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Tadashi Arao, Yosuke Okada, Keiichi Torimoto, Kei Sugai, Takashi Otsuka, Akira Kurozumi, Yoshiya Tanaka
We analyzed the effects of 100 mg/day sitagliptin and a switch to mitiglinide calcium hydrate/voglibose compound tablets (MIT/VOG) in patients with type 2 diabetes mellitus (T2DM) treated with 50 mg/day sitagliptin. Five patients with T2DM treated with 50 mg/day sitagliptin and hemoglobin A1c (HbA1c) of ≥6.5% were switched to MIT/VOG, or the dose of sitagliptin was increased to 100 mg/day. The effects of the changes in therapy were compared in a crossover fashion by continuous glucose monitoring. The primary endpoint was mean amplitude of glycemic excursions (MAGE), and the secondary end points were 24-hour mean blood glucose level and mean blood glucose level from 0:00 a...
2017: Journal of UOEH
Noriko Ihana-Sugiyama, Ritsuko Yamamoto-Honda, Takehiro Sugiyama, Tetsuro Tsujimoto, Masafumi Kakei, Mitsuhiko Noda
BACKGROUND Although the efficacy of combination therapy consisting of basal insulin and oral hypoglycemic agents (OHAs) has been shown, which OHAs are the most efficient remains unclear. MATERIAL AND METHODS Five patients with type 2 diabetes were enrolled and treated with insulin degludec and metformin as a basal therapy. The patients were randomized in a cross-over fashion to receive a combination of mitiglinide (10 mg) and voglibose (0.2 mg) (M+V) 3 times daily or linagliptin (5 mg) (L) once daily for 8 weeks...
February 28, 2017: Medical Science Monitor Basic Research
Bum-Ho Bin, Sung Tae Kim, Jinhyuk Bhin, Kyounghee Byoun, Tae Ryong Lee, Eun-Gyung Cho
Melanocytes play an important role in maintaining epidermal homeostasis by producing melanin and protecting the skin from harmful environmental factors. However, excessive up- or down-regulation of melanin production often causes hyper- or hypo-pigmented disorders, respectively, which affect the patient's quality of life. Therefore, various strategies for modulating melanin levels have been developed by the pharmaceutical and cosmetic industries. We reported previously that voglibose, which is a well-known anti-hyperglycemic agent, could be used as an anti-melanogenic agent by inhibiting α-glucosidase activity and reducing tyrosinase protein levels...
April 2017: Archives of Dermatological Research
Ranjeet Prasad Dash, R Jayachandra Babu, Nuggehally R Srinivas
1. Amidst the new strategies being developed for the management of type 2 diabetes mellitus (T2DM) with both established and newer therapies, alpha glucosidase inhibitors (AGIs) have found a place in several treatment protocols. 2. The objectives of the review were: (a) to compile and evaluate the various clinical pharmacokinetic drug interaction data for AGIs such as acarbose, miglitol and voglibose; (b) provide perspectives on the drug interaction data since it encompasses coadministered drugs in several key areas of comorbidity with T2DM...
January 19, 2017: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
Seok Joon Shin, Sungjin Chung, Soo Jung Kim, Eun-Mi Lee, Young-Hye Yoo, Ji-Won Kim, Yu-Bae Ahn, Eun-Sook Kim, Sung-Dae Moon, Myung-Jun Kim, Seung-Hyun Ko
BACKGROUND: Renal renin-angiotensin system (RAS) activation is one of the important pathogenic mechanisms in the development of diabetic nephropathy in type 2 diabetes. The aim of this study was to investigate the effects of a sodium-glucose co-transporter 2 (SGLT-2) inhibitor, dapagliflozin, on renal RAS in an animal model with type 2 diabetes. METHODS: Dapagliflozin (1.0 mg/kg, OL-DA) or voglibose (0.6 mg/kg, OL-VO, diabetic control) (n = 10 each) was administered to Otsuka Long-Evans Tokushima Fatty (OLETF) rats for 12 weeks...
