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Kappa Receptor

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https://www.readbyqxmd.com/read/28091892/bariatric-roux-en-y-gastric-bypass-surgery-adipocyte-proteins-involved-in-increased-bone-remodeling-in-humans
#1
Maria Fernanda G Biagioni, Adriana L Mendes, Célia Regina Nogueira, Celso V Leite, Loraine Gollino, Gláucia Mfs Mazeto
PURPOSE: Bariatric surgery has been associated with bone remodeling changes. The action of adipokines on the expression of receptor activator of nuclear factor kappa β ligand (RANKL) and osteoprotegerin (OPG) and on an increase in sclerostin could be related to these changes. MATERIALS AND METHODS: This study aimed to assess the repercussions of weight loss, fat mass (FM), and fat-free mass (FFM) loss and biochemical and hormonal changes on bone remodeling markers after Roux-en-Y gastric bypass (RYGB)...
January 13, 2017: Obesity Surgery
https://www.readbyqxmd.com/read/28088671/melatonin-attenuates-titanium-particle-induced-osteolysis-via-activation-of-wnt-%C3%AE-catenin-signaling-pathway
#2
Zichuan Ping, Xuanyang Hu, Liangliang Wang, Jiawei Shi, Yunxia Tao, Xiexing Wu, Zhenyang Hou, Xiaobin Guo, Wen Zhang, Huilin Yang, Yaozeng Xu, Zhirong Wang, Dechun Geng
: Wear debris-induced inhibition of bone regeneration and extensive bone resorption were common features in peri-prosthetic osteolysis (PPO). Here, we investigated the effect of melatonin on titanium particle-stimulated osteolysis in a murine calvariae model and mouse-mesenchymal-stem cells (mMSCs) culture system. Melatonin inhibited titanium particle-induced osteolysis and increased bone formation at osteolytic sites, confirmed by radiological and histomorphometric data. Furthermore, osteoclast numbers decreased dramatically in the low- and high-melatonin administration mice, as respectively, compared with the untreated animals...
January 11, 2017: Acta Biomaterialia
https://www.readbyqxmd.com/read/28088520/palmitic-acid-increases-invasiveness-of-pancreatic-cancer-cells-aspc-1-through-tlr4-ros-nf-%C3%AE%C2%BAb-mmp-9-signaling-pathway
#3
Makena J Binker-Cosen, Daniel Richards, Brenda Oliver, Herbert Y Gaisano, Marcelo G Binker, Laura I Cosen-Binker
Pancreatic cancer (PC) is an aggressive malady with proclivity for early metastasis. Overexpression of toll-like receptor 4 (TLR4) in pancreatic ductal adenocarcinoma, the most common type of pancreatic malignancy, correlates to tumor size, lymph node involvement, venous invasion and pathological stage. Lipopolysaccharides (LPS) are natural TLR4 ligands that have been shown to increase the invasive ability of PC cells. However, rapid inactivation of circulating LPS and low systemic absorption of inhaled LPS from the bronchoalveolar compartment make other agonists such as saturated fatty acids more suitable to be considered for TLR4-related cell invasiveness...
January 11, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/28088389/nalfurafine-is-a-g-protein-biased-agonist-having-significantly-greater-bias-at-the-human-than-rodent-form-of-the-kappa-opioid-receptor
#4
Selena S Schattauer, Jamie R Kuhar, Allisa Song, Charles Chavkin
Nalfurafine is a moderately selective kappa opioid receptor (KOR) analgesic with low incidence of dysphoric side effects in clinical development for the treatment of uremic pruritis. The basis for its reduced dysphoric effect compared to other KOR agonists is not clear, but prior studies suggest that the aversive properties of KOR agonists require p38α MAPK activation through an arrestin-dependent mechanism. To determine whether nalfurafine is a functionally selective KOR agonist, we measured its potency to activate the G protein-dependent early phase of Extracellular Signal-Regulated Kinase (ERK1/2) phosphorylation and the arrestin-dependent late phase of p38 MAPK signaling...
