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Oral Anti-hyperglycemics

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https://www.readbyqxmd.com/read/28629341/protective-effects-of-cynara-scolymus-leaves-extract-on-metabolic-disorders-and-oxidative-stress-in-alloxan-diabetic-rats
#1
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
#2
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
#3
Siti M Sheikh Ghadzi, Mats O Karlsson, Maria C Kjellsson
In anti-hyperglycemic drug development, drug effects are usually characterized using glucose provocations. Analyzing provocation data using pharmacometrics has been shown powerful, enabling small studies. In pre-clinical 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
#4
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
#5
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
#6
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
#7
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...
March 24, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28330423/geraniol-a-natural-monoterpene-ameliorates-hyperglycemia-by-attenuating-the-key-enzymes-of-carbohydrate-metabolism-in-streptozotocin-induced-diabetic-rats
#8
Sukumar Babukumar, Veerasamy Vinothkumar, Chandrasekaran Sankaranarayanan, Subramani Srinivasan
CONTEXT: Geraniol, an acyclic monoterpene alcohol is found in medicinal plants, is used traditionally for several medical purposes including diabetes. OBJECTIVES: The present study evaluates the antihyperglycemic potential of geraniol on key enzymes of carbohydrate metabolism in streptozotocin (STZ)-induced diabetic rats. MATERIALS AND METHODS: Diabetes was induced in experimental rats, by a single intraperitoneal (i.p) injection of STZ [40 mg/kg body weight (b...
December 2017: Pharmaceutical Biology
https://www.readbyqxmd.com/read/28306534/ameliorative-potential-of-blighia-sapida-k-d-koenig-bark-against-pancreatic-%C3%AE-cell-dysfunction-in-alloxan-induced-diabetic-rats
#9
Oluwafemi Adeleke Ojo, Basiru Olaitan Ajiboye, Adebola Busola Ojo, Babatunji Emmanuel Oyinloye, Oluwatosin Debbie Imiere, Oluwatosin Adeyonu
Background In West Africa, the fruit, seed, leaf and stem of Blighia sapida K.D. Koenig are commonly used as remedy against a variety of diseases, including diabetes mellitus. This study investigated the ameliorative potential of B. sapida K.D. Koenig stem bark ethanol extract against pancreatic β-cell dysfunction in diabetic rats. Methods Diabetes was induced by intraperitoneal injection of alloxan (65 mg/kg body weight) for 21 days, and orally administered with glibenclamide (5 mg/kg body weight), 50-150 mg/kg body weight of B...
March 17, 2017: Journal of Complementary & Integrative Medicine
https://www.readbyqxmd.com/read/28282223/analytical-methods-for-metformin-estimation
#10
Durgawati Patel, Puspendra Kumar, Swapnil Sharma, Jaya Dwivedi
Metformin is a widely prescribed oral anti-hyperglycemic agent used in the management of non-insulin dependent diabetes mellitus (NIDDM) or type II diabetes. This article accentuates various analytical methods viz. HPLC, HPTLC, spectrophotometric, electrochemical, capillary electrophoresis and LC-MS for the estimation of metformin in pharmaceutical formulations and in biological matrices.
March 10, 2017: Critical Reviews in Analytical Chemistry
https://www.readbyqxmd.com/read/28261096/antioxidant-activities-metabolic-profiling-proximate-analysis-mineral-nutrient-composition-of-salvadora-persica-fruit-unravel-a-potential-functional-food-and-a-natural-source-of-pharmaceuticals
#11
Asha Kumari, Asish K Parida, Jaykumar Rangani, Ashok Panda
Salvadora persica is a medicinally important plant mainly used in oral hygiene. However, little attention has been given towards the nutritional prominence of this plant. This study encloses the proximate and mineral nutrient contents, amino acid composition, metabolite profiling and antioxidant potential of S. persica fruit. The ripen fruit contained substantial amount of sugars, mineral nutrients, carotenoids, polyphenols and flavonoids. The metabolic profiling of the fruit extract by GC-MS revealed a total of 22 metabolites comprising of sugars, sugar alcohols, organic acids, organic base, and aromatic silica compound...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/28258533/current-therapeutic-approaches-in-the-management-of-hyperglycemia-in-chronic-renal-disease
#12
REVIEW
Vishnu Garla, Licy Yanes-Cardozo, Lillian F Lien
Diabetes mellitus (DM) and chronic kidney disease (CKD) are intricately intertwined. DM is the most common cause of CKD. Adequate control of DM is necessary for prevention of progression of CKD, while careful management of the metabolic abnormalities in CKD will assist in achieving better control of DM. Two of the key organs involved in glucose production are the kidney and the liver. Furthermore, the kidney also plays a role in glucose filtration and reabsorption. In CKD, monitoring of glycemic control using traditional methods such as Hemoglobin A1c (Hba1c) must be done with caution secondary to associated hematological abnormalities in CKD...
