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glibenclamide

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https://www.readbyqxmd.com/read/29316509/synthesis-molecular-modelling-studies-and-adme-prediction-of-benzothiazole-clubbed-oxadiazole-mannich-bases-and-evaluation-of-their-anti-diabetic-activity-through-in-vivo-model
#1
Rubina Bhutani, Dharam Pal Pathak, Garima Kapoor, Asif Husain, Ravi Kant, Md Azhar Iqbal
A small library of new benzothiazole clubbed oxadiazole-Mannich bases (M-1 to M-22) were synthesized and characterized by IR, NMR, Mass and Elemental analysis results. Molecular docking studies were done to assess the binding mode and interactions of synthesized hits at binding site of receptor Peroxisome proliferator-activated receptor, PPAR-γ or PPARG (PDB 1FM9). Among the synthesized compounds, nine compounds were selected on the basis of docking score and evaluated for their in vivo anti-diabetic activity using Oral Glucose Tolerance Test (OGTT) in normal rats followed by Streptozotocin (STZ) - induced diabetes...
January 3, 2018: Bioorganic Chemistry
https://www.readbyqxmd.com/read/29309877/development-of-a-mechanistic-biokinetic-model-for-hepatic-bile-acid-handling-to-predict-possible-cholestatic-effects-of-drugs
#2
Sylvia Notenboom, Karl M Weigand, Johannes H Proost, Marola M van Lipzig, Evita van de Steeg, Petra H H van den Broek, Rick Greupink, Frans G M Russel, Geny M M Groothuis
Drug-induced liver injury (DILI) is a common reason for drug withdrawal from the market. An important cause of DILI is drug-induced cholestasis. One of the major players involved in drug-induced cholestasis is the bile salt efflux pump (BSEP; ABCB11). Inhibition of BSEP by drugs potentially leads to cholestasis due to increased (toxic) intrahepatic concentrations of bile acids with subsequent cell injury. In order to investigate the possibilities for in silico prediction of cholestatic effects of drugs, we developed a mechanistic biokinetic model for human liver bile acid handling populated with human in vitro data...
January 5, 2018: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29307659/atp-sensitive-potassium-channel-inhibitor-glibenclamide-attenuates-hpa-axis-hyperactivity-depression-and-anxiety-related-symptoms-in-a-rat-model-of-alzheimer-s-disease
#3
Mohammad Hossein Esmaeili, Behnam Bahari, Ali-Akbar Salari
Affective disorders including depression and anxiety are among the most prevalent behavioral abnormalities in patients with Alzheimer's disease (AD), which affect the quality of life and progression of the disease. Dysregulation of the hypothalamic-pituitary-adrenal-(HPA) axis has been reported in affective disorders and AD. Recent studies revealed that current antidepressant drugs are not completely effective for treating anxiety- and depression-related disorders in people with dementia. ATP-sensitive-potassium-(KATP) channels are well-known to be involved in AD pathophysiology, HPA axis function and the pathogenesis of depression and anxiety-related behaviors...
January 4, 2018: Brain Research Bulletin
https://www.readbyqxmd.com/read/29305569/emergence-of-insulin-resistance-following-empirical-glibenclamide-therapy-a-case-report-of-neonatal-diabetes-with-a-recessive-ins-gene-mutation
#4
Melek Yildiz, Teoman Akcay, Banu Aydin, Abdurrahman Akgun, Beyza Belde Dogan, Elisa De Franco, Sian Ellard, Hasan Onal
BACKGROUND: As KATP channel mutations are the most common cause of neonatal diabetes mellitus (NDM) and patients with these mutations can be treated with oral sulfonylureas, empiric therapy is a common practice for NDM patients. CASE PRESENTATION: A non-syndromic, small for gestational age baby born to first-degree consanguineous parents was diagnosed with NDM. Because of hypo- and hyperglycemic episodes and variability in insulin requirement, we initiated a trial of glibenclamide, with a presumptive diagnosis of NDM caused by a KATP channel mutation...
January 6, 2018: Journal of Pediatric Endocrinology & Metabolism: JPEM
https://www.readbyqxmd.com/read/29291445/design-synthesis-and-biological-evaluation-of-novel-ring-opened-cromakalim-analogues-with-relaxant-effects-on-vascular-and-respiratory-smooth-muscles-and-as-stimulators-of-elastin-synthesis
#5
Mourad Bouhedja, Basile Peres, Wassim Fhayli, Zeinab Ghandour, Ahcène Boumendjel, Gilles Faury, Smail Khelili
Two new series of ring-opened analogues of cromakalim bearing sulfonylurea moieties (series A: with N-unmethylated sulfonylureas, series B: with N-methylated sulfonylureas) were synthesized and tested as relaxants of vascular and respiratory smooth muscles (rat aorta and trachea, respectively). Ex vivo biological evaluations indicated that the most active compounds, belonging to series B, displayed a marked vasorelaxant activity on endothelium-intact aortic rings and the trachea. A majority of series B compounds exhibited a higher vasorelaxant activity (EC50 < 22 μM) than that of the reference compound diazoxide (EC50 = 24 μM)...
