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Sample records for antidiabetic agents effect

  1. Oral Antidiabetic Agents and Cardiovascular Outcomes

    DEFF Research Database (Denmark)

    Pareek, Manan; Bhatt, Deepak L

    2018-01-01

    Cardiovascular disease is the leading cause of morbidity and mortality among patients with type 2 diabetes; however, a direct protective effect of tight glycemic control remains unproven. In fact, until 2008, when concerns related to rosiglitazone prompted regulatory agencies to mandate assessment...... of cardiovascular safety of new antidiabetic agents, little was known about how these medications affected cardiovascular outcomes. Since then, there has been a considerable increase in the number of cardiovascular trials, which employ a noninferiority design and focus on high-risk populations to establish safety...... in the shortest time possible. In this article, we summarize the 4 major cardiovascular outcome trials of oral antidiabetic agents, completed so far. These include 3 dipeptidyl peptidase-4 inhibitors (saxagliptin, alogliptin, and sitagliptin) and 1 sodium-glucose cotransporter-2 inhibitor (empagliflozin). We...

  2. Comparative Efficacy and Acceptability of Anti-Diabetic Agents for Alzheimer's Disease and Mild Cognitive Impairment: A Systematic Review and Network Meta-analysis.

    Science.gov (United States)

    Cao, Bing; Rosenblat, Joshua D; Brietzke, Elisa; Park, Caroline; Lee, Yena; Musial, Natalie; Pan, Zihang; Mansur, Rodrigo B; McIntyre, Roger S

    2018-05-23

    The current meta-analysis compares the efficacy (i.e., pro-cognitive effects) and acceptability of anti-diabetic agents for Alzheimer's disease (AD) and mild cognitive impairment (MCI). Cochrane Library (CENTRAL), PubMed/MEDLINE, EMBASE and PsycINFO were searched from inception to January 15, 2018 for randomized controlled trials (RCTs) comparing anti-diabetic agents with placebo and/or another active anti-diabetic agent for the treatment of AD or MCI. Nineteen eligible studies (n = 4,855) evaluating the effects of six different anti-diabetic drugs (i.e., intranasal insulin, pioglitazone, rosiglitazone, metformin, sitagliptin and liraglutide) were included. The results of 29 pairwise comparisons indicated that cognition was significantly improved in subjects treated with anti-diabetic agents compared to placebo. Pioglitazone 15-30 mg demonstrated the greatest efficacy compared to placebo in network meta-analysis. No significant differences in acceptability were identified when comparing agents with each other and with placebo. The current findings indicate a pro-cognitive class effect of anti-diabetic agents in AD/MCI. Other anti-diabetic agents should also be investigated in future studies. This study is registered with PROSPERO (CRD42018085967). This article is protected by copyright. All rights reserved. This article is protected by copyright. All rights reserved.

  3. Factors Associated with Treatment Response to Antidiabetic Agents ...

    African Journals Online (AJOL)

    Tropical Journal of Pharmaceutical Research March 2014; 13 (3): 429-435. ISSN: 1596-5996 (print); ... Antidiabetic Agents in Compliant Type 2 Diabetes Mellitus. Patients: A Brief Summary of ..... Qualitative Analysis. There were no significant ...

  4. Nano-preparation of Andrographis paniculata extract by casein micelle for antidiabetic agent

    Science.gov (United States)

    Arbianti, Rita; Dewi, Veronica; Imansari, Farisa; Hermansyah, Heri; Sahlan, Muhamad

    2017-02-01

    Side effects caused by oral medications for person with diabetic are the background of the development of alternative treatments by traditional medicine, herbs. Andrographis paniculata (AP) is one of the herbs that is potent to be anti-diabetic agent. The active compound of AP, andrographolide have been examined to have anti-diabetic activity as α-glucosidase enzyme inhibitor. This research aims to encapsulate sambiloto's extract with casein micelle and produce nanoparticles which have anti-diabetic activity as α-glucosidase inhibitor. Extract of AP is encapsulated by casein micelle and made into nano size using sonicator. The dominant active compounds in AP extract coated by casein are andrographolide, neoandrographolide, 14-deoxy-11,12didehydroandrographolide with encapsulation efficiency of 68.83%, 89.15% and 81.69%, the average diameter of the particles is about 120.57 nm and its loading capacity is 28.85%. AP's extract has antidiabetic activity as α-glucosidase inhibitor with percent inhibition of 95%. The morphology of nanoencapsulated AP's extract analyzed by FE-SEM, were similar with casein micelle.

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

    Directory of Open Access Journals (Sweden)

    Campbell-Tofte JI

    2012-08-01

    , should be used for cost-effective validation of the safety and anti-diabetic efficacy of promising medicinal plants. The application of such approaches to studying entire mixtures of plant materials will ensure proper elucidation of novel therapies with improved mechanisms of action, as well as facilitate a personalized clinical use of medicinal plants as anti-diabetic agents.Keywords: medicinal plants, anti-diabetes therapy, natural products, systems biology, 'omics technologies, drug discovery

  6. Antidiabetic Effects of Resveratrol: The Way Forward in Its Clinical Utility

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    Omolola R. Oyenihi

    2016-01-01

    Full Text Available Despite recent advances in the understanding and management of diabetes mellitus, the prevalence of the disease is increasing unabatedly with resulting disabling and life-reducing consequences to the global human population. The limitations and side effects associated with current antidiabetic therapies have necessitated the search for novel therapeutic agents. Due to the multipathogenicity of diabetes mellitus, plant-derived compounds with proven multiple pharmacological actions have been postulated to “hold the key” in the search for an affordable, efficacious, and safer therapeutic agent in the treatment of the disease and associated complications. Resveratrol, a phytoalexin present in few plant species, has demonstrated beneficial antidiabetic effects in animals and humans through diverse mechanisms and multiple molecular targets. However, despite the enthusiasm and widespread successes achieved with the use of resveratrol in animal models of diabetes mellitus, there are extremely limited clinical data to confirm the antidiabetic qualities of resveratrol. This review presents an update on the mechanisms of action and protection of resveratrol in diabetes mellitus, highlights challenges in its clinical utility, and suggests the way forward in translating the promising preclinical data to a possible antidiabetic drug in the near future.

  7. ANTI-DIABETIC EFFECTS OF TURMERIC IN ALLOXAN INDUCE D DIABETIC RATS

    OpenAIRE

    Jeevangi; Manjunath; Deepak D; Prakash G; Prashant; Chetan

    2013-01-01

    ABSTRACT: OBJECTIVE AND BACKGROUND: Turmeric (Curcuma longa) is one of the common constituents of our daily food. The present study wa s undertaken to evaluate the anti-diabetic effects of ethanolic extract of Rhizomes of curcuma longa in alloxan induced diabetic rats and compared with of Pioglitazone, which is the standard anti-diabetic agent. METHODS: Alloxan monohydrate is used to induce diabetes mellitus in albino rats in the dose of 120mg/kg i.p. and ...

  8. Cinnamic Acid Derivatives as Antidiabetics Agents

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    Teni Ernawati

    2017-04-01

    Full Text Available Diabetes mellitus is a metabolic disorder of carbohydrate metabolism. Treatment of type II diabetes is usually done by prescribing diet and exercise for the patient however it can also be treated with antidiabetic drugs. The purpose of this paper is to illustrate some cinnamic acid derivative compounds which are either isolated from natural materials or the results of the chemical synthesis. In addition, their biological activities as an agent of α-glucosidase inhibitors have also been evaluated. Chemically, cinnamic acid has three main functional groups:  first is the substitution on the phenyl group, second is the additive reaction into the α-β unsaturated, and third is the chemical reaction with carboxylic acid functional groups. Chemical aspects of cinnamic acid derivative compounds have received much attention in the research and development of drugs, especially modifications within three functional groups are very influential. In the last 10 years, a lot of research and development of cinnamic acid derivatives as inhibitors of the α-glucosidase enzyme has been done. One example of the research done in this field is the modification of para position in the structure of cinnamic acid and addition of alkyl groups in the carboxylic group which would increase the activity of the α-glucosidase enzyme therefore the level of inhibition is 100 times higher than that of cinnamic acid compound itself. The novelty of this review article is to focus on the antidiabetic activity of cinnamic acid derivatives.

  9. Ficus Deltoidea: A potential source for new oral antidiabetic agent

    International Nuclear Information System (INIS)

    Zainah Adam; Juliana Mahamad Napiah; Shafii Khamis; Muhajir Hamid

    2012-01-01

    Ficus deltoidea or locally known as Mas Cotek is one of the common medicinal plant used in Malaysia. Ethno botanical approaches showed that this plant possess antidiabetic property. Previous study had shown that F. deltoidea reduced hyperglycemia in type I diabetic rats at different prandial state. This study was done to elucidate the possible antihyperglycemic mechanisms of F. deltoidea. The results showed that F. deltoidea significantly stimulated insulin secretion from pancreatic β-cells with the highest magnitude of stimulation was 7.31-fold (p 50 value was 4.15±0.25 mg/ml. Kinetic analysis of the enzyme activity revealed the F. deltoidea exhibited a mixed-type inhibition mechanism against sucrase activity. Such observations showed that F. deltoidea has the potential to be developed as new oral antidiabetic agent for the treatment of diabetes mellitus. (author)

  10. Utilization study of antidiabetic agents in a teaching hospital of Sikkim and adherence to current standard treatment guidelines.

    Science.gov (United States)

    Satpathy, Sushrut Varun; Datta, Supratim; Upreti, Binu

    2016-01-01

    Diabetes has gradually emerged as one of the most serious public health problems in our country. This underlines the need for timely disease detection and decisive therapeutic intervention. This prospective cross-sectional observational study aims at analyzing the utilization pattern of antidiabetic agents in a remote North-East Indian tertiary care teaching hospital in the perspective of current standard treatment guidelines. Diabetic patients receiving antidiabetic medication, both as outpatients and inpatients in our hospital over a period of 12 months (May 2013-May 2014), were included in this study. The data obtained were sorted and analyzed on the basis of gender, type of therapy, and hospital setting. A total of 310 patients were included in the study. Metformin was the single most frequently prescribed antidiabetic agent (66.8%) followed by the sulfonylureas group (37.4%). Insulin was prescribed in 23.2% of the patients. Combination antidiabetic drug therapy (65.1%) was used more frequently than monotherapy (34.8%). The use of biguanides (P standard treatment guidelines. Increased use of generic drugs is an area with scope for improvement.

  11. Potential of Lichen Compounds as Antidiabetic Agents with Antioxidative Properties: A Review

    Science.gov (United States)

    Karunaratne, Veranja

    2017-01-01

    The advancement in the knowledge of potent antioxidants has uncovered the way for greater insight in the treatment of diabetic complications. Lichens are a rich resource of novel bioactive compounds and their antioxidant potential is well documented. Herein we review the antidiabetic potential of lichens which have received considerable attention, in the recent past. We have correlated the antidiabetic and the antioxidant potential of lichen compounds. The study shows a good accordance between antioxidant and antidiabetic activity of lichens and points out the need to look into gathering the scarce and scattered data on biological activities for effective utilization. The review establishes that the lichen extracts, especially of Parmotrema sp. and Ramalina sp. have shown promising potential in both antidiabetic and antioxidant assays. Ubiquitous compounds, namely, zeorin, methylorsellinate, methyl-β-orcinol carboxylate, methyl haematommate, lecanoric acid, salazinic acid, sekikaic acid, usnic acid, gyrophoric acid, and lobaric acid have shown promising potential in both antidiabetic as well as antioxidant assays highlighting their potential for effective treatment of diabetic mellitus and its associated complications. The available compilation of this data provides the future perspectives and highlight the need for further studies of this potent herbal source to harvest more beneficial therapeutic antidiabetic drugs. PMID:28491237

  12. Chemical and Biological Aspects of Extracts from Medicinal Plants with Antidiabetic Effects.

    Science.gov (United States)

    Gushiken, Lucas F; Beserra, Fernando P; Rozza, Ariane L; Bérgamo, Patrícia L; Bérgamo, Danilo A; Pellizzon, Cláudia H

    2016-01-01

    Diabetes mellitus is a chronic disease and a leading cause of death in western countries. Despite advancements in the clinical management of the disease, it is not possible to control the late complications of diabetes. The main characteristic feature of diabetes is hyperglycemia, which reflects the deterioration in the use of glucose due to a faulty or poor response to insulin secretion. Alloxan and streptozotocin (STZ) are the chemical tools that are most commonly used to study the disease in rodents. Many plant species have been used in ethnopharmacology or to treat experimentally symptoms of this disease. When evaluated pharmacologically, most of the plants employed as antidiabetic substances have been shown to exhibit hypoglycemic and antihyperglycemic activities, and to contain chemical constituents that may be used as new antidiabetic agents. There are many substances extracted from plants that offer antidiabetic potential, whereas others may result in hypoglycemia as a side effect due to their toxicity, particularly their hepatotoxicity. In this article we present an updated overview of the studies on extracts from medicinal plants, relating the mechanisms of action by which these substances act and the natural principles of antidiabetic activity.

  13. Metformin-like antidiabetic, cardio-protective and non-glycemic effects of naringenin: Molecular and pharmacological insights.

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    Nyane, Ntsoaki Annah; Tlaila, Thabiso Bethwel; Malefane, Tanki Gabriel; Ndwandwe, Dudu Edith; Owira, Peter Mark Oroma

    2017-05-15

    Metformin is a widely used drug for the treatment of type 2 diabetes (T2D). Its blood glucose-lowering effects are initially due to inhibition of hepatic glucose production and increased peripheral glucose utilization. Metformin has also been shown to have several beneficial effects on cardiovascular risk factors and it is the only oral antihyperglycaemic agent thus far associated with decreased macrovascular complications in patients with diabetes. Adenosine Monophosphate Activated-Protein Kinase (AMPK) is a major cellular regulator of lipid and glucose metabolism. Recent evidence shows that pharmacological activation of AMPK improves blood glucose homeostasis, lipid profiles, blood pressure and insulin-resistance making it a novel therapeutic target in the treatment of T2D. Naringenin a flavonoid found in high concentrations as its glycone naringin in citrus fruits, has been reported to have antioxidant, antiatherogenic, anti- dyslipidemic and anti-diabetic effects. It has been shown that naringenin exerts its anti-diabetic effects by inhibition of gluconeogenesis through upregulations of AMPK hence metformin-like effects. Naringin has further been shown to have non-glycemic affects like metformin that mitigate inflammation and cell proliferation. This review evaluates the potential of naringenin as anti-diabetic, anti-dyslipidemic anti-inflammatory and antineoplastic agent similar to metformin and proposes its further development for therapeutic use in clinical practice. Copyright © 2017 Elsevier B.V. All rights reserved.

  14. Insulin-releasing action of the novel antidiabetic agent BTS 67 582.

    Science.gov (United States)

    McClenaghan, N H; Flatt, P R; Bailey, C J

    1998-02-01

    1. BTS 67582 (1,1-dimethyl-2-(2-morpholinophenyl)guanidine fumarate) is a novel antidiabetic agent with a short-acting insulin-releasing effect. This study examined its mode of action in the clonal B-cell line BRIN-BD11. 2. BTS 67582 increased insulin release from BRIN-BD11 cells in a concentration-dependent manner (10[-8] to 10[-4] M) at both non-stimulating (1.1 mM) and stimulating (16.7 mM) concentrations of glucose. 3. BTS 67582 (10[-4] M) potentiated the insulin-releasing effect of a depolarizing concentration of K+ (30 mM), whereas the K+ channel openers pinacidil (400 microM) and diazoxide (300 microM) inhibited BTS 67582-induced release. 4. Suppression of Ca+ channel activity with verapamil (20 microM) reduced the insulin-releasing effect of BTS 67582 (10[-4] M). 5. BTS 67582 (10[-4] M) potentiated insulin release induced by amino acids (10 mM), and enhanced the combined stimulant effects of glucose plus either the fatty acid palmitate (10 mM), or agents which raise intracellular cyclic AMP concentrations (25 microM forskolin and 1 mM isobutylmethylxanthine), or the cholinoceptor agonist carbachol (100 microM). 6. Inhibition of glucose-stimulated insulin release by adrenaline or noradrenaline (10 microM) was partially reversed by BTS 67582 (10[-4] M). 7. These data suggest that the insulin-releasing effect of BTS 67582 involves regulation of ATP-sensitive K+ channel activity and Ca2+ influx, and that the drug augments the stimulant effects of nutrient insulin secretagogues and agents which enhance adenylate cyclase and phospholipase C. BTS 67582 may also exert insulin-releasing effects independently of ATP-sensitive K+ channel activity.

  15. Antidiabetic Effect of Galantamine: Novel Effect for a Known Centrally Acting Drug.

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    Mennatallah A Ali

    Full Text Available The cholinergic anti-inflammatory pathway is one of the putative biochemical pathways that link diabetes with Alzheimer disease. Hence, we aimed to verify the potential antidiabetic effect of galantamine, unveil the possible mechanisms and evaluate its interaction with vildagliptin. The n5-STZ rat model was adopted and the diabetic animals were treated with galantamine and/or vildagliptin for 4 weeks. Galantamine lowered the n5-STZ-induced elevation in body weight, food/water intake, serum levels of glucose, fructosamine, and ALT/AST, as well as AChE in the tested organs. Moreover, it modulated successfully the lipid profile assessed in serum, liver, and muscle, and increased serum insulin level, as well as % β-cell function, in a pattern similar to that of vildagliptin. Additionally, galantamine confirmed its antioxidant (Nrf2, TAC, MDA, anti-inflammatory (NF-κB, TNF-α, visfatin, adiponectin and anti-apoptotic (caspase-3, cytochrome c capabilities by altering the n5-STZ effect on all the aforementioned parameters. On the molecular level, galantamine/vildagliptin have improved the insulin (p-insulin receptor, p-Akt, GLUT4/GLUT2 and Wnt/β-catenin (p-GSK-3β, β-catenin signaling pathways. On almost all parameters, the galantamine effects surpassed that of vildagliptin, while the combination regimen showed the best effects. The present results clearly proved that galantamine modulated glucose/lipid profile possibly through its anti-oxidant, -apoptotic, -inflammatory and -cholinesterase properties. These effects could be attributed partly to the enhancement of insulin and Wnt/β-catenin signaling pathways. Galantamine can be strongly considered as a potential antidiabetic agent and as an add-on therapy with other oral antidiabetics.

  16. Sodium glucose co-transporter 2 (SGLT2) inhibitors: new among antidiabetic drugs.

    Science.gov (United States)

    Opie, L H

    2014-08-01

    Type 2 diabetes is characterized by decreased insulin secretion and sensitivity. The available oral anti-diabetic drugs act on many different molecular sites. The most used of oral anti-diabetic agents is metformin that activates glucose transport vesicles to the cell surface. Others are: the sulphonylureas; agents acting on the incretin system; GLP-1 agonists; dipetidylpeptidase-4 inhibitors; meglinitide analogues; and the thiazolidinediones. Despite these many drugs acting by different mechanisms, glycaemic control often remains elusive. None of these drugs have a primary renal mechanism of action on the kidneys, where almost all glucose excreted is normally reabsorbed. That is where the inhibitors of glucose reuptake (sodium-glucose cotransporter 2, SGLT2) have a unique site of action. Promotion of urinary loss of glucose by SGLT2 inhibitors embodies a new principle of control in type 2 diabetes that has several advantages with some urogenital side-effects, both of which are evaluated in this review. Specific approvals include use as monotherapy, when diet and exercise alone do not provide adequate glycaemic control in patients for whom the use of metformin is considered inappropriate due to intolerance or contraindications, or as add-on therapy with other anti-hyperglycaemic medicinal products including insulin, when these together with diet and exercise, do not provide adequate glycemic control. The basic mechanisms are improved β-cell function and insulin sensitivity. When compared with sulphonylureas or other oral antidiabetic agents, SGLT2 inhibitors provide greater HbA1c reduction. Urogenital side-effects related to the enhanced glycosuria can be troublesome, yet seldom lead to discontinuation. On this background, studies are analysed that compare SGLT2 inhibitors with other oral antidiabetic agents. Their unique mode of action, unloading the excess glycaemic load, contrasts with other oral agents that all act to counter the effects of diabetic

  17. Antidiabetic Effects of Tea.

    Science.gov (United States)

    Fu, Qiu-Yue; Li, Qing-Sheng; Lin, Xiao-Ming; Qiao, Ru-Ying; Yang, Rui; Li, Xu-Min; Dong, Zhan-Bo; Xiang, Li-Ping; Zheng, Xin-Qiang; Lu, Jian-Liang; Yuan, Cong-Bo; Ye, Jian-Hui; Liang, Yue-Rong

    2017-05-20

    Diabetes mellitus (DM) is a chronic endocrine disease resulted from insulin secretory defect or insulin resistance and it is a leading cause of death around the world. The care of DM patients consumes a huge budget due to the high frequency of consultations and long hospitalizations, making DM a serious threat to both human health and global economies. Tea contains abundant polyphenols and caffeine which showed antidiabetic activity, so the development of antidiabetic medications from tea and its extracts is increasingly receiving attention. However, the results claiming an association between tea consumption and reduced DM risk are inconsistent. The advances in the epidemiologic evidence and the underlying antidiabetic mechanisms of tea are reviewed in this paper. The inconsistent results and the possible causes behind them are also discussed.

  18. Recommendations on the effect of antidiabetic drugs in bone.

    Science.gov (United States)

    Rozas-Moreno, Pedro; Reyes-García, Rebeca; Jódar-Gimeno, Esteban; Varsavsky, Mariela; Luque-Fernández, Inés; Cortés-Berdonces, María; Muñoz-Torres, Manuel

    2017-03-01

    To provide recommendations on the effect of antidiabetic drugs on bone fragility to help select the most adequate antidiabetic treatment, especially in diabetic patients with high risk of fracture. Members of the Bone Metabolism Working Group of the Spanish Society of Endocrinology. The GRADE system (Grading of Recommendations, Assessment, Development, and Evaluation) was used to establish both the strength of recommendations and the quality of evidence. A systematic search was made in MEDLINE (Pubmed) using the following terms associated to the name of each antidiabetic drug: AND "osteoporosis", "fractures", "bone mineral density", "bone markers", "calciotropic hormones". Papers in English with publication date before 30 April 2016 were reviewed. Recommendations were jointly discussed by the Working Group. The document summaries the data on the potential effects of antidiabetic drugs on bone metabolism and fracture risk. Copyright © 2017 SEEN. Publicado por Elsevier España, S.L.U. All rights reserved.

  19. Newer antidiabetic drugs and calorie restriction mimicry

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    Sanjay Kalra

    2016-01-01

    Full Text Available De-acceleration of aging and delayed development of age-related morbidity accompanies the restriction of calories (without malnutrition in laboratory mice, nematodes, yeast, fish, and dogs. Recent results from long-term longitudinal studies conducted on primates have suggested longevity benefits of a 30% restriction of calories in rhesus monkeys as well. Among calorie restricted rhesus monkeys one of the mechanisms for the improvement in lifespan was the reduction in the development of glucose intolerance and cardiovascular disease. Although there are no comparable human studies, it is likely that metabolic and longevity benefits will accompany a reduction in calories in humans as well. However, considering the difficulties in getting healthy adults to limit food intake science has focused on understanding the biochemical processes that accompany calorie restriction (CR to formulate drugs that would mimic the effects of CR without the need to actually restrict calories. Drugs in this emerging therapeutic field are called CR mimetics. Some of the currently used anti-diabetic agents may have some CR mimetic like effects. This review focuses on the CR mimetic properties of the currently available anti-diabetic agents.

  20. Anti-Diabetic Effects of Dung Beetle Glycosaminoglycan on db Mice and Gene Expression Profiling.

    Science.gov (United States)

    Ahn, Mi Young; Kim, Ban Ji; Yoon, Hyung Joo; Hwang, Jae Sam; Park, Kun-Koo

    2018-04-01

    Anti-diabetes activity of Catharsius molossus (Ca, a type of dung beetle) glycosaminoglycan (G) was evaluated to reduce glucose, creatinine kinase, triglyceride and free fatty acid levels in db mice. Diabetic mice in six groups were administrated intraperitoneally: Db heterozygous (Normal), Db homozygous (CON), Heuchys sanguinea glycosaminoglycan (HEG, 5 mg/kg), dung beetle glycosaminoglycan (CaG, 5 mg/kg), bumblebee ( Bombus ignitus ) queen glycosaminoglycan (IQG, 5 mg/kg) and metformin (10 mg/kg), for 1 month. Biochemical analyses in the serum were evaluated to determine their anti-diabetic and anti-inflammatory actions in db mice after 1 month treatment with HEG, CaG or IQG treatments. Blood glucose level was decreased by treatment with CaG. CaG produced significant anti-diabetic actions by inhiting creatinine kinase and alkaline phosphatase levels. As diabetic parameters, serum glucose level, total cholesterol and triglyceride were significantly decreased in CaG5-treated group compared to the controls. Dung beetle glycosaminoglycan, compared to the control, could be a potential therapeutic agent with anti-diabetic activity in diabetic mice. CaG5-treated group, compared to the control, showed the up-regulation of 48 genes including mitochondrial yen coded tRNA lysine (mt-TK), cytochrome P450, family 8/2, subfamily b, polypeptide 1 (Cyp8b1), and down-regulation of 79 genes including S100 calcium binding protein A9 (S100a9) and immunoglobulin kappa chain complex (Igk), and 3-hydroxy-3-methylglutaryl-CoenzymeAsynthase1 (Hmgcs1). Moreover, mitochondrial thymidine kinase (mt-TK), was up-regulated, and calgranulin A (S100a9) were down-regulated by CaG5 treatment, indicating a potential therapeutic use for anti-diabetic agent.

  1. Simultaneous Quantification of Antidiabetic Agents in Human Plasma by a UPLC-QToF-MS Method.

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    Mariana Millan Fachi

    Full Text Available An ultra-performance liquid chromatography quadrupole time-of-flight mass spectrometry method for the simultaneous quantification of chlorpropamide, glibenclamide, gliclazide, glimepiride, metformin, nateglinide, pioglitazone, rosiglitazone, and vildagliptin in human plasma was developed and validated, using isoniazid and sulfaquinoxaline as internal standards. Following plasma protein precipitation using acetonitrile with 1% formic acid, chromatographic separation was performed on a cyano column using gradient elution with water and acetonitrile, both containing 0.1% formic acid. Detection was performed in a quadrupole time-of-flight analyzer, using electrospray ionization operated in the positive mode. Data from validation studies demonstrated that the new method is highly sensitive, selective, precise (RSD 0.99, free of matrix and has no residual effects. The developed method was successfully applied to volunteers' plasma samples. Hence, this method was demonstrated to be appropriate for clinical monitoring of antidiabetic agents.

  2. Anti-Diabetic Effects of Madecassic Acid and Rotundic Acid

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    Yuan-Man Hsu

    2015-12-01

    Full Text Available Anti-diabetic effects of madecassic acid (MEA and rotundic acid (RA were examined. MEA or RA at 0.05% or 0.1% was supplied to diabetic mice for six weeks. The intake of MEA, not RA, dose-dependently lowered plasma glucose level and increased plasma insulin level. MEA, not RA, intake dose-dependently reduced plasminogen activator inhibitor-1 activity and fibrinogen level; as well as restored antithrombin-III and protein C activities in plasma of diabetic mice. MEA or RA intake decreased triglyceride and cholesterol levels in plasma and liver. Histological data agreed that MEA or RA intake lowered hepatic lipid droplets, determined by ORO stain. MEA intake dose-dependently declined reactive oxygen species (ROS and oxidized glutathione levels, increased glutathione content and maintained the activity of glutathione reductase and catalase in the heart and kidneys of diabetic mice. MEA intake dose-dependently reduced interleukin (IL-1β, IL-6, tumor necrosis factor-α and monocyte chemoattractant protein-1 levels in the heart and kidneys of diabetic mice. RA intake at 0.1% declined cardiac and renal levels of these inflammatory factors. These data indicated that MEA improved glycemic control and hemostatic imbalance, lowered lipid accumulation, and attenuated oxidative and inflammatory stress in diabetic mice. Thus, madecassic acid could be considered as an anti-diabetic agent.

  3. Molecular Modeling Studies of Thiophenyl C-Aryl Glucoside SGLT2 Inhibitors as Potential Antidiabetic Agents

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    Mukesh C. Sharma

    2014-01-01

    Full Text Available A QSAR study on thiophenyl derivatives as SGLT2 inhibitors as potential antidiabetic agents was performed with thirty-three compounds. Comparison of the obtained results indicated the superiority of the genetic algorithm over the simulated annealing and stepwise forward-backward variable method for feature selection. The best 2D QSAR model showed satisfactory statistical parameters for the data set (r2=0.8499, q2=0.8267, and pred_r2=0.7729 with four descriptors describing the nature of substituent groups and the environment of the substitution site. Evaluation of the model implied that electron-rich substitution position improves the inhibitory activity. The good predictive 3D-QSAR models by k-nearest neighbor (kNN method for molecular field analysis (MFA have cross-validated coefficient q2 value of 0.7663 and predicted r2 value of 0.7386. The results have showed that thiophenyl groups are necessary for activity and halogen, bulky, and less bulky groups in thiophenyl nucleus enhanced the biological activity. These studies are promising for the development of novel SGLT2 inhibitor, which may have potent antidiabetic activity.

  4. Stereospermum tetragonam as an antidiabetic agent by activating PPARγ and GLUT4

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    Bino Kingsley

    2014-06-01

    Full Text Available Present study evaluates the anti-diabetic activity of S. tetragonam LC-MSMS experiments showed the presence of two novel molecules C1 and C2, which were further taken for in silico study against PPARγ. Cell culture studies with A431 cells in the presence of crude aqueous extract showed the elevated level of PPARγ and GLUT4 and also confirmed using in silico studies. Thus, the present study proves the mecode of action of S. tetragonam as an antidiabetic drug.

  5. Effects of Antidiabetic Drugs on Gut Microbiota Composition

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    Sophie A. Montandon

    2017-09-01

    Full Text Available Gut microbiota forms a catalog of about 1000 bacterial species; which mainly belong to the Firmicutes and Bacteroidetes phyla. Microbial genes are essential for key metabolic processes; such as the biosynthesis of short-chain fatty acids (SCFA; amino acids; bile acids or vitamins. It is becoming clear that gut microbiota is playing a prevalent role in pathologies such as metabolic syndrome; type 2 diabetes (T2D; inflammatory and bowel diseases. Obesity and related diseases; notably type 2 diabetes, induce gut dysbiosis. In this review; we aim to cover the current knowledge about the effects of antidiabetic drugs on gut microbiota diversity and composition as well as the potential beneficial effects mediated by specific taxa. Metformin is the first-line treatment against T2D. In addition to its glucose-lowering and insulin sensitizing effects, metformin promotes SCFA-producing and mucin-degrading bacteria. Other antidiabetic drugs discussed in this review show positive effects on dysbiosis; but without any consensus specifically regarding the Firmicutes to Bacteroidetes ratio. Thus, beneficial effects might be mediated by specific taxa.

  6. Antidiabetic and antioxidant potentials of spent turmeric oleoresin, a by-product from curcumin production industry

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    Suresh V Nampoothiri

    2012-05-01

    Full Text Available Objective: To investigate the antidiabetic and antioxidant activity of spent turmeric oleoresin (STO. Methods: Antidiabetic activity of STO evaluated by α - amylase and α - glucosidase enzyme inhibition assays. The antioxidant capacity studied by DPPH. , ABTS., superoxide radical scavenging and metal chelating activity methods. Results: The STO showed good antidiabetic activity by inhibiting key enzymes linked to type 2 diabetes, viz α -glucosidase and α -amylase with an IC50values of 0.71 and 0.16毺 g/mL respectively. The IC50 values for DPPH. and ABTS. assay were 58.1 and 33 毺 g/mL respectively. STO effectively scavenged the superoxide free radical with an IC50 value of 61.5毺 g/mL and showed a moderate iron chelation property. Conclusions: The above study reveals that the spent turmeric oleoresin being wasted at present can be used as antioxidant and antidiabetic agent in food and neutraceutical products.

  7. Antidiabetic Properties, Bioactive Constituents, and Other Therapeutic Effects of Scoparia dulcis

    OpenAIRE

    Geethi Pamunuwa; D. Nedra Karunaratne; Viduranga Y. Waisundara

    2016-01-01

    This review discusses the antidiabetic activities of Scoparia dulcis as well as its antioxidant and anti-inflammatory properties in relation to the diabetes and its complications. Ethnomedical applications of the herb have been identified as treatment for jaundice, stomach problems, skin disease, fever, and kidney stones, reproductory issues, and piles. Evidence has been demonstrated through scientific studies as to the antidiabetic effects of crude extracts of S. dulcis as well as its bioact...

  8. Recent Advances in Astragalus membranaceus Anti-Diabetic Research: Pharmacological Effects of Its Phytochemical Constituents

    Directory of Open Access Journals (Sweden)

    Kojo Agyemang

    2013-01-01

    Full Text Available The disease burden of diabetes mellitus is increasing throughout the world. The need for more potent drugs to complement the present anti-diabetic drugs has become an imperative. Astragalus membranaceus, a key component of most Chinese herbal anti-diabetic formulas, has been an important prospect for lead anti-diabetic compounds. It has been progressively studied for its anti-diabetic properties. Ethnopharmacological studies have established its potential to alleviate diabetes mellitus. Recent studies have sought to relate its chemical constituents to types 1 and 2 diabetes mellitus. Its total polysaccharides, saponins, and flavonoids fractions and several isolated compounds have been the most studied. The total polysaccharides fraction demonstrated activity to both types 1 and 2 diabetes mellitus. This paper discusses the anti-diabetic effects and pharmacological action of the chemical constituents in relation to types 1 and 2 diabetes mellitus.

  9. Antidiabetic and haematinic effects of Parquetina nigrescens on ...

    African Journals Online (AJOL)

    Antidiabetic and haematinic effects of Parquetina nigrescens on alloxan induced type-1 diabetes and normocytic normochromic anaemia in Wistar rats. ... Background: The plant, Parquetina nigrescens is used in folklore medicine to treat diabetes mellitus and its complications in several parts of West Africa. Objective: To ...

  10. Antidiabetic effect of total flavonoids from Sanguis draxonis in type 2 diabetic rats.

    Science.gov (United States)

    Chen, Fufeng; Xiong, Hui; Wang, Jianxia; Ding, Xin; Shu, Guangwen; Mei, Zhinan

    2013-10-07

    Sanguis draxonis (SD) is a kind of red resin obtained from the wood of Dracaena cochinchinensis (Lour.) S. C. Chen (Dracaena cochinchinensis). It is a Chinese traditional herb that is prescribed for the handling of diabetic disorders, which is also supported by an array of scientific studies published in recent years. Although chemical constituents of this plant material have also been previously evaluated (Tang et al., 1995; Wei et al., 1998), it still remains poorly understood which constituent is the major contributor to its antidiabetic activities. Moreover, very little is known about the molecular mechanisms underlying antidiabetic activities of SD. Flavonoids exist at a high level in SD. The aim of this study is to evaluate the antidiabetic effects of total flavonoids from SD (SDF) in type 2 Diabetes mellitus (T2DM) rats. T2DM rats were induced by 4 weeks high-fat diet and a singular injection of streptozotocin (STZ) (35mg/kg). Then T2DM rats were treated with SDF for 21 days, using normal saline as the negative control. For comparison, a standard antidiabetic drug, metformin (200mg/kg), was used as a positive control. Three weeks later, relative biochemical indexes were determined and histopathological examinations were performed to assess the antidiabetic activities of SDF. SDF not only exhibited a significant hypoglycemic activity, but also alleviated dyslipidemia, tissue steatosis, and oxidative stress associated with T2DM. Moreover, considerable pancreatic islet protecting effects could be observed after SDF treatment. Further investigations revealed a potential anti-inflammation activity of SDF by determining serum levels of interleukin-6 (IL-6), tumor necrosis factor-α (TNF-α) and C-reactive protein (CRP). This study demonstrates both hypoglycemic and hypolipidemic effects of SDF in T2DM rats, suggesting that flavonoids are the major active ingredients accounting for the antidiabetic activity of SD. Alleviating chronic inflammation responses and

  11. Anti-diabetic effect of Cyclo-His-Pro (CHP)-enriched yeast ...

    African Journals Online (AJOL)

    Anti-diabetic effect of Cyclo-His-Pro (CHP)-enriched yeast hydrolysate in ... The present study was designed to investigate the hypoglycemic effects of the daily ... in the area under curve (AUC) value of YH supplemented groups as compared ...

  12. Beliefs related to adherence to oral antidiabetic treatment according to the Theory of Planned Behavior.

    Science.gov (United States)

    Jannuzzi, Fernanda Freire; Rodrigues, Roberta Cunha Matheus; Cornélio, Marilia Estevam; São-João, Thaís Moreira; Gallani, Maria Cecília Bueno Jayme

    2014-01-01

    to identify salient behavioral, normative, control and self-efficacy beliefs related to the behavior of adherence to oral antidiabetic agents, using the Theory of Planned Behavior. cross-sectional, exploratory study with 17 diabetic patients in chronic use of oral antidiabetic medication and in outpatient follow-up. Individual interviews were recorded, transcribed and content-analyzed using pre-established categories. behavioral beliefs concerning advantages and disadvantages of adhering to medication emerged, such as the possibility of avoiding complications from diabetes, preventing or delaying the use of insulin, and a perception of side effects. The children of patients and physicians are seen as important social references who influence medication adherence. The factors that facilitate adherence include access to free-of-cost medication and taking medications associated with temporal markers. On the other hand, a complex therapeutic regimen was considered a factor that hinders adherence. Understanding how to use medication and forgetfulness impact the perception of patients regarding their ability to adhere to oral antidiabetic agents. medication adherence is a complex behavior permeated by behavioral, normative, control and self-efficacy beliefs that should be taken into account when assessing determinants of behavior.

  13. Prescription trends and the selection of initial oral antidiabetic agents for patients with newly diagnosed type 2 diabetes: a nationwide study.

    Science.gov (United States)

    Liu, C-H; Chen, S-T; Chang, C-H; Chuang, L-M; Lai, M-S

    2017-11-01

    The aim of this study was to examine the characteristics of patients, physicians, and medical facilities, and their association with prescriptions that do not include metformin as the initial oral antidiabetic agent. Observational, cross-sectional study. Patients with incident type 2 diabetes between January 1, 2006, and December 31, 2010, were identified from the Taiwan National Insurance Research Database. We describe trends in the initial prescription of antidiabetic medications that do not contain metformin during the study period. A multivariable logistic model and a multilevel linear model were used in the analysis of factors at a range of levels (patient, physician, and medical facility), which may be associated with the selection of oral antidiabetic drugs. During the study period, the proportion of prescriptions that did not include metformin declined from 43.8% to 26.2%. Male patients were more likely to obtain non-metformin prescriptions (adjusted odds ratio [OR]: 1.15; 95% confidence interval [CI]: 1.08-1.23), and the likelihood that a patient would be prescribed a non-metformin prescription increased with age. Physicians aged ≥35 years and those with specialties other than endocrinology tended to prescribe non-metformin prescriptions. Metformin was less commonly prescribed in for-profit hospitals (adjusted OR: 1.34, 95% CI: 1.11-1.61) and hospitals in smaller cities (adjusted OR: 1.28, 95% CI: 1.05-1.57) and rural areas (adjusted OR: 1.83, 95% CI: 1.32-2.54). Disparities continue to exist in clinical practice with regard to the treatment of diabetes. These inequalities appear to be linked to a variety of factors related to patients, physicians, and medical facilities. Further study will be required to understand the effects of continuing medical education in enhancing adherence to clinical guidelines. Copyright © 2017 The Royal Society for Public Health. Published by Elsevier Ltd. All rights reserved.

  14. Antidiabetic effects of Momordica charantia (bitter melon) and its medicinal potency

    Science.gov (United States)

    Joseph, Baby; Jini, D

    2013-01-01

    Diabetes mellitus is among the most common disorder in developed and developing countries, and the disease is increasing rapidly in most parts of the world. It has been estimated that up to one-third of patients with diabetes mellitus use some form of complementary and alternative medicine. One plant that has received the most attention for its anti-diabetic properties is bitter melon, Momordica charantia (M. charantia), commonly referred to as bitter gourd, karela and balsam pear. Its fruit is also used for the treatment of diabetes and related conditions amongst the indigenous populations of Asia, South America, India and East Africa. Abundant pre-clinical studies have documented in the anti-diabetic and hypoglycaemic effects of M. charantia through various postulated mechanisms. However, clinical trial data with human subjects are limited and flawed by poor study design and low statistical power. The present review is an attempt to highlight the antidiabetic activity as well as phytochemical and pharmacological reports on M. charantia and calls for better-designed clinical trials to further elucidate its possible therapeutic effects on diabetes.

  15. Antidiabetic effects of Momordica charantia (bitter melon and its medicinal potency

    Directory of Open Access Journals (Sweden)

    Baby Joseph

    2013-04-01

    Full Text Available Diabetes mellitus is among the most common disorder in developed and developing countries, and the disease is increasing rapidly in most parts of the world. It has been estimated that up to one-third of patients with diabetes mellitus use some form of complementary and alternative medicine. One plant that has received the most attention for its anti-diabetic properties is bitter melon, Momordica charantia (M. charantia, commonly referred to as bitter gourd, karela and balsam pear. Its fruit is also used for the treatment of diabetes and related conditions amongst the indigenous populations of Asia, South America, India and East Africa. Abundant pre-clinical studies have documented in the anti-diabetic and hypoglycaemic effects of M. charantia through various postulated mechanisms. However, clinical trial data with human subjects are limited and flawed by poor study design and low statistical power. The present review is an attempt to highlight the antidiabetic activity as well as phytochemical and pharmacological reports on M. charantia and calls for better-designed clinical trials to further elucidate its possible therapeutic effects on diabetes.

  16. Effectiveness and clinical inertia in patients with antidiabetic therapy.

    Science.gov (United States)

    Machado-Duque, Manuel Enrique; Ramírez-Riveros, Adriana Carolina; Machado-Alba, Jorge Enrique

    2017-06-01

    To establish the effectiveness of antidiabetic therapy and the frequency of clinical inertia in the management of type 2 diabetes mellitus in Colombia. A cross-sectional study with follow-up of patients who had been treated for at least 1 year and were receiving medical consultation for antidiabetic treatment. Effectiveness was established when haemoglobin-A1c levels were inertia was reached, which was defined as no therapeutic modifications despite not achieving management controls. Sociodemographic, clinical and pharmacological variables were evaluated, and multivariate analyses were performed. In total, 363 patients with type 2 diabetes mellitus were evaluated, with a mean age of 62.0±12.2 years. A total of 1,016 consultations were evaluated, and the therapy was effective at the end of the follow-up in 57.9% of cases. Clinical inertia was found in 56.8% of patients who did not have metabolic control. The most frequently prescribed medications were metformin (84.0%), glibenclamide (23.4%) and insulin glargine (20.7%). Moreover, 57.6% of the patients were treated with two or more antidiabetic medications. Having metabolic control in the first consult of the follow-up was a protective factor against clinical inertia in the subsequent consultations (OR: 0.08; 95%CI: 0.04-0.15; Pinertia was identifiable and quantifiable and found in similar proportions to other countries. Clinical inertia is a relevant condition given that it interferes with the possibility of controlling this pathology. © 2017 John Wiley & Sons Ltd.

  17. Beliefs related to adherence to oral antidiabetic treatment according to the Theory of Planned Behavior1

    Science.gov (United States)

    Jannuzzi, Fernanda Freire; Rodrigues, Roberta Cunha Matheus; Cornélio, Marilia Estevam; São-João, Thaís Moreira; Gallani, Maria Cecília Bueno Jayme

    2014-01-01

    OBJECTIVE: to identify salient behavioral, normative, control and self-efficacy beliefs related to the behavior of adherence to oral antidiabetic agents, using the Theory of Planned Behavior. METHOD: cross-sectional, exploratory study with 17 diabetic patients in chronic use of oral antidiabetic medication and in outpatient follow-up. Individual interviews were recorded, transcribed and content-analyzed using pre-established categories. RESULTS: behavioral beliefs concerning advantages and disadvantages of adhering to medication emerged, such as the possibility of avoiding complications from diabetes, preventing or delaying the use of insulin, and a perception of side effects. The children of patients and physicians are seen as important social references who influence medication adherence. The factors that facilitate adherence include access to free-of-cost medication and taking medications associated with temporal markers. On the other hand, a complex therapeutic regimen was considered a factor that hinders adherence. Understanding how to use medication and forgetfulness impact the perception of patients regarding their ability to adhere to oral antidiabetic agents. CONCLUSION: medication adherence is a complex behavior permeated by behavioral, normative, control and self-efficacy beliefs that should be taken into account when assessing determinants of behavior. PMID:25296135

  18. Antidiabetic effect of polyphenolic extracts from selected edible plants as α-amylase, α -glucosidase and PTP1B inhibitors, and β pancreatic cells cytoprotective agents - a comparative study.

    Science.gov (United States)

    Zakłos-Szyda, Małgorzata; Majewska, Iwona; Redzynia, Małgorzata; Koziołkiewicz, Maria

    2015-01-01

    Type 2 diabetes mellitus, which is usually a result of wrong dietary habits and reduced physical activity, represents 85-95% of all diabetes cases and among other diet related diseases is the major cause of deaths. The disease is characterized mainly by hyperglycemia, which is associated with attenuated insulin sensitivity or beta cells dysfunction caused by multiple stimuli, including oxidative stress and loss of insulin secretion. Since polyphenols possess multiple biological activities and constitute an important part of the human diet, they have recently emerged as critical phytochemicals in type 2 diabetes prevention and treatment. Their hypoglycemic action results from their antioxidative effect involved in recovering of altered antioxidant defenses and restoring insulin secreting machinery in pancreatic cells, or abilities to inhibit the activity of carbohydrates hydrolyzing enzymes (α-amylase and α-glucosidase) or protein tyrosine phosphatase 1B (PTP1B), which is known as the major negative regulator in insulin signaling. This study investigates the total phenolic content (Folin-Ciocalteu and HPLC methods) and antioxidant capacity (ABTS) of 20 polyphenolic extracts obtained from selected edible plants, which were screened in terms of α -amylase, α - glucosidase and protein tyrosine phosphatase 1B inhibitors or protective agents against oxidative stress induced by tertbutylhydroperoxide (t-BOOH) in βTC3 pancreatic beta cells used as a model target for antidiabetes drugs. The study concludes that Chaenomeles japonica, Oenothera paradoxa and Viburnum opulus may be promising natural sources for active compounds with antidiabetic properties.

  19. Separation, Identification, and Antidiabetic Activity of Catechin Isolated from Arbutus unedo L. Plant Roots.

    Science.gov (United States)

    Mrabti, Hanae Naceiri; Jaradat, Nidal; Fichtali, Ismail; Ouedrhiri, Wessal; Jodeh, Shehdeh; Ayesh, Samar; Cherrah, Yahia; Faouzi, My El Abbes

    2018-04-12

    Phytopharmaceuticals play an essential role in medicine, since the need to investigate highly effective and safe drugs for the treatment of diabetes mellitus disease remains a significant challenge for modern medicine. Arbutus unedo L. root has various therapeutic properties, and has been used widely in the traditional medicine as an antidiabetic agent. The current study aimed to isolate the pharmacologically active compound from A. unedo roots using accelerated solvent extraction technology, to determine its chemical structure using different instrumental analytical methods, and also to evaluate the α-glucosidase inhibitory activity. The roots of A. unedo were exhaustively extracted by high-pressure static extraction using the Zippertex ® technology (Dionex-ASE, Paris, France), and the extract was mixed with XAD-16 resin to reach quantifiable amounts of active compounds which were identified by high-pressure liquid chromatography (HPLC), ¹H NMR (300 MHz), and 13 C NMR. The antidiabetic activity of the isolated compound was evaluated using the α-glucosidase inhibitory assay. The active compound was isolated, and its structure was identified as catechin using instrumental analysis.The results revealed that the isolated compound has potential α-glucosidase inhibitory activity with an IC 50 value of 87.55 ± 2.23 μg/mL greater than acarbose. This was used as a positive control, which has an IC 50 value of 199.53 ± 1.12 μg/mL. According to the results achieved, the roots of A. unedo were considered the best source of catechin and the Zippertex ® technology method of extraction is the best method for isolation of this therapeutic active compound. In addition, the α-glucosidase inhibitory activity results confirmed the traditional use of A. unedo roots as an antidiabetic agent. Future clinical trials and investigations of antidiabetic and other pharmacological effects such as anticancer are required.

  20. Separation, Identification, and Antidiabetic Activity of Catechin Isolated from Arbutus unedo L. Plant Roots

    Directory of Open Access Journals (Sweden)

    Hanae Naceiri Mrabti

    2018-04-01

    Full Text Available Phytopharmaceuticals play an essential role in medicine, since the need to investigate highly effective and safe drugs for the treatment of diabetes mellitus disease remains a significant challenge for modern medicine. Arbutus unedo L. root has various therapeutic properties, and has been used widely in the traditional medicine as an antidiabetic agent. The current study aimed to isolate the pharmacologically active compound from A. unedo roots using accelerated solvent extraction technology, to determine its chemical structure using different instrumental analytical methods, and also to evaluate the α-glucosidase inhibitory activity. The roots of A. unedo were exhaustively extracted by high-pressure static extraction using the Zippertex® technology (Dionex-ASE, Paris, France, and the extract was mixed with XAD-16 resin to reach quantifiable amounts of active compounds which were identified by high-pressure liquid chromatography (HPLC, 1H NMR (300 MHz, and 13C NMR. The antidiabetic activity of the isolated compound was evaluated using the α-glucosidase inhibitory assay. The active compound was isolated, and its structure was identified as catechin using instrumental analysis.The results revealed that the isolated compound has potential α-glucosidase inhibitory activity with an IC50 value of 87.55 ± 2.23 μg/mL greater than acarbose. This was used as a positive control, which has an IC50 value of 199.53 ± 1.12 μg/mL. According to the results achieved, the roots of A. unedo were considered the best source of catechin and the Zippertex® technology method of extraction is the best method for isolation of this therapeutic active compound. In addition, the α-glucosidase inhibitory activity results confirmed the traditional use of A. unedo roots as an antidiabetic agent. Future clinical trials and investigations of antidiabetic and other pharmacological effects such as anticancer are required.

  1. Systematic Review of Efficacy and Safety of Newer Antidiabetic Drugs Approved from 2013 to 2017 in Controlling HbA1c in Diabetes Patients

    Directory of Open Access Journals (Sweden)

    Sivanandy Palanisamy

    2018-06-01

    Full Text Available Type 2 Diabetes Mellitus (T2DM is the most common form of diabetes mellitus and accounts for about 95% of all diabetes cases. Many newer oral as well as parenteral antidiabetic drugs have been introduced in to the market in recent years to control hyperglycemic conditions in diabetes patients and many of these drugs produce potential side effects in diabetes patients. Hence, this systematic review was aimed to analyze and compare the efficacy and safety of oral antidiabetic agents in controlling HbA1c in T2DM patients, that were approved by the United States-Food and Drug Administration (US-FDA from 2013 to 2017. All randomized controlled, double-blind trials published in English during the search period involving the newer antidiabetic agents were selected. In the outcome assessment comparison, semaglutide demonstrated the highest efficacy in lowering HbA1c, with a 1.6% reduction (p < 0.0001 when given at a dose of 1.0 mg. The safety profile of all the agents as compared to placebo or control were similar, with no or slight increase in the occurrence of adverse events (AEs but no fatal reaction was reported. The most common AEs of all the antidiabetic agents were gastrointestinal in nature, with several cases of hypoglycemic events. However, among all these agents, semaglutide seems to be the most efficacious drug to improve glycemic control in terms of HbA1c. Alogliptin has the least overall frequency of AEs compared to other treatment groups.

  2. Antidiabetic effect of Sida cordata in alloxan induced diabetic rats.

    Science.gov (United States)

    Shah, Naseer Ali; Khan, Muhammad Rashid

    2014-01-01

    Medicinal plants are efficient ameliorator of oxidative stress associated with diabetes mellitus. In this study, ethyl acetate fraction (SCEE) of Sida cordata was investigated for scientific validation of its folk use in diabetes. Antidiabetic effect of SCEE was confirmed by antihyperglycemic activity in normal glucose loaded and diabetic glucose loaded animals as well as normal off feed animals. Confirmation of antidiabetic activity and toxicity ameliorative role of S. cordata was investigated in a chronic multiple dose treatment study of fifteen days. A single dose of alloxan (120 mg/kg) produced a decrease in insulin level, hyperglycemia, elevated total lipids, triglycerides, and cholesterol and decreased the high-density lipoproteins. Concurrent with these changes, there was an increase in the concentration of lipid peroxidation (TBARS), H2O2, and nitrite in pancreas, liver, and testis. This oxidative stress was related to a decrease in glutathione content (GSH) and antioxidant enzymes. Administration of SCEE for 15 days after diabetes induction ameliorated hyperglycemia, restored lipid profile, blunted the increase in TBARS, H2O2, and nitrite content, and stimulated the GSH production in the organs of alloxan-treated rats. We suggested that SCEE could be used as antidiabetic component in case of diabetes mellitus. This may be related to its antioxidative properties.

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

    Science.gov (United States)

    Ganogpichayagrai, Aunyachulee; Palanuvej, Chanida; Ruangrungsi, Nijsiri

    2017-01-01

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

  4. Induced desensitization of the insulinotropic effects of antidiabetic drugs, BTS 67 582 and tolbutamide.

    Science.gov (United States)

    McClenaghan, N H; Ball, A J; Flatt, P R

    2000-05-01

    Acute and chronic mechanisms of action of novel insulinotropic antidiabetic drug, BTS 67 582 (1, 1-dimethyl-2-(2-morpholinophenyl)guanidine fumarate), were examined in the stable cultured BRIN-BD11 cell line. BTS 67 582 (100 - 400 microM) stimulated a concentration-dependent increase (PBTS 67 582 in culture time-dependently decreased subsequent responsiveness to acute challenge with 200 microM BTS 67 582 or 200 microM tolbutamide at 12 - 18 h (PBTS 67 582 and tolbutamide. Culture with 100 microM BTS 67 582 or 100 microM tolbutamide did not affect basal insulin secretion, cellular insulin content, or cell viability and exerted no influence on the secretory responsiveness to 200 microM of the imidazoline, efaroxan. While 18 h BTS 67 582 culture did not affect the insulin-releasing actions (PBTS 67 582 shares a common signalling pathway to sulphonylurea but not imidazoline drugs. Desensitization of drug action may provide an important approach to dissect sites of action of novel and established insulinotropic antidiabetic agents.

  5. Determination of in vitro antidiabetic effects of Zingiber officinale Roscoe

    Directory of Open Access Journals (Sweden)

    Naila Abdul Sattar

    2012-12-01

    Full Text Available Aqueous extracts of Zingiber officinale rhizomes were studied to evaluate their antidiabetic effects on protein glycation and on the diffusion of glucose in vitro in the present study. Zingiber officinale rhizome aqueous extract were examined at concentrations of 5, 10, 20 and 40 g/L. The antidiabetic effects were found to be dose-dependent. Antidiabetic potential of Zingiber officinale was mainly through inhibition of the glucose diffusion and to a limited extent by reducing the glycation. However, further studies are needed to determine in vitro effects of therapeutic potential by restraining postprandial glucose absorptions and plasma protein glycations in diabetic subjects.Extratos aquosos de rizomas Zingiber officinale foram estudados para avaliar os seus efeitos antidiabéticos em glicação de proteínas e sobre a difusão de glicose in vitro, no presente estudo. Extratos aquosos de Zingiber officinale foram examinados nas concentrações de 5, 10, 20 e 40 g extrato de planta/L. Os efeitos antidiabéticos observados eram dependentes da dose. O potencial antidiabético de Zingiber officinale se verificou, principalmente, através da inibição da difusão de glicose e, em menor extensão, através da redução da glicação. Estudos adicionais são necessários para elucidar se efeitos in vitro representam potencial terapêutico, restringindo a absorção de glicose pós-prandial e a glicação de proteínas plasmáticas em indivíduos diabéticos.

  6. Antidiabetic Properties, Bioactive Constituents, and Other Therapeutic Effects of Scoparia dulcis

    Science.gov (United States)

    Karunaratne, D. Nedra

    2016-01-01

    This review discusses the antidiabetic activities of Scoparia dulcis as well as its antioxidant and anti-inflammatory properties in relation to the diabetes and its complications. Ethnomedical applications of the herb have been identified as treatment for jaundice, stomach problems, skin disease, fever, and kidney stones, reproductory issues, and piles. Evidence has been demonstrated through scientific studies as to the antidiabetic effects of crude extracts of S. dulcis as well as its bioactive constituents. The primary mechanisms of action of antidiabetic activity of the plant and its bioactive constituents are through α-glucosidase inhibition, curbing of PPAR-γ and increased secretion of insulin. Scoparic acid A, scoparic acid D, scutellarein, apigenin, luteolin, coixol, and glutinol are some of the compounds which have been identified as responsible for these mechanisms of action. S. dulcis has also been shown to exhibit analgesic, antimalarial, hepatoprotective, sedative, hypnotic, antiulcer, antisickling, and antimicrobial activities. Given this evidence, it may be concluded that S. dulcis could be promoted among the masses as an alternative and complementary therapy for diabetes, provided further scientific studies on the toxicological and pharmacological aspects are carried out through either in vivo or clinical means. PMID:27594892

  7. Antidiabetic Properties, Bioactive Constituents, and Other Therapeutic Effects of Scoparia dulcis.

    Science.gov (United States)

    Pamunuwa, Geethi; Karunaratne, D Nedra; Waisundara, Viduranga Y

    2016-01-01

    This review discusses the antidiabetic activities of Scoparia dulcis as well as its antioxidant and anti-inflammatory properties in relation to the diabetes and its complications. Ethnomedical applications of the herb have been identified as treatment for jaundice, stomach problems, skin disease, fever, and kidney stones, reproductory issues, and piles. Evidence has been demonstrated through scientific studies as to the antidiabetic effects of crude extracts of S. dulcis as well as its bioactive constituents. The primary mechanisms of action of antidiabetic activity of the plant and its bioactive constituents are through α-glucosidase inhibition, curbing of PPAR-γ and increased secretion of insulin. Scoparic acid A, scoparic acid D, scutellarein, apigenin, luteolin, coixol, and glutinol are some of the compounds which have been identified as responsible for these mechanisms of action. S. dulcis has also been shown to exhibit analgesic, antimalarial, hepatoprotective, sedative, hypnotic, antiulcer, antisickling, and antimicrobial activities. Given this evidence, it may be concluded that S. dulcis could be promoted among the masses as an alternative and complementary therapy for diabetes, provided further scientific studies on the toxicological and pharmacological aspects are carried out through either in vivo or clinical means.

  8. Antidiabetic Properties, Bioactive Constituents, and Other Therapeutic Effects of Scoparia dulcis

    Directory of Open Access Journals (Sweden)

    Geethi Pamunuwa

    2016-01-01

    Full Text Available This review discusses the antidiabetic activities of Scoparia dulcis as well as its antioxidant and anti-inflammatory properties in relation to the diabetes and its complications. Ethnomedical applications of the herb have been identified as treatment for jaundice, stomach problems, skin disease, fever, and kidney stones, reproductory issues, and piles. Evidence has been demonstrated through scientific studies as to the antidiabetic effects of crude extracts of S. dulcis as well as its bioactive constituents. The primary mechanisms of action of antidiabetic activity of the plant and its bioactive constituents are through α-glucosidase inhibition, curbing of PPAR-γ and increased secretion of insulin. Scoparic acid A, scoparic acid D, scutellarein, apigenin, luteolin, coixol, and glutinol are some of the compounds which have been identified as responsible for these mechanisms of action. S. dulcis has also been shown to exhibit analgesic, antimalarial, hepatoprotective, sedative, hypnotic, antiulcer, antisickling, and antimicrobial activities. Given this evidence, it may be concluded that S. dulcis could be promoted among the masses as an alternative and complementary therapy for diabetes, provided further scientific studies on the toxicological and pharmacological aspects are carried out through either in vivo or clinical means.

  9. Evidence based study of antidiabetic potential of C. maxima seeds - In vivo.

    Science.gov (United States)

    Kushawaha, Devesh Kumar; Yadav, Manjulika; Chatterji, Sanjukta; Srivastava, Amrita Kumari; Watal, Geeta

    2017-10-01

    In vitro antidiabetic efficacy of Cucurbita maxima seed extract (CMSE) has already been studied in our previous findings. Thus, in order to validate these findings in biological system, in vivo antidiabetic activity of aqueous extract was investigated in normal as well as diabetic experimental models. Variable doses of extract were administered orally to normal and STZ induced mild diabetic rats during fasting blood glucose (FBG) and glucose tolerance test (GTT) studies. In order to determine the extract's antidiabetic potential long-term FBG and post prandial glucose (PPG) studies were also carried out. Most effective dose of 200 mg kg -1 of CMSE decreases the blood glucose level (BGL) in normal rats by 29.02% at 6 h during FBG studies and 23.23% at 3 h during GTT. However, the maximum reduction observed in BGL of mild diabetic rats during GTT the same interval of time was 26.15%. Moreover, in case of severely diabetic rats a significant reduction of 39.33% was observed in FBG levels whereas, in case of positive control, rats treated with 2.5 mg kg -1 of glipizide, a fall of 42.9% in FBG levels was observed after 28 days. Results of PPG level also showed a fall of 33.20% in severely diabetic rats as compared to the positive control showing a fall of 44.2% at the end of the 28 days. Thus, the present study validate the hypoglycemic and antidiabetic effect of CMSE and hence this extract could be explored further for developing as a novel antidiabetic agent.

  10. Nanostructured Lipid Carriers Loaded with Baicalin: An Efficient Carrier for Enhanced Antidiabetic Effects.

    Science.gov (United States)

    Shi, Feng; Wei, Zheng; Zhao, Yingying; Xu, Ximing

    2016-01-01

    Recent studies have demonstrated that baicalin has antihyperglycemic effects by inhibiting lipid peroxidation. Baicalin is low hydrophilic and poorly absorbed after oral administration. Thus, a suitable formulation is highly desired to overcome the disadvantages of baicalin. The objective of this work was to prepare baicalin-loaded nanostructured lipid carriers (B-NLCs) for enhanced antidiabetic effects. B-NLCs were prepared by high-pressure homogenization method using Precirol as the solid lipid and Miglyol as the liquid lipid. The properties of the NLCs, such as particle size, zeta potential (ZP), and drug encapsulation efficiency (EE), were investigated. The morphology of NLCs was observed by transmission electron microscopy. In addition, drug release and antidiabetic activity were also studied. The results revealed that B-NLCs particles were uniformly in the nanosize range and of spherical morphology with a mean size of 92 ± 3.1 nm, a ZP of -31.35 ± 3.08 mV, and an EE of 85.29 ± 3.42%. Baicalin was released from NLCs in a sustained manner. In addition, B-NLCs showed a significantly higher antidiabetic efficacy compared with baicalin. B-NLCs described in this study are well-suited for the delivery of baicalin. Currently, herbal medicines have attracted increasing attention as a complementary approach for type 2 diabetesBaicalin has antihyperglycemic effects by inhibiting lipid peroxidationA suitable formulation is highly desired to overcome the disadvantages (poor solubility and low bioavailability) of baicalinNanostructured lipid carriers could enhance the antidiabetic effects of baicalin. Abbreviations used: B-NLCs: Baicalin-Loaded Nanostructured Lipid Carriers, B-SUS: Baicalin Water Suspension, EE: Encapsulation Efficiency, FBG: Fasting Blood Glucose, HbAlc: Glycosylated Hemoglobin, HPLC: High-performance Liquid Chromatography; NLCs: Nanostructured Lipid Carriers, PI: Polydispersity Index, SD: Sprague-Dawley, SLNs: Solid lipid nanoparticles, STZ

  11. Antidiabetic Plants of Iran

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    Ashrafeddin Goushegir

    2011-10-01

    Full Text Available To identify the antidiabetic plants of Iran, a systematic review of the published literature on the efficacy of Iranian medicinal plant for glucose control in patients with type 2 diabetes mellitus was conducted. We performed an electronic literature search of MEDLINE, Science Direct, Scopus, Proquest, Ebsco, Googlescholar, SID, Cochrane Library Database, from 1966 up to June 2010. The search terms were complementary and alternative medicine (CAM, diabetes mellitus, plant (herb, Iran, patient, glycemic control, clinical trial, RCT, natural or herbal medicine, hypoglycemic plants, and individual herb names from popular sources, or combination of these key words. Available Randomized Controlled Trials (RCT published in English or Persian language examined effects of an herb (limited to Iran on glycemic indexes in type 2 diabetic patients were included. Among all of the articles identified in the initial database search, 23 trials were RCT, examining herbs as potential therapy for type 2 diabetes mellitus. The key outcome for antidiabetic effect was changes in blood glucose or HbA1 c, as well as improves in insulin sensitivity or resistance. Available data suggest that several antidiabetic plants of Iran need further study. Among the RCT studies, the best evidence in glycemic control was found in Citrullus colocynthus, Ipomoea betatas, Silybum marianum and Trigonella foenum graecum.

  12. Antidiabetic Effect of an Active Components Group from Ilex kudingcha and Its Chemical Composition

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    Chengwu Song

    2012-01-01

    Full Text Available The leaves of Ilex kudingcha are used as an ethnomedicine in the treatment of symptoms related with diabetes mellitus and obesity throughout the centuries in China. The present study investigated the antidiabetic activities of an active components group (ACG obtained from Ilex kudingcha in alloxan-induced type 2 diabetic mice. ACG significantly reduced the elevated levels of serum glycaemic and lipids in type 2 diabetic mice. 3-Hydroxy-3-methylglutaryl coenzyme A reductase and glucokinase were upregulated significantly, while fatty acid synthetase, glucose-6-phosphatase catalytic enzyme was downregulated in diabetic mice after treatment of ACG. These findings clearly provided evidences regarding the antidiabetic potentials of ACG from Ilex kudingcha. Using LC-DAD/HR-ESI-TOF-MS, six major components were identified in ACG. They are three dicaffeoylquinic acids that have been reported previously, and three new triterpenoid saponins, which were the first time to be identified in Ilex kudingcha. It is reasonable to assume that antidiabetic activity of Ilex kudingcha against hyperglycemia resulted from these six major components. Also, synergistic effects among their compounds may exist in the antidiabetic activity of Ilex kudingcha.

  13. Fishing for Nature's Hits: Establishment of the Zebrafish as a Model for Screening Antidiabetic Natural Products.

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    Tabassum, Nadia; Tai, Hongmei; Jung, Da-Woon; Williams, Darren R

    2015-01-01

    Diabetes mellitus affects millions of people worldwide and significantly impacts their quality of life. Moreover, life threatening diseases, such as myocardial infarction, blindness, and renal disorders, increase the morbidity rate associated with diabetes. Various natural products from medicinal plants have shown potential as antidiabetes agents in cell-based screening systems. However, many of these potential "hits" fail in mammalian tests, due to issues such as poor pharmacokinetics and/or toxic side effects. To address this problem, the zebrafish (Danio rerio) model has been developed as a "bridge" to provide an experimentally convenient animal-based screening system to identify drug candidates that are active in vivo. In this review, we discuss the application of zebrafish to drug screening technologies for diabetes research. Specifically, the discovery of natural product-based antidiabetes compounds using zebrafish will be described. For example, it has recently been demonstrated that antidiabetic natural compounds can be identified in zebrafish using activity guided fractionation of crude plant extracts. Moreover, the development of fluorescent-tagged glucose bioprobes has allowed the screening of natural product-based modulators of glucose homeostasis in zebrafish. We hope that the discussion of these advances will illustrate the value and simplicity of establishing zebrafish-based assays for antidiabetic compounds in natural products-based laboratories.

  14. Rapid increase in the use of oral antidiabetic drugs in the United States, 1990-2001.

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    Wysowski, Diane K; Armstrong, George; Governale, Laura

    2003-06-01

    To describe the use of oral antidiabetic drugs for management of type 2 diabetes in the U.S. from 1990 through 2001. Data on oral antidiabetic drugs were derived from two pharmaceutical marketing databases from IMS Health, the National Prescription Audit Plus and the National Disease and Therapeutic Index. In 1990, 23.4 million outpatient prescriptions of oral antidiabetic agents were dispensed. By 2001, this number had increased 3.9-fold, to 91.8 million prescriptions. Glipizide and glyburide, two sulfonylurea medications, accounted for approximately 77% of prescriptions of oral antidiabetic drugs in 1990 and 35.5% of prescriptions in 2001. By 2001, the biguanide metformin (approved in 1995) had captured approximately 33% of prescriptions, and the thiazolidinedione insulin sensitizers (rosiglitazone and pioglitazone marketed beginning in 1999) accounted for approximately 17% of market share. Compared with patients treated in 1990, those in 2001 were proportionately younger and they more often used oral antidiabetic drugs and insulin in combination. Internists and general and family practitioners were the primary prescribers of this class of drugs. Consistent with the reported increase in the prevalence of type 2 diabetes, the number of dispensed outpatient prescriptions of oral antidiabetic drugs increased rapidly between 1990 and 2001. This period was marked by an increase in the treatment of younger people and the use of oral antidiabetic drugs in combination. With the approval in the last decade of several new types of oral antidiabetic medications with different mechanisms of action, options for management of type 2 diabetes have expanded.

  15. Analysis of glycation induced protein cross-linking inhibitory effects of some antidiabetic plants and spices.

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    Perera, Handunge Kumudu Irani; Handuwalage, Charith Sandaruwan

    2015-06-09

    Protein cross-linking which occurs towards the latter part of protein glycation is implicated in the development of chronic diabetic complications. Glycation induced protein cross-linking inhibitory effects of nine antidiabetic plants and three spices were evaluated in this study using a novel, simple, electrophoresis based method. Methanol extracts of thirteen plants including nine antidiabetic plants and three spices were used. Lysozyme and fructose were incubated at 37 °C in the presence or absence of different concentrations of plant extracts up to 31 days. Standard glycation inhibitor aminoguanidine and other appropriate controls were included. A recently established sodium dodecyl polyacrylamide gel electrophoresis (SDS-PAGE) method was used to detect the products of protein cross-linking in the incubation mixtures. High molecular weight protein products representing the dimer, trimer and tetramer of lysozyme were detected in the presence of fructose. Among the nine antidiabetic plants, seven showed glycation induced protein cross-linking inhibitory effects namely Ficus racemosa (FR) stem bark, Gymnema sylvestre (GS) leaves, Musa paradisiaca (MP) yam, Phyllanthus debilis (PD) whole plant, Phyllanthus emblica (PE) fruit, Pterocarpus marsupium (PM) latex and Tinospora cordifolia (TC) leaves. Inhibition observed with Coccinia grandis (CG) leaves and Strychnos potatorum (SP) seeds were much low. Leaves of Gymnema lactiferum (GL), the plant without known antidiabetic effects showed the lowest inhibition. All three spices namely Coriandrum sativum (CS) seeds, Cinnamomum zeylanicum (CZ) bark and Syzygium aromaticum (SA) flower buds showed cross-link inhibitory effects with higher effects in CS and SA. PD, PE, PM, CS and SA showed almost complete inhibition on the formation of cross-linking with 25 μg/ml extracts. Methanol extracts of PD, PE, PM, CS and SA have shown promising inhibitory effects on glycation induced protein cross-linking.

  16. Comparative Study of Antidiabetic Activity and Oxidative Stress Induced by Zinc Oxide Nanoparticles and Zinc Sulfate in Diabetic Rats.

    Science.gov (United States)

    Nazarizadeh, Ali; Asri-Rezaie, Siamak

    2016-08-01

    In the current study, antidiabetic activity and toxic effects of zinc oxide nanoparticles (ZnO) were investigated in diabetic rats compared to zinc sulfate (ZnSO4) with particular emphasis on oxidative stress parameters. One hundred and twenty male Wistar rats were divided into two healthy and diabetic groups, randomly. Each major group was further subdivided into five subgroups and then orally supplemented with various doses of ZnO (1, 3, and 10 mg/kg) and ZnSO4 (30 mg/kg) for 56 consecutive days. ZnO showed greater antidiabetic activity compared to ZnSO4 evidenced by improved glucose disposal, insulin levels, and zinc status. The altered activities of erythrocyte antioxidant enzymes as well as raised levels of lipid peroxidation and a marked reduction of total antioxidant capacity were observed in rats receiving ZnO. ZnO nanoparticles acted as a potent antidiabetic agent, however, severely elicited oxidative stress particularly at higher doses.

  17. 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. ...

  18. Induced desensitization of the insulinotropic effects of antidiabetic drugs, BTS 67 582 and tolbutamide

    Science.gov (United States)

    McClenaghan, Neville H; Ball, Andrew J; Flatt, Peter R

    2000-01-01

    Acute and chronic mechanisms of action of novel insulinotropic antidiabetic drug, BTS 67 582 (1,1-dimethyl-2-(2-morpholinophenyl)guanidine fumarate), were examined in the stable cultured BRIN-BD11 cell line. BTS 67 582 (100–400 μM) stimulated a concentration-dependent increase (PBTS 67 582 in culture time-dependently decreased subsequent responsiveness to acute challenge with 200 μM BTS 67 582 or 200 μM tolbutamide at 12–18 h (PBTS 67 582 and tolbutamide. Culture with 100 μM BTS 67 582 or 100 μM tolbutamide did not affect basal insulin secretion, cellular insulin content, or cell viability and exerted no influence on the secretory responsiveness to 200 μM of the imidazoline, efaroxan. While 18 h BTS 67 582 culture did not affect the insulin-releasing actions (PBTS 67 582 shares a common signalling pathway to sulphonylurea but not imidazoline drugs. Desensitization of drug action may provide an important approach to dissect sites of action of novel and established insulinotropic antidiabetic agents. PMID:10807689

  19. Antidiabetic Effects of a Chinese Herbal Medicinal Compound Sangguayin Preparation via PI3K/Akt Signaling Pathway in db/db Mice

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    Qichang Xing

    2018-01-01

    Full Text Available Sangguayin (SGY, comprising four types of Chinese herbs, can be used as both food and medicine and has been clinically used to treat type 2 diabetes mellitus (T2DM for a long time. Our previous study demonstrated the antidiabetic effect of SGY in experimental T2DM rats fed with a high-fat diet and treated with a low dose of streptozotocin. However, its mechanism of action is questionable. In this study, we refined the traditional SGY decoction and investigated its antidiabetic activity in db/db mice. We evaluated the possible molecular mechanism using skeletal muscle tissues. The results show that the treatment with SGY preparation resulted in a decrease in the blood glucose, glycated serum protein, and blood lipid levels and an improvement in the glucose tolerance as well as insulin resistance. In addition, SGY preparation remarkably upregulated the expression of insulin receptor, insulin receptor substrate-1, phosphoinositide 3 kinase (PI3K, protein kinase B (Akt, and glucose transporter type 4 (GLUT4. Thus, SGY preparation is an effective agent for the treatment of T2DM, and its molecular mechanism may be related to the regulation of PI3K/Akt signaling in the skeletal muscle.

