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Oral agentes antidiabetes

Sung-Ho Kim, Jung-Hwa Yoo, Woo Je Lee, Cheol-Young Park
Dipeptidyl peptidase-4 (DPP-4) inhibitors are a new class of oral antidiabetic agent for the treatment of type 2 diabetes mellitus. They increase endogenous levels of incretin hormones, which stimulate glucose-dependent insulin secretion, decrease glucagon secretion, and contribute to reducing postprandial hyperglycemia. Although DPP-4 inhibitors have similar benefits, they can be differentiated in terms of their chemical structure, pharmacology, efficacy and safety profiles, and clinical considerations. Gemigliptin (brand name: Zemiglo), developed by LG Life Sciences, is a potent, selective, competitive, and long acting DPP-4 inhibitor...
October 2016: Diabetes & Metabolism Journal
Kaitlin A Doucette, Kelly N Hassell, Debbie C Crans
Improving efficacy and lowering resistance to metal-based drugs can be addressed by consideration of the coordination complex speciation and key reactions important to vanadium antidiabetic drugs or platinum anticancer drugs under biological conditions. The methods of analyses vary depending on the specific metal ion chemistry. The vanadium compounds interconvert readily, whereas the reactions of the platinum compounds are much slower and thus much easier to study. However, the vanadium species are readily differentiated due to vanadium complexes differing in color...
October 3, 2016: Journal of Inorganic Biochemistry
Katsunori Suzuki, Yurie Mitsuma, Takaaki Sato, Takumi Anraku, Mariko Hatta
BACKGROUND: Some patients with type 2 diabetes mellitus (T2DM) on insulin have poor glycemic control and require add-on therapy to reach target glucose values. Increased insulin doses or the addition of an oral antidiabetic drug (OAD) may improve glycemic control, but many patients fail to achieve target values. The aim of this study was to compare the treatment efficacy and safety of three different therapies in such patients. METHODS: T2DM outpatients with poor glycemic control (HbA1c ≥ 7...
November 2016: Journal of Clinical Medicine Research
KhaderSyed Zameer Ahmed, Syed Zameer Ahmed Sidhra, Ponnusamy Ponmurugan, Balasubramanian Senthil Kumar
Solanum trilobatum Linn is a medicinal plants used in India from many centuries to cure various diseases. The purpose of the study is to evaluate the ameliorative potential of the ethanolic leaf extract and fractions of Solanum trilobatum (St) against alloxan induced diabetic rats. Solanum trilobatum leaf extract and fractions were administered orally at two different concentration (100-200mg/kg body weight) to alloxan induced diabetic rats. The antidiabetic efficacy was validated through various biochemical parameters, enzyme assays, renal markers and antioxidant properties were also determined...
September 2016: Pakistan Journal of Pharmaceutical Sciences
Mouna Sghir, Mohamed Guedria, Marwa Maraoui, Wafa Haj Hamad, Wafa Said, Saida Jerbi, Wassia Kessomtini
OBJECTIVE: The femur aplasia is a congenital developmental defect of the femur often associated with malformations of the pelvis and lower limb. There are all intermediaries between the short femur and vestigial femoral. The total femur absence (agenesis) is rare. We report a case of a child followed in our Physical Medicine Department for proximal bilateral femoral agenesis. OBSERVATIONS: This is M.S., a 5 years old child, addressed for a waddling gait and a deformation of the trunk...
September 2016: Annals of Physical and Rehabilitation Medicine
Vanita R Aroda, Julio Rosenstock, Carol Wysham, Jeffrey Unger, Diego Bellido, Guillermo González-Gálvez, Akane Takami, Hailing Guo, Elisabeth Niemoeller, Elisabeth Souhami, Richard M Bergenstal
OBJECTIVE: This study was conducted to demonstrate the efficacy and safety of LixiLan (iGlarLixi), a novel, titratable, fixed-ratio combination of insulin glargine (iGlar) (100 units) and lixisenatide, compared with iGlar in patients with type 2 diabetes inadequately controlled on basal insulin with or without up to two oral glucose-lowering agents. RESEARCH DESIGN AND METHODS: After a 6-week run-in when iGlar was introduced and/or further titrated, and oral antidiabetic drugs other than metformin were stopped, 736 basal insulin-treated patients (mean diabetes duration 12 years, BMI 31 kg/m(2)) were randomized 1:1 to open-label, once-daily iGlarLixi or iGlar, both titrated to fasting plasma glucose <100 mg/dL (<5...
