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Miglitol

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https://www.readbyqxmd.com/read/28495082/synthesis-and-%C3%AE-glucosidase-inhibition-activity-of-dihydroxy-pyrrolidines
#1
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/28349245/effect-of-miglitol-on-the-suppression-of-nonalcoholic-steatohepatitis-development-and-improvement-of-the-gut-environment-in-a-rodent-model
#2
Yumi Kishida, Hirofumi Okubo, Haruya Ohno, Kenji Oki, Masayasu Yoneda
BACKGROUND: The gut environment has been considered to play a role in the development of nonalcoholic steatohepatitis (NASH). α-glucosidase inhibitors (α-GIs) delay carbohydrate absorption and may change the gut environment. We considered that the protective effect of α-GIs against NASH development is related to changes in the gut environment and thus investigated the effects of miglitol, an α-GI, on NASH development and the gut environment. METHODS: Mice were divided into three groups and fed a normal chow diet (NCD), a high-fat high-sucrose diet (HFHSD), or HFHSD plus 0...
March 27, 2017: Journal of Gastroenterology
https://www.readbyqxmd.com/read/28321087/myelodysplastic-syndrome-diagnosed-on-the-occasion-of-fournier-s-gangrene
#3
Masaaki Adachi, Kimiyoshi Mitsuhashi, Hiroyuki Matsuda, Junko Watanabe, Katsuya Nakanishi
Fournier's gangrene (FG) is a fulminant infective necrotizing fasciitis, which includes the genital, perineal, and perianal regions. A 77-year-old man had previously been diagnosed as having diabetes mellitus (DM) and was treated with pioglitazone (15 mg) and miglitol (150 mg). He developed sudden perineal discomfort, fever with painful penile, and scrotal edema, subsequently leading to urinary retention. According to physical examination and CT scan results for the swollen penis and scrotum, he was diagnosed with FG...
2017: [Rinshō Ketsueki] the Japanese Journal of Clinical Hematology
https://www.readbyqxmd.com/read/28170007/lactucaxanthin-a-potential-anti-diabetic-carotenoid-from-lettuce-lactuca-sativa-inhibits-%C3%AE-amylase-and-%C3%AE-glucosidase-activity-in-vitro-and-in-diabetic-rats
#4
Sowmya Shree Gopal, Magisetty Jhansi Lakshmi, Gurunathan Sharavana, Gunaseelan Sathaiah, Yadahally N Sreerama, Vallikannan Baskaran
Intestinal and pancreatic α-amylase and α-glucosidase inhibitors offer an approach to lower the levels of post-prandial hyperglycemia through the control of dietary starch breakdown in digestion. This study hypothesized that lactucaxanthin (Lxn) in lettuce (Lactuca sativa) inhibits the activity of α-amylase and α-glucosidase. In this study, the interaction of Lxn with α-amylase and α-glucosidase in silico and its inhibitory effect on these enzymes were studied using in vitro and STZ-induced diabetic rat models...
February 7, 2017: Food & Function
https://www.readbyqxmd.com/read/28097882/antidiabetic-agents-and-cardiovascular-outcomes-in-patients-with-heart-diseases
#5
Judy W M Cheng, Hisham A Badreldin, Dhiren K Patel, Snehal H Bhatt
INTRODUCTION: This article reviews evidence of the benefits and risk of antidiabetic agents in cardiovascular (CV) outcomes, with a focus on medications approved by the FDA since 2008. STUDY SELECTION: Peer-reviewed articles were identified from MEDLINE and Current Content databases (both 1966 to 1 October 2016) using the search terms insulin, metformin, rosiglitazone, pioglitazone, glyburide, glipizide, glimepiride, acarbose, miglitol, albiglutide, exenatide, liraglutide, lixisenatide, dulaglutide, pramlintide, meglitinide, alogliptin, linagliptin, saxagliptin, sitagliptin, canagliflozin, dapagliflozin, empagliflozin, colesevalam, bromocriptine, mortality, myocardial infarction (MI), heart failure (HF), and stroke...
