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https://www.readbyqxmd.com/read/28706420/maytenus-erythroxylon-reissek-celastraceae-ethanol-extract-presents-antidiarrheal-activity-via-antimotility-and-antisecretory-mechanisms
#1
Rodrigo de Oliveira Formiga, Zelma Glebya Maciel Quirino, Margareth de Fátima Formiga Melo Diniz, Alexsandro Fernandes Marinho, Josean Fechine Tavares, Leônia Maria Batista
AIM: To investigate the acute toxicity, phytochemical profile, antidiarrheal activity and mechanisms of action of Maytenus erythroxylon (M. erythroxylon) ethanol extract. METHODS: A castor oil-induced diarrhea model was used to evaluate antidiarrheal activity. Intestinal transit and gastric emptying protocols were used to evaluate a possible antimotility effect. KATP channels, nitric oxide, presynaptic α2-adrenergic and tissue adrenergic receptors were investigated to uncover antimotility mechanisms of action and castor oil-induced enteropooling to elucidate antisecretory mechanisms...
June 28, 2017: World Journal of Gastroenterology: WJG
https://www.readbyqxmd.com/read/28699234/investigation-of-morin-induced-insulin-secretion-in-cultured-pancreatic-cells
#2
Mang Hung Lin, Chia-Chen Hsu, Jenshinn Lin, Juei Tang Cheng, Ming Chang Wu
Morin is a flavonoid contained in guava that is known to reduce hyperglycemia in diabetes. Insulin secretion has been demonstrated to increase following the administration of morin. The present study is designed to investigate the potential mechanism(s) of morin-induced insulin secretion in the MIN6 cell line. First, we identified that morin induced a dose-dependent increase in insulin secretion and intracellular calcium content in MIN6 cells. Morin potentiated glucose-stimulated insulin secretion (GSIS). Additionally, we used siRNA for the ablation of imidazoline receptor protein (NISCH) expression in MIN6 cells...
July 12, 2017: Clinical and Experimental Pharmacology & Physiology
https://www.readbyqxmd.com/read/28697955/nesfatin-1-inhibits-voltage-gated-k-channels-in-pancreatic-beta-cells
#3
Yuko Maejima, Shoichiro Horita, Daisuke Kobayashi, Miho Aoki, Rie O'hashi, Ryota Imai, Kazuho Sakamoto, Masatomo Mori, Katsuya Takasu, Kazuma Ogawa, Seiichi Takenoshita, Songji Zhao, Akihiro Hazama, Kenju Shimomura
The anorexigenic neuropeptide NEFA/nucleobindin 2 (NUCB2)/nesfatin-1-containing neurons are distributed in the brain regions involved in feeding regulation. In spite of the growing knowledge of its physiological functions through extensive studies, its molecular mechanism of reaction, including its receptor, remains unknown. NUCB2/nesfatin-1 is also involved in various peripheral regulations, including glucose homeostasis. In pancreatic beta-cells, NUCB2/nesfatin-1 is reported to enhance glucose-stimulated insulin secretion (GSIS) but its exact mechanism remains unknown...
July 8, 2017: Peptides
https://www.readbyqxmd.com/read/28695353/cardioprotection-by-the-transfer-of-coronary-effluent-from-ischaemic-preconditioned-rat-hearts-identification-of-cardioprotective-humoral-factors
#4
Leonardo Maciel, Dahienne F de Oliveira, Giovani C Verissimo da Costa, Paulo M Bisch, Jose Hamilton Matheus Nascimento
Ischaemic preconditioning (IPC) provides myocardial resistance to ischaemia/reperfusion (I/R) injuries. The protection afforded by IPC is not limited to the target tissue but extends to remote tissues, suggesting a mechanism mediated by humoral factors. The aim of the present study was to identify the humoral factors that are responsible for the cardioprotection induced by the coronary effluent transferred from IPC to naïve hearts. Isolated rat hearts were submitted to IPC (three cycles of 5 min I/R) before 30-min global ischaemia and 60-min reperfusion...
