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https://www.readbyqxmd.com/read/28738539/lncrna-ab073614-regulates-proliferation-and-metastasis-of-colorectal-cancer-cells-via-the-pi3k-akt-signaling-pathway
#1
Yanan Wang, Haoyu Kuang, Jinfang Xue, Liya Liao, Fang Yin, Xiaojun Zhou
The expression profiles of long noncoding RNAs (lncRNAs) in colorectal cancer (CRC) have remained unclear. LncRNA AB073614 is known to be upregulated in ovarian cancer and glioma tissues, and is associated with the occurrence and progression of those cancers. In the present study, we investigated the lncRNA AB073614 gene expression patterns in CRC cell lines and tissue samples from CRC patients, and then analyzed them for possible associations with various clinicopathological characteristics. Furthermore, the roles played by lncRNA AB073614 in CRC cell proliferation, apoptosis, cell cycle progression, migration, and invasion were examined in vitro by using gene knockdown and overexpression techniques...
July 20, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28738523/a-natriuretic-peptides-clearance-receptor-s-agonist-reduces-pulmonary-artery-pressures-and-enhances-cardiac-performance-in-preclinical-models-new-hope-for-patients-with-pulmonary-hypertension-due-to-left-ventricular-heart-failure
#2
Emmanuel Eroume Egom, Tiam Feridooni, Rebabonye B Pharithi, Barkat Khan, Haaris A Shiwani, Vincent Maher, Yassine El Hiani, Kishore B S Pasumarthi, Hilaire A Ribama
BACKGROUND: In patients with left ventricular heart failure (HF), the development of pulmonary hypertension (PH) is common and represents a strong predictor of death. Despite recent advances in the pathophysiological understanding there is as yet no prospect of cure of this deadly clinical entity and the majority of patients continue to progress to right ventricular failure and die. Furthermore, there is no single medical treatment currently approved for PH related to HF. There is, therefore an urgent unmet need to identify novel pharmacological agents that will prevent the progressive increased or reverse the elevated pulmonary arterial pressures while enhancing cardiac performance in HF...
July 19, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28738351/major-depression-as-a-neuroprogressive-prelude-to-dementia-what-is-the-evidence
#3
Brian E Leonard
Epidemiological studies implicate chronic depression as a predisposing factor for dementia in later life. However, the link is incompletely understood and controversial. The aim of this review is to consider some of the biological factors that contribute to neuroprogressive brain dysfunction in late life as a consequence of prolonged, low-grade inflammation in the course of depressive episodes. As chronic inflammation is known to precipitate increased apoptosis of neurons and astrocytes, this could be a contributing factor to brain dysfunction...
2017: Modern Trends in Pharmacopsychiatry
https://www.readbyqxmd.com/read/28738113/estrogen-status-gates-effects-of-kappa-opioid-receptor-on-temporomandibular-joint-responsive-neurons-at-the-spinomedullary-junction-in-female-rats
#4
Akimasa Tashiro, David A Bereiter, Yasuhiro Nishida
AIMS: To determine whether estrogen status alters κ-opioid inhibition of nociceptive processing by affecting temporomandibular joint (TMJ) input to neurons in the trigeminal subnucleus caudalis [Vc]/C1-2 region at the spinomedullary junction in female rats. METHODS: TMJ-responsive neurons were recorded in laminae I-II of the Vc/C1-2 region at the spinomedullary junction of ovariectomized female rats treated for 2 days with low-dose estradiol (LE group; 2 mg/day) or high-dose estradiol (HE group; 20 mg/day)...
July 2017: Journal of Oral & Facial Pain and Headache
https://www.readbyqxmd.com/read/28738010/effects-of-the-%C3%AE-2-adrenoceptor-agonist-medetomidine-on-the-distribution-and-clearance-of-alfaxalone-during-coadministration-by-constant-rate-infusion-in-dogs
#5
Rachel C Bennett, Kati M Salla, Marja R Raekallio, Mika Scheinin, Outi M Vainio
OBJECTIVE To assess the possible impact of medetomidine on concentrations of alfaxalone in plasma, when coadministered as a constant rate infusion (CRI) to dogs, and to determine the possible impact of medetomidine on the cardiopulmonary effects of alfaxalone during CRI. ANIMALS 8 healthy adult Beagles. PROCEDURES 3 treatments were administered in a randomized crossover design as follows: 1 = saline (0.9% NaCl) solution injection, followed in 10 minutes by induction of anesthesia with alfaxalone (loading dose, 2...
