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https://www.readbyqxmd.com/read/28334715/potassium-channel-independent-relaxing-influence-of-adipose-tissue-on-mouse-carotid-artery
#1
Marta Laskowski, Cathrin Andersson, Emilie Eliasson, Veronika Golubinskaya, Holger Nilsson
Since the cardiovascular consequences of obesity reportedly vary in different types of obesity, we investigated the influence of adipose tissue from different locales on the phenylephrine-induced tone of the mouse carotid artery. Vessels were mounted in a Mulvany-Halpern-type wire myograph, and adipose tissue, from the back (brown) or mesenteric or inguinal subcutaneous (white), was placed around the artery. Contractile responses to phenylephrine were not affected by brown adipose tissue but were reduced (p < 0...
March 24, 2017: Journal of Vascular Research
https://www.readbyqxmd.com/read/28332266/11-12-epoxyeicosatrienoic-acid-induces-vasodilator-response-in-the-rat-perfused-mesenteric-vasculature
#2
S M Bihzad, M H M Yousif
Epoxyeicosatrienoic acids (EETs) are endogenous ligands that undergo hydrolysis by soluble epoxide hydrolase (sEH). The responses of 11, 12-EET in comparison with other vasodilator agonists including carbachol and sodium nitroprusside (SNP) were investigated. The effect of 1-cyclohexyl-3-dodecyl urea (CDU), a sEH, was tested on the vasodilator effect induced by 11, 12-EET in the perfused mesenteric beds isolated from normo-glycaemic and type-1 STZ-diabetic rats. In the perfused mesenteric beds of control and diabetic animals, 11, 12-EET produced vasodilation in a dose-dependent manner...
January 2017: Autonomic & Autacoid Pharmacology
https://www.readbyqxmd.com/read/28332176/a-naphthoquinone-from-sinningia-canescens-inhibits-inflammation-and-fever-in-mice
#3
Luís A Lomba, Paulo H Vogt, Victor E P Souza, Mariane C G Leite-Avalca, Maria H Verdan, Maria Elida A Stefanello, Aleksander R Zampronio
We previously showed that plants from the genus Sinningia are a source of antiinflammatory and analgesic compounds with different mechanisms of action. The present study evaluated the antiinflammatory, antinociceptive, and antipyretic effects of a crude extract (CE) from Sinningia canescens, its fractions, and 6-methoxy-7-hydroxy-α-dunnione (MHD) in mice. These effects were evaluated using carrageenan (Cg)-induced paw edema, acetic acid- and formalin-induced nociception, mechanical hyperalgesia, lipopolysaccharide (LPS)-induced fever, and plasma cytokine levels...
March 22, 2017: Inflammation
https://www.readbyqxmd.com/read/28330524/rapid-simultaneous-separation-of-four-oral-antidiabetic-drugs-and-quantitative-determination-of-glibenclamide-using-conventional-and-fused-core-silica-columns
#4
Laura Maria Fontes Prado Moraes, Gerson Antônio Pianetti, Isabela da Costa César, Christian Fernandes
Diabetes mellitus is a chronic disease with high and growing prevalence worldwide. Therefore, the development of fast and efficient methods for the QC of antidiabetic drugs is of fundamental importance. Two ultra-fast methods, using a conventional (C18 100 × 2.1 mm, 5 μm fully porous particle) column or a fused-core (C18 100 × 2.1 mm, 2.7 μm fused-core particle) column, were developed for the simultaneous determination of four antidiabetic drugs (chlorpropamide, glibenclamide, gliclazide, and glimepiride)...
February 15, 2017: Journal of AOAC International
https://www.readbyqxmd.com/read/28322941/small-dosing-clinical-study-pharmacokinetic-pharmacogenomic-slco2b1-and-abcg2-and-interaction-atorvastatin-and-grapefruit-juice-profiles-of-five-probes-for-oatp2b1-and-bcrp
#5
Yushi Kashihara, Ichiro Ieiri, Takashi Yoshikado, Maeda Kazuya, Masato Fukae, Miyuki Kimura, Takeshi Hirota, Shunji Matsuki, Shin Irie, Noritomo Izumi, Hiroyuki Kusuhara, Yuichi Sugiyama
The aims of this study were (1) to investigate the effects of atorvastatin (10 mg, therapeutic dose) and grapefruit juice (GFJ), inhibitors of OATP2B1, on the pharmacokinetics of substrates for OATP2B1 and BCRP under oral small-dosing conditions (300 μg sulfasalazine, 250 μg rosuvastatin, 300 μg glibenclamide, 1200 μg celiprolol, and 600 μg sumatriptan), and (2) to evaluate the contribution of SLCO2B1*3 and ABCG2 c.421C>A polymorphisms to the pharmacokinetics of the five test drugs in 23 healthy volunteers...