  20. Marine Algae As A Prospective Source For Antidiabetic Compounds - A Brief Review.

    Science.gov (United States)

    Unnikrishnan, Pulikkaparambil Sasidharan; Jayasri, Mangalam Achuthananda

    2018-01-01

    Diabetes Mellitus (DM) is a metabolic disorder characterized by chronic hyperglycaemia, which is attributed to several life threatening complications including atherosclerosis, nephropathy, and retinopathy. The current therapies available for the management of DM mainly include oral antidiabetic drugs and insulin injections. However, continuous use of synthetic drugs provides lower healing with many side effects. Therefore, there is an urge for safe and efficient antidiabetic drugs for the management of DM. In the continuing search for effective antidiabetic drugs, marine algae (seaweeds) remains as a promising source with potent bioactivity. It is anticipated that the isolation, characterization, and pharmacological study of unexplored marine algae can be useful in the discovery of novel antidiabetic compounds with high biomedical value. Among marine algae, brown and red algae are reported to exhibit antidiabetic activity. Majority of the investigations on algal derived compounds controls the blood glucose levels through the inhbition of carbohydrate hydroloyzing enzymes and protein tyrosine phosphatase 1B enzymes, insulin sensitization, glucose uptake effect and other protective effects against diabetic complications. Based on the above perspective this review provides; profiles for various marine algae posessing antidiabetic activity. This study also highlights the therapeutic potential of compounds isolated from marine algae for the effective management of diabetes and its associated complications. Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.org.

  1. Physicochemical and crystal structure analyses of the antidiabetic agent troglitazone.

    Science.gov (United States)

    Kobayashi, Katsuhiro; Fukuhara, Hiroshi; Hata, Tadashi; Sekine, Akiko; Uekusa, Hidehiro; Ohashi, Yuji

    2003-07-01

    The antidiabetic agent troglitazone has two asymmetric carbons located at the chroman ring and the thiazolidine ring and is produced as a mixture of equal amounts of four optical isomers, 2R-5S, 2S-5R, 2R-5R, and 2S-5S. The crystalline powdered drug substance consists of two diastereomer pairs, 2R-5R/2S-5S and 2R-5S/2S-5R. There are many types of crystals obtained from various crystallization conditions. The X-ray structure analysis and the physicochemical analyses of troglitazone were performed. The solvated crystals of the 2R-5R/2S-5S pair were crystallized from several solutions: methanol, ethanol, acetonitrile, and dichloromethane. The ratio of solvent and troglitazone was 1 : 2 (L1/2-form). The monohydrate crystals were obtained from aqueous acetone solution (L1-form). On the other hand, only an anhydrate crystal of the 2R-5S/2S-5R pair was crystallized from various solutions (H0-form). The dihydrous mixed crystal (MA2-form) was obtained from a mixture of the two diastereomer pairs of 2R-5R/2S-5S and 2R-5S/2S-5R in equal amounts by the slow evaporation of aqueous acetone solution. The crystal structure of the MA2-form is similar to the H0-form. When the MA2 crystal was kept under low humidity, it was converted into the dehydrated form (MA0-form) with retention of the single crystal form. The structure of the MA0-form is isomorphous to the H0-form. The MA2-form was converted into the MA0-form and vice versa with retention of the single crystal under low and high humidity, respectively. The crystallization and storage conditions of the drug substances were successfully analyzed.

  2. Phytochemical Compositions and In vitro Assessments of Antioxidant and Antidiabetic Potentials of Fractions from Ehretia cymosa Thonn.

    Science.gov (United States)

    Ogundajo, Akintayo; Ashafa, Anofi Tom

    2017-10-01

    Ehretia cymosa Thonn. is a popular medicinal plant used in different parts of West Africa for the treatment of various ailments including diabetes mellitus. The current study investigates bioactive constituents and in vitro antioxidant and antidiabetic potentials of fractions from extract of E. cymosa . Phytochemical investigation and antioxidant assays were carried out using standard procedures. Antidiabetic potential was assessed by evaluating the inhibitory effects of the fractions on the activities of α-amylase and α-glucosidase, while bioactive constituent's identification was carried out using gas chromatography-mass spectrometric (GC-MS) analysis. The phytochemistry tests of the fractions revealed the presence of tannins, phenols, flavonoids, steroids, terpene, alkaloid, and cardiac glycosides. Methanol fraction shows higher phenolic (27.44 mg gallic acid/g) and flavonoid (235.31 mg quercetin/g) contents, while ethyl acetate fraction revealed higher proanthocyanidins (28.31 mg catechin/g). Methanol fraction displayed higher ( P fractions displayed higher inhibition ( P fraction also inhibited α-amylase and α-glucosidase in competitive and noncompetitive modes, respectively. The GC-MS chromatogram of the methanol fraction revealed 24 compounds, which include phytol (1.78%), stearic acid (1.02%), and 2-hexadecyloxirane (34.18%), which are known antidiabetic and antioxidant agents. The results indicate E. cymosa leaves as source of active phytochemicals with therapeutic potentials in the management of diabetes. E. cymosa fractions possess antioxidant and antidiabetic activities. Hence, it is a source of active phytochemicals with therapeutic potentials in the management of diabetesThe high flavonoid, phenolic, and proanthocyanidin contents of fractions from E. cymosa also contribute to its antioxidant and antidiabetic propertiesMethanol fraction of E. cymosa displayed better antidiabetic activities compared to acarbose as revealed by their half maximal

  3. 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.

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

    Science.gov (United States)

    But, Anna; Wang, Haining; Männistö, Satu; Pukkala, Eero; Haukka, Jari

    2014-01-01

    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.

  5. Phospholipid complex enriched micelles: A novel drug delivery approach for promoting the antidiabetic effect of repaglinide.

    Science.gov (United States)

    Kassem, Ahmed Alaa; Abd El-Alim, Sameh Hosam; Basha, Mona; Salama, Abeer

    2017-03-01

    To enhance the oral antidiabetic effect of repaglinide (RG), a newly emerging approach, based on the combination of phospholipid complexation and micelle techniques, was employed. Repaglinide-phospholipid complex (RG-PLC) was prepared by the solvent-evaporation method then characterized using Differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy (FT-IR) and X-ray powder diffraction (XPRD). The results revealed obvious disappearance of the characteristic peaks of the prepared RG-PLCs confirming the formation of drug-phospholipid complex. RG-PLC enriched micelles (RG-PLC-Ms) were prepared by the solvent-evaporation technique employing poloxamer 188 as surfactant. The prepared RG-PLC-Ms showed high drug encapsulation efficiencies (93.81-99.38%), with nanometric particle diameters (500.61-665.32nm) of monodisperse distribution and high stability (Zeta potential < -29.8mV). The in vitro release of RG from RG-PLC-Ms was pH-dependant according to the release media. A higher release pattern was reported in pH=1.2 compared to a more retarded release in pH=6.8 owing to two different kinetics of drug release. Oral antidiabetic effect of two optimized RG-PLC-M formulations was evaluated in an alloxan-induced diabetic rat model for 7-day treatment protocol. The two investigated formulations depicted normal blood glucose, serum malondialdehyde and insulin levels as well as an improved lipid profile, at the end of daily oral treatment, in contrast to RG marketed tablets implying enhanced antidiabetic effect of the drug. Hence, phospholipid-complex enriched micelles approach holds a promising potential for promoting the antidiabetic effect of RG. Copyright © 2016 Elsevier B.V. All rights reserved.

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

    Science.gov (United States)

    Orhan, Nilüfer; Hoçbaç, Sanem; Orhan, Didem Deliorman; Asian, Mustafa; Ergun, Fatma

    2014-01-01

    Objective(s): Ethnopharmacological field surveys demonstrated that many plants, such as Gentiana olivieri, Helichrysum graveolens, Helichrysum plicatum ssp. plicatum, Juniperus oxycedrus ssp. oxycedrus, Juniperus communis var. saxatilis, Viscum album (ssp. album, ssp. austriacum), are used as traditional medicine for diabetes in different regions of Anatolia. The present study was designed to evaluate the in vitro antidiabetic effects of some selected plants, tested in animal models recently. Materials and Methods: α-glucosidase and α-amylase enzyme inhibitory effects of the plant extracts were investigated and Acarbose was used as a reference drug. Additionally, radical scavenging capacities were determined using 2,2’-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) ABTS radical cation scavenging assay and total phenolic content of the extracts were evaluated using Folin Ciocalteu method. Results: H. graveolens ethanol extract exhibited the highest inhibitory activity (55.7 % ± 2.2) on α-amylase enzyme. Additionally, J. oxycedrus hydro-alcoholic leaf extract had potent α-amylase inhibitory effect, while the hydro-alcoholic extract of J. communis fruit showed the highest α-glucosidase inhibitory activity (IC50: 4.4 μg/ml). Conclusion: Results indicated that, antidiabetic effect of hydro-alcoholic extracts of H. graveolens capitulums, J. communis fruit and J. oxycedrus leaf might arise from inhibition of digestive enzymes. PMID:25140204

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

    Directory of Open Access Journals (Sweden)

    Nilüfer Orhan

    2014-06-01

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

  8. Antidiabetic therapies and male reproductive function: where do we stand?

    Science.gov (United States)

    Tavares, R S; Escada-Rebelo, S; Silva, A F; Sousa, M I; Ramalho-Santos, J; Amaral, S

    2018-01-01

    Diabetes mellitus has been increasing at alarming rates in recent years, thus jeopardizing human health worldwide. Several antidiabetic drugs have been introduced in the market to manage glycemic levels, and proven effective in avoiding, minimizing or preventing the appearance or development of diabetes mellitus-related complications. However, and despite the established association between such pathology and male reproductive dysfunction, the influence of these therapeutic interventions on such topics have been scarcely explored. Importantly, this pathology may contribute toward the global decline in male fertility, giving the increasing preponderance of diabetes mellitus in young men at their reproductive age. Therefore, it is mandatory that the reproductive health of diabetic individuals is maintained during the antidiabetic treatment. With this in mind, we have gathered the available information and made a critical analysis regarding the effects of several antidiabetic drugs on male reproductive function. Unlike insulin, which has a clear and fundamental role on male reproductive function, the other antidiabetic therapies' effects at this level seem incoherent. In fact, studies are highly controversial possibly due to the different experimental study approaches, which, in our opinion, suggests caution when it comes to prescribing such drugs to young diabetic patients. Overall, much is still to be determined and further studies are needed to clarify the safety of these antidiabetic strategies on male reproductive system. Aspects such as the effects of insulin levels variations, consequent of insulin therapy, as well as what will be the impact of the side effect hypoglycemia, common to several therapeutic strategies discussed, on the male reproductive system are still to be addressed. © 2018 Society for Reproduction and Fertility.

  9. Antidiabetic and antihiperlipidemic effect of Andrographis paniculata (Burm. f.) Nees and andrographolide in high-fructose-fat-fed rats

    Science.gov (United States)

    Nugroho, Agung Endro; Andrie, Mohamad; Warditiani, Ni Kadek; Siswanto, Eka; Pramono, Suwidjiyo; Lukitaningsih, Endang

    2012-01-01

    Objectives: Andrographis paniculata (Burm. f.) Nees originates from India and grows widely in many areas in Southeast Asian countries. Andrographis paniculata (Burm. f.) Nees has shown an antidiabetic effect in type 1 DM rats. The present study investigates the purified extract of the plant and its active compound andrographolide for antidiabetic and antihyperlipidemic effects in high-fructose-fat-fed rats, a model of type 2 DM rats. Materials and Methods: Hyperglycemia in rats was induced by high-fructose-fat diet containing 36% fructose, 15% lard, and 5% egg yolks in 0.36 g/200 gb.wt. 55 days. The rats were treated with the extract or test compound on the 50th day. Antidiabetic activity was measured by estimating mainly the pre– and postprandial blood glucose levels and other parameters such as cholesterol, LDL, triglyceride, and body weight. Results: The purified extract and andrographolide significantly (PAndrographis paniculata (Burm. f.) Nees or its active compound andrographolide showed hypoglycemic and hypolipidemic effects in high-fat-fructose-fed rat. PMID:22701250

  10. Cost-effectiveness of exenatide twice daily vs insulin glargine as add-on therapy to oral antidiabetic agents in patients with type 2 diabetes in China.

    Science.gov (United States)

    Gu, Shuyan; Wang, Xiaoyong; Qiao, Qing; Gao, Weiguo; Wang, Jian; Dong, Hengjin

    2017-12-01

    To estimate the long-term cost-effectiveness of exenatide twice daily vs insulin glargine once daily as add-on therapy to oral antidiabetic agents (OADs) for Chinese patients with type 2 diabetes (T2DM). The Cardiff Diabetes Model was used to simulate disease progression and estimate the long-term effects of exenatide twice daily vs insulin glargine once daily. Patient profiles and treatment effects required for the model were obtained from literature reviews (English and Chinese databases) and from a meta-analysis of 8 randomized controlled trials comparing exenatide twice daily with insulin glargine once daily add-on to OADs for T2DM in China. Medical expenditure data were collected from 639 patients with T2DM (aged ≥18 years) with and without complications incurred between January 1, 2014 and December 31, 2015 from claims databases in Shandong, China. Costs (2014 Chinese Yuan [¥]) and benefits were estimated, from the payers' perspective, over 40 years at a discount rate of 3%. A series of sensitivity analyses were performed. Patients on exenatide twice daily + OAD had a lower predicted incidence of most cardiovascular and hypoglycaemic events and lower total costs compared with those on insulin glargine once daily + OAD. A greater number of quality-adjusted life years (QALYs; 1.94) at a cost saving of ¥117 706 gained was associated with exenatide twice daily vs insulin glargine once daily. (i.e. cost saving of ¥60 764/QALY) per patient. In Chinese patients with T2DM inadequately controlled by OADs, exenatide twice daily is a cost-effective add-on therapy alternative to insulin glargine once daily, and may address the problem of an excess of medical needs resulting from weight gain and hypoglycaemia in T2DM treatment. © 2017 John Wiley & Sons Ltd.

  11. Antidiabetic Properties of Germinated Brown Rice: A Systematic Review

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    Mustapha Umar Imam

    2012-01-01

    Full Text Available Diet is an important variable in the course of type 2 diabetes, which has generated interest in dietary options like germinated brown rice (GBR for effective management of the disease among rice-consuming populations. In vitro data and animal experiments show that GBR has potentials as a functional diet for managing this disease, and short-term clinical studies indicate encouraging results. Mechanisms for antidiabetic effects of GBR due to bioactive compounds like γ-aminobutyric acid (GABA, γ-oryzanol, dietary fibre, phenolics, vitamins, acylated steryl β-glucoside, and minerals include antihyperglycemia, low insulin index, antioxidative effect, antithrombosis, antihypertensive effect, hypocholesterolemia, and neuroprotective effects. The evidence so far suggests that there may be enormous benefits for diabetics in rice-consuming populations if white rice is replaced with GBR. However, long-term clinical studies are still needed to verify these findings on antidiabetic effects of GBR. Thus, we present a review on the antidiabetic properties of GBR from relevant preclinical and clinical studies, in order to provide detailed information on this subject for researchers to review the potential of GBR in combating this disease.

  12. Characterization and comparison of sodium-glucose cotransporter 2 inhibitors: Part 2. Antidiabetic effects in type 2 diabetic mice

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    Atsuo Tahara

    2016-07-01

    Full Text Available Previously we investigated the pharmacokinetic, pharmacodynamic, and pharmacologic properties of all six sodium-glucose cotransporter (SGLT 2 inhibitors commercially available in Japan using normal and diabetic mice. We classified the SGLT2 inhibitors with respect to duration of action as either long-acting (ipragliflozin and dapagliflozin or intermediate-acting (tofogliflozin, canagliflozin, empagliflozin, and luseogliflozin. In the present study, antidiabetic effects of repeated administration of these SGLT2 inhibitors in type 2 diabetic mice were investigated. When repeatedly administered for 4 weeks, all SGLT2 inhibitors significantly exhibited antihyperglycemic, antihyperinsulinemic, and pancreas-protective effects, as well as insulin resistance-improving effects. When compared at doses producing comparable reduction in hyperglycemia across all drugs, the antidiabetic effects of ipragliflozin and dapagliflozin were more potent than those of the other four drugs, but these differences among the six drugs were not statistically significant. Further, an oral glucose tolerance test performed after repeated administration demonstrated significant improvement in glucose tolerance only with ipragliflozin and dapagliflozin, implying improved insulin resistance and secretion. Taken together, these findings demonstrate that, although all SGLT2 inhibitors exert antidiabetic effects in type 2 diabetic mice, these pharmacologic effects might be slightly superior with the long-acting drugs, which are able to provide favorable blood glucose control throughout the day.

  13. Short-term antidiabetic treatment with insulin or metformin has a similar impact on the components of metabolic syndrome in women with gestational diabetes mellitus requiring antidiabetic agents: results of a prospective, randomised study.

    Science.gov (United States)

    Zawiejska, A; Wender-Ozegowska, E; Grewling-Szmit, K; Brazert, M; Brazert, J

    2016-04-01

    Gestational diabetes mellitus (GDM) is associated with an increased prevalence of fetal and maternal complications primarily caused by maternal hyperglycemia, which results in abnormal fetal growth. Diet modification is a common first step in the treatment of GDM, followed by antidiabetic pharmacotherapy if this approach fails. Insulin therapy is generally accepted; however, oral hypoglycemic agents have been used in this population. In this prospective, randomised study, we compared maternal metabolic status after treatment with insulin or metformin. Pregnant women (gestational age: ≥ 20 weeks) with GDM requiring medical hypoglycemic treatment were randomly allocated to the Metformin (n = 35) or Insulin (n = 43) Groups. Maternal metabolic status - assessed by glycated hemoglobin (HBA1c) level, glycemic profile, insulin concentration, Homeostatic Model Assessment - Insulin Resistance index, and lipids - was recorded at booking and throughout pregnancy. The characteristics of the study group were: maternal age 33.5 ± 5.9 years, gestational age at baseline 28.5 ± 3.5 weeks, prepregnancy body mass index (BMI) 32.2 ± 3.5 kg/m(2), HbA1c at baseline 5.6 ± 0.6%, and average daily glycemia 5.9 ± 0.6 mmol/dl. Fasting glycemia at term was significantly lower in the Insulin Group but there were no significant differences in mean daily glycemia, HbA1c and BMI at term between the groups. Longitudinally, there was a small but significant increase in BMI and a significant increase in high-density lipoprotein-cholesterol in the Insulin Group and a significant increase in the atherogenic index of plasma (AIP) and a trend towards higher triglycerides in the Metformin Group. Both fasting and average daily glycemia were significantly reduced following treatment in both groups. No such change was evident for HbA1c. In a relative risk analysis, metformin treatment was associated with an insignificant elevated risk of HbA1c, triglycerides and lipid indices falling within the

  14. Antidiabetic and protective effects of the aqueous extract of Arbutus unedo L. in streptozotocin-nicotinamide-induced diabetic mice.

    Science.gov (United States)

    Mrabti, Hanae Naceiri; Sayah, Karima; Jaradat, Nidal; Kichou, Faouzi; Ed-Dra, Abdelaziz; Belarj, Badiaa; Cherrah, Yahia; Faouzi, My El Abbes

    2018-02-21

    Background Diabetes mellitus (DM) is currently a major health problem and the most common chronic disease worldwide. Traditional medicinal plants remedies remain a potential adjunct therapy to maintain better glycemic control while also imparting few side-effects. Arbutus unedo L. has been traditionally used to manage several diseases including diabetes. This study was undertaken to contribute the validation of the traditional use of Arbutus unedoL. (Ericaceae) in the treatment of diabetes. Methods In-vitro antidiabetic effect of the A. unedo roots aqueous extract was conducted using α-glucosidase and α-amylase assays. While in-vivo antidiabetic activity was conducted using streptozotocin-nicotinamide (STZ-NA) induced diabetic mice. Diabetic animals were orally administered the aqueous extract in 500 mg/kg of body weight to assess the antidiabetic effect. The blood glucose level and body weight of the experimental animals were monitored for 4 weeks. In addition, the histopathological examination of the treated mice pancreas was also conducted to observe the changes of β-cells during the treatment process. Results The extract produced a significant decrease in blood glucose level in diabetic mice. This decrease was equivalent to that which observed in mice treated with a standard after 2-4 weeks. In addition, the plant extract exhibited a potent inhibitory effect on α-amylase and α-glucosidase activity with IC50 values of 730.15±0.25 μg/mL and 94.81±5.99 μg/mL, respectively. Moreover, the histopathologic examination of the pancreas showed a restoration of normal pancreatic islet cell architecture which observed in the diabetic mice treated with plant extract. Conclusions The aqueous A. unedo roots extract has a significant in vitro and in vivo antidiabetic effects and improves metabolic alterations. The revealed results justify its traditional medicinal use.

  15. Effectiveness and tolerability of second-line therapy with vildagliptin versus other oral agents in type 2 diabetes (EDGE): post-hoc subanalysis of the Belgian data.

    Science.gov (United States)

    Hoste, J; Daci, E; Mathieu, C

    2014-06-01

    To assess the efficacy and safety of vildagliptin versus other oral glucose-lowering drugs added to antidiabetic monotherapy in Belgian patients with type 2 diabetes mellitus, in comparison to the global EDGE study results. This is a pre-specified post-hoc subanalysis of the Belgian patient cohort from a worldwide 1-year observational study that compared the effectiveness and tolerability of vildagliptin to other oral antidiabetic agents in type 2 diabetes patients failing monotherapy with oral glucose-lowering agents (EDGE). A total of 1793 Belgian patients were enrolled. Physicians could add any oral antidiabetic drug and patients entered either into the vildagliptin or the comparator cohort. The primary effectiveness and tolerability endpoint was defined as the proportion of patients having a treatment response (HbA1c reduction from baseline to month 12 endpoint >0·3%) without hypoglycemia, weight gain, peripheral oedema, or gastrointestinal side-effects. In the Belgian population, 37·8% of patients in the vildagliptin group and 32·8% in the comparator group had a decrease in HbA1c of >0·3% without the predefined tolerability issues of hypoglycemia, weight gain, oedema or, gastrointestinal complaints (primary endpoint), resulting in an unadjusted odds ratio of 1·24 (95% CI: 0·96-1·61). Mean HbA1c change from baseline was -0·81% in the vildagliptin cohort and -0·75% in the comparator cohort. Overall, vildagliptin was well tolerated with similarly low incidences of total adverse events (14·9% versus 14·5% in the compactor group) and serious adverse events (2·7% versus 2·5% in the comparator group). In this EDGE subgroup of Belgian patients with type 2 diabetes who do not achieve the glycemic targets with monotherapy, a similar trend as in the global EDGE study was observed. Adding vildagliptin as a second oral glucose-lowering agent resulted in lowering HbA1c to <7% without weight gain, hypoglycemia or peripheral oedema in a higher proportion of

  16. Antidiabetic effects of Cuscuta reflexa Roxb. in streptozotocin induced diabetic rats.

    Science.gov (United States)

    Rath, Diptirani; Kar, Durga Madhab; Panigrahi, Sandeep Kumar; Maharana, Laxmidhar

    2016-11-04

    Cuscuta reflexa Roxb. (Convolvulaceae) is traditionally used to treat diabetes mellitus by tribal people of north-east India and Bangladesh. To evaluate the anti-diabetic effects of methanol and aqueous extracts of the aerial parts of Cuscuta reflexa Roxb. in normal, glucose loaded and Streptozotocin (STZ) induced diabetic rats. The methanol (MECR) and aqueous (AECR) extracts (200 and 400mg/kg body weight) were administered orally to normal and diabetic rats with Metformin and solvent control as comparison groups. Long term effects like FBG, OGTT, lipid profile, HbA1c, body weight, histopathology of major organs, etc. were investigated. MECR and AECR did not have hypoglycemic effects in normal rats. Both AECR and MECR (400mg/kg) treatments showed significant reduction in blood glucose during OGTT in diabetic rats at 3h. Single oral administration of methanol and aqueous extracts (400mg/kg) to diabetic rats significantly reduced (p<0.05) blood glucose level to 61.90% and 55.39% respectively as compared to the Metformin group i.e. 68.32% at the end of 8h. MECR (400mg/kg body weight for 30 days to diabetic rats) showed a significant decrease (p<0.01) of blood glucose level to 60.00% as compared to other groups. The treatment also resulted an improvement in body weights, decreased HbA1c and restored lipid profile. Histopathological injury was not observed, rather repair of beta cells was seen in extract treated diabetic rats. Methanolic extract of C. reflexa has significant antidiabetic effects and improves metabolic alterations thereby justifying its traditional folkloric claims. Copyright © 2016 Elsevier Ireland Ltd. All rights reserved.

  17. Antidiabetic and antihyperlipidemic activity of Piper longum root aqueous extract in STZ induced diabetic rats

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    Nabi Shaik Abdul

    2013-02-01

    Full Text Available Abstract Background The available drugs for diabetes, Insulin or Oral hypoglycemic agents have one or more side effects. Search for new antidiabetic drugs with minimal or no side effects from medicinal plants is a challenge according to WHO recommendations. In this aspect, the present study was undertaken to evaluate the antihyperglycemic and antihyperlipidemic effects of Piper longum root aqueous extract (PlrAqe in streptozotocin (STZ induced diabetic rats. Methods Diabetes was induced in male Wister albino rats by intraperitoneal administration of STZ (50 mg/kg.b.w. Fasting blood glucose (FBG levels were measured by glucose-oxidase & peroxidase reactive strips. Serum biochemical parameters such as glycosylated hemoglobin (HbA1c, total cholesterol (TC, triglycerides (TG, very low density lipoprotein (VLDL, low density lipoprotein (LDL and high density lipoprotein (HDL cholesterol were estimated. The activities of liver and kidney functional markers were measured. The statistical analysis of results was carried out using Student t-test and one-way analysis (ANOVA followed by DMRT. Results During the short term study the aqueous extract at a dosage of 200 mg/kg.b.w was found to possess significant antidiabetic activity after 6 h of the treatment. The administration of aqueous extract at the same dose for 30 days in STZ induced diabetic rats resulted in a significant decrease in FBG levels with the corrections of diabetic dyslipidemia compared to untreated diabetic rats. There was a significant decrease in the activities of liver and renal functional markers in diabetic treated rats compared to untreated diabetic rats indicating the protective role of the aqueous extract against liver and kidney damage and its non-toxic property. Conclusions From the above results it is concluded that the plant extract is capable of managing hyperglycemia and complications of diabetes in STZ induced diabetic rats. Hence this plant may be considered as one of the

  18. CoMFA and CoMSIA studies on C-aryl glucoside SGLT2 inhibitors as potential anti-diabetic agents.

    Science.gov (United States)

    Vyas, V K; Bhatt, H G; Patel, P K; Jalu, J; Chintha, C; Gupta, N; Ghate, M

    2013-01-01

    SGLT2 has become a target of therapeutic interest in diabetes research. CoMFA and CoMSIA studies were performed on C-aryl glucoside SGLT2 inhibitors (180 analogues) as potential anti-diabetic agents. Three different alignment strategies were used for the compounds. The best CoMFA and CoMSIA models were obtained by means of Distill rigid body alignment of training and test sets, and found statistically significant with cross-validated coefficients (q²) of 0.602 and 0.618, respectively, and conventional coefficients (r²) of 0.905 and 0.902, respectively. Both models were validated by a test set of 36 compounds giving satisfactory predicted correlation coefficients (r² pred) of 0.622 and 0.584 for CoMFA and CoMSIA models, respectively. A comparison was made with earlier 3D QSAR study on SGLT2 inhibitors, which shows that our 3D QSAR models are better than earlier models to predict good inhibitory activity. CoMFA and CoMSIA models generated in this work can provide useful information to design new compounds and helped in prediction of activity prior to synthesis.

  19. Anti-Diabetic Effect of Portulaca oleracea L. Polysaccharideandits Mechanism in Diabetic Rats.

    Science.gov (United States)

    Bai, Yu; Zang, Xueli; Ma, Jinshu; Xu, Guangyu

    2016-07-25

    Diabetes mellitus (DM) is a metabolic syndrome caused by multiple genetic and environmental factors. Traditional Chinese medicine preparations have shown a comprehensive and function-regulating characteristic. Purslane (Portulaca oleracea L.) is an annual succulent herb. Currently, there have been some related reports on the treatment of diabetes with purslane. The current study was designed to separate and purify the polysaccharide, a systematic study of its physical and chemical properties, antioxidant activity, and anti-diabetic mechanism, in order to provide a theoretical basis for the development of drugs of purslane. A crude water soluble polysaccharide extracted from purslane was named CPOP (crude Portulaca oleracea L. polysaccharide). Effects of CPOP on bodyweight, glucose tolerance test (GTT), fasting blood glucose (FBG), fasting serum insulin (FINS), insulin sensitivity index (ISI), interleukin-6 (IL-6), tumor necrosis factor-α (TNF-α), methane dicarboxylic aldehyde (MDA), and superoxygen dehydrogenises (SOD) were investigated. The results indicate that the oral administration of CPOP could significantly increase the body weight and significantly improve the glucose tolerance in diabetic rats. Meanwhile, CPOP could significantly reduce the FBG level, and elevate the FINS level and ISI value in diabetic rats. In addition, CPOP could significantly reduce TNF-α and IL-6 levels in diabetic rats; CPOP could also reduce MDA and SOD activities in the liver tissue of diabetic rats. These results suggest that the anti-diabetic effect of CPOP may be associated with its antioxidant and anti-inflammatory effects.

  20. Anti-Diabetic Effect of Portulaca oleracea L. Polysaccharideandits Mechanism in Diabetic Rats

    Directory of Open Access Journals (Sweden)

    Yu Bai

    2016-07-01

    Full Text Available Diabetes mellitus (DM is a metabolic syndrome caused by multiple genetic and environmental factors. Traditional Chinese medicine preparations have shown a comprehensive and function-regulating characteristic. Purslane (Portulaca oleracea L. is an annual succulent herb. Currently, there have been some related reports on the treatment of diabetes with purslane. The current study was designed to separate and purify the polysaccharide, a systematic study of its physical and chemical properties, antioxidant activity, and anti-diabetic mechanism, in order to provide a theoretical basis for the development of drugs of purslane. A crude water soluble polysaccharide extracted from purslane was named CPOP (crude Portulaca oleracea L. polysaccharide. Effects of CPOP on bodyweight, glucose tolerance test (GTT, fasting blood glucose (FBG, fasting serum insulin (FINS, insulin sensitivity index (ISI, interleukin-6 (IL-6, tumor necrosis factor-α (TNF-α, methane dicarboxylic aldehyde (MDA, and superoxygen dehydrogenises (SOD were investigated. The results indicate that the oral administration of CPOP could significantly increase the body weight and significantly improve the glucose tolerance in diabetic rats. Meanwhile, CPOP could significantly reduce the FBG level, and elevate the FINS level and ISI value in diabetic rats. In addition, CPOP could significantly reduce TNF-α and IL-6 levels in diabetic rats; CPOP could also reduce MDA and SOD activities in the liver tissue of diabetic rats. These results suggest that the anti-diabetic effect of CPOP may be associated with its antioxidant and anti-inflammatory effects.

  1. Effects of antidiabetic drugs on the incidence of macrovascular complications and mortality in type 2 diabetes mellitus: a new perspective on sodium-glucose co-transporter 2 inhibitors.

    Science.gov (United States)

    Rahelić, Dario; Javor, Eugen; Lucijanić, Tomo; Skelin, Marko

    2017-02-01

    Elevated hemoglobin A 1c (HbA 1c ) values correlate with microvascular and macrovascular complications. Thus, patients with type 2 diabetes mellitus (T2DM) are at an increased risk of developing macrovascular events. Treatment of T2DM should be based on a multifactorial approach because of its evidence regarding reduction of macrovascular complications and mortality in T2DM. It is well known that intensive glucose control reduces the risk of microvascular complications in T2DM, but the effects of antidiabetic drugs on macrovascular complications and mortality in T2DM are less clear. The results of recent trials have demonstrated clear evidence that empagliflozin and liraglutide reduce cardiovascular (CV) and all-cause mortality in T2DM, an effect that is absent in other members of antidiabetic drugs. Empagliflozin is a member of a novel class of antidiabetic drugs, the sodium-glucose co-transporter 2 (SGLT2) inhibitors. Two ongoing randomized clinical trials involving other SGLT2 inhibitors, canagliflozin and dapagliflozin, will provide additional evidence of the beneficial effects of SGLT2 inhibitors in T2DM population. The aim of this paper is to systematically present the latest evidence regarding the usage of antidiabetic drugs, and the reduction of macrovascular complications and mortality. A special emphasis is put on the novel class of antidiabetic drugs, of SGLT2 inhibitors. Key messages Macrovascular complications and mortality are best clinical trial endpoints for evaluating the efficacy of antidiabetic drugs. The first antidiabetic drug that demonstrated a reduction in mortality in the treatment of type 2 diabetes mellitus (T2DM) was empagliflozin, a sodium-glucose co-transporter 2 (SGLT2) inhibitor. SGLT2 inhibitors are novel class of antidiabetic drugs that play a promising role in the treatment of T2DM.

  2. [Use of new antidiabetics in the elderly population].

    Science.gov (United States)

    Besse, Sarah; Besse, Arun; Jornayvaz, François R

    2016-06-01

    Over the last few years, we have noticed the arrival on the market of new antidiabetic treatments. These represent an potential advantage because of the increase in the prevalence of type 2 diabetes, particularly in the elderly population. Nevertheless, elderly patients have a number of frailties that should be considered in the treatment of this condition. There is a lack of literature in this population as elderly are frequently excluded from randomized controlled trials. Therefore, guidelines were developed based on the consensus of experts in geriatrics and diabetology for this specific population. We have to consider the potential benefits and adverse effects of the new antidiabetics in older patients.

  3. Stevia rebaudiana loaded titanium oxide nanomaterials as an antidiabetic agent in rats

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    Ariadna Langle

    Full Text Available Abstract Stevia rebaudiana (Bertoni Bertoni, Asteraceae, is a plant with hypoglycemic and antihyperlipidemic properties. S. rebaudiana (SrB has become a lead candidate for the treatment of the diabetes mellitus. However, chronic administrations of S. rebaudiana are required to cause the normoglycemic effect. Importantly, nanomaterials in general and titanium dioxide (TiO2 in particular have become effective tools for drug delivery. In this work, we obtained TiO2 nanomaterials with SrB at different concentrations (10, 20 and 30 µM by sol–gel method. After this nanomaterials were characterized by Fourier transform infrared spectroscopy and transmission electron microscopy. Where it was demonstrated, the presence of the S. rebaudiana in TiO2 nanomaterials, which were observed as hemispherical agglomerated particles of different sizes. The nanomaterials were evaluated in male rats whose diabetes mellitus-phenotype was induced by alloxan (200 mg/kg, i.p.. The co-administration of TiO2-SrB (20 and 30 µM induced a significant and permanent decrease in the glucose concentration since 4 h, until 30 days post-administration. Likewise, the concentrations of insulin, glycosylated hemoglobin, cholesterol, and triacylglycerides showed a significant recovery to basal levels. The major finding of the study was that the TiO2-SrB (20 and 30 µM has a potent and prolonged activity antidiabetic. TiO2 can be considered like an appropriated vehicle in the continuous freeing of active substances to treat of diabetes mellitus.

  4. Effect of capping agents: Structural, optical and biological properties of ZnO nanoparticles

    Energy Technology Data Exchange (ETDEWEB)

    Javed, Rabia [Department of Biotechnology, Faculty of Biological Sciences, Quaid-i-Azam University, Islamabad 45320 (Pakistan); Usman, Muhammad, E-mail: uk_phy@yahoo.com [Department of Physics, Faculty of Natural Sciences, Quaid-i-Azam University, Islamabad 45320 (Pakistan); Department of Physics, School of Science and Engineering, Lahore University of Management Sciences, Lahore 54729 (Pakistan); Tabassum, Saira; Zia, Muhammad [Department of Biotechnology, Faculty of Biological Sciences, Quaid-i-Azam University, Islamabad 45320 (Pakistan)

    2016-11-15

    Highlights: • ZnO nanoparticles have been effectively capped with polyethylene glycol (PEG) and polyvinyl pyrrolidone (PVP) shown by the data of XRD, FTIR and UV–visible spectroscopy. • Reduction in size occurred from 34 nm to 26 nm due to capping agent and band gap energy increases with the decrease in the particle size. • Antibacterial activity against Gram-positive bacteria is greater than the Gram-negative bacteria. • All biological assays reveal highest activities in capped ZnO nanoparticles as compared to the uncapped ZnO nanoparticles. • Highest antibacterial activity has been exhibited by ZnO-PVP while highest antioxidant and antidiabetic activities have been conferred by ZnO- PEG. - Abstract: Different biological activities of capped and uncapped ZnO nanoparticles were investigated, and the effects of potential capping agents on these biological activities were studied. ZnO nanoparticles were synthesized and capped by polyethylene glycol (PEG) and polyvinyl pyrrolidone (PVP) using a simple chemical method of co-precipitation. Characterization by X-ray diffraction (XRD), Fourier transform Infrared spectroscopy (FTIR) and UV–vis spectroscopy confirmed the crystallinity, size, functional group, and band gap of synthesized nanoparticles. Reduction in size occurred from 34 nm to 26 nm due to surfactant. Results of all biological activities indicated significantly higher values in capped as compared to uncapped nanoparticles. Antibacterial activity against Staphylococcus aureus (ATCC 6538), Bacillus subtilis (ATCC 6633), Escherichia coli (ATCC15224), and Acetobacter was obtained. This activity was more prominent against Gram-positive bacteria, and ZnO-PVP nanoparticles elucidated highest antibacterial activity (zone of inhibition 17 mm) against Gram-positive, Bacillus subtilis species. Antioxidant activities including total flavonoid content, total phenolic content, total antioxidant capacity, total reducing power and %age inhibition of DPPH, and

  5. Effect of capping agents: Structural, optical and biological properties of ZnO nanoparticles

    International Nuclear Information System (INIS)

    Javed, Rabia; Usman, Muhammad; Tabassum, Saira; Zia, Muhammad

    2016-01-01

    Highlights: • ZnO nanoparticles have been effectively capped with polyethylene glycol (PEG) and polyvinyl pyrrolidone (PVP) shown by the data of XRD, FTIR and UV–visible spectroscopy. • Reduction in size occurred from 34 nm to 26 nm due to capping agent and band gap energy increases with the decrease in the particle size. • Antibacterial activity against Gram-positive bacteria is greater than the Gram-negative bacteria. • All biological assays reveal highest activities in capped ZnO nanoparticles as compared to the uncapped ZnO nanoparticles. • Highest antibacterial activity has been exhibited by ZnO-PVP while highest antioxidant and antidiabetic activities have been conferred by ZnO- PEG. - Abstract: Different biological activities of capped and uncapped ZnO nanoparticles were investigated, and the effects of potential capping agents on these biological activities were studied. ZnO nanoparticles were synthesized and capped by polyethylene glycol (PEG) and polyvinyl pyrrolidone (PVP) using a simple chemical method of co-precipitation. Characterization by X-ray diffraction (XRD), Fourier transform Infrared spectroscopy (FTIR) and UV–vis spectroscopy confirmed the crystallinity, size, functional group, and band gap of synthesized nanoparticles. Reduction in size occurred from 34 nm to 26 nm due to surfactant. Results of all biological activities indicated significantly higher values in capped as compared to uncapped nanoparticles. Antibacterial activity against Staphylococcus aureus (ATCC 6538), Bacillus subtilis (ATCC 6633), Escherichia coli (ATCC15224), and Acetobacter was obtained. This activity was more prominent against Gram-positive bacteria, and ZnO-PVP nanoparticles elucidated highest antibacterial activity (zone of inhibition 17 mm) against Gram-positive, Bacillus subtilis species. Antioxidant activities including total flavonoid content, total phenolic content, total antioxidant capacity, total reducing power and %age inhibition of DPPH, and

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

    Science.gov (United States)

    Salib, Josline Y.; Michael, Helana N.; Eskande, Emad Fawzy

    2013-01-01

    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-Lrhamnopyranosyl]-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 PMID:23598921

  7. Synthesis, pharmacological evaluation and molecular docking studies of pyrimidinedione based DPP-4 inhibitors as antidiabetic agents

    Science.gov (United States)

    Jha, Vibhu; Bhadoriya, Kamlendra Singh

    2018-04-01

    Dipeptidyl peptidase-4 (DPP-4) inhibitors are a class of newly developed antidiabetic drugs that bock DPP-4. DPP-4 is responsible for degradation of incretins harmones such as GLP-1 (Glucagon like Peptide) and GIP (Gastric inhibitory polypeptide) that maintain blood-glucose level. Pyrimidinedione based compounds were designed and synthesized for DPP-4 inhibitory activity. These heterocycles were designed by taking Alogliptin as a reference DPP-4 inhibitors and synthesized as N-methylated and N-benzylated pyrimidinediones. These compounds were subjected to DPP-4 assay, five out of nine synthesized compounds have shown in vitro DPP-4 inhibitory activity in significant range. Further, molecular docking studies of these compounds were performed on DPP-4 subunit and compared with natural DPP-4 inhibitors like Flavone, Resveratrol, Quercetin, Diprotin A. Docking studies have led to the conclusion that there are some identical amino acid interactions as Tyr 666 and Tyr 662, seen in both synthesized compounds and natural DPP-4 inhibitors. This study completely gives a good scope for further derivatisation and optimization of synthesized compounds to get clinical candidate as DPP-4 inhibitor for antidiabetic activity.

  8. Antidiabetic effect of Scoparia dulcis: effect on lipid peroxidation in streptozotocin diabetes.

    Science.gov (United States)

    Pari, L; Latha, M

    2005-03-01

    Oxidative damage has been suggested to be a contributory factor in the development and complications of diabetes. The antioxidant effect of an aqueous extract of Scoparia dulcis, an indigenous plant used in Ayurvedic medicine in India was studied in rats with streptozotocin-induced diabetes. Oral administration of Scoparia dulcis plant extract (SPEt) (200 mg/kg body weight) for 3 weeks resulted in a significant reduction in blood glucose and an increase in plasma insulin. The aqueous extract also resulted in decreased free radical formation in tissues (liver and kidney) studied. The decrease in thiobarbituric acid reactive substances (TBARS) and hydroperoxides (HPX) and increase in the activities of superoxide dismutase (SOD), catalase (CAT), glutathione peroxidase (GPx), reduced glutathione (GSH) and glutathione-S-transferase (GST) clearly show the antioxidant properties of SPEt in addition to its antidiabetic effect. The effect of SPEt at 200 mg/kg body weight was better than glibenclamide, a reference drug.

  9. Antidiabetic plant-derived nutraceuticals: a critical review.

    Science.gov (United States)

    Naveen, Jayapal; Baskaran, Vallikannan

    2018-06-01

    Diabetes mellitus (DM) is one of the major health problems in the world, especially amongst the urban population. Chemically synthesized drugs used to decrease the ill effects of DM and its secondary complications cause adverse side effects, viz., weight gain, gastrointestinal disturbances, and heart failure. Currently, various other approaches, viz., diet control, physical exercise and use of antidiabetic plant-derived molecules/foods are advocated to manage DM, as they are economical with fewer or no side effects. This review mainly focuses on antidiabetic plants, chemically characterized plant molecules and plant-based foods in the treatment of DM. Very little science-based evidence is available on the mechanism of action of plant-derived food molecules on the DM targets. Critical DM targets include α-amylase, α-glucosidase, DPP-IV, aldose reductase, PPAR-γ, AMP kinase and GLUT4. In-depth studies carried out on a few of those targets with specific mechanisms of action are addressed in this review. This review may help future researchers in identifying a right plant molecule to treat DM or to develop food formulations for DM management.

  10. Antidiabetic potential of Brachylaena discolor | Mellem | African ...

    African Journals Online (AJOL)

    Background: The traditional African herbal medicinal system has many reports of anti-diabetic food plants with no known side effects. Such plants and their products have been widely prescribed for diabetic treatment with little known mechanistic basis of their functioning. Therefore, these natural products need to be ...

  11. Evaluation of Antioxidant, Antidiabetic and Anticholinesterase Activities of Smallanthus sonchifolius Landraces and Correlation with Their Phytochemical Profiles.

    Science.gov (United States)

    Russo, Daniela; Valentão, Patrícia; Andrade, Paula B; Fernandez, Eloy C; Milella, Luigi

    2015-07-31

    The present study aimed to investigate the phytochemical profile of leaf methanol extracts of fourteen Smallanthus sonchifolius (yacon) landraces and their antioxidant, anticholinesterase and antidiabetic activities that could lead to the finding of more effective agents for the treatment and management of Alzheimer's disease and diabetes. For this purpose, antioxidant activity was assessed using different tests: ferric reducing ability power (FRAP), 2,2-diphenyl-1-picryl hydrazyl (DPPH), nitric oxide (˙NO) and superoxide (O2˙-) scavenging and lipid peroxidation inhibition assays. Anticholinesterase activity was investigated by quantifying the acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activities, whereas antidiabetic activity was investigated by α-amylase and α-glucosidase inhibition tests. To understand the contribution of metabolites, phytochemical screening was also performed by high performance liquid chromatography-diode array detector (HPLC-DAD) system. Among all, methanol extract of PER09, PER04 and ECU44 landraces exhibited the highest relative antioxidant capacity index (RACI). ECU44 was found to be rich in 4,5-di-O-caffeoylquinic acid (CQA) and 3,5-di-O-CQA and displayed a good α-amylase and α-glucosidase inhibition, showing the lowest IC50 values. Flavonoids, instead, seem to be involved in the AChE and BChE inhibition. The results of this study revealed that the bioactive compound content differences could be determinant for the medicinal properties of this plant especially for antioxidant and antidiabetic activities.

  12. Evaluation of Antioxidant, Antidiabetic and Anticholinesterase Activities of Smallanthus sonchifolius Landraces and Correlation with Their Phytochemical Profiles

    Science.gov (United States)

    Russo, Daniela; Valentão, Patrícia; Andrade, Paula B.; Fernandez, Eloy C.; Milella, Luigi

    2015-01-01

    The present study aimed to investigate the phytochemical profile of leaf methanol extracts of fourteen Smallanthus sonchifolius (yacon) landraces and their antioxidant, anticholinesterase and antidiabetic activities that could lead to the finding of more effective agents for the treatment and management of Alzheimer’s disease and diabetes. For this purpose, antioxidant activity was assessed using different tests: ferric reducing ability power (FRAP), 2,2-diphenyl-1-picryl hydrazyl (DPPH), nitric oxide (˙NO) and superoxide (O2˙−) scavenging and lipid peroxidation inhibition assays. Anticholinesterase activity was investigated by quantifying the acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activities, whereas antidiabetic activity was investigated by α-amylase and α-glucosidase inhibition tests. To understand the contribution of metabolites, phytochemical screening was also performed by high performance liquid chromatography-diode array detector (HPLC-DAD) system. Among all, methanol extract of PER09, PER04 and ECU44 landraces exhibited the highest relative antioxidant capacity index (RACI). ECU44 was found to be rich in 4,5-di-O-caffeoylquinic acid (CQA) and 3,5-di-O-CQA and displayed a good α-amylase and α-glucosidase inhibition, showing the lowest IC50 values. Flavonoids, instead, seem to be involved in the AChE and BChE inhibition. The results of this study revealed that the bioactive compound content differences could be determinant for the medicinal properties of this plant especially for antioxidant and antidiabetic activities. PMID:26263984

  13. Evaluation of Antioxidant, Antidiabetic and Anticholinesterase Activities of Smallanthus sonchifolius Landraces and Correlation with Their Phytochemical Profiles

    Directory of Open Access Journals (Sweden)

    Daniela Russo

    2015-07-01

    Full Text Available The present study aimed to investigate the phytochemical profile of leaf methanol extracts of fourteen Smallanthus sonchifolius (yacon landraces and their antioxidant, anticholinesterase and antidiabetic activities that could lead to the finding of more effective agents for the treatment and management of Alzheimer’s disease and diabetes. For this purpose, antioxidant activity was assessed using different tests: ferric reducing ability power (FRAP, 2,2-diphenyl-1-picryl hydrazyl (DPPH, nitric oxide (˙NO and superoxide (O2˙− scavenging and lipid peroxidation inhibition assays. Anticholinesterase activity was investigated by quantifying the acetylcholinesterase (AChE and butyrylcholinesterase (BChE inhibitory activities, whereas antidiabetic activity was investigated by α-amylase and α-glucosidase inhibition tests. To understand the contribution of metabolites, phytochemical screening was also performed by high performance liquid chromatography-diode array detector (HPLC-DAD system. Among all, methanol extract of PER09, PER04 and ECU44 landraces exhibited the highest relative antioxidant capacity index (RACI. ECU44 was found to be rich in 4,5-di-O-caffeoylquinic acid (CQA and 3,5-di-O-CQA and displayed a good α-amylase and α-glucosidase inhibition, showing the lowest IC50 values. Flavonoids, instead, seem to be involved in the AChE and BChE inhibition. The results of this study revealed that the bioactive compound content differences could be determinant for the medicinal properties of this plant especially for antioxidant and antidiabetic activities.

  14. In Vitro Antidiabetic Effects and Antioxidant Potential of Cassia nemophila Pods

    Directory of Open Access Journals (Sweden)

    Gauhar Rehman

    2018-01-01

    Full Text Available The antidiabetic and antioxidant potential of ethanolic extract of Cassia nemophila pod (EECNP was evaluated by three in vitro assays, including yeast glucose uptake assay, glucose adsorption assay, and DPPH radical scavenging activity. The result revealed that the extracts have enhanced the uptake of glucose through the plasma membrane of yeast cells. A linear increase in glucose uptake by yeast cells was noticed with gradual increase in the concentration of the test samples. Moreover, the adsorption capacity of the EECNP was directly proportional to the molar concentration of glucose. Also, the DPPH radical scavenging capacity of the extract was increased to a maximum value of 43.3% at 80 μg/ml, which was then decreased to 41.9% at 100 μg/ml. From the results, it was concluded that EECNP possess good antidiabetic and antioxidant properties as shown by in vitro assays.

  15. Synthesis, spectroscopic, structural and thermal characterizations of vanadyl(IV) adenine complex prospective as antidiabetic drug agent

    Science.gov (United States)

    El-Megharbel, Samy M.; Hamza, Reham Z.; Refat, Moamen S.

    2015-01-01

    The vanadyl(IV) adenine complex; [VO(Adn)2]ṡSO4; was synthesized and characterized. The molar conductivity of this complex was measured in DMSO solution that showed an electrolyte nature. Spectroscopic investigation of the green solid complex studied here indicate that the adenine acts as a bidentate ligand, coordinated to vanadyl(IV) ions through the nitrogen atoms N7 and nitrogen atom of amino group. Thus, from the results presented the vanadyl(IV) complex has square pyramid geometry. Further characterizations using thermal analyses and scanning electron techniques was useful. The aim of this paper was to introduce a new drug model for the diabetic complications by synthesized a novel mononuclear vanadyl(IV) adenine complex to mimic insulin action and reducing blood sugar level. The antidiabetic ability of this complex was investigated in STZ-induced diabetic mice. The results suggested that VO(IV)/adenine complex has antidiabetic activity, it improved the lipid profile, it improved liver and kidney functions, also it ameliorated insulin hormone and blood glucose levels. The vanadyl(IV) complex possesses an antioxidant activity and this was clear through studying SOD, CAT, MDA, GSH and methionine synthase. The current results support the therapeutic potentiality of vanadyl(IV)/adenine complex for the management and treatment of diabetes.

  16. A nuclear-receptor-dependent phosphatidylcholine pathway with antidiabetic effects.

    Science.gov (United States)

    Lee, Jae Man; Lee, Yoon Kwang; Mamrosh, Jennifer L; Busby, Scott A; Griffin, Patrick R; Pathak, Manish C; Ortlund, Eric A; Moore, David D

    2011-05-25

    Nuclear hormone receptors regulate diverse metabolic pathways and the orphan nuclear receptor LRH-1 (also known as NR5A2) regulates bile acid biosynthesis. Structural studies have identified phospholipids as potential LRH-1 ligands, but their functional relevance is unclear. Here we show that an unusual phosphatidylcholine species with two saturated 12 carbon fatty acid acyl side chains (dilauroyl phosphatidylcholine (DLPC)) is an LRH-1 agonist ligand in vitro. DLPC treatment induces bile acid biosynthetic enzymes in mouse liver, increases bile acid levels, and lowers hepatic triglycerides and serum glucose. DLPC treatment also decreases hepatic steatosis and improves glucose homeostasis in two mouse models of insulin resistance. Both the antidiabetic and lipotropic effects are lost in liver-specific Lrh-1 knockouts. These findings identify an LRH-1 dependent phosphatidylcholine signalling pathway that regulates bile acid metabolism and glucose homeostasis.

  17. Antidiabetic and Antioxidant Impacts of Desert Date (Balanites aegyptiaca and Parsley (Petroselinum sativum Aqueous Extracts: Lessons from Experimental Rats

    Directory of Open Access Journals (Sweden)

    Nasser S. Abou Khalil

    2016-01-01

    Full Text Available Medicinal plants are effective in controlling plasma glucose level with minimal side effects and are commonly used in developing countries as an alternative therapy for the treatment of type 1 diabetes mellitus. The aim of this study is to evaluate the potential antidiabetic and antioxidant impacts of Balanites aegyptiaca and Petroselinum sativum extracts on streptozotocin-induced diabetic and normal rats. The influences of these extracts on body weight, plasma glucose, insulin, total antioxidant capacity (TAC, malondialdehyde (MDA levels, and liver-pyruvate kinase (L-PK levels were assessed. Furthermore, the weight and histomorphological changes of the pancreas were studied in the different experimental groups. The herbal preparations significantly reduced the mean plasma glucose and MDA levels and significantly increased the mean plasma insulin, L-PK, and TAC levels in the treated diabetic groups compared to the diabetic control group. An obvious increase in the weight of the pancreas and the size of the islets of Langerhans and improvement in the histoarchitecture were evident in the treated groups compared to untreated ones. In conclusion, the present study provides a scientific evidence for the traditional use of these extracts as antidiabetic and antioxidant agents in type 1 diabetes mellitus.

  18. Antidiabetic and Antioxidant Impacts of Desert Date (Balanites aegyptiaca) and Parsley (Petroselinum sativum) Aqueous Extracts: Lessons from Experimental Rats.

    Science.gov (United States)

    Abou Khalil, Nasser S; Abou-Elhamd, Alaa S; Wasfy, Salwa I A; El Mileegy, Ibtisam M H; Hamed, Mohamed Y; Ageely, Hussein M

    2016-01-01

    Medicinal plants are effective in controlling plasma glucose level with minimal side effects and are commonly used in developing countries as an alternative therapy for the treatment of type 1 diabetes mellitus. The aim of this study is to evaluate the potential antidiabetic and antioxidant impacts of Balanites aegyptiaca and Petroselinum sativum extracts on streptozotocin-induced diabetic and normal rats. The influences of these extracts on body weight, plasma glucose, insulin, total antioxidant capacity (TAC), malondialdehyde (MDA) levels, and liver-pyruvate kinase (L-PK) levels were assessed. Furthermore, the weight and histomorphological changes of the pancreas were studied in the different experimental groups. The herbal preparations significantly reduced the mean plasma glucose and MDA levels and significantly increased the mean plasma insulin, L-PK, and TAC levels in the treated diabetic groups compared to the diabetic control group. An obvious increase in the weight of the pancreas and the size of the islets of Langerhans and improvement in the histoarchitecture were evident in the treated groups compared to untreated ones. In conclusion, the present study provides a scientific evidence for the traditional use of these extracts as antidiabetic and antioxidant agents in type 1 diabetes mellitus.

  19. EFEK ANTIDIABETES EKSTRAK AIR KULIT BUAH PISANG AMBON (Musa paradisiaca L. TERHADAP MENCIT (Mus musculus MODEL HIPERGLIKEMIA

    Directory of Open Access Journals (Sweden)

    Sri Indrawati

    2015-10-01

    Full Text Available Pisang Ambon (Musa paradisiaca L. is one type of bananas usually consumed by Indonesian people. Besides its flesh which has high nutrition, its peels also has antioxidant activity. Antioxidants has the ability to reduce oxidative damage in people’s body with diabetes mellitus. Therefore, this study aimed to determine the antioxidant activity of the aqueous  extract of Pisang Ambon peels and to determine it’s effective dose as an antidiabetic agent in hyperglycemic mice. This study used male mice which all have been intravenously induced with alloxan at a dose of 50 mg/kgBW. They were then divided into five groups. The first two groups got Na CMC 0.5% (negative control and glibenclamide 0.65 mg/kgBW (positive control, while the other three got  the aqueous  extract of Pisang Ambon peels successively at doses of 400, 800, and 1200 mg/kgBW. The data were statistically analyzed using ANOVA (Analysis of Variance at 95% confidence interval with parameter of blood glucose levels difference between before and after treatment. The results showed that the aqueous extract of Pisang Ambon peels had antidiabetic activity at an effective dose of 400 mg/kgBW in hyperglycemic mice which was comparable to glibenclamide

  20. Pattern of pharmaceutical retailing of anti-diabetic products in Ibadan, Nigeria.

    Science.gov (United States)

    Famuyiwa, O O

    1991-01-01

    Twenty-four pharmacists in the city of Ibadan were surveyed through a self-administered structured questionnaire as to the extent of their involvement in the pharmaceutical retailing of antidiabetic products and their cost. Oral hypoglycemic agents especially, chlorpropamide (Diabenese) and glibenclamide (Daonil) were the most readily available drugs being obtainable from 21 (87.5%) pharmacies. Insulin was stocked regularly by only 14 (58.3%) of the pharmacists and insulin syringes and needles could be obtained from only 10 (41.6%) of the pharmacies. Among materials for urine testing, clinistix strip was the most readily available and fully one-third of the pharmacies did not stock any such material. The prices of all the products were disturbingly high and between 1983 and 1986 when retail prices were re-assessed, the cost of some materials had escalated by as much as 400%. Scarcity of antidiabetic products and their high cost pose serious challenges for those involved in the care of diabetic patients in Nigeria. Some suggestions have been made as to what steps both the government and the pharmaceutical industry can take in ensuring the availability of these life sustaining products for the increasingly large Nigerian diabetic population.

  1. Customization of biliopancreatic limb length to modulate and sustain antidiabetic effect of gastric bypass surgery.

    Science.gov (United States)

    Pal, A; Rhoads, D B; Tavakkoli, A

    2018-02-01

    Although Roux-en-Y Gastric Bypass (RYGB) remains the most effective treatment for obesity and type 2 diabetes (T2D), many patients fail to achieve remission, or relapse. Increasing intestinal limb lengths of RYGB may improve outcomes, but the mechanistic basis for this remains unclear. We hypothesize biliopancreatic (BP) limb length modulates the antidiabetic effect of RYGB. Rats underwent RYGB with a 20-cm (RYGB-20cm) or 40-cm (RYGB-40cm) BP limb and were compared with control animals. After 2 and 4 wk, portal and systemic blood was sampled during intestinal glucose infusion. Portosystemic gradient was used to calculate intestinal glucose utilization (G util ), absorption (G absorp ), and hormone secretion. Intestinal morphology and gene expression were assessed. At 2 wk, G absorp progressively decreased with increasing BP limb length; this pattern persisted at 4 wk. G util increased ≈70% in both RYGB-20cm and -40cm groups at 2 wk. At 4 wk, G util progressively increased with limb length. Furthermore, Roux limb weight, and expression of hexokinase and preproglucagon, exhibited a similar progressive increase. At 4 wk, glucagon-like peptide-1 and -2 levels were higher after RYGB-40cm, with associated increased secretion. We conclude that BP limb length modulates multiple antidiabetic mechanisms, analogous to the dose-response relationship of a drug. Early postoperatively, a longer BP limb reduces G absorp . Later, G util , Roux limb hypertrophy, hormone secretion, and hormone levels are increased with longer BP limb. Sustained high incretin levels may prevent weight regain and T2D relapse. These data provide the basis for customizing BP limb length according to patient characteristics and desired metabolic effect. NEW & NOTEWORTHY Biliopancreatic limb length in gastric bypass modulates multiple antidiabetic mechanisms, analogous to the dose-response relationship of a drug. With a longer biliopancreatic limb, Roux limb hypertrophy, increased glucose utilization

  2. Antidiabetic Evaluation of Momordica charantia L Fruit Extracts

    Science.gov (United States)

    Tahira, S; Hussain, F

    2014-01-01

    To investigate hypoglycaemic, hypolipidaemic and pancreatic beta cell regeneration activities of Momordica charantia L fruits (MC). Alloxan-induced diabetic rabbits were treated with methanolic and ethanolic MC extract. Effects of plant extracts and the drug glibenclamide on serum glucose, lipid profile and pancreatic beta cell were determined after two weeks of treatment. Serum glucose and lipid profiles were assayed by kit methods. Pancreatic tissue histopathology was performed to study pancreatic beta cell regeneration. Momordica charantia extracts produced significant hypoglycaemic effects (p Momordica charantia supplementations were unable to normalize glucose and lipid profiles. Glibenclamide, a standard drug, not only lowered hyperglycaemia and hyperlipidaemia but also restored the normal levels. Regeneration of pancreatic beta cells by MC extracts was minimal, with fractional improvement produced by glibenclamide. The most significant finding of the present study was a 28% reduction in hyperglycaemia by MC ethanol extracts. To determine reliable antidiabetic potentials of MC, identification of the relevant antidiabetic components and underlying mechanisms is warranted. PMID:25429471

  3. Antidiabetic Effects of Carassius auratus Complex Formula in High Fat Diet Combined Streptozotocin-Induced Diabetic Mice

    Directory of Open Access Journals (Sweden)

    Zhi-Hong Wang

    2014-01-01

    Full Text Available Carassius auratus complex formula, including Carassius auratus, Rhizoma dioscoreae, Lycium chinense, and Rehmannia glutinosa Libosch, is a combination prescription of traditional Chinese medicine, which has always been used to treat diabetes mellitus in ancient China. In this study, we provided experimental evidence for the use of Carassius auratus complex formula in the treatment of high fat diet combined streptozotocin- (STZ- induced type 2 diabetes. Carassius auratus complex formula aqueous extract was prepared and the effects of it on blood glucose, serum insulin, adipose tissue weight, oral glucose tolerance test (OGTT, total cholesterol, and triglyceride (TG levels in mice were measured. Moreover, adiponectin, TG synthesis related gene expressions, and the inhibitory effect of aldose reductase (AR were performed to evaluate its antidiabetic effects. After the 8-week treatment, blood glucose, insulin levels, and adipose tissue weight were significantly decreased. OGTT and HOMA-IR index showed improved glucose tolerance. It could also lower plasma TG, TC, and liver TG levels. Furthermore, Carassius auratus complex formula could inhibit the activity of AR and restore adiponectin expression in serum. Based on these findings, it is suggested that Carassius auratus complex formula possesses potent anti-diabetic effects on high fat diet combined STZ-induced diabetic mice.

  4. Differential anti-diabetic effects and mechanism of action of charantin-rich extract of Taiwanese Momordica charantia between type 1 and type 2 diabetic mice.

    Science.gov (United States)

    Wang, Hsien-Yi; Kan, Wei-Chih; Cheng, Tain-Junn; Yu, Sung-Hsun; Chang, Liang-Hao; Chuu, Jiunn-Jye

    2014-07-01

    Momordica charantia Linn. (Cucurbitaceae), also called bitter melon, has traditionally been used as a natural anti-diabetic agent for anti-hyperglycemic activity in several animal models and clinical trials. We investigated the differences in the anti-diabetic properties and mechanism of action of Taiwanese M. charantia (MC) between type 1 diabetic (T1D) and type 2 diabetic (T2D) mice. To clarify the beneficial effects of MC, we measured non-fasting glucose, oral glucose tolerance, and plasma insulin levels in KK/HIJ mice with high-fat diet-induced diabetes (200 mg/kg/day of charantin-rich extract of MC [CEMC]) and in ICR mice with STZ-induced diabetes. After 8 weeks, all the mice were exsanguinated, and the expression of the insulin-signaling-associated proteins in their tissue was evaluated, in coordination with the protective effects of CEMC against pancreatic β-cell toxicity (in vitro). Eight weeks of data indicated that CEMC caused a significant decline in non-fasting blood glucose, plasma glucose intolerance, and insulin resistance in the KK/HIJ mice, but not in the ICR mice. Furthermore, CEMC decreased plasma insulin and promoted the sensitivity of insulin by increasing the expression of GLUT4 in the skeletal muscle and of IRS-1 in the liver of KK/HIJ mice; however, CEMC extract had no effect on the insulin sensitivity of ICR mice. In vitro study showed that CEMC prevented pancreatic β cells from high-glucose-induced cytotoxicity after 24 h of incubation, but the protective effect was not detectable after 72 h. Collectively, the hypoglycemic effects of CEMC suggest that it has potential for increasing insulin sensitivity in patients with T2D rather than for protecting patients with T1D against β-cell dysfunction. Copyright © 2014 Elsevier Ltd. All rights reserved.

  5. Potential of Icariin Metabolites from Epimedium koreanum Nakai as Antidiabetic Therapeutic Agents

    Directory of Open Access Journals (Sweden)

    Da Hye Kim

    2017-06-01

    Full Text Available The therapeutic properties of Epimedium koreanum are presumed to be due to the flavonoid component icariin, which has been reported to have broad pharmacological potential and has demonstrated anti-diabetic, anti-Alzheimer’s disease, anti-tumor, and hepatoprotective activities. Considering these therapeutic properties of icariin, its deglycosylated icaritin and glycosylated flavonoids (icaeriside II, epimedin A, epimedin B, and epimedin C were evaluated for their ability to inhibit protein tyrosine phosphatase 1B (PTP1B and α-glucosidase. The results show that icaritin and icariside II exhibit potent inhibitory activities, with 50% inhibition concentration (IC50 values of 11.59 ± 1.39 μM and 9.94 ± 0.15 μM against PTP1B and 74.42 ± 0.01 and 106.59 ± 0.44 μM against α-glucosidase, respectively. With the exceptions of icaritin and icariside II, glycosylated flavonoids did not exhibit any inhibitory effects in the two assays. Enzyme kinetics analyses revealed that icaritin and icariside II demonstrated noncompetitive-type inhibition against PTP1B, with inhibition constant (Ki values of 11.41 and 11.66 μM, respectively. Moreover, molecular docking analysis confirmed that icaritin and icariside II both occupy the same site as allosteric ligand. Thus, the molecular docking simulation results were in close agreement with the experimental data with respect to inhibition activity. In conclusion, deglycosylated metabolites of icariin from E. koreanum might offer therapeutic potential for the treatment of type 2 diabetes mellitus.

  6. Antidiabetic Effect of Salvianolic Acid A on Diabetic Animal Models via AMPK Activation and Mitochondrial Regulation

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    Guifen Qiang

    2015-05-01

    Full Text Available Background/Aims: Diabetes mellitus (DM characterized by hyperglycemia contributes to macrovascular and microvascular complications. Salvianolic acid A (SalA is a polyphenolic compound isolated from the root of Salvia miltiorrhiza Bunge, which is a traditional Chinese medicine widely used to treat cardiovascular diseases. However, little is known about its antidiabetic effect. Our study aimed to investigate the in vivo and in vitro antidiabetic effect of SalA and the underlying mechanisms. Methods: Alloxan-induced type 1 diabetic mice and high-fat diet (HFD and low-dose streptozotocin (STZ-induced type 2 diabetic rats received SalA treatment. Blood glucose, oral glucose tolerance test (OGTT, 24-h food and water intake were monitored. In vitro, glucose consumption and uptake were measured in HepG2 cells and L6 myotubes. Mitochondrial function was detected in hepatic and skeletal muscle mitochondria. AMP-activated protein kinase (AMPK and Akt were analyzed by western blot. Results: In both type 1 and type 2 diabetic animals, SalA lowered fasting blood glucose (FBG and fed blood glucose in dose-dependent manner, as well as reduced 24-h food and water intake. In vitro, SalA caused dose-dependent increase in glucose consumption and enhanced glucose uptake. SalA significantly increased ATP production from 10 min to 12 h in HepG2 cells and L6 myotubes. Interestingly, SalA decreased mitochondrial membrane potential (MMP in HepG2 cells. Furthermore, SalA improved hepatic and skeletal muscle mitochondrial function, increased ATP production, and concurrently decreased MMP. In particularly, SalA activated AMPK phosphorylation through Ca2+/calmodulin-dependent protein kinase kinase β (CaMKKβ/AMPK signaling pathway, independent of liver kinase 1 (LKB1/AMPK pathway. However, SalA didn't show any effect on insulin secretagogue and activation of PI3K/Akt signaling pathway. Conclusion: SalA exhibits the antidiabetic effects in diabetic animal models through

  7. Synthesis of (+)-Antroquinonol: An Antihyperglycemic Agent.

    Science.gov (United States)

    Sulake, Rohidas S; Lin, Hsiao-Han; Hsu, Chia-Yu; Weng, Ching-Feng; Chen, Chinpiao

    2015-06-19

    The total synthesis of antroquinonol has been accomplished through Suzuki-Miyaura cross-coupling and Barton-McCombie reaction, and the α,β-unsaturation was achieved through selenylation and oxidation protocols. In vitro and in vivo studies on the glucose-lowering properties of antroquinonol indicate that it is a potential antidiabetic agent.

  8. Comparative effectiveness of vildagliptin in combination with other oral anti-diabetes agents in usual-care conditions: the EDGE-Latin America study.

    Science.gov (United States)

    Mendivil, Carlos O; Márquez-Rodríguez, Eduardo; Angel, Iván D; Paz, Gustavo; Rodríguez, Cruz; Almada, Jorge; Szyskowsky, Ofelia

    2014-09-01

    To assess the proportion of patients on vildagliptin add-on dual therapy who respond to treatment over a 12 month follow-up, relative to comparator oral anti-diabetes dual therapy, in a usual care setting. Participants were patients with type 2 diabetes (T2DM) aged 18 years and older from 311 centers in Argentina, Colombia, Ecuador, Mexico and Venezuela. Patients were taking monotherapy with an oral anti-diabetes drug (OAD), and were prescribed a new add-on OAD based on the judgment of their personal physician. According to this choice, patients were assigned to one of the two cohorts: vildagliptin or comparator OADs. The primary endpoint was the proportion of patients achieving an A1c drop >0.3% without edema, hypoglycemia, weight gain or discontinuation due to gastrointestinal (GI) events. The secondary endpoint was the proportion of patients with baseline A1c ≥7% who reached the goal of an A1c vildagliptin cohort and 771 in the comparator cohort. The proportion of patients reaching the primary endpoint was higher in the vildagliptin cohort (60.3%) than the comparator cohort (50.7%), OR 1.48 (95% CI: 1.25-1.73). The same was observed for the secondary endpoint (44.8 versus 33.1%) OR 1.64 (95% CI: 1.37-1.98). The incidence of adverse events was low and similar between treatment cohorts. In a usual care setting, patients treated with a vildagliptin combination succeeded in lowering A1c to <7%, without weight gain, hypoglycemia or peripheral edema more often than patients treated with comparator combinations, without increased risk of adverse events. Key limitations are the observational nature of the study and its relatively limited 12 month timeframe.

  9. Sodium glucose co-transporter 2 (SGLT2) inhibitors: novel antidiabetic agents.

    Science.gov (United States)

    Washburn, William N

    2012-05-01

    Maintenance of glucose homeostasis in healthy individuals involves SGLT2 (sodium glucose co-transporter 2)-mediated recovery of glucose from the glomerular filtrate which otherwise would be excreted in urine. Clinical studies indicate that SGLT2 inhibitors provide an insulin-independent means to reduce the hyperglycemia that is the hallmark of type 2 diabetes mellitus (T2DM) with minimal risk of hypoglycemia. The pharmacophore common to the SGLT2 inhibitors currently in development is a diarylmethane C-glucoside which is discussed in this review. The focus is how this pharmacophore was further modified as inferred from the patents publishing from 2009 to 2011. The emphasis is on the strategy that each group employed to circumvent the constraints imposed by prior art and how the resulting SGLT2 potency and selectivity versus SGLT1 compared with that of the lead clinical compound dapagliflozin. SGLT2 inhibitors offer a new fundamentally different approach for treatment of diabetes. To date, the clinical results suggest that for non-renally impaired patients this class of inhibitors could be safely used at any stage of T2DM either alone or in combination with other marketed antidiabetic medications.

  10. A novel oral dual amylin and calcitonin receptor agonist (KBP-042) exerts antiobesity and antidiabetic effects in rats

    DEFF Research Database (Denmark)

    Andreassen, Kim V; Feigh, Michael; Hjuler, Sara T

    2014-01-01

    -induced obese (DIO) and Zucker diabetic fatty (ZDF) rats. In vitro, KBP-042 demonstrated superior binding affinity and activation of amylin and calcitonin receptors, and ex vivo, KBP-042 exerted inhibitory action on stimulated insulin and glucagon release from isolated islets. In vivo, KBP-042 induced...... a superior and pronounced reduction in food intake in conjunction with a sustained pair-fed corrected weight loss in DIO rats. Concomitantly, KBP-042 improved glucose homeostasis and reduced hyperinsulinemia and hyperleptinemia in conjunction with enhanced insulin sensitivity. In ZDF rats, KBP-042 induced...... antiobesity and antidiabetic efficacy by dual modulation of insulin sensitivity and directly decelerating stress on the pancreatic α- and β-cells. These results could provide the basis for oral KBP-042 as a novel therapeutic agent in type 2 diabetes....

  11. Factors Associated with Treatment Response to Antidiabetic Agents ...

    African Journals Online (AJOL)

    (sitagliptin and metformin) were the only thiazolidinedione, α-glucosidase inhibitor, DPP-4 inhibitor, and combination agents used, respectively, among the study subjects. Use of Concurrent Medications. Statins were the most commonly prescribed concurrent medication, with 70.0% of subjects receiving statins. This was ...

