient proteins, and potential bioactive peptides of improved common bean cultivars grown in Mexico and Brazil. Bean protein isolates (BPI) were prepared from 15 common bean cultivars and hydrolyzed using pepsin/pancreatin. Thirteen proteins were identified by SDS-PAGE and protein in-gel tryptic-digestion-LC/MS. Protein profile was similar among common bean cultivars with high concentrations of defense-related proteins. Major identified proteins were phaseolin, lectin, protease and α-amylase inhibitors. Lectin (159.2 to 357.9 mg lectin/g BPI), Kunitz trypsin inhibitor (inh) (4.3 to 75.5 mg trypsin inh/g BPI), Bowman-Birk inhibitor (5.4 to 14.3 μg trypsin-chymotrypsin inh/g BPI) and α-amylase inhibitor activity (2.5 to 14.9% inhibition relative to acarbose/mg BPI) were higher in Mexican beans compared to Brazilian beans. Abundant peptides were identified by HPLC-MS/MS with molecular masses ranging from 300 to 1500 Da and significant sequences were SGAM, DSSG, LLAH, YVAT, EPTE and KPKL. Potential bioactivities of sequenced peptides were angiotensin converting enzyme inhibitor (ACE), dipeptidyl peptidase IV inhibitor (DPP-IV) and antioxidant capacity. Peptides from common bean proteins presented potential biological activities related to control of hypertension and type-2 diabetes.

  14. 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.

  15. 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.

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

    Directory of Open Access Journals (Sweden)

    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.

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

    Directory of Open Access Journals (Sweden)

    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.

  18. Extraction optimization and in vitro and in vivo anti-postprandial hyperglycemia effects of inhibitor from Phoenix dactylifera L. parthenocarpic fruit.

    Science.gov (United States)

    El Abed, Hanen; Chakroun, Mouna; Fendri, Imen; Makni, Mohamed; Bouaziz, Mohamed; Drira, Noureddine; Mejdoub, Hafedh; Khemakhem, Bassem

    2017-04-01

    Phoenix dactylifera L. plays an important role in social, economic, and ecological Tunisian sectors. Some date palms produce parthenocarpic fruit named Sish. The aqueous ethanolic extract from P. dactylifera parthenocarpic dates demonstrated a potent inhibition of the enzymes related to type II diabetes. In this work, extraction optimization of amylase inhibitors was carried out using Box-Behnken Design. Bioactivity-guided fractionation of the 70% aqueous ethanol extract was performed to identify the active compounds. The physicochemical results by liquid chromatography-tandem mass spectrometry (LC-MS/MS) analysis showed the presence of 13 phenolic compounds. The in vitro study showed that the extract exhibited a more specific inhibitor of α-glucosidase than α-amylase with an IC50 value of 0.6 and 2.5mg/mL, respectively. The in vivo study of this extract effect on the postprandial hyperglycemia activity showed a decrease in plasma glucose levels after 30min stronger than the Acarbose effect. These results confirmed the anti-postprandial hyperglycemia activity of the aqueous ethanolic extract from P. dactylifera parthenocarpic dates, which could lend support for its pharmaceutical use.

  19. α-Glucosidase inhibitory activity and cytotoxic effects of some cyclic urea and carbamate derivatives.

    Science.gov (United States)

    Popović-Djordjević, Jelena B; Jevtić, Ivana I; Grozdanić, Nadja Dj; Šegan, Sandra B; Zlatović, Mario V; Ivanović, Milovan D; Stanojković, Tatjana P

    2017-12-01

    The inhibitory activities of selected cyclic urea and carbamate derivatives (1-13) toward α-glucosidase (α-Gls) in in vitro assay were examined in this study. All examined compounds showed higher inhibitory activity (IC50) against α-Gls compared to standard antidiabetic drug acarbose. The most potent was benzyl (3,4,5-trimethoxyphenyl)carbamate (12) with IC50 = 49.85 ± 0.10 µM. In vitro cytotoxicity of the investigated compounds was tested on three human cancer cell lines HeLa, A549 and MDA-MB-453 using MTT assay. The best antitumour activity was achieved with compound 2 (trans-5-phenethyl-1-phenylhexahydro-1H-imidazo[4,5-c]pyridin-2(3H)-one) against MDA-MB-453 human breast cancer cell line (IC50 = 83.41 ± 1.60 µM). Cyclic ureas and carbamates showed promising anti-α-glucosidase activity and should be further tested as potential antidiabetic drugs. The PLS model of preliminary QSAR study indicated that, in planing the future synthesis of more potent compounds, the newly designed should have the substituents capable of polar interactions with receptor sites in various positions, while avoiding the increase of their lipophilicity.

  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. Effect of dietary supplementation of Padauk (Pterocarpus soyauxii) leaf on high fat diet/streptozotocin induced diabetes in rats' brain and platelets.

    Science.gov (United States)

    Saliu, Jamiyu A; Oboh, Ganiyu; Omojokun, Olasunkanmi S; Rocha, João B T; Schetinger, Maria R; Guterries, Jessie; Stefanello, Naiara; Carvalho, Fabiano; Schmatz, Roberta; Morsch, Vera M; Boligon, Aline

    2016-12-01

    This study investigated the effects of Padauk leaf on brain malondialdehyde (MDA) content, acetylcholinesterase (AChE) activities, ectonucleotidases and adenosine deaminase (ADA) activities in the platelet of high fat diet and streptozotocin (STZ)-induced diabetic rats. The animals were divided into six groups (n=7): normal control rats; diabetic rats+high fat diet (HFD); diabetic rats+HFD+Metformin; diabetic rats+HFD+acarbose; diabetic rats+HFD+10% Padauk leaf; normal rats+basal diet+10% Padauk leaf. After 30days of experiment comprising of acclimatization, dietary manipulation, pre-treatment with STZ and supplementation with Padauk leaf, the animals were sacrificed and the rats' brain and blood were collected for subsequent analysis. The results demonstrated that the elevated MDA content and AChE activity in the diabetic rats were significantly reduced when compared with the control rats. Furthermore, the increased NTPDases, 5'-nucleotidase and ADA activities in the diabetic rats were significantly reduced when compared with the control rats. This study demonstrated that Padauk leaf exhibited modulatory effects on purinergic and cholinergic enzymes involved in the prevention of platelet abnormality and consequent vascular complications in diabetic state. Copyright © 2016 Elsevier Masson SAS. All rights reserved.

  2. 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.

  3. 草麻黄对α-葡萄糖苷酶的抑制作用研究%α-Glucosidase Inhibitory Activity of Ephedrae sinica

    Institute of Scientific and Technical Information of China (English)

    康文艺; 曹乃锋

    2012-01-01

    采用96微孔板法测定草麻黄抑制α-葡萄糖苷酶活性.草麻黄正丁醇(IC50=6.86 μg/mL)、乙酸乙酯(IC50 =77.28 μg/mL)和石油醚部位(IC50=190.20 μg/mL)抑制活性远高于阳性对照阿卡波糖(IC50=1081.27μg/mL).研究表明,草麻黄各部位均具有很好的α-筒萄糖苷酶抑制活性,可进行活性追踪分离活性成分.%α-Clucosidase inhibitory activity of Ephedrae sinica was screened by the method of 96-microplates. The activities of n-Butanol (IC50 =6.86 μg/mL) ,ethyl acetate (IC50 = 77.28 μg/mL) and petroleum ether (IC50 = 190.20 μg/ mL) were higher than that of acarbose (IC50 = 1081.27 μg/mL) . The results showed that all parts from E. sinica had α-glucosidase inhibitory activity and active compounds should be isolated by the method of bioassay-guided fractionation in further study.

  4. 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.

  5. Modulation of starch digestion for slow glucose release through "toggling" of activities of mucosal α-glucosidases.

    Science.gov (United States)

    Lee, Byung-Hoo; Eskandari, Razieh; Jones, Kyra; Reddy, Kongara Ravinder; Quezada-Calvillo, Roberto; Nichols, Buford L; Rose, David R; Hamaker, Bruce R; Pinto, B Mario

    2012-09-14

    Starch digestion involves the breakdown by α-amylase to small linear and branched malto-oligosaccharides, which are in turn hydrolyzed to glucose by the mucosal α-glucosidases, maltase-glucoamylase (MGAM) and sucrase-isomaltase (SI). MGAM and SI are anchored to the small intestinal brush-border epithelial cells, and each contains a catalytic N- and C-terminal subunit. All four subunits have α-1,4-exohydrolytic glucosidase activity, and the SI N-terminal subunit has an additional exo-debranching activity on the α-1,6-linkage. Inhibition of α-amylase and/or α-glucosidases is a strategy for treatment of type 2 diabetes. We illustrate here the concept of "toggling": differential inhibition of subunits to examine more refined control of glucogenesis of the α-amylolyzed starch malto-oligosaccharides with the aim of slow glucose delivery. Recombinant MGAM and SI subunits were individually assayed with α-amylolyzed waxy corn starch, consisting mainly of maltose, maltotriose, and branched α-limit dextrins, as substrate in the presence of four different inhibitors: acarbose and three sulfonium ion compounds. The IC(50) values show that the four α-glucosidase subunits could be differentially inhibited. The results support the prospect of controlling starch digestion rates to induce slow glucose release through the toggling of activities of the mucosal α-glucosidases by selective enzyme inhibition. This approach could also be used to probe associated metabolic diseases.

  6. Investigating on the Correlation Between Some Biological Activities of Marine Sponge-Associated Bacteria Extracts and Isolated Diketopiperazines.

    Science.gov (United States)

    Abd El-Hady, Faten K; Fayad, Walid; Iodice, Carmine; El-Shahid, Zeinab A; Abdel-Aziz, Mohamed S; Crudele, Egle; Tommonaro, Giuseppina

    2017-01-01

    Marine organisms have been considered as the richest sources of novel bioactive metabolites, which can be used for pharmaceutical purposes. In the last years, the interest for marine microorganisms has grown for their enormous biodiversity and for the evidence that many novel compounds isolated from marine invertebrates are really synthesized by their associated bacteria. Nevertheless, the discovery of a chemical communication Quorum sensing (QS) between bacterial cells and between bacteria and host has gained the researchers to expand the aim of their study toward the role of bacteria associated with marine invertebrates, such as marine sponge. In the present paper, we report the evaluation of biological activities of different extracts of bacteria Vibrio sp. and Bacillus sp. associated with marine sponges Dysidea avara and Ircinia variabilis, respectively. Moreover, we evaluated the biological activities of some diketopiperazines (DKPs), previously isolated, and able to activate QS mechanism. The results showed that all extracts, fractions, and DKPs showed low scavenging activity against DPPH and superoxide anion, low cytotoxic and anti-tyrosinase activities, but no antimicrobial and acetylcholinesterase inhibitory activities. One DKP [cyclo-(trans-4-hydroxy-L-prolyl-L-leucine)] has the highest α-glucosidase inhibitory activity even than the standard acarbose.

  7. Enzyme inhibitory and radical scavenging effects of some antidiabetic plants of Turkey

    Directory of Open Access Journals (Sweden)

    Nilüfer Orhan

    2014-06-01

    Full Text Available Objective(s:Ethnopharmacological field surveys demonstrated that many plants, such as Gentiana olivieri, Helichrysum graveolens, Helichrysum plicatum ssp. plicatum, Juniperus oxycedrus ssp. oxycedrus, Juniperus  communis var. saxatilis, Viscum album (ssp. album, ssp. austriacum, are used as traditional medicine for diabetes in different regions of Anatolia. The present study was designed to evaluate the in vitro antidiabetic effects of some selected plants, tested in animal models recently. Materials and Methods: α-glucosidase and α-amylase enzyme inhibitory effects of the plant extracts were investigated and Acarbose was used as a reference drug. Additionally, radical scavenging capacities were determined using 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid ABTS radical cation scavenging assay and total phenolic content of the extracts were evaluated using Folin Ciocalteu method. Results: H. graveolens ethanol extract exhibited the highest inhibitory activity (55.7 % ± 2.2 on α-amylase enzyme. Additionally, J. oxycedrus hydro-alcoholic leaf extract had potent α-amylase inhibitory effect, while the hydro-alcoholic extract of J. communis fruit showed the highest α-glucosidase inhibitory activity (IC50: 4.4 μg/ml. Conclusion:Results indicated that, antidiabetic effect of hydro-alcoholic extracts of H. graveolens capitulums, J. communis fruit and J. oxycedrus leaf might arise from inhibition of digestive enzymes.

  8. 2型糖尿病三种治疗方案的成本-效果分析%Cost-Effectiveness Analysis of 3 Therapeutic Schemes in the Treatment of Type2 Diabetes

    Institute of Scientific and Technical Information of China (English)

    张建柱

    2013-01-01

    Objective:To evaluate the clinical and economic effects of three hypoglycemic drugs for type 2 diabetes. Methods:273 cases of type 2 diabetes were randomly divided into 3 groups,each group 91 persons.Group A was treated by Metformin combined with Glibenclamide;Group B was treated by Metformin combined with Acarbose; Group C was treated by Acarbose combined with Repaglinide. The blood glucose level of patients in each group was regularly monitored.The economic effectiveness,adverse reactions,and medication effects were analyzed before treatment and after 6 months treatment.Results:The FPG, PBG and HbA1c of three groups were ideally controlled.The total effective rates of group A, B and C were 82.4%,84.6% and 85.7%, respectively (P>0. 05).The cost-effect ratio of group A、B、C is respectively:1.376、16.276 and 23.733.The overrun cost-effect ratio of group B、C to group A is 574.36 and 582.0, respectively.Conclusion:The three groups of treatment of type 2 diabetes have better efficacy of the program.However,considering from cost and total effective rate,the scheme Metformin combined with Glibenclamide is the better choice.%  目的:评价我院三种治疗2型糖尿病方法的临床疗效及经济成本.方法:选择我院273例2型糖尿病患者,随机分为三组,实施三种联合用药治疗方案.A组二甲双胍+格列本脲,B组二甲双胍+阿卡波糖,C组阿卡波糖+瑞格列奈;定期对各组患者的血糖水平进行监测,经过6个月的治疗,进行经济效果、不良反应及药物疗效分析.结果:三组在治疗后的FPG、PGB、HbA1c均得到较理想的控制.A、B、C组总有效率分别为82.4%,84.6%和85.7%(P>0.05)无显著性差异;A、B、C、组成本-效果比(C/E)分别为1.376、16.276和23.733,B、C组对于A组的增量成本-效果比(△C/△E)分别为74.36和582.0.结论:各组治疗2型糖尿病的用药方案疗效均较好,但从经济成本及总有效率等方面综合考虑,二甲双胍+格列本脲方案为较佳选择.

  9. 具斑芒毛苣苔抑制α-葡萄糖苷酶活性成分研究%α-Glucosidase inhibitory activity of Aeschynanthus maculatus

    Institute of Scientific and Technical Information of China (English)

    田璞玉; 康文艺

    2012-01-01

    Objective: To study the inhibitory activity of Aeschynanthus maculatus on α-glucosidase. Method; The inhibilitory model of in vitro α-glucosidase was established. Active extracts of A. maculatus were isolated and identified bymultiple chromatographic methods, and their molecular structures were identifiied by spectral techniques. Result; Seven coumpounts were isolated from A. maculatus and isolated as lupeol(l) , stigmasterol(2) , ursolic acid(3) , stigmast-5 ,22( E)-diene-3β-ol(4) , β-daucosterol(5) , 3-hydro xy-12-taraxasten-28-oic-acid(6) and oleanic acid(7). Compounds 1 (IC50 25.41 mg · L-1 ) ,3( IC50 4. 42 mg · L-1),4(IC50 11.50 mg · L-1 ) ,6( IC50 14. 17 mg · L-1 ) and 7(IC5() 2. 88 mg · L-1 ) had higher inhibitory activities than that of acarbose( IC501 103.01 mg · L-1 ) as the positive control drug. Conclusion; Compound 1-7 were isolated from this plant for the first time. Compound 6 was isolated from Gesneriaceae family for the first time. Compound 7 was isolated from Aeschynanthus genus for the first time.%目的:研究具斑芒毛苣苔抑制α-葡萄糖苷酶的活性成分.方法:用体外α-葡萄糖苷酶抑制模型筛选;采用各种色谱法对高活性部位分离,运用多种波谱技术鉴定结构.结果:从具斑芒毛苣苔分离得到7个化合物,分别为羽扇豆醇(1),豆甾醇(2),熊果酸(3),豆甾-5,22(E)-二烯-3β-醇(4)和β-胡萝卜苷(5),3-hydroxy-12-taraxasten-28-oic-acid(6),齐墩果酸(7).化合物1(IC50 25.41 mg·L-1),3(IC50 4.42 mg·L-1),4(IC50 11.50 mg·L-1),6(IC50 14.17 mg·L-1)和7(IC50 2.88mg·L-1)的体外抑制α-葡萄糖苷酶活性高于阳性对照药物acarbose(IC50 1 103.01 mg· L-1).结论:化合物1~7为首次从该植物中分离得到,6为首次从该科中分离得到,7为首次从该属植物中分离得到.