August 2017: American Journal of Veterinary Research
https://www.readbyqxmd.com/read/28737971/fluticasone-furoate-vilanterol-and-lung-function-decline-in-patients-with-moderate-copd-and-heightened-cardiovascular-risk
#6
Peter M A Calverley, Julie A Anderson, Robert D Brook, Courtney Crim, Natacha Gallot, Sally Kilbride, Fernando Martinez, Julie Yates, David E Newby, Jørgen Vestbo, Robert Wise, Bartolome R Celli
RATIONALE: Many patients with chronic obstructive pulmonary disease (COPD) have an accelerated loss of lung function. It is unclear whether drug treatment can modify this in moderately severe disease. OBJECTIVES: In a pre-specified analysis of the key secondary outcome in the Study to Understand Mortality and MorbidITy (SUMMIT), we investigated whether the inhaled corticosteroid fluticasone furoate 100 μg (FF), the long-acting beta-agonist vilanterol 25 µg (VI) or the combination (FF/VI) modified the rate of decline in FEV1 compared with placebo...
July 24, 2017: American Journal of Respiratory and Critical Care Medicine
https://www.readbyqxmd.com/read/28737760/channel-opening-and-gating-mechanism-in-ampa-subtype-glutamate-receptors
#7
Edward C Twomey, Maria V Yelshanskaya, Robert A Grassucci, Joachim Frank, Alexander I Sobolevsky
AMPA-subtype ionotropic glutamate receptors mediate fast excitatory neurotransmission throughout the central nervous system. Gated by the neurotransmitter glutamate, AMPA receptors are critical for synaptic strength and dysregulation of AMPA receptor-mediated signalling is linked to numerous neurological diseases. Here, we use cryo-electron microscopy to solve the structures of AMPA receptor-auxiliary subunit complexes in the apo, antagonist and agonist-bound states and elucidate the iris-like mechanism of ion channel opening...
July 24, 2017: Nature
https://www.readbyqxmd.com/read/28737453/the-metabolism-and-drug-drug-interaction-potential-of-the-selective-prostacyclin-receptor-agonist-selexipag
#8
Carmela Gnerre, Jérôme Segrestaa, Swen Seeland, Päivi Äänismaa, Thomas Pfeifer, Stephane Delahaye, Ruben de Kanter, Tomohiko Ichikawa, Tetsuhiro Yamada, Alexander Treiber
- The metabolism of selexipag has been studied in vivo in man and the main excreted metabolites were identified. Also, metabolites circulating in human plasma have been structurally identified and quantified. - The main metabolic pathway of selexipag in man is the formation of the active metabolite ACT-333679. Other metabolic pathways include oxidation and dealkylation reactions. All primary metabolites undergo subsequent hydrolysis of the sulphonamide moiety to their corresponding acids. ACT-333679 undergoes conjugation with glucuronic acid and aromatic hydroxylation to P10, the main metabolite detected in human faeces...
July 24, 2017: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
https://www.readbyqxmd.com/read/28737448/mast-cell-and-m1-macrophage-infiltration-and-local-pro-inflammatory-factors-were-attenuated-with-incretin-based-therapies-in-obesity-related-glomerulopathy
#9
Jiao He, Geheng Yuan, Fangxiao Cheng, Junqing Zhang, Xiaohui Guo
BACKGROUND: The global increase of obesity parallels the obesity-related glomerulopathy (ORG) epidemic. Dipeptidyl peptidase 4 inhibitors and glucagon-like peptide-1 receptor agonists were well recognized to attenuate renal injury independent of glucose control in diabetic nephropathy. There are limited studies focusing on their effects on ORG. We explored the effects of incretin-based therapies on early ORG and the inflammatory responses involved mainly concentrated on mast cell (MC) and macrophage (M) infiltration and local pro-inflammatory factors...
July 24, 2017: Metabolic Syndrome and related Disorders
https://www.readbyqxmd.com/read/28737050/efficacy-of-elagolix-in-the-treatment-of-endometriosis
#10
Alexandra Perricos, René Wenzl
Much research has gone into developing medications that can be used to alleviate endometriosis-associated symptoms. In addition to already established medications, a new GnRH antagonist, elagolix, is in development. The novelty of this drug compared to other GnRH antagonists, is its nonpeptide structure, allowing it to be administered orally. Areas covered: We analyzed several Phase I, II and III clinical trials that have evaluated the safety and efficacy of this new medication. Expert opinion: Since many medications have been put on the market and have gained popularity for the treatment of endometriosis-associated symptoms, the demonstration of equality or superiority of effect, tolerability, as well as patient compliance should be assessed when introducing a new drug...
