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Oral Anti-hyperglycemics

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https://www.readbyqxmd.com/read/29027251/new-biguanides-as-anti-diabetic-agents-part-ii-synthesis-and-anti-diabetic-properties-evaluation-of-1-arylamidebiguanide-derivatives-as-agents-of-insulin-resistant-type-ii-diabetes
#1
Wahid M Basyouni, Samir Y Abbas, Mohamed F El Shehry, Khairy A M El-Bayouki, Hanan F Aly, Azza Arafa, Mahmoud S Soliman
New 1-arylamidebiguanide hydrochloride salts were synthesized via reaction of hydrazide derivatives with dicyandiamide in acidic medium. The structure of the obtained derivatives was characterized by spectroscopic and elemental analysis tools. The anti-diabetic properties of the synthesized compounds were determined. Oral treatment of hyperglycemic rats with the synthesized biguanide derivatives showed a significant decrease of the elevated glucose in comparison with the anti-diabetic standard drug, metformin...
October 13, 2017: Archiv der Pharmazie
https://www.readbyqxmd.com/read/28925888/a-self-nanoemulsifying-drug-delivery-system-for-poorly-water-soluble-tolbutamide-development-optimization-and-pharmacodynamic-studies
#2
Deepti Pandita, Neelam Kumari, Viney Lather
The current investigation involves the development of a thermodynamically stable and dilutable self-nanoemulsifying drug delivery system (SNEDDS) for tolbutamide, a poorly water soluble hypoglycemic drug, in order to achieve higher water solubility and enhanced dissolution rate which in turn improves its oral bioavailability. Pseudo-ternary phase diagrams suggested the suitability of oleic acid (lipid), Tween 20 (surfactant) and PEG 400 (co-surfactant) for developing the SNEEDS formulations. The optimal SNEDDS formulation having mean globule diameter, viscosity, polydispersity value of 58...
September 15, 2017: Pharmaceutical Nanotechnology
https://www.readbyqxmd.com/read/28859934/acacia-nilotica-leaf-improves-insulin-resistance-and-hyperglycemia-associated-acute-hepatic-injury-and-nephrotoxicity-by-improving-systemic-antioxidant-status-in-diabetic-mice
#3
Manas Ranjan Saha, Priyankar Dey, Indrani Sarkar, Dilip De Sarker, Biswajit Haldar, Tapas Kumar Chaudhuri, Arnab Sen
ETHNOPHARMACOLOGICAL RELEVANCE: Acacia nilotica (L.) Delile is used as a traditional anti-diabetic remedy in Bangladesh, Pakistan, Egypt, Nigeria and is mentioned in Ayurveda as well. AIM: The objective of the study was to evaluate the ethnomedicinal claim of A. nilotica leaf (ANL) extract for its efficiency in ameliorating diabetic complications. MATERIALS AND METHODS: ANL was orally administrated (50 and 200mg/kg) to alloxanized mice (blood glucose > 200mg/dL) for 20d...
August 30, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/28843149/berberine-chloride-ameliorates-oxidative-stress-inflammation-and-apoptosis-in-the-pancreas-of-streptozotocin-induced-diabetic-rats
#4
Govindasami Chandirasegaran, Chakkaravarthy Elanchezhiyan, Kavisa Ghosh, Subramaniam Sethupathy
Berberine chloride (BC) has been widely used as an unprescribed oral drug in China for the treatment of various diseases, and it is an active ingredient in many traditionally used medicinal plants. The present study was undertaken to evaluate the beneficial effects of BC on oxidative stress, inflammation and apoptosis in the pancreas of Streptozotocin (STZ) induced diabetic rats. Diabetes was induced in the male Wistar albino rats using a single intraperitoneal injection of STZ of 40mg/kg b.w. Diabetic rats were treated with BC (50mg/kg b...
August 23, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28822685/28-homocastasterone-down-regulates-blood-glucose-cholesterol-triglycerides-srebp1c-and-activates-lxr-expression-in-normal-diabetic-male-rat
#5
Velan Athithan, Kotteazeth Srikumar
Plant steroids are being recognized as influential secondary bio factors, assimilating in animal tissues through diet and affecting their cellular metabolic function to varying degree. They modulate catalytic and signaling functions in mammalian cells, affecting cellular homeostasis. The effect of phyto brassinosteroid ketoisoform 28-homocastasterone (28-HC), was assessed for its influence on blood glucose, plasma lipid and selective signal marker levels in normal and diabetic male wistar rat models. A 15 day oral feed regimen employing the experimental rat, noted that circulating blood glucose, cholesterol and triglyceride level in diabetic rat were markedly reduced by this compound...
