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https://www.readbyqxmd.com/read/29458170/downregulation-of-metabotropic-glutamate-receptor-5-inhibits-hepatoma-development-in-a-neurotoxin-rotenone-induced-parkinson-s-disease-model
#1
Xiao Xu Bai, Li Gu, Hui Min Yang, Shao Song Xi, Ning Xia, Song Zhang, Hong Zhang
Clinical epidemiological studies have shown that there is a link between Parkinson's disease (PD) and cancer, but how PD regulates cancer development remains unknown. In our study, the effect of metabotropic glutamate receptor 5 (mGlu5 ) on hepatoma was explored in a rotenone-induced PD model both in vitro and in vivo. We found that conditioned media derived from MN9D dopaminergic neuronal cells by rotenone-induced toxicity inhibited the growth, migration, invasion and promoted apoptosis of Hepa1-6 cells, which corresponded with decreased expression of mGlu5 ...
February 16, 2018: Toxicology Letters
https://www.readbyqxmd.com/read/29458169/inhibition-of-microsomal-prostaglandin-e-synthase-1-facilitates-liver-repair-after-hepatic-injury-in-mice
#2
Nobuyuki Nishizawa, Yoshiya Ito, Koji Eshima, Hirotoki Ohkubo, Ken Kojo, Tomoyoshi Inoue, Joan Raouf, Per-Johan Jakobsson, Satoshi Uematsu, Shizuo Akira, Shuh Narumiya, Masahiko Watanabe, Masataka Majima
BACKGROUND & AIMS: Liver repair following hepatic ischemia/reperfusion (I/R) injury is crucial to survival. This study aims to examine the role of endogenous prostaglandin E2 (PGE2 ) produced by inducible microsomal PGE synthase-1 (mPGES-1), a terminal enzyme of PGE2 generation, in liver injury and repair following hepatic I/R. METHODS: mPGES-1 deficient (mPGES-1-/- ) mice or their wild counterparts (WT) were subjected to partial hepatic ischemia followed by reperfusion...
February 16, 2018: Journal of Hepatology
https://www.readbyqxmd.com/read/29458104/a-new-l-glutaminase-from-streptomyces-pratensis-nrc-10-gene-identification-enzyme-purification-and-characterization
#3
Sanaa E Tork, Magda M Aly, Omar Elsemin
In the current study, the purified l-glutaminase from Streptomyces pratensis NRC10 (GenBank number KC857622) was characterized. Its molecular weight was estimated to be 46 kDa and isoelectric point 7.4. Its Vmax was calculated to be 2.19 U/mg/min, while Km was 0.175 mM. The optimum pH and temperature were 9 and 45 °C, respectively. It was thermostable at 45 °C but thermally inactivated at 60 °C after 50 min. Moreover, its enzymatic activity was enhanced by K+ ions and inhibited by Mg2+ , Cu2+ , Ag+ , Hg2+ , Ni2+ , Fe2+ , Cr2 , Na+ , Ca2+ , and EDTA...
February 16, 2018: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/29458098/spermine-protects-from-lps-induced-memory-deficit-via-bdnf-and-trkb-activation
#4
Pâmella K Frühauf-Perez, Fernanda R Temp, Micheli M Pillat, Cristiane Signor, Arithane Lorena Wendel, Henning Ulrich, Carlos F Mello, Maribel A Rubin
Lipopolysaccharide (LPS) has been long known to promote neuroinflammation and learning and memory deficits. Since spermine, one of the main natural polyamines in the central nervous system, protects from LPS-induced memory deficit by a mechanism that comprises GluN2B receptors, the aim of the present study was to determine whether brain-derived neurotrophic factor (BDNF), tropomyosin-related kinase B (TrkB) receptor and cAMP response element binding (CREB) are involved in this protective effect of spermine...
February 16, 2018: Neurobiology of Learning and Memory
https://www.readbyqxmd.com/read/29458097/topographical-memory-analyzed-in-mice-using-the-hamlet-test-a-novel-complex-maze
#5
Lucie Crouzier, Damien Gilabert, Mireille Rossel, Françoise Trousse, Tangui Maurice
The Hamlet test is an innovative device providing a complex environment for testing topographic memory in mice. Animals were trained in groups for weeks in a small village with a central agora, streets expanding from it towards five functionalized houses, where they can drink, eat, hide, run, interact with a stranger mouse. Memory was tested by depriving mice from water or food and analyzing their ability to locate the Drink/Eat house. Exploration and memory were analysed in different strains, gender, and after different training periods and delays...