  12. Glycemic control and antidiabetic drugs in type 2 diabetes mellitus patients with renal complications

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    Huri HZ

    2015-08-01

    Full Text Available Hasniza Zaman Huri,1,2 Lay Peng Lim,1 Soo Kun Lim3 1Department of Pharmacy, Faculty of Medicine, University of Malaya, 2Clinical Investigation Centre, University Malaya Medical Centre, 3Renal Unit, Department of Medicine, Faculty of Medicine, University of Malaya, Kuala Lumpur, Malaysia Background: Good glycemic control can delay the progression of kidney diseases in type 2 diabetes mellitus (T2DM patients with renal complications. To date, the association between antidiabetic agents and glycemic control in this specific patient population is not well established.Purpose: This study aimed to identify antidiabetic regimens as well as other factors that associated with glycemic control in T2DM patients with different stages of chronic kidney disease (CKD.Patients and methods: This retrospective, cross-sectional study involved 242 T2DM inpatients and outpatients with renal complications from January 2009 to March 2014 and was conducted in a tertiary teaching hospital in Malaysia. Glycated hemoglobin (A1C was used as main parameter to assess patients’ glycemic status. Patients were classified to have good (A1C <7% or poor glycemic control (A1C ≥7% based on the recommendations of the American Diabetes Association.Results: Majority of the patients presented with CKD stage 4 (43.4%. Approximately 55.4% of patients were categorized to have poor glycemic control. Insulin (57.9% was the most commonly prescribed antidiabetic medication, followed by sulfonylureas (43%. Of all antidiabetic regimens, sulfonylureas monotherapy (P<0.001, insulin therapy (P=0.005, and combination of biguanides with insulin (P=0.038 were found to be significantly associated with glycemic control. Other factors including duration of T2DM (P=0.004, comorbidities such as anemia (P=0.024 and retinopathy (P=0.033, concurrent medications such as erythropoietin therapy (P=0.047, a-blockers (P=0.033, and antigouts (P=0.003 were also correlated with A1C.Conclusion: Identification of

  13. Cardiometabolic effects of antidiabetic drugs in non-alcoholic fatty liver disease

    DEFF Research Database (Denmark)

    Rix, Iben; Steen Pedersen, Julie; Storgaard, Heidi

    2018-01-01

    PURPOSE: Non-alcoholic fatty liver disease (NAFLD) affects about 25% of the population worldwide. NAFLD may be viewed as the hepatological manifestation of metabolic syndrome. Patients with metabolic syndrome due to diabetes or obesity have an increased risk of cardiovascular disease....... This narrative review describes cardiometabolic effects of antidiabetic drugs in NAFLD. METHODS: We conducted a systematic search in PubMed and manually scanned bibliographies in trial databases and reference lists in relevant articles. RESULTS: Heart disease is the leading cause of death in NAFLD. Conversely......, NAFLD is an independent cardiovascular risk factor in patients suffering from metabolic syndrome. NAFLD is associated with markers of atherosclerosis, and patients have increased risk of ischaemic heart disease. Additionally, patients with NAFLD have increased risk of cardiac dysfunction and heart...

  14. Comparative effectiveness of oral antidiabetic drugs in preventing cardiovascular mortality and morbidity: A network meta-analysis.

    Directory of Open Access Journals (Sweden)

    Gyeongsil Lee

    Full Text Available In the Guidance for Industry from the Food and Drug Administration in 2008, excess cardiovascular risk should be ruled out in trials of all new antidiabetic drugs; however, relatively few studies have focused on cardiovascular safety with antidiabetic drug use. We aimed to examine mortality and cardiovascular risk using a network meta-analysis. We searched the Medline, Embase, Cochrane, and ClinicalTrials.gov registry databases in March 2016 to identify randomized controlled trials reporting cardiovascular risk with the following oral antidiabetic drugs: metformin, sulfonylureas, thiazolidinedione (TZD, dipeptidyl peptidase-4 (DPP4 inhibitors, and sodium-glucose co-transporter-2 (SGLT2 inhibitors. We assessed the differences in the risks of all-cause mortality, cardiovascular-related mortality, acute coronary syndrome (ACS, and myocardial infarction (MI among antidiabetic drugs with fixed effect models for direct pairwise comparisons and Bayesian network meta-analyses to integrate direct and indirect comparisons. Of the 101,183 patients in 73 randomized controlled trials, 3,434 (3.4% died. The relative risks of all-cause mortality with SGLT2 inhibitor use were 0.68 (95% credible interval: 0.57-0.80, 0.74 (0.49-1.10, 0.63 (0.46-0.87, 0.71 (0.55-0.90, and 0.65 (0.54-0.78, compared with placebo, metformin, sulfonylurea, TZD, and DPP4 inhibitor, respectively. The relative risks of cardiovascular-related mortality with SGLT2 inhibitor use were 0.61 (0.50-0.76, 0.81(0.36-1.90, 0.52(0.31-0.88, 0.66(0.49-0.91, and 0.61(0.48-0.77, compared with placebo, metformin, sulfonylurea, TZD, and DPP4 inhibitor, respectively. The relative risks of ACS with SGLT2 inhibitor use was consistent with that of all-cause mortality. SGLT2 inhibitor use was associated with a lower risk of ACS than the other OADs and placebo. The relative risks of MI with SGLT2 inhibitor use were 0.77 (0.63-0.93 and 0.75 (0.60-0.94, compared with placebo and DPP4 inhibitor, respectively. The

  15. ORGANIZATION OF AVAILABILITY OF THE CIRCULATION OF ANTIDIABETIC MEDICINES BASED ON PHARMACEUTICAL LAW IN UKRAINE

    Directory of Open Access Journals (Sweden)

    Zbrozhek SI

    2016-12-01

    contingent of citizens to timely access to vital antidiabetic drugs in full and the required range. It was also studied the availability of treatment antidiabetic medicines by pharmacoeconomic, forensic and pharmaceutical indicators and found the changes to the average price of antidiabetic drugs for the period from 2012 to 2015 according to changes of the US dollar exchange course, which reduced the availability of antidiabetic drugs for patients with diabetes. In difficult conditions, healthcare financing of urgent issues needs to achieve effective supplement of antidiabetic drugs with optimal use of funds. At the national and regional levels consistently implemented organizational and legal measures to improve the availability of antidiabetic drugs in the healthcare system for patients with diabetes: the development of a system of recovery of insulin; pharmaceutical needs for support from the targeted expenditure of regional budgets; targeted distribution of expenditures among local budgets of administrative units; control over pricing for antidiabetic drugs; optimization of implementation of the statement of the Cabinet of Ministers of Ukraine № 73 "Questions of the realization of the pilot project concerning the introduction of state regulation of prices for insulin" by drafting the amendments thereto. Conclusions. Our studies indicate the need for in-depth reform of the healthcare system by providing subsidies from the state budget of Ukraine, the increase the accessibility of antidiabetic medicines for diabetics.

  16. Evidence of Immunosuppressive and Th2 Immune Polarizing Effects of Antidiabetic Momordica charantia Fruit Juice.

    Science.gov (United States)

    Fachinan, Rufine; Fagninou, Adnette; Nekoua, Magloire Pandoua; Amoussa, Abdou Madjid; Adjagba, Marius; Lagnika, Latifou; Lalèyè, Anatole; Moutairou, Kabirou; Yessoufou, Akadiri

    2017-01-01

    The mechanism of action of the antidiabetic capacity of Momordica charantia is still under investigation. Here, we assessed phytochemical compositions, antioxidant activity, and effects of total and filtered fruit and leafy stem juices of Momordica charantia on human T cell proliferation and differentiation through quantification of Th1/Th2 cytokines. In the absence of stimulation, total fruit and leafy stem juices induced significant T cell proliferation. Under PHA stimulation, both juices potentiated plant-induced T cell proliferation. However, the filtered fruit and leafy stem juices significantly inhibited PHA-stimulated T cell proliferation, while neither juice influenced T cell proliferation. Moreover, total and filtered fruit juice increased IL-4 secretion, while total and filtered leafy stem juice enhanced IFN- γ production. Phytochemical screening revealed the presence of tannins, flavonoids, anthocyans, steroids, and triterpenoids in both juices. Alkaloids, quinone derivatives, cardenolides, and cyanogenic derivatives were undetectable. The saponins present in total juices were undetectable after filtration. Moreover, both juices had appreciable antioxidant capacity. Our study supports the type 1 antidiabetic effect of filtered fruit juice of M. charantia which may be related to its immunosuppressive and T-helper 2 cell inducing capacities. Due to their immune-stimulatory activities and their ability to increase T-helper 1 cell cytokines, total fruit and leafy stem juices may serve in the treatment of immunodeficiency and certain infections.

  17. Isolated flavonoids from Ficus racemosa stem bark possess antidiabetic, hypolipidemic and protective effects in albino Wistar rats.

    Science.gov (United States)

    Keshari, Amit K; Kumar, Ghanendra; Kushwaha, Priya S; Bhardwaj, Monika; Kumar, Pranesh; Rawat, Atul; Kumar, Dinesh; Prakash, Anand; Ghosh, Balaram; Saha, Sudipta

    2016-04-02

    Ficus racemosa (FR) has been used for thousands of years in Ayurvedic system of medicine in India and is closely associated with prevention, treatment and cure of various human ailments like obesity and diabetes. It is popularly known as gular. A vast and wide range of chemical compounds like polyphenols, friedelane-type triterpenes, norfriedelane type triterpene, eudesmane-type sesquiterpene including various glycosides had been isolated from this plant. However, no detail studies related to isolation of flavonoids has been reported previously with their antidiabetic, hypolipidemic and toxicological consequences. The present study was undertaken to evaluate antidiabetic, hypolipidemic and toxicological assessments of flavonoids isolated from Ficus racemosa (FR) stem bark. We isolated four flavonoids from stem bark of FR and structures were confirmed by Infrared spectroscopy (IR), Nuclear Magnetic Resonance (NMR) (both 1D and 2D), mass spectroscopy (MS). Later, these flavonoids were administered to streptozotocin (STZ) rats once in a day for a period of seven days at 100mg/kg dose. We measured blood glucose level and body weight changes at different days (1st, 3rd, 5th and 7th days). Serum lipid profiles were also estimated to investigate the hypolipidemic potential of flavonoids in the similar experiment. Various oxidative stress parameters in pancreas and liver and hepatic biomarker enzymes in plasma were also determined to investigate the toxicity potential of isolated flavonoids. Finally, we performed docking studies to find out the mechanism of action. Our results collectively suggested that four flavonoids reduced blood glucose level and restored body weight, signifying antidiabetic action. There were reduction of other lipid profile parameters and increase of high density lipoprotein (HDL) during administration of flavonoids, also signifying hypolipidemic action. Various oxidative stress biomarkers and hepatic enzymes levels were also normalized with respect

  18. Pharmacogenetics of Anti-Diabetes Drugs

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    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.

  19. Identification of novel human dipeptidyl peptidase-IV inhibitors of natural origin (Part II: in silico prediction in antidiabetic extracts.

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    Laura Guasch

    Full Text Available BACKGROUND: Natural extracts play an important role in traditional medicines for the treatment of diabetes mellitus and are also an essential resource for new drug discovery. Dipeptidyl peptidase IV (DPP-IV inhibitors are potential candidates for the treatment of type 2 diabetes mellitus, and the effectiveness of certain antidiabetic extracts of natural origin could be, at least partially, explained by the inhibition of DPP-IV. METHODOLOGY/PRINCIPAL FINDINGS: Using an initial set of 29,779 natural products that are annotated with their natural source and an experimentally validated virtual screening procedure previously developed in our lab (Guasch et al.; 2012 [1], we have predicted 12 potential DPP-IV inhibitors from 12 different plant extracts that are known to have antidiabetic activity. Seven of these molecules are identical or similar to molecules with described antidiabetic activity (although their role as DPP-IV inhibitors has not been suggested as an explanation for their bioactivity. Therefore, it is plausible that these 12 molecules could be responsible, at least in part, for the antidiabetic activity of these extracts through their inhibitory effect on DPP-IV. In addition, we also identified as potential DPP-IV inhibitors 6 molecules from 6 different plants with no described antidiabetic activity but that share the same genus as plants with known antidiabetic properties. Moreover, none of the 18 molecules that we predicted as DPP-IV inhibitors exhibits chemical similarity with a group of 2,342 known DPP-IV inhibitors. CONCLUSIONS/SIGNIFICANCE: Our study identified 18 potential DPP-IV inhibitors in 18 different plant extracts (12 of these plants have known antidiabetic properties, whereas, for the remaining 6, antidiabetic activity has been reported for other plant species from the same genus. Moreover, none of the 18 molecules exhibits chemical similarity with a large group of known DPP-IV inhibitors.

  20. Antidiabetic potential of Conocarpus lancifolius

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    Malik Saadullah

    2014-06-01

    Full Text Available The antidiabetic activity of Conocarpus lancifolius extract was investigated in vitro, as alpha glucosidase inhibition and in vivo as alloxan induced diabetic rabbits with other biochemical parameters (LDL, HDL, SGPT, SGOT, cretinine, urea and triglyceride. Alpha-glucosidase inhibition activity was performed by using acorbose as standred. Methanolic extract show alpha-glucosidase inhibition activity. The dose of 200 mg/kg body weight significantly (p<0.05 decreases the blood glucose level, plasma total cholesterol, triglycerides and LDL in treated rabbits as compared to diabetic rabbits. This dose significantly increased the level of HDL in treated group. The activity of SGOT and SGPT also significantly (p<0.05 decreased in treated diabetic rabbits. Phytochemical studies show the presence of glycosides, tannins, saponins and terpenoids. The antidiabetic potential is may be due to its saponin contents.

  1. [Glucokinase and glucokinase regulatory proteins as molecular targets for novel antidiabetic drugs].

    Science.gov (United States)

    Rubtsov, P M; Igudin, E L; Tiulpakov, A N

    2015-01-01

    The impairment of glucose homeostasis leads to hyperglycemia and type-2 diabetes mellitus. Glucokinase (GK), an enzyme that catalyzes the conversion of glucose to glucose-6-phosphate in pancreatic ß-cells, liver hepatocytes, specific hypothalamic neurons, and intestine enterocytes, is a key regulator of glucose homeostasis. In hepatocytes, GK controls the glucose uptake and glycogen synthesis and inhibits the glucose synthesis via the gluconeogenesis pathway. Glucokinase regulatory protein (GKRP) synthesized in hepatocytes acts as an endogenous GK inhibitor. During fasting, GKRP binds GK, inactivates it, and transports it into the cell nucleus, thus isolating it from the hepatocyte carbohydrate metabolism. In the beginning of the 2000s, the research was mainly focused on the development and trials of the small molecule GK activators as potential antidiabetic glucose-lowering drugs. However, the use of such substances increased the risk of hypoglycemia, and clinical studies of most synthetic GK activators are currently discontinued. Allosteric inhibitors of the GK-GKRP interaction are coming as alternative agents increasing the GK activity that can substitute GKA. In this review, we discuss the recent advances and the current state of art in the development of potential antidiabetic drugs targeted to GK as a key regulator of glucose homeostasis.

  2. Identification of PPARgamma partial agonists of natural origin (II: in silico prediction in natural extracts with known antidiabetic activity.

    Directory of Open Access Journals (Sweden)

    Laura Guasch

    Full Text Available BACKGROUND: Natural extracts have played an important role in the prevention and treatment of diseases and are important sources for drug discovery. However, to be effectively used in these processes, natural extracts must be characterized through the identification of their active compounds and their modes of action. METHODOLOGY/PRINCIPAL FINDINGS: From an initial set of 29,779 natural products that are annotated with their natural source and using a previously developed virtual screening procedure (carefully validated experimentally, we have predicted as potential peroxisome proliferators-activated receptor gamma (PPARγ partial agonists 12 molecules from 11 extracts known to have antidiabetic activity. Six of these molecules are similar to molecules with described antidiabetic activity but whose mechanism of action is unknown. Therefore, it is plausible that these 12 molecules could be the bioactive molecules responsible, at least in part, for the antidiabetic activity of the extracts containing them. In addition, we have also identified as potential PPARγ partial agonists 10 molecules from 16 plants with undescribed antidiabetic activity but that are related (i.e., they are from the same genus to plants with known antidiabetic properties. None of the 22 molecules that we predict as PPARγ partial agonists show chemical similarity with a group of 211 known PPARγ partial agonists obtained from the literature. CONCLUSIONS/SIGNIFICANCE: Our results provide a new hypothesis about the active molecules of natural extracts with antidiabetic properties and their mode of action. We also suggest plants with undescribed antidiabetic activity that may contain PPARγ partial agonists. These plants represent a new source of potential antidiabetic extracts. Consequently, our work opens the door to the discovery of new antidiabetic extracts and molecules that can be of use, for instance, in the design of new antidiabetic drugs or functional foods focused

  3. Effectiveness and content analysis of interventions to enhance oral antidiabetic drug adherence in adults with type 2 diabetes: systematic review and meta-analysis

    NARCIS (Netherlands)

    Vignon Zomahoun, H.T.; de Bruin, M.; Guillaumie, L.; Moisan, J.; Grégoire, J.P.; Pérez, N.; Vézina-Im, L.A.; Guénette, L.

    2015-01-01

    Objectives To estimate the pooled effect size of oral antidiabetic drug (OAD) adherence-enhancing interventions and to explore which of the behavior change techniques (BCTs) applied in the intervention groups modified this pooled intervention effect size. Methods We searched relevant studies

  4. Abolishing coinsurance for oral antihyperglycemic agents: effects on social insurance budgets.

    Science.gov (United States)

    Athanasakis, Kostas; Skroumpelos, Anastasis G; Tsiantou, Vassiliki; Milona, Katerina; Kyriopoulos, John

    2011-02-01

    To assess the effects of abolishing coinsurance for oral antihyperglycemic agents (OAAs) on the social insurance fund budget in Greece. A mathematical model estimating the effect of a decrease in patient coinsurance rate on demand for and adherence to OAAs and the subsequent clinical and economic outcomes. Price elasticity of demand for antidiabetic agents was used to estimate quantity demand change as a result of a coinsurance rate decrease and consequent increased adherence to OAAs. Given the inverse relationship between OAA adherence and glycated hemoglobin (A1C) level, the model calculated the mean decrease in A1C level and associated cost savings based on the cost difference between patients with controlled versus uncontrolled A1C levels. A decrease in patient coinsurance rate from 25% to 0% led to an incremental increase in OAA adherence of 30.5% and a mean decrease in A1C level of 0.6%. The A1C level decrease contributed to an 18.5% "shift" of uncontrolled patients to controlled A1C levels (<7%), which in economic terms translated into savings of 324 euro per patient over a 3-year period and an investment return rate of 122.8%. A series of 1-way and 2-way sensitivity analyses were conducted to verify the robustness and validity of the outcomes. The introduction of policies aimed at abolishing coinsurance for OAAs can result in improved patient outcomes and cost savings for the healthcare system.

  5. Anti-diabetic potential of aerial parts of Galium tricornutum (Dandy ...

    African Journals Online (AJOL)

    Anti-diabetic potential of aerial parts of Galium tricornutum (Dandy) Rubiaceae. ... In addition, the effect of the extract on fasting blood glucose, as well as serum lipid profile, urea, creatinine, alanine transaminase (ALT), aspartate transaminase (AST), bilirubin, alkaline phosphatase (ALP) and protein were investigated in ...

  6. Comparison of the Chemical Profiles and Antioxidant and Antidiabetic Activities of Extracts from Two Ganoderma Species (Agaricomycetes).

    Science.gov (United States)

    Tang, Xiaoqing; Cai, Weixi; Xu, Baojun

    2016-01-01

    The objective of this study was to compare the mycochemical profiles, antioxidant activities, and antidiabetic effects of 2 species of genus Ganoderma, the red lingzhi (G. lucidum) and purple lingzhi (G. sinense) mushrooms. In Chinese medicinal practice, hot water and ethanol are used as solvents to extract samples. In this study, a total of 4 extracts (ethanol and hot water extracts from G. lucidum and G. sinense) were prepared for further assays. Hot water extracts presented much higher values for total phenolic content and ferric-reducing antioxidant power than the ethanol extracts. Ethanol (70%) extract of G. lucidum had the strongest α-glycosidase inhibitory capacity, but the lingzhi polysaccharides showed no inhibitory effect. It also had the largest amount of total ganoderic acids. The results indicated that ethanol extracts from both G. lucidum and G. sinense showed better antidiabetic effects than the hot water extracts. Ganoderic acids, rather than polysaccharides, may contribute the antidiabetic effects of both the Ganoderma species.

  7. Phyto-metals screening of selected anti-diabetic herbs and infused concoctions

    Directory of Open Access Journals (Sweden)

    Olanrewaju O. Olujimi

    2017-10-01

    Conclusions: The study thus shows that the herbs and concoctions are safe from the heavy metals considered. However, right dosage of the anti-diabetic concoctions should always be considered to prevent possible chronic side effects from bio-accumulation of heavy metals.

  8. Assessment of antidiabetic potential of Cynodon dactylon extract in streptozotocin diabetic rats.

    Science.gov (United States)

    Singh, Santosh Kumar; Kesari, Achyut Narayan; Gupta, Rajesh Kumar; Jaiswal, Dolly; Watal, Geeta

    2007-11-01

    This study was undertaken to investigate the hypoglycemic and antidiabetic effect of single and repeated oral administration of the aqueous extract of Cynodon dactylon (Family: Poaceae) in normal and streptozotocin induced diabetic rats, respectively. The effect of repeated oral administration of aqueous extract on serum lipid profile in diabetic rats was also examined. A range of doses, viz. 250, 500 and 1000mg/kg bw of aqueous extract of Cynodon dactylon were evaluated and the dose of 500mg/kg was identified as the most effective dose. It lowers blood glucose level around 31% after 4h of administration in normal rats. The same dose of 500mg/kg produced a fall of 23% in blood glucose level within 1h during glucose tolerance test (GTT) of mild diabetic rats. This dose has almost similar effect as that of standard drug tolbutamide (250mg/kg bw). Severely diabetic rats were also treated daily with 500mg/kg bw for 14 days and a significant reduction of 59% was observed in fasting blood glucose level. A reduction in the urine sugar level and increase in body weight of severe diabetic rats were additional corroborating factors for its antidiabetic potential. Total cholesterol (TC), low density lipoprotein (LDL) and triglyceride (TG) levels were decreased by 35, 77 and 29%, respectively, in severely diabetic rats whereas, cardioprotective, high density lipoprotein (HDL) was increased by 18%. These results clearly indicate that aqueous extract of Cynodon dactylon has high antidiabetic potential along with significant hypoglycemic and hypolipidemic effects.

  9. Antidiabetic and Antioxidant Activity of Scoparia dulcis Linn.

    Science.gov (United States)

    Mishra, M R; Mishra, A; Pradhan, D K; Panda, A K; Behera, R K; Jha, S

    2013-09-01

    The hypoglycaemic activity of methanol extract of Scoparia dulcis was performed on both in vitro and in vivo models along with determination of total extractable polyphenol. Methanol extract of Scoparia dulcis contains 4.9% and water extract contains 3.2% of total extractable polyphenol. The antioxidant activity showed very promising result in both the tested methods that is 2,2-diphenyl-1-picrylhydrazyl and ferric ion reducing capacity. The antioxidant activity is directly correlated to the antidiabetic potential of drug. The two enzymes (amylase and glycosidase) found in intestine are responsible for the increasing postprandial glucose in body. In vitro model was performed on these enzymes and the results showed that methanol extract of Scoparia dulcis was effective to check the postprandial glucose level. The in vivo hypoglycaemic activity of methanol extract of Scoparia dulcis was performed on streptozotocin-induced diabetes mellitus showed significant inhibition of blood glucose level as compared to control and similar to that of standard glibenclamide. The overall data potentiates the traditional value of Scoparia dulcis as an antidiabetic drug.

  10. Isolation of Antidiabetic Principle from Fruit Rinds of Punica granatum

    Directory of Open Access Journals (Sweden)

    Vishal Jain

    2012-01-01

    Full Text Available Present study was aimed to isolate and evaluate the antidiabetic activity of phytoconstituents from fruit rinds of Punica granatum. With the above objectives Valoneic acid dilactone (VAD was isolated from methanolic fruit rind extracts of Punica granatum (MEPG and confirmed by 1H-NMR, 13C-NMR, and mass spectral data. Antidiabetic activity was evaluated by Aldose reductase, α-amylase and PTP1B inhibition assays in in vitro and Alloxan-induced diabetes in rats was used as an in vivo model. In bioactivity studies, MEPG and VAD have showed potent antidiabetic activity in α-amylase, aldose reductase, and PTP1B inhibition assays with IC50 values of 1.02, 2.050, 26.25 μg/mL and 0.284, 0.788, 12.41 μg/mL, respectively. Furthermore, in alloxan-induced diabetes model MEPG (200 and 400 mg/kg, p.o. and VAD (10, 25, and 50 mg/kg, p.o. have showed significant and dose dependent antidiabetic activity by maintaining the blood glucose levels within the normal limits. Inline with the biochemical findings histopathology of MEPG (200 and 400 mg/kg, p.o., VAD (10, 25, and 50 mg/kg, p.o., and glibenclamide (10 mg/kg, p.o. treated animals showed significant protection against alloxan-induced pancreatic tissue damage. These findings suggest that MEPG and VAD possess significant antidiabetic activity in both in vitro and in vivo models.

  11. Isolation of Antidiabetic Principle from Fruit Rinds of Punica granatum

    Science.gov (United States)

    Jain, Vishal; Viswanatha, G. L.; Manohar, D.; Shivaprasad, H. N.

    2012-01-01

    Present study was aimed to isolate and evaluate the antidiabetic activity of phytoconstituents from fruit rinds of Punica granatum. With the above objectives Valoneic acid dilactone (VAD) was isolated from methanolic fruit rind extracts of Punica granatum (MEPG) and confirmed by 1H-NMR, 13C-NMR, and mass spectral data. Antidiabetic activity was evaluated by Aldose reductase, α-amylase and PTP1B inhibition assays in in vitro and Alloxan-induced diabetes in rats was used as an in vivo model. In bioactivity studies, MEPG and VAD have showed potent antidiabetic activity in α-amylase, aldose reductase, and PTP1B inhibition assays with IC50 values of 1.02, 2.050, 26.25 μg/mL and 0.284, 0.788, 12.41 μg/mL, respectively. Furthermore, in alloxan-induced diabetes model MEPG (200 and 400 mg/kg, p.o.) and VAD (10, 25, and 50 mg/kg, p.o.) have showed significant and dose dependent antidiabetic activity by maintaining the blood glucose levels within the normal limits. Inline with the biochemical findings histopathology of MEPG (200 and 400 mg/kg, p.o.), VAD (10, 25, and 50 mg/kg, p.o.), and glibenclamide (10 mg/kg, p.o.) treated animals showed significant protection against alloxan-induced pancreatic tissue damage. These findings suggest that MEPG and VAD possess significant antidiabetic activity in both in vitro and in vivo models. PMID:22919408

  12. Antidiabetic and Antihyperlipidemic Activity of Cucurbita maxima Duchense (Pumpkin) Seeds on Streptozotocin Induced Diabetic Rats

    OpenAIRE

    Ashish K. Sharma; Ashok Sharma

    2013-01-01

    The objective of the present study was to evaluate the antidiabetic and antihyperlipidemic effect of petroleum ether, ethyl acetate and alcohol extract of seeds of Cucurbita maxima for its purported use in diabetes. The antidiabetic and antihyperlipidemic activity of different extracts of Cucurbita maxima seeds was evaluated in wistar albino rats against streptozotocin (50 mg/kg i.p.) at dose of 200 mg/kg p.o. for 21 days. Glibenclamide (500µg/kg) was used as reference drug. Fasting blood g...

  13. Antidiabetic and antihyperlipidemic effects of ethanolic extract of leaves of Punica granatum in alloxan-induced non–insulin-dependent diabetes mellitus albino rats

    Science.gov (United States)

    Das, Swarnamoni; Barman, Sarajita

    2012-01-01

    Objectives: Punica granatum L., (Family: Punicaceae) is used in Indian Unani medicine for treatment of diabetes mellitus. Therefore, the present study was done to evaluate the antidiabetic and antihyperlipidemic effects of ethanolic extract of leaves of P. granatum in alloxan-induced diabetic rats. Materials and Methods: Healthy Wistar albino rats (100-150 g) were divided into four groups of six animals each. Groups A and B received normal saline [(10 ml/kg/day/per oral (p.o.)]; group C received ethanolic extract of leaves of P. granatum (500 mg/kg/p.o.); and group D received glibenclamide (0.5 mg/kg/day/p.o.). The extracts were given for 1 week in all groups. To induce diabetes, alloxan 150 mg/kg, intraperitoneal (i.p.) single dose was administered to groups B, C, and D. Blood glucose and serum lipids [Total Cholesterol (TC), Triglycerides (TG), Low Density Lipoproteins (LDL), and High Density Lipoproteins (HDL)] and the atherogenic index were estimated after one week. For mechanism of antidiabetic action glycogen estimation on the liver, cardiac and skeletal muscle, and intestinal glucose absorption was done. Results: Group B showed a significant (Pgranatum leaves possess significant antidiabetic and antihyperlipidemic activity. PMID:22529479

  14. Anti-diabetic potential of aerial parts of Galium tricornutum (Dandy ...

    African Journals Online (AJOL)

    Purpose: To evaluate the anti-diabetic potential of methanol extract of the aerial parts of Galium tricornutum (Dandy) in diabetic rats. Methods: The methanol extract of the aerial parts of Galium tricornutum was first subjected to acute toxicity studies. Thereafter, the effect of the extract on oral glucose tolerance was determined ...

  15. Capparis spinosa L. aqueous extract evokes antidiabetic effect in streptozotocin-induced diabetic mice

    Directory of Open Access Journals (Sweden)

    Mohamed Eddouks

    2017-02-01

    Full Text Available Objective: As the aqueous extract of Capparis spinosa (CS possess antidiabetic effect, he present study aims to reveal the possible  mechanism of action of CS in diabetic mice.Materials and Methods: Both single and repeated oral administrations of aqueous extract of CS were performed in multi-low dose streptozotocin-induced (MLDS diabetic mice. Euglycemic hyperinsulinemic clamp was used in association with the endogenous glucose production (perfusion rate of 3-3H glucose to evaluate the effect of CS aqueous extract on insulin sensitivity.Results: Our study showed that aqueous extract of CS possess a potent hypoglycaemic activity in MLDS diabetic mice. Furthermore, the analysis perfusion of 3-3H glucose demonstrated  the parallel decrease of basal endogenous glucose production (EGP with the hypoglycaemic activity. EGP was lower in CS-Treated group when compared to the control group (p

  16. The Antidiabetic Drug Metformin Inhibits the Proliferation of Bladder Cancer Cells in Vitro and in Vivo

    Directory of Open Access Journals (Sweden)

    Tao Zhang

    2013-12-01

    Full Text Available Recent studies suggest that metformin, a widely used antidiabetic agent, may reduce cancer risk and improve prognosis of certain malignancies. However, the mechanisms for the anti-cancer effects of metformin remain uncertain. In this study, we investigated the effects of metformin on human bladder cancer cells and the underlying mechanisms. Metformin significantly inhibited the proliferation and colony formation of 5637 and T24 cells in vitro; specifically, metformin induced an apparent cell cycle arrest in G0/G1 phases, accompanied by a strong decrease of cyclin D1, cyclin-dependent kinase 4 (CDK4, E2F1 and an increase of p21waf-1. Further experiments revealed that metformin activated AMP-activated protein kinase (AMPK and suppressed mammalian target of rapamycin (mTOR, the central regulator of protein synthesis and cell growth. Moreover, daily treatment of metformin led to a substantial inhibition of tumor growth in a xenograft model with concomitant decrease in the expression of proliferating cell nuclear antigen (PCNA, cyclin D1 and p-mTOR. The in vitro and in vivo results demonstrate that metformin efficiently suppresses the proliferation of bladder cancer cells and suggest that metformin may be a potential therapeutic agent for the treatment of bladder cancer.

  17. Antidiabetic, hypolipidemic and hepatoprotective effects of Arctium lappa root's hydro-alcoholic extract on nicotinamide-streptozotocin induced type 2 model of diabetes in male mice.

    Science.gov (United States)

    Ahangarpour, Akram; Heidari, Hamid; Oroojan, Ali Akbar; Mirzavandi, Farhang; Nasr Esfehani, Khalil; Dehghan Mohammadi, Zeinab

    2017-01-01

    Arctium lappa (burdock), (A. lappa) root has hypoglycemic and antioxidative effects, and has been used for treatment of diabetes in tradition medicine. This study was conducted to evaluate the antidiabetic and hypolipidemic properties of A. lappa root extract on nicotinamide-streptozotocin (NA-STZ)-induced type2 diabetes in mice. In this investigation, 70 adult male NMRI mice (30-35g) randomly divided into 7 groups (n=10) as follow: 1-control, 2-type 2 diabetic mice, 3-diabetic mice that received glibenclamide (0.25 mg/kg) as an anti-diabetic drug, 4, 5, 6 and 7- diabetic and normal animals that were pre-treated with 200 and 300 mg/kg A. lappa root extract, respectively, for 28 days. Diabetes has been induced by intraperitoneal injection of NA and STZ. Finally, the blood sample was taken and insulin, glucose, SGOT, SGPT, alkaline phosphatase, leptin and lipid levels was evaluated. Induction of diabetes decreased the level of insulin, leptin and high density lipoprotein (HDL) and increased the level of other lipids, glucose, and hepatic enzymes significantly (plappa root extract, at specific doses, has an anti-diabetic effect through its hypolipidemic and insulinotropic properties. Hence, this plant extract may be beneficial in the treatment of diabetes.

  18. Antidiabetic Effects of Aronia melanocarpa and Its Other Therapeutic Properties

    Directory of Open Access Journals (Sweden)

    Ines Banjari

    2017-11-01

    Full Text Available Diabetes is a global pandemic which warrants urgent attention due to its rising prevalence and economic burden. Thus, many alternative therapies are being researched for antidiabetic properties, given the inefficacy of current medicinal treatments. From this perspective, Aronia melanocarpa or black chokeberry has been investigated for its therapeutic properties in many studies, especially for its ability to combat hyperglycemia-induced oxidative stress and the macrovascular complications of diabetes including cardiovascular disease. Though A. melanocarpa is native to the eastern areas of North America, it has been planted extensively in Europe and Asia as well. Several in vivo studies have displayed the antioxidant properties of A. melanocarpa berry juice and plant extract in rat models where oxidative stress markers were observed to have significant reductions. Some of the potent bioactive compounds present in the fruits and other parts of the plant were identified as (−-epicatechin, chlorogenic acid, neochlorogenic acid, and cyanidin-3-galactoside. Overall, A. melanocarpa could be considered a good source of antioxidants which is effective in combating hyperglycemia-induced oxidative stress.

  19. Generic substitution of antidiabetic drugs in the elderly does not affect adherence

    Directory of Open Access Journals (Sweden)

    Francesco Trotta

    2014-12-01

    Full Text Available INTRODUCTION: The possibility that variation in packaging and pill appearance may reduce adherence is a reason for concern, especially for chronic diseases. The objectives of the study were to quantify the extent of switches between generic antidiabetics and to verify whether switching between different products of the same substance affects adherence. MATERIALS AND METHODS: All elderly residents of the Umbria Region who received at least 2 prescriptions of antidiabetics in 2010 and 2011 were included in the study. Switching was defined as the dispensing of two different products of the same substance in a series of two prescriptions. Single and multiple switchers were identified according to the number of switches during 2011. Switching relevant to the three off-patent substances with generic use ≥ 5% (metformin, gliclazide and repaglinide was quantified. The effect of switching on adherence, defined as the proportion of days in 2011 covered by prescriptions (Medication Possession Ratio, MPR, was estimated. RESULTS: Among the 15 964 patients receiving antidiabetics (14.4% of the elderly population 9211 were prescribed at least one of the generic substances. Of these patients, 23.3% experienced a single switch and 15.7% were multiple switchers (61.0% never switched. The proportion of multiple switchers increased with the number of prescriptions, reaching 26% among patients with ≥ 11 prescriptions. MPR was 62%, 62% and 72%, respectively among non-switchers, single and multiple switchers. CONCLUSIONS: In elderly patients treated with antidiabetics, the substitution between branded and unbranded products (as well as between generics of the same substance, did not negatively affect adherence.

  20. Plants used as antidiabetics in popular medicine in Rio Grande do Sul, southern Brazil.

    Science.gov (United States)

    Trojan-Rodrigues, M; Alves, T L S; Soares, G L G; Ritter, M R

    2012-01-06

    Plants are widely as antidiabetics. The study of these plants is essential because many of them may have undesirable effects, such as acute or chronic toxicity; or their use may even delay or discourage the adoption of the proper and effective treatment. The present study surveyed the plant species that are popularly used to treat diabetes mellitus in the state of Rio Grande do Sul in southern Brazil. Sixteen ethnobotanical surveys performed in the state were consulted, and the species used to treat diabetes were listed. For species cited in at least two of the studies, scientific data related to antidiabetic activity were searched in the ISI Knowledge database. The scientific binomial of each species was used as keywords, and data found in review papers were also included. A total of 81 species in 42 families were mentioned; the most important families were Asteraceae and Myrtaceae. Twenty eight species were cited at least twice as being used to treat diabetes in the state. For 11 of these, no scientific data regarding antidiabetic activity could be located. The species most frequently mentioned for use with diabetes were Syzygium cumini (Myrtaceae) and Bauhinia forficata (Fabaceae), in 12 studies each, followed by Sphagneticola trilobata (Asteraceae), in six studies; and Baccharis trimera (Asteraceae), Bidens pilosa (Asteraceae), Cynara scolymus (Asteraceae), and Leandra australis (Melastomataceae) in four studies each. Bauhinia forficata and Syzygium cumini have been studied in more detail for antidiabetic activity. A considerable number of plant species are traditionally used for the treatment of diabetes melitus in the Rio Grande do Sul State. The majority of those plants that have been studied for antidiabetic activity showed promising results, mainly for Bauhinia forficata and Syzygium cumini. However, for most of the plants mentioned, the studies are not sufficient to guarantee the efficacy and safety in the use of these plants in the treatment against

  1. In vitro and in vivo antidiabetic potential of extracts and a furostanol saponin from Balanites aegyptiaca.

    Science.gov (United States)

    Ezzat, Shahira Mohammed; Abdel Motaal, Amira; El Awdan, Sally Abdel Wanees

    2017-12-01

    Balanites aegyptiaca Del. (Zygophyllaceae) fruits are well-known antidiabetic drug in Egyptian folk medicine. Nevertheless, its mechanism of action is still unclear. Searching for the possible mechanisms of action of the plant and identification of its bioactive compounds. A bio-guided protocol based on the evaluation of α-glucosidase (AG) and aldose reductase (AR) inhibitory activities was adopted to isolate the biologically active compounds from the methanol extract (MeEx). An in vivo antidiabetic study was conducted for the active extract, fraction and compound using streptozotocin-induced diabetic male albino Wistar rats at two dose levels (100 and 200 mg/kg.b/wt) for 2 weeks. Three compounds were isolated and identified: a sterol, (1) stigmasterol-3-O-β-d-glucopyranoside; a pregnane glucoside, (2) pregn-5-ene-3β,16β,20(R)-trio1-3-O-β-d-glucopyranoside; a furostanol saponin, (3) 26-(O-β-d-glucopyranosyl)-22-O-methylfurost-5-ene-3β,26-diol-3-O-β-d-glucopyranosyl-(1 → 4)-[α-l-rhamnopyranosyl-(1 → 2)]-β-d-glucopyranoside. Only compound 3 possessed significant AG and AR inhibitory activities (IC 50  = 3.12 ± 0.17 and 1.04 ± 0.02 μg/mL, respectively), while compounds 1 and 2 were inactive. The in vivo antidiabetic study revealed that MeEx and furostanol saponin 3 possessed significant activities at a dose of 200 mg/kg through reducing the fasting plasma glucose level by 46.14% and 51.39%, respectively, as well as reducing the total cholesterol by 24.44% and 31.90%, respectively. Compound 3 also caused increment in insulin and C-peptide levels by 63.56% and 65%, respectively. We presented a scientific base for using Balanites aegyptiaca, and shed the light on one of its saponins, as an antidiabetic agent in fasting and postprandial hyperglycaemia along with the improvement of diabetic complications.

  2. Antidiabetic, hypolipidemic and hepatoprotective effects of Arctium lappa root’s hydro-alcoholic extract on nicotinamide-streptozotocin induced type 2 model of diabetes in male mice

    Science.gov (United States)

    Ahangarpour, Akram; Heidari, Hamid; Oroojan, Ali Akbar; Mirzavandi, Farhang; Nasr Esfehani, Khalil; Dehghan Mohammadi, Zeinab

    2017-01-01

    Objective: Arctium lappa (burdock), (A. lappa) root has hypoglycemic and antioxidative effects, and has been used for treatment of diabetes in tradition medicine. This study was conducted to evaluate the antidiabetic and hypolipidemic properties of A. lappa root extract on nicotinamide-streptozotocin (NA-STZ)-induced type2 diabetes in mice. Materials and Methods: In this investigation, 70 adult male NMRI mice (30-35g) randomly divided into 7 groups (n=10) as follow: 1-control, 2-type 2 diabetic mice, 3-diabetic mice that received glibenclamide (0.25 mg/kg) as an anti-diabetic drug, 4, 5, 6 and 7- diabetic and normal animals that were pre-treated with 200 and 300 mg/kg A. lappa root extract, respectively, for 28 days. Diabetes has been induced by intraperitoneal injection of NA and STZ. Finally, the blood sample was taken and insulin, glucose, SGOT, SGPT, alkaline phosphatase, leptin and lipid levels was evaluated. Results: Induction of diabetes decreased the level of insulin, leptin and high density lipoprotein (HDL) and increased the level of other lipids, glucose, and hepatic enzymes significantly (plappa root extract, at specific doses, has an anti-diabetic effect through its hypolipidemic and insulinotropic properties. Hence, this plant extract may be beneficial in the treatment of diabetes. PMID:28348972

  3. Anti-Diabetic, Anti-Oxidant and Anti-Hyperlipidemic Activities of Flavonoids from Corn Silk on STZ-Induced Diabetic Mice.

    Science.gov (United States)

    Zhang, Yan; Wu, Liying; Ma, Zhongsu; Cheng, Jia; Liu, Jingbo

    2015-12-23

    Corn silk is a well-known ingredient frequently used in traditional Chinese herbal medicines. This study was designed to evaluate the anti-diabetic, anti-oxidant and anti-hyperlipidemic activities of crude flavonoids extracted from corn silk (CSFs) on streptozotocin (STZ)-induced diabetic mice. The results revealed that treatment with 300 mg/kg or 500 mg/kg of CSFs significantly reduced the body weight loss, water consumption, and especially the blood glucose (BG) concentration of diabetic mice, which indicated their potential anti-diabetic activities. Serum total superoxide dismutase (SOD) and malondialdehyde (MDA) assays were also performed to evaluate the anti-oxidant effects. Besides, several serum lipid values including total cholesterol (TC), triacylglycerol (TG), low density lipoprotein cholesterol (LDL-C) were reduced and the high density lipoprotein cholesterol level (HDL-C) was increased. The anti-diabetic, anti-oxidant and anti-hyperlipidemic effect of the CSFs suggest a potential therapeutic treatment for diabetic conditions.

  4. Antidiabetic effects of Mangifera indica Kernel Flour?supplemented diet in streptozotocin?induced type 2 diabetes in rats

    OpenAIRE

    Irondi, Emmanuel A.; Oboh, Ganiyu; Akindahunsi, Afolabi A.

    2016-01-01

    Abstract Our previous report showed that Mangifera indica kernel flour (MIKF) is a rich source of pharmacologically important flavonoids and phenolic acids; and that its methanolic extract inhibits some key enzymes linked to the pathology and complications of type 2 diabetes (T2D) in vitro. Hence, this study evaluated the antidiabetic effects of 10% and 20% MIKF?supplemented diets in T2D in rats. T2D was induced in rats using a high?fat diet (HFD), low?dose streptozotocin (HFD/STZ) model, by ...

  5. Antidiabetic medication adherence and associated factors among ...

    African Journals Online (AJOL)

    Godfrey Mutashambara Rwegerera

    2017-03-06

    Mar 6, 2017 ... tive of the study was to determine current antidiabetic medication adherence in ...... A systematic review of adherence with medications for diabetes. .... Pascal IGU, Ofoedu JN, Uchenna NP, Nkwa AA, Uchamma GUE.

  6. Thiazolidinediones are associated with a decreased risk of atrial fibrillation compared with other antidiabetic treatment

    DEFF Research Database (Denmark)

    Pallisgaard, Jannik Langtved; Lindhardt, Tommi Bo; Staerk, Laila

    2017-01-01

    sensitizer that also has anti-inflammatory effects, which might decrease the risk of AF compared with other antidiabetic drugs. We used data from the Danish nationwide registries to study 108 624 patients with diabetes and without prior AF who were treated with metformin or sulfonylurea as first-line drugs...... drugs. The decreased risk of AF remained significant after adjusting for age, sex, and comorbidities with a hazard ratio (95% CI) of 0.76 (0.57-1.00), P = 0.047 associated with TZD treatment compared with other antidiabetic drugs. CONCLUSION: Use of a TZD to treat diabetes was associated with reduced...

  7. POTENTIAL APPLICATIONS OF SOS-GFP BIOSENSOR TO IN VITRO RAPID SCREENING OF CYTOTOXIC AND GENOTOXIC EFFECT OF ANTICANCER AND ANTIDIABETIC PHARMACIST RESIDUES IN SURFACE WATER

    Directory of Open Access Journals (Sweden)

    Marzena Matejczyk

    2014-12-01

    Full Text Available Escherichia coli K-12 GFP-based bacterial biosensors allowed the detection of cytotoxic and genotoxic effect of anticancer drug– cyclophosphamide and antidiabetic drug – metformin in PBS buffer and surface water. Experimental data indicated that recA::gfpmut2 genetic system was sensitive to drugs and drugs mixture applied in experiment. RecA promoter was a good bioindicator in cytotoxic and genotoxic effect screening of cyclophosphamide, metformin and the mixture of the both drugs in PBS buffer and surface water. The results indicated that E. coli K-12 recA::gfp mut2 strain could be potentially useful for first-step screening of cytotoxic and genotoxic effect of anticancer and antidiabetic pharmacist residues in water. Next steps in research will include more experimental analysis to validate recA::gfpmut2 genetic system in E. coli K-12 on different anticancer drugs.

  8. Biomolecular Characterization of Putative Antidiabetic Herbal Extracts

    Science.gov (United States)

    Stadlbauer, Verena; Haselgrübler, Renate; Lanzerstorfer, Peter; Plochberger, Birgit; Borgmann, Daniela; Jacak, Jaroslaw; Winkler, Stephan M.; Schröder, Klaus; Höglinger, Otmar; Weghuber, Julian

    2016-01-01

    Induction of GLUT4 translocation in the absence of insulin is considered a key concept to decrease elevated blood glucose levels in diabetics. Due to the lack of pharmaceuticals that specifically increase the uptake of glucose from the blood circuit, application of natural compounds might be an alternative strategy. However, the effects and mechanisms of action remain unknown for many of those substances. For this study we investigated extracts prepared from seven different plants, which have been reported to exhibit anti-diabetic effects, for their GLUT4 translocation inducing properties. Quantitation of GLUT4 translocation was determined by total internal reflection fluorescence (TIRF) microscopy in insulin sensitive CHO-K1 cells and adipocytes. Two extracts prepared from purslane (Portulaca oleracea) and tindora (Coccinia grandis) were found to induce GLUT4 translocation, accompanied by an increase of intracellular glucose concentrations. Our results indicate that the PI3K pathway is mainly responsible for the respective translocation process. Atomic force microscopy was used to prove complete plasma membrane insertion. Furthermore, this approach suggested a compound mediated distribution of GLUT4 molecules in the plasma membrane similar to insulin stimulated conditions. Utilizing a fluorescent actin marker, TIRF measurements indicated an impact of purslane and tindora on actin remodeling as observed in insulin treated cells. Finally, in-ovo experiments suggested a significant reduction of blood glucose levels under tindora and purslane treated conditions in a living organism. In conclusion, this study confirms the anti-diabetic properties of tindora and purslane, which stimulate GLUT4 translocation in an insulin-like manner. PMID:26820984

  9. Cinnamomum zeylanicum (Ceylon cinnamon) as a potential pharmaceutical agent for type-2 diabetes mellitus: study protocol for a randomized controlled trial

    OpenAIRE

    Ranasinghe, Priyanga; Galappaththy, Priyadarshani; Constantine, Godwin Roger; Jayawardena, Ranil; Weeratunga, Hasitha Dhananjaya; Premakumara, Sirimal; Katulanda, Prasad

    2017-01-01

    Background Previous studies have explored the anti-diabetic effects of Cinnamomum cassia extract in vivo and in vitro. However, there are no studies at present exploring the effects of the indigenous species of Sri Lankan cinnamon (Cinnamomum zeylanicum) in patients with diabetes mellitus. The present study aims to evaluate the potential effects of Cinnamomum zeylanicum extract as a pharmaceutical agent in patients with type-2 diabetes mellitus. Methods/design The study will be conducted as a...

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

    Directory of Open Access Journals (Sweden)

    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.

  11. Phyto-metals screening of selected anti-diabetic herbs and infused concoctions

    OpenAIRE

    Olanrewaju O. Olujimi; Olusegun N. Onifade; Adeleke T. Towolawi; Temilade F. Akinhanmi; Adeniyi A. Afolabi; Kabir A. Olanite

    2017-01-01

    Objective: To determine the levels of some selected heavy metals in both the selected anti-diabetic herbal plants and infused concoctions for diabetes treatment. Methods: Ten anti-diabetic plant samples: pawpaw leaves (Carica papaya), bitter melon leaves (Momordica charantia), holy basil leaves (Ocimum sanctum), bitter leaf (Vernonia amygdalina), ginger rhizome (Zingiber officinale), garlic (Allium sativum), African red pepper fruits (Capsicum frutescens), negro pepper grain (Xylopia aethi...

  12. Anti-Diabetic, Anti-Oxidant and Anti-Hyperlipidemic Activities of Flavonoids from Corn Silk on STZ-Induced Diabetic Mice

    Directory of Open Access Journals (Sweden)

    Yan Zhang

    2015-12-01

    Full Text Available Corn silk is a well-known ingredient frequently used in traditional Chinese herbal medicines. This study was designed to evaluate the anti-diabetic, anti-oxidant and anti-hyperlipidemic activities of crude flavonoids extracted from corn silk (CSFs on streptozotocin (STZ-induced diabetic mice. The results revealed that treatment with 300 mg/kg or 500 mg/kg of CSFs significantly reduced the body weight loss, water consumption, and especially the blood glucose (BG concentration of diabetic mice, which indicated their potential anti-diabetic activities. Serum total superoxide dismutase (SOD and malondialdehyde (MDA assays were also performed to evaluate the anti-oxidant effects. Besides, several serum lipid values including total cholesterol (TC, triacylglycerol (TG, low density lipoprotein cholesterol (LDL-C were reduced and the high density lipoprotein cholesterol level (HDL-C was increased. The anti-diabetic, anti-oxidant and anti-hyperlipidemic effect of the CSFs suggest a potential therapeutic treatment for diabetic conditions.

  13. Antidiabetic and Antioxidant Effects and Phytochemicals of Mulberry Fruit (Morus alba L.) Polyphenol Enhanced Extract

    Science.gov (United States)

    Wang, Yihai; Xiang, Limin; Wang, Chunhua; Tang, Chao; He, Xiangjiu

    2013-01-01

    The antidiabetic and antioxidant activities of the ethyl acetate-soluble extract (MFE) of mulberry fruit (Morus alba L.) were investigated. In vitro, MFE showed potent α-glucosidase inhibitory activity and radical-scavenging activities against DPPH and superoxide anion radicals. In vivo, MFE could significantly decrease fasting blood glucose (FBG) and glycosylated serum protein (GSP), and increase antioxidant enzymatic activities (SOD, CAT, GSH-Px) in streptozotocin (STZ)-induced diabetic mice. Bioactivity-guided fractionation of the MFE led to the isolation of 25 phenolic compounds, and their structures were identified on the basis of MS and NMR data. All the 25 compounds were isolated from mulberry fruit for the first time. Also, the α-glucosidase inhibitory activity and antioxidant activity of the phenolics were evaluated. Potent α-glucosidase inhibitory and radical-scavenging activities of these phenolics suggested that they may be partially responsible for the antidiabetic and antioxidant activities of mulberry fruit. PMID:23936259

  14. Antidiabetic and antioxidant effects and phytochemicals of mulberry fruit (Morus alba L. polyphenol enhanced extract.

    Directory of Open Access Journals (Sweden)

    Yihai Wang

    Full Text Available The antidiabetic and antioxidant activities of the ethyl acetate-soluble extract (MFE of mulberry fruit (Morus alba L. were investigated. In vitro, MFE showed potent α-glucosidase inhibitory activity and radical-scavenging activities against DPPH and superoxide anion radicals. In vivo, MFE could significantly decrease fasting blood glucose (FBG and glycosylated serum protein (GSP, and increase antioxidant enzymatic activities (SOD, CAT, GSH-Px in streptozotocin (STZ-induced diabetic mice. Bioactivity-guided fractionation of the MFE led to the isolation of 25 phenolic compounds, and their structures were identified on the basis of MS and NMR data. All the 25 compounds were isolated from mulberry fruit for the first time. Also, the α-glucosidase inhibitory activity and antioxidant activity of the phenolics were evaluated. Potent α-glucosidase inhibitory and radical-scavenging activities of these phenolics suggested that they may be partially responsible for the antidiabetic and antioxidant activities of mulberry fruit.

  15. Anti-Diabetic Potential of the Leaves of Anisomeles malabarica in Streptozotocin Induced Diabetic Rats

    Directory of Open Access Journals (Sweden)

    Peddanna Kotha

    2017-10-01

    Full Text Available Background/Aims: Diabetes mellitus is a pandemic metabolic disorder that is affecting a majority of populations in recent years. There is a requirement for new drugs that are safer and cheaper due to the side effects associated with the available medications. Methods: We investigated the anti-diabetic activity of leaves of Anisomeles malabarica following bioactivity guided fractionation. The different solvent (hexane, ethyl acetate, methanol and water extracts of A. malabarica leaves were used in acute treatment studies to evaluate and identify the active fraction. The ethyl acetate extract was subjected to further fractionation using silica gel column chromatography and the compounds were identified by LC-SRM/MS and GC-MS. Additional chronic treatment studies were carried out using this active fraction (AMAF for 30 days in experimental diabetic rats. Fasting blood glucose (FBG, glycosylated hemoglobin (HbA1c, plasma insulin levels and glucose tolerance were measured along with insulin resistance/sensitivity indicators (HOMA-IR, HOMA-β and QUICKI to assess the beneficial effects of A. malabarica in the management of diabetes mellitus. Results: Among the different solvent extracts tested, ethyl acetate extract showed maximum (66% anti-hyperglycemic activity. The hexane and ethyl acetate (1: 1 fraction that has maximum anti-diabetic activity was identified as active fraction of A. malabarica (AMAF. The FBG, HbA1c, plasma insulin levels and insulin sensitivity/resistance indicators such as glucose tolerance, HOMA-IR, HOMA-β and QUICKI were significantly improved to near normal in diabetic rats treated with AMAF. Further, we identified key flavonoids and fatty acids as the anti-diabetic active principles from the AMAF of A. malabarica leaves. Conclusion: The results of our study suggest that Anisomeles malabarica has potential anti-diabetic activity in STZ induced diabetic rats.

  16. Validation of the antidiabetic effects of Vernonia amygdalina delile leaf fractions in fortified diet-fed streptozotocin-treated rat model of type-2 diabetes

    Directory of Open Access Journals (Sweden)

    Stanley Irobekhian Reuben Okoduwa

    2017-01-01

    Full Text Available Background: Vernonia amygdalina (VA is used in the traditional management of diabetes in Nigeria. Previous scientific verification of VA is on Type-1 diabetes model, in spite of the continuous increase in Type-2 diabetes (T2D among adults. This study aimed to validate the antidiabetic effects of VA leaf fraction (VALF in a unique T2D rat model. Materials and Methods: Methanol crude extract of VA leaf was fractionated with solvents of increasing order of polarity (n-hexane, chloroform, ethyl-acetate, n- butanol and water. The antidiabetic activities of the fractions were evaluated in vivo in T2D model rats. Albino Wistar rats were induced with T2D and treated with the VALF. Several T2D-related parameters were measured. Results: T2D rats showed significant increase in serum levels of fasting blood glucose (FBG, liver and kidney biomarkers. At 28-day post-oral treatment with the VALF, FBG levels were significantly (P < 0.05 reduced (n- hexane [29.3%], chloroform [66.7%], ethyl acetate [36.2%], n- butanol [45.59%] and aqueous [39.3%]. The glucose tolerance ability was significantly improved in the chloroform fraction (Vernonia amygdalina chloroform fraction [VAc]-treated groups compared to the other fractions-treated group and diabetic control group. Furthermore, the VAc was found to be most effective as it ameliorates most of the alterations caused in the studied parameters in diabetic rats when compared with n- hexane, ethyl acetate, n- butanol and aqueous fractions. Conclusion: The study validates the anti-diabetic effects of VALF in fortified diet-fed streptozotocin-treated rat model of T2D, and suggests that the VAc is a potential candidate for development of a more effective drug for the management of T2D.

  17. Indexing Natural Products for Their Potential Anti-Diabetic Activity: Filtering and Mapping Discriminative Physicochemical Properties.

    Science.gov (United States)

    Zeidan, Mouhammad; Rayan, Mahmoud; Zeidan, Nuha; Falah, Mizied; Rayan, Anwar

    2017-09-17

    Diabetes mellitus (DM) poses a major health problem, for which there is an unmet need to develop novel drugs. The application of in silico techniques and optimization algorithms is instrumental to achieving this goal. A set of 97 approved anti-diabetic drugs, representing the active domain, and a set of 2892 natural products, representing the inactive domain, were used to construct predictive models and to index anti-diabetic bioactivity. Our recently-developed approach of 'iterative stochastic elimination' was utilized. This article describes a highly discriminative and robust model, with an area under the curve above 0.96. Using the indexing model and a mix ratio of 1:1000 (active/inactive), 65% of the anti-diabetic drugs in the sample were captured in the top 1% of the screened compounds, compared to 1% in the random model. Some of the natural products that scored highly as potential anti-diabetic drug candidates are disclosed. One of those natural products is caffeine, which is noted in the scientific literature as having the capability to decrease blood glucose levels. The other nine phytochemicals await evaluation in a wet lab for their anti-diabetic activity. The indexing model proposed herein is useful for the virtual screening of large chemical databases and for the construction of anti-diabetes focused libraries.

  18. 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.

  19. The antidiabetic drug ciglitazone induces high grade bladder cancer cells apoptosis through the up-regulation of TRAIL.

    Directory of Open Access Journals (Sweden)

    Marie-Laure Plissonnier

    Full Text Available Ciglitazone belongs to the thiazolidinediones class of antidiabetic drug family and is a high-affinity ligand for the Peroxisome Proliferator-Activated Receptor γ (PPARγ. Apart from its antidiabetic activity, this molecule shows antineoplastic effectiveness in numerous cancer cell lines.Using RT4 (derived from a well differentiated grade I papillary tumor and T24 (derived from an undifferentiated grade III carcinoma bladder cancer cells, we investigated the potential of ciglitazone to induce apoptotic cell death and characterized the molecular mechanisms involved. In RT4 cells, the drug induced G2/M cell cycle arrest characterized by an overexpression of p53, p21(waf1/CIP1 and p27(Kip1 in concomitance with a decrease of cyclin B1. On the contrary, in T24 cells, it triggered apoptosis via extrinsic and intrinsic pathways. Cell cycle arrest and induction of apoptosis occurred at high concentrations through PPARγ activation-independent pathways. We show that in vivo treatment of nude mice by ciglitazone inhibits high grade bladder cancer xenograft development. We identified a novel mechanism by which ciglitazone kills cancer cells. Ciglitazone up-regulated soluble and membrane-bound TRAIL and let TRAIL-resistant T24 cells to respond to TRAIL through caspase activation, death receptor signalling pathway and Bid cleavage. We provided evidence that TRAIL-induced apoptosis is partially driven by ciglitazone-mediated down-regulation of c-FLIP and survivin protein levels through a proteasome-dependent degradation mechanism.Therefore, ciglitazone could be clinically relevant as chemopreventive or therapeutic agent for the treatment of TRAIL-refractory high grade urothelial cancers.

  20. studies on in vitro evaluation of antidiabetic potentials

    African Journals Online (AJOL)

    userpc

    Keywords: fruit peels, antidiabetic activity, α-amylase enzyme, glycosylated haemoglobin. INTRODUCTION ... absorption of starch into the body thereby .... room temperature for 72 hrs (Abirami et al.,. 2014). ... carbohydrate digestion. One of ...

  1. Indexing Natural Products for Their Potential Anti-Diabetic Activity: Filtering and Mapping Discriminative Physicochemical Properties

    Directory of Open Access Journals (Sweden)

    Mouhammad Zeidan

    2017-09-01

    Full Text Available Diabetes mellitus (DM poses a major health problem, for which there is an unmet need to develop novel drugs. The application of in silico techniques and optimization algorithms is instrumental to achieving this goal. A set of 97 approved anti-diabetic drugs, representing the active domain, and a set of 2892 natural products, representing the inactive domain, were used to construct predictive models and to index anti-diabetic bioactivity. Our recently-developed approach of ‘iterative stochastic elimination’ was utilized. This article describes a highly discriminative and robust model, with an area under the curve above 0.96. Using the indexing model and a mix ratio of 1:1000 (active/inactive, 65% of the anti-diabetic drugs in the sample were captured in the top 1% of the screened compounds, compared to 1% in the random model. Some of the natural products that scored highly as potential anti-diabetic drug candidates are disclosed. One of those natural products is caffeine, which is noted in the scientific literature as having the capability to decrease blood glucose levels. The other nine phytochemicals await evaluation in a wet lab for their anti-diabetic activity. The indexing model proposed herein is useful for the virtual screening of large chemical databases and for the construction of anti-diabetes focused libraries.

  2. New amides from seeds of Silybum marianum with potential antioxidant and antidiabetic activities.

    Science.gov (United States)

    Qin, Ning-Bo; Jia, Cui-Cui; Xu, Jun; Li, Da-Hong; Xu, Fan-Xing; Bai, Jiao; Li, Zhan-Lin; Hua, Hui-Ming

    2017-06-01

    Two new amide compounds, mariamides A and B (1-2), were obtained together with fourteen known compounds from the seeds of milk thistle (Silybum marianum). Their structures were established on the basis of extensive 1D and 2D NMR analyses, as well as HR-ESI-MS data. Most of the compounds showed significant antioxidant activities than positive control in ABTS and FRAP assays. However, only amide compounds 1-4 showed moderate DPPH radical scavenging activity and compounds 7 and 16 showed the most potent activity against DPPH. Most of the compounds showed moderate to stronger α-glucosidase inhibitory activities. Nevertheless, only flavonoids showed strong PTP1B inhibitory activities. These results indicate a use of milk thistle seed extracts as promising antioxidant and antidiabetic agents. Copyright © 2017 Elsevier B.V. All rights reserved.

  3. Antidiabetic activities of aqueous and ethanolic extracts of Piper betle leaves in rats.

    Science.gov (United States)

    Arambewela, L S R; Arawwawala, L D A M; Ratnasooriya, W D

    2005-11-14

    Leaves of Piper betle (Piperaceae) possess several bioactivities and are used in traditional medicinal systems. However, its antidiabetic activity has not been scientifically investigated so far. The aim of this study therefore, was to investigate the antidiabetic activity of Piper betle leaves. This was tested in normoglycaemic and strepozotocin (STZ)-induced diabetic rats using oral administration of hot water extract (HWE) and cold ethanolic extract (CEE). In normoglycaemic rats, both HWE and CEE significantly lowered the blood glucose level in a dose-dependent manner. In glucose tolerance test, both extracts markedly reduced the external glucose load. The antidiabetic activity of HWE is comparable to that of CEE. Moreover, HWE failed to inhibit the glucose absorption from the small intestine of rats. Both extracts were found to be non-toxic and well tolerated after following chronic oral administration (no overt signs of toxicity, hepatotoxicity or renotoxicity). However, the weight of the spleen had increased in treated groups possibly indicating lymphoproliferative activity. It is concluded that HWE and CEE of Piper betle leaves possess safe and strong antidiabetic activity.

  4. Effectiveness testing of spill-treating agents

    International Nuclear Information System (INIS)

    Fingas, M.F.; Stoodley, R.; Laroche, N.

    1990-01-01

    Laboratory effectiveness tests are described for four classes of spill-treating agents: solidifiers, demulsifying agents, surface-washing agents and dispersants. Many treating agents in these four categories have been tested for effectiveness and the results are presented. Solidifiers or gelling agents solidify oil, requiring a large amount of agent to solidify oil-ranging between 16% by weight, to over 200%. Emulsion breakers prevent or reverse the formation of water-in-oil emulsions. A newly-developed effectiveness test shows that only one product is highly effective; however, many products will work, but require large amounts of spill-treating agent. Surfactant--containing materials are of two types, surface-washing agents and dispersants. Testing has shown that an agent that is a good dispersant is conversely a poor surface-washing agent, and vice versa. Tests of surface-washing agents show that only a few agents have effectiveness of 25-40%, where this effectiveness is the percentage of heavy oil removed from a test surface. Results using the 'swirling flask' test for dispersant effectiveness are reported. Heavy oils show effectiveness values of about 1%, medium crudes of about 10%, light crude oils of about 30% and very light oils of about 90%. (author)

  5. Antidiabetic Activity of Different Extracts of Myrtus Communis in Streptozotocin Induced Diabetic Rats

    Directory of Open Access Journals (Sweden)

    Panjeshahin Mohammad Reza

    2016-06-01

    Full Text Available Background and aim: Hydroalcoholic (70° extract of leaves of Myrtus communis has been shown to have antidiabetic effect in streptozotocin induced diabetic rats in our previous study. In this study, we intended to determine the components of the mentioned extract and identify the mechanism for its action.

  6. 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.

  7. Plant foods in the management of diabetes mellitus: spices as beneficial antidiabetic food adjuncts.

    Science.gov (United States)

    Srinivasan, K

    2005-09-01

    Diet has been recognized as a corner stone in the management of diabetes mellitus. Spices are the common dietary adjuncts that contribute to the taste and flavour of foods. Besides, spices are also known to exert several beneficial physiological effects including the antidiabetic influence. This review considers all the available information from animal experimentation as well as clinical trials where spices, their extracts or their active principles were examined for treatment of diabetes. Among the spices, fenugreek seeds (Trigonella foenumgraecum), garlic (Allium sativum), onion (Allium cepa), and turmeric (Curcuma longa) have been experimentally documented to possess antidiabetic potential. In a limited number of studies, cumin seeds (Cuminum cyminum), ginger (Zingiber officinale), mustard (Brassica nigra), curry leaves (Murraya koenigii) and coriander (Coriandrum sativum) have been reported to be hypoglycaemic.

  8. Preparation and antidiabetic activity of polysaccharide from ...

    African Journals Online (AJOL)

    Extraction parameters of polysaccharide from Portulaca oleracea L. (POP) and antidiabetic activity of POP on alloxan induced diabetic mice were studied. Better extraction parameters of POP were obtained by the single factor test, as follows: extraction temperature 95°C, extraction time 5 h, and ratio of solvent to raw ...

  9. Compositional Studies: Antioxidant and Antidiabetic Activities of Capparis decidua (Forsk. Edgew

    Directory of Open Access Journals (Sweden)

    Muhammad Zia-Ul-Haq

    2011-12-01

    Full Text Available Capparis decidua is one of the traditional remedies used for various medicinal treatments in Pakistan. This study presents the determination of proximate composition, amino acids, fatty acids, tocopherols, sterols, glucosinolate and phenolic content in extracts obtained from different aerial parts of C. decidua, as well as their antidiabetic and antioxidant activity. All examined extracts were prominently rich in phenolics and glucosinates, and they showed potent antidiabetic and antihemolytic activity. The present study could be helpful in developing medicinal preparations for the treatment of diabetes and related symptoms.

  10. Antidiabetic effect of gomisin N via activation of AMP-activated protein kinase.

    Science.gov (United States)

    Jung, Dae Young; Kim, Ji-Hyun; Lee, Hoyoung; Jung, Myeong Ho

    2017-12-16

    Gomisin N (GN) is a lignan derived from Schisandra chinensis. AMP-activated kinase (AMPK) has gained attention as a therapeutic target for the treatment of metabolic syndrome. Previously, we reported that GN activated the AMPK pathway and ameliorated high-fat diet (HFD)-induced hepatic steatosis. In this study, we investigated the anti-diabetic effects of GN in C2C12 myotubes and HFD obese mice. GN enhanced the phosphorylation of AMPK/acetyl-CoA carboxylase (ACC) and Akt. In addition, GN promoted glucose uptake in C2C12 myotubes, which was accompanied by the translocation of glucose transporter 4 (GLUT4) to the plasma membrane. Treatment with compound C, an AMPK inhibitor, suppressed GN-mediated stimulation of glucose uptake. Furthermore, GN increased the expression of mitochondria biogenesis and fatty acid oxidation genes in C2C12 myotubes. In the in vivo study, administration of GN to HFD mice decreased the levels of fasting blood glucose and insulin, and improved glucose tolerance in HFD obese mice. GN administration rescued the decreased phosphorylation of AMPK and Akt and stimulated the expression of mitochondria biogenesis genes in the skeletal muscle of HFD mice. These findings suggested that GN exerted anti-hyperglycemic effects through AMPK activation. Copyright © 2017 Elsevier Inc. All rights reserved.

  11. Anti-diabetic potential of the essential oil of Pinus koraiensis leaves toward streptozotocin-treated mice and HIT-T15 pancreatic β cells.

    Science.gov (United States)

    Joo, Hye-Eun; Lee, Hyo-Jung; Sohn, Eun Jung; Lee, Min-Ho; Ko, Hyun-Suk; Jeong, Soo-Jin; Lee, Hyo-Jeong; Kim, Sung-Hoon

    2013-01-01

    The metabolic syndrome creates risk factors for coronary heart disease, diabetes, fatty liver, obesity and several cancers. Our group has already reported that the essential oil from leaves of Pinus koraiensis SIEB (EOPK) exerted antihyperlipidemic effects by upregulating the low-density lipoprotein receptor and inhibiting acyl-coenzyme A, cholesterol acyltransferases. We evaluated in the current study the anti-diabetic effects of EOPK on mice with streptozotocin (STZ)-induced type I diabetes and on HIT-T15 pancreatic β cells. EOPK significantly protected HIT-T15 cells from STZ-induced cytotoxicity and reduced the blood glucose level in STZ-induced diabetic mice when compared with the untreated control. EOPK consistently and significantly suppressed the α-amylase activity in a dose-dependent manner and enhanced the expression of insulin at the mRNA level in STZ-treated HIT-T15 cells, while the expression of insulin was attenuated. EOPK also significantly abrogated the population of reactive oxygen species when compared to the untreated control in STZ-treated HIT-T15 cells. Furthermore, EOPK significantly reduce nitric oxide production, suppressed the phosphorylation of endothelial nitric oxide (NO) synthase and suppressed the production of vascular endothelial growth factor (VEGF) in STZ-treated HIT-T15 cells, implying its potential application to diabetic retinopathy. Overall, our findings suggest that EOPK had hypoglycemic potential by inhibiting reactive oxygene species (ROS), endothelial NO synthase (eNOS) and VEGF in STZ-treated mice and HIT-T15 pancreatic β cells as a potent anti-diabetic agent.

  12. Evaluating the antidiabetic effects of Chinese herbal medicine: Xiao-Ke-An in 3T3-L1 cells and KKAy mice using both conventional and holistic omics approaches.

    Science.gov (United States)

    Yang, Zhenzhong; Wang, Linli; Zhang, Feng; Li, Zheng

    2015-08-13

    Xiao-Ke-An (XKA) is a Chinese medicine widely used for treating type 2 diabetes mellitus (T2D). It is composed of eight herbal medicines traditionally used for T2D, including Rehmannia glutinosa Libosch, Anemarrhena asphodeloides Bunge, Coptis chinensis Franch, etc. The aim of the present study was to investigate the antidiabetic effects of XKA with both conventional and holistic omics approaches. The antidiabetic effect of XKA was first investigated in 3T3-L1 cells to study the effect of XKA on adipogenesis in vitro. Oil Red O staining was performed to determine the lipid accumulation. The intracellular total cholesterol (TC) and triglyceride (TG) contents in XKA treated 3T3-L1 cells were also evaluated. The therapeutic effects of XKA was further evaluated in KKAy mice with both conventional and holistic omics approaches. Body weight, fasting and non-fasting blood glucose, and oral glucose tolerance were measured during the experiment. At the time of sacrifice, serum was collected for the measurement of TG, TC, high-density lipoprotein cholesterol (HDL-c) and low-density lipoprotein cholesterol (LDL-c). The liver, kidney, spleen, pancreas, heart and adipose tissues were harvested and weighted. The liver was used for further microarray experiment. Omics approaches were adopted to evaluate the holistic rebalancing effect of XKA at molecular network level. XKA significantly inhibited adipogenic differentiation, lowered the intracellular TC and TG contents in 3T3-L1 cells. XKA improved the glucose homeostasis and lipid metabolism, ameliorated insulin resistance in KKAy mice. Furthermore, XKA also exhibited effective therapeutic effects by reversing the molecular T2D disease network from an unbalanced state. This study investigated the antidiabetic effects of XKA with both conventional and holistic omics approaches, providing both phenotypic evidence and underlying action mechanisms for the clinical use of XKA treating T2D.

  13. Oral anti-diabetics in Ramadan.

    Science.gov (United States)

    Islam, Najmul

    2015-05-01

    A large proportion of Muslim patients with type 2 diabetes fast during the month of Ramadan worldwide. Hypoglycaemia is one of the major complications associated with long periods without food during the fasting hours. There is also a risk of hyperglycaemia due to over indulgence in food during the two main meals of Suhur and Iftar. Healthcare providers need to be cognizant of the risk of fasting and be competent to provide Ramadan adjusted diabetes care particularly adjustment of oral anti diabetics. This review article has taken into consideration observational studies, randomized trial data, pathophysiology and practical experience in recommending adjustment in oral anti-diabetics during fasting in type-2 diabetics. Metformin and Thiazolidinediones (TZD'S) being insulin sensitizers need minimum adjustment with low risk of hypoglycaemia. Older generation Sulphonylureas (SU) pose a high risk of hypoglycaemia but the newer generations of Sulphonylureas have a reasonable safety profile. Alpha- Glucosidase inhibitors are safe during fasting but their use is limited due to the side effects.

