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Sample records for oral anti-diabetic agents

  1. Use of oral anti-diabetic agents in pregnancy: A pragmatic approach

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    Bharti Kalra

    2015-01-01

    Full Text Available Insulin is the gold standard for treatment of hyperglycemia during pregnancy, when lifestyle measures do not maintain glycemic control during pregnancy. However, recent studies have suggested that certain oral hypoglycemic agents (metformin and glyburide may be safe and be acceptable alternatives. There are no serious safety concerns with metformin, despite it crossing the placenta. Neonatal outcomes are also comparable, with benefit of reductions in neonatal hypoglycemia, maternal hypoglycemia and weight gain, and improved treatment satisfaction. Glibenclamide is more effective in lowering blood glucose in women with gestational diabetes, and with a lower treatment failure rate than metformin. Although generally well-tolerated, some studies have reported higher rates of pre-eclampsia, neonatal jaundice, longer stay in the neonatal care unit, macrosomia, and neonatal hypoglycaemia. There is also paucity of long-term follow-up data on children exposed to oral agents in utero. This review aims to provide an evidence-based approach, concordant with basic and clinical pharmacological knowledge, which will help medical practitioners use oral anti-diabetic agents in a rational and pragmatic manner. Pubmed search was made using Medical Subject Headings (MESH terms "Diabetes" and "Pregnancy" and "Glyburide"; "Diabetes" and "Pregnancy" and "Metformin". Limits were randomized controlled trials (RCTs and meta-analysis. The expert reviews on the topic were also used for discussion. Additional information (studies/review pertaining to discussion under sub-headings like safety during breastfeeding; placental transport; long-term safety data were searched (pubmed/cross-references/expert reviews.

  2. Harnessing the potential clinical use of medicinal plants as anti-diabetic agents

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    Campbell-Tofte JI

    2012-08-01

    Full Text Available Joan IA Campbell-Tofte,1 Per Mølgaard,2 Kaj Winther11Department of Clinical Biochemistry, Frederiksberg University Hospital, Frederiksberg, Denmark; 2Department of Medicinal Chemistry, Faculty of Pharmaceutical Sciences, University of Copenhagen, Copenhagen, DenmarkAbstract: Diabetes is a metabolic disorder arising from complex interactions between multiple genetic and/or environmental factors. The characteristic high blood sugar levels result from either lack of the hormone insulin (type 1 diabetes, T1D, or because body tissues do not respond to the hormone (type 2 diabetes, T2D. T1D patients currently need exogenous insulin for life, while for T2D patients who do not respond to diet and exercise regimes, oral anti-diabetic drugs (OADs and sometimes insulin are administered to help keep their blood glucose as normal as possible. As neither the administration of insulin nor OADs is curative, many patients develop tissue degenerative processes that result in life-threatening diabetes comorbidities. Several surveys of medicinal plants used as anti-diabetic agents amongst different peoples have been published. Some of this interest is driven by the ongoing diabetes pandemic coupled with the inadequacies associated with the current state of-the-art care and management of the syndrome. However, there is a huge cleft between traditional medicine and modern (Western medicine, with the latter understandably demanding meaningful and scientific validation of anecdotal evidence for acceptance of the former. The main problems for clinical evaluation of medicinal plants with promising anti-diabetic properties reside both with the complexity of components of the plant materials and with the lack of full understanding of the diabetes disease etiology. This review is therefore focused on why research activities involving an integration of Systems Biology-based technologies of pharmacogenomics, metabolomics, and bioinformatics with standard clinical data

  3. Synthesis and biological activity of trans-tiliroside derivatives as potent anti-diabetic agents.

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    Zhu, Yujin; Zhang, Yanjun; Liu, Yi; Chu, Hongwan; Duan, Hongquan

    2010-12-10

    A set of novel trans-tiliroside derivatives were synthesized. The structures of the derivatives were identified by their IR, 1H-NMR, and MS spectra analysis. Their anti-diabetic activities were evaluated on the insulin resistant (IR) HepG2 cell model. As a result, compounds 7a, 7c, 7h, and trans-tiliroside exhibited significant glucose consumption-enhancing effects in IR-HepG2 cells compared with the positive control (metformin). This research provides useful clues for further design and discovery of anti-diabetic agents.

  4. Synthesis and Biological Activity of trans-Tiliroside Derivatives as Potent Anti-Diabetic Agents

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    Yi Liu

    2010-12-01

    Full Text Available A set of novel trans-tiliroside derivatives were synthesized. The structures of the derivatives were identified by their IR, 1H-NMR, and MS spectra analysis. Their anti-diabetic activities were evaluated on the insulin resistant (IR HepG2 cell model. As a result, compounds 7a, 7c, 7h, and trans-tiliroside exhibited significant glucose consumption-enhancing effects in IR-HepG2 cells compared with the positive control (metformin. This research provides useful clues for further design and discovery of anti-diabetic agents.

  5. Synthesis and Biological Activity of Isoflavone Derivatives from Chickpea as Potent Anti-Diabetic Agents

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    Pengshou Li

    2015-09-01

    Full Text Available A set of novel isoflavone derivatives from chickpea were synthesized. The structures of derivatives were identified by proton nuclear magnetic resonance (1H-NMR, carbon-13 (13C-NMR and mass spectrometry (MS spectral analyses. Their anti-diabetic activities were evaluated using an insulin-resistant (IR HepG2 cell model. Additionally, the structure-activity relationships of these derivatives were briefly discussed. Compounds 1c, 2h, 3b, and 5 and genistein exhibited significant glucose consumption-enhancing effects in IR-HepG2 cells. In addition, the combinations of genistein, 2h, and 3b (combination 6 and of 3b, genistein, and 1c (combination 10 exhibited better anti-diabetic activity than the individual compounds. At the same dosage, there was no difference in effect between the combination 10 and the positive control (p > 0.05. Aditionally, we found the differences between the combination 10 and combination 6 for the protective effect of HUVEC (human umbilical vein endothelial cells under high glucose concentration. The protective effects of combination 10 was stronger than combination 6, which suggested that combination 10 may have a better hypoglycemic activity in future studies. This study provides useful clues for the further design and discovery of anti-diabetic agents.

  6. Adverse drug reaction monitoring of newer oral anti diabetic drugs – a pharmacovigilance perspective

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    Ankita Bhattacharjee

    2016-04-01

    Full Text Available Objective: To monitor and evaluate adverse drug reactions (ADRs of newer oral anti-diabetic drugs in type II diabetics by spontaneous/solicited ADR monitoring.Material and methods: Two hundred and thirty two diabetic patients on newer oral antidiabetic drugs were evaluated prospectively in a cross-sectional study over a period of eighteen months. All patients were followed up for ADRs which were evaluated for incidence, frequency, severity and causality. ADR severity was graded according to University of Virginia Health System Adverse Drug Reaction Reporting program criteria and causality assessment was done using WHO-UMC scale.Results: 190 out of 232 patients (42 patients lost to follow up were evaluated. ADRs were observed in 34 cases (17.9%. Most common ADRs were gastrointestinal (44.2% followed by musculoskeletal (17.6%, metabolic (14.7%, infections (5.9% and others (17.6%. The maximal frequency of ADRs was seen with sitagliptin (6.4% followed by vildagliptin(3.8%, saxagliptin(2.7%, saroglitazar(2.1%, linagliptin(1.6%, canagliflozin(1.6%. 25(73.5%, 8(23.5% and 1(3% ADRs were mild, moderate and severe respectively. 24(70% ADRs were classified as possible, 9(27% probable and 1(3% unlikely on causality assessment. Conclusion: Newer oral antidiabetic drugs like gliptins and SGLT-2 inhibitors have potential to cause ADRs. Gastro-intestinal, musculoskeletal, metabolic were most common ADRs. Active pharmacovigilance should be carried out for risk identification and management. 

  7. Comparative evaluation of effects of combined oral anti-diabetic drugs (sulfonylurea plus pioglitazone and sulfonylurea plus metformin over lipid parameters in type 2 diabetic patients

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    Sukanta Sen

    2013-06-01

    Full Text Available Background: Type 2 diabetes is associated with significant cardiovascular morbidity and mortality. Dyslipidemia, which affects almost 50% of patients with type 2 diabetes, is a cardiovascular risk factor characterized by elevated triglyceride levels, low high-density lipoprotein (HDL cholesterol levels, and a preponderance of small, dense, low-density lipoprotein (LDL particles. In addition to their glucose-lowering properties, oral anti-diabetic agents may have effects on lipid levels, especially triglycerides (TGs, HDL-C, LDL-C and total cholesterol levels. Methods: A prospective, open-labeled, randomized, parallel-group study was carried out in sizable number of patients (n=40 of established type 2 diabetes on combined oral anti-diabetic drugs, to investigate the effects of combined oral anti-diabetic on lipid parameters who was not receiving any hypolipidemic agent in addition. Results: Statistically significant mean reduction of triglycerides (TGs of 25.1mg/dl (a 15.30% reduction from baseline value and by 13.5 mg/dl (a 8.94% reduction from baseline value in the SU (sulfonylurea plus PIO (pioglitazone and SU plus MET (metformin group respectively. Present study also shows improvement in HDL cholesterol with SU plus PIO group by 13.18% which is almost twice that observed in SU plus MET group (8.06%. Present study also shows increase in LDL cholesterol with SU plus PIO group by 2.10%, is just opposite to SU plus MET group (4.92 % decrease. With SU plus PIO group, a statistically significant mean reduction of total cholesterol (TC of 8.33mg/dl (5.14 % decrease and by 7.62 mg/dl (4.28% decrease in the SU plus MET group. Conclusions: Pioglitazone, a thiazolidinedione, has been shown to improve the lipid profile in patients with type 2 diabetes by increasing HDL-C levels and by decreasing triglyceride and total cholesterol levels in monotherapy or combination regimens with sulfonylurea. Metformin also has been shown to reduce LDL-C, TC, and TG

  8. Synthesis, solubility, plasma stability, and pharmacological evaluation of novel sulfonylhydrazones designed as anti-diabetic agents

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    Zapata-Sudo G

    2016-09-01

    Full Text Available Gisele Zapata-Sudo,1,2 Isabelle Karine da Costa Nunes,2 Josenildo Segundo Chaves Araujo,1,2 Jaqueline Soares da Silva,2 Margarete Manhães Trachez,2,3 Tiago Fernandes da Silva,1 Filipe P da Costa,2 Roberto Takashi Sudo,1,2 Eliezer J Barreiro,1,2 Lídia Moreira Lima1,2 1National Institute of Science and Technology on Drugs and Medicines, Federal University of Rio de Janeiro, Laboratory of Evaluation and Synthesis of Bioactive Compounds, Center of Health Sciences, Rio de Janeiro, Brazil; 2Program of Research in Drug Development, Institute of Biomedical Sciences, Federal University of Rio de Janeiro, Rio de Janeiro, Brazil; 3Department of Anesthesiology, Fluminense Federal University, Rio de Janeiro, Brazil Abstract: Neuropathy is a serious complication of diabetes that has a significant socioeconomic impact, since it frequently demands high levels of health care consumption and compromises labor productivity. Recently, LASSBio-1471 (3 was demonstrated to improve oral glucose tolerance, reduce blood glucose levels, and display an anti-neuropathy effect in a murine streptozotocin-induced diabetes model. In the present work, we describe the design, synthesis, solubility, plasma stability, and pharmacological evaluation of novel sulfonylhydrazone derivatives (referred to herein as compounds 4–9, which were designed by molecular modification based on the structure of the prototype LASSBio-1471 (3. Among the compounds tested, better plasma stability was observed with 4, 5, and 9 in comparison to compounds 6, 7, and 8. LASSBio-1773 (7, promoted not only hypoglycemic activity but also the reduction of thermal hyperalgesia and mechanical allodynia in a murine model of streptozotocin-induced diabetic neuropathic pain. Keywords: diabetes, sulfonylhydrazone, hypoglycemic activity, druglikeness, plasma stability, metabolite

  9. Adherence to oral anti-diabetic drugs among patients attending a Ghanaian teaching hospital

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    Bruce SP

    2015-03-01

    Full Text Available Background: The burden of diabetes mellitus, especially Type-2, continues to increase across the world. Medication adherence is considered an integral component in its management. Poor glycemic controls due to medication nonadherence accelerates the development of long-term complications which consequently leads to increased hospitalization and mortality. Objective: This study examined the level of adherence to oral antidiabetic drugs among patients who visited the teaching hospital and explored the probable contributory factors to non-adherence. Methods: A cross-sectional descriptive study using systematic sampling to collect quantitative data was undertaken. Questionnaires were administered to out-patients of the medical department of a teaching hospital in Ghana. Logistic regression was performed with statistical significance determined at p<0.05. Results: A total of 200 diabetic patients participated in the study. Using the Morisky Medication Adherence scale, the level of adherence determined was 38.5%. There were significant correlations between level of adherence and educational level [(OR=1.508; (CI 0.805- 2.825, P=0.019, and mode of payment [(OR=1.631; (CI 0.997- 2.669, P=0.05. Conclusion: Adherence in diabetic patients was low among respondents and this can be improved through education, counseling and reinforcement of self-care. There were several possible factors that contributed to the low adherence rate which could benefit from further studies.

  10. Reactivity-activity relationships of oral anti-diabetic vanadium complexes in gastrointestinal media: an X-ray absorption spectroscopic study.

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    Levina, Aviva; McLeod, Andrew I; Kremer, Lauren E; Aitken, Jade B; Glover, Christopher J; Johannessen, Bernt; Lay, Peter A

    2014-10-01

    The reactions of oral V(V/IV) anti-diabetic drugs within the gastrointestinal environment (particularly in the presence of food) are a crucial factor that affects their biological activities, but to date these have been poorly understood. In order to build up reactivity-activity relationships, the first detailed study of the reactivities of typical V-based anti-diabetics, Na3V(V)O4 (A), [V(IV)O(OH2)5](SO4) (B), [V(IV)O(ma)2] (C, ma = maltolato(-)) and (NH4)[V(V)(O)2(dipic)] (D, dipic = pyridine-2,5-dicarboxylato(2-)) with simulated gastrointestinal (GI) media in the presence or absence of food components has been performed by the use of XANES (X-ray absorption near edge structure) spectroscopy. Changes in speciation under conditions that simulate interactions in the GI tract have been discerned using correlations of XANES parameters that were based on a library of model V(V), V(IV), and V(III) complexes for preliminary assessment of the oxidation states and coordination numbers. More detailed speciation analyses were performed using multiple linear regression fits of XANES from the model complexes to XANES obtained from the reaction products from interactions with the GI media. Compounds B and D were relatively stable in the gastric environment (pH ∼ 2) in the absence of food, while C was mostly dissociated, and A was converted to [V10O28](6-). Sequential gastric and intestinal digestion in the absence of food converted A, B and D to poorly absorbed tetrahedral vanadates, while C formed five- or six-coordinate V(V) species where the maltolato ligands were likely to be partially retained. XANES obtained from gastric digestion of A-D in the presence of typical food components converged to that of a mixture of V(IV)-aqua, V(IV)-amino acid and V(III)-aqua complexes. Subsequent intestinal digestion led predominantly to V(IV) complexes that were assigned as citrato or complexes with 2-hydroxyacidato donor groups from other organic compounds, including certain

  11. The Recent Progress in Oral Anti-diabetic Drug Research and Development%口服抗糖尿病药物研发新进展

    Institute of Scientific and Technical Information of China (English)

    穆曼娜

    2011-01-01

    The study of oral anti - diabetic drug ( OAD ) is continuously progressing in recent years. Thiazolidinediones, glucagon-like peptide-1 receptor activator, dipeptidyl peptidase Ⅳ inhibitors and amylin analogs are already in the market; Glucokinase activator, vanadium complex compounds and bioactive chromium are in study. Besides,the formulations of the existing drugs are also in constant improvement. Gastrointestinal therapeutic system ( GITS ) tablets, sustained - release tablets and complex compounds are emerging gradually. These progresses provide more ways to treat diabetes for better effects.%口服抗糖尿病药物的研发不断取得成功,已经上市的有噻唑烷二酮类、胰高糖素样肽1受体激动剂、二肽基肽酶Ⅳ抑制剂和胰淀素类似物等,正在进行研究的有葡萄糖激酶激活剂、钒复合物和生物活性铬等.原有的药物也在剂型上不断改进,控释剂、缓释剂和复方型逐渐出现.这些研究的成功为糖尿病的治疗提供更多的手段,以期达到更好的治疗效果.

  12. Novel exenatide analogs with peptidic albumin binding domains: potent anti-diabetic agents with extended duration of action.

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    Odile E Levy

    Full Text Available The design, synthesis and pharmacology of novel long-acting exenatide analogs for the treatment of metabolic diseases are described. These molecules display enhanced pharmacokinetic profile and potent glucoregulatory and weight lowering actions compared to native exenatide. [Leu(14]exenatide-ABD is an 88 residue peptide amide incorporating an Albumin Binding Domain (ABD scaffold. [Leu(14]exenatide-ABP is a 53 residue peptide incorporating a short Albumin Binding Peptide (ABP. [Leu(14]exenatide-ABD and [Leu(14]exenatide-ABP exhibited nanomolar functional GLP-1 receptor potency and were metabolically stable in vitro in human plasma and in a pancreatic digestive enzyme mixture. Both molecules displayed picomolar and nanomolar binding association with albumin across multiple species and circulating half lives of 16 and 11 hours, respectively, post a single IV dose in rats. Unlike exenatide, both molecules elicited robust glucose lowering when injected 1 day prior to an oral glucose tolerance test, indicative of their extended duration of action. [Leu(14]exenatide-ABD was compared to exenatide in a Lep (ob/ob mouse model of diabetes. Twice-weekly subcutaneously dosed [Leu(14]exenatide-ABD displayed superior glucose lowering and weight loss in diabetic mice when compared to continuously infused exenatide at the same total weekly dose. A single oral administration of each molecule via an enteric coated capsule to cynomolgus monkeys showed superior pharmacokinetics for [Leu(14]exenatide-ABD as compared to [Leu(14]exenatide-ABP with detectable exposure longer than 14 days. These studies support the potential use of these novel long acting exenatide analogs with different routes of administration for the treatment of type 2 diabetes.

  13. Sodium-glucose co-transporter 2 (SGLT2 inhibitors: a growing class of anti-diabetic agents

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    Eva M Vivian

    2014-12-01

    Full Text Available Although several treatment options are available to reduce hyperglycemia, only about half of individuals with diagnosed diabetes mellitus (DM achieve recommended glycemic targets. New agents that reduce blood glucose concentrations by novel mechanisms and have acceptable safety profiles are needed to improve glycemic control and reduce the complications associated with type 2 diabetes mellitus (T2DM. The renal sodium-glucose co-transporter 2 (SGLT2 is responsible for reabsorption of most of the glucose filtered by the kidney. Inhibitors of SGLT2 lower blood glucose independent of the secretion and action of insulin by inhibiting renal reabsorption of glucose, thereby promoting the increased urinary excretion of excess glucose. Canagliflozin, dapagliflozin, and empagliflozin are SGLT2 inhibitors approved as treatments for T2DM in the United States, Europe, and other countries. Canagliflozin, dapagliflozin, and empagliflozin increase renal excretion of glucose and improve glycemic parameters in patients with T2DM when used as monotherapy or in combination with other antihyperglycemic agents. Treatment with SGLT2 inhibitors is associated with weight reduction, lowered blood pressure, and a low intrinsic propensity to cause hypoglycemia. Overall, canagliflozin, dapagliflozin, and empagliflozin are well tolerated. Cases of genital infections and, in some studies, urinary tract infections have been more frequent in canagliflozin-, dapagliflozin-, and empagliflozin-treated patients compared with those receiving placebo. Evidence from clinical trials suggests that SGLT2 inhibitors are a promising new treatment option for T2DM.

  14. Re-Training of Type 2 Diabetic Patients for Better Adherence to Diabetes Care Plan in Oral Anti-Diabetics and Plus Insulin Treatment Groups

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    Soner Cander

    2015-06-01

    Full Text Available Purpose: This prospective observational single-centre study was designed to evaluate the effect of patient re-training for better adherence to regular self-monitoring of blood glucose (SMBG, standard diabetic diet and exercise program in ambulatory patients with type 2 diabetes mellitus (T2DM receiving oral anti-diabetic (OAD and OAD plus insulin treatments. Material and Method: In this study, we enrolled a total of 61 patients with T2DM in whom ongoing therapy with OAD (n=34 and OAD+insulin (n=27 failed to achieve adequate glycemic control. The patients were educated for lifestyle behavior, adherence to diet and exercise therapy, close monitoring with SMBG without change in their ongoing drugs and dosing. Changes in glycemic parameters, serum lipids and anthropometrics at the end of 3rd month were compared between the treatment groups. Results: During the course of the study, a significant decrease in the body weight and fat were observed in OAD (p<0.001 and p=0.002 and OAD+insulin groups (p=0.044 and p=0.008, respectively. A significant decrease in the HbA1c % (6.1%; 8.2% to 7.6% was observed in the overall population (p<0.001 as well as in OAD (p=0.011 and OAD+insulin (p=0.001 groups. A significant decrease was noted in the post-prandial capillary blood glucose levels in only OAD+insulin group. Discussion: Re-training approach with close follow-up and frequent SMBG seems to be important factors for the maintenance of achieved glycemic control. In our study, the effect of diabetes education on postprandial capillary blood glucose levels was more pronounced in OAD+insulin group. Turk Jem 2015; 19: 49-54

  15. A Hamster Model of Diet-Induced Obesity for Preclinical Evaluation of Anti-Obesity, Anti-Diabetic and Lipid Modulating Agents.

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    Louise S Dalbøge

    Full Text Available Unlike rats and mice, hamsters develop hypercholesterolemia, and hypertriglyceridemia when fed a cholesterol-rich diet. Because hyperlipidemia is a hallmark of human obesity, we aimed to develop and characterize a novel diet-induced obesity (DIO and hypercholesterolemia Golden Syrian hamster model.Hamsters fed a highly palatable fat- and sugar-rich diet (HPFS for 12 weeks showed significant body weight gain, body fat accumulation and impaired glucose tolerance. Cholesterol supplementation to the diet evoked additional hypercholesterolemia. Chronic treatment with the GLP-1 analogue, liraglutide (0.2 mg/kg, SC, BID, 27 days, normalized body weight and glucose tolerance, and lowered blood lipids in the DIO-hamster. The dipeptidyl peptidase-4 (DPP-4 inhibitor, linagliptin (3.0 mg/kg, PO, QD also improved glucose tolerance. Treatment with peptide YY3-36 (PYY3-36, 1.0 mg/kg/day or neuromedin U (NMU, 1.5 mg/kg/day, continuously infused via a subcutaneous osmotic minipump for 14 days, reduced body weight and energy intake and changed food preference from HPFS diet towards chow. Co-treatment with liraglutide and PYY3-36 evoked a pronounced synergistic decrease in body weight and food intake with no lower plateau established. Treatment with the cholesterol uptake inhibitor ezetimibe (10 mg/kg, PO, QD for 14 days lowered plasma total cholesterol with a more marked reduction of LDL levels, as compared to HDL, indicating additional sensitivity to cholesterol modulating drugs in the hyperlipidemic DIO-hamster. In conclusion, the features of combined obesity, impaired glucose tolerance and hypercholesterolemia in the DIO-hamster make this animal model useful for preclinical evaluation of novel anti-obesity, anti-diabetic and lipid modulating agents.

  16. Experimental strategy of animal trial for the approval of anti-diabetic agents prior to their use in pre-human clinical trials

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    Vivek K. Bajpai

    2016-03-01

    Full Text Available Although several naturally available drugs have been historically used for the treatment of diabetes mellitus throughout the world, few of them have been validated by scientific criteria. Before approval of any drug developed it should pass through animal trial prior to clinical human trial, which should followed by some standard ethical rules. Recently, a large diversity of animal models have been developed to better understand the pathogenesis of diabetes mellitus, and new drugs have been introduced in the market to treat this autoimmune disease. In the present article, we demonstrated some standard handling procedure of animal trial for the approval of anti-diabetic drug, which could be helpful for both academics and industrial scientific community to conduct the animal experiments. This research also contributes in the field of ethnopharmacology to design new strategies for the development of novel drugs to treat this serious condition of diabetes mellitus that constitutes a global public health.

  17. Oral hypoglycaemic agents in 118 diabetic pregnancies

    DEFF Research Database (Denmark)

    Hellmuth, E; Damm, P; Mølsted-Pedersen, L

    2000-01-01

    AIMS: To assess maternal and neonatal complications in pregnancies of diabetic women treated with oral hypoglycaemic agents during pregnancy. METHODS: A cohort study including all consecutively registered, orally treated pregnant diabetic patients set in a diabetic obstetrical service at a univer......AIMS: To assess maternal and neonatal complications in pregnancies of diabetic women treated with oral hypoglycaemic agents during pregnancy. METHODS: A cohort study including all consecutively registered, orally treated pregnant diabetic patients set in a diabetic obstetrical service...... compared to women treated with sulphonylurea or insulin (32 vs. 7 vs. 10%, P neonatal morbidity was observed between the orally treated and insulin-treated group; no cases of severe hypoglycaemia or jaundice were seen in the orally treated groups. However, in the group of women...

  18. Potential therapeutic applications of multifunctional host-defense peptides from frog skin as anti-cancer, anti-viral, immunomodulatory, and anti-diabetic agents.

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    Conlon, J Michael; Mechkarska, Milena; Lukic, Miodrag L; Flatt, Peter R

    2014-07-01

    Frog skin constitutes a rich source of peptides with a wide range of biological properties. These include host-defense peptides with cytotoxic activities against bacteria, fungi, protozoa, viruses, and mammalian cells. Several hundred such peptides from diverse species have been described. Although attention has been focused mainly on antimicrobial activity, the therapeutic potential of frog skin peptides as anti-infective agents remains to be realized and no compound based upon their structures has yet been adopted in clinical practice. Consequently, alternative applications are being explored. Certain naturally occurring frog skin peptides, and analogs with improved therapeutic properties, show selective cytotoxicity against tumor cells and viruses and so have potential for development into anti-cancer and anti-viral agents. Some peptides display complex cytokine-mediated immunomodulatory properties. Effects on the production of both pro-inflammatory and anti-inflammatory cytokines by peritoneal macrophages and peripheral blood mononuclear cells have been observed so that clinical applications as anti-inflammatory, immunosuppressive, and immunostimulatory agents are possible. Several frog skin peptides, first identified on the basis of antimicrobial activity, have been shown to stimulate insulin release both in vitro and in vivo and so show potential as incretin-based therapies for treatment of patients with Type 2 diabetes mellitus. This review assesses the therapeutic possibilities of peptides from frogs belonging to the Ascaphidae, Alytidae, Pipidae, Dicroglossidae, Leptodactylidae, Hylidae, and Ranidae families that complement their potential role as anti-infectives for use against multidrug-resistant microorganisms.

  19. Pharmacological investigations of the anti-diabetic effect of Cortex Moutan and its active component paeonol.

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    Lau, C H; Chan, C M; Chan, Y W; Lau, K M; Lau, T W; Lam, F C; Law, W T; Che, C T; Leung, P C; Fung, K P; Ho, Y Y; Lau, C B S

    2007-11-01

    Cortex Moutan (CM, root bark of Paeonia suffruticosa Andr.) is one of the common herbs found in anti-diabetic traditional Chinese medicine formulae. To study the potential anti-diabetic mechanisms of CM, four in vitro models (intestinal brush border membrane vesicles (BBMV), rat hepatoma cell line H4IIE, human skin fibroblasts cell line Hs68 and mouse adipocytes 3T3-L1) were used. CM showed significant in vitro anti-diabetic effects by inhibiting glucose uptake of BBMV and enhancing glucose uptake into Hs68 and 3T3-L1 cells. Using bioassay-guided fractionation, paeonol was confirmed to be one of the active constituents for inhibiting BBMV glucose uptake. With neonatal-streptozotocin diabetic rats, paeonol (200 and 400mg/kgbody wt.) was found to improve oral glucose tolerance in vivo. To the best of our knowledge, this is the first report on the anti-diabetic effect of paeonol.

  20. 21 CFR 872.6030 - Oral cavity abrasive polishing agent.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 8 2010-04-01 2010-04-01 false Oral cavity abrasive polishing agent. 872.6030... (CONTINUED) MEDICAL DEVICES DENTAL DEVICES Miscellaneous Devices § 872.6030 Oral cavity abrasive polishing agent. (a) Identification. An oral cavity abrasive polishing agent is a device in paste or powder...

  1. Monitoring anticoagulant therapy with new oral agents

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    Ramos-Esquivel, Allan

    2015-01-01

    Thromboembolic disease is a major leading cause of mortality and morbidity in industrialized countries. Currently, the management of these patients is challenging due to the availability of new drugs with proven efficacy and security compared to traditional oral vitamin K antagonists. These compounds are characterized by a predictable pharmacokinetic profile for which blood monitoring is not routinely needed. Nevertheless, some data have suggested inter-patient variability in the anticoagulant effect of these drugs, raising concerns about their effectiveness and safety. Although mass-spectrometry is the gold standard to determine drug plasma concentrations, this method is not widely available in every-day practice and some coagulation assays are commonly used to determine the anticoagulant effect of these drugs. The present review aims to summarize the current knowledge regarding the clinical question of how and when to monitor patients with new anticoagulant oral agents. PMID:26713281

  2. Oral anticancer agent medication adherence by outpatients.

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    Kimura, Michio; Usami, Eiseki; Iwai, Mina; Nakao, Toshiya; Yoshimura, Tomoaki; Mori, Hiromi; Sugiyama, Tadashi; Teramachi, Hitomi

    2014-11-01

    In the present study, medication adherence and factors affecting adherence were examined in patients taking oral anticancer agents. In June 2013, 172 outpatients who had been prescribed oral anticancer agents by Ogaki Municipal Hospital (Ogaki, Gifu, Japan) completed a questionnaire survey, with answers rated on a five-point Likert scale. The factors that affect medication adherence were evaluated using a customer satisfaction (CS) analysis. For patients with good and insufficient adherence to medication, the median ages were 66 years (range, 21-85 years) and 73 years (range, 30-90 years), respectively (P=0.0004), while the median dosing time was 131 days (range, 3-3,585 days) and 219 days (24-3,465 days), respectively (P=0.0447). In 36.0% (62 out of 172) of the cases, there was insufficient medication adherence; 64.5% of those cases (40 out of 62) showed good medication compliance (4-5 point rating score). However, these patients did not fully understand the effects or side-effects of the drugs, giving a score of three points or less. The percentage of patients with good medication compliance was 87.2% (150 out of 172). Through the CS analysis, three items, the interest in the drug, the desire to consult about the drug and the condition of the patient, were extracted as items for improvement. Overall, the medication compliance of the patients taking the oral anticancer agents was good, but the medication adherence was insufficient. To improve medication adherence, a better understanding of the effectiveness and necessity of drugs and their side-effects is required. In addition, the interest of patients in their medication should be encouraged and intervention should be tailored to the condition of the patient. These steps should lead to improved medication adherence.

  3. Anti diabetic effect of Momordica charantia (bitter melone on alloxan induced diabetic rabbits.

    Directory of Open Access Journals (Sweden)

    Yakaiah Vangoori, Mishra SS, Ambudas B, Ramesh P, Meghavani G, Deepika K, Prathibha A

    2013-02-01

    Full Text Available Objective: to investigate the anti diabetic effect of the bitter melon on Alloxan induced diabetes in experimental animals (rabbits. Materials and Methods: the alcohol extract of whole fruit was tested for its efficacy in Alloxan (150mg/kg induced diabetic rabbit. The diabetic rabbits were divided into 5groups. Group I (control received 2% gumacasia, groupie (positive control received standard drug Metformin (62.5mg+2%GA, group III, IV, V (T1 T2 T3 were treated orally with a daily dose of 0.5(gm 1gm, 1.5gm respectively for 35 days, for all diabetic rabbits after giving TEST,NC,PC preparations, the blood samples were collected and determined the blood glucose level 0,1,3,24hrs intervals. 0hr reading is before drug giving and remaining 3 readings after drugs giving. 24th her reading is considered as 0hr reading for the next day. Results: administration of alcohol of an extract of bitter melon produced a dose dependent decrease in blood glucose levels in Alloxan induced rabbits. There was a significant fall in blood sugar level in High dose (1.5GM/kg in comparison to low dose (0.5gm/kg and median dose (1gm/kg shown by LSD test. This is comparable to the effect of Metformin. Conclusion: the results of this study show that chronic oral administration of an extract of Momordica charantia fruit at an appropriate dosage may be good alternative anti diabetic agent.

  4. Marine Organisms with Anti-Diabetes Properties.

    Science.gov (United States)

    Lauritano, Chiara; Ianora, Adrianna

    2016-12-01

    Diabetes is a chronic degenerative metabolic disease with high morbidity and mortality rates caused by its complications. In recent years, there has been a growing interest in looking for new bioactive compounds to treat this disease, including metabolites of marine origin. Several aquatic organisms have been screened to evaluate their possible anti-diabetes activities, such as bacteria, microalgae, macroalgae, seagrasses, sponges, corals, sea anemones, fish, salmon skin, a shark fusion protein as well as fish and shellfish wastes. Both in vitro and in vivo screenings have been used to test anti-hyperglycemic and anti-diabetic activities of marine organisms. This review summarizes recent discoveries in anti-diabetes properties of several marine organisms as well as marine wastes, existing patents and possible future research directions in this field.

  5. Marine Organisms with Anti-Diabetes Properties

    Directory of Open Access Journals (Sweden)

    Chiara Lauritano

    2016-12-01

    Full Text Available Diabetes is a chronic degenerative metabolic disease with high morbidity and mortality rates caused by its complications. In recent years, there has been a growing interest in looking for new bioactive compounds to treat this disease, including metabolites of marine origin. Several aquatic organisms have been screened to evaluate their possible anti-diabetes activities, such as bacteria, microalgae, macroalgae, seagrasses, sponges, corals, sea anemones, fish, salmon skin, a shark fusion protein as well as fish and shellfish wastes. Both in vitro and in vivo screenings have been used to test anti-hyperglycemic and anti-diabetic activities of marine organisms. This review summarizes recent discoveries in anti-diabetes properties of several marine organisms as well as marine wastes, existing patents and possible future research directions in this field.

  6. Assessment and measurement of adherence to oral antineoplastic agents.

    Science.gov (United States)

    Spoelstra, Sandra L; Given, Charles W

    2011-05-01

    The increase in oral anticancer medications with complex regimens creates a need to assure that patients are taking therapeutic dosages as prescribed. This article reviews the assessment and measurement of adherence to oral antineoplastic agents. Research and journal articles from CINAHL and PubMed. Assessing and measuring adherence to oral antineoplastics should include three dimensions: the percentage of medications taken, the duration, and the timing of taking the medication. Clinicians need to conduct ongoing assessment and measurement of adherence to oral antineoplastic agents. This includes eliciting patient report of adherence, pill counts, drug diaries, and pharmacy or medical record audits. Copyright © 2011 Elsevier Inc. All rights reserved.

  7. Oral Antineoplastic Agents: Assessing the Delay in Care

    OpenAIRE

    2015-01-01

    The study was undertaken to determine the length of time between when a prescription for an oral antineoplastic agent is written by the provider and when the medication is received by the patient and to identify risk factors that significantly increase time to medication receipt. First-time fill prescriptions for oral antineoplastic agents were identified. The date the prescription was written and received by the patient was determined. A retrospective review was completed to gather additiona...

  8. Discovery of diethyl 2,5-diaminothiophene-3,4-dicarboxylate derivatives as potent anticancer and antimicrobial agents and screening of anti-diabetic activity: synthesis and in vitro biological evaluation. Part 1.

    Science.gov (United States)

    Bozorov, Khurshed; Ma, Hai-Rong; Zhao, Jiang-Yu; Zhao, Hai-Qing; Chen, Hua; Bobakulov, Khayrulla; Xin, Xue-Lei; Elmuradov, Burkhon; Shakhidoyatov, Khusnutdin; Aisa, Haji A

    2014-09-12

    Series of diethyl 2,5-diaminothiophene-3,4-dicarboxylate (DDTD) derivatives: azomethines of DDTD (2a-l) have been synthesized and screened for their anticancer, antimicrobial and anti-diabetic activities. The novel synthesized compounds were characterized by (1)H, (13)C NMR, MS and FT-IR analyses. All compounds were evaluated for their antiproliferative activity against three types of cancer cell line such as T47D and MCF-7 (human breast cancer), Hela (human cervical cancer) and Ishikawa (human endometrial cancer) lines. The results showed that most compounds exhibited significant antiproliferative activity against breast cancer cells. The majority of azomethines DDTD influenced strongly against breast cancer cells T47D and MCF-7, among them compounds 2b (2.3 μM), 2c (12.1 μM), 2e (13.2 μM), 2i (14.9 μM), 2j (16.0 μM), 2k (7.1 μM), 2l (8.6 μM) manifest potent anticancer activity against cancer cell T47D than Doxorubicin (DOX, 15.5 μM). Compound 2j has shown potent activity on all three types of cancer cells concurrently and IC50 values were considerably low in comparison with positive control DOX. In addition, all compounds were tested for antimicrobial activity against Staphylococcus aureus ATCC 6538 (Gram positive bacteria), Escherichia coli ATCC 11229 (Gram negative bacteria) and Candida albicans ATCC 10231 (Fungi) strains and 2j which contains in the ring nitrofurfural fragment, showed the highest effect on the three species of microbial pathogens simultaneously. Some compounds induced enzymatic inhibition in a concentration-dependent manner on PTP-1B inhibitor.

  9. A Novel Diphenylthiosemicarbazide Is a Potential Insulin Secretagogue for Anti-Diabetic Agen

    Science.gov (United States)

    Sugawara, Kenji; Honda, Kohei; Reien, Yoshie; Yokoi, Norihide; Seki, Chihiro; Takahashi, Harumi; Minami, Kohtaro; Mori, Ichiro; Matsumoto, Akio; Nakaya, Haruaki; Seino, Susumu

    2016-01-01

    Insulin secretagogues are used for treatment of type 2 diabetes. We attempted to discover novel small molecules to stimulate insulin secretion by using in silico similarity search using sulfonylureas as query, followed by measurement of insulin secretion. Among 38 compounds selected by in silico similarity search, we found three diphenylsemicarbazides and one quinolone that stimulate insulin secretion. We focused on compound 8 (C8), which had the strongest insulin-secreting effect. Based on the structure-activity relationship of C8-derivatives, we identified diphenylthiosemicarbazide (DSC) 108 as the most potent secretagogue. DSC108 increased the intracellular Ca2+ level in MIN6-K8 cells. Competitive inhibition experiment and electrophysiological analysis revealed sulfonylurea receptor 1 (SUR1) to be the target of DSC108 and that this diphenylthiosemicarbazide directly inhibits ATP-sensitive K+ (KATP) channels. Pharmacokinetic analysis showed that DSC108 has a short half-life in vivo. Oral administration of DSC108 significantly suppressed the rises in blood glucose levels after glucose load in wild-type mice and improved glucose tolerance in the Goto-Kakizaki (GK) rat, a model of type 2 diabetes with impaired insulin secretion. Our data indicate that DSC108 is a novel insulin secretagogue, and is a lead compound for development of a new anti-diabetic agent. PMID:27764176

  10. Pharmacogenetics of Anti-Diabetes Drugs

    Directory of Open Access Journals (Sweden)

    Johanna K. DiStefano

    2010-08-01

    Full Text Available A variety of treatment modalities exist for individuals with type 2 diabetes mellitus (T2D. In addition to dietary and physical activity interventions, T2D is also treated pharmacologically with nine major classes of approved drugs. These medications include insulin and its analogues, sulfonylureas, biguanides, thiazolidinediones (TZDs, meglitinides, α-glucosidase inhibitors, amylin analogues, incretin hormone mimetics, and dipeptidyl peptidase 4 (DPP4 inhibitors. Pharmacological treatment strategies for T2D are typically based on efficacy, yet favorable responses to such therapeutics are oftentimes variable and difficult to predict. Characterization of drug response is expected to substantially enhance our ability to provide patients with the most effective treatment strategy given their individual backgrounds, yet pharmacogenetic study of diabetes medications is still in its infancy. To date, major pharmacogenetic studies have focused on response to sulfonylureas, biguanides, and TZDs. Here, we provide a comprehensive review of pharmacogenetics investigations of these specific anti-diabetes medications. We focus not only on the results of these studies, but also on how experimental design, study sample issues, and definition of ‘response’ can significantly impact our interpretation of findings. Understanding the pharmacogenetics of anti-diabetes medications will provide critical baseline information for the development and implementation of genetic screening into therapeutic decision making, and lay the foundation for “individualized medicine” for patients with T2D.

  11. Pharmacogenetics of Anti-Diabetes Drugs.

    Science.gov (United States)

    Distefano, Johanna K; Watanabe, Richard M

    2010-08-01

    A variety of treatment modalities exist for individuals with type 2 diabetes mellitus (T2D). In addition to dietary and physical activity interventions, T2D is also treated pharmacologically with nine major classes of approved drugs. These medications include insulin and its analogues, sulfonylureas, biguanides, thiazolidinediones (TZDs), meglitinides, α-glucosidase inhibitors, amylin analogues, incretin hormone mimetics, and dipeptidyl peptidase 4 (DPP4) inhibitors. Pharmacological treatment strategies for T2D are typically based on efficacy, yet favorable responses to such therapeutics are oftentimes variable and difficult to predict. Characterization of drug response is expected to substantially enhance our ability to provide patients with the most effective treatment strategy given their individual backgrounds, yet pharmacogenetic study of diabetes medications is still in its infancy. To date, major pharmacogenetic studies have focused on response to sulfonylureas, biguanides, and TZDs. Here, we provide a comprehensive review of pharmacogenetics investigations of these specific anti-diabetes medications. We focus not only on the results of these studies, but also on how experimental design, study sample issues, and definition of 'response' can significantly impact our interpretation of findings. Understanding the pharmacogenetics of anti-diabetes medications will provide critical baseline information for the development and implementation of genetic screening into therapeutic decision making, and lay the foundation for "individualized medicine" for patients with T2D.

  12. Gestational diabetes mellitus management with oral hypoglycemic agents.

    Science.gov (United States)

    Ryu, Rachel J; Hays, Karen E; Hebert, Mary F

    2014-12-01

    Oral hypoglycemic agents such as glyburide (second-generation sulfonylurea) and metformin (biguanide) are attractive alternatives to insulin due to lower cost, ease of administration, and better patient adherence. The majority of evidence from retrospective and prospective studies suggests comparable efficacy and safety of oral hypoglycemic agents such as glyburide and metformin as compared to insulin when used in the treatment of women with gestational diabetes mellitus (GDM). Glyburide and metformin have altered pharmacokinetics during pregnancy and both agents cross the placenta. In this article, we review the efficacy, safety, and dosage of oral hypoglycemic agents for the treatment of gestational diabetes mellitus. Additional research is needed to evaluate optimal dosage for glyburide and metformin during pregnancy. Comparative studies evaluating the effects of glyburide and metformin on long-term maternal and fetal outcomes are also needed.

  13. [Progress in study of oral biofilm dispersal-inducing agents].

    Science.gov (United States)

    Yan, Zhu; Jingmei, Yang; Dingyu, Duan; Yi, Xu

    2014-12-01

    Communities of bacteria wrapped in self-generated extracellular polymeric matrix and attached to a solid surface are known as biofilm. Biofilm formation and development can be divided into three stages: adhesion of cells to a surface, reproduction of the cells, and dispersion of cells. The procedure, which surface-attached biofilm disperses bacterial cells into the environment to colonize new sites, is defined as biofilm dispersal. Biofilm dispersal is an essential stage of biofilm life cycle. It plays an important role in the transmission of bacteria. For many pathogenic bacteria, biofilm dispersal can transform bacteria in biofilm into planktonic state and promote the spread of infection. The formation of biofilm may increase the resistance of bacteria to antimicrobial agent and host defence response compared with planktonic cells. In the oral cavity, oral microorganism can attach to the surface of oral tissue and prosthesis to form biofilm. Dental caries and periodontal disease are oral chronic infections diseases of the oral tissue. The occurrence of them has a close relationship with biofilm. The mechanism of dispersal is a hot topic in recent years. Some agents which promote dispersal might be a therapeutic potential against biofilm infections. The clinical implication of dispersal agents and potential application are promising. This article reviews the dispersal-inducing agents of oral biofilms.

  14. Therapeutic options for herpes labialis, I: Oral agents.

    Science.gov (United States)

    Elish, Diana; Singh, Fiza; Weinberg, Jeffrey M

    2004-07-01

    Given the prevalence of herpes labialis, effective therapy has the potential to affect the lives of many and presents a challenge for clinicians. Over the last several years, most of the focus of herpes research has been on the treatment of genital herpes. Recently, however, several studies have been published examining the efficacy of therapies specifically for herpes labialis. Several therapeutic agents, both prescription and over-the-counter, are available for controlling and managing the disease. In this series of articles, we review oral and topical therapeutic agents that are available in the treatment of herpes labialis and its associated symptoms. This article will review oral treatment options.

  15. Garcinia xanthones as orally active antitumor agents.

    Science.gov (United States)

    Zhang, Xiaojin; Li, Xiang; Sun, Haopeng; Wang, Xiaojian; Zhao, Li; Gao, Yuan; Liu, Xiaorong; Zhang, Shenglie; Wang, Yanyan; Yang, Yingrui; Zeng, Su; Guo, Qinglong; You, Qidong

    2013-01-10

    Using a newly developed strategy whose key step is the regioselective propargylation of hydroxyxanthone substrates, 99 structurally diverse Garcinia natural-product-like xanthones based on gambogic acid were designed and synthesized and their in vitro antitumor activity was evaluated. A set of 40 related compounds was chosen for determination of their physicochemical properties including polar surface area, log D₇.₄, aqueous solubility, and permeability at pH 7.4. In the light of the in vitro antitumor activity and the physicochemical properties, two compounds were advanced into in vivo efficacy experiments. The antitumor activity of compound 112, administered po, showed more potent in vivo oral antitumor activity than gambogic acid.

  16. GC-MS analysis, preliminary phytochemical screening, physicochemical analysis and anti-diabetic activity of ethanol extract of Jasminum cuspidatum leaves

    Directory of Open Access Journals (Sweden)

    Singumsetty Vinay

    2014-12-01

    Full Text Available The purpose of the present study was investigating the GC-MS analysis, preliminary phytochemical screening, physicochemical analysis and anti-diabetic activity of ethanol extract of the leaves of Jasminum cuspidatum. The anti-diabetic activity was investigated in streptozotocin-induced diabetes rats with treatment of ethanol extract at the dose level of 200 and 400 mg/kg, which was compared with glibenclamide at a dose level of 4 mg/kg and the parameter measured being the blood glucose, total cholesterol, HDL, LDL, VLDL, triglycerides, and total protein. An oral glucose tolerance test (OGTT was also investigated in experimental rats. The GC-MS analysis revealed that the ethanol extract contained seven phytoconstituents. Preliminary phytochemical screening showed the presence of triterpenoids, flavonoids, glycosides and steroids. The result of in vivo anti-diabetic activity revealed that the ethanol extract of J. cuspidatum showed significant anti-diabetic activity.

  17. Protective effect of camel milk as anti-diabetic supplement ...

    African Journals Online (AJOL)

    Protective effect of camel milk as anti-diabetic supplement: biochemical, molecular ... CM contains vital active particles with insulin like action that cure diabetes and its ... Tissues from liver and adipose tissues were examined using RT-PCR ...

  18. ANTI-DIABETIC EFFECT OF MORUS ALBA ON RABBIT AS ANIMAL MODEL

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    Laddha G. P.

    2012-04-01

    Full Text Available A study of ancient literature indicates that diabetes was fairly well known and well conceived as an entity in India. The nature has provided abundant plant wealth for all the living creatures, which possess medicinal virtues. Therefore, there is a necessity to explore their uses and to conduct Pharmacognostic and pharmacological studies to ascertain their therapeutic properties. In fact, nowadays diabetes is a global problem. Hence, the present study aims to open new avenues for the improvement of medicinal uses of Morus alba. for the area for diabetes. Another important objective of such study is to bring the anti-diabetic medicinal plants sector on a firm scientific footing, raise awareness and add value to the resource. Dried petroleum ether (60-80°C extracts of leaves of Morus alba. were subjected for hypoglycemic activity in New Zealand rabbits (1.5-3.5 kg. Blood sugar level was determined using digital glucometer. The oral administration of leaf extracts at doses of 200 mg/ kg− lead to a significant blood glucose reduction. This laid the foundation to study the active compounds of such anti-diabetic plants that are responsible for the hypoglycemic activities. It also proves the traditional claim of Kachh region with regard to Morus Alba for its anti-diabetic activity.

  19. The safety and effectiveness of once daily detemir in patients with type 2 diabetes previously failing oral agents:the Chinese cohort from SOL-VETM observational study

    Institute of Scientific and Technical Information of China (English)

    潘长玉

    2013-01-01

    Objective To evaluate the safety and effectiveness of initiating once-daily insulin detemir(Levemir) as add-on therapy in patients with type 2 diabetes mellitus(T2DM) who failed treatment of oral anti-diabetic drugs(OAD).Methods The present study was derived from the data of

  20. Bromophenols from Marine Algae with Potential Anti-Diabetic Activities

    Institute of Scientific and Technical Information of China (English)

    LIN Xiukun; LIU Ming

    2012-01-01

    Marine algae contain various bromophenols with a variety of biological activities,including antimicrobial,anticancer,and anti-diabetic effects.Here,we briefly review the recent progress in researches on the biomaterials from marine algae,emphasizing the relationship between the structure and the potential anti-diabetic applications.Bromophenols from marine algae display their hyperglycemic effects by inhibiting the activities of protein tyrosine phosphatase 1B,α-glucosidase,as well as other mechanisms.

  1. 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.

  2. Granulated colloidal silicon dioxide-based self-microemulsifying tablets, as a versatile approach in enhancement of solubility and therapeutic potential of anti-diabetic agent: formulation design and in vitro/in vivo evaluation.

    Science.gov (United States)

    Pandey, Vikas; Gilhotra, Ritu M; Kohli, Seema

    2017-06-01

    The current research work was executed with an aim to explore and promote the potential of self-microemusifying drug delivery systems (SMEDDS) in the form of tablets, in order to enhance solubility and oral bioavailability of poorly aqueous soluble drug Repaglinide (RPG). RPG-loaded liquid SMEDDS were developed consisting Labrafil M 1944CS, Kolliphor EL and Propylene glycol, which were then characterized on various parameters. After characterization and optimization, liquid SMEDDS were converted into solid form by adsorbing on Aeroperl® 300 pharma and polyplasdone(TM) XL. Further, selection of suitable excipients was done and mixed with prepared solidified SMEDDS powder followed by the preparation of self-microemulsifying tablets (SMET's) wet granulation-compression method. SMET's were subjected to differential scanning calorimetry (DSC) and particle X-ray diffraction (RXRD) studies, results of which indicated transformation of crystalline structure of RPG because of dispersion of RPG at molecular level in liquid SMEDDS. This was further assured by micrographs obtained from scanning electron microscope. SMET's shown more than 85% (30 min) of in vitro drug release in contrast to conventional marketed tablets (13.2%) and pure RPG drug (3.2%). Results of in vivo studies furnished that SMET's had shown marked decrease in the blood glucose level and prolonged duration of action (up to 8 h) in comparison with conventional marketed tablets and pure RPG drug. In conclusion, SMET's serves as a promising tool for successful oral delivery of poorly aqueous soluble drug(s) such as RPG.

  3. Finding needles in a haystack: application of network analysis and target enrichment studies for the identification of potential anti-diabetic phytochemicals.

    Science.gov (United States)

    Fayaz, Shaik M; Suvanish Kumar, Valsala S; Rajanikant, Krishnamurthy G

    2014-01-01

    Diabetes mellitus is a debilitating metabolic disorder and remains a significant threat to public health. Herbal medicines have been proven to be effective anti-diabetic agents compared to synthetic drugs in terms of side effects. However, the complexity in their chemical constituents and mechanism of action, hinder the effort to discover novel anti-diabetic drugs. Hence, understanding the biological and chemical basis of pharmacological action of phytochemicals is essential for the discovery of potential anti-diabetic drugs. Identifying important active compounds, their protein targets and the pathways involved in diabetes would serve this purpose. In this context, the present study was aimed at exploring the mechanism of action of anti-diabetic plants phytochemicals through network and chemical-based approaches. This study also involves a focused and constructive strategy for preparing new effective anti-diabetic formulations. Further, a protocol for target enrichment was proposed, to identify novel protein targets for important active compounds. Therefore, the successive use of network analysis combined with target enrichment studies would accelerate the discovery of potential anti-diabetic phytochemicals.

  4. Finding needles in a haystack: application of network analysis and target enrichment studies for the identification of potential anti-diabetic phytochemicals.

    Directory of Open Access Journals (Sweden)

    Shaik M Fayaz

    Full Text Available Diabetes mellitus is a debilitating metabolic disorder and remains a significant threat to public health. Herbal medicines have been proven to be effective anti-diabetic agents compared to synthetic drugs in terms of side effects. However, the complexity in their chemical constituents and mechanism of action, hinder the effort to discover novel anti-diabetic drugs. Hence, understanding the biological and chemical basis of pharmacological action of phytochemicals is essential for the discovery of potential anti-diabetic drugs. Identifying important active compounds, their protein targets and the pathways involved in diabetes would serve this purpose. In this context, the present study was aimed at exploring the mechanism of action of anti-diabetic plants phytochemicals through network and chemical-based approaches. This study also involves a focused and constructive strategy for preparing new effective anti-diabetic formulations. Further, a protocol for target enrichment was proposed, to identify novel protein targets for important active compounds. Therefore, the successive use of network analysis combined with target enrichment studies would accelerate the discovery of potential anti-diabetic phytochemicals.

  5. Oral Antineoplastic Agents: Assessing the Delay in Care

    Directory of Open Access Journals (Sweden)

    Brandi Anders

    2015-01-01

    Full Text Available The study was undertaken to determine the length of time between when a prescription for an oral antineoplastic agent is written by the provider and when the medication is received by the patient and to identify risk factors that significantly increase time to medication receipt. First-time fill prescriptions for oral antineoplastic agents were identified. The date the prescription was written and received by the patient was determined. A retrospective review was completed to gather additional information, including prescribed medication, indication, insurance coverage, patient assistance program use, dispensing pharmacy, and prior authorization requirements. The data was analyzed through multivariate statistical analysis and used to identify risk factors that may significantly increase the time to medication receipt. A total of 58 patients were included in the study. A median of 8 days elapsed between when the medication was prescribed and when it was received by the patient. Medication prescribed, absence of a Risk Evaluation Mitigation Strategies (REMS program, and insurance type are factors that increased time to medication receipt. An understanding of the median time involved, as well as factors affecting the time to delivery of prescriptions, will help healthcare providers better plan and prepare for the use of oral antineoplastic agents.

  6. Oral Antineoplastic Agents: Assessing the Delay in Care.

    Science.gov (United States)

    Anders, Brandi; Shillingburg, Alexandra; Newton, Michael

    2015-01-01

    The study was undertaken to determine the length of time between when a prescription for an oral antineoplastic agent is written by the provider and when the medication is received by the patient and to identify risk factors that significantly increase time to medication receipt. First-time fill prescriptions for oral antineoplastic agents were identified. The date the prescription was written and received by the patient was determined. A retrospective review was completed to gather additional information, including prescribed medication, indication, insurance coverage, patient assistance program use, dispensing pharmacy, and prior authorization requirements. The data was analyzed through multivariate statistical analysis and used to identify risk factors that may significantly increase the time to medication receipt. A total of 58 patients were included in the study. A median of 8 days elapsed between when the medication was prescribed and when it was received by the patient. Medication prescribed, absence of a Risk Evaluation Mitigation Strategies (REMS) program, and insurance type are factors that increased time to medication receipt. An understanding of the median time involved, as well as factors affecting the time to delivery of prescriptions, will help healthcare providers better plan and prepare for the use of oral antineoplastic agents.

  7. Fast and environmentally friendly quantitative analysis of active agents in anti-diabetic tablets by an alternative laser-induced breakdown spectroscopy (LIBS) method and comparison to a validated reversed-phase high-performance liquid chromatography (RP-HPLC) method.

    Science.gov (United States)

    Contreras, Victor Ulises; Meneses-Nava, Marco A; Ornelas-Soto, Nancy; Barbosa-García, Oracio; López-de-Alba, Pedro L; Maldonado, José L; Ramos-Ortiz, Gabriel; Acevedo-Aguilar, Francisco J; López-Martínez, Leticia

    2012-11-01

    Laser-induced breakdown spectroscopy (LIBS) is evaluated as a potential analytic technique for rapid screening and quality control of anti-diabetic tablets. This paper proposes a simple LIBS-based method for the quantitative analysis of two active pharmaceutical ingredients (APIs): metformin (Met) and glybenclamide (Gly). In order to quantify both APIs, chlorine (Cl) concentration was estimated by employing the Cl/Br optical emission ratio, where Br was introduced as internal standard. Calibration curves were prepared, achieving linearity higher than 99%. On the other hand, for comparison to the proposed method, an isocratic reversed-phase high-performance liquid chromatography (RP-HPLC) method was also developed for quantitative determination of the same analytes by ultraviolet (UV) detection. The chromatographic separation was achieved on a Phenomenex Hypersil C18, 250 mm × 4.6 mm, 5 μm column. The mobile phase was K(2)HPO(4)/H(3)PO(4)-CH(3)OH and flow rate was 1.0 mL min(-1). The method is linear over a range of 10-60 μg mL(-1) for Gly and 5-30 μg mL(-1) for Met and the correlation coefficients were ≥0.99. Recoveries were found to be in the range of 95-101%. Furthermore, four different commercial brands of each active agent were evaluated by both proposed LIBS and chromatographic methods and results were compared with each other. The comparison was satisfactorily validated by analysis of variance (ANOVA).

  8. Effects of C-glycosylation on anti-diabetic, anti-Alzheimer's disease and anti-inflammatory potential of apigenin.

    Science.gov (United States)

    Choi, Jae Sue; Islam, Md Nurul; Ali, Md Yousof; Kim, Eon Ji; Kim, Young Myeong; Jung, Hyun Ah

    2014-02-01

    Apigenin has gained particular interests in recent years as a beneficial and health promoting agent because of its low intrinsic toxicity. Vitexin and isovitexin, naturally occurring C-glycosylated derivatives of apigenin, have been known to possess potent anti-diabetic, anti-Alzheimer's disease (anti-AD), and anti-inflammatory activities. The present study was designed to investigate the anti-diabetic, anti-AD, and anti-inflammatory potential of apigenin and its two C-glycosylated derivatives, vitexin and isovitexin by in vitro assays including rat lens aldose reductase (RLAR), human recombinant aldose reductase (HRAR), advanced glycation endproducts (AGEs), protein tyrosine phosphatase 1B (PTP1B), acetylcholinesterase (AChE), butyrylcholinesterase (BChE), β-site amyloid precursor (APP) cleaving enzyme 1 (BACE1), and nitric oxide (NO), inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) in lipopolysaccharide (LPS)-induced RAW 264.7 cells. Among them, isovitexin was found as the most potent inhibitor against RLAR, HRAR, AGE, AChE, and BChE while vitexin showed the most potent PTP1B inhibitory activity. Despite the relatively weak anti-diabetic and anti-AD potentials, apigenin showed powerful antiinflammatory activity by inhibiting NO production and iNOS and COX-2 expression while vitexin and isovitexin were inactive. Therefore, it could be speculated that C-glycosylation of apigenin at different positions might be closely linked to relative intensity of anti-diabetic, anti-AD, and anti-inflammatory potentials.

  9. A drug utilization and pharmacoeconomic study of anti-diabetic drugs prescribed to type 2 diabetes mellitus patients visiting the medicine out-patient department of a tertiary care hospital of north India

    Directory of Open Access Journals (Sweden)

    Amandeep Singh

    2016-08-01

    Conclusions: Metformin was the most common OAD agent and insulin aspart was the most common injectable anti-diabetic drug prescribed in patients with T2DM. The newer anti-diabetic drugs sitagliptin and newer insulin analogues were also prescribed to a great extent. Overall, the prescribing trend was rational to a great extent and had improved since the earlier study in the same institute. The most cost-effective anti-diabetic therapy was combination therapy of glipizide and metformin. The cost of diabetes management is high, especially for insulin therapy. [Int J Basic Clin Pharmacol 2016; 5(4.000: 1220-1227

  10. Effect of insulin detemir versus neutral protamine zinc insulin combined with oral anti-diabetes drugs in treating type 2 diabetes mellitus%地特胰岛素对比中性鱼精蛋白锌胰岛素联合口服降糖药治疗2型糖尿病的疗效和安全性观察

    Institute of Scientific and Technical Information of China (English)

    吕蕾; 郭俊杰; 郭晓霏

    2012-01-01

    Objective To compare of effect of insulin detemir (Det) versus neutral protamine hagedorn (NPI1) combined with oral anti-diabetes drugs (OADs) in treating type 2 diabetes mellitus (T2DM). Methods The 60 T2DM patients divided into two groups were treated with Det + OADs versus NPH + OADs respectively. The comparisons of fasting plasma glucose (FPG), two-hour postprandial plasma glucose (2 hPG), incidence of hypoglycemia, body mass index (BMI), and hemoglobin A1c (HbA1c) between the two groups before versus after treatment were performed to observe the final effect. Results The levels of FPG, 2 hPG, and HbA1c of the two groups were decreased after treatment for 12 weeks, while the decrease in the Det+OADs group was more significant (P<0. 05). The Det+OADs group was superior to the NPH + OADs group in the BMI control (P<0. 05) and less hypoglycemia. Conclusion Comparing with NPH+ OADs, the effect of Det+OADs is better in treating T2DM with less incidence of hypoglycemia and less influence on body weight.%目的 探讨地特胰岛素(Det)对比中性鱼精蛋白锌胰岛素(NPH)联合口服降糖药(OADs)治疗T2DM的疗效和安全性.方法 选择60例T2DM患者分别应用Det和NPH联合OADs治疗,比较两组治疗前后FPG、2 hPG、低血糖事件发生、BMI及HbA1 c变化.结果 两组患者治疗12周后FPG、2 hPG、HbA1 c均较治疗前下降(P<0.05),但Det组下降更显著(P<0.05),Det组对BMI控制优于NPH组(P<0.05),低血糖发生率低.结论 与NPH相比,Det联合OADs治疗T2DM疗效更好,低血糖发生率低,对体重影响小.

  11. Oral available agents in the treatment of RRMS

    Directory of Open Access Journals (Sweden)

    Aupérin T

    2013-10-01

    Full Text Available Thierry Aupérin Medical Communications, Global MS Medical Affairs, Genzyme Corporation, Cambridge, MA, USAWe read with interest the article by Drs Thöne and Ellrichmann entitled "Oral available agents in the treatment of relapsing remitting multiple sclerosis: an overview of merits and culprits" recently published in Drug, Healthcare and Patient Safety.1 The review provides a valuable overview of a number of new therapeutic options for multiple sclerosis (MS, with a focus on proposed mechanisms of action and efficacy and safety profiles of the respective agents.In reading the article, however, we did note a number of errors pertaining to teriflunomide, a once-daily oral immunomodulator approved in several countries for the treatment of relapsing forms of MS (RMS and relapsing-remitting MS (RRMS. The most significant error pertains to a statement made within the safety section, which states: "Serious adverse effects (AEs included pathological liver function, neutropenia, and trigeminal neuralgia as well as one case of progressive multifocal leukoencephalopathy (PML in a patient with systemic lupus erythematosus." We would like to draw the authors’ attention to the fact that this case of PML pertains to the use of the related drug, leflunomide, and not teriflunomide as suggested. It is important to note that leflunomide is licensed to treat active rheumatoid arthritis in adults, and has not been evaluated or approved for the treatment of MS; as such it is inappropriate to extrapolate this observation to the use of teriflunomide. Furthermore, the case of PML cited in the article is complicated by the fact that the patient received prior multiple immunosuppressant therapies before leflunomide (ie, prednisone, azathioprine, chloroquine, danazol, cyclosporin A and methotrexate, which may have contributed to the development of PML.View original paper by Thöne and Ellrichmann.

  12. Prospective, non-interventional, uncontrolled, open-chart, pharmacoepidemiologic study of prescribing patterns for anti-diabetic drugs at tertiary care hospital in Erode

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    Radhika P

    2009-01-01

    Full Text Available The aim of this study is to determine current prescribing patterns for anti-diabetic drugs adopted by physicians in Erode. The prospective, non interventional, uncontrolled, open-chart, pharmacoepidemiological study was conducted from January -2007 to April -2007 at a diabetic care centre having 350 diabetic patients. The pattern of prescribing anti-diabetic drugs was recorded along with glycosylated haemoglobin levels, total cholesterol, high-density lipoprotein, low-density lipoprotein, very low-density lipoprotein and triglycerides in insulin-dependent diabetes mellitus and non-insulin-dependent diabetes mellitus patients and the values were observed. The prescribing pattern of the oral anti-diabetic drugs shows that out of the various oral anti-diabetic drugs′ available, drugs from only two groups were prescribed. Sulphonylureas, biguanides and combination therapy accounts for 31.43%, 20.28% and 33.71% of prescriptions, respectively, while insulin alone and with OAD′s accounts for 6.28% and 8.29% prescriptions, respectively. Overall, prescribing trend is away from monotherapy with insulin and sulphonylureas and towards combination therapies.

  13. Safe handling and administration considerations of oral anticancer agents in the clinical and home setting.

    Science.gov (United States)

    Lester, Joanne

    2012-12-01

    The use of hormonal, chemotherapeutic, and targeted biologic oral agents has exponentially increased since the early 2000s. Oral therapies have the advantage of persistent exposure of the cytotoxic drug to tumor cells and the tumor environment. The use of oral anticancer agents provides therapeutic drug treatment for patients with cancer in the comfort of their home or alternative settings, such as retirement homes and assisted living or extended-care facilities. Practices to ensure safe storage, handling, administration, and disposal of oral agents are necessary to prevent additional exposure of hazardous substances to the environment, professionals, patients, family members, and caretakers. Providers should consider potential barriers to adherence and compliance, and develop strategies to ensure optimal therapeutic benefit prior to initiation of oral agents.

  14. COST-EFFECTIVENESS ANALYSIS OF ANTI-DIABETIC THERAPY IN A UNIVERSITY TEACHING HOSPITAL

    OpenAIRE

    Giwa Abdulganiyu; Tayo Fola

    2014-01-01

    Purpose: To conduct cost-effectiveness analysis of anti-diabetic therapy in a University Teaching Hospital in 2010. Methods: A retrospective review of selected case-notes was conducted. World Health Organization Defined Daily Dose Method of evaluating drug use and probability method for potential effectiveness of antidiabetic therapeutic options from literature analysis was employed in determining cost-effectiveness of each anti-diabetic therapeutic option identified from anti-diabetic dru...

  15. A new anti-diabetic sesquiterpenoid from Acorus calamus

    Institute of Scientific and Technical Information of China (English)

    Chang Xin Zhou; Di Qiao; You You Yan; Hao Shu Wu; Jian Xia Mo; Li She Gan

    2012-01-01

    A new sesquiterpenoid,1β,5α-guaiane-4β,10α-diol-6-one (1),was isolated from 70% EtOH extract of the rhizomes of Acorus calamus.The structure was determined on spectroscopic methods,especially 2D NMR techniques.The absolute configuration of 1 was confirmed by TDDFT quantum chemical calculation of its ECD spectrum.Compound 1 showed promising anti-diabetic activity on a insulin-mediated glucose consumption model of HepG2 cells.

  16. High-throughput screening for GPR119 modulators identifies a novel compound with anti-diabetic efficacy in db/db mice.

    Directory of Open Access Journals (Sweden)

    Meng Zhang

    Full Text Available G protein-coupled receptor 119 (GPR119 is highly expressed in pancreatic β cells and enteroendocrine cells. It is involved in glucose-stimulated insulin secretion and glucagon-like peptide-1 (GLP-1 release, thereby representing a promising target for the treatment of type 2 diabetes. Although a number of GPR119 agonists were developed, no positive allosteric modulator (PAM to this receptor has been reported. Here we describe a high-throughput assay for screening GPR119 PAMs and agonists simultaneously. Following screening of a small molecule compound library containing 312,000 synthetic and natural product-derived samples, one potent GPR119 agonist with novel chemical structure, MW1219, was identified. Exposure of MIN6 and GLUTag cells to MW1219 enhanced glucose-stimulated insulin secretion and GLP-1 release; once-daily oral dosing of MW1219 for 6 weeks in diabetic db/db mice reduced hemoglobin A1c (HbA1c and improved plasma glucose, insulin and GLP-1 levels; it also increased glucose tolerance. The results demonstrate that MW1219 is capable of effectively controlling blood glucose level and may have the potential to be developed as a new class of anti-diabetic agents.

  17. Anti-Diabetic Effect of Balanced Deep-Sea Water and Its Mode of Action in High-Fat Diet Induced Diabetic Mice

    Directory of Open Access Journals (Sweden)

    Yun Hee Shon

    2013-10-01

    Full Text Available In this study, we investigated the effects of balanced deep-sea water (BDSW on hyperglycemia and glucose intolerance in high-fat diet (HFD-induced diabetic C57BL/6J mice. BDSW was prepared by mixing deep-sea water (DSW mineral extracts and desalinated water to give a final hardness of 500–2000. Mice given an HFD with BDSW showed lowered fasting plasma glucose levels compared to HFD-fed mice. Oral and intraperitoneal glucose tolerance tests showed that BDSW improves impaired glucose tolerance in HFD-fed mice. Histopathological evaluation of the pancreas showed that BDSW recovers the size of the pancreatic islets of Langerhans, and increases the secretion of insulin and glucagon in HFD-fed mice. Quantitative reverse transcription polymerase chain reaction results revealed that the expression of hepatic genes involved in glucogenesis, glycogenolysis and glucose oxidation were suppressed, while those in glucose uptake, β-oxidation, and glucose oxidation in muscle were increased in mice fed HFD with BDSW. BDSW increased AMP-dependent kinase (AMPK phosphorylation in 3T3-L1 pre- and mature adipocytes and improved impaired AMPK phosphorylation in the muscles and livers of HFD-induced diabetic mice. BDSW stimulated phosphoinositol-3-kinase and AMPK pathway-mediated glucose uptake in 3T3-L1 adipocytes. Taken together, these results suggest that BDSW has potential as an anti-diabetic agent, given its ability to suppress hyperglycemia and improve glucose intolerance by increasing glucose uptake.

  18. Anti-diabetic effect of balanced deep-sea water and its mode of action in high-fat diet induced diabetic mice.

    Science.gov (United States)

    Ha, Byung Geun; Shin, Eun Ji; Park, Jung-Eun; Shon, Yun Hee

    2013-10-29

    In this study, we investigated the effects of balanced deep-sea water (BDSW) on hyperglycemia and glucose intolerance in high-fat diet (HFD)-induced diabetic C57BL/6J mice. BDSW was prepared by mixing deep-sea water (DSW) mineral extracts and desalinated water to give a final hardness of 500-2000. Mice given an HFD with BDSW showed lowered fasting plasma glucose levels compared to HFD-fed mice. Oral and intraperitoneal glucose tolerance tests showed that BDSW improves impaired glucose tolerance in HFD-fed mice. Histopathological evaluation of the pancreas showed that BDSW recovers the size of the pancreatic islets of Langerhans, and increases the secretion of insulin and glucagon in HFD-fed mice. Quantitative reverse transcription polymerase chain reaction results revealed that the expression of hepatic genes involved in glucogenesis, glycogenolysis and glucose oxidation were suppressed, while those in glucose uptake, β-oxidation, and glucose oxidation in muscle were increased in mice fed HFD with BDSW. BDSW increased AMP-dependent kinase (AMPK) phosphorylation in 3T3-L1 pre- and mature adipocytes and improved impaired AMPK phosphorylation in the muscles and livers of HFD-induced diabetic mice. BDSW stimulated phosphoinositol-3-kinase and AMPK pathway-mediated glucose uptake in 3T3-L1 adipocytes. Taken together, these results suggest that BDSW has potential as an anti-diabetic agent, given its ability to suppress hyperglycemia and improve glucose intolerance by increasing glucose uptake.

  19. Insulino-mimetic and anti-diabetic effects of zinc.

    Science.gov (United States)

    Vardatsikos, George; Pandey, Nihar R; Srivastava, Ashok K

    2013-03-01

    While it has long been known that zinc (Zn) is crucial for the proper growth and maintenance of normal biological functions, Zn has also been shown to exert insulin-mimetic and anti-diabetic effects. These insulin-like properties have been demonstrated in isolated cells, tissues, and different animal models of type 1 and type 2 diabetes. Zn treatment has been found to improve carbohydrate and lipid metabolism in rodent models of diabetes. In isolated cells, it enhances glucose transport, glycogen and lipid synthesis, and inhibits gluconeogenesis and lipolysis. The molecular mechanism responsible for the insulin-like effects of Zn compounds involves the activation of several key components of the insulin signaling pathways, which include the extracellular signal-regulated kinase 1/2 (ERK1/2) and phosphatidylinositol 3-kinase (PI3-K)/protein kinase B/Akt (PKB/Akt) pathways. However, the precise molecular mechanisms by which Zn triggers the activation of these pathways remain to be clarified. In this review, we provide a brief history of zinc, and an overview of its insulin-mimetic and anti-diabetic effects, as well as the potential mechanisms by which zinc exerts these effects.

  20. Management of Antithrombotic Agents in Oral Surgery Maria Martinez and Dimitrios A. Tsakiris *

    OpenAIRE

    Maria Martinez; Dimitrios A. Tsakiris

    2015-01-01

    Systemic anticoagulation with intravenous or oral anticoagulants and antiplatelet agents is an efficient treatment against thromboembolic or cardiovascular disease. Invasive dental procedures or oral surgery might be associated with bleeding complications if carried out under anticoagulants. Patients on vitamin K antagonists, new direct anticoagulants or antiplatelet agents having dental interventions with low-risk for bleeding do not need interruption of anticoagulation. In case of bleeding ...

  1. 口服降糖药不良反应对2型糖尿病患者心理健康和生活质量的影响%Association between side effects of oral anti-diabetic drugs and self- reported mental health and quality of life among patients with type 2 diabetes

    Institute of Scientific and Technical Information of China (English)

    陈宗存; 张少玲; 严励; 吴木潮; 陈黎红; 纪立农

    2011-01-01

    目的 探讨口服降糖药常见不良反应低血糖和体重增加对2型糖尿病患者心理建康和生存质量的影响.方法 全国16家三甲医院于2007年1至6月对486例2型糖尿病患者采用统一的患者问卷(AP RECAP-DM研究)进行病史采集,以低血糖担忧勘测量表(HFS-Ⅱ)测量患者治疗后对低血糖的担忧状况,欧洲生存质量五维量表(EQ-5D)测量患者治疗后的健康相关生存质量.结果 203例(41.8%)发生低血糖,其中18例(8.8%)为严重或极严重低血糖.93例(19.2%)有体重增加,其中11例(11.7%)体重增加超过5 kg.发生低血糖组HFS-Ⅱ分值高于无低血糖组[7.00(2.00~19.00)比0.00(0.00~7.00),P<0.01]而EQ-5D健康指数低于未发生低血糖组(0.90±0.12比0.93±0.13,P=0.003),其中严重或极严重低血糖组HFS-Ⅱ分值高于轻度低血糖组[20.00(8.00~30.00)比5.00(0.00~14.00),P<0.01].回归分析显示,HFS-Ⅱ分值与低血糖反应呈正相关(β=5.78,P<0.01),EQ-5D健康指数与低血糖反应呈负相关(β=-0.04,P<0.05),其中相对于轻度低血糖,严重低血糖或极严重低血糖组的HFS-Ⅱ分值较高(β=10.92,P<0.01).结论 在口服降糖药治疗过程中存在着较高的低血糖发生风险,与自我感觉不良和负性心理健康相关,有可能影响糖尿病远期预后.%Objective To examine the association between the side effects of oral anti-diabetic drugs (OAD) and self-reported mental health and quality of life among patients with type 2 diabetes mellitus (T2DM). Methods An observational, cross-sectional multicenter study with a retrospective medical chart review was conducted at 16 medical centers from around China. The T2DM patients were followed-up and treated with OAD alone prior to the index visit from January to September 2007. All subjects were ≥30 years old at the time of T2DM diagnosis and had received monotherapy or combination therapy of OAD for at least 6 months. Health-related quality of life was measured

  2. Influence of an anti-diabetic foot ulcer formula and its component herbs on tissue and systemic glucose homeostasis.

    Science.gov (United States)

    Chan, C M; Chan, Y W; Lau, C H; Lau, T W; Lau, K M; Lam, F C; Che, C T; Leung, P C; Fung, K P; Lau, C B S; Ho, Y Y

    2007-01-03

    Complications of diabetes impose major public health burdens worldwide. The positive effect of a Radix Astragali-based herbal preparation on healing diabetic foot ulcers in patients has been reported. Formula 1 is also referred as the 'Herbal drink to strengthen muscle and control swelling'. This formula contains six Chinese medical herbs, including Radix Astragali, Radix Rehmanniae, Rhizoma Smilacis Chinensis, Rhizoma Atractylodis Macrocephalae, Radix Polygoni Multiflori Preparata, and Radix Stephania Tetrandrae. Three of these herbs (Radix Astragali, Radix Rehmanniae, Rhizoma Atractylodis Macrocephalae) are commonly used in different anti-diabetic formulae of Chinese medicine. The objective of the current study is to use an interdisciplinary approach to test the hypothesis that Formula 1 and its components influence tissue and systemic glucose homeostasis. In vitro and in vivo models have been established including: (1) glucose absorption into intestinal brush border membrane vesicles (BBMV); (2) gluconeogenesis by H4IIE hepatoma cells; (3) glucose uptake by 3T3-L1 adipocytes and Hs68 skin fibroblasts; (4) normalization of glycaemic control in a diabetic rat model. The results of in vitro studies indicated that all herbal extracts can modify cellular glucose homeostasis. Since Formula 1 and Rhizoma Smilacis Chinensis extracts demonstrated potent effects on modifying glucose homeostasis in multiple tissues in vitro, they were further studied for their anti-diabetic activities in vivo using a streptozotocin (STZ)-induced diabetic rat model. The results showed that Formula 1 and Rhizoma Smilacis Chinensis extracts did not significantly improve oral glucose tolerance or basal glycaemia in diabetic rats. In conclusion, the anti-diabetic foot ulcer Formula 1 contains ingredients active in modifying tissue glucose homeostasis in vitro but these biological activities could not be associated with improved glycaemic control of diabetes in vivo.