  10. Effect of Extracts from Coriopsis ticntoria Flowers of Xinjiang Kunlun Mountain on α-glucosidase Activity%新疆昆仑雪菊5种提取物对α-葡萄糖昔酶活性的影响

    Institute of Scientific and Technical Information of China (English)

    张燕; 李琳琳; 木合布力·阿布力孜; 王丽凤; 景兆均; 毛新民

    2011-01-01

    目的:研究昆仑雪菊(CTF)提取物对α-葡萄糖苷酶活性的影响.方法:用水提法和有机溶剂萃取法制备昆仑雪菊的提取物,得到雪菊乙酸乙酯提取物、雪菊正丁醇提取物、雪菊总黄酮、雪菊水提物和雪菊中性黄酮;用体外α-葡萄糖昔酶抑制模型,对5种雪菊提取物进行α-葡萄糖苷酶抑制活性筛选,并与阳性对照药阿卡波糖进行比较.结果:昆仑雪菊的5种提取物对α-葡萄糖苷酶的活性均有较强的抑制作用,有4个提取物的抑制率高于阿卡波糖,其中雪菊中性黄酮的活性最强,在0.05 g·L-1时,其酶抑制率高达87.26 %a.阿卡波糖及5种提取物对α-葡萄糖苷酶抑制作用的IC50分别为:阿卡波糖IC50858.0mg·L-1,雪菊乙酸乙酸提取物IC50 12.5 mg·L-1,雪菊正T醇提取物IC50 139.5 mg·L-1,雪菊总黄酮IC50 163.5 mg·L-1,雪菊水提物IC50 367.6 mg·L-1,雪菊中性黄酮IC50 5.8 mg·L-1.结论:昆仑雪菊提取物能显著抑制α-葡萄糖苷酶活性.%Objective: To study the effect extracts from Xinjiang Coriopsis ticntoria flowers (CTF) on α-glucosidase activity. Method: Five extracts of CTF were prepared by water extraction and organic solvent abstraction. Including CTF ethylacetate extraction, CTF normal butyl alcohol extraction, CTF total flavanone, CTF water extraction and CTF neutral flavanone. The inhibitory effects of these extracts to α-glucosidase activity were investigated by in vitro enzymatic method; and akarbose was used as positive reference substance. Result: The extracts of CTF showed obviously inhibitory action against α-glucosidase activity in which 4 extracts have higher effects compared to those of acarbose, among them, the extract of CTF neutral flavanone was more effective for enzyme inhibition with a inhibitory rate of 87.26%. The CTF IC50 of the five extracts were: Acarbose IC50858.0 mg · L-1, CTF ethylacetate extraction IC50 12. 5 mg·L-1, CTF normal butyl alcohol extraction IC50 139.5 mg

  11. α-Glucosidase Inhibitory and Antioxidant Activity of Ardisia crenata%朱砂根抑制α-葡萄糖苷酶与抗氧化活性研究

    Institute of Scientific and Technical Information of China (English)

    李园园; 李锟; 王俊霞; 康文艺

    2012-01-01

    To investigate the a-glucosidase inhibitory and antioxidant activity of Ardisia crenata,96-microplate-based method was used to assay a-glucosidase inhibitory activity of A. crenata and antioxidant activity was determined by the method of DPPH,ABTS,and FRAP. The results showed that the ethyl acetate extract (IC50 =39. 27 μg/mL) had the highest a-glucosidase inhibitory activity,the petroleum ether extract came second (IC50 =56.11 μg/mL) ,and the n-bu-tanol extract was the weakest (IC50 = 62.05 μg/mL). But all of them showed higher activity than that of Acarbose (IC50 = 1081.27 μg/mL). The ethyl acetate extract showed the highest antioxidant activity which was higher than that of n-butanol extract. The DPPH radical scavenging activity of ethyl acetate extract (IC50 = 38.55 mg/L) was half of BHT (IC50 = 18.71 mg/L) while ABTS radical scavenging activity (IC50 = 3.60 mg/L) was higher than that of BHT (IC50 = 7.44 mg/L) and lower than that of BHA (IC50 = 1.74 mg/L). It exhibited the ferric reducing antioxidant power ( FRAP = 512.99 ± 6.80 μmol TE/g) which was almost one third of BHT ( FRAP = 1581.68 ± 97.41 μmol TE/g). The results indicated that the ethyl acetate extract of A. crenata exhibited the strongest activity of a-glucosidase inhibitory and antioxidant activities.%对朱砂根抑制α-葡萄糖苷酶与抗氧化活性进行研究.利用96微孔板法筛选α-葡萄糖苷酶抑制活性;采用DPPH、ABTS和FRAP方法分析抗氧化活性.结果表明,乙酸乙酯部位抑制α-葡萄糖苷酶的活性最高(IC50=39.27 μg/mL),石油醚部位次之(IC50 =56.11 μg/mL),正丁醇部位活性最弱(IC50=62.05μg/mL),但均远大于阳性对照Acarbose(IC50=1081.27 μg/mL);乙酸乙酯部位抗氧化能力最强,正丁醇部位次之.乙酸乙酯部位清除DPPH自由基(IC50=38.55 mg/L)的能力比BHT( IC50=18.71 mg/L)低1/2,清除ABTS自由基的能力(IC50=3.60 mg/L)比BHT(IC50=7.44 mg/L)强,但比BHA(IC50=1.74 mg/L)弱,还原Fe3+的能力(FRAP=512.99

  12. Potent α-glucosidase and protein tyrosine phosphatase 1B inhibitors from Artemisia capillaris.

    Science.gov (United States)

    Nurul Islam, Md; Jung, Hyun Ah; Sohn, Hee Sook; Kim, Hye Mi; Choi, Jae Sue

    2013-05-01

    As a part of our ongoing effort to identify anti-diabetic constituents from natural sources, we examined the inhibitory activity of the methanol extracts of 12 species of the genus Artemisia, against α-glucosidase and protein tyrosine phosphatase 1B (PTP1B). The methanol extracts of different species exhibited promising α-glucosidase and PTP1B inhibitory activities. Since the methanol extract of Artemisia capillaris exhibited the highest α-glucosidase inhibitory activity together with significant PTP1B inhibitory activity, it was selected for further investigation. Repeated column chromatography based on bioactivity guided fractionation yielded 10 coumarins (esculetin, esculin, scopolin, isoscopolin, daphnetin, umbelliferone, 7-methoxy coumarin, scoparone, scopoletin, 6-methoxy artemicapin C), 8 flavonoids (hyperoside, quercetin, isorhamnetin, cirsilineol, arcapillin, isorhamnetin 3-robinobioside, linarin, isorhamnetin 3-glucoiside), 6 phenolic compounds (1,5-dicaffeoylquinic acid, 3,4-dicaffeoylquinic acid, 3,5-dicaffeoylquinic acid, 3,5-dicaffeoylquinic acid methyl ester, 4,5-dicaffeoylquinic acid, 3-caffeoylquinic acid), and one chromone (capillarisin). Among these compounds, esculetin, scopoletin, quercetin, hyperoside, isorhamnetin, 3,5-dicaffeoylquinic acid methyl ester, 3,4-dicaffeoylquinic acid, and 1,5-dicaffeoylquinic acid exhibited potent α-glucosidase inhibitory activity when compared to the positive control acarbose. In addition, esculetin and 6-methoxy artemicapin C displayed PTP1B inhibitory activity. Interestingly, all isolated dicaffeoylquinic acids showed significant PTP1B inhibitory activity. Therefore, the results of the present study clearly demonstrate the potential of the A. capillaris extract to inhibit α-glucosidase and PTP1B. These inhibitory properties can be largely attributed to a combination of different chemical structures, including coumarins, flavonoids, and dicaffeoylquinic acids, which could be further explored to develop

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

    Directory of Open Access Journals (Sweden)

    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

  14. Postprandial hypoglycemic syndrome

    Directory of Open Access Journals (Sweden)

    Т.V. Chaychenko

    2017-06-01

    Full Text Available Postprandial hypoglycemic syndrome, or reactive hypoglycemia, — vegetative symptoms, such as weakness, fatigue, hunger, nausea, palpitations, anxiety, tremor, sweating occurring one to two hours after ingestion. The syndrome is poorly described in literature and most of the information is disparate. Laboratory criteria for the diagnosis of postprandial reactive hypoglycemia are quite controversial, but most authors tend to consider that it is a blood glucose level, which is below 3.9 mmol/l for two hours after meal. Hypoglycemia is an unbalance between glucose influx to the circulation (from endogenous glucose production or exogenous glucose delivery and glucose efflux. The balance between glucose intake and consumption is controlled by a complex balance of glycoregulatory hormones. Insulin, glucagon and adrenaline are effective for several minutes, but cortisol and growth hormone — for seve-ral hours. This explains the presence of immediate and delayed various effects: adrenergic, neuroglycopenic ones and gastroin-testinal discomfort. Postprandial syndrome mechanisms are similar to post-gastric bypass patients with morbid obesity. The most likely cause of reactive hypoglycemia is post-prandial hypersecretion of insulin under the influence of glucose and glucagon-like peptide-1 (GLP-1, which is a component of the enteroendocrine system and acts at the cephalic phase of satiety. Both post-gastric bypass and relatively healthy individuals have symptoms after the meal rich of simple carbohydrates. Symptoms could be effectively reduced by low glycemic index diet rich of dietary fibers. When the effect is insufficient, it is recommended to use acarbose as an α-glucosidase inhibitor, which is the main stimulation of GLP-1 secretion. Thus, obesity epidemics based on the inadequate nutritional habits in the children makes the postprandial syndrome feasible, and it requires further studies. At the same time, healthy diet can significantly improve

  15. The role of co-morbidity in the selection of antidiabetic pharmacotherapy in type-2 diabetes.

    Science.gov (United States)

    Tschöpe, Diethelm; Hanefeld, Markolf; Meier, Juris J; Gitt, Anselm K; Halle, Martin; Bramlage, Peter; Schumm-Draeger, Petra-Maria

    2013-04-10

    Metformin is, if not contraindicated and if tolerated, usually preferred over other antidiabetic drugs for the first line treatment of type-2 diabetes. The particular decision on which antidiabetic agent to use is based on variables such as efficacy, cost, potential side effects, effects on weight, comorbidities, hypoglycemia, risk, and patient preferences. However, there is no guidance how to consider these in the selection of antidiabetic drug treatment. In this work, we aimed to summarize available evidence and tried to give pragmatic treatment recommendations from a clinical practice perspective.There are clear contraindications for some drugs in those with impaired renal and liver function and precautions in those with heart failure for the use of metformin (NYHA III-IV) and glitazones. On the other hand, GLP-1 analogs, DPP-4 inhibitors and acarbose are generally less critical and can be used in the majority of patients. We identified the following gaps with respect to the selection of antidiabetic drug treatment in patients with co-morbid disease conditions: 1) Guidelines fail to give advice on the use of specific antidiabetic drugs in patients with co-morbidity. 2) The literature is deficient in studies documenting antidiabetic drug use in patients with severely impaired renal function, diabetic retinopathy, cerebrovascular disease and systolic heart failure. 3) Further there are no specific data on patients with multiple of these co-morbid disease conditions. We postulate that differential use of antidiabetic drugs in patients with co-morbid disease constellations will help to reduce treatment related complications and might improve prognosis.

  16. A physarum-inspired prize-collecting steiner tree approach to identify subnetworks for drug repositioning.

    Science.gov (United States)

    Sun, Yahui; Hameed, Pathima Nusrath; Verspoor, Karin; Halgamuge, Saman

    2016-12-05

    Drug repositioning can reduce the time, costs and risks of drug development by identifying new therapeutic effects for known drugs. It is challenging to reposition drugs as pharmacological data is large and complex. Subnetwork identification has already been used to simplify the visualization and interpretation of biological data, but it has not been applied to drug repositioning so far. In this paper, we fill this gap by proposing a new Physarum-inspired Prize-Collecting Steiner Tree algorithm to identify subnetworks for drug repositioning. Drug Similarity Networks (DSN) are generated using the chemical, therapeutic, protein, and phenotype features of drugs. In DSNs, vertex prizes and edge costs represent the similarities and dissimilarities between drugs respectively, and terminals represent drugs in the cardiovascular class, as defined in the Anatomical Therapeutic Chemical classification system. A new Physarum-inspired Prize-Collecting Steiner Tree algorithm is proposed in this paper to identify subnetworks. We apply both the proposed algorithm and the widely-used GW algorithm to identify subnetworks in our 18 generated DSNs. In these DSNs, our proposed algorithm identifies subnetworks with an average Rand Index of 81.1%, while the GW algorithm can only identify subnetworks with an average Rand Index of 64.1%. We select 9 subnetworks with high Rand Index to find drug repositioning opportunities. 10 frequently occurring drugs in these subnetworks are identified as candidates to be repositioned for cardiovascular diseases. We find evidence to support previous discoveries that nitroglycerin, theophylline and acarbose may be able to be repositioned for cardiovascular diseases. Moreover, we identify seven previously unknown drug candidates that also may interact with the biological cardiovascular system. These discoveries show our proposed Prize-Collecting Steiner Tree approach as a promising strategy for drug repositioning.

  17. A systematic review of acute pancreatitis as an adverse event of type 2 diabetes drugs: from hard facts to a balanced position.

    Science.gov (United States)

    Giorda, C B; Nada, E; Tartaglino, B; Marafetti, L; Gnavi, R

    2014-11-01

    The question whether antidiabetes drugs can cause acute pancreatitis dates back to the 1970s. Recently, old concerns have re-emerged following claims that use of incretins, a new class of drugs for type 2 diabetes, might increase the relative risk of acute pancreatitis up to 30-fold. Given that diabetes is per se a potent risk factor for acute pancreatitis and that drug-related acute pancreatitis is rare and difficult to diagnose, we searched the medical databases for information linking acute pancreatitis and type 2 diabetes drugs. Among the biguanides, both phenformin and metformin (the latter in patients with renal insufficiency) have been cited in case reports as a potential cause of acute pancreatitis. Sulphonylureas, as both entire class and single compound (glibenclamide), have also been found in cohort studies to increase its risk. No direct link was found between pancreatic damage and therapy with metaglinide, acarbose, pramlintide or SGLT-2 inhibitors. In animal models, thiazolinediones have demonstrated proprieties to attenuate pancreatic damage, opening perspectives for their use in treating acute pancreatitis in humans. Several case reports and the US Food and Drug Administration pharmacovigilance database indicate an association between acute pancreatitis and incretins, dipeptidyl peptidase-4 (DPP-4) inhibitors, and GLP-1 receptor agonists. To date, however, a clear-cut odds ratio for this association has been reported in only one of eight pharmacoepidemiological studies. Finally, none of the intervention trials investigating these compounds, including two large randomized controlled trials with cardiovascular endpoints, confirmed the purportedly increased risk of acute pancreatitis with incretin use.

  18. 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

  19. Antidiabetic Effect of Fresh Nopal (Opuntia ficus-indica) in Low-Dose Streptozotocin-Induced Diabetic Rats Fed a High-Fat Diet.

    Science.gov (United States)

    Hwang, Seung Hwan; Kang, Il-Jun; Lim, Soon Sung

    2017-01-01

    The objective of the present study was to evaluate α-glucosidase inhibitory and antidiabetic effects of Nopal water extract (NPWE) and Nopal dry power (NADP) in low-dose streptozotocin- (STZ-) induced diabetic rats fed a high-fat diet (HFD). The type 2 diabetic rat model was induced by HFD and low-dose STZ. The rats were divided into four groups as follows: (1) nondiabetic rats fed a regular diet (RD-Control); (2) low-dose STZ-induced diabetic rats fed HFD (HF-STZ-Control); (3) low-dose STZ-induced diabetic rats fed HFD and supplemented with NPWE (100 mg/kg body weight, HF-STZ-NPWE); and (4) low-dose STZ-induced diabetic rats fed HFD and supplemented with comparison medication (rosiglitazone, 10 mg/kg, body weight, HF-STZ-Rosiglitazone). In results, NPWE and NADP had IC50 values of 67.33 and 86.68 μg/mL, both of which exhibit inhibitory activities but lower than that of acarbose (38.05 μg/mL) while NPWE group significantly decreased blood glucose levels compared to control and NPDP group on glucose tolerance in the high-fat diet fed rats model (P < 0.05). Also, the blood glucose levels of HR-STZ-NPWE group were significantly lower (P < 0.05) than HR-STZ-Control group on low-dose STZ-induced diabetic rats fed HFD. Based on these findings, we suggested that NPWE could be considered for the prevention and/or treatment of blood glucose and a potential use as a dietary supplement.

  20. Antidiabetic Effect of Fresh Nopal (Opuntia ficus-indica in Low-Dose Streptozotocin-Induced Diabetic Rats Fed a High-Fat Diet

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    Seung Hwan Hwang

    2017-01-01

    Full Text Available The objective of the present study was to evaluate α-glucosidase inhibitory and antidiabetic effects of Nopal water extract (NPWE and Nopal dry power (NADP in low-dose streptozotocin- (STZ- induced diabetic rats fed a high-fat diet (HFD. The type 2 diabetic rat model was induced by HFD and low-dose STZ. The rats were divided into four groups as follows: (1 nondiabetic rats fed a regular diet (RD-Control; (2 low-dose STZ-induced diabetic rats fed HFD (HF-STZ-Control; (3 low-dose STZ-induced diabetic rats fed HFD and supplemented with NPWE (100 mg/kg body weight, HF-STZ-NPWE; and (4 low-dose STZ-induced diabetic rats fed HFD and supplemented with comparison medication (rosiglitazone, 10 mg/kg, body weight, HF-STZ-Rosiglitazone. In results, NPWE and NADP had IC50 values of 67.33 and 86.68 μg/mL, both of which exhibit inhibitory activities but lower than that of acarbose (38.05 μg/mL while NPWE group significantly decreased blood glucose levels compared to control and NPDP group on glucose tolerance in the high-fat diet fed rats model (P<0.05. Also, the blood glucose levels of HR-STZ-NPWE group were significantly lower (P<0.05 than HR-STZ-Control group on low-dose STZ-induced diabetic rats fed HFD. Based on these findings, we suggested that NPWE could be considered for the prevention and/or treatment of blood glucose and a potential use as a dietary supplement.

  1. In vitro α-amylase inhibitory activity and in vivo hypoglycemic effect of methanol extract of Citrus macroptera Montr. fruit

    Institute of Scientific and Technical Information of China (English)

    Nizam Uddin; Md. Rakib Hasan; Md. Monir Hossain; Arjyabrata Sarker; A.H.M. Nazmul Hasan; A.F.M. Mahmudul Islam; Mohd. Motaher H. Chowdhury; Md. Sohel Rana

    2014-01-01

    Objective: To investigate the therapeutic effects of methanol extract of Citrus macroptera Montr. fruit in α-amylase inhibitory activity (in vitro) and hypoglycemic activity in normal and glucose induced hyperglycemic rats (in vivo). Methods: Fruits of Citrus macroptera without rind was extracted with pure methanol following cold extraction and tested for presence of phytochemical constituents, α-amylase inhibitory activity, and hypoglycemic effect in normal rats and glucose induced hyperglycemic rats.Results:showed that fruit extract had moderate α-amylase inhibitory activity [IC50 value=(3.638±0.190) mg/mL] as compared to acarbose. Moreover at 500 mg/kg and 1 000 mg/kg doses fruit extract significantly (P<0.05 and P<0.01 respectively) reduced fasting blood glucose level in normal rats as compared to glibenclamide (5 mg/kg). In oral glucose tolerance test, 500 mg/kg dose significantly reduced blood glucose level (P<0.05) at 2 h but 1000 mg/kg dose significantly reduced blood glucose level at 2 h and 3 h (P<0.05 and P<0.01 respectively) whereas glibenclamide (5 mg/kg) significantly reduced glucose level at every hour after administration. Overall time effect is also considered extremely significant with F value=23.83 and P value=0.0001 in oral glucose tolerance test.Conclusion:These findings suggest that the plant may be a potential source for the development Presence of saponin, steroid and terpenoid were identified in the extract. The results of new oral hypoglycemic agent.

  2. 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.

  3. Cultivar evaluation and effect of fermentation on antioxidant capacity and in vitro inhibition of α-amylase and α-glucosidase by highbush blueberry (Vaccinium corombosum).

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    Johnson, Michelle H; Lucius, Anita; Meyer, Tessa; de Mejia, Elvira Gonzalez

    2011-08-24

    The berry fruits of highbush blueberry (Vaccinium corymbosum) contain bioactive compounds with potential health benefits. The objective was to evaluate blueberries grown in southern Illinois as well as the effect of fermentation, at two different temperatures, on chemical and physical parameters. Fruits from fifteen blueberry cultivars were analyzed. Fruit diameter ranged from 12.8 mm to 18.7 mm, pH from 2.6 to 3.7, reducing sugars from 6.4% to 15.2%, total sugars from 13.9% to 21.6%, total polyphenols from 0.39 to 1.00 mg gallic acid equivalents (GAE)/g blueberry and antioxidant capacity from 5.8 to 10.9 μM Trolox equivalents (TE)/g. In vitro α-amylase and α-glucosidase inhibitory capacity relative to the positive control acarbose, a known anti-diabetic drug, showed a range from 91.8 to 103.3% for α-amylase and from 103.2% to 190.8% for α-glucosidase. Wines prepared from several of these blueberry cultivars were analyzed throughout fermentation and compared at room temperature and cold temperature fermentation for pH (3.5 to 6.3), °Brix (13.6 to 29.7), total polyphenols (375.4 to 657.1 μg GAE/mL wine), and antioxidant capacity (4.5 to 25.1 mM TE). The wines were also tested for their in vitro capacity to inhibit α-amylase and α-glucosidase and maintained similar inhibitory action as the berries. Highbush blueberry cultivars and their fermented beverages are good natural sources of antioxidants and starch-degrading enzyme inhibitors important for type 2 diabetes management.