August 16, 2017: Chemico-biological Interactions
https://www.readbyqxmd.com/read/28770335/erythritol-reduces-small-intestinal-glucose-absorption-increases-muscle-glucose-uptake-improves-glucose-metabolic-enzymes-activities-and-increases-expression-of-glut-4-and-irs-1-in-type-2-diabetic-rats
#6
Chika Ifeanyi Chukwuma, Ramgopal Mopuri, Savania Nagiah, Anil Amichund Chuturgoon, Md Shahidul Islam
PURPOSE: Studies have reported that erythritol, a low or non-glycemic sugar alcohol possesses anti-hyperglycemic and anti-diabetic potentials but the underlying mode of actions is not clear. This study investigated the underlying mode of actions behind the anti-hyperglycemic and anti-diabetic potentials of erythritol using different experimental models (experiment 1, 2 and 3). METHODS: Experiment 1 examined the effects of increasing concentrations (2.5-20%) of erythritol on glucose absorption and uptake in isolated rat jejunum and psoas muscle, respectively...
August 2, 2017: European Journal of Nutrition
https://www.readbyqxmd.com/read/28759757/navel-orange-peel-hydroethanolic-extract-naringin-and-naringenin-have-anti-diabetic-potentials-in-type-2-diabetic-rats
#7
Osama M Ahmed, Mohamed A Hassan, Sanaa M Abdel-Twab, Manal N Abdel Azeem
The therapy of Type 2 Diabetes Mellitus (T2DM) stays a challenging issue. During the last decade, there has been an interest in the expansion of anti-diabetic drugs especially those of natural sources. Thus, the aim of this study was to assess the anti-hyperglycemic and the anti-hyperlipidemic effects as well as the anti-oxidant activities of navel orange hydroethanolic extract and its constituting flavonoids naringin and naringenin on nicotineamide (NA)/streptozotocin (STZ)-induced type 2 diabetic rats. To induce T2DM, 16h-fasted rats were intraperitoneally injected with STZ at dose of 50mg/kg body weight (b...
October 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28738518/teucrium-polium-extract-reverses-symptoms-of-streptozotocin-induced-diabetes-in-rats-via-rebalancing-the-pdx1-and-foxo1-expressions
#8
Parvaneh Sadat Tabatabaie, Razieh Yazdanparast
BACKGROUND AND OBJECTIVE: Teucrium polium Lamiaceae. an antidiabetic traditional medicine was observed to stimulate insulin secretion and β-cell mass restoration in pancreatic of diabetic rats. Bioactive compounds in T. polium such as terpenoids and flavonoids have a wide range of antioxidant properties. Given this background, our research was aimed at probing the effective molecular mechanism of T. polium which in turn protects the pancreatic β-cells of diabetic rats through attenuation of streptozotocin-induced oxidative stress...
September 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28690682/autologous-bone-marrow-derived-mononuclear-cells-transplantation-in-type-2-diabetes-mellitus-effect-on-%C3%AE-cell-function-and-insulin-sensitivity
#9
Shobhit Bhansali, Pinaki Dutta, Mukesh Kumar Yadav, Ashish Jain, Sunder Mudaliar, Meredith Hawkins, Anura V Kurpad, Deepak Pahwa, Ashok Kumar Yadav, Ratti Ram Sharma, Vivekanand Jha, Neelam Marwaha, Shipra Bhansali, Anil Bhansali
BACKGROUND: Insulin resistance and insulin deficiency are the cardinal defects in the pathogenesis of type 2 diabetes mellitus (T2DM). Despite the plethora of anti-diabetic medications, drugs specifically targeting the β-cells are still desired. Stem cell therapy has emerged as a novel therapeutics strategy to target β-cells; however, their mechanism of action has not been well defined. This study aims to examine the efficacy and safety of autologous bone marrow-derived mononuclear cells (ABM-MNCs) transplantation in T2DM, and explores the mechanistic insights into stem cells action through metabolic studies...
2017: Diabetology & Metabolic Syndrome
https://www.readbyqxmd.com/read/28677319/effect-of-the-polyphenol-rich-ethyl-acetate-fraction-from-the-leaves-of-lycium-chinensemill-on-oxidative-stress-dyslipidemia-and-diabetes-mellitus-in-streptozotocin-nicotinamide-induced-diabetic-rats
#10
Opeyemi J Olatunji, Hongxia Chen, Yifeng Zhou
Lycium chinenseMill., popularly known as boxthorn, is a plant that is traditionally used for treating night sweat, cough, inflammation and diabetes mellitus. However, the leaves have received little or no attention despite their potentials as a potent therapeutic agent. This study was aimed at investigating the hypoglycemic and hypolipidemic effects of the polyphenols-rich ethyl acetate fraction from the leaves of Lycium chinenseMill. on streptozotocin-nicotinamide induced diabetic rats. The ethyl acetate fraction (LFE) was selected and orally gavaged at 100, 200, and 400 mg/kg dose to streptozotocin (STZ)-nicotinamide induced diabetic rats...