  3. 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.

  4. Anti-diabetic potentials of Momordica charantia and Andrographis paniculata and their effects on estrous cyclicity of alloxan-induced diabetic rats.

    Science.gov (United States)

    Reyes, B A S; Bautista, N D; Tanquilut, N C; Anunciado, R V; Leung, A B; Sanchez, G C; Magtoto, R L; Castronuevo, P; Tsukamura, H; Maeda, K-I

    2006-04-21

    Momordica charantia and Andrographis paniculata are the commonly used herbs by the diabetic patients in Pampanga, Philippines. While the anti-diabetic potential of Momordica charantia is well established in streptozocin- or alloxan-induced diabetic animals, the anti-diabetic potential of Andrographis paniculata in alloxan-induced diabetic rat is not known. Neither the effects of these herbs on estrous cyclicity of alloxan-induced diabetic rats are elucidated. Thus, in these experiments, Momordica charantia fruit juice or Andrographis paniculata decoction was orally administered to alloxan-induced diabetic rats. Rats that were treated with Momordica charantia and Andrographis paniculata had higher body weight (BW) compared with diabetic positive control (P Momordica charantia and Andrographis paniculata-treated diabetic rats (5 days; P Momordica charantia and Andrographis paniculata could restore impaired estrous cycle in alloxan-induced diabetic rats.

  5. Adherence, compliance and persistence to oral antineoplastic therapy: a review focused on chemotherapeutic and biologic agents.

    Science.gov (United States)

    Gebbia, Vittorio; Bellavia, Giuseppe; Ferraù, Francesco; Valerio, Maria Rosaria

    2012-05-01

    To date, orally administered chemotherapy and biologic agents represent a significant percentage of all antineoplastic treatments in several types of cancer, which are most likely to increase in the near future. In this scenario, the issue of adherence and persistence to oral therapy is a key issue since poor compliance to oral antineoplastic treatments may negatively influence patients' clinical outcomes and, in turn, cause an increase in costs, number of hospitalizations and time spent in the hospital. The issue of adherence to new oral chemotherapeutic and/or biologic agents has not been deeply evaluated and data published in medical literature are quite scarce. Adherence is a multidimensional phenomenon, which may be influenced by patient- and health-care provider-related factors, anticancer therapy itself, education and socioeconomic aspects. Patients' selection plays, therefore, a key role in maximizing adherence and persistence to oral therapies. Treating health-care practitioners should first evaluate patient reliability to avoid prescribing oral treatments to patients with socioeconomic and medical conditions, which may predict poor adherence. Adherence and persistence to new oral biologic agents, which are linked to several side effects and whose use is constantly widening, should represent a main endpoint of clinical research in the nearest future.

  6. Anti-diabetic properties of flavonoid compounds isolated from Hyphaene thebaica epicarp on alloxan induced diabetic rats

    Directory of Open Access Journals (Sweden)

    Josline Y Salib

    2013-01-01

    Full Text Available Background: Diabetes mellitus, becoming the third killer of mankind after cancer and cardiovascular diseases, is one of the most challenging diseases facing health care professionals today. That is why; there has been a growing interest in the therapeutic use of natural products for diabetes, especially those derived from plants. Aim: To evaluate the anti-diabetic activity together with the accompanying biological effects of the fractions and the new natural compounds of Hyphaene thebaica (HT epicarp. Materials and Methods: 500 g of coarsely powdered of (HT fruits epicarp were extracted by acetone. The acetone crude extract was fractionated with methanol and ethyl acetate leaving a residual water-soluble fraction WF . The anti-diabetic effects of the WF and one of its compounds of the acetone extract of the (HT epicarp were investigated in this study using 40 adult male rats. Results: Phytochemical investigation of active WF revealed the presence of ten different flavonoids, among which two new natural compounds luteolin 7-O-[6″-O-α-L-rhamnopyranosyl]-β-D-galactopyranoside 3 and chrysoeriol 7-O-β-D-galactopyranosyl (1®2-α-L-arabinofuranoside 5 were isolated. Supplementation of the WF improved glucose and insulin tolerance and significantly lowered blood glycosylated hemoglobin levels. On the other hand, compound 5 significantly reduced AST and ALT levels of liver, respectively. Likewise, the kidney functions were improved for both WF and compound 5 , whereby both urea and creatinine levels in serum were highly significant. Conclusion: The results justify the use of WF and compound 5 of the (HT epicarp as anti-diabetic agent, taking into consideration that the contents of WF were mainly flavonoids.

  7. [Temozolomide, an oral chemotherapeutic agent with potential severe toxicity

    NARCIS (Netherlands)

    Soetekouw, P.M.M.B.; Gijtenbeek, J.M.M.; Maazen, R.W.M. van der; Kappelle, A.C.; Herpen, C.M.L. van

    2007-01-01

    Two patients, a 58-year-old man and a 55-year-old woman, both under treatment for glioblastoma multiforme, were admitted with fever and neutropenia a few weeks after starting to take the oncolytic agent temozolomide. The man died of a cerebral haemorrhage against a background of severe thrombocytope

  8. Anti-diabetic potential of chloroform extract of flowers of Calotropis gigantea: An in vitro and in vivo study

    Directory of Open Access Journals (Sweden)

    N K Choudhary

    2011-01-01

    Full Text Available The chloroform extract of Calotropis gigantea flowers was evaluated for anti-diabetic activity in alloxan-induced hyperglycemia in vivo and inhibition of α-amylase and α-glucosidase in vitro. It was also intended to establish correlation between the serum marker antioxidant enzymes and diabetes. Diabetes was induced by a single intraperitoneal injection of alloxan monohydrate freshly prepared in a dose of 150 mg/kg. Chloroform extract showing presence of flavonoids was administered orally at the doses of 100 and 200 mg/kg for 21 consecutive days. Fasting blood glucose level, glycosylated haemoglobin, blood glutathione, serum creatinine kinase, serum lactate dehydrogenase levels as well as final change in body weight were evaluated. In vitro inhibition of carbohydrate digestive enzymes (α-amylase and α-glucosidase was also determined. Experimental findings showed moderately significant anti-diabetic potential of extract in terms of reduction of fasting glucose level in diabetic rats. The extract was found statistically significant in maintaining the level of serum marker antioxidant enzymes. Overall, the effect of chloroform extract particularly 200 mg/kg was moderate as compared to that of standard drug glibenclamide.

  9. Anti-diabetic effect of methanolic leaf extract of Pongamia pinnata on streptozotocin induced diabetic rats

    Institute of Scientific and Technical Information of China (English)

    Selvaraju Kavipriya; Narayanaswamy Tamilselvan; Thirunavukkarasu Thirumalai; Gangaipillai Arumugam

    2013-01-01

    Objective: To study the anti-diabetic effect of methanolic leaf extract of Pongamia pinnata (P. pinnata) on streptozotocin induced diabetic rats.Methods:Anti-diabetic activity of P. pinnata leaf extract at dosage of 500 mg/kg and 1 g/kg body weight was evaluated.Results:The levels of glucose, triglycerides, total cholesterol and serum glutamic pyruvic transaminase were significantly increased in streptozotocin induced diabetic rats when compared to that of the normal rats. After supplemented with plant extract, significant lower blood glucose level was recorded.Conclusions:The methanolic leaf extract of P. pinnata has been potent anti-diabetic effect in male albino rats.

  10. Comparison of oral ketamine and oral midazolam as sedative agents in pediatric dentistry

    Directory of Open Access Journals (Sweden)

    Damle S

    2008-09-01

    Full Text Available The safe and effective treatment of uncooperative or combative preschool children with extensive dental needs is one of pediatric dentist′s ongoing challenges. The traditional methods of behavior management are no longer acceptable to parents as they are not ready to spare more time for dental treatment of their children. Keeping this in mind, the present study was designed and carried out to evaluate the sedative effects of oral ketamine and oral midazolam prior to general anesthesia. Twenty uncooperative children in the age-group of 2-6 years were selected after thorough medical examination and investigations. Informed consent was obtained from the parent. This was a randomized double-blind study. An anesthesiologist administered either 0.5 mg/kg midazolam or 5 mg/kg ketamine orally. The heart rate, respiratory rate, and oxygen saturation were recorded at regular intervals. The sedation and anxiolysis scores were also recorded. The parents were asked to answer a questionnaire at the follow-up session the next day on the surgical experience of the parent and the child and side effects experienced, if any. When the data was subjected to statistical analysis, it was observed that both drugs resulted in adequate sedation at the end of 30 min, with oral midazolam providing significantly better anxiolysis. The heart rate and respiratory rate were marginally higher with oral ketamine. The questionnaire revealed a better response with oral midazolam; side effects were more prominent with oral ketamine.

  11. Management of oral Graft versus Host Disease with topical agents: A systematic review

    OpenAIRE

    Albuquerque, Rui; Khan, Zahid; Poveda, Ana; Higham, Jonathan; Richards, Andrea; Monteiro,Luís Silva; Jane Salas, Enric; López López, José, 1958-; Warnakulasuriya, Saman

    2015-01-01

    Background Oral Graft-versus-Host Disease (oGvHD) is a common complication of haematopoietic stem cell transplantation. Choosing the right topical application to be used intra orally can be a challenge. Consequently, the aim of this work is to review the effectiveness and safety of topical agents currently used in the management of the inflammatory mucosal lesions encountered in oGVHD. Material and Methods We carried out electronic searches of publications up to May 2015 of the databases Pubm...

  12. The role of diet on the clinical pharmacology of oral antineoplastic agents.

    Science.gov (United States)

    Ruggiero, Antonio; Cefalo, Maria G; Coccia, Paola; Mastrangelo, Stefano; Maurizi, Palma; Riccardi, Riccardo

    2012-02-01

    The number of oral anticancer agents has greatly increased in recent years. It is a well-known fact that food intake can induce significant variations in the bioavailability of these drugs. The aim of this review is to describe the interactions between diet and oral anticancer drugs in terms of the possible effects of such interactions on reducing the antineoplastic activity of the drug or increasing its side effects. This was an analytical study of the numerous mechanisms leading to changes in the bioavailability of oral antineoplastic agents due to diet. Food-drug interactions can induce a delay, decrease or increase in the absorption of the oral chemotherapeutic agent. The concomitant intake of food and antineoplastic drugs influence the pharmacokinetic and pharmacodynamic drug processes depending on the composition of the food consumed and the specific interactions of the food with transport mechanisms (p-glycoprotein, multidrug resistance proteins) and intestinal enzymatic systems (cytochrome P450). In prescribing an oral anticancer agent, clinicians must consider the possibility that the consumption of specific food items has the potential to interfere with the pharmacokinetics and pharmacodynamics of the prescribed drug.

  13. Systematic review of natural agents for the management of oral mucositis in cancer patients

    DEFF Research Database (Denmark)

    Yarom, Noam; Ariyawardana, Anura; Hovan, Allan

    2013-01-01

    Association of Supportive Care in Cancer/International Society for Oral Oncology. The body of evidence for each intervention, in each cancer treatment setting, was assigned an evidence level. Based on the evidence level, one of the following three guideline determinations was possible: recommendation......, suggestion, and no guideline possible. RESULTS: A total of 49 papers across 15 interventions were examined. A new suggestion was developed in favor of systemic zinc supplements administered orally in the prevention of oral mucositis in oral cancer patients receiving radiation therapy or chemoradiation (Level......Abstract PURPOSE: The aim of this study was to review the available literature and define clinical practice guidelines for the use of natural agents for the prevention and treatment of oral mucositis. METHODS: A systematic review was conducted by the Mucositis Study Group of the Multinational...

  14. Compositional analysis and in vivo anti-diabetic activity of wild Algerian Marrubium vulgare L. infusion.

    Science.gov (United States)

    Boudjelal, Amel; Henchiri, Cherifa; Siracusa, Laura; Sari, Madani; Ruberto, Giuseppe

    2012-03-01

    Marrubium vulgare (Lamiaceae) is a plant traditionally used for the treatment of diabetes in Algeria. Compositional analysis of the aqueous infusion revealed the presence of fifteen metabolites, all belonging to the class of polyphenols. Particularly, seven flavonoids have been detected, together with 5-caffeoylquinic (chlorogenic) acid in small amounts; the extract is dominated by the presence of a series of complex molecules, characterized as verbascoside (acteoside) derivatives. Concerning the anti-diabetic effectiveness a series of in vivo experiments were carried out on albinos Wistar rats. Diabetes was induced in the animals by intra-peritoneal injection of alloxane; they were treated twice a day with aqueous extract from aerial part infusion (100, 200 and 300 mg/kg body weight) and glibenclamide (5mg/kg body weight) for 15 days. Oral administration of 200 and 300 mg/kg body weight of aqueous extract the Marrubium vulgare induced an significant effect antidiabetic and antihyperlipidemic (dose-dependent effect). A decrease in blood glucose by 50% for the dose 100 mg/kg and more than 60% for doses 200 and 300 mg/kg, as well as a significant lowering of total lipids, triglycerides, and total cholesterol levels in treated animals, compared with diabetic controls group (p<0.001), have been observed. Glibenclamide was used as reference and showed similar effects.

  15. Development and phytochemical characterization of high polyphenol red lettuce with anti-diabetic properties.

    Directory of Open Access Journals (Sweden)

    Diana M Cheng

    Full Text Available Polyphenol-rich Rutgers Scarlet Lettuce (RSL (Lactuca sativa L. was developed through somaclonal variation and selection in tissue culture. RSL may contain among the highest reported contents of polyphenols and antioxidants in the category of common fruits and vegetables (95.6 mg/g dry weight and 8.7 mg/g fresh weight gallic acid equivalents and 2721 µmol/g dry weight and 223 µmol/g fresh weight Trolox equivalents. Three main compounds accumulate at particularly high levels in RSL: chlorogenic acid, up to 27.6 mg/g dry weight, cyanidin malonyl-glucoside, up to 20.5 mg/g dry weight, and quercetin malonyl-glucoside, up to 35.7 mg/g dry weight. Major polyphenolic constituents of RSL have been associated with health promotion as well as anti-diabetic and/or anti-inflammatory activities. Daily oral administration of RSL (100 or 300 mg/kg for up to eight days acutely reduced hyperglycemia and improved insulin sensitivity in high fat diet-induced obese hyperglycemic mice compared to vehicle (water control. Data presented here support possible use of RSL as a functional food for the dietary management of diabetes.

  16. Anti-diabetic properties of Momordica charantia L. polysaccharide in alloxan-induced diabetic mice.

    Science.gov (United States)

    Xu, Xin; Shan, Bin; Liao, Cai-Hu; Xie, Jian-Hua; Wen, Ping-Wei; Shi, Jia-Yi

    2015-11-01

    A water-soluble polysaccharide (MCP) was isolated from the fruits of Momordica charantia L., and the hypoglycemic effects of MCP were investigated in both normal healthy and alloxan-induced diabetic mice. MCP was orally administered once a day after 3 days of alloxan-induction at 100, 200 and 300mg/kg body weight for 28 day. Results showed that fasting blood glucose level (BGL) was significantly decreased, whereas the glucose tolerance was marked improvement in alloxan-induced diabetic mice, and loss in body weight was also prevented in diabetic mice compared to the diabetic control group. The dosage of 300mg/kg body weight exhibited the best effects. In addition, MCP did not exhibit any toxic symptoms in the limited toxicity evaluation in mice. The results suggest that MCP possess significantly dose-dependent anti-diabetic activity on alloxan-induced diabetic mice. Hence, MCP can be incorporated as a supplement in health-care food, drugs and/or combined with other hypoglycemic drugs. Copyright © 2015 Elsevier B.V. All rights reserved.

  17. Oral (Systemic) Botanical Agents for the Treatment of Psoriasis: A Review.

    Science.gov (United States)

    Farahnik, Benjamin; Sharma, Divya; Alban, Joseph; Sivamani, Raja

    2017-06-01

    Patients with psoriasis often use botanical therapies as part of their treatment. It is important for clinicians to be aware of the current evidence regarding these agents as they treat patients. A systematic literature search was conducted using the PubMed, MEDLINE, and EMBASE database for randomized clinical trials assessing the use of botanical therapeutics for psoriasis. The search included the following keywords: "psoriasis" and "plant" or "herbal" or "botanical." Citations within articles were also reviewed to identify relevant sources. The results were then further refined by route of administration, and the oral (systemic) botanical agents are reviewed herein. A total of 12 controlled and uncontrolled clinical trials addressing the use of oral, systemic botanical agents for psoriasis were assessed in this review. While overall evidence is limited in quantity and quality, HESA-A, curcumin, neem extract, and, to a lesser degree, Traditional Chinese Medicine seem to be the most efficacious agents. The literature addresses a large amount of studies in regards to botanicals for the treatment of psoriasis. While most agents appear to be safe, further research is necessary for evidence-based recommendation of oral botanical agents to psoriasis patients.

  18. Anti-diabetic activity-guided screening of aqueous-ethanol Moringa ...

    African Journals Online (AJOL)

    1School of Pharmaceutical Sciences, Universiti Sains Malaysia, Pulau Pinang, Malaysia, 2Faculty of Pharmacy, ... increasing among Malaysians, reaching 23.8 % ... (Roche,. ACCU-CHEK. Performa no. 55404068967). Anti-diabetic studies.

  19. Anti-diabetic activity of crude Pistacia lentiscus in alloxan-induced diabetes in rats

    OpenAIRE

    Muhammad Saad Ur Rehman; Sairah Hafeez Kamran; Mobasher Ahmad; Usman Akhtar

    2015-01-01

    The purpose of this study was to investigate the anti-diabetic effect of crude Pistacia lentiscus gum (mastic gum) in alloxan-treated diabetic rat model. The crude P. lentiscus (100 mg/kg) showed significant (p

  20. The anti-diabetic effects and pharmacokinetic profiles of berberine in mice treated with Jiao-Tai-Wan and its compatibility.

    Science.gov (United States)

    Chen, Guang; Lu, Fuer; Xu, Lijun; Dong, Hui; Yi, Ping; Wang, Fang; Huang, Zhaoyi; Zou, Xin

    2013-07-15

    Jiao-Tai-Wan (JTW), a classical Chinese prescription, has been clinically employed to treat diabetes mellitus in recent years. To investigate the comparative evaluations on anti-diabetic effects and pharmacokinetics of the active ingredient berberine in mice treated with JTW in various combinations of its constituent herbs. In our study, the anti-diabetic study was carried out in diabetic mice induced by intraperitoneal injection of streptozotocin. The diabetic mice were randomly assigned to three therapy groups and orally administered with different prescription proportions of Rhizoma Coptidis and Cinnamomum cassia respectively. The level of plasma glucose, lipid profile and parameters related to oxidative stress were determined. The concentrations of berberine in non-diabetic mice plasma were determined using HPLC, and main pharmacokinetic parameters were investigated. The results indicated that the compatibility effects of ingredients present in Cinnamomum cassia could affect the anti-diabetic ability and pharmacokinetics of berberine in JTW. Copyright © 2013 Elsevier GmbH. All rights reserved.

  1. Screening and design of anti-diabetic compounds sourced from the leaves of neem (Azadirachta indica)

    OpenAIRE

    2013-01-01

    Diabetes Mellitus is affecting people of all age groups worldwide. Many synthetic medicines available for type 2 diabetes mellitus in the market. However, there is a strong requirement for the development of better anti-diabetes compounds sourced especially from natural sources like medicinal plants. The extracts from the leaves of neem (Azadirachta indica) is traditionally known to have anti-diabetes properties. Therefore, there is an increased interest to identify potential compounds identi...

  2. Interactions between oral antineoplastic agents and concomitant medication: a systematic review.

    Science.gov (United States)

    Carcelero, Esther; Anglada, Helena; Tuset, Montse; Creus, Natalia

    2013-05-01

    In recent years, the number of oral antitumoral agents has considerably increased. Oral administration increases the risk of interactions, because most oral anticancer drugs are taken on a daily basis. Interactions can increase exposure to antitumoral agents or cause treatment failure. Many antitumoral drugs undergo enzymatic metabolism by cytochrome P450. As some act as inducers or inhibitors of one or more isoenzymes, they can lead to decreases or increases in plasma concentrations of concomitant drugs. Hence, cytostatic drugs can act not only as victims but also as perpetrators. P-glycoprotein, an efflux transporter, can also be involved in pharmacokinetic interactions. A Medline search was performed to summarize the available evidence of the most clinically relevant interactions between oral chemotherapy agents and other drugs. The search covered the period from 1966 until August 2012 for each antitumoral drug using the medical subject headings 'Drug Interactions' OR 'Pharmacokinetics'. While the present review is not exhaustive, it aims to increase clinicians' awareness of potential drug-drug interactions. As cancer patients are often polymedicated and treated by different physicians, the risk of drug interactions between antitumoral agents and other medications is high. More clinical interaction studies are encouraged to ensure appropriate antineoplastic pharmacokinetics in clinical practice.

  3. Systematic review of anti-inflammatory agents for the management of oral mucositis in cancer patients

    NARCIS (Netherlands)

    Nicolatou-Galitis, Ourania; Sarri, Triantafyllia; Bowen, Joanne; Di Palma, Mario; Kouloulias, Vassilios E.; Niscola, Pasquale; Riesenbeck, Dorothea; Stokman, Monique; Tissing, Wim; Yeoh, Eric; Elad, Sharon; Lalla, Rajesh V.

    2013-01-01

    Purpose The aim of this project was to review the available literature and define clinical practice guidelines for the use of anti-inflammatory agents for the prevention and treatment of oral mucositis in cancer patients. Materials and methods A systematic review was conducted by the Mucositis Study

  4. Topical Hemostatic Agents: What the Oral and Maxillofacial Surgeon Needs to Know.

    Science.gov (United States)

    Vezeau, Patrick J

    2016-11-01

    Hemostasis is a key step in safe and predictable surgery. Knowledge of normal blood clotting mechanisms and abnormal diathesis is necessary to anticipate potential problems during and after surgery. As an adjunct to bleeding control, topical hemostatic agents have long been used in all surgical disciplines. This article provides a brief review of hemostasis and a topical summary of different classes of topical hemostatic agents useful to oral and maxillofacial surgery, including indications and potential complications/side effects. This rapidly evolving field promises to yield future agents with increased efficacy, cost efficiency, and decreased complications. Copyright © 2016 Elsevier Inc. All rights reserved.

  5. Comparative study of the effects of two bleaching agents on oral microbiota.

    Science.gov (United States)

    Alkmin, Yara Tardelli; Sartorelli, Renata; Flório, Flávia Martão; Basting, Roberta Tarkany

    2005-01-01

    This study evaluated the in vivo effects of bleaching agents containing 10% carbamide peroxide (Platinum/Colgate) or 7.5% hydrogen peroxide (Day White 2Z/Discus Dental) on mutans Streptococcus during dental bleaching. The products were applied on 30 volunteers who needed dental bleaching. In each volunteer, one of the two bleaching agents was used on both dental arches one hour a day for three weeks. Analysis of the bacterial counts was made by collecting saliva before (baseline values), during (7 and 21 days) bleaching treatments and 14 days posttreatment. The Friedman non-parametric analysis (alpha=0.05) found no differences in microorganism counts at different times for each group for both agents (p>0.05). The Mann Whitney nonparametric test (alpha=0.05) showed no differences in micro-organism counts for both agents (p>0.05). Different bleaching agents did not change the oral cavity mutans Streptococcus counts.

  6. Effects of oral contraceptive agents and sex steroids on carbohydrate metabolism.

    Science.gov (United States)

    Kalkhoff, R K

    1972-01-01

    The article offers a general interpretation of the influence of oral contraceptive agents on glucose tolerance, emphasizing comparisons of synthetic sex hormones. Although there are conflicting reports on steroid-induced diabetes in normal women, their glucose curves are often higher when under oral contraceptive treatment, suggesting that oral contraceptives may induce a form of subclinical diabetes melitus that is reversible. Evidence from diabetic women suggests definite deliterious effects from contraceptive administration. Estradiol, estriol, and estrone may improve glucose tolerance in nondiabetic women and reduce insulin requirements in diabetics. Progesterone has little effect on carbohydrate tolerance, as did synthetic progestin. Conjugated equine estrogens (equilenine or Premarin) may provoke mild to moderate deterioration of carbohydrate tolerance. Parenterally administered natural estrogens and orally administered synthetic derivatives appear to differ sharply in their effects. Sex hormones' effects on carbohydrate metabolism likely involve interactions with insulin and endogenous glucocorticoids.

  7. Insulin versus oral agents in the management of Cystic Fibrosis Related Diabetes: a case based study

    Directory of Open Access Journals (Sweden)

    Langdon Leora J

    2006-06-01

    Full Text Available Abstract Background Insulin is the recommend therapeutic agent of choice for the management of Cystic Fibrosis Related Diabetes (CFRD, despite only sub-optimal reductions in glycemic control and increased morbidity and mortality reported by centers using this agent. The newer insulin sensitizing agents demonstrated to have anti-inflammatory mechanisms may provide an alternative management option for CFRD. Methods A prospective case based therapeutic comparison between insulin, sulfonylurea, metformin and thiazolidinedione was observed over one decade with 20 CFRD patients diagnosed using American Diabetes Association guideline standards. Patients entering the study elected treatment based on risk and benefit information provided for treatment options. Patients receiving organ transplant or requiring combination diabetic medications were excluded from the study. Results No statistical advantage was achieved regarding overall glycemic control for oral agents over insulin. Additional outcome measures including changes in weight, liver function testing and FEV1 were not statistically significant. Conclusion Insulin alone may not be the only therapeutic option in managing CFRD. Oral hypoglycemic agents were equally effective in treating CFRD and may provide an alternative class of agents for patients reluctant in using insulin.

  8. Systematic review of miscellaneous agents for the management of oral mucositis in cancer patients

    DEFF Research Database (Denmark)

    Jensen, Siri Beier; Jarvis, Virginia; Zadik, Yehuda

    2013-01-01

    : A total of 32 papers across 10 interventions were examined. New suggestions were developed against the use of systemic pilocarpine administered orally for prevention of OM during RT in head and neck cancer patients and in patients receiving high-dose chemotherapy, with or without total body irradiation......, prior to hematopoietic stem cell transplantation. A suggestion was also made against the use of systemic pentoxifylline administered orally for the prevention of OM in patients undergoing bone marrow transplantation. No guideline was possible for any other agent reviewed due to inadequate and...

  9. Experimental Transmission of the Chronic Wasting Disease Agent to Swine after Oral or Intracranial Inoculation.

    Science.gov (United States)

    Moore, S Jo; West Greenlee, M Heather; Kondru, Naveen; Manne, Sireesha; Smith, Jodi D; Kunkle, Robert A; Kanthasamy, Anumantha; Greenlee, Justin J

    2017-10-01

    Chronic wasting disease (CWD) is a naturally occurring, fatal neurodegenerative disease of cervids. The potential for swine to serve as hosts for the agent of CWD is unknown. The purpose of this study was to investigate the susceptibility of swine to the CWD agent following experimental oral or intracranial inoculation. Crossbred piglets were assigned to three groups, intracranially inoculated (n = 20), orally inoculated (n = 19), and noninoculated (n = 9). At approximately the age at which commercial pigs reach market weight, half of the pigs in each group were culled ("market weight" groups). The remaining pigs ("aged" groups) were allowed to incubate for up to 73 months postinoculation (mpi). Tissues collected at necropsy were examined for disease-associated prion protein (PrP(Sc)) by Western blotting (WB), antigen capture enzyme immunoassay (EIA), immunohistochemistry (IHC), and in vitro real-time quaking-induced conversion (RT-QuIC). Brain samples from selected pigs were also bioassayed in mice expressing porcine prion protein. Four intracranially inoculated aged pigs and one orally inoculated aged pig were positive by EIA, IHC, and/or WB. By RT-QuIC, PrP(Sc) was detected in lymphoid and/or brain tissue from one or more pigs in each inoculated group. The bioassay was positive in four out of five pigs assayed. This study demonstrates that pigs can support low-level amplification of CWD prions, although the species barrier to CWD infection is relatively high. However, detection of infectivity in orally inoculated pigs with a mouse bioassay raises the possibility that naturally exposed pigs could act as a reservoir of CWD infectivity.IMPORTANCE We challenged domestic swine with the chronic wasting disease agent by inoculation directly into the brain (intracranially) or by oral gavage (orally). Disease-associated prion protein (PrP(Sc)) was detected in brain and lymphoid tissues from intracranially and orally inoculated pigs as early as 8 months of age (6 months

  10. Oral hypoglycaemic agents, insulin resistance and cardiovascular disease in patients with type 2 diabetes

    DEFF Research Database (Denmark)

    Hemmingsen, Bianca; Lund, Søren S; Wetterslev, Jørn

    2009-01-01

    This article is a narrative review of the current evidence of the effects on cardiovascular disease (CVD) of oral hypoglycaemic agents that increase insulin sensitivity in patients with type 2 diabetes (T2D). In overweight T2D patients, metformin has been demonstrated to reduce CVD risk, and this......This article is a narrative review of the current evidence of the effects on cardiovascular disease (CVD) of oral hypoglycaemic agents that increase insulin sensitivity in patients with type 2 diabetes (T2D). In overweight T2D patients, metformin has been demonstrated to reduce CVD risk......, and this beneficial effect may be conserved with the combination of metformin and insulin treatment. However, the effect of glitazones on CVD is uncertain. There is conflicting evidence from large randomized trials to support a protective effect against CVD of lowering blood glucose per se but a systematic review...

  11. Review of atrial fibrillation outcome trials of oral anticoagulant and antiplatelet agents.

    Science.gov (United States)

    Bassand, Jean-Pierre

    2012-03-01

    Atrial fibrillation (AF) is strongly associated with cardioembolic stroke, and thromboprophylaxis is an established means of reducing stroke risk in patients with AF. Oral vitamin K antagonists such as warfarin have been the mainstay of therapy for stroke prevention in patients with AF. However, they are associated with a number of limitations, including excessive bleeding when not adequately controlled. Antiplatelet agents do not match vitamin K antagonists in terms of their preventive efficacy. Dual-antiplatelet therapy (clopidogrel and acetylsalicylic acid) or combined antiplatelet-vitamin K antagonist therapy in AF has also failed to provide convincing evidence of their additional benefit over vitamin K antagonists alone. Novel oral anticoagulants, including the direct thrombin inhibitor dabigatran and direct Factor Xa inhibitors such as rivaroxaban, apixaban, and edoxaban, have now been approved or are currently in late-stage clinical development in AF. These newer agents may provide a breakthrough in the optimal management of stroke risk.

  12. [Reflections around the performance of community health agents in oral health strategies].

    Science.gov (United States)

    de Holanda, Ana Larissa Fernandes; Barbosa, Aldenísia Alves de Albuquerque; Brito, Ewerton William Gomes

    2009-10-01

    The Community Health Agent (CHA) has traditionally been linked to doctors and nurses, being considered exclusive 'property' of these professionals. Historically, oral health tended to operate isolated, disconnecting the mouth from the rest of the body and the individual from his environment. The Family Health Program (FHP) points to important changes in the organization of services as well as in the work process. One of the differences is the teamwork joining different professionals, including oral health which was previously excluded. The objective of the study is to show the experience of the CHA qualifying course, which allowed the entrance of different professional categories into teaching. The course included three odontologists as lecturers, and CHA recognized other individuals as health team members, as well as expand the view of its role within oral health. The professors also had their practices modified, given that they could understand the often ignored suffering and limitations of the CHAs.

  13. Herbal oral gel induced contact stomatitis along with desquamative gingivitis due to a coloring agent

    Directory of Open Access Journals (Sweden)

    Baljeet Singh

    2015-01-01

    Full Text Available Report of a rare case of contact stomatitis manifesting as irregular erosions partially covered with pseudomembrane along with desquamative gingivitis in a 32-year-old female patient is presented. The patient was otherwise healthy and not taking any medication. She gave the history of using curcumin-based oral gel 2 days back. Allergy test to curcumin oral gel was found to be positive, which on detailed allergy testing proved to be the coloring agent, erythrosine present in the gel. Contrary to the popular belief some folk medicine preparations can lead to unwanted side effects due to the antigenic potential of ingredients present in them. In addition, every clinician, during differential diagnosis of oral lesions must bear in mind unwanted reactions to any local ointment.

  14. Herbal oral gel induced contact stomatitis along with desquamative gingivitis due to a coloring agent.

    Science.gov (United States)

    Singh, Baljeet; Sharma, Alka; Garg, Avnika

    2015-01-01

    Report of a rare case of contact stomatitis manifesting as irregular erosions partially covered with pseudomembrane along with desquamative gingivitis in a 32-year-old female patient is presented. The patient was otherwise healthy and not taking any medication. She gave the history of using curcumin-based oral gel 2 days back. Allergy test to curcumin oral gel was found to be positive, which on detailed allergy testing proved to be the coloring agent, erythrosine present in the gel. Contrary to the popular belief some folk medicine preparations can lead to unwanted side effects due to the antigenic potential of ingredients present in them. In addition, every clinician, during differential diagnosis of oral lesions must bear in mind unwanted reactions to any local ointment.

  15. Pharmacogenetics in type 2 diabetes: influence on response to oral hypoglycemic agents

    OpenAIRE

    Dawed AY; Zhou K.; Pearson ER

    2016-01-01

    Adem Yesuf Dawed, Kaixin Zhou, Ewan Robert Pearson  Division of Cardiovascular and Diabetes Medicine, Medical Research Institute, University of Dundee, Dundee, Scotland, UK Abstract: Type 2 diabetes is one of the leading causes of morbidity and mortality, consuming a significant proportion of public health spending. Oral hypoglycemic agents (OHAs) are the frontline treatment approaches after lifestyle changes. However, huge interindividual variation in response to OHAs resu...

  16. Computed tomography enterography: a comparison of different neutral oral contrast agents

    Energy Technology Data Exchange (ETDEWEB)

    D' Ippolito, Giuseppe, E-mail: giuseppe_dr@uol.com.br [Department of Imaging Diagnosis, Universidade Federal de Sao Paulo (UNIFESP), Sao Paulo, SP (Brazil); Braga, Fernanda Angeli; Resende, Marcelo Cardoso; Bretas, Elisa Almeida Sathler; Nunes, Thiago Franchi; Rosas, George de Queiroz; Tiferes, Dario Arie [Abdominal Imaging Section, Department of Imaging Diagnosis - Universidade Federal de Sao Paulo (Unifesp), Sao Paulo, SP (Brazil)

    2012-05-15

    Objective: The purpose of this study was to assess the performance of neutral oral contrast agents, comparing intestinal distension, distinction of intestinal wall, acceptance and side effects. Materials and Methods: Prospective, randomized, and double-blinded study involving 30 patients who underwent computed tomography of abdomen and pelvis with administration of neutral oral contrast agents, divided into three groups according the contrast agent type: milk, water, and polyethylene glycol. The images were consensually analyzed by two observers, considering the degree of bowel distension and intestinal wall distinction. The patients responded to a questionnaire regarding the taste of the ingested solution and on their side effects. Kruskal-Wallis and chi-square tests were employed for statistical analysis. Results: Among 40 studied intestinal segments, appropriate bowel distension (intestinal loop diameter > 2 cm) was observed in 14 segments (35%) in the milk group, 10 segments (25%) in the water group and 23 segments (57%) in the polyethylene glycol group (p = 0.01). Preparation with polyethylene glycol resulted in the best bowel distension, but it presented the worst taste and highest incidence of diarrhea as reported by patients. Conclusion: Bowel preparation with oral polyethylene glycol results in higher degree of bowel distension than with water or milk, but presents worst acceptance related to its taste and frequency of diarrhea as a side effect. (author)

  17. Evaluation of anti-diabetic activity of Glucova Active Tablet on Type I and Type II diabetic model in rats

    Directory of Open Access Journals (Sweden)

    Hardik Soni

    2014-01-01

    Full Text Available Background: Glucova Active Tablet is a proprietary Ayurvedic formulation with ingredients reported for anti-hyperglycemic, anti-hyperlipidemic activity and antioxidant properties. Objective: Evaluation of anti-diabetic activity of Glucova Active Tablet on Type I and Type II diabetic model in rats. Materials and Methods: Experimental Type I diabetes was induced in 24 albino rats with intra-peritoneal injection of streptozotocin (50 mg/kg. Type II diabetes was induced in 18 albino rats by intra-peritoneal injection of streptozotocin (35 mg/kg along with high fat diet. The rats were divided in 5 groups for Type I model and 4 groups for Type II model. Normal control group was kept common for both experimental models. Glucova Active Tablet (108 mg/kg treatment was provided for 28 days twice daily orally. Fasting blood glucose level, serum lipid profile and liver anti-oxidant parameters like superoxide dismutase and reduced glutathione was carried out in both experimental models. Pancreas histopathology was also done. Statistical analysis were done by ′analysis of variance′ test followed by post hoc Tukey′s test, with significant level of P < 0.05.Results and Discussion: Glucova Active Tablet showed significant effect on fasting blood glucose level. It also showed significant alteration in lipid profile and antioxidant parameters. Histopathology study revealed restoration of beta cells in pancreas in Glucova Active Tablet treated group. Conclusion: Finding of this study concludes that Glucova Active Tablet has shown promising anti-diabetic activity in Type I and Type II diabetic rats. It was also found showing good anti-hyperlipidemic activity and anti-oxidant property.

  18. Evaluation of anti-diabetic activity of Glucova Active Tablet on Type I and Type II diabetic model in rats

    Science.gov (United States)

    Soni, Hardik; Patel, Sejal; Patel, Ghanshyam; Paranjape, Archana

    2014-01-01

    Background: Glucova Active Tablet is a proprietary Ayurvedic formulation with ingredients reported for anti-hyperglycemic, anti-hyperlipidemic activity and antioxidant properties. Objective: Evaluation of anti-diabetic activity of Glucova Active Tablet on Type I and Type II diabetic model in rats. Materials and Methods: Experimental Type I diabetes was induced in 24 albino rats with intra-peritoneal injection of streptozotocin (50 mg/kg). Type II diabetes was induced in 18 albino rats by intra-peritoneal injection of streptozotocin (35 mg/kg) along with high fat diet. The rats were divided in 5 groups for Type I model and 4 groups for Type II model. Normal control group was kept common for both experimental models. Glucova Active Tablet (108 mg/kg) treatment was provided for 28 days twice daily orally. Fasting blood glucose level, serum lipid profile and liver anti-oxidant parameters like superoxide dismutase and reduced glutathione was carried out in both experimental models. Pancreas histopathology was also done. Statistical analysis were done by ‘analysis of variance’ test followed by post hoc Tukey's test, with significant level of P < 0.05. Results and Discussion: Glucova Active Tablet showed significant effect on fasting blood glucose level. It also showed significant alteration in lipid profile and antioxidant parameters. Histopathology study revealed restoration of beta cells in pancreas in Glucova Active Tablet treated group. Conclusion: Finding of this study concludes that Glucova Active Tablet has shown promising anti-diabetic activity in Type I and Type II diabetic rats. It was also found showing good anti-hyperlipidemic activity and anti-oxidant property. PMID:24948860

  19. Uso de anti-hipertensivos e antidiabéticos por idosos: inquérito em Belo Horizonte, Minas Gerais, Brasil Use of anti-hypertensive and anti-diabetic drugs by the elderly: a survey in Belo Horizonte, Minas Gerais State, Brazil

    Directory of Open Access Journals (Sweden)

    Mônica de Fátima Gontijo

    2012-07-01

    Full Text Available A preocupação com efeitos prejudiciais do uso de medicamentos por idosos tem motivado estudos com o objetivo de identificar problemas nessa utilização. Realizou-se um inquérito domiciliar entre aposentados, com idade > 60 anos, residentes em Belo Horizonte, Minas Gerais, Brasil (2003, que declararam ter diabetes ou hipertensão arterial. A qualidade do uso de medicamentos anti-hipertensivos e antidiabéticos foi avaliada com base em redundância, associações medicamentosas e fármacos inapropriados. Entre os 283 (89% idosos autodeclarados hipertensos, em uso de farmacoterapia, 68,2% utilizavam diuréticos, e 37,8% utilizavam IECA. Entre os 22 (64,7% autodeclarados diabéticos sob farmacoterapia, 45,5% utilizavam insulina, e 77,3%, antidiabéticos orais. Entre os 89 autodeclarados diabéticos hipertensos, 80 (90% utilizavam anti-hipertensivos, e 51 (57,3%, antidiabéticos. Observou-se o uso de associações medicamentosas, medicamentos redundantes ou inadequados, o que indica a necessidade de seguimento de protocolos terapêuticos e maior atenção à saúde dos pacientes idosos.Concern over the harmful effects of drug use by the elderly has motivated studies aimed at identifying problems in such utilization. This was a household survey with retirees aged > 60 years living in Belo Horizonte, Minas Gerais State, Brazil, in 2003, who reported having a diagnosis of diabetes and/or hypertension. Quality of anti-hypertensive and anti-diabetic medication was measured by redundancy, combinations of drugs, and inappropriate drugs. Among 283 elderly patients (89% with self-reported hypertension and use of anti-hypertensive pharmacotherapy, 68.2% were using diuretics and 37.8% ACE inhibitors. Among the 22 (64.7% self-reported diabetic patients under pharmacotherapy, 45.5% were using insulin and 77.3% oral anti-diabetic agents. Among the 89 self-reported diabetic and hypertensive patients, 80 (90% were using anti-hypertensive drugs and 51 (57.3% anti-diabetic

  20. Anti-diabetic related health food properties of traditional rice (Oryza sativa L.) in Sri Lanka

    Institute of Scientific and Technical Information of China (English)

    Wanigasekara Daya Ratnasooriya; Muhammad Iqbal Choudhary; Kourosh Dalvandi

    2015-01-01

    Objective:To evaluate a range of anti-diabetic related properties and some consumer preferred physicochemical properties of selected Sri Lankan traditional rice varieties. Methods: Sudu Heeneti, Goda Heeneti, Masuran and Dik Wee varieties were used in this study. Anti-diabetic related properties of bran extracts of selected varieties were studied for methylglyoxal mediated protein glycation inhibition, acetyl and butyryl-cholinesterase inhibitionin vitro and anti-hyperglycemic activityin vivo. Further, selected varieties were studied for starch hydrolysis ratein vitro. Physicochemical properties including grain color, size, shape, crude protein, crude fat, ash, dietary fiber and total carbohydrate contents were studied. Results: Brans of selected varieties had significant (P Conclusions: It is concluded that selected varieties could be promoted as physicochemically sound rices with a range of anti-diabetic related properties in the management of diabetes and its complications.

  1. Difficult to swallow: issues affecting optimal adherence to oral anticancer agents.

    Science.gov (United States)

    Cheung, Winson Y

    2013-01-01

    The number of anticancer drugs currently available in oral formulation has increased dramatically over the past 15 to 20 years, especially with the recent development of new hormonal and targeted therapies. At present, approximately 25% of all cancer drugs are available in oral formulation, with numbers expected to increase exponentially in the coming years. The convenience associated with the self-administration of oral therapy, the requirement of fewer trips to the physician's office, and the lack of infusion reactions are all benefits for patients, allowing them to potentially maintain their relative independence while undergoing active anticancer treatment. On the other hand, there are growing concerns regarding patients' poor adherence to oral therapy as well as the challenges of monitoring patient compliance when treatment administration does not occur in the presence of health care professional (HCPs). More importantly, poor adherence to proven therapies may detrimentally affect the patients' clinical outcomes, such as survival. Thus, there is an urgent need to identify more effective strategies to measure and monitor adherence to oral anticancer agents in an effort to maximize their therapeutic benefits.

  2. Adherence and patients' experiences with the use of oral anticancer agents.

    Science.gov (United States)

    Timmers, Lonneke; Boons, Christel C L M; Kropff, Femke; van de Ven, Peter M; Swart, Eleonora L; Smit, Egbert F; Zweegman, Sonja; Kroep, Judith R; Timmer-Bonte, Johanna N H; Boven, Epie; Hugtenburg, Jacqueline G

    2014-02-01

    A rapidly growing number of oral anticancer agents has become available in oncology and hematology. Though these introductions have several benefits, medication adherence is an issue of concern. Little is known about the factors influencing adherence to treatment with oral anticancer agents in daily practice. Material and methods. In this observational, multicenter study including 216 patients, carried out between October 2010 and March 2012, the use of oral anticancer drugs was assessed by means of a telephonic pill count, a questionnaire and a review of the patient's medical file and pharmacy medication records. Parameters collected were patients' demographics, treatment characteristics, beliefs and attitude towards disease and medicines, self-reported adherence, side effects, quality of life and satisfaction about information. Patients off treatment filled out a questionnaire about the reasons for discontinuation. Optimal adherence was defined as ≥ 95%-≤ 105%. Results. The mean adherence rate (AR) (n = 177) was 99.1% with 20.3% of patients having a sub-optimal AR ( 105%) consisting both of under- and over-adherence. Multivariate analyses showed that being on a cyclic dosing regimen (rather than a continuous regimen), not living alone and being highly educated increased the chances of optimal adherence (ORs = 4.88, 4.59 and 2.53, respectively). In addition, optimal adherence was found to be less common in patients reporting treatment control (OR = 0.77). One third of 79 patients off treatment reported their experienced side effects as one of the reasons for discontinuation. Discussion. Although most patients are fully adherent to oral anticancer agents, there is a substantial number tending to non-adherence. Patients living alone and those on a continuous dosing regimen are most likely to adhere sub-optimally. Interventions to improve adherence should specifically address these patients and be tailored to the needs of the individual patient.

  3. Management of Antithrombotic Agents in Oral Surgery Maria Martinez and Dimitrios A. Tsakiris *

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    Maria Martinez

    2015-10-01

    Full Text Available Systemic anticoagulation with intravenous or oral anticoagulants and antiplatelet agents is an efficient treatment against thromboembolic or cardiovascular disease. Invasive dental procedures or oral surgery might be associated with bleeding complications if carried out under anticoagulants. Patients on vitamin K antagonists, new direct anticoagulants or antiplatelet agents having dental interventions with low-risk for bleeding do not need interruption of anticoagulation. In case of bleeding complications local hemostatic measures, such as local surgical sutures, fibrin glue, local antifibrinolytic treatment with tranexamic acid, or e-aminocaproic acid suffice to stop bleeding. In patients with high risk of bleeding an individual assessment of the benefit/risk ratio of interrupting anticoagulation should be carried out. Bridging the long-term anticoagulation with short-term anticoagulants should be planned according to national or international guidelines. The introduction of the newer direct oral anticoagulants having more flexible pharmacokinetic properties has facilitated bridging, allowing short-term interruption without increasing the risk of relapsing thrombotic or cardiovascular events.

  4. Anti-diabetic property of ethanolic extract of Andrographis paniculata in streptozotocin-diabetic rats

    Institute of Scientific and Technical Information of China (English)

    Xiang-Fan ZHANG; Benny Kwong-Huat TAN

    2000-01-01

    AIM: To investigate the anti-diabetic effect of a crude ethanolic extract of Andrographis paniculata in normal and streptozotocin ( STZ )-induced diabetic rats.METHODS & RESULTS: Oral administration of the extract at different doses (0.1, 0.2, and 0.4 g/body weight) significantly reduced the fasting serum glucose level in STZ-diabetic rats compared to the vehicle ( distilled water), but not in normal rots. This effect was dose-dependent. A similar result was seen with metfomnin (0.5 g/body weight). In the glucose tolerance test, an oral administration of the extract at the same doses suppressed the elevated glucose level in normal and diabetic rots, as did mefformin. The effects were also dose-respondent. In the long-term experiment, the extract ( 0.4 g/body weight ), mefformin ( 0.5 gz/body weight), and vehicle were given twice daily to diabetic rats for 14 d. On d 15, fasting serum glucose levels were found to be significantly lower in the extract-and mefformin-treated groups ( P<0.001 ) than in the vehicle-treated group. The mean food and water intakes over 14 days were significantly lower in the extract-treated group ( P < 0.05, P < 0.01, respectively) and also in the mefformin-treated group (both P < 0.001 ) when compared to the vehicle-treated group. No significant change in insulin level was observed among the 3 groups of diabetic rats. The extract, like mefformin, maintained the leptin levels after 14-d treatment, whereas this level was significantly decreased ( P < 0.05) in the vehicle-treated group. The activity of hepatic glucose-6-phosphatase (G-6-Pase) was significantly reduced by the extract as well as by mefformin (both P < 0.05). No significant difference in hepatic glycogen stores was noted among the 3 groups. The extract caused 49.8 % reduction of fasting serum triglyceride levels, compared to 27.7 % with metformin. However, neither the extract nor mefformin significantly affected serum cholesterol level. CONCLUSION: The ethanolic

  5. Pineapple juice as a negative oral contrast agent in magnetic resonance cholangiopancreatography: a preliminary evaluation.

    Science.gov (United States)

    Riordan, R D; Khonsari, M; Jeffries, J; Maskell, G F; Cook, P G

    2004-12-01

    The quality of magnetic resonance cholangiopancreatography (MRCP) images is frequently degraded by high signal from the gastrointestinal tract. The aim of this study is to evaluate pineapple juice (PJ) as an oral negative contrast agent in MRCP. Preliminary in vitro evaluation demonstrated that PJ shortened T(2) relaxation time and hence decreased T(2) signal intensity on a standard MRCP sequence to a similar degree to a commercially available negative contrast agent (ferumoxsil). Electrothermal atomic absorption spectrometry assay demonstrated a high manganese concentration in PJ of 2.76 mg dl(-1), which is likely to be responsible for its T(2) imaging properties. MRCP was subsequently performed in 10 healthy volunteers, before and at 15 min and 30 min following ingestion of 400 ml of PJ. Images were assessed blindly by two Consultant Radiologists using a standard grading technique based on contrast effect (degree of suppression of bowel signal), and image effect (diagnostic quality). There were statistically significant improvements in contrast and image effect between pre and post PJ images. There was particularly significant improvement in visualization of the pancreatic duct, but no significant difference between 15 min and 30 min post PJ images. Visualization of the ampulla, common bile duct, common hepatic and central intrahepatic ducts were also significantly improved at 15 min following PJ. Our results demonstrate that PJ, may be used as an alternative to commercially available negative oral contrast agent in MRCP.

  6. Pattern of anti-diabetic drugs prescribed in a tertiary care hospital of Bangladesh

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    Zuhayer Ahmed

    2016-02-01

    Conclusions: The findings can serve as a guide to choose the formulation and combination of anti-diabetic drugs in this part of the world before developing and marketing any new drug. [Int J Basic Clin Pharmacol 2016; 5(1.000: 6-12

  7. Anti-diabetic effects of rice hull smoke extract in alloxan-induced diabetic mice

    Science.gov (United States)

    We investigated the protective effect of a liquid rice hull smoke extract (RHSE) against diabetes in alloxan-induced diabetic mice. Anti-diabetic effects of RHSE were evaluated in both the rat insulinoma-1 cell line (INS-1) and diabetic ICR mice induced by inraperitoneal (ip) injection of alloxan. ...

  8. Comparison of anti-diabetic drug prescribing in children and adolescents in seven European countries

    NARCIS (Netherlands)

    Neubert, Antje; Hsia, Yingfen; de Jong-van den Berg, Lolkje T. W.; Janhsen, Katrin; Glaeske, Gerd; Furu, Kari; Kieler, Helle; Norgaard, Mette; Clavenna, Antonio; Wong, Ian C. K.

    2011-01-01

    AIMS The aim of this study was to compare the prevalence of diabetes in children across seven European countries, when using prescribing of anti-diabetics as a proxy for diabetes. A secondary aim was to assess the potential for collaboration between countries using different databases in diabetes re

  9. Cost variation analysis of Oral Hypoglycaemic agents available in Indian market: An Economic Perspective

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    Salman Hussain

    2015-05-01

    Full Text Available Introduction: Diabetes, a chronic disorder and requires life-long treatment. Cost of drug treatment is a major hurdle related to medication compliance in Type2 Diabetes Mellitus. Objective: To compare the cost and percentage price variation of single and combination therapy of oral hypoglycaemic agents across the different brands available in the Indian market. Methods: India’s medical research body, particularly Indian Council of Medical Research (ICMR issue guidelines for the management of T2DM. ICMR guidelines were perused to understand the management of T2DM. Current Index of Medical Specialities (CIMS Oct.-Jan.2015 edition and Indian Drug Review (IDR Issue 1, Jan.2015 were used to capture the price of oral hypoglycaemic agents across the different brands available in the Indian market. Percentage price variations between minimum and maximum cost of drugs were computed. Results: In the single drug therapy sulfonylurea group of drugs like Glipizide 5mg shows maximum variation of 780% followed by Glimepiride 2mg formulation by 682%, while the non-sulfonylurea groups of drug say, Pioglitazone 15mg shows maximum variation of 600%. In combination therapy Glimepiride 1mg + Metformin 500mg shows maximum price variation of 533%. Positive correlation exists between the number of manufacturing companies and percentage price variation of drugs. Conclusion: There is wide variation exist between the minimum and maximum cost among single as well as combination therapy of oral hypoglycaemic agents. A maximum of 9 & 6 fold price variation was reported in single and combination therapy respectively.

  10. Warfarin and Newer Agents: What the Oral Surgeon Needs to Know.

    Science.gov (United States)

    Steed, Martin B; Swanson, Matthew T

    2016-11-01

    The new direct oral anticoagulants-dabigatran etexilate, rivaroxaban, and apixaban- have predictable pharmacokinetic and pharmacodynamic profiles and are alternatives to warfarin. However, many surgeons are wary of these drugs, as there is limited evidence on how to manage bleeding in patients taking them, and only recently has a specific antidote been developed to reverse their anticoagulant effect. Management of the newer agents requires careful adherence to primary measures of bleeding care, knowledge of their mechanism of action, and familiarity with the unapproved and untested reversal strategies that may be required in patients with life-threatening bleeding. Copyright © 2016 Elsevier Inc. All rights reserved.

  11. Why develop antidotes and reversal agents for non-vitamin K oral anticoagulants?

    Science.gov (United States)

    Washam, Jeffrey B; Piccini, Jonathan P

    2016-02-01

    Over the past several years, non-vitamin K oral anticoagulants (NOACs) have been introduced into clinical practice for the treatment of venous thromboembolism and prevention of stroke in patients with nonvalvular atrial fibrillation. Clinical trials have shown these agents to have similar or less risk of major bleeding as compared to warfarin therapy. Moreover, when patients do experience a major bleeding event administration of advanced factor products is rare, and post-bleed outcomes are similar in those receiving a NOAC compared to those receiving warfarin. However, there are situations where urgent reversal of NOAC anticoagulation would be desirable. The following review focuses on the outcomes and management strategies for patients experiencing a major bleed with warfarin or NOAC agents and describes the rationale for the development of therapies capable of targeted NOAC-reversal.

  12. Pharmacogenetics in type 2 diabetes: influence on response to oral hypoglycemic agents

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    Dawed AY

    2016-04-01

    Full Text Available Adem Yesuf Dawed, Kaixin Zhou, Ewan Robert Pearson  Division of Cardiovascular and Diabetes Medicine, Medical Research Institute, University of Dundee, Dundee, Scotland, UK Abstract: Type 2 diabetes is one of the leading causes of morbidity and mortality, consuming a significant proportion of public health spending. Oral hypoglycemic agents (OHAs are the frontline treatment approaches after lifestyle changes. However, huge interindividual variation in response to OHAs results in unnecessary treatment failure. In addition to nongenetic factors, genetic factors are thought to contribute to much of such variability, highlighting the importance of the potential of pharmacogenetics to improve therapeutic outcome. Despite the presence of conflicting results, significant progress has been made in an effort to identify the genetic markers associated with pharmacokinetics, pharmacodynamics, and ultimately therapeutic response and/or adverse outcomes to OHAs. As such, this article presents a comprehensive review of current knowledge on pharmacogenetics of OHAs and provides insights into knowledge gaps and future directions. Keywords: pharmacogenetics, type 2 diabetes, oral hypoglycemic agents, pharmacokinetics, pharmacodynamics, response

  13. The Usage of Oral Anti Hyperglycemic Agent in Gestational Diabetes: Pros and Cons

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    Bram Pradipta

    2014-06-01

    Full Text Available The prevalence of gestational diabetes mellitus (GDM  is increasing as the pregnant population becomes older and more obese. Fifteen percent of GDM patients require medical intervention. Insulin is still the drug of choice because it has not been implicated as a teratogen in human pregnancies.Insulin has its disadvantages such as the need for injections, the risk of hypoglycaemia, excessive weight gain and the costs. The use of oral anti hyperglicemic agent (OAHA, traditionally contraindicated, now can be considered as an alternative for insulin which can be beneficial in developing countries. From four groups of OAHA, sulfonylurea and biguanides can be used during pregnancy. Studies and randomized controlled trial (RCT have been done and most summarized that it does not increase any maternal and perinatal morbidity. Most data also show that thereare also no differences in glycemic control or pregnancy outcomes compared with insulin. There are conflicting data shows metformin increase prevalence of preeclampsia patient and perinatal morbidity. OAHA usage, although not yet recommended internationally, can be considered in GDMpatients with uncontrolled blood sugar levels that require medical intervention but can not use insulin. Wellconducted, prospective, controlled studies regarding itsfeasibility in pregnant women with diabetes are still needed.Keywords:oral antihyperglycemic agent, gestational, diabetes

  14. In vitro evaluation of alternative oral contrast agents for MRI of the gastrointestinal tract

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    Babos, Magor [University of Szeged, Faculty of Science (Hungary); Euromedic Diagnostics Szeged, 6720 Szeged, Semmelweiss u. 6 (Hungary)], E-mail: babosmagor@yahoo.com; Schwarcz, Attila [University of Pecs, Department of Neurosurgery, Pecs Diagnostic Institute, 7624 Pecs, Retu. 2 (Hungary)], E-mail: attila.schwarcz@aok.pte.hu; Randhawa, Manjit Singh [University of Szeged, Faculty of Medicine, Department of Radiology, 6720 Szeged, Semmelweiss u. 6 (Hungary)], E-mail: majyaal@hotmail.com; Marton, Balazs [University of Szeged, Faculty of Medicine, Department of Radiology, 6720 Szeged, Semmelweiss u. 6 (Hungary)], E-mail: balazsmarton@freemail.hu; Kardos, Lilla [Euromedic Diagnostics Szeged, 6720 Szeged, Semmelweiss u. 6 (Hungary)], E-mail: medlis@tiszanet.hu; Palko, Andras [Euromedic Diagnostics Szeged, 6720 Szeged, Semmelweiss u. 6 (Hungary); University of Szeged, Faculty of Medicine, Department of Radiology, 6720 Szeged, Semmelweiss u. 6 (Hungary)], E-mail: palko@radio.szote.u-szeged.hu

    2008-01-15

    Purpose: In vitro evaluation of different materials as potential alternative oral contrast agents for small bowel MRI. Materials and methods: The T1 and T2 relaxation times of rose hip syrup, black currant extract, cocoa, iron-deferoxamine solution and a commonly used oral contrast material (1 mM Gd-DTPA) were determined in vitro at different concentrations on a 1.0 T clinical MR scanner. T1 values were obtained with an inversion prepared spoiled gradient echo sequence. T2 values were obtained using multiple echo sequences. Finally the materials were visualized on T1-, T2- and T2*-weighted MR images. Results: The relaxation times of the undiluted rose hip syrup (T1 = 110 {+-} 5 ms, T2 = 86 {+-} 3 ms), black currant extract (T1 = 55 {+-} 3 ms, T2 = 39 {+-} 2 ms) and 5 mM iron-deferoxamine solution (T1 = 104 {+-} 4 ms, T2 = 87 {+-} 2 ms) were much shorter than for a 1 mM Gd-DTPA solution (T1 = 180 {+-} 8 ms, T2 = 168 {+-} 5 ms). Dilution of black currant extract to 30% or a 3 mM iron-deferoxamine solution conducted to T1 relaxation times which are quite comparable to a 1 mM Gd-DTPA solution. Despite its much lower metal content an aqueous cocoa suspension (100 g/L) produced T2 relaxation times (T1 = 360 {+-} 21 ms, T2 = 81 {+-} 3 ms) more or less in the same range like the 5 mM iron-deferoxamine solution. Imaging of our in vitro model using clinical sequences allowed to anticipate the T1-, T2- and T2*-depiction of all used substances. Cocoa differed from all other materials with its low to moderate signal intensity on T1- and T2-weighted sequences. While all substances presented a linear 1/T1 and 1/T2 relationship towards concentration, rose hip syrup broke ranks with a disproportionately high increase of relaxation at higher concentrations. Conclusions: Rose hip syrup, black currant extract and iron-deferoxamine solution due to their positive T1 enhancement characteristics and drinkability appear to be valuable oral contrast agents for T1-weighted small bowel MRI

  15. Management of oral Graft versus Host Disease with topical agents: A systematic review

    Science.gov (United States)

    Khan, Zahid; Poveda, Ana; Higham, Jonathan; Richards, Andrea; Monteiro, Luis; Jané-Salas, Enric; Lopez-Lopez, José; Warnakulasuriya, Saman

    2016-01-01

    Background Oral Graft-versus-Host Disease (oGvHD) is a common complication of haematopoietic stem cell transplantation. Choosing the right topical application to be used intra orally can be a challenge. Consequently, the aim of this work is to review the effectiveness and safety of topical agents currently used in the management of the inflammatory mucosal lesions encountered in oGVHD. Material and Methods We carried out electronic searches of publications up to May 2015 of the databases Pubmed, National Library of Medicine’s Medline, Embase and the Cochrane Central Register of Controlled Clinical trials to identify potentially relevant studies (keywords: “oral”, “graft”, “versus”, “host”, “disease” and “treatment”). The main inclusion criterion was the reported use of a topical agent which was not intentionally swallowed when used for the treatment of oGVHD. A 3-point grading system, described by the Swedish Council on Technology Assessment in Health Care and the Centre for Reviews and Dissemination, University of York, was used to rate the methodological quality of the papers. Results From the 902 entries identified in the search, 7 studies qualifying for inclusion were analysed. Overall, there is limited evidence with regards to the effectiveness of topical steroids for oGVHD. However, the studies showed some effect of Budesonide alone and when combined with dexamethasone. Topical tacrolimus also appears to have some effect and clobetasol propionate mouthwash had a significantly better clinical response than dexamethasone mouthwash in treating oGVHD. Conclusions As the number of clinical trials conducted is limited, there is little evidence to support the use of topical therapies to treat the inflammatory mucosal lesions found in oGVHD. High quality randomised control trials are needed in order to measure the effectiveness of any topical application for the treatment of the inflammatory mucosal lesions found in oGVHD. Key words:Oral

  16. Orally Active and Selective Tubulin Inhibitors as Anti-Trypanosome Agents.

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    Vishal Nanavaty

    Full Text Available There is an urgent need to develop a safe, effective, orally active, and inexpensive therapy for African trypanosomiasis due to the drawbacks of current drugs. Selective tubulin inhibitors have the potential to be promising drug candidates for the treatment of this disease, which is based on the tubulin protein structural difference between mammalian and trypanosome cells. We propose to identify novel tubulin inhibitors from a compound library developed based on the lead compounds that selectively target trypanosomiasis.We used Trypanosoma brucei brucei as the parasite model, and human normal kidney cells and mouse microphage cells as the host model. Growth rates of both trypanosomes and mammalian cells were determined as a means to screen compounds that selectively inhibit the proliferation of parasites. Furthermore, we examined the cell cycle profile of the parasite and compared tubulin polymerization dynamics before and after the treatment using identified compounds. Last, in vivo anti-parasite activities of these compounds were determined in T. brucei-infected mice.Three compounds were selected that are 100 fold more effective against the growth of T. brucei cells than mammalian cells. These compounds caused cell cycle progression defects in T. brucei cells. Western analyses indicated that these compounds decreased tubulin polymerization in T. brucei cells. The in vivo investigation revealed that these compounds, when admitted orally, inhibited T. brucei cell proliferation in mouse blood. However, they were not potent enough to clear up the infection completely.These compounds are promising lead compounds as orally active agents for drug development of anti-trypanosome agents. A more detail structure activity relationship (SAR was summarized that will be used to guide future lead optimization to improve the selectivity and potency of the current compounds.

  17. Intentional weight loss and dose reductions of anti-diabetic medications--a retrospective cohort study.

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    Anita Ashok Kumar

    Full Text Available BACKGROUND AND AIM: Intentional weight loss, primarily by improving insulin resistance, is known to decrease the need for anti-diabetic medications. In this study, we assess the magnitude of weight loss that resulted in dose reductions or discontinuation of anti-diabetic medications in overweight or obese patients with type 2 diabetes (DM undergoing weight loss treatment. METHODS: Case records of 50 overweight or obese patients with DM who successfully decreased dosage or discontinued diabetes medications after losing weight via attendance at two University-based, outpatient weight management centers were analyzed. Follow-up visits, weight reduction interventions, and decisions for dose reductions or discontinuation of medications were individualized to patient needs by the treating physician. RESULTS: Mean starting BMI was 35 kg/m(2, mean age 53.4 years, and 58% were male. All 50 used at least one anti-diabetic medication (30 metformin, 39 sulfonylureas, 31 insulin, 21 sitagliptin to manage blood sugar. Mean duration of follow-up was 30.2 months. Mean weight loss was 10.8 ± 4.1 kgs (11.1% of initial body weight ± 4.7%. 22/50 patients (44% discontinued anti-diabetes medications (14 sulfonylureas [36%], 7 insulin [23%], 4 sitagliptin [19%]. The mean percentage weight loss achieved at the point of successful discontinuation of medication was 11.2% ± 3.5% (14% for sulphonylureas, 11% for insulin, and 7.1% for sitagliptin. Mean percentage weight loss of 5.6% ± 2.8% (5.1% for sulphonylureas, 4.3% for insulin, and 7.1% for sitagliptin was required for initial dose reduction. For every 5% weight loss, predicted dose reductions were sulphonylureas, 39%; insulin, 42%; and any anti-diabetic medications, 49%. CONCLUSION: Among overweight or obese patients with type 2 diabetes, intentional weight loss of 7-14% was typically required for full discontinuation of at least one anti-diabetic medication. Discontinuation of insulin was achieved at a mean

  18. ORAL HYPOGLYCAEMIC AGENTS IN THE MANAGEMENT OF TYPE II DIABETES MELLITUS

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    Durgaprasad M.

    2016-06-01

    Full Text Available OBJECTIVES Diabetes is fast gaining the status of a potential epidemic globally. The number of people with diabetes has risen from 108 million in 1980 to 422 million in 2014, the rise seen more rapidly in developing and under developed countries. Type 2 Diabetes Mellitus (T2DM being the most common type, accounting for an estimated 85-95% of all diabetes cases. Diabetes remains a major cause of blindness, renal failure, and cardiovascular events including heart attacks, stroke and limb amputations. 1 Being an heterogeneous disorder, many adults with T2DM have difficulty controlling their blood sugar levels and associated complications as most of available antidiabetic agents aim to achieve only normoglycaemia and relieve diabetes symptoms, such as polydipsia, polyuria, weight loss, ketoacidosis while the longterm goals to prevent the development of or slow the progression of longterm complications of the disease is often unaddressed, therefore, there remains, a significant unmet demand for new agents that will help diabetic patients achieve treatment targets without increasing the risk for weight gain or hypoglycaemia. Among the new classes of oral agents, SGLT-2 inhibitors and mTOT insulin sensitisers appear to hold some good promise. However, recent articles published describing its adverse effect profile of SGLT-2 inhibitors had put a question mark on its utility. In this article, we have reviewed the plethora of available OHAs along with the newer OHAs for managing T2DM optimally.

  19. Helical CT of the abdomen: whole milk as a low-density oral contrast agent; Tomografia helicoidal do abdome: avaliacao do leite integral como contraste oral de baixa densidade

    Energy Technology Data Exchange (ETDEWEB)

    Collares, Felipe Birchal; Diniz, Renata Lopes Furletti Caldeira; Motta, Emilia Guerra Pinto Coelho; Moreira, Wanderval; Ribeiro, Marcelo Almeida [Hospital Mater Dei, Belo Horizonte, MG (Brazil). Dept. de Radiologia

    2000-08-01

    We evaluated 90 abdominal helical computed tomography scans from patients who received 1% iodine solution, whole milk or no oral contrast agent before scanning. Four parameters were evaluated: gastrointestinal distension, mural visualization, pancreas-duodenum discrimination and bowel loop discrimination. Better results were obtained with the use of whole milk compared to iodine contrast or no oral contrast agent. Whole milk is an effective low density oral contrast agent. (author)

  20. Gastric stromal tumor: two-phase dynamic CT findings with water as oral contrast agents

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    Lee, Se Hyo; Cho, June Sik; Shin, Kyung Sook; Jeong, Ki Ho; Park, Jin Yong; Yu, Ho Jun; Kim, Young Min; Jeon, Kwang Jin [College of Medicine, Chungnam National University, Taejon (Korea, Republic of)

    2000-01-01

    To evaluate two-phase dynamic CT with water as oral contrast agents in the CT diagnosis of gastric stromal tumors. We retrospectively reviewed the CT findings in 21 patients with pathologically proven gastric stromal tumors. Six were found to be benign, twelve were malignant, and there were three cases of STUMP (stromal tumor uncertain malignant potential). Two-phase dynamic CT scans with water as oral contrast agents were obtained 60-70 secs (portal phase) and 3 mins (equilibrium phase) after the start of IV contrast administration. We determined the size, growth pattern, and enhancement pattern of the tumors and overlying mucosa, the presence or absence of ulceration and necrosis, tumor extent, and lymph nod and distant metastasis. The CT and pathologic findings were correlated. All six benign tumors and three STUMP were less than 5.5 cm in size, and during the portal phase showed round endogastric masses with highly enhanced, intact overlying mucosa. Twelve malignant tumors were 4.5-15.5 cm in size (mean, 11.5 cm); an endogastric mass was seen in three cases, an exogastric mass in one, and a mixed pattern in eight. On portal phase images the tumors were not significantly enhanced, but highly enhanced feeding vessels were noted in five larger tumors (greater than 10 cm). All 12 malignant tumors showed ulceration and necrosis, and interruption of overlying mucosa was clearly seen during the portal phase. We were readily able to evaluate tumor extent during this phase, and in ten malignant tumors there was no invasion of adjacent organs. Seven malignant tumors showed air density within their necrotic portion (p less than 0.05). On equilibrium phase images, all malignant tumors showed heterogeneous enhancement due to necrosis, and poorly enhanced overlying mucosa. Dynamic CT during the portal phase with water as oral contrast agents was useful for depicting the submucosal origin of gastric stromal tumors and for evaluating the extent of malignant stromal tumors. Our

  1. Long-lasting anti-diabetic efficacy of PEGylated FGF-21 and liraglutide in treatment of type 2 diabetic mice.

    Science.gov (United States)

    Ye, Xianlong; Qi, Jianying; Ren, Guiping; Xu, Pengfei; Wu, Yunzhou; Zhu, Shenglong; Yu, Dan; Li, Shujie; Wu, Qiang; Muhi, Rasool Lubna; Li, Deshan

    2015-08-01

    Fibroblast growth factor-21 (FGF-21) is a new member of the FGF family and potential drug candidate for the treatment of type 2 diabetes mellitus. However, FGF-21 protein has short half-life in vivo, which severely affects its clinical application. In the present study, PEGylated FGF-21 was prepared by modifying the N-terminus of hFGF-21 with 20 kDa mPEG-ALD. The long-acting hypoglycemic effect of PEGylated FGF-21 and liraglutide was compared on type 2 diabetic db/db mice. The pharmacological efficacy of the compounds was evaluated by blood glucose levels, body weight, glycosylated hemoglobin levels, insulin levels, oral glucose tolerance test, lipid levels, and liver function parameters. We noticed that both PEGylated FGF-21 and liraglutide could significantly decrease plasma glucose in db/db mice. However, comparing to liraglutide treatments, PEGylated FGF-21 therapy resulted in more significant effect in lowering blood glucose levels and glycosylated hemoglobin levels, alleviating insulin resistance, improving lipid profile, liver function, and glucose control of the experimental mice. Our results suggest that PEGylated FGF-21 appears more beneficial anti-diabetic effect in type 2 diabetic mice than liraglutide, which holds significant promise as an ideal candidate for the treatment of type 2 diabetic patients.

  2. Assay method for quality control and stability studies of a new anti-diabetic and anti-dyslipidemic flavone (S002-853FNx01

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    Arshi Naqvi

    2015-01-01

    Full Text Available Background: Flavonoid-rich extract of the plant is long known for its anti-diabetic activities in traditional medicine. S002-853, a new flavone derivative synthesized by Central Drug Research Institute (CDRI has been used for the present study. Objectives: The present study aimed at development of an assay method for quality control (QC and stability studies of a new anti-diabetic and anti-dyslipidemic agent CDRI compound S002-853. Materials and Methods: A validated high-performance liquid chromatography analysis method for S002-853 was developed for in process QC and stability studies. The separation was achieved on a RP-C18 (25 cm × 0.4 cm, 5 μm, Phenomenex at 240 nm with flow rate of 1.0 ml/min. This method was applied successfully in establishing forced degradation and drug-excipient testing protocols as per International Conference on Harmonization guidelines. Results: The result of estimation and stress testing studies indicated a high degree of selectivity of this method. S002-853 was most stable at pH 7 and under photolytic conditions. The temperature degradation pattern of S002-853 was found to follow the zero order degradation. Conclusion: The method described is easy and simple hence can be easily reproduced. This method can be very useful for bulk manufacture QC, and drug development process.

  3. Anti-diabetic effects of Caulerpa lentillifera:stimulation of insulin secretion in pancreatic β-cells and enhancement of glucose uptake in adipocytes

    Institute of Scientific and Technical Information of China (English)

    Bhesh Raj Sharma; Dong Young Rhyu

    2014-01-01

    Objective: To evaluate anti-diabetic effect of Caulerpa lentillifera (C. lentillifera).Methods:The inhibitory effect of C. lentillifera extract on dipeptidyl peptidase-IV andα-glucosidase enzyme was measured in a cell free system. Then, interleukin-1β and interferon-γinduced cell death and insulin secretion were measured in rat insulinoma (RIN) cells by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay and ELISA kit, respectively. Glucose uptake and glucose transporter expression were measured by fluorometry and western blotting, using 3T3-L1 adipocytes.Results: C. lentillifera extract significantly decreased dipeptidyl peptidase-IV and α-glucosidase enzyme activities, and effectively inhibited cell death and iNOS expression in interleukin-1βand interferon-γ induced RIN cells. Furthermore, C. lentillifera extract significantly enhanced insulin secretion in RIN cells and glucose transporter expression and glucose uptake in 3T3-L1 adipocytes.Conclusions:Thus, our results suggest that C. lentillifera could be used as a potential anti-diabetic agent.

  4. Anti-diabetic effects of Caulerpa lentillifera: stimulation of insulin secretion in pancreatic β-cells and enhancement of glucose uptake in adipocytes.

    Science.gov (United States)

    Sharma, Bhesh Raj; Rhyu, Dong Young

    2014-07-01

    To evaluate anti-diabetic effect of Caulerpa lentillifera (C. lentillifera). The inhibitory effect of C. lentillifera extract on dipeptidyl peptidase-IV and α-glucosidase enzyme was measured in a cell free system. Then, interleukin-1β and interferon-γ induced cell death and insulin secretion were measured in rat insulinoma (RIN) cells by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay and ELISA kit, respectively. Glucose uptake and glucose transporter expression were measured by fluorometry and western blotting, using 3T3-L1 adipocytes. C. lentillifera extract significantly decreased dipeptidyl peptidase-IV and α-glucosidase enzyme activities, and effectively inhibited cell death and iNOS expression in interleukin-1β and interferon-γ induced RIN cells. Furthermore, C. lentillifera extract significantly enhanced insulin secretion in RIN cells and glucose transporter expression and glucose uptake in 3T3-L1 adipocytes. Thus, our results suggest that C. lentillifera could be used as a potential anti-diabetic agent.

  5. Comparative genotoxic and cytotoxic effects of the oral antidiabetic drugs sitagliptin, rosiglitazone, and pioglitazone in patients with type-2 diabetes: a cross-sectional, observational pilot study.

    Science.gov (United States)

    Oz Gul, Ozen; Cinkilic, Nilufer; Gul, Cuma Bulent; Cander, Soner; Vatan, Ozgur; Ersoy, Canan; Yılmaz, Dilek; Tuncel, Ercan

    2013-09-18

    This cross-sectional, observational pilot study was designed to investigate the frequency of different endpoints of genotoxicity (sister-chromatid exchange, total chromosome aberrations, and micronucleus formation) and cytotoxicity (mitotic index, replication index, and nuclear division index) in the peripheral lymphocytes of patients with type-2 diabetes treated with different oral anti-diabetic agents for 6 months. A total of 104 patients who met the American Diabetes Association criteria for type-2 diabetes were enrolled in the study. Of the 104 patients, 33 were being treated with sitagliptin (100mg/day), 25 with pioglitazone (30mg/day), 22 with rosiglitazone (4mg/day), and 24 with medical nutrition therapy (control group). The results for all the genotoxicity endpoints were significantly different across the four study groups. Post hoc analysis revealed that the genotoxicity observed in the sitagliptin group was significantly higher than that observed in the medical nutrition therapy group, but lower than that occurring in subjects who received thiazolidinediones. All of the three cytotoxicity endpoints were significantly lower in patients treated by oral anti-diabetic agents compared with those who received medical nutrition therapy. However, the three indexes did not differ significantly in the sitagliptin, rosiglitazone, and pioglitazone groups. Taken together, these pilot data indicate that sitagliptin and thiazolidinediones may exert genotoxic and cytotoxic effects in patients with type-2 diabetes. Further investigations are necessary to clarify the possible long-term differences between oral anti-diabetic drugs in terms of genotoxicity and cytotoxicity, and how these can modulate the risk of developing diabetic complications in general and cancer in particular.