  4. Hypoglycemic, antihyperglycemic, and antioxidant effects of the edible plant Anoda cristata.

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    Juárez-Reyes, Krutzkaya; Brindis, Fernando; Medina-Campos, Omar N; Pedraza-Chaverri, José; Bye, Robert; Linares, Edelmira; Mata, Rachel

    2015-02-23

    Some studies refer that the entire plant of Anoda cristata is consumed as food and medicine; in particular for treating diabetes, inflammation, fever, cough, and wounds. The aim of this study was to establish the preclinical efficacy of Anoda cristata as hypoglycemic and/or antihyperglycemic agent using well-known animal models. The acute toxicity was analyzed by the Lorke method. Acute hypoglycemic as well as oral glucose and sucrose tolerance tests were used to determine the hypoglycemic and antihyperglycemic action of Anoda cristata. Several preparations of the plant, including a mucilage (M), an aqueous (T-AE), a free mucilage aqueous (FM-AE), and an organic (OE) extracts, were tested in healthy and NA-STZ-hyperglycemic mice. Glibenclamide (15mg/kg), acarbose (5mg/kg ) and metformin (200mg/kg) were used as positive controls. The major compounds acacetin (1) and diosmetin (2), isolated from an infusion of the plant applying chromatographic methods, were evaluated as hypoglycemic agents using the same assays. The FM-AE was tested also in rats with metabolic syndrome induced by a high-fructose fed. Finally some assays were performed to determine the antioxidant capacity of the FM-AE in vitro. The results demonstrated that the extracts and compounds from Anoda cristata were effective for reducing blood glucose levels in healthy and NA-STZ-hyperglycemic mice when compared with vehicle groups (pAnoda cristata is effective to diminish glucose levels in vivo and to ameliorate different disorders related with the metabolic syndrome in rats. According to the results, the efficacy of Anoda cristata preparations could be due to the presence of active principles with different mode of actions at the molecular level, including α-glycosidases inhibitors, insulin secretagogues, glucose entrapment and radical trapping agents. Copyright © 2014 Elsevier Ireland Ltd. All rights reserved.

  5. Study of Antiglycation, Hypoglycemic, and Nephroprotective Activities of the Green Dwarf Variety Coconut Water (Cocos nucifera L.) in Alloxan-Induced Diabetic Rats.

    Science.gov (United States)

    Pinto, Isabella F D; Silva, Railmara P; Chaves Filho, Adriano de B; Dantas, Lucas S; Bispo, Vanderson S; Matos, Isaac A; Otsuka, Felipe A M; Santos, Aline C; Matos, Humberto Reis

    2015-07-01

    Coconut water (CW) is a natural nutritious beverage, which contains several biologically active compounds that are traditionally used in the treatment of diarrhea and rehydration. Several works with CW have been related with antioxidant activity, which is very important in the diabetic state. To evaluate the hypoglycemic and nephroprotective activities of CW, alloxan-induced diabetic rats were pre- and post-treated by gavage with CW (3 mL/kg), caffeic acid (CA) (10 and 15 mg/kg), and acarbose (Acb) (714 μg/kg) during a period of 16 days. Body weight, blood glucose, glycated hemoglobin (HbA1c), and Amadori products in plasma and kidney homogenates were evaluated in all groups and used as parameters for the monitoring of the diabetic state. The results showed that rats of the CW+diabetic group had maintenance in blood glucose compared with the control group (P<.05) in addition to a decrease of HbA1c levels and increase of body weight when compared with the diabetic group rats (P<.05). The animals of the CA and CA+diabetic groups did not have significant variation of body weight (P<.05) during the experiment; however, they showed decrease in their HbA1c and urea levels in plasma as well as Amadori products in kidney homogenates when compared with the diabetic group (P<.05). Our results indicate that CW has multiple beneficial effects in diabetic rats for preventing hyperglycemia and oxidative stress caused by alloxan.

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

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    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.

  7. Inhibition of key enzymes linked to type 2 diabetes by compounds isolated from Aframomum melegueta fruit.

    Science.gov (United States)

    Mohammed, Aminu; Gbonjubola, Victoria Awolola; Koorbanally, Neil Anthony; Islam, Md Shahidul

    2017-12-01

    The use of Aframomum melegueta K. Schum. (Zingiberaceae) fruit for treatment of diabetes has recently been established in Nigeria. However, compounds responsible for the antidiabetic action have not been identified. The present study carried out the bioassay-guided isolation of possible bioactive compounds responsible for the antidiabetic action of A. melegueta fruit. The A. melegueta fruit was sequentially extracted using ethyl acetate (EtOAc), ethanol and water, and the most active extract (EtOAc) was subjected to column chromatography on a silica gel column using solvent gradient systems of hexane (HEX):EtOAc and EtOAc:MeOH and the isolation of compounds was guided by α-glycosidase and α-amylase inhibitory activities at various concentrations (30-240 μg/mL). According to the results, 3 arylalkanes, 6-paradol (1), 6-shogaol (2) and 6-gingerol (3) and a pentacyclic triterpene, oleanolic acid (4) were isolated from A. melegueta fruit. All the compounds exhibited inhibitory effects against α-amylase and α-glucosidase. 6-Gingerol (3) and oleanolic acid (4) showed higher inhibitory activity against α-amylase (IC50: 6-gingerol: 81.78 ± 7.79 μM; oleanolic acid: 91.72 ± 1.63 μM) and α-glucosidase (IC50: 6-gingerol: 21.55 ± 0.45 μM; oleanolic acid: 17.35 ± 0.88 μM) compared to the standard drug, acarbose and other isolated compounds. The kinetics of the enzyme action of the compounds showed a noncompetitive mode of inhibition. The data of this study suggest that the 6-gingerol (3) and oleanolic acid (4) showed higher α-amylase and α-glucosidase inhibitory action and therefore could be responsible for the antidiabetic activity of A. melegueta fruit.

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

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    Shuxia Yan

    2016-08-01

    Full Text Available 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.

  9. Evaluation of anti-diabetic and anti-tumoral activities of bioactive compounds from Phoenix dactylifera L's leaf: In vitro and in vivo approach.

    Science.gov (United States)

    Chakroun, Mouna; Khemakhem, Bassem; Mabrouk, Hazem Ben; El Abed, Hanen; Makni, Mohamed; Bouaziz, Mohamed; Drira, Noureddine; Marrakchi, Naziha; Mejdoub, Hafedh

    2016-12-01

    Among various chronic disorders, cancer and diabetes mellitus are the most common disorders. This study was designed to evaluate the effectiveness of hydroalcoholic extract of Phoenix dactylifera L. leaves (HEPdL) in animal models of type II diabetes in vitro/in vivo and in a human melanoma-derived cell line (IGR-39). A liquid chromatography-tandem mass spectrometry (LC-MS/MS) analysis was also performed to determine the amount of phenolic and flavonoid compounds in this plant. The physicochemical results by LC-MS/MS analysis of HEPdL showed the presence of 10 phenolic compounds. The in vitro study showed that the extract exhibited a more specific and potent inhibitor of α-glucosidase than α-amylase with an IC50 value of 20±1μg/mL and 30±0.8μg/mL, respectively. More importantly, the in vivo study of the postprandial hyperglycemia activity with (20mg/kg) of HEPdL showed a decrease in plasma glucose levels after 60min in resemblance to the glucor (acarbose) (50mg/kg) effect. The oral administration of HEPdL (20mg/kg) in alloxan-induced diabetic mices for 28days showed a more significant anti-diabetic activity than that of the drug (50mg/kg). Moreover, cytotoxicity effects of HEPdL in IGR-39 cancer cell lines were tested by MTT assay. This extract was effective in inhibiting cancer cells growth (IGR-39) at dose 35 and 75μg/mL. These results confirm ethnopharmacological significance of the plant and could be taken further for the development of an effective pharmaceutical drug against diabetes and cancer. Copyright © 2016 Elsevier Masson SAS. All rights reserved.

  10. 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. © 2016 American Heart Association, Inc.

  11. Total phenolic compounds, antioxidant potential and α-glucosidase inhibition by Tunisian Euphorbia paralias L.

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    Malek Besbes Hlila

    2016-08-01

    Full Text Available Objective: To examine the potential antioxidant and anti-α-glucosidase inhibitory activities of Tunisian Euphorbia paralias L. leaves and stems extracts and their composition of total polyphenol and flavonoids. Methods: The different samples were tested for their antiradical activities by using 2, 2’- azinobis(3-ethylbenzothiazoline-6-sulfonic acid (ABTS and 1,1-diphenyl-2-picrylhydrazyl (DPPH assays. In α-glucosidase activity, α-glucosidase (0.3 IU/mL and substrate, 2500 µmol/ L p-nitrophenyl α-D-glucopyranoside were used; absorbance was registered at 405 nm. Results: The leaves acetonic extract exhibited the strongest α-glucosidase inhibition [IC50 = (0.0035 ± 0.001 µg/mL], which was 20-fold more active than the standard product (acarbose [IC50 = (0.07 ± 0.01 µg/mL]. Acetonic extract of the leaves exhibited the highest quantity of total phenolic [(95.54 ± 0.04 µg gallic acid equivalent/mg] and flavonoid [(55.16 ± 0.25 µg quercetin equivalent/mg]. The obtained findings presented also that this extract was detected with best antioxidant capacity [IC50 = (0.015 ± 0.01 µg/mL] against DPPH and a value of IC50 equal to (0.02 ± 0.01 µg/mL against ABTS. Positive relationship between polyphenolic content of the tested Euphorbia paralias L. leaves and stems extracts and its antioxidant activity (DPPH and ABTS was detected. Elevated positive linear correlation was got between ABTS and total phenolic (R2 = 0.751. Conclusions: The findings clearly demonstrate that the use of a polar solvent enables extraction of significant quantities of phenol compounds and flavonoids.

  12. Anti-hyperlipidemic and hypoglycemic effects of Gynostemma pentaphyllum in the Zucker fatty rat.

    Science.gov (United States)

    Megalli, Samer; Davies, Neal M; Roufogalis, Basil D

    2006-01-01

    Gynostemma pentaphyllum is a traditional Chinese medicine used for a variety of conditions, including elevated cholesterol. We have examined the pharmacological anti-hyperlipidemic and hypoglycemic effectiveness of Gynostemma pentaphyllum in the obese Zucker fatty diabetic rat model. After treatment for 4 days Gynostemma pentaphyllum 250 mg/kg reduced triglyceride (33%), total cholesterol, (13%) and low density lipoprotein cholesterol levels (33%). These effects were dose-dependent and maintained for at least 5 weeks. Chronic treatment for 3-5 weeks also reduced post-prandial hypertriglyceridemia induced by olive oil 10 mg/kg in the Zucker fatty rats but had no significant effect in lowering sucrose-induced hyperglycemia in Sprague-Dawley rats. A novel regulation by Gynostemma of glucose levels was also observed in the Zucker fatty rat model. In a glucose tolerance test in obese and lean Zucker rats pretreatment with Gynostemma pentaphyllum 250 mg/kg demonstrated glucose levels were significantly less 2 hours post challenge (20%) in the Gynostemma pentaphyllum obese rats compared to the control group. Gynostemma pentaphyllum did not significantly reduce glucose levels at 120 min in the lean strain, in contrast to the 20% decrease seen in the obese rat. In vitro, Gynostemma pentaphyllum inhibited alpha-glucosidase activity (50% inhibition at 42.8), which compared to acarbose (50% at 53.9 microg/mL). The improvement in glucose tolerance at 120 min by Gynostemma pentaphyllum in obese Zucker fatty rats but not lean rats suggests that it may improve insulin receptor sensitivity and together with the significant reduction of hypertriglyceridemia, cholesterol and low density lipoprotein cholesterol suggests that Gynostemma should be examined further by oral hypoglycemic/anti-hyperlipidemic therapy.

  13. COST ANALYSIS OF ANTIDIABETIC DRUGS FOR DIABETES MELLITUS OUTPATIENT IN KODYA YOGYAKARTA HOSPITAL

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    TRI MURTI ANDAYANI

    2007-01-01

    Full Text Available Diabetes mellitus is a chronic disorder that has been recognised by the Indonesian government as a major public health problem with far reaching consequences not just for its adverse impact on the healthof Indonesians, but also for the economic burden it places on the healthcare systems. The objectives of this study were to describe the healthcare cost for outpatient diabetes mellitus treatment and to examine the cost of different classes of antidiabetic drug. The medical records of Type 2 diabetes mellitus outpatients without compelling indication were retrospectively reviewed. Data was collected for patients treated from January 1st to December 31st, 2004 in Kodya Yogyakarta Hospital. Data collected includedpatient demographics, drug acquisition cost, medical consultation cost and laboratory cost. We analysed charts of 100 consecutive patients, of whom 71% are women and 29% are men. The average age ofpatient was 61.2 ± 13.7 years. The monthly mean cost of Type 2 diabetes mellitus was found to be equivalent to USD19.97 ± 13.71. Most of the direct medical costs were spent on drugs (96.4%. Bloodglucose control using combination therapy was more frequently attained in patients taking glibenclamide and metformin (25%. The combination of gliquidone-metformin-acarbose (21% was themost expensive, which was equivalent to USD39.44. The potential saving was 6.10% of total drug cost if generic substitutions were prescribed for diabetes mellitus in place of more expensive drugs. Inconclusion, we identified that the costs of diabetes mellitus outside of hospitals are mainly dependent on the expenses with blood glucose-lowering drugs.

  14. In Vitro and In Vivo Antidiabetic Evaluation of Selected Culinary-Medicinal Mushrooms (Agaricomycetes).

    Science.gov (United States)

    Singh, Varinder; Bedi, Gurleen Kaur; Shri, Richa

    2017-01-01

    Management of type 2 diabetes by delaying or preventing glucose absorption using natural products is gaining significant attention. Edible mushrooms are well documented for their nutritional and medicinal properties. This investigation was designed to evaluate the antidiabetic activity of aqueous extracts of selected culinary-medicinal mushrooms, namely, Pleurotus ostreatus, Calocybe indica, and Volvariella volvacea, using in vitro models (α-amylase inhibition assay, glucose uptake by yeast cells, and glucose adsorption capacity). The most active extract was subsequently examined in vivo using the oral starch tolerance test in mice. All prepared extracts showed dose-dependent inhibition of α-amylase and an increase in glucose transport across yeast cells. C. indica extract was the most active α-amylase inhibitor (half-maximal inhibitory concentration, 18.07 ± 0.75 mg/mL) and exhibited maximum glucose uptake by yeast cells (77.53 ± 0.97% at 35 mg/mL). All extracts demonstrated weak glucose adsorption ability. The positive in vitro tests for C. indica paved the way for in vivo studies. C. indica extract (200 and 400 mg/kg) significantly (P < 0.05) reduced postprandial blood glucose peaks in mice challenged with starch. The extract (400 mg/kg) and acarbose normalized blood glucose levels at 180 minutes, when they were statistically similar to values in normal mice. Thus, it may be concluded that the antidiabetic effect of C. indica is mediated by inhibition of starch metabolism (α-amylase inhibition), increased glucose uptake by peripheral cells (promotion of glucose uptake by yeast cells), and mild entrapment (adsorption) of glucose. Hence, C. indica can be developed as antidiabetic drug after detailed pharmacological studies.

  15. 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.

  16. Total phenolic compounds, antioxidant potential andα-glucosidase inhibition by TunisianEuphorbia paralias L.

    Institute of Scientific and Technical Information of China (English)

    Malek Besbes Hlila; Kaouther Majouli; Fethia Harzallah Skhiri; Hichem Ben Jannet; Mahjoub Aouni; Maha Mastouri; Boulbaba Selmi

    2016-01-01

    Objective:To examine the potential antioxidant and anti-α-glucosidase inhibitory activities of TunisianEuphorbia paralias L. leaves and stems extracts and their composition of total polyphenol and flavonoids. Methods: The different samples were tested for their antiradical activities by using 2, 2’-azinobis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) and 1,1-diphenyl-2-picrylhydrazyl (DPPH) assays. In α-glucosidase activity,α-glucosidase (0.3 IU/mL) and substrate, 2 500µmol/Lp-nitrophenylα-D-glucopyranoside were used; absorbance was registered at 405 nm. Results:The leaves acetonic extract exhibited the strongestα-glucosidase inhibition [IC50=(0.0035 ± 0.001)µg/mL], which was 20-fold more active than the standard product (acarbose) [IC50 = (0.07 ± 0.01)µg/mL]. Acetonic extract of the leaves exhibited the highest quantity of total phenolic [(95.54 ± 0.04)µg gallic acid equivalent/mg] and flavonoid [(55.16 ± 0.25)µg quercetin equivalent/mg]. The obtained findings presented also that this extract was detected with best antioxidant capacity [IC50 = (0.015 ± 0.01)µg/mL] againstDPPH and a value of IC50 equal to (0.02 ± 0.01)µg/mL againstABTS. Positive relationship between polyphenolic content of the testedEuphorbia paralias L. leaves and stems extracts and its antioxidant activity (DPPH andABTS) was detected. Elevated positive linear correlation was got betweenABTS and total phenolic (R2 = 0.751). Conclusions: The findings clearly demonstrate that the use of a polar solvent enables extraction of significant quantities of phenol compounds and flavonoids.

  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. A fluorescence resonance energy transfer (FRET) based "Turn-On" nanofluorescence sensor using a nitrogen-doped carbon dot-hexagonal cobalt oxyhydroxide nanosheet architecture and application to α-glucosidase inhibitor screening.

    Science.gov (United States)

    Li, Guoliang; Kong, Weiheng; Zhao, Mei; Lu, Shuaimin; Gong, Peiwei; Chen, Guang; Xia, Lian; Wang, Hua; You, Jinmao; Wu, Yongning

    2016-05-15

    The medicines targeted at α-glucosidase played an important role in anti-diabetes and anti-HIV therapy. Unfortunately, the method based on fluorescent assay strategy for α-glucosidase inhibitor screening remains poorly investigated. In this study, a novel "Turn On" fluorescence sensor platform has been developed for trace α-glucosidase inhibitor screening from natural medicines. Firstly, carbon dots were prepared by one-pot synthesis and used as the signal output. Combining with the carbon dots, cobalt oxyhydroxide (CoOOH) nanoflakes were employed to build the fluorescence resonance energy transfer (FRET) based sensor platform. Secondly, L-ascorbic acid-2-O-α-D-glucopyranosyl (AAG) was innovatively introduced as α-glucosidase substrate. With hydrolysis of AAG by α-glucosidase, ascorbic acids (AA) were released that can rapidly reduce CoOOH nanoflakes to Co(2+), and then FRET was stopped accompanying with the fluorescence recovery of CDs. The sensor platform was ultrasensitive to AA with a detection limit of 5 nM, ensuring the sensitive monitoring of enzyme activity. Acarbose was used as the inhibitor model and its inhibition rate is proportional to the logarithm of concentration in range of 10(-9)-10(-3)M with the correlation coefficient of R(2)=0.996, and an ultralow limit of detection of ~1×10(-9)M was obtained. The inhibiting ability of seven compounds isolated from natural medicines was also evaluated. The constructed sensor platform was proven to be sensitive and selective as well as cost-effective, facile and reliable, making it promising as a candidate for trace α-glucosidase inhibitor screening.

  19. Effects of alpha-amylase and its inhibitors on acid production from cooked starch by oral streptococci.

    Science.gov (United States)

    Aizawa, S; Miyasawa-Hori, H; Nakajo, K; Washio, J; Mayanagi, H; Fukumoto, S; Takahashi, N

    2009-01-01

    This study evaluated acid production from cooked starch by Streptococcus mutans, Streptococcus sobrinus, Streptococcus sanguinis and Streptococcus mitis, and the effects of alpha-amylase inhibitors (maltotriitol and acarbose) and xylitol on acid production. Streptococcal cell suspensions were anaerobically incubated with various carbohydrates that included cooked potato starch in the presence or absence of alpha-amylase. Subsequently, the fall in pH and the acid production rate at pH 7.0 were measured. In addition, the effects of adding alpha-amylase inhibitors and xylitol to the reaction mixture were evaluated. In the absence of alpha-amylase, both the fall in pH and the acid production rate from cooked starch were small. On the other hand, in the presence of alpha-amylase, the pH fell to 3.9-4.4 and the acid production rate was 0.61-0.92 micromol per optical density unit per min. These values were comparable to those for maltose. When using cooked starch, the fall in pH by S. sanguinis and S. mitis was similar to that by S. mutans and S. sobrinus. For all streptococci, alpha-amylase inhibitors caused a decrease in acid production from cooked starch, although xylitol only decreased acid production by S. mutans and S. sobrinus. These results suggest that cooked starch is potentially acidogenic in the presence of alpha-amylase, which occurs in the oral cavity. In terms of the acidogenic potential of cooked starch, S. sanguinis and S. mitis were comparable to S. mutans and S. sobrinus. Alpha-amylase inhibitors and xylitol might moderate this activity.

