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https://www.readbyqxmd.com/read/29334672/oxidative-and-interactive-challenge-of-cadmium-and-ocean-acidification-on-the-smooth-scallop-flexopecten-glaber
#1
Alessandro Nardi, Maura Benedetti, Daniele Fattorini, Francesco Regoli
Ocean acidification (OA) may affect sensitivity of marine organisms to metal pollution modulating chemical bioavailability, bioaccumulation and biological responsiveness of several cellular pathways. In this study, the smooth scallop Flexopecten glaber was exposed to various combinations of reduced pH (pH/pCO2 7.4/∼3000 μatm) and Cd (20 μg/L). The analyses on cadmium uptake were integrated with those of a wide battery of biomarkers including metallothioneins, single antioxidant defenses and total oxyradical scavenging capacity in digestive gland and gills, lysosomal membrane stability and onset of genotoxic damage in haemocytes...
January 8, 2018: Aquatic Toxicology
https://www.readbyqxmd.com/read/29334671/glucosamine-promotes-osteoblast-proliferation-by-modulating-autophagy-via-the-mammalian-target-of-rapamycin-pathway
#2
Chen Lv, Lu Wang, Xiongbai Zhu, Wenjun Lin, Xin Chen, Zhengxiang Huang, Lintuo Huang, Shengwu Yang
Glucosamine is effective in the treatment of osteoarthritis; however, its effect on osteoporosis remains unclear. Decreased activity of osteoblasts is the main cause of osteoporosis. Here, we examined the effects of glucosamine on osteoblasts. The potential underlying mechanisms were explored. The results showed that glucosamine had a biphasic effect on the viability of hFOB1.19 osteoblasts. At low concentrations (<0.6 mM), glucosamine induced hFOB1.19 cell proliferation, whereas at high concentrations (>0...
January 12, 2018: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29334668/lidanpaidu-prescription-alleviates-lipopolysaccharide-induced-acute-kidney-injury-by-suppressing-the-nf-%C3%AE%C2%BAb-signaling-pathway
#3
Fan Zhang, Shan Lu, Siyi Jin, Keli Chen, Juan Li, Bisheng Huang, Yan Cao
The Lidanpaidu Prescription (LDP), a hospital preparation, composed of Chinese classical preparations, has been reported to have antiendotoxin, anticoagulant and other effects. However, its therapeutic effect on lipopolysaccharide (LPS)-induced acute kidney injury (AKI) and the mechanisms remain unclear. Therefore, we administered LPD pretreatment at different doses to examine the protective effects and mechanisms in LPS-induced AKI in mice. The kidney injury induced by LPS was assessed by histological examination...
January 12, 2018: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29334665/i-7ab-inhibited-the-growth-of-tnbc-cells-via-targeting-hdac3-and-promoting-the-acetylation-of-p53
#4
Mei Yang, Xuefei Dang, Yue Tan, Meixing Wang, Xiaojing Li, Gang Li
Triple negative breast cancer (TNBC) is a heterogenous disease with high aggressive and poor outcome. The lack of biomarkers and targeted therapies makes it a challenge for the treatment of TNBC. Histone deacetylase inhibitors (HDACis) are emerging as novel anti-tumor agents in many types of human cancers. In this study, we found that I-7ab, a novel HDACi, inhibited the cell viability of TNBC cells and induced the cell apoptosis. Mechanistically, I-7ab specifically decreased the expression of HDAC3 and promoted the acetylation of p53 at both Lys373 and Lys382 amino acids...
January 12, 2018: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29334656/activated-protein-c-suppresses-osteoclast-differentiation-via-endothelial-protein-c-receptor-protease-activated-receptor-1-sphingosine-1-phosphate-receptor-and-apolipoprotein-e-receptor-2
#5
Kakunoshin Yoshida, Nobuyuki Akita, Takayuki Okamoto, Kunihiro Asanuma, Atsumasa Uchida, Akihiro Sudo, Motomu Shimaoka, Koji Suzuki, Tatsuya Hayashi
INTRODUCTION: Bone remodeling relies on a delicate balance between formation and resorption of bone tissues, processes in which bone-forming osteoblasts and bone-resorbing osteoclasts play central roles. Recently, we reported that anticoagulant activated protein C (APC) promotes osteoblast proliferation, but the role of the blood coagulation system in bone remodeling remains unclear. In this study, to further elucidate the relationship between bone remodeling and blood coagulation, we investigated the effect of APC on osteoclast differentiation...