  6. COST-EFFECTIVENESS ANALYSIS OF ANTI-DIABETIC THERAPY IN A UNIVERSITY TEACHING HOSPITAL

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    Giwa Abdulganiyu

    2014-03-01

    Full Text Available Purpose: To conduct cost-effectiveness analysis of anti-diabetic therapy in a University Teaching Hospital in 2010. Methods: A retrospective review of selected case-notes was conducted. World Health Organization Defined Daily Dose Method of evaluating drug use and probability method for potential effectiveness of antidiabetic therapeutic options from literature analysis was employed in determining cost-effectiveness of each anti-diabetic therapeutic option identified from anti-diabetic drug utilization studies. Sample Size, n=1200. Subjects’ case-notes were selected by systematic random sampling (Sampling Interval = 1. Results: Glibenclamide (N1.76/unit of effectiveness which was more cost-effective than chlopropamide (N2.97/unit of effectiveness in the management of moderate hyperglycemia in non-obese Type II Diabetes Mellitus was more frequently prescribed (81.5%. Glibenclamide + Metformin (N7.63/unit of effectiveness which was more frequently prescribed (92.5% was not necessarily more cost-effective than Chlopropamide + Metformin (N9.76/unit of effectiveness in the management of moderate hyperglycemia in obese Type II Diabetes- Mellitus. Biphasic Isophane Insulin (N12.65/unit of effectiveness which was more cost-effective than soluble insulin + insulin zinc (N30.37/unit of effectiveness in the management of serve hyperglycemia in non-obese Type II Diabetes Mellitus was less frequently prescribed (42.3%. Biphasic Isophane Insulin + Metformin (N15.91/unit of effectiveness which was more cost-effective than soluble insulin + insulin zinc + metformin (N34.45/ unit of effectiveness in the management of severe hyperglycemia in obese Type II Diabetes Mellitus patients was less frequently prescribed (25%. Conclusions: Prescription of lees cost-effective anti-diabetic drugs was rampant in Hospitals.

  7. An invertebrate hyperglycemic model for the identification of anti-diabetic drugs.

    Science.gov (United States)

    Matsumoto, Yasuhiko; Sumiya, Eriko; Sugita, Takuya; Sekimizu, Kazuhisa

    2011-03-30

    The number of individuals diagnosed with type 2 diabetes mellitus, which is caused by insulin resistance and/or abnormal insulin secretion, is increasing worldwide, creating a strong demand for the development of more effective anti-diabetic drugs. However, animal-based screening for anti-diabetic compounds requires sacrifice of a large number of diabetic animals, which presents issues in terms of animal welfare. Here, we established a method for evaluating the anti-diabetic effects of compounds using an invertebrate animal, the silkworm, Bombyx mori. Sugar levels in silkworm hemolymph increased immediately after feeding silkworms a high glucose-containing diet, resulting in impaired growth. Human insulin and 5-aminoimidazole-4-carboxamide-1-β-D-ribofuranoside (AICAR), an AMP-activated protein kinase (AMPK) activator, decreased the hemolymph sugar levels of the hyperglycemic silkworms and restored growth. Treatment of the isolated fat body with human insulin in an in vitro culture system increased total sugar in the fat body and stimulated Akt phosphorylation. These responses were inhibited by wortmannin, an inhibitor of phosphoinositide 3 kinase. Moreover, AICAR stimulated AMPK phosphorylation in the silkworm fat body. Administration of aminoguanidine, a Maillard reaction inhibitor, repressed the accumulation of Maillard reaction products (advanced glycation end-products; AGEs) in the hyperglycemic silkworms and restored growth, suggesting that the growth defect of hyperglycemic silkworms is caused by AGE accumulation in the hemolymph. Furthermore, we identified galactose as a hypoglycemic compound in jiou, an herbal medicine for diabetes, by monitoring its hypoglycemic activity in hyperglycemic silkworms. These results suggest that the hyperglycemic silkworm model is useful for identifying anti-diabetic drugs that show therapeutic effects in mammals.

  8. An invertebrate hyperglycemic model for the identification of anti-diabetic drugs.

    Directory of Open Access Journals (Sweden)

    Yasuhiko Matsumoto

    Full Text Available The number of individuals diagnosed with type 2 diabetes mellitus, which is caused by insulin resistance and/or abnormal insulin secretion, is increasing worldwide, creating a strong demand for the development of more effective anti-diabetic drugs. However, animal-based screening for anti-diabetic compounds requires sacrifice of a large number of diabetic animals, which presents issues in terms of animal welfare. Here, we established a method for evaluating the anti-diabetic effects of compounds using an invertebrate animal, the silkworm, Bombyx mori. Sugar levels in silkworm hemolymph increased immediately after feeding silkworms a high glucose-containing diet, resulting in impaired growth. Human insulin and 5-aminoimidazole-4-carboxamide-1-β-D-ribofuranoside (AICAR, an AMP-activated protein kinase (AMPK activator, decreased the hemolymph sugar levels of the hyperglycemic silkworms and restored growth. Treatment of the isolated fat body with human insulin in an in vitro culture system increased total sugar in the fat body and stimulated Akt phosphorylation. These responses were inhibited by wortmannin, an inhibitor of phosphoinositide 3 kinase. Moreover, AICAR stimulated AMPK phosphorylation in the silkworm fat body. Administration of aminoguanidine, a Maillard reaction inhibitor, repressed the accumulation of Maillard reaction products (advanced glycation end-products; AGEs in the hyperglycemic silkworms and restored growth, suggesting that the growth defect of hyperglycemic silkworms is caused by AGE accumulation in the hemolymph. Furthermore, we identified galactose as a hypoglycemic compound in jiou, an herbal medicine for diabetes, by monitoring its hypoglycemic activity in hyperglycemic silkworms. These results suggest that the hyperglycemic silkworm model is useful for identifying anti-diabetic drugs that show therapeutic effects in mammals.

  9. New Oral Hypoglycemic Agents and Cardiovascular Risk. Crossing the Metabolic Border.

    Science.gov (United States)

    Dalama, Belén; Mesa, Jordi

    2016-11-01

    Sodium-glucose cotransporter 2 inhibitors are a novel pharmacological class of oral hypoglycemic agents that lower glucose levels by increasing renal glucose excretion in an insulin-independent manner. However, this seemingly simple mechanism has more complex indirect metabolic effects. The results of randomized clinical trials have shown that these inhibitors effectively lower blood glucose and glycated hemoglobin levels without increasing the risk of hypoglycemia and, at the same time, also reduce bodyweight and systolic blood pressure. In this review, we describe the mechanism of action, efficacy, and safety of currently marketed drugs, as well as other risk factors besides glucose that can potentially be modulated positively. Recent data on empagliflozin showing a significant cardiovascular benefit have compelled us to update knowledge of this new therapeutic class for the treatment of type 2 diabetes. Copyright © 2016 Sociedad Española de Cardiología. Published by Elsevier España, S.L.U. All rights reserved.

  10. Efficacy of Black Tea as a Negative Oral Contrast Agent for MR Cholangiopancreatography (MRCP

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    Amir Hossein Jalali

    2010-05-01

    Full Text Available Background/Objective: Evaluation of the use of black tea as negative oral contrast agent in MR cholangiopancreatography (MRCP."nPatients and Methods: Thirty-five patients (mean age, 50.3±19.2 years, who were referred for MRCP, entered in this study. MRCP was performed before, after 5 minutes and after 15 minutes following consumption of 300 ml of black tea. Depiction of the gall bladder, cystic duct, proximal and distal parts of the common bile duct (CBD, intra hepatic ducts, ampula of Vater, main pancreatic duct (MPD and signal loss of the stomach and three different segments of the duodenum were investigated according to VAS and Lickert scores."nResults: Regarding visibility of seven different anatomical parts of the pancreatobiliary tree (gall bladder, cystic duct, CBD, common hepatic duct, intrahepatic duct, ampula of Vater and MPD, the post procedure images were better visualized only in the distal part of CBD, ampula of vater and MPD both in Lickert and VAS scoring (all Ps≤0.001."nThere was no significant difference between the images 5 and 15 minutes after tea consumption. Regarding the obliteration of high signal in the stomach and three different parts of the duodenum, all post tea images of the mentioned parts showed significant disappearance of high signal in Lickert and VAS scoring systems (all Ps≤0.001. "nConclusion: Black tea is an affordable, cheap, available, safe, and efficient oral negative contrast agent for MRCP which reduces the signal intensity of fluids in the gastrointestinal tract and is also efficient for better depiction of MPD, distal part of CBD and ampula.

  11. A survey of prescription pattern of anti-diabetic drugs on diabetic patients with cardiovascular complications within Dhaka metropolis

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    Rubaba Karim

    2016-12-01

    Conclusions: The findings can serve as a guide to choose the formulation and combination of anti-diabetic drugs in this part of the world before developing and marketing any new drug. Therefore it is necessary to create better awareness among people, focus on rational use of anti-diabetic drugs and also motivate our physicians to prescribe the generic drugs. [Int J Basic Clin Pharmacol 2016; 5(6.000: 2397-2402

  12. Anti-diabetic effects of brown algae derived phlorotannins, marine polyphenols through diverse mechanisms.

    Science.gov (United States)

    Lee, Seung-Hong; Jeon, You-Jin

    2013-04-01

    Marine algae are popular and abundant food ingredients mainly in Asian countries, and also well known for their health beneficial effects due to the presence of biologically active components. The marine algae have been studied for biologically active components and phlorotannins, marine polyphenols are among them. Among marine algae, brown algae have extensively studied for their potential anti-diabetic activities. Majority of the investigations on phlorotannins derived from brown algae have exhibited their various anti-diabetic mechanisms such as α-glucosidase and α-amylase inhibitory effect, glucose uptake effect in skeletal muscle, protein tyrosine phosphatase 1B (PTP 1B) enzyme inhibition, improvement of insulin sensitivity in type 2 diabetic db/db mice, and protective effect against diabetes complication. In this review, we have made an attempt to discuss the various anti-diabetic mechanisms associated with phlorotannins from brown algae that are confined to in vitro and in vivo. Copyright © 2013 Elsevier B.V. All rights reserved.

  13. In vitro evaluation of anti-diabetic activity and cytotoxicity of chemically analysed Ocimum basilicum extracts.

    Science.gov (United States)

    Kadan, Sleman; Saad, Bashar; Sasson, Yoel; Zaid, Hilal

    2016-04-01

    The aim of this study was to evaluate the role of glucose transporter-4 (GLUT4) in the anti-diabetic effects of methanol, hexane and dichloromethane extracts of the aerial parts of Ocimum basilicum (OB) and to analyze their phytochemical composition. Phytochemical analysis of the three extracts by GC/MS using the silylation derivatization technique revealed 53 compounds, 17 of them were found for the first time in OB. Cytotoxic and anti-diabetic properties of the extracts were evaluated using L6-GLUT4myc muscle cells stably expressing myc epitope at the exofacial loop (GLUT4). No cytotoxic effects were observed in treated cells up to 0.25 mg/ml extract as measured with MTT and LDH-leakage assays. GLUT4 translocation to the plasma membrane was elevated by 3.5 and 7 folds (-/+ insulin) after treatment with OB extracts for 20 h. Our findings suggest that the observed anti-diabetic properties of OB extracts are possibly mediated in part through one or more of the 17 new identified compound.

  14. Anti-diabetic drugs inhibit obesity-linked phosphorylation of PPARgamma by Cdk5.

    Science.gov (United States)

    Choi, Jang Hyun; Banks, Alexander S; Estall, Jennifer L; Kajimura, Shingo; Boström, Pontus; Laznik, Dina; Ruas, Jorge L; Chalmers, Michael J; Kamenecka, Theodore M; Blüher, Matthias; Griffin, Patrick R; Spiegelman, Bruce M

    2010-07-22

    Obesity induced in mice by high-fat feeding activates the protein kinase Cdk5 (cyclin-dependent kinase 5) in adipose tissues. This results in phosphorylation of the nuclear receptor PPARgamma (peroxisome proliferator-activated receptor gamma), a dominant regulator of adipogenesis and fat cell gene expression, at serine 273. This modification of PPARgamma does not alter its adipogenic capacity, but leads to dysregulation of a large number of genes whose expression is altered in obesity, including a reduction in the expression of the insulin-sensitizing adipokine, adiponectin. The phosphorylation of PPARgamma by Cdk5 is blocked by anti-diabetic PPARgamma ligands, such as rosiglitazone and MRL24. This inhibition works both in vivo and in vitro, and is completely independent of classical receptor transcriptional agonism. Similarly, inhibition of PPARgamma phosphorylation in obese patients by rosiglitazone is very tightly associated with the anti-diabetic effects of this drug. All these findings strongly suggest that Cdk5-mediated phosphorylation of PPARgamma may be involved in the pathogenesis of insulin-resistance, and present an opportunity for development of an improved generation of anti-diabetic drugs through PPARgamma.

  15. Direct oral anticoagulants and antiplatelet agents. Clinical relevance and options for laboratory testing.

    Science.gov (United States)

    Sibbing, D; Spannagl, M

    2014-01-01

    Oral anticoagulants and platelet receptor blockers are widely used in clinical practice with the aim of reducing the risk of thrombotic complications in patients with cardiovascular diseases. Their regular intake and adequate antithrombotic action is vital and this is way numerous assays have been developed for laboratory testing and monitoring of these agents. Available assays can be stratified into pharmacokinetic and pharmacodynamic assays. Such assays are increasingly used in clinical routine and their daily use is triggered by the advent of the novel direct oral anticoagulants (DOACs) as an alternative for vitamin K antagonist (VKA) treatment, which are dabigatran, rivaroxaban and apixaban, and by the advent of prasugrel or ticagrelor as an alternative for clopidogrel with regard to platelet P2Y12 receptor inhibition. In this review the most important and most commonly used laboratory assays are summarized as well as their clinical implications with the focus on DOACs as an alternative for VKAs and the different P2Y12 receptor blockers for antiplatelet treatment.

  16. Dabigatran and other oral antithrombotic agents for the prevention of stroke in patients with atrial fibrillation

    Directory of Open Access Journals (Sweden)

    Testai F

    2011-06-01

    Full Text Available Fernando D Testai, Venkatesh AiyagariSection of Neurological Critical Care and Stroke, Department of Neurology and Rehabilitation, Center for Stroke Research, University of Illinois College of Medicine, Chicago, IL, USAAbstract: Atrial fibrillation (AF is considered to be one of the most prevalent abnormal heart rhythm disorders and a leading cause of cerebral ischemia. The risk of stroke in AF is associated with vascular risk factors including advancing age, hypertension, congestive heart disease, diabetes mellitus, vascular disease, and prior history of stroke or transient ischemic attack. The classic management of patients with AF at risk of suffering stroke includes the use of warfarin. The use of this medication in clinical practice is, however, limited owing to its narrow therapeutic window, multiple drug and food interactions, prolonged half-life, and the need for periodic anticoagulation monitoring. Recently, newer oral anticoagulants with better pharmacokinetic and pharmacodynamic profiles have been developed and compared to warfarin in phase III trials for the prevention of stroke and systemic embolism in patients with AF. Dabigatran stands out from these studies as a safe and efficacious alternative to warfarin for treating patients with AF at risk of stroke. In this article we review classic and novel approaches for stroke prevention in AF with special emphasis on dabigatran.Keywords: oral anticoagulants, vitamin K antagonists, antiplatelet agents, stroke prevention, atrial fibrillation

  17. Small Bowel Obstruction Following Computed Tomography and Magnetic Resonance Enterography Using Psyllium Seed Husk As an Oral Contrast Agent

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    Yingming Amy Chen

    2014-01-01

    Full Text Available The authors report a case series describing four patients who developed small bowel obstruction following the use of psyllium seed husk as an oral contrast agent for computed tomography or magnetic resonance enterography. Radiologists who oversee computed tomography and magnetic resonance enterography should be aware of this potential complication when using psyllium seed husk and other bulking agents, particularly when imaging patients with known or suspected small bowel strictures or active inflammation.

  18. Small bowel obstruction following computed tomography and magnetic resonance enterography using psyllium seed husk as an oral contrast agent.

    Science.gov (United States)

    Chen, Yingming Amy; Cervini, Patrick; Kirpalani, Anish; Vlachou, Paraskevi A; Grover, Samir C; Colak, Errol

    2014-01-01

    The authors report a case series describing four patients who developed small bowel obstruction following the use of psyllium seed husk as an oral contrast agent for computed tomography or magnetic resonance enterography. Radiologists who oversee computed tomography and magnetic resonance enterography should be aware of this potential complication when using psyllium seed husk and other bulking agents, particularly when imaging patients with known or suspected small bowel strictures or active inflammation.

  19. Analysis of FHS community health agents knowledge about oral health - doi: 10.4025/actascihealthsci.v35i2.11723

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    Nicole Patricia de Lima Vinagre

    2013-06-01

    Full Text Available The community health agents (CHA are considered health promoters in Brazilian communities teaching them about health promotion and disease prevention, including oral health. According to the Ministry of Health, CHAs must know about seven major oral health issues in Brazil. Thus, the objective of this study was to evaluate the oral health knowledge level of CHAs in the city of Belem, Pará State, Brazil. The study was based on a self-guided script, through a pre-prepared questionnaire containing 16 multiple-choice questions related to oral health knowledge. The survey was conducted with 94 agents from seven Family Health stations featuring oral health teams in Belem. It was concluded that community agents should be better prepared about oral care, as not all oral health issues were known by the CHAs oral health teams in Belem.

  20. Computational pharmacokinetics and in vitro-in vivo correlation of anti-diabetic synergistic phyto-composite blend

    Institute of Scientific and Technical Information of China (English)

    Baishakhi; De; Koushik; Bhandari; Nishant; Chakravorty; Ranjan; Mukherjee; Rohit; Gundamaraju; Rajeev; K; Singla; Prakash; Katakam; Shanta; K; Adiki; Biswajoy; Ghosh; Analava; Mitra

    2015-01-01

    Despite tremendous strides in modern medicine stringent control over insulin resistance or restoration of normoglycemia has not yet been achieved.With the growth of molecular biology,omics technologies,docking studies,and in silico pharmacology,modulators of enzymes and receptors affecting the molecular pathogenesis of the disease are being considered as the latest targets for anti-diabetic therapy.Therapeutic molecular targets are now being developed basing on the up or down regulation of different signaling pathways affecting the disease.Phytosynergistic antidiabetic therapy is in vogue both with classical and non-classical medicinal systems.However its chemoprofiling,structural and pharmacokinetic validation awaits providing recognition to such formulations for international acceptance.Translational health research with its focus on benchside product development and its sequential transition to patient bedside puts the pharma RDs to a challenge to develop bio-waiver protocols.Pharmacokinetic simulation models and establishment of in vitro-in vivo correlation can help to replace in vivo bioavailability studies and provide means of quality control for scale up and post approval modification.Thisreview attempts to bring different shades highlighting phyto-synergy,molecular targeting of antidiabetic agents via different signaling pathways and bio-waiver studies under a single umbrella.

  1. Garlic as an anti-diabetic agent: recent progress and patent reviews.

    Science.gov (United States)

    Padiya, Raju; Banerjee, Sanjay K

    2013-08-01

    This article reviews recent literature on the usage and relevance of garlic and its bioactive components in controlling diabetes and diabetes-associated pathologies; and also updates recent patents on the subject. Antidiabetic effect of garlic is well documented even in ancient medical literature. Garlic and its active ingredients have been extensively studied for their antidiabetic efficacies in either experimentally induced or genetic animal models of diabetes. Human studies are also available where hypoglycemic effect of garlic was reported. The beneficial effects of garlic are mainly attributed to the presence of volatile sulfur compounds like alliin, allicin, diallyl disulfide, diallyl trisulfide, diallyl sulfide, S-allyl cysteine, ajoene and allyl mercaptan. Garlic and garlic extracts have been shown to be effective in reducing insulin resistance. Therefore, considering the importance of garlic in controlling diabetic complications, several preparations and food processes containing garlic have been patented. This review discusses some of the recent progresses made in this field and consolidates the results.

  2. Anti-diabetes Agents---Ⅰ: Tetralone Derivative from Juglans regia

    Institute of Scientific and Technical Information of China (English)

    2003-01-01

    A new compound, 4-hydroxy-α-tetralone-4-O-β-D-[6′-O-(3″,4″,5″-trihydroxybenzoyl) glucopyranoside (1), together with a known compound, 4-hydroxy-(-tetralone (2), has been isolated from the roots of Juglans regia.2 showed moderate bioactivity against protein tyrosine phosphatase 1B (PTP1B).

  3. Association between Gastroenterological Malignancy and Diabetes Mellitus and Anti-Diabetic Therapy: A Nationwide, Population-Based Cohort Study.

    Directory of Open Access Journals (Sweden)

    Chien-Ming Lin

    Full Text Available The relationship between diabetes mellitus (DM and cancer incidence has been evaluated in limited kinds of cancer. The effect of anti-diabetic therapy (ADT on carcinogenesis among diabetic patients is also unclear.Using population-based representative insurance claims data in Taiwan, 36,270 DM patients and 145,080 comparison subjects without DM were identified from claims from 2005 to 2010. The association between the top ten leading causes of cancer-related death in Taiwan and DM was evaluated. Whether ADT altered the risk of developing cancer was also investigated.Incidence of cancer at any site was significantly higher in patients with DM than in those without (p<0.001. The risk of carcinogenesis imparted by DM was greatest in gastroenterological malignancies (liver, pancreas, and colorectal cancer as well as lung, breast and oral cancer (p<0.001. Among the oral types of ADT, metformin decreased the risk of lung and liver cancer, but had less effect on reducing the risk of colorectal cancer. α-glucosidase inhibitor decreased the risk of developing liver, colorectal, and breast cancer. Apart from intermediate-acting insulin, rapid-acting, long-acting, and combination insulin treatment significantly reduced the overall cancer risk among all DM patients. In subgroup analysis, long-acting insulin treatment significantly decreased the risk of lung, liver, and colorectal cancer.Our results supported the notion that pre-existing DM increases the incidence of gastroenterological cancer. ADT, especially metformin, α-glucosidase inhibitor, and long-acting insulin treatment, may protect patients with DM against these malignancies. It is crucial that oncologists should closely collaborate with endocrinologists to provide an optimal cancer-specific therapy and diabetic treatment to patients simultaneously with cancer and DM.

  4. Systematic review of antimicrobials, mucosal coating agents, anesthetics, and analgesics for the management of oral mucositis in cancer patients.

    NARCIS (Netherlands)

    Saunders, D.P.; Epstein, J.B.; Elad, S.; Allemano, J.; Bossi, P.; Wetering, M.D. van de; Rao, N.G.; Potting, C.M.J.; Cheng, K.K.; Freidank, A.; Brennan, M.T.; Bowen, J.; Dennis, K.; Lalla, R.V.

    2013-01-01

    PURPOSE: The aim of this project was to develop clinical practice guidelines on the use of antimicrobials, mucosal coating agents, anesthetics, and analgesics for the prevention and management of oral mucositis (OM) in cancer patients. METHODS: A systematic review of the available literature was

  5. The effect of structured education to patients receiving oral agents for cancer treatment on medication adherence and self-efficacy

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    Gamze Tokdemir

    2017-01-01

    Full Text Available Objective: This study was conducted to examine the effect of structured education on medication adherence and self-efficacy through the use of the MASCC Oral Agent Teaching Tool (MOATT for patients receiving oral agents for cancer treatment. Methods: This quasi-experimental study has been conducted at two hospitals; 41 patients were included in the study. Data were obtained using a questionnaire, medication adherence self-efficacy scale (MASES, memorial symptom assessment scale, and a follow-up form (diary. Patients were educated through the use of the MOATT at a scheduled time; drug-specific information was provided along with a treatment scheme and follow-up diary. Phone interviews were completed 1 and 2 weeks after the educational session. At the next treatment cycle, the patients completed the same questionnaires. Results: Majority of the patients were receiving capecitabine (90.2%; n = 37 as an oral agent for breast (51.2%; n = 21 and stomach cancer (24.6%; n = 10 treatment. About 90.2% of patients (n = 37 stated that they did not forget to take their medication and experienced medication-related side effects (78%; n = 32. The total score of MASES was increased after the education (66.39 vs. 71.04, P < 0.05. Conclusions: It was shown that individual education with the MOATT and follow-up for patients receiving oral agents for cancer treatment increased patient medication adherence self-efficacy.

  6. Systematic review of antimicrobials, mucosal coating agents, anesthetics, and analgesics for the management of oral mucositis in cancer patients.

    NARCIS (Netherlands)

    Saunders, D.P.; Epstein, J.B.; Elad, S.; Allemano, J.; Bossi, P.; Wetering, M.D. van de; Rao, N.G.; Potting, C.M.J.; Cheng, K.K.; Freidank, A.; Brennan, M.T.; Bowen, J.; Dennis, K.; Lalla, R.V.

    2013-01-01

    PURPOSE: The aim of this project was to develop clinical practice guidelines on the use of antimicrobials, mucosal coating agents, anesthetics, and analgesics for the prevention and management of oral mucositis (OM) in cancer patients. METHODS: A systematic review of the available literature was con

  7. 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.

  8. Insulin versus an oral antidiabetic agent as add-on therapy in type 2 diabetes after failure of an oral antidiabetic regimen: a meta-analysis

    OpenAIRE

    Gamble, JM; Simpson, Scot H.; Brown, Lauren C.; Johnson, Jeffrey A

    2008-01-01

    Background Although evidence-based guidelines for the treatment of type 2 diabetes mellitus provide clear recommendations for initial therapy, evidence on an optimal treatment strategy after secondary failure is unclear. Purpose To compare the efficacy of add-on therapy using basal insulin versus an additional oral antidiabetic agent in patients with type 2 diabetes and secondary failure. Data sources We searched the following electronic databases from inception until June 2007: MEDLINE; EMBA...

  9. Anti-diabetic Effects of Polysaccharides from Ethanol-insoluble Residue of Schisandra chinensis(Turcz.) Baill on Alloxan-induced Diabetic Mice

    Institute of Scientific and Technical Information of China (English)

    ZHAO Ting; WU Xiang-yang; MAO Guang-hua; ZHANG Min; LI Fang; ZOU Ye; ZHOU Ye; ZHENG Wei; ZHENG Da-heng; YANG Liu-qing

    2013-01-01

    The ethanol-insoluble residue of Schisandra generated during lignans industrial production is usually treated as solid waste.However,there is active polysaccharide which could be used in it.In this work,the water-soluble polysaccharides from the ethanol-insoluble residue of Schisandra(ESCP) were obtained and their anti-diabetic effect was evaluated.The results indicate that ESCP could significantly reduce the blood glucose level in alloxan-induced diabetic mice.Moreover,the ESCP could significantly improve the lipid metabolism and increase the content of liver glycogen in ailoxan-induced diabetic mice.The results indicate that ESCP could be developed into a potential natural hypoglycemic agent.

  10. Anti-diabetic related health food properties of traditional rice (Oryza sativa L. in Sri Lanka

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    Walimuni Kanchana Subhashini Mendis Abeysekera

    2015-10-01

    Full Text Available Objective: To evaluate a range of anti-diabetic related properties and some consumer preferred physicochemical properties of selected Sri Lankan traditional rice varieties. Methods: Sudu Heeneti, Goda Heeneti, Masuran and Dik Wee varieties were used in this study. Anti-diabetic related properties of bran extracts of selected varieties were studied for methylglyoxal mediated protein glycation inhibition, acetyl and butyryl-cholinesterase inhibition in vitro and anti-hyperglycemic activity in vivo. Further, selected varieties were studied for starch hydrolysis rate in vitro. Physicochemical properties including grain color, size, shape, crude protein, crude fat, ash, dietary fiber and total carbohydrate contents were studied. Results: Brans of selected varieties had significant (P < 0.05 and dose dependent methylglyoxal mediated protein glycation inhibition [IC50: (174.77 ± 6.65 to (342.87 ± 0.43 µg/mL] and acetyl [(IC50: (37.00 ± 0.68 to (291.00 ± 3.54 µg/mL] and butyryl-cholinesterase [IC50: (18.50 ± 0.60 to (96.60 ± 0.56 µg/mL] inhibitory activities. Further, Sudu Heeneti, Masuran and Dik Wee had low starch digestion rate (52.40 ± 1.44 to 53.76 ± 1.19 indicating that these varieties may be low glycemic index rices. Brans of Masuran tested in rat model showed anti-hyperglycemic activity. Physicochemical properties studied showed that selected varieties were red in color and grain size and shape were mostly medium and bold respectively. Moisture, crude protein, crude fat, ash and total carbohydrate contents varied significantly (P < 0.05 among the varieties. Conclusions: It is concluded that selected varieties could be promoted as physicochemically sound rices with a range of anti-diabetic related properties in the management of diabetes and its complications.

  11. Use of pharmacy dispensing data to measure adherence and identify nonadherence with oral hypoglycemic agents.

    Science.gov (United States)

    Sodihardjo-Yuen, Fong; van Dijk, Liset; Wensing, Michel; De Smet, Peter A G M; Teichert, Martina

    2017-02-01

    A framework for calculation of adherence for oral hypoglycemic agents (OHAs) based on data from health-insurance claims is available. Pharmacy dispensing data aid identification of nonadherent patients in pharmacy practices. However, use of these data for calculation of OHA adherence requires additional methodological categories. We examined the impact of different methodological choices on estimation of OHA adherence using pharmacy dispensing data. Four methodological categories were added to the framework available to be used for adherence calculation with pharmacy dispensing data. Three adherence measures were defined to supply pharmacists with significant information on OHA use of their patients: (i) percentage of days covered by use periods of dispensed medication (PDC), (ii) mean rate of adherent patients with a PDC ≥80 % (MRAP80), and (iii) mean number of nonadherent patients (MNNP80) per pharmacy with a PDC pharmacies in the Netherlands. For the basic scenario, mean PDC for OHA was 88.3 %. MRAP80 was 80.3 %, which corresponded to an average of 69 nonadherent patients per pharmacy. Different choices for parameter values resulted in score variations for PDC of 85.0-91.8 %, for MRAP80 of 75.3-86.1 %, and between 49 and 92 MNNP80 per pharmacy. Sixteen methodological categories specified calculation of OHA adherence based on pharmacy dispensing data. Adherence scores expressed as percentages were relatively robust to variation in parameter values, but differed substantially for the absolute numbers of nonadherent patients per pharmacy.

  12. [Effect of new oral antimicrobial agents in outpatient treatment of pneumonia in children].

    Science.gov (United States)

    Ouchi, Kazunobu; Sunakawa, Keisuke

    2014-06-01

    In November 2004, "Guidelines for the Management of Respiratory Infectious Diseases in Children in Japan" was published ahead of the rest of the world, by Japanese Society of Pediatric Pulmonology/Japanese Society for Pediatric Infectious Diseases, based on the data on causative organisms in the lower respiratory tract. In its 2011 version, classification of the severity of pneumonia was renewed based on the latest information. As a result, many types of pneumonia in children are now classified as mild or moderate. This means that many patients who might have conventionally required hospital treatment can now be managed on an outpatient basis. The reason for realization of the wider range of outpatient treatment is the availability of two new oral antimicrobial agents, tebipenem pivoxil and tosufloxacin tosilate hydrate, for the treatment of infections in children. Analysis of data on medical expenses shows a decreased rate of hospitalization due to pneumonia year by year after launch of these two drugs, suggesting that these drugs have contributed to wider range of outpatient treatment. This manuscript discusses the effect of tebipenem pivoxil and tosufloxacin tosilate hydrate in the treatment of pneumonia.

  13. Comparative adherence to oral hormonal agents in older women with breast cancer.

    Science.gov (United States)

    Cheung, Winson Y; Lai, Edward Chia-Cheng; Ruan, Jenny Y; Chang, Jennifer T; Setoguchi, Soko

    2015-07-01

    We aim to (1) compare compliance of anastrozole, letrozole, exemestane, and tamoxifen in women and (2) identify clinical factors associated with medication non-adherence and non-persistence. Female Medicare beneficiaries who were new users of anastrozole, letrozole, exemestane, or tamoxifen between 2007 and 2010 were analyzed. Multivariate-modified Poisson and Cox regression models were constructed to compare non-adherence and non-persistence, respectively, across the different oral agents. A total of 5,150 women were included: mean age was 76.4 years, 2352 initiated anastrozole, 1401 letrozole, 248 exemestane, and 1149 tamoxifen. Non-adherence and non-persistence were 41 and 49% respectively, with exemestane being associated with the worst non-adherence and non-persistence (RR 1.57, 95% CI 1.37-1.80, p adherence (RR 0.89, 95 % CI 0.82-0.96, p = 0.002 and RR 0.84, 95 % CI 0.76-0.92, p adherence) and persistence (HR 0.86, 95 % CI 0.79-0.94, p adherence and persistence in older women with breast cancer.

  14. 2010-2012年我院抗糖尿病药物应用分析%Use of anti-diabetic drugs of 2010-2012 in our hospital

    Institute of Scientific and Technical Information of China (English)

    陈娟娟; 杨世民; 薛京会

    2013-01-01

    Objective: To analyze use of anti-diabetic drugs in our hospital from 2010 through 2012 in order to provide some references for guiding and managing clinical use of anti-diabetic drugs. Methods: We analyzed consumption sum, defined daily dose(DDD), DDDs ,DDC and constituent ratio for anti-diabetic drugs use. Results: The sales amount of anti-diabetic drugs was increasing steadily. The top 3 DDDs were insulin glargine injection, repaglinide tablets and isophane protamine biosynthetic human insulin injection(pre-mixed 30R). The top 3 DDC were epalrestat tablets,insulin glargine injection and mixed protamine zinc recombinant human insulin lispro injection(25R). Conclusion: The use of anti-diabetic drugs was most rational in our hospital from 2010 to 2012. Non-sulfonylureas insulin secretagogues were often used in the clinic. The new , expensive oral drug and insulin preparations wil occupy a larger market, and we should pay close attention to this in clinic.%目的:分析我院2010-2012年抗糖尿病药物的应用情况,为其合理用药提供依据。方法:对我院2010-2012年抗糖尿病药物的使用数据用Excel2003软件进行销售金额、用药频度(DDDs)、构成比、日均费用(DDC)等统计分析。结果:我院抗糖尿病药物的用药金额逐年稳定上升,DDDs排在前3位的为甘精胰岛素、瑞格列奈、精蛋白生物合成人胰岛素(预混30R);DDC排名前3位的为依帕司他、甘精胰岛素、精蛋白锌重组赖脯胰岛素混合注射液(25R)。结论:我院2010-2012年抗糖尿病药物的使用状况较为合理,非磺脲类促胰岛素分泌剂的选用倾向较大,口服新贵药和胰岛素制剂将会占据更大份额,临床应引起足够重视。

  15. Anti-diabetic activity of crude Pistacia lentiscus in alloxan-induced diabetes in rats

    Directory of Open Access Journals (Sweden)

    Muhammad Saad Ur Rehman

    2015-08-01

    Full Text Available The purpose of this study was to investigate the anti-diabetic effect of crude Pistacia lentiscus gum (mastic gum in alloxan-treated diabetic rat model. The crude P. lentiscus (100 mg/kg showed significant (p<0.001 reduction in blood glucose as compared to control. Liver function test also showed significant changes (p<0.001 as compared to alloxan-treated group. The results of this study showed that crude P. lentiscus gum have considerable efficacy in curing diabetes and have hepatoprotective effect.

  16. Anti-diabetic and anti-cholesterolemic activity of methanol extracts of three species ofAmaranthus

    Institute of Scientific and Technical Information of China (English)

    Girija K; Lakshman K; Udaya Chandrika; Sabhya Sachi Ghosh; Divya T

    2011-01-01

    Objective:To investigate the anti-diabetic and anti-cholesterolemic activity of methanol extracts of leaves ofAmaranthus caudatus,Amaranthus spinosus andAmaranthus viridis in normal and streptozotocin (STZ) induced diabetic rats.Methods:In this study, the anti-diabetic and anti-cholesterolemic activity of methanol extracts of leaves of all three plants was evaluated by using normal andSTZ induced diabetic rats at a dose of200 mg/kg and400 mg/kg p.o.daily for21days. Blood glucose levels and body weight were monitored at specific intervals, and different biochemical parameters, serum cholesterol, serum triglyceride, high density lipoprotein, low density lipoprotein and very low density lipoprotein were also assessed in the experimental animals. Histology of pancreas was performed.Results:It was found that all the three plants at 400 mg/kg dose showed significant anti-diabetic and anti-cholesterolemic activity (P<0.01), while at200 mg/kg dose less significant anti-diabetic activity (P<0.05) was observed.Conclusions:Methanol extracts ofAmaranthus caudatus,Amaranthus spinosus andAmaranthus viridis showed significant anti-diabetic and anti-cholesterolemic activity, which provides the scientific proof for their traditional claims.

  17. Assessing the effect of treatment duration on the association between anti-diabetic medication and cancer risk.

    Directory of Open Access Journals (Sweden)

    Anna But

    Full Text Available Most studies that have evaluated the association between anti-diabetic medication and cancer risk have suffered from methodological drawbacks. To avoid time-related biases, we evaluated the effect of treatment duration on the cancer risk among naive users of anti-diabetic medication as compared to non-users. In addition, we addressed the influence of common risk factors such as smoking and BMI. The study population comprised 23,394 participants of FINRISK surveys. Data on cancer and anti-diabetic medication were linked with the study cohorts. We applied Lexis tabulation to the data and analyzed split records by using Poisson regression. Changes in cancer incidence in relation to treatment duration were examined by modeling the rate ratio (RR. After a median follow-up of 9 years, 53 cancer cases among users of anti-diabetic medication and 1,028 among non-users were diagnosed. No significant difference in cancer risk between users and non-users was observed after adjustment. The RR for all medication regardless of its duration was 1.01 [95% CI 0.75-1.33], and 1.37 [0.94-1.94] for period of 1-4 years. The results were similar for metformin, sulfonylurea, and insulin. This study demonstrates that evaluation of the variation in cancer risk in relation to treatment duration is of particular importance for enhancing the accuracy of conclusions on the link between exposure to anti-diabetic medication and cancer risk.

  18. C{sub 18}-attached membrane funnel-based spray ionization mass spectrometry for quantification of anti-diabetic drug from human plasma

    Energy Technology Data Exchange (ETDEWEB)

    Li, Wan [Department of Chemistry, The Chinese University of Hong Kong, Hong Kong Special Administrative Region (Hong Kong); Chen, Xiangfeng, E-mail: xiangfchensdas@163.com [Department of Chemistry, The Chinese University of Hong Kong, Hong Kong Special Administrative Region (Hong Kong); Shandong Analysis and Test Centre, Shandong Academy of Sciences, Jinan, Shandong (China); Wong, Y.-L. Elaine; Hung, Y.-L. Winnie; Wang, Ze; Deng, Liulin [Department of Chemistry, The Chinese University of Hong Kong, Hong Kong Special Administrative Region (Hong Kong); Dominic Chan, T.-W., E-mail: twdchan@cuhk.edu.hk [Department of Chemistry, The Chinese University of Hong Kong, Hong Kong Special Administrative Region (Hong Kong)

    2016-08-24

    In this work, sorbent-attached membrane funnel-based spray ionization mass spectrometry was explored for quantitative analysis of anti-diabetic drugs spiked in human plasma. C{sub 18}-attached membrane funnel was fabricated for in situ extraction and clean-up to alleviate matrix suppression effect in the ionization process. Repaglinide was used as a target analyte of anti-diabetic drugs. Under optimal working conditions, good linearity (R{sup 2} > 0.99) was obtained in the concentration range of 1–100 ng mL{sup −1}. The method detection limit of target drugs spiked in the human plasma was around 0.30 ng mL{sup −1}. Through the application of an isotope-labeled internal standard, the signal fluctuation caused by residual background matrices was largely alleviated and the precision of measurement (RSD) was below 15%. The recovery of repaglinide for 5, 25, and 100 ng mL{sup −1} of spiked human plasma matrixes ranged from 87% to 112%. The developed method was successfully applied to determine repaglinide in plasma volunteers who orally received a dose of drug association. Our results demonstrated that membrane funnel-based spray is a simple and sensitive method for rapid screening analysis of complex biological samples. - Highlights: • Sorbent attached membrane funnel based spray platform was used for drug determination in human plasma. • The matrix suppression effect of human plasma was largely eliminated. • The method was applied to determine repaglinide in plasma volunteers. • Membrane funnel-based spray is promising for analysis of biological samples.

  19. Anti-Diabetic Potential of Noni: The Yin and the Yang

    Directory of Open Access Journals (Sweden)

    Pratibha V. Nerurkar

    2015-09-01

    Full Text Available Escalating trends of chronic diseases such as type-2 diabetes (T2D have sparked a renewed interest in complementary and alternative medicine, including herbal products. Morinda citrifolia (noni has been used for centuries by Pacific Islanders to treat various ailments. Commercial noni fruit juice has been marketed as a dietary supplement since 1996. In 2003, the European Commission approved Tahitian noni juice as a novel food by the Health and Consumer Protection Directorate General. Among noni’s several health benefits, others and we have demonstrated the anti-diabetic effects of fermented noni fruit juice in animal models. Unfortunately, noni’s exciting journey from Polynesian medicine to the research bench does not reach its final destination of successful clinical outcomes when translated into commercial products. Noni products are perceived to be safe due to their “natural” origin. However, inadequate evidence regarding bioactive compounds, molecular targets, mechanism of action, pharmacokinetics, long-term safety, effective dosages, and/or unanticipated side effects are major roadblocks to successful translation “from bench side to bedside”. In this review we summarize the anti-diabetic potential of noni, differences between traditional and modern use of noni, along with beneficial clinical studies of noni products and challenges in clinical translation of noni’s health benefits.

  20. Anti-Diabetic Potential of Noni: The Yin and the Yang.

    Science.gov (United States)

    Nerurkar, Pratibha V; Hwang, Phoebe W; Saksa, Erik

    2015-01-01

    Escalating trends of chronic diseases such as type-2 diabetes (T2D) have sparked a renewed interest in complementary and alternative medicine, including herbal products. Morinda citrifolia (noni) has been used for centuries by Pacific Islanders to treat various ailments. Commercial noni fruit juice has been marketed as a dietary supplement since 1996. In 2003, the European Commission approved Tahitian noni juice as a novel food by the Health and Consumer Protection Directorate General. Among noni's several health benefits, others and we have demonstrated the anti-diabetic effects of fermented noni fruit juice in animal models. Unfortunately, noni's exciting journey from Polynesian medicine to the research bench does not reach its final destination of successful clinical outcomes when translated into commercial products. Noni products are perceived to be safe due to their "natural" origin. However, inadequate evidence regarding bioactive compounds, molecular targets, mechanism of action, pharmacokinetics, long-term safety, effective dosages, and/or unanticipated side effects are major roadblocks to successful translation "from bench side to bedside". In this review we summarize the anti-diabetic potential of noni, differences between traditional and modern use of noni, along with beneficial clinical studies of noni products and challenges in clinical translation of noni's health benefits.

  1. Triglyceride/HDL ratio as a screening tool for predicting success at reducing anti-diabetic medications following weight loss.

    Directory of Open Access Journals (Sweden)

    Ghanshyam Palamaner Subash Shantha

    Full Text Available BACKGROUND AND OBJECTIVES: Intentional weight loss, by reducing insulin resistance, results in both better glycemic control and decreased need for anti-diabetic medications. However, not everyone who is successful with weight loss is able to reduce anti-diabetic medication use. In this retrospective cohort study, we assessed the predictive accuracy of baseline triglyceride (TGL/HDL ratio, a marker of insulin resistance, to screen patients for success in reducing anti-diabetic medication use with weight loss. METHODS: Case records of 121 overweight and obese attendees at two outpatient weight management centers were analyzed. The weight loss intervention consisted of a calorie-restricted diet (~1000Kcal/day deficit, a behavior modification plan, and a plan for increasing physical activity. RESULTS: Mean period of follow-up was 12.5 ± 3.5 months. By study exit, mean weight loss and mean HbA1c% reduction were 15.4 ± 5.5 kgs and 0.5 ± 0.2% respectively. 81 (67% in the study cohort achieved at least 1 dose reduction of any anti-diabetic medication. Tests for predictive accuracy of baseline TGL/HDL ratio ≤ 3 to determine success with dose reductions of anti-diabetic medications showed a sensitivity, specificity, positive predictive value, negative predictive value, area under the curve, likelihood ratio (LR + and LR-of 81, 83, 90, 70, 78, 4.8 and 0.2, respectively. Reproducibility of TGL/HDL ratio was acceptable. CONCLUSION: TGL/HDL ratio shows promise as an effective screening tool to determine success with dose reductions of anti-diabetic medications. The results of our study may inform the conduct of a systematic review using data from prior weight loss trials.

  2. Triglyceride/HDL ratio as a screening tool for predicting success at reducing anti-diabetic medications following weight loss.

    Science.gov (United States)

    Palamaner Subash Shantha, Ghanshyam; Kumar, Anita Ashok; Kahan, Scott; Irukulla, Pavan Kumar; Cheskin, Lawrence Jay

    2013-01-01

    Intentional weight loss, by reducing insulin resistance, results in both better glycemic control and decreased need for anti-diabetic medications. However, not everyone who is successful with weight loss is able to reduce anti-diabetic medication use. In this retrospective cohort study, we assessed the predictive accuracy of baseline triglyceride (TGL)/HDL ratio, a marker of insulin resistance, to screen patients for success in reducing anti-diabetic medication use with weight loss. Case records of 121 overweight and obese attendees at two outpatient weight management centers were analyzed. The weight loss intervention consisted of a calorie-restricted diet (~1000Kcal/day deficit), a behavior modification plan, and a plan for increasing physical activity. Mean period of follow-up was 12.5 ± 3.5 months. By study exit, mean weight loss and mean HbA1c% reduction were 15.4 ± 5.5 kgs and 0.5 ± 0.2% respectively. 81 (67%) in the study cohort achieved at least 1 dose reduction of any anti-diabetic medication. Tests for predictive accuracy of baseline TGL/HDL ratio ≤ 3 to determine success with dose reductions of anti-diabetic medications showed a sensitivity, specificity, positive predictive value, negative predictive value, area under the curve, likelihood ratio (LR) + and LR-of 81, 83, 90, 70, 78, 4.8 and 0.2, respectively. Reproducibility of TGL/HDL ratio was acceptable. TGL/HDL ratio shows promise as an effective screening tool to determine success with dose reductions of anti-diabetic medications. The results of our study may inform the conduct of a systematic review using data from prior weight loss trials.

  3. Pharmacoeconomic comparison of ziprasidone with other atypical oral antipsychotic agents in schizophrenia

    Directory of Open Access Journals (Sweden)

    Andrea Fagiolini

    2011-03-01

    Full Text Available Objective: to comparatively investigate – by means of computer simulations – the economic cost and clinical outcomes of five atypical oral antipsychotic agents (ziprasidone, olanzapina, risperidone, paliperidone and aripiprazolo.Methods: a cyclical stochastic model representing patient evolution, taking into account main adverse reactions (akathisia, weight gain and extra-pyramidal ARs, drug efficacy on psychosis stabilization and probability of relapse, was developed. Ten different scenarios were compared, each starting with one of the considered antipsychotics, prescribed either at home or in a hospital setting. Switching to another medication was allowed until no untried drugs were available, in which case clozapine treatment or admission to a Psychiatric Therapeutic Rehabilitation Center were irreversibly assigned. Model inputs were probabilities of ARs, probabilities of stabilization and probabilities of destabilization (assumed equal for all; as well as costs attributable to drugs, hospitalization, outpatient care and costs adverse reactions in terms of concomitant medications. Sources for the inputs were the trials reported in the most recent literature (from the year 2000, selected based on the homogeneity of the observational period and antipsychotic dosage used.Results: in each scenario, the hospitalization cost represented the highest component of the overall cost (approximately 67%. Assuming equal drug effectiveness, ziprasidone fared better than all other considered competitors, showing the lowest average annual costs per patient (and also the lowest average annual hospitalization costs as well as the largest numbers of controlled months without adverse reactions, independently of the initial setting. Conclusions: the most important determinant of total cost appears to be hospitalization, whose cost is about 600% higher than the medications cost. Medication effectiveness and tolerability remain however of utmost importance for

  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. N-succinyl chitosan as buccal penetration enhancer for delivery of herbal agents in treatment of oral mucositis.

    Science.gov (United States)

    Dhawan, Neha; Kumar, Krishan; Kalia, A N; Arora, Saahil

    2014-01-01

    Oral mucositis is one of the major side effects of cancer chemotherapy (30-76%) and radiotherapy (over 50%). Current palliative treatments of oral mucositis include specialized agents like pelifermin, platelet derived factors etc. or oral hygienic agents which suffered from various drawbacks like systemic side effect, least effect owing to fast wash out of buccal mucosa, patient unfriendly delivery systems, and mere symptomatic relief. In this research work, N-succinyl chitosan gel delivery system of microemulsified eugenol, honey and sodium hyaluronate was prepared to explore their multiple and synergistic effects on various pathological factors of oral mucositis. N-succinyl chitosan was synthesized in our laboratory and loaded with microemulsified eugenol (10% v/v), honey (10% v/v) and sodium hyaluronate (0.2% w/v) to prepare orogel with optimum pH, spreadability, mucoadhesion strength, and viscosity. In vitro eugenol release from N-succinyl chitosan gel after 8 hours in PBS (pH-6.4) was found to be 87.45±0.14%, which was better in comparison to that released from chitosan gel. Ex vivo penetration studies using rat buccal mucosal tissue also suggested better J-efflux of eugenol through N-succinyl chitosan in comparison to chitosan gel with enhancement ratio (ER) of 1.71. The antimicrobial effect of N-succinyl chitosan based orogel against S. aureus and C. albicans efficacy was found to be statistically high in comparison to chitosan based orogel as well as marketed formulation of chlorhexidine (pgel formulation within 15 days. The formulation was successful in elevating the survival and reducing the inflammation in the oral mucosa of animals compared to disease control (p<0.05) and hence suggesting the potential of N-succinyl chitosan orogel in the treatment of oral mucositis.

  6. A new manganese-based oral contrast agent (CMC-001) for liver MRI. Pharmacological and pharmaceutical aspects

    Energy Technology Data Exchange (ETDEWEB)

    Joergensen, Jan Troest [Research and Development, CMC Contrast AB, Scion DTU, Lyngby (Denmark)], email: jtj@cmc-contrast.dk; Rief, Matthias; Wagner, Moritz [Dept. of Radiology, Charite - Universitaetsmedizin Berlin, Berlin (Germany); Brismar, Torkel B.; Albiin, Nils [Dept. of Radiology, Karolinska Inst., Karolinska Univ. Hospital, Stockholm (Sweden)

    2012-09-15

    Manganese is one of the most abundant metals on earth and is found as a component of more than 100 different minerals. Besides being an essential trace element in relation to the metabolic processes in the body, manganese is also a paramagnetic metal that possesses similar characteristics to gadolinium with regards to T1-weighted (T1-w) magnetic resonance imaging (MRI). Manganese, in the form of manganese (II) chloride tetrahydrate, is the active substance in a new targeted oral contrast agent, currently known as CMC-001, indicated for hepatobiliary MRI. Under physiological circumstances manganese is poorly absorbed from the intestine after oral intake, but by the use of specific absorption promoters, L-alanine and vitamin D3, it is possible to obtain a sufficiently high concentration in the liver in order to achieve a significant signal enhancing effect. In the liver manganese is exposed to a very high first-pass effect, up to 98 %, which prevents the metal from reaching the systemic circulation, thereby reducing the number of systemic side-effects. Manganese is one of the least toxic trace elements, and due to its favorable safety profile it may be an attractive alternative to gadolinium-based contrast agents for patients undergoing an MRI evaluation for liver metastases in the future. In this review the basic pharmacological and pharmaceutical aspects of this new targeted oral hepatobiliary specific contrast agent will be discussed.

  7. Enteric-coated tablet of risedronate sodium in combination with phytic acid, a natural chelating agent, for improved oral bioavailability.

    Science.gov (United States)

    Kim, Jeong S; Jang, Sun W; Son, Miwon; Kim, Byoung M; Kang, Myung J

    2016-01-20

    The oral bioavailability (BA) of risedronate sodium (RS), an antiresorptive agent, is less than 1% due to its low membrane permeability as well as the formation of non-absorbable complexes with multivalent cations such as calcium ion (Ca(2+)) in the gastrointestinal tract. In the present study, to increase oral BA of the bisphosphonate, a novel enteric-coated tablet (ECT) dosage form of RS in combination with phytic acid (IP6), a natural chelating agent recognized as safe, was formulated. The chelating behavior of IP6 against Ca(2+), including a stability constant for complex formulation was characterized using the continuous variation method. Subsequently, in vitro dissolution profile and in vivo pharmacokinetic profile of the novel ECT were evaluated comparatively with that of the marketed product (Altevia, Sanofi, US), an ECT containing ethylenediaminetetraacetic acid (EDTA) as a chelating agent, in beagle dogs. The logarithm of stability constant for Ca(2+)-IP6 complex, an equilibrium constant approximating the strength of the interaction between two chemicals to form complex, was 19.05, which was 3.9-fold (pIP6-containing ECT were approximately 7.9- (pIP6 for an oral therapy with the bisphosphonate for improved BA. Copyright © 2015 Elsevier B.V. All rights reserved.

  8. A new manganese-based oral contrast agent (CMC-001) for liver MRI: pharmacological and pharmaceutical aspects.

    Science.gov (United States)

    Jørgensen, Jan Trøst; Rief, Matthias; Brismar, Torkel B; Wagner, Moritz; Albiin, Nils

    2012-09-01

    Manganese is one of the most abundant metals on earth and is found as a component of more than 100 different minerals. Besides being an essential trace element in relation to the metabolic processes in the body, manganese is also a paramagnetic metal that possesses similar characteristics to gadolinium with regards to T1-weighted (T1-w) magnetic resonance imaging (MRI). Manganese, in the form of manganese (II) chloride tetrahydrate, is the active substance in a new targeted oral contrast agent, currently known as CMC-001, indicated for hepatobiliary MRI. Under physiological circumstances manganese is poorly absorbed from the intestine after oral intake, but by the use of specific absorption promoters, L-alanine and vitamin D(3), it is possible to obtain a sufficiently high concentration in the liver in order to achieve a significant signal enhancing effect. In the liver manganese is exposed to a very high first-pass effect, up to 98%, which prevents the metal from reaching the systemic circulation, thereby reducing the number of systemic side-effects. Manganese is one of the least toxic trace elements, and due to its favorable safety profile it may be an attractive alternative to gadolinium-based contrast agents for patients undergoing an MRI evaluation for liver metastases in the future. In this review the basic pharmacological and pharmaceutical aspects of this new targeted oral hepatobiliary specific contrast agent will be discussed.

  9. ZnO and TiO2 nanoparticles as novel antimicrobial agents for oral hygiene: a review

    Science.gov (United States)

    Khan, Shams Tabrez; Al-Khedhairy, Abdulaziz A.; Musarrat, Javed

    2015-06-01

    Oral cavity is inhabited by more than 25,000 different bacterial phylotypes; some of them cause systemic infections in addition to dental and periodontal diseases. Emergence of multiple antibiotic resistance among these bacteria necessitates the development of alternative antimicrobial agents that are safe, stable, and relatively economic. This review focuses on the significance of metal oxide nanoparticles, especially zinc oxide and titanium dioxide nanoparticles as supplementary antimicrobials for controlling oral infections and biofilm formation. Indeed, the ZnO NPs and TiO2 NPs have exhibited significant antimicrobial activity against oral bacteria at concentrations which is not toxic in in vivo toxicity assays. These nanoparticles are being produced at an industrial scale for use in a variety of commercial products including food products. Thus, the application of ZnO and TiO2 NPs as nanoantibiotics for the development of mouthwashes, dental pastes, and other oral hygiene materials is envisaged. It is also suggested that these NPs could serve as healthier, innocuous, and effective alternative for controlling both the dental biofilms and oral planktonic bacteria with lesser side effects and antibiotic resistance.

  10. ZnO and TiO{sub 2} nanoparticles as novel antimicrobial agents for oral hygiene: a review

    Energy Technology Data Exchange (ETDEWEB)

    Khan, Shams Tabrez, E-mail: shamsalig75@gmail.com; Al-Khedhairy, Abdulaziz A. [King Saud University, Department of Zoology, College of Science (Saudi Arabia); Musarrat, Javed [AMU, Department of Agricultural Microbiology, Faculty of Agricultural Sciences (India)

    2015-06-15

    Oral cavity is inhabited by more than 25,000 different bacterial phylotypes; some of them cause systemic infections in addition to dental and periodontal diseases. Emergence of multiple antibiotic resistance among these bacteria necessitates the development of alternative antimicrobial agents that are safe, stable, and relatively economic. This review focuses on the significance of metal oxide nanoparticles, especially zinc oxide and titanium dioxide nanoparticles as supplementary antimicrobials for controlling oral infections and biofilm formation. Indeed, the ZnO NPs and TiO{sub 2} NPs have exhibited significant antimicrobial activity against oral bacteria at concentrations which is not toxic in in vivo toxicity assays. These nanoparticles are being produced at an industrial scale for use in a variety of commercial products including food products. Thus, the application of ZnO and TiO{sub 2} NPs as nanoantibiotics for the development of mouthwashes, dental pastes, and other oral hygiene materials is envisaged. It is also suggested that these NPs could serve as healthier, innocuous, and effective alternative for controlling both the dental biofilms and oral planktonic bacteria with lesser side effects and antibiotic resistance.

  11. Preschool teachers as agents of oral health promotion: an intervention study in Sri Lanka.

    Science.gov (United States)

    Fernando, S; Kanthi, R D F C; Johnson, N W

    2013-09-01

    According to National Oral Health Survey reports and research, Early Childhood Caries has been identified as a serious public health problem in Sri Lanka. More than 65% of preschool-aged children have dental decay and only 2% of them have had treatment. With proper interventions and commitment from public health personnel and responsible community leaders this should be a largely preventable disease. An intervention study was conducted among preschool teachers in the District of Colombo, Sri Lanka, to assess their influence on oral health promotion in the school environment. All the available 52 preschools and all 72 teachers registered under a local government authority were involved in the study. Preschools were divided into intervention group and control group based on geographically defined areas. The intervention included training preschool teachers using a manual covering health education, health promotion, incorporation of oral-health-friendly activities into the preschool curriculum, and hands-on experience of oral examination. Pre- and post- assessments were conducted with a 6 month interval. After 6 months, the median oral health knowledge score of the intervention group improved from 55 to 72 (p = 0.005) and the mean score for oral health related practices from 32 to 35 (p = 0.032). The variables: oral-health-friendly preschool environment (p = 0.02), availability of brushing facilities (p = 0.005) and availability of information, education and communication materials related to oral health (p = 0.004) were significantly different between the two groups after 6 months. Oral health promotion activities can be effectively instilled in a pre-school environment by the education of teachers.

  12. Anti Diabetic Plants Present In West Godavari District Of Andhra Pradesh India- A Short Review.

    Directory of Open Access Journals (Sweden)

    Venkata Narasimha Kadali

    2016-02-01

    Full Text Available Diabetes is considered as one of the chronic disease more prevalent in India and rest of the world. Chronic hyperglycemia leads to the destruction of different organs in the body.There are lots of synthetic drugs present in the market for the treatment of diabetes but they are prone to noxious effects to human systems. Herbs have natural inhibiting potency against various sorts of diseases and they are the ultimate source of bio active compounds which lacks toxic effects. Medicinal plants which have potent anti hyperglycemic effect have been identified and proved experimentally. In this short review an attempt has been made to review some of the medicinal plants such as Annona reticulata, Carica papaya, Coccinia grandis, Moringa oleifera, Murraya koenigi etc., of about 10 species which are proved to be anti diabetic present in the west godavari district of Andhra Pradesh, India.

  13. Estimation of trace elements in some anti-diabetic medicinal plants using PIXE technique

    Energy Technology Data Exchange (ETDEWEB)

    Naga Raju, G.J. [Swami Jnanananda Laboratories for Nuclear Research, Andhra University, Visakhapatnam-530 003, Andhra Pradesh (India); Sarita, P. [Swami Jnanananda Laboratories for Nuclear Research, Andhra University, Visakhapatnam-530 003, Andhra Pradesh (India); Ramana Murty, G.A.V. [Swami Jnanananda Laboratories for Nuclear Research, Andhra University, Visakhapatnam-530 003, Andhra Pradesh (India); Ravi Kumar, M. [Swami Jnanananda Laboratories for Nuclear Research, Andhra University, Visakhapatnam-530 003, Andhra Pradesh (India); Seetharami Reddy, B. [Swami Jnanananda Laboratories for Nuclear Research, Andhra University, Visakhapatnam-530 003, Andhra Pradesh (India); John Charles, M. [Swami Jnanananda Laboratories for Nuclear Research, Andhra University, Visakhapatnam-530 003, Andhra Pradesh (India); Lakshminarayana, S. [Swami Jnanananda Laboratories for Nuclear Research, Andhra University, Visakhapatnam-530 003, Andhra Pradesh (India); Seshi Reddy, T. [Swami Jnanananda Laboratories for Nuclear Research, Andhra University, Visakhapatnam-530 003, Andhra Pradesh (India); Reddy, S. Bhuloka [Swami Jnanananda Laboratories for Nuclear Research, Andhra University, Visakhapatnam-530 003, Andhra Pradesh (India)]. E-mail: sbr-r@yahoo.com; Vijayan, V. [Institute of Physics, Sachivalaya Marg, Bhubaneswar-751 005, Orissa (India)

    2006-08-15

    Trace elemental analysis was carried out in various parts of some anti-diabetic medicinal plants using PIXE technique. A 3 MeV proton beam was used to excite the samples. The elements Cl, K, Ca, Ti, Cr, Mn, Fe, Ni, Cu, Zn, Br, Rb and Sr were identified and their concentrations were estimated. The results of the present study provide justification for the usage of these medicinal plants in the treatment of diabetes mellitus (DM) since they are found to contain appreciable amounts of the elements K, Ca, Cr, Mn, Cu, and Zn, which are responsible for potentiating insulin action. Our results show that the analyzed medicinal plants can be considered as potential sources for providing a reasonable amount of the required elements other than diet to the patients of DM. Moreover, these results can be used to set new standards for prescribing the dosage of the herbal drugs prepared from these plant materials.

  14. Oral available agents in the treatment of relapsing remitting multiple sclerosis an overview of merits and culprits

    Directory of Open Access Journals (Sweden)

    Thöne J

    2013-02-01

    Full Text Available Jan Thöne, Gisa Ellrichmann Department of Neurology, St Josef-Hospital Bochum, Ruhr-University Bochum, Bochum, Germany Abstract: Multiple sclerosis (MS is a chronic immunological disease of the central nervous system characterized by early inflammatory demyelination and subsequent neurodegeneration. Major therapeutic progress has occurred during the past decade, in particular since the introduction of immunomodulatory agents, however, MS is still an incurable disease. In addition, parenteral application of the currently licensed drugs is associated with injection-related adverse events (AEs and low patient compliance. Thus, there remains an unmet need for the development of more effective and well tolerated oral therapies for the treatment of MS. A number of new orally administered agents including fingolimod, laquinimod, teriflunomide, cladribine, and BG-12 have been licensed recently or are currently under investigation in relapsing remitting MS patients. In multi-center, randomized, placebo-controlled phase III clinical studies, all of these agents have already shown their efficacy on both clinical disease parameters and magnetic resonance imaging-based measures of disease activity in patients with relapsing remitting MS. However, there are essential differences concerning their clinical efficacy and side-effect profiles. Additionally, the mechanisms by which these substances exert clinical efficacy have not been fully elucidated. In this article, we review the pharmaceutical properties of fingolimod, laquinimod, teriflunomide, cladribine, and BG-12; and their suggested mechanisms of action, clinical efficacy, and side-effect profiles. Keywords: cladribine, fingolimod (FTY, fumaric acid esters (BG-12, laquinimod, teriflunomide

  15. Antioxidant agents: a future alternative approach in the prevention and treatment of radiation-induced oral mucositis?

    Science.gov (United States)

    de Freitas Cuba, Letícia; Salum, Fernanda Gonçalves; Cherubini, Karen; de Figueiredo, Maria Antonia Zancanaro

    2015-01-01

    Radiotherapy is a therapeutic modality frequently employed for patients with head and neck cancer (HNC). It destroys tumor cells, but it is not selective, also affecting healthy tissues and producing adverse effects. One that stands out is oral mucositis because of the morbidity that it is capable of causing. This lesion is characterized by the presence of erythema, ulcerations, pain, opportunistic infections, and weight loss. These side effects can lead to serious situations that require the interruption of the antineoplastic treatment and can result in hospitalization and even death. The complex mechanisms linked to the pathogenesis of oral mucositis were recently established, and since then, the control of oxidative stress (OS) has been tied to the prevention and management of this disease. The authors have carried out a review of the literature about the use of antioxidant agents in the prevention and treatment of radiation-induced oral mucositis, using the PubMed database. This review has shown that the research on use of antioxidants (AOX) has proved insufficient to justify suggesting the products in treatment protocols. Results are promising, however, and AOX may represent a future alternative in the prevention and treatment of oral mucositis.

  16. Combination of Estrogen and Immunosuppressive Agents to Establish a Mouse Model of Candidiasis with Concurrent Oral and Vaginal Mucosal Infection.

    Science.gov (United States)

    Wang, Le; Wang, Chong; Mei, Huan; Shen, Yongnian; Lv, Guixia; Zeng, Rong; Zhan, Ping; Li, Dongmei; Liu, Weida

    2016-02-01

    Mouse model is an appropriate tool for pathogenic determination and study of host defenses during the fungal infection. Here, we established a mouse model of candidiasis with concurrent oral and vaginal mucosal infection. Two C. albicans strains sourced from clinical candidemia (SC5314) and mucosal infection (ATCC62342) were tested in ICR mice. The different combinational panels covering estrogen and immunosuppressive agents, cortisone, prednisolone and cyclophosphamide were used for concurrent oral and vaginal candidiasis establishment. Prednisolone in combination with estrogen proved an optimal mode for concurrent mucosal infection establishment. The model maintained for 1 week with fungal burden reached at least 10(5) cfu/g of tissue. This mouse model was evaluated by in vivo pharmacodynamics of fluconazole and host mucosal immunity of IL-17 and IL-23. Mice infected by SC5314 were cured by fluconazole. An increase in IL-23 in both oral and vaginal homogenates was observed after infection, while IL-17 only had a prominent elevation in oral tissue. This model could properly mimic complicated clinical conditions and provides a valuable means for antifungal assay in vivo and may also provide a useful method for the evaluation of host-fungal interactions.

  17. Influence of mycotoxins and a mycotoxin adsorbing agent on the oral bioavailability of commonly used antibiotics in pigs.

    Science.gov (United States)

    Goossens, Joline; Vandenbroucke, Virginie; Pasmans, Frank; De Baere, Siegrid; Devreese, Mathias; Osselaere, Ann; Verbrugghe, Elin; Haesebrouck, Freddy; De Saeger, Sarah; Eeckhout, Mia; Audenaert, Kris; Haesaert, Geert; De Backer, Patrick; Croubels, Siska

    2012-04-01

    It is recognized that mycotoxins can cause a variety of adverse health effects in animals, including altered gastrointestinal barrier function. It is the aim of the present study to determine whether mycotoxin-contaminated diets can alter the oral bioavailability of the antibiotics doxycycline and paromomycin in pigs, and whether a mycotoxin adsorbing agent included into diets interacts with those antibiotics. Experiments were conducted with pigs utilizing diets that contained blank feed, mycotoxin-contaminated feed (T-2 toxin or deoxynivalenol), mycotoxin-contaminated feed supplemented with a glucomannan mycotoxin binder, or blank feed supplemented with mycotoxin binder. Diets with T-2 toxin and binder or deoxynivalenol and binder induced increased plasma concentrations of doxycycline administered as single bolus in pigs compared to diets containing blank feed. These results suggest that complex interactions may occur between mycotoxins, mycotoxin binders, and antibiotics which could alter antibiotic bioavailability. This could have consequences for animal toxicity, withdrawal time for oral antibiotics, or public health.

  18. Efficacy and tolerability of pioglitazone in patients with type 2 diabetes mellitus: comparison with other oral antihyperglycaemic agents.

    Science.gov (United States)

    Derosa, Giuseppe

    2010-10-22

    Diabetes mellitus is a debilitating disease that is estimated to affect 366 million people by the year 2030. Type 2 diabetes mellitus (T2DM) is characterized by a progressive decline in pancreatic β-cell function and increased insulin resistance, and accounts for approximately 90% of people with diabetes. Oral antihyperglycaemic agents are extensively used in the treatment of T2DM. Thiazolidinediones are insulin sensitizers developed specifically for T2DM, which act via activation of peroxisome proliferator-activated receptors (PPARs). Pioglitazone is a thiazolidinedione that displays high affinity for PPARγ(1) and PPARγ(2), which are predominately expressed in adipose tissue. This review examines the published literature comparing the efficacy and tolerability of pioglitazone with other oral antihyperglycaemic agents in the treatment of patients with T2DM. Glycosylated haemoglobin, fasting glucose, insulin parameters and β-cell function are all improved with pioglitazone treatment, with efficacy similar to third-generation sulfonylureas, metformin and dipeptidyl peptidase-4 inhibitors. Pioglitazone reduces vascular risk and inflammatory markers, and improves carotid intima media thickness independent of its glycaemic effect. When compared with rosiglitazone, pioglitazone is associated with a reduction in the risk of hospitalization for acute myocardial infarction. Blood pressure is reduced and lipid profiles are favourably improved with pioglitazone; however, an increased risk for the development/exacerbation of heart failure, which is related to the increased incidence of oedema due to fluid retention, and fractures remain a concern. A low incidence of hypoglycaemia is observed with pioglitazone, especially compared with sulfonylureas. In conclusion, pioglitazone is an effective oral antihyperglycaemic agent with additional cardiovascular and lipid benefits that allows for the successful management of patients with T2DM.

  19. Determination of Biguanides in Anti-diabetic Health Foods by HPLC%HPLC法检测降血糖保健食品中的双胍类药物

    Institute of Scientific and Technical Information of China (English)

    王俊苏; 郗存显; 陈冬东; 张雷; 李贤良; 彭涛; 王国民

    2013-01-01

    OBJECTIVE: To establish the method for simultaneous determination of metformin and phenformin in anti-diabetic heath foods. METHODS: Metformin and phenformin were extracted from anti-diabetic heath foods ultrasonically with methanol-eth-anol(50:50, V/V), including anti-diabetic powder, milk powder, oral liquid, capsule and diabetes tea. The extraction liquid was cleaned up with WCX solid-phase extraction column, and determined by HPLC. Quantification was done by matrix-matched standard curve. RESULTS: The linear range of metformin and phenformin were 0.1-5.0 mg/L 0=0.999 9, r=0.999 5). Average recoveries of them were 91.9%-102.7% and 89.8%-107.0% , respectively (RSD<9.46%). The limits of quantification (LOQ) of them were 0.1 μg/g. None of metformin and phenformin was found in 5 samples. CONCLUSION: The method is simple, reliable and sensitive, which can be used to monitor biguanides in anti-diabetic health foods.%目的:建立同时检测降血糖保健食品中二甲双胍和苯乙双胍含量的方法.方法:采用甲醇-乙醇(50∶50,V/V)超声提取降血糖保健食品降糖粉、奶粉、口服液、胶囊、清渴茶中的二甲双胍和苯乙双胍,提取液经WCX固相萃取柱净化,高效液相色谱法测定,基质回收标准曲线定量.结果:二甲双胍和苯乙双胍检测质量浓度线性范围均为0.1~5.0 mg/L(r分别为0.999 9、0.999 5),回收率分别为91.9%~102.7%、89.8%~107.0%,RSD均低于9.46%,定量限均为0.1μg/g;5种试样中均未检出二甲双胍和苯乙双胍.结论:本方法简单、可靠、灵敏,可用于降血糖保健食品中双胍类药物的检测.

  20. Impact of brief exposure to antifungal agents on the post-antifungal effect and hemolysin activity of oral Candida albicans

    Directory of Open Access Journals (Sweden)

    Arjuna Nishantha ELLEPOLA

    2015-08-01

    Full Text Available AbstractPost-antifungal effect (PAFE of Candida and its production of hemolysin are determinants of candidal pathogenicity. Candida albicans is the foremost aetiological agent of oral candidosis, which can be treated with polyene, azole, and echinocandin antifungals. However, once administered, the intraoral concentrations of these drugs tend to be subtherapeutic and transient due to the diluent effect of saliva and cleansing effect of the oral musculature. Hence, intra-orally, Candidamay undergo a brief exposure to antifungal drugs.Objective Therefore, the PAFE and hemolysin production of oral C. albicans isolates following brief exposure to sublethal concentrations of the foregoing antifungals were evaluated.Material and Methods A total of 50 C. albicans oral isolates obtained from smokers, diabetics, asthmatics using steroid inhalers, partial denture wearers and healthy individuals were exposed to sublethal concentrations of nystatin, amphotericin B, caspofungin, ketoconazole and fluconazole for 60 min. Thereafter, the drugs were removed and the PAFE and hemolysin production were determined by previously described turbidometric and plate assays, respectively.Results Nystatin, amphotericin B, caspofungin and ketoconazole induced mean PAFE (hours of 2.2, 2.18, 2.2 and 0.62, respectively. Fluconazole failed to produce a PAFE. Hemolysin production of these isolates was suppressed with a percentage reduction of 12.27, 13.47, 13.33, 8.53 and 4.93 following exposure to nystatin, amphotericin B, caspofungin, ketoconazole and fluconazole, respectively.Conclusions Brief exposure to sublethal concentrations of antifungal drugs appears to exert an antifungal effect by interfering with the growth as well as hemolysin production of C. albicans.

  1. Non-vitamin K antagonist oral anticoagulation agents in anticoagulant naive atrial fibrillation patients

    DEFF Research Database (Denmark)

    Olesen, Jonas Bjerring; Sørensen, Rikke; Hansen, Morten Lock

    2015-01-01

    the drug came on market. By October, 2013, 40% were being started on warfarin and dabigatran, respectively, and another 20% were started on either rivaroxaban or apixaban. Rivaroxaban and apixaban users generally had a higher predicted risk of stroke and bleeding compared with warfarin and dabigatran users....... Older age, female gender, and prior stroke were some of the factors associated with NOAC use vs. warfarin, whereas chronic kidney disease, myocardial infarction, and heart failure showed the opposite association. CONCLUSION: Among oral anticoagulation-naïve AF patients initiated on oral anticoagulation...

  2. Management of Bleeding With Non-Vitamin K Antagonist Oral Anticoagulants in the Era of Specific Reversal Agents.

    Science.gov (United States)

    Ruff, Christian T; Giugliano, Robert P; Antman, Elliott M

    2016-07-19

    Vitamin K antagonists are commonly used by clinicians to provide anticoagulation to patients who have or are at risk of having thrombotic events. In addition to familiarity with the dosing and monitoring of vitamin K antagonists, clinicians are accustomed to using vitamin K if there is a need to reverse the anticoagulant effect of vitamin K antagonists. There are now 4 new non-vitamin K antagonist oral anticoagulants (NOACs) that are attractive alternatives to vitamin K antagonists. Despite similar or lower rates of serious bleeding with NOACs in comparison with warfarin, there is a pressing need for strategies to manage bleeding when it does occur with NOACs and to reverse the pharmacological effect of these agents if needed. Important steps in minimizing bleeding risks with NOACs include dose adjustment of the agents in the setting of renal dysfunction and avoidance of the concomitant use of other antithrombotic agents if feasible. Laboratory measurement of the anticoagulant effect of NOACs is best accomplished with specialized assays, although some of the more widely available coagulation tests can provide information that is potentially useful to clinicians. Nonspecific hemostatic agents such as prothrombin complex concentrates and recombinant factor VIIa can be used to reverse the effect of NOACs. More specific reversing agents include the approved humanized monoclonal antibody fragment idarucizumab for reversing the effects of dabigatran, the investigational factor Xa decoy andexanet alfa, and the synthetic small molecule ciraparantag. Both andexanet and ciraparantag have been reported to reverse the effects of the anti-Xa NOACs (rivaroxaban, apixaban, and edoxaban), and a number of other anticoagulant agents in common clinical use, as well.

  3. Imaging liver metastases with a new oral manganese-based contrast agent.

    NARCIS (Netherlands)

    Chabanova, E.; Logager, V.; Moller, J.M.; Dekker, H.M.; Barentsz, J.O.; Thomsen, H.S.

    2006-01-01

    RATIONALE AND OBJECTIVES: The purpose of the study was a preliminary evaluation of a new oral, manganese-based, liver-specific contrast medium (CMC-001; CMC Contrast AB, Malmoe, Sweden) for magnetic resonance imaging (MRI) in patients with liver metastases. MATERIALS AND METHODS: The study included

  4. Imaging liver metastases with a new oral manganese-based contrast agent.

    NARCIS (Netherlands)

    Chabanova, E.; Logager, V.; Moller, J.M.; Dekker, H.M.; Barentsz, J.O.; Thomsen, H.S.

    2006-01-01

    RATIONALE AND OBJECTIVES: The purpose of the study was a preliminary evaluation of a new oral, manganese-based, liver-specific contrast medium (CMC-001; CMC Contrast AB, Malmoe, Sweden) for magnetic resonance imaging (MRI) in patients with liver metastases. MATERIALS AND METHODS: The study included

  5. Fabrication and evaluation of oral tablets using natural mucoadhesive agent from seeds of Caesalpinia pulcherrima (L. SW

    Directory of Open Access Journals (Sweden)

    Jeevanandham S

    2010-01-01

    Full Text Available Oral mucoadhesive sustained drug delivery systems of salbutamol sulfate were formulated using an isolated natural agent from the seeds of Caesalpinia pulcherrima. The isolated material was evaluated for various parameters, such as, melting point, viscosity, pH, elemental analysis, swelling index, phytochemical constituents, and solubility studies. The mucoadhesive characters of the isolated substance were identified by a comparative study with hydroxyl propyl cellulose and sodium alginate, by various in vitro methods, such as, Shear stress measurement, Wilhelmy′s method, Falling sphere method, and Detachment force measurement. Formulation and evaluation of mucoadhesive oral tablets of salbutamol sulfate (100 mg, using isolated natural materials in different proportions, and in vitro release studies, were carried out for three different formulations according to the U.S.P apparatus two (paddle method. Each 100 mg tablet was taken in 900 ml of acid buffer 1.2 and maintained at 37˚C. After two hours the filtrate was collected and replaced in buffer 7.4. In vitro releases of three different formulations for nine hours were studied, which showed the sustained action of drug release with increasing the concentration of the isolated natural mucoadhesive agent in the formulations.