  20. Study on the Assistant Hypoglycemic Efficacy of Six Functional Food Materials%六种保健食品原料的辅助降血糖功效研究

    Institute of Scientific and Technical Information of China (English)

    董义; 王斯慧; 曾里; 曾凡骏

    2014-01-01

    选择苦瓜、苦荞、葛根、桑叶、西洋参、绞股蓝6种具有辅助降血糖功能的保健食品原料进行降血糖功效研究。采用相同提取工艺得到提取物,以检测其对α-淀粉酶和α-葡萄糖苷酶活力的抑制作用作为辅助降血糖体外评价方法,与拜糖平在相同条件下进行对比,分别研究其辅助降血糖功效。实验得出,六种原料均有明显辅助降血糖功效。其中,苦瓜效果最好,其次为苦荞和绞股蓝,可作为辅助降血糖功能食品的原料。%Six materials, balsam melon, Tartary buckwheat, kudzu root, mulberry leaves, American ginseng and gynostemma pentaphylla, which could be used in functional food were chosen to have tests on its assistant hypoglycemic efficacy. The extractions were prepared through same process. By detecting the inhibition effect toα-amylase andα-glucosidase as the in-vitro evaluation method, the assistant hypoglycemic efficacy of these six materials' extracts were compared with Acarbose under the same condition. The result showed that all of these six materials could help to reduce the blood sugar levels. Among them, balsam melon has the best effect followed by Tartary buckwheat and gynostemma pentaphylla, which can be used as the raw material in functional foods.

  1. 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.

  2. Enzyme Inhibitory Properties, Antioxidant Activities, and Phytochemical Profile of Three Medicinal Plants from Turkey

    Directory of Open Access Journals (Sweden)

    Gokhan Zengin

    2015-01-01

    Full Text Available We aimed to investigate the inhibitory potential of three medicinal plants (Hedysarum varium, Onobrychis hypargyrea, and Vicia truncatula from Turkey against key enzymes involved in human pathologies, namely, diabetes (α-amylase and α-glucosidase, neurodegenerative disorders (tyrosinase, acetylcholinesterase, and butyrylcholinesterase, and hyperpigmentation (tyrosinase. The antioxidant potential, phenolic and flavonoid content of ethyl acetate, and methanolic and aqueous extracts were investigated using in vitro assays. The total antioxidant capacity (TAC, β-carotene/linoleic acid bleaching activity, 1,1-diphenyl-2-picrylhydrazyl free radical (DPPH•, 2,2-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid (ABTS•+, cupric ion reducing antioxidant capacity (CUPRAC, ferric reducing antioxidant power (FRAP, and metal chelating activity on ferrous ions were used to evaluate the antioxidant capabilities of the extracts. The half-maximal inhibitory concentrations (IC50 of the extracts on cholinesterase, tyrosinase, and α-amylase were significantly higher than the references, galantamine, kojic acid, and acarbose, respectively. The half-maximal effective concentrations (EC50 of the extracts on TAC, CUPRAC, and FRAP were significantly higher than trolox. The phenol and flavonoid contents of the plant extracts were in the range 20.90±0.190–83.25±0.914 mg gallic acid equivalent/g extract and 1.45±0.200–39.71±0.092 mg rutin equivalent/g extract, respectively. The plants were found to possess moderate antioxidant capacities and interesting inhibitory action against key enzymes.

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

    Directory of Open Access Journals (Sweden)

    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.

  4. Cardiovascular disease and oral agent glucose-lowering therapies in the management of type 2 diabetes.

    Science.gov (United States)

    Home, Philip

    2012-06-01

    Although glucose-lowering oral agents have been available for clinical use for over 60 years, the formal evidence base supporting their advantage and safety in regard of cardiovascular (CV) outcomes remains less than optimal. However, a synthesis of the evidence results in a high probability of benefit. For metformin, the United Kingdom Prospective Diabetes Study (UKPDS) substudy is convincing for a definite effect in reducing myocardial infarction (MI), but the quantitative extent of that is uncertain. For sulfonylureas, support for reduction in MI comes from the UKPDS extension study, where the central estimate for risk reduction remains the same as in the original planned end to the study, but the greater number of events was statistically significant for the sulfonylurea/insulin arm. Other studies do not support the view that metformin and sulfonylureas differ with respect to MI or indeed CV outcomes more generally. The data available for acarbose, an α-glucosidase inhibitor, are weak but not of concern, although some positive substudy data are available for people with impaired glucose tolerance. For peroxisome proliferator-activated receptor-γ agonists the CV data are more controversial, but the purpose-designed randomized controlled trials are clear that pioglitazone is advantageous to placebo (except for heart failure [HF]), whereas rosiglitazone is indistinguishable from metformin/sulfonylureas (even when including HF data). Lower-quality data do, however, lead to significant concerns for MI with rosiglitazone. Early and somewhat low-quality data for the dipeptidyl peptidase inhibitors show they are safe and hold promise for cardiovascular advantage, with major randomized controlled trials being underway. Preliminary CV data are available for one sodium/glucose cotransporter 2 inhibitor and look reassuring.

  5. Preventing type 2 diabetes mellitus: room for residual risk reduction after lifestyle changes?

    Science.gov (United States)

    Athyros, Vasilios G; Tziomalos, Konstantinos; Karagiannis, Asterios; Mikhailidis, Dimitri P

    2010-01-01

    It is well known that type 2 diabetes mellitus (T2DM) is a major risk factor for cardiovascular diseases (CVD). A predicted worldwide increase in the incidence of T2DM, taking the form of an epidemic, is expected to induce a substantial increase in CVD incidence. Impaired glucose tolerance (IGT) and impaired fasting glucose (IFG) are related to an increased risk of developing T2DM, especially in obese people. Prevention of T2DM aiming to reversal of pre-diabetes to normal glucose tolerance seems to be a very attractive target, and favourably affects CVD risk factors. The Diabetes Prevention Program and the Finnish Diabetes Prevention studies showed that changes in lifestyle prevented or delayed the onset of new cases of T2DM in subjects with pre-diabetes by 58%. However, a fraction of participants still developed T2DM, suggesting a residual risk. Moreover, lifestyle changes are not usually followed on a long-term basis as shown in EUROASPIRE with an increase in new onset T2DM by 60% in subjects with CVD in just over a decade. T2DM is characterized by insulin resistance and/or β-cell dysfunction (impaired insulin secretion). Various interventions targeting those two mechanisms (e.g. metformin, thiazolidinediones, acarbose, orlistate, bariatric surgery, renin-angiotensin-aldosterone system axis inhibitors, fibrates, incretin mimetics or enhancers) can prevent or delay T2DM. Widespread application of these measures has, however, been limited by financial considerations, even though cost-effectiveness might be achieved at the population level. This review will investigate feasibility and usefulness of T2DM prevention, further to that achieved with lifestyle changes, in a cost-effective manner.

  6. Human salivary alpha-amylase Trp58 situated at subsite -2 is critical for enzyme activity.

    Science.gov (United States)

    Ramasubbu, Narayanan; Ragunath, Chandran; Mishra, Prasunkumar J; Thomas, Leonard M; Gyémánt, Gyöngyi; Kandra, Lili

    2004-06-01

    The nonreducing end of the substrate-binding site of human salivary alpha-amylase contains two residues Trp58 and Trp59, which belong to beta2-alpha2 loop of the catalytic (beta/alpha)(8) barrel. While Trp59 stacks onto the substrate, the exact role of Trp58 is unknown. To investigate its role in enzyme activity the residue Trp58 was mutated to Ala, Leu or Tyr. Kinetic analysis of the wild-type and mutant enzymes was carried out with starch and oligosaccharides as substrates. All three mutants exhibited a reduction in specific activity (150-180-fold lower than the wild type) with starch as substrate. With oligosaccharides as substrates, a reduction in k(cat), an increase in K(m) and distinct differences in the cleavage pattern were observed for the mutants W58A and W58L compared with the wild type. Glucose was the smallest product generated by these two mutants in the hydrolysis oligosaccharides; in contrast, wild-type enzyme generated maltose as the smallest product. The production of glucose by W58L was confirmed from both reducing and nonreducing ends of CNP-labeled oligosaccharide substrates. The mutant W58L exhibited lower binding affinity at subsites -2, -3 and +2 and showed an increase in transglycosylation activity compared with the wild type. The lowered affinity at subsites -2 and -3 due to the mutation was also inferred from the electron density at these subsites in the structure of W58A in complex with acarbose-derived pseudooligosaccharide. Collectively, these results suggest that the residue Trp58 plays a critical role in substrate binding and hydrolytic activity of human salivary alpha-amylase.

  7. 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.

  8. 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.

  9. [The possibility of prevention of type 2 diabetes].

    Science.gov (United States)

    Strus, Adam; Szepietowska, Barbara; Zonenberg, Anna; Nikołajuk, Agnieszka; Górska, Maria; Szelachowska, Małgorzata

    2008-01-01

    The aim of this study was to examine usefulness of oral glucose tolerance test (OGTT) in clinical evaluation of different glucose metabolism disturbances in subjects with at least one risk factor of type 2 diabetes. We compared the effectiveness of non-pharmacological and pharmacological prevention and treatment regiments on metabolic control in these individuals. The study involved 130 patients, with the following characteristics: age between 18 to 76 years, mean body mass index (BMI) - 31.82 +/- 7.24 kg/m(2), and presence of at least one of the risk factor of type 2 diabetes. Glucose metabolism disturbances were diagnosed according to World Health Organization (WHO) criteria. Non-pharmacological regiments were applied for 3 months for patients with impaired glucose tolerance (IGT) and type 2 diabetes. Patients, whose still met criteria for type 2 diabetes during OGTT after non-pharmacological treatment were scheduled for pharmacological interventions. These patients were assigned at random to two groups, that were treated with either metformin or acarbose. The measurements of total cholesterol (TC), HDL-cholesterol , LDL-cholesterol, trigliceryde (TG), glucose, HbA(1c) and/or OGGT were performed during each visit. We also assessed risk factors for type 2 diabetes in these subjects. The prevalence of abnormal glucose tolerance in subjects with at least one of the risk factor of diabetes type 2 was near 40%. OGTT in these subjects increased the possibility of diagnosis diabetes type 2 and IGT. Hypertension (81%), hypercholesterolemia (71.4%), hypertriglicerydemia (71.4%) and obesity (66.7%) were the most frequent risk factors observed. There were no differences in biochemical measurements between these groups of patients. Individuals with at least one risk factor of type 2 diabetes should have screening test to diagnose glucose intolerance. Both non-pharmacological and pharmacological intervention was effective in normalization of glucose OGTT in patients with

  10. Antidiabetic Effect of Fresh Nopal (Opuntia ficus-indica) in Low-Dose Streptozotocin-Induced Diabetic Rats Fed a High-Fat Diet

    Science.gov (United States)

    Hwang, Seung Hwan; Kang, Il-Jun

    2017-01-01

    The objective of the present study was to evaluate α-glucosidase inhibitory and antidiabetic effects of Nopal water extract (NPWE) and Nopal dry power (NADP) in low-dose streptozotocin- (STZ-) induced diabetic rats fed a high-fat diet (HFD). The type 2 diabetic rat model was induced by HFD and low-dose STZ. The rats were divided into four groups as follows: (1) nondiabetic rats fed a regular diet (RD-Control); (2) low-dose STZ-induced diabetic rats fed HFD (HF-STZ-Control); (3) low-dose STZ-induced diabetic rats fed HFD and supplemented with NPWE (100 mg/kg body weight, HF-STZ-NPWE); and (4) low-dose STZ-induced diabetic rats fed HFD and supplemented with comparison medication (rosiglitazone, 10 mg/kg, body weight, HF-STZ-Rosiglitazone). In results, NPWE and NADP had IC50 values of 67.33 and 86.68 μg/mL, both of which exhibit inhibitory activities but lower than that of acarbose (38.05 μg/mL) while NPWE group significantly decreased blood glucose levels compared to control and NPDP group on glucose tolerance in the high-fat diet fed rats model (P < 0.05). Also, the blood glucose levels of HR-STZ-NPWE group were significantly lower (P < 0.05) than HR-STZ-Control group on low-dose STZ-induced diabetic rats fed HFD. Based on these findings, we suggested that NPWE could be considered for the prevention and/or treatment of blood glucose and a potential use as a dietary supplement. PMID:28303158

  11. In vitro inhibitory effects on a-glucosidase and a-amylase level and antioxidant potential of seeds of Phoenix dactylifera L.

    Institute of Scientific and Technical Information of China (English)

    Shah Alam Khan; Amira Rashid Al Kiyumi; Manal Saif Al Sheidi; Tagreed Salim Al Khusaibi; Noura Mohammed Al Shehhi; Tanveer Alam

    2016-01-01

    Objective:To evaluate and compare the antioxidant activity,total phenolic contents(TPCs) and in vitro antidiabetic activity of various pits extracts obtained from five Omani date cultivars.Methods:Sun-dried mature fruits of five Omani date varieties,namely,Fardh,Naghal,Khalas,Khinazi and Khasab were purchased from the local market in Muscat,Oman in the month of September 2014.Four seed extracts viz.water,ethanol,methanol and acetone were prepared for each date variety and their antioxidant activities were investigated by 1,1-diphenyl-2-picrylhydrazyl,hydrogen peroxide scavenging method and reducing power assay method,respectively.In vitro antidiabetic activity of the date pit extracts was evaluated by measuring their inhibitory effect on a-glucosidase and aamylase level.TPCs were also quantified colorimetrically.Results:The results indicated that TPC of date seeds was solvent dependent.Acetone,ethanol and methanol were found to be significantly better solvents than water in extracting phenolic compounds from the date seeds.Pit extracts exhibited moderate to good in vitro antioxidant activity and increased reducing power.Among all date pit extracts,water extract exhibited significant in vitro antidiabetic activity in comparison to standard drug,acarbose.Conclusions:The present study confirms that disposed waste of Omani dates is a rich source of dietary antioxidant because of its high TPC.The pits due to their inhibitory effects on a-glucosidase and a-amylase level could be used as a monotherapy along with an appropriate diabetic diet and exercise or might be in conjunction with antidiabetic therapy to manage and prevent progression of diabetes.

  12. Medical management of clomiphene-resistant polycystic ovarian syndrome: an update

    Directory of Open Access Journals (Sweden)

    Sharonjeet Kaur

    2014-02-01

    Full Text Available Clomiphene citrate is the traditional first-line treatment for chronic anovulation that characterizes polycystic ovary syndrome (PCOS. A gold standard therapy has always been Clomiphene Citrate (CC. However, 20%-25% of PCOS women fail to ovulate with incremental doses of CC. A good body of evidence suggest that alternatives for PCOS women with CC-resistant anovulation include insulin sensitizers like metformin and pioglitazone. Insulin sensitizers improves pregnancy outcome and ovulation rate by and acts by ameliorating insulin sensitivity and hyperandrogenemia. Metformin is preferred in obese women. Gonadotropins induce ovulation and maintain optimal follicle growth via controlled administration of follicle stimulation hormone. Two regimens are used which includes high and low dose regimen. Low dose regimen is preferred but is associated adverse effects like ovarian hyperstimulation syndrome (OHSS and increased cost. Extending clomiphene therapy reduces cost and improves pregnancy outcome. Glucocorticoids are preferably used when serum Dehydroepiandrosterone levels are > 200µg/dL. Bromocriptine improves ovulation rate by decreasing prolactin levels. Human Chorionic Gonadotropin restores ovulation but its use is limited during intrauterine insemination. Tamoxifen acts in a similar way as CC but has lesser antiestrogenic effect on the endometrium, cervical mucus, and granulosa cells, hence an added advantage of monofollicular ovulation. Aromatase inhibitors block conversion androstenedione and testosterone to estrogen in ovary and improves ovulation rate. Added advantage includes lesser cost, simple to use, no danger of multiple pregnancies and convenient for patient. Combination of GnRH analogues and Gonadotropins are associated with increased risk of OHSS. D-chiro-inositol, N-Acetylcysteine, melatonin and acarbose are tried with little success. [Int J Basic Clin Pharmacol 2014; 3(1.000: 1-9

  13. Contribution of mucosal maltase-glucoamylase activities to mouse small intestinal starch alpha-glucogenesis.

    Science.gov (United States)

    Quezada-Calvillo, Roberto; Robayo-Torres, Claudia C; Opekun, Antone R; Sen, Partha; Ao, Zihua; Hamaker, Bruce R; Quaroni, Andrea; Brayer, Gary D; Wattler, Sigrid; Nehls, Michael C; Sterchi, Erwin E; Nichols, Buford L

    2007-07-01

    Digestion of starch requires activities provided by 6 interactive small intestinal enzymes. Two of these are luminal endo-glucosidases named alpha-amylases. Four are exo-glucosidases bound to the luminal surface of enterocytes. These mucosal activities were identified as 4 different maltases. Two maltase activities were associated with sucrase-isomaltase. Two remaining maltases, lacking other identifying activities, were named maltase-glucoamylase. These 4 activities are better described as alpha-glucosidases because they digest all linear starch oligosaccharides to glucose. Because confusion persists about the relative roles of these 6 enzymes, we ablated maltase-glucoamylase gene expression by homologous recombination in Sv/129 mice. We assayed the alpha-glucogenic activities of the jejunal mucosa with and without added recombinant pancreatic alpha-amylase, using a range of food starch substrates. Compared with wild-type mucosa, null mucosa or alpha-amylase alone had little alpha-glucogenic activity. alpha-Amylase amplified wild-type and null mucosal alpha-glucogenesis. alpha-Amylase amplification was most potent against amylose and model resistant starches but was inactive against its final product limit-dextrin and its constituent glucosides. Both sucrase-isomaltase and maltase-glucoamylase were active with limit-dextrin substrate. These mucosal assays were corroborated by a 13C-limit-dextrin breath test. In conclusion, the global effect of maltase-glucoamylase ablation was a slowing of rates of mucosal alpha-glucogenesis. Maltase-glucoamylase determined rates of digestion of starch in normal mice and alpha-amylase served as an amplifier for mucosal starch digestion. Acarbose inhibition was most potent against maltase-glucoamylase activities of the wild-type mouse. The consortium of 6 interactive enzymes appears to be a mechanism for adaptation of alpha-glucogenesis to a wide range of food starches.