2016: PloS One
Yoshio Fujitani, Shimpei Fujimoto, Kiyohito Takahashi, Hiroaki Satoh, Takahisa Hirose, Toru Hiyoshi, Masumi Ai, Yosuke Okada, Masahiko Gosho, Tomoya Mita, Hirotaka Watada
AIMS: To compare the efficacy on glycemic parameters between a 12-week administration of once-daily linagliptin and thrice-daily voglibose in Japanese patients with type 2 diabetes. METHODS: In a multi-center, randomized, parallel-group study, 382 patients with diabetes were randomized to the linagliptin group (n=192) or the voglibose group (n=190). A meal tolerance test was performed at weeks 0 and 12. Primary outcomes were the change from baseline to week 12 in serum glucose levels at 2h during the meal tolerance test, HbA1c levels, and serum fasting glucose levels, which were compared between the 2 groups...
November 2016: Diabetes Research and Clinical Practice
C H Shi, L Wang, R Bai, Y B Wang, D Liu, X Y Zhang, H Wang, Y Yang, J L Du
OBJECTIVE: To compare the therapeutic effects between sitagliptin and voglibose both with sensor-augmented insulin pump (SAP) in newly diagnosed type 2 diabetes mellitus (T2DM). METHODS: Fifty-six newly diagnosed hospitalized T2DM patients in Department of Endocrinology of the First Affiliated Hospital of Dalian Medical University, with hemoglobin A1c (HbA1c) value of 9%-11%, were randomized into the sitagliptin (S) group (n=28) and the voglibose (V) group (n=28) by block randomisation...
August 23, 2016: Zhonghua Yi Xue za Zhi [Chinese medical journal]
Katsuhito Mori, Masanori Emoto, Tetsuo Shoji, Masaaki Inaba
OBJECTIVE: Focusing on efficacy and tolerability, we compared linagliptin monotherapy with voglibose monotherapy in patients with type 2 diabetes undergoing hemodialysis (HD). RESEARCH DESIGN AND METHODS: In this multicenter, randomized, open-label, parallel-group, active-controlled study, 78 patients were randomized (1:1) to receive a 12-week treatment with 5 mg linagliptin once daily or 0.2 mg voglibose three times a day. To assess whether linagliptin was superior to voglibose, the primary efficacy end point was the change in glycated hemoglobin (HbA1c) level between baseline and week 12...
2016: BMJ Open Diabetes Research & Care
Takashi Tomita, Hidekazu Goto, Kenji Sumiya, Tadashi Yoshida, Katsuya Tanaka, Yukinao Kohda
The aim of this study was to examine the effects of food thickeners on the pharmacodynamics of voglibose, an α-glucosidase inhibitor. The pharmacodynamics of voglibose were examined in an open-label study in 9 healthy participants after the ingestion of a single oral dose of a voglibose oral-disintegrating tablet, with and without food thickener immersion. The area under the incremental blood sugar concentration-time curve was larger and the rate of increments in the blood sugar concentration was higher with the voglibose oral-disintegrating tablets immersed in the food thickener than with the tablets that were not immersed...
2016: Yakugaku Zasshi: Journal of the Pharmaceutical Society of Japan
Hyun Ju Do, Youn Sue Lee, Min Jin Ha, Yoonsu Cho, Hana Yi, Yu-Jin Hwang, Geum-Sook Hwang, Min-Jeong Shin
This study was designed with the goal of examining the effects of voglibose administration on body weight and lipid metabolism and underlying mechanism high fat diet-induced obese mice. Male C57BL/6 mice were randomly assigned to one of four groups: a control diet (CTL), high-fat diet (HF), high-fat diet supplemented with voglibose (VO), and high fat diet pair-fed group (PF). After 12 weeks, the following characteristics were investigated: serum lipid and glucose levels, serum polar metabolite profiles, and expression levels of genes involved in lipid and bile acid metabolism...