  14. Magnetic solid-phase extraction based on mesoporous silica-coated magnetic nanoparticles for analysis of oral antidiabetic drugs in human plasma

    Energy Technology Data Exchange (ETDEWEB)

    Souza, Karynne Cristina de; Andrade, Gracielle Ferreira [Centro de Desenvolvimento da Tecnologia Nuclear, CDTN/CNEN, Rua Professor Mário Werneck, s/n. Campus Universitário, Belo Horizonte, MG CEP 30.123-970 (Brazil); Vasconcelos, Ingrid; Oliveira Viana, Iara Maíra de; Fernandes, Christian [Departamento de Produtos Farmacêuticos, Faculdade de Farmácia, Universidade Federal de Minas Gerais, Belo Horizonte, MG (Brazil); Martins Barros de Sousa, Edésia, E-mail: sousaem@cdtn.br [Centro de Desenvolvimento da Tecnologia Nuclear, CDTN/CNEN, Rua Professor Mário Werneck, s/n. Campus Universitário, Belo Horizonte, MG CEP 30.123-970 (Brazil)

    2014-07-01

    In the present work, magnetic nanoparticles embedded into mesoporous silica were prepared in two steps: first, magnetite was synthesized by oxidation–precipitation method, and next, the magnetic nanoparticles were coated with mesoporous silica by using nonionic block copolymer surfactants as structure-directing agents. The mesoporous SiO{sub 2}-coated Fe{sub 3}O{sub 4} samples were functionalized using octadecyltrimethoxysilane as silanizing agent. The pure and functionalized silica nanoparticles were physicochemically and morphologically characterized by X-ray diffraction (XRD), Fourier transform infrared spectroscopy (FTIR), N{sub 2} adsorption, scanning electron microscopy (SEM) and transmission electron microscopy (TEM). The resultant magnetic silica nanoparticles were applied as sorbents for magnetic solid-phase extraction (MSPE) of oral antidiabetic drugs in human plasma. Our results revealed that the magnetite nanoparticles were completely coated by well-ordered mesoporous silica with free pores and stable pore walls, and that the structural and magnetic properties of the Fe{sub 3}O{sub 4} nanoparticles were preserved in the applied synthesis route. Indeed, the sorbent material was capable of extracting the antidiabetic drugs from human plasma, being useful for the sample preparation in biological matrices. - Highlights: • SBA-15/Fe{sub 3}O{sub 4} was synthesized and functionalized with octadecyltrimethoxysilane. • Magnetite nanoparticles were completely coated by well-ordered mesoporous silica. • The samples were used as sorbent for magnetic solid-phase extraction (MSPE). • The sorbent material was capable of extracting drugs from human plasma. • The extraction ability makes the material a candidate to be employed as MSPE.

  15. Antidiabetic And Toxicological Evaluation Of Aqueous Ethanol Leaf ...

    African Journals Online (AJOL)

    Secamone afzelii Rhoem is used in ethnomedicine for hepatic diseases, diabetes, venereal diseases, amenorrhoea and toothaches. This present study was aimed at evaluating the antidiabetic activity and to establish the toxicological profile of the plant to confirm its traditional application and justify continuous usage.

  16. Immunological effects of hypomethylating agents.

    Science.gov (United States)

    Lindblad, Katherine E; Goswami, Meghali; Hourigan, Christopher S; Oetjen, Karolyn A

    2017-08-01

    Epigenetic changes resulting from aberrant methylation patterns are a recurrent observation in hematologic malignancies. Hypomethylating agents have a well-established role in the management of patients with high-risk myelodysplastic syndrome or acute myeloid leukemia. In addition to the direct effects of hypomethylating agents on cancer cells, there are several lines of evidence indicating a role for immune-mediated anti-tumor benefits from hypomethylating therapy. Areas covered: We reviewed the clinical and basic science literature for the effects of hypomethylating agents, including the most commonly utilized therapeutics azacitidine and decitabine, on immune cell subsets. We summarized the effects of hypomethylating agents on the frequency and function of natural killer cells, T cells, and dendritic cells. In particular, we highlight the effects of hypomethylating agents on expression of immune checkpoint inhibitors, leukemia-associated antigens, and endogenous retroviral elements. Expert commentary: In vitro and ex vivo studies indicate mixed effects on the function of natural killer, dendritic cells and T cells following treatment with hypomethylating agents. Clinical correlates of immune function have suggested that hypomethylating agents have immunomodulatory functions with the potential to synergize with immune checkpoint therapy for the treatment of hematologic malignancy, and has become an active area of clinical research.

  17. Racial differences in long-term adherence to oral antidiabetic drug therapy: a longitudinal cohort study

    Directory of Open Access Journals (Sweden)

    Meigs James B

    2009-02-01

    Full Text Available Abstract Background Adherence to oral antidiabetic medications is often suboptimal. Adherence differences may contribute to health disparities for black diabetes patients, including higher microvascular event rates, greater complication-related disability, and earlier mortality. Methods In this longitudinal retrospective cohort study, we used 10 years of patient-level claims and electronic medical record data (1/1/1992–12/31/2001 to assess differences in short- and long-term adherence to oral antidiabetic medication among 1906 newly diagnosed adults with diabetes (26% black, 74% white in a managed care setting in which all members have prescription drug coverage. Four main outcome measures included: (1 time from diabetes diagnosis until first prescription of oral antidiabetic medication; (2 primary adherence (time from first prescription to prescription fill; (3 time until discontinuation of oral antidiabetic medication from first prescription; and (4 long-term adherence (amount dispensed versus amount prescribed over a 24-month follow-up from first oral antidiabetic medication prescription. Results Black patients were as likely as whites to initiate oral therapy and fill their first prescription, but experienced higher rates of medication discontinuation (HR: 1.8, 95% CI: 1.2, 2.7 and were less adherent over time. These black-white differences increased over the first six months of therapy but stabilized thereafter for patients who initiated on sulfonylureas. Significant black-white differences in adherence levels were constant throughout follow-up for patients initiated on metformin therapy. Conclusion Racial differences in adherence to oral antidiabetic drug therapy persist even with equal access to medication. Early and continued emphasis on adherence from initiation of therapy may reduce persistent racial differences in medication use and clinical outcomes.

  18. Why Antidiabetic Vanadium Complexes are Not in the Pipeline of "Big Pharma" Drug Research? A Critical Review.

    Science.gov (United States)

    Scior, Thomas; Guevara-Garcia, Jose Antonio; Do, Quoc-Tuan; Bernard, Philippe; Laufer, Stefan

    2016-01-01

    Public academic research sites, private institutions as well as small companies have made substantial contributions to the ongoing development of antidiabetic vanadium compounds. But why is this endeavor not echoed by the globally operating pharmaceutical companies, also known as "Big Pharma"? Intriguingly, today's clinical practice is in great need to improve or replace insulin treatment against Diabetes Mellitus (DM). Insulin is the mainstay therapeutically and economically. So, why do those companies develop potential antidiabetic drug candidates without vanadium (vanadium- free)? We gathered information about physicochemical and pharmacological properties of known vanadium-containing antidiabetic compounds from the specialized literature, and converted the data into explanations (arguments, the "pros and cons") about the underpinnings of antidiabetic vanadium. Some discoveries were embedded in chronological order while seminal reviews of the last decade about the Medicinal chemistry of vanadium and its history were also listed for further understanding. In particular, the concepts of so-called "noncomplexed or free" vanadium species (i.e. inorganic oxido-coordinated species) and "biogenic speciation" of antidiabetic vanadium complexes were found critical and subsequently documented in more details to answer the question.

  19. Anti-diabetic effects of Sargassum oligocystum on Streptozotocin- induced diabetic rat

    Directory of Open Access Journals (Sweden)

    Samad Akbarzadeh

    2018-03-01

    Full Text Available Objective(s: Diabetes is a metabolic syndrome which is associated with the worldwide major public health problems. There are many natural compounds from the sea-market, as a valuable aquatic source, along with the variety of health and therapeutic benefits. In the present research, with respect to the traditional and ethnic uses of Sargassum oligocystum algae for healing of some diseases which have similar metabolic mechanism to the diabetes, its anti-diabetic effects in animal model was proposed. Materials and Methods: The animals (rat were divided into the normal control, diabetic control, positive control and, the test groups. The test groups were gavaged with oral doses of 150 and 300 mg/kg of algae hydroalcoholic extracts. After 30 days of intervention the serum glucose, cholesterol, triglyceride, HDLC, LDLC, insulin, insulin resistance, β-cells function and, the histopathology of pancreatic tissue were evaluated. Results: In animals that were fed with algae extracts a significant decrease in the fasting blood glucose, triglyceride and HOMA-IR and an increase in the HOMA-B with no significant impacts on the insulin, cholesterol and HDL were observed. Also, the histopathology evaluations in the groups which were treated with algae extract revealed the regeneration and reconstitution of damaged pancreatic β-cells. Conclusion: The results give evidence that, the S. oligocystum algae extract has a healing effect on diabetes which can be considered as a new research prospect for the natural therapy of diabetes.

  20. Antioxidant and antidiabetic properties of tartary buckwheat rice flavonoids after in vitro digestion*

    Science.gov (United States)

    Bao, Tao; Wang, Ye; Li, Yu-ting; Gowd, Vemana; Niu, Xin-he; Yang, Hai-ying; Chen, Li-shui; Chen, Wei; Sun, Chong-de

    2016-01-01

    Oxidative stress and diabetes have a tendency to alter protein, lipid, and DNA moieties. One of the strategic methods used to reduce diabetes-associated oxidative stress is to inhibit the carbohydrate-digesting enzymes, thereby decreasing gastrointestinal glucose production. Plant-derived natural antioxidant molecules are considered a therapeutic tool in the treatment of oxidative stress and diabetes. The objective of this study was to identify tartary buckwheat rice flavonoids and evaluate the effect of in vitro digestion on their antioxidant and antidiabetic properties. High performance liquid chromatography (HPLC) analysis indicated the presence of rutin as a major component and quercitrin as a minor component of both digested and non-digested flavonoids. Both extracts showed a significant antioxidant capacity, but digested flavonoids showed reduced activity compared to non-digested. There were some decreases of the antioxidant activities (2,2'-azino-bis-(3-ethylbenzthiazoline-6-sulfonic acid) diammonium salt (ABTS), 2,2-diphenyl-1-picrylhydrazy (DPPH) radical, and ferric reducing antioxidant power (FRAP)) of digested tartary buckwheat rice flavonoids compared with non-digested. Flavonoids from both groups significantly inhibited reactive oxygen species (ROS) production and α-glucosidase activity. Both digested and non-digested flavonoids markedly increased glucose consumption and glycogen content in HepG2 cells. Tartary buckwheat rice flavonoids showed appreciable antioxidant and antidiabetic properties, even after digestion. Tartary buckwheat rice appears to be a promising functional food with potent antioxidant and antidiabetic properties. PMID:27921399

  1. Antioxidant and antidiabetic properties of tartary buckwheat rice flavonoids after in vitro digestion.

    Science.gov (United States)

    Bao, Tao; Wang, Ye; Li, Yu-Ting; Gowd, Vemana; Niu, Xin-He; Yang, Hai-Ying; Chen, Li-Shui; Chen, Wei; Sun, Chong-de

    Oxidative stress and diabetes have a tendency to alter protein, lipid, and DNA moieties. One of the strategic methods used to reduce diabetes-associated oxidative stress is to inhibit the carbohydrate-digesting enzymes, thereby decreasing gastrointestinal glucose production. Plant-derived natural antioxidant molecules are considered a therapeutic tool in the treatment of oxidative stress and diabetes. The objective of this study was to identify tartary buckwheat rice flavonoids and evaluate the effect of in vitro digestion on their antioxidant and antidiabetic properties. High performance liquid chromatography (HPLC) analysis indicated the presence of rutin as a major component and quercitrin as a minor component of both digested and non-digested flavonoids. Both extracts showed a significant antioxidant capacity, but digested flavonoids showed reduced activity compared to non-digested. There were some decreases of the antioxidant activities (2,2'-azino-bis-(3-ethylbenzthiazoline-6-sulfonic acid) diammonium salt (ABTS), 2,2-diphenyl-1-picrylhydrazy (DPPH) radical, and ferric reducing antioxidant power (FRAP)) of digested tartary buckwheat rice flavonoids compared with non-digested. Flavonoids from both groups significantly inhibited reactive oxygen species (ROS) production and α-glucosidase activity. Both digested and non-digested flavonoids markedly increased glucose consumption and glycogen content in HepG2 cells. Tartary buckwheat rice flavonoids showed appreciable antioxidant and antidiabetic properties, even after digestion. Tartary buckwheat rice appears to be a promising functional food with potent antioxidant and antidiabetic properties.

  2. 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.

  3. Antidiabetic effects of Morus alba fruit polysaccharides on high-fat diet- and streptozotocin-induced type 2 diabetes in rats.

    Science.gov (United States)

    Jiao, Yukun; Wang, Xueqian; Jiang, Xiang; Kong, Fansheng; Wang, Shumei; Yan, Chunyan

    2017-03-06

    group. Moreover, MFP50 and MFP90 induced repair of damaged pancreatic tissues of the diabetic rats. The hypoglycemic effect of MFP50 was more stable than MFP90, whereas the hypolipidemic effect of MFP90 was slightly better than MFP50. Moreover, the expression levels of InsR, IRS-2, Akt and GLUT4 in the MFP90 group significantly increased relative to that of the T2DM group. MFP50 and MFP90 have markedly antihyperglycemic and antihyperlipidemic effects and can clearly relieve diabetes symptoms in the T2DM rat model. The M. alba fruit polysaccharides may potentially be utilized as an effective treatment for T2DM. Further research into the structures of active M. alba fruit polysaccharides and their mechanisms in promoting antidiabetic effects are underway. Copyright © 2017 Elsevier Ireland Ltd. All rights reserved.

  4. Antidiabetic, antioxidant and anti inflammatory properties of water and n-butanol soluble extracts from Saharian Anvillea radiata in high-fat-diet fed mice.

    Science.gov (United States)

    Kandouli, Chouaib; Cassien, Mathieu; Mercier, Anne; Delehedde, Caroline; Ricquebourg, Emilie; Stocker, Pierre; Mekaouche, Mourad; Leulmi, Zineb; Mechakra, Aicha; Thétiot-Laurent, Sophie; Culcasi, Marcel; Pietri, Sylvia

    2017-07-31

    According to Saharian traditional medicine, Anvillea radiata Coss. & Dur. (Asteraceae) has been valued for treating a variety of ailments such as gastro-intestinal, liver and pulmonary diseases, and has gained awareness for its beneficial effect on postprandial hyperglycemia. However, to best of our knowledge, no detailed study of the antidiabetic curative effects of this plant has been conducted yet. To determine the hypoglycemic and antidiabetic effect of dietary supplementation with Anvillea radiata extracts on high-fat-diet (HFD)-induced obesity and insulin resistance in C57BL/6J mice in relation with antioxidant, anti-inflammatory, pancreatic beta-cells and skeletal muscle protection, and digestive enzyme inhibiting properties. Six extracts (water soluble and organic) from aerial parts of the plant were analyzed phytochemically (total phenolic and flavonoid content) and screened for in vitro superoxide (by chemiluminescence) and hydroxyl radical (by electron paramagnetic resonance spin-trapping) scavenging, antioxidant (DPPH, TRAP and ORAC assays), xanthine oxidase, metal chelating, α-amylase and α-glucosidase inhibitory property, and protective effects on copper-induced lipoprotein oxidation. Then selected hydroalcoholic and aqueous extracts were assessed for toxicity in normal human lung fibroblasts and A549 cancer cells using FMCA and MTT assays. Two water-soluble extracts having the best overall properties were assessed for their (i) protective effect at 1-15µg/mL on metabolic activity of rat insulinoma-derived INS-1 cells exposed to hyperglycemic medium, and (ii) acute hypoglycemic effect on 16-weeks HFD-induced diabetic mice. Then diabetic mice were administered HFD supplemented by extracts (up to 150mg/kg/day) for 12 additional weeks using standard diet as control and the antidiabetic drug, metformin (150mg/kg), as positive control. Then the antidiabetic, anti-inflammatory and antioxidant activity of extracts were determined. Of the highly efficient

  5. 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

  6. Anti-diabetic drug utilization of pregnant diabetic women in us managed care.

    Science.gov (United States)

    Knox, Caitlin A; Delaney, Joseph A C; Winterstein, Almut G

    2014-01-17

    With the increasing prevalence of type 2 diabetes in young adulthood, treatment of diabetes in pregnancy faces new challenges. Anti-diabetic drug utilization patterns of pregnant women with pre-existing diabetes are poorly described. We aim to describe anti-diabetic (AD) agent utilization among diabetic pregnant women. We utilized IMS LifeLink, including administrative claims data of patients in US managed care plans, to establish a retrospective cohort of women, age 18-46 years (N = 96,740) with billed procedures for a live birth, and a 12 month eligibility period before and 3 month after delivery. Diabetes mellitus was identified from ≥2 in- or outpatient claims with diagnoses (ICD-9-CM 250.XX) before pregnancy. We estimated the prevalence of AD drugs before, during and after pregnancy, and secular trends across the study period (1999-2009), using linear regression. A sensitivity analysis was conducted to identify the extent of misclassification of trimesters. Almost six percent (n = 5,581) of the live birth cohort had diabetes mellitus. Throughout the study, 48% (1999) and 78% (2009) (p metformin, sulfonylureas, thiazolidinediones (TZD), and combination AD. The annual prevalence of insulin use increased by only 1% from 39% (1999) to 40% (2009) (p = 0.589) during pregnancy, while use of sulfonylureas and metformin increased from 2.5% and 4.2% (1999) to 17.3% and 15.3% (2009) (p use steadily increased in prevalence from the 1st to 3rd trimester (16.5% and 3.3% to 33.0% and 7.5%), while metformin and TZD use decreased (11.4% and 1.6% to 3.8% and 0.2%). AD use during pregnancy demonstrates the need for additional investigation regarding safety and efficacy of AD drugs on maternal outcomes.

  7. Antidiabetic Activity of Cocor Bebek Leaves (Kalanchoe pinnata Lam.Pers. Ethanolic Extract from Various Areas

    Directory of Open Access Journals (Sweden)

    Indah Dwiatmi Dewiyanti

    2012-05-01

    Full Text Available Antidiabetic activity of Cocor Bebek leaves (Kalanchoe pinnata Lam.Pers. ethanolic extract from Bogor city, kabupaten Bogor and south of Tangerang city has been studied. The study was conducted in vitro using α glucosidase inhibitor method. The results of the study showed that IC50 of the extract from Bogor city, kabupaten Bogor, and Tangerang Selatan city is 40.94 ppm, 33.58 ppm and 16.12 ppm respectively. Meanwhile, IC50 of quersetin which has antidiabetic activity is 10.22 ppm. The results showed that Cocor Bebek leaves (Kalanchoe pinnata Lam.Pers. ethanolic extract had antidiabetic activity with IC50 less than 100 ppm. However, the activity is lesser than quercetin.

  8. An overview of anti-diabetic plants used in Gabon: Pharmacology and toxicology.

    Science.gov (United States)

    Bading Taika, B; Bouckandou, M; Souza, A; Bourobou Bourobou, H P; MacKenzie, L S; Lione, L

    2018-04-24

    The management of diabetes mellitus management in African communities, especially in Gabon, is not well established as more than 60% of population rely on traditional treatments as primary healthcare. The aim of this review was to collect and present the scientific evidence for the use of medicinal plants that are in currect by Gabonese traditional healers to manage diabetes or hyperglycaemia based here on the pharmacological and toxicological profiles of plants with anti-diabetic activity. There are presented in order to promote their therapeutic value, ensure a safer use by population and provide some bases for further study on high potential plants reviewed. Ethnobotanical studies were sourced using databases such as Online Wiley library, Pubmed, Google Scholar, PROTA, books and unpublished data including Ph.D. and Master thesis, African and Asian journals. Keywords including 'Diabetes', 'Gabon', 'Toxicity', 'Constituents', 'hyperglycaemia' were used. A total of 69 plants currently used in Gabon with potential anti-diabetic activity have been identified in the literature, all of which have been used in in vivo or in vitro studies. Most of the plants have been studied in human or animal models for their ability to reduce blood glucose, stimulate insulin secretion or inhibit carbohydrates enzymes. Active substances have been identified in 12 out of 69 plants outlined in this review, these include Allium cepa and Tabernanthe iboga. Only eight plants have their active substances tested for anti-diabetic activity and are suitables for further investigation. Toxicological data is scarce and is dose-related to the functional parameters of major organs such as kidney and liver. An in-depth understanding on the pharmacology and toxicology of Gabonese anti-diabetic plants is lacking yet there is a great scope for new treatments. With further research, the use of Gabonese anti-diabetic plants is important to ensure the safety of the diabetic patients in Gabon. Copyright

  9. Efek Antidiabetes Kombinasi Ekstrak Bawang Putih (Allium sativum Linn. dan Rimpang Kunyit (Curcumma domestica Val. dengan Pembanding Glibenklamid pada Penderita Diabetes Melitus Tipe 2

    Directory of Open Access Journals (Sweden)

    Ame Suciati Setiawan

    2011-03-01

    Full Text Available The combination of garlic (Allium sativum Linn. and curcumin extract (Curcumma domestica Val. can be used as an antidiabetic oral to type 2 diabetes mellitus (DM patients and the clinical trial showed that the extract can decrease blood glucose at a dose 2.4 g/day. This clinical trial was conducted to know the antidiabetic effect of the combination of garlic and curcumin extract compared with antidiabetic oral, glibenclamide. The subjects were >35 years of age with type 2 DM who came to internal and endocrine clinic RSUP. Hasan Sadikin Bandung and has been treated with medical nutrition therapy for 2 weeks period November 2007–December 2008. The research design was parallel, randomized and double blind. The combination of garlic and curcumin extract decreased mean value of fasting blood glucose 9.25 mg/dL, 2h PP blood glucose 22.25 mg/dL, HbA1c 1,30% and insulin 12.57 mg/ dL compared with baseline whereas glibenclamide decreased the mean value of fasting blood glucose 72.37 mg/dL, 2h PP 114,25 mg/dL, HbA1c 4.12% and increased insulin 3.34 mg/dL. In conclusion, the extract combination has antidiabetic effect eventhough the effect was not as high as glibenclamide

  10. Drug-class-specific changes in the volume and cost of antidiabetic medications in Poland between 2012 and 2015.

    Science.gov (United States)

    Śliwczyński, Andrzej; Brzozowska, Melania; Jacyna, Andrzej; Iltchev, Petre; Iwańczuk, Tymoteusz; Wierzba, Waldemar; Marczak, Michał; Orlewska, Katarzyna; Szymański, Piotr; Orlewska, Ewa

    2017-01-01

    to investigate the drug-class-specific changes in the volume and cost of antidiabetic medications in Poland in 2012-2015. This retrospective analysis was conducted based on the National Health Fund database covering an entire Polish population. The volume of antidiabetic medications is reported according to ATC/DDD methodology, costs-in current international dollars, based on purchasing power parity. During a 4-year observational period the number of patients, consumption of antidiabetic drugs and costs increased by 17%, 21% and 20%, respectively. Biguanides are the basic diabetes medication with a 39% market share. The insulin market is still dominated by human insulins, new antidiabetics (incretins, thiazolidinediones) are practically absent. Insulins had the largest share in diabetes medications expenditures (67% in 2015). The increase in antidiabetic medications costs over the analysed period of time was mainly caused by the increased use of insulin analogues. The observed tendencies correspond to the evidence-based HTA recommendations. The reimbursement status, the ratio of cost to clinical outcomes and data on the long-term safety have a deciding impact on how a drug is used.

  11. SOME EFFECTS ASSOCIATED WITH THE USE OF THE BIOPREPARATION FROM Picralima nitida SEEDS EXTRACT AS ANTIDIABETIC AGENT

    Directory of Open Access Journals (Sweden)

    O. A. Akinloye

    2014-04-01

    Full Text Available The study was aimed to investigate some untoward effects that could be associated with the use of P. nitida as hypoglycemic agent using some biochemical and histological evidences. The antioxidant property of the plant was determined by using 1, 1-diphenyl-2-picrylhydrazyl radical scavenging activity. Biochemical studies in plasma using determining the testes such as blood glucose, alanine and aspartate aminotransferases, gamma glutamyl transferase activities, electrolytes (sodium, potassium and bicarbonate, lipid peroxidation levels, haematological parameters (red blood cell and whole blood cell, platelets, and lymphocyte counts, blood glucose level, lipid profile, and also liver and kidney function tests were performed. Histopathological examinations of the liver, kidney and pancreas were done following the standard Heamatoxylin and Eosin staining method. Methanol extract of the seeds has the highest antioxidant level (36.73%, indicating higher free radical scavenging activity; followed by aqueous extract (19.36% and coconut water extract (4.09%. There was significant reduction (p<0.05 in blood glucose of all the treated rats at the end of the experiment (ranging from 55.59% to 41.66%. Significant increase (p<0.05 in body weights of the treated rats were also observed at the end of the treatment (ranging from 9.26% to 38.89%. There was a significant (p<0.05 increase in the hematological parameters in all the extract treated groups. There was also significant decrease (p<0.05 in the lipid profiles of the treated groups. Plasma studied enzymes activities decreased in all treated groups. Ionoregulatory disturbances observed included hyperkalemia and hypernatremia in all the treated groups but were reduced significantly (p<0.05 at the end of the treatment. Urea and bicarbonate concentrations and also of lipid peroxidation level decreased significantly in all the groups. The histopathological studies revealed that the extracts were unable to

  12. Moringa olifeira Lam. Stimulates Activation of the Insulin-Dependent Akt Pathway. Antidiabetic Effect in a Diet-Induced Obesity (DIO) Mouse Model.

    Science.gov (United States)

    Attakpa, E S; Sangaré, M M; Béhanzin, G J; Ategbo, J-M; Seri, B; Khan, N A

    2017-01-01

    We investigated the antidiabetic effect of Moringa olifeira Lam. in a diet-induced obesity (DIO) mouse model. Six mice were randomly selected as normal controls. Moringa olifeira Lam. leaf extract at a dose of 200, 400 or 600 mg/kg body weight, glibenclamide (Glib) at the dose of 10 mg/kg (positive control) and distilled water at 10 ml/kg (control group) were administered orally by gastric intubation, and each group consisted of six mice. Insulinsensitive tissues (liver, skeletal muscle) were collected to investigate antidiabetic effects and examine the plant's molecular mechanisms. Moringa olifeira Lam. leaf extract prevented weight gain. It also reduced blood glucose in DIO mice. Glib and Moringa olifeira Lam. leaf extract, 400 mg/kg, treatments restored insulin levels towards normal values (P < 0.05 versus diabetic control group). Western immunoblot analysis of different tissues, collected at the end of the study, demonstrated that Moringa olifeira Lam. stimulated activation of the insulin-dependent Akt pathway and increased the protein content of Glut 4 in skeletal muscle. The improvement of hepatic steatosis observed in DIO-treated mice was associated with a decrease in the hepatic content of SREBP-1, a transcription factor involved in de novo lipogenesis. The hepatic PPARα protein content in the plant extract- treated mice remained significantly higher than those of the control group (P < 0.05). In conclusion, this study provides the first evidence for direct action of Moringa olifeira Lam. on pancreatic β-cells, enhancing glucose-stimulated insulin secretion. This correlated with hypoglycaemic effects in diabetic mice associated with restored levels of plasma insulin.

  13. Characterization, antibacterial, antioxidant, antidiabetic, anti-inflammatory and antityrosinase activity of green synthesized silver nanoparticles using Calophyllum tomentosum leaves extract

    Science.gov (United States)

    Govindappa, M.; Hemashekhar, B.; Arthikala, Manoj-Kumar; Ravishankar Rai, V.; Ramachandra, Y. L.

    2018-06-01

    The current research study is to develop an easy and eco-friendly method for the synthesis of AgNPs using aqueous leaf extract of Calophyllum tomentosum (CtAgNPs) and evaluated the extract to know the effects of anti-bacterial, antioxidant, anti-diabetic, anti-inflammatory and anti-tyrosinase activity. Using UV-vis spectrophotometer, Fourier transform infrared spectroscopy (FTIR), X-ray diffraction (XRD), energy dispersive X-ray spectroscopy (EDX) characterized the Calophyllum tomentosum mediated silver nanoparticles. The leaf extract of C. tomentosum yielded flavonoids, saponins, tannins, alkaloids, glycosides, phenols, terpenoids and coumarins. AgNPs formation was confirmed by UV-vis spectra at 438 nm. Crystalline structure with a face centered cubic (fcc) of AgNPs was observed in XRD. FTIR had shown that the phytochemicals were responsible for the reduction and capping material of silver nanoparticles. The size and shape of the AgNPs were determined using SEM. From EDX study analysed the strong absorption property of AgNPs. The CtAgNPs have showed significant antibacterial activity on multi drug resistance bacteria. The CtAgNPs had shown strong antioxidant (DPPH, H2O2 scavenging, nitric oxide scavenging power, reducing power) activities. The CtAgNPs had strongly inhibited the α-glucosidase and DPPIV compared to α-amylase. The CtAgNPs exhibited strong anti-inflammatory activity (albumin denaturation, membrane stabilization, heat haemolytic, protein inhibitory, lipoxygenase, xanthine oxidase) and tyrosinase inhibitory activity. To our best knowledge, this is the first attempt on the synthesis of silver nanoparticles using Calophyllum tomentosum leaves extract. Hence, to validate our results the in vivo studies at molecular level are needed to develop an antioxidant, anti-diabetic and anti-inflammatory agent.

  14. Hypoglycemic and beta cell protective effects of andrographolide analogue for diabetes treatment

    Directory of Open Access Journals (Sweden)

    Larrick James W

    2009-07-01

    Full Text Available Abstract Background While all anti-diabetic agents can decrease blood glucose level directly or indirectly, few are able to protect and preserve both pancreatic beta cell mass and their insulin-secreting functions. Thus, there is an urgent need to find an agent or combination of agents that can lower blood glucose and preserve pancreatic beta cells at the same time. Herein, we report a dual-functional andrographolide-lipoic acid conjugate (AL-1. The anti-diabetic and beta cell protective activities of this novel andrographolide-lipoic acid conjugate were investigated. Methods In alloxan-treated mice (a model of type 1 diabetes, drugs were administered orally once daily for 6 days post-alloxan treatment. Fasting blood glucose and serum insulin were determined. Pathologic and immunohistochemical analysis of pancreatic islets were performed. Translocation of glucose transporter subtype 4 in soleus muscle was detected by western blot. In RIN-m cells in vitro, the effect of AL-1 on H2O2-induced damage and reactive oxidative species production stimulated by high glucose and glibenclamide were measured. Inhibition of nuclear factor kappa B (NF-κB activation induced by IL-1β and IFN-γ was investigated. Results In alloxan-induced diabetic mouse model, AL-1 lowered blood glucose, increased insulin and prevented loss of beta cells and their dysfunction, stimulated glucose transport protein subtype 4 (GLUT4 membrane translocation in soleus muscles. Pretreatment of RIN-m cells with AL-1 prevented H2O2-induced cellular damage, quenched glucose and glibenclamide-stimulated reactive oxidative species production, and inhibited cytokine-stimulated NF-κB activation. Conclusion We have demonstrated that AL-1 had both hypoglycemic and beta cell protective effects which translated into antioxidant and NF-κB inhibitory activity. AL-1 is a potential new anti-diabetic agent.

  15. Amorfrutins are potent antidiabetic dietary natural products

    Science.gov (United States)

    Weidner, Christopher; de Groot, Jens C.; Prasad, Aman; Freiwald, Anja; Quedenau, Claudia; Kliem, Magdalena; Witzke, Annabell; Kodelja, Vitam; Han, Chung-Ting; Giegold, Sascha; Baumann, Matthias; Klebl, Bert; Siems, Karsten; Müller-Kuhrt, Lutz; Schürmann, Annette; Schüler, Rita; Pfeiffer, Andreas F. H.; Schroeder, Frank C.; Büssow, Konrad; Sauer, Sascha

    2012-01-01

    Given worldwide increases in the incidence of obesity and type 2 diabetes, new strategies for preventing and treating metabolic diseases are needed. The nuclear receptor PPARγ (peroxisome proliferator-activated receptor gamma) plays a central role in lipid and glucose metabolism; however, current PPARγ-targeting drugs are characterized by undesirable side effects. Natural products from edible biomaterial provide a structurally diverse resource to alleviate complex disorders via tailored nutritional intervention. We identified a family of natural products, the amorfrutins, from edible parts of two legumes, Glycyrrhiza foetida and Amorpha fruticosa, as structurally new and powerful antidiabetics with unprecedented effects for a dietary molecule. Amorfrutins bind to and activate PPARγ, which results in selective gene expression and physiological profiles markedly different from activation by current synthetic PPARγ drugs. In diet-induced obese and db/db mice, amorfrutin treatment strongly improves insulin resistance and other metabolic and inflammatory parameters without concomitant increase of fat storage or other unwanted side effects such as hepatoxicity. These results show that selective PPARγ-activation by diet-derived ligands may constitute a promising approach to combat metabolic disease. PMID:22509006

  16. Prescribing of Antidiabetic Medicines before, during and after Pregnancy

    DEFF Research Database (Denmark)

    Charlton, Rachel A; Klungsøyr, Kari; Neville, Amanda J

    2016-01-01

    AIM: To explore antidiabetic medicine prescribing to women before, during and after pregnancy in different regions of Europe. METHODS: A common protocol was implemented across seven databases in Denmark, Norway, The Netherlands, Italy (Emilia Romagna/Tuscany), Wales and the rest of the UK. Women...

  17. Contrast agents for cardiac angiography: effects of a nonionic agent vs. a standard ionic agent

    International Nuclear Information System (INIS)

    Bettmann, M.A.; Bourdillon, P.D.; Barry, W.H.; Brush, K.A.; Levin, D.C.

    1984-01-01

    The effects on cardiac hemodynamics and of a standard contrast agent, sodium methylglucamine diatrizoate [Renografin 76] were compared with the effects of a new nonionic agent (iohexol) in a double-blind study in 51 patietns undergoing coronary angiography and left ventriculography. No significant alteration in measured blood parameters occurred with either contrast agent. Hemodynamic changes occurred with both, but were significantly greater with the standard renografin than with the low-osmolality, nonionic iohexol. After left ventriculography, heart rate increased and peripheral arterial pressure fell with both agents, but less with iohexol. It is concluded that iohexol causes less alteration in cardiac function than does the agent currently most widely used. Nonionic contrast material is likely to improve the safety of coronary angiography, particularly in those patients at greatest risk

  18. 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.

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

    Science.gov (United States)

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

    2017-01-01

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

  20. Preliminary evaluation of the encapsulation of new antidiabetic sulphonylhydrazone and antitumor N-acylhydrazone derivatives using PLGA nanoparticles

    International Nuclear Information System (INIS)

    Costa, F N; Ibiapino, A L; De Figueiredo, L P; De Castro, C E; Giacomelli, F C; Ferreira, F F; Barreiro, E J; Lima, L M; Do Amaral, D N

    2015-01-01

    It has been demonstrated the feasibly of using PLGA nanoparticles to promote the encapsulation of novel anti-diabetic sulphonylhydrazone and antitumor N-acylhydrazone derivatives. The motivation is to further demonstrate the possibility of long-term release of anti-diabetic as well as higher accumulation of the antitumor derivative by using the nanotechnology-based production. The produced nanoparticles were obtained by the nanoprecipitation method, which revealed to be effective in the encapsulation of the bioactive compounds. The determined sizes were in the range of ∼100 nm, which are supposed to be suitable for both potential applications. The preliminary experimental data demonstrated the formation of stable nanosystems and further experiments are underway in order to determine the loading content, encapsulation efficiency and release profile of the hydrophobic bioactive compounds. (paper)

  1. Antidiabetic and Renoprotective Effects of Cladophora glomerata Kützing Extract in Experimental Type 2 Diabetic Rats: A Potential Nutraceutical Product for Diabetic Nephropathy

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    Chutima Srimaroeng

    2015-01-01

    Full Text Available Cladophora glomerata extract (CGE has been shown to exhibit antigastric ulcer, anti-inflammatory, analgesic, hypotensive, and antioxidant activities. The present study investigated antidiabetic and renoprotective effects of CGE in type 2 diabetes mellitus (T2DM rats. The rats were induced by high-fat diet and streptozotocin and supplemented daily with 1 g/kg BW of CGE for 12 weeks. The renal transport function was assessed by the uptake of para-aminohippurate mediated organic anion transporters 1 (Oat1 and 3 (Oat3, using renal cortical slices. These two transporters were known to be upregulated by insulin and PKCζ while they were downregulated by PKCα activation. Compared to T2DM, CGE supplemented rats had significantly improved hyperglycaemia, hypertriglyceridemia, insulin resistance, and renal morphology. The baseline uptake of para-aminohippurate was not different among experimental groups and was correlated with Oat1 and 3 mRNA expressions. Nevertheless, while insulin-stimulated Oat1 and 3 functions in renal slices were blunted in T2DM rats, they were improved by CGE supplementation. The mechanism of CGE-restored insulin-stimulated Oat1 and 3 functions was clearly shown to be associated with upregulated PKCζ and downregulated PKCα expressions and activations. These findings indicate that CGE has antidiabetic effect and suggest it may prevent diabetic nephropathy through PKCs in a T2DM rat model.

  2. Antidiabetic and renoprotective effects of Cladophora glomerata Kützing extract in experimental type 2 diabetic rats: a potential nutraceutical product for diabetic nephropathy.

    Science.gov (United States)

    Srimaroeng, Chutima; Ontawong, Atcharaporn; Saowakon, Naruwan; Vivithanaporn, Pornpun; Pongchaidecha, Anchalee; Amornlerdpison, Doungporn; Soodvilai, Sunhapas; Chatsudthipong, Varanuj

    2015-01-01

    Cladophora glomerata extract (CGE) has been shown to exhibit antigastric ulcer, anti-inflammatory, analgesic, hypotensive, and antioxidant activities. The present study investigated antidiabetic and renoprotective effects of CGE in type 2 diabetes mellitus (T2DM) rats. The rats were induced by high-fat diet and streptozotocin and supplemented daily with 1 g/kg BW of CGE for 12 weeks. The renal transport function was assessed by the uptake of para-aminohippurate mediated organic anion transporters 1 (Oat1) and 3 (Oat3), using renal cortical slices. These two transporters were known to be upregulated by insulin and PKCζ while they were downregulated by PKCα activation. Compared to T2DM, CGE supplemented rats had significantly improved hyperglycaemia, hypertriglyceridemia, insulin resistance, and renal morphology. The baseline uptake of para-aminohippurate was not different among experimental groups and was correlated with Oat1 and 3 mRNA expressions. Nevertheless, while insulin-stimulated Oat1 and 3 functions in renal slices were blunted in T2DM rats, they were improved by CGE supplementation. The mechanism of CGE-restored insulin-stimulated Oat1 and 3 functions was clearly shown to be associated with upregulated PKCζ and downregulated PKCα expressions and activations. These findings indicate that CGE has antidiabetic effect and suggest it may prevent diabetic nephropathy through PKCs in a T2DM rat model.

  3. The effectiveness testing of oil spill-treating agents

    International Nuclear Information System (INIS)

    Fingas, M.F.; Kyle, D.A.; Laroche, N.; Fieldhouse, B.; Sergy, G.; Stoodley, G.

    1995-01-01

    Laboratory effectiveness tests have been developed for four classes of oil spill treating agents: solidifiers, demulsifying agents, surface-washing agents and dispersants. Several treating agent products in these four categories have been tested for effectiveness. The aquatic toxicity of these agents is an important factor and has been measured for many products. These results are presented. Solidifiers or gelling agents solidify oil. Test results show that solidifiers require between 16% and 200% of agent by weight compared to the oil. De-emulsifying agents or emulsion breakers prevent the formation of or break water-in-oil emulsions. Surfactant-containing materials are of two types, surface-washing agents and dispersants. Testing has shown that effectiveness is orthogonal for these two types of treating agents. Tests of surface washing agents show that only a few agents have effectiveness of 25 to 55%, where this is defined as the percentage of oil removed from a test surface. Dispersant effectiveness results using the swirling flask test are reported. Heavy oils show effectiveness values of about 1%, medium crudes of about 10%, light crude oils of about 30% and very light oils of about 90%

  4. Changes in Adenosine Deaminase Activity in Patients with Type 2 Diabetes Mellitus and Effect of DPP-4 Inhibitor Treatment on ADA Activity

    Science.gov (United States)

    Lee, Jae-Geun; Kang, Dong Gu; Yu, Jung Re; Kim, Youngree; Kim, Jinsoek; Koh, Gwanpyo

    2011-01-01

    Background Dipeptidyl peptidase 4 (DPP-4, also known as CD26) binds with adenosine deaminase (ADA) to activate T lymphocytes. Here, we investigated whether ADA activity is specifically affected by treatment with DPP-4 inhibitor (DPP4I) compared with other anti-diabetic agents. Methods Fasting ADA activity, in addition to various metabolic and biochemical parameters, were measured in 262 type 2 diabetes mellitus (T2DM) patients taking various anti-diabetic agents and in 46 non-diabetic control subjects. Results ADA activity was increased in T2DM patients compared with that in non-diabetic control subjects (mean±standard error, 23.1±0.6 U/L vs. 18.6±0.8 U/L; PADA activity was correlated with fasting plasma glucose (r=0.258, P9%) showed significantly increased ADA activity (21.1±0.8 U/L vs. 25.4±1.6 U/L; PADA activity in T2DM patients did not differ from those of other oral anti-diabetic agents or insulin. T2DM patients on metformin monotherapy showed a lower ADA activity (20.9±1.0 U/L vs. 28.1±2.8 U/L; PADA activity is increased in T2DM patients compared to that in non-diabetic patients, is positively correlated with blood glucose level, and that DPP4I has no additional specific effect on ADA activity, except for a glycemic control- or HbA1c-dependent effect. PMID:21738897

  5. Changes in Adenosine Deaminase Activity in Patients with Type 2 Diabetes Mellitus and Effect of DPP-4 Inhibitor Treatment on ADA Activity.

    Science.gov (United States)

    Lee, Jae-Geun; Kang, Dong Gu; Yu, Jung Re; Kim, Youngree; Kim, Jinsoek; Koh, Gwanpyo; Lee, Daeho

    2011-04-01

    Dipeptidyl peptidase 4 (DPP-4, also known as CD26) binds with adenosine deaminase (ADA) to activate T lymphocytes. Here, we investigated whether ADA activity is specifically affected by treatment with DPP-4 inhibitor (DPP4I) compared with other anti-diabetic agents. Fasting ADA activity, in addition to various metabolic and biochemical parameters, were measured in 262 type 2 diabetes mellitus (T2DM) patients taking various anti-diabetic agents and in 46 non-diabetic control subjects. ADA activity was increased in T2DM patients compared with that in non-diabetic control subjects (mean±standard error, 23.1±0.6 U/L vs. 18.6±0.8 U/L; PADA activity was correlated with fasting plasma glucose (r=0.258, P9%) showed significantly increased ADA activity (21.1±0.8 U/L vs. 25.4±1.6 U/L; PADA activity in T2DM patients did not differ from those of other oral anti-diabetic agents or insulin. T2DM patients on metformin monotherapy showed a lower ADA activity (20.9±1.0 U/L vs. 28.1±2.8 U/L; PADA activity is increased in T2DM patients compared to that in non-diabetic patients, is positively correlated with blood glucose level, and that DPP4I has no additional specific effect on ADA activity, except for a glycemic control- or HbA1c-dependent effect.

  6. Antidiabetic, hypolipidemic and hepatoprotective effects of Arctium lappa root’s hydro-alcoholic extract on nicotinamide-streptozotocin induced type 2 model of diabetes in male mice

    Directory of Open Access Journals (Sweden)

    Akram Ahangarpour

    2017-02-01

    Full Text Available Objective: Arctium lappa (burdock, (A. lappa root has hypoglycemic and antioxidative effects, and has been used for treatment of diabetes in tradition medicine. This study was conducted to evaluate the antidiabetic and hypolipidemic properties of A. lappa root extract on nicotinamide-streptozotocin (NA-STZ-induced type2 diabetes in mice.Materials and Methods: In this investigation, 70 adult male NMRI mice (30-35g randomly divided into 7 groups (n=10 as follow: 1-control, 2-type 2 diabetic mice, 3-diabetic mice that received glibenclamide (0.25 mg/kg as an anti-diabetic drug, 4, 5, 6 and 7- diabetic and normal animals that were pre-treated with 200 and 300 mg/kg A. lappa root extract, respectively, for 28 days. Diabetes has been induced by intraperitoneal injection of NA and STZ. Finally, the blood sample was taken and insulin, glucose, SGOT, SGPT, alkaline phosphatase, leptin and lipid levels was evaluated.Results: Induction of diabetes decreased the level of insulin, leptin and high density lipoprotein (HDL and increased the level of other lipids, glucose, and hepatic enzymes significantly (p

  7. Synthesis and in vitro antidiabetic activity of some alkyl carbazole ...

    African Journals Online (AJOL)

    admin

    ... or their institutions for access and distributed under the terms of the Creative Commons Attribution License ... Thus, the search for new leads for antidiabetic drugs with lower ... precoated plate (0.25mm) using toluene: ethyl acetate (7:2v/v) as ...

  8. The kidney as a new target for antidiabetic drugs: SGLT2 inhibitors.

    Science.gov (United States)

    Cangoz, S; Chang, Y-Y; Chempakaseril, S J; Guduru, R C; Huynh, L M; John, J S; John, S T; Joseph, M E; Judge, R; Kimmey, R; Kudratov, K; Lee, P J; Madhani, I C; Shim, P J; Singh, S; Singh, S; Ruchalski, C; Raffa, R B

    2013-10-01

    A novel class of antidiabetic drugs - SGLT2 (Na(+) /glucose cotransporter type 2) inhibitors - target renal reabsorption of glucose and promote normal glucose levels, independent of insulin production or its action at receptors. We review this new mechanistic approach and the reported efficacy and safety of clinical testing of lead compounds. Information was obtained from various bibliographic sources, including PubMed and others, on the basic science and the clinical trials of SGLT2 inhibitors. The information was then summarized and evaluated from the perspective of contribution to a fuller understanding of the potential and current status of the lead clinical candidates. Diabetes mellitus is a spectrum of disorders that involves inadequate insulin function resulting in adverse health sequelae due to acute and chronic hyperglycaemia. Current antidiabetic pharmacotherapy primarily addresses either insulin production at the pancreatic β-cells or insulin action at insulin receptors. These drugs have less than full clinical effectiveness and sometimes therapy-limiting adverse effects. The third major component of glucose balance, namely elimination, has not been a significant therapeutic target to date. SGLT2 inhibitors are a novel approach. A sufficient number of clinical trials have been conducted on sufficiently chemically diverse SGLT2 inhibitors to reasonably conclude that they have efficacy (HbA1c reductions of 0·4-1%), and thus far, the majority of adverse effects have been mild and transitory or treatable, with the caveat of possible association with increased risk of breast cancer in women and bladder cancer in men. © 2013 John Wiley & Sons Ltd.

  9. How to fight obesity with antidiabetic drugs: targeting gut or kidney?

    Science.gov (United States)

    Baretić, M; Troskot, R

    2015-03-01

    The increased prevalence of type 2 diabetes follows the increased prevalence of obesity. Both diseases share common pathophysiological pathways; obesity is in most cases the first step, whereas diabetes is the second one. Weight gain occurs during the treatment of diabetes with drugs causing endogenous or exogenous hyperinsulinemia. Insulin and sulfonylurea are making patients more obese and more insulin resistant. Glucagon-like peptide-1 receptor agonists (GLP-1 agonists) and sodium/glucose cotransporter 2 inhibitors (SGLT2 inhibitors) are antidiabetic drugs with weight loss property. GLP-1 agonists mimic an incretin action. They release insulin after a meal during hyperglycemia and suppress glucagon. The weight loss effect is a consequence of central action increased satiety. Some of GLP-1 agonists weight loss is a result of decelerated gastric emptying rate. SGLT2 inhibitors block sodium glucose cotransporter in proximal tubule brush border and produce glucose excretion with urinary loss. Urinary glucose leak results in calories and weight loss. Even a modest weight loss has positive outcome on metabolic features of diabetic patient; such drugs have important role in treatment of type 2 diabetic patients. However, there are some still unresolved questions. The weight loss they produce is modest. Those drugs are expensive and not available to many diabetic patients, they are significantly more expensive compared to "traditional" hypoglycemic drugs. The hypoglycemic endpoint of GLP-1 agonists and SGLT2 inhibitors often requires adding another antidiabetic drug. The most radical and most effective therapy of type 2 diabetes and obesity is bariatric surgery having significant number of diabetes remission.

  10. Phytochemical screening and study of antioxidant, antimicrobial, antidiabetic, anti-inflammatory and analgesic activities of extracts from stem wood of Pterocarpus marsupium Roxburgh.

    Science.gov (United States)

    Pant, Dipak Raj; Pant, Narayan Dutt; Saru, Dil Bahadur; Yadav, Uday Narayan; Khanal, Dharma Prasad

    2017-01-01

    The main aims of the study were to evaluate the phytochemical constituents and to study the antioxidant, antimicrobial, antidiabetic, anti-inflammatory, and analgesic activities of extracts from stem wood of Pterocarpus marsupium . Ethanol, acetone and isopropyl alcohol (IPA) (1:1) extracts of stem wood of P. marsupium were subjected to phytochemical screening and analysis of biological activities from August 2015 to January 2016. The antioxidant assay was carried out using 2, 2-diphenyl-1-picrylhydrazyl scavenging method, antimicrobial activity testing by cup diffusion method, antidiabetic test evaluation by oral glucose tolerance test in mice, anti-inflammatory effect was evaluated by hind paw edema method in mice and analgesic test evaluation by a chemical writhing method in mice. The results of the study revealed that P. marsupium is a source of various phytoconstituents such as alkaloids, glycosides, saponins, tannins, proteins, carbohydrates, cardiac glycosides, flavonoids, and terpenoids. Both the acetone and IPA extract as well as the ethanol extract of stem wood of P. marsupium exhibited a dose-dependent antioxidant activity. Acetone and IPA extract showed antibacterial activity against Gram-positive bacteria, while the ethanolic extract was found to possess antidiabetic activity. The antidiabetic activity of the extract was found to be time and dose-dependent. Similarly, the acetone and IPA extract was found to have anti-inflammatory activity, which was also time and dose-dependent. Furthermore, the ethanolic extract showed analgesic activity, which was dose-dependent. The ethanolic extract was found to be nontoxic. Thus, this study laid sufficient background for the further research on extracts from stem wood of P. marsupium for identification, subsequent purification and isolation of compounds having antibacterial, antidiabetic, anti-inflammatory, and analgesic activities.

  11. Redox properties of ginger extracts: Perspectives of use of Zingiber officinale Rosc. as antidiabetic agent.

    Science.gov (United States)

    Račková, Lucia; Cupáková, Máriá; Tažký, Anton; Mičová, Júlia; Kolek, Emil; Košt'álová, Daniela

    2013-03-01

    In traditional medicine, several medicinal plants or their extracts have been used to treat diabetes. Zingiber officinale Roscoe, known commonly as ginger, is consumed worldwide in cookeries as a spice and flavouring agent. It has been used as the spice and medicine for thousands of years. The present study was undertaken to investigate the potential protective effect of Zingiber officinale Rosc. in a model of oxidative damage to pancreatic β cells. The free radical scavenging activities and composition of the isolated n-hexane and ethanolic extracts were confronted with their protective, antioxidant and cytotoxic effects in INS-1E β cells. Unlike the n-hexane extract (exerting, paradoxically, stronger antiradical capacity), both low cytotoxicity and remarkable protective effects on β cell viability, followed by lowering oxidative stress markers were found for the ethanolic extract Zingiber officinale Rosc. The present study is the first pilot study to assess the protective potential of Zingiber officinale Rosc. in a model of cytotoxic conditions imposed by diabetes in β cells.

  12. Antidiabetic Effect of Brain-Derived Neurotrophic Factor and Its Association with Inflammation in Type 2 Diabetes Mellitus

    Directory of Open Access Journals (Sweden)

    Ceren Eyileten

    2017-01-01

    Full Text Available Brain-derived neurotrophic factor (BDNF is a neurotrophin, which plays an important role in the central nervous system, and systemic or peripheral inflammatory conditions, such as acute coronary syndrome and type 2 diabetes mellitus (T2DM. BDNF is also expressed in several nonneuronal tissues, and platelets are the major source of peripheral BDNF. Here, we reviewed the potential role of BDNF in platelet reactivity in T2DM and its association with selected inflammatory and platelet activation mediators. Besides that, we focused on adipocytokines such as leptin, resistin, and adiponectin which are considered to take part in inflammation and both lipid and glucose metabolism in diabetic patients as previous studies showed the relation between adipocytokines and BDNF. We also reviewed the evidences of the antidiabetic effect of BDNF and the association with circulating inflammatory cytokines in T2DM.

  13. The antidiabetic action of camel milk in experimental type 2 diabetes mellitus: an overview on the changes in incretin hormones, insulin resistance, and inflammatory cytokines.

    Science.gov (United States)

    Korish, A A

    2014-06-01

    Folk medicine stories accredited the aptitude of camel milk (CMK) as a hypoglycemic agent and recent studies have confirmed this in the diabetic patients and experimental animals. However, the mechanism(s) by which CMK influences glucose homeostasis is yet unclear. The current study investigated the changes in the glucose homeostatic parameters, the incretin hormones, and the inflammatory cytokines in the CMK-treated diabetic animals. A model of type 2 diabetes mellitus was induced in rats by intraperitoneal injection of streptozotocin 40 mg/kg/day for 4 repeated doses. Camel milk treatment was administered for 8 weeks. The changes in glucagon like peptide-1 (GLP-1), glucose dependent insulinotropic peptide (GIP), glucose tolerance, fasting and glucose-stimulated insulin secretion, insulin resistance (IR), TNF-α, TGF-β1, lipid profile, atherogenic index (AI), and body weight were investigated. The untreated diabetic animals showed hyperglycemia, increased HOMA-IR, hyperlipidemia, elevated AI, high serum incretins [GLP-1 and GIP], TNF-α, and TGF-β1 levels and weight loss as compared with the control group. Camel milk treatment to the diabetic animals resulted in significant lowered fasting glucose level, hypolipidemia, decreased HOMA-IR, recovery of insulin secretion, weight gain, and no mortality during the study. Additionally, CMK inhibits the diabetes-induced elevation in incretin hormones, TNF-α and TGF-β1 levels. The increase in glucose-stimulated insulin secretion, decreased HOMA-IR, modulation of the secretion and/or the action of incretins, and the anti-inflammatory effect are anticipated mechanisms to the antidiabetic effect of CMK and suggest it as a valuable adjuvant antidiabetic therapy. © Georg Thieme Verlag KG Stuttgart · New York.

  14. Comparative study of the hypocholesterolemic, antidiabetic effects of four agro-waste Citrus peels cultivars and their HPLC standardization

    Directory of Open Access Journals (Sweden)

    Nesrin M. Fayek

    Full Text Available ABSTRACT Citrus is an economically important fruit for Egypt, but its peel also is one of the major sources of agricultural waste. Due to its fermentation, this waste causes many economic and environmental problems. Therefore it is worthwhile to investigate ways to make use of this citrus waste generated by the juice industry. This study was aimed to explore the hypocholesterolemic, antidiabetic activities of four varieties of citrus peels agrowastes, to isolate the main flavonoids in the active fractions and to quantify them by HPLC method for nutraceutical purposes. All the tested samples of the agro-waste Citrus fruits peels showed significant decrease in cholesterol, triacylglyceride and glucose. The most decrease in cholesterol level was observed by mandarin peels aqueous homogenate and its hexane fraction (59.3% and 56.8%, respectively reaching the same effect as the reference drug used (54.7%. Mostly, all samples decrease triacylglyceride (by 36%–80.6% better than the reference drug used (by 35%, while, glucose was decreased (by 71.1%–82.8 and 68.6%–79.6%, respectively mostly by the aqueous homogenates (except lime and alcoholic extracts (except mandarin of Citrus fruits peels better than the reference drug used (by 68.3%. All the isolated pectin, from the four cultivars, has significant effect on the three parameters. The comparative HPLC rapid quantification of nobiletin in the different by-product citrus varieties hexane fractions revealed that nobiletin is present in higher concentration in mandarin (10.14% than the other species. Nobiletin and 4′,5,7,8-tetramethoxy flavone were isolated from mandarin peels hexane fraction by chromatographic fractionation. This is the first report of the comparative HPLC quantification of nobiletin and biological studies of different citrus peels species as agro-waste products. Based on these results, we suggest the possibility that Citrus fruits peels may be considered as an antidiabetic and

  15. Oxidative stress and expression of insulin signaling proteins in the brain of diabetic rats: Role of Nigella sativa oil and antidiabetic drugs.

    Science.gov (United States)

    Balbaa, Mahmoud; Abdulmalek, Shaymaa A; Khalil, Sofia

    2017-01-01

    oxidative stress, the pro-inflammatory mediators and amyloidogenic pathway. Moreover, it lowers the insulin receptor inhibitory effect of IOMe-AG538 and modifies the insulin-signaling pathway. Therefore, it prevents the neurotoxicity, amyloid plaque formation and Tau hyper-phosphorylation and restores AD-related miRNA normal levels. These data suggest that NSO or its combined treatments with anti-diabetic drugs have a possible benefit as disease modifying agents for the insulin resistance in the brain through enhancing brain insulin signaling pathway.

  16. Strychnos nux-vomica seeds: Pharmacognostical standardization, extraction, and antidiabetic activity

    Directory of Open Access Journals (Sweden)

    Rajesh Bhati

    2012-01-01

    Full Text Available Background: Strychnos nux-vomica, commonly known as kuchla, contains strychnine and brucine as main constituents. Minor alkaloids present in the seeds are protostrychnine, vomicine, n-oxystrychnine, pseudostrychnine, isostrychnine, chlorogenic acid, and a glycoside. Seeds are used traditionally to treat diabetes, asthma, aphrodisiac and to improve appetite. Objective: The present study was aimed to evaluate the various pharmacognostical characters and antidiabetic activity of S. nux-vomica seed. Materials and Methods: Pharmacognostical characters were performed as per the WHO guideline. Extraction was carried out in petroleum ether, chloroform, alcohol, hydroalcoholic, aqueous, and phytochemical constituents present in extracts were detected by different chemical tests. Among these extracts hydroalcoholic, aqueous extracts were evaluated for antidiabetic activity on the basis of extractive yield and phytoconstituents, in alloxan-induced diabetic rats using gliclazide as standard. Results: Various analytical values of S. nux-vomica extract were established. Phytoconstituents present in S. nux-vomica extracts were detected. Conclusion: S. nux-vomica extracts show antihyperglycemic activity in experimental animals.

  17. Pharmacognostical Standardization of Upodika- Basella alba L.: An Important Ayurvedic Antidiabetic Plant

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    T R Shantha

    2016-01-01

    Full Text Available Objective: To establish the pharmacognostic standards for the correct identification and standardization of an important Antidiabetic plant described in Ayurveda. Materials and Methods: Standardization was carried out on the leaf and stem of Basella alba L. with the help of the macro-morphological, microscopic, physicochemical and qualitative phytochemical studies. Results: Several specific characters were identified viz. clustered calcium oxalate crystals in the cortex region, absence of trichomes, succulent, thick, mucilaginous, fibrous stem. Rubiaceous type of stomata on both sides of the leaf. Quantitative microscopy along with physicochemical and qualitative phytochemical analysis were also established. Conclusion: The pharmacognostic standards could serve as the reference for the proper identification of the Basella alba L. which is an important anti-diabetic plant described in Ayurveda.

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

    Science.gov (United States)

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

    2016-12-01

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

  19. Epifluorescent imaging study of the effect of anti-diabetic drug metformin on colorectal cancer cell lines in vitro

    Directory of Open Access Journals (Sweden)

    Venkatasubramani P

    2017-12-01

    Full Text Available Metformin, a widely used anti-diabetic drug, has recently been associated with inhibition of cell proliferation in multiple cancers. However, it is not clear if the reduction in proliferation on treatment with metformin is a result of cell death or slowdown in the rate of growth of cancer cells, because cell viability assays measure only the number of cells at the beginning and end of the experiment. The aim of this study is to utilize a fluorescent imaging technique to directly follow cell death overtime in order to investigate the effect of metformin on colorectal cancer cells HCT116 and SW480. Epifluorescent imaging analysis carried out using ImageXpress Micro XLS High-Content Imaging System show that there is no significant change in cell death observed in the cancer cell lines, as compared to the control, over multiple closely spaced time points, suggesting that metformin in pharmacological doses may not be an effective inducer of cell death in these colon cancer cell lines.

  20. Evaluating the Effect of Ramadan Fasting on Muslim Patients with Diabetes in relation to Use of Medication and Lifestyle Patterns: A Prospective Study

    Directory of Open Access Journals (Sweden)

    Melanie Yee Lee Siaw

    2014-01-01

    Full Text Available Objectives. This study aimed to examine the effect of Ramadan fasting on HbA1c in Muslim patients with type 2 diabetes. The incidence of hypoglycemia and glycemic changes in relation to the adjustment of doses of antidiabetic agents, diet, and physical activity during Ramadan was also evaluated. Methods. This was a prospective study conducted in an outpatient endocrine clinic. A set of questionnaires was administered to Muslim patients with diabetes who fasted for ≥10 days. Those who were hospitalized for diabetic ketoacidosis or severe hypoglycemia a month prior to Ramadan or were given short-term corticosteroid therapy were excluded. The patients’ responses and clinical outcomes from the clinic database were collected before, during, and after Ramadan. Results. A total of 153 participants completed the study. The mean HbA1c improved from 8.9% before Ramadan to 8.6% during Ramadan (P<0.05. Although diet and physical activity did not contribute to changes in glycemia, a significant improvement in HbA1c was observed in patients who had adjustments made to their doses of antidiabetic agents during Ramadan (P<0.001. In addition, their rate of hypoglycemia was minimal. Conclusions. Ramadan fasting appeared to improve glycemic control, especially in those whose doses of antidiabetic agents were adjusted during Ramadan.

  1. Evaluation of antidiabetic, antioxidant and antiglycating activities of the Eysenhardtia polystachya

    Science.gov (United States)

    Gutierrez, Rosa Martha Perez; Baez, Efren Garcia

    2014-01-01

    Background: Many diseases are associated with oxidative stress caused by free radicals. The aim of the present study was to evaluate the antidiabetic, antioxidant and antiglycation properties of Eysenhardtia polystachya (EP) bark methanol-water extract. Materials and Methods : The antioxidant capacities were evaluated by studying in vitro the scavenging of DPPH and ABTS free radical, reactive oxygen species such as RO2, O2·-, H2O2, OH., H2O2, ONOO-, NO, HOCl,1 O2, chelating ability, ORAC, β-carotene-bleaching and lipid peroxidation. The antiglycation activities of EP were evaluated by haemoglobin, bovine serum albumin (BSA)-glucose, BSA-methylglyoxal and BSA-glucose assays. Oral administration of EP at the doses of 100 mg/kg, 200 mg/kg and 400 mg/g was studied in normal, glucose-loaded and antidiabetic effects on streptozotocin-induced mildly diabetic (MD) and severely diabetic (SD) mice. Results: EP showed Hdonor activity, free radical scavenging activity, metal chelating ability and lipid peroxidation Antioxidant activity may be attributed to the presence of phenolic and flavonoid compounds. EP is an inhibitor of fluorescent AGE, methylglyoxal and the glycation of haemoglobin. In STZ-induced diabetic mice, EP reduced the blood glucose, increased serum insulin, body weight, marker enzymes of hepatic function, glycogen, HDL, GK and HK while there was reduction in the levels of triglyceride, cholesterol, TBARS, LDL and G6Pase. Conclusions: Eysenhardtia polystachya possesses considerable antioxidant activity with reactive oxygen species (ROS) scavenging activity and demonstrated an anti-AGEs and hepatoprotective role, inhibits hyperglycemic, hyperlipidemic and oxidative stress indicating that these effects may be mediated by interacting with multiple targets operating in diabetes mellitus. PMID:24991120

  2. Clinical usage of hypolipidemic and antidiabetic drugs in the prevention and treatment of cancer.

    Science.gov (United States)

    Berstein, Lev M

    2005-06-28

    Factors predisposing hormone-dependent tissues to the development of tumors coincide, at least partly, with hormonal-metabolic promoters (like insulin resistance, glucose intolerance, visceral obesity, etc.) of other main non-communicable diseases. This important knowledge poses the question of whether the same approach which is applied for prevention/treatment of a metabolic syndrome and the associated endocrine disorders might also be used in preventive and therapeutic oncology. Whereas an answer to this question remains controversial and is based mainly on experimental evidence, there is accumulating clinical data suggesting a practical significance of such a strategy, even though it is not to be considered as directly cytostatic. Among the many drugs under discussion, three groups of medicines (statins, antidiabetic biguanides, and thiazolidinediones) are the most attractive. The concept of metabolic rehabilitation is proposed and used practically in an adjuvant setting for the correction of the above-mentioned endocrine-metabolic disorders commonly found in cancer patients. The current use and aim of this approach is to improve the survival of patients and limit cancer progression. Nonetheless, it also appears potentially useful as a neoadjuvant therapy as well as a prophylactic treatment earlier in life for specific groups of people with hormone-associated enhanced oncological risk. It seems possible that certain hypolipidemic and antidiabetic medicines with pleiotropic effects might be combined with traditional antisteroid prevention/therapeutic approaches in routine clinical situations as well as for overcoming resistance to standard cancer hormonal therapies including receptor-negative cases. Characteristic at the end of the 20th and at the beginning of the 21st century is an epidemic of diabetes and obesity, which might further increase the incidence of certain cancers. This makes it timely to apply hypolipidemic and antidiabetic drugs (in combination

  3. Trivaric acid, a new inhibitor of PTP1b with potent beneficial effect on diabetes.

    Science.gov (United States)

    Sun, Wenlong; Zhang, Bowei; Zheng, Haizhou; Zhuang, Chunlin; Li, Xia; Lu, Xinhua; Quan, Chunshan; Dong, Yuesheng; Zheng, Zhihui; Xiu, Zhilong

    2017-01-15

    To screen a potential PTP1b inhibitor from the microbial origin-based compound library and to investigate the potential anti-diabetic effects of the inhibitor in vivo and determine its primary anti-diabetic mechanism in vitro and in silico. PTP1b inhibitory activity was measured using recombination protein as the enzyme and p-NPP as the substrate. The binding of the inhibitor to PTP1b was analysed by docking in silico and confirmed by ITC experiments. The intracellular signalling pathway was detected by Western blot analysis in HepG2 cells. The anti-diabetic effects were evaluated using a diabetic mice model in vivo. Among 545 microbial origin-based pure compounds tested, trivaric acid, a tridepside, was selected as a PTP1B inhibitor exhibiting strong inhibitory activity with an IC 50 of 173nM. Docking and ITC studies showed that trivaric acid was able to spontaneously bind to PTP1b and may inhibit PTP1b by blocking the catalytic domain of the phosphatase. Trivaric acid also enhanced the ability of insulin to stimulate the IR/IRS/Akt/GLUT2 pathway and increase the glucose consumption in HepG2 cells. In diabetic mice, trivaric acid that had been encapsulated into Eudrgit L100-5.5 showed significant anti-diabetic effects, improving insulin resistance, leptin resistance and lipid profile and weight control at doses of 5mg/kg and 50mg/kg. Trivaric acid is a potential lead compound in the search for anti-diabetic agents targeting PTP1b. Copyright © 2016 Elsevier Inc. All rights reserved.

  4. Synthesis and antidiabetic activity of β-acetamido ketones

    Directory of Open Access Journals (Sweden)

    Xing-hua Zhang

    2011-08-01

    Full Text Available This paper reports the use of trifluoroacetic acid as a catalyst in the Dakin–West reaction for the synthesis of β-acetamido ketones. The method has several advantages such as requiring only mild conditions and a low concentration of catalyst. Screening of 19 β-acetamido ketones for antidiabetic activity in vitro showed that their activity as peroxisome proliferator-activated receptor (PPAR agonists and as dipeptidyl peptidase 4 (DPP-IV inhibitors was fairly weak.

  5. Treating Diet-Induced Diabetes and Obesity with Human Embryonic Stem Cell-Derived Pancreatic Progenitor Cells and Antidiabetic Drugs

    Directory of Open Access Journals (Sweden)

    Jennifer E. Bruin

    2015-04-01

    Full Text Available Human embryonic stem cell (hESC-derived pancreatic progenitor cells effectively reverse hyperglycemia in rodent models of type 1 diabetes, but their capacity to treat type 2 diabetes has not been reported. An immunodeficient model of type 2 diabetes was generated by high-fat diet (HFD feeding in SCID-beige mice. Exposure to HFDs did not impact the maturation of macroencapsulated pancreatic progenitor cells into glucose-responsive insulin-secreting cells following transplantation, and the cell therapy improved glucose tolerance in HFD-fed transplant recipients after 24 weeks. However, since diet-induced hyperglycemia and obesity were not fully ameliorated by transplantation alone, a second cohort of HFD-fed mice was treated with pancreatic progenitor cells combined with one of three antidiabetic drugs. All combination therapies rapidly improved body weight and co-treatment with either sitagliptin or metformin improved hyperglycemia after only 12 weeks. Therefore, a stem cell-based therapy may be effective for treating type 2 diabetes, particularly in combination with antidiabetic drugs.

  6. Human Adipose-Derived Mesenchymal Stem Cells Respond to Short-Term Hypoxia by Secreting Factors Beneficial for Human Islets In Vitro and Potentiate Antidiabetic Effect In Vivo

    OpenAIRE

    Schive, Simen W.; Mirlashari, Mohammad Reza; Hasvold, Grete; Wang, Mengyu; Josefsen, Dag; Gullestad, Hans Petter; Korsgren, Olle; Foss, Aksel; Kvalheim, Gunnar; Scholz, Hanne

    2017-01-01

    Adipose-derived mesenchymal stem cells (ASCs) release factors beneficial for islets in vitro and protect against hyperglycemia in rodent models of diabetes. Oxygen tension has been shown to induce metabolic changes and alter ASCs? release of soluble factors. The effects of hypoxia on the antidiabetic properties of ASCs have not been explored. To investigate this, we incubated human ASCs for 48 h in 21% (normoxia) or 1% O2 (hypoxia) and compared viability, cell growth, surface markers, differe...

  7. Antidiabetic and Synergistic Effects of Anthocyanin Fraction from Berberis integerrima Fruit on Streptozotocin-Induced Diabetic Rats Model

    Directory of Open Access Journals (Sweden)

    Zahra Sabahi

    2016-03-01

    Full Text Available Diabetes mellitus is a complex endocrine disorder. There is a serious attempt to identify antidiabetic compounds from natural sources to use with other drugs for reduction of diabetes complications. Present study is based on the investigation of antihyperglycemic effect of anthocyanin fraction of Berberis integerrima Bunge (AFBI fruits on some physiological parameters (glucose level, glycogen content, and body weight in normal and streptozotocin-induced (STZ-induced diabetic rats and evaluation of synergic effect of this fraction with metformin and glibenclamide. Male Sprague dawley rats were divided into nine groups: healthy control group, diabetic control group, diabetic groups treated with anthocyanin fraction (200, 400 and 1000 mg/kg, respectively; diabetic groups treated with glibenclamide and metformin separately, diabetic groups treated with glibenclamide + anthocyanin fraction (1000 mg/kg, metformin + anthocyanin fraction (1000 mg/kg. Treatment of diabetic rats with AFBI (400, 1000mg/kg significantly decreased blood glucose as compared with control. Moreover, AFBI (400, 1000mg/kg significantly increased liver glycogen and body weight compared to control. Nevertheless, there were no synergistic effects between anthocyanin fraction and metformin or glibenclamide on blood glucose, liver glycogen, and body weight. The results of this study indicate that AFBI possesses hypoglycemic effects and may be considered for evaluation in future diabetes clinical studies.

  8. Assessment of antidiabetic activity and acute toxicity of leaf extracts from Physalis peruviana L. in guinea-pig

    Science.gov (United States)

    Kasali, Félicien Mushagalusa; Kadima, Justin Ntokamunda; Mpiana, Pius Tshimankinda; Ngbolua, Koto-te-Nyiwa; Tshibangu, Damien Sha-Tshibey

    2013-01-01

    Objective To verify the antidiabetic activity of leaf extracts from Physalis peruviana L. popularly used in the Eastern part of the Democratic Republic of the Congo and to point out the possible toxicity. Method Aqueous decoctions prepared from dried leaves powder were administrated to guinea pigs at the dose range of 100 mg/kg to 3.2 g/kg of body weight. The hypoglycemic activity was evaluated by glucose tolerance test, loading animals with glucose 4 g/kg and measuring blood glucose concentrations at various times. The effect was compared to the control and glibenclamide as antidiabetic reference drug. Acute toxicity was evaluated by recording mortality rate, changes on blood biomarkers and damage caused to vital organs. Results At a dose of 100 mg/kg, the aqueous extract induced a significant reduction of peak concentration at 30 min after glucose loading as compared with control or reference (PPhysalis peruviana L. present hypoglycemic activity in animal model, but at high doses the plant may cause severe intoxication.

  9. A comprehensive review on anti-diabetic property of rice bran

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    Bhagavathi Sundaram Sivamaruthi

    2018-01-01

    Full Text Available Rice bran (RB is one of the nutrient-rich agricultural byproducts. It is a composite of carbohydrates, lipids, proteins, fibers, minerals, and trace elements such as phosphorus, potassium, magnesium, calcium and manganese. The extraction and purification process influences the quality and quantity of rice bran oil, which is rich in tocopherols, tocotrienols, γ-oryzanol, and unsaturated fatty acids. The bioactive components of RB have been reported for exhibiting antioxidant, anti-inflammatory, hypocholesterolemic, anti-cancer, anti-colitis, and antidiabetic properties. In vitro and in vivo studies, and clinical trials in human volunteers revealed the anti-hyperglycemic activity of RB derived compounds. An updated comprehensive review on the antidiabetic property of RB and its derivative is required to appraise the current knowledge in the particular field. Thus, the present paper covered the composition and bioactivities of RB, and influence of extraction methods on the biological property of rice bran oil and rice bran extract. And the current review also focused on the reported anti-hyperglycemia activity of rice bran derivatives, and its probable mechanism.

  10. Anti-diabetic Potential of the Aqueous Leaf Extracts of Ocimum ...

    African Journals Online (AJOL)

    The anti-diabetic potential of aqueous extracts of leaves of both Ocimum gratissimum and Vernonia amygdalina were investigated in rabbits. Ten female rabbits were grouped into five groups (1-5) of two rabbits each. Group 1 is the control. Groups (2-5) was alloxan induced diabetic. Group 3 was then treated with 200mg/kg ...

  11. Dgroup: DG00113 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available n hydrochloride (JP17/USP) ... Antidiabetic agent ... DG01685 ... Insulin sensitizer ... DG01684 ... Biguanide antidiabetic... Unclassified ... DG02044 ... Hypoglycemics ... DG01684 ... Biguanide antidiabetic ATC code: A10BA02 Biganide antidiabetic

  12. Comparative efficacy and safety of antidiabetic drug regimens added to metformin monotherapy in patients with type 2 diabetes: a network meta-analysis.