  6. Oral distension methods for small bowel MRI: comparison of different agents to optimize bowel distension.

    Science.gov (United States)

    Schmidt, Stefan A; Baumann, Julia A; Stanescu-Siegmund, Nora; Froehlich, Eckhart; Brambs, Hans-Juergen; Juchems, Markus S

    2016-12-01

    Background Different methods for bowel distension prior to magnetic resonance imaging (MRI) examinations were described in recent years. Purpose To compare orally administered psyllium or locust bean gum / mannitol (LBM) with tylose administered through a duodenal catheter for bowel distension in patients undergoing MRI examination of the small bowel. Material and Methods Three different methods of bowel distension prior to MRI were compared: tylose applied through a duodenal catheter and orally administered psyllium and LBM in three groups with 15 patients each. Datasets were blinded and reviewed independently by two experienced radiologists, who assessed the diagnostic value and the maximum luminal diameter. Results Tylose was superior to psyllium and LBM in the examination of the duodenum and proximal jejunum. LBM was superior to the other methods for distension of the ileum and terminal ileum. The greatest luminal diameter of the duodenum was achieved after tylose and distension of the terminal ileum was the best in patients receiving LBM. The psyllium group was inferior to the other two groups in all segments. Conclusion By using LBM as an oral method of bowel distension, many patients can avoid the unpleasant placement of a duodenal catheter without compromising the diagnostic value of the examination.

  7. Improving adherence with oral antiemetic agents in patients with breast cancer receiving chemotherapy.

    Science.gov (United States)

    Hendricks, Carolyn B

    2015-05-01

    In this small breast cancer-dedicated solo practice, a retrospective medical record review disclosed the following: significant rate of chemotherapy-related nausea and vomiting and discordance between patient-reported compliance with prescribed antiemetics and medical record documentation of compliance. As part of the curriculum for the American Society of Clinical Oncology (ASCO) Quality Training Program, a quality improvement project was developed to improve adherence to oral antiemetics in our patients with breast cancer receiving highly emetogenic chemotherapy. The following steps were undertaken in plan-do-study-act cycles to improve adherence: enhanced patient education at time of chemotherapy consent, implementation of standardized in-person or e-mail contact with our patients receiving chemotherapy, and improvement of our electronic health record documentation of adherence to oral antiemetics. A run chart was generated to analyze our data. After our interventions, the percentage of patients who took their antiemetics as prescribed rose from a baseline of 49% to 79%. Significant improvement in adherence to oral antiemetics among patients with breast cancer receiving chemotherapy was achieved and sustained in this small-practice setting using the framework provided by participation in the ASCO Quality Training Program. Copyright © 2015 by American Society of Clinical Oncology.

  8. Adherence to oral antineoplastic agents by cancer patients: definition and literature review.

    Science.gov (United States)

    Bassan, F; Peter, F; Houbre, B; Brennstuhl, M J; Costantini, M; Speyer, E; Tarquinio, C

    2014-01-01

    Since the 1990s, oral chemotherapy has been gaining ground as cancer treatment. This therapy seems to have few toxic effects and offers patients good quality of life. However, in addition to the fears the therapy might generate in patients, oral treatment raises a new issue, which, until now, has been marginal in this field: therapeutic observance or adherence. We investigated the research into adherence to oral chemotherapy among cancer patients published between 1990 and July 2013. Studies showed considerable diversity in terms of both the definition and measurement of adherence. As well, adherence to antineoplastic therapy is affected by the patient's understanding of the treatment and ability to remember information provided by the physician, treatment length and psychological distress. Our review of the few studies on adherence to anticancer drug treatment raises some questions that could be pursued in future research. In light of our findings, patients should receive 'therapy education' to help them and their support groups better understand the disease and its treatment and to achieve optimal health management and improved treatment effectiveness. © 2013 John Wiley & Sons Ltd.

  9. ANTI-DIABETIC EFFICACY AND PHYTOCHEMICAL SCREENING OF METHANOLIC LEAF EXTRACT OF PAWPAW (Carica papaya GROWN IN NORTH CENTRAL NIGERIA.

    Directory of Open Access Journals (Sweden)

    Ayorinde Victor Ogundele

    2016-10-01

    Full Text Available Carica papaya leaves samples (Green were freshly harvested from Islamic village in Ilorin, Ilorin west local Government, Kwara State Nigeria. The leaves were extracted with methanol; the resulting extracts were screened for the phytochemical constituents using standard procedure. Phytochemical screening revealed the presence of bioactive compounds such as tannins, saponins, terpenoids, glycosides and alkaloids. The in-vitro anti-diabetic potential of the plant was also determined so as to justify the traditional usage of the plant in treating diabetes. The result of the present study confirmed that the methanolic extract of C.papaya leaves possess significant anti-diabetic activity in-vitro, this shows that the leaves has the potential for the development of drugs in combating diabetes.

  10. GC-MS analysis, preliminary phytochemical screening, physicochemical analysis and anti-diabetic activity of ethanol extract of Jasminum cuspidatum leaves

    National Research Council Canada - National Science Library

    Singumsetty Vinay; Shaik Karimulla; Devarajan Saravanan

    2014-01-01

    The purpose of the present study was investigating the GC-MS analysis, preliminary phytochemical screening, physicochemical analysis and anti-diabetic activity of ethanol extract of the leaves of Jasminum cuspidatum...

  11. Comparative study to evaluate the anti-diabetic activity of commercially available extract of Tinospora cordifolia and Phyllanthus emblica in streptozocin induced diabetic rat

    Directory of Open Access Journals (Sweden)

    Nishant Pathak

    2016-08-01

    Conclusions: Commercially available extract of Tinospora cordifolia and Phyllanthus emblica have significant anti-diabetic activity in streptozocin induced diabetic rats. [Int J Basic Clin Pharmacol 2016; 5(4.000: 1641-1646

  12. Nonadherence and factors affecting adherence of diabetic patients to anti-diabetic medication in Assela General Hospital, Oromia Region, Ethiopia

    Directory of Open Access Journals (Sweden)

    Ashebir Kassahun

    2016-01-01

    Full Text Available Background: Diabetes mellitus is a major global health problem covering approximately 347 million persons worldwide. Glycemic control has a main role in its management which mainly depends upon patient adherence to the treatment plan. Accurate assessment of medication adherence is necessary for effective management of diabetes. Objective: To assess nonadherence and factors affecting adherence of diabetic patients to anti-diabetic medication in Assela General Hospital (AGH, Oromia Region, Ethiopia. Materials and Methods: A descriptive cross-sectional study was conducted on patients seeking anti-diabetic drug treatment and follow-up at AGH using structured questionnaire and reviewing the patient record card using check list from January 24, 2014 to February 7, 2014. Descriptive analysis was used to describe the percentages and number of distributions of the variables in the study; and association was identified for categorical data. P ≤ 0.05 was considered as statistically significant. Result: Of all respondents, 149 (52.3% and 136 (47.7% were female and male, respectively. The majority of the study participants 189 (66.3% were in the age group of 30–60 years. Two-hundred nineteen (76.8% of respondents were married currently. The majority, 237 (83.2% of respondents did not have blood glucose self-monitoring equipment (glucometer. A total of 196 (68.8% respondents were adhered to anti-diabetic medication. There was a significant association between adherence to the medication and side effect, level of education, monthly income and presence of glucometer at home (P < 0.05. Conclusion: The participants in the area of study were moderately adherent to their anti-diabetic medications with nonadherence rate of 31.2%. Different factors of medication nonadherence were identified such as side effect and complexity of regimen, failure to remember, and sociodemographic factors such as educational level and monthly income.

  13. ANTI-DIABETIC ACTIVITY OF LAGENARIA SICERARIA PULP AND SEED EXTRACT IN NORMAL AND ALLOXAN-INDUCED DIABETIC RATS

    OpenAIRE

    Somshuvra Bhattacharya et al

    2012-01-01

    The aim of the present study was to evaluate the possible anti-diabetic potential of Lagenaria siceraria pulp extract (LSPE) and Lagenaria siceraria seed extract (LSSE) against the pancreatic damage from alloxan-induced diabetes in rats related to diabetes mellitus. Lagenaria siceraria induced significant reduction in blood glucose and increasing of serum insulin, our data indicate that the level of glucose in the animals that were subjected with alloxan was 210 mg/dl comparing with normal 70...

  14. Anti-obesity and anti-diabetic actions of histamine neurons

    Institute of Scientific and Technical Information of China (English)

    2001-01-01

    The present study aimed to examine roles of histamine neurons in leptin signaling pathways and leptin resistant states. H1-receptor knockout (H1KO) mice showed no change in daily food intake, adiposity, growth curve, basal expression of hypothalamic neuropeptides, uncoupling proteins (UCPs) or ob gene. However, H1KO mice fed with high fat diet increased fat deposition and ob gene expression more excessively. Leptin-induced feeding suppression was attenuated in H1KO mice. Chronic leptin treatment decreased visceral fat and up-regulated UCPs expression in brown and white fat. These effects of leptin were attenuated in pair-fed H1KO mice. Chronic histamine or histidine treatment decreased body weight, body fat deposition, and serum glucose and insulin in diet-induced obese, ob/ob and db/db mice. Activation of histamine neurons suppressed ob gene expression in the fat tissue together with elevation of seurm leptin and UCPs mRNA. These actions of neuronal histamine were attenuated in the double knockout mice, i.e., db/db mice with H1KO. Taken together, H1KO mice, a novel leptin resistant model, elucidate essential roles of H1-R in energy intake and expenditure as a down-stream-signaling message of leptin actions in the brain. The anti-obesity and anti-diabetic effects of histamine neurons provide a new insight into therapeutic strategies on human obesity and diabetes with leptin resistance.

  15. Molecular Mechanisms of the Anti-Obesity and Anti-Diabetic Properties of Flavonoids

    Directory of Open Access Journals (Sweden)

    Mohammed Kawser Hossain

    2016-04-01

    Full Text Available Obesity and diabetes are the most prevailing health concerns worldwide and their incidence is increasing at a high rate, resulting in enormous social costs. Obesity is a complex disease commonly accompanied by insulin resistance and increases in oxidative stress and inflammatory marker expression, leading to augmented fat mass in the body. Diabetes mellitus (DM is a metabolic disorder characterized by the destruction of pancreatic β cells or diminished insulin secretion and action insulin. Obesity causes the development of metabolic disorders such as DM, hypertension, cardiovascular diseases, and inflammation-based pathologies. Flavonoids are the secondary metabolites of plants and have 15-carbon skeleton structures containing two phenyl rings and a heterocyclic ring. More than 5000 naturally occurring flavonoids have been reported from various plants and have been found to possess many beneficial effects with advantages over chemical treatments. A number of studies have demonstrated the potential health benefits of natural flavonoids in treating obesity and DM, and show increased bioavailability and action on multiple molecular targets. This review summarizes the current progress in our understanding of the anti-obesity and anti-diabetic potential of natural flavonoids and their molecular mechanisms for preventing and/or treating obesity and diabetes.

  16. Molecular Mechanisms of the Anti-Obesity and Anti-Diabetic Properties of Flavonoids.

    Science.gov (United States)

    Kawser Hossain, Mohammed; Abdal Dayem, Ahmed; Han, Jihae; Yin, Yingfu; Kim, Kyeongseok; Kumar Saha, Subbroto; Yang, Gwang-Mo; Choi, Hye Yeon; Cho, Ssang-Goo

    2016-04-15

    Obesity and diabetes are the most prevailing health concerns worldwide and their incidence is increasing at a high rate, resulting in enormous social costs. Obesity is a complex disease commonly accompanied by insulin resistance and increases in oxidative stress and inflammatory marker expression, leading to augmented fat mass in the body. Diabetes mellitus (DM) is a metabolic disorder characterized by the destruction of pancreatic β cells or diminished insulin secretion and action insulin. Obesity causes the development of metabolic disorders such as DM, hypertension, cardiovascular diseases, and inflammation-based pathologies. Flavonoids are the secondary metabolites of plants and have 15-carbon skeleton structures containing two phenyl rings and a heterocyclic ring. More than 5000 naturally occurring flavonoids have been reported from various plants and have been found to possess many beneficial effects with advantages over chemical treatments. A number of studies have demonstrated the potential health benefits of natural flavonoids in treating obesity and DM, and show increased bioavailability and action on multiple molecular targets. This review summarizes the current progress in our understanding of the anti-obesity and anti-diabetic potential of natural flavonoids and their molecular mechanisms for preventing and/or treating obesity and diabetes.

  17. Bioactivity screening of microalgae for antioxidant, anti-inflammatory, anticancer, anti-diabetes and antibacterial activities

    Directory of Open Access Journals (Sweden)

    Chiara eLauritano

    2016-05-01

    Full Text Available Marine microalgae are considered a potentially new and valuable source of biologically active molecules for applications in the food industry as well as in the pharmaceutical, nutraceutical and cosmetic sectors. They can be easily cultured, have short generation times and enable an environmentally-friendly approach to drug discovery by overcoming problems associated with the over-utilization of marine resources and the use of destructive collection practices. In this study, 21 diatoms, 7 dinoflagellates and 4 flagellate species were grown in three different culturing conditions and the corresponding extracts were tested for possible antioxidant, anti-inflammatory, anticancer, anti-diabetes, antibacterial and anti-biofilm activities. In addition, for two diatoms we also tested two different clones to disclose diversity in clone bioactivity. Six diatom species displayed specific anti-inflammatory, anticancer (blocking human melanoma cell proliferation and anti-biofilm (against the bacteria Staphylococcus epidermidis activities whereas, none of the other microalgae were bioactive against the conditions tested for. Furthermore, none of the 6 diatom species tested were toxic on normal human cells. Culturing conditions (i.e. nutrient starvation conditions greatly influenced bioactivity of the majority of the clones/species tested. This study denotes the potential of diatoms as sources of promising bioactives for the treatment of human pathologies.

  18. Anti-diabetic activity of Ferula assafoetida extract in normal and alloxan-induced diabetic rats.

    Science.gov (United States)

    Abu-Zaiton, Ahmed Saber

    2010-01-15

    The aim of the present study was to evaluate the possible anti-diabetic potential of Asafetida extract against the pancreatic beta-cells damage from alloxan-induced diabetes in rats and some hormones related to diabetes mellitus. Asafetida induced significant reduction in blood glucose and increasing of serum insulin, our data indicate that the level of glucose in the animals that subjected with alloxan was 10.28 +/- 0.85 mmol L(-1) p < 0.05 comparing with control group 3.27 +/- 0.25 p < 0.05, the level of blood glucose in diabetic group when subjected with Asafetida extract decreasing to 6.75 +/- 0.31 p < 0.05. There was significant amount of insulin secretion in diabetic animals when subjected with Asafetida extract 0.48 +/- 0.05 p < 0.05 in comparison with diabetic animal's 0.33 +/- 0.06 p < 0.05. These findings suggested that Asafetida extract treatment exerts therapeutic protective effect in diabetes by preserving pancreatic beta-cells integrity and significant activity extract, which supports traditional usage to prevent diabetic complications.

  19. Quinoa seeds leach phytoecdysteroids and other compounds with anti-diabetic properties.

    Science.gov (United States)

    Graf, Brittany L; Poulev, Alexander; Kuhn, Peter; Grace, Mary H; Lila, Mary Ann; Raskin, Ilya

    2014-11-15

    Quinoa (Chenopodium quinoa Willd.) contains high levels of biologically active phytoecdysteroids, which have been implicated in plant defense from insects, and have shown a range of beneficial pharmacological effects in mammals. We demonstrated that the most prevalent phytoecdysteroid, 20-hydroxyecdysone (20HE), was secreted (leached) from intact quinoa seeds into water during the initial stages of seed germination. Leaching efficiency was optimized by ethanol concentration (70% ethanol), temperature (80°C), time (4h), and solvent ratio (5 ml/g seed). When compared to extraction of macerated seeds, the leaching procedure released essentially all the 20HE available in the seeds (491 μg/g seed). The optimized quinoa leachate (QL), containing 0.86% 20HE, 1.00% total phytoecdysteroids, 2.59% flavonoid glycosides, 11.9% oil, and 20.4% protein, significantly lowered fasting blood glucose in obese, hyperglycemic mice. Leaching effectively releases and concentrates bioactive phytochemicals from quinoa seeds, providing an efficient means to produce a food-grade mixture that may be useful for anti-diabetic applications.

  20. PIXE analysis of some anti-diabetic medicinal plants in Nigeria

    Energy Technology Data Exchange (ETDEWEB)

    Olabanji, S.O. [ICTP Fellow on sabbatical leave from Centre for Energy Research and Development, Obafemi Awolowo University, lIe-lfe (Nigeria); Omobuwajo, O.R.; Adebajo, A.C. [Department of Pharmacognosy, Faculty of Pharmacy, Obafemi Awolowo University, lIe-lfe (Nigeria); Ceccato, D. [Dipartmento di Fisica, Universita di Padova, Padova (Italy); Buoso, M.C.; Moschini, G., E-mail: skayode2002@yahoo.co.uk [lstituto Nazionale di Fisica Nucleare (INFN), Laboratori Nazionali di Legnaro (LNL), Padova (Italy)

    2013-07-01

    Full text: Diabetes mellitus, a metabolic disease characterized by high blood glucose levels (hyperglycemia) due to defects in insulin secretion, or action, or both. It is a dangerous disease leading to death of many people in the world. Some of the medicinal plants implicated in the herbal recipes for the treatment of diabetes in Nigeria have been reported{sup 1}. Additional medicinal plants used for the treatment of diabetes in Nigeria are presented in this work. These medicinal plants are becoming increasingly important and relevant as herbal drugs due to their use as antioxidants, neutraceuticals, food additives and supplements in combating diabetes. Elemental compositions of these anti-diabetic medicinal plants were determined using PIXE technique. The 1.8 MV collimated proton beam from the 2.5 MV AN 2000 Van de Graaff accelerator at Instituto Nazionale di Fisica Nucleare (INFN), Laboratori Nazionali di Legnaro (LNL) Legnaro (Padova) Italy was employed for the work. The results show the presence of twenty two elements at various concentrations in the medicinal plants. The leaves of Murraya, P amarus, O. gratissimum, O.subscopodica, P pellucida and the whole plant of B. diffusa, B. pinnalum and C. occidenlalis could be taken as vegetables, food additives, neutraceuticals and supplements in the management of diabetes. [1] S.O. Olabanji, OR Omobuwajo, D. Ceccato, A.C. Adebajo, M.C. Buoso, G. Moschini. Nucl. Instrum. Methods Phys. Res. Sect. B 266 (2008) 2387 - 2390. (author)

  1. Anti-Diabetic and Hepato-Renal Protective Effects of Ziyuglycoside II Methyl Ester in Type 2 Diabetic Mice

    Directory of Open Access Journals (Sweden)

    Dong Ju Son

    2015-07-01

    Full Text Available Type 2 diabetes is a metabolic disorder caused by abnormal carbohydrate metabolism, and closely associated with abnormal lipid metabolism and hepato-renal dysfunction. This study investigated the anti-diabetic and hepato-renal protective properties of ziyuglycoside I (ZG01 derivative on type 2 diabetes. ZG01 was isolated from roots of Sanguisorba officinalis and chemically modified by deglycosylation and esterification to obtained ziyuglycoside II methyl ester (ZG02-ME. Here, we showed that ZG02-ME has stronger anti-diabetic activity than the original compound (ZG01 through decreasing blood glucose, glycated hemoglobin (HbA1c, and insulin levels in a mouse model of type 2 diabetes (db/db mice. We further found that ZG02-ME treatment effectively ameliorated serum insulin, leptin and C-peptide levels, which are key metabolic hormones, in db/db mice. In addition, we showed that elevated basal blood lipid levels were decreased by ZG02-ME treatment in db/db mice. Furthermore, treatment of ZG02-ME significantly decreased serum AST, ALT, BUN, creatinine, and liver lipid peroxidation in db/db mice. These results demonstrated that compared to ZG01, chemically modified ZG02-ME possess improved anti-diabetic properties, and has hepato-renal protective activities in type 2 diabetes.

  2. Boron microquantification in oral mucosa and skin following administration of a neutron capture therapy agent

    Energy Technology Data Exchange (ETDEWEB)

    Kiger, S.W. III; Micca, P.L.; Morris, G.M.; Coderre, J.A

    2002-07-01

    Clinical trials of boron neutron capture therapy (BNCT) for intracranial tumours using boronphenylalanine-fructose undertaken at Harvard-MIT and Brookhaven National Laboratory have observed acute normal tissue reactions in the skin and oral mucosa. Because the range of the {sup 10}B(n,a){sup 7}Li reaction products is very short, 10-14 {mu}m combined, knowledge of the 10B microdistribution in tissue is critical for understanding the microdosimetry and radiobiology of BNCT. This paper reports measurements of the microdistribution of {sup 10}B in an animal model, rat skin and tongue, using high resolution quantitative autoradiography (HRQAR), a neutron-induced track etch autoradiographic technique. The steep spatial gradient and high absolute value relative to blood of the {sup 10}B concentration observed in some strata of the rat tongue epithelium and skin are important for properly evaluating the radiobiology and the biological effectiveness factors for normal tissue reactions such as oral mucositis, which are generally assessed using the blood boron concentration rather than the tissue boron concentration. (author)

  3. Influence of dental exposure to oral environment on smear layer removal and collagen exhibition after using different conditioning agents.

    Science.gov (United States)

    Fontanari, Lucas Amaral; Pinto, Shelon Cristina Souza; Cavassim, Rodrigo; Spin-Neto, Rubens; Ishi, Eduardo de Paula; Sampaio, José Eduardo Cezar

    2011-01-01

    Although in vitro studies have shown encouraging results for root surface conditioning with demineralizing agents, in vivo studies have failed to show its benefits in periodontal healing. This can be attributed to several factors, among which, the hypermineralization of dental surface. Therefore, this in vitro study compared, using scanning electron microscopy (SEM), the effect of root surface conditioning with different conditioners (1% and 25% citric acid, 24% EDTA and 50 mg/mL tetracycline hydrochloride) in impacted teeth and in teeth that had their roots exposed to the oral environment. One trained examiner assessed the SEM micrographs using a root surface modification index. There was a tendency of more root surface modification in the group of impacted teeth, suggesting that the degree of root mineralization influences its chemical demineralization.

  4. Topical polyethylene glycol as a novel chemopreventive agent for oral cancer via targeting of epidermal growth factor response.

    Directory of Open Access Journals (Sweden)

    Ramesh K Wali

    Full Text Available Head and neck squamous cell carcinoma (HNSCC is a major cause of morbidity and mortality underscoring the need for safe and effective chemopreventive strategies. Targeting epidermal growth factor receptor (EGFR is attractive in that it is an early critical event in HNSCC pathogenesis. However, current agents lack efficacy or have unacceptable toxicity. Several groups have demonstrated that the over-the-counter medication, polyethylene glycol (PEG has remarkable chemopreventive efficacy against colon carcinogenesis. Importantly, we reported that this effect is mediated through EGFR internalization/degradation. In the current study, we investigated the chemopreventive efficacy of this agent against HNSCC, using both the well validated animal model 4-NQO (4-nitroquinoline 1-oxide rat model and cell culture with the human HNSCC cell line SCC-25. We demonstrated that daily topical application of 10% PEG-8000 in the oral cavity (tongue and cavity wall post 4NQO initiation resulted in a significant reduction in tumor burden (both, tumor size and tumors/tumor bearing rat without any evidence of toxicity. Immunohistochemical studies depicted decreased proliferation (number of Ki67-positive cells and reduced expression of EGFR and its downstream effectors cyclin D1 in the tongue mucosa of 4NQO-rats treated with PEG. We showed that EGFR was also markedly downregulated in SCC-25 cells by PEG-8000 with a concomitant induction of G1-S phase cell-cycle arrest, which was potentially mediated through upregulated p21(cip1/waf1. In conclusion, we demonstrate, for the first time, that PEG has promising efficacy and safety as a chemopreventive efficacy against oral carcinogenesis.

  5. Oral salmon calcitonin attenuates hyperglycaemia and preserves pancreatic beta-cell area and function in Zucker diabetic fatty rats

    DEFF Research Database (Denmark)

    Feigh, M; Andreassen, K V; Neutzsky-Wulff, A V

    2012-01-01

    Oral salmon calcitonin (sCT), a dual-action amylin and calcitonin receptor agonist, improved glucose homeostasis in diet-induced obese rats. Here, we have evaluated the anti-diabetic efficacy of oral sCT using parameters of glycaemic control and beta-cell morphology in male Zucker diabetic fatty...

  6. Influence of Mycotoxins and a Mycotoxin Adsorbing Agent on the Oral Bioavailability of Commonly Used Antibiotics in Pigs

    Directory of Open Access Journals (Sweden)

    Siska Croubels

    2012-04-01

    Full Text Available It is recognized that mycotoxins can cause a variety of adverse health effects in animals, including altered gastrointestinal barrier function. It is the aim of the present study to determine whether mycotoxin-contaminated diets can alter the oral bioavailability of the antibiotics doxycycline and paromomycin in pigs, and whether a mycotoxin adsorbing agent included into diets interacts with those antibiotics. Experiments were conducted with pigs utilizing diets that contained blank feed, mycotoxin-contaminated feed (T-2 toxin or deoxynivalenol, mycotoxin-contaminated feed supplemented with a glucomannan mycotoxin binder, or blank feed supplemented with mycotoxin binder. Diets with T-2 toxin and binder or deoxynivalenol and binder induced increased plasma concentrations of doxycycline administered as single bolus in pigs compared to diets containing blank feed. These results suggest that complex interactions may occur between mycotoxins, mycotoxin binders, and antibiotics which could alter antibiotic bioavailability. This could have consequences for animal toxicity, withdrawal time for oral antibiotics, or public health.

  7. Combining insulins with oral antidiabetic agents: effect on hyperglycemic control, markers of cardiovascular risk and disease

    Directory of Open Access Journals (Sweden)

    Kjeld Hermansen

    2008-06-01

    Full Text Available Kjeld Hermansen, Lene Sundahl Mortensen, Marie-Louise HermansenDepartment of Endocrinology and Metabolism C, Aarhus University Hospital, DK-8000 Aarhus, DenmarkAbstract: Patients with type 2 diabetes mellitus (T2DM have an increased risk of cardiovascular disease (CVD. Unfortunately, several potential barriers exist for CVD risk management in diabetes, including the need for significant lifestyle changes, potential problems with hypoglycemia, weight gain, injection tolerability, treatment complexity with current diabetes therapies and other, unmodifiable factors. Improving glycemic control may impact CVD risk. Treatment of T2DM usually starts with lifestyle changes such as diet and exercise. When these become insufficient, pharmacotherapy is required. Various oral antidiabetic drugs (OADs are available that reduce hyperglycemia. The first line of therapy is usually metformin, since it does not increase weight and seems to have a beneficial effect on CVD mortality and risk factors. As T2DM progresses, insulin treatment becomes necessary for the majority of patients. The last few years have seen the development of long-acting, rapid-acting, and premixed insulin analog formulations. The treat-to-target algorithms of recent studies combining OADs plus insulin analogs have demonstrated that patients can reach glycemic treatment targets with low risk of hypoglycemia, greater convenience, and – with some analogs – limited weight gain vs conventional insulins. These factors may possibly have a positive influence on CVD risk. Future studies will hopefully elucidate the benefits of this approach.Keywords: diabetes mellitus, type 2 diabetes, cardiovascular disease, hyperglycemia, insulin, oral antidiabetic drugs

  8. SITUASI PATEN OBAT ANTI DIABETES, ANTI HIPERTENSI, ANTI MALARIA DAN ANTI TUBERKULOSIS DI INDONESIA

    Directory of Open Access Journals (Sweden)

    Basundari Sri Utami

    2014-10-01

    Full Text Available AbstrakIndonesia merupakan negara berpenduduk keempat terbanyak setelah Cina, India dan Amerika. Indonesia sedang mengalami transisi epidemiologi, dimana terjadi peningkatan penyakit tidak menular (PTM, sementara penyakit menular (PM seperti malaria, tuberkulosis dan demam dengue prevalensinya masih tinggi. Tingginya morbiditas merupakan lahan yang bagus untuk melaksanakan obat anti PM dan anti PTM yang mendapat paten karena pangsa pasarnya yang sangat luas. Sayangnya potensi pasar yang masih luas ini hanya ditangkap oleh luar negeri. Data dari Direktorat Jendral Hak Kekayaan Intelektual (Ditjen HKI pada tahun 2010 menunjukkan pemohon paten dalam negeri yang mendapatkan persetujuan perlindungan paten (granted hanya 4,6% sedangkan dari luar negeri sebanyak 92,03%. Hal yang sangat ironis bagi Indonesia yang merupakan negara dengan potensi bahan dasar obat alam dan keanekaragaman hayati terbanyak ketiga setelah Brazil dan Cina. Tujuan penelitian ini untuk mengevaluasi situasi paten obat yang terdaftar di Direktorat Paten, Ditjen HKI, Kementerian Hukum dan Hak Asasi Manusia RI dalam 7 tahun terakhir (tahun 2005 sampai 2011 untuk PM (malaria dan tuberkulosis dan PTM (hipertensi dan diabetes. Metode observasional dengan penelusuran dokumen paten dari alamat web instansi terkait. Hasilnya Indonesia hanya mendaftarkan 4,9% dari seluruh paten yang didaftarkan di Dirjen HKI dari tahun 2005 sampai dengan 2011, sebagai berikut untuk obat anti-hipertensi 3,4% dari 89 paten, anti-diabetes hanya 4,8% dari 250 paten, anti malaria 21,1% dari 18 paten anti-tuberkulosis 7,1% dari 14 paten. Sebagian besar paten yang didaftarkan oleh pendaftar Indonesia merupakan paten obat ekstrak herbal atau komposisinya. Kesimpulan dari penelitian ini adalah paten obat untuk PTM dan PM di Indonesia masih didominasi paten luar negeri.Kata Kunci : Situasi paten, obat, Ditjen HKI, IndonesiaAbstractIndonesia is the fourth most populous country after China, India and America. There

  9. Effect of oral hypoglycaemic agents on bone metabolism in patients with type 2 diabetes mellitus

    Directory of Open Access Journals (Sweden)

    B. Siddhartha Kumar

    2012-04-01

    Full Text Available Diabetes mellitus (DM and osteoporosis are the two important public health problems in India. The burden of both these conditions is expected to increase in the near future in view of changing lifestyle habits and ageing population. Indians are at risk of osteoporosis due to their low body mass index (BMI, genetic predisposition and nutritional factors. The diseases type 1 DM and type 2 DM (T2DM are associated with increased fracture risk in the disease population, in spite of difference in the bone mineral density (BMD. An increase in fracture risk is also reported among older patients with T2DM despite frequently reported normal or increased BMD. Administration of insulin stimulates osteoblast activity and bone mineral apposition rates. The impact of endogenous insulin production, insulin sensitivity, and exogenous insulin administration as an anabolic agent for bone in T2DM has not been clarified. Biguanides and sulphonylureas do not appear to have adverse effects on BMD. Preclinical evidence suggests that incretin-based drugs may be beneficial for bone, but clinical evidence to support this hypothesis is not yet available. Thiazolidinedione (TZD group of agents have been implicated in causing osteoporosis in various animal studies and some human studies available till date. The debate regarding this is issue is still ongoing. Randomized controlled studies with larger sample size preferably involving multiple centres, multiple ethnicities are required to answer these queries.

  10. An artemisinin derivative of praziquantel as an orally active antischistosomal agent.

    Directory of Open Access Journals (Sweden)

    Lanlan Dong

    Full Text Available Schistosomiasis is a major health problem in tropical and sub-tropical areas caused by species of trematode belonging to the genus Schistosoma. The treatment and control of this disease has been relying on the use of a single drug praziquantel. However, the drug resistance concern urged the development of new drugs against schistosoma. Here, we report our systematic biological evaluation of DW-3-15, a new lead compound developed based on our conjugation design rationale as an effective anti-schistosomal agent.The antischistosomal activity of DW-3-15 was systematically evaluated in S. japonicum infected mouse model for its stage-sensitivity and dose response. The results revealed that DW-3-15 exhibited 60-85% worm reduction rate against different development stage of worm. Scanning electron microscopy (SEM observation indicated that DW-3-15 may damage to the tegument of male schistosomes.Our results demonstrated that DW-3-15 showed potent anti-schistosomal activities in vivo. The results strongly support our conjugation design strategy of artemisinin analogs and further development of DW-3-15 as a new lead compound as anti-schistosomal agent.

  11. Anti-diabetic effect of Capparis spinosa L. root extract in diabetic rats

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    Mostafa Kazemian Mansur Abad

    2015-06-01

    Full Text Available Objective: Diabetes mellitus is the most common metabolic disorders with severe impact on quality of life. Reducing serum glucose levels and normalization of serum lipid is of great clinical importance for treating diabetes. To our knowledge, there are not any evidences about the anti-diabetic action of capparis spinosa root. In the present study the effects of the C. spinosa root extract on diabetic metabolic disorders have been studied in experimental diabetes. Materials and Methods: Rats were divided into six groups: normal control (NC, diabetic control (DC, diabetic rats receiving 0.2, 0.4 g/kg of plant extract or 0.6 mg/kg glibenclamide (groups D0.2, D0.4 or DG respectively. A normal group of rats was also designed to receive 0.2 g/kg of plant extract (N0.2. Rats were rendered diabetic (streptozotocin 60 mg/kg, i.p. and treated with 0.2, 0.4 g/ kg of plant extract or glibenclamide for four weeks. At the end of the experiment, blood was drawn through heart puncture under deep anesthesia. Weight was measured weekly, glucose levels were measured at the first and fourth week and lipid profiles, insulin and liver enzymes at the end of the study. Results: Glucose levels significantly decreased after treating with plant extract (p=0.003. However, insulin levels did not increase in any treating groups. Plant extract could significantly raise HDL and reduce levels of LDL and liver enzymes (ALT and ALP. Conclusion: These results showed that C. spinosa rootextract could improve diabetic related metabolic derangement such as hyperglycemia, dyslipidemia, and elevated liver markers in an insulin-independent manner.

  12. Saffron (Crocus sativus L.) powder as an ingredient of rye bread: an anti-diabetic evaluation.

    Science.gov (United States)

    Bajerska, Joanna; Mildner-Szkudlarz, Sylwia; Podgórski, Tomasz; Oszmatek-Pruszyńska, Ewa

    2013-09-01

    In this study, a most consumer-acceptable rye bread (RB) containing saffron (S) powder (RB+S) was designed to verify its anti-diabetic properties, and to compare these effects with those of RB and S separately, matched to a similar dose of bioactive components, used in the high-fat (HF) diet in streptozotocin (STZ)-induced Wistar rats. After baking, beneficial antioxidant and sensory properties for RB enriched with 0.12% S were achieved. Twenty-four severely diabetic rats (fasting blood glucose (FBG) ≥350 mg/dL) were randomized to incorporate either 0.08% of pure S, or RB enriched with 0.12% S (the diet provided 0.08% of S), or RB alone into their diet for 5 weeks. As controls, nontreated, HF-feeding STZ-induced rats (positive control-HF/STZ) and rats receiving normal laboratory diet (negative control-C) were used. A significant FBG-lowering effect was observed (47%, 53%, and 54% reduction vs. HF/STZ; P<.05) after S, RB, and RB+S treatment. Improvements in the rats' glycemia were achieved by β-cell regeneration and increases in insulin secretion. Only in the S and RB+S group of rats, a significant (P<.05) increase in relative pancreas (vs. HF/STZ) was noted. A significant (P<.05) reduction in the concentration of thiobarbituric acid-reactive substances (TBARS) was achieved, whereas the ferric-reducing ability of plasma (FRAP) was not changed after S, RB and RB+S treatment (vs. HF/STZ). Triglyceride (TG) concentrations after S, RB, and RB+S treatment were significantly decreased (P<.05) versus HF/STZ. Both S and RB can be used in diabetic therapy, but no additional metabolic effect was achieved after consumption of RB+S.

  13. In vitro dissection of anti-diabetic effects of compound a, a dissociating glucocorticoid receptor ligand

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    Vujičić Milica

    2015-01-01

    Full Text Available Compound A (CpdA, or 2-(4-acetoxyphenyl-2-chloro-N-methyl-ethyl-ammonium chloride, is a stable analog of the hydroxyl phenyl aziridine precursor found in the Namibian shrub Salsola tuberculatiformis Botschantzev. It belongs to the group of so-called “dissociated” GC receptor ligands that downmodulate pro-inflammatory gene expression via the transrepression mechanism, but without physically binding to DNA. We have recently reported that the in vivo administration of CpdA exerts a strong protective effect in a pharmacological model of type 1 diabetes in mice. The goal of this study was to investigate in more detail the effects of CpdA on multiple immune system components, as well as on target pancreatic beta cells in direct in vitro exposure. The utility of CpdA in diabetes prevention was evaluated through its addition to mitogen-activated spleen, lymph node and peritoneal cells of C57BL/6 mice, and to murine pancreatic islets and INS-1 and RINm5F beta cell lines. CpdA modulated immune cell-derived cytokine production in vitro by restraining the pro-inflammatory M1/Th1/Th17 response and switching it towards an anti-inflammatory Th2 profile. However, it did not preserve beta cells from the cytotoxic action of inflammatory cytokines. Thus, the anti-diabetic properties of CpdA are mediated through the modulation of immune cell differentiation pathways rather than through rescue of target cells from autoimmune attack. [Projekat Ministarstva nauke Republike Srbije, br. 173013

  14. Changes in endotoxin levels in T2DM subjects on anti-diabetic therapies

    Directory of Open Access Journals (Sweden)

    Kumar Sudhesh

    2009-04-01

    Full Text Available Abstract Introduction Chronic low-grade inflammation is a significant factor in the development of obesity associated diabetes. This is supported by recent studies suggesting endotoxin, derived from gut flora, may be key to the development of inflammation by stimulating the secretion of an adverse cytokine profile from adipose tissue. Aims The study investigated the relationship between endotoxin and various metabolic parameters of diabetic patients to determine if anti-diabetic therapies exerted a significant effect on endotoxin levels and adipocytokine profiles. Methods Fasting blood samples were collected from consenting Saudi Arabian patients (BMI: 30.2 ± (SD5.6 kg/m2, n = 413, consisting of non-diabetics (ND: n = 67 and T2DM subjects (n = 346. The diabetics were divided into 5 subgroups based on their 1 year treatment regimes: diet-controlled (n = 36, metformin (n = 141, rosiglitazone (RSG: n = 22, a combined fixed dose of metformin/rosiglitazone (met/RSG n = 100 and insulin (n = 47. Lipid profiles, fasting plasma glucose, insulin, adiponectin, resistin, TNF-α, leptin, C-reactive protein (CRP and endotoxin concentrations were determined. Results Regression analyses revealed significant correlations between endotoxin levels and triglycerides (R2 = 0.42; p 2 = 0.10; p 2 = 0.076; p 2 = 0.032; p 2 = 0.055; p Conclusion We conclude that sub-clinical inflammation in T2DM may, in part, be mediated by circulating endotoxin. Furthermore, that whilst the endotoxin and adipocytokine profiles of diabetic patients treated with different therapies were comparable, the RSG group demonstrated significant differences in both adiponectin and endotoxin levels. We confirm an association between endotoxin and serum insulin and triglycerides and an inverse relationship with HDL. Lower endotoxin and higher adiponectin in the groups treated with RSG may be related and indicate another mechanism for the effect of RSG on insulin sensitivity.

  15. PIXE analysis of some Nigerian anti-diabetic medicinal plants (II)

    Science.gov (United States)

    Olabanji, S. O.; Adebajo, A. C.; Omobuwajo, O. R.; Ceccato, D.; Buoso, M. C.; Moschini, G.

    2014-01-01

    Diabetes mellitus, a metabolic disease characterized by high blood glucose levels (hyperglycemia) due to defects in insulin secretion, or action, or both, is a debilitating disease leading to other complications and death of many people in the world. Some of the medicinal plants implicated in the herbal recipes for the treatment of diabetes in Nigeria have been reported. Additional medicinal plants used for the treatment of diabetes in Nigeria are presented in this work. These medicinal plants are becoming increasingly important and relevant as herbal drugs due to their use as antioxidants, nutraceuticals, food additives and supplements in combating diabetes. Elemental compositions of these anti-diabetic medicinal plants were determined using PIXE technique. The 1.8 MV collimated proton beam from the 2.5 MV AN 2000 Van de Graaff accelerator at Istituto Nazionale di Fisica Nucleare (INFN), Laboratori Nazionali di Legnaro (LNL) Legnaro (Padova) Italy was employed for the work. The results show the detection of twenty-one elements which include Mg, P, Ca, K, Mn, Cu, Zn, S, Cr, Co, Ni and V that are implicated in the regulation of insulin and the control of the blood-sugar levels in the human body. The entire plant of Boerhavia diffusa, Securidaca longipedunculata stem, leaves of Peperomia pellucida, Macrosphyra longistyla, Olax subscorpioidea, Phyllanthus muerillanus, Jatropha gossypifolia, Cassia occidentalis, Phyllanthus amarus, and leaf and stem of Murraya koenigii, which have high concentrations of these elements could be recommended as vegetables, nutraceuticals, food additives, supplements and drugs in the control and management of diabetes, if toxicity profiles indicate that they are safe. However, significantly high contents of Al and Si in the entire plant of Bryophyllum pinnatum, and As, Cr, and Cu in Ocimum gratissimum leaf suggest that these plants should be avoided by diabetic patients to prevent complications.

  16. PIXE analysis of some Nigerian anti-diabetic medicinal plants (II)

    Energy Technology Data Exchange (ETDEWEB)

    Olabanji, S.O., E-mail: skayode2002@yahoo.co.uk [Istituto Nazionale di Fisica Nucleare (INFN), Laboratori Nazionali di Legnaro (LNL), I-35020 Padova (Italy); ICTP Fellow on Sabbatical Leave from Centre for Energy Research and Development, Obafemi Awolowo University, Ile-Ife (Nigeria); Adebajo, A.C. [Department of Pharmacognosy, Faculty of Pharmacy, Obafemi Awolowo University, Ile-Ife (Nigeria); Omobuwajo, O.R. [Department of Pharmacognosy and Herbal Medicine, Faculty of Pharmacy, Niger Delta University, Wilberforce Island (Nigeria); Ceccato, D. [Istituto Nazionale di Fisica Nucleare (INFN), Laboratori Nazionali di Legnaro (LNL), I-35020 Padova (Italy); Dipartmento di Fisica, Universita di Padova, Padova (Italy); Buoso, M.C. [Istituto Nazionale di Fisica Nucleare (INFN), Laboratori Nazionali di Legnaro (LNL), I-35020 Padova (Italy); Moschini, G. [Istituto Nazionale di Fisica Nucleare (INFN), Laboratori Nazionali di Legnaro (LNL), I-35020 Padova (Italy); Dipartmento di Fisica, Universita di Padova, Padova (Italy)

    2014-01-01

    Diabetes mellitus, a metabolic disease characterized by high blood glucose levels (hyperglycemia) due to defects in insulin secretion, or action, or both, is a debilitating disease leading to other complications and death of many people in the world. Some of the medicinal plants implicated in the herbal recipes for the treatment of diabetes in Nigeria have been reported. Additional medicinal plants used for the treatment of diabetes in Nigeria are presented in this work. These medicinal plants are becoming increasingly important and relevant as herbal drugs due to their use as antioxidants, nutraceuticals, food additives and supplements in combating diabetes. Elemental compositions of these anti-diabetic medicinal plants were determined using PIXE technique. The 1.8 MV collimated proton beam from the 2.5 MV AN 2000 Van de Graaff accelerator at Istituto Nazionale di Fisica Nucleare (INFN), Laboratori Nazionali di Legnaro (LNL) Legnaro (Padova) Italy was employed for the work. The results show the detection of twenty-one elements which include Mg, P, Ca, K, Mn, Cu, Zn, S, Cr, Co, Ni and V that are implicated in the regulation of insulin and the control of the blood-sugar levels in the human body. The entire plant of Boerhavia diffusa, Securidaca longipedunculata stem, leaves of Peperomia pellucida, Macrosphyra longistyla, Olax subscorpioidea, Phyllanthus muerillanus, Jatropha gossypifolia, Cassia occidentalis, Phyllanthus amarus, and leaf and stem of Murraya koenigii, which have high concentrations of these elements could be recommended as vegetables, nutraceuticals, food additives, supplements and drugs in the control and management of diabetes, if toxicity profiles indicate that they are safe. However, significantly high contents of Al and Si in the entire plant of Bryophyllum pinnatum, and As, Cr, and Cu in Ocimum gratissimum leaf suggest that these plants should be avoided by diabetic patients to prevent complications.

  17. Comparing DNA extraction methods for analysis of botanical materials found in anti-diabetic supplements.

    Science.gov (United States)

    Llongueras, Jose P; Nair, Saraswathy; Salas-Leiva, Dayana; Schwarzbach, Andrea E

    2013-03-01

    A comparative performance evaluation of DNA extraction methods from anti-diabetic botanical supplements using various commercial kits was conducted, to determine which produces the best quality DNA suitable for PCR amplification, sequencing and species identification. All plant materials involved were of suboptimal quality showing various levels of degradation and therefore representing real conditions for testing herbal supplements. Eight different DNA extraction methods were used to isolate genomic DNA from 13 medicinal plant products. Two methods for evaluation, DNA concentration measurements that included absorbance ratios as well as PCR amplifiability, were used to determine quantity and quality of extracted DNA. We found that neither DNA concentrations nor commonly used UV absorbance ratio measurements at A(260)/A(280) between 1.7 and 1.9 are suitable for globally predicting PCR success in these plant samples, and that PCR amplifiablity itself was the best indicator of extracted product quality. However, our results suggest that A(260)/A(280) ratios below about 1.3 and above 2.3 indicated a DNA quality too poor to amplify. Therefore, A(260)/A(280) measurements are not useful to identify samples that likely will amplify but can be used to exclude samples that likely will not amplify reducing the cost for unnecessarily subjecting samples to PCR. The two Nucleospin(®) plant II kit extraction methods produced the most pure and amplifiable genomic DNA extracts. Our results suggest that there are clear, discernable differences between extraction methods for low quality plant samples in terms of producing contamination-free, high-quality genomic DNA to be used for further analysis.

  18. Study on how nanosilver-based inorganic antibacterial agent functions on biofilm formation of Candida albicans, inside the oral cavity.

    Science.gov (United States)

    Wang, Huili; Xie, Bing

    2016-09-01

    Candida albicans is a common symbiotic fungus in the oral cavity, which can easily adhere to the surface of implanted materials. Highlighted by a broad antibacterial spectrum and potent antibacterial effects, nanosilver-based inorganic antibacterial agents (NSBIAA) are currently being hotly discussed with regard to their influences on biofilm formation of Candida albicans. This paper aims to explore the influence of NSBIAA on biofilm formation of Candida albicans. The XTT reduction method and the method of crystal violet determination were applied in measuring the influence of NSBIAA on biofilm formation of Candida albicans. In addition, biofilm morphology was determined by crystal violet staining. It was observed that with the application of liquid antibacterial agent, at a concentration of 0.62 mg/ml, the biofilm activity of Candida albicans reduced (96.1 ± 3.0) %, along with a reduction in the biomass (95.4 ± 2.7) %, and biofilm formation was not observed under an inverted microscope. NSBIAA are able to inhibit biofilm formation.

  19. Lipid-based cochleates: a promising formulation platform for oral and parenteral delivery of therapeutic agents.

    Science.gov (United States)

    Rao, Ravi; Squillante, Emilio; Kim, Kwon H

    2007-01-01

    Cochleates are lipid-based supramolecular assemblies that display great potential as delivery systems for systemic delivery of drugs, including peptides, proteins, vaccines, oligonucleotides, and genes. This is mainly attributed to their high stability and biocompatibility and their ability to deliver both hydrophilic and lipophilic drugs. Cochleates have a unique multilayered spiral structure, which is composed of a negatively charged phospholipid and a divalent cation, and can encapsulate diverse drug molecules of various shapes and sizes while minimizing toxicity associated with polymeric materials present in micro- and nanoparticle systems. This review describes current technological advances in the preparation methods, physicochemical characterization, and potential applications of cochleates as a drug delivery system for systemic delivery of various types of therapeutic agents.

  20. New oral agents for erectile dysfunction: what is changing in our practice?

    Institute of Scientific and Technical Information of China (English)

    Antonio Aversa; Andrea Fabbri

    2001-01-01

    Erectile dysfunction (ED) is a highly prevalent disorder affecting an estimated 152 million men worldwide and is associated with a variety of behavioral risk factors, such as cigarette smoking and excessive alcohol consumption, as well as numerous age-related medical conditions, notably type-2 diabetes mellitus and cardiovascular disease. A rational step-wise approach which includes comprehensive medical and sexual history, a focused physical examination and essential laboratory tests such as fasting glucose, lipid profile and testosterone assay is to be preferred. Current diagnostic work-up does not recommend any of the specialized tests which were previously considered mandatory-i. e. penile pharmacotesting, Duplex ultrasound and nocturnal penile tumescence. Hormonal replacement therapy is appropriate only in the hypogonadal male with ED. Prior to direct intervention, the physician should consider altering modifiable risk factors or causes, although frequently insufficient to reverse ED completely. When indicated, oral therapy with new molecules (phosphodiesterase inhibitors or apomorphine) is the first-line treatment for the majority of patients because of potential benefits and lack of invasiveness.

  1. Role of oral hypoglycemic agents in the management of type 2 diabetes mellitus during Ramadan

    Directory of Open Access Journals (Sweden)

    Mir Iftikhar Bashir

    2012-01-01

    Full Text Available It is obligatory for all adult Muslims to observe fast during the holy month of Ramadan, but sick individuals including those with diabetes mellitus are exempted from the duty of fasting. Specific medical advice must be provided to individual patients concerning the potential risks they must accept if they decide to fast. Any alteration in medications deemed necessary to provide an effective and safe antidiabetic regimen should be instituted well before the start of Ramadan. Diet-controlled patients and those well controlled on insulin sensitizers have low risk of hypoglycemia and may safely fast with some modification in the timing of the doses. Newer generation sulfonylureas (gliclazide MR and glimepiride have reasonable safety profile during Ramadan fasting and are economical options for a large number of diabetics worldwide, especially in the developing countries; older, long acting sulfonylureas like glibenclamide and chlorpropamide should be avoided during fasting. Oral DPP-IV inhibitors are important substitutes to sulfonylureas for patients with diabetes mellitus during fasting owing to their glucose-dependent mechanism of action, efficacy, and tolerability. This group of drugs causes a moderate A1c reduction, are weight neutral, and have a very low risk of hypoglycemia. Short-acting insulin secretagogues are an option in the subset of fasting diabetic patients who have predominantly post-prandial hyperglycemia.

  2. FORMULATION AND EVALUATION OF ORAL CONTROLLED RELEASE DOSAGE FORM OF ANTI-HYPERTENSIVE AGENT

    Directory of Open Access Journals (Sweden)

    Lakshmi Parvathi A

    2012-12-01

    Full Text Available The aim of present investigation is preparation, characterization and evaluation of oral controlled release matrix tablets of Propranolol HCl in order to improve efficacy and to reduce the side effects. Tablets were prepared by direct compression method using different polymers like Guar gum, HPMC K4M, PVP and MCC used as the directly compressible vehicle. The granules were evaluated for pre-formulation characteristics and the tablets were subjected to post compression parameters, drug content and in-vitro dissolution release studies. In-vitro dissolution studies were carried out for 12 hrs and the results showed that among the nine formulations F8 and F9 showed good dissolution profile to control the drug release respectively. The drug release follows first order kinetics and the mechanism was found to be diffusion controlled for all the formulations (except F-9. The mechanism of drug release from F-9 was diffusion coupled with erosion. The Stability studies were carried out according to ICH guideline which indicates that the selected formulations (F8 and F9 were stable. In conclusion the results suggest that the developed matrix tablets of Propranolol HCl could perform therapeutically better than conventional dosage form, leading to improved efficacy and better patient compliance.

  3. Nattokinase: An Oral Antithrombotic Agent for the Prevention of Cardiovascular Disease

    Science.gov (United States)

    Weng, Yunqi; Yao, Jian; Sparks, Sawyer; Wang, Kevin Yueju

    2017-01-01

    Natto, a fermented soybean product, has been consumed as a traditional food in Japan for thousands of years. Nattokinase (NK), a potent blood-clot dissolving protein used for the treatment of cardiovascular diseases, is produced by the bacterium Bacillus subtilis during the fermentation of soybeans to produce Natto. NK has been extensively studied in Japan, Korea, and China. Recently, the fibrinolytic (anti-clotting) capacity of NK has been recognized by Western medicine. The National Science Foundation in the United States has investigated and evaluated the safety of NK. NK is currently undergoing a clinical trial study (Phase II) in the USA for atherothrombotic prevention. Multiple NK genes have been cloned, characterized, and produced in various expression system studies. Recombinant technology represents a promising approach for the production of NK with high purity for its use in antithrombotic applications. This review covers the history, benefit, safety, and production of NK. Opportunities for utilizing plant systems for the large-scale production of NK, or for the production of edible plants that can be used to provide oral delivery of NK without extraction and purification are also discussed. PMID:28264497

  4. Nattokinase: An Oral Antithrombotic Agent for the Prevention of Cardiovascular Disease

    Directory of Open Access Journals (Sweden)

    Yunqi Weng

    2017-02-01

    Full Text Available Natto, a fermented soybean product, has been consumed as a traditional food in Japan for thousands of years. Nattokinase (NK, a potent blood-clot dissolving protein used for the treatment of cardiovascular diseases, is produced by the bacterium Bacillus subtilis during the fermentation of soybeans to produce Natto. NK has been extensively studied in Japan, Korea, and China. Recently, the fibrinolytic (anti-clotting capacity of NK has been recognized by Western medicine. The National Science Foundation in the United States has investigated and evaluated the safety of NK. NK is currently undergoing a clinical trial study (Phase II in the USA for atherothrombotic prevention. Multiple NK genes have been cloned, characterized, and produced in various expression system studies. Recombinant technology represents a promising approach for the production of NK with high purity for its use in antithrombotic applications. This review covers the history, benefit, safety, and production of NK. Opportunities for utilizing plant systems for the large-scale production of NK, or for the production of edible plants that can be used to provide oral delivery of NK without extraction and purification are also discussed.

  5. Nattokinase: An Oral Antithrombotic Agent for the Prevention of Cardiovascular Disease.

    Science.gov (United States)

    Weng, Yunqi; Yao, Jian; Sparks, Sawyer; Wang, Kevin Yueju

    2017-02-28

    Natto, a fermented soybean product, has been consumed as a traditional food in Japan for thousands of years. Nattokinase (NK), a potent blood-clot dissolving protein used for the treatment of cardiovascular diseases, is produced by the bacterium Bacillus subtilis during the fermentation of soybeans to produce Natto. NK has been extensively studied in Japan, Korea, and China. Recently, the fibrinolytic (anti-clotting) capacity of NK has been recognized by Western medicine. The National Science Foundation in the United States has investigated and evaluated the safety of NK. NK is currently undergoing a clinical trial study (Phase II) in the USA for atherothrombotic prevention. Multiple NK genes have been cloned, characterized, and produced in various expression system studies. Recombinant technology represents a promising approach for the production of NK with high purity for its use in antithrombotic applications. This review covers the history, benefit, safety, and production of NK. Opportunities for utilizing plant systems for the large-scale production of NK, or for the production of edible plants that can be used to provide oral delivery of NK without extraction and purification are also discussed.

  6. Insulin monotherapy compared with the addition of oral glucose-lowering agents to insulin for people with type 2 diabetes already on insulin therapy and inadequate glycaemic control

    NARCIS (Netherlands)

    Vos, Rimke C; van Avendonk, Mariëlle JP; Jansen, Hanneke; Goudswaard, Alexander N; van den Donk, Maureen; Gorter, Kees; Kerssen, Anneloes; Rutten, Guy EHM

    2016-01-01

    BACKGROUND: It is unclear whether people with type 2 diabetes mellitus on insulin monotherapy who do not achieve adequate glycaemic control should continue insulin as monotherapy or can benefit from adding oral glucose-lowering agents to the insulin therapy. OBJECTIVES: To assess the effects of insu

  7. LOW RISK OF CARDIOVASCULAR DISEASES WITH METFORMIN COMPARED WITH OTHER ANTI-DIABETIC DRUGS IN PATIENTS WITH TYPE 2 DIABETES

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    Prathima Raj Dara

    2016-07-01

    Full Text Available BACKGROUND Diabetes is treatable, yet not withstanding when glucose levels are under control. It significantly increase the risk of coronary illness and stroke. Especially, type 2 diabetes may have the accompanying conditions that add to their danger for creating cardiovascular illness, for example, hypertension, weight, and abdominal cholesterol. This study to investigate the risk of cardiovascular malady (CVD in people with diabetes mellitus treated with metformin or other antidiabetic medications. SUBJECTS AND METHODS This was an observational study conducted in the Department of Medicine at Government General Hospital, Nizamabad. 500 patients were aged between 60 and below individuals diagnosed with cardiovascular problem irrespective of metformin or other anti-diabetic drugs from past years. Patient’s comparison with previous use of metformin or other anti-diabetic drugs among the individuals and calculated the risk of cardiovascular disease who is on metformin or anti-diabetic drugs. RESULTS In comparison with metformin, long-term use of other than metformin were at greater risk of developing CVD (Adjusted OR (AOR=0.83, 95% CI=1.12-2.60, but there was no consistent trend with increasing number of prescriptions. Long-term use of other antidiabetic drugs such as sulphonylurea (AOR=0.80, 95% CI=0.72-1.42, thiazolidinediones (AOR=0.69, 95% CI=0.31-2.40, or meglitinides (AOR=0.61, 95% CI=0.58-1.73 was showed related risk of developing CVD. CONCLUSION Long-term utilization of sulphonylurea, thiazolidinediones, or meglitinides was showed risk of developing CVD. There was a recommendation of a slightly bring down risk of CVD in long-term use of metformin.

  8. Acute oral toxicity study of ethanol extract of Ceiba pentandra leaves as a glucose lowering agent in diabetic rats

    Institute of Scientific and Technical Information of China (English)

    Hadiza Lami Muhammad; Adamu Yusuf Kabiru; Musa Bola Busari; Abdullah Mann; Abubakar Siddique Abdullah; Abdulrazaq Taye Usman; Usman Adamu

    2016-01-01

    Objective: To evaluate the use of Ceiba pentandra (C. pentandra) as a glucose lowering agent and the attendant physiological changes in albino rats. Methods: Acute oral toxicity study of the extract was carried out by the administration of 10, 100, 1 000, 1 600, 2 900, and 5 000 mg/kg body weight of C. pentandra to rats in their respective groups. Twenty healthy albino rats weighing between 140 and 150 g were randomly allotted to five groups of four rats each. 100 mg/kg body weight of alloxan monohydrate was i.p. administered to rats and rats with blood glucose ? 200 mg/dL were considered diabetic. 5 mg/kg body weight of standard drug, 200 and 400 mg/kg body weight of ethanol extract of C. pentandra were orally administered to diabetic rats in their respective groups once daily for 12 days while the control groups received 0.1 mL of normal saline for the same period. The blood glucose was checked after every 4 days and the experiment was terminated on the 17th day. Results: The safe dose (LD50) of the extract was greater than 5 000 mg/kg body weight. The extract treated groups exhibited a remarkable reduction in blood glucose [(87.72 ± 7.67) mg/dL for 200 mg/kg body weight dose and (86.33 ± 4.54) mg/dL for 400 mg/kg body weight dose] competitively with the normoglycemic group [(88.71 ± 4.56) mg/dL]. The body weight of the extract and standard drug treated groups appreciated significantly (P Conclusions: Ethanol extract of C. pentandra has glucose lowering effect and can ameliorate the biochemical abnormalities associated with diabetes mellitus.

  9. Scrapie Agent (Strain 263K can transmit disease via the oral route after persistence in soil over years.

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    Bjoern Seidel

    Full Text Available The persistence of infectious biomolecules in soil constitutes a substantial challenge. This holds particularly true with respect to prions, the causative agents of transmissible spongiform encephalopathies (TSEs such as scrapie, bovine spongiform encephalopathy (BSE, or chronic wasting disease (CWD. Various studies have indicated that prions are able to persist in soil for years without losing their pathogenic activity. Dissemination of prions into the environment can occur from several sources, e.g., infectious placenta or amniotic fluid of sheep. Furthermore, environmental contamination by saliva, excrements or non-sterilized agricultural organic fertilizer is conceivable. Natural transmission of scrapie in the field seems to occur via the alimentary tract in the majority of cases, and scrapie-free sheep flocks can become infected on pastures where outbreaks of scrapie had been observed before. These findings point to a sustained contagion in the environment, and notably the soil. By using outdoor lysimeters, we simulated a contamination of standard soil with hamster-adapted 263K scrapie prions, and analyzed the presence and biological activity of the soil-associated PrP(Sc and infectivity by Western blotting and hamster bioassay, respectively. Our results showed that 263K scrapie agent can persist in soil at least over 29 months. Strikingly, not only the contaminated soil itself retained high levels of infectivity, as evidenced by oral administration to Syrian hamsters, but also feeding of aqueous soil extracts was able to induce disease in the reporter animals. We could also demonstrate that PrP(Sc in soil, extracted after 21 months, provides a catalytically active seed in the protein misfolding cyclic amplification (PMCA reaction. PMCA opens therefore a perspective for considerably improving the detectability of prions in soil samples from the field.

  10. Uso do contraste oral negativo em exames de colangiografia por ressonância magnética Use of oral negative contrast agent in magnetic resonance cholangiopancreatography examinations

    Directory of Open Access Journals (Sweden)

    Mário de Melo Galvão Filho

    2002-10-01

    Full Text Available OBJETIVO: Realizamos estudo prospectivo das vias biliares e pancreáticas através de colangiografia por ressonância magnética, com a utilização de meio de contraste oral negativo. Os nossos objetivos foram verificar se este novo meio de contraste melhora a visualização das vias biliar e pancreática, além de identificar a freqüência de efeitos colaterais ao contraste e sua aceitação pelo paciente. MATERIAL E MÉTODO: Quinze voluntários (oito homens e sete mulheres com idades variando entre 18 e 54 anos (média de 29 anos, sem queixas ou cirurgias abdominais, foram submetidos a colangiografia por ressonância magnética. Foram realizadas duas seqüências colangiográficas em apnéia, antes e cinco minutos após a ingestão de 300 ml de contraste oral negativo. Os exames foram realizados em equipamento operando a 1,0 T. RESULTADOS: Setenta e três por cento dos voluntários consideraram o gosto ruim ou muito ruim, sugerindo uma aceitação discutível; 27% dos voluntários apresentaram náuseas; 20%, cólicas; 14%, azia ou parestesia labial; e 7%, diarréia. A visualização da via biliar extra-hepática foi considerada melhor após o contraste oral negativo em 9/15 voluntários (60% e do ducto pancreático principal em todos os cinco em que havia interposição de alças. CONCLUSÃO: O contraste oral negativo melhora a visualização dos ductos hepatocolédoco e pancreático principal em exames de colangiografia por ressonância magnética, apesar da baixa aceitação e dos seus efeitos colaterais.OBJECTIVE: The aim of this prospective study was to investigate the feasibility of using a negative oral contrast agent to null the bowel signal during magnetic resonance cholangiopancreatography. MATERIAL AND METHOD: Fifteen healthy volunteers with no previous history of pancreaticobiliary disease or surgery were imaged with a single-shot fast spin-echo pulse sequence, using a magnetic resonance imaging system operating at 1.0 T. Data

  11. 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.

  12. Therapeutic potential of the anti-diabetic agent metformin in targeting the skin cancer stem cell diaspora.

    Science.gov (United States)

    Reddi, Anand; Powers, Matthew A; Dellavalle, Robert P

    2014-05-01

    Type II diabetes is associated with increased prevalence of cancer including both melanoma and squamous cell carcinoma (SCC) of the skin. Emerging evidence from epidemiological studies suggest that diabetic patients on metformin have a lower risk of cancer incidence and mortality in a broad range of neoplasms. In both melanoma and SCC, populations of cancer stem cells (CSC) contribute to tumor initiation and metastasis. We propose that metformin constitutes a new class of targeted therapy that acts on the skin CSC diaspora. We posit that metformin selectively and simultaneously targets CSCs of the primary tumor as well as in metastatic niches thereby disrupting the dynamic dispersal of circulating CSCs between the primary tumor and metastatic site. This hypothesis suggests a new concept in dermato-oncology that treatment of type II diabetes and prevention of skin cancer are two sides of the same coin.

  13. Novel anti-diabetic agents in non-alcoholic fatty liver disease:a mini-review

    Institute of Scientific and Technical Information of China (English)

    Manhal Olaywi; Taruna Bhatia

    2013-01-01

    BACKGROUND: Non-alcoholic  fatty  liver  disease  (NAFLD) encompasses  a  spectrum  that  ranges  from  simple  steatosis  to non-alcoholic  steatohepatitis  (NASH)  and  to  cirrhosis.  The recommended  treatment  for  this  disease  includes  measures that target obesity and insulin resistance. The present review summarizes the role of newer anti-diabetic agents in treatment of NAFLD. DATA  SOURCES: PubMed,  MEDLINE  and  Ovid  databases were searched to identify human studies between January 1990 and January 2013 using specified key words. Original studies that  enrolled  patients  with  a  diagnosis  of  NAFLD  or  NASH and involved use of newer classes of anti-diabetic agents for a duration of at least 3 months were included. RESULTS: Out  of  the  screened  articles,  four  met  eligibility criteria and were included in our review. The classes of newer anti-diabetic medications described were dipeptidyl peptidase IV inhibitors and glucagon-like peptide-1 analogues. CONCLUSIONS: Liraglutide and Exenatide showed improvement in  transaminases  as  well  as  histology  in  patients  with  NASH. Sitagliptin showed improvement in transaminases but limited studies are there to access its effect on histology. Further studies are needed to support use of newer anti-diabetic medications in patients with NAFLD.

  14. Poor adherence with ACE inhibitors is a risk factor of CVA with oral hypoglycemic agents in diabetic patients.

    Science.gov (United States)

    Aftab, Muhammad Tariq; Dharamshi, Hasnain Abbas; Faraz, Ahmed; Shakeel, Saba; Shakeel, Osama

    2017-03-01

    Poor adherence with medicine declines the clinical outcome of pharmacotherapy. It may carry serious sequelae especially in case of antihypertensive drugs like cerebrovascular accident (CVA). This study has been planned to find the association of poor adherence with anti-hypertensive with CVA in diabetic and non- diabetic patients. One hundred CVA patients who were admitted through Emergency in Abbasi Shaheed hospital, a tertiary care hospital in Karachi, were recruited from Jun 2013 till Dec 2013. The criteria of inclusion was, diagnosed case of CVA, with primary hypertension, availability of patient's therapeutic record, consent of the patient or legal successor/heir. The criteria of exclusion was, secondary hypertension, newly diagnosed primary hypertensive patients and complete adherence with medication. Morisky medication adherence scale was applied. Therapeutic record was accessed. The mean age was 62.15 years with 3:1 male to female ratio. Adherence to medicine was graded 0.05) was seen in any combination (p>0.05). Thus it is concluded that poor adherence with ACE inhibitors may be a risk factor of CVA in diabetic patients using oral hypoglycemic agents.

  15. In Vivo Anti-Diabetic Activity of the Ethanolic Crude Extract of Sorbus decora C.K.Schneid. (Rosacea: A Medicinal Plant Used by Canadian James Bay Cree Nations to Treat Symptoms Related to Diabetes

    Directory of Open Access Journals (Sweden)

    Rose Vianna

    2011-01-01

    Full Text Available A number of potential anti-diabetic plants were identified through an ethnobotanical survey of the traditional pharmacopeia of the Cree of Eeyou Istchee (CEI—Northeastern Canada used against symptoms of diabetes and their biological activity assessed by in vitro bioassays. Among these, Sorbus decora C.K.Schneid. (Rosacea ranked highly and increased the transport of glucose in skeletal muscle cells in culture. The present study thus aimed at confirming the antidiabetic potential of S. decora in in vivo models of insulin resistance and diabetes, notably the streptozotocin Type 1 diabetic rat (STZ, the genetic KK-Ay Type 2 diabetic mouse and the rat rendered insulin resistant with 10% glucose water consumption for 6 weeks. Sorbus decora ethanolic crude extract (SDEE was administered orally (200 mg kg-1 and compared to metformin (150 or 500 mg kg-1. The intragastric (i.g. gavage of SDEE transiently decreased glycemia in STZ rats in a bi-phasic manner but the effect was cumulative over several days. In KK-Ay mice, SDEE incorporated in food (0.12% decreased glycemia by 15% within 1 week as compared to vehicle controls. In pre-diabetic insulin-resistant rats, SDEE fed daily by i.g. gavage for 2 weeks significantly decreased the slight hyperglycemia and hyperinsulinemia, without affecting sugar water intake. Using the HOMA insulin resistance parameter, the effect of SDEE was equivalent to that of metformin. In conclusion, the ethanolic crude extract of S. decora demonstrates both anti-hyperglycemic and insulin-sensitizing activity in vivo, thereby confirming anti-diabetic potential and validating CEI traditional medicine.

  16. Anti-diabetic effect of citrus pectin in diabetic rats and potential mechanism via PI3K/Akt signaling pathway.

    Science.gov (United States)

    Liu, Yanlong; Dong, Man; Yang, Ziyu; Pan, Siyi

    2016-08-01

    This study was performed to investigate the anti-diabetic effect of citrus pectin in type 2 diabetic rats and its potential mechanism of action. The results showed that fasting blood glucose levels were significantly decreased after 4 weeks of citrus pectin administration. Citrus pectin improved glucose tolerance, hepatic glycogen content and blood lipid levels (TG, TC, LDL-c and HDL-c) in diabetic rats. Citrus pectin also significantly reduced insulin resistance, which played an important role in the resulting anti-diabetic effect. Moreover, after the pectin treatment, phosphorylated Akt expression was upregulated and GSK3β expression was downregulated, indicating that the potential anti-diabetic mechanism of citrus pectin might occur through regulation of the PI3K/Akt signaling pathway. Together, these results suggested that citrus pectin could ameliorate type 2 diabetes and potentially be used as an adjuvant treatment.

  17. High performance thin layer chromatography fingerprinting, phytochemical and physico-chemical studies of anti-diabetic herbal extracts

    Science.gov (United States)

    Itankar, Prakash R.; Sawant, Dattatray B.; Tauqeer, Mohd.; Charde, Sonal S.

    2015-01-01

    Introduction: Herbal medicines have gained increasing popularity in the last few decades, and this global resurgence of herbal medicines increases their commercial value. However, this increasing demand has resulted in a decline in their quality, primarily due to a lack of adequate regulations pertaining to herbal medicines. Aim: To develop an optimized methodology for the standardization of herbal raw materials. Materials and Methods: The present study has been designed to examine each of the five herbal anti-diabetic drugs, Gymnema sylvester R. Br., Pterocarpus marsupium Roxburgh., Enicostema littorale Blume., Syzygium cumini (L.) Skeels. and Emblica officinalis Gaertn. The in-house extracts and marketed extracts were evaluated using physicochemical parameters, preliminary phytochemical screening, quantification of polyphenols (Folin–Ciocalteu colorimetric method) and high performance thin layer chromatography (HPTLC) fingerprint profiling with reference to marker compounds in plant extracts. Results: All the plants mainly contain polyphenolic compounds and are quantified in the range of 3.6–21.72% w/w. E. officinalis contain the highest and E. littorale contain the lowest content of polyphenol among plant extracts analyzed. HPTLC fingerprinting showed that the in-house extracts were of better quality than marketed extracts. Conclusion: The results obtained from the study could be utilized for setting limits for the reference phytoconstituents (biomarker) for the quality control and quality assurance of these anti-diabetic drugs. PMID:27011722

  18. Nutrient-deprivation autophagy factor-1 (NAF-1: biochemical properties of a novel cellular target for anti-diabetic drugs.

    Directory of Open Access Journals (Sweden)

    Sagi Tamir

    Full Text Available Nutrient-deprivation autophagy factor-1 (NAF-1 (synonyms: Cisd2, Eris, Miner1, and Noxp70 is a [2Fe-2S] cluster protein immune-detected both in endoplasmic reticulum (ER and mitochondrial outer membrane. It was implicated in human pathology (Wolfram Syndrome 2 and in BCL-2 mediated antagonization of Beclin 1-dependent autophagy and depression of ER calcium stores. To gain insights about NAF-1 functions, we investigated the biochemical properties of its 2Fe-2S cluster and sensitivity of those properties to small molecules. The structure of the soluble domain of NAF-1 shows that it forms a homodimer with each protomer containing a [2Fe-2S] cluster bound by 3 Cys and one His. NAF-1 has shown the unusual abilities to transfer its 2Fe-2S cluster to an apo-acceptor protein (followed in vitro by spectrophotometry and by native PAGE electrophoresis and to transfer iron to intact mitochondria in cell models (monitored by fluorescence imaging with iron fluorescent sensors targeted to mitochondria. Importantly, the drug pioglitazone abrogates NAF-1's ability to transfer the cluster to acceptor proteins and iron to mitochondria. Similar effects were found for the anti-diabetes and longevity-promoting antioxidant resveratrol. These results reveal NAF-1 as a previously unidentified cell target of anti-diabetes thiazolidinedione drugs like pioglitazone and of the natural product resveratrol, both of which interact with the protein and stabilize its labile [2Fe-2S] cluster.

  19. Biospectroscopy for studying the influences of anti-diabetic metals (V, Cr, Mo, and W) to the insulin signaling pathway

    Science.gov (United States)

    Safitri, Anna; Levina, Aviva; Lee, Joonsup; Carter, Elizabeth A.; Lay, Peter A.

    2017-03-01

    The prevalence of diabetes, particularly with respect to type 2 diabetes, has reached epidemic proportions and continues to grow worldwide. One of the potential therapeutic targets in the treatment of type 2 diabetes involves the role of protein tyrosine phosphatases in the negative regulation of insulin signaling. The complexes of V(V/IV), Cr(III), W(VI), and Mo(VI), have all been proposed as possible drugs in the treatment of diabetes mellitus. Anti-diabetic activities of V(V/IV), Cr(III), Mo(VI), and W(VI) compounds are likely to be based on similar mechanisms, which involve phosphorylation/dephosphorylation reactions in the glucose uptake and metabolism. In order to clearly understand biological activities and phosphorylation/dephosphorylation reactions involved in anti-diabetic actions of Cr(III), V(V/IV), Mo(VI), and W(VI) complexes, the current research involves the use of cultured insulin-sensitive cells treated with these compounds. These reactions were investigated through vibrational spectroscopy. Protein phosphorylation/dephosphorylation induced conformational changes in secondary protein structure from α-helix to β-sheet, and these changes were detected by the IR spectra, which showed changes in the wavenumber and intensities of signals within the composite protein amide I band.

  20. Anti-Diabetic Activity and Metabolic Changes Induced by Andrographis paniculata Plant Extract in Obese Diabetic Rats

    Directory of Open Access Journals (Sweden)

    Muhammad Tayyab Akhtar

    2016-08-01

    Full Text Available Andrographis paniculata is an annual herb and widely cultivated in Southeast Asian countries for its medicinal use. In recent investigations, A. paniculata was found to be effective against Type 1 diabetes mellitus (Type 1 DM. Here, we used a non-genetic out-bred Sprague-Dawley rat model to test the antidiabetic activity of A. paniculata against Type 2 diabetes mellitus (Type 2 DM. Proton Nuclear Magnetic Resonance (1H-NMR spectroscopy in combination with multivariate data analyses was used to evaluate the A. paniculata and metformin induced metabolic effects on the obese and obese–diabetic (obdb rat models. Compared to the normal rats, high levels of creatinine, lactate, and allantoin were found in the urine of obese rats, whereas, obese-diabetic rats were marked by high glucose, choline and taurine levels, and low lactate, formate, creatinine, citrate, 2-oxoglutarate, succinate, dimethylamine, acetoacetate, acetate, allantoin and hippurate levels. Treatment of A. paniculata leaf water extract was found to be quite effective in restoring the disturbed metabolic profile of obdb rats back towards normal conditions. Thisstudy shows the anti-diabetic potential of A. paniculata plant extract and strengthens the idea of using this plant against the diabetes. Further classical genetic methods and state of the art molecular techniques could provide insights into the molecular mechanisms involved in the pathogenesis of diabetes mellitus and anti-diabetic effects of A. paniculata water extract.

  1. Anti-Diabetic Activity and Metabolic Changes Induced by Andrographis paniculata Plant Extract in Obese Diabetic Rats.

    Science.gov (United States)

    Akhtar, Muhammad Tayyab; Bin Mohd Sarib, Mohamad Syakir; Ismail, Intan Safinar; Abas, Faridah; Ismail, Amin; Lajis, Nordin Hj; Shaari, Khozirah

    2016-08-09

    Andrographis paniculata is an annual herb and widely cultivated in Southeast Asian countries for its medicinal use. In recent investigations, A. paniculata was found to be effective against Type 1 diabetes mellitus (Type 1 DM). Here, we used a non-genetic out-bred Sprague-Dawley rat model to test the antidiabetic activity of A. paniculata against Type 2 diabetes mellitus (Type 2 DM). Proton Nuclear Magnetic Resonance (¹H-NMR) spectroscopy in combination with multivariate data analyses was used to evaluate the A. paniculata and metformin induced metabolic effects on the obese and obese-diabetic (obdb) rat models. Compared to the normal rats, high levels of creatinine, lactate, and allantoin were found in the urine of obese rats, whereas, obese-diabetic rats were marked by high glucose, choline and taurine levels, and low lactate, formate, creatinine, citrate, 2-oxoglutarate, succinate, dimethylamine, acetoacetate, acetate, allantoin and hippurate levels. Treatment of A. paniculata leaf water extract was found to be quite effective in restoring the disturbed metabolic profile of obdb rats back towards normal conditions. Thisstudy shows the anti-diabetic potential of A. paniculata plant extract and strengthens the idea of using this plant against the diabetes. Further classical genetic methods and state of the art molecular techniques could provide insights into the molecular mechanisms involved in the pathogenesis of diabetes mellitus and anti-diabetic effects of A. paniculata water extract.

