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https://www.readbyqxmd.com/read/28100083/%C3%AE-glucosidase-inhibitory-activity-and-cytotoxic-effects-of-some-cyclic-urea-and-carbamate-derivatives
#1
Jelena B Popović-Djordjević, Ivana I Jevtić, Nadja Dj Grozdanić, Sandra B Šegan, Mario V Zlatović, Milovan D Ivanović, Tatjana P Stanojković
The inhibitory activities of selected cyclic urea and carbamate derivatives (1-13) toward α-glucosidase (α-Gls) in in vitro assay were examined in this study. All examined compounds showed higher inhibitory activity (IC50) against α-Gls compared to standard antidiabetic drug acarbose. The most potent was benzyl (3,4,5-trimethoxyphenyl)carbamate (12) with IC50 = 49.85 ± 0.10 µM. In vitro cytotoxicity of the investigated compounds was tested on three human cancer cell lines HeLa, A549 and MDA-MB-453 using MTT assay...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28097882/antidiabetic-agents-and-cardiovascular-outcomes-in-patients-with-heart-diseases
#2
Judy W M Cheng, Hisham A Badreldin, Dhiren K Patel, Snehal H Bhatt
This article reviews evidence of benefits and risk of antidiabetic agents in cardiovascular (CV) outcomes, with a focus on medications approved by the FDA since 2008. Peer-reviewed articles were identified from MEDLINE and Current Content database (both 1966 to October 1, 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...
January 18, 2017: Current Medical Research and Opinion
https://www.readbyqxmd.com/read/28095353/liver-alpha-amylase-gene-expression-as-an-early-obesity-biomarker
#3
Marzieh Mojbafan, Zohreh Afsartala, Mahsa M Amoli, Mahdi Mahmoudi, Parichehreh Yaghmaei, Bagher Larijani, Azadeh Ebrahim-Habibi
BACKGROUND: Obesity is a major health problem worldwide, for which preventive and therapeutic means are still needed. Alpha-amylase is a digestive enzyme whose inhibition has been targeted as a potential anti-obesity strategy. However, alpha-amylase gene expression has not been particularly attended to, and in contrast with pancreatic and salivary amylases, fewer studies have focused on liver alpha-amylase. The present study aimed at investigating the expression of alpha-amylase gene in obese and normal mice at RNA and protein level as well as acarbose effect on this gene expression in hepatocyte cell culture...
November 5, 2016: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/28093873/diagnostic-and-management-challenges-from-childhood-puberty-through-to-transition-in-severe-insulin-resistance-due-to-insulin-receptor-mutations
#4
Christina Wei, Christine P Burren
Two Caucasian girls, both of normal weight and body mass indices, were diagnosed with type A insulin resistance (IR) in childhood. Case 1 presented with premature adrenarche aged 7 years, then by age 12 years had hirsutism, acne, acanthosis nigricans, and asymptomatic diabetes. Subsequent investigation revealed raised adiponectin (15.3 mg/L) and heterozygous p.Pro1205Leu mutation in the INSR gene encoding the insulin receptor. She experienced postprandial hypoglycaemia on metformin; acarbose was trialled and discontinued aged 16 years, as she became normoglycaemic...
January 17, 2017: Pediatric Diabetes
https://www.readbyqxmd.com/read/28069265/8-hydroxyirilone-5-methyl-ether-and-8-hydroxyirilone-new-antioxidant-and-%C3%AE-amylase-inhibitors-isoflavonoids-from-iris-germanica-rhizomes
#5
Sabrin R M Ibrahim, Gamal A Mohamed, Mohamed F Zayed, Samir A Ross
Iris species are well recognized as wealthy sources of isoflavonoids. In the present study, phytochemical investigation of the rhizomes of Iris germanica (Iridaceae) procure the isolation of two new isoflavonoids namely, 8-hydroxyirilone 5-methyl ether (2) and 8-hydroxyirilone (3), along with eight known isoflavonoids: irilone 4'-methyl ether (1), irilone (4), irisolidone (5), irigenin S (6), irigenin (7), irilone 4'-O-β-d-glucopyranoside (8), iridin S (9), and iridin (10). The isolated flavonoids were structurally characterized with the assist of comprehensive spectroscopic analyses (UV, IR, 1D and 2D NMR, and HRMS) and comparing with the published data...