July 24, 2017: Expert Opinion on Pharmacotherapy
https://www.readbyqxmd.com/read/28736919/a-g326e-substitution-in-the-glutamate-gated-chloride-channel-3-glucl3-of-the-two-spotted-spider-mite-tetranychus-urticae-abolishes-the-agonistic-activity-of-macrocyclic-lactones
#11
Catherine Mermans, Wannes Dermauw, Sven Geibel, Thomas Van Leeuwen
BACKGROUND: The macrocyclic lactones abamectin and milbemectin are frequently used to control phytophagous mites such as Tetranychus urticae. Consequently, resistance has developed and was genetically linked with substitutions in the glutamate-gated chloride channel (GluCl) subunits TuGluCl1 and TuGluCl3. Here, we functionally validated a G326E substitution in TuGluCl3 by functional expression in Xenopus laevis oocytes followed by two-electrode voltage-clamp electrophysiology. RESULTS: Homomeric wild-type and mutated GluCl3 were successfully expressed...
July 24, 2017: Pest Management Science
https://www.readbyqxmd.com/read/28736839/the-neurotensin-nts1-receptor-agonist-pd149163-produces-antidepressant-like-effects-in-the-forced-swim-test-further-support-for-neurotensin-as-a-novel-pharmacologic-strategy-for-antidepressant-drugs
#12
Lawrence M Carey, Remington J Rice, Adam J Prus
Preclinical Research Neurotensin is a nonbrain penetrant neuropeptide neurotransmitter that alters dopaminergic and serotonergic neurotransmission. Previous animal behavioral studies have demonstrated that intra-ventral tegmental administration of neurotensin and system administration of the selective neurotensin NTS1 receptor agonist, PD149163 produce antidepressant-like effects in a forced swim test and a differential reinforcement of low rate task, respectively. The present study sought to expand upon these past findings by assessing systemic administration of PD149163 in a forced swim test, a primary antidepressant preclinical screening model, in mice...
July 24, 2017: Drug Development Research
https://www.readbyqxmd.com/read/28736546/zb-16-a-novel-gpr119-agonist-relieves-the-severity-of-streptozotocin-nicotinamide-induced-diabetes-in-rats
#13
Ivan N Tyurenkov, Denis V Kurkin, Dmitry A Bakulin, Elena V Volotova, Mikhail A Chafeev, Alexey V Smirnov, Evgeny I Morkovin
GPR119 is involved in the regulation of incretin and insulin secretion, so the GPR119 agonists have been suggested as novel antidiabetic medications. The purpose of this work was to assess the influence of novel GPR119 agonist ZB-16 on the glucose utilization, insulin, and glucagon-like peptide-1 (GLP-1) secretion and the morphology of pancreas in rats with streptozotocin-nicotinamide-induced diabetes. 45 male Wistar rats were used in the study. The criteria of streptozotocin-nicotinamide-induced diabetes were blood glucose levels of 9-14 mmol/l measured in fasting conditions on the third day since administration of streptozotocin (65 mg/kg) and nicotinamide (230 mg/kg)...
2017: Frontiers in Endocrinology
https://www.readbyqxmd.com/read/28736297/1%C3%AE-hydroxy-derivatives-of-7-dehydrocholesterol-are-selective-liver-x-receptor-modulators
#14
Kaori Endo-Umeda, Atsushi Aoyama, Masato Shimizu, Minoru Ishikawa, Yuichi Hashimoto, Sachiko Yamada, Makoto Makishima
The nuclear receptors liver X receptor (LXR) α and LXRβ are involved in the regulation of lipid metabolism, inflammation, immunity, cellular proliferation, and apoptosis. Oxysterols are endogenous LXR ligands, and also interact with other nuclear and membrane receptors. We previously reported that a phytosterol derivative with a 1α-hydroxy group acts as a potent LXR agonist with intestine-selective action and that 25-hydroxy and 26/27-hydroxy metabolites of 7-dehydrocholsterol (7-DHC) exhibit partial LXR agonism...
July 20, 2017: Journal of Steroid Biochemistry and Molecular Biology
https://www.readbyqxmd.com/read/28736253/selective-er-%C3%AE-agonist-alleviates-vascular-endothelial-dysfunction-in-ovariectomized-type-2-diabetic-rats
#15
Seema Bansal, Kanwaljit Chopra
Postmenopausal diabetic women represent a specific risk group with a greater incidence of vascular deficits as compared with age-matched men or non-diabetic women. 17β-estradiol is the mainstay therapy for menopause and associated complications; however, its vasculoprotective effect is lost in women with diabetes. Although, exact mechanism of dichotomous effect of estrogen has not been delineated but it may be due to, differential activation of ER-α and β during disease conditions such as diabetes. Thus main objective of our study was to characterize the specific estrogen receptor which could be selectively targeted to achieve vasculoprotection in postmenopausal diabetic situation...