February 16, 2018: Neurobiology of Learning and Memory
https://www.readbyqxmd.com/read/29458061/decreased-mcp-1-ccr2-axis-mediated-chemotactic-effect-of-conjunctival-fibroblasts-after-transdifferentiation-into-myofibroblasts
#6
Utako Tsutsumi-Kuroda, Toshihiro Inoue, Akiko Futakuchi, Kohei Shobayashi, Eri Takahashi, Sachi Kojima, Miyuki Inoue-Mochita, Tomokazu Fujimoto, Hidenobu Tanihara
The purpose of this study is to investigate the change in chemotactic effects of human conjunctival fibroblasts (HConFs) after transdifferentiation into myofibroblasts, and to explore related molecular mechanisms. HConFs were treated with 5 ng/mL transforming growth factor (TGF)-β2 for 48 h to induce transdifferentiation into myofibroblasts. The cytokine concentrations in the conditioned media of HConFs were measured by multiplex bead-based immunoassays. The Boyden chamber assay was used to assess the chemotactic effects using the monocyte cell line, THP-1 cells...
February 16, 2018: Experimental Eye Research
https://www.readbyqxmd.com/read/29458046/bmp-2-induces-angiogenesis-by-provoking-integrin-%C3%AE-6-expression-in-human-endothelial-progenitor-cells
#7
Wei-Cheng Chen, Ching-Hu Chung, Yung-Chang Lu, Min-Huan Wu, Po-Hsun Chou, Juei-Yu Yen, Yu-Wei Lai, Guo-Shou Wang, Shih-Chia Liu, Jen-Kun Cheng, Yih-Jer Wu, Hung-I Yeh, Li-Yu Wang, Shih-Wei Wang
Bone morphogenetic proteins-2 (BMP-2) is a multifunctional cytokine, capable of governing several cellular functions, including proliferation, motility, differentiation, and angiogenesis. Circulating endothelial progenitor cells (EPCs) have been shown to facilitate tissue repair, postnatal neovascularization, and tumor associated angiogenesis. Nevertheless, the impact of BMP-2 on angiogenesis of human EPCs has largely remained a mystery. In this study, we found that BMP-2 promoted cell migration and tube formation of EPCs in a concentration-dependent manner, indicating BMP-2 induced in vitro angiogenesis in human EPCs...
February 16, 2018: Biochemical Pharmacology
https://www.readbyqxmd.com/read/29457805/urinary-metabolomic-study-of-the-antagonistic-effect-of-p-ginseng-in-rats-with-estrogen-decline-using-ultra-performance-liquid-chromatography-coupled-with-quadrupole-time-of-flight-mass-spectrometry
#8
He Lin, Zhongying Liu, Zifeng Pi, Lihui Men, Weijia Chen, Zhiqiang Liu
Estrogens are biologically active steroid hormones mainly released from the ovary by ovarian secretion of estrogen into the circulating blood to regulate or function at the distal target. Estrogens play an important role in the central nervous system, cardiovascular system and immune system, especially for post-menopausal women. Panax ginseng Mayer has been reported to relieve women's menopausal symptoms and affect estrogen activities. However, the mechanism of its estrogen regulation has not yet been clearly investigated...
February 19, 2018: Food & Function
https://www.readbyqxmd.com/read/29457123/general-anesthesia-with-propofol-for-ovarian-teratoma-excision-associated-with-anti-n-methyl-d-aspartate-receptor-encephalitis
#9
Masami Sato, Hiroaki Yasumoto, Toshiyuki Arai
Anti-N-methyl-D-aspartate receptor (NMDAR) encephalitis is an autoimmune disorder caused by production of anti-NMDAR antibodies that is often associated with ovarian teratoma and exhibits various manifestations including psychiatric symptoms, seizures, hypoventilation, and autonomic nerve instability. Patients with this disorder who receive early surgical tumor resection along with immunotherapy have better outcome than the rest of the patients. To establish an anesthetic plan, it is important to understand the pharmacological interaction between the anesthetic agents and the disabled NMDAR, because NMDAR is one of the major sites of action for commonly-used anesthetic agents...
2018: JA Clin Rep
https://www.readbyqxmd.com/read/29456983/the-role-of-mas-receptor-on-renal-hemodynamic-responses-to-angiotensin-1-7-in-both-irreversible-and-reversible-unilateral-ureteral-obstruction-rats
#10
Jalal Hassanshahi, Mehdi Nematbakhsh
Background: Unilateral ureteral obstruction (UUO) alters the expression of renin-angiotensin system (RAS) components and angiotensin 1-7 (Ang 1-7) as a main arm of RAS is affected by UUO. The role of Mas receptor antagonist (A779) was examined in renal hemodynamic responses to Ang 1-7 in 3-day UUO and UUO removal (RUUO) in rats. Materials and Methods: Forty-five male Wistar rats were randomly divided into three groups of sham operated, UUO, and RUUO, while each group was divided into two subgroups treated with vehicle or A779...