June 2017: Current Medical Research and Opinion
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
#6
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/27956035/synthesis-and-characterization-of-novel-conjugated-fluorescent-dnj-derivatives-for-%C3%AE-glucosidase-recognition
#7
Akihiko Hatano, Yuichi Kanno, Yuya Kondo, Yuta Sunaga, Hatsumi Umezawa, Munehiro Okada, Hideshi Yamada, Ren Iwaki, Atsushi Kato, Koji Fukui
A series of five new fluorescent deoxynojirimycin (DNJ) conjugates were synthesized and evaluated for their inhibitory effect (IC50) on several α- and β-glucosidases. Three of the conjugates showed enhanced activity. The two synthetic conjugates, DNJ-CF31 and DNJ-Me 2, exhibited improved α-glucosidase inhibitory effects compared to DNJ and miglitol. Interestingly, conjugates 1 and 2 showed strong inhibition of almond-derived β-glucosidase, in contrast to the inhibition tendencies of other inhibitors. Conjugate 5 strongly inhibited rat intestinal maltase, even at 0...
January 15, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/27923989/metabolic-control-of-tobacco-pollination-by-sugars-and-invertases
#8
Marc Goetz, Anne Guivarćh, Jörg Hirsche, Martin Andreas Bauerfeind, María-Cruz González, Tae Kyung Hyun, Seung Hee Eom, Dominique Chriqui, Thomas Engelke, Dominik K Großkinsky, Thomas Roitsch
Pollination in flowering plants is initiated by germination of pollen grains on stigmas followed by fast growth of pollen tubes representing highly energy-consuming processes. The symplastic isolation of pollen grains and tubes requires import of Suc available in the apoplast. We show that the functional coupling of Suc cleavage by invertases and uptake of the released hexoses by monosaccharide transporters are critical for pollination in tobacco (Nicotiana tabacum). Transcript profiling, in situ hybridization, and immunolocalization of extracellular invertases and two monosaccharide transporters in vitro and in vivo support the functional coupling in supplying carbohydrates for pollen germination and tube growth evidenced by spatiotemporally coordinated expression...
February 2017: Plant Physiology
https://www.readbyqxmd.com/read/27917299/a-male-with-extreme-subcutaneous-insulin-resistance-a-case-report
#9
Zuhayer Ahmed, Indrajit Prasad, Hafizur Rahman, Jalil Ansari, Khaled Hassan
INTRODUCTION: Though insulin has no upper limit in dosage, we do not encounter very high dose requirements too often. The reported case is the first in Bangladesh to require more than 1000 international units (IU) of subcutaneous insulin per day. CASE PRESENTATION: A 44-year old male diabetic patient from Bangladesh presented with unusually uncontrolled diabetes mellitus due to extreme insulin resistance. Despite dramatic increase in insulin step by step up to 1110 IU of concomitant short and intermediate acting insulin per day by subcutaneous route, his blood glucose remained over 12 mmol/L persistently, in all the fasting, pre-prandial, postprandial and random samples...
June 2016: Romanian Journal of Diabetes, Nutrition, & Metabolic Diseases
https://www.readbyqxmd.com/read/27904400/16s-rrna-in-situ-hybridization-followed-by-flow-cytometry-for-rapid-identification-of-acetic-acid-bacteria-involved-in-submerged-industrial-vinegar-production
#10
Janja Trček, Luka Lipoglavšek, Gorazd Avguštin
Acetic acid bacteria are involved in many biotechnological processes such as vitamin C, gluconic acid, miglitol or acetic acid production, and others. For a technologist trying to control the industrial process, the ability to follow the microbiological development of the process is thus of importance. During the past few years hybridization in a combination with flow cytometry has often been used for this purpose. Since vinegar is a liquid, it is an ideal matrix for flow cytometry analysis. In this work we have constructed a specific probe for highly acetic acid-resistant species of the acetic acid bacteria and a protocol for in situ hybridization, which in combination with flow cytometry enables direct monitoring of bacteria producing vinegar with >10% of acetic acid...