    Directory of Open Access Journals (Sweden)

    Elizabeth S Mearns

    Full Text Available When first line therapy with metformin is insufficient for patients with type 2 diabetes (T2D, the optimal adjunctive therapy is unclear. We assessed the efficacy and safety of adjunctive antidiabetic agents in patients with inadequately controlled T2D on metformin alone.A search of MEDLINE and CENTRAL, clinicaltrials.gov, regulatory websites was performed. We included randomized controlled trials of 3-12 months duration, evaluating Food and Drug Administration or European Union approved agents (noninsulin and long acting, once daily basal insulins in patients experiencing inadequate glycemic control with metformin monotherapy (≥ 1500 mg daily or maximally tolerated dose for ≥ 4 weeks. Random-effects network meta-analyses were used to compare the weighted mean difference for changes from baseline in HbA1c, body weight (BW and systolic blood pressure (SBP, and the risk of developing hypoglycemia, urinary (UTI and genital tract infection (GTI.Sixty-two trials evaluating 25 agents were included. All agents significantly reduced HbA1c vs. placebo; albeit not to the same extent (range, 0.43% for miglitol to 1.29% for glibenclamide. Glargine, sulfonylureas (SUs and nateglinide were associated with increased hypoglycemia risk vs. placebo (range, 4.00-11.67. Sodium glucose cotransporter-2 (SGLT2 inhibitors, glucagon-like peptide-1 analogs, miglitol and empagliflozin/linagliptin significantly reduced BW (range, 1.15-2.26 kg whereas SUs, thiazolindinediones, glargine and alogliptin/pioglitazone caused weight gain (range, 1.19-2.44 kg. SGLT2 inhibitors, empagliflozin/linagliptin, liraglutide and sitagliptin decreased SBP (range, 1.88-5.43 mmHg. No therapy increased UTI risk vs. placebo; however, SGLT2 inhibitors were associated with an increased risk of GTI (range, 2.16-8.03.Adding different AHAs to metformin was associated with varying effects on HbA1c, BW, SBP, hypoglycemia, UTI and GTI which should impact clinician choice when selecting adjunctive

  13. Antidiabetic Activity of Aqueous Leaves Extract of Sesbania sesban (L) Merr. in Streptozotocin Induced Diabetic Rats

    Science.gov (United States)

    Pandhare, Ramdas B.; Sangameswaran, B.; Mohite, Popat B.; Khanage, Shantaram G.

    2011-01-01

    The aqueous leaves extract of Sesbania sesban (L) Merr. (Family: Fabaceae) was evaluated for its antidiabetic potential on normal and streptozotocin (STZ)-induced diabetic rats. In the chronic model, the aqueous extract was administered to normal and STZ- induced diabetic rats at the doses of 250 and 500 mg/kg body weight (b.w.) p.o. per day for 30 days. The fasting Blood Glucose Levels (BGL), serum insulin level and biochemical data such as glycosylated hemoglobin, Total Cholesterol (TC), Triglycerides (TG), High Density Lipoproteins (HDL) and Low Density Lipoproteins (LDL) were evaluated and all were compared to that of the known anti-diabetic drug glibenclamide (0.25 mg/kg b.w.). The statistical data indicated significant increase in the body weight, liver glycogen, serum insulin and HDL levels and decrease in blood glucose, glycosylated hemoglobin, total cholesterol and serum triglycerides when compared with glibenclamide. Thus the aqueous leaves extract of Sesbania sesban had beneficial effects in reducing the elevated blood glucose level and lipid profile of STZ-induced diabetic rats. PMID:23407749

  14. Antidiabetic Effects of Add-On Gynostemma pentaphyllum Extract Therapy with Sulfonylureas in Type 2 Diabetic Patients

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    V. T. T. Huyen

    2012-01-01

    Full Text Available Aims. To investigate the antidiabetic effect of the traditional Vietnamese herb Gynostemma pentaphyllum (GP together with sulfonylurea (SU in 25 drug-naïve type 2 diabetic patients. Methods. After 4-week treatment with gliclazide (SU, 30 mg daily, all patients were randomly assigned into 2 groups to add on GP extract or placebo extract, 6 g daily, during eight weeks. Results. After 4-week SU treatment, fasting plasma glucose (FPG and HbA1C decreased significantly (P<0.001. FPG was further reduced after add-on therapy with 2.9 ± 1.7 and 0.9 ± 0.6 mmol/L in the GP and placebo groups, respectively (P<0.001. Therapy with GP extract also reduced 30- and 120-minute oral glucose tolerance test postload values. HbA1C levels decreased approximately 2% units in the GP group compared to 0.7% unit in the placebo group (P<0.001. Conclusion. GP extract in addition to SU offers an alternative to addition of other oral medication to treat type 2 diabetic patients.

  15. Development of polyherbal antidiabetic formulation encapsulated in the phospholipids vesicle system

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    Vinod Kumar Gauttam

    2013-01-01

    Full Text Available Multifactorial metabolic diseases, for instance diabetes develop several complications like hyperlipidemia, hepatic toxicity, immunodeficiency etc., Hence, instead of mono-drug therapy the management of the disease requires the combination of herbs. Marketed herbal drugs comprise of irrational combinations, which makes their quality control more difficult. Phytoconstituents, despite having excellent bioactivity in vitro demonstrate less or no in vivo actions due to their poor lipid solubility, resulting in high therapeutic dose regimen; phospholipids encapsulation can overcome this problem. Hence, present study was designed to develop a phospholipids encapsulated polyherbal anti-diabetic formulation. In the present study, polyherbal formulation comprises of lyophilized hydro-alcoholic (50% v/v extracts of Momordica charantia, Trigonella foenum-graecum and Withania somnifera 2:2:1, respectively, named HA, optimized based on oral glucose tolerance test model in normal Wistar rats. The optimized formulation (HA entrapped in the phosphatidylcholine and cholesterol (8:2 vesicle system is named HA lipids (HAL. The vesicles were characterized for shape, morphology, entrapment efficiency, polar-dispersity index and release profile in the gastric pH. The antidiabetic potential of HA, marketed polyherbal formulation (D-fit and HAL was compared in streptozotocin-induced diabetic rat model of 21 days study. The parameters evaluated were behavioral changes, body weight, serum glucose level, lipid profile and oxidative stress. The antidiabetic potential of HA (1000 mg/kg was at par with the D-fit (1000 mg/kg. However, the potential was enhanced by phospholipids encapsulation; as HAL (500 mg/kg has shown more significant (P < 0.05 potential in comparison to HA (1000 mg/kg and at par with metformin (500 mg/kg.

  16. Antioxidant and antidiabetic properties of condensed tannins in acetonic extract of selected raw and processed indigenous food ingredients from Kenya.

    Science.gov (United States)

    Kunyanga, Catherine Nkirote; Imungi, Jasper Kathenya; Okoth, Michael; Momanyi, Clare; Biesalski, Han Konrad; Vadivel, Vellingiri

    2011-05-01

    Recently, tannins have received considerable attention as health-promoting component in various plant foods and several studies have reported on its nutraceutical properties. However, no study has established the role of condensed tannins in indigenous foods of Kenya. Therefore, this study was designed to evaluate the antioxidant activity (DPPH and FRAP) and antidiabetic effects (α-amylase and α-glucosidase inhibition activities) of condensed tannins in some selected raw and traditionally processed indigenous cereals, legumes, oil seeds, and vegetables. The condensed tannin content of the grains and vegetables ranged between 2.55 and 4.35 g/100 g DM and 1.53 and 5.73 g/100 g DM, respectively. The scavenging effect of acetonic extract on DPPH radical ranged from 77% to 90% while the reducing power was found to be 31 to 574 mmol Fe(II)/g DM in all the investigated food ingredients. The condensed tannin extracts of the analyzed samples showed promising antidiabetic effects with potential α-amylase and α-glucosidase inhibition activities of 23% to 44% and 58% to 88%, respectively. Condensed tannins extracted from the amaranth grain, finger millet, field bean, sunflower seeds, drumstick, and amaranth leaves exerted significantly higher antioxidant and antidiabetic activities than other food ingredients. Among the traditional processing methods, roasting of grains and cooking of vegetables were found to be more suitable mild treatments for preserving the tannin compound and its functional properties as opposed to soaking + cooking and blanching treatments. The identified elite sources of optimally processed indigenous food ingredients with promising results could be used as health-promoting ingredients through formulation of therapeutic diets. © 2011 Institute of Food Technologists®

  17. Novel Inhibitory Effect of N-(2-Hydroxycyclohexylvaliolamine on Melanin Production in a Human Skin Model

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    Bum-Ho Bin

    2014-07-01

    Full Text Available Hyper-pigmentation causes skin darkness and medical disorders, such as post-inflammatory melanoderma and melasma. Therefore, the development of anti-melanogenic agents is important for treating these conditions and for cosmetic production. In our previous paper, we demonstrated that the anti-diabetic drug voglibose, a valiolamine derivative, is a potent anti-melanogenic agent. In addition, we proposed an alternative screening strategy to identify valiolamine derivatives with high skin permeability that act as anti-melanogenic agents when applied topically. In this study, we synthesized several valiolamine derivatives with enhanced lipophilicity and examined their inhibitory effects in a human skin model. N-(2-hydroxycyclohexylvaliolamine (HV possesses a stronger inhibitory effect on melanin production than voglibose in a human skin model, suggesting that HV is a more potent anti-melanogenic agent for the skin.

  18. The Antidiabetic Mechanisms of Polyphenols Related to Increased Glucagon-Like Peptide-1 (GLP1 and Insulin Signaling

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    J. Abraham Domínguez Avila

    2017-05-01

    Full Text Available Type-2 diabetes mellitus (T2DM is an endocrine disease related to impaired/absent insulin signaling. Dietary habits can either promote or mitigate the onset and severity of T2DM. Diets rich in fruits and vegetables have been correlated with a decreased incidence of T2DM, apparently due to their high polyphenol content. Polyphenols are compounds of plant origin with several documented bioactivities related to health promotion. The present review describes the antidiabetic effects of polyphenols, specifically related to the secretion and effects of insulin and glucagon-like peptide 1 (GLP1, an enteric hormone that stimulates postprandial insulin secretion. The evidence suggests that polyphenols from various sources stimulate L-cells to secrete GLP1, increase its half-life by inhibiting dipeptidyl peptidase-4 (DPP4, stimulate β-cells to secrete insulin and stimulate the peripheral response to insulin, increasing the overall effects of the GLP1-insulin axis. The glucose-lowering potential of polyphenols has been evidenced in various acute and chronic models of healthy and diabetic organisms. Some polyphenols appear to exert their effects similarly to pharmaceutical antidiabetics; thus, rigorous clinical trials are needed to fully validate this claim. The broad diversity of polyphenols has not allowed for entirely describing their mechanisms of action, but the evidence advocates for their regular consumption.

  19. Quantal health effects of three toxic agents combined

    International Nuclear Information System (INIS)

    Seiler, F.A.

    1988-01-01

    Quantal health effects such as cancer, correlated with the combined action of three toxic agents, are considered. Data on the combined effects of two agents are scarce and no such data exist for three toxicants, yet concerns have arisen about simultaneous exposure of radiation workers to three different agents. Using models developed from the analysis of health effects involving two toxicants, equations for the combined effects of three agents are derived from a more general formalism. An application of practical interest is the incidence of cancer of the esophagus and its correlation with concurrent exposures to alcohol, tobacco, and either low- or high-LET radiation. (author)

  20. Adherence to treatment for diabetes mellitus: validation of instruments for oral antidiabetics and insulin.

    Science.gov (United States)

    Boas, Lilian Cristiane Gomes-Villas; Lima, Maria Luisa Soares Almeida Pedroso de; Pace, Ana Emilia

    2014-01-01

    to verify the face validity, criterion-related validity and the reliability of two distinct forms of presentation of the instrument Measurement of Adherence to Treatment, one being for ascertaining the adherence to the use of oral antidiabetics and the other for adherence to the use of insulin, as well as to assess differences in adherence between these two modes of drug therapy. a methodological study undertaken with 90 adults with Type 2 Diabetes Mellitus. The criterion-related validity was verified using the Receiver Operating Characteristic curves; and for the reliability, the researchers calculated the Cronbach alpha coefficient, the item-total correlation, and the Pearson correlation coefficient. the oral antidiabetics and the other showed sensitivity of 0.84, specificity of 0.35 and a Cronbach correlation coefficient of 0.84. For the adherence to the use of insulin, the values found were, respectively, 0.60, 0.21 and 0.68. A statistically significant difference was found between the final scores of the two forms of the instrument, indicating greater adherence to the use of insulin than to oral antidiabetics. it is concluded that the two forms of the Measurement of Adherence to Treatment instrument are reliable and should be used to evaluate adherence to drug treatment among people with diabetes mellitus.

  1. Comparative Evaluation of the Antidiabetic Effects of Different Parts of Cassia fistula Linn, a Southeast Asian Plant

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    John Wilking Einstein

    2013-01-01

    Full Text Available The hypoglycemic effect of the methanolic and aqueous extracts of whole parts of Cassia fistula in both normoglycemic and streptozotocin-nictotinamide induced Type 2 diabetic rats were investigated. Acute toxicity, oral glucose tolerance test and glucose uptake in isolated rat hemidiaphragm were performed in normal rats. Diabetes was induced in Sprague Dawley rats by the administration of streptozotocin-nictotinamide (50, 110 mg/kg b.w., resp. intraperitoneally. Different extracts of Cassia was administered to diabetic rats at 250 and 500 mg/kg doses for 21 days. Biochemical parameters like blood glucose, insulin, glycosylated hemoglobin, lipid profile, and serum marker enzymes were determined. The methanolic extract of the bark and leaves were show more effective in causing hypoglycemia in normoglycemic rats. Diabetic rats showed increased levels of glycosylated hemoglobin, reduced levels of plasma insulin, were significantly reverted to near normal after oral administration of the bark and leaf methanolic extracts. Glucose uptake studies in isolated rat hemidiaphragm have shown enhanced peripheral utilization of glucose. Chronic treatment of Cassia remarkably restored the normal status of the histopathological changes observed in the selected tissues. Dose dependent anti-diabetic effects with the cohorts receiving the methanolic extract of bark followed by leaves of Cassia was revealed.

  2. Drug Transport Mechanism of Oral Antidiabetic Nanomedicines

    Science.gov (United States)

    Gundogdu, Evren; Yurdasiper, Aysu

    2014-01-01

    Context: Over the last few decades, extensive efforts have been made worldwide to develop nanomedicine delivery systems, especially via oral route for antidiabetic drugs. Absorption of insulin is hindered by epithelial cells of gastrointestinal tract, acidic gastric pH and digestive enzymes. Evidence Acquisition: Recent reports have identified and explained the beneficial role of several structural molecules like mucoadhesive polymers (polyacrylic acid, sodium alginate, chitosan) and other copolymers for the efficient transport and release of insulin to its receptors. Results: Insulin nanomedicines based on alginate-dextran sulfate core with a chitosan-polyethylene glycol-albumin shell reduced glycaemia in a dose dependent manner. Orally available exendin-4 formulations exerted their effects in a time dependent manner. Insulin nanoparticles formed by using alginate and dextran sulfate nucleating around calcium and binding to poloxamer, stabilized by chitosan, and subsequently coated with albumin showed a threefold increase of the hypoglycemic effect in comparison to free insulin in animal models. Solid lipid nanoparticles showed an enhancement of the bioavailability of repaglinide (RG) within optimized solid lipid nanoparticle formulations when compared with RG alone. Conclusions: Nanoparticles represent multiparticulate delivery systems designed to obtain prolonged or controlled drug delivery and to improve bioavailability as well as stability. Nanoparticles can also offer advantages like limiting fluctuations within therapeutic range, reducing side effects, protecting drugs from degradation, decreasing dosing frequency, and improving patient compliance and convenience PMID:24696697

  3. Drug transport mechanism of oral antidiabetic nanomedicines.

    Science.gov (United States)

    Gundogdu, Evren; Yurdasiper, Aysu

    2014-01-01

    Over the last few decades, extensive efforts have been made worldwide to develop nanomedicine delivery systems, especially via oral route for antidiabetic drugs. Absorption of insulin is hindered by epithelial cells of gastrointestinal tract, acidic gastric pH and digestive enzymes. Recent reports have identified and explained the beneficial role of several structural molecules like mucoadhesive polymers (polyacrylic acid, sodium alginate, chitosan) and other copolymers for the efficient transport and release of insulin to its receptors. Insulin nanomedicines based on alginate-dextran sulfate core with a chitosan-polyethylene glycol-albumin shell reduced glycaemia in a dose dependent manner. Orally available exendin-4 formulations exerted their effects in a time dependent manner. Insulin nanoparticles formed by using alginate and dextran sulfate nucleating around calcium and binding to poloxamer, stabilized by chitosan, and subsequently coated with albumin showed a threefold increase of the hypoglycemic effect in comparison to free insulin in animal models. Solid lipid nanoparticles showed an enhancement of the bioavailability of repaglinide (RG) within optimized solid lipid nanoparticle formulations when compared with RG alone. Nanoparticles represent multiparticulate delivery systems designed to obtain prolonged or controlled drug delivery and to improve bioavailability as well as stability. Nanoparticles can also offer advantages like limiting fluctuations within therapeutic range, reducing side effects, protecting drugs from degradation, decreasing dosing frequency, and improving patient compliance and convenience.

  4. A Novel Therapeutic Agent for Type 2 Diabetes Mellitus: SGLT2 Inhibitor

    Directory of Open Access Journals (Sweden)

    Chang Hee Jung

    2014-08-01

    Full Text Available Type 2 diabetes mellitus (T2DM is a complex endocrine and metabolic disorder, and a major public health problem that is rapidly increasing in prevalence. Although a wide range of pharmacotherapies for glycemic control is now available, management of T2DM remains complex and challenging. The kidneys contribute immensely to glucose homeostasis by reabsorbing glucose from the glomerular filtrate. Sodium-glucose cotransporter 2 (SGLT2 inhibitors, a new class of antidiabetic agents that inhibit glucose absorption from the kidney independent of insulin, offer a unique opportunity to improve the outcomes of patients with T2DM. In this review, we provide an overview of two globally-approved SGLT2 inhibitors, dapagliflozin and canagliflozin, and discuss their effects and safety. This information will help clinicians to decide whether these drugs will benefit their patients.

  5. Effect of Methanolic extract of Musa sapientum leaves on ...

    African Journals Online (AJOL)

    . Hyperglycaemia particularly has been reported to inhibit gastrointestinal transit time while glibenclamide, a sulphonylurea and insulin, both increased transit time. Musa sapientum has also been reported as an antidiabetic agent but there is ...

  6. The effects of corn silk on glycaemic metabolism

    OpenAIRE

    Han Linna; Liu Tongjun; Guo Jianyou; Liu Yongmei

    2009-01-01

    Abstract Background Corn silk contains proteins, vitamins, carbohydrates, Ca, K, Mg and Na salts, fixed and volatile oils, steroids such as sitosterol and stigmasterol, alkaloids, saponins, tannins, and flavonoids. Base on folk remedies, corn silk has been used as an oral antidiabetic agent in China for decades. However, the hypoglycemic activity of it has not yet been understood in terms of modern pharmacological concepts. The purpose of this study is to investigate the effects of corn silk ...

  7. Dgroup: DG01685 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available DG01685 DGroup Insulin sensitizer ... DG01684 ... Biguanide antidiabetic ... DG00112 ... Phen...litazar (USAN/INN) ... D09350 ... Indeglitazar (USAN) Antidiabetic agent ... Antidiabetics ...

  8. Next generation sequencing and de novo transcriptome analysis of Costus pictus D. Don, a non-model plant with potent anti-diabetic properties

    Directory of Open Access Journals (Sweden)

    Annadurai Ramasamy S

    2012-11-01

    Full Text Available Abstract Background Phyto-remedies for diabetic control are popular among patients with Type II Diabetes mellitus (DM, in addition to other diabetic control measures. A number of plant species are known to possess diabetic control properties. Costus pictus D. Don is popularly known as “Insulin Plant” in Southern India whose leaves have been reported to increase insulin pools in blood plasma. Next Generation Sequencing is employed as a powerful tool for identifying molecular signatures in the transcriptome related to physiological functions of plant tissues. We sequenced the leaf transcriptome of C. pictus using Illumina reversible dye terminator sequencing technology and used combination of bioinformatics tools for identifying transcripts related to anti-diabetic properties of C. pictus. Results A total of 55,006 transcripts were identified, of which 69.15% transcripts could be annotated. We identified transcripts related to pathways of bixin biosynthesis and geraniol and geranial biosynthesis as major transcripts from the class of isoprenoid secondary metabolites and validated the presence of putative norbixin methyltransferase, a precursor of Bixin. The transcripts encoding these terpenoids are known to be Peroxisome Proliferator-Activated Receptor (PPAR agonists and anti-glycation agents. Sequential extraction and High Performance Liquid Chromatography (HPLC confirmed the presence of bixin in C. pictus methanolic extracts. Another significant transcript identified in relation to anti-diabetic, anti-obesity and immuno-modulation is of Abscisic Acid biosynthetic pathway. We also report many other transcripts for the biosynthesis of antitumor, anti-oxidant and antimicrobial metabolites of C. pictus leaves. Conclusion Solid molecular signatures (transcripts related to bixin, abscisic acid, and geranial and geraniol biosynthesis for the anti-diabetic properties of C. pictus leaves and vital clues related to the other phytochemical functions

  9. Antidiabetic effect of hydroalcoholic extract of Carthamus tinctorius L. in alloxan-induced diabetic rats

    Directory of Open Access Journals (Sweden)

    Sedigheh Asgary

    2012-01-01

    Full Text Available Background: Carthamus tinctorius L. (Compositae has been used in Iranian traditional medicine for treatment of diabetes. In this study, anti-diabetic effect of its hydroalcoholic extract was compared with that of glibenclamide. Methods: Male white Wistar rats were randomly allocated into four groups of six each: nondiabetic control; diabetic control; diabetic treated with hydroalcoholic extract of Carthamus tinctorius (200 mg kg -1 BW; diabetic rats treated with glibenclamide (0.6 mg kg -1 BW. Alloxan was administered (120 mg kg -1 BW, intraperitoneally to induce diabetes. Fasting blood samples were collected three times, before injection of alloxan, two weeks and six weeks after injection of alloxan and fasting blood sugar (FBS, Hb A1C, insulin, cholesterol, LDL-C, HDL-C, VLDL-C, triglyceride, alkaline phosphatase (ALP, alanine aminotransferase (ALT and aspartate aminotransferase (AST were measured each time. Results: FBS, triglyceride, cholesterol, LDL-C and VLDL-C had a meaningful decrease in diabetic rats treated with Carthamus tinctorius and diabetic rats treated with glibenclamide as compared with diabetic rats with no treatment. Insulin level increased significantly in diabetic groups received treatment (glibenclamide or Carthamus tinctorius L in comparison with diabetic group with no treatment. The histological study revealed size of islets of Langerhans enlarged significantly consequentially as compared with diabetic rats with no treatment. The extract appeared non toxic as evidenced by normal levels of AST, ALP and ALT. Effects of administrating glibenclamide or extract of Carthamus tinctorius L on all biochemical parameters discussed above showed no difference and both tend to bring the values to near normal. Conclusion: These results suggested that the hydroalcoholic extract of Carthamus tinctorius possesses beneficial effect on treatment of diabetes.

  10. The antidiabetic effect of L-carnitine in rats: the role of nitric oxide system

    Directory of Open Access Journals (Sweden)

    Shaghayegh Hajian-Shahri

    2017-11-01

    Full Text Available Background: Nowadays, the use of L-carnitine in the treatment of diabetes is increasing. This study was conducted to investigate the effect of co-administration of L-arginine (precursor for the synthesis of nitric oxide and nitro-L-arginine (nitric oxide synthesis inhibitor on antidiabetic activity of L-carnitine in diabetic rats. Materials and Methods: In this study, 50 male rats weighing 180-201g were divided into five groups: (1 non diabetic control rats; (2 untreated diabetic rats; (3 diabetic rats treated with L-carnitine 300 mg/kg (4; diabetic rats treated with L-carnitine 300 mg/kg + L-arginine 300 mg/kg; and (5 diabetic rats treated with L-carnitine (300 mg/kg + nitro-L-arginine (1mg/kg. Type 1 diabetes was induced by a single intraperitoneal injection of 110 mg/kg body weight alloxan. After 30 days, liver malondialdehyde levels, lipid profile, serum glucose, and glycated hemoglobin serum levels were measured. Results: Blood glucose, liver enzymes, glycated hemoglobin, and liver malondialdehyde levels significantly decreased in diabetic rats treated with L-carnitine compared to the untreated diabetic group (P<0.05. The co-administration of L-arginine and L-carnitine led to a significant decrease in glycated hemoglobin levels and serum glucose, in a manner similar to the group received only L-carnitine. Also, L-arginine and nitro-l-arginine had similar effects on liver lipid peroxidation and serum biochemical parameters. Conclusion: The results suggest that the hypoglycemic effect of L-carnitine is mediated independently from nitric oxide pathways. The interaction between L-carnitine and L-arginine may not be synergistic. So, their combined administration is not recommended for the diabetic patients.

  11. Dgroup: DG00114 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available ydrochloride (JP17) ... Antidiabetic agent ... DG01685 ... Insulin sensitizer ... DG01684 ... Biguanide antidiabetic Unc...lassified ... DG02044 ... Hypoglycemics ... DG01684 ... Biguanide antidiabetic ATC code: A10BA03 Biganide antidiabetics AMPK (PRKAA) [HSA:5562 5563] [KO:K07198] ...

  12. Co-prescription of medication for bipolar disorder and diabetes mellitus: a nationwide population-based study with focus on gender differences

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    Svendal Gjertrud

    2012-11-01

    Full Text Available Abstract Background Studies have shown a correlation between bipolar disorder and diabetes mellitus. It is unclear if this correlation is a part of common pathophysiological pathways, or if medication for bipolar disorder has negative effects on blood sugar regulation. Methods The Norwegian prescription database was analyzed. Prescriptions for lithium, lamotrigine, carbamazepine and valproate were used as proxies for bipolar disorder. Prescriptions for insulin and oral anti-diabetic agents were used as proxies for diabetes mellitus. We explored the association between medication for bipolar disorder and diabetes medication by logistic regression Results We found a strong association between concomitant use of medication to treat diabetes mellitus and mood stabilizers for the treatment of bipolar disorder. Females had a 30% higher risk compared to men of being treated for both disorders. Persons using oral anti-diabetic agents had higher odds of receiving valproate than either lithium or lamotrigine. Use of insulin as monotherapy seemed to have lower odds than oral anti-diabetic agents of co-prescription of mood stabilizers, compared to the general population. Conclusions This study showed a strong association between the use of mood stabilizers and anti-diabetic agents. The association was stronger among women than men.

  13. Comparison of the Efficacy of Glimepiride, Metformin, and Rosiglitazone Monotherapy in Korean Drug-Naïve Type 2 Diabetic Patients: The Practical Evidence of Antidiabetic Monotherapy Study

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    Kun Ho Yoon

    2011-02-01

    Full Text Available BackgroundAlthough many anti-diabetic drugs have been used to control hyperglycemia for decades, the efficacy of commonly-used oral glucose-lowering agents in Korean type 2 diabetic patients has yet to be clearly demonstrated.MethodsWe evaluated the efficacy of glimepiride, metformin, and rosiglitazone as initial treatment for drug-naïve type 2 diabetes mellitus patients in a 48-week, double-blind, randomized controlled study that included 349 Korean patients. Our primary goal was to determine the change in HbA1c levels from baseline to end point. Our secondary goal was to evaluate changes in fasting plasma glucose (FPG levels, body weight, frequency of adverse events, and the proportion of participants achieving target HbA1c levels.ResultsHbA1c levels decreased from 7.8% to 6.9% in the glimepiride group (P<0.001, from 7.9% to 7.0% in the metformin group (P<0.001, and from 7.8% to 7.0% (P<0.001 in the rosiglitazone group. Glimepiride and rosiglitazone significantly increased body weight and metformin reduced body weight during the study period. Symptomatic hypoglycemia was more frequent in the glimepiride group and diarrhea was more frequent in the metformin group.ConclusionThe efficacy of glimepiride, metformin, and rosiglitazone as antidiabetic monotherapies in drug-naïve Korean type 2 diabetic patients was similar in the three groups, with no statistical difference. This study is the first randomized controlled trial to evaluate the efficacy of commonly-used oral hypoglycemic agents in Korean type 2 diabetic patients. An additional subgroup analysis is recommended to obtain more detailed information.

  14. An adenovirus-derived protein: A novel candidate for anti-diabetic drug development.

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    Hegde, Vijay; Na, Ha-Na; Dubuisson, Olga; Burke, Susan J; Collier, J Jason; Burk, David; Mendoza, Tamra; Dhurandhar, Nikhil V

    2016-02-01

    Exposure to human adenovirus Ad36 is causatively and correlatively linked with better glycemic control in animals and humans, respectively. Although the anti-hyperglycemic property of Ad36 may offer some therapeutic potential, it is impractical to use an infectious agent for therapeutic benefit. Cell-based studies identified that Ad36 enhances cellular glucose disposal via its E4orf1 protein. Ability to improve glycemic control in vivo is a critical prerequisite for further investigating the therapeutic potential of E4orf1. Therefore, the aim of this study was to determine the ability of E4orf1 to improve glycemic control independent of insulin despite high fat diet. 8-9wk old male C57BL/6J mice fed a high-fat diet (60% kcal) were injected with a retrovirus plasmid expressing E4orf1, or a null vector (Control). Glycemic control was determined by glucose and insulin tolerance test. Islet cell size, amount of insulin and glucagon were determined in formalin-fixed pancreas. Rat insulinoma cell line (832/13) was infected with E4orf1 or control to determine changes in glucose stimulated insulin secretion. Protein from flash frozen adipose tissue depots, liver and muscle was used to determine molecular signaling by western blotting. In multiple experiments, retrovirus-mediated E4orf1 expression in C57BL/6J mice significantly and reproducibly improved glucose excursion following a glucose load despite a high fat diet (60% energy). Importantly, E4orf1 improved glucose clearance without increasing insulin sensitivity, production or secretion, underscoring its insulin-independent effect. E4orf1 modulated molecular signaling in mice tissue, which included greater protein abundance of adiponectin, p-AKT and Glucose transporter Glu4. This study provides the proof of concept for translational development of E4orf1 as a potential anti-diabetic agent. High fat intake and impaired insulin signaling are often associated with obesity, diabetes and insulin resistance. Hence, the

  15. Evaluating the Effect of Ramadan Fasting on Muslim Patients with Diabetes in relation to Use of Medication and Lifestyle Patterns: A Prospective Study.

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    Siaw, Melanie Yee Lee; Chew, Daniel Ek Kwang; Dalan, Rinkoo; Abdul Shakoor, Shaikh Abdul Kader Kamaldeen; Othman, Noorani; Choo, Chor Hui; Shamsuri, Nur Hidayah; Abdul Karim, Siti Nurhana; Chan, Sui Yung; Lee, Joyce Yu-Chia

    2014-01-01

    Objectives. This study aimed to examine the effect of Ramadan fasting on HbA1c in Muslim patients with type 2 diabetes. The incidence of hypoglycemia and glycemic changes in relation to the adjustment of doses of antidiabetic agents, diet, and physical activity during Ramadan was also evaluated. Methods. This was a prospective study conducted in an outpatient endocrine clinic. A set of questionnaires was administered to Muslim patients with diabetes who fasted for ≥10 days. Those who were hospitalized for diabetic ketoacidosis or severe hypoglycemia a month prior to Ramadan or were given short-term corticosteroid therapy were excluded. The patients' responses and clinical outcomes from the clinic database were collected before, during, and after Ramadan. Results. A total of 153 participants completed the study. The mean HbA1c improved from 8.9% before Ramadan to 8.6% during Ramadan (P Ramadan (P Ramadan fasting appeared to improve glycemic control, especially in those whose doses of antidiabetic agents were adjusted during Ramadan.

  16. Antidiabetic and Neuroprotective Effects of Trigonella Foenum-graecum Seed Powder in Diabetic Rat Brain

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    P. Kumar

    2012-01-01

    Full Text Available Trigonella foenum-graecum seed powder (TSP has been reported to have hypoglycemic and hyperinsulinemic action. The objective of the study was to examine the antidiabetic and neuroprotective role of TSP in hyperglycemiainduced alterations in blood glucose, insulin levels and activities of membrane linked enzymes (Na+K+ATPase, Ca2+ATPase, antioxidant enzymes (superoxide dismutase, glutathione S-transferase, calcium (Ca2+ levels, lipid peroxidation, membrane fluidity and neurolipofuscin accumulation in the diabetic rat brain. Female Wistar rats weighing between 180 and 220 g were made diabetic by a single injection of alloxan monohydrate (15 mg/100 g body weight, diabetic rats were given 2 IU insulin, per day with 5% TSP in the diet for three weeks. A significant increase in lipid peroxidation was observed in diabetic brain. The increased lipid peroxidation following chronic hyperglycemia was accompanied with a significant increase in the neurolipofuscin deposition and Ca2+ levels with decreased activities of membrane linked ATPases and antioxidant enzymes in diabetic brain. A decrease in synaptosomal membrane fluidity may influence the activity of membrane linked enzymes in diabetes. The present study showed that TSP treatment can reverse the hyperglycemia induced changes to normal levels in diabetic rat brain. TSP administration amended effect of hyperglycemia on alterations in lipid peroxidation, restoring membrane fluidity, activities of membrane bound and antioxidant enzymes, thereby ameliorating the diabetic complications.

  17. The Antihyperglycemic Effects of Rhizoma Coptidis and Mechanism of Actions: A Review of Systematic Reviews and Pharmacological Research

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    Hui Wang

    2014-01-01

    Full Text Available Rhizoma Coptidis (Huang Lian in Chinese pinyin is among the most widely used traditional Chinese herbal medicines and has a profound history of more than 2000 years of being used as a therapeutic herb. The antidiabetic effects of Rhizoma Coptidis have been extensively investigated in animal experiments and clinical trials and its efficacy as a promising antihyperglycemic agent has been widely discussed. In the meantime, findings from modern pharmacological studies have contributed the majority of its bioactivities to berberine, the isoquinoline alkaloids component of the herb, and a number of experiments testing the antidiabetic effects of berberine have been initiated. Therefore, we conducted a review of the current evidence profile of the antihyperglycemic effects of Rhizoma Coptidis as well as its main component berberine and the possible mechanism of actions, in order to summarize research evidence in this area and identify future research directions.

  18. Inhibitory effects of antimicrobial agents against Fusarium species.

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    Kawakami, Hideaki; Inuzuka, Hiroko; Hori, Nobuhide; Takahashi, Nobumichi; Ishida, Kyoko; Mochizuki, Kiyofumi; Ohkusu, Kiyofumi; Muraosa, Yasunori; Watanabe, Akira; Kamei, Katsuhiko

    2015-08-01

    We investigated the inhibitory effects of antibacterial, biocidal, and antifungal agents against Fusarium spp. Seven Fusarium spp: four F. falciforme (Fusarium solani species complex), one Fusarium spp, one Fusarium spp. (Fusarium incarnatum-equiseti species complex), and one F. napiforme (Gibberella fujikuroi species complex), isolated from eyes with fungal keratitis were used in this study. Their susceptibility to antibacterial agents: flomoxef, imipenem, gatifloxacin, levofloxacin, moxifloxacin, gentamicin, tobramycin, and Tobracin® (contained 3,000 μg/ml of tobramycin and 25 μg/ml of benzalkonium chloride (BAK), a biocidal agent: BAK, and antifungal agents: amphotericin B, pimaricin (natamycin), fluconazole, itraconazole, miconazole, voriconazole, and micafungin, was determined by broth microdilution tests. The half-maximal inhibitory concentration (IC50), 100% inhibitory concentration (IC100), and minimum inhibitory concentration (MIC) against the Fusarium isolates were determined. BAK had the highest activity against the Fusarium spp. except for the antifungal agents. Three fluoroquinolones and two aminoglycosides had inhibitory effects against the Fusarium spp. at relatively high concentrations. Tobracin® had a higher inhibitory effect against Fusarium spp. than tobramycin alone. Amphotericin B had the highest inhibitory effect against the Fusarium spp, although it had different degrees of activity against each isolate. Our findings showed that fluoroquinolones, aminoglycosides, and BAK had some degree of inhibitory effect against the seven Fusarium isolates, although these agents had considerably lower effect than amphotericin B. However, the inhibitory effects of amphotericin B against the Fusarium spp. varied for the different isolates. Further studies for more effective medications against Fusarium, such as different combinations of antibacterial, biocidal, and antifungal agents are needed. © The Author 2015. Published by Oxford University Press on

  19. Antidiabetic Effect of Hydroalcholic Urtica dioica Leaf Extract in Male Rats with Fructose-Induced Insulin Resistance

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    Ahangarpour, Akram; Mohammadian, Maryam; Dianat, Mahin

    2012-01-01

    Background: Urtica dioica has been used as antihypertensive, antihyperlipidemic and antidiabetic herbal medicine. The purpose of this study was to study the effect of hydroalcoholic extract of Urtica dioica on fructose-induced insulin resistance rats. Methods: Forty male Wistar rats were randomly divided into five groups including control, fructose, extract 50, extract 100 and extract 200. The control rat received vehicle, the fructose and extract groups received fructose 10% for eight weeks. The extract groups received single daily injection of vehicle, 50, 100 or 200 mg/kg/day for the two weeks. Blood glucose, insulin, last fasting insulin resistance index (FIRI), serum triglyceride (TG), low-density lipoprotein (LDL), very low-density lipoprotein (VLDL), high-density lipoprotein (HDL), alanin trasaminase (AST) and alkaline phosphatase (ALP), leptin and LDL/HDL ratio were determined. Results: Compared to control group, daily administration of fructose was associated with significant increase in FIRI, blood glucose and insulin, significant decrease in lepin, and no significant change in TG, HDL, LDL, LDL/HDL ratio, VLDL, ALT, and ALP. The extract significantly decreased serum glucose, insulin, LDL and leptin, and LDL/HDL ratio and FIRI. It also significantly increased serum TG, VLDL, and AST, but did not change serum ALP. Conclusion: We suggest that Urtica dioica extract, by decreasing serum glucose, and FIRI, may be useful to improve type 2 diabetes mellitus. Also, by positive effect on lipid profile and by decreasing effect on leptin, it may improve metabolic syndrome. PMID:23115450

  20. Antidiabetic Effect of Hydroalcholic Urtica dioica Leaf Extract in Male Rats with Fructose-Induced Insulin Resistance

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    Akram Ahangarpour

    2012-09-01

    Full Text Available Background: Urtica dioica has been used as antihypertensive, antihyperlipidemic and antidiabetic herbal medicine. The purpose of this study was to study the effect of hydroalcoholic extract of Urtica dioica on fructose-induced insulin resistance rats. Methods: Forty male Wistar rats were randomly divided into five groups including control, fructose, extract 50, extract 100 and extract 200. The control rat received vehicle, the fructose and extract groups received fructose 10% for eight weeks. The extract groups received single daily injection of vehicle, 50, 100 or 200 mg/kg/day for the two weeks. Blood glucose, insulin, last fasting insulin resistance index (FIRI, serum triglyceride (TG, low-density lipoprotein (LDL, very low-density lipoprotein (VLDL, high-density lipoprotein (HDL, alanin trasaminase (AST and alkaline phosphatase (ALP, leptin and LDL/HDL ratio were determined.Results: Compared to control group, daily administration of fructose was associated with significant increase in FIRI, blood glucose and insulin, significant decrease in lepin, and no significant change in TG, HDL, LDL, LDL/HDL ratio, VLDL, ALT, and ALP. The extract significantly decreased serum glucose, insulin, LDL and leptin, and LDL/HDL ratio and FIRI. It also significantly increased serum TG, VLDL, and AST, but did not change serum ALP.Conclusion: We suggest that Urtica dioica extract, by decreasing serum glucose, and FIRI, may be useful to improve type 2 diabetes mellitus. Also, by positive effect on lipid profile and by decreasing effect on leptin, it may improve metabolic syndrome.

  1. Antidiabetic Properties and Mechanism of Action of Gynura procumbens Water Extract in Streptozotocin-Induced Diabetic Rats

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    Mariam Ahmad

    2010-12-01

    Full Text Available Gynura procumbens (Lour. Merr (family Compositae is cultivated in Southeast Asia, especially Indonesia, Malaysia and Thailand, for medicinal purposes. This study evaluated the in vivo hypoglycemic properties of the water extract of G. procumbens following 14 days of treatment and in vitro in RIN-5F cells. Glucose absorption from the intestines and its glucose uptake in abdominal skeletal muscle were assessed. The antidiabetic effect of water extract of G. procumbens leaves was investigated in streptozotocin-induced diabetic rats. The intraperitoneal glucose tolerance test (IPGTT was performed in diabetic rats treated with G. procumbens water extract for 14 days. In the IPGTT, blood was collected for insulin and blood glucose measurement. After the IPGTT, the pancreases were collected for immunohistochemical study of β-cells of the islets of Langerhans. The possible antidiabetic mechanisms of G. procumbens were assessed through in vitro RIN-5F cell study, intestinal glucose absorption and glucose uptake by muscle. The results showed that G. procumbens significantly decreased blood glucose levels after 14 days of treatment and improved outcome of the IPGTT. However, G. procumbens did not show a significant effect on insulin level either in the in vivo test or the in vitro RIN-5F cell culture study. G. procumbens also showed minimal effects on β-cells of the islets of Langerhans in the pancreas. However, G. procumbens only significantly increased glucose uptake by muscle tissues. From the findings we can conclude that G. procumbens water extract exerted its hypoglycemic effect by promoting glucose uptake by muscles.

  2. Review of antidiabetic fruits, vegetables, beverages, oils and spices commonly consumed in the diet.

    Science.gov (United States)

    Beidokhti, Maliheh Najari; Jäger, Anna K

    2017-04-06

    Type 2 diabetes is the most common type of diabetes and its prevalence is rapidly increasing throughout the world. Modifications of lifestyle such as suitable diet and exercise programs along with pharmacotherapy and education of patients are beneficial therapies for patients with type 2 diabetes. The ethnopharmacological use of herbal medicines, many of them part of our diet as spices, vegetables and fruits, has been developed for the treatment of diabetes due to inexpensiveness, easy availability and few side effects. Our aim is to present a review for researchers who are interested in the biologically active dietary plants traditionally utilized in the treatment of diabetes. Information was obtained from a literature search of electronic databases such as Google Scholar, Pubmed, Sci Finder and Cochrane. Common and scientific name of the fruits, vegetables, beverages, oils and spices and the words 'antidiabetic', 'hypoglycemic', 'anti-hyperglycemic', 'type 2 diabetes' were used as keywords for search. Certain fruits and vegetables are functional foods and their consumption reduces the incidence of type 2 diabetes. Hypoglycemic effects of fruits and vegetables may be due to their inducing nature on pancreatic β-cells for insulin secretion, or bioactive compounds such as flavonoids, alkaloids and anthocyanins, which act as insulin-like molecules or insulin secretagogues. This write-up covers hypoglycemic, anti-hyperglycemic and anti-diabetic activities of some dietary fruits, vegetables, beverages, oils and spices and their active hypoglycemic constituents. Including such plant species in the diet might improve management of type 2 diabetes. Copyright © 2017 Elsevier Ireland Ltd. All rights reserved.

  3. Lansoprazole enhances the antidiabetic effect of sitagliptin in mice with diet-induced obesity and healthy human subjects.

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    Hao, ShaoJun; Sun, JianHua; Tian, XiKui; Sun, Xu; Zhang, ZhenXing; Gao, Yuan

    2014-08-01

    Proton pump inhibitors as adjunctive therapy would improve diabetes control and could enhance the hypoglycaemic activity of DPP-4 inhibitors. The aim of the study was to investigate the short-term effects of lansoprazole (LPZ), sitagliptin (SITA) and their combination therapy on glucose regulation and gut peptide secretion. Glucose and gut peptide were determined and compared after short-term administration of LPZ or SITA, or in combination to mice with diet-induced obesity (DIO) and to healthy human subjects (n = 16) in a 75 g oral glucose tolerance test (OGTT) by a crossover design. In DIO mice, LPZ significantly improve glucose metabolism, increase plasma C-peptide and insulin compared with vehicle treatment. Furthermore, the combination of LPZ and SITA improved glucose tolerance additively, with higher plasma insulin and C-peptide levels compared with SITA-treated mice. Similarly, in human in the OGTT, the combination showed significant improvement in glucose-lowering and insulin increase vs SITA-treated group. However, no significant differences in area under curve (AUC) of insulin, glucose and C-peptide between the LPZ-treated group and baseline, except that mean AUCgastrin was significantly increased by LPZ. LPZ and SITA combination therapy appears to have complementary mechanisms of action and additive antidiabetic effect. © 2014 Royal Pharmaceutical Society.

  4. Studies on the antidiabetic effects of Mangifera indica stem-barks and leaves on nondiabetic, type 1 and type 2 diabetic model rats

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    Amrita Bhowmik

    2009-06-01

    Full Text Available Mangifera indica Linn, locally known as mango tree has been claimed to possess antidiabetic properties by many investigators. The present study was undertaken to screen the hypo- and antihyperglycemic activity of both ethanol and water extracts of leaves and stem-barks of M. indica in nondiabetic and diabetic model rats in different prandial states. The results showed that all of the extracts had significant antihyperglycemic effect in type 2 model rats when fed simultaneously with glucose load (p< 0.05-0.01; p< 0.005-0.001. Moreover, the ethanol extract of stem-barks showed significant antihyperglycemic effect when the extract was fed 30 min prior to the glucose load (p< 0.01. Investigations were carried out to evaluate the effect of M. indica on glucose absorption using a rat intestinal preparation in situ. The ethanol extracts of stem-barks reduced glucose absorption gradually during the whole perfusion period in type 2 rats.

  5. Studies on the antidiabetic effects of Mangifera indica stem-barks and leaves on nondiabetic, type 1 and type 2 diabetic model rats

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    Amrita Bhowmik, Liakot Ali Khan, Masfida Akhter and Begum Rokeya

    2009-12-01

    Full Text Available Mangifera indica Linn, locally known as mango tree has been claimed to possess antidiabetic properties by many investigators. The present study was undertaken to screen the hypoglycemic and antihyperglycemic activity of both ethanol and water extracts of leaves and stem-barks of M. indica in nondiabetic and diabetic model rats in different prandial state. The results showed that all of the extracts had significant antihyperglycemic effect in type 2 diabetic model rats when fed simultaneously with glucose load (p<0.05-0.01; p<0.005-0.001. Moreover, the ethanol extract of stem-barks showed significant antihyperglycemic effect when the extract was fed 30 min prior to the glucose load (p<0.01. Investigations were carried out to evaluate the effect of M. indica on glucose absorption using a rat intestinal preparation in situ. The ethanol extracts of stem-barks reduced glucose absorption gradually during the whole perfusion period in type 2 diabetic rats.

  6. Antidiabetic activity and phytochemical screening of extracts of the leaves of Ajuga remota Benth on alloxan-induced diabetic mice.

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    Tafesse, Tadesse Bekele; Hymete, Ariaya; Mekonnen, Yalemtsehay; Tadesse, Mekuria

    2017-05-02

    Ajuga remota Benth is traditionally used in Ethiopia for the management of diabetes mellitus. Since this claim has not been investigated scientifically, the aim of this study was to evaluate the antidiabetic effect and phytochemical screening of the aqueous and 70% ethanol extracts on alloxan-induced diabetic mice. After acute toxicity test, the Swiss albino mice were induced with alloxan to get experimental diabetes animals. The fasting mean blood glucose level before and after treatment for two weeks in normal, diabetic untreated and diabetic mice treated with aqueous and 70% ethanol extracts were performed. Data were statistically evaluated by using Statistical Package for the Social Sciences software version 20. P-value Phytochemical screening of both extracts indicated the presence of phenolic compounds, flavonoids, saponins, tannins, and steroids, which might contribute to the antidiabetic activity. The extracts, however, did not contain alkaloids and anthraquinones. The aqueous extract (500 mg/kg) showed the highest percentage reduction in blood glucose levels and the ability of A. remota extracts in reducing blood glucose levels presumably due to the presence of antioxidant constituents such as flavonoids. The effect of the extract supported the traditional claim of the plant.

  7. 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.

  8. Combretum lanceolatum flowers extract shows antidiabetic activity through activation of AMPK by quercetin

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    Carlos Roberto Porto Dechandt

    2012-12-01

    Full Text Available The present study evaluated the antidiabetic activity of the Combretum lanceolatum Pohl ex Eichler, Combretaceae, flowers extract (ClEtOH in diabetic rats. Streptozotocin-diabetic rats were divided into four groups: diabetic control, diabetic treated with 500 mg/kg of metformin and diabetic treated with 250 or 500 mg/kg of ClEtOH for 21 days. The treatment of diabetic rats with 500 mg/kg of ClEtOH promoted an increase in the weight of liver, white adipose tissues and skeletal muscles, improving body weight gain. Diabetic rats treated with 500 mg/kg of ClEtOH also presented reduction in glycemia, glycosuria and urinary urea levels, and increase in liver glycogen content. HPLC chromatogram showed that quercetin is the major compound in the extract. The phosphorylation levels of adenosine monophosphate-activated protein kinase were increased in liver slices incubated in vitro with 50 µg/mL of ClEtOH, similarly to the incubation with metformin (50 µg/mL or quercetin (10 µg/mL. The antihyperglycemic effect of ClEtOH was similar to that of metformin and appears to be through inhibition of gluconeogenesis, since urinary urea was reduced and skeletal muscle mass was increased. These data indicate that the antidiabetic activity of the Combretum lanceolatum extract could be mediated, at least in part, through activation of adenosine monophosphateactivated protein kinase by quercetin.

  9. Comparison of antioxidant, anticholinesterase, and antidiabetic activities of three curcuminoids isolated from Curcuma longa L.

    Science.gov (United States)

    Kalaycıoğlu, Zeynep; Gazioğlu, Işıl; Erim, F Bedia

    2017-12-01

    Antioxidant, anticholinesterase and antidiabetic activities of three curcuminoids isolated from the Curcuma longa were simultaneously tested and compared in this study. The highest antioxidant power was detected for curcumin with the applied methods. The drug potentials of curcuminoids for Alzheimer's disease were controlled. Bisdemethoxycurcumin (BDMC) showed substantial inhibitory activity. The activity of demethoxycurcumin (DMC) followed BDMC, whereas curcumin showed very little acetylcholinesterase inhibition activity. Antidiabetic activity of curcuminoids was evaluated by their α-glucosidase inhibitory activities. All curcuminoids show activities with decreasing order as BDMC > curcumin > DMC. The significant activities of BDMC compared to its isomers and examination of chemical structures of isomers might be a starting point in designing new drugs for Alzheimer's and Diabetes Mellitus.

  10. Anti-Diabetic Activities of Jiaotaiwan in db/db Mice by Augmentation of AMPK Protein Activity and Upregulation of GLUT4 Expression

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    Na Hu

    2013-01-01

    Full Text Available Jiaotaiwan (JTW, which is composed of Coptis chinensis (CC and cinnamon (CIN, is one of the most well-known traditional Chinese medicines. In this study, we investigated the antidiabetic effects and mechanism of JTW in db/db mice. Results showed that JTW significantly decreased the level of fasting blood glucose and improved glucose and insulin tolerance better than CC or CIN alone. JTW also effectively protected the pancreatic islet shape, augmented the activation of AMP-activated protein kinase (AMPK in the liver, and increased the expression of glucose transporter 4 (GLUT4 protein in skeletal muscle and white fat. AMPK and GLUT4 contributed to glucose metabolism regulation and had an essential function in the development of diabetes mellitus (DM. Therefore, the mechanisms of JTW may be related to suppressing gluconeogenesis by activating AMPK in the liver and affecting glucose uptake in surrounding tissues through the upregulation of GLUT4 protein expression. These findings provided a new insight into the antidiabetic clinical applications of JTW and demonstrated the potential of JTW as a new drug candidate for DM treatment.

  11. QSAR studies in the discovery of novel type-II diabetic therapies.

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    Abuhammad, Areej; Taha, Mutasem O

    2016-01-01

    Type-II diabetes mellitus (T2DM) is a complex chronic disease that represents a major therapeutic challenge. Despite extensive efforts in T2DM drug development, therapies remain unsatisfactory. Currently, there are many novel and important antidiabetic drug targets under investigation by many research groups worldwide. One of the main challenges to develop effective orally active hypoglycemic agents is off-target effects. Computational tools have impacted drug discovery at many levels. One of the earliest methods is quantitative structure-activity relationship (QSAR) studies. QSAR strategies help medicinal chemists understand the relationship between hypoglycemic activity and molecular properties. Hence, QSAR may hold promise in guiding the synthesis of specifically designed novel ligands that demonstrate high potency and target selectivity. This review aims to provide an overview of the QSAR strategies used to model antidiabetic agents. In particular, this review focuses on drug targets that raised recent scientific interest and/or led to successful antidiabetic agents in the market. Special emphasis has been made on studies that led to the identification of novel antidiabetic scaffolds. Computer-aided molecular design and discovery techniques like QSAR have a great potential in designing leads against complex diseases such as T2DM. Combined with other in silico techniques, QSAR can provide more useful and rational insights to facilitate the discovery of novel compounds. However, since T2DM is a complex disease that includes several faulty biological targets, multi-target QSAR studies are recommended in the future to achieve efficient antidiabetic therapies.

  12. Binding Energy calculation of GSK-3 protein of Human against some anti-diabetic compounds of Momordica charantia linn (Bitter melon).

    Science.gov (United States)

    Hazarika, Ridip; Parida, Pratap; Neog, Bijoy; Yadav, Raj Narain Singh

    2012-01-01

    Diabetes is one of the major life threatening diseases worldwide. It creates major health problems in urban India. Glycogen Synthase Kinase-3 (GSK-3) protein of human is known for phosphorylating and inactivating glycogen synthase which also acts as a negative regulator in the hormonal control of glucose homeostasis. In traditional medicine, Momordica charantia is used as antidiabetic plant because of its hypoglycemic effect. Hence to block the active site of the GSK-3 protein three anti-diabetic compounds namely, charantin, momordenol & momordicilin were taken from Momordica charantia for docking study and calculation of binding energy. The aim of present investigation is to find the binding energy of three major insulin-like active compounds against glycogen synthase kinase-3 (GSK-3), one of the key proteins involved in carbohydrate metabolism, with the help of molecular docking using ExomeTM Horizon suite. The study recorded minimum binding energy by momordicilin in comparison to the others.

  13. Anti-diabetic drugs in the private and public sector in Dar es Salaam ...

    African Journals Online (AJOL)

    Objectives: To compare availability, cost, affordability and sources of anti-diabetic drugs between private and public health facilities in Dar es Salaam, Tanzania. Design: Cross sectional descriptive study. Setting: Diabetic clinics in private and public health facilities in Dar es Salaam, Tanzania. Subjects: Eighty patients ...

  14. Evaluation of antioxidative and antidiabetic activity of bark of holarrhena pubescens wall.

    Science.gov (United States)

    Bhusal, Anup; Jamarkattel, Nirmala; Shrestha, Aasmin; Lamsal, Nisha Kiran; Shakya, Sangam; Rajbhandari, Sneha

    2014-09-01

    The objectives of the study are to screen out various phytochemicals and to evaluate the antioxidant and antidiabetic potential of the stem bark of Holarrhena pubescens Wall (Holarrhena antidysenterica). The antioxidant activity was determined by the DPPH (2,2-diphenyl-1-picrylhydrazyl) radical scavenging activity where ascorbic acid was taken as positive control. The antioxidant property was later exploited and the methanolic extract of plant was tested for antihyperglycemic activity in glucose overloaded hyperglycemic mice. The extract was tested for its hypoglycemic activity at two-dose levels, 250 and 500 mg/kg respectively where Glipizide 5 mg/kg was taken as standard reference drug. All results are presented as mean ± SD (Standard Deviation). Significant differences between experimental groups were determined by Student's t-test. The methanolic and water extract showed strong antioxidant activity with inhibition of more than 90% DPPH free radicals at the concentration of 100μg/mL. The hypoglycemic activity of methanolic extract on glucose tolerance test were significant (p flavonoides, phenolic compounds suggested that they may be partially responsible for antioxidant and antidiabetic activity.

  15. A novel antidiabetic drug, fasiglifam/TAK-875, acts as an ago-allosteric modulator of FFAR1.

    Directory of Open Access Journals (Sweden)

    Chiori Yabuki

    Full Text Available Selective free fatty acid receptor 1 (FFAR1/GPR40 agonist fasiglifam (TAK-875, an antidiabetic drug under phase 3 development, potentiates insulin secretion in a glucose-dependent manner by activating FFAR1 expressed in pancreatic β cells. Although fasiglifam significantly improved glycemic control in type 2 diabetes patients with a minimum risk of hypoglycemia in a phase 2 study, the precise mechanisms of its potent pharmacological effects are not fully understood. Here we demonstrate that fasiglifam acts as an ago-allosteric modulator with a partial agonistic activity for FFAR1. In both Ca(2+ influx and insulin secretion assays using cell lines and mouse islets, fasiglifam showed positive cooperativity with the FFAR1 ligand γ-linolenic acid (γ-LA. Augmentation of glucose-induced insulin secretion by fasiglifam, γ-LA, or their combination was completely abolished in pancreatic islets of FFAR1-knockout mice. In diabetic rats, the insulinotropic effect of fasiglifam was suppressed by pharmacological reduction of plasma free fatty acid (FFA levels using a lipolysis inhibitor, suggesting that fasiglifam potentiates insulin release in conjunction with plasma FFAs in vivo. Point mutations of FFAR1 differentially affected Ca(2+ influx activities of fasiglifam and γ-LA, further indicating that these agonists may bind to distinct binding sites. Our results strongly suggest that fasiglifam is an ago-allosteric modulator of FFAR1 that exerts its effects by acting cooperatively with endogenous plasma FFAs in human patients as well as diabetic animals. These findings contribute to our understanding of fasiglifam as an attractive antidiabetic drug with a novel mechanism of action.

  16. Drug: D00595 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available D00595 Drug Buformin (USAN/INN) ... C6H15N5 D00595.gif ... Antidiabetic agent ... DG01685... ... Insulin sensitizer ... DG01684 ... Biguanide antidiabetic Unclassified ... DG02044 ... Hypoglycemics ... DG01684 ... Biguanide antidiabetic

  17. Progression to insulin for patients with diabetes mellitus on dual oral antidiabetic therapy using the US Department of Defense Database.

    Science.gov (United States)

    Rascati, K; Richards, K; Lopez, D; Cheng, L-I; Wilson, J

    2013-10-01

    To compare 'progression to insulin' for three cohorts on oral antidiabetic medication combinations: metformin/sulphonylurea (Met/SU), metformin/thiazolidinedione (Met/TZD) and sulphonylurea/thiazolidinedione (SU/TZD). Retrospective cohort analysis design was used. The subjects were US nationwide members of military and their families. A total of 5608 patients who were on antidiabetic monotherapy for at least 1 year before adding a second agent to their medication regimen between October 2001 and September 2008 participated in this study. Mean age ranged from 64 to 71 years among the cohorts. Cox regression compared the progression to insulin, adjusting for demographics, months of follow-up and co-morbidities [measured with Chronic Disease Score (CDS)]. By the end of the 2- to 6-year follow-up period, 14.3% of the Met/TZD cohort, 23.6% of the Met/SU cohort and 28.2% of the SU/TZD cohort had insulin added to their regimen. Those in the Met/SU cohort had a 1.8 times higher probability of progression to insulin than those in the Met/TZD cohort [odds ratio (OR) = 1.80, 95% confidence interval (CI) = 1.51-2.14), and those in the SU/TZD cohort had a 2.5 times higher probability of progression to insulin than those in the Met/TZD cohort (OR = 2.51, 95% CI = 2.04-3.08). When sensitizers were paired (Met/TZD), a lower percentage of patients progressed to insulin during the study period, as opposed to patients who used a combination of a secretagogue with a sensitizer (SU/TZD or Met/SU). © 2013 John Wiley & Sons Ltd.

  18. Anti-diabetic activity of Holothuria thomasi saponin.

    Science.gov (United States)

    El Barky, Amira R; Hussein, Samy A; Alm-Eldeen, Abeer A; Hafez, Yehia A; Mohamed, Tarek M

    2016-12-01

    Diabetes mellitus represents a global health problem. It characterized by hyperglycemia that induces oxidative stress leading to a generation of free radicals. A wide variety of natural products in plants and other marine animals represent antioxidant activity and other health benefits like those of sea cucumber. Therefore, this study aimed to investigate the antidiabetic activity of glycosidic compound - saponin - derived from the Egyptian sea cucumber, Holothuria thomasi. Saponin has been extracted from the Egyptian sea cucumber and confirmed by hemolysis, Salkowski tests, FT/IR, UV and GC-MS analysis. Eighty white female albino rats were divided into four equal groups. The first two groups of rats; control normal and control normal saponin-treated groups. The last two groups which were made diabetic by intraperitoneal injection of streptozotocin had one diabetic control and the other diabetic group that got 300mg/kg B.wt. of saponin extract after Thirty-five days after diabetes induction and lasted for six weeks. The functional group of saponin extract which established with FT/IR spectroscopy demonstrated the presence of saponin in the extracted materials as shown in the peak of the functional group in relevance to the standard one. The UV spectra revealed that λ max of saponin extract was 282nm which in accordance to the standard saponin. Also, GC-MS analysis indicated that the aglycone part of saponin was methyl esters of octadecanoic acid. Saponin extract significantly decreased serum glucose, α-amylase activity, adiponectin, IL-6, TNF-α concentrations and liver L-MDA. However, serum insulin and liver glycogen levels were significantly increased as compared with the diabetic non-treated groups. The histopathological results supported that saponin extract markedly reduced the degenerative change in β-cells. This study, therefore, depicts that the Egyptian Holothuria thomasi, sea cucumber saponin as a hypoglycemic agent with the potential to normalize

  19. Antidiabetic and antioxidant activities of seed extract from Leucaena leucocephala (Lam. de Wit

    Directory of Open Access Journals (Sweden)

    Pichaya Chowtivannakul

    2016-09-01

    These results indicated that seed extract from L. leucocephala has antidiabetic and antioxidant activities. The antioxidant activity is likely due to the phenolic content. An application of this extract should be considered as it can affect renal function by reducing the levels of albumin, ALP and total protein.

  20. Weight Considerations in Pharmacotherapy for Type 2 Diabetes

    Directory of Open Access Journals (Sweden)

    Vicky Cheng

    2011-01-01

    Full Text Available Obesity has been increasing in prevalence worldwide and the majority of patients with type 2 diabetes are either overweight or obese. Diabetes management in this population has been difficult since a number of antidiabetes agents are associated with weight gain. The effects of various antidiabetes agents and antiobesity agents on glycemic control and body weight will be reviewed. Briefly, sulfonylureas, thiazolidinediones, and insulin are associated with weight gain, whereas metformin and amylin analogs are weight neutral or associated with modest weight loss. Dipeptidyl-peptidase-4 inhibitors are weight neutral, whereas glucagon-like peptide-1 analogs are associated with weight loss. The effect of orlistat and sibutramine in type 2 diabetes is also evaluated. The treatment of diabetes should not only focus on glycemic control as its sole intention, but it should factor in the effect of these various agents on weight, as well, since obesity aggravates insulin resistance, beta cell failure, and cardiovascular risk.

  1. In Vitro Antioxidant Effects of Aloe barbadensis Miller Extracts and the Potential Role of These Extracts as Antidiabetic and Antilipidemic Agents on Streptozotocin-Induced Type 2 Diabetic Model Rats

    Directory of Open Access Journals (Sweden)

    Md. Ibrahim Khalil

    2012-11-01

    Full Text Available In this study, the total phenolic and flavonoid contents, the 2,2-diphenyl-1-picryl hydrazyl (DPPH radical scavenging ability and the ferric reducing power (FRAP of Aloe vera were measured to determine the antioxidant activity of this species. The in vivo antidiabetic effects of the plant were also investigated using streptozotocin-induced type 2 diabetic model rats that were divided into five groups based on the treatment received: (1 water (WC; (2 glibenclamide; (3 concentrated gel extract (Gel-C; (4 ethanol (80% gel extract (Gel-Et; and (5 ethanol (80% skin extract of Aloe vera (Skin-Et. Skin-Et, which contained the highest level of total phenolics (62.37 ± 1.34 mggallic acid/kg and flavonoids (20.83 ± 0.77 mg/kg, exhibited the highest scavenging activity (85.01 ± 0.52% and the greatest reducing power (185.98 ± 0.41 µM, indicating that the skin contained the highest level of antioxidants. The oral consumption of Gel-Et for 4 weeks a caused significant reduction in the fasting serum glucose levels of the rats. The rats in the Gel-C-, Gel-Et- and Skin-Et-treated groups experienced a reduction in their total cholesterol levels by 11%, 17% and 25%, respectively and a reduction in their LDL cholesterol levels by 45%, 3% and 69%, respectively. The in vivo experimental antioxidant parameter MDA is strongly correlated with the in vitro antioxidant parameters of flavonoids and polyphenols, namely the DPPH and FRAP values (r = 0.94, 0.92, 0.93, 0.90, thus confirming the antioxidant potential of the Aloe vera extracts.

  2. Drug: D04966 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available D04966 Drug Metformin (USAN/INN) ... C4H11N5 D04966.gif ... Antidiabetic agent ... DG0168...5 ... Insulin sensitizer ... DG01684 ... Biguanide antidiabetic Unclassified ... DG02044 ... Hypoglycemics ... DG01684 ... Biguanide antidiabetic

  3. Continuous-Flow Synthesis of Deuterium-Labeled Antidiabetic Chalcones: Studies towards the Selective Deuteration of the Alkynone Core

    Directory of Open Access Journals (Sweden)

    Sándor B. Ötvös

    2016-03-01

    Full Text Available Flow chemistry-based syntheses of deuterium-labeled analogs of important antidiabetic chalcones were achieved via highly controlled partial C≡C bond deuteration of the corresponding 1,3-diphenylalkynones. The benefits of a scalable continuous process in combination with on-demand electrolytic D2 gas generation were exploited to suppress undesired over-reactions and to maximize reaction rates simultaneously. The novel deuterium-containing chalcone derivatives may have interesting biological effects and improved metabolic properties as compared with the parent compounds.

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

    Science.gov (United States)

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

    2011-12-01

    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 research. Data were obtained from population-based clinical databases in seven European countries. The study population comprised children aged 0-18 years. Prescriptions were categorized using the Anatomic Therapeutic Chemical (ATC) classification. The one-year user prevalence in 2008 was calculated for each country and stratified by age and sex. We studied a total of 5.8 million children and adolescents. The prevalence of insulin prescribing varied between 1.1 and 3.5 per 1000 population, being highest in Sweden and lowest in Italy. In all countries, novel insulin analogues were the most commonly used insulins. The prevalence of oral anti-diabetic prescribing ranged from 0.08 per 1000 individuals in Sweden and Germany to 0.21 per 1000 population in the UK. Overall, the absolute number of oral anti-diabetic users was very low. This study shows that there is a varying frequency of type 1 diabetes in children and adolescents across Europe. We also demonstrated that it is possible to obtain similar information from different clinical databases within Europe, which would allow continuous monitoring of type 1 diabetes. Owing to the lack of indications in most of the databases, this approach is less suitable for type 2 diabetes. © 2011 The Authors. British Journal of Clinical Pharmacology © 2011 The British Pharmacological Society.

  5. Antidiabetic and antioxidant functionality associated with phenolic constituents from fruit parts of indigenous black jamun (Syzygium cumini L.) landraces.

    Science.gov (United States)

    Gajera, H P; Gevariya, Shila N; Hirpara, Darshna G; Patel, S V; Golakiya, B A

    2017-09-01

    Fruit phenolics are important dietary antioxidant and antidiabetic constituents. The fruit parts (pulp, seed, seed coat, kernel) of underutilized indigenous six black jamun landraces ( Syzygium cumini L.), found in Gir forest region of India and differed in their fruit size, shape and weight, are evaluated and correlated with antidiabetic, DPPH radical scavenging and phenolic constituents. The α-amylase inhibitors propose an efficient antidiabetic strategy and the levels of postprandial hyperglycemia were lowered by restraining starch breakdown. The sequential solvent systems with ascending polarity-petroleum ether, ethyl acetate, methanol and water were performed for soxhlet extraction by hot percolation method and extractive yield was found maximum with methanolic fruit part extracts of six landraces. The methanolic extracts of fruit parts also evidenced higher antidiabetic activity and hence utilized for further characterization. Among the six landraces, pulp and kernel of BJLR-6 (very small, oblong fruits) evidenced maximum 53.8 and 98.2% inhibition of α-amylase activity, respectively. The seed attained inhibitory activity mostly contributed by the kernel fraction. The inhibition of DPPH radical scavenging activity was positively correlated with phenol constituents. An HPLC-PDA technique was used to quantify the seven individual phenolics. The seed and kernel of BJLR-6 exhibited higher individual phenolics-gallic, catechin, ellagic, ferulic acids and quercetin, whereas pulp evidenced higher with gallic acid and catechin as α-amylase inhibitors. The IC 50 value indicates concentration of fruit extracts exhibiting ≥50% inhibition on porcine pancreatic α-amylase (PPA) activity. The kernel fraction of BJLR6 evidenced lowest (8.3 µg ml -1 ) IC 50 value followed by seed (12.9 µg ml -1 ), seed coat (50.8 µg ml -1 ) and pulp (270 µg ml -1 ). The seed and kernel of BJLR-6 inhibited PPA at much lower concentrations than standard acarbose (24.7

  6. Evaluation of the Antidiabetic and Antibacterial Activity of Cissus sicyoides

    Directory of Open Access Journals (Sweden)

    Flavio Luis Beltrame

    2002-03-01

    Full Text Available In this work we investigated the antidiabetic and antibacterial effect of Cissus sicyoides (CS from Brazil. Diabetic rats that received water (A group or extracts from the aerial parts of the plant (Cs group during four weeks were employed. After this period, serum levels of glucose, cholesterol and triglycerides were measured. Glycemia was not affected by treatment with CS. However, there was an increased cholesterol and triglyceride level in Cs group. In addition, bioassay-guided fractionation of methanolic extract from aerial parts of CS was performed for isolation of antibacterial compounds.beta-Sitosterol and sitosterol-beta-D-glucopyranoside isolated showed antibacterial activity against Bacillus subtilis with minimal inhibitory concentrations (MICs of 50 mug/ml and 100 mug/ml, respectively. In spite of popular belief, CS did not show antidiabetic activity. However, two compounds isolated from aerial parts of the plant (beta-sitosterol and sitosterol-beta-D-glucopyranoside showed antibacterial activity.No presente trabalho foram investigados os efeitos antibacteriano e antidiabético da planta Cissus sicyoides (CS coletada no Brasil. Ratos diabéticos receberam água (grupo A ou extratos da parte aérea da planta (grupo CS durante 4 semanas. Após este período, os níveis séricos de glicose, colesterol e triglicerídeos dos ratos foram determinados. A glicemia não foi afetada pelo tratamento com CS. Entretanto, houve aumento nos níveis de colesterol e triglicerídeos nos ratos do grupo CS. Em adição, fracionamento bio-monitorado foi realizado para o isolamento de compostos com atividade antibacteriana. beta-Sitosterol e sitosterol-beta-D-glucopiranosídeo isolados mostram atividade antibacteriana contra Bacillus subtilis com concentrações mínimas inibitórias (MICs de 50 mig/ml e 100 mig/ml, respectivamente. Apesar da crença popular, CS não mostrou atividade antidiabética. Entretanto, dois compostos isolados da parte aérea da

  7. Effect of Anti-Parasite Chemotherapeutic Agents on Immune Reactions.

    Science.gov (United States)

    1980-08-01

    observations). Similar effects of a number of other alkylating agents have been noticed (9, and personal observa- tions). Similarly, corticosteroids inhibit...Wellham, L. L., and Sigel, M. M. Ef- fect of anti-cancer chemotherapeutic agents on immune reactions of mice. I. Comparison of two nitrosoureas . J...7 D-Ri138 852 EFFECT OF ANTI-PARASITE CHEMOTHERAPEUTIC AGENTS ON i/i IMMUNE REACTIONS(U) SOUTH CAROLINA UNIV COLUMBIA DEPT OF MICROBIOLOGY AND

  8. Anti-Diabetic Effects of Phenolic Extract from Rambutan Peels (Nephelium lappaceum) in High-Fat Diet and Streptozotocin-Induced Diabetic Mice.

    Science.gov (United States)

    Ma, Qingyu; Guo, Yan; Sun, Liping; Zhuang, Yongliang

    2017-07-26

    Recent studies have shown that rambutan peel phenolic (RPP) extract demonstrate high antioxidant and antiglycation activities in vitro and in vivo. This study further evaluated the anti-diabetic activity of RPP in a mouse model of Type II diabetes induced by streptozotocin combined with high-fat diet. Results showed that RPP increased the body weight and reduced the fasting blood glucose level of the diabetic mice. RPP significantly reduced the serum levels of total cholesterol, triglyceride, creatinine, and glycated serum protein in diabetic mice in a dose-dependent manner. Glycogen content in mice liver was recovered by RPP, which further increased the activity of superoxide dismutase and glutathione peroxidase and reduced lipid peroxidation in diabetic mice. Histological analysis showed that RPP effectively protected the tissue structure of the liver, kidney, and pancreas. In addition, RPP decreased the mesangial index and inhibited the expression of TGF-β in the kidney of diabetic mice.

  9. Development of Quality Control Method for Glucofarmaka Antidiabetic Jamu by HPLC Fingerprint Analysis

    Directory of Open Access Journals (Sweden)

    Hanifullah Habibie

    2017-04-01

    Full Text Available Herbal medicines become increasingly popular all over the world for preventive and therapeutic purposes. Quality control of herbal medicines is important to make sure their safety and efficacy. Chromatographic fingerprinting has been accepted by the World Health Organization as one reliable strategy for quality control method in herbal medicines. In this study, high-performance liquid chromatography fingerprint analysis was developed as a quality control method for glucofarmaka antidiabetic jamu. The optimum fingerprint chromatogram were obtained using C18 as the stationary phase and linear gradient elution using 10–95% acetonitrile:water as the mobile phase within 60 minutes of elution and detection at 210 nm. About 20 peaks were detected and could be used as fingerprint of glucofarmaka jamu. To evaluate the analytical performance of the method, we determined the precision, reproducibility, and stability. The result of the analytical performance showed reliable results. The proposed method could be used as a quality control method for glucofarmaka antidiabetic jamu and also for its raw materials.

  10. Comprehensive Evidence-Based Assessment and Prioritization of Potential Antidiabetic Medicinal Plants: A Case Study from Canadian Eastern James Bay Cree Traditional Medicine

    Directory of Open Access Journals (Sweden)

    Pierre S. Haddad

    2012-01-01

    Full Text Available Canadian Aboriginals, like others globally, suffer from disproportionately high rates of diabetes. A comprehensive evidence-based approach was therefore developed to study potential antidiabetic medicinal plants stemming from Canadian Aboriginal Traditional Medicine to provide culturally adapted complementary and alternative treatment options. Key elements of pathophysiology of diabetes and of related contemporary drug therapy are presented to highlight relevant cellular and molecular targets for medicinal plants. Potential antidiabetic plants were identified using a novel ethnobotanical method based on a set of diabetes symptoms. The most promising species were screened for primary (glucose-lowering and secondary (toxicity, drug interactions, complications antidiabetic activity by using a comprehensive platform of in vitro cell-based and cell-free bioassays. The most active species were studied further for their mechanism of action and their active principles identified though bioassay-guided fractionation. Biological activity of key species was confirmed in animal models of diabetes. These in vitro and in vivo findings are the basis for evidence-based prioritization of antidiabetic plants. In parallel, plants were also prioritized by Cree Elders and healers according to their Traditional Medicine paradigm. This case study highlights the convergence of modern science and Traditional Medicine while providing a model that can be adapted to other Aboriginal realities worldwide.