July 4, 2017: Chemistry & Biodiversity
https://www.readbyqxmd.com/read/28669771/antidiabetic-antioxidant-and-anti-inflammatory-properties-of-water-and-n-butanol-soluble-extracts-from-saharian-anvillea-radiata-in-high-fat-diet-fed-mice
#11
Chouaib Kandouli, Mathieu Cassien, Anne Mercier, Caroline Delehedde, Emilie Ricquebourg, Pierre Stocker, Mourad Mekaouche, Zineb Leulmi, Aicha Mechakra, Sophie Thétiot-Laurent, Marcel Culcasi, Sylvia Pietri
ETHNOPHARMACOLOGICAL RELEVANCE: 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. AIM OF THE STUDY: 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...
July 31, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/28651259/new-biguanides-as-anti-diabetic-agents-part-i-synthesis-and-evaluation-of-1-substituted-biguanide-derivatives-as-anti-diabetic-agents-of-type-ii-diabetes-insulin-resistant
#12
Samir Y Abbas, Wahid M Basyouni, Khairy A M El-Bayouk, Wael M Tohamy, Hanan F Aly, Azza Arafa, Mahmoud S Soliman
New 1-substituted-biguanide hydrochloride salts were synthesized via reacting benzo[1,3-d]dioxol-5-amine, phenylhydrazine, N,N-dimethylhydrazinecarboxamide, benzohydrazide and 2-phenyl acetohydrazide with dicyandiamide in acidic medium. Structures of the obtained biguanide salts were characterized by spectroscopic tools. The synthesized compounds were screened for their anti-diabetic activity with standard metformin drug. Oral treatment of hyperglycemic rats with the synthesized biguanide derivatives significantly decreased the elevated blood glucose level...
October 2017: Drug Research
https://www.readbyqxmd.com/read/28650327/anti-hyperglycemic-potential-of-lactobacillus-spp-in-alloxan-induced-wistar-rats
#13
Vandana Bharti, Archana Mehta, Gajendra Kumar Mourya, Laxmi Ahirwal, Vivek K Bajpai, Shruti Shukla
This research was aimed to investigate anti-hyperglycemic effects of two Lactobacillus spp. on alloxan induced diabetic rats. Alloxan was administered intraperitoneally to induce the diabetic conditions in experimental rats. Animals were treated with oral administration of Lactobacillus spp., such as L. plantarum and L. acidophilus at the dose of 10(8) CFU/ml. As a result, administration of Lactobacillus spp. significantly (P<0.05) lowered blood glucose levels in diabetic rats by (201-220mg/dl) as compared to diabetic control (265mg/dl)...
March 2017: Pakistan Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28629341/protective-effects-of-cynara-scolymus-leaves-extract-on-metabolic-disorders-and-oxidative-stress-in-alloxan-diabetic-rats
#14
Maryem Ben Salem, Rihab Ben Abdallah Kolsi, Raouia Dhouibi, Kamilia Ksouda, Slim Charfi, Mahdi Yaich, Serria Hammami, Zouheir Sahnoun, Khaled Mounir Zeghal, Kamel Jamoussi, Hanen Affes
BACKGROUND: Diabetes mellitus (DM) is associated with hyperglycemia, inflammatory disorders and abnormal lipid profiles, currently the extracts from leaves of cynara scolymus has been discovered to treat metabolic disorders and has been stated by multitudinous scientists according to a good source of polyphenols compounds. The present study aimed to evaluate the protective effect of the ethanol leaves extract of C. scolymus in alloxan induced stress oxidant, hepatic-kidney dysfunction and histological changes in liver, kidney and pancreas of different experimental groups of rats...
June 19, 2017: BMC Complementary and Alternative Medicine
https://www.readbyqxmd.com/read/28598027/a-novel-gip-analog-zp4165-enhances-glp-1-induced-body-weight-loss-and-improves-glycemic-control-in-rodents
#15
P K Nørregaard, M A Deryabina, P Tofteng Shelton, J U Fog, J R Daugaard, P Eriksson, L F Larsen, L Jessen
AIM: To investigate the effects of the novel GIP analog, ZP4165, on body weight and glycemic control in rodents. Additionally, to investigate if ZP4165 modulates the anti-obesity and anti-hyperglycemic effects of a GLP-1 agonist (liraglutide). METHODS: The acute insulinotropic effect of ZP4165 was investigated in rats during an oral glucose tolerance test. Long-term effects of ZP4165 on body weight and glycemic control, either alone or in combination with liraglutide, were assessed in diet-induced obese mice and diabetic db/db mice...
