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https://www.readbyqxmd.com/read/29189010/diastereoselective-synthesis-of-salacinol-type-%C3%AE-glucosidase-inhibitors
#1
Fumihiro Ishikawa, Kazumi Jinno, Eri Kinouchi, Kiyofumi Ninomiya, Shinsuke Marumoto, Weijia Xie, Osamu Muraoka, Toshio Morikawa, Genzoh Tanabe
A facile and highly diastereoselective approach towards the synthesis of potent salacinol-type α-glucosidase inhibitors, originally isolated from plants of the genus "Salacia", was developed using the S-alkylation of thiosugars with epoxides in HFIP (~90%, dr, α/β = ~26/1). The dr ratio of the product was significantly improved by the protocol as compared to that of the conventional S-alkylation of thiosugars (dr, α/β = ~8/1). The protocol could be used for gram scale synthesis of the desired compounds...
November 30, 2017: Journal of Organic Chemistry
https://www.readbyqxmd.com/read/29151501/the-efficacy-of-corticosteroid-therapy-in-a-patient-with-nonalcoholic-steatohepatitis-overlapping-autoimmune-hepatitis-a-case-report
#2
Takuya Komura, Hajime Ohta, Takuya Seike, Yoshiaki Shimizu, Ryotaro Nakai, Hitoshi Omura, Takashi Kagaya, Satomi Kasashima, Atsuhiro Kawashima, Sakae Oba, Kennichi Harada, Shuichi Kaneko, Masashi Unoura
The overlap of multiple liver diseases can cause the disease activity and severity to worsen rapidly in some cases. We rarely see patients with non-alcoholic steatohepatitis (NASH) with overlapping autoimmune hepatitis (AIH). A 64-year-old woman who had been prescribed oral drugs to treat diabetes and hypertension (metformin 500 mg/day and voglibose 0.9 mg/day, and termisartan 40 mg/day and amlodipine 5 mg/day, respectively) was diagnosed with NASH with histological confirmation. At 68 years of age, her liver injury worsened with an IgG of 2,871 mg/dL and a high serum anti-nuclear antibody (ANA) level of 2,560...
November 20, 2017: Internal Medicine
https://www.readbyqxmd.com/read/29123848/a-case-of-type-2-diabetes-mellitus-with-metformin-associated-lactic-acidosis-initially-presenting-the-appearance-of-a-sulfonylurea-related-hypoglycemic-attack
#3
Kota Nishihama, Kanako Maki, Yuko Okano, Rei Hashimoto, Yasuhiro Hotta, Mei Uemura, Taro Yasuma, Toshinari Suzuki, Toyomi Hayashi, Eiji Ishikawa, Yutaka Yano, Esteban C Gabazza, Masaaki Ito, Yoshiyuki Takei
Case: A 64-year-old Japanese woman with diabetes mellitus was admitted for hypoglycemia. Her diabetes had been under good control with glimepiride, voglibose, exenatide, and metformin for a few years. Although overt proteinuria was observed, the serum creatinine values were within normal range during the routine outpatient follow-up. Hypoglycemic attack caused by glimepiride and loss of appetite by urinary tract infection were diagnosed. Then, metformin-associated lactic acidosis with acute renal failure caused by dehydration was detected...
January 2017: Acute Medicine & Surgery
https://www.readbyqxmd.com/read/29080007/rapid-analysis-of-pharmaceutical-drugs-using-libs-coupled-with-multivariate-analysis
#4
P K Tiwari, S Awasthi, R Kumar, R K Anand, P K Rai, A K Rai
Type 2 diabetes drug tablets containing voglibose having dose strengths of 0.2 and 0.3 mg of various brands have been examined, using laser-induced breakdown spectroscopy (LIBS) technique. The statistical methods such as the principal component analysis (PCA) and the partial least square regression analysis (PLSR) have been employed on LIBS spectral data for classifying and developing the calibration models of drug samples. We have developed the ratio-based calibration model applying PLSR in which relative spectral intensity ratios H/C, H/N and O/N are used...
October 27, 2017: Lasers in Medical Science
https://www.readbyqxmd.com/read/29058089/evidence-based-treatment-of-neurogenic-orthostatic-hypotension-and-related-symptoms
#5
REVIEW
Sabine Eschlböck, Gregor Wenning, Alessandra Fanciulli
Neurogenic orthostatic hypotension, postprandial hypotension and exercise-induced hypotension are common features of cardiovascular autonomic failure. Despite the serious impact on patient's quality of life, evidence-based guidelines for non-pharmacological and pharmacological management are lacking at present. Here, we provide a systematic review of the literature on therapeutic options for neurogenic orthostatic hypotension and related symptoms with evidence-based recommendations according to the Grading of Recommendations Assessment, Development and Evaluation (GRADE)...