2018: Advanced Biomedical Research
https://www.readbyqxmd.com/read/29456793/synthesis-of-novel-tetrahydroisoquinoline-cxcr4-antagonists-with-rigidified-side-chains
#11
Edgars Jecs, Eric J Miller, Robert J Wilson, Huy H Nguyen, Yesim A Tahirovic, Brook M Katzman, Valarie M Truax, Michelle B Kim, Katie M Kuo, Tao Wang, Chi S Sum, Mary E Cvijic, Gretchen M Schroeder, Lawrence J Wilson, Dennis C Liotta
A structure-activity relationship study of potent TIQ15-derived CXCR4 antagonists is reported. In this investigation, the TIQ15 side-chain was constrained to improve its drug properties. The cyclohexylamino congener 15a was found to be a potent CXCR4 inhibitor (IC50 = 33 nM in CXCL12-mediated Ca2+ flux) with enhanced stability in liver microsomes and reduced inhibition of CYP450 (2D6). The improved CXCR4 antagonist 15a has potential therapeutic application as a single agent or combinatory anticancer therapy...
February 8, 2018: ACS Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/29456791/nonacidic-chemotype-possessing-n-acylated-piperidine-moiety-as-potent-farnesoid-x-receptor-fxr-antagonists
#12
Naoki Teno, Yukiko Yamashita, Yusuke Iguchi, Ko Fujimori, Mizuho Une, Tomoko Nishimaki-Mogami, Takie Hiramoto, Keigo Gohda
Farnesoid X receptor (FXR) plays a major role in the control of cholesterol metabolism. Antagonizing transcriptional activity of FXR is an effective means to treat the relevant metabolic syndrome. Some of antagonists so far have the charged functions; however, they may negatively affect the pharmacokinetics. We describe herein a structure-activity relationship (SAR) exploration of nonacidic FXR antagonist 6 focusing on two regions in the structure and biological evaluation of nonacidic 10 with the characteristic N -acylated piperidine group obtained from SAR studies...
February 8, 2018: ACS Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/29456602/review-of-management-in-cardiotoxic-overdose-and-efficacy-of-delayed-intralipid-use
#13
Edward Walter, James McKinlay, Jade Corbett, Justin Kirk-Bayley
We present the case of a 51-year-old woman admitted to our intensive care unit following an intentional overdose of a calcium channel antagonist and a beta blocker. The resultant hypotension was reversed with glucagon, noradrenaline, calcium and high-dose insulin. Despite these interventions, she remained vasoplegic and received a delayed, standard dose of intralipid. Subsequently, the vasoplegia resolved rapidly, and the vasopressor was stopped. Here, we review the management of overdose of calcium channel and beta-adrenergic receptor blockers, concentrating on the pharmacology of lipid emulsion therapy...
February 2018: Journal of the Intensive Care Society
https://www.readbyqxmd.com/read/29456560/the-effect-of-testosterone-gel-on-fertility-outcomes-in-women-with-a-poor-response-in-in-vitro-fertilization-cycles-a-pilot-randomized-clinical-trial
#14
Nasrin Saharkhiz, Shahrzad Zademodares, Saghar Salehpour, Sedighe Hosseini, Leyla Nazari, Hatav Ghasemi Tehrani
Background: In this study, the effect of testosterone gel administration during ovulation induction on the fertility rate was examined in women with a poor ovarian response in in vitro fertilization (IVF) cycles. Materials and Methods: The current study is a single-blinded, randomized clinical trial. Patients who met inclusion (Bologna) criteria were placed in the antagonist cycle group. The patients were randomly divided into two groups each included 25 participants treated with a placebo (lubricant gel, the controls) and testosterone gel (intervention)...
2018: Journal of Research in Medical Sciences: the Official Journal of Isfahan University of Medical Sciences
https://www.readbyqxmd.com/read/29456511/p2y-12-receptors-in-tumorigenesis-and-metastasis
#15
REVIEW
Patrizia Ballerini, Melania Dovizio, Annalisa Bruno, Stefania Tacconelli, Paola Patrignani
Platelets, beyond their role in hemostasis and thrombosis, may sustain tumorigenesis and metastasis. These effects may occur via direct interaction of platelets with cancer and stromal cells and by the release of several platelet products. Platelets and tumor cells release several bioactive molecules among which a great amount of adenosine triphosphate (ATP) and adenosine diphosphate (ADP). ADP is also formed extracellularly from ATP breakdown by the ecto-nucleoside-triphosphate-diphosphohydrolases. Under ATP and ADP stimulation the purinergic P2Y1 receptor (R) initiates platelet activation followed by the ADP-P2Y12 R-mediated amplification...