March 17, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28322929/exogenous-h2s-prevents-high-glucose-induced-damage-to-osteoblasts-through-regulation-of-katp-channels
#6
Yuanyuan Liu, Jianyong Liu, Xin Li, Fantao Wang, Xin Xu, Chunling Wang
Association between diabetes and osteoporosis has been extensively investigated. However, whether the effects of H2S on osteoblast function under high glucose (HG) condition relate to ATP-sensitive potassium (KATP) channels is unclear. To investigate the effects of H2S on the proliferation, apoptosis, and mineralization of osteoblasts under HG condition, and to observe whether H2S exert this effect through the KATP channels. Primary osteoblasts (POBs) were obtained from the calvaria of Sprague-Dawley rats. Cells were pre-treated with 400 μmol/L NaHS (a H2S donor), and/or 0...
March 16, 2017: Biochimie
https://www.readbyqxmd.com/read/28322830/antidiabetic-antidyslipidemic-and-toxicity-profile-of-env-2-a-potent-pyrazole-derivative-against-diabetes-and-related-diseases
#7
Eduardo Hernández-Vázquez, Hugo Ocampo-Montalban, Litzia Cerón-Romero, Miguel Cruz, Jaime Gomez-Zamudio, Guadalupe Hiriart-Valencia, Rafael Villalobos-Molina, Angelica Flores-Flores, Samuel Estrada-Soto
Diabetes is a major health problem and a predisposition factor for further degenerative complications and, therefore, novel therapies are urgently needed. Currently, cannabinoid receptor 1 (CB1 receptor) antagonists have been considered as promissory entities for metabolic disorders treatment. Accordingly, the purpose of this work was the evaluation of the sub-acute antidiabetic, anti-hyperglycemic, antidyslipidemic and toxicological profile of ENV-2, a potent hypoglycemic and antioxidant CB1 receptor antagonist...
March 17, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28321889/antihyperglycaemic-activity-of-the-methanol-extract-from-leaves-of-eremophila-maculata-scrophulariaceae-in-streptozotocin-induced-diabetic-rats
#8
Fadia S Youssef, Mohamed L Ashour, Sherif S Ebada, Mansour Sobeh, Hesham A El-Beshbishy, Abdel Nasser Singab, Michael Wink
OBJECTIVES: This study was designed to evaluate the antihyperglycaemic activity of the methanol leaf extract of Eremophila maculata (EMM) both in vitro and in vivo. METHODS: The antihyperglycaemic activity was assessed in vitro using differentiated 3T3-L1 adipocytes, whereas in-vivo effect was evaluated in streptozotocin-induced diabetic rats. Chemical profiling of EMM was done using LC-ESI-MS techniques. Molecular modelling experiments of the identified compounds were performed using C-Docker protocol...
March 21, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28320833/inflammatory-changes-in-bone-marrow-microenvironment-associated-with-declining-b-lymphopoiesis
#9
Domenick E Kennedy, Katherine L Knight
B lymphopoiesis arrests precipitously in rabbits such that by 2-4 mo of age, before sexual maturity, little to no B lymphopoiesis occurs in the bone marrow (BM). Previously, we showed that in mice, adipocytes inhibit B lymphopoiesis in vitro by inducing inflammatory myeloid cells, which produce IL-1β. In this study, we characterized rabbit BM after the arrest of B lymphopoiesis and found a dramatic increase in fat, increased CD11b(+) myeloid cells, and upregulated expression of the inflammatory molecules, IL-1β and S100A9, by the myeloid cells...
March 20, 2017: Journal of Immunology: Official Journal of the American Association of Immunologists
https://www.readbyqxmd.com/read/28319297/tandem-coupling-of-azide-with-isonitrile-and-boronic-acid-facile-access-to-functionalized-amidines
#10
Zhen Zhang, Baoliang Huang, Guanyu Qiao, Liu Zhu, Fan Xiao, Feng Chen, Bin Fu, Zhenhua Zhang
Amidine is a notable nitrogen-containing structural motif found in bioactive natural products and pharmaceuticals. Herein, a novel rhodium(I)-catalyzed tandem reaction of readily accessible azides with isonitriles and boronic acids via a carbodiimide intermediate is achieved. This protocol offers an alternative approach toward N-sulfonyl-, N-acyl-, and N- phosphoryl-functionalized, as well as general N-aryl and N-alkyl amidines with broad substrate scope. In addition, functionalized guanidines can also been synthesized when amines are used instead...