  2. Anti-diabetic functions of soy isoflavone genistein: mechanisms underlying its effects on pancreatic β-cell function.

    Science.gov (United States)

    Gilbert, Elizabeth R; Liu, Dongmin

    2013-02-01

    Type 2 diabetes is a result of chronic insulin resistance and loss of functional pancreatic β-cell mass. Strategies to preserve β-cell mass and a greater understanding of the mechanisms underlying β-cell turnover are needed to prevent and treat this devastating disease. Genistein, a naturally occurring soy isoflavone, is reported to have numerous health benefits attributed to multiple biological functions. Over the past 10 years, numerous studies have demonstrated that genistein has anti-diabetic effects, in particular, direct effects on β-cell proliferation, glucose-stimulated insulin secretion and protection against apoptosis, independent of its functions as an estrogen receptor agonist, antioxidant, or tyrosine kinase inhibitor. Effects are structure-specific and not common to all flavonoids. While there are limited data on the effects of genistein consumption in humans with diabetes, there are a plethora of animal and cell-culture studies that demonstrate a direct effect of genistein on β-cells at physiologically relevant concentrations (<10 μM). The effects appear to involve cAMP/PKA signaling and there are some studies that suggest an effect on epigenetic regulation of gene expression. This review focuses on the anti-diabetic effects of genistein in both in vitro and in vivo models and potential mechanisms underlying its direct effects on β-cells.

  3. Periodontitis exposure within one year before anti-diabetic treatment and the risk of rheumatoid arthritis in diabetes mellitus patients: a population-based cohort study.

    Science.gov (United States)

    Chen, Hsin-Hua; Chen, Der-Yuan; Lin, Shih-Yi; Lai, Kuo-Lung; Chen, Yi-Ming; Chou, Yiing-Jenq; Chou, Pesus; Lin, Ching-Heng; Huang, Nicole

    2014-01-01

    To examine whether a history of periodontitis (PD) before anti-diabetic treatment is associated with risk of rheumatoid arthritis (RA) development in newly-treated diabetes mellitus (DM) patients. We conducted a population-based retrospective cohort study using the 1997-2009 National Health Insurance (NHI) claims data of one million representative individuals from all NHI enrollees. Adults with DM (aged ≥ 20 years) starting anti-diabetic treatment during 2001-2009 were classified as newly-treated DM patients. We identified 7097 DM subjects with PD history within one year before initiating anti-diabetes treatment (index date). By matching these 7097 subjects for age on the index date, sex, and year of the index date, we randomly extracted 14,194 DM subjects without PD history within one year before antidiabetic treatment. Adjusted hazard ratios (aHRs) with a 95% confidence interval (CI) were calculated by applying Cox proportional hazards models to quantify the association between PD history and RA risk. Compared with DM patients without PD exposure within one year before anti-diabetic treatment, crude HR and adjusted HR of RA among DM patients with PD exposure within one year before anti-diabetic treatment were 4.51 (95% CI, 1.39-14.64) and 3.77 (95% CI, 1.48-9.60). PD exposure within one year before anti-diabetic treatment was associated with increased RA risk in newly treated DM patients. The lack of knowledge about individual smoking status is a major limitation of this study.

  4. 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.

  5. Optimization of dose and technique for magnetic resonance studies with an oral contrast agent; Ottimizzazione della dose e della tecnica di esame nell'utilizzazione di un mezzo di contrasto orale nella risonanza magnetica

    Energy Technology Data Exchange (ETDEWEB)

    Broglia, L.; Tortora, A.; Maccioni, F.; Arpesani, R.; Marcelli, G.; Ascarelli, A.; Rossi, P. [Rome Policlinico Umberto I, Rome (Italy). Ist. di radiologia

    1999-05-01

    The aim of the study was to optimize the dose, scan delay and sequences for use in magnetic resonance (MR) studies with an oral contrast agent (FerriSeltz, Bracco Spa, Milan, Italy) to obtain positive or negative contrast enhancement in the bowel lumen. Ferric ammonium citrate, being positive or negative contrast agent according to its dilution, permits to tailor the dose to optimize bowel lumen opacification. [Italian] Obiettivo del lavoro e' stato di ottimizzare la dose, il ritardo dell'esecuzione dell'esame e le sequenze da selezionare utilizzando un mezzo di contrasto in risonanza magnetica con somministrazione orale (FerriSeltz, Bracco SpA) per ottenere l'opacizzazione positiva o negativa dell'intestino. Il FerriSeltz si comporta come un mdc positivo o negativo sulla base della sua diluizione e pertanto consente di adattare la dose per ottenere il tipo di opacizzazione adeguata alla malattia da esaminare.

  6. EDGE study in Russian Federation: efficacy and safety of vildagliptine in comparison with other oral antidiabetic agents in patients with type 2 diabetes mellitus

    Directory of Open Access Journals (Sweden)

    G R Galstyan

    2013-06-01

    Full Text Available According to international consensus, metformin is acknowledged as a first-line therapeutic agent for type 2 diabetes mellitus (T2DM. However, in most cases this treatment eventually requires intensification by supplementation with other hypoglycemic medications. The aim of the EDGE study (Effective Diabetes control with vildaGliptin and vildagliptin/mEtformin was to assess the efficacy and safety of vildagliptin in comparison with other oral agents in routine management of patients with T2DM that has been poorly controlled by metformin monotherapy.

  7. Efficacy of combination chemotherapy using a novel oral chemotherapeutic agent, TAS-102, together with bevacizumab, cetuximab, or panitumumab on human colorectal cancer xenografts

    OpenAIRE

    Tsukihara, Hiroshi; NAKAGAWA, FUMIO; SAKAMOTO, KAZUKI; Ishida, Keiji; TANAKA, NOZOMU; OKABE, HIROYUKI; Uchida, Junji; Matsuo, Kenichi; Takechi, Teiji

    2015-01-01

    TAS-102 is a novel oral nucleoside antitumor agent that consists of trifluridine (FTD) and tipiracil hydrochloride (TPI) at a molecular ratio of 1:0.5, and was approved in Japan in March 2014 for the treatment of patients with unresectable advanced or recurrent colorectal cancer that is refractory to standard therapies. In the present study, we used colorectal cancer xenografts to assess whether the efficacy of TAS-102 could be improved by combining it with bevacizumab, cetuximab or panitumum...

  8. In vitro and in vivo clinical pharmacology of dimethyl benzoylphenylurea, a novel oral tubulin-interactive agent.

    Science.gov (United States)

    Rudek, Michelle A; Zhao, Ming; Smith, Nicola F; Robey, Robert W; He, Ping; Hallur, Gurulingappa; Khan, Saeed; Hidalgo, Manuel; Jimeno, Antonio; Colevas, A Dimitrios; Messersmith, Wells A; Wolff, Antonio C; Baker, Sharyn D

    2005-12-01

    Dimethyl benzoylphenylurea (BPU) is a novel tubulin-interactive agent with poor and highly variable oral bioavailability. In a phase I clinical trial of BPU, higher plasma exposure to BPU and metabolites was observed in patients who experienced dose-limiting toxicity. The elucidation of the clinical pharmacology of BPU was sought. BPU, monomethylBPU, and aminoBPU were metabolized by human liver microsomes. Studies with cDNA-expressed human cytochrome P450 enzymes revealed that BPU was metabolized predominantly by CYP3A4 and CYP1A1 but was also a substrate for CYP2C8, CYP2D6, CYP3A5, and CYP3A7. BPU was not a substrate for the efflux transporter ABCG2. Using simultaneous high-performance liquid chromatography/diode array and tandem mass spectrometry detection, we identified six metabolites in human liver microsomes, plasma, or urine: monomethylBPU, aminoBPU, G280, G308, G322, and G373. In patient urine, aminoBPU, G280, G308, and G322 collectively represented BPU dose. G280, G308, G322, and G373 showed minimal cytotoxicity. When BPU was given p.o. to mice in the presence and absence of the CYP3A and ABCG2 inhibitor, ritonavir, there was an increase in BPU plasma exposure and decrease in metabolite exposure but no overall change in cumulative exposure to BPU and the cytotoxic metabolites. Thus, we conclude that (a) CYP3A4 and CYP1A1 are the predominant cytochrome P450 enzymes that catalyze BPU metabolism, (b) BPU is metabolized to two cytotoxic and four noncytotoxic metabolites, and (c) ritonavir inhibits BPU metabolism to improve the systemic exposure to BPU without altering cumulative exposure to BPU and the cytotoxic metabolites.

  9. Factors Associated with Long-Term Oral Hypoglycemic Agent Responsiveness in Korean Patients with Type 2 Diabetes Mellitus

    Directory of Open Access Journals (Sweden)

    Bo-Yeon Kim

    2011-06-01

    Full Text Available BackgroundThis study was performed to determine the factors associated with long-term oral hypoglycemic agent (OHA responsiveness in Korean type 2 diabetic patients.MethodsTwo groups of patients were selected among the type 2 diabetic patients who were followed for more than two years at a university hospital diabetes clinic. The OHA responsive group consisted of 197 patients whose HbA1c levels were maintained at ≤7% with OHA for more than two years. The OHA failure group consisted of 180 patients whose HbA1c levels were >8% in spite of optimal combined OHA therapy or patients who required insulin therapy within the two years of the study.ResultsThe OHA failure group had higher baseline values of fasting and postprandial glucose, HbA1c, and lower fasting, postprandial, and delta C-peptide compared to those of the OHA responsive group. The OHA failure group also had a higher proportion of female patients, longer diabetic duration, and more family history of diabetes. There were no significant differences in body mass index (BMI or insulin resistance index between the two groups. Multiple logistic regression analysis showed that the highest quartile of baseline fasting, postprandial glucose, and HbA1c and the lowest quartile of postprandial and delta C-peptide were associated with an increased odds ratio of OHA failure after adjustment for age, sex, body mass index, and family history of diabetes.ConclusionLower baseline values of postprandial and delta C-peptide and elevated fasting glucose and HbA1c are associated with long-term OHA responsiveness in Korean patients with type 2 diabetes mellitus.

  10. Synthesis and biological evaluation of novel gigantol derivatives as potential agents in prevention of diabetic cataract

    Science.gov (United States)

    As a continuation of our efforts directed towards the development of natural anti-diabetic cataract agents, gigantol was isolated from Herba dendrobii and was found to inhibit both aldose reductase (AR) and inducible nitric oxide synthase (iNOS) activity, which play a significant role in the develop...

  11. Effect of an oxygenating agent on oral bacteria in vitro and on dental plaque composition in healthy young adults

    OpenAIRE

    Mercedes eFernandez y Mostajo; Wil evan der Reijden; Mark eBuijs; Wouter eBeertsen; Fridus evan der Weijden; Wim eCrielaard; Egija eZaura

    2014-01-01

    Oral bacteria live in symbiosis with the host. Therefore, when mouthwashes are indicated, selective inhibition of taxa contributing to disease is preferred instead of broad-spectrum antimicrobials. The potential selectivity of an oxygenating mouthwash, Ardox-X® (AX), has not been assessed. The aim of this study was to determine the antimicrobial potential of AX and the effects of a twice-daily oral rinse on dental plaque composition. Material and methods: In vitro, 16 oral bacterial strains w...

  12. Discovery of WQ-3810: Design, synthesis, and evaluation of 7-(3-alkylaminoazetidin-1-yl)fluoro-quinolones as orally active antibacterial agents.

    Science.gov (United States)

    Itoh, Kenji; Kuramoto, Yasuhiro; Amano, Hirotaka; Kazamori, Daichi; Yazaki, Akira

    2015-10-20

    Novel 7-(3-alkylaminoazetidin-1-yl)fluoroquinolones were designed, synthesized, and evaluated for their antibacterial activities and oral absorption rates. Against Gram-negative bacteria, 10a-e, which have various alkyl groups containing different numbers of carbon atoms (C0-C3) at the C-7 alkylaminoazetidine position, showed potent and similar antibacterial activities, whereas the activity of 10f (C4, t-Bu) was significantly lower than those of 10a-e. Conversely, the oral absorption rates of 10a-e in rats increased depending on the number of carbon atoms in the alkyl groups; 10d (C3, n-Pr) and 10e (C3, i-Pr) had high oral absorption rates (>90% at 10 mg/kg). These results demonstrated that the introduction of alkyl groups onto C-7 aminoazetidine is useful for the improvement of the oral absorption rates of these drugs while maintaining their antibacterial activities. As a conclusion, from this series of fluoroquinolones, WQ-3810 (10e), having 3-isopropylaminoazetidine as the C-7 substituent, was identified as an orally active antibacterial agent with a potent in vitro activity.

  13. Randomized and double-blinded pilot clinical study of the safety and anti-diabetic efficacy of the Rauvolfia-Citrus tea, as used in Nigerian Traditional Medicine

    DEFF Research Database (Denmark)

    Campbell-Tofte, Joan I A; Mølgaard, Per; Josefsen, Knud

    2011-01-01

    The aim of this randomized and double blinded pilot clinical trial was to investigate the anti-diabetic efficacy of the Rauvolfia-Citrus (RC) tea in humans. We have earlier shown that a combination of calorie-restriction and chronic administration of the RC tea to the genetic diabetic (BKS-db) mice...

  14. Tissue lipid lowering-effect of a traditional Nigerian anti-diabetic infusion of Rauwolfia vomitoria foilage and Citrus aurantium fruit

    DEFF Research Database (Denmark)

    Campbell, J. I. A.; Mortensen, Alicja; Mølgaard, P.

    2006-01-01

    The toxicity and anti-diabetic properties of an aqueous plant extract made by boiling Rauwolfia vomitoria foilage and Citrus aurantium fruits were evaluated in mice. A single dosage corresponding to 70 x the human-daily-dose was non-toxic when administered to 6-week-old NMRI lean mice or 6- or 11...

  15. pattern of anti diabetic drug prescription at a health facility in jos ...

    African Journals Online (AJOL)

    Administrator

    Introduction: Type 2 diabetes mellitus is a disorder that can be managed with oral or parenteral medications. ... 1 glucose intolerance . In the United States, it is estimated that as at the year 2000, 11 million. Americans had .... 7 Worth J., Soran H., Is there a role for low carbohydrate diet in management of Type 2. Diabetes?

  16. ANTI-DIABETIC ACTIVITY OF LAGENARIA SICERARIA PULP AND SEED EXTRACT IN NORMAL AND ALLOXAN-INDUCED DIABETIC RATS

    Directory of Open Access Journals (Sweden)

    Somshuvra Bhattacharya et al

    2012-09-01

    Full Text Available The aim of the present study was to evaluate the possible anti-diabetic potential of Lagenaria siceraria pulp extract (LSPE and Lagenaria siceraria seed extract (LSSE against the pancreatic damage from alloxan-induced diabetes in rats related to diabetes mellitus. Lagenaria siceraria induced significant reduction in blood glucose and increasing of serum insulin, our data indicate that the level of glucose in the animals that were subjected with alloxan was 210 mg/dl comparing with normal 70 mg/dl, the level of blood glucose in diabetic group when subjected with Lagenaria siceraria extract decreased to 89-106.5 mg/dl. These findings suggest that LSPE and LSSE treatment exerts therapeutic protective effect in diabetes by preserving pancreatic cell integrity and significant activity extract, which supports traditional usage of the plant to prevent diabetic complications.

  17. Molecular interaction between glimepiride and Soluplus®-PEG 4000 hybrid based solid dispersions: Characterisation and anti-diabetic studies.

    Science.gov (United States)

    Reginald-Opara, Joy Nneji; Attama, Anthony; Ofokansi, Kenneth; Umeyor, Chukwuebuka; Kenechukwu, Frankline

    2015-12-30

    The objective of this study was to evaluate a novel blend of polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol 6000 grafted copolymer (Soluplus®) and polyethylene glycol (PEG) 4000 for solubility enhancement, physicochemical stability and anti-diabetic efficacy of the produced solid dispersions containing glimepiride, a biopharmaceutics classification system (BCS) class II sulphonylurea. Different batches of glimepiride solid dispersions (SD) were prepared by the solvent evaporation method using the individual polymers and blends of the polymers at different ratios. The Soluplus®-PEG 4000 (sol-PEG) hybrid polymer based glimepiride solid dispersions were characterized by differential scanning calorimetry (DSC), fourier transform infrared (FTIR) spectroscopy, micromeritics and dissolution studies. In vivo anti-diabetic activity was determined by measuring the changes in blood glucose concentrations in albino rats. The solid dispersions showed good flow properties and excellent practical yield. Drug content and release from the different formulations increased when Soluplus® was used as the main matrix polymer. The kinetics of drug release from all the solid dispersions followed first order. Solid state characterization confirmed the formation of amorphous glimepiride solid dispersions in the Sol-PEG hybrid polymer and no strong drug-polymer interaction was observed. The blood glucose reduction in albino rats by the Sol-PEG-Glim SDs was significantly (p<0.05) higher and more sustained when compared with the plain drug sample and commercially available product. Optimized SD batches (SP1 and SP3) showed a reduction in blood glucose level from 100% to 9.81% and 8.97%, respectively, at Tmax of 3h. The Sol-PEG-Glim SD was found to be stable over a period of 6 months (at 40°C, 70% RH) with no significant changes in the drug content. Thus, the Sol-PEG polymeric hybrids represent a promising tool for enhanced delivery of glimepiride.

  18. Anti-diabetic and renoprotective effects of aliskiren in streptozotocin-induced diabetic nephropathy in female rats.

    Science.gov (United States)

    Mahfoz, Amal M; El-Latif, Hekma A Abd; Ahmed, Lamiaa A; Hassanein, Nahed M; Shoka, Afaf A

    2016-12-01

    Since chronic kidney disease due to diabetic nephropathy (DN) is becoming an ever larger health burden worldwide, more effective therapies are desperately needed. In the present study, the anti-diabetic and renoprotective effects of aliskiren have been evaluated in streptozotocin (STZ)-induced DN in rats. DN was induced by a single intraperitoneal injection of STZ (65 mg/kg). Three weeks after STZ, rats were divided into four groups; normal, diabetic, diabetic treated with gliclazide (10 mg/kg/day) for 1 month, and diabetic treated with aliskiren (50 mg/kg/day) for 1 month. At the end of the experiment, mean arterial blood pressure and heart rate were recorded. Rats were then euthanized and serum was separated for determination of glucose, insulin, kidney function tests, superoxide dismutase activity (SOD), adiponectin, and tumor necrosis factor-alpha (TNF-α). One kidney was used for estimation of malondialdehyde (MDA), reduced glutathione (GSH), and nitric oxide (NO) contents. Other kidney was used for histopathological study and immunohistochemical measurement of caspase-3 and transforming growth factor beta (TGF-β). In addition, islets of Langerhans were isolated from normal rats by collagenase digestion technique for in vitro study. Aliskiren normalized STZ-induced hyperglycemia, increased insulin level both in vivo and in vitro, normalized kidney function tests and blood pressure, and alleviated STZ-induced kidney histopathological changes. This could be related to the ability of aliskiren toward preserving hemodynamic changes and alleviating oxidative stress and inflammatory and apoptotic markers induced by STZ in rats. However, aliskiren was more effective than gliclazide in relieving STZ-induced DN. These findings support the beneficial effect of aliskiren treatment in DN which could be attributed to its anti-diabetic, renoprotective, antioxidant, anti-inflammatory, and anti-apoptotic effects. Moreover, clinical studies are required to establish the

  19. A better anti-diabetic recombinant human fibroblast growth factor 21 (rhFGF21 modified with polyethylene glycol.

    Directory of Open Access Journals (Sweden)

    Zhifeng Huang

    Full Text Available As one of fibroblast growth factor (FGF family members, FGF21 has been extensively investigated for its potential as a drug candidate to combat metabolic diseases. In the present study, recombinant human FGF21 (rhFGF21 was modified with polyethylene glycol (PEGylation in order to increase its in vivo biostabilities and therapeutic potency. At N-terminal residue rhFGF21 was site-selectively PEGylated with mPEG20 kDa-butyraldehyde. The PEGylated rhFGF21 was purified to near homogeneity by Q Sepharose anion-exchange chromatography. The general structural and biochemical features as well as anti-diabetic effects of PEGylated rhFGF21 in a type 2 diabetic rat model were evaluated. By N-terminal sequencing and MALDI-TOF mass spectrometry, we confirmed that PEG molecule was conjugated only to the N-terminus of rhFGF21. The mono-PEGylated rhFGF21 retained the secondary structure, consistent with the native rhFGF21, but its biostabilities, including the resistance to physiological temperature and trypsinization, were significantly enhanced. The in vivo immunogenicity of PEGylated rhFGF21 was significantly decreased, and in vivo half-life time was significantly elongated. Compared to the native form, the PEGylated rhFGF21 had a similar capacity of stimulating glucose uptake in 3T3-L1 cells in vitro, but afforded a significantly long effect on reducing blood glucose and triglyceride levels in the type 2 diabetic animals. These results suggest that the PEGylated rhFGF21 is a better and more effective anti-diabetic drug candidate than the native rhFGF21 currently available. Therefore, the PEGylated rhFGF21 may be potentially applied in clinics to improve the metabolic syndrome for type 2 diabetic patients.

  20. Anti-diabetic and anti-oxidant potential of aged garlic extract (AGE) in streptozotocin-induced diabetic rats.

    Science.gov (United States)

    Thomson, Martha; Al-Qattan, Khaled K; Js, Divya; Ali, Muslim

    2016-01-19

    Although aged garlic extract (AGE) shares some active components with fresh garlic and in spite of its palatability and milder side effects, the anti-diabetic and related anti-oxidant properties of AGE have not been investigated extensively, and the reported findings are inconsistent. This study investigated the anti-diabetic effects of 3 incremental doses of AGE in streptozotocin (STZ)-induced diabetic rats (fasting blood sugar > 20 mM). Diabetic rats were divided into a control diabetic group (CD) and AGE-treated diabetic group (AGE-D). The AGE-D was divided into 3 groups and accordingly treated with AGE i.p. at 100, 300 and 600 mg/kg daily for 8 weeks. A control normal group (CN) was also included for reference. Compared to the CN group, the CD group showed significant loss of body weight (over 50 %); and decreased serum insulin concentration (10 fold) and total anti-oxidant level and catalase activity (45-70 %) in serum, kidney and liver. Conversely, the CD rats had an elevated blood glucose (nearly 4 fold), serum cholesterol (nearly 2 fold) and triglycerides (>2 fold), erythrocyte glycated hemoglobin (GHb, 3 fold) and kidney and liver lipid peroxidation (MDA levels). Treatment with AGE positively reversed the diabetic changes in the targeted parameters to levels significantly lower than those measured in the CD group and the degrees of attenuation were almost dose dependent especially with the two higher doses. AGE exhibits a dose-dependent ameliorative action on indicators of diabetes in STZ-induced diabetic rats.

  1. 糖尿病治疗药物的再评价%Reappraisal of anti-diabetic drugs

    Institute of Scientific and Technical Information of China (English)

    刘静; 靳立英; 王云芳

    2011-01-01

    自从2007年糖尿病指南颁布3年以来,在糖尿病防治研究领域陆续完成了一系列重要研究,这些研究结论为糖尿病防治注入了大量新信息.在此背景下,对2007版糖尿病指南进行了再评价,并重新评估了常用糖尿病药物在糖尿病治疗治疗中的地位.文中结合《2010年中国2型糖尿病防治指南(讨论稿)》对各类糖尿病药物作用特点做一简要介绍.%In the 3 years since the publication of the 2007 guidelines of diabetes mellitus guidelines, research on diabetes mellitus has actively been pursued, and the results of new important studies (including several large-scale randomized trials) have been published. Some of these studies have reinforced the evidence on which the recommendations of the 2007 diabetes mellitus guidelines were based. Other studies have widened the information available in 2007, modifying some of the previous concepts. It is suggested that new evidence based on recommendations could be appropriated, especially in the aspects of anti-diabetic drugs. The aim of this review article was to address the renewed concepts of the clinical recommendations of anti-diabetic drugs based on the 2010 edition of diabetes mellitus guidelines.

  2. Aderência de diabéticos ao tratamento medicamentoso com hipoglicemiantes orais Adhesión de diabéticos al tratamiento con hipoglucemiantes orales Adherence of diabetics patient to pharmacological treatment with oral hypoglycemic agents

    Directory of Open Access Journals (Sweden)

    Márcio Flávio Moura de Araújo

    2010-06-01

    Full Text Available Objetivou-se identificar a adesão de diabéticos de Sobral CE ao tratamento farmacológico com hipoglicemiantes orais. Investigaram-se 79 diabéticos de seis unidades básicas de saúde de Sobral CE mediante visitas domiciliárias durante o período de março a junho de 2007. Para coleta de dados utilizou-se um formulário estruturado e a aplicação do Teste de Morisky e Green adaptado. Um pouco mais da metade dos estudados, 54,5%, referiu não ter o cuidado de cumprir o horário de ingestão dos fármacos preestabelecido; a maioria não se esquece de tomar a medicação (66%. Ademais, 90% dos investigados apresentam sentimento de pesar ao deixar de tomar os hipoglicemiantes orais. Identificou-se que 54,4% e 45,5% eram menos aderentes e mais aderentes à terapia medicamentosa com hipoglicemiantes orais, respectivamente. A adesão à terapia farmacológica com hipoglicemiantes orais é fundamental para um bom controle glicêmico e a prevenção de complicações micro e macrovasculares.El objetivo fue identificar la adhesión de diabéticos de Sobral CE, Brasil, al tratamiento farmacológico con agentes hipoglucemiantes orales.Fueron investigados 79 diabéticos de seis unidades básicas de salud de Sobral-CE, Brasil, mediante visitas domiciliarias durante el período de marzo a junio de 2007. Para la recolecta de datos fue utilizado un cuestionario estructurado y la aplicación del Test de Morisky y Green adaptado. Poco más de la mitad de los estudiados, 54.5%, dijo no tener cuidado de cumplir con el horario preestablecido para la ingestión de los fármacos; la mayoría no se olvida de tomar la medicación (66%. Además, el 90% de los investigados presentó sentimientos de aflicción al dejar de tomar los hipoglucemiantes orales. Se identificó que el 54.4% y el 45.5% presentaban menos adherencia y mayor adherencia respectivamente - a la terapia con fármacos hipoglucemiantes orales. .La adhesión a la terapia farmacológica con

  3. Development of oral agent in the treatment of multiple sclerosis: how the first available oral therapy, Fingolimod will change therapeutic paradigm approach

    Directory of Open Access Journals (Sweden)

    Gasperini C

    2012-07-01

    Full Text Available Claudio Gasperini,1 Serena Ruggieri21Department of Neurosciences, S Camillo Forlanini Hospital, 2Department of Neurology and Psychiatry, University of Rome “Sapienza,” Rome, ItalyAbstract: Multiple sclerosis (MS is a chronic inflammatory disorder of the central nervous system, traditionally considered to be an autoimmune, demyelinating disease. Based on this understanding, the initial therapeutic strategies were directed at immune modulation and inflammation control. At present, there are five licensed first-line disease-modifying drugs and two second-line treatments in MS. Currently available MS therapies have shown significant efficacy throughout many trials, but they produce different side-effect profiles in patients. Since they are well known and safe, they require regular and frequent parenteral administration and are associated with limited long-term treatment adherence. Thus, there is an important need for the development of new therapeutic strategies. Several oral compounds are in late-stage development for treating MS. Fingolimod (FTY720; Novartis, Basel, Switzerland is an oral sphingosine-1-phosphase receptor modulator which has demonstrated superior efficacy compared with placebo and interferon β-1a in Phase III studies and has been approved in the treatment of MS. We summarily review the oral compounds in study, focusing on the recent development, approval and the clinical experience with FTY720.Keywords: multiple sclerosis, oral compounds, fingolimod, fty720, sphingosine 1, phosphate, patient satisfaction

  4. Anti-Diabetic Effects of CTB-APSL Fusion Protein in Type 2 Diabetic Mice

    Directory of Open Access Journals (Sweden)

    Yunlong Liu

    2014-03-01

    Full Text Available To determine whether cholera toxin B subunit and active peptide from shark liver (CTB-APSL fusion protein plays a role in treatment of type 2 diabetic mice, the CTB-APSL gene was cloned and expressed in silkworm (Bombyx mori baculovirus expression vector system (BEVS, then the fusion protein was orally administrated at a dose of 100 mg/kg for five weeks in diabetic mice. The results demonstrated that the oral administration of CTB-APSL fusion protein can effectively reduce the levels of both fasting blood glucose (FBG and glycosylated hemoglobin (GHb, promote insulin secretion and improve insulin resistance, significantly improve lipid metabolism, reduce triglycerides (TG, total cholesterol (TC and low density lipoprotein (LDL levels and increase high density lipoprotein (HDL levels, as well as effectively improve the inflammatory response of type 2 diabetic mice through the reduction of the levels of inflammatory cytokines tumor necrosis factor-α (TNF-α and interleukin-6 (IL-6. Histopathology shows that the fusion protein can significantly repair damaged pancreatic tissue in type 2 diabetic mice, significantly improve hepatic steatosis and hepatic cell cloudy swelling, reduce the content of lipid droplets in type 2 diabetic mice, effectively inhibit renal interstitial inflammatory cells invasion and improve renal tubular epithelial cell nucleus pyknosis, thus providing an experimental basis for the development of a new type of oral therapy for type 2 diabetes.

  5. Anti-diabetic effects of CTB-APSL fusion protein in type 2 diabetic mice.

    Science.gov (United States)

    Liu, Yunlong; Gao, Zhangzhao; Guo, Qingtuo; Wang, Tao; Lu, Conger; Chen, Ying; Sheng, Qing; Chen, Jian; Nie, Zuoming; Zhang, Yaozhou; Wu, Wutong; Lv, Zhengbing; Shu, Jianhong

    2014-03-13

    To determine whether cholera toxin B subunit and active peptide from shark liver (CTB-APSL) fusion protein plays a role in treatment of type 2 diabetic mice, the CTB-APSL gene was cloned and expressed in silkworm (Bombyx mori) baculovirus expression vector system (BEVS), then the fusion protein was orally administrated at a dose of 100 mg/kg for five weeks in diabetic mice. The results demonstrated that the oral administration of CTB-APSL fusion protein can effectively reduce the levels of both fasting blood glucose (FBG) and glycosylated hemoglobin (GHb), promote insulin secretion and improve insulin resistance, significantly improve lipid metabolism, reduce triglycerides (TG), total cholesterol (TC) and low density lipoprotein (LDL) levels and increase high density lipoprotein (HDL) levels, as well as effectively improve the inflammatory response of type 2 diabetic mice through the reduction of the levels of inflammatory cytokines tumor necrosis factor-α (TNF-α) and interleukin-6 (IL-6). Histopathology shows that the fusion protein can significantly repair damaged pancreatic tissue in type 2 diabetic mice, significantly improve hepatic steatosis and hepatic cell cloudy swelling, reduce the content of lipid droplets in type 2 diabetic mice, effectively inhibit renal interstitial inflammatory cells invasion and improve renal tubular epithelial cell nucleus pyknosis, thus providing an experimental basis for the development of a new type of oral therapy for type 2 diabetes.

  6. Oral misoprostol in the prevention of uterine bleeding after surgical evacuation of first trimester abortion: a comparative study of three uterotonic agents.

    Science.gov (United States)

    Aramide, T M; Olusegun, A K; Akinfolarin, A C; Oriola, D F

    2014-01-01

    This comparative study was aimed at determining the effectiveness of oral Misoprostol compared with intravenous Ergometrine and intravenous Oxytocin in reducing vaginal bleeding following surgical evacuation for first trimester abortions. This was a single-blind placebo-controlled study in which patients with first trimester uncomplicated abortions were divided into three groups using computer-generated randomization table. The first group was administered oral Misoprostol, the second group had intravenous Ergometrine, and the third group was administered intravenous Oxytocin. The uterotonic agents were administered before the surgical evacuation was carried out. There was statistically significant reduction in blood loss after the evacuation in the Misoprostol group ( P Misoprostol group (2.00 ± 0.86) compared with 4.43 ± 0.92 and 4.64 ± 1.06 days in the Ergometrine and Oxytocin groups, respectively ( P Misoprostol and Ergometrine groups (60.7% and 57.1%, respectively) compared with the Oxytocin group. Oral Misoprostol appeared to demonstrate superior efficacy in reducing uterine bleeding after surgical evacuation, compared to the other commonly used uterotonic agents.

  7. The effect of single agent oral fusaric acid (FA) on the growth of subcutaneously xenografted SCC-1 cells in a nude mouse model.

    Science.gov (United States)

    Ruda, James M; Beus, Kirt S; Hollenbeak, Christopher S; Wilson, Ronald P; Stack, Brendan C

    2006-09-01

    To determine whether oral administration of fusaric acid (FA) inhibits tumor growth in an animal model of head and neck cancer (HNSCC). In vivo murine model, two arm controlled study. Thirty-eight (38) 5-week-old athymic nude mice were randomly assigned to a fusaric acid treatment group (1 mg/mL) (n = 19) or a sterile saline group (n = 19). A left, lateral flank subcutaneous injection of 2.0 x 10(6) UM-SCC-1 cells were administered to all mice on day 1. Both groups were gavaged daily with either 0.25 mLs of oral FA or sterile saline throughout the experiment (32 days). Latency to a measurable tumor (> or =65 mm3), and tumor volumes were recorded after tumor xenografting. Tumor weights were recorded at the conclusion of the experiment. Tumor volume growth curves were modeled as polynomial functions of time with treatment interaction effects. Survivorship functions for time to measurable tumor were estimated using the Kaplan-Meier product limit estimator. Survival analysis showed mice treated with FA developed measurable tumors after a significantly longer interval post-xenografting than control mice (p = 0.00451). By Day 9, all mice in the control group had developed measurable tumors in comparison to only 78% of mice in the FA group. Likewise, estimated growth curves for both groups suggested that mice receiving FA demonstrated significantly slower tumor growth rates throughout the entire study period (p < 0.0001). At the conclusion of the experiment, tumor weights from both the control and FA groups were also significantly different (p = 0.0142). Single agent oral fusaric acid (1 mg/mL) is an inhibitor of UM-SCC-1 in a murine model. As an orally active agent, it may have a potential role in the treatment of human squamous cell carcinoma of the head and neck.

  8. SU-F-P-29: Impact of Oral Contrast Agent for Assisting in Outlining Small Intestine On Pelvic IMAT Dose in Patients with Cervical Cancer

    Energy Technology Data Exchange (ETDEWEB)

    Zhang, R; Bai, W; Fan, X [The Fourth Hospital of Hebei Medical University, Shijiazhuang, Hebei (China)

    2016-06-15

    Purpose: As the advanced intensity modulated arc therapy(IMAT) delivery systems becoming a main role of treatment ways, which places even greater demands on delivering accuracy. The impact of oral contrast agent (meglumine diatrizoate) for assisting in outlining the small intestine on pelvic IMAT dose in patients with cervical cancer was investigated. Methods: Ten cervical cancer patients for postoperative radiotherapy underwent CT scans, and the planning target volumes (PTV) and organs at risk (including the small intestine, rectum, bladder, colon and the left and right femoral head) were contoured. The IMAT plans were generated on Oncentra v4.1 planning system for each case, PTV was prescribed to 50.4 Gy in 28 fractions. Then another plan was generated by re-calculating the radiation dose after changing the electron density of the small bowel. The first plan (plan A) was the conventional IMAT plan (with oral contrast agent), and the second one (plan B) specified the electron density of the small bowel (without oral contrast agent). Paired t-test was used to compare the dose distribution between the two plans. Results: The PTV’s D2, D50, D95, V110, conformity index, and homogeneity index of plans A and B were 5610.5 vs. 5611.4 cGy (P=0.175), 5348.5 vs. 5348.0 cGy (P=0.869), 5039 vs. 5042.3 (P=0.518), 6.0% vs. 6.1 %( P=0.886), 0.1269 vs. 0.1271 (P=0.34) and 0.8421 vs. 0.8416 (P=0.598), respectively. The volumes of the small bowel receiving at least 30 Gy (V30) and the minimum dose of 2% volume accepted (D2) for plans A and B were 31.6% vs. 31.9% (P=0.371) and 5067.8 vs. 5085.4 cGy (P=0.377), while rectum V50 of the two plans was 12.4% vs. 12.1% (P=0.489). Conclusion: The oral contrast agent (meglumine diatrizoate) filling the small intestine does not lead to a significant increase in the pelvic IMAT dose in patients with cervical cancer.

  9. Anti-diabetic constituents of mulberry leaf%桑叶抗糖尿病活性成分研究

    Institute of Scientific and Technical Information of China (English)

    王娅; 李嘉盈

    2016-01-01

    目的:研究桑叶抗糖尿病的活性成分。方法桑叶用80%乙醇和水提取。利用硅胶、凝胶等柱色谱及制备液相色谱进行分离,并根据理化性质和有机波谱技术鉴定了化合物的结构,进一步通过测定生物碱类化合物和黄酮苷类化合物对胰岛素抵抗的 HepG2细胞葡萄糖消耗量来评价其抗糖尿病活性。结果从桑叶中分离鉴定了8个化合物,分别为:1-脱氧野尻霉素(1),1,4-dideoxy -1,4-imino -D -arabinitol(2),山奈酚-3-O -β-D -吡喃葡萄糖苷(3),β-谷甾醇(4),正三十四烷醇(5),oxyresveratrol(6),熊果酸(7),葡萄糖乙醇苷(8),此外化合物3能够显著提高胰岛素抵抗 HepG2细胞葡萄糖消耗量。结论化合物3具有较强的抗糖尿病活性。%Objective To study the chemical constituents and their anti -diabetic activity from the mulberry leaf.Methods Extrac-ted with 80% ethyl alcohol and water,the constituents were isolated by chromatography of silica gel,ODS and p -HPLC,whose struc-tures were identified on the basis of the physical properties and spectral analysis.Furthermore,glucose consumption assays in insulin -resistance HepG2 cells were used to assay the anti -diabetic activity of flavonoid glycosides and alkaloids.Results Eight compounds were isolated from mulberry leaf and identified as 1 -deoxynojirimycin(1),1,4 -dideoxy -1,4 -imino -D -arabinitol(2),Kaemper-ol -3 -O -β-D -glucopyranoside(3),β-stigmasterol (4),n -tetratriacontanol (5),oxyresveratrol (6),ursolic acid (7),ethyl-β-D -glucopyranoside(8)and compound 3 significantly stimulated glucose consumption and phosphorylation of Akt in insulin re-sistance HepG2 cells.Conclusions Compound 3 exhibits excellent anti -diabetic activity.

  10. Novel anti-diabetic effect of SCM-198 via inhibiting the hepatic NF-κB pathway in db/db mice.

    Science.gov (United States)

    Huang, Hui; Xin, Hong; Liu, Xinhua; Xu, Yajun; Wen, Danyi; Zhang, Yahua; Zhu, Yi Zhun

    2012-04-01

    There are reports of early evidence that suggest the involvement of chronic low-grade inflammation in the pathogenesis of Type 2 diabetes. Thus, substances that have effects in reducing inflammation could be potential drugs for Type 2 diabetes. Leonurine (4-guanidino-n-butyl syringate; SCM-198) is an alkaloid in HL (Herba leonuri), which was reported to possess anti-inflammatory properties. We hypothesize that SCM-198 may have beneficial effects on Type 2 diabetes. In the present study, we attempted to test this hypothesis by evaluating the anti-diabetic effect of SCM-198 and the possible underlying mechanisms of its effects in db/db mice. SCM-198 (50, 100 and 200 mg/kg of body weight), pioglitazone (50 mg/kg of body weight, as a positive control) or 1% CMC-Na (sodium carboxymethylcellulose) were administered to the db/db or db/m mice once daily for 3 weeks. After 3 weeks, SCM-198 (200 mg/kg of body weight) treatment significantly reduced the fasting blood glucose level and increased the plasma insulin concentration in the db/db mice, meanwhile it significantly lowered the plasma TAG (triacylglycerol) concentration and increased the HDL (high-density lipoprotein)-cholesterol concentration. Moreover, the dysregulated transcription of the hepatic glucose metabolic enzymes, including GK (glucokinase), G6Pase (glucose-6-phosphatase) and PEPCK (phosphoenolpyruvate carboxykinase), was recovered by an Akt-dependent pathway. The pro-inflammatory mediators {such as TNFα (tumour necrosis factor α), IL (interleukin)-6, IL-1β, degradation of IκB [inhibitor of NF-κB (nuclear factor-κB)] α and thereafter activation of NF-κB} were reversed by SCM-198 treatment in the db/db mice. The present study provides first evidence that SCM-198 exhibits anti-inflammatory activity and has an ameliorating effect on diabetic symptoms via inhibiting of NF-κB/IKK (IκB kinase) pathway. Consequently, we suggest that SCM-198 may be a prospective agent for prevention and

  11. The Anti-diabetic Effects of GLP-1-gastrin Dual Agonist ZP3022 in ZDF rats

    DEFF Research Database (Denmark)

    Skarbaliene, Jolanta; Secher, Thomas; Jelsing, Jacob

    2015-01-01

    diabetic Zucker Diabetic Fatty (ZDF) rats. METHODS: ZDF rats aged 11 weeks were dosed s.c, b.i.d for 8 weeks with vehicle, ZP3022, liraglutide, exendin-4, or gastrin-17 with or without exendin-4. Glycemic control was assessed by measurements of HbA1c and blood glucose levels, as well as glucose tolerance...... during an oral glucose tolerance test (OGTT). Beta cell dynamics were examined by morphometric analyses of beta and alpha cell fractions. RESULTS: ZP3022 improved glycemic control as measured by terminal HbA1c levels (6.2±0.12 (high dose) vs. 7.9±0.07% (vehicle), P

  12. Effect of an oxygenating agent on oral microorganisms in vitro and on dental plaque composition in healthy young adults

    Directory of Open Access Journals (Sweden)

    Mercedes eFernandez y Mostajo

    2014-07-01

    Full Text Available Oral bacteria live in symbiosis with the host. Therefore, when mouthwashes are indicated, selective inhibition of taxa contributing to disease is preferred instead of broad-spectrum antimicrobials. The potential selectivity of an oxygenating mouthwash, Ardox-X® (AX, has not been assessed. The aim of this study was to determine the antimicrobial potential of AX and the effects of a twice-daily oral rinse on dental plaque composition. Material and methods: In vitro, 16 oral bacterial strains were tested using agar diffusion susceptibility, minimum inhibitory and minimum bactericidal concentration tests. A pilot clinical study was performed with 25 healthy volunteers. Clinical assessments and microbiological sampling of supragingival plaque were performed at one month before the experiment (Pre-exp, at the start of the experiment (Baseline and after the one-week experimental period (Post-exp. During the experiment individuals used AX mouthwash twice daily in absence of other oral hygiene measures. The microbiological composition of plaque was assessed by 16S rRNA gene amplicon sequencing. Results: AX showed high inter-species variation in microbial growth inhibition. The tested Prevotella strains and Fusobacterium nucleatum showed the highest sensitivity, while streptococci and Lactobacillus acidophilus were most resistant to AX. Plaque scores at Pre-exp and Baseline visits did not differ significantly (p = 0.193, nor did the microbial composition of plaque during a period of 7-days non-brushing but twice daily rinsing. Plaque scores increased from 2.21 (0.31 at Baseline to 2.43 (0.39 Post-exp. A significant microbial shift in composition was observed: genus Streptococcus and Veillonella increased while Corynebacterium, Haemophilus, Leptotrichia, Cardiobacterium and Capnocytophaga decreased (p ≤ 0.001. Conclusion: AX has the potential for selective inhibition of oral bacteria. The shift in oral microbiome after one week of rinsing deserves

  13. Treatment of oral malodour. Medium-term efficacy of mechanical and/or chemical agents: a systematic review

    NARCIS (Netherlands)

    Slot, D.E.; van der Geest, S.; van der Weijden, F.A.; Quirynen, M.

    2015-01-01

    Focused question What is the effect of a dentifrice (DF), a mouthwash (MW), tongue cleaning (TC), or any combination of these as adjunct to toothbrushing on intra-oral malodour and tongue coating as compared to toothbrushing alone in systemically healthy patients, when used for a minimum follow-up p

  14. Effect of an oxygenating agent on oral bacteria in vitro and on dental plaque composition in healthy young adults

    NARCIS (Netherlands)

    Fernandez y Mostajo, M.; van der Reijden, W.A.; Buijs, M.J.; Beertsen, W.; van der Weijden, F.; Crielaard, W.; Zaura, E.

    2014-01-01

    Oral bacteria live in symbiosis with the host. Therefore, when mouthwashes are indicated, selective inhibition of taxa contributing to disease is preferred instead of broad-spectrum antimicrobials. The potential selectivity of an oxygenating mouthwash, Ardox-X® (AX), has not been assessed. The aim o

  15. Impact of compliance with oral antihyperglycemic agents on health outcomes in type 2 diabetes mellitus: a focus on frequency of administration.

    Science.gov (United States)

    Guillausseau, Pierre-Jean

    2005-01-01

    Compliance with treatment is crucial to the optimal management of any chronic disease. Non-compliance with antihyperglycemic treatment is clearly a significant issue for patients with type 2 diabetes mellitus as it decreases the efficacy of the treatment and increases the risk of developing microvascular and macrovascular complications, therefore increasing the human and economic costs of this disease. The effect of low compliance on metabolic control has been shown to represent an increase of up to 1.4% in glycosylated hemoglobin. Achieving optimal compliance is therefore a therapeutic objective of prime importance. Many factors have been cited as contributing to poor compliance. Some of these, such as age, severe complications and disabilities, and social, educational, and financial difficulties, affect compliance with treatment in quite a significant manner, but are not modifiable by the healthcare provider. Other factors, such as the number of tablets per dose and polymedication, are modifiable but do not appear to be of major importance, whereas the frequency of administration is both an important and a modifiable factor affecting compliance with treatment. One strategy for optimization of compliance involves treatment of type 2 diabetes using oral antihyperglycemic agents with once-daily formulations. Recent data indicate that reducing the daily administration frequency of oral antihyperglycemic agents improves compliance with treatment and consequently metabolic control. Therefore, optimization of treatment through a reduction in the frequency of antihyperglycemic administration could be a valuable weapon in the battle to improve health outcomes and reduce the burden of type 2 diabetes.

  16. Progress of pharmacogenomic studies on anti-diabetic drugs%口服降糖药的药物基因组学研究进展

    Institute of Scientific and Technical Information of China (English)

    王婕; 贾伟平

    2009-01-01

    药物基因组学是研究基因组变异与药物疗效、安全性间关系的学科.本文主要介绍临床常用降糖药的药物基因组学研究进展.%Pharmacogenomics aims to identify the effects of genomie variants on drug efficacy and safety. This article summarized the progress of pharmacogenomic study on anti-diabetic drugs.

  17. Anti-diabetic effects of Caulerpa lentillifera: stimulation of insulin secretion in pancreatic β-cells and enhancement of glucose uptake in adipocytes

    OpenAIRE

    Sharma, Bhesh Raj; Rhyu, Dong Young

    2014-01-01

    Objective: To evaluate anti-diabetic effect of Caulerpa lentillifera (C. lentillifera). Methods: The inhibitory effect of C. lentillifera extract on dipeptidyl peptidase-IV and α-glucosidase enzyme was measured in a cell free system. Then, interleukin-1β and interferon-γ induced cell death and insulin secretion were measured in rat insulinoma (RIN) cells by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay and ELISA kit, respectively. Glucose uptake and glucose transporter...

  18. 口腔微生物生物膜分散物质的研究进展%Progress in study of oral biofilm dispersal-inducing agents

    Institute of Scientific and Technical Information of China (English)

    朱彦; 杨靖梅; 段丁瑜; 徐屹

    2014-01-01

    Communities of bacteria wrapped in self-generated extracellular polymeric matrix and attached to a solid surface are known as biofilm. Biofilm formation and development can be divided into three stages: adhesion of cells to a surface, reproduction of the cells, and dispersion of cells. The procedure, which surface-attached biofilm disperses bacterial cells into the environment to colonize new sites, is defined as biofilm dispersal. Biofilm dispersal is an essential stage of biofilm life cycle. It plays an important role in the transmission of bacteria. For many pathogenic bacteria, biofilm dispersal can transform bacteria in biofilm into planktonic state and promote the spread of infection. The formation of biofilm may increase the resistance of bacteria to antimicrobial agent and host defence response compared with planktonic cells. In the oral cavity, oral microorganism can attach to the surface of oral tissue and prosthesis to form biofilm. Dental caries and periodontal disease are oral chronic infections diseases of the oral tissue. The occurrence of them has a close relationship with biofilm. The mechanism of dispersal is a hot topic in recent years. Some agents which promote dispersal might be a therapeutic potential against biofilm infections. The clinical implication of dispersal agents and potential application are promising. This article reviews the dispersal-inducing agents of oral biofilms.%生物膜是黏附在固体表面,包裹在自身产生的胞外多聚基质中的细菌群体。生物膜的形成和发展包括细菌的黏附、繁殖和分散。附着于某表面的生物膜将其中的细菌释放、分散到周围环境以传播到新的位置形成新的群落即生物膜的分散。生物膜分散是生物膜生长发展周期中一个重要的阶段,起到重要的传播作用。对许多致病菌而言,生物膜的分散能使生物膜的细菌转化为浮游状态,促进感染的扩散。生物膜的形成能提高细菌对抗

  19. The Relation of Changes in Prescribing Patterns of Anti-diabetic Drugs and HbA1c Levels Among Patients with Type 2 Diabetes Mellitus: Systematic Analysis of Studies From the the Past 20 Years in Turkey

    Directory of Open Access Journals (Sweden)

    Hasan İlkova

    2011-12-01

    48.4% to 32.9%. Most of patients (60.5±10.8% included in the analysis were identified to receive ongoing oral anti-diabetic (OAD treatment followed by insulin (17.1%±12.5%, diet (14.3%±14.4% and OAD+insulin (9.2%±10.5%. In conclusion, analysis of a total of 26.898 patients with type 2 DM in the present review revealed a positive change mainly towards a better glycemic control and comparatively lower risk of diabetes-related complication , by means of substantial increase in use of analogue insulin as well as introduction of novel glitazones from 1990-1999 to 2000-2008 in Turkey. Turk Jem 2011; 15: 77-105

  20. Exploratory Characterization of Phenolic Compounds with Demonstrated Anti-Diabetic Activity in Guava Leaves at Different Oxidation States

    Science.gov (United States)

    Díaz-de-Cerio, Elixabet; Verardo, Vito; Gómez-Caravaca, Ana María; Fernández-Gutiérrez, Alberto; Segura-Carretero, Antonio

    2016-01-01

    Psidium guajava L. is widely used like food and in folk medicine all around the world. Many studies have demonstrated that guava leaves have anti-hyperglycemic and anti-hyperlipidemic activities, among others, and that these activities belong mainly to phenolic compounds, although it is known that phenolic composition in guava tree varies throughout seasonal changes. Andalusia is one of the regions in Europe where guava is grown, thus, the aim of this work was to study the phenolic compounds present in Andalusian guava leaves at different oxidation states (low, medium, and high). The phenolic compounds in guava leaves were determined by HPLC-DAD-ESI-QTOF-MS. The results obtained by chromatographic analysis reported that guava leaves with low degree of oxidation had a higher content of flavonols, gallic, and ellagic derivatives compared to the other two guava leaf samples. Contrary, high oxidation state guava leaves reported the highest content of cyanidin-glucoside that was 2.6 and 15 times higher than guava leaves with medium and low oxidation state, respectively. The QTOF platform permitted the determination of several phenolic compounds with anti-diabetic properties and provided new information about guava leaf phenolic composition that could be useful for nutraceutical production. PMID:27187352

  1. Anti-Obesity and Anti-Diabetic Effect of Neoagarooligosaccharides on High-Fat Diet-Induced Obesity in Mice.

    Science.gov (United States)

    Hong, Sun Joo; Lee, Je-Hyeon; Kim, Eun Joo; Yang, Hea Jung; Park, Jae-Seon; Hong, Soon-Kwang

    2017-03-23

    Neoagarooligosaccharides (NAOs), mainly comprising neoagarotetraose and neoagarohexaose, were prepared by hydrolyzing agar with β-agarase DagA from Streptomyces coelicolor, and the anti-obesity and anti-diabetic effects of NAOs on high-fat diet (HFD)-induced obesity in mice were investigated after NAOs-supplementation for 64 days. Compared to the HFD group, the HFD-0.5 group that was fed with HFD + NAOs (0.5%, w/w) showed remarkable reduction of 36% for body weight gain and 37% for food efficiency ratios without abnormal clinical signs. Furthermore, fat accumulation in the liver and development of macrovesicular steatosis induced by HFD in the HFD-0.5 group were recovered nearly to the levels found in the normal diet (ND) group. NAOs intake could also effectively reduce the size (area) of adipocytes and tissue weight gain in the perirenal and epididymal adipose tissues. The increased concentrations of total cholesterol, triglyceride, and free fatty acid in serum of the HFD group were also markedly ameliorated to the levels found in serum of the ND group after NAOs-intake in a dose dependent manner. In addition, insulin resistance and glucose intolerance induced by HFD were distinctly improved, and adiponectin concentration in the blood was notably increased. All these results strongly suggest that intake of NAOs can effectively suppress obesity and obesity-related metabolic syndromes, such as hyperlipidemia, steatosis, insulin resistance, and glucose intolerance, by inducing production of adiponectin in the HFD-induced obese mice.

  2. Isolation and characterization of anti-diabetic component (bioactivity-guided fractionation) fromOcimum sanctum L. (Lamiaceae) aerial part

    Institute of Scientific and Technical Information of China (English)

    Raju Patil; Ravindra Patil; Bharati Ahirwar; Dheeraj Ahirwar

    2011-01-01

    Objective:To isolate and characterize antidiabetic component (bioactivity-guided fractionation) from hydro alcoholic extract ofOcimum sanctum (O. sanctum) aerial part.Methods: Ten fractions(F1 - F10) were isolated from hydro alcoholic extract ofO. sanctum aerial part by column chromatography. All the fractions F1 toF10 were screened for antidiabetic activity in alloxan induced diabetic rats by estimating serum glucose level and lipid parameters. The isolated bioactive component was elucidated on the basis of extensive spectroscopic (UV, IR, MS,1H and 13C NMR) data analysis.Results:The bioactive fraction(F5) was found to be potent antidiabetic by ameliorating glucose and lipid parameters (total cholesterol, triglycerides, low and high density lipoprotein cholesterol). The extensive spectroscopic data analysis reveals that, the isolated bioactive compound elucidated as tetracyclic triterpenoid [16-Hydroxy-4,4,10,13-tetramethyl-17-(4-methyl-pentyl)-hexadecahydro-cyclopenta[a]phenanthren-3-one]. Conclusions:Our present study concluded that, tetracyclic triterpenoid isolated from aerial part ofO. sanctum has a great anti-diabetic potential.

  3. Biotransformation of Momordica charantia fresh juice by Lactobacillus plantarum BET003 and its putative anti-diabetic potential

    Science.gov (United States)

    Mazlan, Farhaneen Afzal; Annuar, M. Suffian M.

    2015-01-01

    Lactobacillus plantarum BET003 isolated from Momordica charantia fruit was used to ferment its juice. Momordica charantia fresh juice was able to support good growth of the lactic acid bacterium. High growth rate and cell viability were obtained without further nutrient supplementation. In stirred tank reactor batch fermentation, agitation rate showed significant effect on specific growth rate of the bacterium in the fruit juice. After the fermentation, initially abundant momordicoside 23-O-β-Allopyranosyle-cucurbita-5,24-dien-7α,3β,22(R),23(S)-tetraol-3-O-β-allopyranoside was transformed into its corresponding aglycone in addition to the emergence of new metabolites. The fermented M. charantia juice consistently reduced glucose production by 27.2%, 14.5%, 17.1% and 19.2% at 15-minute intervals respectively, when compared against the negative control. This putative anti-diabetic activity can be attributed to the increase in availability and concentration of aglycones as well as other phenolic compounds resulting from degradation of glycosidic momordicoside. Biotransformation of M. charantia fruit juice via lactic acid bacterium fermentation reduced its bitterness, reduced its sugar content, produced aglycones and other metabolites as well as improved its inhibition of α-glucosidase activity compared with the fresh, non-fermented juice. PMID:26539336

  4. Anti-diabetes drug pioglitazone ameliorates synaptic defects in AD transgenic mice by inhibiting cyclin-dependent kinase5 activity.

    Directory of Open Access Journals (Sweden)

    Jinan Chen

    Full Text Available Cyclin-dependent kinase 5 (Cdk5 is a serine/threonine kinase that is activated by the neuron specific activators p35/p39 and plays many important roles in neuronal development. However, aberrant activation of Cdk5 is believed to be associated with the pathogenesis of several neurodegenerative diseases, including Alzheimer's disease (AD and Parkinson's disease (PD. Here in the present study, enhanced Cdk5 activity was observed in mouse models of AD; whereas soluble amyloid-β oligomers (Aβ, which contribute to synaptic failures during AD pathogenesis, induced Cdk5 hyperactivation in cultured hippocampal neurons. Inhibition of Cdk5 activity by pharmacological or genetic approaches reversed dendritic spine loss caused by soluble amyloid-β oligomers (Aβ treatment. Interestingly, we found that the anti-diabetes drug pioglitazone could inhibit Cdk5 activity by decreasing p35 protein level. More importantly, pioglitazone treatment corrected long-term potentiation (LTP deficit caused by Aβ exposure in cultured slices and pioglitazone administration rescued impaired LTP and spatial memory in AD mouse models. Taken together, our study describes an unanticipated role of pioglitazone in alleviating AD and reveals a potential therapeutic drug for AD curing.

  5. Production and anti-diabetic activity of soluble dietary fiber from apricot pulp by Trichoderma viride fermentation.

    Science.gov (United States)

    Cui, Jie; Gu, Xin; Zhang, Qiaohui; Ou, Yangjie; Wang, Jianzhong

    2015-05-01

    Soluble dietary fiber (SDF) was prepared by Trichoderma viride fermentation by using apricot pulp as the raw material. A four-factor and three-level response surface methodology was applied to optimize the fermentation conditions affecting the extraction rate of SDF. The optimum fermentation conditions were listed: crude enzyme volume, 9.59 mL g(-1); fermentation temperature, 43 °C; initial pH, 5.36; fermentation time, 6.47 h. Under these conditions, 15.69% yield was obtained and its relative error with the predicted theoretical value (15.87%) was 1.14%. The dietary fiber content of SDF was 84.0% whereas it was found to be 43.1% in apricot pulp flour. The anti-diabetic effect of apricot pulp SDF on rat models of diabetes was investigated. Both the blood glucose level and body weight were significantly changed in apricot pulp SDF-treated groups compared with the diabetic group (p pulp SDF relieved the symptoms of diabetic rats.

  6. Exploratory Characterization of Phenolic Compounds with Demonstrated Anti-Diabetic Activity in Guava Leaves at Different Oxidation States.

    Science.gov (United States)

    Díaz-de-Cerio, Elixabet; Verardo, Vito; Gómez-Caravaca, Ana María; Fernández-Gutiérrez, Alberto; Segura-Carretero, Antonio

    2016-05-11

    Psidium guajava L. is widely used like food and in folk medicine all around the world. Many studies have demonstrated that guava leaves have anti-hyperglycemic and anti-hyperlipidemic activities, among others, and that these activities belong mainly to phenolic compounds, although it is known that phenolic composition in guava tree varies throughout seasonal changes. Andalusia is one of the regions in Europe where guava is grown, thus, the aim of this work was to study the phenolic compounds present in Andalusian guava leaves at different oxidation states (low, medium, and high). The phenolic compounds in guava leaves were determined by HPLC-DAD-ESI-QTOF-MS. The results obtained by chromatographic analysis reported that guava leaves with low degree of oxidation had a higher content of flavonols, gallic, and ellagic derivatives compared to the other two guava leaf samples. Contrary, high oxidation state guava leaves reported the highest content of cyanidin-glucoside that was 2.6 and 15 times higher than guava leaves with medium and low oxidation state, respectively. The QTOF platform permitted the determination of several phenolic compounds with anti-diabetic properties and provided new information about guava leaf phenolic composition that could be useful for nutraceutical production.

  7. Accelerator-based analytical technique in the study of some anti-diabetic medicinal plants of Nigeria

    Science.gov (United States)

    Olabanji, S. O.; Omobuwajo, O. R.; Ceccato, D.; Adebajo, A. C.; Buoso, M. C.; Moschini, G.

    2008-05-01

    Diabetes mellitus, a clinical syndrome characterized by hyperglycemia due to deficiency of insulin, is a disease involving the endocrine pancreas and causes considerable morbidity and mortality in the world. In Nigeria, many plants, especially those implicated in herbal recipes for the treatment of diabetes, have not been screened for their elemental constituents while information on phytochemistry of some of them is not available. There is therefore the need to document these constituents as some of these plants are becoming increasingly important as herbal drugs or food additives. The accelerator-based technique PIXE, using the 1.8 MeV collimated proton beam from the 2.5 MV AN 2000 Van de Graaff accelerator at INFN, LNL, Legnaro (Padova) Italy, was employed in the determination of the elemental constituents of these anti-diabetic medicinal plants. Leaves of Gardenia ternifolia, Caesalpina pulcherrima, Solemostenon monostachys, whole plant of Momordica charantia and leaf and stem bark of Hunteria umbellata could be taken as vegetables, neutraceuticals, food additives and supplements in the management of diabetes. However, Hexabolus monopetalus root should be used under prescription.

  8. Accelerator-based analytical technique in the study of some anti-diabetic medicinal plants of Nigeria

    Energy Technology Data Exchange (ETDEWEB)

    Olabanji, S.O. [Istituto Nazionale di Fisica Nucleare (INFN), Laboratori Nazionali di Legnaro (LNL), I-35020 Legnaro, Padova (Italy)], E-mail: skayode2002@yahoo.co.uk; Omobuwajo, O.R. [Department of Pharmacognosy, Obafemi Awolowo University, Ile-Ife (Nigeria); Ceccato, D. [Istituto Nazionale di Fisica Nucleare (INFN), Laboratori Nazionali di Legnaro (LNL), I-35020 Legnaro, Padova (Italy); Dipartmento di Fisica, Universita di Padova, Padova (Italy); Adebajo, A.C. [Department of Pharmacognosy, Obafemi Awolowo University, Ile-Ife (Nigeria); Buoso, M.C. [Istituto Nazionale di Fisica Nucleare (INFN), Laboratori Nazionali di Legnaro (LNL), I-35020 Legnaro, Padova (Italy); Moschini, G. [Istituto Nazionale di Fisica Nucleare (INFN), Laboratori Nazionali di Legnaro (LNL), I-35020 Legnaro, Padova (Italy); Dipartmento di Fisica, Universita di Padova, Padova (Italy)

    2008-05-15

    Diabetes mellitus, a clinical syndrome characterized by hyperglycemia due to deficiency of insulin, is a disease involving the endocrine pancreas and causes considerable morbidity and mortality in the world. In Nigeria, many plants, especially those implicated in herbal recipes for the treatment of diabetes, have not been screened for their elemental constituents while information on phytochemistry of some of them is not available. There is therefore the need to document these constituents as some of these plants are becoming increasingly important as herbal drugs or food additives. The accelerator-based technique PIXE, using the 1.8 MeV collimated proton beam from the 2.5 MV AN 2000 Van de Graaff accelerator at INFN, LNL, Legnaro (Padova) Italy, was employed in the determination of the elemental constituents of these anti-diabetic medicinal plants. Leaves of Gardenia ternifolia, Caesalpina pulcherrima, Solemostenon monostachys, whole plant of Momordica charantia and leaf and stem bark of Hunteria umbellata could be taken as vegetables, neutraceuticals, food additives and supplements in the management of diabetes. However, Hexabolus monopetalus root should be used under prescription.

  9. Exploratory Characterization of Phenolic Compounds with Demonstrated Anti-Diabetic Activity in Guava Leaves at Different Oxidation States

    Directory of Open Access Journals (Sweden)

    Elixabet Díaz-de-Cerio

    2016-05-01

    Full Text Available Psidium guajava L. is widely used like food and in folk medicine all around the world. Many studies have demonstrated that guava leaves have anti-hyperglycemic and anti-hyperlipidemic activities, among others, and that these activities belong mainly to phenolic compounds, although it is known that phenolic composition in guava tree varies throughout seasonal changes. Andalusia is one of the regions in Europe where guava is grown, thus, the aim of this work was to study the phenolic compounds present in Andalusian guava leaves at different oxidation states (low, medium, and high. The phenolic compounds in guava leaves were determined by HPLC-DAD-ESI-QTOF-MS. The results obtained by chromatographic analysis reported that guava leaves with low degree of oxidation had a higher content of flavonols, gallic, and ellagic derivatives compared to the other two guava leaf samples. Contrary, high oxidation state guava leaves reported the highest content of cyanidin-glucoside that was 2.6 and 15 times higher than guava leaves with medium and low oxidation state, respectively. The QTOF platform permitted the determination of several phenolic compounds with anti-diabetic properties and provided new information about guava leaf phenolic composition that could be useful for nutraceutical production.

  10. The anti-diabetic drug metformin reduces BACE1 protein level by interfering with the MID1 complex.

    Directory of Open Access Journals (Sweden)

    Moritz M Hettich

    Full Text Available Alzheimer's disease (AD, the most common form of dementia in the elderly, is characterized by two neuropathological hallmarks: senile plaques, which are composed of Aβ peptides, and neurofibrillary tangles, which are composed of hyperphosphorylated TAU protein. Diabetic patients with dysregulated insulin signalling are at increased risk of developing AD. Further, several animal models of diabetes show increased Aβ expression and hyperphosphorylated tau. As we have shown recently, the anti-diabetic drug metformin is capable of dephosphorylating tau at AD-relevant phospho-sites. Here, we investigated the effect of metformin on the main amyloidogenic enzyme BACE1 and, thus, on the production of Aβ peptides, the second pathological hallmark of AD. We find similar results in cultures of primary neurons, a human cell line model of AD and in vivo in mice. We show that treatment with metformin decreases BACE1 protein expression by interfering with an mRNA-protein complex that contains the ubiquitin ligase MID1, thereby reducing BACE1 activity. Together with our previous findings these results indicate that metformin may target both pathological hallmarks of AD and may be of therapeutic value for treating and/or preventing AD.

  11. Anti-diabetic activity of Zingiber officinale in streptozotocin-induced type I diabetic rats.

    Science.gov (United States)

    Akhani, Sanjay P; Vishwakarma, Santosh L; Goyal, Ramesh K

    2004-01-01

    The fresh and dried rhizome of Zingiber officinale Roscoe (commonly known as ginger) is widely used in traditional medicine. We have studied the effect of the juice of Z. officinale (4 mL kg(-1), p.o. daily) for 6 weeks on streptozotocin (STZ)-induced type I diabetic rats with particular reference to the involvement of serotonin (5-hydroxytryptamine; 5-HT) receptors in glycaemic control. In normoglycaemic rats, 5-HT (1mg kg(-1), i.p.) produced hyperglycaemia and hypoinsulinaemia, which was significantly prevented by the juice of Z. officinale. STZ-diabetes produced a significant increase in fasting glucose levels that was associated with a significant decrease in serum insulin levels. Treatment with Z. officinale produced a significant increase in insulin levels and a decrease in fasting glucose levels in diabetic rats. In an oral glucose tolerance test, treatment with Z. officinale was found to decrease significantly the area under the curve of glucose and to increase the area under the curve of insulin in STZ-diabetic rats. Treatment with Z. officinale also caused a decrease in serum cholesterol, serum triglyceride and blood pressure in diabetic rats. Our data suggest a potential antidiabetic activity of the juice of Z. officinale in type I diabetic rats, possibly involving 5-HT receptors.

  12. Anti-diabetic activity of insulin-degrading enzyme inhibitors mediated by multiple hormones.

    Science.gov (United States)

    Maianti, Juan Pablo; McFedries, Amanda; Foda, Zachariah H; Kleiner, Ralph E; Du, Xiu Quan; Leissring, Malcolm A; Tang, Wei-Jen; Charron, Maureen J; Seeliger, Markus A; Saghatelian, Alan; Liu, David R

    2014-07-03

    Despite decades of speculation that inhibiting endogenous insulin degradation might treat type-2 diabetes, and the identification of IDE (insulin-degrading enzyme) as a diabetes susceptibility gene, the relationship between the activity of the zinc metalloprotein IDE and glucose homeostasis remains unclear. Although Ide(-/-) mice have elevated insulin levels, they exhibit impaired, rather than improved, glucose tolerance that may arise from compensatory insulin signalling dysfunction. IDE inhibitors that are active in vivo are therefore needed to elucidate IDE's physiological roles and to determine its potential to serve as a target for the treatment of diabetes. Here we report the discovery of a physiologically active IDE inhibitor identified from a DNA-templated macrocycle library. An X-ray structure of the macrocycle bound to IDE reveals that it engages a binding pocket away from the catalytic site, which explains its remarkable selectivity. Treatment of lean and obese mice with this inhibitor shows that IDE regulates the abundance and signalling of glucagon and amylin, in addition to that of insulin. Under physiological conditions that augment insulin and amylin levels, such as oral glucose administration, acute IDE inhibition leads to substantially improved glucose tolerance and slower gastric emptying. These findings demonstrate the feasibility of modulating IDE activity as a new therapeutic strategy to treat type-2 diabetes and expand our understanding of the roles of IDE in glucose and hormone regulation.

  13. Identification of cancer specific ligands from one-bead one compound combinatorial libraries to develop theranostics agents against oral squamous cell carcinoma

    Science.gov (United States)

    Yang, Frances Fan

    Background: Oral squamous cell carcinoma (OSCC) is one of the most prevalent disease worldwide. One-bead one-compound (OBOC) combinatorial technology is a powerful method to identify peptidomimetic ligands against a variety of receptors on cell surfaces. We therefore hypothesized that cancer specific ligands against OSCC might be identified and can be conjugated to optical dyes or nanocarriers to develop theranostic agents against OSCC. Material and methods: Different OSCC cell lines were incubated with OBOC libraries and beads with cell binding were sorted and then screened with normal human cells to identify peptide-beads binding to different OSCC cell lines but not binding to normal human cells. The molecular probes of OSCC were developed by biotinylating the carboxyl end of the ligands. OSCC theranostic agents were developed by decorating LLY13 with NPs and evaluated by using orthotopic bioluminescent oral cancer model. Results: Six OSCC specific ligands were discovered. Initial peptide-histochemistry study indicated that LLY12 and LLY13 were able to specifically detect OSCC cells grown on chamber slides at the concentration of 1 muM. In addition, LLY13 was found to penetrate into the OSCC cells and accumulate in the cytoplasm, and nucleus. After screened with a panel of integrin antibodies, only anti-alpha3 antibody was able to block most of OSCC cells binding to the LLY13 beads. OSCC theranostic agents developed using targeting LLY13 micelles (25+/- 4nm in diameter) were more efficient in binding to HSC-3 cancer cells compared to non-targeting micelles. Ex vivo images demonstrated that xenografts from the mice with targeting micelles appeared to have higher signals than the non-targeting groups. Conclusion: LLY13 has promising in vitro and in vivo targeting activity against OSCC. In addition, LLY13 is also able to penetrate into cancer cells via endocytosis. Initial study indicated that alpha3 integrin might partially be the corresponding receptor involved

  14. Evaluation of the anti-diabetic properties ofMucuna pruriensseed extract

    Institute of Scientific and Technical Information of China (English)

    Stephen O Majekodunmi; Ademola A Oyagbemi; Solomon Umukoro; Oluwatoyin A Odeku

    2011-01-01

    Objective:To explore the antidiabetic properties ofMucuna pruriens(M. pruriens).Methods:Diabetes was induced in Wistar rats by single intravenous injection of120 mg/kg of alloxan monohydrate and different doses of the extract were administered to diabetic rats. The blood glucose level was determined using a glucometer and results were compared with normal and untreated diabetic rats. The acute toxicity was also determined in albino mice.Results:Results showed that the administration of5, 10, 20, 30, 40, 50, and100 mg/kg of the crude ethanolic extract ofM. pruriens seeds to alloxan-induced diabetic rats (plasma glucose> 450mg/dL) resulted in18.6%, 24.9%, 30.8%, 41.4%, 49.7%, 53.1% and 55.4% reduction, respectively in blood glucose level of the diabetic rats after 8h of treatment while the administration of glibenclamide (5mg/kg/day) resulted in59.7% reduction. Chronic administration of the extract resulted in a significant dose dependent reduction in the blood glucose level (P<0.001). It also showed that the antidiabetic activity ofM. pruriens seeds resides in the methanolic and ethanolic fractions of the extract. Acute toxicity studies indicated that the extract was relatively safe at low doses, although some adverse reactions were observed at higher doses (8-32 mg/kg body weight), no death was recorded. Furthermore, oral administration ofM. pruriens seed extract also significantly reduced the weight loss associated with diabetes.Conclusions: The study clearly supports the traditional use ofM. pruriens for the treatment of diabetes and indicates that the plant could be a good source of potent antidiabetic drug.

  15. Analysis of Oral Hypoglycemic Agents Used in Our Hospital during 2008-2010%我院2008-2010年口服降糖药的用药分析

    Institute of Scientific and Technical Information of China (English)

    朱寅

    2011-01-01

    目的 了解医院口服降糖药的使用情况,促进合理用药.方法 对重庆医科大学附属第二医院2008年至2010年口服降糖药的应用频率、消耗金额进行统计分析.结果 该院口服降糖药的消耗金额逐年增长,其中二甲双胍增幅较大;临床最常用的口服降糖药是二甲双胍、阿卡波糖和格列吡嗪.结论 医院口服降糖药的使用呈增长趋势.%Objective To evaluate the application status of oral hypoglycemic agents used in the hospital for promoting rational drug use.Methods The frequency and sum of money in consumption of oral hypoglycemic agents during 2008 - 2010 were statistically analyzed.Results The sum of money in consumption of oral hypoglycemic agents in the hospital was increased year by year, in which, the increment of metformin was maximum. The commonest used oral hypoglycemic agents in clinic were metformin, glipizide and pioglipazong. Conclusion The use of oral hypoglycemic agents presents the increasing trend.

  16. Experimental and Clinical Evaluation of Plantago australis Extract as an Anti-Inflammatory Agent to Treat Oral Pathologies

    Directory of Open Access Journals (Sweden)

    Flores

    2016-09-01

    Full Text Available Background Plantago australis is a native plant from Southern Brazil used to reduce inflammation. Interestingly, there are no previous studies evaluating its use to treat oral lesions. Objectives The study aimed to investigate in vivo the anti-inflammatory activity of 10% ethanol extract of P. australis in recurrent aphthous stomatitis (RAS, erosive lichen planus (ELP and actinic cheilitis (AC. Methods Thirty patients with RAS, ELP and AC were treated topically with 10% P. australis solution-based or cream. Results In the comparison of in vivo data before and after the treatment and between different lesions, all P values were less than 0.05. Conclusions The pharmaceutical formulation of 10% P. australis was therapeutically effective in the subjects with inflammatory oral lesions of RAS, ELP and AC.

  17. [Bacteriological study of oral cavity of people of Mexican origin to determine etiology agents of human infections in hand bite].

    Science.gov (United States)

    Cañedo-Guzmán, Cristhyan Baruch; Espinosa-Gutiérrez, Alejandro; Guzmán-Murillo, María Antonia

    2013-01-01

    Hand infections secondary to human bites often leave serious consequences on the functioning of the hand. Such infections are caused by different bacteria. Most bacteriological studies have been made to people of Anglo-Saxon origin or descent, and based on these findings; provide treatment to patients of different origins which may not always be as effective. Descriptive, internal stratified 17 patients were isolated samples of oral cavity and dental plaque bacterial species to identify and define the possible treatment according to the species identified. Microorganisms were isolated Gram (+) and Gram (-) belonging to the normal flora of the oral cavity and dental plaque in all the cases studied, presenting a variable number of microorganisms according to age but not by sex. The group of Gram-positive bacteria isolated showed sensitivity to: erythromycin, chloramphenicol and ciprofloxacin. In the group of Gram negative: kanamycin, amoxicillin + clavulanic acid, ciprofloxacin and norfloxacin, E. Corrodens sensitive to the group of quinolones as ciprofloxacin, norfloxacin as well as ceftriaxone and cefoperazone sulbactam. The bacterial species that are commonly found in normal flora of the oral cavity and dental plaque may be potential pathogens in a hand injury where to find the appropriate conditions for their development.

  18. An oral recombinant vaccine in dogs against Echinococcus granulosus, the causative agent of human hydatid disease: a pilot study.

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    Anne-Francoise Petavy

    Full Text Available Dogs are the main source of human cystic echinococcosis. An oral vaccine would be an important contribution to control programs in endemic countries. We conducted two parallel experimental trials in Morocco and Tunisia of a new oral vaccine candidate against Echinococcus granulosus in 28 dogs. The vaccine was prepared using two recombinant proteins from adult worms, a tropomyosin (EgTrp and a fibrillar protein similar to paramyosin (EgA31, cloned and expressed in a live attenuated strain of Salmonella enterica serovar typhimurium.In each country, five dogs were vaccinated with the associated EgA31 and EgTrp; three dogs received only the vector Salmonella; and six dogs were used as different controls. The vaccinated dogs received two oral doses of the vaccine 21 d apart, and were challenged 20 d later with 75,000 living protoscoleces. The controls were challenged under the same conditions. All dogs were sacrificed 26-29 d postchallenge, before the appearance of eggs, for safety reasons.We studied the histological responses to both the vaccine and control at the level of the duodenum, the natural localization of the cestode. Here we show a significant decrease of parasite burden in vaccinated dogs (70% to 80% and a slower development rate in all remaining worms. The Salmonella vaccine EgA31-EgTrp demonstrated a high efficacy against E. granulosus promoting its potential role in reducing transmission to humans and animals.