2018: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/29456508/the-molecular-determinants-of-small-molecule-ligand-binding-at-p2x-receptors
#16
Gaia Pasqualetto, Andrea Brancale, Mark T Young
P2X receptors are trimeric eukaryotic ATP-gated cation channels. Extracellular ATP-their physiological ligand-is released as a neurotransmitter and in conditions of cell damage such as inflammation, and substantial evidence implicates P2X receptors in diseases including neuropathic pain, cancer, and arthritis. In 2009, the first P2X crystal structure, Danio rerio P2X4 in the apo - state, was published, and this was followed in 2012 by the ATP-bound structure. These structures transformed our understanding of the conformational changes induced by ATP binding and the mechanism of ligand specificity, and enabled homology modeling of mammalian P2X receptors for ligand docking and rational design of receptor modulators...
2018: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/29456408/inhibitory-effects-of-patchouli-alcohol-on-stress-induced-diarrhea-predominant-irritable-bowel-syndrome
#17
Tian-Ran Zhou, Jing-Jing Huang, Zi-Tong Huang, Hong-Ying Cao, Bo Tan
AIM: To elucidate the mechanism of patchouli alcohol (PA) in treatment of rat models of diarrhea-predominant irritable bowel syndrome (IBS-D). METHODS: We studied the effects of PA on colonic spontaneous motility using its cumulative log concentration (3 × 10-7 mol/L to 1 × 10-4 mol/L). We then determined the responses of the proximal and distal colon segments of rats to the following stimuli: (1) carbachol (1 × 10-9 mol/L to 1 × 10-5 mol/L); (2) neurotransmitter antagonists including Nω -nitro-L-arginine methyl ester hydrochloride (10 μmol/L) and (1R*, 2S*)-4-[2-Iodo-6-(methylamino)-9H-purin-9-yl]-2-(phosphonooxy)bicyclo[3...
February 14, 2018: World Journal of Gastroenterology: WJG
https://www.readbyqxmd.com/read/29456377/molecular-simulation-studies-of-3-3-diindolylmethane-as-a-potent-microrna-21-antagonist
#18
Md Junaid, Raju Dash, Nazrul Islam, Jui Chowdhury, Md Jahangir Alam, Saikat Dev Nath, Mohammad Abu Sayem Shakil, Ashifa Azam, Syed Mustyen Quader, S M Zahid Hosen
Objective: In recent decades, the overexpression of microRNA-21 (miR-21) is found to be progressively linked with many diseases such as different types of cancers, cardiovascular diseases, and inflammation. Thereby, it has become an attractive target for pharmacological and genetic modulation in various diseases, and also for overcoming the resistance to chemotherapy in several cancers. Here, in this study, the role of molecular therapeutics of 3,3'-diindolylmethane (DIM) has been investigated for its ability to bind with the precursor miRNA as a target of miR-21 (hsa-mir-21), which may alter the catalyzation process of dicer, a RNase III enzyme, involved in miRNA transcription...
October 2017: Journal of Pharmacy & Bioallied Sciences
https://www.readbyqxmd.com/read/29456150/antidepressants-as-antipruritic-agents-a-review
#19
REVIEW
Randeep Kaur, V R Sinha
Pruritus is a concomitant symptom of various underlying disorders viz. dermatological, systemic and psychiatric disorders that provoke the person to scratch the skin. Many natural as well as, antipruritic therapies are usually practiced in the treatment of pruritus including general preventive measures, topical therapies such as cooling agents, antihistamines, anesthetics, capsaicin, corticosteroids, immunomodulators and; systemic therapies including administration of antihistamines, opioid antagonists/agonists, antiepileptic drugs/neuroleptics (e...
February 15, 2018: European Neuropsychopharmacology: the Journal of the European College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/29456134/parietal-control-network-activation-during-memory-tasks-may-be-associated-with-the-co-occurrence-of-externally-and-internally-directed-cognition-a-cross-function-meta-analysis
#20
Hongkeun Kim
Functional neuroimaging studies on episodic memory retrieval consistently indicated the activation of the precuneus (PCU), mid-cingulate cortex (MCC), and lateral intraparietal sulcus (latIPS) regions. Although studies typically interpreted these activations in terms of memory retrieval processes, resting-state functional connectivity data indicate that these regions are part of the frontoparietal control network, suggesting a more general, cross-functional role. In this regard, this study proposes a novel hypothesis which suggests that the parietal control network plays a strong role in accommodating the co-occurrence of externally directed cognition (EDC) and internally directed cognition (IDC), which are typically antagonistic to each other...
March 15, 2018: Brain Research
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