September 2017: Basic Research in Cardiology
https://www.readbyqxmd.com/read/28685055/identification-of-genetic-variants-in-pharmacogenetic-genes-associated-with-type-2-diabetes-in-a-mexican-mestizo-population
#5
Nidia Samara Rodríguez-Rivera, Patricia Cuautle-Rodríguez, Fernando Castillo-Nájera, Juan Arcadio Molina-Guarneros
Type 2 diabetes mellitus (T2DM) is one of the most prevalent chronic pathologies in the world. In developing countries, such as Mexico, its prevalence represents an important public health and research issue. Determining factors triggering T2DM are environmental and genetic. While diet, exercise and proper weight control are the first measures recommended to improve the quality of life and life expectancy of patients, pharmacological treatment is usually the next step. Within every population there are variations in interindividual drug response, which may be due to genetic background...
July 2017: Biomedical Reports
https://www.readbyqxmd.com/read/28675783/insulin-and-leptin-excite-anorexigenic-proopiomelanocortin-neurons-via-activation-of-trpc5-channels
#6
REVIEW
Jian Qiu, Edward J Wagner, Oline K Rønnekleiv, Martin J Kelly
Proopiomelanocortin (POMC) neurons within the hypothalamic arcuate nucleus are vital anorexigenic neurons. Both the insulin receptor and leptin receptor are coupled to activation of phosphatidylinositide-3 kinase (PI3K) to regulate multiple functions that increase POMC neuronal excitability. Using whole-cell recording in several mammalian species, we have found that both insulin and leptin depolarized POMC neurons via activation of TRPC5 channels. TRPC5 channels have been rigorously characterized as the downstream effector based on their biophysical properties, pharmacological profile and localization by immunocytochemistry and scRT-PCR...
July 4, 2017: Journal of Neuroendocrinology
https://www.readbyqxmd.com/read/28672904/katp-channels-in-high-glucose-induced-rat-mesangial-cell-proliferation-and-release-of-mmp-2-and-fibronectin
#7
Bei Zhang, Yongquan Shi, Junjie Zou, Xiangfang Chen, Wei Tang, Fei Ye, Zhimin Liu
ATP-sensitive potassium (KATP) channels are well characterized in cardiac, pancreatic and many other muscle cells. The purpose of this study was to determine if KATP channels play a role in diabetic nephropathy (DN). In the present study, functional expression of the KATP channel was examined in rat mesangial cells with or without high glucose (HG) stimulation. The mesangial cell proliferation and the release of matrix metalloproteinase (MMP)-2 and fibronectin in response to high glucose with a selective opener of KATP (diazoxide, DZX), or with a selective inhibitor of KATP (5-hydroxydecanoate, 5-HD) were also measured...
July 2017: Experimental and Therapeutic Medicine
https://www.readbyqxmd.com/read/28667052/hearts-lacking-plasma-membrane-katp-channels-display-changes-in-basal-aerobic-metabolic-substrate-preference-and-ampk-activity
#8
Nermeen Youssef, Scott Campbell, Amy Barr, Manoj Gandhi, Beth Hunter, Vernon Dolinksy, Jason R B Dyck, Alexander S Clanachan, Peter E Light
Cardiac ATP-sensitive potassium (KATP) channels couple changes in cellular metabolism to membrane excitability and are activated during metabolic stress. Although under basal aerobic conditions, KATP channels are thought to be predominately closed. Despite intense research into the roles of KATP channels during metabolic stress, their contribution to aerobic basal cardiac metabolism has not been investigated previously. METHODS: Hearts from Kir6.2+/+ and Kir6.2 -/- mice were perfused in working mode and rates of glycolysis, fatty acid oxidation and glucose oxidation were measured...