September 20, 2016: Diabetes Care
Ido Laskov, Paul Abou-Nader, Oreekha Amin, Charles-Andre Philip, Marie-Claude Beauchamp, Amber Yasmeen, Walter H Gotlieb
PURPOSE: Epithelial-mesenchymal transition (EMT) is a critical process for cancer metastasis and recurrence. Metformin, an effective oral antidiabetic drug, has been associated with decreased cancer risk and mortality. In this pilot study, we started to evaluate the effect of metformin on EMT in vivo and in vitro in endometrial cancer (EC). METHODS: Endometrial cancer cell lines and freshly isolated EC tumor specimens were used to assess EMT after metformin treatment...
September 2016: International Journal of Gynecological Cancer
Rahul Sarma, Sima Kumari, Ramakrishnan Elancheran, Meetali Deori, Rajlakshmi Devi
Fatty foods, the most common diet today are the crux of many metabolic disorders which need urgent attention. Garcinia pedunculata Roxb. (GP, Clusiaceae) is a plant found available in Northeast (NE) region of India, is considered to have versatile therapeutic properties. The people of this region has been using dried pulp of GP fruit for the treatment of different stomach related diseases traditionally. This study aimed at evaluating the potential therapeutic action of the polyphenol-rich methanolic extract of the fruit in experimental induced obese rats...
2016: Frontiers in Pharmacology
Yousra M El-Far, Mahmoud M Zakaria, Mahmoud M Gabr, Amal M El Gayar, Ibrahim M El-Sherbiny, Laila A Eissa
AIM: This study aimed to develop a new stable nanoformulation of silymarin (SM) with optimum enhanced oral bioavailability and to evaluate its effect as well as mechanism of action as a superior antidiabetic agent over native SM using streptozotocin-induced diabetic rats. MATERIALS AND METHODS: SM-loaded pluronic nanomicelles (SMnp) were prepared and fully characterized. Biochemical parameters were performed as well as histological, confocal and reverse-transcription polymerase chain reaction studies on pancreatic target tissues...
October 2016: Nanomedicine
Sunil Garg, Sajal Srivastava, Kisanpal Singh, Alok Sharma, Kavita Garg
INTRODUCTION: Available data indicated that diabetes mellitus (DM) increases the vulnerability of the gastric ulcers and the need of the hour is to develop effective agents to treat ulcer with diabetes for better patient compliance and cost effectiveness. The ulcer-healing properties of ethanolic extract of Caralluma attenuata (CAEt) against both chemically- and physically induced gastric ulcers in experimental rats are recently studied. AIM: To assess the ulcer healing potential of Ethanolic Extract of Caralluma attenuata on Experimental Diabetic Rats...
April 2016: Ancient Science of Life
Chang-Ik Choi
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...
2016: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
Julie Brown, Tineke J Crawford, Jane Alsweiler, Caroline A Crowther
BACKGROUND: Gestational diabetes mellitus (GDM) is any degree of glucose intolerance that first presents and is recognised during pregnancy and usually resolves after the birth of the baby. GDM is associated with increased short- and long-term morbidity for the mother and her baby. Treatment usually includes lifestyle modification and/or pharmacological therapy (oral antidiabetic agents or insulin) with the aim to maintain treatment targets for blood glucose concentrations. Finding novel treatment agents which are effective, acceptable and safe for the mother and her baby are important...
September 7, 2016: Cochrane Database of Systematic Reviews
Chien-Yi Hsu, Yu-Wen Su, Yung-Tai Chen, Shih-Hung Tsai, Chun-Chin Chang, Szu-Yuan Li, Po-Hsun Huang, Jaw-Wen Chen, Shing-Jong Lin
BACKGROUND: Pleiotropic effects on cardiovascular protection have been suggested in several oral antidiabetic drugs (OAD). The impacts of OADs on aortic aneurysm (AA) growth have been found in animal studies, but the evidence of their beneficial effects for AA protection in human are lacking. We investigated the relationship between OAD therapy and the risk of developing AA. METHODS: We conducted a nested case-control analysis using the database extracted from Taiwan's National Health Insurance Research Database...
2016: Cardiovascular Diabetology
Abhijit A Ghadge, Aniket A Kuvalekar
AIM: As diabetes mellitus is multi-factorial disease, use of several oral hypoglycemic agents (OHAs) is the main stay of pharmacological treatment. The treatment has become more challenging and controversial as OHAs are heterogeneous in their mode of action that causes unwanted side effects. Complementary approaches such as use of medicinal plants and dietary polyunsaturated fatty acids (PUFA) with hypoglycemic and hypolipidemic activities are therefore imperative. A vast literature has independently documented the effects of OHAs, medicinal plants and PUFA for management of diabetes...