June 9, 2017: Diabetes, Obesity & Metabolism
https://www.readbyqxmd.com/read/28575547/implications-for-drug-characterization-in-glucose-tolerance-tests-without-insulin-simulation-study-of-power-and-predictions-using-model-based-analysis
#16
S M Sheikh Ghadzi, M O Karlsson, M C Kjellsson
In antihyperglycemic drug development, drug effects are usually characterized using glucose provocations. Analyzing provocation data using pharmacometrics has shown powerful, enabling small studies. In preclinical drug development, high power is attractive due to the experiment sizes; however, insulin is not always available, which potentially impacts power and predictive performance. This simulation study was performed to investigate the implications of performing model-based drug characterization without insulin...
June 2, 2017: CPT: Pharmacometrics & Systems Pharmacology
https://www.readbyqxmd.com/read/28513455/glucose-tolerance-disorders-during-treatment-with-glucocorticoids-in-patients-with-inflammatory-diseases-of-the-musculoskeletal-system-based-on-the-analysis-of-data-from-the-literature-and-own-research-results
#17
Piotr Dąbrowski, Maria Majdan
Glucocorticoids are among the most frequently used anti-inflammatory and immunosuppressive drugs. They are widely used in the treatment of numerous autoimmune disorders. However, the treatment with glucocorticoids is connected with the risk of a number of side effects. Among them, glucose tolerance disorders play an important role. The results of meta-analyses show that the risk of diabetes is from 1.4 to 2.5 times higher in the case of treated patients in comparison to the general population. Glucocorticoids can directly impair pancreatic β-cell secretion...
May 4, 2017: Postȩpy Higieny i Medycyny Doświadczalnej
https://www.readbyqxmd.com/read/28457895/an-approach-for-half-life-extension-and-activity-preservation-of-an-anti-diabetic-peptide-drug-based-on-genetic-fusion-with-an-albumin-binding-aptide
#18
Daejin Kim, Hyungsu Jeon, Sukyung Ahn, Won Il Choi, Sunghyun Kim, Sangyong Jon
Although the peptide, exenatide, has been widely used as a drug for the treatment of type 2 diabetes, its short plasma half-life requires frequent subcutaneous injection, resulting in poor patient compliance in addition to side effects such as infection at the sites of injection. Here, we report a novel long-acting fusion peptide comprising exenatide and a human serum albumin (HSA)-binding aptide. A phage display screen of a library of aptides, yielded an HSA-specific aptide (APTHSA) that bound HSA with a Kd of 188nM...
June 28, 2017: Journal of Controlled Release: Official Journal of the Controlled Release Society
https://www.readbyqxmd.com/read/28452143/zy15557-a-novel-long-acting-inhibitor-of-dipeptidyl-peptidase-4-for-the-treatment-of-type-2-diabetes-mellitus
#19
Mukul R Jain, Amit A Joharapurkar, Samadhan G Kshirsagar, Vishal J Patel, Rajesh H Bahekar, Harilal V Patel, Pradip A Jadav, Pankaj R Patel, Ranjit C Desai
BACKGROUND AND PURPOSE: Dipeptidyl peptidase (DPP)-4 inhibitors increase levels of glucagon-like peptide-1 (GLP-1) and provide clinical benefit in the treatment of type 2 diabetes mellitus. As longer acting inhibitors have therapeutic advantages, we developed a novel DPP-4 inhibitor, ZY15557, that has a sustained action and long half-life. EXPERIMENTAL APPROACH: We studied the potency, selectivity, efficacy and duration of action of ZY15557, in vitro, with assays of DPP-4 activity...
July 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28390958/discovery-of-liver-directed-glucokinase-activator-having-anti-hyperglycemic-effect-without-hypoglycemia
#20
Anil M Deshpande, Debnath Bhuniya, Siddhartha De, Bhavesh Dave, Vinod P Vyavahare, Santosh H Kurhade, Sachin R Kandalkar, Keshav P Naik, Balasaheb S Kobal, Rahul D Kaduskar, Sujay Basu, Vaibhav Jain, Pratima Patil, Sandhya Chaturvedi Joshi, Ganesh Bhat, Amol A Raje, Satyanarayana Reddy, Jayasagar Gundu, Vamsi Madgula, Suhas Tambe, Prasad Shitole, Dhananjay Umrani, Anita Chugh, Venkata P Palle, Kasim A Mookhtiar
Glucokinase activators (GKAs) are among the emerging drug candidates for the treatment of type 2 diabetes (T2D). Despite effective blood glucose lowering in clinical trials, many pan-GKAs "acting both in pancreas and liver" have been discontinued from clinical development mainly because of their potential to cause hypoglycemia. Pan-GKAs over sensitize pancreatic GK, resulting in insulin secretion even at sub-normoglycemic level which might be a possible explanation for hypoglycemia. An alternative approach to minimize the risk of hypoglycemia is to use liver-directed GKAs, which are reported to be advancing well in clinical development...
June 16, 2017: European Journal of Medicinal Chemistry
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