  11. Antioxidant and antidiabetic profiles of two African medicinal plants: Picralima nitida (Apocynaceae) and Sonchus oleraceus (Asteraceae).

    Science.gov (United States)

    Teugwa, Clautilde Mofor; Mejiato, Pascaline Chouadeu; Zofou, Denis; Tchinda, Bruno Tugnoua; Boyom, Fabrice Fekam

    2013-07-15

    Diabetes mellitus (DM) is a metabolic disease characterized by chronic hyperglycaemia generally associated with oxidative stress. The present study aims at evaluating the antioxidant and antidiabetic potential of methanol and hydroethanol extracts of the stem bark and leaves of Pricralima nitida and the Sonchus oleraceus whole plant respectively. The in vitro antioxidant activity was assessed using 1,1-Diphenyl-2-picrilhydrazyl (DPPH) for free radical-scavenging properties of the extracts, and the Folin-Ciocalteu method in determining their phenol contents. The antidiabetic activity was tested in mice following streptozotocin diabetes induction, and selected oxidative stress markers (Malondialdehyde, Hydrogen peroxides and Catalase) were measured in order to evaluate the level of oxidative stress in treated animals. The in vitro antioxidant activity using DPPH showed IC50 ranging from 0.19 ± 0.08 to 1.00 ± 0.06 mg/mL. The highest activity was obtained with the hydroethanol extracts of S. oleraceus (0.19 mg/mL and P. nitida (0.24 mg/mL). Polyphenol contents ranged from 182.25 ± 16.76 to 684.62 ± 46.66 μg Eq Cat/g. The methanol extract of P. nitida showed the highest activity, followed by the hydroethanol extract of S. oleraceus (616.89 ± 19.20 μEq Cat/g). The hydroethanol extract of whole plants (150 mg/Kg) and methanol leave extract of P. nitida (300 mg/Kg) exhibited significant antidiabetic activities with 39.40% and 38.48% glycaemia reduction, respectively. The measurement of stress markers in plasma, liver and kidney after administration of both extracts showed significant reduction in MDA and hydrogen peroxide levels, coupled with a substantial increase in catalase activity. These findings suggest that S. oleraceus whole plant and P. nitida leaves possess both antidiabetic and antioxidant properties, and therefore could be used as starting point for the development of herbal medicines and/or source of new drug molecules against

  12. Antidiabetic potential of Caesalpinia sumatrana, a medicinal herbs traditionally used by local tribe in East Kalimantan

    Science.gov (United States)

    Wicaksono, D. A.; Rosamah, E.; Kusuma, I. W.

    2018-04-01

    The aims of the research was to analyze the content of phytochemicals, to examine the antioxidant and antidiabeticpotentials of n-hexane, chloroform, ethyl acetate, and ethanol extracts of Caesalpinia sumatrana. Method to measure antioxidant capacity of sample involves the use of the free radical, 1,1-diphenyl-2-picrylhydrazyl (DPPH) which is widely used to test the ability of compounds to act as free radical. Analysis the potential of antidiabeticactivity of the extracts was determined by α-glucosidase and α-amylase inhibitory assay. Of all extracts obtained by successive maceration, ethanol maceration gave the highest extract by 2.63% of extract on the dry weigh basis. The result of phytochemicals showed that all extracts contain alkaloid and flavonoid. The highest antioxidant activity was 82.32% with IC50 value of 5.00 µg/ml obtained by ethanol extract. The results of enzyme inhibitory assay of α-glucosidase showed that ethanol extract of C. sumatrana had IC50 value 17.16 µg/mL to inhibit ɑ-glucosidase activity and IC50 value 16.78 µg/mL for ɑ-amylase. The present result displayed potential of the plant to be developed as natural antidiabetic and antioxidant agents.

  13. Behavioral effects of nerve agents: laboratory animal models

    International Nuclear Information System (INIS)

    Myers, T. M.

    2009-01-01

    Diverse and often subtle behavioral consequences have been reported for humans exposed to nerve agents. Laboratory studies of nerve agent exposure offer rigorous control over important variables, but species other than man must be used. Nonhuman primate models offer the best means of identifying the toxic nervous system effects of nerve agent insult and the countermeasures best capable of preventing or attenuating these effects. Comprehensive behavioral models must evaluate preservation and recovery of function as well as new learning ability. The throughput and sensitivity of the tests chosen are important considerations. A few nonhuman primate studies will be discussed to elaborate recent successes, current limitations, and future directions.(author)

  14. 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)

    Gagik Radikovich 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.

  15. 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.

    Science.gov (United States)

    Campbell-Tofte, Joan I A; Mølgaard, Per; Josefsen, Knud; Abdallah, Zostam; Hansen, Steen Honoré; Cornett, Claus; Mu, Huiling; Richter, Erik A; Petersen, Henning Willads; Nørregaard, Jens Christian; Winther, Kaj

    2011-01-27

    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 resulted in the normalization of blood sugar, reduction in lipid accumulated in the mice eyes and prevention of the degeneration of the otherwise brittle BKS-db pancreas. The tea is made by boiling foliage of Rauvolfia vomitoria and fruits of Citrus aurantium and is used to treat diabetes in Nigerian folk medicine. The RC tea was produced using the Nigerian traditional recipe and tested in the traditional dosage on 23 Danish type 2 diabetes (T2D) patients. The participants were divided into two equivalent groups after stratification by sex, age and BMI, in a 4-month double-blinded, placebo-controlled and randomized clinical trial. Most of the study subjects (19/23) were using oral anti-diabetic agents (OADs). Mean disease duration was 6±4.6 years, mean age was 64±7 years and mean BMI was 28.7±3.8 kg/m(2). Prior to starting the treatment, the participants received individual dietician consultations. At the end of the 4-month treatment period, the treated group showed an 11% decrease in 2-h postprandial plasma glucose relative to the 3% increase in the placebo group (p=0.004). The improvement in blood glucose clearance with RC tea treatment was reflected in a 6% reduction in HbA(1c) (p=0.02) and in a 10% reduction in fasting plasma glucose (p=0.02), when comparing the post 4-month treatment to pre-treatment baseline values. Though the basal levels of phosphorylated acetyl CoA carboxylase enzyme in skeletal muscle were significantly reduced in the treated group (p=0.04), as compared to the placebo, only the pattern of reductions in the tissue fatty acids (FAs) differed in the two groups. While all types of FAs were reduced in placebo, only saturated (SFA) and

  16. Effectiveness Of Different House-Hold Hand Washing Agents On ...

    African Journals Online (AJOL)

    Hand hygiene is a very important procedure in infection control. Washing agents commonly in use were investigated for their effectiveness in reducing hand floral and cotton towel was used as drying agent. Agents studied include; water alone, carex soap, dettol, and imperial leather. The hands were inoculated (deliberate ...

  17. Physicochemical properties and antidiabetic effects of a polysaccharide from corn silk in high-fat diet and streptozotocin-induced diabetic mice.

    Science.gov (United States)

    Pan, Yuxiang; Wang, Cong; Chen, Zhongqin; Li, Weiwei; Yuan, Guoqi; Chen, Haixia

    2017-05-15

    This study aimed to investigate the physicochemical properties and antidiabetic effects of a polysaccharide obtained from corn silk (PCS2). PCS2 was isolated and the physicochemical properties were characterized. The hypoglycemic effects were determined using the high-fat diet and streptozocin induced type 2 diabetic mellitus (T2DM) insulin resistance mice. The results showed that PCS2 was a heteropolysaccharide with the average molecular weight of 45.5kDa. PCS2 was composed of d-galactose, d-mannose, d-(+)-glucose, d-(+)-xylose, l-arabinose and l-rhamnose. PCS2 treatment significantly reduced the body weight loss, decreased blood glucose and serum insulin levels, and improved glucose intolerance (P<0.05). The levels of serum lipid profile were regulated and the levels of glycated serum protein, non-esterified fatty acid were decreased significantly (P<0.01). The activities of superoxide dismutase, glutathione peroxidase and catalase were notably improved (P<0.05). PCS2 also exerted cytoprotective action from histopathological observation. These results suggested that PCS2 could be a good candidate of functional food or medicine for T2DM treatment. Copyright © 2017 Elsevier Ltd. All rights reserved.

  18. The Action of Antidiabetic Plants of the Canadian James Bay Cree Traditional Pharmacopeia on Key Enzymes of Hepatic Glucose Homeostasis

    Directory of Open Access Journals (Sweden)

    Abir Nachar

    2013-01-01

    Full Text Available We determined the capacity of putative antidiabetic plants used by the Eastern James Bay Cree (Canada to modulate key enzymes of gluconeogenesis and glycogen synthesis and key regulating kinases. Glucose-6-phosphatase (G6Pase and glycogen synthase (GS activities were assessed in cultured hepatocytes treated with crude extracts of seventeen plant species. Phosphorylation of AMP-dependent protein kinase (AMPK, Akt, and Glycogen synthase kinase-3 (GSK-3 were probed by Western blot. Seven of the seventeen plant extracts significantly decreased G6Pase activity, Abies balsamea and Picea glauca, exerting an effect similar to insulin. This action involved both Akt and AMPK phosphorylation. On the other hand, several plant extracts activated GS, Larix laricina and A. balsamea, far exceeding the action of insulin. We also found a significant correlation between GS stimulation and GSK-3 phosphorylation induced by plant extract treatments. In summary, three Cree plants stand out for marked effects on hepatic glucose homeostasis. P. glauca affects glucose production whereas L. laricina rather acts on glucose storage. However, A. balsamea has the most promising profile, simultaneously and powerfully reducing G6Pase and stimulating GS. Our studies thus confirm that the reduction of hepatic glucose production likely contributes to the therapeutic potential of several antidiabetic Cree traditional medicines.

  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

    2014-01-01

    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 (4 h), 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. PMID:24912714

  20. Effect of sitagliptin on blood glucose control in patients with type 2 diabetes mellitus who are treatment naive or poorly responsive to existing antidiabetic drugs: the JAMP study.

    Science.gov (United States)

    Sakura, Hiroshi; Hashimoto, Naotake; Sasamoto, Kazuo; Ohashi, Hiroshi; Hasumi, Sumiko; Ujihara, Noriko; Kasahara, Tadasu; Tomonaga, Osamu; Nunome, Hideo; Honda, Masashi; Iwamoto, Yasuhiko

    2016-12-01

    To investigate the ameliorating effect of sitagliptin, a dipeptidyl peptidase-4 inhibitor, on blood glucose control in patients with type 2 diabetes mellitus who were previously untreated with or who have a poor responsive to existing antidiabetic drugs. Sitagliptin (50 mg/day) was added on to the pre-existing therapy for type 2 diabetes and changes in the glycated hemoglobin (HbA1c) level after 3 months of treatment were compared with the baseline and performed exploratory analysis. HbA1c levels were significantly decreased after 1 month of treatment compared to baseline, with a mean change in HbA1c level from baseline of -0.73% (range, -0.80 to -0.67) in the entire study population at 3 months. Patients who received a medium dose of glimepiride showed the least improvement in HbA1c levels. The percentage of patients who achieved an HbA1c level of blood glucose level of type 2 diabetes mellitus who were previously untreated with, or poorly responsive to, existing antidiabetic drugs. Thus, sitagliptin is expected to be useful in this patient group. However, the additional administration of sitagliptin in patients treated with medium-dose glimepiride only slightly improved blood glucose control when corrected for baseline HbA1c level.

  1. Antidiabetic actions of a phosphatidylcholine ligand for nuclear receptor LRH-1

    Science.gov (United States)

    Lee, Jae Man; Lee, Yoon Kwang; Mamrosh, Jennifer L.; Busby, Scott A.; Griffin, Patrick R.; Pathak, Manish C.; Ortlund, Eric A.; Moore, David D.

    2011-01-01

    Nuclear hormone receptors regulate diverse metabolic pathways and the orphan nuclear receptor LRH-1 (NR5A2) regulates bile acid biosynthesis1,2. Structural studies have identified phospholipids as potential LRH-1 ligands3–5, but their functional relevance is unclear. Here we show that an unusual phosphatidylcholine species with two saturated 12 carbon fatty acid acyl side chains (dilauroyl phosphatidylcholine, DLPC) is an LRH-1 agonist ligand in vitro. DLPC treatment induces bile acid biosynthetic enzymes in mouse liver, increases bile acid levels, and lowers hepatic triglycerides and serum glucose. DLPC treatment also decreases hepatic steatosis and improves glucose homeostasis in two mouse models of insulin resistance. Both the antidiabetic and lipotropic effects are lost in liver specific Lrh-1 knockouts. These findings identify an LRH-1 dependent phosphatidylcholine signaling pathway that regulates bile acid metabolism and glucose homeostasis. PMID:21614002

  2. 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.

  3. Anti-diabetic effect of amorphastilbol through PPARα/γ dual activation in db/db mice

    International Nuclear Information System (INIS)

    Lee, Woojung; Ham, Jungyeob; Kwon, Hak Cheol; Kim, Yong Kee; Kim, Su-Nam

    2013-01-01

    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. Drug–drug Interaction between Pravastatin and Gemfibrozil (Antihyperlipidemic) with Gliclazide (Antidiabetic) in Rats

    Science.gov (United States)

    Sultanpur, CM; Satyanarayana, S; Reddy, NS; Kumar, KE; Kumar, S

    2010-01-01

    Diabetes mellitus is a condition of increased blood glucose level in the body. Antihyperlipidemic drugs like statins and fibrates are widely used for prophylactic treatment in dyslipideamia and atherosclerosis. Diabetic dislipidemia exists with increased triglycerides, low HDL and high LDL levels. Hence, with oral hypoglycemic drugs, the addition of a lipid-lowering drug is necessary for controlling dislipidemia. In such a situation, there may be chances of drug–drug interactions between antidiabetic and antihyperlipidemic drugs. The present study is planned to evaluate the safety of gliclazide (antidiabetic) in the presence of pravastatin and gemfibrozil (antihyperlpidemic) in rats. Studies in normal and alloxan-induced diabetic rats were conducted with oral doses of gliclazide and their combination with pravastatin and gemfibrozil, with an adequate washout period in between the treatments. Blood samples were collected in rats by retroorbital puncture at 0, 1, 2, 3, 4, 6, 8, 10 and 12 h. All the blood samples were analyzed for glucose by GOD –POD. Gliclazide (½ TD) produced hypoglycemic activity in normal and diabetic rats, with peak activity at 2 and 8 h. Pravastatin (TD) + gemfibrozil (TD) combination treatment increased the hypoglycemic effect of gliclazide in normal rats or diabetic rats when administered together. The interaction observed due to inhibition of both the enzymes (CYP 450 2C9 and CYP 450 3A4) responsible for the metabolism of gliclazide showed increased half-life, which was seen in the present study. Because concomitant administration of gliclazide with provastatin and gemfibrozil in diabetes is associated with atherosclerosis, it should be contraindicated or used with caution. PMID:21264118

  5. Metformin, other antidiabetic drugs, and endometrial cancer risk: a nested case-control study within Italian healthcare utilization databases.

    Science.gov (United States)

    Franchi, Matteo; Asciutto, Rosario; Nicotra, Federica; Merlino, Luca; La Vecchia, Carlo; Corrao, Giovanni; Bosetti, Cristina

    2017-05-01

    Metformin may reduce the risk of endometrial cancer whereas other drugs for the treatment of type 2 diabetes mellitus appear to increase it, although the evidence is still limited. We investigated this issue using data from a nested case-control study within the healthcare utilization databases of the Lombardy Region, Italy. This study included 376 diabetic women with endometrial cancer and 7485 diabetic controls matched for cases on age, date at cohort entry, and duration of follow-up. We used conditional logistic regression models to estimate the odds ratio (OR) of endometrial cancer in relation to use of antidiabetic drugs, adjusted for the Charlson's comorbidity index, selected medical conditions, prescription of selected drugs, and concomitant use of other antidiabetic drugs. At cohort entry, no significant associations were observed for metformin [OR=0.99, 95% confidence interval (CI) 0.80-1.23], sulfonylureas (OR=1.14, 95% CI 0.91-1.42), insulin (OR=0.72, 95% CI 0.34-1.56), and other antidiabetic drugs (OR=1.21, 95% CI 0.75-1.95). When we considered use during follow-up, a borderline significant excess risk was found for metformin (OR=1.30, 95% CI 1.00-1.70). However, this estimate decreased to 1.07 (95% CI 0.82-1.41) when taking into account BMI using a Monte Carlo sensitivity analysis. No significant associations were found for sulfonylureas (OR=1.16, 95% CI 0.91-1.47), thiazolidinediones (OR=0.77, 95% CI 0.48-1.24), repaglinide (OR=1.32, 95% CI 0.94-1.87), incretins (OR=1.21, 95% CI 0.63-2.32), and insulin (OR=1.19, 95% CI 0.82-1.71). Our data indicate that metformin, insulin, and other antidiabetic drugs did not meaningfully affect the risk of endometrial cancer.

  6. Antidiabetic effect of Chloroxylon swietenia bark extracts on streptozotocin induced diabetic rats

    Directory of Open Access Journals (Sweden)

    B. Jayaprasad

    2016-03-01

    Full Text Available Diabetes has been increasing at an alarming rate around the world, and experts have relied on remedies from the utilization of ancient drugs that are essentially derived from plants. The present study aimed to evaluate the antidiabetic potential of Chloroxylon swietenia bark extracts on streptozotocin induced diabetic rats. Diabetes was induced in male albino Wistar rats by single intraperitoneal injection of streptozotocin (STZ (50 mg/kg b.w.. The diabetic rats were administered orally with C. swietenia bark (CSB methanolic (CSBMEt and aqueous (CSBAEt (250 mg/kg b.w. extracts and glibenclamide (600 µg/kg b.w. by intragastric intubation for 45 days. The result showed a heavy loss in weight, increase in blood glucose and glycosylated hemoglobin level, and decline in plasma insulin and total hemoglobin content. Furthermore, glucose-6-phosphatase and fructose-1,6-bis phosphatase were found to be increased whereas hexokinase and glycogen contents were decreased in STZ induced diabetic rats. CSBAEt, CSBMEt and glibenclamide treated diabetic rats showed moderate reduction in blood glucose and glycosylated hemoglobin levels; in addition, plasma insulin and hemoglobin levels were elevated. The altered activities of carbohydrate metabolizing enzymes and liver glycogen were improved remarkably. CSBMEt results were comparable to the standard drug glibenclamide. The present findings support the usage of the plant extracts for the traditional treatment of diabetes.

  7. Prescribing of Antidiabetic Medicines before, during and after Pregnancy : A Study in Seven European Regions

    NARCIS (Netherlands)

    Charlton, Rachel A.; Klungsoyr, Kari; Neville, Amanda J.; Jordan, Sue; Pierini, Anna; de Jong-van den Berg, Lolkje T. W.; Bos, H. Jens; Puccini, Aurora; Engeland, Anders; Gini, Rosa; Davies, Gareth; Thayer, Daniel; Hansen, Anne V.; Morgan, Margery; Wang, Hao; McGrogan, Anita; Andersen, Anne-Marie Nybo; Dolk, Helen; Garne, Ester

    2016-01-01

    Aim To explore antidiabetic medicine prescribing to women before, during and after pregnancy in different regions of Europe. Methods A common protocol was implemented across seven databases in Denmark, Norway, The Netherlands, Italy (Emilia Romagna/Tuscany), Wales and the rest of the UK. Women with

  8. Barriers of Adherence and Possible Solutions to Nonadherence to Antidiabetic Therapy in Women with Diabetes in Pregnancy: Patients’ Perspective

    Directory of Open Access Journals (Sweden)

    Doreen Mukona

    2017-01-01

    Full Text Available Diabetes in pregnancy contributes to maternal mortality and morbidity though it receives little attention in developing countries. The purpose of the study was to explore the barriers to adherence and possible solutions to nonadherence to antidiabetic therapy in women with diabetes in pregnancy. Antidiabetic therapy referred to diet, physical activity, and medications. Four focus group discussions (FGDs, each with 7 participants, were held at a central hospital in Zimbabwe. Included were women with a diagnosis of diabetes in pregnancy, aged 18 to 49 years, and able to speak Shona or English. Approval was obtained from respective ethical review boards. FGDs followed a semistructured questionnaire. Detailed notes were taken during the interviews which were also being audiotaped. Data were analysed thematically and manually. Themes identified were barriers and possible solutions to nonadherence to therapy. Barriers were poor socioeconomic status, lack of family, peer and community support, effects of pregnancy, complicated therapeutic regimen, pathophysiology of diabetes, cultural and religious beliefs, and poor health care system. Possible solutions were fostering social support, financial support, and improvement of hospital services. Individualised care of women with diabetes is essential, and barriers and possible solutions identified can be utilised to improve care.

  9. INVESTIGACIONES ETNOBOTÁNICAS, FITOQUÍMICAS, ANTIOXIDANTES Y PRECLÍNICAS EN CINCO PLANTAS MEDICINALES QUE SE CONSUMEN COMO ANTIDIABÉTICAS EN MACHALA, PROVINCIA DE EL ORO, ECUADOR | ETHNOBOTANICAL, PHYTOCHEMICAL, ANTIOXIDANT AND PRECLINICAL INVESTIGATIONS IN FIVE MEDICINAL PLANTS CONSUMED AS ANTIDIABETICS IN MACHALA, EL ORO PROVINCE, ECUADOR

    Directory of Open Access Journals (Sweden)

    Keyla Moreno Maldonado

    2016-08-01

    Full Text Available Diabetes is a serious public health problem worldwide. In Ecuador, diabetes is one of the first causes of human deaths. The community makes use of medicinal plants to treat diabetes, but without any scientific evaluation. Data about plants with antidiabetic activity were collected from oral surveys to herbalist retailers and consumers. Antidiabetic activity and acute toxicity were evaluated using Wistar rats (females and OF1 (females mice, respectively. The secondary metabolites and antioxidant capacity were quantitatively determined in plants with antidiabetic activity demonstrated in the preclinical study. The information obtained from oral surveys led to the identification of the medicinal plants that were mainly denominated as antidiabetics, the parts of the plants used and form of consumption for the treatment of diabetes. The plants Artemisia absintium, Cynara scolymus, Schkuhria pinnata, Chuquiraga jussieui y Taraxacum officinale were mostly nominated for the treatment of diabetes. However, only A. absinthium, C. scolymus and T. officinale presented antidiabetic activities and did not show preclinical acute toxicity in experimental animals at doses of 2000 mg/kg. This study shows that plants with antioxidant activities can be an effective therapy to prevent and fight chronic diseases such as diabetes.

  10. Quantal health effects for a combination of several toxic agents

    Energy Technology Data Exchange (ETDEWEB)

    Seiler, F A

    1988-12-01

    Quantal health effects caused by the combined action of a number of toxic agents are modeled using the information available for each toxicant acting in isolation. Two basic models are used; one assumes no interaction, the other postulates a separable kind of interaction in which each agent contributes an enhancement factor independent of all other agents. These two models provide yardsticks by which to measure synergisms and antagonisms in the interaction between the effects of toxic agents. Equations are given in approximations for small and large values of the risk. (author)

  11. Quantal health effects for a combination of several toxic agents

    International Nuclear Information System (INIS)

    Seiler, F.A.

    1988-01-01

    Quantal health effects caused by the combined action of a number of toxic agents are modeled using the information available for each toxicant acting in isolation. Two basic models are used; one assumes no interaction, the other postulates a separable kind of interaction in which each agent contributes an enhancement factor independent of all other agents. These two models provide yardsticks by which to measure synergisms and antagonisms in the interaction between the effects of toxic agents. Equations are given in approximations for small and large values of the risk. (author)

  12. Effect of once-daily insulin detemir on oral antidiabetic drug (OAD) use in patients with type 2 diabetes.

    Science.gov (United States)

    Vora, J; Caputo, S; Damci, T; Orozco-Beltran, D; Pan, C; Svendsen, A L; Sølje, K S; Khunti, K

    2014-04-01

    There are acknowledged benefits to continuing metformin when initiating insulin, but there appears to be growing concern over the role of sulphonylureas and thiazolidinediones when used in combination with insulin. This analysis investigates the effects of continuing or discontinuing oral antidiabetic drugs (OADs) following the initiation of once-daily insulin detemir. SOLVE is a 24-week, multinational observational study of insulin detemir initiation in patients with type 2 diabetes mellitus treated with one or more OADs. In the total cohort (n = 17 374), there were significant improvements in HbA1c (-1·3%, 95% CI -1·34; -1·27%) and weight (-0·6 kg, 95% CI -0·65; -0·47 kg), with an increase in the incidence rate of minor hypoglycaemia (+0·256 events ppy, P use either prior to (n = 17 086) or during insulin initiation (n = 16 346). HbA1c reductions were significantly greater in patients continuing treatment with metformin (-1·3% vs. -1·1%, P < 0·01), thiazolidinediones (-1·3% vs. -1·0%, P < 0·01) and DPP-IV inhibitors (-1·3% vs. -0·9%, P < 0·001). Final insulin doses were significantly greater in patients discontinuing treatment with sulphonylureas (0·29 vs. 0·26 IU/kg, P < 0·001), glinides (0·28 vs. 0·26 IU/kg, P < 0·01), thiazolidinediones (0·31 vs. 0·26 IU/kg, P < 0·001) and DPP-IV inhibitors (0·35 vs. 0·29 IU/kg, P < 0·001) compared with patients continuing these respective agents. All patient subgroups had a mean weight loss irrespective of OAD continuation, apart from those continuing thiazolidinediones (+0·2 kg). The largest improvements in weight were seen following the withdrawal of sulphonylureas and thiazolidinediones (-1·1 and -1·1 kg, respectively). Discontinuation (or switching) of OADs at the time of insulin initiation appears to be governed principally by concerns about hypoglycaemia and weight. HbA1c improvements were smaller in patients discontinuing OADs at the time of insulin

  13. Effective ODE Zones in a Multi- Agent System

    DEFF Research Database (Denmark)

    Hjorth, Poul G.

    Simulations which contain a large number of agents with rules for agent-agent interactions may grow to a level of complexity where it is cumbersome to extract useful information, difficult to split or agregate parts, and taxing on computational resources. We present here an example where a coarse...... graining of the system, and replacement of individual interactions with ODEs describing dynamical interactions between ‘effective zones’, leads to a fast and useful simplified model of the original complex system....

  14. The impact of anti-diabetic drugs on colorectal cancer risk in a large ...

    African Journals Online (AJOL)

    risk of cancers (1Б4). In Decensi et al.'s meta-analysis, a. 31% reduction of overall cancer risk (95% CI00.61Б0.79) is found in patients using metformin compared with the other anti-diabetic drugs (2). The present study also showed women with ever-use of metformin could have a. 58% reduced risk of colorectal cancer.

  15. Lowering Plasma Glucose Concentration by Inhibiting Renal Sodium-Glucose Co-Transport

    Science.gov (United States)

    Abdul-Ghani, Muhammad A; DeFronzo, Ralph A

    2017-01-01

    Maintaining normoglycaemia not only reduces the risk of diabetic microvascular complications but also corrects the metabolic abnormalities that contribute to the development and progression of hyperglycaemia (i.e. insulin resistance and beta-cell dysfunction). Progressive beta-cell failure, in addition to the multiple side effects associated with many current antihyperglycaemic agents (e.g., hypoglycaemia and weight gain) presents major obstacle to the achievement of the recommended goal of glycaemic control in patients with diabetes mellitus (DM). Thus, novel effective therapies are needed for optimal glucose control in subjects with DM. Recently, specific inhibitors of renal sodium glucose cotransporter 2 (SGLT2) have been developed to produce glucosuria and lower the plasma glucose concentration. Because of their unique mechanism of action (which is independent of the secretion and action of insulin), these agents are effective in lowering the plasma glucose concentration in all stages of DM and can be combined with all other antidiabetic agents. In this review, we summarize the available data concerning the mechanism of action, efficacy and safety of this novel class of antidiabetic agent. PMID:24690096

  16. In vitro evaluation of antioxidant and antidiabetic activities of Syzygium densiflrum fruits

    Directory of Open Access Journals (Sweden)

    Gopinath Krishnasamy

    2015-11-01

    Full Text Available Objective: To provide experimental support for the traditional knowledge of Syzygium densiflorum (S. densiflorum fruits. Methods: Powered S. densiflorum dried fruits were subjected to successive extraction with n-hexane, ethyl acetate, and ethanol using a Soxhlet extractor. Further, preliminary phytochemical screening was carried out with a series of tests. In vitro free radical scavenging was evaluated using total antioxidant estimation, 2,2-diphenyl-1-picrylhydrazyl radical, superoxide radical scavenging, and hydroxyl radical scavenging assays. Antidiabetic activity was estimated using α-amylase inhibition assay. Results: Preliminary phytochemical estimation confirmed the presence of alkaloids, flavonoids, sterols, terpenoids, anthocyanin, phenols, carbohydrates, fixed oils, and fats in fruits of S. densiflorum. Ethyl acetate and n-hexane extracts showed less free radical scavenging and α-amylase inhibition activity than ethanol extract. IC50 values of ethanol extracts for 2,2- diphenyl-1-picrylhydrazyl radical, superoxide radical, hydroxyl radical, lipid peroxidation, and α-amylase inhibition assays were found to be 0.01, 0.16, 0.66, 0.46, and 0.46 mg/mL respectively. Conclusions: In vitro evaluations confirmed the antioxidant and antidiabetic potential of S. densiflorum fruits. Ethanol extract of S. densiflorum fruits showed higher activity with statistical significance vs. ethyl acetate and n-hexane extracts.

  17. Drug: D01665 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available D01665 Drug Voglibose (JP17/USAN/INN); Basen (TN) ... C10H21NO7 D01665.gif ... Antidiabetic... agent ... DG01663 ... alpha-Glucosidase inhibitor ... DG01803 ... Antidiabetic, alpha-glucosidase inhibitor Uncla...ssified ... DG02044 ... Hypoglycemics ... DG01803 ... Antidiabetic, alpha-glucosidase inhibitor Therapeutic category: 3

  18. Hypoglycemic and antihyperglycemic effects of Anabasis articulata ...

    African Journals Online (AJOL)

    STORAGESEVER

    2009-10-19

    Oct 19, 2009 ... hyperglycemic mice (glucose treated and alloxan treated mice) to confirm the antidiabetic potential of ... Key word: Anabasis articulata, antihyperglycemic; diabetic mice; antidiabetic effect; saponin, alkaloids. ..... London, pp.

  19. Rapid identification of illegal synthetic adulterants in herbal anti-diabetic medicines using near infrared spectroscopy

    Science.gov (United States)

    Feng, Yanchun; Lei, Deqing; Hu, Changqin

    We created a rapid detection procedure for identifying herbal medicines illegally adulterated with synthetic drugs using near infrared spectroscopy. This procedure includes a reverse correlation coefficient method (RCCM) and comparison of characteristic peaks. Moreover, we made improvements to the RCCM based on new strategies for threshold settings. Any tested herbal medicine must meet two criteria to be identified with our procedure as adulterated. First, the correlation coefficient between the tested sample and the reference must be greater than the RCCM threshold. Next, the NIR spectrum of the tested sample must contain the same characteristic peaks as the reference. In this study, four pure synthetic anti-diabetic drugs (i.e., metformin, gliclazide, glibenclamide and glimepiride), 174 batches of laboratory samples and 127 batches of herbal anti-diabetic medicines were used to construct and validate the procedure. The accuracy of this procedure was greater than 80%. Our data suggest that this protocol is a rapid screening tool to identify synthetic drug adulterants in herbal medicines on the market.

  20. Antidiabetic therapy in real practice: indicators for adherence and treatment cost

    Directory of Open Access Journals (Sweden)

    Colombo GL

    2012-09-01

    Full Text Available Giorgio L Colombo,1,2 Elisa Rossi,4 Marisa De Rosa,4 Danilo Benedetto,3 Antonio V Gaddi31School of Pharmacy, Department of Drug Sciences, University of Pavia, Pavia, 2S.A.V.E. Studi Analisi Valutazioni Economiche, Milan, 3CINECA – Bologna; 4Centro Aterosclerosi GC Descovich, Dipartimento di Medicina Interna e dell'Invecchiamento, University of Bologna, Bologna, ItalyBackground: Type 2 diabetes has become a disease with a high economic and social impact. The ARNO Observatory is a clinical data warehouse consisting of a network of local health care units (ASL scattered throughout the Italian territory which collects data on health care consumption for about 10.5 million people. The purpose of this study was to evaluate the use of antidiabetic drugs with particular reference to type of treatment. The analyses were carried out on a sample of 169,375 patients treated with oral blood glucose-lowering drugs in 2008 from a total population of 4,040,624 health care beneficiaries at 12 local health care units in the ARNO Observatory.Methods: Patients were considered “on treatment with oral blood glucose-lowering drugs” if they had received at least one prescription of an antidiabetic drug (Anatomical Therapeutic Chemical code A10B during 2008. The patients were divided into three treatment groups, ie, monotherapy, fixed-combination drugs, and dual therapy. The following indicators were assessed: number of patients treated with an oral antidiabetic drug, mean number of hospitalizations, mean number of specialist examinations, and mean expenditure per treated patient. Adherence was assessed using the medication possession ratio indicator (MPR.Results: Patients treated with oral blood glucose-lowering drugs comprised 4.2% of the investigated population, and had an average age of 68.9 years. The mean annual number of hospitalizations was lower in the dual therapy group (298 versus 328 per 1000 patients in the sample, while the average number of

  1. Renal sodium-glucose cotransporter inhibition in the management of type 2 diabetes mellitus

    Science.gov (United States)

    Abdul-Ghani, Muhammad A.; Norton, Luke

    2015-01-01

    Hyperglycemia is the primary factor responsible for the microvascular, and to a lesser extent macrovascular, complications of diabetes. Despite this well-established relationship, approximately half of all type 2 diabetic patients in the US have a hemoglobin A1c (HbA1c) ≥7.0%. This is associated in part with the side effects, i.e., weight gain and hypoglycemia, of currently available antidiabetic agents and in part with the failure to utilize medications that reverse the basic pathophysiological defects present in patients with type 2 diabetes. The kidney has been shown to play a central role in the development of hyperglycemia by excessive production of glucose throughout the sleeping hours and enhanced reabsorption of filtered glucose by the renal tubules secondary to an increase in the threshold at which glucose spills into the urine. Recently, a new class of antidiabetic agents, the sodium-glucose cotransporter 2 (SGLT2) inhibitors, has been developed and approved for the treatment of patients with type 2 diabetes. In this review, we examine their mechanism of action, efficacy, safety, and place in the therapeutic armamentarium. Since the SGLT2 inhibitors have a unique mode of action that differs from all other oral and injectable antidiabetic agents, they can be used at all stages of the disease and in combination with all other antidiabetic medications. PMID:26354881

  2. Hydroxychloroquine: Looking into the Future

    Directory of Open Access Journals (Sweden)

    Chakravorty Saibal

    2017-12-01

    Full Text Available Hydroxychloroquine, an antimalarial agent has also been found to possess antidiabetic action. Onset of type-2 diabetes (T2DM and cardiovascular disease is now considered to be the outcome of systemic inflammation. Many clinical trials are targeting systemic inflammation to reduce cardiovascular risk. Anti-inflammatory drugs with cardiovascular effects may be valuable therapeutic intervention to reduce massive cardiovascular risk in T2DM. In this review, antidiabetic action and potential cardioprotective role of hydroxychloroquine has been discussed. By virtue of its antidiabetic, lipid lowering, anti-platelet, anticoagulant and anti-inflammatory properties, hydroxychloroquine can be a key therapeutic alternative to manage patients with T2DM.

  3. Long term trends in oral antidiabetic drug use among children and adolescents in the Netherlands

    NARCIS (Netherlands)

    S. Fazeli Farsani; P. Souverein (Patrick); J.A. Overbeek (Jetty); M.M.J. Van Der Vorst; C.A.J. Knibbe (Catherijne); R.M.C. Herings (Ron); A.C. de Boer (Anton); A.K. Mantel-Teeuwisse (Aukje)

    2015-01-01

    textabstractAim The aim of the study was to document long term trends in oral antidiabetic drug (OAD) use among children and adolescents in the Netherlands. Methods A population-based cohort study was conducted using the Dutch PHARMO Database Network. All patients younger than 20 years old with at

  4. The effects of Ficus carica on the activity of enzymes related to metabolic syndrome

    Directory of Open Access Journals (Sweden)

    Ramgopal Mopuri

    2018-01-01

    Full Text Available The present study aimed to investigate the effects of the various parts of Ficus carica L. (figs on antioxidant, antidiabetic, and antiobesogenic effects in vitro. Fruit, leaves, and stembark of the F. carica plant were sequentially extracted using organic and inorganic solvents and their total polyphenol and flavonoid contents were estimated. The effects of the extracts on antioxidative, antidiabetic (inhibition of α-amylase and α-glucosidase enzymes, and antiobesogenic (antilipase activities were measured using several experimental models. The fruit ethanolic extract contained a high quantity of polyphenols and flavonoids (104.67±5.51 μg/mL and 81.67±4.00 μg/mL compared with all other extracts. The activity of the ethanolic extract of F. carica fruit was significantly (p<0.05 higher than all other extracts and parts of the plant in terms of antioxidative, antidiabetic, and antiobesogenic effects. The IC50 values of the fruit ethanolic extract in terms of antioxidative (134.44±18.43 μg/mL, and inhibition of α-glucosidase (255.57±36.46 μg/mL, α-amylase (315.89±3.83 μg/mL, and pancreatic lipase (230.475±9.65 μg/mL activity indicate that the activity of fruit ethanolic extract is better than all other extracts of the plant. The gas chromatography–mass spectroscopy analysis of the fruit ethanolic extract showed the presence of a number of bioactive compounds such as butyl butyrate, 5-hydroxymethyl furfural, 1-butoxy-1-isobutoxy butane, malic acid, tetradecanoic acid, phytol acetate, trans phytol, n-hexadecanoic acid, 9Z,12Z-octadecadienoic acid, stearic acid, sitosterol, 3,5-dihydroxy-6-methyl-2,3-dihydro-4H-pyran-4-one, and 2,4,5-trimethyl-2,4-dihydro-3H-pyrazol-3-one. The results of this study suggest that the ethanolic extract of the fruit of F. carica may have potential antidiabetic and antiobesogenic agents.

  5. EXPERIENCE WITH THE ROSINSULIN C IN COMBINATION WITH ORAL ANTIDIABETIC DRUGS IN PATIENTS WITH TYPE 2 DIABETES IN ROUTINE CLINICAL PRACTICE

    Directory of Open Access Journals (Sweden)

    O. D. Rymar

    2014-01-01

    Full Text Available This study aimed to estimate the efficacy and safety of intermediate-acting insulin Rosinsulin C in patients with type 2 diabetes mellitus inadequately controlled with oral antidiabetic drugs.The present study is a 6-month, prospective, uncontrolled, clinical experience evaluation study using insulin Rosinsulin С for type 2 diabetes patients in daily clinical practice. Episodes of hypoglycaemia, adverse events were recorded. The study included 28 patients with type 2 diabetes, 4 men and 24 women who treated with metformin in combination with sulfonylureas in the highest dose. Indicators of glycosylated hemoglobin (HbA1c of 8 to 14%, the median HbA1c was 11 (10; 13% of patients age 65 (57; 72 years, body mass index – 33 (30; 35 kg/m2, waist circumference – 105 (99; 111 cm, diabetes duration – 7 (2; 11 years. With the introduction of Rosinsulin С cartridges carried pen Autopen. At the start of the study and after 3 and 6 months, determined the level of HbA1c, fasting plasma glucose.After 6 months' treatment with Rosinsulin С in combination with oral antidiabetic drugs HbA1c was significantly lowered (–3% (p = 0,001, fasting plasma glucose level decreased by 5 mmol/L (p = 0,001. There was not severe hypoglycemia during the observation period.This research showed that Rosinsulin C is effective and safe in the treatment of patients with type 2 diabetes who were decompensated with oral antidiabetic drugs and can be recommended for use as the initiation of insulin therapy in routine clinical practice.

  6. An Effective Method for Protecting the Integrity of Mobile Agent

    OpenAIRE

    YARAHMADI, H.; KAMANKESH, M.

    2015-01-01

    Abstract. A mobile agent is software which performs an action autonomously and independently as a person or organizations assistance. Mobile agents are used for searching information, retrieval information, filtering, intruder recognition in networks, and so on. One of the important issues of mobile agent is their security. It must consider different security issues in effective and secured usage of mobile agent. One of those issues is the integrity’s protection of mobile agents.In this paper...

  7. Dgroup: DG01684 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available DG01684 DGroup Biguanide antidiabetic -formin DG01684.gif DG00112 ... Phenformin ... D08... hydrochloride (JP17) ... D04103 ... Etoformin hydrochloride (USAN) Antidiabetic agen...t ... DG01685 ... Insulin sensitizer Unclassified ... DG02044 ... Hypoglycemics ATC code: A10BA Antidiabetics AMPK (PRKAA) [HSA:5562 5563] [KO:K07198] ...

  8. Drug: D00625 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available D00625 Drug Miglitol (JP17/USAN/INN); Glyset (TN) ... C8H17NO5 D00625.gif ... Antidiabetic... agent ... DG01663 ... alpha-Glucosidase inhibitor ... DG01803 ... Antidiabetic, alpha-glucosidase inhibitor Unclas...sified ... DG02044 ... Hypoglycemics ... DG01803 ... Antidiabetic, alpha-glucosidase inhibitor Same as: C07708 Therapeu

  9. Drug: D00944 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available D00944 Drug Metformin hydrochloride (JP17/USP); Glucophage (TN) ... C4H11N5. HCl D00944.gif ... Antidiabetic... agent ... DG01685 ... Insulin sensitizer ... DG01684 ... Biguanide antidiabetic Unclassified ... DG...02044 ... Hypoglycemics ... DG01684 ... Biguanide antidiabetic Therapeutic category: 3962 ATC code: A10BA02 Chemical

  10. Cost-Effective Location Management for Mobile Agents on the Internet

    Directory of Open Access Journals (Sweden)

    Chien-Sheng Chen

    2015-01-01

    Full Text Available Many mobile agent system-related services and applications require interacting with a mobile agent by passing messages. However, an agent’s mobility raises several challenges in delivering messages to a mobile agent accurately. Consisting of tracking and message delivery phases, most mobile agent location management schemes create or receive many update messages and interaction messages to ensure the effectiveness of the schemes. In addition to downgrading the overall performance of a mobile agent location management scheme, excessive transmission of messages increases the network load. The migration locality of a mobile agent and the interaction rate between mobile agents significantly affect the performance of a mobile agent location management scheme with respect to location management cost. This work presents a novel Dual Home based Scheme (DHS that can lower the location management costs in terms of migration locality and interaction rate. While the DHS scheme uniquely adopts dual home location management architecture, a selective update strategy based on that architecture is also designed for cost-effective location management of mobile agents. Moreover, DHS is compared with available schemes based on formulations and simulation experiments from the perspective of location management costs. Simulation results demonstrate that the proposed DHS scheme performs satisfactorily in terms of migration locality and interaction rate.

  11. Dgroup: DG00112 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available DG00112 Chemical ... DGroup Phenformin ... D08351 ... Phenformin (BAN) D08352 ... Phenformin hydrochloride Antidiabeti...c agent ... DG01685 ... Insulin sensitizer ... DG01684 ... Biguanide antidiabetic Cyp substrat...e ... DG01644 ... CYP2D6 substrate Unclassified ... DG02044 ... Hypoglycemics ... DG01684 ... Biguanide antidiabetic ATC code...: A10BA01 Biganide antidiabetics AMPK (PRKAA) [HSA:5562 5563] [KO:K07198] Enzyme: CYP2D6 [HSA:1565] ...

  12. An embodiment effect in computer-based learning with animated pedagogical agents.

    Science.gov (United States)

    Mayer, Richard E; DaPra, C Scott

    2012-09-01

    How do social cues such as gesturing, facial expression, eye gaze, and human-like movement affect multimedia learning with onscreen agents? To help address this question, students were asked to twice view a 4-min narrated presentation on how solar cells work in which the screen showed an animated pedagogical agent standing to the left of 11 successive slides. Across three experiments, learners performed better on a transfer test when a human-voiced agent displayed human-like gestures, facial expression, eye gaze, and body movement than when the agent did not, yielding an embodiment effect. In Experiment 2 the embodiment effect was found when the agent spoke in a human voice but not in a machine voice. In Experiment 3, the embodiment effect was found both when students were told the onscreen agent was consistent with their choice of agent characteristics and when inconsistent. Students who viewed a highly embodied agent also rated the social attributes of the agent more positively than did students who viewed a nongesturing agent. The results are explained by social agency theory, in which social cues in a multimedia message prime a feeling of social partnership in the learner, which leads to deeper cognitive processing during learning, and results in a more meaningful learning outcome as reflected in transfer test performance.

  13. Management of diabetic complications through fruit flavonoids as a natural remedy.

    Science.gov (United States)

    Tanveer, Amna; Akram, Kashif; Farooq, Umar; Hayat, Zafar; Shafi, Afshan

    2017-05-03

    Diabetes mellitus is a global disorder, and a major issue for health care systems. The current review outlooks the use of fruit flavonoids as natural remedy in the prevention of diabetes mellitus. The onset of diabetes mainly depends upon genetics and lifestyle issues. Currently used therapeutic options for the control of diabetes, like dietary amendments, oral hypoglycemic drugs, and insulin, have their own limitations. Fruit flavonoids possess various antidiabetic, anti-inflammatory, and antioxidant potentials and act on various cellular signaling pathways in pancreas, white adipose tissue, skeletal muscle, and liver function, which in result induces antidiabetic effects. Recently, antidiabetic effect of fruit flavonoids has been studied using various animal models and clinical trials. Research studies revealed a statistically significant potential of fruit flavonoids in managing the altered glucose and oxidative metabolisms in diabetes. Unlike synthetic antidiabetic agents, fruit flavonoids manage diabetes without compromising cellular homeostasis thereby posing no side effects. Further studies are required in purification and characterization of different fruit flavonoids with respect to their beneficial effect for diabetic patients.

  14. Phytochemical, antioxidant and antidiabetic evaluation of eight Bauhinia L. species from Egypt using UHPLC-PDA-qTOF-MS and chemometrics.

    Science.gov (United States)

    Farag, Mohamed A; Sakna, Sarah T; El-Fiky, Nabaweya M; Shabana, Marawan M; Wessjohann, Ludger A

    2015-11-01

    Bauhinia L. (Fabaceae) comprises ca. 300-350 plant species, many of which are traditionally used in folk medicine for their antidiabetic, antioxidant and anti-inflammatory effects. Bauhinia s.l. recently has been subdivided into 9 genera based on phylogenetic data: Bauhinia s.str., Barklya, Brenierea, Gigasiphon, Lysiphyllum, Phanera, Piliostigma, Schnella (American Phanera) and Tylosema. The aerial parts of 8 species corresponding to 5 genera were analyzed: Bauhinia forficata, Bauhinia variegata, B. variegata var. candida, Bauhinia galpinii, Schnella glabra, Piliostigma racemosa, Phanera vahlii and Lysiphyllum hookeri. Leaves and shoots were subjected to metabolite profiling via UHPLC-PDA-qTOF-MS coupled to multivariate data analyzes to identify compound compositional differences. A total of 90 metabolites were identified including polyphenols and fatty acids; flavonoid conjugates accounted for most of the metabolite variation observed. This study provides a comprehensive map of polyphenol composition in Bauhinia and phytochemical species aggregations are consistent with recent Bauhinia genus taxonomic relationship derived from phylogenetic studies. DPPH radical scavenging and α-glucosidase inhibitory assays were also performed to assess selected aspects of the antioxidant and antidiabetic potential for the examined species with respect to metabolite profiles. Copyright © 2015 Elsevier Ltd. All rights reserved.

  15. Evaluation of antidiabetic property of Andrographis paniculata powder in high fat and sucrose-induced type-2 diabetic adult male rat

    Directory of Open Access Journals (Sweden)

    Anne Williams Augustine

    2014-02-01

    Full Text Available Objective: To evaluate the antidiabetic effect of the aerial part of Andrographis paniculata (A. paniculata powder (500 mg/kg body weight in high fat and sucrose-induced type-2 diabetic rat model. Methods: The fasting blood glucose, oral glucose tolerance test, serum insulin, lipid profile, mRNA and protein levels of insulin signaling molecules, 14C-2 deoxy glucose uptake and 14C glucose oxidation in liver were checked. Results: In the type-2 diabetes-induced group, the fasting blood glucose, oral glucose tolerance, serum insulin, lipid profile, glucose uptake and oxidation, Akt and glucose transporter 2 mRNA, insulin receptor and glucose transporter 2 protein (both cytosolic and plasma membrane and phosphorylation of insulin receptor substrate 1 and Akt were impaired. A. paniculata was able to successfully reinstate this impairment. In addition to this, A. paniculata did not cause a hypoglycemic condition in normal rat, affirming its activity in hyperglycemic state alone. Conclusions: A. paniculata possesses significant antidiabetic and antihyperlipidemic activities in high fat and sucrose-induced type-2 diabetic rat and the molecular actions at the level of insulin signaling molecules in liver reinforce it.

  16. Long term trends in oral antidiabetic drug use among children and adolescents in the Netherlands

    NARCIS (Netherlands)

    Fazeli Farsani, S; Souverein, P C; Overbeek, J A; van der Vorst, M M J; Knibbe, C A J; Herings, R M C; de Boer, Anthonius; Mantel-Teeuwisse, A K

    AIM: The aim of the study was to document long term trends in oral antidiabetic drug (OAD) use among children and adolescents in the Netherlands. METHODS: A population-based cohort study was conducted using the Dutch PHARMO Database Network. All patients younger than 20 years old with at least one

  17. The effects of water soluble contrast agents on the respiratory tract

    International Nuclear Information System (INIS)

    Lovett, I.; Donchey, S.; Doust, B.; Branson, J.; Munro, V.

    1989-01-01

    The water soluble contrast agents Gastrografin R (Sodium diatrizoate and meglumine diatrizoate, Schering, Berlin), Iopamiro 300 R (Iopamidol, Schering, Berlin), and Dionosil Aqueous R (propyliodone BP, Glaxo, England) were instilled into the tracheobronchial tree of rats in doses of either 0.1 ml and 0.25 ml. Rats being used as controls, underwent sham operations with the instillation of air instead of contrast agent. In all, 85 rats were used. All rats that had not already died from the effects of contrast agent were sacrificed 30 minutes after instillation. The relative effects of the contrast agents were measured by comparing: survival time; radiographic effects of the contrast agents on the lungs; and pathological changes as estimated by post mortem lung section and microscopy. The least toxic agent was the one with the lowest osmotic activity, namely Aqueous Dionosil. It is therefore recommended that Aqueous Dionosil be used in preference to Gastrografin or Iopamidol for studies of the oesophagus whenever there is a danger of aspiration of contrast agent into the tracheobronchial tree. 11 refs., 3 figs., 5 tabs

  18. Phytochemical distribution in hull and cotyledon of adzuki bean (Vigna angularis L.) and mung bean (Vigna radiate L.), and their contribution to antioxidant, anti-inflammatory and anti-diabetic activities.

    Science.gov (United States)

    Luo, Jiaqiang; Cai, Weixi; Wu, Tong; Xu, Baojun

    2016-06-15

    Total saponin content, total phenolics content, total flavonoids content, condensed tannin content in hull, cotyledon and whole grain of both adzuki bean and mung bean were determined by colorimetric methods. Vitexin and isovitexin contents in mung bean were determined by HPLC. Antioxidant effects were evaluated with DPPH scavenging activity and ferric reducing antioxidant power assay. In vitro anti-inflammatory and anti-diabetic effects of beans were evaluated by protease and aldose reductase inhibitory assays, respectively. The results indicated that the bean hulls were the most abundant in phytochemicals and largely contributed antioxidant activities, anti-inflammatory effects and anti-diabetic effects of whole grains. The result showed that mung bean hull was the most abundant with vitexin at 37.43 mg/g and isovitexin at 47.18 mg/g, respectively. Most of the phytochemicals and bioactivities were most predominantly contributed by the bean hulls with exception for condensed tannin of mung bean; which was more abundant in the cotyledon than its hull. Copyright © 2016 Elsevier Ltd. All rights reserved.

  19. Drug: D02206 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available D02206 Drug Buformin hydrochloride (JP17); Dibetos-B (TN) ... C6H15N5. HCl D02206.gif ... Antidiabetic... agent ... DG01685 ... Insulin sensitizer ... DG01684 ... Biguanide antidiabetic Unclassified ... DG02044 ... Hypoglycemics ... DG01684 ... Biguanide antidiabetic Therapeutic category: 3962 ATC code: A10BA03 Chemical group

  20. Level Of Extension Agents Motivation And Effectiveness In Abia State Nigeria.

    Directory of Open Access Journals (Sweden)

    Machiadikwe N. Benjamin Agbarevo Nwogu

    2015-08-01

    Full Text Available Motivation is known to affect effectiveness of workers but the level of extension agents motivation and how this has affected their effectiveness in Abia state is apparently unknown. A study was therefore conducted to determine the effect of motivation on effectiveness of extension agents in Abia State Nigeria. Two blocks were selected from each of the three zones in the state at the first stage giving total of 6 blocks. The second stage involved the selection of two sub-circles from each of the 6 blocks selected giving a total of 12 extension sub-circles. At the third stage 10 extension agents from each of the sub-circles were randomly selected giving a sample size of 120 extension agents. The data for the study was collected with use of a structured questionnaire. The extension agents level of motivation and effectiveness were measured with the aid of a 5 point Likert rating scale. Data collected was analyzed using both descriptive and inferential statistics. Descriptive statistics used were the mean frequencies and the Pearsons Product Moment Correlation Co-efficient which was used to determine the coefficient of correlation r . The inferential statistic used was the t-test of significance of relationship. The study found a significant relationship between the level of motivation and effectiveness of extension agents. Hence the null hypothesis which stated that there is no significant relationship between the level of motivation and effectiveness of extension agents was rejected and the alternative hypothesis accepted at 95 confidence level and 119 degrees of freedom.

  1. Studies on the antidiabetic activities of Momordica charantia fruit juice in streptozotocin-induced diabetic rats.

    Science.gov (United States)

    Mahmoud, Mona F; El Ashry, Fatma El Zahraa Z; El Maraghy, Nabila N; Fahmy, Ahmed

    2017-12-01

    Momordica charantia Linn (Cucurbitaceae) (MC) is used in folk medicine to treat various diseases including diabetes mellitus. This study investigates the antidiabetic activities of Momordica charantia (bitter gourd) on streptozotocin-induced type 2 diabetes mellitus in rats. Male Wister rats were randomly assigned to 4 groups. Group I, Normal control; Group II, STZ diabetic; Group III and IV, Momordica charantia fruit juice was orally administered to diabetic rats (10 mL/kg/day either as prophylaxis for 14 days before induction of diabetes then 21 days treatment, or as treatment given for 21 days after induction of diabetes). The effects of MC juice were studied both in vivo and in vitro by studying the glucose uptake of isolated rat diaphragm muscles in the presence and absence of insulin. Histopathological examination of pancreas was also performed. This study showed that MC caused a significant reduction of serum glucose (135.99 ± 6.27 and 149.79 ± 1.90 vs. 253.40* ± 8.18) for prophylaxis and treatment respectively, fructosamine (0.99 ± 0.01 and 1.01 ± 0.04 vs. 3.04 ± 0.07), total cholesterol, triglycerides levels, insulin resistance index (1.13 ± 0.08 and 1.19 ± 0.05 vs. 1.48 ± 1.47) and pancreatic malondialdehyde content (p Momordica charantia presents excellent antidiabetic and antioxidant activities and thus has great potential as a new source for diabetes treatment whether it is used for prophylaxis or treatment.

  2. Type of Preadmission Antidiabetic Treatment and Outcome among Patients with Ischemic Stroke: A Nationwide Follow-up Study

    DEFF Research Database (Denmark)

    Horsdal, Henriette Thisted; Mehnert, Frank; Rungby, Jørgen

    2012-01-01

    BACKGROUND: We examined whether the preadmission use of sulfonylureas is associated with improved clinical outcome compared with other antidiabetic treatments after hospitalization with ischemic stroke. METHODS: We conducted a nationwide population-based follow-up study among all Danish patients...... computed mortality rates and rates of readmission recurrent ischemic stroke or myocardial infarction according to type of treatment and used the Cox proportional hazards regression analysis to compute hazard ratios (HRs). RESULTS: We identified 4817 stroke patients with type 2 diabetes mellitus. We found...... lower 30-day mortality rates among users of metformin (adjusted HR 0.32; 95% confidence interval [CI] 0.15-0.68), insulin (adjusted HR 0.47; 95% CI 0.27-0.81), and patients without antidiabetic pharmacotherapy (adjusted HR 0.58; 95% CI 0.36-0.93) compared with users of sulfonylureas. Users of any...

  3. Garlic used as an alternative medicine to control diabetic mellitus in alloxan-induced male rabbits

    International Nuclear Information System (INIS)

    Mahesar, H.; Bhutto, M.A.; Khand, A.A.

    2010-01-01

    Herbal medicines are widely used because of their effectiveness, less side effects and low cost, so investigation on such agents from traditional medicinal plants has become more important in present day studies on medical sciences. Garlic is one of the most popular herbs used as an anti-diabetic agent. In present study possible anti diabetic effects of garlic were studied in alloxan induced diabetic male rabbits, compared to normal control and diabetic control male rabbits. The blood samples were collected every third day and anti-diabetic effects of garlic were observed every time. The serum cholesterol level and body weight were also studied. With an aqueous extract of garlic (1% solution/Kg) body weight for 30 days significantly lowered serum glucose level (38.88%) and serum cholesterol level (57%). Results and Conclusion: The results indicate that garlic possesses a beneficial anti-hyperglycaemic effect in alloxan-induced rabbits. (author)

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

    Directory of Open Access Journals (Sweden)

    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.

  5. In silico, in vitro and in vivo analyses of dipeptidyl peptidase IV inhibitory activity and the antidiabetic effect of sodium caseinate hydrolysate.

    Science.gov (United States)

    Hsieh, Cheng-Hong; Wang, Tzu-Yuan; Hung, Chuan-Chuan; Jao, Chia-Ling; Hsieh, You-Liang; Wu, Si-Xian; Hsu, Kuo-Chiang

    2016-02-01

    The frequency (A), a novel in silico parameter, was developed by calculating the ratio of the number of truncated peptides with Xaa-proline and Xaa-alanine to all peptide fragments from a protein hydrolyzed with a specific protease. The highest in vitro DPP-IV inhibitory activity (72.7%) was observed in the hydrolysate of sodium caseinate by bromelain (Cas/BRO), and the constituent proteins of bovine casein also had relatively high A values (0.10-0.17) with BRO hydrolysis. 1CBR (the <1 kDa fraction of Cas/BRO) showed the greatest in vitro DPP-IV inhibitory activity of 77.5% and was used for in vivo test by high-fat diet-fed and low-dose streptozotocin-induced diabetic rats. The daily administration of 1CBR for 6 weeks was effective to improve glycaemic control in diabetic rats. The results indicate that the novel in silico method has the potential as a screening tool to predict dietary proteins to generate DPP-IV inhibitory and antidiabetic peptides.

  6. Real-world antidiabetic drug use and fracture risk in 12,277 patients with type 2 diabetes mellitus: a nested case-control study.

    Science.gov (United States)

    Losada, E; Soldevila, B; Ali, M S; Martínez-Laguna, D; Nogués, X; Puig-Domingo, M; Díez-Pérez, A; Mauricio, D; Prieto-Alhambra, D

    2018-06-02

    We conducted a nested case-control study to study the association between antidiabetic treatments (alone or in combination) use and fracture risk among incident type 2 Diabetes mellitus patients. We found an increased risk of bone fracture with insulin therapy compared to metformin monotherapy. Patients with type 2 diabetes mellitus (T2DM) have an increased risk of fragility fractures, to which antidiabetic therapies may contribute. We aimed to characterize the risk of fracture associated with different antidiabetic treatments as usually prescribed to T2DM patients in actual practice conditions. A case-control study was nested within a cohort of incident T2DM patients registered in 2006-2012 in the Information System for Research Development in Primary Care (Catalan acronym, SIDIAP), a database which includes records for > 5.5 million patients in Catalonia (Spain). Each case (incident major osteoporotic fracture) was risk-set matched with up to five same-sex controls by calendar year of T2DM diagnosis and year of birth (± 10 years). Study exposure included previous use of all antidiabetic medications (alone or in combination), as dispensed in the 6 months before the index date, with metformin (MTF) monotherapy, the most commonly used drug, as a reference group (active comparator). Data on 12,277 T2DM patients (2049 cases and 10,228 controls) were analyzed. Insulin use was associated with increased fracture risk (adjusted OR 1.63 (95% CI 1.30-2.04)), as was the combination of MTF and sulfonylurea (SU) (adjusted OR 1.29 (1.07-1.56)), compared with MTF monotherapy. Sensitivity analyses suggest possible causality for insulin therapy but not for the MTF + SU combination association. No significant association was found with any other antidiabetic medications. Insulin monotherapy was associated with an increased fracture risk compared to MTF monotherapy in T2DM patients. Fracture risk should be taken into account when starting a glucose-lowering drug as part

  7. 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.

  8. Dgroup: DG00116 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available litazone maleate (JAN/USAN) ... Antidiabetic agent ... DG01685 ... Insulin sensitizer ... DG01795 ... PPAR gamma agonist...44 ... Hypoglycemics ... DG01683 ... Thiazolidinedione ATC code: A10BG02 Antidiabetic, th

  9. Dgroup: DG01735 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available glinide (JP17/USAN/INN) ... D01854 ... Mitiglinide calcium hydrate (JP17) ... Antidiabetic agent Unclassified ... DG02044 ... Hypoglycemics ... Antidiabetics ABCC8 (SUR1) [HSA:6833] [KO:K05032] ...

  10. Effectiveness of a biological control agent Palexorista gilvoides in ...

    African Journals Online (AJOL)

    ACSS

    Effectiveness of a biological control agent Palexorista gilvoides in controlling Gonometa podorcarpi in conifer ... gilvoides as a potential biological control agent for G. podocarpi. Field and laboratory studies further established that P. .... version for windows (SPSS, 2002). Results. Gonometa podocarpi was present in.

  11. Drug: D08352 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available D08352 Drug Phenformin hydrochloride; Debei (TN) ... C10H15N5. HCl D08352.gif ... Antidiabetic... agent ... DG01685 ... Insulin sensitizer ... DG01684 ... Biguanide antidiabetic Cyp substrate ... DG01644 ... CYP2D6... substrate Unclassified ... DG02044 ... Hypoglycemics ... DG01684 ... Biguanide antidiabetic ATC code: A10BA01 Chemical

  12. Cost-Effective Location Management for Mobile Agents on the Internet

    OpenAIRE

    Chien-Sheng Chen; Jiing-Dong Hwang; Chyuan-Der Lu; Ting-Yuan Yeh

    2015-01-01

    Many mobile agent system-related services and applications require interacting with a mobile agent by passing messages. However, an agent’s mobility raises several challenges in delivering messages to a mobile agent accurately. Consisting of tracking and message delivery phases, most mobile agent location management schemes create or receive many update messages and interaction messages to ensure the effectiveness of the schemes. In addition to downgrading the overall performance of a mobile ...

  13. Oral antidiabetic therapy in a large Italian sample: drug supply and compliance for different therapeutic regimens

    CERN Document Server

    Vittorino Gaddi, A; Capello, F; Di Pietro, C; Cinconze, E; Rossi, E; De Sando, V; Cevenini, M; D'Alò, G

    2014-01-01

    Objectives: To define the main features of patients treated with oral antidiabetics, evaluating monotherapy (MT), loose-dose combination therapy (LDCT) and fixed-dose combination therapy (FDCT); to describe medication adherence to the different therapies; and to evaluate the differences in compliance with the prescribed therapy regimen among prevalent and incident patient cohorts. Study design: This study was a retrospective cohort analysis based on the ARNO database, a national record that tracks reimbursable prescription claims submitted from selected pharmacies to the Italian national health system. In total, 169,375 subjects, from an overall population of 4,040,624 were included in this study. The patients represented 12 different local health units. Each patient had at least one oral antidiabetic prescription claim (A10B ATC code). Methods: Patients were divided into four groups according to their treatment regimen during the recruitment period (1 January 2008-31 December 2008): MT, FDCT, LDCT and swi...

  14. Chlorogenic Acid and Rutin Play a Major Role in the In Vivo Anti-Diabetic Activity of Morus alba Leaf Extract on Type II Diabetic Rats

    Science.gov (United States)

    Hunyadi, Attila; Martins, Ana; Hsieh, Tusty-Jiuan; Seres, Adrienn; Zupkó, István

    2012-01-01

    The leaves of the white mulberry tree (Morus alba L.) are used worldwide in traditional medicine as anti-diabetics. Various constituents of mulberry leaves, such as iminosugars (i.e. 1-deoxynojirimicin), flavonoids and related compounds, polysaccharides, glycopeptides and ecdysteroids, have been reported to exert anti-diabetic activity, but knowledge about their contribution to the overall activity is limited. The objective of the present work was to determine the in vivo anti-diabetic activity of an extract of mulberry leaves (MA), and to examine to what extent three major constituents, chlorogenic acid, rutin and isoquercitrin, might contribute to the observed activity. Quantities of the three constituents of interest in the extract were determined by using HPLC-DAD. Activity was determined by using a type II diabetic rat model. After 11 days of per os administration of 250 or 750 mg/kg of MA or the corresponding amounts of each individual compound, a dose dependent decrease of non-fasting blood glucose levels were found for MA, chlorogenic acid and rutin, but not for isoquercitrin. Based on our results, chlorogenic acid and rutin might account for as much as half the observed anti-diabetic activity of MA, hence they can be considered as excellent markers for the quality control of mulberry products. PMID:23185641

  15. Diabesity: are weight loss medications effective?

    Science.gov (United States)

    Halpern, Alfredo; Mancini, Marcio C

    2005-01-01

    Weight reduction has been shown to improve glycemic control and cardiovascular risk factors associated with insulin resistance in obese individuals with type 2 diabetes mellitus. Therapeutic options for these patients include promoting weight loss (non-pharmacologic and pharmacologic treatment) and improving glycemic control, as well as treating common associated risk factors such as arterial hypertension and dyslipidemias. This article provides an overview of anti-obesity drugs used in the treatment of obese individuals with type 2 diabetes. The most widely investigated drugs, sibutramine and orlistat, result in modest, clinically worthwhile weight loss, with demonstrable improvements in many co-morbidities, among them, type 2 diabetes. Clinical trials with these anti-obesity medications in cohorts of obese diabetic patients have been reviewed as well as cathecolaminergic agents (diethylpropion [amfepramone], fenproporex, mazindol, ephedrine-caffeine combination), serotoninergic drugs (fenfluramine, dexfenfluramine, fluoxetine), and other drugs that have some action on weight loss (the antidiabetic agent metformin, anti-epileptic agents topiramate and zonisamide, and the antidepressive bupropion [amfebutamone]). These trials show variable benefits in terms of effects on glucose profiles.

  16. Prescribing of Antidiabetic Medicines before, during and after Pregnancy: A Study in Seven European Regions.

    Science.gov (United States)

    Charlton, Rachel A; Klungsøyr, Kari; Neville, Amanda J; Jordan, Sue; Pierini, Anna; de Jong-van den Berg, Lolkje T W; Bos, H Jens; Puccini, Aurora; Engeland, Anders; Gini, Rosa; Davies, Gareth; Thayer, Daniel; Hansen, Anne V; Morgan, Margery; Wang, Hao; McGrogan, Anita; Nybo Andersen, Anne-Marie; Dolk, Helen; Garne, Ester

    2016-01-01

    To explore antidiabetic medicine prescribing to women before, during and after pregnancy in different regions of Europe. A common protocol was implemented across seven databases in Denmark, Norway, The Netherlands, Italy (Emilia Romagna/Tuscany), Wales and the rest of the UK. Women with a pregnancy starting and ending between 2004 and 2010, (Denmark, 2004-2009; Norway, 2005-2010; Emilia Romagna, 2008-2010), which ended in a live or stillbirth, were identified. Prescriptions for antidiabetic medicines issued (UK) or dispensed (non-UK) during pregnancy and/or the year before or year after pregnancy were identified. Prescribing patterns were compared across databases and over calendar time. 1,082,673 live/stillbirths were identified. Pregestational insulin prescribing during the year before pregnancy ranged from 0.27% (CI95 0.25-0.30) in Tuscany to 0.45% (CI95 0.43-0.47) in Norway, and increased between 2004 and 2009 in all countries. During pregnancy, insulin prescribing peaked during the third trimester and increased over time; third trimester prescribing was highest in Tuscany (2.2%) and lowest in Denmark (0.5%). Of those prescribed an insulin during pregnancy, between 50.5% in Denmark and 88.8% in the Netherlands received an insulin analogue alone or in combination with human insulin, this proportion increasing over time. Oral products were mainly metformin and prescribing was highest in the 3 months before pregnancy. Metformin use during pregnancy increased in some countries. Pregestational diabetes is increasing in many areas of Europe. There is considerable variation between and within countries in the choice of medication for treating pregestational diabetes in pregnancy, including choice of insulin analogues and oral antidiabetics, and very large variation in the treatment of gestational diabetes despite international guidelines.

  17. Prescribing of Antidiabetic Medicines before, during and after Pregnancy: A Study in Seven European Regions.

    Directory of Open Access Journals (Sweden)

    Rachel A Charlton

    Full Text Available To explore antidiabetic medicine prescribing to women before, during and after pregnancy in different regions of Europe.A common protocol was implemented across seven databases in Denmark, Norway, The Netherlands, Italy (Emilia Romagna/Tuscany, Wales and the rest of the UK. Women with a pregnancy starting and ending between 2004 and 2010, (Denmark, 2004-2009; Norway, 2005-2010; Emilia Romagna, 2008-2010, which ended in a live or stillbirth, were identified. Prescriptions for antidiabetic medicines issued (UK or dispensed (non-UK during pregnancy and/or the year before or year after pregnancy were identified. Prescribing patterns were compared across databases and over calendar time.1,082,673 live/stillbirths were identified. Pregestational insulin prescribing during the year before pregnancy ranged from 0.27% (CI95 0.25-0.30 in Tuscany to 0.45% (CI95 0.43-0.47 in Norway, and increased between 2004 and 2009 in all countries. During pregnancy, insulin prescribing peaked during the third trimester and increased over time; third trimester prescribing was highest in Tuscany (2.2% and lowest in Denmark (0.5%. Of those prescribed an insulin during pregnancy, between 50.5% in Denmark and 88.8% in the Netherlands received an insulin analogue alone or in combination with human insulin, this proportion increasing over time. Oral products were mainly metformin and prescribing was highest in the 3 months before pregnancy. Metformin use during pregnancy increased in some countries.Pregestational diabetes is increasing in many areas of Europe. There is considerable variation between and within countries in the choice of medication for treating pregestational diabetes in pregnancy, including choice of insulin analogues and oral antidiabetics, and very large variation in the treatment of gestational diabetes despite international guidelines.

  18. SGLT2 Inhibitors: Glucotoxicity and Tumorigenesis Downstream the Renal Proximal Tubule?

    Science.gov (United States)

    Bertinat, Romina; Nualart, Francisco; Yáñez, Alejandro J

    2016-08-01

    At present, diabetes mellitus is the main cause of end-stage renal disease. Effective glycaemic management is the most powerful tool to delay the establishment of diabetic complications, such as diabetic kidney disease. Together with reducing blood glucose levels, new anti-diabetic agents are expected not only to control the progression but also to restore known defects of the diabetic kidney. Sodium-glucose co-transporter 2 (SGLT2) inhibitors are promising anti-diabetic agents that reduce hyperglycaemia by impairing glucose reabsorption in proximal tubule of the kidney and increasing glucosuria. SGLT2 inhibitors have shown to reduce glucotoxicity in isolated proximal tubule cells and also to attenuate expression of markers of overall kidney damage in experimental animal models of diabetes, but the actual renoprotective effect for downstream nephron segments is still unknown and deserves further attention. Here, we briefly discuss possible undesired effects of enhanced glucosuria and albuminuria in nephron segments beyond the proximal tubule after SGLT2 inhibitor treatment, offering new lines of research to further understand the renoprotective action of these anti-diabetic agents. Strategies blocking glucose reabsorption by renal proximal tubule epithelial cells (RPTEC) may be protective for RPTEC, but downstream nephron segments will still be exposed to high glucose and albumin levels through the luminal face. The actual effect of constant enhanced glucosuria over distal nephron segments remains to be established. J. Cell. Physiol. 231: 1635-1637, 2016. © 2015 Wiley Periodicals, Inc. © 2015 Wiley Periodicals, Inc.

  19. 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.

  20. Dgroup: DG01803 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available DG01803 DGroup Antidiabetic, alpha-glucosidase inhibitor -bose ... D00216 ... Acarbose (...e (USAN) D09779 ... Emiglitate (JAN/INN) Antidiabetic agent ... DG01663 ... alpha-Glucosidase inhibitor Unclassified ... DG02044 ... Hypoglycemics ATC code: A10BF Antidiabetics GAA [HSA:2548] [KO:K12316] GANC [HSA:2595] [KO:K12317] MGAM [HSA:8972] [KO:K12047] ...

  1. Drug: D08351 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available D08351 Drug Phenformin (BAN) ... C10H15N5 D08351.gif ... Antidiabetic agent ... DG01685 ... ...Insulin sensitizer ... DG01684 ... Biguanide antidiabetic Cyp substrate ... DG01644 ... CYP2D6 substrate Unclassified ... ...DG02044 ... Hypoglycemics ... DG01684 ... Biguanide antidiabetic Same as: C07673 ATC code: A10BA01 Chemical group: D

  2. Drug: D04103 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available D04103 Drug Etoformin hydrochloride (USAN) ... C8H19N5. HCl D04103.gif ... Antidiabetic... agent ... DG01685 ... Insulin sensitizer ... DG01684 ... Biguanide antidiabetic Unclassified ... DG02044 ... Hypoglycemics ... ... DG01684 ... Biguanide antidiabetic ... Biganides ... CAS: 53597-26-5 PubChem: 47206055 ChEMBL: CHEMBL2106592 LigandBox: D04103 NIKKAJI: J244.891B ...