June 30, 2017: American Journal of Physiology. Heart and Circulatory Physiology
https://www.readbyqxmd.com/read/28656565/arrhythmia-vulnerability-in-diabetic-cardiac-tissue-is-species-dependent-effects-of-i-katp-uncoupling-and-connexin-lateralization
#9
A Ghazanfari, E Vigmond, A Nygren
Amongst the complications of diabetes is arrhythmia, the risk of which depends on multiple factors. This study was designed to investigate several factors, including the effects of ATP-sensitive potassium current, lateralized connexins, and gap junction uncoupling. ATP-sensitive potassium channel (I KATP) opening is caused by ischemia, which can occur in diabetic or non-diabetic hearts. I KATP opening was simulated in this work to determine if the risk of ischemia-induced arrhythmias is affected by diabetes...
June 27, 2017: Cardiovascular Engineering and Technology
https://www.readbyqxmd.com/read/28654763/effect-of-tolbutamide-on-tea-induced-postsynaptic-zinc-signals-at-hippocampal-mossy-fiber-ca3-synapses
#10
Fatima Mc Bastos, Vanessa N Corceiro, Sandra A Lopes, Jose G Almeida, Carlos Manuel Margarido Matias, Jose C Dionisio, Paulo J Mendes, Fernando Ds Sampaio Dos Aidos, Rosa M Quinta-Ferreira, M Emilia Quinta-Ferreira
The application of tetraethylammonium (TEA), a blocker of voltage-dependent potassium channels, can induce long-term potentiation in the synaptic systems CA3 - CA1 and mossy fibers - CA3 pyramidal cells of the hippocampus. In the mossy fibers the depolarization evoked by extracellular TEA induces a large amount of glutamate and also of zinc release. It is considered that zinc has a neuromodulatory role at the mossy fiber synapses, which can, at least in part, be due to the activation of presynaptic ATP-dependent potassium (KATP) channels...
June 27, 2017: Canadian Journal of Physiology and Pharmacology
https://www.readbyqxmd.com/read/28631579/opening-of-katp-channel-regulates-tonic-currents-from-pyramidal-neurons-in-rat-brain
#11
Zhongxia Li, Jiangping Wang, Huimin Yu, Kewen Jiang
BACKGROUND: ATP-sensitive K+ (KATP) channels couple metabolic state to cellular excitability. Activation of neuronal and astrocytic mitochondrial KATP (mitoKATP) channels regulates a variety of neuronal functions. However, less is known about the impact of mitoKATP on tonic γ-aminobutyric acid (GABA) inhibition. Tonic GABA inhibition is mediated by the binding of ambient GABA on extrasynaptic GABA A-type receptors (GABAARs) and is involved in regulating neuronal excitability. METHODS: We determined the impact of activation of KATP channels with diazoxide (DIZ) on tonic inhibition and recorded tonic current from rat cortical layer 5 pyramidal cells by patch-clamp recordings...
June 20, 2017: Canadian Journal of Neurological Sciences. le Journal Canadien des Sciences Neurologiques
https://www.readbyqxmd.com/read/28625489/diosmin-reduces-chronic-constriction-injury-induced-neuropathic-pain-in-mice
#12
Mariana M Bertozzi, Ana C Rossaneis, Victor Fattori, Daniela T Longhi-Balbinot, Andressa Freitas, Fernando Q Cunha, José C Alves-Filho, Thiago M Cunha, Rubia Casagrande, Waldiceu A Verri
Injury or dysfunction of somatosensory system induces a complex syndrome called neuropathic pain, which still needs adequate pharmacological control. The current pharmacological treatments were in part developed from natural compounds. Flavonoids are natural polyphenolic molecules presenting varied biological activities and low toxicity. The flavonoid diosmin is a safe compound with good tolerability and low toxicity. This study evaluated the antinociceptive effect of diosmin in the sciatic nerve chronic constriction injury (CCI)-induced neuropathic pain model...