March 20, 2017: Angewandte Chemie
https://www.readbyqxmd.com/read/28306534/ameliorative-potential-of-blighia-sapida-k-d-koenig-bark-against-pancreatic-%C3%AE-cell-dysfunction-in-alloxan-induced-diabetic-rats
#11
Oluwafemi Adeleke Ojo, Basiru Olaitan Ajiboye, Adebola Busola Ojo, Babatunji Emmanuel Oyinloye, Oluwatosin Debbie Imiere, Oluwatosin Adeyonu
Background In West Africa, the fruit, seed, leaf and stem of Blighia sapida K.D. Koenig are commonly used as remedy against a variety of diseases, including diabetes mellitus. This study investigated the ameliorative potential of B. sapida K.D. Koenig stem bark ethanol extract against pancreatic β-cell dysfunction in diabetic rats. Methods Diabetes was induced by intraperitoneal injection of alloxan (65 mg/kg body weight) for 21 days, and orally administered with glibenclamide (5 mg/kg body weight), 50-150 mg/kg body weight of B...
March 17, 2017: Journal of Complementary & Integrative Medicine
https://www.readbyqxmd.com/read/28306532/evaluation-of-the-sub-chronic-toxicity-profile-of-the-corm-of-xanthosoma-sagittifolium-on-hematology-and-biochemistry-of-alloxan-induced-diabetic-wistar-rats
#12
Olayinka A Oridupa, Oluyemisi F Folasire, Adedotun J Owolabi
Background Hematological and biochemical changes associated with diabetes mellitus and probable reversal were assessed in alloxan-induced diabetic Wistar rats fed with varied percentages of Xanthosoma sagittifolium corm feed (Xs). The changes were compared to normoglycemic rats and diabetic rats treated with glibenclamide. Methods The study had eight groups in all with group 8 (control) consisting of five normoglycemic rats fed with normal rat pellets (Nrp). Diabetes was experimentally induced by intraperitoneal injection of alloxan to normoglycemic rats...
March 11, 2017: Journal of Complementary & Integrative Medicine
https://www.readbyqxmd.com/read/28291959/the-opening-of-atp-sensitive-k-channels-protects-h9c2-cardiac-cells-against-the-high-glucose-induced-injury-and-inflammation-by-inhibiting-the-ros-tlr4-necroptosis-pathway
#13
Weijie Liang, Meiji Chen, Dongdan Zheng, Jianhao Li, Mingcai Song, Wenzhu Zhang, Jianqiang Feng, Jun Lan
BACKGROUND/AIMS: Hyperglycemia activates multiple signaling molecules, including reactive oxygen species (ROS), toll-like receptor 4 (TLR4), receptor-interacting protein 3 (RIP3, a kinase promoting necroptosis), which mediate hyperglycemia-induced cardiac injury. This study explored whether inhibition of ROS-TLR4-necroptosis pathway contributed to the protection of ATP-sensitive K+ (KATP) channel opening against high glucose-induced cardiac injury and inflammation. METHODS: H9c2 cardiac cells were treated with 35 mM glucose (HG) to establish a model of HG-induced insults...
February 22, 2017: Cellular Physiology and Biochemistry
https://www.readbyqxmd.com/read/28288617/the-effect-of-pomegranate-fresh-juice-versus-pomegranate-seed-powder-on-metabolic-indices-lipid-profile-inflammatory-biomarkers-and-the-histopathology-of-pancreatic-islets-of-langerhans-in-streptozotocin-nicotinamide-induced-type-2-diabetic-sprague-dawley-rats
#14
Seyedeh Zeinab Taheri Rouhi, Md Moklesur Rahman Sarker, Asmah Rahmat, Saad Ahmed Alkahtani, Fauziah Othman
BACKGROUND: Type 2 diabetes mellitus (T2DM) is associated with hyperglycemia, inflammatory disorders and abnormal lipid profiles. Several functional foods have therapeutic potential to treat chronic diseases including diabetes. The therapeutic potential of pomegranate has been stated by multitudinous scientists. The present study aimed to evaluate the effects of pomegranate juice and seed powder on the levels of plasma glucose and insulin, inflammatory biomarkers, lipid profiles, and health of the pancreatic islets of Langerhans in streptozotocin (STZ)-nicotinamide (NAD) induced T2DM Sprague Dawley (SD) rats...
March 14, 2017: BMC Complementary and Alternative Medicine
https://www.readbyqxmd.com/read/28270043/roles-of-atp-sensitive-potassium-channel-in-modulating-gastric-tone-and-accommodation-in-dogs
#15
Shiying Li, Yong Lei, Jiande Dz Chen
OBJECTIVE: The ATP sensitive potassium (KATP) channel plays an important role in the regulation of resting membrane potential and membrane excitability. The role of the KATP channel in modulating gastric motility is unclear. The aim of this study was to investigate the role and mechanism of the KATP channel in modulating gastric tone and accommodation in dogs. MATERIALS AND METHODS: Gastric volume under a constant pressure reflecting gastric tone was measured using a barostat device in dogs equipped with a gastric cannula...