January 3, 2018: Thrombosis Research
https://www.readbyqxmd.com/read/29334622/pyridazinone-hybrids-design-synthesis-and-evaluation-as-potential-anticonvulsant-agents
#6
Sangh Partap, Md Jawaid Akhtar, Mohammed Shahar Yar, Mohd Zaheen Hassan, Anees Ahmad Siddiqui
A series of new hybrid benzothiazole containing pyridazinones derivatives were designed and synthesized fulfilling all the pharmacophoric requirements essential for the anticonvulsant activity. In-silico and in vitro studies revealed that some of these hybrid derivatives demonstrated admirable GABA AT inhibitory activity. An attempt has also been made to validate the results of in vitro GABA AT inhibition of the most potent compound SPS-5F (IC50 9.10 μM) through in vivo anticonvulsant screening. Compound SPS-5F administration significantly increases the whole brain GABA level, might be through the inhibition of GABA AT enzyme...
January 3, 2018: Bioorganic Chemistry
https://www.readbyqxmd.com/read/29334602/high-dose-metformin-plus-temozolomide-shows-increased-anti-tumor-effects-in-glioblastoma-in-vitro-and-in-vivo-compared-with-monotherapy
#7
Jung Eun Lee, Ji Hee Lim, Yong Kil Hong, Seung Ho Yang
Purpose: The purpose of the study is to investigate the efficacy of combined treatment with temozolomide (TMZ) and metformin for glioblastoma (GBM) in vitro and in vivo. Materials and Methods: We investigated the efficacy of combined treatment with TMZ and metformin using cell viability and apoptosis assays. A GBM orthotopic mice model was established by inoculation of 5x105 U87 cells and treated with metformin, TMZ, and the combination for 4 weeks. Western blotting and immunofluorescence of tumor specimens were analyzed to investigate AMP-activated protein kinase (AMPK) and AKT pathway...
January 10, 2018: Cancer Research and Treatment: Official Journal of Korean Cancer Association
https://www.readbyqxmd.com/read/29334566/deficiency-of-transforming-growth-factor-%C3%AE-signaling-disrupts-memory-processes-in-rats
#8
Vladimir I Arkhipov, Ekaterina V Pershina, Sergey G Levin
Cytokines, in addition to their participation in immune and inflammatory processes, play an important role in synaptic plasticity, neoneurogenesis, and cognitive functions. In our work, we aimed to clarify the role of the transforming growth factor-β (TGF-β), which is recognized as a multifunctional cytokine, in memory processes. Behavioral experiments were carried out in rats using step-through passive avoidance test. The results obtained showed that the learning of animals after treatment with SB431542, a selective inhibitor of TGF-β receptors, was impaired, which indicated a significant memory deterioration...
January 12, 2018: Neuroreport
https://www.readbyqxmd.com/read/29334511/evaluation-of-recombinant-factor-viia-tranexamic-acid-and-desmopressin-to-reduce-prasugrel-related-bleeding-a-randomised-placebo-controlled-study-in-a-rabbit-model
#9
Fanny Bonhomme, Thomas Lecompte, Charles M Samama, Anne Godier, Pierre Fontana
BACKGROUND: Prasugrel is a thienopyridine that inhibits platelet aggregation more rapidly and effectively than clopidogrel, with an increased bleeding risk. OBJECTIVE: The current study aimed to evaluate the efficacy of three nonspecific haemostatic drugs - recombinant activated factor VII (rFVIIa), tranexamic acid and desmopressin (DDAVP) - to limit blood loss after administration of prasugrel in a rabbit model of bleeding while also evaluating any prothrombotic effects...