  14. Luminal starch substrate "brake" on maltase-glucoamylase activity is located within the glucoamylase subunit.

    Science.gov (United States)

    Quezada-Calvillo, Roberto; Sim, Lyann; Ao, Zihua; Hamaker, Bruce R; Quaroni, Andrea; Brayer, Gary D; Sterchi, Erwin E; Robayo-Torres, Claudia C; Rose, David R; Nichols, Buford L

    2008-04-01

    The detailed mechanistic aspects for the final starch digestion process leading to effective alpha-glucogenesis by the 2 mucosal alpha-glucosidases, human sucrase-isomaltase complex (SI) and human maltase-glucoamylase (MGAM), are poorly understood. This is due to the structural complexity and vast variety of starches and their intermediate digestion products, the poorly understood enzyme-substrate interactions occurring during the digestive process, and the limited knowledge of the structure-function properties of SI and MGAM. Here we analyzed the basic catalytic properties of the N-terminal subunit of MGAM (ntMGAM) on the hydrolysis of glucan substrates and compared it with those of human native MGAM isolated by immunochemical methods. In relation to native MGAM, ntMGAM displayed slower activity against maltose to maltopentose (G5) series glucose oligomers, as well as maltodextrins and alpha-limit dextrins, and failed to show the strong substrate inhibitory "brake" effect caused by maltotriose, maltotetrose, and G5 on the native enzyme. In addition, the inhibitory constant for acarbose was 2 orders of magnitude higher for ntMGAM than for native MGAM, suggesting lower affinity and/or fewer binding configurations of the active site in the recombinant enzyme. The results strongly suggested that the C-terminal subunit of MGAM has a greater catalytic efficiency due to a higher affinity for glucan substrates and larger number of binding configurations to its active site. Our results show for the first time, to our knowledge, that the C-terminal subunit of MGAM is responsible for the MGAM peptide's "glucoamylase" activity and is the location of the substrate inhibitory brake. In contrast, the membrane-bound ntMGAM subunit contains the poorly inhibitable "maltase" activity of the internally duplicated enzyme.

  15. 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

  16. 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.

  17. 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.

  18. [Bioactivity guided isolation of alpha-glucosidase inhibitor from whole herbs of Crossostephium chinense].

    Science.gov (United States)

    Wu, Qi; Yang, Xiuwei; Zou, Lei; Fu, Dexian

    2009-09-01

    To investigate the chemical constituents of 70% aqueous ethanol extract from the whole plant of Crossostephium chinense for inhibitory activity against alpha-glucosidase. A bioactivity-guided isolation and purification process was used to identify the alpha-glucosidase activity inhibiting components of the whole plant of C. chinense. The dried whole plants were extracted with 70% aqueous ethanol. The extract was suspended in water and then further fractionated successively with cyclohexane, ethyl acetate, and normal butanol,and tested for their inhibitory activity against alpha-glucosidase in vitro. The chemical structures of isolated compounds were determined by spectroscopic methods including NMR and MS, and comparison with data of authentic samples. All of compounds were assayed for their inhibitory activity against alpha-glucosidase in vitro. The ethyl acetate and water layer fractions showed the strong inhibitory activity, and were subjected to column chromatography over the various stationary phases. Tricetin 3',4',5'-trimethylether (1), scopoletin (2), tanacetin, hispidulin (3), apometzgerin (4), chrysoeriol (5), quercetagetin 3,6, 7-trimethylether (6), selagin (7) , scopolin (8), and quercetagetin-3,6-dimethylether (9) were isolated and characterized by different spectroscopic techniques. Among them, compounds 2, 3, 5-7 and 9 for inhibitory activity against alpha-glucosidase with IC50 (micromol x L(-1)) values of (34.36 +/- 2.06), (146.28 +/- 12.44), (246.26 +/- 8.73), (74.06 +/- 3.83), (42.19 +/- 5.25) and (136.20 +/- 25.73), respectively, were assayed as the active components. A positive drug, acarbose, showed the inhibitory activity against alpha-glucosidase with IC50 value of (489.25 +/- 38.55) mciromol x L(-1) in the same assay conditions with the above test com-1) pounds. The IC50 values of compounds 1, 4, 8 and tanacetin were all more than 1 000 micromol x L(-1). The compounds 5 and 9 were isolated from the genus Crossostephium for the first time

  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

    2013-10-11

    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. Cancer risk in patients aged 30 years and above with type 2 diabetes receiving antidiabetic monotherapy: a cohort study using metformin as the comparator

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    Chen YC

    2015-08-01

    Full Text Available Yu-Ching Chen,1 Victor C Kok,1,2 Ching-Hsuan Chien,1 Jorng-Tzong Horng,1,3 Jeffrey J P Tsai11Department of Biomedical Informatics, Asia University, Taichung, 2Department of Internal Medicine, Kuang Tien General Hospital, Taichung, 3Department of Computer Science and Information Engineering, National Central University, Jhongli, TaiwanIntroduction: Accumulating evidence suggests that metformin reduces incident cancer development. Few cohort studies have evaluated the risk of subsequent cancer development in diabetic cohorts receiving antidiabetic monotherapy. We conducted a population-based study in patients with new-onset type 2 diabetes treated with antidiabetic monotherapy.Methods: We identified a cohort of patients with type 2 diabetics aged ≥30 years receiving hypoglycemic monotherapy (n=7,325 from the 1998–2007 Longitudinal Health Insurance Dataset. Patients were grouped according to the antidiabetic therapy they received into metformin (n=2,223, sulfonylurea (n=3,965, glitazone (n=53, meglitinide (n=128, acarbose (n=150, and insulin (n=806 groups. Patients with preexisting cancer were excluded. All patients were followed up until cancer development, dropout, death, or until December 31, 2008. Cox’s model was used to estimate multivariable hazard ratios (HRs adjusted for age, sex, Charlson comorbidity index, smoking-related comorbidities, alcohol use disorders, morbid obesity, pancreatitis, hypertension, monthly income, and urbanization level. The log-rank test was used to compare cumulative cancer incidence. Two-sided P-values <0.05 were required to reject the null hypothesis.Results: The overall median follow-up duration was 2.5 years (interquartile range, 3.6 years. Totally, 367 and 124 cancers developed in the sulfonylurea and metformin groups, respectively, representing an adjusted HR of 1.36 (95% confidence interval [CI], 1.11–1.67; P<0.005. No significant differences were observed between other groups. Increased adjusted HRs

  2. 1294张口服降糖药处方分析%Analysis of 1294 prescriptions of oral hypoglycemic agents

    Institute of Scientific and Technical Information of China (English)

    谢雅君; 吴久鸿; 王杰松; 薛克昌; 许樟荣

    2011-01-01

    Objective: To investigate the utilization of oral hypoglycemic agents in outpatient in our hospital and provide reference for clinical medication. Methods: The prescriptions of oral hypoglycemic agents in outpatient in January 2010 were retrospectively analyzed, in respect of the numbers of prescriptions, recipe quantity and drug combination. The DDDs and DUI were analyzed. Results: Oral hypoglycemic agents used with high frequency were biguanide (54.87%), sulfonylurea (34.47%) and α -glycosidase inhibitor (34.47%). Metformin and acarbose were used most. The DUI of 16 drugs was close to 1 among 20 oral hypoglycemic agents. The proportion of combined oral hypoglycemic agents accounted for 45.98% in all prescriptions. The most common combination use of oral hypoglycemic agents were biguanide and sulfonylurea, sulfonylurea and α -glycosidase inhibitor. Conclusion: The utilization of oral hypoglycemic agents in outpatient of our hospital was reasonable.%目的:了解我院门诊口服降糖药的使用情况,为临床用药提供参考.方法:回顾性分析我院门诊2010年1月份的口服降糖药处方,对处方数、处方量和联合用药等进行统计,并计算用药频度(DDDs)和药物利用指数(DUI).结果:使用频次较多的降糖药分别是双胍类(54.87%)、磺酰脲类(34.47%)和α-葡萄糖苷酶抑制剂(34.47%);格华止和拜唐苹是处方量最多的药物品种;20种口服降糖药中,有16种药物的DUI值接近1;口服降糖药联合应用占总处方数的45.98%,最常见为磺酰脲类+双胍类和磺酰脲类+α-葡萄糖苷酶抑制剂.结论:我院门诊使用降糖药物基本合理.

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

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    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

  4. 本社区卫生服务中心2011-2013年口服降糖药的应用分析%Analysis of the application of oral hypoglycemic agents in a community health service center during 2011-2013

    Institute of Scientific and Technical Information of China (English)

    李旭琴

    2014-01-01

    目的:了解本社区卫生服务中心口服降糖药的应用情况和趋势。方法:对本社区卫生服务中心2011-2013年口服降糖药的主要品种、销售金额、用药频度(DDDs)、限定日费用(DDC)等进行分类统计、综合分析。结果:口服降糖药销售总金额逐年上升,α-葡萄糖苷酶抑制剂3年来均占据销售金额排名第1位,格列齐特缓释片和二甲双胍片连续3年DDDs居第一、第二,DDC最大的3位依次是阿卡波糖片、伏格列波糖片、瑞格列奈片。结论:本中心口服降糖药应用合理,需求量逐年增加,主要以磺酰脲类为主。安全、有效、良好的依从性是糖尿病治疗药物发展的必然趋势。%Objective: To know the usage and trend of oral hypoglycemic agents in our hospital during 2011-2013. Methods: The main species, sales, DDDs and DDC of oral hypoglycemic agents were statistically classiifed and their utilization was comprehensively analyzed.Results: The sales for oral hypoglycemic agents had been increased year by year during 2011-2013 and α-glucosidase inhibitors were ranked number 1. Metformin was ranked ifrst and gliclazide zyban second in DDDs, and the largest three tablets in DDC were acarbose, voglibose and repaglinide.Conclusion: Use of oral hypoglycemic agents was basically reasonable in our hospital. Their demand has been increasing year by year. Sulfonylurea is a mainly used oral antidiabetic drug. The drugs with safety, effectiveness and good compliance are an inevitable development trend for diabetes therapy.

  5. Analysis of cost-effectiveness of three different drugs in the treatment of type 2 diabetes mellitus%3种治疗方案在2型糖尿病患者中的成本-效果分析

    Institute of Scientific and Technical Information of China (English)

    廖祖松; 陈雁

    2011-01-01

    Objective To explore the cost - effectiveness of three different drugs in the treatment of type 2 diabetes mellitus,to provide reference for choice drug. Methods From the patients using of metformin hydrochloride sustained release tablets、acarbose capsules、gliclazide sustained release tablets were randomly selected 80 cases, namely A group、 B group and C group,compared the cost - effectiveness and sensitivity analysis. Results A group of patients with C/E was 170.18, its value was minimal; C patients group of patients with ⊿ C/⊿ E was 6. 87, smaller than the other two groups. Conclusion The metformin hydrochloride sustained release tablets in the treatment of type 2 diabetes mellitus is the most economical solution, but the effect of gliclazide sustained -release tablets is the best, choice of drug should be based on the different clinical conditions.%目的利用成本-效果分析方法,评价3种方案治疗2型糖尿病的药物经济学效果,为治疗2型糖尿病药物选择提供参考.方法 从采用二甲双胍缓释片、阿卡波糖胶囊和格列齐特缓释片治疗的2型糖尿病患者中各随机选取80例,分别为A组、B组和C组,比较其药物经济学效果和敏感性分析.结果 A组C/E 170.18,最小;C组⊿C/⊿E 6.87,小于其他两组.结论 从药物经济学的角度分析,二甲双胍缓释片治疗2型糖尿病方案最经济,但是格列齐特缓释片疗效最佳,在临床治疗中应根据具体情况合理选药.

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

    Directory of Open Access Journals (Sweden)

    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.

  7. Protective effects of Cynara scolymus leaves extract on metabolic disorders and oxidative stress in alloxan-diabetic rats.

    Science.gov (United States)

    Ben Salem, Maryem; Ben Abdallah Kolsi, Rihab; Dhouibi, Raouia; Ksouda, Kamilia; Charfi, Slim; Yaich, Mahdi; Hammami, Serria; Sahnoun, Zouheir; Zeghal, Khaled Mounir; Jamoussi, Kamel; Affes, Hanen

    2017-06-19

    Diabetes mellitus (DM) is associated with hyperglycemia, inflammatory disorders and abnormal lipid profiles, currently the extracts from leaves of cynara scolymus has been discovered to treat metabolic disorders and has been stated by multitudinous scientists according to a good source of polyphenols compounds. The present study aimed to evaluate the protective effect of the ethanol leaves extract of C. scolymus in alloxan induced stress oxidant, hepatic-kidney dysfunction and histological changes in liver, kidney and pancreas of different experimental groups of rats. We determinate the antioxidant activity by ABTS (.+) and antioxidant total capacity (TAC) of all extracts of C. scolymus leaves, the inhibition of α-amylase activity in vitro was also investigated. Forty male Wistar rats were induced to diabetes with a single dose intraperitoneal injection (i.p.) of alloxan (150 mg/kg body weight (b.w.)). Diabetic rats were orally and daily administrated of ethanol extract from C. scolymus at two doses (200-400 mg/kg, b.w) or (12 mg/kg, b.w) with anti-diabetic reference drug, Acarbose for one month. Ethanol extract of C. scolymus effect was confirmed by biochemical analysis, antioxidant activity and histological study. The results indicated that the ethanol extract from leaves of C. scolymus showed the highest antioxidant activity by ABTS (.+) (499.43g± 39.72 Trolox/g dry extract) and (128.75 ± 8.45 mg VC /g dry extract) for TAC and endowed the powerful inhibition in vitro of α-amylase activity with IC50=72,22 ug/uL. In vivo, the results showed that ethanol extract from the leaves of C. scolymus (200-400 mg/kg) decreased significantly (p rats, respectively associated with significant reduction (p rats, moreover, the administration of ethanol extract appears to exert anti-oxidative activity demonstrated by the increase of CAT, SOD and GSH activities in liver, kidney and pancreas of diabetic rats. This positive effect of the ethanol extract from C. scolymus was

  8. 甲泼尼松龙琥珀酸钠致血糖升高1例%One Case of Elevated Blood Glucose Induced by Methylprednisolone Sodium Succinate

    Institute of Scientific and Technical Information of China (English)

    刘俊

    2014-01-01

    An eighty-year-old male patient with acute attack of chronic bronchitis combined with obstructive pulmonary emphysema received methylprednisolone sodium succinate for injection . After five days of treatment , his fasting blood glucose (FBG) increased from 2.62 mmol/L to 5.0 mmol/L, then methylprednisolone sodium succi-nate was withdrawn . On day 7 after stopping use of the medicine , methylprednisolone sodium succinate was read-ministered because of his asthma aggravation. On day 11, FBG rose to 6.2 mmol/L, then he was given acarbose for hypoglycemic treatment. On day 12, his FBG continued to increase to 6.8mmol/L, then he received oral pred-nisone instead of methylprednisolone sodium succinate . After 3 days of treatment , his FBG lowered to 3 . 2 mmol/L .%1例慢性支气管炎急性发作合并阻塞性肺气肿80岁男性患者,给予注射用甲泼尼松龙琥珀酸钠抗炎对症处理,连续使用5天,空腹血糖由2.62 mmol/L升至5.0 mmol/L ,考虑为注射用甲泼尼松龙琥珀酸钠引起,给予停药处理。第7天,因气喘加重给予甲泼尼松龙琥珀酸钠。第11天,患者血糖6.2 mmol/L ,遂给予阿卡波糖降糖处理。第12天,患者空腹血糖上升至6.8 mmol/L ,将注射用甲泼尼松龙琥珀酸钠更换为波尼松口服。继续治疗3天,复查血糖3.2 mmol/L。

  9. 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

  10. The maltodextrin transport system and metabolism in Lactobacillus acidophilus NCFM and production of novel alpha-glucosides through reverse phosphorolysis by maltose phosphorylase.

    Science.gov (United States)

    Nakai, Hiroyuki; Baumann, Martin J; Petersen, Bent O; Westphal, Yvonne; Schols, Henk; Dilokpimol, Adiphol; Hachem, Maher A; Lahtinen, Sampo J; Duus, Jens Ø; Svensson, Birte

    2009-12-01

    A gene cluster involved in maltodextrin transport and metabolism was identified in the genome of Lactobacillus acidophilus NCFM, which encoded a maltodextrin-binding protein, three maltodextrin ATP-binding cassette transporters and five glycosidases, all under the control of a transcriptional regulator of the LacI-GalR family. Enzymatic properties are described for recombinant maltose phosphorylase (MalP) of glycoside hydrolase family 65 (GH65), which is encoded by malP (GenBank: AAV43670.1) of this gene cluster and produced in Escherichia coli. MalP catalyses phosphorolysis of maltose with inversion of the anomeric configuration releasing beta-glucose 1-phosphate (beta-Glc 1-P) and glucose. The broad specificity of the aglycone binding site was demonstrated by products formed in reverse phosphorolysis using various carbohydrate acceptor substrates and beta-Glc 1-P as the donor. MalP showed strong preference for monosaccharide acceptors with equatorial 3-OH and 4-OH, such as glucose and mannose, and also reacted with 2-deoxy glucosamine and 2-deoxy N-acetyl glucosamine. By contrast, none of the tested di- and trisaccharides served as acceptors. Disaccharide yields obtained from 50 mmbeta-Glc 1-P and 50 mm glucose, glucosamine, N-acetyl glucosamine, mannose, xylose or l-fucose were 99, 80, 53, 93, 81 and 13%, respectively. Product structures were determined by NMR and ESI-MS to be alpha-Glcp-(1-->4)-Glcp (maltose), alpha-Glcp-(1-->4)-GlcNp (maltosamine), alpha-Glcp-(1-->4)-GlcNAcp (N-acetyl maltosamine), alpha-Glcp-(1-->4)-Manp, alpha-Glcp-(1-->4)-Xylp and alpha-Glcp-(1-->4)- L-Fucp, the three latter being novel compounds. Modelling using L. brevis GH65 as the template and superimposition of acarbose from a complex with Thermoanaerobacterium thermosaccharolyticum GH15 glucoamylase suggested that loop 3 of MalP involved in substrate recognition blocked the binding of candidate acceptors larger than monosaccharides.

  11. PTP1B, α-glucosidase, and DPP-IV inhibitory effects for chromene derivatives from the leaves of Smilax china L.

    Science.gov (United States)

    Zhao, Bing Tian; Le, Duc Dat; Nguyen, Phi Hung; Ali, Md Yousof; Choi, Jae-Sue; Min, Byung Sun; Shin, Heung Mook; Rhee, Hae Ik; Woo, Mi Hee

    2016-06-25

    Two new flavonoids, bismilachinone (11) and smilachinin (14), were isolated from the leaves of Smilax china L. together with 14 known compounds. Their structures were elucidated using spectroscopic methods. The PTP1B, α-glucosidase, and DPP-IV inhibitory activities of compounds 1-16 were evaluated at the molecular level. Among them, compounds 4, 7, and 10 showed moderate DPP-IV inhibitory activities with IC50 values of 20.81, 33.12, and 32.93 μM, respectively. Compounds 3, 4, 6, 11, 12, and 16 showed strong PTP1B inhibitory activities, with respective IC50 values of 7.62, 10.80, 0.92, 2.68, 9.77, and 24.17 μM compared with the IC50 value for the positive control (ursolic acid: IC50 = 1.21 μM). Compounds 2-7, 11, 12, 15, and 16 showed potent α-glucosidase inhibitory activities, with respective IC50 values of 8.70, 81.66, 35.11, 35.92, 7.99, 26.28, 11.28, 62.68, 44.32, and 70.12 μM. The positive control, acarbose, displayed an IC50 value of 175.84 μM. In the kinetic study for the PTP1B enzyme, compounds 6, 11, and 12 displayed competitive inhibition with Ki values of 3.20, 8.56, and 5.86 μM, respectively. Compounds 3, 4, and 16 showed noncompetitive inhibition with Ki values of 18.75, 5.95, and 22.86 μM, respectively. Molecular docking study for the competitive inhibitors (6, 11, and 12) radically corroborates the binding affinities and inhibition of PTP1B enzymes. These results indicated that the leaves of Smilax china L. may contain compounds with anti-diabetic activity. Copyright © 2016 Elsevier Ireland Ltd. All rights reserved.