May 2017: Scandinavian Journal of Gastroenterology
https://www.readbyqxmd.com/read/28250659/antidiabetic-effects-of-aqueous-and-dichloromethane-methanol-stem-bark-extracts-of-pterocarpus-soyauxii-taub-papilionaceae-on-streptozotocin-induced-diabetic-rats
#16
Marie Claire Tchamadeu, Paul Désiré Djomeni Dzeufiet, Nelly Blaes, Jean-Pierre Girolami, Pierre Kamtchouing, Théophile Dimo
AIM OF THE STUDY: The aim is to evaluate the hypoglycemic and antidiabetic effects of aqueous and CH2Cl2/CH3OH stem bark extracts of Pterocarpus soyauxii Taub in normal and diabetic rats. MATERIALS AND METHODS: Streptozotocin (STZ)-induced diabetic and normal adult Wistar rats were orally administered with aqueous and CH2Cl2/CH3OH plant extracts of P. soyauxii at various doses (38-300 mg/kg) in a single administration. In addition, STZ-induced diabetic rats received prolonged daily administration for 14 days...
January 2017: Pharmacognosy Research
https://www.readbyqxmd.com/read/28245258/doxorubicin-induced-oxidative-stress-the-protective-effect-of-nicorandil-on-hl-1-cardiomyocytes
#17
Mari C Asensio-López, Fernando Soler, Domingo Pascual-Figal, Francisco Fernández-Belda, Antonio Lax
The primary cardiotoxic action of doxorubicin when used as antitumor drug is attributed to the generation of reactive oxygen species (ROS) therefore effective cardioprotection therapies are needed. In this sense, the antianginal drug nicorandil has been shown to be effective in cardioprotection from ischemic conditions but the underlying molecular mechanism to cope with doxorubicin-induced ROS is unclear. Our in vitro study using the HL-1 cardiomyocyte cell line derived from mouse atria reveals that the endogenous nitric oxide (NO) production was stimulated by nicorandil and arrested by NO synthase inhibition...
2017: PloS One
https://www.readbyqxmd.com/read/28213290/zd0947-a-sulphonylurea-receptor-modulator-detects-functional-sulphonylurea-receptor-subunits-in-murine-vascular-smooth-muscle-atp-sensitive-k-channels
#18
Tadashi Yamamoto, Kohei Takahara, Keiichiro Uchida, Noriyoshi Teramoto
In order to identify functional sulphonylurea receptor (SUR.x) subunits of native ATP-sensitive K(+) channels (KATP channels) in mouse portal vein, the effects of ZD0947, a SUR.x modulator, were investigated on spontaneous portal vein contractions, macroscopic membrane currents and unitary currents recorded (using patch-clamp techniques) in freshly dispersed mouse portal vein myocytes. Spontaneous contractions in mouse portal vein were reversibly reduced by ZD0947 in a concentration-dependent manner (Ki =293nM)...
April 5, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28207836/tmg-123-a-novel-glucokinase-activator-exerts-durable-effects-on-hyperglycemia-without-increasing-triglyceride-in-diabetic-animal-models
#19
Yoshinori Tsumura, Yu Tsushima, Azusa Tamura, Makiko Hasebe, Masanobu Kanou, Hirotsugu Kato, Tsunefumi Kobayashi
Glucokinase (GK) plays a critical role for maintaining glucose homeostasis with regulating glucose uptake in liver and insulin secretion in pancreas. GK activators have been reported to decrease blood glucose levels in patients with type 2 diabetes mellitus. However, clinical development of GK activators has failed due to the loss of glucose-lowering effects and increased plasma triglyceride levels after chronic treatment. Here, we generated a novel GK activator, TMG-123, examined its in vitro and in vivo pharmacological characteristics, and evaluated its risks of aforementioned clinical issues...
2017: PloS One
https://www.readbyqxmd.com/read/28192880/ameliorating-effect-of-betanin-a-natural-chromoalkaloid-by-modulating-hepatic-carbohydrate-metabolic-enzyme-activities-and-glycogen-content-in-streptozotocin-nicotinamide-induced-experimental-rats
#20
Indumathi Dhananjayan, Sujithra Kathiroli, Srinivasan Subramani, Vinothkumar Veerasamy
Betanin, a chromoalkaloid of beetroot, has shown significant biological effects of antioxidants, anti-inflammatory and anticarcinogenic activities. So, we attempted to determine whether betanin (a natural pigment) would be protective against hyperglycemia in streptozotocin (STZ) - nicotinamide (NA) induced diabetic rats. Rats were injected with STZ (40mg/kgb.w.) 15 mins after the administration of NA (110mg/kgb.w.) by intraperitonially (i.p.) 30days for the induction of experimental diabetes mellitus. After 72h diabetic rats were treated with betanin orally at a doses of 10, 20 and 40mg/kg b...
April 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
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