  19. Anti-diabetic and hypolipidemic effects of Sargassum yezoense in db/db mice.

    Science.gov (United States)

    Kim, Su-Nam; Lee, Woojung; Bae, Gyu-Un; Kim, Yong Kee

    2012-08-10

    Peroxisome proliferator-activated receptors (PPARs) have been considered to be desirable targets for metabolic syndrome, even though their specific agonists have several side effects including body weight gain, edema and tissue failure. Previously, we have reported in vitro effects of Sargassum yezoense (SY) and its ingredients, sargaquinoic acid (SQA) and sargahydroquinoic acid (SHQA), on PPARα/γ dual transcriptional activation. In this study, we describe in vivo pharmacological property of SY on metabolic disorders. SY treatment significantly improved glucose and lipid impairment in db/db mice model. More importantly, there are no significant side effects such as body weight gain and hepatomegaly in SY-treated animals, indicating little side effects of SY in liver and lipid metabolism. In addition, SY led to a decrease in the expression of G6Pase for gluconeogenesis in liver responsible for lowering blood glucose level and an increase in the expression of UCP3 in adipose tissue for the reduction of total and LDL-cholesterol level. Altogether, our data suggest that SY would be a potential therapeutic agent against type 2 diabetes and related metabolic disorders by ameliorating the glucose and lipid metabolism.

  20. A study on anti-diabetic and anti-hypertension herbs used in Lorestan province, Iran

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    Delfan Bahram

    2014-04-01

    Full Text Available Introduction: Diabetes and hypertension are amongst the most prevalent diseases in the world, while they can be controlled and prevented, create many problems and complications for affected patients. This study was aimed to identify and report the most important and effective herbs for diabetes and high blood pressure treatment in Lorestan province (West of Iran. Methods: By gathering and integrating indigenous data from local inhabitants of Lorestan, Iran, the goal of this study was accomplished. Data were gathered by cooperation of the agents of public health services network all over the towns of Dorud, Boroujerd, Khorramabad, Aleshtar, Poledokhtar, Aligoodarz, Nurabad and Kouhdasht. Results: Results of this study showed that there were overall 17 medicinal plants which were used for treatment and controlling of diabetes and high blood pressure. Conclusion: Medicinal plants reported in this study are indigenous to the Lorestan province. Some of the foresaid herbs seem to have some unknown therapeutic effects which are reported in this study for the first time, and some others have various known therapeutic effects mentioned in other similar studies. It is essential for researchers to find out the actuality of clinical effectiveness of the herbs and their active substances. Once the positive effects of these herbs proved, it would be possible to produce drugs which are useful in curing and controlling diabetes and hypertension.

  1. In-hospital mortality after pre-treatment with antiplatelet agents or oral anticoagulants and hematoma evacuation of intracerebral hematomas.

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    Stein, Marco; Misselwitz, Björn; Hamann, Gerhard F; Kolodziej, Malgorzata; Reinges, Marcus H T; Uhl, Eberhard

    2016-04-01

    Pre-treatment with antiplatelet agents is described to be a risk factor for mortality after spontaneous intracerebral hemorrhage (ICH). However, the impact of antithrombotic agents on mortality in patients who undergo hematoma evacuation compared to conservatively treated patients with ICH remains controversial. This analysis is based on a prospective registry for quality assurance in stroke care in the State of Hesse, Germany. Patients' data were collected between January 2008 and December 2012. Only patients with the diagnosis of spontaneous ICH were included (International Classification of Diseases 10th Revision codes I61.0-I61.9). Predictors of in-hospital mortality were determined by univariate analysis. Predictors with Panticoagulants or antiplatelet agents was documented in 16.3% and 25.1%, respectively. Overall in-hospital mortality was 23.2%. In-hospital mortality was decreased in operatively treated patients compared to conservatively treated patients (11.6% versus 24.0%; Pantiplatelet pre-treatment had a significantly higher risk of death during the hospital stay after hematoma evacuation (odds ratio [OR]: 2.5; 95% confidence interval [CI]: 1.24-4.97; P=0.010) compared to patients without antiplatelet pre-treatment treatment (OR: 0.9; 95% CI: 0.79-1.09; P=0.376). In conclusion a higher rate of in-hospital mortality after pre-treatment with antiplatelet agents in combination with hematoma evacuation after spontaneous ICH was observed in the presented cohort.

  2. Anti-diabetic and hypolipidemic effects of Sargassum yezoense in db/db mice

    Energy Technology Data Exchange (ETDEWEB)

    Kim, Su-Nam, E-mail: snkim@kist.re.kr [Natural Medicine Center, KIST Gangneung Institute, Gangneung 210-340 (Korea, Republic of); Lee, Woojung [Natural Medicine Center, KIST Gangneung Institute, Gangneung 210-340 (Korea, Republic of); Bae, Gyu-Un [College of Pharmacy, Sookmyung Women' s University, Seoul 140-742 (Korea, Republic of); Research Center for Cell Fate Control, Sookmyung Women' s University, Seoul 140-742 (Korea, Republic of); Kim, Yong Kee, E-mail: yksnbk@sookmyung.ac.kr [College of Pharmacy, Sookmyung Women' s University, Seoul 140-742 (Korea, Republic of)

    2012-08-10

    Highlights: Black-Right-Pointing-Pointer Sargassum yezoense (SY) treatment improved glucose and lipid impairment in vivo. Black-Right-Pointing-Pointer This pharmacological action is associated with PPAR{alpha}/{gamma} dual activation. Black-Right-Pointing-Pointer It decreases the expression of G6Pase for gluconeogenesis in liver. Black-Right-Pointing-Pointer It increases the expression of UCP3 for lipid metabolism in adipose tissue. Black-Right-Pointing-Pointer There are no significant side effects such as body weight gain and hepatomegaly. -- Abstract: Peroxisome proliferator-activated receptors (PPARs) have been considered to be desirable targets for metabolic syndrome, even though their specific agonists have several side effects including body weight gain, edema and tissue failure. Previously, we have reported in vitro effects of Sargassum yezoense (SY) and its ingredients, sargaquinoic acid (SQA) and sargahydroquinoic acid (SHQA), on PPAR{alpha}/{gamma} dual transcriptional activation. In this study, we describe in vivo pharmacological property of SY on metabolic disorders. SY treatment significantly improved glucose and lipid impairment in db/db mice model. More importantly, there are no significant side effects such as body weight gain and hepatomegaly in SY-treated animals, indicating little side effects of SY in liver and lipid metabolism. In addition, SY led to a decrease in the expression of G6Pase for gluconeogenesis in liver responsible for lowering blood glucose level and an increase in the expression of UCP3 in adipose tissue for the reduction of total and LDL-cholesterol level. Altogether, our data suggest that SY would be a potential therapeutic agent against type 2 diabetes and related metabolic disorders by ameliorating the glucose and lipid metabolism.

  3. Comparative evaluation of the anti-diabetic activity of Pterocarpus marsupium Roxb. heartwood in alloxan induced diabetic rats using extracts obtained by optimized conventional and non conventional extraction methods.

    Science.gov (United States)

    Devgan, Manish; Nanda, Arun; Ansari, Shahid Husain

    2013-09-01

    The aim of the present study was to assess the anti-diabetic activity of Pterocarpus marsupium Roxb. heartwood in alloxan induced diabetic rats using extracts obtained by optimized conventional and non conventional extraction methods. Aqueous and ethanol extracts of Pterocarpus marsupium heartwood were prepared by conventional methods (infusion, decoction, maceration and percolation) and non conventional methods, such as ultrasound-assisted extraction (UAE) and microwave-assisted extraction (MAE). The crude aqueous extracts were administered orally to both normal and alloxan induced male albino rats (Sprague-Dawley strain). The experimental set up consisted of 48 male albino rats divided into 6 groups: Normal control, diabetic control (sterile normal saline, 1 ml/100 g body weight), standard (gliclazide, 25 mg/1000g of body weight), groups 4-6 (crude aqueous percolation, optimized UAE and MAE extract, 250 mg/1000g of body weight). In acute treatment, the reduction of blood glucose level was statistically significant with the oral administration of UAE and percolation aqueous extracts to the hyperglycemic rats. In sub-acute treatment, the UAE aqueous extract led to consistent and statistically significant (p<0.001) reduction in the blood glucose levels. There was no abnormal change in body weight of the hyperglycemic animals after 10 days of administration of plant extracts and gliclazide. This study justifies the traditional claim and provides a rationale for the use of Pterocarpus marsupium to treat diabetes mellitus. The antidiabetic activity of Pterocarpus marsupium can be enhanced by extracting the heartwood by non conventional method of UAE.

  4. Herpes simplex virus keratitis: an update of the pathogenesis and current treatment with oral and topical antiviral agents.

    Science.gov (United States)

    Tsatsos, Michael; MacGregor, Cheryl; Athanasiadis, Ioannis; Moschos, Marilita M; Hossain, Parwez; Anderson, David

    2016-12-01

    Ophthalmic herpes simplex viral keratitis is responsible for a range of ocular manifestations from superficial epithelial disease to stromal keratitis and endotheliitis. The Herpetic Eye Disease Study has guided the management of herpetic eye disease for almost twenty years, but newer medications such as valacyclovir are now available and are considered to have better bioavailability than acyclovir. In this review, we examine the existing evidence on the pathogenesis of different ophthalmic herpes simplex viral keratitis disease modalities and the role of oral and topically administered antiviral drugs in the treatment of herpes simplex viral keratitis.

  5. Yhhu4488, a novel GPR40 agonist, promotes GLP-1 secretion and exerts anti-diabetic effect in rodent models.

    Science.gov (United States)

    Guo, Dan-yang; Li, De-wen; Ning, Meng-meng; Dang, Xiang-yu; Zhang, Li-na; Zeng, Li-min; Hu, You-hong; Leng, Ying

    2015-10-30

    G protein-coupled receptor 40 (GPR40) is predominantly expressed in pancreatic β-cells and activated by long-chain fatty acids. GPR40 has drawn considerable interest as a potential therapeutic target for type 2 diabetes mellitus (T2DM) due to its important role in enhancing glucose-stimulated insulin secretion (GSIS). Encouragingly, GPR40 is also proven to be highly expressed in glucagon-like peptide-1 (GLP-1)-producing enteroendocrine cells afterwards, which opens a potential role of GPR40 in enhancing GLP-1 secretion to exert additional anti-diabetic efficacy. In the present study, we discovered a novel GPR40 agonist, yhhu4488, which is structurally different from other reported GPR40 agonists. Yhhu4488 showed potent agonist activity with EC50 of 49.96 nM, 70.83 nM and 58.68 nM in HEK293 cells stably expressing human, rat and mouse GPR40, respectively. Yhhu4488 stimulated GLP-1 secretion from fetal rat intestinal cells (FRIC) via triggering endogenous calcium store mobilization and extracellular calcium influx. The effect of yhhu4488 on GLP-1 secretion was further confirmed in type 2 diabetic db/db mice. Yhhu4488 exhibited satisfactory potency in in vivo studies. Single administration of yhhu4488 improved glucose tolerance in SD rats. Chronic administration of yhhu4488 effectively decreased fasting blood glucose level, improved β-cell function and lipid homeostasis in type 2 diabetic ob/ob mice. Taken together, yhhu4488 is a novel GPR40 agonist that enhances GLP-1 secretion, improves metabolic control and β-cell function, suggesting its promising potential for the treatment of type 2 diabetes.

  6. In vitro anti-diabetic, anti-obesity and antioxidant proprieties of Juniperus phoenicea L. leaves from Tunisia

    Institute of Scientific and Technical Information of China (English)

    2014-01-01

    Objective: To examine chemical composition and antioxidant activity as well as the in vitroα-amylase and pancreatic lipase inhibitory activities of the essential oil and various extracts of Juniperus phoenicea (J. phoenicea). Methods: Essential oil obtained by steam distillation were analyzed by gas chromatography-mass spectrometry technique. The antioxidant activity of the essential oil and various extracts of J. phoenicea were determined by DPPH andβ-carotene bleaching methods. Results: Gas chromatography-mass spectrometry analysis of the J. phoenicea essential oil resulted in the identification of 37 compounds, representing 96.98% of the oil; α-Pinene (24.02%), limonene (7.94%), D-3-Carene (16.9%), Germacrene D (11.98%), Germacrene B (5.40%) and δ-cadinene (6.52%) were the major compounds. The IC50 values of essential oil, hexane and methanol extracts against α-amylase were 35.44, 30.15 and 53.76 µg/mL respectively, and those against pancreatic lipase were 66.15, 68.47 and 60.22 µg/mL respectively, suggesting powerful anti-diabetic and anti-obesity effects. Antioxidant activity (IC50=2 µg/mL) and total phenolics content (265 mg as gallic acid equivalent/g extract) of the methanol extract were found to be the highest compared to the other extracts. Conclusions:The findings showed that the extents ofα-amylase and pancreatic lipase inhibitory activities of the J. phoenicea extracts as well as their antioxidant activity are in accordance with total phenolics contents. Leaves of J. phoenicea being rich in phenolics may provide a good source of natural products with interesting medicinal properties.

  7. Establishment of liver specific glucokinase gene knockout mice:a new animal model for screening anti-diabetic drugs

    Institute of Scientific and Technical Information of China (English)

    Ya-li ZHANG; Xiao-hong TAN; Mei-fang XIAO; Hui LI; Yi-qing Mao; Xiao YANG; Huan-ran TAN

    2004-01-01

    AIM: To characterize the liver-specific role of glucokinase in maintaining glucose homeostasis and to create an animal model for diabetes. METHODS: We performed hepatocyte-specific gene knockout of glucokinase in mice using Cre-loxP gene targeting strategy. First, two directly repeated loxP sequences were inserted to flank the exon 9 and exon 10 of glucokinase in genomic DNA. To achieve this, linearized targeting vector was electroporated into ES cells. Then G418- and Gancyclovir-double-resistant clones were picked and screened by PCR analysis and the positives identified by PCR were confirmed by Southern blot. A targeted clone was selected for microinjection into C57BL/6J blastocysts and implanted into pseudopregnant FVB recipient. Chimeric mice and their offspring were analyzed by Southern blot. Then by intercrossing the Alb-Cre transgenic mice with mice containing a conditional gk allele, we obtained mice with liver-specific glucokinase gene knockout. RESULTS: Among 161 double resistant clones 4 were positive to PCR and Southern blot and only one was used for further experiments. Eventually we generated the liver specific glucokinase knockout mice. These mice showed increased glucose level with age and at the age of 6 weeks fasting blood glucose level was significantly higher than control and they also displayed impaired glucose tolerance. CONCLUSION: Our studies indicate that hepatic glucokinase plays an important role in glucose homeostasis and its deficiencies contribute to the development of diabetes. The liver glucokinase knockout mouse is an ideal animal model for MODY2, and it also can be applied for screening anti-diabetic drugs.

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

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    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.

  9. 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

  10. Transcriptional changes in the brains of cattle orally infected with the bovine spongiform encephalopathy agent precede detection of infectivity.

    Science.gov (United States)

    Tang, Yue; Xiang, Wei; Hawkins, Steve A C; Kretzschmar, Hans A; Windl, Otto

    2009-09-01

    Bovine spongiform encephalopathy (BSE) is a fatal, transmissible, neurodegenerative disease of cattle. BSE can be transmitted experimentally between cattle through the oral route, and in this study, brain tissue samples from animals at different time points postinoculation were analyzed for changes in gene expression. The aims of this study were to identify differentially regulated genes during the progression of BSE using microarray-based gene expression profiling and to understand the effect of prion pathogenesis on gene expression. A total of 114 genes were found to be differentially regulated over the time course of the infection, and many of these 114 genes encode proteins involved in immune response, apoptosis, cell adhesion, stress response, and transcription. This study also revealed a broad correlation between gene expression profiles and the progression of BSE in cattle. At 21 months postinoculation, the largest number of differentially regulated genes was detected, suggesting that there are many pathogenic processes in the animal brain even prior to the detection of infectivity in the central nervous systems of these orally infected cattle. Moreover, evidence is presented to suggest that it is possible to predict the infectious status of animals using the expression profiles from this study.

  11. Thrice-daily biphasic insulin aspart 30 may be another therapeutic option for Chinese patients with type 2 diabetes inadequately controlled with oral antidiabetic agents

    Institute of Scientific and Technical Information of China (English)

    YANG Wen-ying; JI Qiu-he; ZHU Da-long; YANG Jin-kui; CHEN Lu-lu; LIU Zhi-min; YU De-min; YAN Li

    2009-01-01

    In subjects with type 2 diabetes inadequately controlled with oral antidiabetic agents (OADs), insulin therapy is usually started to improve glycaemic control after failure of diet, exercise and OADs.1 Although there is no standard way to introduce insulin treatment, premixed formulations are a popular option. They offer an alternative to basal-bolus therapy and provide basal and prandial coverage with a single injection. Indeed, Koivisto et al2 in 1999 reported that 39% of patients with type 2 diabetes worldwide used premixed insulin as part of their therapeutic regimen. The modem premixed insulins, such as biphasic insulin aspart 30 (BIAsp 30) are most frequently prescribed twice-daily (BID) in clinical Department of Endocrinology, China-Japan Friendship Hospital, Beijing 100029, China (Yang WY)

  12. Efficacy of combination chemotherapy using a novel oral chemotherapeutic agent, TAS-102, with irinotecan hydrochloride on human colorectal and gastric cancer xenografts.

    Science.gov (United States)

    Nukatsuka, Mamoru; Nakagawa, Fumio; Saito, Hitoshi; Sakata, Minoru; Uchida, Junji; Takechi, Teiji

    2015-03-01

    TAS-102 is a novel oral nucleoside antitumor agent consisting of trifluridine and tipiracil hydrochloride at a molar ratio of 1:0.5. TAS-102 was approved in Japan in March 2014 for the treatment of patients with unresectable, advanced or recurrent colorectal cancer that is refractory to standard therapies. In the present study, enhancement of the therapeutic efficacy using a combination therapy of TAS-102 and irinotecan hydrochloride (CPT-11) was evaluated in a colorectal and gastric cancer xenograft-bearing nude mouse model. TAS-102 was orally administered twice a day from day 1 to 14, and CPT-11 was administered intravenously on days 1 and 8. The growth-inhibitory activity was evaluated based on the tumor volume and the growth-delay period, which was estimated based on the period required to reach a tumor volume that was five-times greater than the initial volume (RTV5). The tumor growth-inhibitory activity and the RTV5 of the group receiving TAS-102 with CPT-11 were significantly superior to those of both agents as monotherapy for mice with KM12C, KM12C/5-FU, DLD-1/5-FU, and SC-2 xenografts (p<0.01). No significant decrease in body weight was observed. The present pre-clinical findings indicated that the combination of TAS-102 and CPT-11 is a promising treatment option for colorectal or gastric cancer, not only for chemo-naïve tumors, but also for recurrent tumors after 5-fluorouracil (5-FU)-based chemotherapy. Copyright© 2015 International Institute of Anticancer Research (Dr. John G. Delinassios), All rights reserved.

  13. A comparative study to evaluate the effect of intranasal dexmedetomidine versus oral alprazolam as a premedication agent in morbidly obese patients undergoing bariatric surgery

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    Lakshmi Jayaraman

    2013-01-01

    Full Text Available Background: Morbidly obese patients with obstructive sleep apnea are extremely sensitive to sedative premedication. Intranasal dexmedetomidine is painless and quick acting. Intranasal dexmedetomidine can be used for premedication as it produces adequate sedation and also obtund hemodynamic response to laryngoscopy and tracheal intubation. Materials and Methods: Forty morbidly obese patients with BMI > 35 were chosen and divided into two groups. Group DEX received intranasal dexmedetomidine 1 mcg/kg (ideal body weight while other group (AZ received oral alprazolam 0.5 mg. Sedation scale, heart rate and the mean arterial pressure was assessed in both the groups at 0 hour, 45 minutes, during laryngoscopy and tracheal intubation. Results: The demographic profile, baseline heart rate, means arterial pressure, oxygen saturation and sedation scale was comparable between the two groups. The sedation scores, after 45 min, were statistically significant between the two groups i.e., 2.40 ± 1.09 in the AZ group as compared to 3.20 ± 1.79 in DEX group P value 0.034. The heart rate, mean arterial pressure and oxygen saturation were statistically similar between the two groups, after 45 min. The heart rate was significantly lower in the DEX group as compared to the AZ group. There was no statistical difference in the mean arterial pressure between the two groups either during laryngoscopy or tracheal intubation. Conclusion: Intranasal dexmedetomidine is a better premedication agent in morbidly obese patients than oral alprazolam.

  14. A potent oral P-selectin blocking agent improves microcirculatory blood flow and a marker of endothelial cell injury in patients with sickle cell disease.

    Science.gov (United States)

    Kutlar, Abdullah; Ataga, Kenneth I; McMahon, Lillian; Howard, Joanna; Galacteros, Frederic; Hagar, Ward; Vichinsky, Elliott; Cheung, Anthony T W; Matsui, Neil; Embury, Stephen H

    2012-05-01

    Abnormal blood flow accounts for most of the clinical morbidity of sickle cell disease (SCD) [1,2]. Most notably, occlusion of flow in the microvasculature causes the acute pain crises [3] that are the commonest cause for patients with SCD to seek medical attention [4] and major determinants of their quality of life [5]. Based on evidence that endothelial P-selectin is central to the abnormal blood flow in SCD we provide results from four of our studies that are germane to microvascular blood flow in SCD. A proof-of-principle study established that doses of heparin lower than what are used for anticoagulation but sufficient to block P-selectin improved microvascular blood flow inpatients with SCD. An in vitro study showed that Pentosan Polysulfate Sodium (PPS) had greater P-selectin blocking activity than heparin. A Phase I clinical study demonstrated that a single oral dose of PPS increased microvascular blood flow in patients with SCD. A Phase II clinical study that was not completed documented that daily oral doses of PPS administered for 8 weeks lowered plasma levels of sVCAM-1 and tended to improve microvascular blood flow in patients with SCD. These data support the concept that P-selectin on the microvascular endothelium is critical to both acute vascular occlusion and chronically impaired microvascular blood flow in SCD. They also demonstrate that oral PPS is beneficial to microvascular sickle cell blood flow and has potential as an efficacious agent for long-term prophylactic therapy of SCD.

  15. Efficient mucus permeation and tight junction opening by dissociable "mucus-inert" agent coated trimethyl chitosan nanoparticles for oral insulin delivery.

    Science.gov (United States)

    Liu, Min; Zhang, Jian; Zhu, Xi; Shan, Wei; Li, Lian; Zhong, Jiaju; Zhang, Zhirong; Huang, Yuan

    2016-01-28

    Oral administration of protein drugs is greatly impeded by the lack of drug carriers that can efficiently overcome the absorption barriers of mucosa tissue, which consists of not only epithelium but also a blanket of mucus gel. We herein report a novel self-assembled nanoparticle (NP) platform for oral delivery of insulin by facilitating the efficient permeation through both of these two barriers. The NP possesses a core composed of insulin and trimethyl chitosan (TMC), and a dissociable "mucus-inert" hydrophilic coating of N-(2-hydroxypropyl) methacrylamide copolymer (pHPMA) derivative. The NPs exhibited free Brownian motion and excellent permeability in mucus, which enabled the access of the NP core to the epithelial cell surface underneath the mucus. Moreover, investigation of NP behavior showed that the pHPMA molecules started to dissociate as the NP permeates through mucus, and the TMC NP core was then exposed to facilitate transepithelial transport via paracellular pathway. The pHPMA coating significantly improved transepithelial transport of TMC-based NP and their ability to open tight junctions between the mucus-secreting epithelial cells. Moreover, in diabetic rats, pHPMA coated NPs generated a prominent hypoglycemic response following oral administration, and exhibited a relative bioavailability 2.8-fold higher than that of uncoated TMC-based NPs. Our study provided the evidence of using pHPMA as "mucus-inert" agent to enhance mucus permeation of TMC-based NPs, and validated a novel strategy to overcome the multiple absorption barriers using NP platform with dissociable hydrophilic coating and TMC-based core possessing tight junction-opening ability.

  16. Performance Evaluation of Mucoadhesive Potential of Sodium Alginate on Microspheres Containing an Anti-Diabetic Drug: Glipizide

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    Yaswanth Allamneni

    2012-04-01

    Full Text Available The objective of the present investigation was to design mucoadhesive microspheres to achieve a substantial increase in length of stay of the drug in the GI tract of glipizide for treatment of type 2 diabetes mellitus. Glipizide is a second-generation sulfonylurea derivative used for the treatment of type II diabetes. Its short biological half-life (0.3 ± 0.7 h necessitates the need to be administered in two or three doses of 2.5-10 mg per day. Mucoadhesive microsphere exhibit a prolonged residence time at the site of application and facilitate an intimate contact with the underlying absorption surface and thus contribute to improved or better therapeutic performance of drug. It would, therefore be advantageous to have means for providing an intimate contact of the drug delivery system with the absorbing membranes. In the present study, alginate based mucoadhesive microspheres of were prepared by ionotropic external gelation technique utilizing calcium chloride (CaCl2 as a cross linking agent, to take the advantage of swelling and mucoadhesive property of alginate beads for improving the oral delivery of glipizide. Interaction studies performed using FTIR spectroscopy and DSC revealed that there was no drug to polymer interactions. The prepared microspheres are discrete, spherical and free flowing which was characterized by entrapment efficiency, particle size, micromeritic properties, in-vitro release behavior, scanning electron microscopy (SEM, in-vitro wash off test etc. Depending upon the variability in the concentration of sodium alginate, time of cross linking agent, the factors like particle size, and incorporation efficiency and release rate and mucoadhesion properties of microspheres varies. It was observed that increasing the polymer concentration along with the cross-linking time given the better affect on microspheres characteristic and percentage release of drug. Formulation F8 containing 5% w/v sodium alginate was selected as best

  17. 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

  18. 我院门诊口服降糖药应用情况分析%Analysis on Usage of Oral Hypoglycemic Agents by Outpatient in the Hospital

    Institute of Scientific and Technical Information of China (English)

    姜鹏; 鲁薇; 张少华

    2014-01-01

    Objective:To analyze the use of oral hypoglycemic agents by outpatient in the hospital during 2010~2012 , so as to pro-vide preference for clinical rational drug use.Methods:The information of various types of oral hypoglycemic by outpatient during 2010~2012 from the HIS system was obtained , the using frequency and cost per day were statistically analyzed and compared.Results:Acar-bose of sales amount for three consecutive years first row.Metformin of use frequency increased year by year , 2 years in first row, and the cost per day minimum.The serial number ratio greater than 1 is metformin.Conclusion:The use of oral hypoglycemic agent in the hospi-tal is reasonable , metformin of use frequency is high , conform to the principle of safe , effective and economic medication.%目的:分析我院2010~2012年门诊口服降糖药物的应用情况,为临床合理用药提供参考。方法:从HIS系统中调取2010~2012年中门诊各类口服降糖药物的使用数据,对其使用频率、日均费用等进行对比分析。结果:阿卡波糖销售金额连续3年排首位;二甲双胍的使用频率逐年上升,连续2年位居第一,且日平均费用最低;序号比大于1的药物为二甲双胍。结论:该院口服降糖药物的应用基本合理,二甲双胍使用频率高,符合安全、有效、经济的用药原则。

  19. Effectiveness on oral pain of 808-nm diode laser used prior to composite restoration for symptomatic non-carious cervical lesions unresponsive to desensitizing agents.

    Science.gov (United States)

    Femiano, Felice; Femiano, Rossella; Lanza, Alessandro; Lanza, Michele; Perillo, Letizia

    2017-01-01

    This study compares sensitivity reduction after dental restoration with and without prior diode laser (DL) irradiation for cervical dentine hypersensitivity (CDH) from non-carious cervical lesions (NCCLs) unresponsive to desensitizing agents. Eighty-eight teeth of 28 subjects (21 females; age 23-64 years), with CDH from NCCL were included in this study. NCCLs of each oral quadrant were randomized in two groups (study group (SG)) to estimate the sensitivity reduction after dental restoration (SG-1) compared with the DL irradiation used prior to restoration placement (SG-2). The subjects were asked to rate the sensitivity experienced during air stimulation using a visual analog scale before (baseline), immediately after, and at 6 and 12 months from restoration. The outcomes showed a significant reduction of discomfort compared to baseline for NCCLs of SG-2 with the decrease of 78.5, 78.9, and 78.1 % immediately and at 6 and 12 months after restoration, respectively; in comparison with the decrease of 70.1, 67, and 65.3 % for NCCLs of SG-1 immediately and at 6 and 12 months after restoration, respectively; and compared to baseline. The DL irradiation prior to dental restoration can further improve the painful symptomatology of CDH from NCCL unresponsive to desensitizing agents.

  20. 石榴抗糖尿病生物活性的研究进展%Research progress in anti-diabetic actions of pomegranate( Punica granatum L.)

    Institute of Scientific and Technical Information of China (English)

    刘慧; 赵文恩; 康保珊

    2012-01-01

    体外和体内实验均证实石榴汁、石榴皮、石榴花、石榴籽和石榴叶等具有抗糖尿病的功效,综述了石榴多个部位的降血糖效果、降血糖活性成分及其作用机制的研究进展。石榴中的多酚类是抗糖尿病的主要活性物质,主要通过提高胰岛素受体敏感性、增强PPAR-γ(Peroxisome proliferator—activated receptor,过氧化酶体增殖物激活受体)的表达、抑制α-葡萄糖苷酶活性等作用达到抗糖尿病的功效,为石榴的进一步开发利用提供参考。%There are anti-diabetic constituents in several parts of pomegranate including juice, peels, flowers, seeds,and leaves in vivo or vitro research.The anti-diabetic activities, major active compounds and mechanisms of different parts in pomegranate were summarized in this paper.Polyphenols were the major active components for anti-diabetic activity.The sensitivity of insulin receptor and the expression of peroxisome proliferator-activated receptor were improved as well as the activity of a-glucosidase was inhibited, which were major reasons for hypoglycemic activity of pomegranate. The results provide a powerful support for further development of pomegranate utilization.

  1. The effects of C-glycosylation of luteolin on its antioxidant, anti-Alzheimer's disease, anti-diabetic, and anti-inflammatory activities.

    Science.gov (United States)

    Choi, Jae Sue; Islam, Md Nurul; Ali, Md Yousof; Kim, Young Myeong; Park, Hye Jin; Sohn, Hee Sook; Jung, Hyun Ah

    2014-10-01

    To investigate the effect of C-glycosylation at different positions of luteolin, the structure-activity relationships of luteolin and a pair of isomeric C-glycosylated derivatives orientin and isoorientin, were evaluated. We investigated the effects of C-glycosylation on the antioxidant, anti-Alzheimer's disease (AD), anti-diabetic and anti-inflammatory effects of luteolin and its two C-glycosides via in vitro assays of peroxynitrite (ONOO(-)), total reactive oxygen species (ROS), nitric oxide (NO), 1,1-diphenyl-2-picrylhydraxyl (DPPH), aldose reductase, protein tyrosine phosphatase 1B (PTP1B), acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and β-site amyloid precursor cleaving enzyme 1 (BACE1), and cellular assays of NO production and inducible nitric oxide synthase (iNOS)/cyclooxygenase-2 expression in lipopolysaccharide (LPS)-stimulated RAW 264.7 cells. Of the three compounds, isoorientin showed the highest scavenging activity against DPPH, NO, and ONOO(-), while luteolin was the most potent inhibitor of ROS generation. In addition, luteolin showed the most potent anti-AD activity as determined by its inhibition of AChE, BChE, and BACE1. With respect to anti-diabetic effects, luteolin exerted the strongest inhibitory activity against PTP1B and rat lens aldose reductase. Luteolin also inhibited NO production and iNOS protein expression in LPS-stimulated macrophages, while orientin and isoorientin were inactive at the same concentrations. The effects of C-glycosylation at different positions of luteolin may be closely linked to the intensity and modulation of antioxidant, anti-AD, anti-diabetic, and anti-inflammatory effects of luteolin and its C-glycosylated derivatives.

  2. Piracetam Facilitates the Anti-Amnesic but not Anti-Diabetic Activity of Metformin in Experimentally Induced Type-2 Diabetic Encephalopathic Rats.

    Science.gov (United States)

    Pandey, Shruti; Garabadu, Debapriya

    2017-07-01

    Piracetam exhibits anti-amnesic activity in several animal models of dementia. However, its anti-amnesic potential has yet to be evaluated in type-2 diabetes mellitus (T2DM)-induced encephalopathy. Therefore, in the present study, piracetam (25, 50 and 100 mg/kg) was screened for anti-amnesic and anti-diabetic activity in T2DM-induced encephalopathic male rats. Subsequently, anti-amnesic and anti-diabetic activities were evaluated for piracetam, metformin and their combination in T2DM-induced encephalopathic animals. Rats received streptozotocin (45 mg/kg) and nicotinamide (110 mg/kg) injections on day-1 (D-1) of the experimental schedule and were kept undisturbed for 35 days to exhibit T2DM-induced encephalopathy. All drug treatments were continued from D-7 to D-35 in both experiments. Piracetam (100 mg/kg) attenuated loss in learning and memory in terms of increase in escape latency on D-4 (D-34) and decrease in time spent in the target quadrant on D-5 (D-35) of Morris water maze test protocol, and spatial memory in terms of reduced spontaneous alternation behavior in Y-maze test of encephalopathic rats. Additionally, piracetam attenuated altered levels of fasting plasma glucose and insulin, HOMA-IR and HOMA-B in encephalopathic animals, comparatively lesser than metformin. In the next experiment, combination of piracetam and metformin exhibited better anti-amnesic but not anti-diabetic activity than respective monotherapies in encephalopathic rats. Further, the combination attenuated reduced acetylcholine level and increased acetylcholinesterase activity, increased glycogen synthase kinase-3β level and decreased brain-derived neurotropic factor level in hippocampus and pre-frontal cortex of encephalopathic animals. Thus, piracetam could be used as an adjuvant to metformin in the management of dementia in T2DM-induced encephalopathy.

  3. Fusion proteins containing neuropeptides as novel insect contol agents: snowdrop lectin delivers fused allatostatin to insect haemolymph following oral ingestion.

    Science.gov (United States)

    Fitches, Elaine; Audsley, Neil; Gatehouse, John A; Edwards, John P

    2002-12-01

    The mannose-binding lectin from snowdrop (Galanthus nivalis agglutinin: GNA), when fed to insects, binds to the gut epithelium and passes into the haemolymph. The potential for GNA to act as a carrier protein to deliver an insect neuropeptide, Manduca sexta allatostatin (Manse-AS), to the haemolymph of lepidopteran larvae has been examined by expressing a GNA/Manse-AS fusion protein (FP) in Escherichia coli, and feeding purified FP to larvae of the tomato moth Lacanobia oleracea. FP, administered at 1.5 or 0.5% of dietary proteins, was found to strongly inhibit feeding and prevent growth of fifth stadium larvae, whereas neither GNA nor Manse-AS alone, nor a mixture of GNA and Manse-AS in control treatments, had deleterious effects at similar levels. Elevated levels of material reacting with anti-Manse-AS antibodies were detected in the haemolymph of insects fed diets containing FP, suggesting that transport of the peptide had occurred. Evidence for the delivery of intact FP to the haemolymph was provided by the co-elution of Manse-AS-like immunoreactivity with standard FP after size exclusion chromatography of haemolymph from FP-fed larvae. GNA/Manse-AS and similar fusion proteins offer a novel and effective strategy for delivering insect neuropeptides by oral administration, which could be used in conjunction with expression in transgenic plants to give crop protection in the field.

  4. Attenuation of obesity-induced inflammation in mice orally administered with salmon cartilage proteoglycan, a prophylactic agent.

    Science.gov (United States)

    Hirose, Shouhei; Asano, Krisana; Nakane, Akio

    2017-03-11

    Obesity is associated with chronic inflammation of adipose tissue and causes development of type 2 diabetes. M1 macrophage population was increased in adipose tissue of obese mouse. M1 macrophages induce insulin resistance through the secretion of proinflammatory cytokines. Our previous studies demonstrated that salmon cartilage proteoglycan (PG) suppresses excess inflammation in various mouse inflammatory diseases. In this study, we examined the effect of PG on type 2 diabetes using high-fat-diet (HFD) induced obese mouse model. Oral PG administration enhanced the population of small adipocytes (area less than 1000 μm(2)) without body and tissue weight gain. In addition, PG administration suppressed mRNA expression of TNF-α, IL-6 and CXCL2 in adipose tissue. The proportion of M1 macrophages was decreased by PG administration. In addition, PG administration suppressed hyperglycemia after intraperitoneal glucose injection. Fasted serum insulin level was decreased in PG-administered mice. Moreover, insulin-stimulated phosphorylation of Akt was enhanced in the liver and gastrocnemius skeletal muscle of PG-administered mice. These data suggested that PG administration improves hyperglycemia and insulin sensitivity in obese mice by modulation of M1 macrophages which secrete proinflammatory cytokines in adipose tissue and activation of Akt in liver and skeletal muscle.

  5. A systematic review of interventions addressing adherence to anti-diabetic medications in patients with type 2 diabetes--impact on adherence.

    Directory of Open Access Journals (Sweden)

    Sujata Sapkota

    Full Text Available The global prevalence of diabetes is increasing. Medications are a recommended strategy to control hyperglycaemia. However, patient adherence can be variable, impacting health outcomes. A range of interventions for patients with type 2 diabetes have focused on improving treatment adherence. This review evaluates the impact of these interventions on adherence to anti-diabetic medications and focuses on the methods and tools used to measure adherence.Medline, Embase, CINAHL, IPA, PUBmed, and PsychINFO were searched for relevant articles published in 2000-2013, using appropriate search terms.Fifty two studies addressing adherence to anti-diabetic medications in patients with type 2 diabetes met the inclusion criteria and were reviewed. Each study was assessed for research design, method(s used for measuring medication adherence, and impact of intervention on medication adherence and glycaemic control. Fourteen studies were published in 2000-2009 and 38 in 2010-2013. Twenty two interventions led to improvements in adherence to anti-diabetic medications, while only nine improved both medication adherence and glycaemic control. A single strategy could not be identified which would be guaranteed to improve anti-diabetic medication adherence consistently. Nonetheless, most interventions were successful in influencing one or more of the outcomes assessed, indicating the usefulness of these interventions under certain circumstances. Self-report, particularly the Summary of Diabetes Self-Care Activities questionnaire was the most commonly used tool to assess medication adherence, although other self-report tools were used in more recent studies. Overall, there was a slight increase in the number of studies that employed multiple methods to assess medication adherence in studies conducted after 2008.The diversity of interventions and adherence measurements prevented a meta-analysis of the impact of interventions on adherence to therapy, highlighting the

  6. Medicinal Chemistry of the Anti-Diabetic Effects of Momordica Charantia: Active Constituents and Modes of Actions

    Science.gov (United States)

    Singh, Jaipaul; Cumming, Emmanuel; Manoharan, Gunasekar; Kalasz, Huba; Adeghate, Ernest

    2011-01-01

    medicinal chemistry and use(s) of M. charantia and its various extracts and compounds, their biochemical properties and how they act as anti-diabetic (hypoglycemic) drugs and the various mechanisms by which they exert their beneficial effects in controlling and treating DM. PMID:21966327

  7. Retrospective Analysis of Application of Oral Hypoglycemic Agents in a Hospital of Chongqing in Recent 3 Years%重庆市某医院近3年口服降糖药应用分析

    Institute of Scientific and Technical Information of China (English)

    苏湲淇; 龙波

    2012-01-01

    Objective To analyze the application situation and the development trend of oral hypoglycemic agents in a grade A class 3 hospital of Chongqing. Methods The sale amount,DDDs and other indicators of the oral hypoglycemic agent application in the hospital during the year 2007-2009 were statistically analyzed. Results In the last three years,the hospital's total sales of oral hypoglycemic agents and the total amount of DDDs were increased year by year. Biguanide, a - glucosidase inhibitors, thiazolidinediones were mainly selected in clinical use. Conclusion The overall structure of hospital clinical use of oral hypoglycemic agents is reasonably stable.%目的 分析医院口服降糖药的应用情况与发展趋势.方法 对医院2007年至2009年口服降糖药的销售金额、用药频度等指标进行统计分析.结果 口服降糖药的总销售金额和总用药频度逐年增长,临床主要选用双胍类、α-葡萄糖苷酶抑制剂、噻唑烷二酮类药物.结论 口服降糖药临床用药整体结构合理稳定.

  8. 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.

  9. Effects of low-dose aspirin (50-mg/day), low-dose aspirin plus dipyridamole, and oral anticoagulant agents after internal mammary artery bypass-grafting : Patency and clinical outcome at 1 year

    NARCIS (Netherlands)

    van der Meer, J; de la Rivière, Aart Brutel; van Gilst, Wiek H.; Hillege, Hans L.; Pfisterer, M; Kootstra, G. J.; Dunselmann, P. H. J. M.; MULDER, BJM; Lie, Kong I.

    1994-01-01

    Objectives. This study was performed to compare the efficacy and safety of aspirin, aspirin plus dipyridamole, and oral anti coagulant agents in the prevention of internal mammary artery graft occlusion. Background. Antithrombotic drugs increase vein graft patency after coronary artery bypass

  10. Once-daily basal insulin glargine versus thrice-daily prandial insulin lispro in people with type 2 diabetes on oral hypoglycaemic agents (APOLLO): an open randomised controlled trial

    DEFF Research Database (Denmark)

    Bretzel, R.G.; Nuber, U.; Landgraf, W.

    2008-01-01

    BACKGROUND: As type 2 diabetes mellitus progresses, oral hypoglycaemic agents often fail to maintain blood glucose control and insulin is needed. We investigated whether the addition of once-daily insulin glargine is non-inferior to three-times daily prandial insulin lispro in overall glycaemic c...

  11. Oral administration of Bis(aspirinato)zinc(II) complex ameliorates hyperglycemia and metabolic syndrome-like disorders in spontaneously diabetic KK-A(y) mice: structure-activity relationship on zinc-salicylate complexes.

    Science.gov (United States)

    Yoshikawa, Yutaka; Adachi, Yusuke; Yasui, Hiroyuki; Hattori, Masakazu; Sakurai, Hiromu

    2011-01-01

    In recent years, the number of patients suffering from diseases, such as cancer, apoplexy, osteoporosis, hypertension, and type 2 diabetes mellitus is increasing worldwide. Type 2 diabetes, a lifestyle-related disease, is recognized as a serious disease. Various types of pharmaceutics for diabetes have been used. Since the relationship between diabetes and biometals such as vanadium, copper, and zinc ions has been recognized for many years, we have been developing the anti-diabetic metal complexes as new candidates. We found that several zinc(II) (Zn) complexes exhibit glucose-lowering activity for treating type 2 diabetes. High doses of salicylates have been known to reverse hyperglycemia and hyperinsulinemia in type 2 diabetic patients. These findings strongly suggest that the combined use of Zn and salicylates achieves the synergism in treating type 2 diabetes. Because aspirin, acetyl salicylic acid, has a chelating ability, we used it as a ligand to Zn. Several Zn-salicylate complexes were prepared and their biological activities were examined in this study. The complexes with an electron-withdrawing group in the ligand exhibited higher in vitro insulinomimetic activity than those of Zn complexes with an electron-donating group in the ligand. When bis(aspirinato)Zn (Zn(asp)₂) complex was orally administered on KK-A(y) mice with hereditary type 2 diabetes, the diabetic state was improved. In addition, this complex exhibited normalizing effects on serum adiponectin level and high blood pressure in metabolic syndrome. In conclusion, Zn(asp)₂ complex is newly proposed as a potent anti-diabetic and anti-metabolic syndrome agent.

  12. Interacción de los antineoplásicos orales con los alimentos: revisión sistemática Antineoplastic oral agents and drug-nutrient interactions: a sistematic review

    Directory of Open Access Journals (Sweden)

    N. V. Jiménez Torres

    2009-06-01

    cumplir estos estudios. Resultados: En la búsqueda inicial se obtuvieron 850 referencias (98,5% Medline + y 1,4% Cochrane. En la primera fase se excluyeron el 87,7% (746 de los artículos, correspondiendo el 100% a la búsqueda en Medline. En la segunda fase, quedaron 40 artículos (5,2% de los iniciales para su lectura crítica a texto completo, a los que se añadieron cuatro más no indexados en Medline. De la lectura crítica de los 44 artículos finales, se excluyeron 25 artículos (20 artículos originales, 4 comunicaciones cortas y 1 metanálisis por no incluir como medida de resultado el dictamen de bioequivalencia. Los 19 (2,2% artículos restantes proporcionaron información sobre 19 fármacos antineoplásicos orales, en 210 pacientes y 146 voluntarios sanos. De estos 19 fármacos, el 63% no presentan iFA o interacciones fármaco-alimento, pudiéndose administrar indistintamente con/sin alimentos; el 21% se deben administrar con alimentos y sólo el 16% presentan interacción fármaco alimento, por lo que se deben administrar sin alimentos. Discusión: Actualmente, la importancia clínica de las interacciones fármaco alimento con antineoplásicos orales se identifica más directamente con la seguridad del paciente que con la efectividad del tratamiento. Ante el desarrollo de estos agentes orales, su irrupción en la terapia oncológica desplazando a la terapia parenteral, con costes mensuales de miles de euros, hay necesidad de realizar estudios farmacocinéticos y farmacodinámicos bien diseñados. Su objetivo debe de ser comparar su biodisponibilidad en presencia o ausencia de alimentos con la respuesta clínica. Mientras tanto, establecer recomendaciones para su administración en relación con los alimentos, es inconsistente para algunos de estos fármacos y su resultado incierto por la falta de estudios fundamentados en el dictamen de bioequivalencia establecido por la FDA.Introduction: studies on bioavailability are part of the clinical development of

  13. EFFICACY AND SAFETY OF DEFERASIROX WHEN COMPARED TO D EFERIPRONE AS ORAL IRON CHELATING AGENT : A RANDOMIZED CONTROL TRIAL

    Directory of Open Access Journals (Sweden)

    Sanjeeva

    2015-03-01

    Full Text Available BACKGROUND : Thalassemia is one of the most common inherited hemoglobinopathy seen in southern India. With regular blood transfusion, these children live longer but associated morbidity due to iron overload impairs the quality of life. We studied the efficacy and safety of new oral iron chelator, deferasirox, compared with deferiprone which was used for long time. MATERIAL AND METHODS : We cond ucted a prospective randomised control study, between January 2011 to June 2012 at thalassemia day care centre of Indira Gandhi I nstitute of C hild H ealth, Bengaluru. The children who were diagnosed as Thalassemia and receiving regular blood transfusion wit h serum ferritin levels more than 1000ng/ml and not receiving any chelation therapy were included in the study. These children were randomly divided into two groups as group 1 and group 2 by computer generated randomization. The children included in g roup 1 received Deferasirox and group 2 received Deferiprone as chelation therapy. The dosage of deferasirox was 20mg/kg/day once daily and that of deferiprone 75 mg/kg/day in three divided daily doses. The primary study outcome was to measure and compare the d ecrease in serum ferritin levels between the two study groups. The secondary outcome measures were to compare the side effect profiles among the two groups. RESULTS : We included 41 thalessemic children and 19 of them were included in group 1 (Deferasirox and 22 children in Group 2 (Deferiprone. At the end of study period of 18 months three children in group II discontinued therapy due to side effects, hence the remaining 19 were available for final analysis in group 2 whereas no drop outs in the group 1. During the study period, the serum ferritin decreased from 3261±2613ng/dl to 1586±766 ng/dl in group 1 as compared in group 2 from 4109±3153 ng/dl to 1743±1138 ng/dl (fig 2. This was also not statistically significant. In group 2, 68% of the children expe rienced adverse effect as compared

  14. RPR 107393, a potent squalene synthase inhibitor and orally effective cholesterol-lowering agent: comparison with inhibitors of HMG-CoA reductase.

    Science.gov (United States)

    Amin, D; Rutledge, R Z; Needle, S N; Galczenski, H F; Neuenschwander, K; Scotese, A C; Maguire, M P; Bush, R C; Hele, D J; Bilder, G E; Perrone, M H

    1997-05-01

    Squalene synthase catalyzes the reductive dimerization of two molecules of farnesyl pyrophosphate to form squalene and is the first committed step in sterol synthesis. A specific inhibitor of squalene synthase would inhibit cholesterol biosynthesis but not prevent the formation of other products of the isoprenoid pathway, such as dolichol and ubiquinone. RPR 107393 [3-hydroxy-3-[4-(quinolin-6-yl)phenyl]-1-azabicyclo[2-2-2]octane dihydrochloride] and its R and S enantiomers are potent inhibitors of rat liver microsomal squalene synthase, with IC50 values of 0.6 to 0.9 nM. One hour after oral administration to rats, RPR 107393 inhibited de novo [14C]cholesterol biosynthesis from [14C]mevalonate in the liver with an ED50 value of 5 mg/kg. Diacid metabolites of [14C]farnesyl pyrophosphate were identified after acid treatment of the livers of these animals. These results support in vitro data demonstrating that these compounds are inhibitors of squalene synthase. In rats, RPR 107393 (30 mg/kg p.o. b.i.d. for 2 days) reduced total serum cholesterol by RPR 107393 (20 mg/kg b.i.d.) reduced plasma cholesterol concentration by 50% after 1 week of administration; this was greater than the reduction observed with lovastatin or pravastatin, neither of which produced > 31% reduction in plasma cholesterol when administered for 1 week at a dose of 50 mg/kg b.i.d. The R and S enantiomers of RPR 107393 (20 mg/kg p.o. q.d. for 7 days) reduced plasma low density lipoprotein cholesterol by 50% and 43%, respectively, whereas high density lipoprotein cholesterol was unchanged. In summary, RPR 107393 is a potent inhibitor of squalene synthase. It is an orally effective hypocholesterolemic agent in rats and marmosets that has greater efficacy than lovastatin or pravastatin in the marmoset.

  15. Efficacy of combination chemotherapy using a novel oral chemotherapeutic agent, TAS-102, together with bevacizumab, cetuximab, or panitumumab on human colorectal cancer xenografts.

    Science.gov (United States)

    Tsukihara, Hiroshi; Nakagawa, Fumio; Sakamoto, Kazuki; Ishida, Keiji; Tanaka, Nozomu; Okabe, Hiroyuki; Uchida, Junji; Matsuo, Kenichi; Takechi, Teiji

    2015-05-01

    TAS-102 is a novel oral nucleoside antitumor agent that consists of trifluridine (FTD) and tipiracil hydrochloride (TPI) at a molecular ratio of 1:0.5, and was approved in Japan in March 2014 for the treatment of patients with unresectable advanced or recurrent colorectal cancer that is refractory to standard therapies. In the present study, we used colorectal cancer xenografts to assess whether the efficacy of TAS-102 could be improved by combining it with bevacizumab, cetuximab or panitumumab. TAS-102 was orally administered twice a day from day 1 to 14, and bevacizumab, cetuximab and panitumumab were administered intraperitoneally twice a week for 2 weeks. Growth inhibitory activity was evaluated based on the relative tumor volume (RTV) after 2 weeks of drug administration and time taken for the relative tumor volume to increase five-fold (RTV5). Tumor growth inhibition and RTV5 with TAS-102 and bevacizumab combination treatment were significantly better than those with TAS-102 or bevacizumab alone in the SW48 and HCT116 tumor models, and the concentration of phosphorylated FTD in tumors determined by liquid chromatography-tandem mass spectrometry (LC-MS/MS) analysis was higher in the TAS-102 and bevacizumab combination group than in the TAS-102 monotherapy group. The combination of TAS-102 and cetuximab or panitumumab was also significantly more effective than either monotherapy in the SW48 tumor model. There was no significant difference in the body weight between the mice treated with TAS-102 monotherapy and any of the combination therapies on day 29. Our preclinical findings indicate that the combination therapy of TAS-102, bevacizumab and cetuximab or panitumumab is a promising treatment option for colorectal cancer.

  16. Efficacy of Combination Chemotherapy Using a Novel Oral Chemotherapeutic Agent, TAS-102, with Oxaliplatin on Human Colorectal and Gastric Cancer Xenografts.

    Science.gov (United States)

    Nukatsuka, Mamoru; Nakagawa, Fumio; Takechi, Teiji

    2015-09-01

    TAS-102 is a novel oral nucleoside antitumor agent consisting of trifluridine (FTD) and the thymidine phosphorylase inhibitor tipiracil hydrochloride (at a molar ratio of 1:0.5) that was approved in Japan in 2014 for the treatment of unresectable advanced or recurrent colorectal cancer. In the present study, the enhancement of therapeutic efficacy using a combination of TAS-102 and oxaliplatin was evaluated in a xenograft-bearing nude mouse model of colorectal and gastric cancer. TAS-102 was orally administered twice-a-day from day 1 to 14, and oxaliplatin was administered intravenously on days 1 and 8. The in vivo growth-inhibitory activity was evaluated based on the tumor volume and the growth-delay period, was estimated based on the period required to reach a tumor volume five-times greater than the initial volume (RTV5). The tumor growth-inhibitory activity and RTV5 in mice administered TAS-102 with oxaliplatin were significantly superior to those associated with either monotherapy in mice with colorectal (HCT 116, SW-48; p<0.001) and gastric cancer (SC-2, MKN74; p<0.001). MKN74/5FU, a 5-fluorouracil-resistant MKN74 sub-line, was sensitive to both FTD and oxaliplatin in vitro. In vivo, TAS-102 alone was effective in MKN74/5FU, and its anti-tumor activity was significantly enhanced in combination with oxaliplatin (p<0.001). No significant decrease in body weight or toxicity was observed compared to either monotherapy. The present pre-clinical findings indicate that combination of TAS-102 and oxaliplatin is a promising treatment option for colorectal or gastric cancer, and can be utilized in both chemo-naïve tumors and recurrent tumors after 5-fluorouracil treatment. Copyright© 2015 International Institute of Anticancer Research (Dr. John G. Delinassios), All rights reserved.

  17. Switching Patients with Non-Dialysis Chronic Kidney Disease from Oral Iron to Intravenous Ferric Carboxymaltose: Effects on Erythropoiesis-Stimulating Agent Requirements, Costs, Hemoglobin and Iron Status

    Science.gov (United States)

    Toblli, Jorge Eduardo; Di Gennaro, Federico

    2015-01-01

    Background Patients with non-dialysis-dependent chronic kidney disease (ND-CKD) often receive an erythropoiesis-stimulating agent (ESA) and oral iron treatment. This study evaluated whether a switch from oral iron to intravenous ferric carboxymaltose can reduce ESA requirements and improve iron status and hemoglobin in patients with ND-CKD. Methods This prospective, single arm and single-center study included adult patients with ND-CKD (creatinine clearance ≤40 mL/min), hemoglobin 11–12 g/dL and iron deficiency (ferritin iron and ESA during 6 months prior to inclusion. Study patients received an intravenous ferric carboxymaltose dose of 1,000 mg iron, followed by a 6-months ESA/ ferric carboxymaltose maintenance regimen (target: hemoglobin 12 g/dL, transferrin saturation >20%). Outcome measures were ESA dose requirements during the observation period after initial ferric carboxymaltose treatment (primary endpoint); number of hospitalizations and transfusions, renal function before and after ferric carboxymaltose administration, number of adverse reactions (secondary endpoints). Hemoglobin, mean corpuscular volume, ferritin and transferrin saturation were measured monthly from baseline until end of study. Creatinine clearance, proteinuria, C-reactive protein, aspartate aminotransferase, alanine aminotransferase and alkaline phosphatase bimonthly from baseline until end of study. Results Thirty patients were enrolled (age 70.1±11.4 years; mean±SD). Mean ESA consumption was significantly reduced by 83.2±10.9% (from 41,839±3,668 IU/patient to 6,879±4,271 IU/patient; pferric carboxymaltose-related adverse events were reported and no patient withdrew or required transfusions during the study. Conclusion Among patients with ND-CKD and stable normal or borderline hemoglobin, switching from oral iron to intravenous ferric carboxymaltose was associated with significant improvements in hematological and iron parameters and a significant reduction in ESA dose

  18. Anti-diabetic activity of chromium picolinate and biotin in rats with type 2 diabetes induced by high-fat diet and streptozotocin.

    Science.gov (United States)

    Sahin, Kazim; Tuzcu, Mehmet; Orhan, Cemal; Sahin, Nurhan; Kucuk, Osman; Ozercan, Ibrahim H; Juturu, Vijaya; Komorowski, James R

    2013-07-28

    The objective of the present study was to evaluate anti-diabetic effects of chromium picolinate (CrPic) and biotin supplementations in type 2 diabetic rats. The type 2 diabetic rat model was induced by high-fat diet (HFD) and low-dose streptozotocin. The rats were divided into five groups as follows: (1) non-diabetic rats fed a regular diet; (2) diabetic rats fed a HFD; (3) diabetic rats fed a HFD and supplemented with CrPic (80 μg/kg body weight (BW) per d); (4) diabetic rats fed a HFD and supplemented with biotin (300 μg/kg BW per d); (5) diabetic rats fed a HFD and supplemented with both CrPic and biotin. Circulating glucose, cortisol, total cholesterol, TAG, NEFA and malondialdehyde concentrations decreased (Padipose tissue and phosphorylated insulin receptor substrate 1 (p-IRS-1) expression of liver, kidney and muscle tissues, while the supplements increased (Ptissues. Expression of NF-κB in the liver and kidney was greater in diabetic rats fed a HFD, as compared with rats fed a regular diet (P< 0·01). The supplements decreased the expression of NF-κB in diabetic rats (P< 0·05). Results of the present study revealed that supplementing CrPic and biotin alone or in a combination exerts anti-diabetic activities, probably through modulation of PPAR-γ, IRS-1 and NF-κB proteins.

  19. Widening the path and window of opportunity for FDA approval of non-vitamin K oral anticoagulant specific antidotes and reversal agents.

    Science.gov (United States)

    Patel, Sunny; Steen, Dylan

    2016-02-01

    There remains a need for safe, immediately effective, and easy to administer antidotes for patients taking novel oral anticoagulants (NOACs) in the settings of major bleeding, need for emergency surgery, and accidental overdose. We review considerations for the successful safety and effectiveness evaluation of potential antidotes currently under development. These compounds are in expedited regulatory approval programs aimed at accelerating the preclinical and clinical evaluation and approval processes for treatments of serious conditions. We review the features of these expedited programs as well as the FDA's efforts to broadly advance the efficiency of drug development and increase the number of new compounds brought to market. The critical path initiative and regulatory science initiative have resulted in numerous successful programs to address current challenges such as a paucity of validated biomarkers and surrogate endpoints as well as unreliable animal models of toxicity. The FDA has also advocated for increased use of pharmacokinetic/pharmacodynamic modeling and adaptive trial design. These efforts foster collaboration between academia, industry and the public sector across interdisciplinary sciences and may continue to widen the pathway for NOAC-specific reversal agents and other novel compounds.

  20. Comparative Pharmacokinetic Study of Mangiferin After Oral Administration of Pure Mangiferin and US Patented Polyherbal Formulation to Rats

    OpenAIRE

    Kammalla, Ananth Kumar; Ramasamy, Mohan Kumar; Inampudi, Jyothi; Dubey, Govind Prasad; Agrawal, Aruna; Kaliappan, Ilango

    2014-01-01

    The US patented polyherbal formulation for the prevention and management of type II diabetes and its vascular complications was used for the present study. The xanthone glycoside mangiferin is one of the major effector constituents in the Salacia species with potential anti-diabetic activity. The pharmacokinetic differences of mangiferin following oral administration of pure mangiferin and polyherbal formulation containing Salacia species were studied with approximately the same dose 30 mg/kg...

  1. Determination of designer doping agent--2-ethylamino-1-phenylbutane--in dietary supplements and excretion study following single oral supplement dose.

    Science.gov (United States)

    Wójtowicz, Marzena; Jarek, Anna; Chajewska, Katarzyna; Turek-Lepa, Ewa; Kwiatkowska, Dorota

    2015-11-10

    The quantitative analysis of a new designer doping agent, 2-ethylamino-1-phenylbutane (EAPB) and its metabolite, 2-amino-1-phenylbutane (APB) in urine samples, and the determination of EAPB in dietary supplement samples, have been presented. The main purpose of the present study was to develop simple and reliable gas chromatography-mass spectrometry method (GC-MS) for excretion study following a single oral administration of dietary supplements containing EAPB. Three analytical methods for the determination of EAPB in urine and supplement samples, and APB in urine samples using the GC-MS system, have been validated. The method of the determination of EAPB in supplement samples was applied to analyze seventeen dietary supplements, CRAZE and DETONATE. Two other methods were used to determine the urinary excretion profile of EAPB and APB in the case of three healthy volunteers and, on further investigation, it was applied to the anti-doping control in sport. Quantification was obtained on the basis of the ions at m/z 86, 58 and 169, monitored for EAPB, APB and diphenylamine (used as an internal standard), respectively. The limits of detection and quantification were 2.4 and 7.3μg/g for EAPB in the case of supplement analysis, 2.9 and 8.8ng/mL for EAPB in the case of urine analysis, and 3.2 and 9.7ng/mL for APB. The other validation parameters as linearity, precision and trueness have been also investigated with the acceptable results. The extraction yield of all presented methods was above 69%. EAPB was detected in fourteen analyzed supplements (not included EAPB in their labels) and its content varied between 1.8 and 16.1mg/g. Following oral administration of three supplements with EAPB to one male and two female volunteers, the parent compound of EAPB and its metabolite were monitored and the excretion parameters as the maximum concentration of the analyte in urine (2.2-4.2μg/mL for EAPB; 1.1-5.1μg/mL for APB) and the time for the maximum height of the excretion

  2. A Systematic Review of Interventions Addressing Adherence to Anti-Diabetic Medications in Patients with Type 2 Diabetes—Components of Interventions

    Science.gov (United States)

    Sapkota, Sujata; Brien, Jo-anne E.; Greenfield, Jerry R.; Aslani, Parisa

    2015-01-01

    Background Poor adherence to anti-diabetic medications contributes to suboptimal glycaemic control in patients with type 2 diabetes (T2D). A range of interventions have been developed to promote anti-diabetic medication adherence. However, there has been very little focus on the characteristics of these interventions and how effectively they address factors that predict non-adherence. In this systematic review we assessed the characteristics of interventions that aimed to promote adherence to anti-diabetic medications. Method Using appropriate search terms in Medline, Embase, CINAHL, International Pharmaceutical Abstracts (IPA), PUBmed, and PsychINFO (years 2000–2013), we identified 52 studies which met the inclusion criteria. Results Forty-nine studies consisted of patient-level interventions, two provider-level interventions, and one consisted of both. Interventions were classified as educational (n = 7), behavioural (n = 3), affective, economic (n = 3) or multifaceted (a combination of the above; n = 40). One study consisted of two interventions. The review found that multifaceted interventions, addressing several non-adherence factors, were comparatively more effective in improving medication adherence and glycaemic target in patients with T2D than single strategies. However, interventions with similar components and those addressing similar non-adherence factors demonstrated mixed results, making it difficult to conclude on effective intervention strategies to promote adherence. Educational strategies have remained the most popular intervention strategy, followed by behavioural, with affective components becoming more common in recent years. Most of the interventions addressed patient-related (n = 35), condition-related (n = 31), and therapy-related (n = 20) factors as defined by the World Health Organization, while fewer addressed health care system (n = 5) and socio-economic-related factors (n = 13). Conclusion There is a noticeable shift in the literature

  3. A review of the effect of tooth bleaching agents on oral microbes%牙齿美白剂对口腔微生物影响的研究进展

    Institute of Scientific and Technical Information of China (English)

    张博; 霍思蓓; 刘诗雨; 李明云

    2016-01-01

    牙齿美白剂中含有强氧化剂,可产生有效的漂白作用,是牙齿美白剂的主要组成部分.牙齿美白剂是否会增加龋易感性是众多研究者一直关注的问题.因此,本文针对美白剂对口腔致龋微生物浮游状态生长及生物膜形成的影响进行综述,以期为今后相关研究提供参考.%Tooth bleaching agents contain powerful oxidizing agents,which serve as the main part of bleaching agents because of its release of effective bleaching component.It has been a hot topic whether tooth bleaching agents exert negative influence on oral health.In order to provide train of thoughts and reference for further clinical researches and treatments,this review paper focuses on bleaching agents' effects on the growth of oral microbes and the formation of biofilms.

  4. Oral candidiasis.

    Science.gov (United States)

    Millsop, Jillian W; Fazel, Nasim

    2016-01-01

    Oral candidiasis (OC) is a common fungal disease encountered in dermatology, most commonly caused by an overgrowth of Candida albicans in the mouth. Although thrush is a well-recognized presentation of OC, it behooves clinicians to be aware of the many other presentations of this disease and how to accurately diagnose and manage these cases. The clinical presentations of OC can be broadly classified as white or erythematous candidiasis, with various subtypes in each category. The treatments include appropriate oral hygiene, topical agents, and systemic medications. This review focuses on the various clinical presentations of OC and treatment options.

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

    Institute of Scientific and Technical Information of China (English)

    辛海莉; 蔡雯雯; 郭蔚

    2007-01-01

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

  6. Nano-ZnO/ZnO-HAPw prepared via sol-gel method and antibacterial activities of inorganic agents on six bacteria associated with oral infections

    Science.gov (United States)

    Jin, Jianfeng; Liu, Wenying; Zhang, Wenyun; Chen, Qinghua; Yuan, Yanbo; Yang, Lidou; Wang, Qintao

    2014-10-01

    The antibacterial activity of zinc oxide (ZnO) and the strengthening of hydroxylapatite whiskers (HAPws) have been widely studied and applied. However, the antibacterial properties of ZnO-HAPws have scarcely been researched. The aim of this study was to further investigate several types of nano-ZnO morphologies of ZnO-HAPws that were prepared using the sol-gel method at different pondus hydrogenii (pH) values and temperatures. The four morphologies of ZnO-HAPws that were investigated here were granule, triangle, short rod and disc type, and these morphologies were investigated at 70 °C at pH 6.4, 37 °C at pH 6.6, 70 °C at pH 6.6 and 70 °C at pH 6.6, respectively. Next, the antibacterial activity of ZnO-HAPw was compared to that of nano-ZnO, commercially available ZnO and tetrapod-like ZnO whiskers (T-ZnOw) with six bacteria that are associated with oral infections: Streptococcus mutans, Lactobacillus casei, Candida albicans, Actinomyces viscosus, Staphylococcus aureus and Escherichia coli. The results of examinations of the minimal inhibitory concentrations (MICs) and minimal bactericidal concentrations (MBCs) showed that the antibacterial activity of ZnO-HAPw exceeded that of the commercially available ZnO and T-ZnOw. Additionally, analysis of variance (ANOVA) analysis of the MBCs revealed that the four tested antibacterial agents had significantly different effects on S. mutans ( F = 8.940; P = 0.006), S. aureus ( F = 6.924; P = 0.013) and E. coli ( F = 4.468; P = 0.04). ANOVA analyses of the MICs revealed that the four tested antibacterial agents had significantly different effects on S. mutans ( F = 6.183; P = 0.018), A. viscosus ( F = 4.531; P = 0.039) and S. aureus ( F = 18.976; P = 0.001).

  7. Diagnostic accuracy of small intestine ultrasonography using an oral contrast agent in Crohn's disease: Comparative study from the UK

    Energy Technology Data Exchange (ETDEWEB)

    Chatu, S., E-mail: schatu@hotmail.com [Department of Gastroenterology, St George' s Hospital NHS Trust, London (United Kingdom); Pilcher, J. [Department of Radiology, St George' s Hospital NHS Trust, London (United Kingdom); Saxena, S.K. [Department of Primary Care and Public Health Imperial College, London (United Kingdom); Fry, D.H. [P.N. Lee Statistics and Computing Ltd, Sutton (United Kingdom); Pollok, R.C.G. [Department of Gastroenterology, St George' s Hospital NHS Trust, London (United Kingdom)

    2012-06-15

    Aim: To evaluate the usefulness of small intestine contrast-enhanced ultrasonography (SICUS) using an oral contrast agent in routine clinical practice by assessing the level of agreement with the established techniques, small bowel follow-through (SBFT) and computed tomography (CT), and diagnostic accuracy compared with the final diagnosis in the detection of small bowel Crohn's disease (CD) and luminal complications in a regional centre. Materials and methods: All symptomatic known or suspected cases of CD who underwent SICUS were retrospectively reviewed. The level of agreement between SICUS and SBFT, CT, histological findings, and C-reactive protein (CRP) level was assessed using kappa ({kappa}) coefficient. Sensitivity was demonstrated using the final diagnosis as the reference standard defined by the outcome of clinical assessment, follow-up, and results of investigations other than SICUS. Results: One hundred and forty-three patients underwent SICUS of these 79 (55%) were female. Eighty-six (60%) were known to have CD and 57 (40%) had symptoms suggestive of intestinal disease with no previous diagnosis. Forty-six (55%) of the known CD patients had had at least one previous surgical resection. The sensitivity of SICUS in detecting active small bowel CD in known CD and undiagnosed cases was 93%. The kappa coefficient was 0.88 and 0.91 with SBFT and CT, respectively. SICUS detected nine patients who had one or more small bowel strictures and six patients with a fistula all detected by SBFT or CT. Conclusion: SICUS is not only comparable to SBFT and CT but avoids radiation exposure and should be more widely adopted in the UK as a primary diagnostic procedure and to monitor disease complications in patients with CD.

  8. Melatonin as a pro-osteogenic agent in oral implantology: a systematic review of histomorphometric outcomes in animals and quality evaluation using ARRIVE guidelines.

    Science.gov (United States)

    Arora, H; Ivanovski, S

    2017-04-01

    The aim of this review was to evaluate the outcomes of preclinical trials that assessed the use of melatonin as a pro-osteogenic agent in the field of oral implantology. Melatonin is a hormone that has been shown to have beneficial antioxidant and bone-metabolic effects. A number of experimental studies have analysed its effect in promoting osseointegration around dental implants in animals. A bibliographic search in PubMed, Scopus and EBSCOhost was performed. Animal studies that quantitatively analysed the pro-osteogenic effect of melatonin were included. Quality assessment of the included studies was performed using the ARRIVE guidelines. Eight studies met the inclusion criteria. The experimental animals used were dogs, rabbits and rats. Melatonin was used in a lyophilized powdered form, an injectable form or as a dipping solution. Six of the eight studies included showed a statistically significant positive effect of melatonin on bone-implant contact and various other histomorphometric parameters. The ARRIVE criteria were generally well reported by the included studies (17.5 ± 1.60/24), although several criteria (including randomization and blinding) were poorly documented, with most of the studies showing a high/unclear risk of bias. The majority of the studies included showed a statistically significant positive effect of melatonin on bone formation around implants. However, the clinical significance of this effect was unclear given the high/unclear risk of bias in the majority of included studies. Given the limited amount of data available, further research should be conducted to evaluate the clinical potential of this pineal hormone in clinically relevant situations, such as compromised sites or patients. © 2016 John Wiley & Sons A/S. Published by John Wiley & Sons Ltd.

  9. In vitro callus and in vivo leaf extract of Gymnema sylvestre stimulate β-cells regeneration and anti-diabetic activity in Wistar rats.

    Science.gov (United States)

    Ahmed, A Bakrudeen Ali; Rao, A S; Rao, M V

    2010-11-01

    A methanol extract of Gymnema sylvestre leaf and callus showed anti-diabetic activities through regenerating β-cells. Optimum callus was developed under stress conditions of blue light with 2,4-D (1.5 mg/l) and KN (0.5 mg/l), which induced maximum biomass of green compact callus at 45 days, as determined by growth curve analysis. Leaf and optimum callus extracts contains gymnemic acid, which was analyzed using TLC, HPTLC and HPLC methods. The research reported here deals with leaf and callus extracts of G. sylvestre, which significantly increase the weight of the whole body, liver, pancreas and liver glycogen content in alloxan-induced diabetic rats (Wistar rats). The gymnemic acid of leaf and callus extracts significantly increases the regeneration of β-cells in treated rats, when compared with the standard diabetic rats. It could have potential as a pharmaceutical drug for insulin-dependent diabetes mellitus (IDDM).

  10. Anti-diabetic effects of cinnamaldehyde and berberine and their impacts on retinol-binding protein 4 expression in rats with type 2 diabetes mellitus

    Institute of Scientific and Technical Information of China (English)

    ZHANG Wei; XU Ya-cheng; GUO Fang-jian; MENG Ye; LI Ming-li

    2008-01-01

    Background Retinol binding protein 4 (RBP4),as an adipocyte secreted cytokine,was recently found to be inversely correlated with expression of glucose transporter 4 (GLUT4) in insulin resistance (IR) state and to have an intimate relationship with IR and type 2 diabetes mellitus (T2DM).The present study aimed to evaluate the anti-diabetic efficacy of cinnamaldehyde (tin),berberine (Bet),and metformin (Met) as well as their impacts on the RBP4-GLUT4 system.Methods Rat models of T2DM were established by combination of intraperitoneal injection of low-dose streptozotocin and high fat diet induction.Rats were divided into five groups:the control group,the diabetes group,the diabetes+Ber group,the diabetes+Cin group,and the diabetes+Met group.Western blotting was used to detect the serum or tissue RBP4 and GLUT4 protein levels.Results After treatment for four weeks,both Cin and Ber displayed significant hypolipidemic,hypoglycemic,and insulin sensitizing functions (P<0.01) compared with the control group.Their effects on lowering fasting plasma glucose (FPG),low density lipoprotein-cholesterol (LDL-C) and homeostasis model assessment of insulin resistance (HOMA-IR) seem even better than that of Met.Cin and Bet markedly lowered serum RBP4 levels and up-regulated the expression of tissue GLUT4 protein,and Cin seemed more notable in affecting these two proteins.Conclusions Both Cin and Ber display an exciting anti-diabetic efficacy in this study and may be of great value for the treatment of type 2 diabetes.Their mechanisms involve the RBP4-GLUT4 system,during which the serum RBP4 levels are lowered and the expression of tissue GLUT4 protein is up-regulated.

  11. 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。

  12. Anti-proliferative activity of oral anti-hyperglycemic agents on human vascular smooth muscle cells: thiazolidinediones (glitazones have enhanced activity under high glucose conditions

    Directory of Open Access Journals (Sweden)

    de Dios Stephanie T

    2007-10-01

    Full Text Available Abstract Background Inhibition of vascular smooth muscle cell (vSMC proliferation by oral anti-hyperglycemic agents may have a role to play in the amelioration of vascular disease in diabetes. Thiazolidinediones (TZDs inhibit vSMC proliferation but it has been reported that they anomalously stimulate [3H]-thymidine incorporation. We investigated three TZDs, two biguanides and two sulfonylureas for their ability of inhibit vSMC proliferation. People with diabetes obviously have fluctuating blood glucose levels thus we determined the effect of media glucose concentration on the inhibitory activity of TZDs in a vSMC preparation that grew considerably more rapidly under high glucose conditions. We further explored the mechanisms by which TZDs increase [3H]-thymidine incorporation. Methods VSMC proliferation was investigated by [3H]-thymidine incorporation into DNA and cell counting. Activation and inhibition of thymidine kinase utilized short term [3H]-thymidine uptake. Cell cycle events were analyzed by FACS. Results VSMC cells grown for 3 days in DMEM with 5% fetal calf serum under low (5 mM glucose and high (25 mM glucose increased in number by 2.5 and 4.7 fold, respectively. Rosiglitazone and pioglitazone showed modest but statistically significantly greater inhibitory activity under high versus low glucose conditions (P 3H]-thymidine into DNA but did not increase cell numbers. Troglitazone inhibited serum mediated thymidine kinase induction in a concentration dependent manner. FACS analysis showed that troglitazone and rosiglitazone but not pioglitazone placed a slightly higher percentage of cells in the S phase of a growing culture. Of the biguanides, metformin had no effect on proliferation assessed as [3H]-thymidine incorporation or cell numbers whereas phenformin was inhibitory in both assays albeit at high concentrations. The sulfonylureas chlorpropamide and gliclazide had no inhibitory effect on vSMC proliferation assessed by either [3H

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

    Directory of Open Access Journals (Sweden)

    Cárdenas-Elizalde MR

    2012-03-01

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

  14. 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

  15. Safety test of a supplement, 5-aminolevulinic acid phosphate with sodium ferrous citrate, in diabetic patients treated with oral hypoglycemic agents

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    Naohide Yamashita

    2014-09-01

    Full Text Available Objective: This study aimed to examine the safety of 5-aminolevulinic acid phosphate (5-ALA with sodium ferrous citrate (SFC in diabetic patients treated with one or more oral hypoglycemic agents (OHAs. Background: Recent intervention studies performed in the USA and Japan have shown that a nutritional supplement of 5-ALA with SFC efficiently reduced blood glucose levels in pre-diabetic population without any adverse events. Thus, it was anticipated that 5-ALA with SFC may potentially be taken as a beneficial supplement by diabetic patients who were being treated with OHA therapy. Nevertheless, it is important to examine its safety and efficacy in diabetic population. Methods: This study was a prospective single-blinded, randomized, placebo-controlled and parallel-group comparison study. Medically treated diabetic patients between the ages of 30 and 75 were recruited from the Tokyo metropolitan area of Japan and 45 subjects were selected after screening. These subjects were randomly assigned to three groups: daily intake of 15mg 5-ALA, 50mg 5-ALA, and a placebo (n=15, respectively. The supplement or placebo was administered for 12 weeks followed by a four week washout period. The primary endpoint was safety and occurrence of hypoglycemic attack, while the secondary endpoint was changes of fasting blood glucose (FBG and hemoglobin A1c (HbA1c. Results: Adverse events related to 5-ALA with SFC were not observed in all the groups. Abnormalities in blood and urine tests were not observed either. Significant decrease in FBG was not detected in all the groups. However, there was a small but significant decrease in HbA1c at 4 and 8 week in the 15 mg 5-ALA group. Significant decrease in HbA1c was not observed in the 50 mg 5-ALA group, although a tendency to decrease after 4 weeks was apparent. Conclusion: 5-ALA with SFC is a safe and potentially beneficial supplement if taken by diabetic patients treated with OHAs.