  12. Recent developments and emerging therapies for type 2 diabetes mellitus.

    Science.gov (United States)

    Evans, A J; Krentz, A J

    1999-08-01

    Most patients with type 2 (non-insulin-dependent) diabetes mellitus require pharmacotherapy, initially as monotherapy and subsequently in combination, as adjuncts to diet and exercise. Exogenous insulin is ultimately required in a substantial proportion, reflecting the progressive natural history of the disease. Sulphonylureas and biguanides have been employed for over 4 decades as oral antidiabetic agents, but they have a limited capacity to provide long term glycaemic control and can cause serious adverse effects. Thus, more efficacious and tolerable antidiabetic agents are required. Recent years have witnessed the introduction of agents with novel modes of action, that is, the alpha-glucosidase inhibitors acarbose and miglitol (which reduce postprandial hyperglycaemia) and the first of the thiazolidinedione insulinsensitising drugs--troglitazone and rosiglitazone. Although the former has been withdrawn in some countries due to adverse effects, another 'glitazone' pioglitazone is expected to be approved in the near future. Other recently introduced drugs include glimepiride and the meglitinide insulin secretagogue, repaglinide. Attention is also focusing increasingly on combination therapy using insulin together with sulphonylureas, metformin or troglitazone. Rapid-acting insulin analogues are now being used as alternatives to conventional insulins; their role in the management of type 2 diabetes mellitus is presently uncertain but reports of a reduced frequency of hypoglycaemia are encouraging. The development of new drugs aims to counter the principal metabolic defects of the disorder, respectively, relative insulin deficiency and insulin resistance. Novel classes of rapid-acting secretagogues under evaluation include the morphilinoguanide BTS 67582 and the meglitinides mitiglinide (KAD 1229) and senaglinide (A-4166). Succinate ester derivatives represent a potential novel approach to improving beta-cell function through enhancement of insulin biosynthesis and

  13. Synthesis, molecular structure, spectral analysis, and biological activity of new malonamide derivatives as α-glucosidase inhibitors

    Science.gov (United States)

    Barakat, Assem; Islam, Mohammad Shahidul; Al-Majid, Abdullah Mohammed; Soliman, Saied M.; Ghabbour, Hazem A.; Yousuf, Sammer; Choudhary, M. Iqbal; Ul-Haq, Zaheer

    2017-04-01

    Two new malonamide derivatives were synthesized via the Michael addition of N1,N3-di(pyridin-2-yl)malonamide to α,β-unsaturated ketones using a 1,8-diazabicyclo[5.4.0]undec-7-ene (DBU) catalyst at room temperature. All reactions efficiently furnished the desired malonamide derivatives, which differed only in their substitution on one phenyl group, with one derivative bearing a bromine substituent and the other bearing a methyl group. The structures of newly synthesized compounds were then elucidated by single-crystal X-ray diffraction, infrared spectroscopy, NMR spectroscopy, mass spectrometry, and elemental analysis. In addition, the synthesized compounds were evaluated for their in vitro cytotoxicity against cancer cell lines and for α-glucosidase inhibition. The target compounds exhibited enhanced α-glucosidase inhibition activity (i.e., IC50 = 12.8 ± 0.1 and 28.4 ± 0.2 μM) compared to the common drug acarbose (IC50 = 840 ± 1.73 μM). Both compounds were found to be non-cytotoxic against H460 (lung carcinoma) and T3T (normal fibroblast) cell lines. In addition, the bromo-substituted derivative exhibited weak cytotoxic against cervical cancer HeLa (IC50 = 13.8 ± 0.4 μM) and breast cancer MCF-7 (IC50 = 21.11 ± 0.88 μM) cell lines, while the methyl-substituted derivative showed weak cytotoxicity against the MCF-7 cell line (IC50 = 47.9 ± 0.7 μM). Density functional theory (DFT) B3LYP/6-311G(d,p) calculations were employed to examine the molecular structures and electronic properties of the prepared compounds. As expected, the bromo-derivative (2.2377 D) exhibited a higher polarity than the methyl-derivative (1.9160 D). Furthermore, the HOMO and LUMO diagrams were constructed and the electronic spectra of both compounds were assigned using time-dependent (TD)-DFT calculations. Finally, the calculated NMR chemical shifts correlated well with the experimental data.

  14. Trial update: the Diabetes REduction Approaches with ramipril and rosiglitazone Medications (DREAM trial

    Directory of Open Access Journals (Sweden)

    G. Gulli

    2013-05-01

    Full Text Available BACKGROUND Diabetes (T2DM is a worldwide medical and social emergency in the westernized societies. Lifestyle changes, diet and physical activity, have shown a protective effect on the likelihood of developing T2DM and are strongly recommended for primary prevention in people at increased risk for T2DM. However, maintaining adherence to these nonpharmacologic strategies is dishearteningly challenging, and the possible use of drugs to prevent T2DM remains of keen interest. Metformin, glitazones, acarbose and orlistat can reduce the risk of developing T2DM. Recently, post hoc analyses of several clinical studies suggested that ACE-I as well might reduce the risk of T2DM. AIM OF THE STUDY Since none of these trials was designed with this primary end-point, the Diabetes REduction Assessment with ramipril and rosiglitazone Medication (DREAM Investigators studied the effects of ramipril or rosiglitazone on the risk of T2DM in a randomized trial designed with T2DM as a primary outcome. METHOD Subjects with fasting impaired plasma glucose levels or impaired glucose tolerance, without cardiovascular disease, were randomly assigned, in a 2-by-2 factorial design, to receive either ramipril (up to 15 mg daily or placebo and either rosiglitazone or placebo. They were followed for a median of 3 years. RESULTS Rates of the primary end points, T2DM or death, were not significantly lower in the ramipril group than in the placebo group. In contrast to ramipril, the use of rosiglitazone resulted in a significant reduction in T2DM or death. DISCUSSION Disappointingly, 14 participants on rosiglitazone developed non-fatal heart failure, compared with 2 cases in the placebo group, and the group gained 3% (2.2 kg more in body weight than the placebo group. Moreover, we still do not know whether the effect of rosiglitazone on the incidence of T2DM will persist after drug washout. CONCLUSIONS We believe that the high cost of the drug and the study’s negative

  15. 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.

  16. 白苞裸蒴抗菌和抑制α-葡萄糖苷酶活性研究

    Institute of Scientific and Technical Information of China (English)

    陈百泉; 杨再波; 曹乃锋; 赵琳; 康文艺

    2011-01-01

    目的 对白苞裸蒴各提取部位抑制α-葡萄糖苷酶和抗菌活性进行研究.方法 利用96微孔板法检测其α-葡萄糖苷酶抑制活性;采用纸片扩散法测定最低抑菌浓度(MIC)和液体培养法测定半数抑菌浓度(IC50).结果 白苞裸蒴石油醚部位(IC50=0.698μg/mL),远低于阳性对照Acarbose(IC50=1081.27μg/mL),该部位同时对金黄色葡萄球菌(SA)、耐甲氧西林的金黄色葡萄球菌(MRSA)和β-内酰胺酶阳性的金黄色葡萄球菌(ESBLs)的MIC值和IC50值分别为156.5μg/disc,156.5 μg/disc,625 μg/dise和3.47 mg/mL,5.27 mg/mL,3.54 mg/mL;正丁醇部位对SA、MRSA和ESBLs的MIC值和IC50分别为625 μg/disc,625 μg/disc,625 μg/disc和1.50 mg/mL,4.80 mg/mL,2.94 mg/mL.结论 白苞裸蒴石油醚部位具有较好的α-葡萄糖苷酶的抑制活性;并且白苞裸蒴石油醚和正丁醇部位对SA、MRSA和ESBLs均具有良好的抗菌活性.

  17. 苦荞黄酮对α-淀粉酶的抑制作用研究%Research on α- Amylase Inhibition Function of Buckwheat Flavonoids

    Institute of Scientific and Technical Information of China (English)

    王斯慧; 白银花; 黄琬凌; 曾里; 曾凡骏

    2012-01-01

    为了比较研究各种不同提取方法下的苦荞黄酮对α-淀粉酶的抑制作用,分别对苦荞总黄酮溶液、苦荞水溶性黄酮溶液、苦荞醇溶性黄酮溶液用α-淀粉酶进行体外活性抑制作用试验,并绘制抑制曲线,所得的结果与阿卡波糖进行比较。结果表明:阿卡波糖、苦荞总黄酮、苦荞水溶性黄酮、苦荞醇溶性黄酮对α-淀粉酶均有抑制作用,其半抑制浓度(IC50)值分别为0.095、0.086、0.10、0.202 mg/mL。本研究为三种提取产物在防治糖尿病及其并发症等方面的应用提供参考,具有较大的理论意义和应用价值。%For comparison research of various extraction methods of buckwheat flavonoids with α-amylase were identified inhibitory effect respectively, the buckwheat flavonoids solution, buckwheat water soluble flavonoids solution, buckwheat alcohol-soluble flavonoids solution with u-amylase were identified in vitro activity conducted inhibition experiment. Through the rendering of α-amylase activity inhibit curve, calculate the half inhibiting concentration (IC50) of raw material on α-amylase were identified respectively, acarbose is 0.09, buckwheat flavonoids solution is 0.086 ,water-soluble flavonoids solution is 0.108, buckwheat alcohol soluble flavonoids solution is 0.200 mg/mL. The results can provide important references for the value-added utilization of the 3 products and theirs application in preventing and treating diabetes.

  18. 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

  19. 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.

  20. 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.

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

    Directory of Open Access Journals (Sweden)

    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

  2. Effects of Syzygium aromaticum-derived triterpenes on postprandial blood glucose in streptozotocin-induced diabetic rats following carbohydrate challenge.

    Directory of Open Access Journals (Sweden)

    Andile Khathi

    Full Text Available PURPOSE: Recent reports suggest that the hypoglycaemic effects of the triterpenes involve inhibition of glucose transport in the small intestine. Therefore, the effects of Syzygium spp-derived triterpenes oleanolic acid (OA and maslinic acid (MA were evaluated on carbohydrate hydrolyzing enzymes in STZ-induced diabetic rats and consequences on postprandial hyperglycaemia after carbohydrate loading. METHODS: We determined using Western blot analysis the expressions of α-amylase and α-glucosidase and glucose transporters SGLT1 and GLUT2 in the small intestine intestines isolated from diabetic rats treated with OA/MA for 5 weeks. In vitro assays were used to assess the inhibitory activities of OA and MA against α-amylase, α-glucosidase and sucrase. RESULTS: OA and MA ameliorated postprandial hyperglycemia in carbohydrate loaded diabetic rats as indicated by the significantly small glucose area under the curve (AUC in treated diabetic animals compared with that in untreated diabetic rats. Western blotting showed that OA and MA treatment not only down-regulated the increase of SGLT1 and GLUT2 expressions in the small intestine of STZ-induced diabetic rats, but also inhibited small intestine α-amylase, sucrase and α-glucosidase activity. IC50 values of OA against α-amylase (3.60 ± 0.18 mmol/L, α-glucosidase (12.40 ± 0.11 mmol/L and sucrase (11.50 ± 0.13 mmol/L did not significantly differ from those of OA and acarbose. CONCLUSIONS: The results of suggest that OA and MA may be used as potential supplements for treating postprandial hyperglycemia. NOVELTY OF THE WORK: The present observations indicate that besides improving glucose homeostasis in diabetes, OA and MA suppress postprandial hyperglycaemia mediated in part via inhibition of carbohydrate hydrolysis and reduction of glucose transporters in the gastrointestinal tract. Inhibition of α-glucosidase and α-amylase can significantly decrease the postprandial hyperglycaemia after a mixed

  3. Clinical Effcacy and Adverse Reactions of Voglibose Tablets in the Treatment of Type 2 Diabetes Mellitus%伏格列波糖片治疗2型糖尿病的临床效果及不良反应分析

    Institute of Scientific and Technical Information of China (English)

    窦国朝; 李明芬

    2016-01-01

    Objective To observe the voglibose tablets for treatment of type 2 diabetes, analyzing the adverse reactions occur. Methods We treated 80 patients with type 2 diabetes as the research object, the patients were randomly divided into control group and experimental group, with acarbose tablets for control group patients treatment, for application of the experimental group patients voglibose tablets treatment of implementation. Comparison of two groups of patients with therapeutic effect and adverse reactions. Results Two groups of patients after treatment, the fasting blood glucose, glycosylated hemoglobin, two hours after the meal, blood sugar levels are lower than before treatment, P0.05. Incidence of adverse reactions obviously lower than the control group and experimental group patients, P<0.05, differences have statistical significance. Conclusion Using voglibose tablets in the treatment of type 2 diabetes, clinical effect is remarkable, the probability of adverse reaction is lower, should be popularized and applied in clinical.%目的:观察伏格列波糖片治疗2型糖尿病的临床效果,分析不良反应发生情况。方法选取本院收治的2型糖尿病患者80例作为研究对象,将患者随机分成对照组和实验组,为对照组患者应用阿卡波糖片实施治疗,为实验组患者应用伏格列波糖片实施治疗。对比两组患者的治疗效果和不良反应情况。结果两组患者治疗后,空腹血糖、糖化血红蛋白、餐后2小时血糖均低于治疗前,P<0.05。两组患者治疗以后比较,P>0.05。并且实验组患者不良反应发生率低于对照组患者,P<0.05,差异具有统计学意义。结论运用伏格列波糖片治疗2型糖尿病,临床效果显著,发生不良反应的概率比较低。

  4. Molecular structure and spectroscopic investigations combined with hypoglycemic/anticancer and docking studies of a new barbituric acid derivative

    Science.gov (United States)

    Barakat, Assem; Soliman, Saied M.; Elshaier, Yaseen A. M. M.; Ali, M.; Al-Majid, Abdullah Mohammed; Ghabbour, Hazem A.

    2017-04-01

    The one-pot synthesis reaction of barbituric acid derivative, 1,3-cyclohexandione, and 4-fluorobenzaldehyde in water mediated by NHEt2 as base afforded 4 with excellent yield. The synthesized compound was characterized by spectrophotometric tools as well as X-ray single crystal diffraction technique. The stability of the nine possible isomers of the synthesized compound was studied using the B3LYP method and 6-31G(d,p) basis set. The electronic and spectroscopic properties of the most stable isomer were predicted. The UV-Vis absorption spectrum displayed two bands at 203 and 257 nm in the solvent chloroform. The latter was calculated at 235.6 nm (f = 0.1995) in the gas phase due to H-2→L (42%) and H-1→L+2 (14%) excitations. In solution, using chloroform as a solvent, a slight bathochromic shift to 237.6 nm with an increase in the absorption intensity (f = 0.2898) was predicted. The molecular orbital energy level diagram of this transition band was characterized mainly by π-π* transitions. The 13C and 1H NMR chemical shifts correlated well with the experimental data. The correlations had higher correlation coefficients (R2) when solvent effects were considered. The atomic charges were calculated using natural population analysis and the charged regions were presented using a molecular electrostatic potential (MEP) map. The synthesized compound was examined as a hypoglycemic agent via inhibition of α-glucosidase and β-glucuronidase enzymes. Its inhibitory activity against α-glucosidase was 10 times greater than the inhibitory activity of the standard drug acarbose (IC50 77.9 ± 0.3 μM and 840 ± 1.73 μM, respectively). Moreover, the target compound was evaluated for anticancer activity against MCF-7, H460, 3T3, and Hela cell lines. It demonstrated inhibitory activity against the MCF-7 and H460 cell lines with IC50 5.80 ± 0.12 and 19.6 ± 0.5 μM, respectively, in comparison to doxorubicin. The docking study was performed using the OpenEye program.

  5. Effects of Syzygium aromaticum-Derived Triterpenes on Postprandial Blood Glucose in Streptozotocin-Induced Diabetic Rats Following Carbohydrate Challenge

    Science.gov (United States)

    Khathi, Andile; Serumula, Metse R.; Myburg, Rene B.; Van Heerden, Fanie R.; Musabayane, Cephas T.

    2013-01-01

    Purpose Recent reports suggest that the hypoglycaemic effects of the triterpenes involve inhibition of glucose transport in the small intestine. Therefore, the effects of Syzygium spp-derived triterpenes oleanolic acid (OA) and maslinic acid (MA) were evaluated on carbohydrate hydrolyzing enzymes in STZ-induced diabetic rats and consequences on postprandial hyperglycaemia after carbohydrate loading. Methods We determined using Western blot analysis the expressions of α-amylase and α-glucosidase and glucose transporters SGLT1 and GLUT2 in the small intestine intestines isolated from diabetic rats treated with OA/MA for 5 weeks. In vitro assays were used to assess the inhibitory activities of OA and MA against α-amylase, α-glucosidase and sucrase. Results OA and MA ameliorated postprandial hyperglycemia in carbohydrate loaded diabetic rats as indicated by the significantly small glucose area under the curve (AUC) in treated diabetic animals compared with that in untreated diabetic rats. Western blotting showed that OA and MA treatment not only down-regulated the increase of SGLT1 and GLUT2 expressions in the small intestine of STZ-induced diabetic rats, but also inhibited small intestine α-amylase, sucrase and α-glucosidase activity. IC50 values of OA against α-amylase (3.60 ± 0.18 mmol/L), α-glucosidase (12.40 ± 0.11 mmol/L) and sucrase (11.50 ± 0.13 mmol/L) did not significantly differ from those of OA and acarbose. Conclusions The results of suggest that OA and MA may be used as potential supplements for treating postprandial hyperglycemia. Novelty of the Work The present observations indicate that besides improving glucose homeostasis in diabetes, OA and MA suppress postprandial hyperglycaemia mediated in part via inhibition of carbohydrate hydrolysis and reduction of glucose transporters in the gastrointestinal tract. Inhibition of α-glucosidase and α-amylase can significantly decrease the postprandial hyperglycaemia after a mixed carbohydrate diet

  6. [Diabetes and nutrition].

    Science.gov (United States)

    Sanz París, A

    2000-01-01

    -acting insulin, either intravenously or subcutaneously, is recommended in the acute stages of the underlying condition because any instability in the patient makes it difficult to plan the required dose of intermediate-acting NPH insulin. The use of metformin or acarbose is not recommended. In parenteral nutrition, the subcutaneous administration of NPH insulin is often required at doses of 30% of the home dosage as the basal insulin therapy in addition to fast-acting insulin in the nutrition bag and a regimen of subcutaneous fast-acting insulin every 6 hours depending on glycaemia.