January 13, 2018: European Journal of Anaesthesiology
https://www.readbyqxmd.com/read/29334500/overexpression-of-%C3%A2%C2%B5-opioid-receptors-in-peripheral-afferents-but-not-in-combination-with-enkephalin-decreases-neuropathic-pain-behavior-and-enhances-opioid-analgesia-in-mouse
#10
Amanda H Klein, Husam K Mohammad, Rabiah Ali, Brad Peper, Steven P Wilson, Srinivasa N Raja, Matthias Ringkamp, Sarah Sweitzer
BACKGROUND: The current study used recombinant herpes simplex virus type I to increase expression of µ-opiate receptors and the opioid ligand preproenkephalin in peripheral nerve fibers in a mouse model of neuropathic pain. It was predicted that viral vector delivery of a combination of genes encoding the µ-opioid receptor and preproenkephalin would attenuate neuropathic pain and enhance opioid analgesia. The behavioral effects would be paralleled by changes in response properties of primary afferent neurons...
January 15, 2018: Anesthesiology
https://www.readbyqxmd.com/read/29334476/biological-control-of-botrytis-cinerea-interactions-with-native-vineyard-yeasts-from-washington-state
#11
Xuefei Wang, Dean A Glawe, Elizabeth K Kramer, David M Weller, Patricia Ann Okubara
Native yeasts are of increasing interest to researchers, grape growers, and vintners because of their potential for biocontrol activity, and their contributions to the aroma, flavor and mouthfeel qualities of wines. To assess biocontrol activity, we tested 11 yeasts from Washington vineyards, representing isolates of Candida saitoana, Curvibasidium pallidicorallinum, Metschnikowia chrysoperlae, Metschnikowia pulcherrima, Meyerozyma guilliermondii, Saccharomyces cerevisiae and Wickerhamomyces anomalus, for ability to colonize 'Thompson Seedless' grape berries, inhibit the growth of Botrytis cinerea in vitro, and suppress disease symptoms on isolated berries...
January 15, 2018: Phytopathology
https://www.readbyqxmd.com/read/29334438/in-vitro-and-in-vivo-evaluations-of-the-anticalculus-effect-of-a-novel-stabilized-stannous-fluoride-dentifrice
#12
Tao He, Mary Kay Anastasia, Marianne Zsiska, Teresa Farmer, Eva Schneiderman, Jeffery L Milleman
OBJECTIVES: To evaluate the effect of a novel stannous fluoride dentifrice with zinc citrate on calculus inhibition using both in vitro and clinical models. METHODS: Each investigation tested a novel stabilized 0.454% stannous fluoride dentifrice with zinc citrate as an anticalculus agent (Crest® Pro-Health™ smooth formula) compared to a negative control fluoride dentifrice. The in vitro study used the modified Plaque Growth and Mineralization Model (mPGM). Plaque biofilms were prepared and mineralized by alternate immersion of glass rods in human saliva and artificial mineralization solution...
December 2017: Journal of Clinical Dentistry
https://www.readbyqxmd.com/read/29334435/comparative-antiplaque-effect-of-two-antimicrobial-dentifrices-laboratory-and-clinical-evaluations
#13
Lynn R Friesen, C R Goyal, Jimmy G Qaqish, Tao He, Rachelle Eusebio, Marianne Zsiska, Teresa Farmer, Eva Schneiderman
OBJECTIVES: To compare the effect of a stannous fluoride dentifrice versus a triclosan-containing dentifrice on the reduction of plaque using in vitro and clinical models. METHODS: Both investigations evaluated a novel 0.454% stabilized stannous fluoride dentifrice (Crest® Pro-Health™ smooth formula) versus a sodium fluoride/triclosan positive control dentifrice (Colgate® Total®). The in vitro evaluation utilized the Plaque Glycolysis and Regrowth Model (PGRM), wherein the metabolic effects (acid production/glycolysis inhibition) of the dentifrices were assessed on plaque biofilms grown on glass rods after three days growth and a single dentifrice treatment...