June 15, 2017: Chemico-biological Interactions
https://www.readbyqxmd.com/read/28609713/nicorandil-modulated-macrophages-activation-and-polarization-via-nf-%C3%AE%C2%BAb-signaling-pathway
#13
Fengyun Zhang, Yongli Xuan, Jinjin Cui, Xinxin Liu, Zhiying Shao, Bo Yu
Nicorandil, a drug with both nitrate-like and ATP-sensitive potassium (KATP) channel-activating properties, has been well demonstrated in various aspects of myocardial infarction (MI), especially in inhibiting cell apoptosis and increasing coronary flow. However, the role of nicorandil in regulating inflammation and angiogenesis following myocardial infarction is still unrevealed. In the present study, we explored the effect of nicorandil on macrophage phenotype transition and inflammation regulation and the potential underlying mechanisms...
June 10, 2017: Molecular Immunology
https://www.readbyqxmd.com/read/28594895/atp-sensitive-potassium-katp-channel-openers-diazoxide-and-nicorandil-lower-intraocular-pressure-by-activating-the-erk1-2-signaling-pathway
#14
Uttio Roy Chowdhury, Cindy K Bahler, Bradley H Holman, Michael P Fautsch
Elevated intraocular pressure is the most prevalent and only treatable risk factor for glaucoma, a degenerative disease of the optic nerve. While treatment options to slow disease progression are available, all current therapeutic and surgical treatments have unwanted side effects or limited efficacy, resulting in the need to identify new options. Previous reports from our laboratory have established a novel ocular hypotensive effect of ATP-sensitive potassium channel (KATP) openers including diazoxide (DZ) and nicorandil (NCD)...
2017: PloS One
https://www.readbyqxmd.com/read/28587604/kcnj11-abcc8-and-tcf7l2-polymorphisms-and-the-response-to-sulfonylurea-treatment-in-patients-with-type-2-diabetes-a-bioinformatics-assessment
#15
Jingwen Song, Yunzhong Yang, Franck Mauvais-Jarvis, Yu-Ping Wang, Tianhua Niu
BACKGROUND: Type 2 diabetes (T2D) is a worldwide epidemic with considerable health and economic consequences. Sulfonylureas are widely used drugs for the treatment of patients with T2D. KCNJ11 and ABCC8 encode the Kir6.2 (pore-forming subunit) and SUR1 (regulatory subunit that binds to sulfonylurea) of pancreatic β cell KATP channel respectively with a critical role in insulin secretion and glucose homeostasis. TCF7L2 encodes a transcription factor expressed in pancreatic β cells that regulates insulin production and processing...
June 6, 2017: BMC Medical Genetics
https://www.readbyqxmd.com/read/28577450/n-acetylcysteine-induced-vasodilatation-is-modulated-by-katp-channels-na-k-atpase-activity-and-intracellular-calcium-concentration-an-in-vitro-study
#16
Özden Vezir, Ülkü Çömelekoğlu, Nehir Sucu, Ali Erdinç Yalın, Şakir Necat Yılmaz, Serap Yalın, Fatma Söğüt, Selma Yaman, Kezban Kibar, Merih Akkapulu, Meryem İlkay Koç, Didem Seçer
BACKGROUND: In this study, we aimed to investigate the role of ATP-sensitive potassium (KATP) channel, Na(+)/K(+)-ATPase activity, and intracellular calcium levels on the vasodilatory effect of N-acetylcysteine (NAC) in thoracic aorta by using electrophysiological and molecular techniques. METHODS: Rat thoracic aorta ring preparations and cultured thoracic aorta cells were divided into four groups as control, 2mM NAC, 5mM NAC, and 10mM NAC. Thoracic aorta rings were isolated from rats for measurements of relaxation responses and Na(+)/K(+)-ATPase activity...