March 2017: Reviews in Endocrine & Metabolic Disorders
https://www.readbyqxmd.com/read/28250659/antidiabetic-effects-of-aqueous-and-dichloromethane-methanol-stem-bark-extracts-of-pterocarpus-soyauxii-taub-papilionaceae-on-streptozotocin-induced-diabetic-rats
#13
Marie Claire Tchamadeu, Paul Désiré Djomeni Dzeufiet, Nelly Blaes, Jean-Pierre Girolami, Pierre Kamtchouing, Théophile Dimo
AIM OF THE STUDY: The aim is to evaluate the hypoglycemic and antidiabetic effects of aqueous and CH2Cl2/CH3OH stem bark extracts of Pterocarpus soyauxii Taub in normal and diabetic rats. MATERIALS AND METHODS: Streptozotocin (STZ)-induced diabetic and normal adult Wistar rats were orally administered with aqueous and CH2Cl2/CH3OH plant extracts of P. soyauxii at various doses (38-300 mg/kg) in a single administration. In addition, STZ-induced diabetic rats received prolonged daily administration for 14 days...
January 2017: Pharmacognosy Research
https://www.readbyqxmd.com/read/28238911/anti-hyperglycemic-activity-of-polysaccharides-from-calyx-of-physalis-alkekengi-var-franchetii-makino-on-alloxan-induced-mice
#14
Yu Guo, Sujuan Li, Jianxin Li, Zhiyuan Ren, Feng Chen, Xiaowen Wang
The present study was undertaken to investigate the hypoglycemic effect of polysaccharides (PPSC) isolated from calyx of Physalis alkekengi var. franchetii Makino in alloxan-induced diabetic mice. Seven polysaccharide fractions were obtained through a DEAE-52 column and Sephadex G-100 gel column and they were the main composes of PPSC. The PPSC treatment could prevent the loss of body weight in diabetic mice and result in a decrease of fasting blood glucose (FBG) and glycated serum protein (GSP) and an increase of fasting serum insulin in a dose-dependent manner...
June 2017: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/28216594/anti-hyperglycemic-activity-of-major-compounds-from-calea-ternifolia
#15
Sonia Escandón-Rivera, Araceli Pérez-Vásquez, Andrés Navarrete, Mariana Hernández, Edelmira Linares, Robert Bye, Rachel Mata
Demethylisoencecalin (1) and caleins A (4) and C (5) (3.16-31.6 mg/kg, p.o.), the major components from an infusion of Calea ternifolia controlled postprandial glucose levels during an oral sucrose tolerance test (OSTT, 3 g/kg) in normal and nicotinamide/streptozotocin (NA/STZ, 40/100 mg/kg) hyperglicemic mice. The effects were comparable to those of acarbose (5 mg/kg). During the isolation of 1, 4, and 5, four additional metabolites not previously reported for the plant, were obtained, namely 6-acetyl-5-hydroxy-2-methyl-2-hydroxymethyl-2H-chromene (3), herniarin (6), scoparone (7), and 4',7-dimethylapigenin (8)...
February 14, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28182659/metformin-exhibits-preventive-and-therapeutic-efficacy-against-experimental-cystic-echinococcosis
#16
Julia A Loos, Valeria A Dávila, Christian R Rodrígues, Romina Petrigh, Jorge A Zoppi, Fernando A Crocenzi, Andrea C Cumino
Metformin (Met) is an anti-hyperglycemic and potential anti-cancer agent which may exert its anti-proliferative effects via the induction of energetic stress. In this study we investigated the in vitro and in vivo efficacy of Met against the larval stage of Echinococcus granulosus. Metformin showed significant dose- and time-dependent killing effects on in vitro cultured protoscoleces and metacestodes. Notably, the combination of Met together with the minimum effective concentration of ABZSO had a synergistic effect after days 3 and 12 on metacestodes and protoscoleces, respectively...