August 31, 2016: Endocrine Journal
Genzoh Tanabe, Weijia Xie, Gorre Balakishan, Mumen F A Amer, Nozomi Tsutsui, Haruka Takemura, Shinya Nakamura, Junji Akaki, Kiyofumi Ninomiya, Toshio Morikawa, Isao Nakanishi, Osamu Muraoka
Using an in silico method, seven analogs bearing hydrophobic substituents (8a: Me, 8b: Et, 8c: n-Pent, 8d: n-Hept, 8e: n-Tridec, 8f: isoBu and 8g: neoPent) at the 3'-O-position in salacinol (1), a highly potent natural α-glucosidase inhibitor from Ayurvedic traditional medicine 'Salacia', were designed and synthesized. In order to verify the computational SAR assessments, their α-glucosidase inhibitory activities were evaluated in vitro. All analogs (8a-8g) exhibited an equal or considerably higher level of inhibitory activity against rat small intestinal α-glucosidases compared with the original sulfonate (1), and were as potent as or higher in potency than the clinically used anti-diabetics, voglibose, acarbose or miglitol...
August 15, 2016: Bioorganic & Medicinal Chemistry
Rebecca Coleman, Sharon W Lemire, William Bragg, Alaine Garrett, Geovannie Ojeda-Torres, Elizabeth Hamelin, Rudolph C Johnson, Jerry Thomas
Tetrodotoxin (TTX) is an extremely potent paralytic toxin responsible for yearly illness and death around the world. A clinical measurement is necessary to confirm exposure because symptoms of TTX intoxication cannot be distinguished from other paralytic toxins. Our group has developed an online solid phase extraction hydrophilic interaction liquid chromatography (HILIC) method for the analysis of TTX in human urine with tandem mass spectrometry. The reportable range for the method was 2.80 - 249 ng/mL in urine with precision and accuracy within 15% as determined for all quality control samples...
September 1, 2016: Toxicon: Official Journal of the International Society on Toxinology
Yasuhiko Matsumoto, Masaki Ishii, Kazuhisa Sekimizu
Sucrose is a major sweetener added to various foods and beverages. Excessive intake of sucrose leads to increases in blood glucose levels, which can result in the development and exacerbation of lifestyle-related diseases such as obesity and diabetes. In this study, we established an in vivo evaluation system using silkworms to explore substances that suppress the increase in blood glucose levels caused by dietary intake of sucrose. Silkworm hemolymph glucose levels rapidly increased after intake of a sucrose-containing diet...
2016: Scientific Reports
Wisuttaya Worawalai, Pornthep Sompornpisut, Sumrit Wacharasindhu, Preecha Phuwapraisirisan
Voglibose, an N-1,3-dihydroxypropylaminocyclitol, has widely been used as an effective α-glucosidase inhibitor for diabetes therapy. Several attempts have been made to synthesize closely related analogues through the coupling of various aminocyclitols and propane-1,3-diol; however, most of them showed weaker or no inhibition. In this communication, we synthesized a pair of new N-1,3-dihydroxypropylaminocyclitols (10 and 11) using (+)-proto-quercitol (1) as a cyclitol core structure. The newly synthesized compounds revealed potent rat intestinal α-glucosidases, particularly against maltase, with IC50 values at submicromolar...
June 24, 2016: Carbohydrate Research
Yukiko Matsushima, Yumie Takeshita, Yuki Kita, Toshiki Otoda, Ken-Ichiro Kato, Hitomi Toyama-Wakakuri, Hiroshi Akahori, Akiko Shimizu, Erika Hamaguchi, Yasuyuki Nishimura, Takehiro Kanamori, Shuichi Kaneko, Toshinari Takamura
PURPOSE: A step-up strategy for diet therapy and/or single oral antihyperglycemic agent (OHA) regimens has not yet been established. The aim of this study was to evaluate hemoglobin A1c (HbA1c) as a primary end point, and the pleiotropic effects on metabolic and cardiovascular parameters as secondary end points, of sitagliptin versus voglibose in patients with type 2 diabetes with inadequate glycemic control while on diet therapy and/or treatment with a single OHA. METHODS: In this multicenter, randomized, open-label, parallel-group trial, a total of 260 patients with inadequately controlled type 2 diabetes (HbA1c levels >6...