July 20, 2017: Molecular and Cellular Endocrinology
https://www.readbyqxmd.com/read/28736228/dbz-is-a-putative-ppar%C3%AE-agonist-that-prevents-high-fat-diet-induced-obesity-insulin-resistance-and-gut-dysbiosis
#16
Pengfei Xu, Fan Hong, Jialin Wang, Jing Wang, Xia Zhao, Sheng Wang, Tingting Xue, Jingwei Xu, Xiaohui Zheng, Yonggong Zhai
BACKGROUND: The nuclear receptor PPARγ is an effective pharmacological target for some types of metabolic syndrome, including obesity, diabetes, nonalcoholic fatty liver disease, and cardiovascular disease. However, the current PPARγ-targeting thiazolidinedione drugs have undesirable side effects. Danshensu Bingpian Zhi (DBZ), also known as tanshinol borneol ester derived from Salvia miltiorrhiza, is a synthetic derivative of natural compounds used in traditional Chinese medicine for its anti-inflammatory activity...
July 20, 2017: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/28736136/prostaglandin-e2-modulates-presynaptic-regulation-of-gnrh-neurons-via-ep4-receptors-in-accordance-with-estrogen-milieu
#17
Hitomi Fujioka, Toshiya Funabashi, Tatsuo Akema
Prostaglandin E2 (PGE2) promotes gonadotropin secretion by regulating the activity of neurons that release gonadotropin-releasing hormone (GnRH) in the hypothalamus. However, the mechanisms of action of PGE2 at these neurons have yet to be fully explored. We examined the effects of PGE2 on the generation of miniature excitatory postsynaptic currents (mEPSCs) at GnRH neurons as measured by whole-cell, patch-clamp recordings. GnRH neurons were identified in slices prepared from the preoptic areas of female GnRH-EGFP rats...
July 20, 2017: Neuroscience
https://www.readbyqxmd.com/read/28736035/propane-2-sulfonic-acid-octadec-9-enyl-amide-a-novel-ppar%C3%AE-%C3%AE-dual-agonist-protects-against-ischemia-induced-brain-damage-in-mice-by-inhibiting-inflammatory-responses
#18
Ying Li, Lanxi Xu, Kaiyue Zeng, Zhentian Xu, Daqin Suo, Lu Peng, Tong Ren, Zhiheng Sun, Wushuang Yang, Xin Jin, Lichao Yang
Propane-2-sulfonic acid octadec-9-enyl-amide (N15), an analogue of oleoylethanolamide (OEA), is a novel PPARα/γ dual agonist. Our previous studies verified the positive effects of OEA on the acute and delayed stages of cerebral ischemia. However, it is not clear whether N15 is effective against ischemic cerebral injury. In the present study, male Kunming mice were subjected to middle cerebral artery occlusion (MCAO). To evaluate its preventive effects, N15 (50, 100 or 200 mg/kg, ip) was administered for 3 days before ischemia...
July 20, 2017: Brain, Behavior, and Immunity
https://www.readbyqxmd.com/read/28735973/in-vitro-study-on-the-regulation-of-cellular-mrna-levels-by-changes-in-transcription-rate-and-transcript-stability-in-fish-red-blood-cells
#19
Miriam Götting, Mikko Nikinmaa
The interplay of transcriptional and posttranscriptional processes in the regulation of gene expression has been extensively studied in mammals but little is known in other vertebrates so far. Most non-mammalian vertebrates are faced with environmental cues and stressors distinct from those experienced by mammals and thus it is likely that the gene expression strategies differ from those of mammals. Here we performed experiments to study in vitro the various levels of gene expression regulation in nucleated fish red blood cells...
July 20, 2017: Comparative Biochemistry and Physiology. Part B, Biochemistry & Molecular Biology
https://www.readbyqxmd.com/read/28735873/the-therapeutic-potential-of-purinergic-signalling
#20
REVIEW
Geoffrey Burnstock
This review is focused on the pathophysiology and therapeutic potential of purinergic signalling. A wide range of diseases are considered, including those of the central nervous system, skin, kidney, musculoskeletal, liver gut, lower urinary tract, cardiovascular, airways and reproductive systems, the special senses, infection, diabetes and obesity. Several purinergic drugs are already on the market, including P2Y12 receptor antagonists for stroke and thrombosis, P2Y2 receptor agonists for dry eye, A1 receptor agonists for supraventricular tachycardia...
July 20, 2017: Biochemical Pharmacology
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