December 2017: Journal of Clinical Dentistry
https://www.readbyqxmd.com/read/29334430/preclinical-therapeutic-efficacy-of-the-ciprofloxacin-eluting-sinus-stent-for-pseudomonas-aeruginosa-sinusitis
#14
Do-Yeon Cho, Dong-Jin Lim, Calvin Mackey, Daniel Skinner, Christopher Weeks, Gobind S Gill, Robert W Hergenrother, William E Swords, Bradford A Woodworth
BACKGROUND: The ciprofloxacin-coated sinus stent (CSS) has unique therapeutic potential to deliver antibiotics to the sinuses. The objective of this study is to evaluate the efficacy of the CSS stent in eliminating Pseudomonas aeruginosa infection in a rabbit model of sinusitis. METHODS: A ciprofloxacin-eluting sinus stent was created by coating ciprofloxacin/Eudragit RS100 on biodegradable poly-D/L-lactic acid (2 mg). After analyzing in-vitro inhibition of P aeruginosa (PAO-1 strain) biofilm formation, a total of 8 stents (4 shams, 4 CSSs) were placed unilaterally in rabbit maxillary sinuses via dorsal sinusotomy after inducing infection for 1 week with PAO-1...
January 15, 2018: International Forum of Allergy & Rhinology
https://www.readbyqxmd.com/read/29334408/effects-of-metalaxyl-enantiomers-stress-on-root-activity-and-leaf-antioxidant-enzyme-activities-in-tobacco-seedlings
#15
Song Fang, Yi Tao, Yizhi Zhang, Fanyu Kong, Yunbai Wang
The objective of this experiment was to study the effects of metalaxyl enantiomers on the activity of roots and antioxidative enzymes in tobacco seedlings. Water culture experiment was conducted to analyze the effects of different concentrations of metalaxyl enantiomers (30 and 10 mg L-1 ) on root activity and leaf superoxide dismutase (SOD), peroxidase (POD), and catalase (CAT) activities and malondialdehyde (MDA) content of tobacco seedlings. The results showed that metalaxyl significantly inhibited root activity and significantly improved leaf SOD, POD, and CAT activities and MDA content...
January 15, 2018: Chirality
https://www.readbyqxmd.com/read/29334406/dasatinib-induced-pulmonary-arterial-hypertension
#16
REVIEW
Nurgül Özgür Yurttaş, Ahmet Emre Eşkazan
Drug-induced (Group 1) pulmonary hypertension (PH) is an important subgroup of PH involving dasatinib as a likely related agent, which is a second-generation tyrosine kinase inhibitor (TKI), that is used in the treatment of chronic myeloid leukemia (CML). The mechanism of dasatinib-induced pulmonary arterial hypertension (PAH) is unclear. However, the occurence of PAH at a late onset in CML patients suggests a chronic pathological mechanism with an insidious onset rather than an acute inflammatory or cardiac etiology...
January 15, 2018: British Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/29334394/substitution-of-the-laser-borane-anti-b18h22-with-pyridine-a-structural-and-photophysical-study-of-some-unusually-structured-macropolyhedral-boron-hydrides
#17
Michael G S Londesborough, Jiří Dolanský, Tomáš Jelínek, John D Kennedy, Ivana Císařová, Robert D Kennedy, Daniel Roca-Sanjuán, Antonio Francés-Monerris, Kamil Lang, William Clegg
Reaction of anti-B18H221 with pyridine in neutral solvents gives sparingly soluble B16H18-3',8'-Py23a as the major product (ca. 53%) and B18H20-6',9'-Py22 (ca. 15%) as the minor product, with small quantities of B18H20-8'-Py 4 (ca. 1%) also being formed. The three new compounds 2, 3a and 4 are characterized by single-crystal X-ray diffraction analyses and by multinuclear multiple-resonance NMR spectroscopy. Compound 2 is of ten-vertex nido:ten-vertex arachno two-atoms-in-common architecture, long postulated for a species with borons-only cluster constitution, but previously elusive...