December 21, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29281328/altered-potassium-ion-channel-function-as-a-possible-mechanism-of-increased-blood-pressure-in-rats-fed-thermally-oxidized-palm-oil-diets
#6
Etah E Nkanu, Daniel U Owu, Eme E Osim
Intake of thermally oxidized palm oil leads to cytotoxicity and alteration of the potassium ion channel function. This study investigated the effects of fresh and thermally oxidized palm oil diets on blood pressure and potassium ion channel function in blood pressure regulation. Male Wistar rats were randomly divided into three groups of eight rats. Control group received normal feed; fresh palm oil (FPO) and thermally oxidized palm oil (TPO) groups were fed a diet mixed with 15% (weight/weight) fresh palm oil and five times heated palm oil, respectively, for 16 weeks...
December 27, 2017: Journal of Dietary Supplements
https://www.readbyqxmd.com/read/29279019/ameliorative-activity-of-ethanol-extract-of-artocarpus-heterophyllus-stem-bark-on-pancreatic-%C3%AE-cell-dysfunction-in-alloxan-induced-diabetic-rats
#7
Basiru O Ajiboye, Oluwafemi A Ojo, Oluwatosin Adeyonu, Oluwatosin D Imiere, Adewale O Fadaka, Adetutu O Osukoya
This study sought to investigate the ameliorative effects of ethanol extract Artocarpus heterophyllus (EAH) in alloxan-induced diabetic rats. The rats were divided into 6 groups, with groups 1 and 2 serving as nondiabetic and diabetic control, respectively; group 3 serving as diabetic rats treated with 5 mg/kg glibenclamide; and groups 4 to 6 were diabetic rats treated with 50, 100, and 150 mg/kg of EAH, respectively. Assays determined were serum insulin, lipid peroxidation, and antioxidant enzyme activities...
October 2017: Journal of Evidence-based Complementary & Alternative Medicine
https://www.readbyqxmd.com/read/29277019/coencapsulation-of-cyclodextrins-into-poly-anhydride-nanoparticles-to-improve-the-oral-administration-of-glibenclamide-a-screening-on-c-elegans
#8
David Lucio, María Cristina Martínez-Ohárriz, Carlos J González-Navarro, David Navarro-Herrera, Gustavo González-Gaitano, Aurel Radulescu, Juan M Irache
This work describes the feasibility of poly(anhydride) nanoparticles as carriers for the oral administration of glibenclamide (GB) as well as the in vivo evaluation of their hypolipidemic effect in a C. elegans model. For this purpose, and in order to increase the GB payload, the drug was encapsulated in nanoparticles in presence of cyclodextrins (either βCD or HPβCD). The optimized nanoparticles displayed a size of about 220 nm and a negative zeta potential (-40 mV), with a drug loading up to 52 μg/mg...
December 21, 2017: Colloids and Surfaces. B, Biointerfaces
https://www.readbyqxmd.com/read/29275331/cantu-syndrome-associated-sur2-abcc9-mutations-in-distinct-structural-domains-result-in-katp-channel-gain-of-function-by-differential-mechanisms
#9
Conor McClenaghan, Alex Hanson, Monica Sala-Rabanal, Helen I Roessler, Dragana Josifova, Dorothy K Grange, Gijs van Haaften, Colin G Nichols
The complex cardiovascular disorder Cantu syndrome (CS) arises from gain-of-function mutations in either KCNJ8 or ABCC9, the genes encoding the Kir6.1 and SUR2 subunits of ATP-sensitive potassium (KATP) channels, respectively. Recent reports indicate that such mutations can increase channel activity by multiple molecular mechanisms. In this study, we determined the mechanism by which KATP function is altered by several substitutions in distinct structural domains of SUR2: D207E in the intracellular L0-linker and Y985S, G989E, M1060I, and R1154Q/W in TMD2...
December 22, 2017: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/29260608/tonic-regulation-of-middle-meningeal-artery-diameter-by-atp-sensitive-potassium-channels
#10
Arsalan U Syed, Masayo Koide, Joseph E Brayden, George C Wellman
Activation of ATP-sensitive potassium (KATP) channels in arterial smooth muscle (ASM) contributes to vasodilation evoked by a variety of endogenous and exogenous compounds. Although controversial, activation of KATP channels by neuropeptides such as calcitonin gene-related peptide (CGRP) and pituitary adenylate cyclase activating peptide (PACAP) in the trigeminovascular system, including the middle meningeal artery (MMA), has been linked to migraine headache. The objective of the current study was to determine if ongoing KATP channel activity also influences MMA diameter...