2016: BMJ Open Diabetes Research & Care
Kunihiro Suzuki, Daisuke Katsura, Masaaki Sagara, Chie Aoki, Mai Nishida, Yoshimasa Aso
We encountered a 62-year-old woman who experienced frequent episodes of hypoglycemia. She was diagnosed with postprandial reactive hypoglycemia according to the results of oral glucose and sucrose tolerance tests, having undergone an endocrinological examination and image inspection. The administration of low-dose voglibose, an alpha-glucosidase inhibitor (α-GI), improved the glucose fluctuations and inhibited hypoglycemic symptoms. Voglibose is also known to diminish oxidative stress and maintain endothelial function after hyperglycemia...
2016: Internal Medicine
Sudhaa Sharma, Vishal R Tandon, Roshi, Annil Mahajan
INTRODUCTION: Oral antihyperglycaemic prescription trends keep on changing and thus the drug prescription trend study may prove to be powerful exploratory tool for health care providers. AIM: To investigate trends in prescriptions of oral antihyperglycaemic drugs (OHDs) among postmenopausal women suffering from T2DM in India and evaluate the rationality and adherence to ADA treatment guidelines. MATERIALS AND METHODS: An observational, cross-sectional descriptive prescription audit (n=500) was carried...
January 2016: Journal of Clinical and Diagnostic Research: JCDR
Praful A Talaviya, Banshi D Saboo, Hardik G Dodiya, Shaival K Rao, Shashank R Joshi, Vipul B Modh, Sneha V Ghadiya
AIM: The study was aimed to investigate the effect of voglibose or acarbose as an add-on treatment in overweight/obese type 2 diabetes (T2DM) patients who are uncontrolled with metformin and sulfonylureas (SUs) in Western part of India. PARTICIPANTS AND METHODS: A retrospective study included 77 participants (BMI≥25kg/m(2); HbA1c level>8% and<9.5%) with overweight/obese T2DM. These participants were treated with either voglibose or acarbose. Glycemic parameters (fasting blood glucose and glycated hemoglobin [HbA1c]), bodyweight, BMI and lipid parameters were evaluated at baseline, 3-month, 6-month and 9-month of treatment...
April 2016: Diabetes & Metabolic Syndrome
Irena Roskar, Peter Molek, Miha Vodnik, Mateja Stempelj, Borut Strukelj, Mojca Lunder
AIMS/INTRODUCTION: Acute glucose fluctuations during the postprandial period pose great risk for cardiovascular complications and thus represent an important therapeutic approach in type 2 diabetes. In the present study, screening of peptide libraries was used to select peptides with an affinity towards mammalian intestinal alpha-glucosidase as potential leads in antidiabetic agent development. MATERIALS AND METHODS: Three phage-displayed peptide libraries were used in independent selections with different elution strategies to isolate target-binding peptides...
November 2015: Journal of Diabetes Investigation
James J DiNicolantonio, Jaikrit Bhutani, James H O'Keefe
α-Glucosidase inhibitors (AGIs) are a class of oral glucose-lowering drugs used exclusively for treatment or prevention of type 2 diabetes mellitus. AGIs act by altering the intestinal absorption of carbohydrates through inhibition of their conversion into simple sugars (monosaccharides) and thus decrease the bioavailability of carbohydrates in the body, significantly lowering blood glucose levels. The three AGIs used in clinical practice are acarbose, voglibose and miglitol. This review will focus on the cardiovascular properties of acarbose...
2015: Open Heart
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