January 11, 2017: Cellular Signalling
https://www.readbyqxmd.com/read/28088065/methionine-enkephalin-menk-mounts-antitumor-effect-via-regulating-dendritic-cells-dcs
#5
Yiming Meng, Xinghua Gao, Wenna Chen, Nicolas P Plotnikoff, Noreen Griffin, Guirong Zhang, Fengping Shan
MENK, an endogenous opioid peptide has been reported to have many immunological and antitumor activities. So far the detailed mechanisms of antitumor through regulating DCs by MENK have not been elucidated yet. The aim of this work was to investigate the antitumor mechanisms of MENK via regulating DC. The monitoring methods, such as ELISA, MTS assay, CFSE, Real-time PCR and Western blot were included in our research. We found bone marrow derived dendritic cells (BMDCs) in 36 female C57BL/6 mice treated with MENK enhanced expression of key surface molecules, increased production of critical cytokines reduced endocytosis of FITC-dextran, upregulated TLR4 through MyD88/NF-κB signaling pathway and mounted higher antitumor activity...
January 11, 2017: International Immunopharmacology
https://www.readbyqxmd.com/read/28087216/denosumab-and-alendronate-treatment-in-patients-with-back-pain-due-to-fresh-osteoporotic-vertebral-fractures
#6
Tomoko Tetsunaga, Tomonori Tetsunaga, Keiichiro Nishida, Masato Tanaka, Yoshihisa Sugimoto, Tomoyuki Takigawa, Yoshitaka Takei, Toshifumi Ozaki
INTRODUCTION: Denosumab specifically inhibits the receptor activator for nuclear factor-kappa B ligand (RANKL), and prevents osteoporotic fractures. Several reports have analyzed the effects of denosumab and alendronate alone on bone mineral density (BMD) or reduction of fracture risk. The objective of this study was to analyze the effects of antiresorptive osteoporosis pharmacotherapy on pain relief in patients with fresh vertebral fracture. METHODS: This retrospective, single-center study included 80 patients (10 males, 70 females) with fresh osteoporotic vertebral fractures treated using denosumab at a dose of 60 mg subcutaneously every 6 months (40 patients) or alendronate at a dose of 35 mg orally every week (40 patients) for 6 months in our hospital...
January 10, 2017: Journal of Orthopaedic Science: Official Journal of the Japanese Orthopaedic Association
https://www.readbyqxmd.com/read/28086911/enhanced-neuroinflammation-mediated-by-dna-methylation-of-the-glucocorticoid-receptor-triggers-cognitive-dysfunction-after-sevoflurane-anesthesia-in-adult-rats-subjected-to-maternal-separation-during-the-neonatal-period
#7
Yangzi Zhu, Yu Wang, Rui Yao, Ting Hao, Junli Cao, He Huang, Liwei Wang, Yuqing Wu
BACKGROUND: Mounting evidence indicates that children who experience abuse and neglect are prone to chronic diseases and premature mortality later in life. One mechanistic hypothesis for this phenomenon is that early life adversity alters the expression or functioning of the glucocorticoid receptor (GR) throughout the course of life and thereby increases sensitivity to inflammatory stimulation. An exaggerated pro-inflammatory response is generally considered to be a key cause of postoperative cognitive dysfunction (POCD)...
January 7, 2017: Journal of Neuroinflammation
https://www.readbyqxmd.com/read/28079268/renoprotective-effect-of-hypericum-perforatum-against-diabetic-nephropathy-in-rats-insights-in-the-underlying-mechanisms
#8
Dalia M Abd El Motteleb, Dalia I Abd El Aleem
Oxidative stress and inflammation play a key role in the initiation and progression of diabetic nephropathy (DN). The present study aimed to investigate the possible protective effect of hypericum perforatum (HP) against DN. Rats were allocated into six groups; control: received normal saline, diabetic untreated (DM): received single dose of streptozotocin (STZ) after injection of nicotinamide (NA), gliclazide: received STZ,NA+ gliclazide (10mg/kg), DM+HP50, DM+HP100, DM+HP200:received STZ,NA and HP 50, 100, 200 mg/kg respectively...