January 15, 2018: Dalton Transactions: An International Journal of Inorganic Chemistry
https://www.readbyqxmd.com/read/29334376/positively-selected-enhancer-elements-endow-osteosarcoma-cells-with-metastatic-competence
#18
James J Morrow, Ian Bayles, Alister P W Funnell, Tyler E Miller, Alina Saiakhova, Michael M Lizardo, Cynthia F Bartels, Maaike Y Kapteijn, Stevephen Hung, Arnulfo Mendoza, Gursimran Dhillon, Daniel R Chee, Jay T Myers, Frederick Allen, Marco Gambarotti, Alberto Righi, Analisa DiFeo, Brian P Rubin, Alex Y Huang, Paul S Meltzer, Lee J Helman, Piero Picci, Henri Versteeg, John Stamatoyannopolus, Chand Khanna, Peter C Scacheri
Metastasis results from a complex set of traits acquired by tumor cells, distinct from those necessary for tumorigenesis. Here, we investigate the contribution of enhancer elements to the metastatic phenotype of osteosarcoma. Through epigenomic profiling, we identify substantial differences in enhancer activity between primary and metastatic human tumors and between near isogenic pairs of highly lung metastatic and nonmetastatic osteosarcoma cell lines. We term these regions metastatic variant enhancer loci (Met-VELs)...
January 15, 2018: Nature Medicine
https://www.readbyqxmd.com/read/29334375/a-small-molecule-inhibitor-of-the-ubiquitin-activating-enzyme-for-cancer-treatment
#19
Marc L Hyer, Michael A Milhollen, Jeff Ciavarri, Paul Fleming, Tary Traore, Darshan Sappal, Jessica Huck, Judy Shi, James Gavin, Jim Brownell, Yu Yang, Bradley Stringer, Robert Griffin, Frank Bruzzese, Teresa Soucy, Jennifer Duffy, Claudia Rabino, Jessica Riceberg, Kara Hoar, Anya Lublinsky, Saurabh Menon, Michael Sintchak, Nancy Bump, Sai M Pulukuri, Steve Langston, Stephen Tirrell, Mike Kuranda, Petter Veiby, John Newcomb, Ping Li, Jing Tao Wu, Josh Powe, Lawrence R Dick, Paul Greenspan, Katherine Galvin, Mark Manfredi, Chris Claiborne, Benjamin S Amidon, Neil F Bence
The ubiquitin-proteasome system (UPS) comprises a network of enzymes that is responsible for maintaining cellular protein homeostasis. The therapeutic potential of this pathway has been validated by the clinical successes of a number of UPS modulators, including proteasome inhibitors and immunomodulatory imide drugs (IMiDs). Here we identified TAK-243 (formerly known as MLN7243) as a potent, mechanism-based small-molecule inhibitor of the ubiquitin activating enzyme (UAE), the primary mammalian E1 enzyme that regulates the ubiquitin conjugation cascade...
January 15, 2018: Nature Medicine
https://www.readbyqxmd.com/read/29334371/cooperative-targeting-of-melanoma-heterogeneity-with-an-axl-antibody-drug-conjugate-and-braf-mek-inhibitors
#20
Julia Boshuizen, Louise A Koopman, Oscar Krijgsman, Aida Shahrabi, Elke Gresnigt- van den Heuvel, Maarten A Ligtenberg, David W Vredevoogd, Kristel Kemper, Thomas Kuilman, Ji-Ying Song, Nora Pencheva, Jens Thing Mortensen, Marnix Geukes Foppen, Elisa A Rozeman, Christian U Blank, Maarten L Janmaat, David Satijn, Esther C W Breij, Daniel S Peeper, Paul W H I Parren
Intratumor heterogeneity is a key factor contributing to therapeutic failure and, hence, cancer lethality. Heterogeneous tumors show partial therapy responses, allowing for the emergence of drug-resistant clones that often express high levels of the receptor tyrosine kinase AXL. In melanoma, AXL-high cells are resistant to MAPK pathway inhibitors, whereas AXL-low cells are sensitive to these inhibitors, rationalizing a differential therapeutic approach. We developed an antibody-drug conjugate, AXL-107-MMAE, comprising a human AXL antibody linked to the microtubule-disrupting agent monomethyl auristatin E...
January 15, 2018: Nature Medicine
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