  3. Drug: D03342 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available D03342 Drug Camiglibose (USAN) ... (C13H25NO9)2. 3H2O D03342.gif ... Antidiabetic agen...t ... DG01663 ... alpha-Glucosidase inhibitor ... DG01803 ... Antidiabetic, alpha-glucosidase inhibitor Unclassified ... D...G02044 ... Hypoglycemics ... DG01803 ... Antidiabetic, alpha-glucosidase inhibitor ... CAS: 132438-21-2 PubChem: 17397492 LigandBox: D03342 ...

  4. Impact of long-term antihypertensive and antidiabetic medications on the prognosis of post-surgical colorectal cancer: the Fujian prospective investigation of cancer (FIESTA) study.

    Science.gov (United States)

    Peng, Feng; Hu, Dan; Lin, Xiandong; Liang, Binying; Chen, Ying; Zhang, Hejun; Xia, Yan; Lin, Jinxiu; Zheng, Xiongwei; Niu, Wenquan

    2018-05-24

    Hypertension and diabetes mellitus are common comorbidities of colorectal cancer. We designed a prospective cohort study aiming to investigate the impact of long-term antihypertensive and antidiabetic medications on colorectal cancer-specific survival and recurrence among 713 post-surgical patients. All participants received radical resection for colorectal cancer during 2000-08, and they were followed up until July 2017. Colorectal cancer patients without hypertension had better survival than those with hypertension (median survival time [MST]: 190.3 months versus 99.0 months, p colorectal cancer survival was statistically significant, that is, patients receiving antidiabetic medications had longer survival time than untreated diabetic patients (MST: 135.8 months versus 80.2 months, p : 0.007), whereas the prognosis was greatly improved in colorectal cancer patients without diabetes mellitus ( p colorectal cancer relative to those without medications, respectively. Our data indicate that long-term antidiabetic medications can significantly prolong the survival and improve the prognosis of post-surgical colorectal cancer.

  5. Dgroup: DG01732 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available (USAN/INN) D09350 ... Indeglitazar (USAN) Antidiabetic agent ... DG01685 ... Insulin sens...itizer ... DG01795 ... PPAR gamma agonist Other ... DG01733 ... PPAR agonist ... Antidiabetics, PPAR agonist NR1C1 (PPARA)

  6. Effects of Cocoa Antioxidants in Type 2 Diabetes Mellitus

    Directory of Open Access Journals (Sweden)

    Sonia Ramos

    2017-10-01

    Full Text Available Type 2 Diabetes mellitus (T2D is the most common form of diabetes and one of the most common chronic diseases. Control of hyperglycaemia by hypoglycaemic drugs is insufficient in for patients and nutritional approaches are currently being explored. Natural dietary compounds such as flavonoids, abundant in fruits and vegetables, have received broad attention because of their potential capacity to act as anti-diabetic agents. Especially cocoa flavonoids have been proved to ameliorate important hallmarks of T2D. In this review, an update of the most relevant reports published during the last decade in cell culture, animal models and human studies is presented. Most results support an anti-diabetic effect of cocoa flavonoids by enhancing insulin secretion, improving insulin sensitivity in peripheral tissues, exerting a lipid-lowering effect and preventing the oxidative and inflammatory damages associated to the disease. While it could be suggested that daily consumption of flavanols from cocoa or dark chocolate would constitute a potential preventive tool useful for the nutritional management of T2D, this recommendation should be cautious since most of commercially available soluble cocoa products or chocolates contain low amount of flavanols and are rich in sugar and calories that may aggravate glycaemic control in T2D patients.

  7. Anti-Diabetic Potential of Ocimum gratissimum Leaf Fractions in Fortified Diet-Fed Streptozotocin Treated Rat Model of Type-2 Diabetes

    Directory of Open Access Journals (Sweden)

    Stanley I. R. Okoduwa

    2017-10-01

    Full Text Available Background: Ocimum gratissimum (OG is used in the traditional management of diabetes in Nigeria. This study investigated the anti-diabetic potential of OG leaf fractions (OGLF in a rat model of Type-2 diabetes (T2D. Method: Methanol crude extract of OG leaf was fractionated with solvents of increasing order of polarity (n-hexane, chloroform, ethyl-acetate, n-butanol and water. The anti-diabetic potential of the fractions was evaluated in vivo. T2D was induced in Albino Wistar rats and treated with OGLF. Result: The T2D rats showed significant elevation in serum levels of fasting blood glucose (FBG, liver and kidney function biomarkers. At 4-weeks of intervention with OGLF, the untreated diabetic control group maintained severe hyperglycaemia in the presence of 61.7% serum insulin, 17.3% pancreatic β-cell function (HOMA-β and 51.5% Insulin sensitivity. The glucose tolerance ability was enhanced in the n-butanol-fraction (OGb treated group. With 74.8% available serum insulin and 38.6% improvement in insulin sensitivity, the OGb treated group had a 63.5% reduction in FBG and it was found to be most effective as it ameliorates a majority of the changes caused in the studied parameters in diabetic rats. Conclusions: The data from this study suggest that OGb fraction is a potential candidate for the development of an effective drug for the management of T2D.

  8. Dgroup: DG01683 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available /INN) D05739 ... Rivoglitazone (USAN/INN) Antidiabetic agent ... DG01685 ... Insulin sensitizer ... DG01795 ... PPAR gamma... agonist Other ... DG01733 ... PPAR agonist Unclassified ... DG02044 ... Hypoglycemics ATC code: A10BG Antidiabetic

  9. Dgroup: DG01794 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available rtugliflozin (USAN/INN) D10669 ... Sotagliflozin (USAN/INN) Antidiabetic agent Uncla...ssified ... DG02044 ... Hypoglycemics ATC code: A10BK Antidiabetics SLC5A2 (SGLT2) [HSA:6524] [KO:K14382] ...

  10. Dgroup: DG00122 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available Dapagliflozin propanediol (USAN); Dapagliflozin propylene glycolate hydrate (JAN) ... Antidiabetic agent ... DG0...1794 ... SGLT2 inhibitor Unclassified ... DG02044 ... Hypoglycemics ... DG01794 ... SGLT2 inhibitor ATC code: A10BK01 Antidiabetic

  11. Dgroup: DG00115 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available 7 ... Tolbutamide sodium, sterile Antidiabetic agent ... DG01790 ... Sulfonamide hypoglycemic ... DG01734 ... Sulfonamide ... ... DG01734 ... Sulfonamide type sulfonylurea receptor agonist ATC code: A10BB03 V04CA01 Antidiabetic, sulfonylu

  12. Dgroup: DG01283 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available igliptin hydrobromide hydrate (JAN) ... Antidiabetic agent ... DG01601 ... DPP-4 inhibitor Unclassified ... DG02044 ... H...ypoglycemics ... DG01601 ... DPP-4 inhibitor ... DPP4 inhibitor, antidiabetics DPP4 [HSA:1803] [KO:K01278] ...

  13. Antidiabetic effects of Artemisia sphaerocephala Krasch. gum, a novel food additive in China, on streptozotocin-induced type 2 diabetic rats.

    Science.gov (United States)

    Xing, Xiao-Hui; Zhang, Zheng-Mao; Hu, Xin-Zhong; Wu, Rui-Qin; Xu, Chao

    2009-09-25

    Since ancient times, practicians of traditional Chinese medicine have discovered that Artemisia sphaerocephala Krasch. (Asteraceae) seed powder was useful for the treatment of diabetes. Artemisia sphaerocephala Krasch. gum (ASK gum), which is extracted from seed powder of the plant, is a novel food additive favored by the food industry in China. The objective of this study was to determine the antidiabetic function of ASK gum on type 2 diabetes. Type 2 diabetic rat model was induced with high fat diet and low dose of streptozotocin (STZ). The effects of ASK gum on hyperglycemia, hyperlipemia, insulin resistance, and liver fat accumulation in type 2 diabetic rats were evaluated. The results were compared to those of normal rats and diabetic rats treated with metformin. The addition of ASK gum to the rats' food supply significantly lowered fasting blood glucose, glycated serum protein, serum cholesterol, and serum triglyceride in type 2 diabetic rats, and significantly elevated liver glucokinase, liver glycogen, and serum high density protein cholesterol in the diabetic rats. ASK gum significantly reduced insulin resistance and liver fat accumulation of type 2 diabetes. Artemisia sphaerocephala Krasch. gum can alleviate hyperglycemia, hyperlipemia and insulin resistance of type 2 diabetes.

  14. Role of antioxidants in phytomedicine with special reference to antidiabetic herbs

    Directory of Open Access Journals (Sweden)

    Papiya Mitra Mazumder

    2012-10-01

    Full Text Available Diabetes mellitus is a severe health problem with continuously increasing rates of incidence and mortality and it may rise tremendously by 2025. This disease is characterized by elevated plasma glucose concentrations resulting from insufficient insulin and insulin resistance, or both, leading to metabolic abnormalities in carbohydrates, lipids and proteins. Free radicals are well known for their dual role as beneficial and toxic components, higher levels of free radicals causing damage to cellular proteins, membrane lipids and nucleic acids leads to cell death. Antioxidants are effective against free radicals by donating their own electrons. There is an increasing evidence confirmed that free radicals plays a crucial role in the pathogenesis of diabetes mellitus. Herbs are the well known source of non toxic antioxidants. The aim of the present review is to establish the role of free radicals in pathogenesis of various diseases with special consideration to diabetes mellitus. Further more recently reported herbs with antidiabetic action having antioxidant capacity is also with in the scope of this article..

  15. 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.

  16. Dgroup: DG01663 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available DG01663 DGroup alpha-Glucosidase inhibitor -bose, -glustat ... DG01803 ... Antidiabetic,...at ... D09605 ... Duvoglustat (USAN/INN) ... D09606 ... Duvoglustat hydrochloride (USAN) Antidiabetic agent ... alpha-glucosidase [KO:K12316 K12317 K12047] ...

  17. Effect of Biological and Chemical Ripening Agents on the Nutritional ...

    African Journals Online (AJOL)

    Effect of Biological and Chemical Ripening Agents on the Nutritional and Metal Composition of Banana ( Musa spp ) ... Journal Home > Vol 18, No 2 (2014) > ... curcas leaf were used and compared with a control with no ripening agent.

  18. In vitro antidiabetic activity of various crude extracts of Boletus variipes

    Science.gov (United States)

    Muniandy, Sutha; Fazry, Shazrul; Daud, Fauzi; Senafi, Sahidan

    2015-09-01

    Diabetes mellitus is a complex metabolic disease that progressively spread worldwide and difficult to treat due to various physical and metabolic complications. Current treatment using synthetic drugs has lead to various undesirable side effects. Here we determined the effect of Boletus variipes extracts on diabetes related enzymes. In this study, hot water, cold water and methanol extracts of B. variipes were utilized in order to assess their in vitro antidiabetic activity by measuring the effect on α-amylase and α-glucosidase enzyme. Hot water extract possessed the highest inhibition activity of α-amylase and α-glucosidase in a concentration dependent manner with the IC50 value 87 mg/mL and 89 mg/mL respectively. The methanol extract also showed inhibition activity of α-amylase and α-glucosidase but significantly lower than the hot water extract. Whereas cold water extract did not show any inhibition activity towards both the enzymes. Therefore, it is hypothesized that the hot water extract of Boletus variipes contains bioactive compound that can inhibit alpha-amylase and alpha-glucosidase enzyme activity. At the request of all authors of the paper an updated version was published on 11 May 2016. The original version identified the species of mushroom as Boletus variipes, but new findings have proved the species of mushroom to be Boletus qriseipurpureus. The species name has been updated throughout the revised version of this paper.

  19. Effect of different prokinetic agents and a novel enterokinetic agent on postoperative ileus in rats

    NARCIS (Netherlands)

    de Winter, B. Y.; Boeckxstaens, G. E.; de Man, J. G.; Moreels, T. G.; Schuurkes, J. A.; Peeters, T. L.; Herman, A. G.; Pelckmans, P. A.

    1999-01-01

    BACKGROUND/AIM: The effects of different prokinetic agents, the motilide erythromycin and the substituted benzamides metoclopramide and cisapride, were investigated in a rat model of postoperative ileus. These effects were compared with that of granisetron, a 5-hydroxytryptamine (5-HT(3)) receptor

  20. Evaluation of antidiabetic, hypolipedimic and antioxidant activity of hydroalcoholic extract of leaves and fruit peel of Punica granatum in male Wistar albino rats.

    Science.gov (United States)

    Salwe, Kartik J; Sachdev, Devender O; Bahurupi, Yogesh; Kumarappan, Manimekalai

    2015-01-01

    We investigated anti-diabetic, hypolipedimic and antioxidant activity of hydroalcoholic extract from leaves and fruit peel of Punica granatum. Streptozotocin induced diabetic Wister rats were used in this study consisting of seven groups of six animals each. Groups (1) normal control, (2) diabetic control, (3) leaves extract 100 mg/kg b.w. of P. granatum, (4) leaves extract 200 mg/kg b.w. of P. granatum, (5) fruit peel extract 100 mg/kg b.w. of P. granatum, (6) peel extract 200 mg/kg b.w. of P. granatum and (7) glibenclamide respectively. Fasting blood sugar was recorded on 1(st), 7(th), 14(th), 21(st) and 28(th) day. At the end of the experiment Lipid profile and levels of antioxidants were determined. Safety profile of both extracts was evaluated using acute and chronic toxicity studies. Higher dose of fruit peel extract of P. granatum (PEPG) and glibenclamide significantly lowered blood glucose level from 7(th) day onwards however glibenclamide was found to be more effective. Leaves extract at higher dose and fruit extract at lower dose also significantly lowered blood glucose level from 14(th) day onwards. Leaves extract at lower dose also significantly lowered blood glucose level from 21(st) day onwards. Glibenclamide and higher dose of fruit PEPG extract significantly reduced the total cholesterol, triglyceride levels and significantly increased the high density lipoprotein cholesterol level. Glibenclamide followed by higher dose was found more effective in reducing plasma thiobarbituric acid reactive substances and increasing levels of antioxidant enzymes (superoxide dismutase and catalase). No toxicity was observed even when both extracts were administered at 10 times of higher dose used in this study and no significant changes were seen when it were used chronically. Leaves and fruit PEPG possesses significant anti-diabetic, hypolipedimic and antioxidant properties. This study supports the traditional use of P. granatum in diabetes. Fruit peel which is

  1. Ten-Year Trends in the Morbidity of Diabetes Mellitus and Antidiabetic Drug Utilization in Croatia: A Study Based on Routinely Collected Data.

    Science.gov (United States)

    Pavlov, Renata; Topličan, Ivančica; Vrcić Keglević, Mladenka

    2016-01-01

    Objectives. To investigate trends of diabetes mellitus (DM) morbidity and antidiabetic drug utilization in Croatian primary health care (PHC) from 2005 to 2014. Method. Routinely collected morbidity data from all PHC units, presented in Croatian health-statistics yearbooks, were retrieved. Data on drug utilization were retrieved from the Annual Reports of the Croatian Agency for Medicinal Products and Medical Devices (ATC/DDD, antidiabetic, A10). Results. Total morbidity increased by 33.3% and DM increased by 65.6%, mostly in patients over age 65 (from 50% to 57%). Estimated DM prevalence in adults increased from 3.9% to 6.4%. Increased morbidity was followed by an even higher increase in drug utilization (120%). Metformin was first, with a constant increase (from 18% to 39%), followed by glimepiride, while glibenclamide use decreased. Total utilization of insulin increased even more, mostly for aspart (600%) and newly introduced glargine and detemir, while human insulin usage sharply decreased. Spending also increased, mostly for aspart (from 21% to 61% of total). Conclusions. Increased DM is followed by a higher increase in antidiabetic drug utilization; this trend will continue in the future. In Croatian PHC, metformin has primacy along with insulin analogues.

  2. Effects of a Pedagogical Agent's Emotional Expressiveness on Learner Perceptions

    Science.gov (United States)

    Romero, Enilda J.; Watson, Ginger S.

    2012-01-01

    The use of animated pedagogical agents or avatars in instruction has lagged behind their use in entertainment. This is due in part to the cost and complexity of development and implementation of agents in educational settings, but also results from a lack of research to understand how emotions from animated agents influence instructional effectiveness. The phenomenological study presented here assesses the perceptions of eight learners interacting with low and high intensity emotionally expressive pedagogical agents in a computer-mediated environment. Research methods include maximum variation and snowball sampling with random assignment to treatment. The resulting themes incorporate perceptions of importance, agent humanness, enjoyment, implementation barriers, and suggested improvements. Design recommendations and implications for future research are presented.

  3. Repurposing rosiglitazone, a PPAR-γ agonist and oral antidiabetic, as an inhaled formulation, for the treatment of PAH.

    Science.gov (United States)

    Rashid, Jahidur; Alobaida, Ahmad; Al-Hilal, Taslim A; Hammouda, Samia; McMurtry, Ivan F; Nozik-Grayck, Eva; Stenmark, Kurt R; Ahsan, Fakhrul

    2018-06-28

    Peroxisome-proliferator-activated-receptor-gamma (PPAR-γ) is implicated, in some capacity, in the pathogenesis of pulmonary arterial hypertension (PAH). Rosiglitazone, an oral antidiabetic and PPAR-γ agonist, has the potential to dilate pulmonary arteries and to attenuate arterial remodeling in PAH. Here, we sought to test the hypothesis that rosiglitazone can be repurposed as inhaled formulation for the treatment of PAH. We have tested this conjecture by preparing and optimizing poly(lactic-co-glycolic) acid (PLGA) based particles of rosiglitazone, assessing the drug particles for pulmonary absorption, investigating the efficacy of the plain versus particulate drug formulation in improving the respiratory hemodynamics in PAH animals, and finally studying the effect of the drug in regulating the molecular markers associated with PAH pathogenesis. The optimized particles were slightly porous and spherical, and released 87.9% ± 6.7% of the drug in 24 h. The elimination half-life of the drug formulated in PLGA particles was 2.5-fold greater than that of the plain drug administered via the same route at the same dose. The optimized formulation, given via the pulmonary route, produced pulmonary selective vasodilation in PAH animals, but oral rosiglitazone had no effect in pulmonary hemodynamics. Rosiglitazone ameliorates the pathogenesis of PAH by balancing the molecular regulators involved in the vasoconstriction and vasodilation of human pulmonary arterial smooth muscle cells. All in all, data generated using intact animal and cellular models point to the conclusion that PLGA particles of an antidiabetic drug can be used for the treatment of a different disease, PAH. Copyright © 2018 Elsevier B.V. All rights reserved.

  4. Effects of contrast agents on the fallopian tube in a rabbit model

    International Nuclear Information System (INIS)

    Moore, D.E.

    1989-01-01

    Selection of the optimal contrast agent for hysterosalpingography was the focus of this study. The authors have evaluated the effect of different iodinated contrast agents on the fallopian tube of a rabbit. Ethiodol (oil-soluble contrast agent), methylglucamine iothalomate (water-soluble ionic agent) 30% and 60%, and Ioxilan (water-soluble monionic contrast agent) were compared. The agents were introduced by fallopian tube catheterization. Findings suggested that nonionic water-soluble contrast agents were the least detrimental to the fallopian tube and surrounding tissue. Iothalomate 60% resulted in mild inflammatory changes. Oil-soluble contrast agents caused granulomatous reaction and fibrinous adhesions

  5. Metabolic engineering of Saccharomyces cerevisiae for de novo production of dihydrochalcones with known antioxidant, antidiabetic, and sweet tasting properties

    DEFF Research Database (Denmark)

    Eichenberger, Michael; Lehka, Beata Joanna; Folly, Christophe

    2017-01-01

    Dihydrochalcones are plant secondary metabolites comprising molecules of significant commercial interest as antioxidants, antidiabetics, or sweeteners. To date, their heterologous biosynthesis in microorganisms has been achieved only by precursor feeding or as minor by-products in strains...

  6. Antidiabetic Activity from Gallic Acid Encapsulated Nanochitosan

    Science.gov (United States)

    Purbowatiningrum; Ngadiwiyana; Ismiyarto; Fachriyah, E.; Eviana, I.; Eldiana, O.; Amaliyah, N.; Sektianingrum, A. N.

    2017-02-01

    Diabetes mellitus (DM) has become a health problem in the world because it causes death. One of the phenolic compounds that have antidiabetic activity is gallic acid. However, the use of this compound still provides unsatisfactory results due to its degradation during the absorption process. The solution offered to solve the problem is by encapsulated it within chitosan nanoparticles that serve to protect the bioactive compound from degradation, increases of solubility and delivery of a bioactive compound to the target site by using freeze-drying technique. The result of chitosan nanoparticle’s Scanning Electron Microscopy (SEM) showed that chitosan nanoparticle’s size is uniform and it is smaller than chitosan. The value of encapsulation efficiency (EE) of gallic acid which encapsulated within chitosan nanoparticles is about 50.76%. Inhibition test result showed that gallic acid-chitosan nanoparticles at 50 ppm could inhibite α-glucosidase activity in 28.87% with 54.94 in IC50. So it can be concluded that gallic acid can be encapsulated in nanoparticles of chitosan and proved that it could inhibit α-glucosidase.

  7. Evaluation of the anti-diabetic properties of Mucuna pruriens seed extract.

    Science.gov (United States)

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

    2011-08-01

    To explore the antidiabetic properties of Mucuna pruriens(M. pruriens). Diabetes was induced in Wistar rats by single intravenous injection of 120 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 showed that the administration of 5, 10, 20, 30, 40, 50, and 100 mg/kg of the crude ethanolic extract of M. pruriens seeds to alloxan-induced diabetic rats (plasma glucose > 450 mg/dL) resulted in 18.6%, 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 (5 mg/kg/day) resulted in 59.7% reduction. Chronic administration of the extract resulted in a significant dose dependent reduction in the blood glucose level (Ppruriens 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 of M. pruriens seed extract also significantly reduced the weight loss associated with diabetes. The study clearly supports the traditional use of M. pruriens for the treatment of diabetes and indicates that the plant could be a good source of potent antidiabetic drug. Copyright © 2011 Hainan Medical College. Published by Elsevier B.V. All rights reserved.

  8. 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.

  9. Dgroup: DG01248 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available liflozin L-proline (JAN) ... Antidiabetic agent ... DG01794 ... SGLT2 inhibitor Unclassified ... DG02044 ... Hypoglycemic...s ... DG01794 ... SGLT2 inhibitor ... Antidiabetics, SGLT2 inhibitors SLC5A2 (SGLT2) [HSA:6524] [KO:K14382] ...

  10. Tagatose, a new antidiabetic and obesity control drug.

    Science.gov (United States)

    Lu, Y; Levin, G V; Donner, T W

    2008-02-01

    A potentially important new drug for treating type 2 diabetes, tagatose, is now in phase 3 clinical trial. The history, development, additional health benefits, mechanisms of action and the potential for the drug are presented in context with a review of the rapidly growing epidemic of type 2 diabetes and treatments for it. An epimer of fructose, the natural hexose tagatose was originally developed by Spherix Incorporated (formerly Biospherics Inc.) as a low-calorie sugar substitute. Only 20% of orally ingested tagatose is fully metabolized, principally in the liver, following a metabolic pathway identical to that of fructose. Following a decade of studies, tagatose became generally recognized as safe for use in foods and beverages under US FDA regulation. The simple sugar is commercially produced by isomerization of galactose, which is prepared from lactose. Early human studies suggested tagatose as a potential antidiabetic drug through its beneficial effects on postprandial hyperglycaemia and hyperinsulinaemia. A subsequent 14-month trial confirmed its potential for treating type 2 diabetes, and tagatose showed promise for inducing weight loss and raising high-density lipoprotein cholesterol, both important to the control of diabetes and constituting benefits independent of the disease. Furthermore, tagatose was shown to be an antioxidant and a prebiotic, both properties cited in the maintenance and promotion of health. No current therapies for type 2 diabetes provide these multiple health benefits. The predominant side effects of tagatose are gastrointestinal disturbances associated with excessive consumption, generally accommodated within 1- to 2-week period. The health and use potentials for tagatose (branded Naturlose((R)) for this use) are given with respect to current type 2 diabetes drugs and markets. Under an FDA-affirmed protocol, Spherix is currently conducting a phase 3 trial to evaluate a placebo-subtracted treatment effect based on a decrease in Hb

  11. Levels of trace elements in medicinal plants with anti-diabetic potential

    International Nuclear Information System (INIS)

    Ray, D.K.; Jena, S.

    2014-01-01

    Medicinal plants with anti-diabetic potential have been characterized by Particle-Induced X-ray Emission (PIXE) technique. Trace elements such as Ti, V, Cr, Mn, Fe, Co, Ni, Cu, Zn, Rb, Sr and Pb are found to be present in these studied medicinal plant samples. The concentrations of elements like K and Ca are quantified in percentage level whereas other elements are found to be in parts per million levels. Elemental analysis of ten different medicinal plant samples commonly used for management and cure of diabetes, shows variation in concentrations. These elements either directly or indirectly may play some role to control diabetes. (author)

  12. Efeito de herbicidas sobre agentes fitopatogênicos = Effect of herbicides on phytopathogenic agents

    Directory of Open Access Journals (Sweden)

    Daniel Dias Rosa

    2010-07-01

    Full Text Available Na agricultura moderna, diversas tecnologias auxiliam no aumento daprodutividade, sendo o herbicida uma delas, mas existem consequências atreladas ao seu uso, como os diversos efeitos sobre organismos não alvos. Neste trabalho, objetivou-se verificar esses efeitos sobre agentes fitopatogênicos, assim como avaliar o efeito do herbicida glyphosate sobre diversas doenças, em plantas de soja transgênicas.Verificou-se forte ação fungicida com o uso do herbicida glyphosate, assim como os outros avaliados “in vitro”, sobre os fungos testados, e os mesmos resultados foram observados nas plantas em condição de campo.In modern agriculture, several technologies have helped increase productivity, and herbicide is one of them. However, there are consequences linked to its use, such as the various effects on non-target organisms. The purpose of this work was to verify these effects on phytopathogenic agents, as well as assess the effect of glyphosate on diseases in transgenic soybean. There was a strong fungicide action using glyphosate herbicide as well as with the others evaluated in vitro regarding fungi tested. The same results were observed in plants in field conditions.

  13. Dgroup: DG00117 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available azone hydrochloride (JP17/USP) ... Antidiabetic agent ... DG01685 ... Insulin sensitizer ... DG01795 ... PPAR gamma agon...s ... DG01683 ... Thiazolidinedione ATC code: A10BG03 Antidiabetic, thiazolidene NR1C3 (PPARG) [HSA:5468] [KO:K08530] ...

  14. Effect of bleaching agent extracts on murine macrophages.

    Science.gov (United States)

    Fernandes, Aletéia M M; Vilela, Polyana G F; Valera, Marcia C; Bolay, Carola; Hiller, Karl Anton; Schweikl, Helmut; Schmalz, Gottfried

    2018-05-01

    The aim of this study was to evaluate the cytotoxicity and the influence of bleaching agents on immunologically cell surface antigens of murine macrophages in vitro. RAW 264.7 cells were exposed to bleaching gel extracts (40% hydrogen peroxide or 20% carbamide peroxide) and different H 2 O 2 concentrations after 1 and 24-h exposure periods and 1-h exposure and 23-h recovery. Tests were performed with and without N-acetyl cysteine (NAC) and buthionine sulfoximine (BSO). Cell viability was determined by MTT assay. The expression of surface markers CD14, CD40, and CD54 with and without LPS stimulation was detected by flow cytometry, while the production of TNF-α was measured by ELISA. Statistical analysis was performed using the Mann-Whitney U test (α = 0.05). Extracts of bleaching agents were cytotoxic for cells after a 1-h exposure; cells could not recover after 24 h. This effect can be mitigated by the antioxidant NAC and increased by BSO, an inhibitor of glutathione (GSH) synthesis. LPS stimulated expression of all surface markers and TNF-α production. Exposure to bleaching agent extracts and H 2 O 2 leads to a reduction of TNF-α, CD14, and CD40 expression, while the expression of CD54 was upregulated at non-cytotoxic concentrations. Whereas NAC reduced this effect, it was increased in the presence of BSO. Extracts of bleaching agents were irreversibly cytotoxic to macrophages after a 1-h exposure. Only the expression of CD54 was upregulated. The reactions are mediated by the non-enzymatic antioxidant GSH. The addition of an antioxidant can downregulate unfavorable effects of dental bleaching.

  15. Phenolics composition and antidiabetic property of Brachystegia eurycoma seed flur in high-fat diet, low-dose streptozotocin-induced type 2 diabetes in rats

    Directory of Open Access Journals (Sweden)

    Emmanuel Anyachukwu Irondi

    2015-06-01

    Full Text Available Objective: To quantify some major pharmacologically important flavonoids and phenolic acids in Brachystegia eurycoma seed flour (BESF and evaluate its antidiabetic activity in type 2 diabetic rats. Method: Flavonoids and phenolic acids were quantified using a reverse-phase high pressure liquid chromatrography coupled with diode array detection. Type 2 diabetes was induced in rats using high-fat diet, low-dose streptozotocin (HFD/STZ model, by feeding the rats with HFD for 2 weeks followed by single dose administration of STZ (40 mg/kg body weight, intraperitoneally. The diabetic rats were later fed BESF-supplemented (10% and 20% diets, or administered with metformin (25 mg/kg b.w. for 21 days; the control rats were fed basal diet during this period. After the dietary regimen, the rats were sacrificed, and their blood, liver and pancreas samples were collected for biochemical assays. Results: The flavonoids (catechin, rutin, quercitrin, quercetin and kaempferol and phenolic acids (gallic acid, caffeic, chlorogenic and ellagic acid were abundant in BESF. BESFsupplemented diets (BESF-SD significantly (P 0.05 with metformin administration in some of the biomarkers. Conclusion: The flavonoids and phenolic acids in BESF may have acted synergistically to produce the observed antidiabetic effects. BESF could therefore be an effective and affordable dietary therapy for the management of T2DM; and an excellent source for drug discovery.

  16. C_1_8-attached membrane funnel-based spray ionization mass spectrometry for quantification of anti-diabetic drug from human plasma

    International Nuclear Information System (INIS)

    Li, Wan; Chen, Xiangfeng; Wong, Y.-L. Elaine; Hung, Y.-L. Winnie; Wang, Ze; Deng, Liulin; Dominic Chan, T.-W.

    2016-01-01

    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_1_8-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"2 > 0.99) was obtained in the concentration range of 1–100 ng mL"−"1. The method detection limit of target drugs spiked in the human plasma was around 0.30 ng mL"−"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"−"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.

  17. Antidiabetic Activity and Chemical Composition of Sanbai Melon Seed Oil

    Science.gov (United States)

    Li, Haili; Zhao, Hang; Zhang, Ya; Qiu, Pengcheng; Li, Jie

    2018-01-01

    Objectives Many fruits and herbs had been used in Traditional Chinese Medicines for treating diabetes mellitus (DM); however, scientific and accurate evidences regarding their efficacy and possible mechanisms were largely unknown. Sanbai melon seed oil (SMSO) was used in folk medicine in treating DM, but there is no literature about these effects. The present study was aimed at confirming the treatment effects of SMSO in type 1 DM. Methods Diabetes was induced by single intraperitoneal injection of streptozotocin (STZ) at a dose of 65 mg/kg body weight. After diabetes induction, mice were treated with SMSO at dose of 1 g/kg, 2 g/kg, and 4 g/kg. Drugs were given by gavage administration once a day continuously for 28 days. At the end of treatment, several biochemical parameters and molecular mechanisms were determined by biochemical assays, ELISA, and Western blotting. The chemical compositions of SMSO were also tested. Results SMSO treatment significantly improved the symptoms of weight loss, polydipsia, reduced FBG level, increased plasma insulin levels, reduced plasma lipids levels, and protected islet injury. The results also showed that SMSO mitigated oxidative stress and alleviated the liver and renal injury in diabetes mice. SMSO also protected islet cells from apoptotic damage by suppressing ER mediated and mitochondrial dependent apoptotic pathways. Further constituent analysis results showed that SMSO had rich natural resources which had beneficial effects on DM. Conclusions This study showed that SMSO had excellent antidiabetes effect and provided scientific basis for the use of SMSO as the functional ingredients production and dietary supplements production in the food and pharmaceutical industries. PMID:29853958

  18. Anti-diabetic activity of Vaccinium bracteatum Thunb. leaves' polysaccharide in STZ-induced diabetic mice.

    Science.gov (United States)

    Wang, Li; Zhang, Ying; Xu, Maochao; Wang, Yingyao; Cheng, Sujiao; Liebrecht, Alex; Qian, Haifeng; Zhang, Hui; Qi, Xiguang

    2013-10-01

    Vaccinium bracteatum Thunb. (VBT) is a traditional Chinese herbal medicine. The anti-diabetic activity of VBT leaves' polysaccharide (VBTLP) is studied in this paper. The results indicated VBTLP had a dose-dependent decrease on the blood glucose (BG) level, and the time effect of VBTLP on BG level was also significant. The insulin level of high dose group (HDG) was significantly higher (p<0.05) than that of model control (MC) group. Compared to MC, HDG and lose dose group (LDG) had significantly lower (p<0.05) TC and LDL-C levels, however, TG and HDL-C levels are similar. Compared to non-diabetic control (NC), HDG and LDG had similar plasma lipid levels except for higher LDL-C level. Although body weights of LDG and HDG were significant lower (p<0.05) than that of NC from week 2 to week 6, they were similar to that of PC. The results indicate VBTLP possesses a potential hypoglycemic effect in streptozotocin-induced diabetic mice. Copyright © 2013 Elsevier B.V. All rights reserved.

  19. [Effectiveness of phytotherapy in supportive treatment of type 2 diabetes mellitus III. Momordica (Momordica charantia)].

    Science.gov (United States)

    Rudá-Kučerová, Jana; Kotolová, Hana; Koupý, David

    2015-09-01

    Momordica charantia is a thermophilic voluble plant from the tropical and subtropical regions of Asia, Africa and the Caribbean. In central Europe, momordica requires greenhouse plantations. Mature fruits resemble a cucumber or a pumpkin and can be used as other similar vegetables. Crude fruits are very bitter and refreshing. For centuries the plant has been known in Chinese traditional medicine for its antidiabetic effects as well as for the treatment of cancer or infections caused by worms, viruses and malaria. Antidiabetic effects are attributed namely to cucurbitane type triterpenoids, charantin, p-insulin and 9cis-11trans-13trans-conjugated linolenic acid. These substances in momordica preparations show antidiabetic effectiveness in clinical studies by increasing insulin secretion and deceasing insulin resistance or glucose absorption from the gut. Beside this main effect the extract possesses certain neuroprotective and antioxidant effects (especially p9cis-11trans-13trans-conjugated linolenic acid) and contributes to normalize blood lipid and adipokine levels which results in the normalization of metabolic syndrome. Antidiabetic effectiveness of momordica was compared to active treatment with several oral antidiabetic drugs and proved comparable effects. However, the number of studies is limited and their methodological approach variable. Therefore, the evidence is so far inconclusive.

  20. Economic impact of compliance to treatment with antidiabetes medication in type 2 diabetes mellitus: a review paper.

    Science.gov (United States)

    Breitscheidel, L; Stamenitis, S; Dippel, F-W; Schöffski, O

    2010-03-01

    Suboptimal compliance and failure to persist with antidiabetes therapies are of potential economic significance. The present research aims to describe the impact of poor compliance and persistence with antidiabetes medications on the cost of healthcare or its components for patients with type 2 diabetes mellitus (T2DM). Literature search was conducted in PubMed for relevant articles published in the period between 1 January 2000 and 30 April 2009. Thus, it is possible that relevant articles not listed in PubMed, but available in other databases are not included in the current review. Studies describing economic consequence of compliance and/or persistence with pharmaceutical antidiabetes treatment were identified. The variability in the studies reviewed was high, making it extremely difficult to make a comparison between them. Of 449 articles corresponding to the primary search algorithm, 12 studies (all conducted in USA) fulfilled the inclusion criteria regarding the economic impact of compliance and/or persistence with treatment on the overall cost of T2DM care or its components. Compliance was assessed via medication possession ratio (MPR) in ten studies, where it ranged from 0.52 to 0.93 depending on regimen. Persistence was assessed in one study. Mean total annual costs per T2DM patient varied between the studies, ranging from $4570 to $17338. In seven studies, medication compliance was inversely associated with total healthcare costs, while in four other studies inverse associations between medication compliance and hospitalisation costs were reported. In one study increased adherence did not change overall healthcare costs. Improved compliance may lead to reductions of the total healthcare costs in T2DM, Further research is needed in countries other than the US to assess impact of compliance and persistence to pharmacotherapy on T2DM costs in country-specific settings.

  1. ANTIDIABETIC AND ANTIDYSLIPIDEMIC EFFECTS OF HELIOTROPIUM STRIGOSUM IN RAT MODELS OF TYPE I AND TYPE II DIABETES.

    Science.gov (United States)

    Chaudhry, Shafqat Rasul; Akram, Adnan; Aslam, Naveed; Asif, Muhammad; Wajid, Muhammad; Kinfe, Thomas; Jabeen, Qaiser; Muhammad, Sajjad

    2016-11-01

    Heliotropiumz stnigosum Wilid. (Boraginaceae) is used traditionally as a laxative, diuretic, and as a treatment for snake bites and stings of nettles. Recent investigations have shown anti-inflammatory and antioxidant activity of H. sorigosum. However, antihyperglycemic and antidyslipidemic activity of H. strigosum has not been investigated to date and we aimed to explore these activities of the crude aqueous methanolic extract of thEaerial parts of H. strigosum (Hs.Cr). Hs.Cr was administered orally at doses of 100, 300, and 500 mg/kg in alloxan-induced diabetic rats (type I diabetes) and fructose-fed rats (type II diabetes). The fasting blood glucose (FBG) concentration was assessed by glucometer, while semum total cholesterol, triglycerides and HDL were estimated by using standard kits. The FBG concentration significantly (p < 0.05) decreased in dose-dependent pattern in both alloxan-induced diabetic and fructose-fed rats on Hs.Cr administration. The percentage glucose reductions in alloxanized rats with glibenclamide, Hs.Cr 100, 300, and 500 mg/kg were obeserved to be 67, 36, 56 and 62%, respectively. In fructose-fed rats, the percentage glucose redutions associated with metformin, Hs.Cr 100, 300, and 500 mg/kg were 23, 5, 11 and 12%, respectively. The extract also corrected the dyslipidemia associated with fructose and alloxan-induced diabetes by significantly (p < 0.00 1) decreasing the concentration of serum total cholesterol, triglycerides and LDL and by increasing HDL concentration. Our data demonstrate that the H. stigosum has antidiabetic and antidyslipidemic effects, thus encouraging further studies.

  2. Anti-diabetic action of Punica granatum flower extract: Activation of PPAR-γ and identification of an active component

    International Nuclear Information System (INIS)

    Huang, Tom H.W.; Peng Gang; Kota, Bhavani P.; Li, George Q.; Yamahara, Johji; Roufogalis, Basil D.; Li Yuhao

    2005-01-01

    Peroxisome proliferator-activated receptor (PPAR)-γ activators are widely used in the treatment of type 2 diabetes because they improve the sensitivity of insulin receptors. Punica granatum flower (PGF) has been used as an anti-diabetic medicine in Unani medicinal literature. The mechanism of actions is, however, unknown. In the current study, we demonstrated that 6-week oral administration of methanol extract from PGF (500 mg/kg, daily) inhibited glucose loading-induced increase of plasma glucose levels in Zucker diabetic fatty rats (ZDF), a genetic animal model for type 2 diabetes, whereas it did not inhibit the increase in Zucker lean rats (ZL). The treatment did not lower the plasma glucose levels in fasted ZDF and ZL rats. Furthermore, RT-PCR results demonstrated that the PGF extract treatment in ZDF rats enhanced cardiac PPAR-γ mRNA expression and restored the down-regulated cardiac glucose transporter (GLUT)-4 (the insulin-dependent isoform of GLUTs) mRNA. These results suggest that the anti-diabetic activity of PGF extract may result from improved sensitivity of the insulin receptor. From the in vitro studies, we demonstrated that the PGF extract enhanced PPAR-γ mRNA and protein expression and increased PPAR-γ-dependent mRNA expression and activity of lipoprotein lipase in human THP-1-differentiated macrophage cells. Phytochemical investigation demonstrated that gallic acid in PGF extract is mostly responsible for this activity. Thus, our findings indicate that PPAR-γ is a molecular target for PGF extract and its prominent component gallic acid, and provide a better understanding of the potential mechanism of the anti-diabetic action of PGF

  3. Insulin and other antidiabetic drugs and hepatocellular carcinoma risk: a nested case-control study based on Italian healthcare utilization databases.

    Science.gov (United States)

    Bosetti, Cristina; Franchi, Matteo; Nicotra, Federica; Asciutto, Rosario; Merlino, Luca; La Vecchia, Carlo; Corrao, Giovanni

    2015-07-01

    Insulin and other antidiabetic drugs may modulate hepatocellular carcinoma (HCC) risk in diabetics. We have analyzed the role of various antidiabetic drugs on HCC in a nested case-control study using the healthcare utilization databases of the Lombardy Region in Italy. This included 190 diabetic subjects with a hospital discharge reporting a diagnosis of malignant HCC and 3772 diabetic control subjects matched to each case on sex, age, date at cohort entry, and duration of follow-up. Increased risks of HCC were found for use of insulin (odds ratio [OR] = 3.73, 95% confidence interval [CI] 2.52-5.51), sulfonylureas (OR = 1.39, 95%CI 0.98-1.99), and repaglinide (OR = 2.12, 95%CI 1.38-3.26), while a reduced risk was found for use of metformin (OR = 0.57, 95%CI 0.41-0.79). The risk of HCC increased with increasing duration of insulin use (OR = 2.52 for metformin. Our study supports the evidence that patients with diabetes using metformin, and possibly other antidiabetic drugs that increase insulin sensibility, have a reduced risk of HCC, while those using insulin or drugs that increase circulating insulin, such as insulin secretagogues, have an increased risk. Whether these associations are causal, or influenced by different severity of diabetes and/or possible residual bias or misclassification, is still open to discussion. Copyright © 2015 John Wiley & Sons, Ltd.

  4. Optimization and development of antidiabetic phytosomes by the Box-Behnken design.

    Science.gov (United States)

    Rathee, Sushila; Kamboj, Anjoo

    2018-06-01

    Researchers have extensively reviewed on herbs and natural products for their marked clinical efficacy in some recent years, however, maximum of the newly discovered bioactive constituents offer poor bioavailability due to their large size molecules or to their poor miscibility with oils and lipids, thereby limiting their ability to pass across the lipid-rich outer membranes of the enterocytes of the small intestine. Phytosomes are more bioavailable as compared to herbal extracts owing to their enhanced capacity to cross the bio-membranes and thus reaching the systemic circulation. This study was aimed to investigate the development and optimization of antidiabetic phytosomes using a three-factor, three-level the Box-Behnken design (17 batches). The fruits of Citrullus colocynthis (L.) Momordica balsamina and Momordica dioica were extracted using Soxhlet's apparatus. The phytochemical fingerprint profile of the combined methanolic extracts was done by using high-performance thin layer chromatography (HPTLC). The polynomial quadratic equation analysis was designed to study the response (entrapment efficiency (EE), % yield) of independent significant factors at different levels. Phytosomes were characterized in terms of drug content, particle size, EE, zeta potential and in vitro dissolution. TEM analysis revealed good stability and a spherical, self-closed structure of phytosomes in complex formulations. Average particle size was found to 450 nm. Total flavonoid content was found to be 10.0 ± 0.002 μg/g. Optimized formulation was selected and was prepared using A (1:3), B (60 °C) and C (2.5 h) to give maximum yield and entrapment efficiencies (72% and 92.1 ± 5.1%). Phytosomes were found to have antidiabetic activity comparable to metformin in low dose. HPTLC showed the presence of the phyto-constituent quercetin.

  5. Potential of Polygonum cuspidatum Root as an Antidiabetic Food: Dual High-Resolution α-Glucosidase and PTP1B Inhibition Profiling Combined with HPLC-HRMS and NMR for Identification of Antidiabetic Constituents.

    Science.gov (United States)

    Zhao, Yong; Chen, Martin Xiaoyong; Kongstad, Kenneth Thermann; Jäger, Anna Katharina; Staerk, Dan

    2017-06-07

    The worldwide increasing incidence of type 2 diabetes has fueled an intensified search for food and herbal remedies with preventive and/or therapeutic properties. Polygonum cuspidatum Siebold & Zucc. (Polygonaceae) is used as a functional food in Japan and South Korea, and it is also a well-known traditional antidiabetic herb used in China. In this study, dual high-resolution α-glucosidase and protein-tyrosine phosphatase 1B (PTP1B) inhibition profiling was used for the identification of individual antidiabetic constituents directly from the crude ethyl acetate extract and fractions of P. cuspidatum. Subsequent preparative-scale HPLC was used to isolate a series of α-glucosidase inhibitors, which after HPLC-HRMS and NMR analysis were identified as procyanidin B2 3,3″-O-digallate (3) and (-)-epicatechin gallate (5) with IC 50 values of 0.42 ± 0.02 and 0.48 ± 0.0004 μM, respectively, as well as a series of stilbene analogues with IC 50 value in the range from 6.05 ± 0.05 to 116.10 ± 2.04 μM. In addition, (trans)-emodin-physcion bianthrone (15b) and (cis)-emodin-physcion bianthrone (15c) were identified as potent PTP1B inhibitors with IC 50 values of 2.77 ± 1.23 and 7.29 ± 2.32 μM, respectively. These findings show that P. cuspidatum is a potential functional food for management of type 2 diabetes.

  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. Sodium-Glucose Cotransporter 2 (SGLT2) Inhibitors from Natural Products: Discovery of Next-Generation Antihyperglycemic Agents.

    Science.gov (United States)

    Choi, Chang-Ik

    2016-08-27

    Diabetes mellitus is a chronic condition associated with the metabolic impairment of insulin actions, leading to the development of life-threatening complications. Although many kinds of oral antihyperglycemic agents with different therapeutic mechanisms have been marketed, their undesirable adverse effects, such as hypoglycemia, weight gain, and hepato-renal toxicity, have increased demand for the discovery of novel, safer antidiabetic drugs. Since the important roles of the sodium-glucose cotransporter 2 (SGLT2) for glucose homeostasis in the kidney were recently elucidated, pharmacological inhibition of SGLT2 has been considered a promising therapeutic target for the treatment of type 2 diabetes. Since the discovery of the first natural SGLT2 inhibitor, phlorizin, several synthetic glucoside analogs have been developed and introduced into the market. Furthermore, many efforts to find new active constituents with SGLT2 inhibition from natural products are still ongoing. This review introduces the history of research on the development of early-generation SGLT2 inhibitors, and recent progress on the discovery of novel candidates for SGLT2 inhibitor from several natural products that are widely used in traditional herbal medicine.

  8. Dgroup: DG01284 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available liptin succinate (JAN/USAN) ... Antidiabetic agent ... DG01601 ... DPP-4 inhibitor Cyp inhibitor ... DG01915 ... CYP3A5 i...nhibitor Unclassified ... DG02044 ... Hypoglycemics ... DG01601 ... DPP-4 inhibitor ... DPP4 inhibitor, antidiabetics DPP4 [HSA:1803] [KO:K01278] ...

  9. Effect of two mobilizing agents on the elimination of 147Pm from rats

    International Nuclear Information System (INIS)

    Su Kunyuan; Gao Xianhua; Lao Qinhua

    1984-01-01

    A study was performed to determine the effect of two new mobilizing agents: N,N-bis-carboxymethyl amino acetylcysteine and hyaluronidase on the elimination of intracheally-injected 147 Pm from rats. The results showed that both the two agents could promote the elimination of 147 Pm from rats and decrease the body retention of rats. The former agent is much more effective in elimination than the other

  10. Comparative Anti-Diabetic Evaluation of Different Parts of Himalrandia tetrasperma in Alloxan Induced Diabetic in Mice

    International Nuclear Information System (INIS)

    Ajaib, M.

    2016-01-01

    The present experiments were designed to investigate the acute effects of methanolic extracts of various parts of H. tetrasperma in diabetic mice. The basic phyto-chemical study showed the occurrence of alkaloids, saponins, flavonoids and tannins as main phyto-constituents in the methanolic extract. Diabetes was induced experimentally in mice by intra peritoneally injecting alloxan (150 mg/kg i.p.). In acute study, methanolic H. tetrasperma extracts of various parts of plant were evaluated for anti-diabetic potential in alloxan induced diabetic mice. Extracts of leaves, bark and seeds (250 mg/kg, i.p) and metformin (250 mg/kg i.p) were given intra peritoneal in alloxan treated diabetic mice and blood glucose levels were measured at 0, 360 and 24 h. There was significant lowering of blood glucose level at 1 h after treatment, in diabetic mice treated with methanolic extracts of bark (182.3 ± 3.6 mg/dL), leaves (178.5 ± 1.2 mg/dL) and seeds (156.3 ± 11.3 mg/dL) when compared with control diabetic group (280 ± 7.92 mg/dL). Highly significant results were also obtained at 24 h after treatment with methanolic extracts of bark (187.67 ±1.2 mg/dL), leaves (170.66 ± 2.3 mg/dL) and seeds (142 ± 8.7 mg/dL) when compared with control diabetic group (257.7 ± 6.7 mg/dL). It is concluded that methanolic extract of all parts possess significant anti-diabetic activity which is due to the presence of phytochemicals, i.e. alkaloids, flavonoids, phenols, saponins, tannins and it can be further evaluated for the mechanism involved. (author)

  11. Effects of radioprotective agents on mammal cella

    International Nuclear Information System (INIS)

    Schuessler, H.; Pauly, H.

    1983-01-01

    The effects of aminothiols and thiophosphates on cultures of B14 Chinese Hamster cells wee investigated. 30 min before irradiation, the cells were covered with a solution of the radioprotective agent. After irradiation, this solution was removed and substituted by culture medium. The radioprotective effect increases with increasing cystamine concentrations. With a cystamine concentration of 60 mM, a dose reduction factor of 3 was achieved. Further investigations showed that already after 2 min of incubation, the radioprotective effect in the same as after 60 min. (orig./MG) [de

  12. Dgroup: DG00119 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available in hydrate (JAN/USAN) ... D10262 ... Saxagliptin hydrochloride ... Antidiabetic agent ... DG01601 ... DPP-4 inhibitor T...4 inhibitor ATC code: A10BH03 Antidiabetic, Dipeptidyl peptidase-4 (DPP-4) inhibitor DPP4 [HSA:1803] [KO:K01278] Transporter: ABCB1 [HSA:5243] ...

  13. Dgroup: DG01282 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available 601 ... DPP-4 inhibitor ... DPP4 inhibitor, antidiabetics DPP4 [HSA:1803] [KO:K01278] ... ...tin tartrate (USAN) Antidiabetic agent ... DG01601 ... DPP-4 inhibitor Unclassified ... DG02044 ... Hypoglycemics ... DG01... DG01282 Chemical ... DGroup Dutogliptin ... D09333 ... Dutogliptin (USAN) D09334 ... Dutoglip

  14. 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.

  15. Insulin sparing action of adenovirus 36 and its E4orf1 protein.

    Science.gov (United States)

    Dhurandhar, Nikhil V

    2013-01-01

    Additional drugs are required to effectively manage diabetes and its complications. Recent studies have revealed protective effects of Ad36, a human adenovirus, and its E4orf1 protein on glucose disposal, which may be creatively harnessed to develop novel anti-diabetic agents. Experimental Ad36 infection improves hyperglycemia in animal models and natural Ad36 infection in humans is associated with better glycemic control. Available data indicate distinctive advantages for a drug that may mimic the action of Ad36/E4orf1. The key features of such a potential drug include the ability to increase glucose uptake by adipose tissue and skeletal muscle, to reduce hepatic glucose output independent of proximal insulin signaling, and to up-regulate adiponectin and its hepatic action. The effect of Ad36/E4orf1 on hepatocyte metabolism suggests a role for treating hepatic steatosis. Despite these potential advantages, considerable research is required before such a drug is developed. The in vivo efficacy and safety of E4orf1 in improving hyperglycemia remain unknown, and an appropriate drug delivery system is required. Nonetheless, Ad36 E4orf1 offers a research opportunity to develop a new anti-diabetic agent with multiple potential advantages and conceptually advances the use of a rather unconventional source, microbial proteins, for anti-diabetic drug development. Copyright © 2013 Elsevier Inc. All rights reserved.

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

    International Nuclear Information System (INIS)

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

    2012-01-01

    Highlights: ► Sargassum yezoense (SY) treatment improved glucose and lipid impairment in vivo. ► This pharmacological action is associated with PPARα/γ dual activation. ► It decreases the expression of G6Pase for gluconeogenesis in liver. ► It increases the expression of UCP3 for lipid metabolism in adipose tissue. ► 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 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.

  17. Effect of reducing agents on wheat gluten and quality characteristics of flour and cookies

    Directory of Open Access Journals (Sweden)

    Naveen KUMAR

    2013-12-01

    Full Text Available The aim of the present study was to determine the effect of reducing agents (Lcystine, glutathione and proteases on wheat gluten recovery and quality characteristics of dough and cookies. PBW-343 and RAJ-3765 wheat varieties were analysed for physico-chemical properties which indicated that wheat variety RAJ-3765 had superior quality characteristics in comparison to PBW-343. Wet gluten and dry gluten %yields were reduced with addition of reducing agents. As the concentration of reducing agents increased gluten, yield decreased further. The dough strength (resistance to extension decreased, whereas extension of dough increased significantly with the addition of reducing agents. Upon addition of reducing agents, spread factor increased, whereas hardness decreased. Glutathione was found to be the most effective reducing agent out of the three reducing agents used in this study.

  18. 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.

  19. Military chemical warfare agent human subjects testing: part 2--long-term health effects among participants of U.S. military chemical warfare agent testing.

    Science.gov (United States)

    Brown, Mark

    2009-10-01

    Military chemical warfare agent testing from World War I to 1975 produced thousands of veterans with concerns about how their participation affected their health. A companion article describes the history of these experiments, and how the lack of clinical data hampers evaluation of long-term health consequences. Conversely, much information is available about specific agents tested and their long-term health effects in other populations, which may be invaluable for helping clinicians respond effectively to the health care and other needs of affected veterans. The following review describes tested agents and their known long-term health consequences. Although hundreds of chemicals were tested, they fall into only about a half-dozen pharmaceutical classes, including common pharmaceuticals; anticholinesterase agents including military nerve agents and pesticides; anticholinergic glycolic acid esters such as atropine; acetylcholine reactivators such as 2-PAM; psychoactive compounds including cannabinoids, phencyclidine, and LSD; and irritants including tear gas and riot control agents.

  20. Optimization of Extraction Process for Antidiabetic and Antioxidant Activities of Kursi Wufarikun Ziyabit Using Response Surface Methodology and Quantitative Analysis of Main Components.

    Science.gov (United States)

    Edirs, Salamet; Turak, Ablajan; Numonov, Sodik; Xin, Xuelei; Aisa, Haji Akber

    2017-01-01

    By using extraction yield, total polyphenolic content, antidiabetic activities (PTP-1B and α -glycosidase), and antioxidant activity (ABTS and DPPH) as indicated markers, the extraction conditions of the prescription Kursi Wufarikun Ziyabit (KWZ) were optimized by response surface methodology (RSM). Independent variables were ethanol concentration, extraction temperature, solid-to-solvent ratio, and extraction time. The result of RSM analysis showed that the four variables investigated have a significant effect ( p analysis of effective part of KWZ was characterized via UPLC method, 12 main components were identified by standard compounds, and all of them have shown good regression within the test ranges and the total content of them was 11.18%.

  1. The Effect of Silane Coupling Agents on a Composite Polyamide-6/Talc

    Directory of Open Access Journals (Sweden)

    H. Wiebeck

    1998-12-01

    Full Text Available This paper evaluates the effect of the addition of silane agents on the mechanical properties (tensile strength, hardness and flexibility of the composite polyamide-6/talc. For this purpose, 30% and 40% of a talc with and without the addition of silane agents were incorporated into polyamide-6. Three kinds of silane agents were used, resulting in nine formulations. Comparing the experimental results, it is concluded that the silane agents improve the mechanical properties of the composite material.

  2. Assessment of nutritional quality, glycaemic index, antidiabetic and sensory properties of plantain (Musa paradisiaca)-based functional dough meals.

    Science.gov (United States)

    Famakin, Opeyemi; Fatoyinbo, Akindele; Ijarotimi, Oluwole Steve; Badejo, Adebanjo Ayobamidele; Fagbemi, Tayo Nathaniel

    2016-11-01

    Nutrition transition to high energy-dense foods has been implicated as the major causes of diet related diseases. Plantain-based dough meals supplemented with soybean cake and cassava fibre were developed by combining them in different proportions using response surface methodology. The flour blends were analyzed for the nutritional composition while the glycaemic index, antidiabetic potentials and protein digestibility of the dough meals were determined in wistar rats. The nutritional and essential amino acid contents of the flour blends were comparable to that of cerolina (a commercially available food product commonly recommended for diabetic patients). The rats fed with the formulated dough meals had lower glycaemic index and glycaemic load, and the blood glucose was significantly reduced compared to cerolina and metformin (a synthetic antidiabetic drug). All the plantain-based dough meals were comparable to cerolina and metformin in terms of nutritional quality and blood glycaemic control activities, respectively. Hence, the formulated plantain-based dough meals have potential to be used for the prevention and management of diabetes mellitus.

  3. DFT predictions, synthesis, stoichiometric structures and anti-diabetic activity of Cu (II) and Fe (III) complexes of quercetin, morin, and primuletin

    Science.gov (United States)

    Jabeen, Erum; Janjua, Naveed Kausar; Ahmed, Safeer; Murtaza, Iram; Ali, Tahir; Masood, Nosheen; Rizvi, Aysha Sarfraz; Murtaza, Gulam

    2017-12-01

    The current study is aimed at the synthesis of Cu (II) and Fe (III) complexes of three flavonoids {morin (mor), quercetin (quer) and primuletin (prim)} and characterization through UV-Vis spectroscopy, cyclic voltammetry, FTIR, and thermal analysis. Structure prediction through DFT calculation was supported by experimental data. Benesi-Hildebrand equation was modified to function for 1:2 Cu-flavonoid and 1:3 Fe-flavonoid complexes. DFT predictions revealed that out of poly chelation sites present in morin and quercetin, 3-OH site was utilized as preferable chelation site while primuletin chelated through 5-OH position. In-vivo trials revealed the complexes to have better anti-diabetic potential than respective flavonoid. Fls/M-Fls proved as antagonistic to Alloxan induced diabetes and also retained anti-diabetic activity even in the presence of (2-hydroxypropyl)-β-cyclodextrin (HPβCD).

  4. Dgroup: DG01798 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available eutral (USAN); Neutral insulin injection (INN) D04550 ... Insulin zinc, prompt (USP) Antidiabetic... agent ... DG01636 ... Insulin and analogue ... DG01802 ... Human insulin ATC code: A10AB Antidiabetics INSR (CD220) [HSA:3643] [KO:K04527] ... CYP induction: CYP1A2 [HSA:1544

  5. Dgroup: DG01799 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available e (USP) D04547 ... Insulin, isophane (USP); Isophane insulin injection (aqueous suspension) (JAN) Antidiabetic ...agent ... DG01636 ... Insulin and analogue ... DG01802 ... Human insulin ATC code: A10AC Antidiabetics INSR (CD220) [HSA:3643] [KO:K04527] ... CYP induction: CYP1A2 [HSA:1544

  6. Drug: D00216 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available etic agent ... DG01663 ... alpha-Glucosidase inhibitor ... DG01803 ... Antidiabetic, alpha-glu...cosidase inhibitor Unclassified ... DG02044 ... Hypoglycemics ... DG01803 ... Antidiabetic, alpha-glucosidase inhibitor... D00216 Drug Acarbose (JAN/USAN/INN); Precose (TN) ... C25H43NO18 D00216.gif ... Actinoplanes [TAX:1865] Antidiab

  7. Dgroup: DG00118 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available gliptin phosphate (USAN); Sitagliptin phosphate hydrate (JAN) ... Antidiabetic agent ... DG01601 ... DPP-4 inhibito...PP-4 inhibitor ATC code: A10BH01 DPP4 inhibitor, antidiabetics DPP4 [HSA:1803] [KO:K01278] Transporter: ABCB1 [HSA:5243], SLC22A8 [HSA:9376] ...

  8. Barriers and Effective Educational Strategies to Develop Extension Agents' Professional Competencies

    Science.gov (United States)

    Lakai, Dona; Jayaratne, K. S. U.; Moore, Gary E.; Kistler, Mark J.

    2012-01-01

    The study reported here determined the barriers and effective educational strategies to develop Extension agents' professional competencies. This was a descriptive survey research conducted with a random sample of Extension agents. Increased workload and lack of time and funding were identified as the most constraining barriers of Extension agents…

  9. Anti-diabetic Activity of Tabat Barito Leafs (Ficus deltoidea, Jack Extract in Rats

    Directory of Open Access Journals (Sweden)

    Heru Agus Cahyanto

    2013-06-01

    Full Text Available Tabat barito (Ficus deltoidea, Jack leaf is believed could be used to treat diabetes. But more scientific data are needed. The aim of this study is to investigate  antidiabetic activity of  Tabat Barito extract by glucose tolerance method. The treatment was given in three doses (50, 100, and 200 mg/kg BW and two controls using aquoeus and glibenklamid.  Tabat barito extract was obtained by maceration and made into dry extract with addition of starch. The result showed that chemical compound of the ethanol extract were fenolic and saponin. The extract showed effects in lowering blood sugar levels with glucose tolerance methods at 30 to 60 minutes. Blood glucose levels of mice treated with the extract extract ranged between 132.60 to 258.00 mg/dL , glibenklamide ranged from 130.20 to 144.60 mg/dL, and aqua ranged between 227.60 to 260.20 mg/dL. The percentage decrease in blood sugar levels compared to controls is 32.54%.

  10. Antidiabetic Effect of Tibetan Medicine Tang-Kang-Fu-San on High-Fat Diet and Streptozotocin-Induced Type 2 Diabetic Rats

    Directory of Open Access Journals (Sweden)

    Bailu Duan

    2017-01-01

    Full Text Available The aim of this study was to investigate the antidiabetic effects of a Tibetan medicine, Tang-Kang-Fu-San (TKFS, on experimental type 2 diabetes mellitus (T2DM rats and to explore its underlying mechanisms. Firstly two major chemical compositions of TKFS, gallic acid and curcumin, were characterized by HPLC fingerprint analysis. Next T2DM in rats was induced by high-fat diet and a low-dose streptozotocin (STZ 35 mg/kg. Then oral gavage administration of three different doses of TKFS (0.3 g/kg, 0.6 g/kg, and 1.2 g/kg was given to T2DM rats. Experimental results showed that TKFS dramatically reduced the levels of fasting blood glucose, fasting blood insulin, triglyceride, total cholesterol, LDL cholesterol, and HDL cholesterol, even though it did not alter the animal body weight. The downregulation of phosphorylation-AKT (p-AKT and glucose transporter-4 (GLUT4 in skeletal muscle of T2DM rats was restored and abnormal pathological changes in pancreas tissues were also improved. Our work showed that TKFS could alleviate diabetic syndromes, maintain the glucose homeostasis, and protect against insulin resistance in T2DM rats, and the improvement of AKT phosphorylation and GLUT4 translocation in skeletal muscle would be one of its possible underlying mechanisms.

  11. Combined effect of environmental radiation and other agents: Is there a synergism trap?

    International Nuclear Information System (INIS)

    Hornhardt, S.; Jung, T.; Burkart, W.

    2002-01-01

    Most assessments of possible deleterious outcomes from environmental and occupational exposures concentrate on single agents and neglect the potential for combined effects, i.e. synergisms or antagonisms. Biomechanistic considerations based on multistep processes such as carcinogenesis indicate the potential for highly detrimental interactions, if two or more consecutive rate limiting steps are specifically effected by different agents. However, low specificity towards molecular structure or DNA-sequence - and therefore exchangeability - of many genotoxic agents indicate little functional specificity and therefore little vulnerability towards synergism at most occupational and environmental exposure situations. The low potential for significant combined effects for those common low exposure situations where non-genotoxic agents with highly non-linear dose effect relationships and apparent thresholds are involved, is also evident. Nevertheless, a quantitative assessment of the contribution of synergistic interactions to the total detriment from natural and man-made toxicants based on experimental data is far away. The existing database on combined effects is rudimentary, mainly descriptive and rarely covers exposure ranges large enough to make direct inferences to present day low dose exposure situations. In view of the multitude of possible interactions between the large number of potentially harmful agents in the human environment, descriptive approaches will have to be supplemented by the use of mechanistic models for critical health endpoints such as cancer. Finally an important question considering the shape of dose effect relationships for ionizing radiation arises from the unresolved question whether real or apparent thresholds may be used for any genotoxic agent separately or only one time for an exposed genome. (author)

  12. Anti-diabetic effects of Inonotus obliquus polysaccharides-chromium (III) complex in type 2 diabetic mice and its sub-acute toxicity evaluation in normal mice.

    Science.gov (United States)

    Wang, Cong; Chen, Zhongqin; Pan, Yuxiang; Gao, Xudong; Chen, Haixia

    2017-10-01

    Polysaccharides are important bioactive ingredients from Inonotus obliquus. This study aimed to synthesize and characterize a novel I. obliquus polysaccharides-chromium (III) complex (UIOPC) and investigate the anti-diabetic effects in streptozotocin (STZ) induced type 2 diabetes mellitus (T2DM) mice and sub-acute toxicity in normal mice. The molecular weight of UIOPC was about 11.5 × 10 4  Da with the chromium content was 13.01% and the chromium was linked with polysaccharides through coordination bond. After treatment of UIOPC for four weeks, the body weight, fasting blood glucose (FBG) levels, plasma insulin levels of the diabetic mice were significantly reduced when compared with those of the diabetic mice (p < 0.05). The results on serum profiles and antioxidant enzymes activities revealed that UIOPC had a positive effect on hypoglycemic and antioxidant ability. Histopathology results showed that UIOPC could effectively alleviate the STZ-lesioned tissues in diabetic mice. Furthermore, high dose administration of UIOPC had no obviously influence on serum profiles levels and antioxidant ability of the normal mice and the organ tissues maintained organized and integrity in the sub-acute toxicity study. These results suggested that UIOPC might be a good candidate for the functional food or pharmaceuticals in the treatment of T2DM. Copyright © 2017 Elsevier Ltd. All rights reserved.

  13. Bioassay-Guided Antidiabetic Study of Phaleria macrocarpa Fruit Extract

    Directory of Open Access Journals (Sweden)

    Mohd Z. Asmawi

    2012-04-01

    Full Text Available An earlier anti-hyperglycemic study with serial crude extracts of Phaleria macrocarpa (PM fruit indicated methanol extract (ME as the most effective. In the present investigation, the methanol extract was further fractionated to obtain chloroform (CF, ethyl acetate (EAF, n-butanol (NBF and aqueous (AF fractions, which were tested for antidiabetic activity. The NBF reduced blood glucose (p < 0.05 15 min after administration, in an intraperitoneal glucose tolerance test (IPGTT similar to metformin. Moreover, it lowered blood glucose in diabetic rats by 66.67% (p < 0.05, similar to metformin (51.11%, glibenclamide (66.67% and insulin (71.43% after a 12-day treatment, hence considered to be the most active fraction. Further fractionation of NBF yielded sub-fractions I (SFI and II (SFII, and only SFI lowered blood glucose (p < 0.05, in IPGTT similar to glibenclamide. The ME, NBF, and SFI correspondingly lowered plasma insulin (p < 0.05 and dose-dependently inhibited glucose transport across isolated rat jejunum implying an extra-pancreatic mechanism. Phytochemical screening showed the presence of flavonoids, terpenes and tannins, in ME, NBF and SFI, and LC-MS analyses revealed 9.52%, 33.30% and 22.50% mangiferin respectively. PM fruit possesses anti-hyperglycemic effect, exerted probably through extra-pancreatic action. Magniferin, contained therein may be responsible for this reported activity.

  14. 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.

  15. 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.

  16. Antidiabetic and Hypolipidemic Activities of Curculigo latifolia Fruit:Root Extract in High Fat Fed Diet and Low Dose STZ Induced Diabetic Rats

    Directory of Open Access Journals (Sweden)

    Nur Akmal Ishak

    2013-01-01

    Full Text Available Curculigo latifolia fruit is used as alternative sweetener while root is used as alternative treatment for diuretic and urinary problems. The antidiabetic and hypolipidemic activities of C. latifolia fruit:root aqueous extract in high fat diet (HFD and 40 mg streptozotocin (STZ induced diabetic rats through expression of genes involved in glucose and lipid metabolisms were investigated. Diabetic rats were treated with C. latifolia fruit:root extract for 4 weeks. Plasma glucose, insulin, adiponectin, lipid profiles, alanine aminotransferase (ALT, gamma glutamyltransferase (GGT, urea, and creatinine levels were measured before and after treatments. Regulations of selected genes involved in glucose and lipid metabolisms were determined. Results showed the significant (P<0.05 increase in body weight, high density lipoprotein (HDL, insulin, and adiponectin levels and decreased glucose, total cholesterol (TC, triglycerides (TG, low density lipoprotein (LDL, urea, creatinine, ALT, and GGT levels in diabetic rats after 4 weeks treatment. Furthermore, C. latifolia fruit:root extract significantly increased the expression of IRS-1, IGF-1, GLUT4, PPARα, PPARγ, AdipoR1, AdipoR2, leptin, LPL, and lipase genes in adipose and muscle tissues in diabetic rats. These results suggest that C. latifolia fruit:root extract exerts antidiabetic and hypolipidemic effects through altering regulation genes in glucose and lipid metabolisms in diabetic rats.

  17. Nanotechnology based approaches for anti-diabetic drugs delivery.

    Science.gov (United States)

    Kesharwani, Prashant; Gorain, Bapi; Low, Siew Yeng; Tan, Siew Ann; Ling, Emily Chai Siaw; Lim, Yin Khai; Chin, Chuan Ming; Lee, Pei Yee; Lee, Chun Mey; Ooi, Chun Haw; Choudhury, Hira; Pandey, Manisha

    2018-02-01

    Nanotechnology science has been diverged its application in several fields with the advantages to operate with nanometric range of objects. Emerging field of nanotechnology has been also being approached and applied in medical biology for improved efficacy and safety. Increased success in therapeutic field has focused several approaches in the treatment of the common metabolic disorder, diabetes. The development of nanocarriers for improved delivery of different oral hypoglycemic agents compared to conventional therapies includes nanoparticles (NPs), liposomes, dendrimer, niosomes and micelles, which produces great control over the increased blood glucose level and thus becoming an eye catching and most promising technology now-a-days. Besides, embellishment of nanocarriers with several ligands makes it more targeted delivery with the protection of entrapped hypoglycaemic agents against degradation, thereby optimizing prolonged blood glucose lowering effect. Thus, nanocarriers of hypoglycemic agents provide the aim towards improved diabetes management with minimized risk of acute and chronic complications. In this review, we provide an overview on distinctive features of each nano-based drug delivery system for diabetic treatment and current NPs applications in diabetes management. Copyright © 2017 Elsevier B.V. All rights reserved.

  18. Computational and Pharmacological Evaluation of Ferrocene-Based Acyl Ureas and Homoleptic Cadmium Carboxylate Derivatives for Anti-diabetic Potential

    Directory of Open Access Journals (Sweden)

    Shahar Bano

    2018-01-01

    Full Text Available We investigated possible anti-diabetic effect of ferrocene-based acyl ureas: 4-ferrocenyl aniline (PFA, 1-(4-chlorobenzoyl-3-(4-ferrocenylphenyl urea (DPC1, 1-(3-chlorobenzoyl-3-(4-ferrocenylphenyl urea (DMC1, 1-(2-chlorobenzoyl-3-(4-ferrocenylphenyl urea (DOC1 and homoleptic cadmium carboxylates: bis (diphenylacetato cadmium (II (DPAA, bis (4-chlorophenylacetato cadmium (II (CPAA, using in silico and in vivo techniques. PFA, DPC1, DMC1, DOC1, DPAA and CPAA exhibited high binding affinities (ACE ≥ −350 Kcal/mol against targets: aldose reductase, peroxisome proliferator-activated receptor γ, 11β-hydroxysteroid dehydrogenase-1, C-alpha glucosidase and glucokinase, while showed moderate affinities (ACE ≥ −250 Kcal/mol against N-alpha glucosidase, dipeptidyl peptidase-IV, phosphorylated-Akt, glycogen synthase kinase-3β, fructose-1,6-bisphosphatase and phosphoenolpyruvate carboxykinase, whereas revealed lower affinities (ACE < −250 Kcal/mol vs. alpha amylase, protein tyrosine phosphatases 1B, glycogen phosphorylase and phosphatidylinositol 3 kinase. In alloxan (300 mg/Kg-induced diabetic mice, DPAA and DPC1 (1–10 mg/Kg at day 1, 5, 10, 15, and 20th decreased blood glucose levels, compared to diabetic control group and improved the treated animals body weight. DPAA (10 mg/Kg and DPC1 (5 mg/Kg in time-dependent manner (30–120 min. enhanced tolerance of oral glucose overload in mice. DPAA and DPCI dose-dependently at 1, 5, and 10 mg/Kg decreased glycosylated hemoglobin levels in diabetic animals, as caused by metformin. These results indicate that aforementioned derivatives of ferrocene and cadmium possess anti-diabetic potential.

  19. Evaluation of increased adherence and cost savings of an employer value-based benefits program targeting generic antihyperlipidemic and antidiabetic medications.