December 30, 2016: Bioorganic Chemistry
https://www.readbyqxmd.com/read/28067838/effect-of-phenolic-compounds-from-elderflowers-on-glucose-and-fatty-acid-uptake-in-human-myotubes-and-hepg2-cells
#6
Giang Thanh Thi Ho, Eili Tranheim Kase, Helle Wangensteen, Hilde Barsett
Type 2 diabetes (T2D) is manifested by progressive metabolic impairments in tissues such as skeletal muscle and liver, and these tissues become less responsive to insulin, leading to hyperglycemia. In the present study, stimulation of glucose and oleic acid uptake by elderflower extracts, constituents and metabolites were tested in vitro using the HepG2 hepatocellular liver carcinoma cell line and human skeletal muscle cells. Among the crude extracts, the 96% EtOH extract showed the highest increase in glucose and oleic acid uptake in human skeletal muscle cells and HepG2-cells...
January 6, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28056420/synergistic-effects-of-acarbose-and-an-oroxylum-indicum-seed-extract-in-streptozotocin-and-high-fat-diet-induced-prediabetic-mice
#7
Wenlong Sun, Yuanbin Sang, Bowei Zhang, Xiaoxia Yu, Qinmin Xu, Zhilong Xiu, Yuesheng Dong
Prediabetes is defined as blood glucose levels above normal but below diabetes thresholds, and up to 70% of individuals with prediabetes will eventually develop diabetes if left untreated. Acarbose, the first FDA approved anti-prediabetes agent, has some disadvantages, such as reducing the risk of diabetes by only 36%, side effects and limited effects on complications. The aim of this study is to develop a new agent to treat prediabetes and to investigate the anti-prediabetes effects and mechanisms of acarbose and an Oroxylum indicum seed extract (OISE) in prediabetic mice...
January 2, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28043716/synthesis-molecular-docking-studies-of-hybrid-benzimidazole-as-%C3%AE-glucosidase-inhibitor
#8
Nik Khairunissa Nik Abdullah Zawawi, Muhammad Taha, Norizan Ahmat, Nor Hadiani Ismail, Abdul Wadood, Fazal Rahim
Thiourea derivatives having benzimidazole 1-17 have been synthesized, characterized by (1)H NMR, (13)C NMR and EI-MS and evaluated for α-glucosidase inhibition. Identification of potential α-glucosidase inhibitors were done by in vitro screening of 17 thiourea bearing benzimidazole derivatives using Baker's yeast α-glucosidase enzyme. Compounds 1-17 exhibited a varying degree of α-glucosidase inhibitory activity with IC50 values between 35.83±0.66 and 297.99±1.20μM which are more better than the standard acarbose (IC50=774...
December 26, 2016: Bioorganic Chemistry
https://www.readbyqxmd.com/read/28042355/effects-of-the-addition-of-acarbose-to-insulin-and-non-insulin-regimens-in-veterans-with-type-2-diabetes-mellitus
#9
Sara A Wettergreen, Shaila Sheth, Janeca Malveaux
OBJECTIVES: The primary objective of the study was to assess the mean change in hemoglobin A1c (HbA1c) when acarbose was added to insulin and non-insulin regimens in patients with type 2 diabetes mellitus (T2DM). Secondary objectives were to evaluate the discontinuation rate of acarbose, and to assess the number of patients who were placed on insulin despite the addition of acarbose. METHODS: A retrospective chart review was conducted on veterans with T2DM initiated on acarbose between October 1, 2013 and December 31, 2013...