February 2017: PLoS Neglected Tropical Diseases
https://www.readbyqxmd.com/read/28160554/pharmacogenetics-of-dipeptidyl-peptidase-4-inhibitors-in-a-taiwanese-population-with-type-2-diabetes
#17
Wen-Ling Liao, Wen-Jane Lee, Ching-Chu Chen, Chieh Hsiang Lu, Chien-Hsiun Chen, Yi-Chun Chou, I-Te Lee, Wayne H-H Sheu, Jer-Yuarn Wu, Chi-Fan Yang, Chung-Hsing Wang, Fuu-Jen Tsai
Dipeptidyl peptidase-4 (DPP-4) inhibitors are oral anti-hyperglycemic drugs enabling effective glycemic control in type 2 diabetes (T2D). Despite DPP-4 inhibitors' advantages, the patients' therapeutic response varies. In this retrospective cohort study, 171 Taiwanese patients with T2D were classified as sensitive or resistant to treatment based on the mean change in HbA1c levels. Using an assumption-free genome-wide association study, 45 single nucleotide polymorphisms (SNPs) involved in the therapeutic response to DPP-4 inhibitors (P < 1 × 10-4) were identified at or near PRKD1, CNTN3, ASK, and LOC10537792...
March 14, 2017: Oncotarget
https://www.readbyqxmd.com/read/28103701/metformin-prevents-the-progression-of-dysplastic-mucosa-of-the-head-and-neck-to-carcinoma-in-nondiabetic-patients
#18
Michael Zvi Lerner, Niv Mor, Hyung Paek, Andrew Blitzer, Marshall Strome
OBJECTIVE: Metformin is an oral anti-hyperglycemic agent used to treat type 2 diabetes mellitus (DM). In vitro and animal models have shown that metformin can prevent the progression of oral lesions to carcinoma; however, there is conflicting data in the clinical literature regarding risk reduction for malignancy in head and neck cancer (HNC). STUDY DESIGN: Case series. METHODS: We present 3 cases in which adjuvant metformin therapy was used to treat recurrent and multifocal dysplastic lesions in previously treated nondiabetic HNC patients...
April 2017: Annals of Otology, Rhinology, and Laryngology
https://www.readbyqxmd.com/read/28017669/depression-can-be-prevented-by-astaxanthin-through-inhibition-of-hippocampal-inflammation-in-diabetic-mice
#19
Xiao-Yan Zhou, Fang Zhang, Xiao-Tong Hu, Jing Chen, Ren-Xian Tang, Kui-Yang Zheng, Yuan-Jian Song
The critical factor considered in a depression induced by diabetes is the inflammation eliciting hippocampal, amygdala and thalamic neuronal injury. Therefore, inhibiting inflammatory reactions in the brain and reducing neuronal injury can alleviate depression in rodents suffering from diabetes mellitus. The oral administration of astaxanthin has been employed in emotional disorders and diabetic complications due to its anti-depressant, anti-inflammatory and anti-apoptotic functions. However, it has not been reported whether astaxanthin can improve diabetes-related depression-like behavior, and its potential mechanisms have not been elucidated...
December 22, 2016: Brain Research
https://www.readbyqxmd.com/read/28006991/efficacy-of-autologous-bone-marrow-derived-mesenchymal-stem-cell-and-mononuclear-cell-transplantation-in-type-2-diabetes-mellitus-a-randomized-placebo-controlled-comparative-study
#20
Shobhit Bhansali, Pinaki Dutta, Vinod Kumar, Mukesh Kumar Yadav, Ashish Jain, Sunder Mudaliar, Shipra Bhansali, Ratti Ram Sharma, Vivekanand Jha, Neelam Marwaha, Niranjan Khandelwal, Anand Srinivasan, Naresh Sachdeva, Meredith Hawkins, Anil Bhansali
Drugs targeting β-cells have provided new options in the management of T2DM; however, their role in β-cell regeneration remains elusive. The recent emergence of cell-based therapies such as autologous bone marrow-derived mesenchymal stem cells (ABM-MSCs) and mononuclear cells (ABM-MNCs) seems to offer a pragmatic approach to augment β-cell function/mass. This study aims to examine the efficacy and safety of ABM-MSC and ABM-MNC transplantation in T2DM and explores alterations in glucose-insulin homeostasis by metabolic studies...
April 1, 2017: Stem Cells and Development
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