    Science.gov (United States)

    Clark, Bobby; DuChane, Janeen; Hou, John; Rubinstein, Elan; McMurray, Jennifer; Duncan, Ian

    2014-02-01

    A major employer implemented a change to its employee health benefits program to allow beneficiaries with diabetes or high cholesterol to obtain preselected generic antidiabetic or generic antihyperlipidemic medications with a zero dollar copayment. To receive this benefit, plan beneficiaries were required to participate in a contracted vendor's case management and/or wellness program.  To assess changes in medication adherence and the costs for generic antidiabetic and generic antihyperlipidemic medications resulting from participation in a zero copay (ZCP) program.   This was a retrospective pre-post comparison group study, evaluating adherence and cost. Participants using an antihyperlipidemic and/or antidiabetic medication during the study identification period and post-implementation period for the program were considered eligible for the study. Eligible beneficiaries who enrolled in the ZCP program during the post-implementation period were considered participants, while those who did not enroll during this period were considered nonparticipants. ZCP program participants and nonparticipants were matched via a 1-to-1 propensity scoring method using age, gender, comorbidity count, medication type (antihyperlipidemic, antidiabetic, or both), and baseline adherence as matching criteria. The proportion of days covered (PDC) metric expressed as a mean percentage was used to assess adherence to medication therapy, while payer cost was examined using prescription drug utilization expressed as per member per year (PMPY) and cost change per 30 days of medication expressed in dollars.   Among participants who were users of antidiabetic medications, the mean adherence rate was sustained from pre- to post-implementation (81.8% vs. 81.9%); however, it decreased in the matched nonparticipant group (81.9% vs. 73.1%). This difference in mean adherence over time between the participants and nonparticipants was statistically significant (0.1% vs. -8.8%, P  less than  0

  20. Cost-effectiveness of oral antiplatelet agents--current and future perspectives.

    Science.gov (United States)

    Arnold, Suzanne V; Cohen, David J; Magnuson, Elizabeth A

    2011-08-09

    Cardiovascular disease is both highly prevalent and exceedingly costly to treat. Several novel antiplatelet agents have been found to be effective in reducing the morbidity and mortality associated with cardiovascular disease. Understanding both the economic and the clinical implications of these novel therapies is particularly important. In this article, the results of published evaluations of the cost-effectiveness of oral antiplatelet strategies for use across a range of clinical conditions and treatment settings are reviewed. The results of these studies support the use of aspirin for primary prevention in high-risk patients and for secondary prevention in all patients with previous cardiovascular events. Although the optimal duration of dual antiplatelet therapy after an event remains uncertain, favorable cost-effectiveness estimates have been demonstrated for aspirin plus clopidogrel versus aspirin alone after a myocardial infarction or percutaneous coronary intervention. Moreover, prasugrel has been shown to be more cost-effective than clopidogrel for patients with an acute coronary syndrome and planned percutaneous coronary intervention. As novel antiplatelet agents emerge and existing agents are tested in different patient populations, the evaluation of the relative economic efficiency of these oral antiplatelet treatment strategies will continue to be instrumental to optimally inform clinical and health-policy decision-making.

  1. Fundamental studies of oral contrast agents for MR. Comparison of manganese agent and iron agent

    International Nuclear Information System (INIS)

    Fujita, Osamu; Hiraishi, Kumiko; Suginobu, Yoshito; Takeuchi, Masayasu; Narabayashi, Isamu

    1996-01-01

    We investigated and compared signal intensity and the effect of imaging the upper abdomen with blueberry juice (B.J.), a Mn agent utilizing the properties of paramagnetic metals, and FerriSeltz (F.S.), an iron agent. Since the relaxation effect was much stronger with B.J. than with F.S., the signal intensity required of a peroral contrast agent was able to be obtained at a much lower concentration of B.J. In imaging the upper abdomen, B.J. had a positive effect on imaging in T1-weighted images, and a negative effect in T2-weighted images. F.S. had a positive imaging effect in both, and because it showed extremely high signals in T2-weighted images, motion artifact arose. (author)

  2. Beneficial and adverse effects of chemopreventive agents

    Energy Technology Data Exchange (ETDEWEB)

    Lee, Byung Mu; Park, Kwang-Kyun

    2003-03-01

    The beneficial and adverse effects of some chemopreventive agents, such as Vitamins A, C, E, beta-carotene, indole-3-carbinol, capsaicin, garlic, and aloe are reviewed. Two large randomized trials with a lung cancer endpoint, the Alpha-Tocopherol, Beta-Carotene (ATBC) Prevention Study and the Beta-Carotene and Retinol Efficacy Trial (CARET), suggested that antioxidants might be harmful in smokers. However, the results of the Linxian study and of the ATBC or the CARET studies were significantly different in this respect, and therefore, the relationship between antioxidant and carcinogenesis remains open to debate. Indole-3-carbinol has cancer promoting activities in the colon, thyroid, pancreas, and liver, whereas capsaicin alters the metabolism of chemical carcinogens and may promote carcinogenesis at high doses. Organosulfur compounds and selenium from garlic have no or a little enhancing effect on cancer promotion stage. Information upon chemopreventive mechanisms that inhibit carcinogenesis is imperfect, although the causes and natures of certain human cancers are known. Therefore, definitive preventive guidelines should be carefully offered for various types of tumors, which properly consider ethnic variations, and the efficacies and the safety of chemopreventive agents.

  3. Beneficial and adverse effects of chemopreventive agents

    International Nuclear Information System (INIS)

    Lee, Byung Mu; Park, Kwang-Kyun

    2003-01-01

    The beneficial and adverse effects of some chemopreventive agents, such as Vitamins A, C, E, beta-carotene, indole-3-carbinol, capsaicin, garlic, and aloe are reviewed. Two large randomized trials with a lung cancer endpoint, the Alpha-Tocopherol, Beta-Carotene (ATBC) Prevention Study and the Beta-Carotene and Retinol Efficacy Trial (CARET), suggested that antioxidants might be harmful in smokers. However, the results of the Linxian study and of the ATBC or the CARET studies were significantly different in this respect, and therefore, the relationship between antioxidant and carcinogenesis remains open to debate. Indole-3-carbinol has cancer promoting activities in the colon, thyroid, pancreas, and liver, whereas capsaicin alters the metabolism of chemical carcinogens and may promote carcinogenesis at high doses. Organosulfur compounds and selenium from garlic have no or a little enhancing effect on cancer promotion stage. Information upon chemopreventive mechanisms that inhibit carcinogenesis is imperfect, although the causes and natures of certain human cancers are known. Therefore, definitive preventive guidelines should be carefully offered for various types of tumors, which properly consider ethnic variations, and the efficacies and the safety of chemopreventive agents

  4. Training strategic community agents in health effects of ionizing radiation

    International Nuclear Information System (INIS)

    Leite, Teresa C.S.B.; Silva, IIson P.M. da; Jannuzzi, Denise M.S.; Maurmo, Alexandre M.

    2013-01-01

    The main motivation for the development of training was the need to train agents (opinion makers) with proximity and credibility among the population, to clarify the most frequently asked questions in relation to ionizing radiation, the operation of nuclear power plants, emergency plans and about the possibility of there effects of radiation on the health of inhabitants in regions close to the central Nuclear Almirante Alvaro Alberto - CNAAA. The project has a target audience of 420 agents, 60 of them have already been trained in a pilot project . The results indicate that the topics of training were adequate and the agents have expanded their knowledge. On the other hand, the information passed on to communities by agents, recognized by this population as ' the most reliable people', is of greater credibility and likelihood of success in communicating important issues for the population living in the vicinity of the CNAAA. (author)

  5. Farmer to Pharmacist: Curcumin as an Anti-invasive and Antimetastatic Agent for the Treatment of Cancer

    Science.gov (United States)

    Bandyopadhyay, Debasish

    2014-12-01

    A huge number of compounds are widely distributed in nature and many of these possess medicinal/biological/pharmacological activity. Curcumin, a polyphenol derived from the rhizomes (underground stems) of Curcuma longa Linn (a member of the ginger family, commonly known as turmeric) is a culinary spice and therapeutic used in India for thousands of years to induce color and flavor in food as well as to treat a wide array of diseases. The origin of turmeric as spice and folklore medicine is so old that it is lost in legend. Curcumin has many beneficial pharmacological effects which includes, but are not limited with, antimicrobial, anti-inflammatory, antioxidant, antiviral, antiangiogenic, and antidiabetic activities. Most importantly curcumin possesses immense antitumorigenic effect. It prevents tumor invasion and metastasis in a number of animal models, including models of lung, liver, stomach, colon, breast, esophageal cancer etc. Invasion and metastasis are considered as one of the hallmarks in cancer biology. The pertinent recent applications of curcumin as anti-invasive and antimetastatic agent in in vitro and in vivo and ex vivo studies as well as associated molecular mechanisms have been discussed in this review. Curcumin has also demonstrated the ability to improve patient outcomes in clinical trials.

  6. Farmer to Pharmacist: Curcumin as an Anti-invasive and Antimetastatic Agent for the Treatment of Cancer

    Directory of Open Access Journals (Sweden)

    Debasish eBandyopadhyay

    2014-12-01

    Full Text Available A huge number of compounds are widely distributed in nature and many of these possess medicinal/biological/pharmacological activity. Curcumin, a polyphenol derived from the rhizomes (underground stems of Curcuma longa Linn (a member of the ginger family, commonly known as turmeric is a culinary spice and therapeutic used in India for thousands of years to induce color and flavor in food as well as to treat a wide array of diseases. The origin of turmeric as spice and folklore medicine is so old that it is lost in legend. Curcumin has many beneficial pharmacological effects which includes, but are not limited with, antimicrobial, anti-inflammatory, antioxidant, antiviral, antiangiogenic, and antidiabetic activities. Most importantly curcumin possesses immense antitumorigenic effect. It prevents tumor invasion and metastasis in a number of animal models, including models of lung, liver, stomach, colon, breast, esophageal cancer etc. Invasion and metastasis are considered as one of the hallmarks in cancer biology. The pertinent recent applications of curcumin as anti-invasive and antimetastatic agent in in vitro and in vivo and ex vivo studies as well as associated molecular mechanisms have been discussed in this review. Curcumin has also demonstrated the ability to improve patient outcomes in clinical trials.

  7. Measuring the effects of topically applied skin optical clearing agents and modeling the effects and consequences for laser therapies

    Science.gov (United States)

    Verkruysse, Wim; Khan, Misbah; Choi, Bernard; Svaasand, Lars O.; Nelson, J. Stuart

    2005-04-01

    Human skin prepared with an optical clearing agent manifests reduced scattering as a result of de-hydration and refractive index matching. This has potentially large effects for laser therapies of several skin lesions such as port wine stain, hair removal and tattoo removal. With most topically applied clearing agents the clearing effect is limited because they penetrate poorly through the intact superficial skin layer (stratum corneum). Agent application modi other than topical are impractical and have limited the success of optical clearing in laser dermatology. In recent reports, however, a mixture of lipofylic and hydrofylic agents was shown to successfully penetrate through the intact stratum corneum layer which has raised new interest in this field. Immediately after application, the optical clearing effect is superficial and, as the agent diffuses through the skin, reduced scattering is manifested in deeper skin layers. For practical purposes as well as to maximize therapeutic success, it is important to quantify the reduced scattering as well as the trans-cutaneous transport dynamics of the agent. We determined the time and tissue depth resolved effects of optically cleared skin by inserting a microscopic reflector array in the skin. Depth dependent light intensity was measured by quantifying the signal of the reflector array with optical coherence tomography. A 1-dimensional mass diffusion model was used to estimate a trans-cutaneous transport diffusion constant for the clearing agent mixture. The results are used in Monte Carlo modeling to determine the optimal time of laser treatment after topical application of the optical clearing agent.

  8. 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.

  9. Dgroup: DG01800 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available ulin human zinc (USP) D04543 ... Insulin human zinc, extended (USP) D05622 ... Proinsulin human (USAN) Antidiabetic... agent ... DG01636 ... Insulin and analogue ... DG01802 ... Human insulin ATC code: A10AE Antidiabetics INSR (CD220) [HSA:3643] [KO:K04527] ... CYP induction: CYP1A2 [HSA:1544

  10. Iodinated contrast media and contrast-induced nephropathy: is there a preferred cost-effective agent?

    Science.gov (United States)

    Sharma, Samin K

    2008-05-01

    Over 20 years have passed since the introduction of the tri-iodinated low-osmolar nonionic contrast agents such as iopamidol, iohexol, ioversol and iopromide. During this time, most cardiology practices have switched to these nonionic agents to avoid the nuisance side effects and cardiac adverse events associated with the older ionic contrast agents. Although the improved tolerability of the nonionic agents is generally attributed to their decreased osmolality (approximately half that of the older ionic contrast agents), in fact, these contrast agents also differ from the older agents in their ionicity, viscosity and direct chemotoxicity. The impact of these properties on safety, together with cost differences, should be considered when selecting a contrast agent.

  11. Jiang Tang Xiao Ke Granule Play an Anti-diabetic Role in Diabetic Mice Pancreatic Tissue by Regulating the mRNAs and MicroRNAs Associated with PI3K-Akt Signaling Pathway

    Directory of Open Access Journals (Sweden)

    Fang-Fang Mo

    2017-11-01

    Full Text Available Purpose: To investigate the effect of JTXK granule on the expression pattern of miRNA in pancreatic tissue of KKAy diabetic mice, and to explore the molecular mechanism and pathways of JTXK granule in anti-diabetic effect.Methods: We used high fat diet (HFD to induce the KKAy diabetic mice and screened the differentially expressed miRNAs (DEMs between JTXK-treated group (n = 6 and the diabetic group (n = 6 using MicroRNA (miRNA Microarray. C57BL/6J mice were given a normal diet as the control group (n = 6. Subsequently, miRNA target gene prediction, GO and Pathway analysis were used to explore the function of DEMs. Finally, the mechanism of anti-diabetic effects of JTXK granule was tested by in vitro INS-1 pancreatic β-cell experiment.Results: The blood glucose and body weight of JTXK-treated group was significantly lower compared with the model group. Moreover, a total of 45 miRNAs with significant differences were detected in the model group and the JTXK-treated group (P ≤ 0.05, Fold Change > 2. Further, miRNA-mRNA analysis showed that the differential expression of mmu-miR-192-5p, mmu-miR-291a-3p, mmu-miR-320-3p, mmu-miR-139-5p and mmu-miR-378a-3p are closely related to pancreatic histological changes. In addition, pathway analysis showed that the DEMs were closely related to PI3K-Akt Signaling Pathway. Furthermore, the levels of serine/threonine-protein kinase (Akt, phosphorylated Akt (p-Akt and phosphorylated forkhead transcription factor O1 (p-Foxo1 in INS-1-FOXO1 overexpressing model cells were lower than those in normal group, while JTXK granules could increase the expression of Akt, p-Akt and p-Foxo1.Conclusions: The results showed that JTXK granule could play an anti-diabetic role by regulating the mRNA and miRNAs associated with PI3K-Akt pathway in diabetic mice pancreatic tissue.

  12. Sodium-Glucose Cotransporter 2 (SGLT2 Inhibitors from Natural Products: Discovery of Next-Generation Antihyperglycemic Agents

    Directory of Open Access Journals (Sweden)

    Chang-Ik Choi

    2016-08-01

    Full Text Available Diabetes mellitus is a chronic condition associated with the metabolic impairment of insulin actions, leading to the development of life-threatening complications. Although many kinds of oral antihyperglycemic agents with different therapeutic mechanisms have been marketed, their undesirable adverse effects, such as hypoglycemia, weight gain, and hepato-renal toxicity, have increased demand for the discovery of novel, safer antidiabetic drugs. Since the important roles of the sodium-glucose cotransporter 2 (SGLT2 for glucose homeostasis in the kidney were recently elucidated, pharmacological inhibition of SGLT2 has been considered a promising therapeutic target for the treatment of type 2 diabetes. Since the discovery of the first natural SGLT2 inhibitor, phlorizin, several synthetic glucoside analogs have been developed and introduced into the market. Furthermore, many efforts to find new active constituents with SGLT2 inhibition from natural products are still ongoing. This review introduces the history of research on the development of early-generation SGLT2 inhibitors, and recent progress on the discovery of novel candidates for SGLT2 inhibitor from several natural products that are widely used in traditional herbal medicine.

  13. Multi-agent systems: effective approach for cancer care information management.

    Science.gov (United States)

    Mohammadzadeh, Niloofar; Safdari, Reza; Rahimi, Azin

    2013-01-01

    Physicians, in order to study the causes of cancer, detect cancer earlier, prevent or determine the effectiveness of treatment, and specify the reasons for the treatment ineffectiveness, need to access accurate, comprehensive, and timely cancer data. The cancer care environment has become more complex because of the need for coordination and communication among health care professionals with different skills in a variety of roles and the existence of large amounts of data with various formats. The goals of health care systems in such a complex environment are correct health data management, providing appropriate information needs of users to enhance the integrity and quality of health care, timely access to accurate information and reducing medical errors. These roles in new systems with use of agents efficiently perform well. Because of the potential capability of agent systems to solve complex and dynamic health problems, health care system, in order to gain full advantage of E- health, steps must be taken to make use of this technology. Multi-agent systems have effective roles in health service quality improvement especially in telemedicine, emergency situations and management of chronic diseases such as cancer. In the design and implementation of agent based systems, planning items such as information confidentiality and privacy, architecture, communication standards, ethical and legal aspects, identification opportunities and barriers should be considered. It should be noted that usage of agent systems only with a technical view is associated with many problems such as lack of user acceptance. The aim of this commentary is to survey applications, opportunities and barriers of this new artificial intelligence tool for cancer care information as an approach to improve cancer care management.

  14. Meta-analysis of the effects of prokinetic agents in patients with functional dyspepsia.

    Science.gov (United States)

    Hiyama, Toru; Yoshihara, Masaharu; Matsuo, Keitaro; Kusunoki, Hiroaki; Kamada, Tomoari; Ito, Masanori; Tanaka, Shinji; Nishi, Nobuo; Chayama, Kazuaki; Haruma, Ken

    2007-03-01

    Functional dyspepsia (FD) is often treated with prokinetic agents; however, the efficacy of prokinetic agents in patients with FD has been questioned recently. The aim of this study was to perform a meta-analysis of the effects of prokinetic agents in patients with FD. Prokinetic agents, including metoclopramide, domperidone, trimebutine, cisapride, itopride and mosapride, used for treatment of FD between 1951 and 2005 were identified. Twenty-seven studies were selected. Difference in the probability of response between the interventional drug and placebo was used as a summary statistic for the treatment effect. Meta-regression analysis was used to detect sources of heterogeneity. In total, 1844 subjects were assigned to an experimental arm, and 1591 subjects were assigned to a placebo arm. Publication bias was ruled out by funnel plot and statistical testing (P = 0.975). In the overall analysis, the summary statistic was 0.295 (95% confidence interval: 0.208-0.382, P < 0.001), indicating that the interventional drug has 30% excess probability of producing a response compared with placebo. The most significant source of heterogeneity was the year of publication (P < 0.001). The data clearly indicate that prokinetic agents are significantly more effective than placebo in the treatment of FD. Although FD is a chronic condition, efficacy was assessed over short periods. Long-term randomized controlled trials are needed to confirm the effect.

  15. Antioxidant, anti-diabetic and renal protective properties of Stevia rebaudiana.

    Science.gov (United States)

    Shivanna, Naveen; Naika, Mahadev; Khanum, Farhath; Kaul, Vijay K

    2013-01-01

    Stevia rebaudiana Bertoni has been used for the treatment of diabetes in, for example, Brazil, although a positive effect on antidiabetic and its complications has not been unequivocally demonstrated. This herb also has numerous therapeutic properties which have been proven safe and effective over hundreds of years. Streptozotocin is a potential source of oxidative stress that induces genotoxicity. We studied the effects of stevia leaves and its extracted polyphenols and fiber on streptozotocin induced diabetic rats. We hypothesize that supplementation of polyphenols extract from stevia to the diet causes a reduction in diabetes and its complications. Eighty Wistar rats were randomly divided into 8 groups; a standard control diet was supplemented with either stevia whole leaves powder (4.0%) or polyphenols or fiber extracted from stevia separately and fed for one month. Streptozotocin (60 mg/kg body weight, i.p) was injected to the diabetic groups on the 31st day. Several indices were analyzed to assess the modulation of the streptozotocin induced oxidative stress, toxicity and blood glucose levels by stevia. The results showed a reduction of blood glucose, ALT and AST, and increment of insulin level in the stevia whole leaves powder and extracted polyphenols fed rats compared to control diabetic group. Its feeding also reduced the MDA concentration in liver and improved its antioxidant status through antioxidant enzymes. Glucose tolerance and insulin sensitivity were improved by their feeding. Streptozotocin was also found to induce kidney damage as evidenced by decreased glomerular filtration rate; this change was however alleviated in the stevia leaves and extracted polyphenol fed groups. The results suggested that stevia leaves do have a significant role in alleviating liver and kidney damage in the STZ-diabetic rats besides its hypoglycemic effect. It might be adequate to conclude that stevia leaves could protect rats against streptozotocin induced diabetes

  16. An Agent-Based Intervention to Assist Drivers Under Stereotype Threat: Effects of In-Vehicle Agents' Attributional Error Feedback.

    Science.gov (United States)

    Joo, Yeon Kyoung; Lee-Won, Roselyn J

    2016-10-01

    For members of a group negatively stereotyped in a domain, making mistakes can aggravate the influence of stereotype threat because negative stereotypes often blame target individuals and attribute the outcome to their lack of ability. Virtual agents offering real-time error feedback may influence performance under stereotype threat by shaping the performers' attributional perception of errors they commit. We explored this possibility with female drivers, considering the prevalence of the "women-are-bad-drivers" stereotype. Specifically, we investigated how in-vehicle voice agents offering error feedback based on responsibility attribution (internal vs. external) and outcome attribution (ability vs. effort) influence female drivers' performance under stereotype threat. In addressing this question, we conducted an experiment in a virtual driving simulation environment that provided moment-to-moment error feedback messages. Participants performed a challenging driving task and made mistakes preprogrammed to occur. Results showed that the agent's error feedback with outcome attribution moderated the stereotype threat effect on driving performance. Participants under stereotype threat had a smaller number of collisions when the errors were attributed to effort than to ability. In addition, outcome attribution feedback moderated the effect of responsibility attribution on driving performance. Implications of these findings are discussed.

  17. A protocol for a randomised, double-blind, placebo-controlled study of the effect of LIraglutide on left VEntricular function in chronic heart failure patients with and without type 2 diabetes (The LIVE Study)

    DEFF Research Database (Denmark)

    Jorsal, Anders; Wiggers, Henrik; Holmager, Pernille

    2014-01-01

    INTRODUCTION: Heart failure is one of the most common cardiovascular complications of diabetes and the most disabling and deadly complication too. Many antidiabetic agents have been associated with increased morbidity and mortality in a subset of patients with chronic heart failure (CHF); thus, new...... treatment modalities are warranted. Interestingly, a beneficial effect of the incretin hormone, GLP-1, on cardiac function has been suggested in patients with diabetes and patients without diabetes. Liraglutide (Victoza) is a GLP-1 analogue developed for the treatment of type 2 diabetes (T2D); however, its...

  18. 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.

  19. Essential Oil Composition, Antioxidant, Antidiabetic and Antihypertensive Properties of Two Afromomum Species.

    Science.gov (United States)

    Adefegha, Stephen Adeniyi; Olasehinde, Tosin Abiola; Oboh, Ganiyu

    2017-01-01

    This study was designed to assess the antioxidant, antidiabetic and antihypertensive effects of essential oils from A. melegueta and A. danielli seeds. The essential oils were extracted via hydrodistillation, dried with anhydrous Na 2 SO 4 and characterized using gas chromatography-mass spectrometry (GC-MS). Antioxidant properties and inhibition of some pro-oxidant induced lipid peroxidation in rats' pancreas and heart homogenates were also determined. The results revealed that eugenol, eucalyptol, α-terpineol, α-caryophyllene and β-caryophyllene were the most abundant components in A. melegueta and A. danielli seeds. The essential oils inhibited α-amylase, α-glucosidase and angiotensin-I-converting enzyme in vitro. A.melegueta oil showed a higher α-amylase and α- glucosidase inhibitory activities with EC 50 values of 139.00 µL/mL and 91.83 µL/mL respectively than A. danielli. However, A. danielli oil (EC 50 = 48.73 µL/mL) showed the highest ACE inhibitory acivity. The highest NO radical scavenging ability was observed in A. melegueta oil while A. danielli had the highest OH radical scavenging and Fe 2+ - chelating ability. Furthermore, both essential oils inhibited SNP and Fe 2+ - induced lipid peroxidation in rats' pancreas and heart respectively in a dose dependent manner. This study reveals the biochemical principle by which essential oils from A. danielli and A.melegueta seed elicits their therapeutic effects on type-2 diabetes and hypertension.

  20. Hypoglycemic Activity and Antioxidative Stress of Extracts and Corymbiferin from Swertia bimaculata In Vitro and In Vivo

    Directory of Open Access Journals (Sweden)

    Zhaoxia Liu

    2013-01-01

    Full Text Available The present study was to investigate the anti-diabetic activities of Swertia bimaculata. Based on the glucose consumption of S. bimaculata extractsand different fractions (petroleum, dichloromethane, ethyl acetate, n-butanol and water extracts in 3T3-L1 adipocyte assay, ethanol (ETH and dichloromethane (DTH extracts had the most effective potency. Furthermore, ETH, DTH and corymbiferin (the most abundant component of DTH were evaluated for anti-diabetic effects in high fat and sucrose fed combined with low dose streptozocin induced diabetic rats. DTH and corymbiferin displayed remarkable anti-diabetic activities. The fasting blood glucose levels were significantly decreased, while the serum insulin levels were obviously increased. The oral glucose tolerance was also improved. The lowed serum total cholesterol, low density lipoprotein (LDL and triglyceride levels and increased ratio of HDL (high density lipoprotein/LDL were observed. The insulin sensitivity was improved on the basis of increased expressions of insulin-receptor substrate-2, phosphatidylinositol 3-kinase and Ser/Thr kinase AKT2. And also DTH and corymbiferin improved antioxidant capacity and carbohydrate metabolism in diabetic rats, along with the improvement of histopathology of livers and pancreatic β cells. Corymbiferin was one of active constituents, responsible for anti-diabetic properties. Therefore, S. bimaculata could be considered as an alternative agent against diabetes mellitus.

  1. 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.

  2. Clinical effect of Cystenosine on leukocytopenia at the time of therapy with radiation and antineoplastic agents

    International Nuclear Information System (INIS)

    Sato, Kazuhide; Usui, Ryu; Inoue, Hiroshi; Mihashi, Norio; Niibe, Hideo.

    1977-01-01

    Out of 62 cases, 25 cases received only radiotherapy, 11 cases received both radiotherapy and antineoplastic agents, and 26 cases received only antineoplastic agents. Total dose of x-ray ranges from 3000 to 6200 rad in 18 of 36 cases of the former two groups, and 2600 to 6260 rad of 60 Co dose were irradiated to 18 cases of the rest. This agent was administered 9 tablets per a day (one tablet contains 200 mg of inosine and 20 mg of cystine) for 19 to 142 days. Its effects on leukocytopenia showed marked effectiveness in 9 out of 25 cases treated with only radiation, effectiveness in 8 cases, and ineffectiveness in 3 cases. Its effective rate was 72.8%. The effective rate was 65.4% in the cases treated with only antineoplastic agents, and was 67.7% in all cases. A certain relationship between dose and the effective rate was not recognized. Radiation sickness, such as loss of appetite general fatigue and mausea, decreased gradually by using this agent. Side effect was not recognized particularly. (Kanao. N.)

  3. Antidiabetic effects of the medicinal plants

    Directory of Open Access Journals (Sweden)

    Waleska C. Dornas

    Full Text Available Diabetes mellitus (DM is a chronic metabolic disease characterized by hyperglycemy that has a significant impact for their patients. Its incidence is raising leading to an increase in the cost of the cares of the disease and of its complications. The treatment involves, besides dietary control and physical activity, the use of drugs that cause side effects to reach wanted pharmacological actions. However, products of plants are, frequently, considered less poisonous and with fewer side effects than synthetic drugs and widely used by the population. In this paper, several species of plants, used experimentally or in the popular medicine, acting by different ways to control glycemia and/or to inhibit symptoms and characteristic complications of the diabetes, they will be reviewed for evaluation of their supposed therapeutic effects.

  4. Extracts and compounds with anti-diabetic complications and anti-cancer activity from Castanea mollissina Blume (Chinese chestnut).

    Science.gov (United States)

    Zhang, Lin; Gao, Hui-yuan; Baba, Masaki; Okada, Yoshihito; Okuyama, Toru; Wu, Li-jun; Zhan, Li-bin

    2014-10-28

    Castanea mollissima Blume (Chinese chestnut), as a food product is known for its various nutrients and functional values to the human health. The present study was carried out to analyze the anti-diabetic complications and anti-cancer activities of the bioactive compounds present in C. mollissima. The kernels (CK), shells (CS) and involucres (CI) parts of C. Blume were extracted with 90% alcohol. The water suspension of these dried alcohol extracts were extracted using EtOAc and n-BuOH successively. The n-BuOH fraction of CI (CI-B) was isolated by silica gel column, Sephadex LH 20 column and preparative HPLC. The isolated compounds were identified by 1H-NMR, 13C-NMR, HMBC, HMQC and ESI-Q-TOF MS, All the fractions and compounds isolated were evaluated on human recombinant aldose reductase (HR-AR) assay, advanced glycation end products (AGEs) formation assay and human COLO 320 DM colon cancer cells inhibitory assay. CI-B was found to show a significant inhibitory effect in above biological screenings. Six flavonoids and three polyphenolic acids were obtained from CI-B. They were identified as kaempferol (1), kaempferol-3-O-[6''-O-(E)-p-coumaroyl]-β-D-glucopyranoside (2), kaempferol-3-O-[6''-O-(E)-p-coumaroyl]-β-D-galactopyranoside (3), kaempferol-3-O-[2''-O-(E)-p-coumaroyl]-β-D-glucopyranoside (4), kaempferol-3-O-[2", 6"-di-O-(E)-p-coumaroyl]-β-D-glucopyranoside (5) and kaempferol-3-O-[2", 6"-di-O-(E)-p-coumaroyl]-β-D-galactopyranoside (6), casuariin (7), casuarinin (8) and castalagin (9). Compounds 2-9 were found to show higher activity than quercetin (positive control) in the AR assay. Compounds 3-6, 8, and 9 showed stronger inhibitory effects than amino guanidine (positive control) on AGEs production. Compounds 4-6, 7, and 8 showed much higher cytotoxic activity than 5-fluorouracil (positive control) against the human COLO 320 DM colon cancer cells. Our results suggest that flavonoids and polyphenolic acids possesses anti-diabetes complications and anti

  5. Xylitol improves pancreatic islets morphology to ameliorate type 2 diabetes in rats: a dose response study.

    Science.gov (United States)

    Rahman, Md Atiar; Islam, Md Shahdiul

    2014-07-01

    Xylitol has been reported as a potential antidiabetic sweetener in a number of recent studies; however, the most effective dietary dose and organ-specific effects are still unclear. Six-week-old male Sprague-Dawley rats were randomly divided into 5 groups: normal control (NC), diabetic control (DBC), diabetic xylitol 2.5% (DXL2.5), diabetic xylitol 5.0% (DXL5), and diabetic xylitol 10.0% (DXL10). Diabetes was induced only in the animals in DBC and DXL groups and considered diabetic when their nonfasting blood glucose level was >300 mg/dL. The DXL groups were fed with 2.5%, 5.0%, and 10% xylitol solution, whereas the NC and DBC groups were supplied with normal drinking water. After 4-wk intervention, body weight, food and fluid intake, blood glucose, serum fructosamine, liver glycogen, serum alanine transaminase, aspartate transaminase, lactate dehydrogenase, creatine kinase, uric acid, creatinine, and most serum lipids were significantly decreased, and serum insulin concentration, glucose tolerance ability, and pancreatic islets morphology were significantly improved in the DXL10 group compared to the DBC group. The data of this study suggest that 10% xylitol has the better antidiabetic effects compared to 2.5% and 5.0% and it can be used as an excellent antidiabetic sweetener and food supplement in antidiabetic foods. Xylitol is widely used as a potential anticariogenic and sweetening agent in a number of oral care and food products when many of its health benefits are still unknown. Due to its similar sweetening power but lower calorific value (2.5 compared with 4 kcal) and lower glycemic index (13 compared with 65) compared to sucrose, recently it has been widely used as a sugar substitute particularly by overweight, obese, and diabetic patients in order to reduce their calorie intake from sucrose. However, the potential antidiabetic effects of xylitol have been discovered recently. The results of this study confirmed the effective dietary dose of xylitol for

  6. 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.

  7. Mesoscopic effects in an agent-based bargaining model in regular lattices.

    Science.gov (United States)

    Poza, David J; Santos, José I; Galán, José M; López-Paredes, Adolfo

    2011-03-09

    The effect of spatial structure has been proved very relevant in repeated games. In this work we propose an agent based model where a fixed finite population of tagged agents play iteratively the Nash demand game in a regular lattice. The model extends the multiagent bargaining model by Axtell, Epstein and Young modifying the assumption of global interaction. Each agent is endowed with a memory and plays the best reply against the opponent's most frequent demand. We focus our analysis on the transient dynamics of the system, studying by computer simulation the set of states in which the system spends a considerable fraction of the time. The results show that all the possible persistent regimes in the global interaction model can also be observed in this spatial version. We also find that the mesoscopic properties of the interaction networks that the spatial distribution induces in the model have a significant impact on the diffusion of strategies, and can lead to new persistent regimes different from those found in previous research. In particular, community structure in the intratype interaction networks may cause that communities reach different persistent regimes as a consequence of the hindering diffusion effect of fluctuating agents at their borders.

  8. Mesoscopic effects in an agent-based bargaining model in regular lattices.

    Directory of Open Access Journals (Sweden)

    David J Poza

    Full Text Available The effect of spatial structure has been proved very relevant in repeated games. In this work we propose an agent based model where a fixed finite population of tagged agents play iteratively the Nash demand game in a regular lattice. The model extends the multiagent bargaining model by Axtell, Epstein and Young modifying the assumption of global interaction. Each agent is endowed with a memory and plays the best reply against the opponent's most frequent demand. We focus our analysis on the transient dynamics of the system, studying by computer simulation the set of states in which the system spends a considerable fraction of the time. The results show that all the possible persistent regimes in the global interaction model can also be observed in this spatial version. We also find that the mesoscopic properties of the interaction networks that the spatial distribution induces in the model have a significant impact on the diffusion of strategies, and can lead to new persistent regimes different from those found in previous research. In particular, community structure in the intratype interaction networks may cause that communities reach different persistent regimes as a consequence of the hindering diffusion effect of fluctuating agents at their borders.

  9. Advances on Practical Applications of Agents and Multi-Agent Systems 10th International Conference on Practical Applications of Agents and Multi-Agent Systems

    CERN Document Server

    Müller, Jörg; Rodríguez, Juan; Pérez, Javier

    2012-01-01

    Research on Agents and Multi-Agent Systems has matured during the last decade and many effective applications of this technology are now deployed. PAAMS provides an international forum to present and discuss the latest scientific developments and their effective applications, to assess the impact of the approach, and to facilitate technology transfer. PAAMS started as a local initiative, but has since grown to become THE international yearly platform to present, to discuss, and to disseminate the latest developments and the most important outcomes related to real-world applications. It provides a unique opportunity to bring multi-disciplinary experts, academics and practitioners together to exchange their experience in the development and deployment of Agents and Multi-Agent Systems. PAAMS intends to bring together researchers and developers from industry and the academic world to report on the latest scientific and technical advances on the application of multi-agent systems, to discuss and debate the major ...

  10. Highlights on Practical Applications of Agents and Multi-Agent Systems 10th International Conference on Practical Applications of Agents and Multi-Agent Systems

    CERN Document Server

    Sánchez, Miguel; Mathieu, Philippe; Rodríguez, Juan; Adam, Emmanuel; Ortega, Alfonso; Moreno, María; Navarro, Elena; Hirsch, Benjamin; Lopes-Cardoso, Henrique; Julián, Vicente

    2012-01-01

    Research on Agents and Multi-Agent Systems has matured during the last decade and many effective applications of this technology are now deployed. PAAMS provides an international forum to present and discuss the latest scientific developments and their effective applications, to assess the impact of the approach, and to facilitate technology transfer. PAAMS started as a local initiative, but has since grown to become THE international yearly platform to present, to discuss, and to disseminate the latest developments and the most important outcomes related to real-world applications. It provides a unique opportunity to bring multi-disciplinary experts, academics and practitioners together to exchange their experience in the development and deployment of Agents and Multi-Agent Systems. PAAMS intends to bring together researchers and developers from industry and the academic world to report on the latest scientific and technical advances on the application of multi-agent systems, to discuss and debate the major ...

  11. Evaluation of the antidiabetic property of aqueous leaves extract of Zanthoxylum armatum DC. using in vivo and in vitro approaches

    Directory of Open Access Journals (Sweden)

    Carey Vana Rynjah

    2018-01-01

    Full Text Available The present study was designed to evaluate the antidiabetic potential of the aqueous leaves extract of Zanthoxylum armatum DC. leaves using in vivo and in vitro approaches. For in vivo studies, blood glucose level was monitored at different intervals after administration of varying doses of the extract for its hypoglycemic (100–6000 mg/kg b.w. and antihyperglycemic (250 mg/kg b.w. effect in normoglycemic and diabetic mice. In vitro enzymatic inhibition activity was tested against α-amylase, α- and β-glucosidase and lipase. Additionally hydroxyl radical, hydrogen peroxide scavenging assay and phytochemical screening were also performed. Element analysis of the plant was studied by Atomic Absorption Spectrometry (AAS and Inductively Coupled Plasma Atomic Emission Spectrometer (ICP-AES. The plant extract showed significant hypoglycemic and antihyperglycemic effect in normoglycemic and diabetic mice. The IC50 values of extract for α-amylase, β-glucosidase, lipase, hydroxyl radical scavenging activity, hydrogen peroxide scavenging activity were 7.40 mg/ml, 0.30 mg/ml, 8.35 mg/ml, 3.25 mg/ml, 9.62 mg/ml respectively and the percentage of inhibition for α-glucosidase was 79.82% at 0.8 mg/ml. In vitro studies were compared with their respective standards. Elemental analysis revealed the presence of essential elements such as Mg, V, Fe, Cr, Zn, Cu, Mo, Mn, K, Ca, P and Sr which are all known to play a role in regulating blood glucose. The results demonstrate that Z. armatum aqueous leaves extract possess antidiabetic property in both in vivo and in vitro condition.

  12. Ecological effects of various toxic agents on the aquatic microcosm in comparison with acute ionizing radiation

    International Nuclear Information System (INIS)

    Fuma, S.; Ishii, N.; Takeda, H.; Miyamoto, K.; Yanagisawa, K.; Ichimasa, Y.; Saito, M.; Kawabata, Z.; Polikarpov, G.G.

    2003-01-01

    The purpose of this study was an evaluation of the effect levels of various toxic agents compared with acute doses of ionizing radiation for the experimental model ecosystem, i.e., microcosm mimicking aquatic microbial communities. For this purpose, the authors used the microcosm consisting of populations of the flagellate alga Euglena gracilis as a producer, the ciliate protozoan Tetrahymena thermophila as a consumer and the bacterium Escherichia coli as a decomposer. Effects of aluminum and copper on the microcosm were investigated in this study, while effects of γ-rays, ultraviolet radiation, acidification, manganese, nickel and gadolinium were reported in previous studies. The microcosm could detect not only the direct effects of these agents but also the community-level effects due to the interspecies interactions or the interactions between organisms and toxic agents. The authors evaluated doses or concentrations of each toxic agent which had the following effects on the microcosm: (1) no effects; (2) recognizable effects, i.e., decrease or increase in the cell densities of at least one species; (3) severe effects, i.e., extinction of one or two species; and (4) destructive effects, i.e., extinction of all species. The resulting effects data will contribute to an ecological risk assessment of the toxic agents compared with acute doses of ionizing radiation

  13. [New SGLT2 inhibitor empagliflozin: modern and safe treatment of diabetes].

    Science.gov (United States)

    Rušavý, Zdeněk

    2014-11-01

    Empagliflozin is agent of new antidiabetic drugs that cause glycosuria blocking the glucose reuptake in the proxi-mal tubule. The loss of 50-100 g of glucose / 24 hours in the urine results in a reduction of fasting glucose, especially post-prandial glucose, the energy expenditure of 200-400 kcal / day and blood pressure lowering. Treatment efficacy does not decrease over time, as it is not dependent on its own insulin production. The work evaluates the safety of modern treatment with empagliflozin which will soon appear in the portfolio of antidiabetic agents in the Czech Republic. The conducted studies with a special focus on empagliflozin treatment have shown high efficacy, safety and good tolerability of drug. It has been described a higher incidence of genital infections with non-severe course, especially in women. The drug does not cause hypoglycaemia. In combination with sulfonylurea hypoglycaemia may occur. Empagliflozin does not cause clinically significant dehydration or hypotension in patients about 60 years of age, but some caution in empagliflozin treatment should be in elderly and fragile patients. The big convenience of empagliflozin is its clinically non-significant interactions with other drugs and simple dosage of 1 tablet / day orally. In conclusion, empagliflozin is highly effective oral antidiabetic agent with a potential of wide application in all stages of type 2 diabetes in monotherapy or combined with other medication. The treatment is associated with weight loss and blood pressure lowering. The drug is effective and safe until eGFR 45 ml / s, in lower values the treatment should be discontinued. The occurrence of side effects is rare, except increased incidence of genital infections especially in women and increased risk of hypoglycaemia when empagliflozin is combined with sulfonylurea.

  14. Topical antifungal agents: an update.

    Science.gov (United States)

    Diehl, K B

    1996-10-01

    So many topical antifungal agents have been introduced that it has become very difficult to select the proper agent for a given infection. Nonspecific agents have been available for many years, and they are still effective in many situations. These agents include Whitfield's ointment, Castellani paint, gentian violet, potassium permanganate, undecylenic acid and selenium sulfide. Specific antifungal agents include, among others, the polyenes (nystatin, amphotericin B), the imidazoles (metronidazole, clotrimazole) and the allylamines (terbinafine, naftifine). Although the choice of an antifungal agent should be based on an accurate diagnosis, many clinicians believe that topical miconazole is a relatively effective agent for the treatment of most mycotic infections. Terbinafine and other newer drugs have primary fungicidal effects. Compared with older antifungal agents, these newer drugs can be used in lower concentrations and shorter therapeutic courses. Studies are needed to evaluate the clinical efficacies and cost advantages of both newer and traditional agents.

  15. The effect of calcium phosphate-containing desensitizing agent on ...

    African Journals Online (AJOL)

    Objective: The aim of this study was to investigate the effect of calcium phosphate containing desensitizing pretreatments on the microtensile bond strength (MTBS) and microleakage of the multimode adhesive agent to dentin. Materials and Methods: In this study, twelve noncarious, freshly extracted human third molar teeth ...

  16. Antioxidant, antihyperglycemic, and antidiabetic activity of Apis mellifera bee tea.

    Directory of Open Access Journals (Sweden)

    Janielle da Silva Melo da Cunha

    Full Text Available Diabetes has emerged as one of the largest global epidemics; it is estimated that by 2035, there will be 592 million diabetic people in the world. Brazilian biodiversity and the knowledge of traditional peoples have contributed to the treatment of several diseases, including diabetes. Apis mellifera bee tea is used by indigenous Brazilians to treat diabetes, and this traditional knowledge needs to be recorded and studied.The objective of this study was to record the use and to evaluate the antioxidant, antihyperglycemic, and antidiabetic activity of Apis mellifera bee tea, which is used by the Guarani and Kaiowá indigenous people for the treatment of diabetes. Semi-structured interviews were performed with Guarani and Kaiowá ethnic indigenous people from the State of Mato Grosso do Sul, Brazil, seeking to identify the animal species used for medicinal purposes. For the experimental procedures, tea prepared with macerated Apis mellifera bees was used. In vitro assays were performed to evaluate antioxidant activity; direct free radical scavenging, protection against oxidative hemolysis, lipid peroxidation were evaluated in human erythrocytes and potential in inhibiting the formation of advanced glycation end products (AGEs. In vivo, normoglycemic Swiss male mice treated with Apis mellifera tea (AmT were subjected to the oral glucose tolerance test and compared with control and metformin-treated groups. Diet-induced diabetic mice were treated for 21 days with AmT and evaluated for glycemia and malondialdehyde levels in the blood, liver, nervous system, and eyes. During interviews, the indigenous people described the use of Apis mellifera bee tea for the treatment of diabetes. In in vitro assays, AmT showed direct antioxidant activity and reduced oxidative hemolysis and malondialdehyde generation in human erythrocytes. The AmT inhibited the formation of AGEs by albumin-fructose pathways and methylglyoxal products. In vivo, after oral glucose

  17. Antioxidant, antihyperglycemic, and antidiabetic activity of Apis mellifera bee tea.

    Science.gov (United States)

    Melo da Cunha, Janielle da Silva; Alfredo, Tamaeh Monteiro; Dos Santos, Jéssica Maurino; Alves Junior, Valter Vieira; Rabelo, Luiza Antas; Lima, Emerson Silva; Boleti, Ana Paula de Araújo; Carollo, Carlos Alexandre; Dos Santos, Edson Lucas; de Picoli Souza, Kely

    2018-01-01

    Diabetes has emerged as one of the largest global epidemics; it is estimated that by 2035, there will be 592 million diabetic people in the world. Brazilian biodiversity and the knowledge of traditional peoples have contributed to the treatment of several diseases, including diabetes. Apis mellifera bee tea is used by indigenous Brazilians to treat diabetes, and this traditional knowledge needs to be recorded and studied.The objective of this study was to record the use and to evaluate the antioxidant, antihyperglycemic, and antidiabetic activity of Apis mellifera bee tea, which is used by the Guarani and Kaiowá indigenous people for the treatment of diabetes. Semi-structured interviews were performed with Guarani and Kaiowá ethnic indigenous people from the State of Mato Grosso do Sul, Brazil, seeking to identify the animal species used for medicinal purposes. For the experimental procedures, tea prepared with macerated Apis mellifera bees was used. In vitro assays were performed to evaluate antioxidant activity; direct free radical scavenging, protection against oxidative hemolysis, lipid peroxidation were evaluated in human erythrocytes and potential in inhibiting the formation of advanced glycation end products (AGEs). In vivo, normoglycemic Swiss male mice treated with Apis mellifera tea (AmT) were subjected to the oral glucose tolerance test and compared with control and metformin-treated groups. Diet-induced diabetic mice were treated for 21 days with AmT and evaluated for glycemia and malondialdehyde levels in the blood, liver, nervous system, and eyes. During interviews, the indigenous people described the use of Apis mellifera bee tea for the treatment of diabetes. In in vitro assays, AmT showed direct antioxidant activity and reduced oxidative hemolysis and malondialdehyde generation in human erythrocytes. The AmT inhibited the formation of AGEs by albumin-fructose pathways and methylglyoxal products. In vivo, after oral glucose overload, normoglycemic

  18. Optimizing weight control in diabetes: antidiabetic drug selection

    Directory of Open Access Journals (Sweden)

    S Kalra

    2010-08-01

    Full Text Available S Kalra1, B Kalra1, AG Unnikrishnan2, N Agrawal3, S Kumar41Bharti Hospital, Karnal; 2Amrita Institute of Medical Science, Kochi; 3Medical College, Gwalior; 4Excel Life Sciences, Noida, IndiaDate of preparation: 18th August 2010Conflict of interest: SK has received speaker fees from Novo Nordisk, sanofi-aventis, MSD, Eli Lilly, BMS, and AstraZeneca.Clinical question: Which antidiabetic drugs provide optimal weight control in patients with type 2 diabetes?Results: Metformin reduces weight gain, and may cause weight loss, when given alone or in combination with other drugs. Pioglitazone and rosiglitazone use is associated with weight gain. Use of the glucagon-like peptide-1 (GLP-1 analogs, liraglutide and exenatide, is associated with weight loss. Dipeptidyl peptidase-4 (DPP-4 inhibitors are considered weight-neutral. Results with insulin therapy are conflicting. Insulin detemir provides weight control along with glycemic control.Implementation: • Weight gain is considered an inevitable part of good glycemic control using conventional modalities of treatment such as sulfonylureas.• Use of metformin, weight-sparing insulin analogs such as insulin detemir, and liraglutide, should be encouraged as monotherapy, or in combination with other drugs.Keywords: weight control, diabetes

  19. Natural Products for the Treatment of Type 2 Diabetes Mellitus.

    Science.gov (United States)

    Ríos, José Luis; Francini, Flavio; Schinella, Guillermo R

    2015-08-01

    Type 2 diabetes mellitus is a metabolic disease characterized by persistent hyperglycemia. High blood sugar can produce long-term complications such as cardiovascular and renal disorders, retinopathy, and poor blood flow. Its development can be prevented or delayed in people with impaired glucose tolerance by implementing lifestyle changes or the use of therapeutic agents. Some of these drugs have been obtained from plants or have a microbial origin, such as galegine isolated from Galega officinalis, which has a great similarity to the antidiabetic drug metformin. Picnogenol, acarbose, miglitol, and voglibose are other antidiabetic products of natural origin. This review compiles the principal articles on medicinal plants used for treating diabetes and its comorbidities, as well as mechanisms of natural products as antidiabetic agents. Inhibition of α-glucosidase and α-amylase, effects on glucose uptake and glucose transporters, modification of mechanisms mediated by the peroxisome proliferator-activated receptor, inhibition of protein tyrosine phosphatase 1B activity, modification of gene expression, and activities of hormones involved in glucose homeostasis such as adiponectin, resistin, and incretin, and reduction of oxidative stress are some of the mechanisms in which natural products are involved. We also review the most relevant clinical trials performed with medicinal plants and natural products such as aloe, banaba, bitter melon, caper, cinnamon, cocoa, coffee, fenugreek, garlic, guava, gymnema, nettle, sage, soybean, green and black tea, turmeric, walnut, and yerba mate. Compounds of high interest as potential antidiabetics are: fukugetin, palmatine, berberine, honokiol, amorfrutins, trigonelline, gymnemic acids, gurmarin, and phlorizin. Georg Thieme Verlag KG Stuttgart · New York.

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

    Directory of Open Access Journals (Sweden)

    Seung Hwan Hwang

    2017-01-01

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

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

    Science.gov (United States)

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

    2017-01-01

    The objective of the present study was to evaluate α -glucosidase inhibitory and antidiabetic effects of Nopal water extract (NPWE) and Nopal dry power (NADP) in low-dose streptozotocin- (STZ-) induced diabetic rats fed a high-fat diet (HFD). The type 2 diabetic rat model was induced by HFD and low-dose STZ. The rats were divided into four groups as follows: (1) nondiabetic rats fed a regular diet (RD-Control); (2) low-dose STZ-induced diabetic rats fed HFD (HF-STZ-Control); (3) low-dose STZ-induced diabetic rats fed HFD and supplemented with NPWE (100 mg/kg body weight, HF-STZ-NPWE); and (4) low-dose STZ-induced diabetic rats fed HFD and supplemented with comparison medication (rosiglitazone, 10 mg/kg, body weight, HF-STZ-Rosiglitazone). In results, NPWE and NADP had IC 50 values of 67.33 and 86.68  μ g/mL, both of which exhibit inhibitory activities but lower than that of acarbose (38.05  μ g/mL) while NPWE group significantly decreased blood glucose levels compared to control and NPDP group on glucose tolerance in the high-fat diet fed rats model ( P < 0.05). Also, the blood glucose levels of HR-STZ-NPWE group were significantly lower ( P < 0.05) than HR-STZ-Control group on low-dose STZ-induced diabetic rats fed HFD. Based on these findings, we suggested that NPWE could be considered for the prevention and/or treatment of blood glucose and a potential use as a dietary supplement.

  2. Training strategic community agents in health effects of ionizing radiation; Capacitacao de agentes comunitarios de saude em efeitos das radiacoes ionizantes

    Energy Technology Data Exchange (ETDEWEB)

    Leite, Teresa C.S.B.; Silva, IIson P.M. da; Jannuzzi, Denise M.S. [Fundacao Eletronuclear de Assistencia Medica (CIRA/FEAM), Angra dos Reis, RJ (Brazil). Centro de Informacoes em Radioepidemiologia; Maurmo, Alexandre M., E-mail: ammaurmo@gmail.com [Fundacao Eletronuclear de Assistencia Medica (CMRl/CTNV/FEAM), Angra dos Reis, RJ (Brazil). Centro de Treinamento Prof. Nelson Valverde. Centro de Medicina das Radiacoes Ionizantes

    2013-11-01

    The main motivation for the development of training was the need to train agents (opinion makers) with proximity and credibility among the population, to clarify the most frequently asked questions in relation to ionizing radiation, the operation of nuclear power plants, emergency plans and about the possibility of there effects of radiation on the health of inhabitants in regions close to the central Nuclear Almirante Alvaro Alberto - CNAAA. The project has a target audience of 420 agents, 60 of them have already been trained in a pilot project . The results indicate that the topics of training were adequate and the agents have expanded their knowledge. On the other hand, the information passed on to communities by agents, recognized by this population as ' the most reliable people', is of greater credibility and likelihood of success in communicating important issues for the population living in the vicinity of the CNAAA. (author)

  3. GC-MS analysis and screening of antidiabetic, antioxidant and hypolipidemic potential of Cinnamomum tamala oil in streptozotocin induced diabetes mellitus in rats

    Directory of Open Access Journals (Sweden)

    Kumar Suresh

    2012-08-01

    Full Text Available Abstract Aim of the study This study was made to investigate the antidiabetic, antioxidant and hypolipidemic potential of Cinnamomum tamala, (Buch.-Ham. Nees & Eberm (Tejpat oil (CTO in streptozotocin (STZ induced diabetes in rats along with evaluation of chemical constituents. Materials and methods The GC-MS (Gas chromatography–mass spectrometry analysis of the oil showed 31 constituents of which cinnamaldehyde was found the major component (44.898%. CTO and cinnamaldehyde was orally administered to diabetic rats to study its effect in both acute and chronic antihyperglycemic models. The body weight, oral glucose tolerance test and biochemical parameters viz. glucose level, insulin level, liver glycogen content, glycosylated hemoglobin, total plasma cholesterol, triglyceride and antioxidant parameters were estimated for all treated groups and compared against diabetic control group. Results CTO (100 mg/kg and 200 mg/kg, cinnamaldehyde (20 mg/kg and glibenclamide (0.6 mg/kg in respective groups of diabetic animals administered for 28 days reduced the blood glucose level in streptozotocin induced diabetic rats. There was significant increase in body weight, liver glycogen content, plasma insulin level and decrease in the blood glucose, glycosylated hemoglobin and total plasma cholesterol in test groups as compared to control group. The results of CTO and cinnamaldehyde were found comparable with standard drug glibenclamide. In vitro antioxidant studies on CTO using various models showed significant antioxidant activity. In vivo antioxidant studies on STZ induced diabetic rats revealed decreased malondialdehyde (MDA and increased reduced glutathione (GSH. Conclusion Thus the investigation results that CTO has significant antidiabetic, antioxidant and hypolipidemic activity.

  4. Effect of some stabilizing agents on globule characteristics and ...

    African Journals Online (AJOL)

    This study investigated the effects of some stabilizing agents (cassava, maize and bentonite mucilages) on globule characteristics and rheological properties of oil in water emulsions. Emulsions were prepared by mixing varying proportions of the mucilages with Arachis oil in the ratio of 60:40 (oil: water) with the aid of a ...

  5. Antidiabetic activities of aqueous ethanol and n-butanol fraction of Moringa stenopetala leaves in streptozotocin-induced diabetic rats.

    Science.gov (United States)

    Toma, Alemayehu; Makonnen, Eyasu; Mekonnen, Yelamtsehay; Debella, Asfaw; Adisakwattana, Sirichai

    2015-07-18

    Moringa stenopetala has been used in traditional health systems to treat diabetes mellitus. The aim of this study was to investigate the antidiabetic activity of aqueous ethanol and n-butanol fraction of Moringa stenopetala leaves in streptozotocin (STZ) induced diabetic rats. The aqueous ethanol extract and n-butanol fraction of Moringa stenopetala leaves hydroalcoholic (500 mg/kg body weight) and metformin (150 mg/kg body weight) were administered to diabetic rats. Blood glucose, lipid profiles, liver and kidney function were examined after 14 days of experiment. Histopathological profile of the pancreas was also observed in diabetic rats at the end of study. An oral sucrose challenge test was also carried out to assess the post prandial effect of the extract. Oral administration of the aqueous ethanol and n-butanol extracts of Moringa stenopetala leaves (500 mg/kg body weight) and metformin (150 mg/kg) significantly reduced blood glucose level (PMoringa stenopetala leaves possess antihyperglycemic and antihyperlipidemic properties, and alleviate STZ-induced pancreatic damage in diabetic rats. The beneficial effects of plant material in inhibition of diabetes-induced complications are being investigated.

  6. Dipeptidyl peptidase-4 (DPP-4) inhibitors are favourable to glucagon-like peptide-1 (GLP-1) agonists

    DEFF Research Database (Denmark)

    Madsbad, Sten

    2012-01-01

    Incretin-based therapies, which include the GLP-1 receptor agonists and DPP-4 inhibitors, use the antidiabetic properties of potentiating the GLP-1 receptor signalling via the regulation of insulin and glucagon secretion, inhibition of gastric emptying and suppression of appetite. Most physicians...... will start antidiabetic treatment with metformin, but adding a GLP-1 receptor agonist as the second drug seems to be optimal since more patients will reach an HbA1c below 7% than with a DPP-4 inhibitor or another oral antidiabetic agents and with minimal risk of hypoglycaemia. The GLP-1 receptor agonists...

  7. Current Therapies That Modify Glucagon Secretion

    DEFF Research Database (Denmark)

    Grøndahl, Magnus F.; Keating, Damien J.; Vilsbøll, Tina

    2017-01-01

    and provide insights into how antidiabetic drugs influence glucagon secretion as well as a perspective on the future of glucagon-targeting drugs. Recent Findings: Several older as well as recent investigations have evaluated the effect of antidiabetic agents on glucagon secretion to understand how glucagon...... may be involved in the drugs’ efficacy and safety profiles. Based on these findings, modulation of glucagon secretion seems to play a hitherto underestimated role in the efficacy and safety of several glucose-lowering drugs. Summary: Numerous drugs currently available to diabetologists are capable...... of altering glucagon secretion: metformin, sulfonylurea compounds, insulin, glucagon-like peptide-1 receptor agonists, dipeptidyl peptidase-4 inhibitors, sodium-glucose cotransporter 2 inhibitors and amylin mimetics. Their diverse effects on glucagon secretion are of importance for their individual efficacy...

  8. Chronic antidiabetic sulfonylureas in vivo: reversible effects on mouse pancreatic beta-cells.

    Directory of Open Access Journals (Sweden)

    Maria Sara Remedi

    2008-10-01

    Full Text Available Pancreatic beta-cell ATP-sensitive potassium (K ATP channels are critical links between nutrient metabolism and insulin secretion. In humans, reduced or absent beta-cell K ATP channel activity resulting from loss-of-function K ATP mutations induces insulin hypersecretion. Mice with reduced K ATP channel activity also demonstrate hyperinsulinism, but mice with complete loss of K ATP channels (K ATP knockout mice show an unexpected insulin undersecretory phenotype. Therefore we have proposed an "inverse U" hypothesis to explain the response to enhanced excitability, in which excessive hyperexcitability drives beta-cells to insulin secretory failure without cell death. Many patients with type 2 diabetes treated with antidiabetic sulfonylureas (which inhibit K ATP activity and thereby enhance insulin secretion show long-term insulin secretory failure, which we further suggest might reflect a similar progression.To test the above hypotheses, and to mechanistically investigate the consequences of prolonged hyperexcitability in vivo, we used a novel approach of implanting mice with slow-release sulfonylurea (glibenclamide pellets, to chronically inhibit beta-cell K ATP channels. Glibenclamide-implanted wild-type mice became progressively and consistently diabetic, with significantly (p < 0.05 reduced insulin secretion in response to glucose. After 1 wk of treatment, these mice were as glucose intolerant as adult K ATP knockout mice, and reduction of secretory capacity in freshly isolated islets from implanted animals was as significant (p < 0.05 as those from K ATP knockout animals. However, secretory capacity was fully restored in islets from sulfonylurea-treated mice within hours of drug washout and in vivo within 1 mo after glibenclamide treatment was terminated. Pancreatic immunostaining showed normal islet size and alpha-/beta-cell distribution within the islet, and TUNEL staining showed no evidence of apoptosis.These results demonstrate that

  9. Synergistic Effects of Nucleating Agents and Plasticizers on the Crystallization Behavior of Poly(lactic acid

    Directory of Open Access Journals (Sweden)

    Xuetao Shi

    2015-01-01

    Full Text Available The synergistic effect of nucleating agents and plasticizers on the thermal and mechanical performance of PLA nanocomposites was investigated with the objective of increasing the crystallinity and balancing the stiffness and toughness of PLA mechanical properties. Calcium carbonate, halloysite nanotubes, talc and LAK (sulfates were compared with each other as heterogeneous nucleating agents. Both the DSC isothermal and non-isothermal studies indicated that talc and LAK were the more effective nucleating agents among the selected fillers. Poly(D-lactic acid (PDLA acted also as a nucleating agent due to the formation of the PLA stereocomplex. The half crystallization time was reduced by the addition of talc to about 2 min from 37.5 min of pure PLA by the isothermal crystallization study. The dynamic mechanical thermal study (DMTA indicated that nanofillers acted as both reinforcement fillers and nucleating agents in relation to the higher storage modulus. The plasticized PLA studied by DMTA indicated a decreasing glass transition temperature with the increasing of the PEG content. The addition of nanofiller increased the Young’s modulus. PEG had the plasticization effect of increasing the break deformation, while sharply decreasing the stiffness and strength of PLA. The synergistic effect of nanofillers and plasticizer achieved the balance between stiffness and toughness with well-controlled crystallization.

  10. Rediscovering medicinal plants' potential with OMICS: microsatellite survey in expressed sequence tags of eleven traditional plants with potent antidiabetic properties.

    Science.gov (United States)

    Sahu, Jagajjit; Sen, Priyabrata; Choudhury, Manabendra Dutta; Dehury, Budheswar; Barooah, Madhumita; Modi, Mahendra Kumar; Talukdar, Anupam Das

    2014-05-01

    Herbal medicines and traditionally used medicinal plants present an untapped potential for novel molecular target discovery using systems science and OMICS biotechnology driven strategies. Since up to 40% of the world's poor people have no access to government health services, traditional and folk medicines are often the only therapeutics available to them. In this vein, North East (NE) India is recognized for its rich bioresources. As part of the Indo-Burma hotspot, it is regarded as an epicenter of biodiversity for several plants having myriad traditional uses, including medicinal use. However, the improvement of these valuable bioresources through molecular breeding strategies, for example, using genic microsatellites or Simple Sequence Repeats (SSRs) or Expressed Sequence Tags (ESTs)-derived SSRs has not been fully utilized in large scale to date. In this study, we identified a total of 47,700 microsatellites from 109,609 ESTs of 11 medicinal plants (pineapple, papaya, noyontara, bitter orange, bermuda brass, ratalu, barbados nut, mango, mulberry, lotus, and guduchi) having proven antidiabetic properties. A total of 58,159 primer pairs were designed for the non-redundant 8060 SSR-positive ESTs and putative functions were assigned to 4483 unique contigs. Among the identified microsatellites, excluding mononucleotide repeats, di-/trinucleotides are predominant, among which repeat motifs of AG/CT and AAG/CTT were most abundant. Similarity search of SSR containing ESTs and antidiabetic gene sequences revealed 11 microsatellites linked to antidiabetic genes in five plants. GO term enrichment analysis revealed a total of 80 enriched GO terms widely distributed in 53 biological processes, 17 molecular functions, and 10 cellular components associated with the 11 markers. The present study therefore provides concrete insights into the frequency and distribution of SSRs in important medicinal resources. The microsatellite markers reported here markedly add to the genetic

  11. Myopic and Forward Looking Behavior in Branded Oral Anti-Diabetic Medication Consumption: An Example from Medicare Part D.

    Science.gov (United States)

    Sacks, Naomi C; Burgess, James F; Cabral, Howard J; Pizer, Steven D

    2017-06-01

    We evaluate consumption responses to the non-linear Medicare Part D prescription drug benefit. We compare propensity-matched older patients with diabetes and Part D Standard or low-income-subsidy (LIS) coverage. We evaluate monthly adherence to branded oral anti-diabetics, with high end-of-year donut hole prices (>$200) for Standard patients and consistent, low (≤$6) prices for LIS. As an additional control, we examine adherence to generic anti-diabetics, with relatively low, consistent prices for Standard patients. If Standard patients are forward looking, they will reduce branded adherence in January, and LIS-Standard differences will be constant through the year. Contrary to this expectation, branded adherence is lower for Standard patients in January and diverges from LIS as the coverage year progresses. Standard-LIS generic adherence differences are minimal. Our findings suggest that seniors with chronic conditions respond myopically to the nonlinear Part D benefit, reducing consumption in response to high deductible, initial coverage and gap prices. Thus, when the gap is fully phased out in 2020, cost-related nonadherence will likely remain in the face of higher spot prices for more costly branded medications. These results contribute to studies of Part D plan choice and medication adherence that suggest that seniors may not make optimal healthcare decisions. Copyright © 2016 John Wiley & Sons, Ltd. Copyright © 2016 John Wiley & Sons, Ltd.

  12. Potential use of bitter melon (Momordica charantia) derived compounds as antidiabetics: In silico and in vivo studies.

    Science.gov (United States)

    Elekofehinti, Olusola Olalekan; Ariyo, Esther Opeyemi; Akinjiyan, Moses Orimoloye; Olayeriju, Olanrewaju Sam; Lawal, Akeem Olalekan; Adanlawo, Isaac Gbadura; Rocha, Joao Batista Teixeira

    2018-05-12

    Momordica charantia (bitter lemon) belongs to the cucurbitaceae family which has been extensively used in traditional medicines for the cure of various ailments such as cancer and diabetes. The underlying mechanism of M. charantia to maintain glycemic control was investigated. GLP-1 and DPP-4 gene modulation by M. charantia (5-20% inclusion in rats diet) was investigated in vivo by RT-PCR and possible compounds responsible for diabetic action predicted through in silico approach. Phytochemicalss previously characterized from M. charantia were docked into glucacon like peptide-1 receptor (GLP-1r), dipeptidyl peptidase (DPP4) and Takeda-G-protein-receptor-5 (TGR5) predicted using Autodock Vina. The results of the in silico suggests momordicosides D (ligand for TGR5), cucurbitacin (ligand for GLP-1r) and charantin (ligand for DPP-4) as the major antidiabetic compounds in bitter lemon leaf. M. charantia increased the expression of GLP-1 by about 295.7% with concomitant decreased in expression of DPP-4 by 87.2% with 20% inclusion in rat's diet. This study suggests that the mechanism underlying the action of these compounds is through activation of TGR5 and GLP-1 receptor with concurrent inhibition of DPP4. This study confirmed the use of this plant in diabetes management and the possible bioactive compounds responsible for its antidiabetic property are charantin, cucurbitacin and momordicoside D and all belong to the class of saponins. Copyright © 2018 Elsevier B.V. All rights reserved.

  13. ATP-modulated K+ channels sensitive to antidiabetic sulfonylureas are present in adenohypophysis and are involved in growth hormone release.

    OpenAIRE

    Bernardi, H; De Weille, J R; Epelbaum, J; Mourre, C; Amoroso, S; Slama, A; Fosset, M; Lazdunski, M

    1993-01-01

    The adenohypophysis contains high-affinity binding sites for antidiabetic sulfonylureas that are specific blockers of ATP-sensitive K+ channels. The binding protein has a M(r) of 145,000 +/- 5000. The presence of ATP-sensitive K+ channels (26 pS) has been demonstrated by electrophysiological techniques. Intracellular perfusion of adenohypophysis cells with an ATP-free medium to activate ATP-sensitive K+ channels induces a large hyperpolarization (approximately 30 mV) that is antagonized by an...

  14. ANALISIS PROKSIMAT DAN TOKSISITAS AKUT EKSTRAK DAUN SIRIH MERAH YANG BERPOTENSI SEBAGAI ANTIDIABETES

    Directory of Open Access Journals (Sweden)

    Mega Safithri

    2012-11-01

    Full Text Available ABSTRACTThe aim of this study was to explore the analysis proximate and toxicity of the decoctions of P. crocatum. Fresh leaves of P. crocatum were boiled in water in order to obtain decoction and were examined for its chemical compounds by using SNI 01-2891-1992 method for proximate analysis. Toxicity of decoction extract of P. crocatum was orally fed to rats (Sprague dawley. The results showed that P. crocatum leaves contains 9.27% water, 14.33% ash, 3.96% fat, 22.63% proteins, and 59.08% carbohydrates. Acute toxicity test showed that all rats were still alive after 7 days treatment with P. crocatum decoction for all dose groups (0, 5, 10, and 20 g/kg BB. LC50 value of P. crocatum decoction was 544.82 ppm, meaning that the decoction was relatively harmless and bioactive.Key words: Piper crocatum, proximate analysis, toxicity, antidiabeticABSTRAKPenelitian ini bertujuan menentukan kadar air, abu, protein, lemak, dan karbohidrat dari rebusan daun sirih merah (Piper crocatum serta mempelajari toksisitasnya. Daun segar sirih merah direbus dalam air mendidihuntuk mendapatkan dekokta/rebusan yang akan dianalisis kandungan senyawa kimianya menggunakan metode SNI 01-2891-1992. Uji toksisitas menggunakan tikus putih galur Sprague dawley untuk menentukan LD50nya dan menggunakan larva udang untuk menentukan LC50 nya. Hasil analisis proksimat menunjukkan bahwa daun sirih merah mengandung 9.27% air, 14.33% abu, 3.96% lemak, 22.63 % protein, dan 59.08% karbohidrat.Hasil uji toksisitas menunjukkan bahwa selama 24 jam sampai 7 hari setelah diberikan dekokta, tidak ada tikus yang mati pada semua kelompok dosis (0, 5, 10, maupun 20 g/kg BB. Tidak adanya kematian pada semua dosis yang diujikan dapat dikatakan bahwa dekokta sirih merah tidak toksik. Nilai LC50 untuk air rebusan sirih merah terjadi pada konsentrasi 544.82 ppm. Hal ini menunjukkan bahwa air rebusan sirih merah memiliki potensi bioaktivitas.Kata kunci: Piper crocatum, analisis proksimat, toksisitas

  15. [Effect of autogenic training on glucose regulation and lipid status in non-insulin dependent diabetics].

    Science.gov (United States)

    Kostić, N; Secen, S

    2000-01-01

    The objective of this study was to examine the benefits of autogenic training in patients with type 2 diabetes and 40 diabetics treated with oral antidiabetic agents were assigned to receive autogenic training. Treatment effects on GHb levels, glycemia, lipids and lipid peroxidases were evaluated after 12 weeks. Subjects demonstrated significant improvements of GHb level (8.94 +/- 2.21% vs. 7.9 +/- 2.395) (p autogenic training (1.21 +/- 0.11 vs. 1.36 +/- 1.42) (p training (6.63 +/- 1.66 mmol/l vs. 6.10 +/- 1.12 mmol/l) (p Autogenic training in selected patients, especially those who are most responsive to stress would provide benefits for glucosE control and lipid metabolism that are not always achieved by conventional treatment.

  16. Ecological effects of ionizing radiation and other toxic agents on the aquatic microcosm

    International Nuclear Information System (INIS)

    Fuma, Shoichi; Ishii, Nobuyoshi; Tanaka, Nobuyuki; Takeda, Hiroshi; Miyamoto, Kiriko; Yanagisawa, Kei; Kawabata, Zen'ichiro

    2004-01-01

    The purpose of this study was comparative evaluation of effects of ionizing radiation and other various toxic agents on aquatic microbial communities. For this purpose, the authors investigated effects of γ-rays, ultraviolet (UV) radiation, acidification, aluminum, manganese, nickel, copper and gadolinium on the microcosm, i.e., the experimental model ecosystem consisting of populations of the flagellate alga Euglena gracilis as a producer, the ciliate protozoan Tetrahymena thermophila as a consumer and the bacterium Eseherichia coli as a decomposer. Effects of toxic agents in the microcosm were not only direct effects but also community-level effects due to interactions among the constituting species or between organisms and toxic agents. In general, the degrees of effects observed in the microcosm could be categorized as follows: no effects; recognizable effects, i.e., decrease or increase in the cell densities of at least one species; severe effects, i.e., extinction of one or two species; and destructive effects, i.e., extinction of all species. These results were analyzed by the ecological effect index (EEI), in which differences in the cell densities between exposed and control microcosm were represented by the Euclidean distance function. A 50% effect doses for the microcosm (ED M50 ), at which the EEI became 50%, were evaluated to be 530 Gy for γ-rays, 2100 J m -2 for UV, 4100 μM for manganese, 45 μM for nickel, 110 μM for copper and 250 μM for gadolinium. (author)

  17. Effect of hypolipidemic drugs on basal and stimulated adenylate cyclase activity in tumor cells

    International Nuclear Information System (INIS)

    Bershtein, L.M.; Kovaleva, I.G.; Rozenberg, O.A.

    1986-01-01

    This paper studies adenylate cyclase acticvity in Ehrlich's ascites carcinoma (EAC) cells during administration of drugs with a hypolipidemic action. Seven to eight days before they were killed, male mice ingested the antidiabetic biguanide phenformin, and the phospholipid-containing preparation Essentiale in drinking water. The cAMP formed was isolated by chromatography on Silufol plates after incubation of the enzyme preparation with tritium-ATP, or was determined by the competitive binding method with protein. It is shown that despite the possible differences in the concrete mechanism of action of the hypolipidemic agents chosen for study on the cyclase system, the use of such agents, offers definite prospects for oriented modification of the hormone sensitivity of tumor cells

  18. Nutritional efects of antidiabetic diets on concentartion of tissue antioksidant on rats with induced diabetes mellitus

    Directory of Open Access Journals (Sweden)

    Crceva - Nikolovska Radmila

    2009-05-01

    Full Text Available Oxidative stress is currently suggested to play as a pathogenesis in the development of diabetes mellitus. There are many reports indicating the changes in parameters of oxidative stress in diabetes mellitus. The role of dietary management in diabetes mellitus is to provide a proper balance of total nutrients while meeting the special dietary needs of the patient. Complex carbohydrates and dietary fiber help to delay the absorption of glucose from the intestinal tract and minimize postprandial fluctuation of glucose. The present study was designated to evaluate the effect of special antidiabetic diet treatment upon oxidative stress parameters in the initial stages of the development of diabetes. The findings of the present study suggest that special diet formula useful for prevention of progressive hyperglycaemia in aged provoked diabetes in dogs could not restore the imbalance of cellular defense mechanism provoked by streptozotocin. Soluble fiber in the diet may also prolong gastrointestinal transit time, allow greater water absorption, and promote the production of short chain fatty acids which nourish the intestinal mucosa.

  19. Radiographic scanning agent

    International Nuclear Information System (INIS)

    Bevan, J.A.

    1983-01-01

    This invention relates to radiodiagnostic agents and more particularly to a composition and method for preparing a highly effective technetium-99m-based bone scanning agent. One deficiency of x-ray examination is the inability of that technique to detect skeletal metastases in their incipient stages. It has been discovered that the methanehydroxydiphosphonate bone mineral-seeking agent is unique in that it provides the dual benefits of sharp radiographic imaging and excellent lesion detection when used with technetium-99m. This agent can also be used with technetium-99m for detecting soft tissue calcification in the manner of the inorganic phosphate radiodiagnostic agents

  20. Lapse of time effects on tax evasion in an agent-based econophysics model

    Science.gov (United States)

    Seibold, Götz; Pickhardt, Michael

    2013-05-01

    We investigate an inhomogeneous Ising model in the context of tax evasion dynamics where different types of agents are parameterized via local temperatures and magnetic fields. In particular, we analyze the impact of lapse of time effects (i.e. backauditing) and endogenously determined penalty rates on tax compliance. Both features contribute to a microfoundation of agent-based econophysics models of tax evasion.