October 2016: Pharmacy Practice
https://www.readbyqxmd.com/read/28035868/a-randomized-clinical-trial-of-the-safety-and-efficacy-of-sitagliptin-in-patients-with-type-2-diabetes-mellitus-inadequately-controlled-by-acarbose-alone
#10
Weiqing Wang, Guang Ning, Jianhua Ma, Xiaomin Liu, Shaoxiong Zheng, Fan Wu, Lei Xu, Edward A O'Neill, Kenji P Fujita, Samuel S Engel, Keith D Kaufman, R Ravi Shankar
OBJECTIVE: To evaluate the safety and efficacy of sitagliptin when added to the treatment of patients with type 2 diabetes mellitus (T2DM) and inadequate glycemic control on acarbose monotherapy. RESEARCH DESIGN AND METHODS: This was a multicenter, randomized, placebo-controlled, double-blind clinical trial. Patients (N = 381) with T2DM and inadequate glycemic control (glycated hemoglobin [HbA1c] ≥7.0% and ≤10.0%) on acarbose monotherapy (at least 50 mg three times daily) were randomized in a 1:1 ratio to receive the addition of sitagliptin 100 mg or matching placebo once daily for 24 weeks...
December 30, 2016: Current Medical Research and Opinion
https://www.readbyqxmd.com/read/28035340/targeting-glucose-metabolism-for-healthy-aging
#11
REVIEW
Rachel A Brewer, Victoria K Gibbs, Daniel L Smith
Advancing age is the greatest single risk factor for numerous chronic diseases. Thus, the ability to target the aging process can facilitate improved healthspan and potentially lifespan. Lack of adequate glucoregulatory control remains a recurrent theme accompanying aging and chronic disease, while numerous longevity interventions result in maintenance of glucoregulatory control. In this review, we propose targeting glucose metabolism to enhance regulatory control as a means to ameliorate the aging process...
October 27, 2016: Nutr Healthy Aging
https://www.readbyqxmd.com/read/28017142/gliclazide-induced-insulin-autoimmune-syndrome-a-rare-case-report-and-review-on-literature
#12
Xiu Feng, Lu Yuan, Hu Yun, Yunqing Zhu, Fan Yang, Lanlan Jiang, Rengna Yan, Yong Luo, Enhui Zhao, Chenxiao Liu, Ying Wang, Qi Li, Xin Cao, Qian Li, Jianhua Ma
Insulin Autoimmune Syndrome (IAS) is a rare condition characterized by the combination of recurrent severely spontaneous hypoglycemia without evidence of exogenous insulin administration, high concentration of total serum insulin, and the presence of a high titer of insulin autoantibody (IAA)[ ]. But now we describe a case with IAS caused by gliclazide and hardly occuring hypoglycemia. A 70-year-old man with type 2 diabetes presented to our department with poor glycemic control without evidence of hypoglycemia, but the levels of serum insulin and IAA were very high...
December 23, 2016: Endocrine, Metabolic & Immune Disorders Drug Targets
https://www.readbyqxmd.com/read/28013556/%C3%AE-glucosidase-inhibitors-and-phytotoxins-from-streptomyces-xanthophaeus
#13
Jing Wei, Xiu-Yun Zhang, Shan Deng, Lin Cao, Quan-Hong Xue, Jin-Ming Gao
Twenty-four metabolites 1-24 were isolated from the fermentation broth of Streptomyces xanthophaeus. Their structures were elucidated on the basis of spectroscopic analysis and by comparison of their NMR data with literature data reported. Daidzein (1), genistein (2) and gliricidin (3) inhibited α-glucosidase in vitro with IC50 values of 174.2, 36.1 and 47.4 μM, respectively, more potent than the positive control, acarbose. Docking study revealed that the amino acid residue Thr 215 is the essential binding site for active ligands 2...