December 2017: Journal of Neural Transmission
https://www.readbyqxmd.com/read/28978579/nocturnal-reactive-hypoglycaemia-well-treated-subjectively-and-objectively-with-voglibose
#6
Hiroyuki Koyama, Hideomi Ohguchi, Takashi Yagi, Kenro Imaeda
Clinicians sometimes encounter difficulty in diagnosing hypoglycaemia. Here, we present a case report of a 53-year-old woman with recurrent nocturnal hypoglycaemia. A continuous glucose monitoring system (CGMS) revealed postprandial hyperglycaemia and subsequent hypoglycaemia, and an oral glucose tolerance test showed an impaired glycaemic and delayed hyperinsulinaemic pattern. On the basis of these clinical findings, we diagnosed her unexplained hypoglycaemia as reactive hypoglycaemia. CGMS showed a sharp contrast of diurnal variation in blood glucose levels including hypoglycaemia between before and after treatment with an alpha-glucosidase inhibitor, voglibose...
October 4, 2017: BMJ Case Reports
https://www.readbyqxmd.com/read/28931726/impaired-insulin-igf-1-is-responsible-for-diabetic-gastroparesis-by-damaging-myenteric-cholinergic-neurones-and-interstitial-cells-of-cajal
#7
Shu Yang, Bo Wu, Haimei Sun, Tingyi Sun, Kai Han, Dandan Li, Fengqing Ji, Guoquan Zhang, Deshan Zhou
Diabetic gastroparesis is a common complication of diabetes mellitus (DM) that is characterized by decreased serum insulin and insulin-like growth factor-1 (IGF-1). Despite the fact that insulin treatment not glycemic control potently accelerated gastric emptying in type 1 DM patients, the role of insulin/InsR and IGF-1/IGF-1R signaling in diabetic gastroparesis remains incompletely elucidated. In the present study, type 1 DM mice were established and treated with insulin or Voglibose for 8 weeks. The gastric emptying was delayed from DM week 4 when the gastric InsR and IGF-1R were declined...
October 31, 2017: Bioscience Reports
https://www.readbyqxmd.com/read/28792171/glycemic-pentad
#8
Glycemic Pentad Forum
BACKGROUND: Conventionally, diabetes management involved targeting the triad of FPG, PPG, and HbA1c. However, several studies have suggested the quintessential need for a paradigm shift to incorporate glycemic variability and quality of life in the holistic diabetes control regimen. AIM: To generate a consensus and ratify the position of Glycemic Variability (GV) and Quality of Life (QOL), along with the traditional triad, in diabetes management in India. To evaluate whether the triple fixed dose combination of metformin, glimepiride, and voglibose can accomplish the goals of glycemic pentad...
July 2017: Journal of the Association of Physicians of India
https://www.readbyqxmd.com/read/28743290/pneumatosis-intestinalis-with-a-benign-clinical-course-a-report-of-two-cases
#9
Aya Takase, Nobuhiro Akuzawa, Hiroshi Naitoh, Jun Aoki
BACKGROUND: Pneumatosis intestinalis (PI) is a rare condition characterized by the presence of gas within the gastrointestinal tract wall. Most cases of PI have a benign clinical course, although some have serious outcomes. Mechanical stress on or bacterial infection of the gastrointestinal tract wall may be responsible for the onset of PI, but the detailed mechanism of PI pathogenesis is still unclear. Here, we describe two Japanese patients presenting with benign PI. CASE PRESENTATION: Case 1, a 37-year-old previously healthy male patient, had a 1-week history of abdominal pain, and case 2, a 78-year-old female diabetic patient, had a 2-week history of voglibose treatment and abdominal pain...
July 25, 2017: BMC Research Notes
https://www.readbyqxmd.com/read/28672278/hydrazinyl-arylthiazole-based-pyridine-scaffolds-synthesis-structural-characterization-in%C3%A2-vitro-%C3%AE-glucosidase-inhibitory-activity-and-in-silico-studies
#10
Farman Ali, Khalid Mohammed Khan, Uzma Salar, Muhammad Taha, Nor Hadiani Ismail, Abdul Wadood, Muhammad Riaz, Shahnaz Perveen
Acarbose, miglitol, and voglibose are the inhibitors of α-glucosidase enzyme and being clinically used for the management of type-II diabetes mellitus. However, many adverse effects are also associated with them. So, the development of new therapeutic agents is an utmost interest in medicinal chemistry research. Current study is based on the identification of new α-glucosidase inhibitors. For that purpose, hydrazinyl arylthiazole based pyridine derivatives 1-39 were synthesized via two step reaction and fully characterized by spectroscopic techniques EI-MS, HREI-MS, (1)H-, and (13)C NMR...