August 22, 2016: Diabetes & Metabolic Syndrome
Xiangfei Li, Na Wang, Boxing Yin, Dongsheng Fang, Tian Jiang, Shuguang Fang, Jianxin Zhao, Hao Zhang, Gang Wang, Wei Chen
AIMS: The aim of this study was to rapidly screen potential hypoglycemic strain by α-glucosidase inhibitory activity in vitro, then explored the antidiabetic effect of L. plantarum CCFM0236 in vivo. METHODS AND RESULTS: The cell-free supernatant of L. plantarum CCFM0236 significantly inhibited α-glucosidase activity in vitro. Therefore, the effects of L. plantarum CCFM0236 with potential hypoglycemia activity on insulin resistance and hyperglycemia were explored in high-fat and streptozotocin induced type 2 diabetes mice...
August 23, 2016: Journal of Applied Microbiology
Naznin Ara Khatune, Bytul Mokaddesur Rahman, Ranjan Kumar Barman, Mir Imam Ibne Wahed
BACKGROUND: Inspite of introduction of oral hypoglycemic agents, diabetes and its related complications remains to be a major clinical problem. The aim of this study was to investigate the antidiabetic, antihyperlipidemic and antioxidant activities of Grewia asiatica (Linn) stem bark in alloxan induced diabetic rats. METHODS: Diabetes was induced by a single dose of intraperitoneal injection of alloxan (110 mg/kg) in Norwegian Long Evans rats. Ethanol extract of barks from Grewia asiatica (GAE 200 and 400 mg/kg) and metformin (150 mg/kg) were orally administered once daily for 15 days...
2016: BMC Complementary and Alternative Medicine
Julio Rosenstock, Ronnie Aronson, George Grunberger, Markolf Hanefeld, PierMarco Piatti, Pierre Serusclat, Xi Cheng, Tianyue Zhou, Elisabeth Niemoeller, Elisabeth Souhami, Melanie Davies
OBJECTIVE: To evaluate efficacy and safety of LixiLan (iGlarLixi), a novel titratable fixed-ratio combination of insulin glargine (iGlar) and lixisenatide (Lixi), compared with both components, iGlar and Lixi, given separately in type 2 diabetes inadequately controlled on metformin with or without a second oral glucose-lowering drug. RESEARCH DESIGN AND METHODS: After a 4-week run-in to optimize metformin and stop other oral antidiabetic drugs, participants (N = 1,170, mean diabetes duration ∼8...
August 15, 2016: Diabetes Care
Harith Rajagopalan, Alan D Cherrington, Christopher C Thompson, Lee M Kaplan, Francesco Rubino, Geltrude Mingrone, Pablo Becerra, Patricia Rodriguez, Paulina Vignolo, Jay Caplan, Leonardo Rodriguez, Manoel P Galvao Neto
OBJECTIVE: To assess procedural safety and glycemic indices at 6 months in a first-in-human study of duodenal mucosal resurfacing (DMR), a novel, minimally invasive, upper endoscopic procedure involving hydrothermal ablation of the duodenal mucosa, in patients with type 2 diabetes and HbA1c ≥7.5% (58 mmol/mol) on one or more oral antidiabetic agents. RESEARCH DESIGN AND METHODS: Using novel balloon catheters, DMR was conducted on varying lengths of duodenum in anesthetized patients at a single medical center...
August 12, 2016: Diabetes Care
Jean-Luc Faillie, Oriana H Yu, Hui Yin, Dominique Hillaire-Buys, Alan Barkun, Laurent Azoulay
Importance: The use of dipeptidyl-peptidase-4 (DPP-4) inhibitors and glucagon-like peptide 1 (GLP-1) analogues-a group of drugs used in the management of type 2 diabetes mellitus-may be associated with an increased risk of bile duct and gallbladder disease. To date, no observational study has assessed this possible association. Objective: To determine whether the use of DPP-4 inhibitors and GLP-1 analogues is associated with an increased risk of incident bile duct and gallbladder disease in patients with type 2 diabetes...
October 1, 2016: JAMA Internal Medicine
Lynda Bourebaba, Souaad Saci, Damia Touguit, Lynda Gali, Schahinez Terkmane, Naima Oukil, Fatiha Bedjou
BACKGROUND: Hyoscyamus albus L. (Solanaceae) an old medicinal plant is a rich source of tropane and nortropane alkaloids which confers to this plant a number of very interesting and beneficial therapeutic effects. PURPOSE: Calystegines that are polyhydroxylated alkaloids and imino-sugars poccess significant glycosidases inhibitory activities and are therefore good candidats for the treatment of diabetes mellitus. STUDY DESIGN: Calystegines extracted from Hyoscyamys albus seeds were tested for teir acute oral toxicity and investigated for their in-vivo antidiabetic effect on Streptozotocine induced diabetes in mice...
August 2016: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
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