March 2016: Food Technology and Biotechnology
https://www.readbyqxmd.com/read/27780736/add-on-therapy-with-anagliptin-in-japanese-patients-with-type-2-diabetes-mellitus-treated-with-metformin-and-miglitol-can-maintain-higher-concentrations-of-biologically-active-glp-1-total-gip-and-a-lower-concentration-of-leptin
#11
Takeshi Osonoi, Miyoko Saito, Natsuyo Hariya, Moritaka Goto, Kazuki Mochizuki
Metformin, α-glucosidase inhibitors (α-GIs), and dipeptidyl peptidase 4 inhibitors (DPP-4Is) reduce hyperglycemia without excessive insulin secretion, and enhance postprandial plasma concentration of glucagon-like peptide-1 (GLP-1) in type-2 diabetes mellitus (T2DM) patients. We assessed add-on therapeutic effects of DPP-4I anagliptin in Japanese T2DM patients treated with metformin, an α-GI miglitol, or both drugs on postprandial responses of GLP-1 and glucose-dependent insulinotropic polypeptide (GIP), and on plasma concentration of the appetite-suppressing hormone leptin...
December 2016: Peptides
https://www.readbyqxmd.com/read/27754407/development-and-validation-of-miglitol-and-its-impurities-by-rp-hplc-and-characterization-using-mass-spectrometry-techniques
#12
Kesavan Balakumaran, Mosesbabu Janagili, Nagaraju Rajana, Sureshbabu Papureddy, Jayashree Anireddy
Alpha glucoside inhibitors used to treat type-2 diabetes mellitus (DM) are likely to be safe and effective. These agents are most effective for postprandial hyperglycemia. Miglitol is a type of drug used to treat type-2 DM. A simple, selective, linear, precise and accurate reversed-phase high-performance liquid chromatography (RP-HPLC) method was developed and validated for a related substance of miglitol and its identification, and characterization was done by different mass spectrometry techniques. The gradient method at a flow rate of 1...
October 14, 2016: Scientia Pharmaceutica
https://www.readbyqxmd.com/read/27664368/one-pot-oxidative-dehydration-oxidation-of-polyhydroxyhexanal-oxime-to-polyhydroxy-oxohexanenitrile-a-versatile-methodology-for-the-facile-access-of-azasugar-alkaloids
#13
Sandip R Khobare, Vikas Gajare, E Vishnuvardhan Reddy, Rajender Datrika, Malavika Banda, Vidavalur Siddaiah, Sharad S Pachore, Upadhya Timanna, Vilas H Dahanukar, U K Syam Kumar
A unique oxidative dehydration-oxidation of polyhydroxy-oxime (7) to the corresponding ketonitrile (8) in one pot is reported for the first time in carbohydrate literature. Key ketonitrile intermediate (8) upon palladium hydroxide mediated cascade reaction afforded 1-deoxynojirimycin (DNJ) 1b in moderate diastereoselectivity. The cascade reaction involves the conversion of nitrile to amine, heteroannulation, reduction of the imine and subsequent debenzylation to furnish the azasugars. This oxidative dehydration-oxidation and reductive heteroannulation methodology is successfully utilized for the total synthesis of 1-deoxynojirimycin (1b), miglitol (2) and miglustat (3)...
November 29, 2016: Carbohydrate Research
https://www.readbyqxmd.com/read/27640062/insulin-monotherapy-compared-with-the-addition-of-oral-glucose-lowering-agents-to-insulin-for-people-with-type-2-diabetes-already-on-insulin-therapy-and-inadequate-glycaemic-control
#14
REVIEW
Rimke C Vos, Mariëlle Jp van Avendonk, Hanneke Jansen, Alexander N Goudswaard, Maureen van den Donk, Kees Gorter, Anneloes Kerssen, Guy Ehm Rutten
BACKGROUND: It is unclear whether people with type 2 diabetes mellitus on insulin monotherapy who do not achieve adequate glycaemic control should continue insulin as monotherapy or can benefit from adding oral glucose-lowering agents to the insulin therapy. OBJECTIVES: To assess the effects of insulin monotherapy compared with the addition of oral glucose-lowering agents to insulin monotherapy for people with type 2 diabetes already on insulin therapy and inadequate glycaemic control...
September 18, 2016: Cochrane Database of Systematic Reviews
https://www.readbyqxmd.com/read/27539431/rapid-identification-of-miglitol-and-its-isomers-by-electrospray-ionization-tandem-mass-spectrometry
#15
Qiuhong Yin, Lin Wang, Cuirong Sun
RATIONALE: Miglitol (1) derived from 1-deoxynojirimycin is an iminosugar that is useful in the treatment of type 2 diabetes mellitus. Isomers (2, 3, 4) that differ at the C2 and C3 positions of hydroxyl groups from miglitol are impurities resulting from the synthesis of miglitol. The impurity profile of a drug substance is critical to its safety assessment and is important for monitoring the manufacturing process. Therefore, developing a fast and simple method that can rapidly identify the configuration of miglitol and its isomers (2, 3, 4) is necessary...