January 1, 2017: Journal of Cerebral Blood Flow and Metabolism
https://www.readbyqxmd.com/read/29239973/involvement-of-adenosine-triphosphate-sensitive-potassium-channels-in-the-neuroprotective-activity-of-hydrogen-sulfide-in-the-6-hydroxydopamine-induced-animal-model-of-parkinson-s-disease
#11
Mohammad Reza Sarookhani, Hashem Haghdoost-Yazdi, Ali Sarbazi-Golezari, Arvin Babayan-Tazehkand, Nafiseh Rastgoo
Studies have shown that hydrogen sulfide (H2S) exerts a neuroprotective effect and may have a therapeutic value for treating neurodegenerative diseases including Parkinson's disease. However, little is known about the mechanisms underlying the neuroprotective activity of H2S in vivo. Here, we evaluated the effect of glibenclamide, an ATP-sensitive potassium channel blocker, on the neuroprotective activity of H2S in the 6-hydroxydopamine (6-OHDA) animal model of Parkinson's disease. 6-OHDA was administered by stereotaxic surgery into the medial forebrain bundle...
December 12, 2017: Behavioural Pharmacology
https://www.readbyqxmd.com/read/29224994/antitussive-and-expectorant-activities-of-licorice-and-its-major-compounds
#12
Yi Kuang, Bin Li, Jingran Fan, Xue Qiao, Min Ye
Licorice has been used as an antitussive and expectorant herbal medicine for a long history. This work evaluated the activities of 14 major compounds and crude extracts of licorice, using the classical ammonia-induced cough model and phenol red secretion model in mice. Liquiritin apioside (1), liquiritin (2), and liquiritigenin (3) at 50 mg/kg (i.g.) could significantly decrease cough frequency by 30-78% (p < .01). The antitussive effects could be partially antagonized by the pretreatment of methysergide or glibenclamide, but not naloxone...
December 2, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/29222687/chrysophyllum-cainito-apple-star-a-fruit-with-gastroprotective-activity-in-experimental-ulcer-models
#13
Roseane Leandra da Rosa, Camila Leandra de Almeida, Lincon Bordigon Somensi, Thaise Boeing, Luisa Nathália Bolda Mariano, Clarissa de Medeiros Amorim Krueger, Priscila de Souza, Valdir Cechinel Filho, Luisa Mota da Silva, Sérgio Faloni de Andrade
The gastroprotective potential of the methanolic extracts from peels (MEPe), seeds (MESe) and pulp (MEPu) of Chrysophyllum cainito L. (Sapotaceae) fruits was evaluated in mice using ethanol/HCl- and indomethacin-induced ulcer, as well as the antiulcer effect of the juice and flour from this fruit. The lowest oral gastroprotective dose of MEPe, MESe and MEPu against ethanol/HCl was 3, 3 and 10 mg/kg, respectively. Moreover, all extracts increased mucin secretion at 176, 198 and 193%. Intraperitoneal administration of MEPe (0...
December 8, 2017: Inflammopharmacology
https://www.readbyqxmd.com/read/29205356/molecular-and-functional-characterization-of-inwardly-rectifying-k-currents-in-murine-proximal-colon
#14
Xu Huang, Si Hyung Lee, Hongli Lu, Kenton M Sanders, Sang Don Koh
Membrane potentials of gastrointestinal (GI) muscles are important because voltage dependent Ca2+ channels in smooth muscle cells (SMC) provide the Ca2+ that triggers contraction. Regulation of membrane potential is complicated because SMC are electrically coupled to interstitial cells of Cajal (ICC) and PDGFRα+ cells. Activation of conductances in any of these cells affects the excitability of the syncytium. We explored the role of inward rectifier K+ conductances in colonic ICC that might contribute to regulation of membrane potential...
December 3, 2017: Journal of Physiology
https://www.readbyqxmd.com/read/29201919/dynamics-of-insulin-secretion-from-endoc-%C3%AE-h1-%C3%AE-cell-pseudoislets-in-response-to-glucose-and-other-nutrient-and-nonnutrient-secretagogues
#15
Hiroki Teraoku, Sigurd Lenzen
The dynamics of insulin secretion were characterized in response to a variety of physiological and pharmacological stimulators and other compounds in perifused pseudoislets generated from cells of the EndoC-βH1 β-cell line. Perifusion of EndoC-βH1 pseudoislets with the physiological stimulus glucose (16.7 mM) induced sustained insulin secretion, which was inhibited by mannoheptulose. The adenylate cyclase activators IBMX and forskolin strongly potentiated this secretion. Glibenclamide, a Kir 6.2 potassium channel blocker, and Bay K 8644, an opener of the voltage-sensitive Ca2+ channel, also potentiated glucose-induced insulin secretion...