January 12, 2017: Clinical and Experimental Pharmacology & Physiology
https://www.readbyqxmd.com/read/28078198/multidisciplinary-approach-to-management-of-temporal-bone-giant-cell-tumor
#9
Taija K Nicoli, Riste Saat, Risto Kontio, Anna Piippo, Maija Tarkkanen, Jussi Tarkkanen, Jussi Jero
Background Giant cell tumors (GCTs) are rare osseous tumors that rarely appear in the skull. Methods We review the clinical course of a 28-year-old previously healthy woman with a complicated GCT. Results The reviewed patient presented with a middle cranial fossa tumor acutely complicated by reactive mastoiditis. Left tympanomastoidectomy was performed for drainage of the mastoiditis and for biopsies of the tumor. Due to the challenging tumor location, the patient was treated with denosumab, a fully humanized monoclonal antibody against receptor activator of nuclear factor kappa-B ligand, for 7 months, which resulted in significant preoperative tumor shrinkage...
July 2016: Journal of Neurological Surgery Reports
https://www.readbyqxmd.com/read/28078083/over-expression-of-toll-like-receptor-2-up-regulates-heme-oxygenase-1-expression-and-decreases-oxidative-injury-in-dairy-goats
#10
Shoulong Deng, Kun Yu, Wuqi Jiang, Yan Li, Shuotian Wang, Zhuo Deng, Yuchang Yao, Baolu Zhang, Guoshi Liu, Yixun Liu, Zhengxing Lian
BACKGROUND: Mastitis, an infection caused by Gram-positive bacteria, produces udder inflammation and oxidative injury in milk-producing mammals. Toll-like receptor 2 (TLR2) is important for host recognition of invading Gram-positive microbes. Over-expression of TLR2 in transgenic dairy goats is a useful model for studying various aspects of infection with Gram-positive bacteria, in vivo. METHODS: We over-expressed TLR2 in transgenic dairy goats. Pam3CSK4, a component of Gram-positive bacteria, triggered the TLR2 signal pathway by stimulating the monocytes-macrophages from the TLR2-positive transgenic goats, and induced over-expression of activator protein-1 (AP-1), phosphatidylinositol 3-kinase (PI3K) and transcription factor nuclear factor kappa B (NF-κB) and inflammation factors downstream of the signal pathway...
2017: Journal of Animal Science and Biotechnology
https://www.readbyqxmd.com/read/28077890/effect-of-lead-nanoparticles-inhalation-on-bone-calcium-sensing-receptor-hydroxyapatite-crystal-and-receptor-activator-of-nuclear-factor-kappa-b-in-rats
#11
Rendra Leonas, Zairin Noor, Hermawan Nagar Rasyid, Tita Husnitawati Madjid, Fachry Ambia Tanjung
This study aimed to investigate whether Pb nanoparticle exposure affects the bone calcium sensing receptor (CaSR), hydroxyapatite crystal, and receptor activator of nuclear factor-kappa B (RANK) in rats exposed to subchronic and chronic inhalation. Thirty two rats were randomly divided into eight groups. One group is a non-exposed group. While three groups were exposed to nanoparticles Pb at the following doses 6.25; 12.5; or 25 mg/m(3) an hour daily for 28 days. Another three groups were exposed to nanoparticles Pb at following doses 6...
October 2016: Acta Informatica Medica: AIM
https://www.readbyqxmd.com/read/28071341/identification-of-novel-hits-as-highly-prospective-dual-agonists-for-mu-and-kappa-opioid-receptors-an-integrated-in-silico-approach
#12
Indrani Bera, Mrinal Vishwas Marathe, Pavan V Payghan, Nanda Ghoshal
Opioid agonists are used clinically for the treatment of acute and chronic pain, however, their clinical use is limited due to the presence of undesired side effects. Dual agonists, simultaneously targeting mu and kappa opioid receptors, show fewer side effects than that of selective agonists. In the present work, 2D- and 3D- Quantitative Structure Activity Relationship studies were performed on a series of aminomorphinan derivatives as dual agonists, using a wide range of descriptors. The aim of the study was to identify the structural requirements for the activity of these compounds towards mu and kappa opioid receptors and using the models, with best external predictability, for predicting the activities of new hits obtained from shape based virtual screening of drug like compounds from ZINC database...