March 31, 2017: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/28577088/role-of-atp-sensitive-k-channels-in-myocardial-infarct-size-limiting-effect-of-chronic-continuous-normobaric-hypoxia
#17
Yu B Lishmanov, N V Naryzhnaya, S Yu Tsibul'nikov, H Wang, L N Maslov
The role of KATP channels in myocardial infarct size-limiting effect of chronic continuous normobaric hypoxia was examined in a rat model based on a 20-min coronary occlusion and subsequent 3-h reperfusion. Rats were adapted to normobaric hypoxia (12% O2) for 21 days. This hypoxia produced a pronounced infarct size-limiting effect, which had been prevented by 0.3 mg/kg glibenclamide, a non-selective inhibitor of entire pool of KATP channels, or 5 mg/kg 5-hydroxydecanoate, an inhibitor of mitochondrial KATP channels...
June 2, 2017: Bulletin of Experimental Biology and Medicine
https://www.readbyqxmd.com/read/28575322/mutant-mice-with-calcium-sensing-receptor-casr-activation-have-hyperglycemia-that-is-rectified-by-calcilytic-therapy
#18
Valerie N Babinsky, Fadil M Hannan, Reshma D Ramracheya, Quan Zhang, M Andrew Nesbit, Alison Hugill, Liz Bentley, Tertius A Hough, Elizabeth Joynson, Michelle Stewart, Abhishek Aggarwal, Maximilian Prinz-Wohlgenannt, Caroline M Gorvin, Enikö Kallay, Sara Wells, Roger D Cox, Duncan Richards, Patrik Rorsman, Rajesh V Thakker
The calcium-sensing receptor (CaSR) is a family C G-protein-coupled receptor (GPCR) that plays a pivotal role in extracellular calcium homeostasis. The CaSR is also highly expressed in pancreatic islet α- and β-cells that secrete glucagon and insulin, respectively. To determine whether the CaSR may influence systemic glucose homeostasis, we characterized a mouse model with a germline gain-of-function CaSR mutation, Leu723Gln, referred to as Nuclear flecks (Nuf). Heterozygous- (CasrNuf/+) and homozygous-affected (CasrNuf/Nuf) mice were shown to have hypocalcemia in association with impaired glucose tolerance and insulin secretion...
June 2, 2017: Endocrinology
https://www.readbyqxmd.com/read/28571494/cardiovascular-pleiotropic-effects-of-statins-and-new-onset-diabetes-is-there-a-common-link-do-we-need-to-evaluate-the-role-of-katp-channels
#19
REVIEW
Devindra Sehra, Sudhish Sehra, Shiv Tej Sehra
Statins are considered the main stay of treatment in the prevention of cardio-vascular morbidity and mortality. They have multiple pleiotropic effects, like stabilization of atherosclerotic plaques, inhibition of platelet aggregation, and vascular smooth muscle proliferation; in addition to their lipid lowering action. Statins manifest these pleiotropic effects because they activate KATP channels in the cardiac and vascular tissue. Simultaneous activation of the KATP channels by statins in β cells of pancreas may inhibit insulin release which may lead to diabetes...
July 2017: Expert Opinion on Drug Safety
https://www.readbyqxmd.com/read/28567099/a-chinese-medicine-formula-xian-jia-tang-for-treating-bladder-outlet-obstruction-by-improving-urodynamics-and-inhibiting-oxidative-stress-through-potassium-channels
#20
Jie Sun, Wei Shen, Wenjin An, Qiufen Li, Shunan Qiu, Shaobo Jiang
The aim of this study is to investigate efficacy of a traditional Chinese medicine formula (named Xian-Jia-Tang, XJT) on bladder outlet obstruction (BOO) in rats and explore its mechanisms. Total 80 BOO model rats were established and randomly divided into 4 groups: physiological saline, XJT, Cesium Chloride (CC), and XJT and CC groups. Meanwhile, 12 rats were used as normal control. Bladder weight and urodynamics were measured. Oxidative stress level and mRNA expressions of potassium channels gene were detected in detrusor...
2017: Evidence-based Complementary and Alternative Medicine: ECAM
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