September 29, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28584404/the-%C3%AE-glucosidase-inhibitor-voglibose-stimulates-delayed-gastric-emptying-in-healthy-subjects-a-crossover-study-with-a-13-c-breath-test
#11
Kenji Kanoshima, Mizue Matsuura, Megumi Kaai, Yumi Inoh, Kanji Ohkuma, Hiroshi Iida, Takashi Nonaka, Koji Fujita, Tomonori Ida, Akihiko Kusakabe, Atsushi Nakajima, Masahiko Inamori
The gastrointestinal effects of α-glucosidase inhibitors have not been sufficiently investigated. The aim of this study was to determine whether a single dose of pre-prandial voglibose might affect the rate of gastric emptying, determined using the (13)C breath test. Ten healthy male volunteers participated in this randomized, two-way crossover study. The subjects fasted overnight and received 0.2 mg voglibose or a placebo 2 h before a test meal. They were then served a liquid test meal consisting of 200 kcal per 200 ml that contained 100 mg (13)C-acetate...
May 2017: Journal of Clinical Biochemistry and Nutrition
https://www.readbyqxmd.com/read/28495082/synthesis-and-%C3%AE-glucosidase-inhibition-activity-of-dihydroxy-pyrrolidines
#12
Sivaprasad Kasturi, Sujatha Surarapu, Srinivas Uppalanchi, Jaya Shree Anireddy, Shubham Dwivedi, Hasitha Shilpa Anantaraju, Yogeeswari Perumal, Dilep Kumar Sigalapalli, Bathini Nagendra Babu, Krishna S Ethiraj
A new series of Deacetylsarmentamide A and B derivatives, amides and sulfonamides of 3,4-dihydroxypyrrolidines as α-glucosidase inhibitors were designed and synthesized. The biological screening test against α-glucosidase showed that some of these compounds have the positive inhibitory activity against α-glucosidase. Saturated aliphatic amides were more potent than the olefinic amides. Among all the compounds, 5o/6o having polar -NH2 group, 10f/11f having polar -OH group on phenyl ring displayed 3-4-fold more potent than the standard drugs...
June 15, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28331117/comparison-between-effectiveness-of-100-mg-day-sitagliptin-and-a-switch-to-mitiglinide-calcium-hydrate-voglibose-from-50-mg-day-sitagliptin-in-patients-with-type-2-diabetes
#13
COMPARATIVE STUDY
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
https://www.readbyqxmd.com/read/28242866/cross-over-study-comparing-postprandial-glycemic-increase-after-addition-of-a-fixed-dose-mitiglinide-voglibose-combination-or-a-dipeptidyl-peptidase-4-inhibitor-to-basal-insulin-therapy-in-patients-with-type-2-diabetes-mellitus
#14
RANDOMIZED CONTROLLED TRIAL
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
https://www.readbyqxmd.com/read/28185012/the-synergistic-effect-of-maltose-enhances-the-anti-melanogenic-activity-of-acarbose
#15
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
https://www.readbyqxmd.com/read/28010166/reappraisal-and-perspectives-of-clinical-drug-drug-interaction-potential-of-%C3%AE-glucosidase-inhibitors-such-as-acarbose-voglibose-and-miglitol-in-the-treatment-of-type-2-diabetes-mellitus
#16
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
https://www.readbyqxmd.com/read/27802313/effect-of-sodium-glucose-co-transporter-2-inhibitor-dapagliflozin-on-renal-renin-angiotensin-system-in-an-animal-model-of-type-2-diabetes
#17
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
https://www.readbyqxmd.com/read/27710821/effects-of-linagliptin-monotherapy-compared-with-voglibose-on-postprandial-blood-glucose-responses-in-japanese-patients-with-type-2-diabetes-linagliptin-study-of-effects-on-postprandial-blood-glucose-l-step
#18
RANDOMIZED CONTROLLED TRIAL
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
https://www.readbyqxmd.com/read/27596550/-comparison-of-therapeutic-effects-between-sitagliptin-and-voglibose-both-combined-with-sensor-augmented-insulin-pump-in-newly-diagnosed-type-2-diabetes
#19
RANDOMIZED CONTROLLED TRIAL
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]
https://www.readbyqxmd.com/read/27547421/linagliptin-monotherapy-compared-with-voglibose-monotherapy-in-patients-with-type-2-diabetes-undergoing-hemodialysis-a-12-week-randomized-trial
#20
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
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