August 2016: Rapid Communications in Mass Spectrometry: RCM
https://www.readbyqxmd.com/read/27440852/liraglutide-improved-glycaemic-instability-in-a-patient-with-diabetes-with-insulin-antibodies
#16
Takehiro Kato, Katsumi Iizuka, Hiroyuki Niwa, Jun Takeda
Insulin antibodies sometimes cause glucose instability. A 52-year-old male patient was admitted to our department for the treatment of diabetes mellitus. From October 2003, he received insulin treatment for autoimmune pancreatitis and diabetes mellitus, but his hemoglobin A1c (HbA1c) levels gradually reached 8.0% (64 mmol/mol IFCC). In January 2010, insulin glargine and insulin aspart were introduced. In April 2010, the insulin antibody titre rose to >13.6 U/mL. In July 2010, treatment was changed to insulin glargine, metformin and miglitol...
July 20, 2016: BMJ Case Reports
https://www.readbyqxmd.com/read/27325449/hydrophobic-substituents-increase-the-potency-of-salacinol-a-potent-%C3%AE-glucosidase-inhibitor-from-ayurvedic-traditional-medicine-salacia
#17
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
https://www.readbyqxmd.com/read/27150868/concurrent-therapy-with-a-low-carbohydrate-diet-and-miglitol-remarkably-improved-the-postprandial-blood-glucose-and-insulin-levels-in-a-patient-with-reactive-hypoglycemia-due-to-late-dumping-syndrome
#18
Sachie Hirose, Yasuyuki Iwahashi, Akane Seo, Michitaka Sumiyoshi, Tetsuya Takahashi, Yoshikazu Tamori
Reactive hypoglycemia induced by late dumping syndrome is often observed after gastrectomy. However, no effective therapy has yet been fully established. We herein describe a case in which concurrent therapy with a low-carbohydrate diet using low-glycemic-index food and an alpha-glucosidase inhibitor, miglitol, very effectively ameliorated the postprandial fluctuations in the blood glucose and plasma insulin levels in a patient with reactive hypoglycemia due to late dumping syndrome following total gastrectomy...
2016: Internal Medicine
https://www.readbyqxmd.com/read/26918556/comparison-of-efficacy-and-safety-of-taking-miglitol-dissolved-in-water-during-a-meal-and-taking-a-miglitol-tablet-just-before-a-meal-in-patients-with-type-2-diabetes
#19
RANDOMIZED CONTROLLED TRIAL
Eriko Shibata, Kazutaka Aoki, Kazuki Tajima, Masataka Taguri, Yasuo Terauchi
OBJECTIVE: We compared the efficacy and safety of taking miglitol dissolved in water during a meal and taking a miglitol tablet just before a meal. Primary efficacy parameter is the area under the curve (AUC) for postprandial plasma glucose. METHODS: Miglitol was administered according to three different intake schedules in each subject: intake schedule A, no miglitol; intake schedule B, administration of miglitol (50 mg) just before breakfast; intake schedule C, dissolving miglitol (50 mg) in water and taking it just before (1/3), during (1/3), and just after breakfast (1/3)...
2016: Expert Opinion on Pharmacotherapy
https://www.readbyqxmd.com/read/26650760/uncovering-the-molecular-mechanism-of-actions-between-pharmaceuticals-and-proteins-on-the-ad-network
#20
Shujuan Cao, Liang Yu, Jingyuan Mao, Quan Wang, Jishou Ruan
This study begins with constructing the mini metabolic networks (MMNs) of beta amyloid (Aβ) and acetylcholine (ACh) which stimulate the Alzheimer's Disease (AD). Then we generate the AD network by incorporating MMNs of Aβ and ACh, and other MMNs of stimuli of AD. The panel of proteins contains 49 enzymes/receptors on the AD network which have the 3D-structure in PDB. The panel of drugs is formed by 5 AD drugs and 5 AD nutraceutical drugs, and 20 non-AD drugs. All of these complexes formed by these 30 drugs and 49 proteins are transformed into dyadic arrays...
2015: PloS One
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