2017: Journal of Diabetes Research
https://www.readbyqxmd.com/read/29201366/survey-on-the-availability-price-and-affordability-of-selected-essential-medicines-for-non-communicable-diseases-in-community-pharmacies-of-kathmandu-valley
#16
Rajeev Shrestha, Anish Ghale, Bijay Raj Chapagain, Mahasagar Gyawali, Trishna Acharya
Background: The access to essential medicines for non-communicable disease treatment is unacceptably low worldwide. The fundamental right to health cannot be fulfilled without equitable access to essential medicines. Methodology: A cross-sectional study was carried out in 94 community pharmacies of Kathmandu valley. Non-probability quota sampling method was adopted for the purpose. Village Development Committees with more than 5000 populations were included in the study...
2017: SAGE Open Medicine
https://www.readbyqxmd.com/read/29200904/taurine-relaxes-human-radial-artery-through-potassium-channel-opening-action
#17
Kemal Gokhan Ulusoy, Erkan Kaya, Kubilay Karabacak, Melik Seyrek, İbrahim Duvan, Vedat Yildirim, Oguzhan Yildiz
The vascular actions and mechanisms of taurine were investigated in the isolated human radial artery (RA). RA rings were suspended in isolated organ baths and tension was recorded isometrically. First, a precontraction was achieved by adding potassium chloride (KCl, 45 mM) or serotonin (5-hydroxytryptamine, 5-HT, 30 µM) to organ baths. When the precontractions were stable, taurine (20, 40, 80 mM) was added cumulatively. Antagonistic effect of taurine on calcium chloride (10 µM to 10 mM)-induced contractions was investigated...
November 2017: Korean Journal of Physiology & Pharmacology
https://www.readbyqxmd.com/read/29197370/tocolytic-action-and-underlying-mechanism-of-galetin-3-6-dimethyl-ether-on-rat-uterus
#18
Juliana da Nóbrega Carreiro, Iara Leão Luna de Souza, Joedna Cavalcante Pereira, Luiz Henrique César Vasconcelos, Rafael de Almeida Travassos, Barbara Viviana de Oliveira Santos, Bagnólia Araújo da Silva
BACKGROUND: Galetin 3,6-dimethyl ether (FGAL) is a flavonoid isolated from aerial parts of Piptadenia stipulacea. Previously, FGAL was shown to inhibit both carbachol- and oxytocin-induced phasic contractions in the rat uterus, which was more potent with oxytocin. Thus, in this study, we aimed to investigate the tocolytic action mechanism of FGAL on the rat uterus. METHODS: Segments of rat uterus ileum were suspended in organ bath containing modified Locke-Ringer solution at 32 °C, bubbled with carbogen mixture under a resting tension of 1 g...
December 2, 2017: BMC Complementary and Alternative Medicine
https://www.readbyqxmd.com/read/29196125/prescription-patterns-and-costs-of-antidiabetic-medications-in-a-large-group-of-patients
#19
Andrés Gaviria-Mendoza, Jorge Andrés Sánchez-Duque, Diego Alejandro Medina-Morales, Jorge Enrique Machado-Alba
AIMS: To determine the prescription patterns of antidiabetic medications and the variables associated with their use in a Colombian population. METHODS: A cross-sectional study using a systematized database of approximately 3.5 million affiliates of the Colombian Health System. Patients of both genders and all ages treated uninterruptedly with antidiabetic medications for three months (June-August 2015) were included. A database was designed that included sociodemographic, pharmacological, comedication, and cost variables...
November 28, 2017: Primary Care Diabetes
https://www.readbyqxmd.com/read/29193528/-epicatechin-induced-relaxation-of-isolated-human-saphenous-vein-roles-of-k-and-ca2-channels
#20
Marija Marinko, Goran Jankovic, Dragoslav Nenezic, Predrag Milojevic, Ivan Stojanovic, Vladimir Kanjuh, Aleksandra Novakovic
In this study, we aimed to investigate relaxant effect of flavanol (-)-epicatechin on the isolated human saphenous vein (HSV), as a part of its cardioprotective action, and to define the mechanisms underlying this vasorelaxation. (-)-Epicatechin induced a concentration-dependent relaxation of HSV pre-contracted by phenylephrine. Among K+ channel blockers, 4-aminopyridine, margatoxin, and iberiotoxin significantly inhibited relaxation of HSV, while glibenclamide considerably reduced effects of the high concentrations of (-)-epicatechin...
November 29, 2017: Phytotherapy Research: PTR
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