December 26, 2016: Natural Product 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
#14
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/27994477/acarbose-promotes-remission-of-both-early-and-late-dumping-syndromes-in-post-bariatric-patients
#15
Flavio A Cadegiani, Osvalmir Sá Silva
OBJECTIVE: Acarbose is a glucosidase inhibitor that slows carbohydrate digestion. It could thus be effective to promote remission of dumping syndrome (DS). Previous studies associating acarbose and late dumping, although not early dumping, have been reported. Herein, we aimed to evaluate the role of acarbose in dumping syndrome prevention and treatment and in resistive exercises resistance in bariatric subjects. METHODS: Bariatric patients with DS and complete adherence to diet plan and resistive exercises were included (n=25)...
2016: Diabetes, Metabolic Syndrome and Obesity: Targets and Therapy
https://www.readbyqxmd.com/read/27994440/use-of-bedaquiline-and-delamanid-in-diabetes-patients-clinical-and-pharmacological-considerations
#16
REVIEW
Minhui Hu, Chunlan Zheng, Feng Gao
Antituberculosis (anti-TB) treatment may be affected by both diabetes and hypoglycemic agents in patients with these 2 comorbidities. However, data supporting this conclusion relate only to standard anti-TB therapies. Sirturo(®) (bedaquiline) and Deltyba(®) (delamanid), novel drugs for multidrug-resistant tuberculosis (MDR-TB), are recommended for diabetes patients when another effective treatment regimen cannot be provided. Currently, there are no clinical data related to the use of these agents in diabetes patients...
2016: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/27974904/evaluation-of-a-standardized-extract-from-morus-alba-against-%C3%AE-glucosidase-inhibitory-effect-and-postprandial-antihyperglycemic-in-patients-with-impaired-glucose-tolerance-a-randomized-double-blind-clinical-trial
#17
Seung Hwan Hwang, Hong Mei Li, Soon Sung Lim, Zhiqiang Wang, Jae-Seung Hong, Bo Huang
To evaluate the antihyperglycemic effect of a standardized extract of the leaves of Morus alba (SEMA), the present study was designed to investigate the α-glucosidase inhibitory effect and acute single oral toxicity as well as evaluate blood glucose reduction in animals and in patients with impaired glucose tolerance in a randomized double-blind clinical trial. SEMA was found to inhibit α-glucosidase at a fourfold higher level than the positive control (acarbose), in a concentration-dependent manner. Moreover, blood glucose concentration was suppressed by SEMA in vivo...
2016: Evidence-based Complementary and Alternative Medicine: ECAM
https://www.readbyqxmd.com/read/27973207/cost-effectiveness-of-saxagliptin-versus-acarbose-as-second-line-therapy-in-type-2-diabetes-in-china
#18
S Gu, H Shao, Y Zeng, L Shi, H Dong
No abstract text is available yet for this article.
November 2016: Value in Health: the Journal of the International Society for Pharmacoeconomics and Outcomes Research
https://www.readbyqxmd.com/read/27973204/cost-effectiveness-of-dapagliflozin-versus-acarbose-as-a-monotherapy-in-type-2-diabetes-in-china
#19
S Gu, H Dong
No abstract text is available yet for this article.
November 2016: Value in Health: the Journal of the International Society for Pharmacoeconomics and Outcomes Research
https://www.readbyqxmd.com/read/27941053/patient-characteristics-related-to-metabolic-disorders-and-chronic-complications-in-type-2-diabetes-mellitus-patients-hospitalized-at-the-qingdao-endocrine-and-diabetes-hospital-from-2006-to-2012-in-china
#20
Yanhu Dong, Weiguo Gao, Lei Zhang, Jia Wei, Niklas Hammar, Claudia S Cabrera, Xiaoli Wu, Qing Qiao
OBJECTIVE: To study the clinical characteristics related to metabolic disorders and complications in type 2 diabetes mellitus patients hospitalized in the Qingdao Endocrine and Diabetes Hospital from 2006 to 2012 in Qingdao, China. PATIENT POPULATION AND METHODS: Data from 14,289 (51% males) type 2 diabetes mellitus patients hospitalized between 2006 and 2012 were collected and analysed. Information on patients' demographic, anthropometric, laboratory and disease histories were extracted from electronic medical records...
January 2017: Diabetes & Vascular Disease Research
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