  16. Oral Carcinogenesis and Oral Cancer Chemoprevention: A Review

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    Takuji Tanaka

    2011-01-01

    Full Text Available Oral cancer is one of the major global threats to public health. The development of oral cancer is a tobacco-related multistep and multifocal process involving field cancerization and carcinogenesis. The rationale for molecular-targeted prevention of oral cancer is promising. Biomarkers of genomic instability, including aneuploidy and allelic imbalance, are possible to measure the cancer risk of oral premalignancies. Understanding of the biology of oral carcinogenesis will yield important advances for detecting high-risk patients, monitoring preventive interventions, and assessing cancer risk and pharmacogenomics. In addition, novel chemopreventive agents based on molecular mechanisms and targets against oral cancers will be derived from studies using appropriate animal carcinogenesis models. New approaches, such as molecular-targeted agents and agent combinations in high-risk oral individuals, are undoubtedly needed to reduce the devastating worldwide consequences of oral malignancy.

  17. Concentração de sódio e glicose em soro de reidratação oral preparado por Agentes Comunitários de Saúde Sodium and glucose concentration in therapeutical solution for oral rehydration prepared by Community Health Agents

    Directory of Open Access Journals (Sweden)

    Liliane Fernandes do Carmo

    2012-02-01

    Full Text Available A diarreia infantil é importante causa de morbimortalidade, sendo indicativo para terapia de reidratação oral (TRO. Este estudo objetivou avaliar o teor de sódio e glicose em soro de reidratação oral preparado por Agentes Comunitários de Saúde (ACS que atuam em Unidades Básicas de Saúde (UBS, caracterizando o perfil e o conhecimento destes sobre a TRO. Após responderem questionário com informações profissionais e sobre a TRO, os ACS a prepararam por três métodos. O teor de glicose e de sódio das TRO foi determinado e comparado ao proposto pela OMS. Na análise estatística foram utilizados ANOVA, Tukey e odds ratio. Participaram do estudo 52 ACS, majoritariamente mulheres e com ensino médio completo (90,4%. A adequação da TRO foi de 3,9; 9,8 e 28,9% para a colher caseira, colher medida e punhado pitada, respectivamente. O preparo da TRO com a colher caseira resultou em 88,0% das amostras com teor de sódio perigoso à saúde (>101 mmol/L. Entre os ACS, 38,5% tinham menos de 2 anos de trabalho, com risco 4,8 vezes maior de preparar TRO inadequada em sódio. Os ACS referiram indicar a TRO no tratamento da diarreia infantil, desconhecendo efeitos colaterais do preparo inadequado. A composição da TRO produzida pelos ACS foi inadequada em todos os métodos. É recomendável treinamento dos ACS no preparo da TRO.Infant Diarrhea is a major cause of morbidity and mortality in children and oral rehydration therapy (ORT is required. This study evaluates the composition of ORT prepared by Community Health Agents (CHAs working in Basic Health Units, assessing their profile and knowledge about ORT. After the CHAs answer specific questions, they are invited to prepare ORT using three methods. Glucose and sodium levels were then quantified and compared with WHO recommendations. ANOVA, Tukey and odds ratio were used for statistical analysis. 52 CHAs participated, mainly females, and 90.4% with full high school education. The adequacy of

  18. Connectivity maps for biosimilar drug discovery in venoms: the case of Gila monster venom and the anti-diabetes drug Byetta®.

    Science.gov (United States)

    Aramadhaka, Lavakumar Reddy; Prorock, Alyson; Dragulev, Bojan; Bao, Yongde; Fox, Jay W

    2013-07-01

    instances and negative correlation with 868 instances. Interestingly, the Gila monster venom and Byetta(®) both showed positive correlation with the anti-diabetic drugs troglitazone, of the thiazolidinedione class, and metformin, of the biguanide class, although Byetta(®) as a glucagon-like peptide-1 (GLP-1) agonist functions in a different manner than either of these two classes of anti-diabetic drugs. In summary, despite the fact that Gila monster venom contains a mixture of biologically active molecules, similarities in terms of perturbation of gene expression profiles on MCF7 cells were observed between the venom and the drug Byetta(®). Furthermore, using Connectivity Mapping the Gila monster venom was demonstrated to have nodes of positive correlation to several anti-diabetic drugs two of which were the same as observed with Byetta(®). Therefore, this study suggests that by using this approach novel drug activities heretofore unconsidered may be discovered in venoms using informatic tools and Connectivity Mapping. Copyright © 2013 Elsevier Ltd. All rights reserved.

  19. Anti-diabetic activity of the chloroform extract of Senecio mikanioides Otto in streptozotocin induced diabetic rats

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    Hanan S. M. Marzouk

    2011-08-01

    Full Text Available Objective: In this study, we examined the effect of oral administration of the chloroform extract of Senecio mikanioides Otto for a period of 30 days at doses of 100, 300 or 500 mg/kg body weight/day on streptozotocin induced diabetic rats. Methods: Male Sprague-Dawley rats were divided into five groups and classified into; extract treatment group received 100, 300 or 500 mg/kg body weight per day by oral gavage for 30 days; diabetic group administered intraperitoneally a single dose (75 mg/kg body weight of streptozotocin (STZ; diabetic rats plus tolbutamide group where diabetic rats received the standard hypoglycemic drug tolbutamide (100 mg/kg body weight per day by oral gavage for 30 days; diabetic rats plus extract group where diabetic rats received the extract (same doses by gavage for 30 days; as well as a normal group for comparison. In all of these groups, the levels of glucose and insulin were checked in blood, while the levels of reduced glutathione (GSH, nitric oxide (NO, lipid peroxidation (TBARS and thioredoxin reductase (TrxR activity were measured in pancreatic tissues. Results: The results revealed that STZ administration resulted in significant elevation in the level of both TBARS and NO with depletion in the level of GSH as compared with control accompanied with hyperglycemia, hypo-insulinemia and low insulin sensitivity. Moreover, the activity of pancreatic TrxR was lower than the control group. Feeding the diabetic rats for 30 days with the extract normalizes the previous biochemical parameters in dose dependent manner reaching near the tolbutamide treated group at the highest dose. Conclusion: The chloroform extract of Senecio mikanioides Otto exhibited antidiabetic activity and it corrected the insulin level and its sensitivity in experimentally induced diabetic rats in dose dependent manner. The current results clearly indicated the beneficial effects of the chloroform extract of Senecio mikanioides Otto in both

  20. Maintaining a Physiological Blood Glucose Level with ‘Glucolevel’, a Combination of Four Anti-Diabetes Plants Used in the Traditional Arab Herbal Medicine

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    Omar Said

    2008-01-01

    Full Text Available Safety and anti-diabetic effects of Glucolevel, a mixture of dry extract of leaves of the Juglans regia L, Olea europea L, Urtica dioica L and Atriplex halimus L were evaluated using in vivo and in vitro test systems. No sign of toxic effects (using LDH assay were seen in cultured human fibroblasts treated with increasing concentrations of Glucolevel. Similar observations were seen in vivo studies using rats (LD50: 25 g/kg. Anti-diabetic effects were evidenced by the augmentation of glucose uptake by yeast cells (2-folds higher and by inhibition of glucose intestinal absorption (∼49% in a rat gut-segment. Furthermore, treatment with Glucolevel of Streptozotocin-induced diabetic rats for 2–3 weeks showed a significant reduction in glucose levels [above 400 ± 50 mg/dl to 210 ± 22 mg/dl (P < 0.001] and significantly improved sugar uptake during the glucose tolerance test, compared with positive control. In addition, glucose levels were tested in sixteen human volunteers, with the recent onset of type 2 diabetes mellitus, who received Glucolevel tablets 1 × 3 daily for a period of 4 weeks. Within the first week of Glucolevel consumption, baseline glucose levels were significantly reduced from 290 ± 40 to 210 ± 20 mg/dl. At baseline, a subgroup of eleven of these subjects had glucose levels below 300 mg% and the other subgroup had levels ≥ 300 mg%. Clinically acceptable glucose levels were achieved during the 2–3 weeks of therapy in the former subgroup and during the 4th week of therapy in the latter subgroup. No side effect was reported. In addition, a significant reduction in hemoglobin A1C values (8.2 ± 1.03 to 6.9 ± 0.94 was found in six patients treated with Glucolevel. Results demonstrate safety, tolerability and efficacy of herbal combinations of four plants that seem to act differently but synergistically to regulate glucose-homeostasis.

  1. 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.

  2. 吉非罗齐对临床几种常用口服降糖药的作用%Effects of Gemfibrozil on several commonly used oral hypoglycemic agents

    Institute of Scientific and Technical Information of China (English)

    淡海丽; 易飞

    2011-01-01

    Drug interactions, particularly the studies of interaction between pharmacokinetics become a hot spot in recent years.Gemfibrozil is a lipid-lowering drugs commonly used in clinical, and there are many opportunities hyperlipidemia be in diabetes clinical situation, so whether there are interactions between gemfibrozil and oral agents should also be the concern of clinicians.We review the effect of Gemfibrozil to the pharmacokinetics and pharmacodynamics of several commonly used oral hypoglycemic drug, and to analyze its mechanism.Gemfibrozil inhibited CYP2C and significant effect the pharmacokinetics and pharmacodynamics of oral hypoglycemic drug, so monitoring the blood glucose concentrations in time or adjust the dosage of oral hypoglycemic agents when they are combined in clinical is necessary.%药物相互作用,尤其是药代学的相互作用的研究近年来成为热点.吉非罗齐是一个临床常用的降脂药物,而在临床高脂血症合并糖尿病情况较多,所以吉非罗齐与口服降糖药合用后是否有相互作用也应该是临床医生的关注点.本文综述吉非罗齐对临床几种常用口服降糖药的药代学和药效学的影响,及从其机制上予以分析.吉非罗齐通过对CYP2C的抑制作用而明显影响口服降糖药的药代学及药效学,所以在临床上合用时需及时监测血糖的浓度或调整口服降糖药的用量.

  3. Anti-diabetic effect of amorphastilbol through PPARα/γ dual activation in db/db mice

    Energy Technology Data Exchange (ETDEWEB)

    Lee, Woojung; Ham, Jungyeob; Kwon, Hak Cheol [Natural Medicine Center, KIST Gangneung Institute, Gangneung 210-340 (Korea, Republic of); Kim, Yong Kee, E-mail: yksnbk@sookmyung.ac.kr [College of Pharmacy, Sookmyung Women’s University, Seoul 140-742 (Korea, Republic of); Kim, Su-Nam, E-mail: snkim@kist.re.kr [Natural Medicine Center, KIST Gangneung Institute, Gangneung 210-340 (Korea, Republic of)

    2013-03-01

    Highlights: ► Amorphastilbol stimulates the transcriptional activities of both PPARα and PPARγ. ► Amorphastilbol improves glucose and lipid impairment in db/db mice. ► There are no side effects, such as hepatomegaly, in amorphastilbol-treated mice. ► Amorphastilbol can be used as a potential therapeutic agent against T2DM. - Abstract: Peroxisome proliferator-activated receptors (PPARs) have been considered as desirable targets for metabolic syndrome treatments, even though their specific agonists have several side effects, including body weight gain, edema, and tissue failure. The effects of amorphastilbol (APH) on glucose- and lipid metabolism were investigated with in vitro 3T3-L1 adipocyte systems and in vivo db/db mice model. APH selectively stimulates the transcriptional activities of both PPARα and PPARγ, which are able to enhance fatty acid oxidation and glucose utilization. Furthermore, APH improves glucose and lipid impairment in db/db mice. More importantly, there are no significant side effects, such as weight gain or hepatomegaly, in APH-treated animals, implying that APH do not adversely affect liver or lipid metabolism. All our data suggest that APH can be used as potential therapeutic agents against type 2 diabetes and related metabolic disorders, including obesity, by enhancing glucose and lipid metabolism.

  4. Anti-Diabetic Effects of an Ethanol Extract of Cassia Abbreviata Stem Bark on Diabetic Rats and Possible Mechanism of Its Action - Anti-diabetic Properties of Cassia abbreviata -

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    Keagile Bati

    2017-03-01

    Full Text Available Objectives: This study aimed to evaluate the hypoglycemic effects of an ethanol extract of Cassia abbreviata (ECA bark and the possible mechanisms of its action in diabetic albino rats. Methods: ECA was prepared by soaking the powdered plant material in 70% ethanol. It was filtered and made solvent-free by evaporation on a rotary evaporator. Type 2 diabetes was induced in albino rats by injecting 35 mg/kg body weight (bw of streptozotocin after having fed the rats a high-fat diet for 2 weeks. Diabetic rats were divided into ECA-150, ECA-300 and Metformin (MET-180 groups, where the numbers are the doses in mg.kg.bw administered to the groups. Normal (NC and diabetic (DC controls were given distilled water. The animals had their fasting blood glucose levels and body weights determined every 7 days for 21 days. Oral glucose tolerance tests (OGTTs were carried out in all animals at the beginning and the end of the experiment. Liver and kidney samples were harvested for glucose 6 phosphatase (G6Pase and hexokinase activity analyses. Small intestines and diaphragms from normal rats were used for α-glucosidase and glucose uptake studies against the extract. Results: Two doses, 150 and 300 mg/kg bw, significantly reduced the fasting blood glucose levels in diabetic rats and helped them maintain normal body weights. The glucose level in DC rats significantly increased while their body weights decreased. The 150 mg/kg bw dose significantly increased hexokinase and decreased G6Pase activities in the liver and the kidneys. ECA inhibited α-glucosidase activity and promoted glucose uptake in the rats’ hemi-diaphragms. Conclusion: This study revealed that ECA normalized blood glucose levels and body weights in type 2 diabetic rats. The normalization of the glucose levels may possibly be due to inhibition of α-glucosidase, decreased G6Pase activity, increased hexokinase activity and improved glucose uptake by muscle tissues.

  5. The complete control of glucose level utilizing the composition of ketogenic diet with the gluconeogenesis inhibitor, the anti-diabetic drug metformin, as a potential anti-cancer therapy.

    Science.gov (United States)

    Oleksyszyn, Józef

    2011-08-01

    In the animal models of glucose dependent cancer growth, the growth is decreased 15-30% through the use of low-carbohydrate, calorically restricted and/or ketogenic diet. The remaining growth depends on glucose formed by the liver-kidney gluconeogenesis as is the case in the cancer cachexia. It is hypothesized that a new treatment for cancer diseases should be explored which includes the ketogenic diet combined with the inhibition of gluconeogenesis by the anti-diabetic drug metformin.

  6. Sitagliptin, An Anti-diabetic Drug, Suppresses Estrogen Deficiency-Induced OsteoporosisIn Vivo and Inhibits RANKL-Induced Osteoclast Formation and Bone Resorption In Vitro

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    Chuandong Wang

    2017-06-01

    Full Text Available Postmenopausal osteoporosis is a disease characterized by excessive osteoclastic bone resorption. Some anti-diabetic drugs were demonstrated for anti-osteoclastic bone-loss effects. The present study investigated the skeletal effects of chronic administration of sitagliptin, a dipeptidyl peptidase IV (DPP IV inhibitor that is increasingly used for type 2 diabetes treatments, in an estrogen deficiency-induced osteoporosis and elucidated the associated mechanisms. This study indicated that sitagliptin effectively prevented ovariectomy-induced bone loss and reduced osteoclast numbers in vivo. It was also indicated that sitagliptin suppressed receptor activator of nuclear factor-κB ligand (RANKL-mediated osteoclast differentiation, bone resorption, and F-actin ring formation in a manner of dose-dependence. In addition, sitagliptin significantly reduced the expression of osteoclast-specific markers in mouse bone-marrow-derived macrophages, including calcitonin receptor (Calcr, dendrite cell-specific transmembrane protein (Dc-stamp, c-Fos, and nuclear factor of activated T-cells cytoplasmic 1 (Nfatc1. Further study indicated that sitagliptin inhibited osteoclastogenesis by suppressing AKT and ERK signaling pathways, scavenging ROS activity, and suppressing the Ca2+ oscillation that consequently affects the expression and/or activity of the osteoclast-specific transcription factors, c-Fos and NFATc1. Collectively, these findings suggest that sitagliptin possesses beneficial effects on bone and the suppression of osteoclast number implies that the effect is exerted directly on osteoclastogenesis.

  7. Fermentation of Green Tea with 2% Aquilariae lignum Increases the Anti-Diabetic Activity of Green Tea Aqueous Extracts in the High Fat-Fed Mouse

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    Ji Eun Lee

    2015-11-01

    Full Text Available Anti-diabetic effects on the metabolomic differences between green tea (GT and Aquilariae lignum-fermented green tea (fGT were investigated in the high fat-fed mouse. To prove the differences, hypoglycemic (blood glucose, insulin and glycated hemoglobin levels, pancreas weights and histopathological-immunohistochemistrical analysis of pancreas–insulin/glucagon cells, hepato- and nephron-protective (the changes in liver and kidney weight, histopathology of liver and kidney, serum aminotransferases (AST and ALT levels, blood urea nitrogen, and serum creatinine levels, and hypolipidemic (the changes of serum total cholesterol, triglyceride, low- and high-density lipoprotein levels with fecal total cholesterol (TC and triglyceride (TG contents effects were evaluated. In addition, liver lipid peroxidation, the glutathione contents, and catalase and superoxide dismutase activities were measured according to the hepatic glucose-regulating enzyme activities of glucokinase (GK, glucose-6-phosphatase (G6pase and phosphoenolpyruvate carboxykinase (PEPCK for action mechanisms. As a result, fGT showed a stronger hypoglycemic, hepato- and nephron-protective, hypolipidemic, and anti-oxidant effect than GT in high fat-fed mice. In addition, fGT-treated mice exerted more favorable inhibitory activities against GK, G6pase, PERCK activities as compared to GT-treated mice. Taken together, fGT fermented with Aquilariae lignum, 1:49 (2%; g/g has a stronger effect compared with GT. Therefore, fGT has the potential to increase bioactivity against type 2 diabetics.

  8. An in silico insight into novel therapeutic interaction of LTNF peptide-LT10 and design of structure based peptidomimetics for putative anti-diabetic activity.

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    Sonali Gopichand Chavan

    Full Text Available Lethal Toxin Neutralizing Factor (LTNF obtained from Opossum serum (Didephis virginiana is known to exhibit toxin-neutralizing activity for envenomation caused by animals, plants and bacteria. Small synthetic peptide- LT10 (10mer derived from N-terminal fraction of LTNF exhibit similar anti-lethal and anti-allergic property. In our in silico study, we identified Insulin Degrading Enzyme (IDE as a potential target of LT10 peptide followed by molecular docking and molecular dynamic (MD simulation studies which revealed relatively stable interaction of LT10 peptide with IDE. Moreover, their detailed interaction analyses dictate IDE-inhibitory interactions of LT10 peptide. This prediction of LT10 peptide as a novel putative IDE-inhibitor suggests its possible role in anti-diabetic treatment since IDE- inhibitors are known to assist treatment of Diabetes mellitus by enhancing insulin signalling. Furthermore, series of structure based peptidomimetics were designed from LT10 peptide and screened for their inhibitory interactions which ultimately led to a small set of peptidomimetic inhibitors of IDE. These peptidomimetic thus might provide a new class of IDE-inhibitors, those derived from LT10 peptide.

  9. Anti-diabetic effects of Caulerpa lentillifera:stimulation of insulin secretion in pancreatic β-cells and enhancement of glucose uptake in adipocytes

    Institute of Scientific and Technical Information of China (English)

    Bhesh; Raj; Sharma; Dong; Young; Rhyu

    2014-01-01

    Objective:To evaluate anti-diabetic effect of Caulrpa kntillifera(C.lentillifera).Methods:The inhibitory effect of C.lentillifera extract on dipeptidyl peptidase-IV and a-glucosidase enzyme was measured in a cell free system.Then,interleukin-1βand interferon-γinduced cell death and insulin secretion were measured in rat insulinoma(RIN)cells by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay and ELISA kit,respectively.Glucose uptake and glucose transporter expression were measured by fluorometry and western blotting,using 3T3-Ll adipocytes.Results:C.lentillifera extract significantly decreased dipeptidyl peptidase-IV and a-glucosidase enzyme activities,and effectively inhibited cell death and iNOS expression in interleukin-1βand interfcron-γinduced RIK cells.Furthermore,C.lntillifera extract significantly enhanced insulin secretion in RTN cells and glucose transporter expression and glucose uptake in 3T3-L1adipocytes.Conclusions:Thus,our results suggest that C.lentillifera could be used as a potential antidiabetic agenl.

  10. Anti-diabetic effects of hydroalcohlic juglans regia male flower extract on blood glucose level and on liver enzymes activity in intact and diabetogenized adult male rat

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    Seyyed Ebrahim Hosseini

    2012-08-01

    Full Text Available Background and Aim: Diabetes is a metabolic disorder resulting from defects in insulin secretion or function. Walnut is a nutrient used in traditional medicine to treat diabetes. In the current study, anti-diabetic effects of the Hydroalcoholic extract of walnut male flowers on diabetogenized rats by using Streptozocin were evaluated.   Materials and Methods: Seventy two adult male Wistar rats weighing 200-225 g each were randomly selected and divided into three main groups, i.e. control, diabetic, and non-diabetic(intact The control group included 8 rats (n=8. The diabetic and non-diabetic groups covered 32 rats each. Each of these groups were divided into four 8 rats including the control, diabetic, experimental 1, 2, and 3 which received 2, 4, or 6 g/kg of the extract per day for 15 days ,respectively. The three diabetic groups were each treated with the above doses of the extract, and the fourth group received no treatment. Diabetes was induced in diabetic rats through intraperitoneal injection of 60 mg/kg of Streptozotocin. At the end, blood samples were taken from the experimental and control groups and the serum levels of insulin and glucose were measured.   Results: A significant reduction in blood sugar and increase of insulin in diabetics receiving Hydroalcoholic extract of male flowers walnut was observed compared with non-diabetic ones.   Conclusion: Hydroalcoholic extract of male Walnut flowers, due to increasing insulin, causes reduction of blood sugar.

  11. Novel Small Molecule Agonist of TGR5 Possesses Anti-Diabetic Effects but Causes Gallbladder Filling in Mice.

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    Daniel A Briere

    Full Text Available Activation of TGR5 via bile acids or bile acid analogs leads to the release of glucagon-like peptide-1 (GLP-1 from intestine, increases energy expenditure in brown adipose tissue, and increases gallbladder filling with bile. Here, we present compound 18, a non-bile acid agonist of TGR5 that demonstrates robust GLP-1 secretion in a mouse enteroendocrine cell line yet weak GLP-1 secretion in a human enteroendocrine cell line. Acute administration of compound 18 to mice increased GLP-1 and peptide YY (PYY secretion, leading to a lowering of the glucose excursion in an oral glucose tolerance test (OGTT, while chronic administration led to weight loss. In addition, compound 18 showed a dose-dependent increase in gallbladder filling. Lastly, compound 18 failed to show similar pharmacological effects on GLP-1, PYY, and gallbladder filling in Tgr5 knockout mice. Together, these results demonstrate that compound 18 is a mouse-selective TGR5 agonist that induces GLP-1 and PYY secretion, and lowers the glucose excursion in an OGTT, but only at doses that simultaneously induce gallbladder filling. Overall, these data highlight the benefits and potential risks of using TGR5 agonists to treat diabetes and metabolic diseases.

  12. Interacción de los antineoplásicos orales con los alimentos: revisión sistemática Antineoplastic oral agents and drug-nutrient interactions: a sistematic review

    OpenAIRE

    N. V. Jiménez Torres; Romero Crespo, I.; Ballester Solaz, M.; A. Albert Marí; V. Jiménez Arenas

    2009-01-01

    Introducción: Los estudios de biodisponibilidad son parte integrante del desarrollo clínico de medicamentos para administración oral con el fin de identificar potenciales interacciones fármaco-alimento (iFA). Actualmente, para los antineoplásicos orales se empieza a reconocer su importancia clínica, aun cuando lamentablemente, la información disponible presenta variabilidad en su evidencia científica. Objetivos: Revisar la evidencia científica disponible sobre las interacciones de los aliment...

  13. Synthesis and Physicochemical Characterization of a Diethyl Ester Prodrug of DTPA and Its Investigation as an Oral Decorporation Agent in Rats.

    Science.gov (United States)

    Huckle, James E; Sadgrove, Matthew P; Leed, Marina G D; Yang, Yu-Tsai; Mumper, Russell J; Semelka, Richard C; Jay, Michael

    2016-07-01

    The increasing threats of nuclear terrorism have made the development of medical countermeasures a priority for international security. Injectable formulations of diethylenetriaminepentaacetic acid (DTPA) have been approved by the FDA; however, an oral formulation is more amenable in a mass casualty situation. Here, the diethyl ester of DTPA, named C2E2, is investigated for potential as an oral treatment for internal radionuclide contamination. C2E2 was synthesized and characterized using NMR, MS, and elemental analysis. The physiochemical properties of solubility, lipophilicity, and stability were investigated in order to predict its oral bioavailability. Finally, an animal efficacy study was conducted in Sprague Dawley rats pre-contaminated by intramuscular injection with (241)Am(NO3)3 to establish effectiveness of the therapy via the oral route. Synthesis of C2E2 yielded a crystalline powder with high solubility and improved lipophilicity over DTPA. The ester was stable in both simulated gastric and intestinal fluids over the anticipated time course of absorption. Capsules containing C2E2 were demonstrated to be stable for 12 months under accelerated stability conditions. After a single dose, C2E2 enhanced the elimination of (241)Am in a dose-dependent manner. Significant improvement was seen in both total (241)Am decorporation and reduction of (241)Am liver and skeletal burden. C2E2 was concluded to be effective when orally administered to (241)Am-contaminated rats. It may therefore have potential for medical countermeasure in treating humans contaminated with (241)Am or other transuranic elements. An oral capsule or powder for reconstitution may be suitable formulations for future development based on the physiochemical properties and anticipated dose required for efficacy.

  14. 沿海和内地两家医院口服降糖药利用分析%Analysis on the Durg Utilization of Oral Hypoglycaemic Agents in an Inland Hospital and a Coastal Hospital

    Institute of Scientific and Technical Information of China (English)

    莫斌斌; 符成海

    2001-01-01

    To get information about the status of use of oral hypoglycaemic agents in an inland and coastal hospitals,the ordes of total cost and DDDs were employed to compare the use of oral hypoglycaemic agents in an inland hospital and a coastal hospital.Our results showed that the much less biguanides were used in the coastal hospital as compared with the inland hospital.It is conclinical practice included dimethyl biguanide,glipizide,gliclazide and glibenclamide.%目的:了解口服降糖药在沿海和内地两家医院的用药情况。方法:应用总金额排序法及用药频度(DDDs)排序法对1998~1999年沿海和内地两家医院口服降糖药的利用情况进行比较分析。结果:沿海地区使用双胍类降糖药的患者远远少于内地。结论:沿海地区肥胖型糖尿病患者少于内地。二甲双胍、格列吡嗪、格列齐特、格列本脲等目前用药活跃,仍为主要降糖药。

  15. Anti-diabetic effects of lemon balm ( Melissa officinalis) essential oil on glucose- and lipid-regulating enzymes in type 2 diabetic mice.

    Science.gov (United States)

    Chung, Mi Ja; Cho, Sung-Yun; Bhuiyan, Muhammad Javidul Haque; Kim, Kyoung Heon; Lee, Sung-Joon

    2010-07-01

    The antioxidant activity of lemon balm (Melissa officinalis) essential oil (LBEO) on 2,2-diphenyl-1-picrylhydrazyl (DPPH) radicals and its hypoglycaemic effect in db/db mice were investigated. LBEO scavenged 97 % of DPPH radicals at a 270-fold dilution. Mice administered LBEO (0.015 mg/d) for 6 weeks showed significantly reduced blood glucose (65 %; P < 0.05) and TAG concentrations, improved glucose tolerance, as assessed by an oral glucose tolerance test, and significantly higher serum insulin levels, compared with the control group. The hypoglycaemic mechanism of LBEO was further explored via gene and protein expression analyses using RT-PCR and Western blotting, respectively. Among all glucose metabolism-related genes studied, hepatic glucokinase and GLUT4, as well as adipocyte GLUT4, PPAR-gamma, PPAR-alpha and SREBP-1c expression, were significantly up-regulated, whereas glucose-6-phosphatase and phosphoenolpyruvate carboxykinase expression was down-regulated in the livers of the LBEO group. The results further suggest that LBEO administered at low concentrations is an efficient hypoglycaemic agent, probably due to enhanced glucose uptake and metabolism in the liver and adipose tissue and the inhibition of gluconeogenesis in the liver.

  16. Incretin hormones and maturity onset diabetes of the young--pathophysiological implications and anti-diabetic treatment potential.

    Science.gov (United States)

    Østoft, Signe Harring

    2015-09-01

    Maturity onset diabetes of the young (MODY) designates monogenic forms of non-autoimmune diabetes characterised by autosomal dominant inheritance, non-insulin dependent diabetes at onset and diagnosis often before 25 years of age. MODY constitutes genetically and clinically heterogeneous forms of diabetes. More than 8 different genes are known to cause MODY, among which hepatocyte nuclear factor 1 alpha (HNF1A) (MODY3) and glucokinase (GCK) (MODY2) mutations are the most common. Both forms of MODY are characterised by specific beta cell dysfunction, with patients with HNF1A-diabetes having a reduced insulin secretory capacity, while patients with GCK-diabetes have a glucose-sensing defect, but preserved insulin secretory capacity. Patients with MODY are effectively treated with sulphonylurea (SU) due to very high sensitivity to these drugs, but they are also prone to develop hypoglycaemia. The objectives of this thesis were to study the pathophysiology of GCK-diabetes and HNF1A-diabetes by investigating the incretin effect, the physiological response to food ingestion and to estimate the treatment potential of a glucagon-like peptide-1 receptor agonist (GLP-1RA) in patients with HNF1A-diabetes. In Study I we investigated the incretin effect and the responses of islet hormones and incretin hormones to oral glucose tolerance test (OGTT) and isoglycaemic IV glucose infusion (IIGI) in patients with GCK-diabetes, in patients with HNF1A-diabetes, and in BMI and age matched healthy individuals (CTRLs). In Study II we investigated responses of islet hormones and incretin hormones to a more physiological stimulus consisting of a standardised meal test in patients with GCK-diabetes, in patients with HNF1A--diabetes, and in BMI and age matched CTRLs. In Study III we conducted a randomised, double-blind, crossover trial investigating the glucose lowering effect and risk of hypoglycaemia during 6 weeks of treatment with the GLP-1RA, liraglutide compared to the SU, glimepiride

  17. Anti-diabetic and anti-adipogenic effects of a novel selective 11β-hydroxysteroid dehydrogenase type 1 inhibitor, 2-(3-benzoyl)-4-hydroxy-1,1-dioxo-2H-1,2-benzothiazine-2-yl-1-phenylethanone (KR-66344).

    Science.gov (United States)

    Park, Ji Seon; Rhee, Sang Dal; Kang, Nam Sook; Jung, Won Hoon; Kim, Hee Youn; Kim, Jun Hyoung; Kang, Seung Kyu; Cheon, Hyae Gyeong; Ahn, Jin Hee; Kim, Ki Young

    2011-04-15

    The selective inhibitors of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) have considerable potential for treating type 2 diabetes mellitus and metabolic syndrome. In the present study, we investigated the anti-diabetic and anti-adipogenic effects of 2-(3-benzoyl)-4-hydroxy-1,1-dioxo-2H-1,2-benzothiazine-2-yl-1-phenylethanone (KR-66344), as a 11β-HSD1 inhibitor; we also investigated the underlying molecular mechanisms in the cortisone-induced 3T3-L1 adipogenesis model system and C57BL/6-Lep(ob/ob) mice. KR-66344 concentration-dependently inhibited 11β-HSD1 activity in human liver microsome, mouse C2C12 myotube and human SW982 cells. In the C57BL/6-Lep(ob/ob) mice study, the administration of KR-66344 (200mg/kg/d, orally for 5 days) improved the glucose intolerance as determined by the oral glucose tolerance test, in which the area under the curve (AUC) of the plasma glucose concentration was significantly reduced by 27% compared with the vehicle treated group. Further, KR-66344 suppressed adipocyte differentiation on cortisone-induced adipogenesis in 3T3-L1 cells is associated with the suppression of the cortisone-induced mRNA levels of FABP4, G3PD, PPARγ2 and Glut4, and 11β-HSD1 expression and activity. Our results additionally demonstrate evidence showing that KR-66344 improved glycemic control and inhibited adipogenesis via 11β-HSD1 enzyme activity. Taken together, these results may provide evidence of the therapeutic potential of KR-66344, as a 11β-HSD1 inhibitor, in obesity and type 2 diabetes patients with metabolic syndrome.

  18. Comparison of baseline characteristics and clinical course in Japanese patients with type 2 diabetes among whom different types of oral hypoglycemic agents were chosen by diabetes specialists as initial monotherapy (JDDM 42)

    Science.gov (United States)

    Fujihara, Kazuya; Igarashi, Risa; Matsunaga, Satoshi; Matsubayashi, Yasuhiro; Yamada, Takaho; Yokoyama, Hiroki; Tanaka, Shiro; Shimano, Hitoshi; Maegawa, Hiroshi; Yamazaki, Katsuya; Kawai, Koichi; Sone, Hirohito

    2017-01-01

    Abstract Little is known about the relationships between patient factors and the antihyperglycemic agents that have been prescribed as initial therapy by diabetes specialists for patients with type 2 diabetes. Moreover, there has been little clarification of the subsequent usage patterns and related factors that influenced the continuation or discontinuation of the drug or the addition of another drug. To provide information on these issues, we evaluated the clinical characteristics of Japanese patients with type 2 diabetes for whom different types of oral hypoglycemic agents (i.e., either sulfonylureas, biguanides, or DPP-4 inhibitors (DPP-4Is)) were chosen as initial monotherapy by diabetes specialists and evaluated subsequent usage patterns. Prescription data on 3 different antidiabetic agents from December 2009 to March 2015 from diabetes specialists’ patient registries were used to identify variables at baseline related to initial prescriptions; also, the addition of another hypoglycemic drug or discontinuation of the initial therapy was evaluated 1 year after the initial prescription. Analyzed were data on 2666 patients who received initial monotherapy with either a sulfonylurea (305 patients), biguanide (951 patients), or DPP-4I (1410 patients). Patients administered sulfonylureas were older, had a lower body mass index (BMI), longer duration of diabetes, and worse glycemic control than recipients of biguanides. Use of biguanides was related to younger age, short duration of diabetes, and obesity but was negatively associated with poor glycemic control. Older age but neither obesity nor poor glycemic control was associated with DPP-4Is. In all 3 groups a high HbA1c value was related to adding another hypoglycemic agent to the initial therapy. Moreover, adding another drug to a DPP-4I was related to a younger age and higher BMI. Patients’ age, duration of diabetes, obesity, and glycemic control at baseline influenced the choice of hypoglycemic agents

  19. Evaluation of fish oil-rich in MUFAs for anti-diabetic and anti-inflammation potential in experimental type 2 diabetic rats

    Science.gov (United States)

    Keapai, Waranya; Apichai, Sopida; Amornlerdpison, Doungporn

    2016-01-01

    The advantages of monounsaturated fatty acids (MUFAs) on insulin resistance and type 2 diabetes mellitus (T2DM) have been well established. However, the molecular mechanisms of the anti-diabetic action of MUFAs remain unclear. This study examined the anti-hyperglycemic effect and explored the molecular mechanisms involved in the actions of fish oil- rich in MUFAs that had been acquired from hybrid catfish (Pangasius larnaudii×Pangasianodon hypophthalmus) among experimental type 2 diabetic rats. Diabetic rats that were fed with fish oil (500 and 1,000 mg/kg BW) for 12 weeks significantly reduced the fasting plasma glucose levels without increasing the plasma insulin levels. The diminishing levels of plasma lipids and the muscle triglyceride accumulation as well as the plasma leptin levels were identified in T2DM rats, which had been administrated with fish oil. Notably, the plasma adiponectin levels increased among these rats. The fish oil supplementation also improved glucose tolerance, insulin sensitivity and pancreatic histological changes. Moreover, the supplementation of fish oil improved insulin signaling (p-AktSer473 and p-PKC-ζ/λThr410/403), p-AMPKThr172 and membrane GLUT4 protein expressions, whereas the protein expressions of pro-inflammatory cytokines (TNF-α and nuclear NF-κB) as well as p-PKC-θThr538 were down regulated in the skeletal muscle. These data indicate that the effects of fish oil-rich in MUFAs in these T2DM rats were partly due to the attenuation of insulin resistance and an improvement in the adipokine imbalance. The mechanisms of the anti-hyperglycemic effect are involved in the improvement of insulin signaling, AMPK activation, GLUT4 translocation and suppression of pro-inflammatory cytokine protein expressions. PMID:27847435

  20. Anti-Obesity and Anti-Diabetic Effects of Acacia Polyphenol in Obese Diabetic KKAy Mice Fed High-Fat Diet

    Directory of Open Access Journals (Sweden)

    Nobutomo Ikarashi

    2011-01-01

    Full Text Available Acacia polyphenol (AP extracted from the bark of the black wattle tree (Acacia meansii is rich in unique catechin-like flavan-3-ols, such as robinetinidol and fisetinidol. The present study investigated the anti-obesity/anti-diabetic effects of AP using obese diabetic KKAy mice. KKAy mice received either normal diet, high-fat diet or high-fat diet with additional AP for 7 weeks. After the end of administration, body weight, plasma glucose and insulin were measured. Furthermore, mRNA and protein expression of obesity/diabetic suppression-related genes were measured in skeletal muscle, liver and white adipose tissue. As a result, compared to the high-fat diet group, increases in body weight, plasma glucose and insulin were significantly suppressed for AP groups. Furthermore, compared to the high-fat diet group, mRNA expression of energy expenditure-related genes (PPARα, PPARδ, CPT1, ACO and UCP3 was significantly higher for AP groups in skeletal muscle. Protein expressions of CPT1, ACO and UCP3 for AP groups were also significantly higher when compared to the high-fat diet group. Moreover, AP lowered the expression of fat acid synthesis-related genes (SREBP-1c, ACC and FAS in the liver. AP also increased mRNA expression of adiponectin and decreased expression of TNF-α in white adipose tissue. In conclusion, the anti-obesity actions of AP are considered attributable to increased expression of energy expenditure-related genes in skeletal muscle, and decreased fatty acid synthesis and fat intake in the liver. These results suggest that AP is expected to be a useful plant extract for alleviating metabolic syndrome.

  1. Anti-diabetic drugs, insulin and metformin, have no direct interaction with hepatitis C virus infection or anti-viral interferon response

    Directory of Open Access Journals (Sweden)

    Mohamad S. Hakim

    2014-01-01

    Full Text Available Hepatitis C virus (HCV infection is associated with insulin resistance (IR and type 2 diabetes (T2D. Chronic HCV patients with IR and T2D appear to have a decreased response to the standard pegylated-interferon-alpha and ribavirin (PEG-IFN/RBV anti-viral therapy. Insulin and metformin are anti-diabetic drugs regularly used in the clinic. A previous in vitro study has shown a negative effect of insulin on interferon signaling. In the clinic, adding metformin to PEG-IFN/RBV therapy was reported to increase the response rate in chronic HCV patients and it has been suggested this effect derives from an improved anti-viral action of interferon. The goal of this study was to further investigate the molecular insight of insulin and metformin interaction with HCV infection and the anti-viral action of interferon. We used two cell culture models of HCV infection. One is a sub-genomic model that assays viral replication through luciferase reporter gene expression. The other one is a full-length infectious model derived from the JFH1 genotype 2a isolate. We found that both insulin and metformin do not affect HCV infection. Insulin and metformin also do not influence the anti-viral potency of interferon. In addition, there is no direct interaction between these two drugs and interferon signaling. Our results do not confirm the previous laboratory observation that insulin interferes with interferon signaling and suggest that classical nutritional signaling through mTOR may be not involved in HCV replication. If metformin indeed can increase the response rate to interferon therapy in patients, our data indicate that this could be mediated via an indirect mechanisms.

  2. Anti-diabetic properties of a non-conventional radical scavenger, as compared to pioglitazone and exendin-4, in streptozotocin-nicotinamide diabetic mice.

    Science.gov (United States)

    Novelli, Michela; Canistro, Donatella; Martano, Manuela; Funel, Niccola; Sapone, Andrea; Melega, Simone; Masini, Matilde; De Tata, Vincenzo; Pippa, Anna; Vecoli, Cecilia; Campani, Daniela; De Siena, Rocco; Soleti, Antonio; Paolini, Moreno; Masiello, Pellegrino

    2014-04-15

    We previously showed that the innovative radical scavenger bis(1-hydroxy-2,2,6,6-tetramethyl-4-piperidinyl)-decandioate (IAC) improves metabolic dysfunctions in a diabetic mouse model. Here, we compared the in vivo effects of IAC with those of the anti-diabetic drugs pioglitazone (PIO) and exendin-4 (EX-4). Diabetes was induced in C57Bl/6J mice by streptozotocin and nicotinamide administration. Paralleled by healthy controls, diabetic animals (D) were randomly assigned to four groups and treated daily for 7 consecutive weeks: D+saline, ip; D+IAC 30mg/kgb.w., ip; D+PIO 10mg/kgb.w. per os; and D+EX-4, 50μg/kgb.w., ip. Our results show that IAC reduced basal hyperglycemia and improved glucose tolerance better than PIO or EX-4. Interestingly, in the heart of diabetic mice, IAC treatment normalized the increased levels of GSSG/GSH ratio and thiobarbituric acid reactive substances, indexes of oxidative stress and damage, while PIO and EX-4 were less effective. As supported by immunohistochemical data, IAC markedly prevented diabetic islet β-cell reduced density, differently from PIO and EX-4 that had only a moderate effect. Interestingly, in diabetic animals, IAC treatment enhanced the activity of pancreatic-duodenal homeobox 1 (PDX-1), an oxidative stress-sensitive transcription factor essential for maintenance of β-cell function, as evaluated by quantification of its nuclear immunostaining, whereas PIO or EX-4 treatments did not. Altogether, these observations support the improvement of the general redox balance and β-cell function induced by IAC treatment in streptozotocin-nicotinamide diabetic mice. Furthermore, in this model, the correction of diabetic alterations was better obtained by treatment with the radical scavenger IAC than with pioglitazone or exendin-4.

  3. Anti-diabetic effects of ethanol extract of Bryonia laciniosa seeds and its saponins rich fraction in neonatally streptozotocin-induced diabetic rats

    Directory of Open Access Journals (Sweden)

    Sandip B Patel

    2015-01-01

    Full Text Available Context: Bryonia laciniosa Linn. (Cucurbitaceae seed is used in traditional medicine for a number of ailments including metabolic disorders. Aim: This study evaluated the anti-diabetic action of the ethanol extract of B. laciniosa seeds and saponin fraction of it through its effect on hyperglycemia, dyslipidaemia and oxidative stress in neonatally streptozotocin (n-STZ-induced diabetic rats (n-STZ diabetic rats. Materials and Methods: Ethanol extract (250 and 500 mg/kg; p.o., saponin fraction (100 and 200 mg/kg; p.o. and standard drug glibenclamide (3 mg/kg; p.o. were administered to diabetic rats when the rats were 6 weeks old and continued for 10 consecutive weeks. Effects of ethanol extract and saponin fraction on various biochemical parameters were studied in diabetic rats. Results: The treatment with ethanol extract and saponin fraction for 10 weeks decrease in the levels of glucose, triglycerides, cholesterol, high-density lipoprotein, low-density lipoprotein, very low-density lipoprotein, serum urea, serum creatinine and diminished activities of aspartate transaminase, and alanine transaminase. The anti-hyperglycemic nature of B. laciniosa is probably brought about by the extra- the pancreatic mechanism as evidenced from unchanged levels of plasma insulin. B. laciniosa modulated effect of diabetes on the liver malondialdehyde, reduced glutathione (GSH, superoxide dismutase (SOD, and catalase (CAT activity. Administration of ethanol extract and saponin fraction to diabetic rats showed a significant reversal of disturbed antioxidant status. Significant increase in SOD, CAT, and levels of GSH was observed in treated n-STZ diabetic rats. Conclusion: The present study reveals the efficacy of B. laciniosa seed extract and its saponin fraction in the amelioration of n-STZ diabetic rats.

  4. Treatment discontinuations with new oral agents for long-term anticoagulation: insights from a meta-analysis of 18 randomized trials including 101,801 patients.

    Science.gov (United States)

    Chatterjee, Saurav; Sardar, Partha; Giri, Jay S; Ghosh, Joydeep; Mukherjee, Debabrata

    2014-07-01

    To systematically examine discontinuation rates with new US Food and Drug Administration-approved oral anticoagulants (NOACs) in patients with various indications for long-term anticoagulation. Poor adherence to medications is considered a potential and frequent cause of treatment failure. We searched the PubMed, Cochrane Central Register of Controlled Trials, EMBASE, EBSCO, Web of Science, and CINAHL databases for articles published from January 1, 2001, through September 15, 2013. The following Medical Subject Heading terms and/or keywords were used for our database searches: rivaroxaban, dabigatran, apixaban, new oral anticoagulants, oral thrombin inhibitors, and oral factor Xa inhibitors. Articles in English that focused on randomized controlled trials (RCTs) comparing NOACs (apixaban, dabigatran, and rivaroxaban) with conventional therapy or placebo were abstracted. Independent extraction of relevant data was performed by 2 authors. The primary end point of interest was discontinuation due to all causes. Other end points of interest were discontinuation due to adverse events, consent withdrawal, and nonadherence. Eighteen RCTs including a total of 101,801 patients were included for analysis. Total study drug discontinuation rates were not statistically different with NOACs in comparison to pharmacologically active comparators for treatment of venous thromboembolism/pulmonary embolism (risk ratio [RR], 0.91; 95% CI, 0.74-1.13; P=.40) and for NOACs in comparison to warfarin and aspirin for prevention of stroke in patients with atrial fibrillation (RR, 1.01; 95% CI, 0.87-1.17; P=.92). In contrast, in acute coronary syndromes, total study drug discontinuation with NOACs was significantly higher than with placebo (RR, 1.40; 95% CI, 1.07-1.83; P=.01). Overall discontinuations were comparable to those with active comparators. Study drug discontinuations with NOACs were not significantly different from those with conventional drugs in treatment of venous

  5. Glycemic control and cost-effectiveness attained by the drug utilization of oral antidiabetic agents in a tertiary care hospital in South India

    OpenAIRE

    Nirmal George; Ajith Kumar PV; Vijayalekshmi Amma S.

    2016-01-01

    Background: Diabetes mellitus require lifelong intervention and Kerala has high prevalence. New expensive agents require comparison with existing regimens for cost-effectiveness. Methods: Socio-demographic, anthropometric, FPG and HbA1C (baseline and post treatment) of 150 patients (73 men; 77 women) were obtained from records using standard case report forms in our retrospective study. ANOVA and paired t test were used for between groups and within group comparison. Results: Metformin ...

  6. In-silico analysis of heat shock protein 47 for identifying the novel therapeutic agents in the management of oral submucous fibrosis

    Directory of Open Access Journals (Sweden)

    Jayasankar P Pillai

    2014-01-01

    Conclusion: HSP47 can be a potential candidate to target, in order to control the production of abundance collagen in OSF. Hence, the binding sites of HSP47 with collagen are identified and some natural compounds with a potential to bind with these binding receptors are also recognized. These natural compounds might act as anti-HSP47 lead molecules in designing novel therapeutic agents for OSF, which are so far unavailable.

  7. Cinacalcet HCl, an oral calcimimetic agent for the treatment of secondary hyperparathyroidism in hemodialysis and peritoneal dialysis: a randomized, double-blind, multicenter study.

    Science.gov (United States)

    Lindberg, Jill S; Culleton, Bruce; Wong, Gordon; Borah, Michael F; Clark, Roderick V; Shapiro, Warren B; Roger, Simon D; Husserl, Fred E; Klassen, Preston S; Guo, Matthew D; Albizem, Moetaz B; Coburn, Jack W

    2005-03-01

    Management of secondary hyperparathyroidism is challenging with traditional therapy. The calcimimetic cinacalcet HCl acts on the calcium-sensing receptor to increase its sensitivity to calcium, thereby reducing parathyroid hormone (PTH) secretion. This phase 3, multicenter, randomized, placebo-controlled, double-blind study evaluated the efficacy and safety of cinacalcet in hemodialysis (HD) and peritoneal dialysis (PD) patients with PTH > or =300 pg/ml despite traditional therapy. A total of 395 patients received once-daily oral cinacalcet (260 HD, 34 PD) or placebo (89 HD, 12 PD) titrated from 30 to 180 mg to achieve a target intact PTH (iPTH) level of or =30% reduction in iPTH from baseline (65 versus 13%), and proportion of patients with > or =20, > or =40, or > or =50% reduction from baseline. Cinacalcet had comparable efficacy in HD and PD patients; 50% of PD patients achieved a mean iPTH < or =300 pg/ml. Cinacalcet also significantly reduced serum calcium, phosphorus, and Ca x P levels compared with control treatment. The most common side effects, nausea and vomiting, were usually mild to moderate in severity and transient. Once-daily oral cinacalcet was effective in rapidly and safely reducing PTH, Ca x P, calcium, and phosphorus levels in patients who received HD or PD. Cinacalcet offers a new therapeutic option for controlling secondary hyperparathyroidism in patients with chronic kidney disease on dialysis.

  8. 两种口服对比剂在多层螺旋CT小肠造影中的应用对比%Contrast of Application of Two Kinds of Oral Contrast Agent in Multislice CT Enterography of Small Intestine

    Institute of Scientific and Technical Information of China (English)

    缪军; 夏裕平; 黄永平

    2013-01-01

    目的:研究多层螺旋CT小肠造影(MSCTE)中口服对比剂的选择应用。方法:回顾性分析70例进行MSCTE检查患者口服对比剂应用情况,50例检查前口服中性对比剂等渗2.5%甘露醇溶液,20例检查前口服阳性对比剂碘海醇的稀释液。结果:两组患者十二指肠、空肠、回肠扩张程度比较:t值分别为7.7807、6.6994和7.9721(P<0.05),差异有统计学意义,中性对比剂组优于阳性对比剂组;两组患者十二指肠和回盲部显示良好率比较χ2=6.6546(P<0.05),差异有统计学意义,中性对比剂组优于阳性对比剂组。结论:在MSCTE检查中,等渗中性对比剂扩张小肠的效果优于低渗的阳性对比剂,等渗中性对比剂可作为MSCTE检查的首选,但最终的选择还要根据临床的实际情况决定。%Objective:Study the application of two kinds of oral contrast agent in multislice CT enterography(MSCTE). Methods:The situation of application of oral contrast agent in 70 patiants who were checked MSCTE, 50 cases took orally neutral contrast agent-2.5%mannitol solution before the check, and 20 cases took orally positive contrast agent-diluent of iohexol. Results:Compared the degree of the expansion of duodenum、jejunum and ileum of the two groups of patients, t-value were 7.7807、6.6994 and 7.972(P<0.05), the difference was statistically significant, neutral contrast group was better than the positive contrast group. Compared the excellent rate that duodenum and ileocecal junction appeared.χ2=6.6546(P<0.05), the difference was statistically significant, the neutral contrast group was better than the positive contrast group. Conclusion:The neutral contrast was better than the positive contrast in the dilatation effects of small intestine in MSCTE check, isotonic neutral contrast can be used as the first choice in MSCTE check, But the final choice should be decided according the clinical condition.

  9. 无机载银抗菌剂在口腔修复中的研究应用现状%Research status of inorganic silver-carrying antibacterial agent in oral prosthodontics

    Institute of Scientific and Technical Information of China (English)

    李庆艳; 郑新颖; 吕俏; 林华; 高宁

    2012-01-01

    BACKGROUND: Oral environment is bacterial, and so the effects of restorative treatments face challenges from micro-organisms. To some extent, the success of treatment depends on the antimicrobial properties of restorative material. The silver antibacterial agent has become a research hotspot for its characteristics of broad spectrum antimicrobial, high biological security and rare drug tolerance. OBJECTIVE: To review the application and research of inorganic silver-carrying antibacterial agent in prosthodontics material and provide a theoretical basis for the further clinical application. METHODS: CNKI, PubMed and OVID databases were retrieved online for articles concerning the application of inorganic silver-carrying antibacterial agent in oral prosthodontics from 1990-01 to 2011-04. Articles highly related to the application and research of inorganic silver-carrying antibacterial agent in oral prosthodontics that published recently or in the authorized journals were included. Twenty-nine articles were included in result analysis. RESUTS AND CONCLUSION: Silver is an effective antibacterial material and has a good effect on oral common pathogenic bacteria, such as candita albicans, streptococcus mutans and lactobacillus. Application of silver into prosthodontics material has a broad prospect. However, silver ion is unstable and tarnished easily. In the modification study of prosthodontics material, it is needed to further research for overcoming oxidizing discoloration, reducing the affection of silver on material physical and chemical properties, as well as the clinical application and evaluation of prosthodontics material.%背景:口腔环境是有菌环境,各种修复治疗的效果面临着来自微生物的挑战,治疗的成败在一定程度上取决于材料的抗菌性能.银系无机抗菌剂由于抗菌谱广,生物安全性高,不易产生耐药性等特点,成为众多学者研究的热点.目的:综述无机载银抗菌剂在口腔修复材料中

  10. Oral heparin: status review

    Directory of Open Access Journals (Sweden)

    Gomez-Orellana Isabel

    2006-05-01

    Full Text Available Abstract Unfractionated heparin and low molecular weight heparin are the most commonly used antithrombotic and thromboprophylactic agents in hospital practice. Extended out-of-hospital treatment is inconvenient in that these agents must be administered parenterally. Current research is directed at development of a safe and effective oral antithrombotic agent as an alternative for the effective, yet difficult to use vitamin K antagonists. A novel drug delivery technology that facilitates transport of drugs across the gastrointestinal epithelium has been harnessed to develop an oral dosage form of unfractionated heparin. Combining unfractionated heparin with the carrier molecule, sodium N-(8 [2-hydroxybenzoyl]amino caprylate, or SNAC has markedly increased the gastrointestinal absorption of this drug. Preclinical and clinical studies to-date suggests that oral heparin-SNAC can confer a clinical efficacious effect; further confirmation is sought in planned clinical trials.

  11. Biomimetic Actinide Chelators: An Update on the Preclinical Development of the Orally Active Hydroxypyridonate Decorporation Agents 3,4,3-LI(1,2-HOPO) and 5-LIO(Me-3,2-HOPO)

    Energy Technology Data Exchange (ETDEWEB)

    Durbin, Patricia W.; Kullgren, Birgitta; Ebbe, Shirley N.; Xu, Jide; Chang, Polly Y.; Bunin, Deborah I.; Blakely, Eleanor A.; Bjornstad, Kathleen A.; Rosen, Chris J.; Shuh, David K.; Raymond, Kenneth N.

    2011-07-13

    The threat of a dirty bomb or other major radiological contamination presents a danger of large-scale radiation exposure of the population. Because major components of such contamination are likely to be actinides, actinide decorporation treatments that will reduce radiation exposure must be a priority. Current therapies for the treatment of radionuclide contamination are limited and extensive efforts must be dedicated to the development of therapeutic, orally bioavailable, actinide chelators for emergency medical use. Using a biomimetic approach based on the similar biochemical properties of plutonium(IV) and iron(III), siderophore-inspired multidentate hydroxypyridonate ligands have been designed and are unrivaled in terms of actinide-affinity, selectivity, and efficiency. A perspective on the preclinical development of two hydroxypyridonate actinide decorporation agents, 3,4,3-LI(1,2-HOPO) and 5-LIO(Me-3,2-HOPO), is presented. The chemical syntheses of both candidate compounds have been optimized for scale-up. Baseline preparation and analytical methods suitable for manufacturing large amounts have been established. Both ligands show much higher actinide-removal efficacy than the currently approved agent, diethylenetriaminepentaacetic acid (DTPA), with different selectivity for the tested isotopes of plutonium, americium, uranium and neptunium. No toxicity is observed in cells derived from three different human tissue sources treated in vitro up to ligand concentrations of 1 mM, and both ligands were well tolerated in rats when orally administered daily at high doses (>100 micromol kg d) over 28 d under good laboratory practice guidelines. Both compounds are on an accelerated development pathway towards clinical use.

  12. A Single Blinded Randomized Controlled Study of the Effect of Conventional Oral Hypoglycemic Agents Versus Intensive Short-Term Insulin Therapy on Pure Tone Audiometry in Type II Diabetes Mellitus.

    Science.gov (United States)

    Asma, A; Azmi, M Nor; Mazita, A; Marina, M B; Salina, H; Norlaila, M

    2011-04-01

    Neuropathy is frequently a late complication of diabetes mellitus. Auditory neuropathy and microangiopathy of inner ear are the possible causes of hearing loss in diabetics. To study the correlation between glycaemic control and hearing threshold in patients with type 2 diabetes mellitus and to determine the differences of hearing threshold between groups treated with different modality. This single blind randomized controlled study was performed at the Department of Medicine and Department of Otorhinolaryngology, Hospital Universiti Kebangsaan Malaysia (UKM) between 1st May 2003 and 31st September 2004. This study was approved by Research Ethics Committee (code number FF-137). Subjects were randomized into two groups. Group 1 were patients treated with conventional oral hypoglycemic agents. The patients in group 2 were those treated with insulin injection. The subjects were seen 4 weekly for 3 months. Audiometric test were performed in all subjects at each visit. Blood were taken for fasting blood glucose, Hb1Ac, and fructosamine at every visit to determine the glycaemic controls of the subject. They were 11 patients (22 ears) treated with oral hypoglycemic agents and 17 patients treated (34 ears) with subcutaneous insulin. There is no significant difference between mean pure tone threshold before and after treatment at all frequencies in both groups. There is also no significance different in fasting glucose level and fructosamine. However, there is significant difference HbA1c levels between the two groups after treatment (P < 0.05). This study has shown that glycaemic control does not have significant impact on hearing. The hearing threshold is neither affected by insulin treatment nor by the glycaemic control.

  13. Bioadhesive agents in addition to oral contrast media - evaluation in an animal model; Evaluierung der Wirkung bioadhaesiver Substanzen als Zugabe zu oralen Kontrastmitteln - eine experimentelle Studie

    Energy Technology Data Exchange (ETDEWEB)

    Conrad, R.; Schneider, G.; Textor, J.; Schild, H.H. [Radiologische Universitaetsklinik Bonn (Germany); Fimmers, R. [Universitaetsklinik Bonn (Germany). Inst. fuer Medizinische Statistik und Datenverarbeitung; Sachse, A. [Schering AG, Berlin (Germany)

    1998-06-01

    Purpose: To evaluate the additional effect of bioadhesives in combination with iotrolan and barium as oral contrast media in an animal model. Method: The bioadhesives Noveon, CMC, Tylose and Carbopol 934 were added to iotrolan and barium. The solutions were administered to rabbits by a feeding tube. The animals were investigated by computed tomography (CT) and radiography after 0,5, 4, 12, 24 and in part after 48 hours. Mucosal coating and contrast filling of the bowel were evaluated. Results: Addition of bioadhesives to oral contrast media effected long-term contrast in the small intestine and colon, but no improvement in continuous filling and coating of the gastrointestinal tract was detected. Mucosal coating was seen only in short regions of the caecum and small intestine. In CT the best results for coating were observed with tylose and CMC, in radiography additionally with carbopol and noveon. All contrast medium solutions were well tolerated. Conclusion: The evaluated contrast medium solutions with bioadhesives have shown long-term contrast but no improvement in coating in comparison to conventional oral contrast media. (orig.) [Deutsch] Ziel: Pruefung der Wirkung von bioadhaesiven Substanzen als Zugabe zu den oralen Kontrastmitteln (KM) Iotrolan und Barium im Tierexperiment. Methode: Die bioadhaesiven Substanzen Noveon, Carboxymethylcellulose (CMC), Tylose und Carbopol 934 wurden Iotrolan-Loesungen und Bariumsulfatsuspensionen beigemischt und anschliessend 30 Kaninchen ueber Magensonde verabreicht. In der Spiral-CT und Radiographie wurden die Tiere nach 0,5, 4, 12, 24 und teilweise nach 48 Stunden untersucht und hinsichtlich Schleimhautbeschlag und kontinuierlicher KM-Fuellung bewertet. Ergebnisse: Die Zugabe adhaesiver Stubstanzen beguenstigte eine langanhaltende Kontrastierung von Duenn- und Dickdarm. Es konnte jedoch weder eine vollstaendige Kontrastierung noch ein durchgehender Beschlag des gesamten Gastrointestinaltraktes bewirkt werden. Ein

  14. Oral fibrinogen-depleting agent lumbrokinase for secondary ischemic stroke prevention: results from a multicenter, randomized, parallel-group and controlled clinical trial

    Institute of Scientific and Technical Information of China (English)

    CAO Yong-jun; ZHANG Xia; WANG Wan-hua; ZHAI Wan-qing; QIAN Ju-fen; WANG Jian-sheng; CHEN Jun

    2013-01-01

    Background Elevated fibrinogen (Fg) level is a known risk factor for ischemic stroke.There are few clinical trials on oral fibrinogen-depleting therapies for secondary ischemic stroke prevention.We aimed to assess the effects of one-year therapy with oral lumbrokinase enteric-coated capsules on secondary ischemic stroke prevention.Methods This is a multicenter,randomized,parallel group and controlled study that began treatment in hospitalized patients with ischemic stroke and continued for 12 months.Patients were randomized to either the control group that received the standard stroke treatment or the fibrinogen-depleting group that received the standard stroke treatment plus enteric-coated lumbrokinase capsules.The NIH Stroke Scale scores (NIHSSs) and plasma Fg level were recorded.The carotid artery intima-media thickness (IMT) and status of plaques were examined through carotid ultrasound examination.Primary outcomes included all-cause mortality,any event of recurrent ischemic stroke/transient ischemic attack (TIA),hemorrhagic stroke,myocardial infarction and angina,and other noncerebral ischemia or hemorrhage.Kaplan-Meier survival analysis and the Long-rank test were used to compare total vascular end point incidence between the two groups.Comparison of median values between two groups was done by the Student t test,one-way analysis of variance (ANOVA),or non-parametric rank sum test.Results A total of 310 patients were enrolled,192 patients in the treatment group and 118 patients in the control group.Compared to the control group,the treatment group showed favorable outcomes in the Fg level,carotid IMT,the detection rate of vulnerable plaques,the volume of carotid plaques,NIHSS scores,and incidence of total vascular (6.78% and 2.08%,respectively) and cerebral vascular events (5.93% and 1.04%,respectively) (P <0.05).In the treatment group,the volume of carotid plaques was significantly related to the carotid IMT,the plaque diameter,width and number (P

  15. Oral inoculation of neonatal Suffolk sheep with the agent of classical scrapie results in PrP(Sc) accumulation in sheep with the PRNP ARQ/ARQ but not the ARQ/ARR genotype.

    Science.gov (United States)

    Greenlee, Justin J; Smith, Jodi D; Hamir, Amir N

    2016-04-01

    Scrapie is a transmissible spongiform encephalopathy that can be transmitted amongst susceptible sheep. The prion protein gene (PRNP) profoundly influences the susceptibility of sheep to the scrapie agent. This study reports the failure to detect PrP(Sc) in nervous or lymphoid tissues of Suffolk sheep of the PRNP ARQ/ARR genotype after oral inoculation with a U.S. scrapie isolate. Lambs were inoculated within the first 24 h of birth with 1 ml of a 10% (wt./vol.) brain homogenate derived from a clinically affected ARQ/ARQ sheep. The inoculated sheep were observed daily throughout the experiment for clinical signs suggestive of scrapie until they were necropsied at 86 months post inoculation. Tissues were collected for examination by immunohistochemistry and enzyme immunoassay, but all failed to demonstrate evidence of scrapie infection. Neonatal sheep of the ARQ/ARQ genotype receiving the same inoculum developed scrapie within 24 months. Lambs of the ARQ/ARR genotype that received the same inoculum by intracranial inoculation develop scrapie with a prolonged incubation period and with abnormal prion present within the central nervous system, but not peripheral lymphoid tissues. Results of this study suggest that ARQ/ARR sheep are resistant to oral infection with the scrapie isolate used even during the neonatal period.

  16. 小球藻和螺旋藻的营养成分及其降血糖活性比较%Comparison of Chlorella and Spirulina on Nutrients and Anti-diabetic Effects

    Institute of Scientific and Technical Information of China (English)

    史珅; 张旗; 王娜; 尚小玉; 栾少萌; 艾君

    2015-01-01

    Providing technical basis for product development and application , by comparing the chlorella and spirulina nutrition composition and anti-diabetic effects. Contrast the concentration of nucleotide, amino acid, inositol, calcium, zinc, chlorophyll, folic acid, biotin in chlorella pyrenoidosa and DunDing spirulina, as well as auxiliary anti-diabetic function , via the biochemical methods and analytical chemistry recorded in national standard, the line mark and “Health food inspection and evaluation of technical specifications”. The results show that the samples of chlorella pyrenoidosa contained lower nucleotide content , especially lower purine nucleotides, higher contents of calcium, zinc, chlorophyll, biotin and folic acid, which could effectively reduce the glycemia concentration in hyperglycemia mice; in another word it had anti-diabetic effects. It is clear that spirulina and chlorella could be used in the development of hypoglycemic kind of health food for their different advantages in nutrients, anti-diabetic function and improving glucose tolerance.%通过对比小球藻和螺旋藻的营养成分和辅助降血糖功能,为产品开发应用提供技术依据。采用国标、行标和《保健食品检验与评价技术规范》等规定的生物化学、分析化学检测方法,对比蛋白核小球藻、钝顶螺旋藻样品的核苷酸、氨基酸、肌醇、钙、锌、叶绿素、叶酸、生物素含量,以及辅助降血糖功能。结果发现,实验中采样的蛋白核小球藻含有更低的核苷酸含量,尤其是更低的嘌呤核苷酸,更高的钙、锌、叶绿素、叶酸和生物素含量,并可以有效降低高血糖小鼠的空腹血糖,具有降血糖功效。可见,螺旋藻和小球藻在营养成分、降低空腹血糖和改善糖耐量方面,具有不同优势,在开发降糖类保健食品时可以配合使用。

  17. 番石榴叶杂源萜类中抗糖尿病活性成分的虚拟筛选%Virtual Screening of Anti-Diabetes Active Components in Meroterpenoids from Psidium guajava Leaves

    Institute of Scientific and Technical Information of China (English)

    刘美凤; 谷灵灵; 蒋利荣; 周惠

    2012-01-01

    来源于番石榴叶的杂源萜类物质对治疗糖尿病的相关靶标有良好的抑制活性,这说明番石榴叶杂源萜类物质中可能含有降糖活性强的成分.因此,文中利用13个二醛杂源萜类化合物作为配体,分析了该类化合物与治疗糖尿病相关的PTP1B、PPARγ、PPARα、α-淀粉酶、α-葡萄糖苷酶的酶/受体分子对接情况,进行相应的虚拟筛选.结果显示:杂源萜类化合物与α-淀粉酶、α-葡萄糖苷酶无对接位点,但与PTP1B、PPARγ、PPARα有对接位点;蛋白和配体间的作用是通过弱非共价键力的相互作用而实现的,如疏水作用、π键和氢键;Euglobal Iia、Euglobal Ib、Euglobal Ic(首次从桉叶中分离得到)与PTP1B、PPARγ、PPARα的结合活性均较高,可为降糖药物的设计和结构修饰提供有用的信息.%The meroterpenoids from Psidium guajava leaves may contain some components with high anti-diabetes activity because they possess high inhibitory activity to the anti-diabetes targets. In this investigation, by using PTPIB, PPARγ, PPARa, α-amylase and α-glycosidase as anti-diabetes targets and 13 dialdehyde meroterpenoid compounds as ligands, the molecular docking conditions between the ligands and the targets were analyzed, thus implementing the corresponding virtual screening. The results show that the meroterpenoids have docking sites with PTPIB, PPARγ and PPARα, but not with a-amylase and a-glycosidase; and that the weak non-covalent interactions, namely hydrophobic interaction, π bonding and hydrogen bonding, all play an important role in the binding of ligands to proteins. In addition, Euglobal Iia, Euglobal Ib and Euglobal Ic firstly extracted from eucalyptus leaves have better affinity to PTPIB, PPARγ and PPARα, which provides some useful information for the design and structural modification of anti-diabetic drugs.

  18. Drug-drug interactions with sodium-glucose cotransporters type 2 (SGLT2) inhibitors, new oral glucose-lowering agents for the management of type 2 diabetes mellitus.

    Science.gov (United States)

    Scheen, André J

    2014-04-01

    Inhibitors of sodium-glucose cotransporters type 2 (SGLT2) reduce hyperglycaemia by decreasing renal glucose threshold and thereby increasing urinary glucose excretion. They are proposed as a novel approach for the management of type 2 diabetes mellitus. They have proven their efficacy in reducing glycated haemoglobin, without inducing hypoglycaemia, as monotherapy or in combination with various other glucose-lowering agents, with the add-on value of promoting some weight loss and lowering arterial blood pressure. As they may be used concomitantly with many other drugs, we review the potential drug-drug interactions (DDIs) regarding the three leaders in the class (dapagliglozin, canagliflozin and empagliflozin). Most of the available studies were performed in healthy volunteers and have assessed the pharmacokinetic interferences with a single administration of the SGLT2 inhibitor. The exposure [assessed by peak plasma concentrations (Cmax) and area under the concentration-time curve (AUC)] to each SGLT2 inhibitor tested was not significantly influenced by the concomitant administration of other glucose-lowering agents or cardiovascular agents commonly used in patients with type 2 diabetes. Reciprocally, these medications did not influence the pharmacokinetic parameters of dapagliflozin, canagliflozin or empagliflozin. Some modest changes were not considered as clinically relevant. However, drugs that could specifically interfere with the metabolic pathways of SGLT2 inhibitors [rifampicin, inhibitors or inducers of uridine diphosphate-glucuronosyltransferase (UGT)] may result in significant changes in the exposure of SGLT2 inhibitors, as shown for dapagliflozin and canagliflozin. Potential DDIs in patients with type 2 diabetes receiving chronic treatment with an SGLT2 inhibitor deserve further attention, especially in individuals treated with several medications or in more fragile patients with hepatic and/or renal impairment.

  19. 罗望子壳降血糖活性化学成分的研究%Study on the Anti-diabetic Activities of Tamarindus pericarp

    Institute of Scientific and Technical Information of China (English)

    庄俊钰; 李汴生; 王三永

    2011-01-01

    In the present study, the anti-diabetic activities of ethanolic extracts from Tamarind pericarp were studied. The butanol extract showed the highest activity, which were further seperated by silica gel column chromatography, reverse phase silica gel (RP-18) column chromatography, highly porous synthetic resin Diaion (HP-20) and sephadex LH-20. Seven fiavonoid compounds were isolated from this extract,which were identified as Quercetin (A), Kaempferol (B), Morin (C), Apigien (D), Naringenin (E), Luteolin (F), and Myricetin (M) by 1H NMR and 13C NMR. The enzyme inhibitory activities against rat intestinal α-glucosidase (sucrase and maltase) and porcine pancreatic α-amylase (PPA) of the active compounds were studied. The result revealed these flavonoid compounds had significant enzyme inhibitory activities except Apigien.%本文测定了罗望子壳醇提取物各个活性部位的降血糖活性,发现其正丁醇相活性最高.接着对正丁醇相的化学成分进行分离鉴定,采用大孔吸附树脂(HP-20),正相硅胶柱层析,反相硅胶柱层析(RP-18),以及葡聚糖凝胶(LH-20)等分离手段分离鉴定其主要化学成分.通过H NMR,C NMR技术并结合文献对照对7个化合物的结构进行了鉴定和确认,他们的分别是:槲皮素(A)、山萘酚(B)、桑黄素(C)、芹菜素(D),柚皮素(E)、木犀草素(F)、和杨梅酮(M).我们通过测定这7个黄酮类化合物对α-葡萄糖苷酶、猪胰液α-淀粉酶(PPA)的抑制活性以评价其降血糖活性,结果显示除了芹菜素之外,其他6个化合物都显示了较好的酶抑制活性.表明黄酮类化合物是罗望子壳降血糖有效成分之一.

  20. Role of phenolics as antioxidants, biomolecule protectors and as anti-diabetic factors - Evaluation on bark and empty pods of Acacia auriculiformis

    Institute of Scientific and Technical Information of China (English)

    Arumugam Sathya; Perumal Siddhuraju

    2012-01-01

    can be used for the preparation of antioxidant/nutraceutical supplements and in anti-diabetic formulations.

  1. Emodin, an 11β-hydroxysteroid dehydrogenase type 1 inhibitor, regulates adipocyte function in vitro and exerts anti-diabetic effect in ob/ob mice

    Institute of Scientific and Technical Information of China (English)

    Yue-jing WANG; Su-ling HUANG; Ying FENG; Meng-meng NING; Ying LENG

    2012-01-01

    Aim:Emodin (1,3,8-trihydroxy 6-methylanthraquinone) is a potent and selective inhibitor of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) with the ability to ameliorate metabolic disorders in diet-induced obese mice.In the present study,we investigated the effects of emodin on adipocyte function and the underlying mechanisms in vitro,and its anti-diabetic effects in ob/ob mice.Methods:3T3-L1 adipocytes were used for in vitro studies.11β-HSD1A activity was evaluated with a scintillation proximity assay.The adipogenesis,glucose uptake,lipolysis and adiponectin secretion were investigated in 3T3-L1 adipocytes treated with emodin in the presence of active (corticosterone) or inactive glucocorticoid (11-dehydrocorticosterone).For in vivo studies,ob/ob mice were administered emodin (25 and 50 mg.kg-1·d-1,ip) for 26 d.On the last day of administration,the serum was collected and the mesenteric and perirenal fat were dissected for analyses.Results:Emodin inhibited the 11β-HSD1 activity in 3T3-L1 adipocytes in concentration- and time dependent manners (the IC50 values were 7,237 and 4.204 μmol/L,respectively,after 1 and 24 h treatment,in 3T3-L1 adipocytes,emodin (30 μmol/L) suppressed 11-dehydrocorticosterone-induced adipogenesis without affecting corticosterone-induced adipogenesis; emodin (3 μmol/L) reduced 11-dehydrocorticosterone-stimulated lipolysis,but had no effect on corticosterone-induced lipolysis.Moreover,emodin (3 μmol/L)partly reversed the impaired insulin-stimulated glucose uptake and adiponectin secretion induced by 11-dehydrocorticosterone but not those induced by corticosterone.In ob/ob mice,long-term emodin administration decreased 11β-HSD1 activity in mesenteric adipose tissues,lowered non-fasting and fasting blood glucose levels,and improved glucose tolerance.Conclusion:Emodin improves the inactive glucocorticoid-induced adipose tissue dysfunction by selective inhibition on 11β-HSD1 in adipocyte in vitro and improves glycemic control in ob

  2. Perfil e práticas de saúde bucal do agente comunitário de saúde em municípios piauienses de pequeno porte Profile and procedures of the community health agents regarding oral health in the countryside of Piauí State, Brazil

    Directory of Open Access Journals (Sweden)

    Marcoeli Silva de Moura

    2010-06-01

    Full Text Available O objetivo desta pesquisa foi traçar o perfil demográfico e práticas de saúde bucal do ACS, em cidades de pequeno porte do Estado do Piauí. Foram selecionados quatro municípios: Água Branca, Piracuruca, Queimada Nova e Simões. O método utilizado foi o transversal observacional descritivo. Foram aplicados questionários a 109 ACS, constituídos de 28 perguntas fechadas. Os dados foram transferidos para planilha do programa ExcelÒ, tabulados e analisados. Pelos dados obtidos, foi possível concluir que: (1 o agente comunitário de saúde do interior do Piauí é predominantemente do sexo feminino, casado, com idade entre 20-39 anos, tem em média de um a três filhos, com grau de escolaridade médio acima de nove anos, renda de um salário mínimo, residindo em média há 24 anos na comunidade; (2 a grande maioria dos ACS não foi capacitada, não assistiu palestras educativas sobre saúde bucal; entretanto, quase a metade realiza atividades em saúde bucal, mas não as registra; (3 a autopercepção sobre o conhecimento em saúde bucal pelos ACS predominou entre conceitos regular e bom, o que coincidiu com o percentual de acertos ao questionário aplicado.The aim of this survey was to draw the demographic profile and the actions concerning oral health carried out by the communitarian agents of health, in small towns of Piauí State, Brazil. Four towns were chosen: Água Branca, Piracuruca, Queimada Nova e Simões. The method used was observational descriptive cross-sectional. One hundred and nine agents were assessed through questionnaires, with 28 multiples choice questions. Data was analyzed in Excel. It was possible to conclude that: the communitarian agents on the countryside of Piauí are predominantly females, married, age between 20-39, with one to three children, nine years of formal education, monthly income of one minimum salary, and has been living in their community for 24 years in average; the large majority of the agents

  3. Effect of a novel oral chemotherapeutic agent containing a combination of trifluridine, tipiracil and the novel triple angiokinase inhibitor nintedanib, on human colorectal cancer xenografts.