January 10, 2017: Journal of Biomolecular Structure & Dynamics
https://www.readbyqxmd.com/read/28066106/modulation-of-hippocampal-gene-expression-of-microrna-146a-microrna-155-nuclear-factor-kappa-b-inflammatory-signaling-by-troxerutin-in-healthy-and-diabetic-rats
#13
Raana Yavari, Reza Badalzadeh, Mohammad Reza Alipour, Seyed Mahmoud Tabatabaei
OBJECTIVES: Inflammation plays a critical role in the progression of diabetic complications such as neurological disorders. Previous reports have indicated the memory-improving effect of troxerutin, in rat hippocampus, but the underlying mechanisms are unclear. Hence, we have investigated the effect of troxerutin pretreatment on gene expressions of inflammation-related microRNAs (miRs), miR-146a and miR-155, and nuclear factor-kappa B (NF-κB) signaling pathway in the hippocampus of healthy and diabetic rats...
November 2016: Indian Journal of Pharmacology
https://www.readbyqxmd.com/read/28064383/algorithms-for-prediction-of-the-oncotype-dx-recurrence-score-using-clinicopathologic-data-a-review-and-comparison-using-an-independent-dataset
#14
REVIEW
Michael R Harowicz, Timothy J Robinson, Michaela A Dinan, Ashirbani Saha, Jeffrey R Marks, P Kelly Marcom, Maciej A Mazurowski
PURPOSE: Given the potential savings in cost and resource utilization, several algorithms have been proposed to predict Oncotype DX recurrence score (ODX RS) using commonly acquired histopathologic variables. Although it is promising, additional independent validation of these surrogate markers is needed prior to guide the patient management. METHODS: In this retrospective study, we analyzed 305 patients with invasive breast cancer at our institution who had ODX RS available...
January 7, 2017: Breast Cancer Research and Treatment
https://www.readbyqxmd.com/read/28061403/berberine-ameliorates-intrahippocampal-kainate-induced-status-epilepticus-and-consequent-epileptogenic-process-in-the-rat-underlying-mechanisms
#15
Reza Sedaghat, Yosra Taab, Zahra Kiasalari, Siamak Afshin-Majd, Tourandokht Baluchnejadmojarad, Mehrdad Roghani
Status epilepticus (SE) is a life-threatening neurologic condition, instigating epileptogenesis to transform normal brain to an epileptic condition. SE is followed by spontaneous recurrent seizures (SRS) and final development of temporal lobe epilepsy (TLE) that is resistant to treatment. Neuroprotective strategies are increasingly put forward as a promising therapy to prevent and/or manage epileptic conditions. In this study, we investigated whether berberis alkaloid, i.e. berberine (BBR), could ameliorate intrahippocampal kainate-induced SE and its consequent epileptogenic process and to explore some underlying mechanisms...
January 3, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28059970/artesunate-protects-against-the-organ-injury-and-dysfunction-induced-by-severe-hemorrhage-and-resuscitation
#16
Regina Sordi, Kiran K Nandra, Fausto Chiazza, Florence L Johnson, Claudia P Cabrera, Hew D Torrance, Noriaki Yamada, Nimesh S A Patel, Michael R Barnes, Karim Brohi, Massimo Collino, Christoph Thiemermann
OBJECTIVE: To evaluate the effects of artesunate on organ injury and dysfunction associated with hemorrhagic shock (HS) in the rat. BACKGROUND: HS is still a common cause of death in severely injured patients and is characterized by impairment of organ perfusion, systemic inflammatory response, and multiple organ failure. There is no specific therapy that reduces organ injury/dysfunction. Artesunate exhibits pharmacological actions beyond its antimalarial activity, such as anticancer, antiviral, and anti-inflammatory effects...