  7. 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

  8. 新型α-葡萄糖苷酶抑制剂类降血糖药的合成及其活性研究%Synthesis of New Type α-Glucosidase Inhibitor Hypoglycemic Drugs and Its Activity Study

    Institute of Scientific and Technical Information of China (English)

    王谦; 边晓丽; 樊向妮; 罗振吉; 赵桂兰

    2013-01-01

    目的:合成一种新型葡萄糖氮苷化合物,并对其α-葡萄糖苷酶抑制活性及降低餐后血糖活性进行初步研究,为寻找具有新型结构的α-葡萄糖苷酶抑制剂类降血糖药奠定基础.方法:取邻苯二甲酰亚胺经硝化、成盐得4-硝基酞酰亚胺钾盐,再与葡萄糖经乙酰化、溴化得到的溴代葡萄糖反应后去乙酰基得到目标化合物.以阿卡波糖为阳性对照药,对目标化合物进行酵母和小鼠肠来源的α-葡萄糖苷酶(麦芽糖酶、乳糖酶和淀粉酶)体外抑制活性[以半数抑制浓度(IC50)为指标]的测定,以及灌胃给药2h内小鼠餐后血糖水平变化的初步研究.结果:合成了目标化合物,其结构经质谱(MS)及核磁共振(1H-NMR)确证;目标化合物对4种酶的活性抑制强弱顺序为:酵母α-葡萄糖苷酶、麦芽糖酶、乳糖酶、淀粉酶(IC50分别为1.49、33.7、101.1、>200 μmol/L);其可降低正常小鼠餐后血糖,其与阳性对照药、空白组餐后2h时血糖水平分别为(10.6±0.4)、(7.4±1.0)、(11.9±0.7) mmol/L.结论:合成了一种新的葡萄糖氮苷化合物5-硝基-2-(β-D-吡喃葡萄糖基)-1H-异吲哚-1,3二酮;其体外具有明显的α-葡萄糖苷酶抑制活性,体内具有降低正常小鼠餐后血糖的活性但不及阿卡波糖.%OBJECTIVE: To synthesize new type glocosaminidase compound, and to study its activity of α-glucosidase and postprandial blood glucose, and to lay a foundation for the development of new type a-glucosidase inhibitor hypoglycemic drugs. METHODS: Phthalimide was nitrified and salified to produce 4-nitro phthalimidopotassium. Target product was obtained after 4-ni-tro phthalimidopotassium reacted with acetylized and bromized glucose, following by deacetylation. The IC50 of a-glucosidase (malt-ase, lactase and amylase) from yeast and mice intestines were determined using acarbose as positive control. Postprandial blood glucose was determined in mice within 2 h after

  9. 没食子酸对α-葡萄糖苷酶的抑制作用及其降糖机制研究%The Research of Gallic Acid' s a - Glycosidase Inhibition and the Hypoglycemic Mechanism

    Institute of Scientific and Technical Information of China (English)

    张海凤; 董亚琳; 张琰

    2011-01-01

    ijeetive To investigate the o. - glycosidase inhibition and inhibition type of gallic acid by using enzyme - inhibition model and Caco ~ 2 cell model. To study the potential value of phenolic acid on treating diabetes and the meaning of Caco - 2 cell model on screening antidiahetic drug. Methods Enzyme - inhibition model and Caco - 2 cell model were used to study the influence of gallic acid on a. -glycosidase activity. Otherwise,using Caco - 2 cell model to study the effect of gallic acid on glucose absorption. Results When we made maltose as substrate, gallic acid displayed a - glycosidase inhibition on enzyme - inhibition model,the Icsc was 577.5 fj_g/mL; Gallic acid also had a - glycosidase inhibition on Caco - 2 cell model, its iC Was 182. 6 jxg/mL. The a - glycosidase inhibition of 250 jLg/mL gallic acid was lower than the same concentration of acarbose( P < 0. 05). Gallic acid is a competitive inhibitor for a - glycosidase. At the same lime, gallic acid inhibited glucose absorption. Conclusion Gallic acid is a a - glycosidase inhibitor, and the traditional Chinese medicines which contain it can be developed to medicine or health product treating non - insulin dependent diabetes. Caco - 2 cell model can be used to screen the antidiabetie drug.%目的 研究没食子酸对α-葡萄糖苷酶的抑制作用及其抑制类型,探索酚酸类化合物在治疗糖尿病方面的价值及Caco-2细胞模型在筛选降糖药方面的作用.方法 以麦芽糖为底物,采用酶-抑制剂模型和Caco-2细胞模型研究没食子酸对α-葡萄糖苷酶活力的影响,采用Caco-2细胞模型研究没食子酸对葡萄糖吸收的影响.结果 没食子酸对两种模型的α-葡萄糖苷酶均有抑制作用,半数抑制量(IC_(50))为577.5 μg/mL和182.6 μg/mL;250 μg/mL的没食子酸对α-葡萄糖苷酶抑制作用低于同浓度的阿卡波糖(P<0.05).没食子酸是α-葡萄糖苷酶的竞争型抑制剂.没食子酸对葡萄糖吸收有抑制作用.结论

  10. Vildagliptin: a review of its use in type 2 diabetes mellitus.

    Science.gov (United States)

    Keating, Gillian M

    2010-11-12

    Vildagliptin (Galvus®, Jalra®, Xiliarx®) is an orally administered dipeptidyl peptidase-4 (DPP-4) inhibitor. In patients with type 2 diabetes mellitus, vildagliptin 50 mg twice daily is indicated for use in combination with metformin or a thiazolidinedione, and vildagliptin 50 mg once daily is indicated for use in combination with a sulfonylurea. A fixed-dose combination of vildagliptin/metformin (Eucreas®, Icandra®, Zomarist®) is also available. This article reviews the clinical efficacy and tolerability of vildagliptin in patients with type 2 diabetes, as well as summarizing its pharmacological properties. The efficacy of monotherapy or combination therapy with oral vildagliptin in patients with type 2 diabetes has been examined in randomized, double-blind, multicentre trials. Monotherapy with vildagliptin 50 mg once or twice daily reduced glycosylated haemoglobin (HbA(1c)) from baseline to a significantly greater extent than placebo, according to the results of 12- to 52-week trials in patients with type 2 diabetes. In terms of the reduction from baseline in HbA(1c) seen in active comparator trials of 12-104 weeks' duration, the noninferiority of vildagliptin 50 mg twice daily was established versus acarbose or rosiglitazone, the noninferiority of vildagliptin 100 mg once daily (an off-label dosage) versus metformin was established in elderly patients and vildagliptin 50 mg twice daily was more effective than voglibose; however, the noninferiority of vildagliptin 50 mg twice daily versus metformin or gliclazide was not established in two other trials. Combination therapy with vildagliptin 50 mg twice daily plus metformin improved HbA(1c) to a significantly greater extent than monotherapy with metformin and/or vildagliptin alone in patients with type 2 diabetes whose disease was inadequately controlled by metformin monotherapy or who were treatment naive, according to the results of 12- or 24-week trials. In addition, vildagliptin 50

  11. 4种方案治疗2型糖尿病的成本-效果分析%Cost-effectiveness Analysis of 4 Therapeutic Schemes in the Treatment of Type 2 Diabetes Meilitus

    Institute of Scientific and Technical Information of China (English)

    沈万香; 张邦升

    2011-01-01

    目的:比较4种方案治疗2型糖尿病的成本-效果.方法:将2009-2010年入选的2型糖尿病患者随机分为A组(72例,阿卡波糖)、B组(72例,格列美脲)、C组(71例,二甲双胍)、D组(71例,瑞格列奈+二甲双胍)并进行治疗.评价其疗效并进行成本-效果分析.结果:治疗后,4组空腹血糖及餐后2h血糖的总有效率两两比较差异均无统计学意义(P>0.05);4组成本分别为798.32、258.54、184.55、210.32元;对空腹血糖的成本-效果比分别为942.53、310.37、225.89、240.92;对餐后2h血糖的成本-效果比分别为845.68、300.28、214.84、237.11;A、B、D组相对于C组对空腹血糖的增量成本-效果比分别为20 459、4 624.38、460.18,对餐后2h血糖的增量成本-效果比分别为7 220.82、36 995.00、920.36.结论:二甲双胍治疗2型糖尿病成本较低,但瑞格列奈联合二甲双胍控制2型糖尿病患者空腹血糖和餐后2h血糖的成本-效果比较优.%OBJECTIVE: To compare the cost-effectiveness of four treatment schemes on type 2 diabetes mellitus. METHODS: Included type 2 diabetes mellitus patients during 2009 - 2010 were randomly divided into group A (72 cases, acarbose), group B (72 cases, glimepride), group C (71 case, metformin), group D (71 cases, repaglinide+metformin). Therapeutic efficacies of those groups were evaluated and cost-effect analysis was conducted. RESULTS: There was no statistical significance in the total effective rate of fasting blood glucose and 2 h blood glucose after meal among 4 groups after treatment (p>0.05). The costs of 4 groups were 798.32 yuan, 258.54 yuan, 184.55 yuan and 210.32 yuan, respectively. The cost-effectiveness ratios of fasting blood sugar were 942.53, 310.37, 225.89 and 240.92. The cost-effectiveness ratio of blood sugar 2 h after meal were 845.68, 300.28, 214.84 and 237.11; The incremental cost-effectiveness ratios of fasting blood glucose in group A, B, D were 20 459, 4 624.38, 460.18, compared with

  12. Analysis of cost-effectiveness of 3 therapeutic schemes for type 2 diabetes mellitus%3种方案治疗2型糖尿病的成本-效果分析

    Institute of Scientific and Technical Information of China (English)

    于丹; 拾倩

    2016-01-01

    Objective To compare the curative effects and pharmacoeconomic costs of 3 therapeutic schemes in the treatment of type 2 diabetes mellitus. Methods By a retrospective survey method, 150 cases of type 2 diabetes mellitus patients were randomly divided into 3 groups. The 50 patients in group A were given Metformin hydrochloride sustained-release tablets, the 50 patients in group B were given Acarbose tablets, and the 50 patients in group C were given Mitiglinide calcium tablets for 12 weeks. The levels of fasting blood glucose (FBG), 2-h postprandial blood glucose (PBG) and HbA1c were observed in the 3 groups before and after treatment. The cost-effectiveness was evaluated by pharmacoeconomic method. Results After 12 weeks, the FPG, 2-h PBG and HbAlc of the 3 groups were decreased to some extent. The costs of the 3 therapeutic schemes were 208.32, 529.20 and 609.84 yuan, respectively. The total effective rate of the groups A, B and C were 70.00%, 74.00% and 82.00%, respectively. The cost-effectiveness ratio of the groups A, B and C was 2.98, 7.15 and 7.44 respectively. Using the group A as a reference, ∆C/∆E for the groups B and C were 80.22 and 33.46 yuan respectively. Conclusions Among the 3 therapeutic schemes, Mitiglinide for the group C has pharmacoeconomic advantage in treating type 2 diabetes mellitus.%目的:比较3种方案治疗2型糖尿病的临床疗效并进行药物经济学成本-效果分析。方法采用回顾性调查方法,150例糖尿病患者随机分为二甲双胍组(A)、阿卡波糖组(B)、米格列奈组(C),疗程均为12周。观察3组患者治疗前后空腹血糖(FBG)、餐后2h血糖(2hPBG)、糖化血红蛋白值(HbA1c),运用成本-效果分析方法进行评价。结果治疗12周后,3组患者的FBG、2hPBG、HbA1c均不同程度降低。3种治疗糖尿病方案的成本分别为208.32、529.20和609.84元;总有效率分别为70.00%、74.00%和82.00%;成本-效果比分别为2.98、7

  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. 三种方案治疗2型糖尿病的药物经济学分析%Pharmaceutical Economics Analysis of 3 Schemes for the Treatment of Type 2 Diabetes Mellitus

    Institute of Scientific and Technical Information of China (English)

    俞聪聪; 张翼

    2016-01-01

    Objective To investigate the drug economic situation of 2 types of treatment for type 3 diabetes melitus.Methods Select November June 2013 to 2015,Jiaxing City,Zhejiang Province the first hospital treated 120 cases of type 2 diabetic patients as the research object,according to the different treatment patients were divided into group A(41 cases),B group (40 cases) and group C(39 cases).Respectively,acarbose and metformin treatment group,glimepiride and metformin treatment group,repaglinide + metformin treatment group.The clinical efficacy and adverse reactions of the 3 groups were compared,and the cost-effectiveness,incremental cost-effectiveness,and sensitivity analysis were performed in 3 groups of patients.Results 3 group cost effectiveness ratio(C/E),B group was significantly lower than that of the group A,group C,the difference is statisticaly significant(P<0.05);from the incremental cost-effectiveness ratio(△C/△E),if get an effect unit,group B to less costly than that in group A and C;test fee increases of 5%,drug costs down 10%,draws the conclusion,the cost of the three groups is stil statisticaly significant(P<0.05).Conclusion A clinical curative effect of treatment group 3,from the perspective of cost - effect of glimepiride and metformin is the best option.%目的:探讨三种方案治疗2型糖尿病的药物经济学分析。方法选取2013年6月至2015年11月浙江省嘉兴市第一医院收治的120例2型糖尿病患者作为研究对象,根据治疗方案不同将患者分为A组(41例)、B组(40例)、C组(39例),分别为阿卡波糖+二甲双胍治疗组、格列美脲+二甲双胍治疗组、瑞格列奈+二甲双胍治疗组。比较3组患者的临床疗效、不良反应发生情况,并采用成本-效果分析法分析3组患者的成本-效果、增量成本-效果,并进行敏感性分析。结果3组成本-效果比(C/E),B组明显低于A组、C组,差异有统计学意义(P<0.05);从增量成

  15. Data Envelopment Analysis of ThreeTherapy Schemes in the Treatment of Type 2 Diabetes%3种用药方案治疗2型糖尿病的数据包络分析

    Institute of Scientific and Technical Information of China (English)

    张正升; 何争民; 陈进; 刘秀珍

    2015-01-01

    OBJECTIVE To evaluate the DEA of three therapy schemes in the treatment of type 2 diabe-tes.METHODS A total of 96 patients were enrolled and randomized to Group A ( metformin+sulfonylureas 32 ) , Group B ( acarbose+Insulinglargineinjection 29 ) or Group C ( protamine zinc recombinant human insulin M30 35 ) .The DEA of the 3 groups was evaluated after treatment for 1 year with clinical randomized trial were followed up.The medical costs of inputs,fasting blood glucose (FBG),2h postprandial blood glucose (2hPG),glycosylated hemoglobin ( HbAlc%) ,quality adjusted life years ( QALYs) as the output,using data envelopment analysis ( DEA) comprehensive evaluation of the economics of input and output.RESULTS DEA results showed that the group C input and output achievd optimal.A and B group investment cost was higher and the clinical curative effect was to be improved.QALYs of A group needed to be improved, B group had reached the ideal value.CONCLUSION Premixed insulin therapy has a better clinical effect and economic effect.%目的:评价3种用药方案治疗2型糖尿病的数据包络分析。方法96名患者分为3组,分别给予二甲双胍肠溶片联合磺脲类药物(A组32人)、阿卡波糖联合甘精胰岛素组(甘精胰岛素,B组29人)、预混胰岛素组(精蛋白重组人胰岛素M30,C组35人)治疗1年,期间每3个月随访1次。以医疗成本为投入,空腹血糖(FBG),餐后2h血糖(PBG2H),糖化血红蛋白(HbAlc%),质量调整生命年(QALYs)为产出,使用数据包络分析(DEA)对投入和产出进行经济学综合评价。结果数据包络分析结果显示C组投入和产出的配比达到最优,A组、B组投入成本偏高且临床疗效有待提高,QALYs值A组有待提高,B组获得的已达到理想值。结论3种治疗方案中预混胰岛素方案更加经济有效。

  16. 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。

  17. 胰岛素自身免疫综合征临床特征及随访资料分析并文献复习%Insulin autoimmune syndrome: An analysis of clinical features, following up data, and review of literature

    Institute of Scientific and Technical Information of China (English)

    陈敏; 母义明; 陆菊明; 窦京涛; 王先令; 谷伟军; 杜锦; 郭清华; 杨国庆; 巴建明; 吕朝晖

    2012-01-01

    Objective To analyze the clinical characteristics and prognosis of patients with insulin autoimmune syndrome (IAS) and to get better understanding of IAS by literatures reviewing.Methods Nine cases of IAS who were diagnosed in the General Hospital of the People's Liberation Army from 2001 to 2011 were analyzed.Results All patients had hypoglycemic syndrome and episodes of hypoglycemia during both postprandial and fasting states.Most cases (8/9) were accompanied with autoimmune diseases,including 6 cases of Graves' disease treated with methimazole.The biochemical data showed extremely elevated serum insulin level (9/9) during hypoglycemic episode.For most patients,the tests of insulin autoantibodies were positive (7/9) while results of imaging examinations were negative(8/9).After removal of possible offending medications and with diet treatment,hypoglycemic episodes were ameliorated in 5 of 9 cases.For severe patients,acarbose (1/9) and prednisone (3/9)therapy were useful.During the period of follow-up,four cases experienced no episode of hypoglycemia and 3 cases with markedly reduced episodes.Conclusions IAS is characterized by hypoglycemic episodes,elevated blood insulin levels,and positive insulin autoantibodies.It is strongly related with autoimmune disease and is able to be induced by methimazole.Most patients undergo remission after diet treatment,drug withdrawal,and oral prednisone.%目的 分析胰岛素自身免疫综合征(IAS)的临床特征和预后,结合文献加深对IAS的认识.方法 回顾性分析9例IAS患者的临床资料并进行随访.结果 9例患者均有低血糖表现,低血糖可发生在空腹和餐后;大部分患者(8/9)合并自身免疫性疾病,其中6例为Graves病,并都在发病前用他巴唑治疗;实验室检查提示低血糖时血胰岛素水平明显升高(9/9),胰岛素自身抗体阳性(7/9);影像学检查多呈阴性(8/9);停用诱发药物和调整饮食后,部分患者(5/9)症状缓解,未

  18. 我院2型糖尿病患者平均住院日及人均医疗费用支出的比较

    Institute of Scientific and Technical Information of China (English)

    崔明迪

    2015-01-01

    Objective To evaluate the method of financial analysis of our hospital patients with type 2 diabetes mellitus average hospitalization days and medical expense per capita spending compared to provide the basis for patients with type 2 diabetes treatment has good effect and low cost.Methods By retrospective analysis, we selected 80 cases of patients, the blood glucose value as the measurement index of health effect of applying the evaluation method of oral hypoglycemic agents of three regimens of cost-effectiveness analysis (A group: Twelve metformin glipizide sustained-release tablets; group B: glipizide + acarbose; group C: glipizide + rosiglitazone) effect of pharmacoeconomics treatment diabetes and sensitivity analysis.Results 3 Schemes of the effective rate were 83.3%, 86.7%, 96.7%.C regimen is better than A and B. The average blood glucose decreased by one percentage point, the three program costs were 15.29 yuan, 27.29 yuan, 34.14 yuan.Conclusion 3 The therapeutic schemes were able to control the blood glucose in the ideal range, from the point of view of the drug by the analysis, the treatment of the twelve a double regimen of metformin hydrochloride is better than the best.%目的:运用我院财务分析的方法评价2型糖尿病患者平均住院日及人均医疗费用支出进行比较,为2型糖尿病患者选择疗效好且费用低的治疗方案提供依据。方法:采用回顾性分析法,选取80例病人,以血糖值为健康效果测量指标,运用成本效果分析方法评价口服降糖药三种给药方案(A组:格列吡嗪十二甲双胍缓释片;B组:格列吡嗪+阿卡波糖;C组:格列吡嗪+罗格列酮)治疗Ⅱ型搪尿病的药物经济学效果.并进行敏感性分析。结果:3种方案的有效率分别为83.3%、86.7%、96.7%,C方案疗效要优于A、B方案。使平均血糖下降一个百分点,三方案费用分别为15.29元、27.29元、34.14元。结论:3种治疗方案都能将血

  19. Screening of pancreatic lipase and α-glucosidase inhibitors from Chinese dietary herbs%药食两用中药中脂肪酶以及α-葡萄糖苷酶抑制剂的筛选

    Institute of Scientific and Technical Information of China (English)

    孙晓丽; 张锴镔; 纪秀红; 王彦文; Jeffrey Zidichouski; 仝燕; 高慧敏; 张君增; 王智民

    2012-01-01

    目的:通过对部分药食两用中药材提取物进行筛选,寻找新的脂肪酶以及α-葡萄糖苷酶的天然抑制剂.方法:采用酶活性测定法,用奥利司他(orlistat),阿卡波糖(acarbose)作为阳性对照对所选39个科别下的63种药食两用中药提取物进行筛选,分别测定其对脂肪酶和α-葡萄糖苷酶活性的抑制效力.结果:荷叶,姜黄,荜茇,桑枝以及桑白皮的药材提取物均显示出了较强的脂肪酶以及α-葡萄糖苷酶的共同抑制作用,它们对脂肪酶的半数抑制浓度分别为(28.00±5.51),(5.24±0.51),( 14.76±2.58),(4.78±0.58),(3.41±0.67) mg·L-1;对α-葡萄糖苷酶的半数抑制浓度分别为( 1.98±0.13),(0.18±0.007),(0.71±0.08),(0.077±0.005),(0.089±0.006)g·L-1.结论:此次筛选为进一步发现新的脂肪酶以及α-葡萄糖苷酶的抑制剂,开发新型降脂降糖天然药物和保健品奠定了一定基础.%The present study was conducted to develop new inhibitors of pancreatic lipase and α-glucosidase from Chinese dietary herbs. Sixty-three dietary herbs from 39 taxonomic families were selected and extracted with aqueous ethanol or water. The extracts were then tested with in vitro enzyme assays for their ability to inhibit pancreatic lipase and a-glucosidase activities. Orlistat and aear-bose were used as two positive controls. The extracts of Nelumbo nucifera, Curcuma longa, Piper longum and Moms alba showed strong pancreatic lipase inhibitory effects with IC50 at (28.00 ±5.51), (124±0.51), (14.76±2.58), (4.78±0.58), (3.41 ±0.67) mg·L-1, respectively. These extracts also showed potent a-glucosidase inhibitory activities with IC50 at (1.98 ±0. 13), (0.18 ± 0. 007), (0.71 ±0.08) , (0.077 ±0.005) , (0.089 ±0.006) g·L-1, respectively. The results provide useful information for developing new drugs or natural health products for hyperlipidemia and hypoglycemia from Chinese dietary herbs.