    Science.gov (United States)

    Suzuki, Norihiko; Nakagawa, Fumio; Matsuoka, Kazuaki; Takechi, Teiji

    2016-12-01

    Trifluridine/tipiracil (TFTD) is a combination drug that is used for the treatment of metastatic colorectal cancer and was formerly known as TAS-102. It is a combination of two active pharmaceutical compounds, trifluridine, an antineoplastic thymidine-based nucleoside analog, and tipiracil, which enhances the bioavailability of trifluridine in vivo. TFTD is used for the treatment of patients with unresectable advanced or recurrent colorectal cancer that is resistant to standard therapies. In the present study, the anticancer effects of trifluridine in combination with nintedanib, an oral triple angiokinase inhibitor, on human colorectal cancer cell lines were investigated. The cytotoxicity against DLD-1, HT-29, and HCT116 cell lines was determined by the crystal violet staining method. The combination of trifluridine and nintedanib exerted an additive effect on the growth inhibition of DLD-1 and HT-29 cells and a sub-additive effect on HCT116 cells, as determined by isobologram analyses. Subsequently, the human colorectal cancer cell lines were implanted subcutaneously into nude mice to allow the evaluation of the in vivo tumor growth inhibitory effects of TFTD and nintedanib combination therapy. TFTD (150 mg/kg/day) and/or nintedanib (40 mg/kg/day) were orally administered to the mice twice daily from day 1 to day 14. The tumor growth inhibition with combination therapy was 61.5, 72.8, 67.6 and 67.5% for the DLD-1, DLD-1/5-FU, HT-29, and HCT116 xenografts, respectively. This was significantly (P<0.05) higher than the effects of monotherapy with either TFTD or nintedanib. These results demonstrated the effectiveness of the combination of TFTD and nintedanib in the treatment of colorectal cancer xenografts. The concentration of trifluridine incorporated into DNA in the HT-29 and HCT116 tumors was determined by liquid chromatography-tandem mass spectrometry. The incorporation levels following treatment with TFTD and nintedanib for 14 consecutive days were

  4. Fusion proteins containing insect-specific toxins as pest control agents: snowdrop lectin delivers fused insecticidal spider venom toxin to insect haemolymph following oral ingestion.

    Science.gov (United States)

    Fitches, Elaine; Edwards, Martin G; Mee, Christopher; Grishin, Eugene; Gatehouse, Angharad M R; Edwards, John P; Gatehouse, John A

    2004-01-01

    The mannose-specific snowdrop lectin (Galanthus nivalis agglutinin: GNA), when fed to insects, binds to the gut epithelium and passes into the haemolymph. The ability of GNA to act as a carrier protein to deliver an insecticidal spider venom neurotoxin (Segestria florentina toxin 1: SFI1) to the haemolymph of lepidopteran larvae was investigated. Constructs encoding SFI1 and an SFI1/GNA fusion protein were expressed in Pichia pastoris. The insecticidal activity of purified recombinant proteins on injection was found to be comparable to published values for SfI1 purified from spider venom [Toxicon 40 (2002) 125]. Whereas neither GNA nor SFI1 alone showed acute toxicity when fed to larvae of tomato moth (Lacanobia oleracea), feeding SFI1/GNA fusion at 2.5% of dietary proteins was insecticidal to first stadium larvae, causing 100% mortality after 6 days. The protein also showed a significant, dose dependent, toxicity towards fourth and fifth stadium larvae, with growth reduced by up to approximately 90% over a 4-day assay period compared to controls. Delivery of intact SFI1/GNA to the haemolymph in these insects was shown by western blotting; haemolymph samples from fusion-fed larvae contained a GNA-immunoreactive protein of the same molecular weight as the SFI1/GNA fusion. SFI1/GNA and similar fusion proteins offer a novel and effective approach for delivering haemolymph active toxins by oral administration, which could be used in crop protection by expression in transgenic plants.

  5. Subacute toxicity evaluation of KR-33493, FAF1 inhibitor for a new anti-parkinson's disease agent, after oral administration in rats and dogs.

    Science.gov (United States)

    Jeong, Jong-Woo; Yu, Changsun; Lee, Jong-Hwa; Moon, Kyoung-Sik; Kim, Eunhee; Yoo, Sung-Eun; Koo, Tae-Sung

    2016-11-01

    KR33493, a newly developed FAS-associated factor 1 (FAF1) inhibitor for Parkinson's disease, is being evaluated in a Phase I clinical trial. In the present study, the subchronic toxicity of KR33493 in Sprague-Dawley (SD) rats and beagle dogs was investigated at various oral doses for 28 and 14 days, respectively. During the study, food consumption, body weights, organ weights, gross findings, and mortality were examined; and ophthalmoscopy, electrocardiography, hematology, serum biochemistry, urinalysis, histopathology, and toxicokinetics were performed. In rats, weight gain decreased in both sexes at 500 mg/kg/day, with no significant differences. In dogs, some significant differences compared with the control were found during the trial; however, at the end of recovery periods, these were no longer observed and there was no dose correlation. Some histopathological findings were observed, but these were considered as incidental changes. Since no other significant changes were observed, doses above 500 and 1000 mg/kg KR33493 in rat and dogs, respectively, caused no observed adverse effects. Therefore, based on these results, the Phase 1 clinical trial for KR33493 was approved by the Korean Food & Drug Administration.

  6. Exposure-safety-efficacy analysis of single-agent ixazomib, an oral proteasome inhibitor, in relapsed/refractory multiple myeloma: dose selection for a phase 3 maintenance study.

    Science.gov (United States)

    Gupta, Neeraj; Labotka, Richard; Liu, Guohui; Hui, Ai-Min; Venkatakrishnan, Karthik

    2016-06-01

    Background Ixazomib is the first oral, small molecule proteasome inhibitor to reach phase 3 trials. The current analysis characterized the exposure-safety and exposure-efficacy relationships of ixazomib in patients with relapsed/refractory multiple myeloma (MM) with a purpose of recommending an approach to ixazomib dosing for maintenance therapy. Methods Logistic regression was used to investigate relationships between ixazomib plasma exposure (area under the curve/day; derived from individual apparent clearance values from a published population pharmacokinetic analysis) and safety/efficacy outcomes (hematologic [grade ≥ 3 vs ≤ 2] or non-hematologic [grade ≥ 2 vs ≤ 1] adverse events [AEs], and clinical benefit [≥stable disease vs progressive disease]) using phase 1 data in relapsed/refractory MM (NCT00963820; N = 44). Results Significant relationships to ixazomib exposure were observed for five AEs (neutropenia, thrombocytopenia, rash, fatigue, and diarrhea) and clinical benefit (p phase 3 maintenance trial will initiate ixazomib at a once-weekly dose of 3 mg, increasing to 4 mg if acceptable tolerability after 4 cycles, to provide maximum clinical benefit balanced with adequate tolerability.

  7. Oral Medication

    Science.gov (United States)

    ... Size: A A A Listen En Español Oral Medication The first treatment for type 2 diabetes blood ... new — even over-the-counter items. Explore: Oral Medication How Much Do Oral Medications Cost? Save money ...

  8. Oral myiasis

    OpenAIRE

    Thalaimalai Saravanan; Mathan A Mohan; Meera Thinakaran; Saneem Ahammed

    2015-01-01

    Myiasis is a pathologic condition in humans occurring because of parasitic infestation. Parasites causing myiasis belong to the order Diptera. Oral myiasis is seen secondary to oral wounds, suppurative lesions, and extraction wounds, especially in individuals with neurological deficit. In such cases, neglected oral hygiene and halitosis attracts the flies to lay eggs in oral wounds resulting in oral myiasis. We present a case of oral myiasis in 40-year-old male patient with mental disability ...

  9. Different HPMC viscosity grades as coating agents for an oral time and/or site-controlled delivery system: an investigation into the mechanisms governing drug release.

    Science.gov (United States)

    Zema, L; Maroni, A; Foppoli, A; Palugan, L; Sangalli, M E; Gazzaniga, A

    2007-06-01

    When used as release-controlling coating agents for tableted core-based pulsatile delivery systems, three different hydroxypropyl methylcellulose (HPMC) grades, Methocel E5, E50, and K4M, provided lag phases of varying duration (Methocel K4M > E50 > E5) and a prompt and quantitative model drug release. Dissolution/mechanical erosion, permeability increase and disruption of the hydrated polymeric layer were assumed to participate in the definition of the overall release pattern. Based on these premises, we investigated what process(es) might prevail in the release-controlling mechanism for each HPMC grade. The polymers were evaluated for dissolution and swelling, while the finished systems were concomitantly evaluated for drug release and polymer dissolution. The obtained results indicated likely similarities between Methocel E5 and E50 performances, which we hypothesized to be mainly dissolution/erosion-controlled, and a clearly different behavior for Methocel K4M. This polymer indeed proved to yield higher viscosity and slower dissolving gel layer, which was able to withstand extensive dissolution/erosion for periods that exceeded the observed lag phases. The particular characteristics of swollen Methocel K4M were shown to be associated with possible drug diffusion phenomena, which might impair the prompt and quantitative release phase that is typical of pulsatile delivery.

  10. Impact factors investigation in oral ultrasonic contrast agent on diagnosis of ulcerative type gastric neoplasms on T staging%胃窗超声造影对溃疡型胃癌T分期判断的影响因素

    Institute of Scientific and Technical Information of China (English)

    薛改琴; 冯秀荣; 郭荣荣; 王宇翔

    2013-01-01

    目的 探讨影响胃窗超声造影检查对溃疡型胃癌T分期准确性的因素.方法 收集术后经病理确诊且术前做过胃窗超声造影检查的82例溃疡型胃癌患者资料,并与术后病理结果进行比较,分析病变部位、大小对溃疡型胃癌T分期的影响.结果 胃窗超声造影检查对胃小弯病变、胃窦病变T分期的准确率分别为91.3 %(21/23) 、85.7 %(24/28),两者与病理结果一致性较好(Kappa值分别为0.763、0.68,P< 0.05),对贲门位置病变的T分期准确率为68.0%(17/25),与术后病理结果比较一致性一般(Kappa值为0.446,P<0.05);因胃大弯病变资料较少,对T分期准确性的影响有待进一步研究;对癌灶最大径≤5.0 cm病灶组T分期的准确率为92.3%(36/39),对>5.0 cm病灶组T分期的准确率为72.1%(31/43),两者比较差异有统计学意义(x2=5.591,P< 0.05).结论 胃窗超声造影对胃小弯和胃窦溃疡性胃癌以及对≤5.0 cm的溃疡型病灶T分期诊断准确性较高.%Objective To explore the factors affecting diagnosis accuracy on T stage of oral ultrasonic contrast agent examination on ulcerative gastric neoplasms.Methods Data from 82 patients were analyzed who were pathologically diagnosed as ulcerative gastric neoplasms ultrasounds data of oral ultrasonic contrast agent before surgery were compared to postoperative pathology,analysis had been done on influence of the lesion site,size of the T staging on ulcerative gastric neoplasms.Results The diagnosis accuracy rate of T stage on lesser curvature of stomach and gastric antrum were 91.3 % (21/23) and 85.7 % (24/28),compared with the pathological results were in good concordancy (Kappa =0.763,0.68,P < 0.05).The accuracy rate of T stage on cardiac lesions was 68.0 % (17/25),compared with the pathological results consistency in general (Kappa =0.446,P < 0.05).Further research on the effects of T stage accuracy would be necessary.The accuracy rate ofT staging on

  11. Effect of Nigella sativa supplementation over a one-year period on lipid levels, blood pressure and heart rate in type-2 diabetic patients receiving oral hypoglycemic agents: nonrandomized clinical trial.

    Science.gov (United States)

    Badar, Ahmed; Kaatabi, Huda; Bamosa, Abdullah; Al-Elq, Abdulmohsen; Abou-Hozaifa, Bodour; Lebda, Fatma; Alkhadra, Akram; Al-Almaie, Sameeh

    2017-01-01

    Diabetic patients with hypertension and dyslipidemia are at a high risk of cardiovascular complications. To determine the effect of Nigella sativa supplementation on the lipid profile, mean arterial pressure, and heart rate in persons with type 2 diabetes on oral hypoglycemic agents (OHA). Single-blind, nonrandomized. Diabetes clinic of a university hospital in Saudi Arabia. Type-2 diabetic patients were recruited by purposive sampling and assigned to treatment or control at the discretion of the investigator with the patient blinded to treatment. Before the in.tervention and every 3 months thereafter until the end of the treatment period, the following parameters were measured: triglycerides (TG), total cholesterol (TC), low density lipoprotein cholesterol (LDL-C), high density lipoprotein cholesterol (HDL-C), systolic blood pressure (SBP), diastolic blood pressure (DBP), mean arterial pressure (MAP), heart rate (HR), and body mass index (BMI). Results at the baseline and each subsequent visit were compared between the two groups. Lipid and cardiovascular parameters, and BMI. Fifty-seven patients were assigned to receive N sativa 2 g daily for one year and 57 were assigned to receive an identical regimen of placebo, along with OHA. A significant decrease in HDL-C and increase in the TC/HDL-C and LDL-C/HDL-C ratios were seen in the control group. The N sativa group had a signifi.cant decline in TC, LDL-C, TC/HDL-C and LDL-C/HDL-C ratios, compared with the respective baseline data and the control group. HDL-C was significantly elevated in the N sativa group. The control group showed a significant elevation in MAP. The N sativa group had a significant reduction in SBP, DBP, MAP and HR and a significant decrease in DBP, MAP and HR as compared with the control group. N sativa supplementation improves total cholesterol, mean arterial pressure and heart rate in type 2 diabetes patients on oral hypoglycemic agents. There were 9 subjects in each group lost to follow up

  12. Reflexões acerca da atuação do agente comunitário de saúde nas ações de saúde bucal Reflections around the performance of community health agents in oral health strategies

    Directory of Open Access Journals (Sweden)

    Ana Larissa Fernandes de Holanda

    2009-10-01

    Full Text Available O agente comunitário de saúde (ACS tradicionalmente esteve mais vinculado ao profissional de enfermagem e ao profissional médico para realização das suas atividades práticas, sendo visto como um elemento de "propriedade" exclusiva desses profissionais da saúde. A saúde bucal historicamente tendeu a trabalhar isoladamente, separando a boca do resto do corpo e o indivíduo do seu meio ambiente. O Programa Saúde da Família (PSF aponta para importantes mudanças na organização dos serviços e no processo de trabalho. Um dos diferenciais é o trabalho de diversos tipos de profissionais em equipe, inclusive a saúde bucal, que até então estava excluída. Este trabalho objetiva mostrar a experiência do curso de qualificação do ACS, que possibilitou a diversidade de categorias profissionais de nível superior, na docência. O curso contou com três docentes odontólogos; nele, foi possível para o ACS reconhecer outros atores como participantes da equipe de saúde, além de ampliar sua visão em relação ao seu papel na saúde bucal. Os docentes também tiveram suas práticas modificadas, uma vez que passaram a entender melhor a angústia e limitações dos ACS, muitas vezes ignoradas.The Community Health Agent (CHA has traditionally been linked to doctors and nurses, being considered exclusive "property" of these professionals. Historically, oral health tended to operate isolated, disconnecting the mouth from the rest of the body and the individual from his environment. The Family Health Program (FHP points to important changes in the organization of services as well as in the work process. One of the differences is the teamwork joining different professionals, including oral health which was previously excluded. The objective of the study is to show the experience of the CHA qualifying course, which allowed the entrance of different professional categories into teaching. The course included three odontologists as lecturers, and CHA

  13. Chemoprevention of oral cancer

    Directory of Open Access Journals (Sweden)

    Yogesh Chhaparwal

    2012-01-01

    Full Text Available Oral cancer is one among the ten most common cancers in the world and shows a marked geographic variation in occurrence. It causes considerable morbidity and is associated with a 5-year survival rate of less than 50%. Current treatment primarily consists of surgery and radiotherapy and improvement in long-term cure rates with these modalities has reached a plateau. As, curative therapy available for oral cancer often results in debilitating changes in appearance, speech, swallowing and breathing, preventive strategies are desirable. Cancer chemoprevention is the use of natural, synthetic or biologic chemical agents to reverse, suppress, or prevent carcinogenic progression. Chemoprevention has been an extensively-studied strategy and continues to hold promise in the management of oral cancer. Many agents have been evaluated as possible chemopreventive agents including vitamin A and retinoids, betacarotene, vitamin E and dietary agents. Recently, molecularly targeted approach has generated interest among researchers worldwide which includes cyclooxygenase-2 (COX-2 inhibitors, EGFR inhibitors and adenovirus vectors. This article reviews the various aspects of chemoprevention and describes important chemopreventive agents and design of chemopreventive trials.

  14. [Evaluation of the association between the use of oral anti-hyperglycemic agents and hypoglycemia in Japan by data mining of the Japanese Adverse Drug Event Report (JADER) database].

    Science.gov (United States)

    Umetsu, Ryogo; Nishibata, Yuri; Abe, Junko; Suzuki, Yukiya; Hara, Hideaki; Nagasawa, Hideko; Kinosada, Yasutomi; Nakamura, Mitsuhiro

    2014-01-01

    Hypoglycemia due to treatment with oral anti-hyperglycemic agents (OHAs) is a major clinical problem in patients with type 2 diabetes mellitus. The aim of the present study was to evaluate the risk of hypoglycemia due to OHA use by using the Japanese Adverse Drug Event Report (JADER) database. To this end, reports of hypoglycemia events included in the JADER database between 2004 and 2012 were analyzed by calculating the reporting odds ratio (OR). The Medical Dictionary for Regulatory Activities Preferred Terms was used to identify hypoglycemia; 254392 reports were found in the JADER database, of which 13269 were excluded because the age and sex of the patient were not reported. Finally, 241123 reports were analyzed. Among OHAs, sulfonylureas showed the highest adjusted OR (adjusted OR, 10.13; 95% confidence interval, 9.08-11.26). The adjusted ORs for meglitinides, biguanide, thiazolidinedione, alpha-glucosidase inhibitors, and dipeptidyl peptidase-4 inhibitors were significantly lower than that of sulfonylureas. The adjusted OR of meglitinides (3.17; 95% confidence interval, 2.23-4.36) was significantly higher than that of alpha-glucosidase inhibitors or thiazolidinedione. We observed no difference between the adjusted ORs for biguanide, thiazolidinedione, alpha-glucosidase inhibitors, and dipeptidyl peptidase-4 inhibitors. Data mining of the JADER database was useful for analyzing OHA-associated hypoglycemia events. The results of our study suggested a low risk of hypoglycemia associated with biguanide, thiazolidinedione, alpha-glucosidase inhibitors, and dipeptidyl peptidase-4 inhibitors in clinical practice.

  15. Efetividade de programa de agentes comunitários na promoção da saúde bucal Efectividad del programa de agentes comunitarios en la promoción de la salud bucal Effectiveness of a community health worker program on oral health promotion

    Directory of Open Access Journals (Sweden)

    Paulo Frazão

    2009-06-01

    y residentes en domicilios de tres a seis cuartos en el municipio de Río Grande da Serra (Sudeste de Brasil. Se escogieron datos sobre conocimientos de salud-enfermedad bucal, prácticas y capacidades auto-referidas con relación al auto-examen, higiene bucal, número de residentes y de cepillos dentales individuales y colectivos en cada domicilio y acceso y uso de servicios odontológicos. Por medio de la prueba t de Student pareado, se compararon los promedios de los valores obtenidos antes y después del programa para cada uno de los grupos estudiados. Las respuestas fueron analizadas adoptándose un nivel de significancia de 5%. RESULTADOS: Se observaron diferencias estadísticamente significativas para cuestiones relacionadas con el conocimiento de salud bucal entre los agentes y entre las mujeres antes y después de la capacitación (pOBJECTIVE: To assess changes of knowledge and attitudes and health service access and utilization after the implementation of a community health worker program for oral health promotion. METHODS: A capacity building project including learning, support, and supervision activities was developed between July 2003 and August 2004. A study to assess changes was conducted including 36 community health workers and a representative sample of homemaker literate women and mothers aged 25 to 39 years living in 3- to 6-room dwelling in the city of Rio Grande da Serra, Southeastern Brazil. Data on oral health knowledge, self-reported practices, and personal skills regarding self-examination, oral hygiene, number of people living in the same household, number of individual and collective toothbrushes, and dental service access and utilization were collected using structured interviews. Mean scores measured pre- and post-intervention program were compared for each group studied using Student's t-test. A 5% significance level was set for the analysis. RESULTS: Statistically significant differences between pre- and post-intervention program were

  16. Oral myiasis

    Directory of Open Access Journals (Sweden)

    Thalaimalai Saravanan

    2015-01-01

    Full Text Available Myiasis is a pathologic condition in humans occurring because of parasitic infestation. Parasites causing myiasis belong to the order Diptera. Oral myiasis is seen secondary to oral wounds, suppurative lesions, and extraction wounds, especially in individuals with neurological deficit. In such cases, neglected oral hygiene and halitosis attracts the flies to lay eggs in oral wounds resulting in oral myiasis. We present a case of oral myiasis in 40-year-old male patient with mental disability and history of epilepsy.

  17. Oral Thrush

    Science.gov (United States)

    ... feeding mothers In addition to the distinctive white mouth lesions, infants may have trouble feeding or be fussy ... candidiasis (yeast infection) patient information. American Academy of Oral & Maxillofacial Pathology. http://www.aaomp.org/public/oral-candidiasis.php. ...

  18. Oral Dysfunction

    OpenAIRE

    鈴木, 規子; スズキ, ノリコ; Noriko, SUZUKI

    2004-01-01

    The major oral functions can be categorized as mastication, swallowing, speech and respiratory functions. Dysfunction of these results in dysphagia, speech disorders and abnormal respiration (such as Sleep Apnea). These functions relate to dentistry in the occurrence of : (1) oral preparatory and oral phases, (2) articulation disorders and velopharyngeal incompetence (VPI), and (3) mouth breathing, respiratory and blowing disorders. These disorders are related to oral and maxillofacial diseas...

  19. 上海市同济医院2011-2014年口服降糖药物使用情况分析%Utilization of oral hypoglycemic agents in Tongji hospital of Shanghai during 2011-2014

    Institute of Scientific and Technical Information of China (English)

    叶显撑; 张玉臣; 祝德秋

    2016-01-01

    The utilization of oral hypoglycemic agents (OHAs) in Shanghai Tongji Hospital during 2011-2014 was statistically analyzed in respect of consumption sum, DDDs, and DDC so as to provide references for clinical medication. There were various categories of OHAs in our hospital. The consumption sum of OHAs showed an upward trend, yet the proportion of the consumption sum of OHAs in the consumption sum of hypoglycemic agents and the total drug consumption sum showed a downward trend. The top 3 of OHAs were a-glycosidase inhibitors, sulfonylureas and biguanides in the list of consumption and sulfonylureas, biguanides and a-glycosidase inhibitors in the list of DDDs, respectively. Metformin occupied the ifrst place in the list of DDDs. The use of OHAs is basically rational with various categories of OHAs.%本文对上海市同济医院2011—2014年口服降糖药物(OHAs)的用药金额、用药频度、日用药金额等进行统计分析,为临床合理用药提供参考。4年来上海市同济医院OHAs品种全面,使用金额呈上升趋势,但OHAs占降糖药使用金额比例、OHAs占全部用药金额比例均处于微降趋势。a-糖苷酶抑制剂、磺脲类、双胍类4年来稳居销售金额排名1~3位;DDDs排序中,磺脲类、双胍类、a-糖苷酶抑制剂稳居1~3位。二甲双胍位列单品种DDDs排序的首位。上海市同济医院2011—2014年OHAs的临床使用基本合理,药物种类全面。

  20. Maintaining women's oral health.

    Science.gov (United States)

    McCann, A L; Bonci, L

    2001-07-01

    Women must adopt health-promoting strategies for both general health and the oral cavity, because the health of a woman's body and oral cavity are bidirectional. For general health-maintenance strategies, dental practitioners should actively advise women to minimize alcohol use, abstain from or cease smoking, stay physically active, and choose the right foods to nourish both the body and mind. For oral health-maintenance strategies, dental practitioners should advise women on how to prevent or control oral infections, particularly dental caries and periodontal diseases. Specifically, women need to know how to remove plaque from the teeth mechanically, use appropriate chemotherapeutic agents and dentifrices, use oral irrigation, and control halitosis. Dental practitioners also need to stress the importance of regular maintenance visits for disease prevention. Adolescent women are more prone to gingivitis and aphthous ulcers when they begin their menstrual cycles and need advice about cessation of tobacco use, mouth protection during athletic activities, cleaning orthodontic appliances, developing good dietary habits, and avoiding eating disorders. Women in early to middle adulthood may be pregnant or using oral contraceptives with concomitant changes in oral tissues. Dental practitioners need to advise them how to take care of the oral cavity during these changes and how to promote the health of their infants, including good nutrition. Older women experience the onset of menopause and increased vulnerability to osteoporosis. They may also experience xerostomia and burning mouth syndrome. Dental practitioners need to help women alleviate these symptoms and encourage them to continue good infection control and diet practices.

  1. [MICROFLORA AND ORAL DISEASE].

    Science.gov (United States)

    Khavkin, A I; Ippolitov, Y A; Aleshina, E O; Komarova O N

    2015-01-01

    Acid-producing microorganisms are base etiological agents of lesions of tooth enamel and destruction of dentin. The process start by specific microflora of tooth deposit--Streptococcus mutans, Lactobacteria and Actinomycetis viscosus which ferment food carbogydrate to form acids. High titre of them in oral cavity may be considered like a marker of carbohydrate food. But the pathogenic bacteria don't have aggression to host organism until they will have virulent factors which help to get over protection of host organism. At the same time, microflora of oral cavity is involved to form pellicula. Pellicula is a biofilm which to protect tooth enamel and dentin. Understanding relationships between safety factors of host and pathogenic microflora of oral cavity will give to create effective methods of prevention and treatment.

  2. What Makes Oral Candidiasis Recurrent Infection? A Clinical View

    Directory of Open Access Journals (Sweden)

    Azmi M. G. Darwazeh

    2014-01-01

    Full Text Available Clinical oral Candida infection (candidiasis is one of the common oral mucosal infections, and its management is usually frustrating due to either treatment failure or recurrence. Historically, oral candidiasis has been branded as disease of diseased. The unsuccessful management of oral candidiasis can due to either incorrect diagnosis, failure to identify (or correct the underlying predisposing factor(s, or inaccurate prescription of antifungal agents. Failure to properly treat oral candidiasis will lead to persistence of the fungal cell in the oral cavity and hence recurrence of infection. The oral health care provider should be aware of these fall pits in order to successfully manage oral candidiasis.

  3. Analysis on the adverse drug reaction signal and its impact factors induced by oral hypoglycemic agents%口服抗糖尿病药物不良反应信号及其相关因素分析

    Institute of Scientific and Technical Information of China (English)

    柯俊; 汤文璐; 薛浩; 庞露微

    2012-01-01

    目的 研究口服抗糖尿病药物不良反应特征,并提供相应临床合理用药的依据.方法 通过上海市不良反应监测中心收集2006至2010年有关口服抗糖尿病药物不良反应的数据,使用描述性统计,logistic回归模型及不相称性,对不良反应发生的特征、风险因子和相关因素进行分析.结果 共获得812例口服抗糖尿病药物的不良反应报告.结果显示老年人和女性占不良反应发生的多数;不良反应级别以一般为主;2009至2010年间作为药品说明书中未记载的新的不良反应有上升的趋势;双胍类及磺酰脲类(SU)不良反应最为突出;logistic回归模型显示女性、日服用药频次多、单一用药是胃肠道不良反应的危险因素.体质量是皮肤损害的危险因素,联合用药、患者年龄大是SU致低血糖的危险因素.不相称性研究同时也得到一些口服抗糖尿病药物致不良反应的信号.结论 口服抗糖尿病药物不良反应累及系统器官广泛,像性别、年龄、体质量、用药频次、是否联合用药都会在一定程度上影响不良反应的发生.故口服抗糖尿病药物在临床使用时应加强不良反应监测,重视和控制其风险因子,以期更合理安全地用药.%AIM To study the feature and regularity of adverse drug reaction (ADR) induced by oral hypoglycemic agents (OHAs) and provide reasonable advice for clinical use.METHODS By collecting ADR reports of OHAs from database of Shanghai ADR spontaneous reporting system from 2006 to 2010,we made through analysis on the character and risk factors of ADR induced by OHAs using descriptive statistics and logistic regression model,and also applied disproportional measures on data mining of ADR signal and its relevant factors.RESULTS A total of 812 ADR reports induced by OHAs were included in this study.The results indicated that the senior and female patients were mostly concerned,and mainly marked as moderately injured

  4. Oral histoplasmosis

    Directory of Open Access Journals (Sweden)

    Patil Karthikeya

    2009-01-01

    Full Text Available Histoplasmosis is a systemic fungal disease that takes various clinical forms, among which oral lesions are rare. The disseminated form of the disease that usually occurs in association with Human Immunodeficiency Virus (HIV is one of the AIDS-defining diseases. Isolated oral histoplasmosis, without systemic involvement, with underlying immunosuppression due to AIDS is very rare. We report one such case of isolated oral histoplasmosis in a HIV-infected patient.

  5. Oral Gastrointestinal Echogenic Contrast Agent in Imaging of the Common Bile Duct%口服胃肠超声助显剂对胆总管显像的影响

    Institute of Scientific and Technical Information of China (English)

    李加平; 孙宇; 朱婷; 龙劲松; 雷震; 程春生

    2013-01-01

      目的探讨口服胃肠超声助显剂对胆总管全程显像的改善情况。资料与方法78例经术后病理证实的胆总管梗阻患者,术前均行常规超声、口服胃肠超声助显剂后超声(超声造影)、磁共振胆管造影(MRCP)、经内镜逆行胰胆管造影(ERCP)检查,并与手术病理结果比较,评价4种影像方法的诊断效果。结果超声造影、常规超声、MRCP、ERCP对胆总管全程的显示率分别为93.59%、21.79%、97.44%、100.00%,对胆管病灶的显示率分别为91.03%、58.97%、92.31%、97.44%,超声造影与MRCP、ERCP对胆总管全程及胆管病灶的显示率均无显著差异(χ2=0.598、3.306, P>0.05),但超声造影对胆总管全程及胆管病灶的显示率明显高于常规超声(χ2=82.360、21.368, P0.05). Ultrasound contrast was superior to routine ultrasound in displaying the whole common bile duct and bile duct lesions (χ2=82.360, 21.368; P<0.001). The rate of ultrasound contrast in displaying whole pancreas head and duodenal papilla was 100.00% and 71.79%, respectively, which was much higher than those of routine ultrasound (χ2=48.504, 80.031; P<0.001). Conclusion Oral gastrointestinal echogenic contrast agent may improve the display rate of the common bile duct and the lesions in it, which is a simple and reliable method in practice.

  6. Influence of breed and genotype on the onset and distribution of infectivity and disease-associated prion protein in sheep following oral infection with the bovine spongiform encephalopathy agent.

    Science.gov (United States)

    McGovern, G; Martin, S; Jeffrey, M; Bellworthy, S J; Spiropoulos, J; Green, R; Lockey, R; Vickery, C M; Thurston, L; Dexter, G; Hawkins, S A C; González, L

    2015-01-01

    The onset and distribution of infectivity and disease-specific prion protein (PrP(d)) accumulation was studied in Romney and Suffolk sheep of the ARQ/ARQ, ARQ/ARR and ARR/ARR prion protein gene (Prnp) genotypes (where A stands for alanine, R for arginine and Q for glutamine at codons 136, 154 and 171 of PrP), following experimental oral infection with cattle-derived bovine spongiform encephalopathy (BSE) agent. Groups of sheep were killed at regular intervals and a wide range of tissues taken for mouse bioassay or immunohistochemistry (IHC), or both. Bioassay results for infectivity were mostly coincident with those of PrP(d) detection by IHC both in terms of tissues and time post infection. Neither PrP(d) nor infectivity was detected in any tissues of BSE-dosed ARQ/ARR or ARR/ARR sheep or of undosed controls. Moreover, four ARQ/ARQ Suffolk sheep, which were methionine (M)/threonine heterozygous at codon 112 of the Prnp gene, did not show any biological or immunohistochemical evidence of infection, while those homozygous for methionine (MARQ/MARQ) did. In MARQ/MARQ sheep of both breeds, initial PrP(d) accumulation was identified in lymphoreticular system (LRS) tissues followed by the central nervous system (CNS) and enteric nervous system (ENS) and finally by the autonomic nervous system and peripheral nervous system and other organs. Detection of infectivity closely mimicked this sequence. No PrP(d) was observed in the ENS prior to its accumulation in the CNS, suggesting that ENS involvement occurred simultaneously to that of, or followed centrifugal spread from, the CNS. The distribution of PrP(d) within the ENS further suggested a progressive spread from the ileal plexus to other ENS segments via neuronal connections of the gut wall. Differences between the two breeds were noted in terms of involvement of LRS and ENS tissues, with Romney sheep showing a more delayed and less consistent PrP(d) accumulation than Suffolk sheep in such tissues. Whether this

  7. Oral lichen planus: An overview.

    Science.gov (United States)

    Krupaa, R Jayasri; Sankari, S Leena; Masthan, K M K; Rajesh, E

    2015-04-01

    Lichen planus is an immunologically mediated mucocutaneous disease that is triggered by varied etiological agents. The oral lichenoid reaction is considered a variant of the disease that needs to be clearly diagnosed as a separate entity from oral lichen planus and treated. They follow a strict cause-effector relationship, protocols that suggest the differentiation. Lichen planus has varied clinical forms in the oral mucosa and cutaneously that has different prognosis. This condition also arises in association with various other systemic conditions such as hypertension, diabetes mellitus. There have been cases reported in the esophagus, larynx, scalp, nail, cutaneous areas, especially arms and wrists, trunk. There is reported malignant transformation that essentiates careful examination, treatment protocol and regular follow-up sessions. This article throws light on the disease condition of oral lichen planus and oral lichenoid reaction that is essential for the differentiation and treatment.

  8. Oral lichen planus: An overview

    Directory of Open Access Journals (Sweden)

    R Jayasri Krupaa

    2015-01-01

    Full Text Available Lichen planus is an immunologically mediated mucocutaneous disease that is triggered by varied etiological agents. The oral lichenoid reaction is considered a variant of the disease that needs to be clearly diagnosed as a separate entity from oral lichen planus and treated. They follow a strict cause-effector relationship, protocols that suggest the differentiation. Lichen planus has varied clinical forms in the oral mucosa and cutaneously that has different prognosis. This condition also arises in association with various other systemic conditions such as hypertension, diabetes mellitus. There have been cases reported in the esophagus, larynx, scalp, nail, cutaneous areas, especially arms and wrists, trunk. There is reported malignant transformation that essentiates careful examination, treatment protocol and regular follow-up sessions. This article throws light on the disease condition of oral lichen planus and oral lichenoid reaction that is essential for the differentiation and treatment.

  9. [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

  10. What Makes Oral Candidiasis Recurrent Infection? A Clinical View

    OpenAIRE

    Darwazeh, Azmi M. G.; Darwazeh, Tamer A.

    2014-01-01

    Clinical oral Candida infection (candidiasis) is one of the common oral mucosal infections, and its management is usually frustrating due to either treatment failure or recurrence. Historically, oral candidiasis has been branded as disease of diseased. The unsuccessful management of oral candidiasis can due to either incorrect diagnosis, failure to identify (or correct) the underlying predisposing factor(s), or inaccurate prescription of antifungal agents. Failure to properly treat oral ca...

  11. 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.

  12. Current status of oral cancer chemoprevention

    Institute of Scientific and Technical Information of China (English)

    Moni Abraham Kuriakose

    2008-01-01

    @@ Chemoprevention is the administration of agents to block or reverse carcinogenesis. Chemoprevention in oral cancer has been directed towards reversal of premalignant lesion and prevention of second primary tumor.

  13. Betel nut chewing, oral premalignant lesions, and the oral microbiome

    Science.gov (United States)

    Hernandez, Brenda Y.; Zhu, Xuemei; Goodman, Marc T.; Gatewood, Robert; Mendiola, Paul; Quinata, Katrina; Paulino, Yvette C.

    2017-01-01

    Oral cancers are attributed to a number of causal agents including tobacco, alcohol, human papillomavirus (HPV), and areca (betel) nut. Although betel nut chewing has been established as an independent cause of oral cancer, the mechanisms of carcinogenesis are poorly understood. An investigation was undertaken to evaluate the influence of betel nut chewing on the oral microbiome and oral premalignant lesions. Study participants were recruited from a dental clinic in Guam. Structured interviews and oral examinations were performed. Oral swabbing and saliva samples were evaluated by 454 pyrosequencing of the V3- V5 region of the 16S rRNA bacterial gene and genotyped for HPV. One hundred twenty-two adults were enrolled including 64 current betel nut chewers, 37 former chewers, and 21 with no history of betel nut use. Oral premalignant lesions, including leukoplakia and submucous fibrosis, were observed in 10 chewers. Within-sample bacterial diversity was significantly lower in long-term (≥10 years) chewers vs. never chewers and in current chewers with oral lesions vs. individuals without lesions. Between-sample bacterial diversity based on Unifrac distances significantly differed by chewing status and oral lesion status. Current chewers had significantly elevated levels of Streptococcus infantis and higher and lower levels of distinct taxa of the Actinomyces and Streptococcus genera. Long-term chewers had reduced levels of Parascardovia and Streptococcus. Chewers with oral lesions had significantly elevated levels of Oribacterium, Actinomyces, and Streptococcus, including Streptococcus anginosus. In multivariate analyses, controlling for smoking, oral HPV, S.anginosus, and S. infantis levels, current betel nut chewing remained the only predictor of oral premalignant lesions. Our study provides evidence that betel nut chewing alters the oral bacterial microbiome including that of chewers who develop oral premalignant lesions. Nonetheless, whether microbial changes

  14. Recurrent oral ulcers--an overview.

    Science.gov (United States)

    Gaffar, A

    2001-01-01

    Recurrent oral ulcers (ROUs) are the most common oral mucosal disease. The etiology of ROUs is complex. The factors include mechanical trauma, genetics, stress, smoking, and viral and bacterial infections. Treatment modalities depend on the differential diagnosis of ROUs and could consist of antimicrobial agents, anti-inflammatory agents, immunomodulators, or over-the-counter medications. New therapy available in the form of a coating polymer, Colgate ORABASE Soothe.N.Seal, is clinically proven to provide rapid relief and healing of ROUs.

  15. RP-HPLC Characterization of Lupenone and β-Sitosterol in Rhizoma Musae and Evaluation of the Anti-Diabetic Activity of Lupenone in Diabetic Sprague-Dawley Rats

    Directory of Open Access Journals (Sweden)

    Feng Xu

    2014-09-01

    Full Text Available With the aim of characterizing the active ingredients lupenone and β-sitosterol in Rhizoma Musae samples a reversed-phase HPLC method for the separation of these two compounds in Rhizoma Musae samples was developed (regression coefficient > 0.9996. The method was further applied to quantify lupenone and β-sitosterol content in Rhizoma Musae samples cultured in different growth environments. Different variables such as geographical location, growth stage, and harvest time, demonstrated differential effects on lupenone and β-sitosterol levels. Moreover, we determined the optimum conditions for cultivation and harvesting of Rhizoma Musae herbs. Lupenone administration caused a significant reduction in fasting blood glucose (FBG levels in diabetic rats at doses of 1.78, 5.33, and 16.00 mg·kg−1·day−1 for 14 days, the glycated hemoglobin (HbA1c levels of diabetic rats also significantly reduced at doses of 5.33, and 16.00 mg·kg−1·day−1, indicating a robust antidiabetic activity. To our knowledge, this is the first report of an optimized HPLC method successfully applied to quantify lupenone and β-sitosterol, and its applicability in optimizing Rhizoma Musae growth. Animal experiments also showed for the first time that lupenone from Rhizoma Musae has anti-diabetic activity.

  16. Data in support of fumosorinone, a novel PTP1B inhibitor, activates insulin signaling in insulin-resistance HepG2 cells and shows anti-diabetic effect in diabetic KKAy mice

    Directory of Open Access Journals (Sweden)

    Du-Qiang Luo

    2015-09-01

    Full Text Available This data article contains data related to the research article entitled “Fumosorinone, a novel PTP1B inhibitor, activates insulin signaling in insulin-resistance HepG2 cells and shows anti-diabetic effect in diabetic KKAy mice” in the Toxicology and Applied Pharmacology [1]. Fumosorinone (FU is a new inhibitor of protein phosphatase 1B inhibitor, which was isolated from insect pathogenic fungi Isaria fumosorosea. FU was found to inhibit PTP1B activity in our previous study [2]. PTP1B is the physiological antagonist of the insulin signalling pathway. Inhibition of PTP 1B may increase insulin sensitivity [3]. PTP1B has been considered promising as an insulin-sensitive drug target for the prevention and the treatment of insulin-based diseases [4]. We determined the effect of FU on the glucose consumption of IR HepG2 cells. FU caused significant enhancement in glucose consumption by insulin-resistant HepG2 cells compared with control cells.

  17. Data in support of fumosorinone, a novel PTP1B inhibitor, activates insulin signaling in insulin-resistance HepG2 cells and shows anti-diabetic effect in diabetic KKAy mice.

    Science.gov (United States)

    Luo, Du-Qiang; Liu, Zhi-Qin; Liu, Ting; Chen, Chuan; Li, Ming-Yan; Wang, Zi-Yu; Chen, Ruo-Song; Wei, Gui-Xiang; Wang, Xiao-Yi

    2015-09-01

    This data article contains data related to the research article entitled "Fumosorinone, a novel PTP1B inhibitor, activates insulin signaling in insulin-resistance HepG2 cells and shows anti-diabetic effect in diabetic KKAy mice" in the Toxicology and Applied Pharmacology [1]. Fumosorinone (FU) is a new inhibitor of protein phosphatase 1B inhibitor, which was isolated from insect pathogenic fungi Isaria fumosorosea. FU was found to inhibit PTP1B activity in our previous study [2]. PTP1B is the physiological antagonist of the insulin signalling pathway. Inhibition of PTP 1B may increase insulin sensitivity [3]. PTP1B has been considered promising as an insulin-sensitive drug target for the prevention and the treatment of insulin-based diseases [4]. We determined the effect of FU on the glucose consumption of IR HepG2 cells. FU caused significant enhancement in glucose consumption by insulin-resistant HepG2 cells compared with control cells.

  18. Anti-diabetic and anti-oxidant effects of Zingiber officinale on alloxan-induced and insulin-resistant diabetic male rats.

    Science.gov (United States)

    Iranloye, B O; Arikawe, A P; Rotimi, G; Sogbade, A O

    2011-11-23

    This study was designed to investigate the hypoglycaemic and anti-oxidant effects of Zingiber officinale on experimentally induced diabetes mellitus using alloxan and insulin resistance. Aqueous extracts of raw ginger was administered orally at a chosen dose of 500mg/ml for a period of 4 weeks to alloxan-induced diabetic and insulin resistant diabetic rats. The experimental rats exhibited hyperglycaemia accompanied with weight loss to confirm their diabetic state. Ginger effectively reduced fasting blood glucose and malonydealdehyde levels in alloxan-induced diabetic and insulin resistant diabetic rats compared to control and ginger only treated rats. Furthermore, ginger increased serum insulin level and also enhanced insulin sensitivity in alloxan-induced diabetic and insulin resistant diabetic rats compared to control and ginger only treated rats. The results of the study clearly show that dietary ginger has hypoglycaemic effect, enhances insulin synthesis in male rats and has high antioxidant activity. One of the likely mechanisms is the action of malonydealdehyde, which acts as a scavenger of oxygen radicals.

  19. Anti-diabetic efficacy and impact on amino acid metabolism of GRA1, a novel small-molecule glucagon receptor antagonist.

    Directory of Open Access Journals (Sweden)

    James Mu

    Full Text Available Hyperglucagonemia is implicated in the pathophysiology of hyperglycemia. Antagonism of the glucagon receptor (GCGR thus represents a potential approach to diabetes treatment. Herein we report the characterization of GRA1, a novel small-molecule GCGR antagonist that blocks glucagon binding to the human GCGR (hGCGR and antagonizes glucagon-induced intracellular accumulation of cAMP with nanomolar potency. GRA1 inhibited glycogenolysis dose-dependently in primary human hepatocytes and in perfused liver from hGCGR mice, a transgenic line of mouse that expresses the hGCGR instead of the murine GCGR. When administered orally to hGCGR mice and rhesus monkeys, GRA1 blocked hyperglycemic responses to exogenous glucagon. In several murine models of diabetes, acute and chronic dosing with GRA1 significantly reduced blood glucose concentrations and moderately increased plasma glucagon and glucagon-like peptide-1. Combination of GRA1 with a dipeptidyl peptidase-4 inhibitor had an additive antihyperglycemic effect in diabetic mice. Hepatic gene-expression profiling in monkeys treated with GRA1 revealed down-regulation of numerous genes involved in amino acid catabolism, an effect that was paralleled by increased amino acid levels in the circulation. In summary, GRA1 is a potent glucagon receptor antagonist with strong antihyperglycemic efficacy in preclinical models and prominent effects on hepatic gene-expression related to amino acid metabolism.

  20. Oral health promotion interventions on oral yeast in hospitalised and medically compromised patients: a systematic review.

    Science.gov (United States)

    Lam, Otto L T; Bandara, H M H N; Samaranayake, Lakshman P; McGrath, Colman; Li, Leonard S W

    2012-03-01

    Yeast are major aetiological agents of localised oral mucosal lesions, and are also leading causes of nosocomial bloodstream infections. The purpose of this systematic review was to examine the effectiveness of oral health promotion interventions on the prevalence and incidence of these opportunistic oral pathogens in hospitalised and medically compromised patients. The PubMed, ISI Web of Science and Cochrane Library databases were searched for clinical trials assessing the effect of oral health promotion interventions on oral yeast. Chlorhexidine delivered in a variety of oral hygiene products appeared to have some effect on oral yeast, although some studies found equivocal effects. Although a wide array of other compounds have also been investigated, their clinical effectiveness remains to be substantiated. Likewise, the utility of mechanical oral hygiene interventions and other oral health promotion measures such as topical application of salivary substitute, remains unsettled. Although many chemical agents contained in oral hygiene products have proven in vitro activity against oral yeast, their clinical effectiveness and potential role as adjuncts or alternative therapies to conventional treatment remains to be confirmed by further high-quality randomised controlled trials. This is pertinent, given the recent emergence of yeast resistance to conventional antifungal agents.

  1. Oral Antithrombotic Use Among Myocardial Infarction Patients

    NARCIS (Netherlands)

    van der Elst, Menno E; Cisneros-Gonzalez, Nelly; de Blaey, Cornelis J; Buurma, Henk; de Boer, Anthonius

    2003-01-01

    OBJECTIVE: To examine the use of oral antithrombotics (i.e., antiplatelet agents, oral anticoagulants) after myocardial infarction (MI) in the Netherlands from 1988 to 1998. METHODS: Retrospective follow-up of 3800 patients with MI, using data from the PHARMO Record Linkage System. RESULTS: From 198

  2. Oral Histoplasmosis.

    Science.gov (United States)

    Folk, Gillian A; Nelson, Brenda L

    2017-02-20

    A 44-year-old female presented to her general dentist with the chief complaint of a painful mouth sore of 2 weeks duration. Clinical examination revealed an irregularly shaped ulcer of the buccal and lingual attached gingiva of the anterior mandible. A biopsy was performed and microscopic evaluation revealed histoplasmosis. Histoplasmosis, caused by Histoplasma capsulate, is the most common fungal infection in the United States. Oral lesions of histoplasmosis are generally associated with the disseminated form of histoplasmosis and may present as a fungating or ulcerative lesion of the oral mucosa. The histologic findings and differential diagnosis for oral histoplasmosis are discussed.

  3. Oral leukoplakia

    DEFF Research Database (Denmark)

    Holmstrup, Palle; Dabelsteen, Erik

    2016-01-01

    The idea of identifying oral lesions with a precancerous nature, i.e. in the sense of pertaining to a pathologic process with an increased risk for future malignant development, of course is to prevent frank malignancy to occur in the affected area. The most common oral lesion with a precancerous...... nature is oral leukoplakia, and for decades it has been discussed how to treat these lesions. Various treatment modalities, such as systemic therapies and surgical removal, have been suggested. The systemic therapies tested so far include retinoids, extracts of green tea, inhibitors of cyclooxygenase-2...

  4. [Uricosuric agent].

    Science.gov (United States)

    Ohno, Iwao

    2008-04-01

    Urate lowering treatment is indicated in patients with recurrent acute attacks, tophi, gouty arthropathy, radiographic changes of gout, multiple joint involvement, or associated uric acid nephrolithiasis. Uricosuric agents like benzbromarone and probenecid are very useful to treat hyperuricemia as well as allopurinol (xanthine oxidase inhibitor). Uricosuric agents act the urate lowering effect through blocking the URAT1, an urate transporter, in brush border of renal proximal tubular cells. In order to avoid the nephrotoxicity and urolithiasis due to increasing of urinary urate excretion by using uricosuric agents, the proper urinary tract management (enough urine volume and correction of aciduria) should be performed.

  5. Oral pathology.

    Science.gov (United States)

    Niemiec, Brook A

    2008-05-01

    Oral disease is exceedingly common in small animal patients. In addition, there is a very wide variety of pathologies that are encountered within the oral cavity. These conditions often cause significant pain and/or localized and systemic infection; however, the majority of these conditions have little to no obvious clinical signs. Therefore, diagnosis is not typically made until late in the disease course. Knowledge of these diseases will better equip the practitioner to effectively treat them. This article covers the more common forms of oral pathology in the dog and cat, excluding periodontal disease, which is covered in its own chapter. The various pathologies are presented in graphic form, and the etiology, clinical signs, recommended diagnostic tests, and treatment options are discussed. Pathologies that are covered include: persistent deciduous teeth, fractured teeth, intrinsically stained teeth, feline tooth resorption, caries, oral neoplasia, eosinophilic granuloma complex, lymphoplasmacytic gingivostomatitis, enamel hypoplasia, and "missing" teeth.

  6. Herpes - oral

    Science.gov (United States)

    ... this page: //medlineplus.gov/ency/article/000606.htm Herpes - oral To use the sharing features on this page, ... 374. Read More Atopic dermatitis Cancer Fever Genital herpes Mouth ulcers Vesicles Review Date 8/14/2015 Updated ...

  7. Vasoactive Agents

    OpenAIRE

    Husedzinovic, Ino; Bradic, Nikola; Goranovic, Tanja

    2006-01-01

    This article is a short review of vasoactive drugs which are in use in todays clinical practice. In the past century, development of vasoactive drugs went through several phases. All of these drugs are today divided into several groups, depending on their place of action, pharmacological pathways and/or effects on target organ or organ system. Hence, many different agents are today in clinical practice, we have shown comparison between them. These agents provide new directions in the treatmen...

  8. Disparities in Oral Health

    Science.gov (United States)

    ... 2020: Oral Health Objectives Site Map Disparities in Oral Health Recommend on Facebook Tweet Share Compartir Oral health ... to get and keep dental insurance. Disparities in Oral Health Some of the oral health disparities that exist ...

  9. Reactivity and Speciation of Anti-Diabetic Vanadium Complexes in Whole Blood and Its Components: The Important Role of Red Blood Cells.

    Science.gov (United States)

    Levina, Aviva; McLeod, Andrew I; Gasparini, Sylvia J; Nguyen, Annie; De Silva, W G Manori; Aitken, Jade B; Harris, Hugh H; Glover, Chris; Johannessen, Bernt; Lay, Peter A

    2015-08-17

    Reactions with blood components are crucial for controlling the antidiabetic, anticancer, and other biological activities of V(V) and V(IV) complexes. Despite extensive studies of V(V) and V(IV) reactions with the major blood proteins (albumin and transferrin), reactions with whole blood and red blood cells (RBC) have been studied rarely. A detailed speciation study of Na3[V(V)O4] (A), K4[V(IV)2O2(citr)2]·6H2O (B; citr = citrato(4-)); [V(IV)O(ma)2] (C; ma = maltolato(-)), and (NH4)[V(V)(O)2(dipic)] (D; dipic = pyridine-2,6-dicarboxylato(2-)) in whole rat blood, freshly isolated rat plasma, and commercial bovine serum using X-ray absorption near-edge structure (XANES) spectroscopy is reported. The latter two compounds are potential oral antidiabetic drugs, and the former two are likely to represent their typical decomposition products in gastrointestinal media. XANES spectral speciation was performed by principal component analysis and multiple linear regression techniques, and the distribution of V between RBC and plasma fractions was measured by electrothermal atomic absorption spectroscopy. Reactions of A, C, or D with whole blood (1.0 mM V, 1-6 h at 310 K) led to accumulation of ∼50% of total V in the RBC fraction (∼10% in the case of B), which indicated that RBC act as V carriers to peripheral organs. The spectra of V products in RBC were independent of the initial V complex, and were best fitted by a combination of V(IV)-carbohydrate (2-hydroxyacid moieties) and/or citrate (65-85%) and V(V)-protein (15-35%) models. The presence of RBC created a more reducing environment in the plasma fraction of whole blood compared with those in isolated plasma or serum, as shown by the differences in distribution of V(IV) and V(V) species in the reaction products of A-D in these media. At physiologically relevant V concentrations (blood plasma. The results reported herein have broad implications for the roles of RBC in the transport and speciation of metal pro

  10. Anti-diabetic potential of Catharanthus roseus Linn. and its effect on the glucose transport gene (GLUT-2 and GLUT-4) in streptozotocin induced diabetic wistar rats.

    Science.gov (United States)

    Al-Shaqha, Waleed M; Khan, Mohsin; Salam, Nasir; Azzi, Arezki; Chaudhary, Anis Ahmad

    2015-10-21

    Catharanthus roseus is an important Ayurvedic medication in traditional medicine. It is potentially used in countries like India, South Africa, China and Malaysia for the healing of diabetes mellitus. Although, the molecular mechanisms behind this effect are yet to be exclusively explored. Due to the great antidiabetic and hyperlipidemic potential of c. roseus, we hypothesized that the insulin mimetic effect of ethanolic extract of c. roseus might add to glucose uptake through improvement in the expression of genes of the glucose transporter (GLUT) family messenger RNA (mRNA) in liver. STZ-induced diabetic rats treated by ethanolic extract of c. roseus 100 mg/kg and 200 mg/kg; and one group treated with Metformin (100 mg/kg). After final administration of treatment of 4 weeks, blood samples were collected under fasting conditions, and the body weights (BWs) were measured. Total RNA from liver was extracted with the Qiagen RNEasy Micro kit (GERMANY) as described in the manufacturer's instructions. First-strand complementary DNA (cDNA) was synthesized at 40 °C by priming with oligo-dT12-18 (Invitrogen, USA) and using Super ScriptII reverse transcriptase according to the protocol provided by the manufacturer (Invitrogen, USA). Real-time polymerase chain reaction (PCR) amplifications for GLUT-4 (gene ID: 25139) were conducted using Light-Cycler 480 (Roche, USA) with the SyBr® I nucleic acid stain (Invitrogen, USA) according to the manufacturer's instructions. Polymerase chain reaction products of β-actin primer gene were used as an internal standard. The proposed study was framed to look at the antidiabetic efficacy of ethanolic extract of c. roseus and an expression of GLUT-2 and GLUT-4 gene in streptozotocin induced diabetic wistar rats. The doses were administered orally at a rate of 100 and 200 mg/kg and detrain the glucose transport system in liver for 4 weeks. The observed results showed a good positive correlation between intracellular calcium and insulin

  11. Anti-diabetic effect of a combination of andrographolide-enriched extract of Andrographis paniculata (Burm f.) Nees and asiaticoside-enriched extract of Centella asiatica L. in high fructose-fat fed rats.

    Science.gov (United States)

    Nugroho, Agung Endro; Lindawati, Novena Yety; Herlyanti, Kyky; Widyastuti, Lina; Pramono, Suwidjiyo

    2013-12-01

    Traditionally, a combination of medicinal plants is commonly used for lowering blood glucose in diabetic patients in order to provide additional benefits of the single drug. A. paniculata and C. asiatica are two traditional medicines form South Asian and Southeast Asain countries consumed by people for treating daibates mellitus and its complications. Hyperglycemia in the rats was stimulated by high fructose-fat diet that consists of 36% fructose, 15% lard, and 5% egg yolks in 0.36 g/200 g body weight for 70 days. The rats were orally administered with the combination of andrographolide-enriched extract of A. paniculata (AEEAP) leaves and asiaticoside-enriched extract of C. asiatica (AEECA) herbs from day 70 for 7 days. Antidiabetic activity was evaluated by estimating mainly the blood glucose levels and other parameters such as HDL, LDL, cholesterol and triglyceride. The results showed that combination at the ratio of 70:30 exhibited a promosing antidiabetic effect in high-fat-fructose-fed rat, and exhibited sinergistic effects on blood cholesterol and HDL levels. It can be concluded that its antidiabetic effect was better than that of single treatment of AEEAP or AEECA. That combination was also potential to develop as a blood glucose-lowering agent for diabetic patients.

  12. Oral delivery of anticancer drugs

    DEFF Research Database (Denmark)

    Thanki, Kaushik; Gangwal, Rahul P; Sangamwar, Abhay T

    2013-01-01

    The present report focuses on the various aspects of oral delivery of anticancer drugs. The significance of oral delivery in cancer therapeutics has been highlighted which principally includes improvement in quality of life of patients and reduced health care costs. Subsequently, the challenges...... incurred in the oral delivery of anticancer agents have been especially emphasized. Sincere efforts have been made to compile the various physicochemical properties of anticancer drugs from either literature or predicted in silico via GastroPlus™. The later section of the paper reviews various emerging...... trends to tackle the challenges associated with oral delivery of anticancer drugs. These invariably include efflux transporter based-, functional excipient- and nanocarrier based-approaches. The role of drug nanocrystals and various others such as polymer based- and lipid based...

  13. [Inotropic agents].

    Science.gov (United States)

    Sasayama, Shigetake

    2003-05-01

    Depression of myocardial contractility plays an important role in the development of heart failure and many inotropic agents were developed to improve the contractile function of the failing heart. Agents that increase cyclic AMP, either by increasing its synthesis or reducing its degradation, exerted dramatic short-term hemodynamic benefits, but these acute effects were not extrapolated into long-term improvement of the clinical outcome of heart failure patients. Administration of these agents to an energy starved failing heart would be expected to increase myocardial energy use and could accelerate disease progression. The role of digitalis in the management of heart failure has been controversial, however, the recent large scale clinical trial has ironically proved that digoxin reduced the rate of hospitalization both overall and for worsening heart failure. More recently, attention was paid to other inotropic agents that have a complex and diversified mechanism. These agents have some phosphodiesterase-inhibitory action but also possess additional effects, including cytokine inhibitors, immunomodulators, or calcium sensitizers. In the Western Societies these agents were again shown to increase mortality of patients with severe heart failure in a dose dependent manner with the long-term administration. However, it may not be the case in the Japanese population in whom mortality is relatively low. Chronic treatment with inotropic agent may be justified in Japanese, as it allows optimal care in the context of relief of symptoms and an improved quality of life. Therefore, each racial group should obtain specific evidence aimed at developing its own guidelines for therapy rather than translating major guidelines developed for other populations.

  14. Sunscreening Agents

    Science.gov (United States)

    Martis, Jacintha; Shobha, V; Sham Shinde, Rutuja; Bangera, Sudhakar; Krishnankutty, Binny; Bellary, Shantala; Varughese, Sunoj; Rao, Prabhakar; Naveen Kumar, B.R.

    2013-01-01

    The increasing incidence of skin cancers and photodamaging effects caused by ultraviolet radiation has increased the use of sunscreening agents, which have shown beneficial effects in reducing the symptoms and reoccurrence of these problems. Many sunscreen compounds are in use, but their safety and efficacy are still in question. Efficacy is measured through indices, such as sun protection factor, persistent pigment darkening protection factor, and COLIPA guidelines. The United States Food and Drug Administration and European Union have incorporated changes in their guidelines to help consumers select products based on their sun protection factor and protection against ultraviolet radiation, whereas the Indian regulatory agency has not yet issued any special guidance on sunscreening agents, as they are classified under cosmetics. In this article, the authors discuss the pharmacological actions of sunscreening agents as well as the available formulations, their benefits, possible health hazards, safety, challenges, and proper application technique. New technologies and scope for the development of sunscreening agents are also discussed as well as the role of the physician in patient education about the use of these agents. PMID:23320122

  15. A randomised phase 1 study to investigate safety, pharmacokinetics and impact on gut microbiota following single and multiple oral doses in healthy male subjects of SMT19969, a novel agent for Clostridium difficile infections.

    Science.gov (United States)

    Vickers, Richard; Robinson, Neil; Best, Emma; Echols, Roger; Tillotson, Glenn; Wilcox, Mark

    2015-02-25

    Clostridium difficile infection (CDI) is a leading cause of diarrhoea in health care settings with symptoms ranging from mild and self-limiting to life threatening. SMT19969 is a novel, non-absorbable antibiotic currently under development for the treatment of CDI. Here we report the results from a Phase I study. A double-blind, randomized, placebo-controlled study assessing safety and tolerability of single and multiple oral doses of SMT19969 in healthy volunteers. Pharmacokinetic assessments included blood and faecal sampling. The effect of food on systemic exposure and analysis of the gut microbiota were also included. Fifty-six healthy male subjects were enrolled. Following single oral doses of up to 2,000 mg in the fasted state, plasma concentrations of SMT19969 were generally below the lower limit of quantification. In the fed state levels ranged from 0.102 to 0.296 ng/mL after single dosing and after repeat dosing at Day 10 from 0.105 to 0.305 ng/mL. Following single and multiple oral doses of SMT19969, mean daily faecal concentrations increased with increasing dose level and were significantly above the typical MIC range for C. difficile (0.06-0.5 μg/mL). At 200 mg BID, mean (± SD) faecal concentrations of 1,466 (±547) μg/g and 1,364 (±446) μg/g were determined on days 5 and 10 of dosing respectively. No notable metabolites were detected in faeces. Overall, all doses of SMT19969 were well tolerated both as single oral doses or BID oral doses for 10 days. The majority (88%) of adverse events (AEs) were classified as gastrointestinal disorders and were mild in severity, resolving without treatment. The gut microbiota was analysed in the multiple dose groups with minimal changes observed in the bacterial groups analysed except for total clostridia which were reduced to below the limit of detection by day 4 of dosing. Oral administration of SMT19969 was considered safe and well tolerated and was associated with negligible plasma concentrations after

  16. Management of Patients with Oral Candidiasis

    DEFF Research Database (Denmark)

    Kragelund, Camilla; Reibel, Jesper; Pedersen, Anne Marie Lynge

    2016-01-01

    Oral candidal infections are medically treated with antifungal agents. In the fungal cell membrane, steroid ergosterol is the target of the antifungals on the market, but similarity with the human cell membrane may cause host toxicity and unintended reactions. Management of oral candidiasis depends...... in particular in patients with recurrent oral candidiasis. This risk can be reduced if different types of antifungal drugs are used over time or are combined. This chapter focuses on antifungal treatment of the medically compromised patient with oral candidiasis by highlighting the advantages and disadvantages...

  17. Mobile Agents

    Science.gov (United States)

    Satoh, Ichiro

    Mobile agents are autonomous programs that can travel from computer to computer in a network, at times and to places of their own choosing. The state of the running program is saved, by being transmitted to the destination. The program is resumed at the destination continuing its processing with the saved state. They can provide a convenient, efficient, and robust framework for implementing distributed applications and smart environments for several reasons, including improvements to the latency and bandwidth of client-server applications and reducing vulnerability to network disconnection. In fact, mobile agents have several advantages in the development of various services in smart environments in addition to distributed applications.

  18. Comparison of neutral oral contrast versus positive oral contrast medium in abdominal multidetector CT

    Energy Technology Data Exchange (ETDEWEB)

    Berther, Ralph; Eckhardt, Boris; Zollikofer, Christoph L. [Kantonsspital, Institute of Radiology, Winterthur (Switzerland); Patak, Michael A. [Kantonsspital, Institute of Radiology, Winterthur (Switzerland); Inselspital, University Hospital of Bern, Institute of Diagnostic, Interventional and Paediatric Radiology, Bern (Switzerland); Erturk, Sukru M. [Sisli Etfal Education and Research Hospital, Department of Radiology, Istanbul (Turkey)

    2008-09-15

    To determine whether neutral contrast agents with water-equivalent intraluminal attenuation can improve delineation of the bowel wall and increase overall image quality for a non-selected patient population, a neutral oral contrast agent (3% mannitol) was administered to 100 patients referred for abdominal multidetector row computed tomography (MDCT). Their results were compared with those of 100 patients given a positive oral contrast agent. Qualitative and quantitative measurements were done on different levels of the gastrointestinal tract by three experienced readers. Patients given the neutral oral contrast agent showed significant better qualitative results for bowel distension (P<0.001), homogeneity of the luminal content (P<0.001), delineation of the bowel-wall to the lumen (P<0.001) and to the mesentery (P<0.001) and artifacts (P<0.001), leading to a significant better overall image quality (P<0.001) than patients receiving positive oral contrast medium. The quantitative measurements revealed significant better distension (P<0.001) and wall to lumen delineation (P<0.001) for the patients receiving neutral oral contrast medium. The present results show that the neutral oral contrast agent (mannitol) produced better distension, better homogeneity and better delineation of the bowel wall leading to a higher overall image quality than the positive oral contrast medium in a non-selected patient population. (orig.)

  19. Adherence to oral antineoplastic therapy

    Directory of Open Access Journals (Sweden)

    R. Olivera-Fernandez

    2014-04-01

    Full Text Available Background: Oral chemotherapy agents offer advantages including cost, patient comfort and potential improvement in quality of life versus intravenous drugs. However ensuring adherence and monitoring adverse effects is more difficult. The aim of this study was to examine the real adherence in patients with oral chemotherapy agents in our hospital, to assess the influence of patient and treatment characteristics, to identify reasons for non adherence, to identify pportunities for improvement pharmaceutical care and to assess the potential relation between adherence and treatment outcomes. Method: observational, prospective study for a period of four month, in the patients who were dispensing oral chemotherapy agents in outpatient setting. The medical prescriptions, medical history and patient interviews were used to collect data. Results: 141 patients were assessing. 72% were considered as fully adherent, while 28% reported some kind of non adherence. Adherence was influenced by time from diagnosis and adverse effects. No relationship between adherence and treatment outcomes was found. Conclusions: Adherence to oral chemotherapy was 72%, identifing opportunities for improvement pharmaceutical care to prevent adverse effects and to improve our patient adherence

  20. Oral myiasis

    Directory of Open Access Journals (Sweden)

    Treville Pereira

    2010-01-01

    Full Text Available Myiasis is a relatively rare condition arising from the invasion of body tissues or cavities of living animals or humans by maggots or larvae of certain species of flies. It is an uncommon clinical condition, being more frequent in underdeveloped countries and hot climate regions, and is associated with poor hygiene, suppurative oral lesions; alcoholism and senility. Its diagnosis is made basically by the presence of larvae. The present article reports a case of oral myiasis involving 20 larvae in a patient with neurological deficiency.

  1. Long-term safety and efficacy of linagliptin as monotherapy or in combination with other oral glucose-lowering agents in 2121 subjects with type 2 diabetes: up to 2 years exposure in 24-week phase III trials followed by a 78-week open-label extension.

    Science.gov (United States)

    Gomis, R; Owens, D R; Taskinen, M-R; Del Prato, S; Patel, S; Pivovarova, A; Schlosser, A; Woerle, H-J

    2012-08-01

    Aim:  The aim of this study was to evaluate the long-term safety, tolerability and efficacy of the dipeptidyl peptidase-4 inhibitor linagliptin given either alone or in combination with other oral glucose-lowering agents in persons with type 2 diabetes. Methods:  A 78-week open-label extension study evaluated subjects who participated in one of four preceding 24-week, randomised, double-blind, placebo-controlled parent trials and who received linagliptin, linagliptin + metformin, linagliptin + metformin + a sulphonylurea or linagliptin + pioglitazone (all with linagliptin administered orally once daily). Individuals receiving one of these treatments during a previous trial continued the same treatment (n = 1532) for up to a total of 102 weeks, whereas those previously receiving placebo were switched to linagliptin (n = 589). All 2121 participants received at least one dose of the trial medication and were included in the primary safety analysis. Results:  In subjects previously receiving active treatment, the glycosylated haemoglobin A(1c) reduction achieved during the 24-week parent trials was sustained through the 78-week extension period (change from baseline to week 102: -0.8%). Drug-related adverse events were experienced by 14.3% of participants. Hypoglycaemia occurred in 13.9% of participants and was similar between those previously receiving treatment (13.6%) and those switching from placebo to linagliptin (14.6%). Hypoglycaemia occurred most frequently with the use of metformin + a sulphonylurea background therapy (11%). Overall, no clinically relevant changes in body weight were observed. Conclusion:  Long-term treatment with linagliptin was well tolerated with no change in the safety profile observed during the extension study. Sustained long-term glycaemic control was maintained for up to 102 weeks with either linagliptin monotherapy or linagliptin in combination with other oral glucose-lowering agents. © 2012

  2. Antibiotic Agents

    Science.gov (United States)

    ... agents. A recent survey reported that 76% of liquid soaps from 10 states in the US contained triclosan ... regulated depends upon its intended use and its effectiveness. The US Food and Drug Administration (FDA) regulates antibacterial soaps and antibacterial substances that will either be used ...

  3. Oral calcitonin

    Directory of Open Access Journals (Sweden)

    Hamdy RC

    2012-09-01

    Full Text Available Ronald C Hamdy,1,2 Dane N Daley11Osteoporosis Center, College of Medicine, East Tennessee State University, 2Veterans Affairs Medical Center, Johnson City, TN, USAAbstract: Calcitonin is a hormone secreted by the C-cells of the thyroid gland in response to elevations of the plasma calcium level. It reduces bone resorption by inhibiting mature active osteoclasts and increases renal calcium excretion. It is used in the management of postmenopausal osteoporosis, Paget's disease of bone, and malignancy-associated hypercalcemia. Synthetic and recombinant calcitonin preparations are available; both have similar pharmacokinetic and pharmacodynamic profiles. As calcitonin is a peptide, the traditional method of administration has been parenteral or intranasal. This hinders its clinical use: adherence with therapy is notoriously low, and withdrawal from clinical trials has been problematic. An oral formulation would be more attractive, practical, and convenient to patients. In addition to its effect on active osteoclasts and renal tubules, calcitonin has an analgesic action, possibly mediated through β-endorphins and the central modulation of pain perception. It also exerts a protective action on cartilage and may be useful in the management of osteoarthritis and possibly rheumatoid arthritis. Oral formulations of calcitonin have been developed using different techniques. The most studied involves drug-delivery carriers such as Eligen® 8-(N-2hydroxy-5-chloro-benzoyl-amino-caprylic acid (5-CNAC (Emisphere Technologies, Cedar Knolls, NJ. Several factors affect the bioavailability and efficacy of orally administered calcitonin, including amount of water used to take the tablet, time of day the tablet is taken, and proximity to intake of a meal. Preliminary results looked promising. Unfortunately, in two Phase III studies, oral calcitonin (0.8 mg with 200 mg 5-CNAC, once a day for postmenopausal osteoporosis and twice a day for osteoarthritis failed to

  4. Radioprotective Agents

    Science.gov (United States)

    1982-01-01

    claimed to be effective are gallic acid derivatives, eg, sodium gallate 12053-21-61 (295-297) and propyl gallate 1121-79-91 (298). p...inhibition of a-adrenergic receptors can be achieved through the use of the antiradiation agents 2-(5-aminopentylamino)ethanephos- phorothioic acid ...tissue was ap- preciated immediately as a potential medical set, and they were put to use en- thusiastically. Early workers did notice an erythematous

  5. Oral Cancer Exam

    Medline Plus

    Full Text Available ... Topics > Oral Cancer > Oral Cancer Exam Video Oral Cancer Exam Video This video shows what happens during an oral cancer examination. Quick and painless, the exam can detect ...

  6. Oral Cancer Exam

    Medline Plus

    Full Text Available ... Topics > Oral Cancer > Oral Cancer Exam Video Oral Cancer Exam Video This video shows what happens during an oral cancer examination. Quick and painless, the exam can detect ...

  7. Oral inoculation of neonatal Suffolk sheep with the agent of classical scrapie results in PrPSc accumulation in sheep with the PRNP ARQ/ARQ but not the ARQ/ARR genotype

    Science.gov (United States)

    Background Scrapie is a transmissible spongiform encephalopathy that can be transmitted amongst susceptible sheep. The prion protein gene (PRNP) profoundly influences the susceptibility of sheep to the scrapie agent. Findings This study reports the failure to detect PrPSc in nervous or lymphoid tis...

  8. Oral health promotion interventions on oral reservoirs of staphylococcus aureus: a systematic review.

    Science.gov (United States)

    Lam, O L T; McGrath, C; Bandara, H M H N; Li, L S W; Samaranayake, L P

    2012-04-01

    The oral cavity serves as a reservoir of Staphylococcus aureus for infection of the lower respiratory tract and cross-infection to other patients. This systematic review was designed to examine the effectiveness of oral health promotion interventions on this pathogen. The PubMed, ISI Web of Science, and Cochrane Library databases were searched for clinical trials assessing the effect of oral health promotion interventions on oral and oropharyngeal carriage of S. aureus. Oral health promotion interventions on oral reservoirs of S. aureus in both systemically healthy and medically compromised groups consisted of oral hygiene interventions only. There was a lack of evidence pertaining to the effectiveness of mechanical oral hygiene interventions against this pathogen. Chlorhexidine delivered in oral hygiene products such as mouthrinses, gels, and sprays appeared to have some utility against S. aureus, although some studies found equivocal effects. There was a dearth of studies investigating the efficacy of other chemical agents. Although many chemical agents contained in oral hygiene products have proven in vitro activity against S. aureus, their clinical effectiveness and potential role as adjuncts or alternative therapies to conventional treatment remain to be confirmed by further high-quality randomized controlled trials.

  9. Use of Oral Antihistamine Agents in Beijing, Shanghai and Guangzhou in 2013%2013年北京、上海、广州地区医院口服抗组胺药应用分析

    Institute of Scientific and Technical Information of China (English)

    曹媛; 罗美娟; 邓蓉蓉; 夏延哲

    2014-01-01

    目的:了解2013年北京、上海和广州地区医院口服抗组胺药的应用情况,促进合理用药。方法:采用《医院处方分析》课题数据库,调查2013年北京、上海、广州地区医院口服抗组胺药的用药频度( DDDs )、限定日费用( DDC )、销售总金额、排序比( B/A)、药物利用指数( DUI)以及各代口服抗组胺药处方数和取药数量占比,并进行回顾性统计、分析。结果:2013年北京、上海和广州地区医院口服抗组胺药使用频率和销售总额排序居首位的分别为西替利嗪、左西替利嗪和地氯雷他定;抗组胺药的DUI均≤1;应用最多的抗组胺药为第2代抗组胺药。结论:北京、上海和广州地区医院使用口服抗组胺药较合理,第2代抗组胺药成为临床上治疗过敏性疾病的常用药物。%OBJECTIVE:To investigate the use of antihistamine agents of in Beijing, Shanghai and Guangzhou in 2013 and its rationality. METHODS:The use of antihistamine agents of in Beijing, Shanghai and Guangzhou in 2013 was investigated retrospectively in respect of DDDs, daily drug cost(DDC), consumption sum, order ratio, drug utilization index( DUI) and the ratio of the number of prescriptions to consumption quantity of antihistamine agents by taking the Project of Hospital Prescription Analysis. RESULTS:The leading antihistamine agents in terms of DDDs and consumption sum in Beijing, Shanghai and Guangzhou in 2013 were Cetirizine, Levocetirizine and Desloratadine respectively. The DUIs of antihistamine agents were all less than 1. The second generation antihistamines were the most frequently used antihistamines. CONCLUSIONS:The use of antihistamine agents in Beijing, Shanghai and Guangzhou was rational and the second generation of antihistamine agents have become the common medications for allergic reactions.

  10. The observation of curative effect of combined with insulin therapy after failure treatment with oral hypoglycemic agents for type 2 diabetes%口服降糖药治疗2型糖尿病失效联合甘精胰岛素治疗疗效观察

    Institute of Scientific and Technical Information of China (English)

    熊东林

    2013-01-01

    目的:观察口服降糖药治疗2型糖尿病失效后,联合甘精胰岛素治疗糖尿病的疗效。方法筛选68例单用口服降糖药血糖控制不理想的2型糖尿病患者,睡前(2130)加用甘精胰岛素(来得时),治疗14周,比较前后空腹血糖(FPG)、餐后2h血糖(2hPG)、糖化血红蛋白(HbA1c)、空腹C肽、餐后2hC肽、体重变化及低血糖的发生。结果加用甘精胰岛素组治疗14周后,患者FPG、2hPG、HbA1c较治疗前明显下降(P<0.01),餐后2hC肽较治疗前明显升高(P<0.01),未见低血糖发生,体重指数影响不大。结论对单用口服药效果不佳的2型糖尿病,需及时加用甘精胰岛素治疗。%Objective To observe the curative effect of combined with insulin therapy after failure treatment with oral hypoglycemic agents for type 2 diabetes. Method Screening 68 cases with oral hypoglycemic agents alone with no ideal blood sugar control in type 2 diabetes, patients bedtime(9 30 pm) plus insulin glargine(Lantus) treatment with 14 weeks treatment, compared before and after FPG, 2hPG, HbA1c, fasting C peptide, 2h postprandial C-peptide, weight changes and the occurrence of low blood sugar. Results Combined with insulin treatment after 14 weeks , patients’s FPG, 2hPG, HbA1c significantly decreased than that before treatment(P<0.01), and with postprandial 2h C-peptide significantly higher(P<0.01). Conclusion It should be timely combined with insulin after failure treatment with oral hypoglycemic agents alone for type 2 diabetes.

  11. Oral dirofilariasis

    Directory of Open Access Journals (Sweden)

    R S Desai

    2015-01-01

    Full Text Available Dirofilaria is parasitic nematodes of domestic and wild animals that can infect humans accidentally via vectors. Its occurrence in the oral cavity is extremely rare. The most frequent presentation of human dirofilariasis is a single submucosal nodule without signs of inflammation. We hereby, report a case of human dirofilariasis affecting the buccal mucosa in a 32-year-old farmer caused by D. repens.

  12. Oral leiomyomas.

    Science.gov (United States)

    Damm, D D; Neville, B W

    1979-04-01

    Oral leiomyomas are considered to be rare neoplasms, but they may be encountered more frequently than generally believed. Three types of leiomyomas are commonly described: solid leiomyomas, angiomyomas, and epithelioid leiomyomas. Three cases of solid leiomyoma are presented, all of which occurred in the anterior mandibular mucobuccal fold. Leiomyomas can be easily confused with other spindle-cell tumors. The necessity of using special stains, especially Mallory's phosphotungstic acid hematoxylin, is discussed.