February 2017: Annals of Surgery
https://www.readbyqxmd.com/read/28056342/pathway-and-cell-specific-kappa-opioid-receptor-modulation-of-excitation-inhibition-balance-differentially%C3%A2-gates-d1-and-d2-accumbens-neuron-activity
#17
Hugo A Tejeda, Jocelyn Wu, Alana R Kornspun, Marco Pignatelli, Vadim Kashtelyan, Michael J Krashes, Brad B Lowell, William A Carlezon, Antonello Bonci
Endogenous dynorphin signaling via the kappa-opioid receptor (KOR) in the nucleus accumbens (NAcc) powerfully mediates negative affective states and stress reactivity. Excitatory inputs from the hippocampus and amygdala play a fundamental role in shaping the activity of both NAcc D1 and D2 MSNs, which encode positive and negative motivational valences, respectively. However, a circuit-based mechanism by which KOR modulation of excitation-inhibition balance modifies D1 and D2 MSN activity is lacking. Here, we provide a comprehensive synaptic framework wherein presynaptic KOR inhibition decreases the excitatory drive of D1 MSN activity by the amygdala, but not the hippocampus...
January 4, 2017: Neuron
https://www.readbyqxmd.com/read/28054961/the-in-vitro-and-in-vivo-anti-inflammatory-effects-of-a-phthalimide-ppar-%C3%AE-agonist
#18
Mingzhi Su, Jiafu Cao, Jin Huang, Sen Liu, Dong Soon Im, Jin-Wook Yoo, Jee H Jung
Previously, the authors found that 4-hydroxy-2-(4-hydroxyphenethyl) isoindoline-1,3-dione (PD1) (a phthalimide analogue) bound to and activated peroxisome proliferator-activated receptor-γ (PPAR-γ). Since PPAR-γ suppresses inflammatory responses, the present study was undertaken to investigate the anti-inflammatory effects of PD1. In lipopolysaccharide (LPS)-stimulated murine RAW264.7 macrophages, PD1 suppressed the inductions of pro-inflammatory factors, including inducible nitric oxide synthase (iNOS), nitric oxide (NO), cyclooxygenase 2 (COX-2), tumor necrosis factor α (TNF-α), interleukin-1β (IL-1β), and interleukin-6 (IL-6)...
January 4, 2017: Marine Drugs
https://www.readbyqxmd.com/read/28049625/regulation-of-the-macrophage-oxytocin-receptor-in-response-to-inflammation
#19
Angela Szeto, Ni Sun-Suslow, Armando J Mendez, Rosa I Hernandez, Klaus V Wagner, Philip M McCabe
It has been demonstrated that the neuropeptide oxytocin (OT) attenuates oxidative stress and inflammation in macrophages. In the current study, we examined the role of inflammation on the expression of the oxytocin receptor (OXTR). We hypothesized that OXTR expression is increased during the inflammation though a nuclear factor kappa B (NF-κB) mediated pathway, thus responding as an acute phase protein. Inflammation was induced by treating macrophages (human primary, THP-1, and murine) with lipopolysaccharide (LPS) and monitored by expression of IL-6...
January 3, 2017: American Journal of Physiology. Endocrinology and Metabolism
https://www.readbyqxmd.com/read/28044208/hepatic-vagus-nerve-regulates-kupffer-cell-activation-via-%C3%AE-7-nicotinic-acetylcholine-receptor-in-nonalcoholic-steatohepatitis
#20
Takahiro Nishio, Kojiro Taura, Keiko Iwaisako, Yukinori Koyama, Kazutaka Tanabe, Gen Yamamoto, Yukihiro Okuda, Yoshinobu Ikeno, Kenji Yoshino, Yosuke Kasai, Masayuki Okuno, Satoru Seo, Takaki Sakurai, Masataka Asagiri, Etsuro Hatano, Shinji Uemoto
BACKGROUND: Nonalcoholic fatty liver disease ranges from simple steatosis to nonalcoholic steatohepatitis (NASH). Kupffer cells play a central role in promoting hepatic inflammation, which leads to the development of NASH. We investigated the anti-inflammatory effect of hepatic vagus-mediated stimulation of the α7 nicotinic acetylcholine receptor (α7nAChR) on Kupffer cells in NASH pathogenesis. METHODS: Wild-type (WT) mice undergoing hepatic vagotomy (HV) were fed a methionine- and choline-deficient (MCD) diet for 1 week...
January 2, 2017: Journal of Gastroenterology
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