  20. "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.

  1. 糖尿病前期人群综合强化干预两年后的转归及影响因素%Outcome and influencing factors of integrated intensive intervention in participants with impaired glucose regulation for two years

    Institute of Scientific and Technical Information of China (English)

    卢艳慧; 张育青; 潘长玉; 陆菊明; 王淑玉; 李春霖; 刘力生; 郑润平; 田慧; 王先令; 杨丽娟

    2009-01-01

    Objective To investigate the outcome and related risk factors of integrated intensive intervention in participants with impaired glucose regulation (IGR) after two years by the criteria of American Diabetes Association 2003. Methods The subjects who remained to be IGR at the end of first year following 75 g oral glucose tolerance test were randomly assigned to either a routine care control group or to an intensive integrated intervention group. The control group received general dietary and exercise advice at baseline and was followed up. In addition to dietary control and exercise advice, mefformin or acarbose were administrated in the intervention group. The latter group was also advised to take antihypertensive agents, lipid-regulating agents if necessary, as well as aspirin. Results The proportion of patients who fulfilled the assigned goals of blood glucose, blood pressure, body mass index or triglycerides was significantly higher in the intensive group than those in the control group. None in the intensive group developed overt diabetes mellitus, while 8 (9.3%) in the control group did. The proportion of patients who reverted to normal glucose tolerance (NGT) was slightly higher in the intensive group than in the control group (29.5% vs 22.1%, P>0.05). Logistic analysis showed that increase of waist circumference and systolic blood pressure was positively while the improvement of islet β-cell function was negatively correlated with the development of diabetes mellitus. Conclusions The intensive integrated intervention could significantly decrease the conversion rate of IGR to diabetes mellitus, and increase the chance of reversion to NGT. The increase of waist circumference or systolic blood pressure, the deterioration of islet β-ccll function were the influencing factors of the conversion of IGR to diabetes mellitus.%目的 采用2003年美国糖尿病学会(ADA)标准分析综合强化干预2年后糖尿病前期人群的转归及影响因素.方法 将

  2. Low-energy diets differing in fibre, red meat and coffee intake equally improve insulin sensitivity in type 2 diabetes: a randomised feasibility trial.

    Science.gov (United States)

    Nowotny, Bettina; Zahiragic, Lejla; Bierwagen, Alessandra; Kabisch, Stefan; Groener, Jan B; Nowotny, Peter J; Fleitmann, Ann Kristin; Herder, Christian; Pacini, Giovanni; Erlund, Iris; Landberg, Rikard; Haering, Hans-Ulrich; Pfeiffer, Andreas F H; Nawroth, Peter P; Roden, Michael

    2015-02-01

    Epidemiological studies have found that a diet high in fibre and coffee, but low in red meat, reduces the risk for type 2 diabetes. We tested the hypothesis that these nutritional modifications differentially improve whole-body insulin sensitivity (primary outcome) and secretion. Inclusion criteria were: age 18-69 years, BMI ≥ 30 kg/m(2), type 2 diabetes treated with diet, metformin or acarbose and known disease duration of ≤ 5 years. Exclusion criteria were: HbA1c >75 mmol/mol (9.0%), type 1 or secondary diabetes types and acute or chronic diseases including cancer. Patients taking any medication affecting the immune system or insulin sensitivity, other than metformin, were also excluded. Of 59 patients (randomised using randomisation blocks [four or six patients] with consecutive numbers), 37 (54% female) obese type 2 diabetic patients completed this controlled parallel-group 8-week low-energy dietary intervention. The participants consumed either a diet high in cereal fibre (whole grain wheat/rye: 30-50 g/day) and coffee (≥ 5 cups/day), and free of red meat (L-RISK, n = 17) or a diet low in fibre (≤ 10 g/day), coffee-free and high in red meat (≥ 150 g/day) diet (H-RISK, n = 20). Insulin sensitivity and secretion were assessed by hyperinsulinaemic-euglycaemic clamp and intravenous glucose tolerance tests with isotope dilution. Whole-body and organ fat contents were measured by magnetic resonance imaging and spectroscopy. Whole-body insulin sensitivity increased in both groups (mean [95% CI]) (H-RISK vs L-RISK: 0.8 [0.2, 1.4] vs 1.0 [0.4, 1.7]mg kg(-1) min(-1), p = 0.59), while body weight decreased (-4.8% [-6.1%, -3.5%] vs -4.6% [-6.0%, -3.3%], respectively). Hepatic insulin sensitivity remained unchanged, whereas hepatocellular lipid content fell in both groups (-7.0% [-9.6%, -4.5%] vs -6.7% [-9.5%, -3.9%]). Subcutaneous fat mass (-1,553 [-2,767, -340] cm(3) vs -751 [-2,047; 546] cm(3), respectively) visceral fat mass (-206 [-783, 371] cm(3) vs -241

  3. 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

  4. α-Glucosidase Inhibitory and Antioxidant Activity of Magnolia Officinalis%凹叶厚朴抑制α-糖苷酶与抗氧化活性研究

    Institute of Scientific and Technical Information of China (English)

    曹乃锋; 康文艺

    2012-01-01

    The α-glucosidase inhibitory activities of Magnolia Officinalis from Guizhou and Henan province was assayed by the method of 96-microplates for the first time,and its antioxidant activity was determined by the method of DPPH, ABTS and FRAP. Ethyl acetate (IC50 = 7.22 μg/mL) and methanolic extracts (IC50 =36.59 μg/mL) of M. officinalis from Guizhou,and the petroleum ether (IC50 = 107. 04 μg/mL) and ethyl acetate extracts (IC30 = 17. 17 μg/mL) of M. officinalis from Henan were higher than that of Acarbose (IC30 = 1081.27 μg/mL) as positive control. Ethyl acetate extracts of M. officinalis from Guizhou had the highest ABTS free radical scavenging activity (IC50 = 8. 81 μg/mL) , which was higher than that of BHT(IC50 = 11.94 μg/mL)as positive control,and followed by ethyl acetate extracts of Magnolia Officinalis from Henan (IC50 =12.73 μg/mL). The results indicated that ethyl acetate extracts of M. officinalis from Guizhou showed the strongest activity of a-glucosidase inhibitory activity and antioxidant activity.%首次采用96微孔板法检测贵州和河南产凹叶厚朴抑制α-葡萄糖苷酶活性;并采用DPPH、ABTS和FRAP三种方法测定其抗氧化活性.贵州产凹叶厚朴乙酸乙酯(IC50 =7.22 μg,/mL)和正丁醇提取部位(IC50=36.59 μg/mL),河南产凹叶厚朴石油醚(IC50=107.04 μg/mL)和乙酸乙酯提取部位(IC50=17.17μg/mL),它们的活性都远高于于阳性对照Acarhose( IC50=1081.27 μg/mL).贵州产凹叶厚朴乙酸乙酯提取部位清除ABTS自由基的能力最强(IC50=8.81 μg/mL),强于阳性对照BHT(IC50=11.94 μg/mL);其次为河南产凹叶厚朴乙酸乙酯提取部位(IC50=12.73 μg/mL).研究结果表明,贵州产凹叶厚朴乙酸乙酯提取部位抑制α-葡萄糖苷酶和抗氧化活性最好.

  5. Clinical Observation of Shenqi Jiangtang Granule in the Adjuvant Treatment of Type 2 Diabetes Knee Arthri-tis%参芪降糖颗粒辅助治疗2型糖尿病性膝关节炎的临床观察

    Institute of Scientific and Technical Information of China (English)

    张鸽; 燕丽君; 刘铜龙; 黄炜; 李春君; 于德民

    2016-01-01

    OBJECTIVE:To observe the efficacy and safety of Shenqi jiangtang granule in the adjuvant treatment of type 2 dia-betes knee arthritis. METHODS:62 patients with type 2 diabetes knee arthritis were randomly divided into control group(31 cas-es) and observation group (31 cases). Control group received hypoglycemic and basic treatment for arthritis,including diet con-trol,exercise therapy and health education,as well as 0.25 g Metformin hydrochloride tablet with a meal,3 times a day + 50 mg Acarbose tablet with a meal,3 times a day,chewing;patients with arthritis pain 100 mg Aspirin enteric-coated tablet after a meal, once a day (chewing or breaking apart was prohibited). Observation group additionally received 3 g Shenqi jiangtang granule half an hour before a meal with 50 ml warm water,3 times a day. The treatment course for both groups was 6 months. Clinical effica-cy,and fasting plasma glucose(FPG),2 h postprandial blood glucose(2 h PG),glycated hemoglobin(HbA1c),interleukin-1β(IL-1β),IL-6 before and after treatment,and the incidence of adverse reactions in 2 groups were observed. RESULTS:The total effective rate in observation group was significantly higher than control group,the difference was statistically significant(P0.05). After treatment,FPG,2 h PG,HbA1c,IL-1β and IL-6 in 2 groups were significantly lower than before,and observation group was lower than control group,the differences were statistically significant(P0.05). CONCLUSIONS:Based on conventional treatment,Shenqi jiangtang granule shows obvious efficacy in the adjuvant treatment of type 2 diabetes knee arthritis.,it can reduce blood glucose and inflammation cy-tokine levels,mild symptoms of adverse reactions.%目的:观察参芪降糖颗粒辅助治疗2型糖尿病性膝关节炎的疗效和安全性。方法:62例2型糖尿病性膝关节炎患者随机分为对照组(31例)和观察组(31例)。对照组患者均给予降糖、针对关节炎的基础治疗,包括饮食控制、

  6. Analysis of hypoglycemic drugs of patients with type 2 diabetes in Qingxin Distric in Qingyuan city%清远市清新区2型糖尿病患者降糖药物的用药分析

    Institute of Scientific and Technical Information of China (English)

    罗金娥; 余德生; 姜学辉

    2016-01-01

    Objective:To provide reference for clinical rational drug use in the local, we investigate hypoglycemic drugs used in type 2 diabetic patients in Qingxin Distric in Qingyuan city in Guangdong Province. Methods:2380 cases of patients with type 2 diabetes in Qingxin Distric in Qingyuan city in Guangdong Province as the research object, questionnaire survey, and analyzed the use of antidiabetic drugs. Results:A higher proportion of drug use is: biguanides, using the rate of 89.97%. Secondly, a sulfonylurea, alpha glucosidase inhibitor, use rates were 71.97% and 55.97%. High frequency of use of drugs, metformin, acarbose, frequency of use are:79.03%, 57.02%. Double guanidine kind+sulfonylurea combination rate:71.47%, is the proportion of previous use of drug combination in the largest category. Followed by : biguanides + sulfonylurea + alpha glucosidase inhibitor drugs combination accounted for 50.63%. Fasting blood glucose (FBG) and lower levels of 2hPBG, were of relatively short duration, hypoglycemic drug varieties less. While the FBG and 2hPBG levels were higher in the patients, the disease is relatively longer, taking more hypoglycemic drugs. A short course of patients, complications and hypoglycemic drug relatively few species. While patients with longer disease duration, complications and use of hypoglycemic drugs more varieties. Conclusion:Hypoglycemic medication is more scientific and reasonable, accord with the clinical treatment of specification, type 2 diabetic patients in Qingxin Distric in Qingyuan city in Guangdong Province. Part of the control blood sugar of patients is not ideal by hypoglycemic drugs, can be used insulin treatment.%目的:调查分析广东省清远市清新区2型糖尿病患者的降糖药物使用情况,为临床合理用药提供参考。方法:选择广东省清远市清新区2380例2型糖尿病患者作为研究对象,发放调查问卷进行调查,并对降糖药物使用情况进行总结分析。结果:药物使

  7. [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

  8. Cost-effectiveness analysis of type 2 diabetes mellitus with oral hypoglycemic drugs in Shunde district%顺德地区2型糖尿病患者口服降糖药的成本-效果分析

    Institute of Scientific and Technical Information of China (English)

    汪周艳; 张丽萍

    2011-01-01

    Objechve: To finish the pharmacoeconomics evaluation on oral hypoglycemic agents in patients with type 2 diabetes meUitus, with reasonably selecting high titer oral hypoglycemic agents to control blood glucose level, for the sake of having a safe, effective, reasonable and economic effect to relief Lhe burdens of patients and society.Methods: The study group and control groups were set up to be researched.400 patients who were diagnosed type 2 diabetes according to the diabetes diagnostic criteria made by American Diabetes Society in 2003 were selected to participate in experiment.They were separated to 1 group as study group (group A) and 3 control groups as control group B.C, D with each goup 100 persons Group A was treated by Gliciazide combined with Metformin (voglibose was used instead of Gibenclami in patients who had significant hypoglycemic reaction).Group B was treated by Rosiglitazone combined with Voglibose.Croup C was treated by Acarbose combined with Repaglinide.Group D was treated by Glimepinde combined with Voglibose.The blood glucose level of patients in each group was regulady monitored.When the experiment ended, the Pharmacoeconomics Evaluation was carried on.Results: It was found that drug cost per day of group A and.total drug cost were obviously lower than that of group B, C, D (P<0.001).But the measuring of FBG, 2hPBG and Glycosylated hemoglobin, in the 4 groups was almost the same and the Hypoglycemia average month incidence and the incidence of advrerse reaction of experiment group by diabetes education didn't have significant difference than that of observation group (P>0.05).Conclusion: The treatment method of group A is the most safe and effective.It was also superior in economy than other three groups%目的:通过对2型糖尿病患者口服降糖药物的药物经济学评价,选择成本效果比最小的给药方案,达到安全、有效、合理、经济用药的效果,减轻患者和社会的负担.方法:在根据2003

  9. The effect of sitagliptin on type 2 diabetes mellitus complicated with early diabetic Kidney disease(DKD)patients%西格列汀对初诊2型糖尿病并发早期糖尿病肾病患者的影响

    Institute of Scientific and Technical Information of China (English)

    郝清顺; 刘玉苓; 费大东

    2015-01-01

    Objective:To observe the clinical efficacy of sitagliptin for newly diagnosed type 2 diabetic complicated with early diabetic kidney disease( DKD)patients. Methods:The newly diagnosed 64 cases T2DM patients complicated with early DKD were selecred and randomly divided into the 30 cases in the control group,and 34 cases in experimental group, with the control group given acarbose in combination with metformin treatment,and experimental group given sitagliptin in combination with metformin treatment and the treatment was for six months,and observation of fasting blood glucose (FBG),glycosylated hemoglobin(HbA1c),triglycerides(TG),total cholesterol(TC),low density lipoprotein choles-terol( LDL-C ), systolic blood pressure ( SBP ), diastolic blood pressure ( DBP ), urine trace albumin/creatinine ( UACR),urine alpha 1-microglobulin( MG),and the changes of glomerular filtration rate( eGFR)were made before and after treatment. Results:Compared with those before the treatment,there was a significant reduction of FBG,HbA1c in the control group after treatment,the difference was statistically significant(P﹤0. 01),TG,TC,LDL-C also fell,and there are statistically significant(P﹤0. 05). BMI and SBP were down after experimental treatment,compared with those before treatment(P﹤ 0. 05),while FBG,HbA1c,TG,TC,LDL-C,UACR were down significantly,compared with those be-fore treatment and difference was statistically significant(P﹤0. 01). TC and UACR had significant difference between the two groups after treating and hsd statistical significance(P﹤ 0. 05). Conclusion:Sitagliptin not only effectively control blood sugar of early diabetic nephropathy,but also can reduce urine protein leakage,which delays the development of early diabetic nephropathy.%目的:观察西格列汀对初诊2型糖尿病( T2DM)并发早期糖尿病肾病( DKD)患者的临床疗效。方法选取初诊T2DM并发早期DKD患者64例,随机分为对照组30例,实验组34例,对照组

  10. 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

  11. 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.

  12. 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).

  13. 降糖通络汤对2型糖尿病患者血糖波动的影响%Hypoglycemic Effect of Jiangtang Tongluo Tang on Blood Glucose Fluctuations of Type 2 Diabetes

    Institute of Scientific and Technical Information of China (English)

    刘莉娟

    2016-01-01

    .93)和(-3.31±0.24)(P<0.01).结论:降糖通络汤能降低T2DM患者2hPG和HbAlc水平,调节日内血糖波动、稳定血糖,其作用机制可能是通过改善β细胞分泌功能,从而提高机体胰岛素敏感性.%Objective:To observe the hypoglycemic effect of Jiangtang Tongluo Tang on blood glucose fluctuations of type 2 diabetes (T2 DM).Methods:90 patients with T2 DM were randomly divided into control group and observation group,with 45 cases in each group.The control group was treated with acarbose tablets and recombinant glargine insulin injections to control blood sugar.Based on that,the observation group was treated with hypoglycemic Jiangtang Tongluo decoction.The treatment lasted for 12 weeks.Glucose monitoring system was applied to monitor the standard deviation (SDBG)of blood glucose levels,mean amplitude of glycemic excursions (MAGE),largest amplitude of glycemic excursions (LAGE),absolute means of daily differences (MODD),mean of postprandial glucose excursion (MPPGE),fasting blood-glucose (FBG),2 hour postprandial blood glucose (2h PBG),glycosylated hemoglobin (HbAlc),fasting insulin (FINS),homeostasis model assessment (HOMA-IR),homa beta cell function index (HOMA-β) and insulin sensitive index (ISI) before and after treatment.Results:The SDBG,MAGE,LAGE,MODD and MPPGE level after treatment was (1.07 ±0.53) mmol · L-1,(1.13 ±0.47) mmol · L-1,(4.69 ±0.75) mmol · L-1,(1.51 ±0.23) mmol · L-1 and (3.05 ± 0.63) mmol · L-1 respectively,each being significantly lower than that of the control group of (1.62 ± 0.55) mmol · L-1,(2.15 ±0.43) mmol · L-1,(5.53 ±0.81) mmol · L-1,(1.83 ±0.21) mmol · L-1 and (3.87 ±0.75) mmol · L-1(P<0.01).After treatment,the 2hPG,HbA1c and FINS level of the observation group was (8.59 ± 1.28) mmol · L-1,(6.83 ±0.76)% and (7.06 ± 0.88) mU · L-1 respectively,each being significantly lower than that of the control group of (9.16 ± 1.77) mmol ·L-1,(7.68 ± 0.79) % and (9.75 ± 0.93) mU · L-1 (P