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https://www.readbyqxmd.com/read/27923259/-established-therapies-and-new-therapeutic-strategies-in-alcoholic-liver-disease
#1
Helmut Karl Seitz, Sebastian Mueller
Chronical alcohol abuse causes more than 200 diseases and/or symptoms and among these alcoholic liver disease (ALD) is of special importance since it occurs frequently and may be life-threatening. In Europe alcohol consumption as well as ALD increased as compared to the rest of the world. It has been estimated that in Europe approximately 500 000 people die every year due to ALD. ALD consists of alcoholic fatty liver, alcoholic steatohepatitis (ASH), alcoholic cirrhosis and hepatocellar cancer (HCC ). Alcohol hepatitis (AH) is a clinical feature with jaundice and liver failure and a high mortality...
December 6, 2016: Zeitschrift Für Gastroenterologie
https://www.readbyqxmd.com/read/27923201/synthesis-and-biological-evaluation-of-a-new-class-of-benzothiazines-as-neuroprotective-agents
#2
Alessandra Mancini, Alessia Chelini, Angela Di Capua, Loretta Castelli, Simone Brogi, Marco Paolino, Germano Giuliani, Andrea Cappelli, Maria Frosini, Lorenzo Ricci, Erminia Leonelli, Gianluca Giorgi, Antonio Giordani, Jacopo Magistretti, Maurizio Anzini
Neurodegenerative diseases are disorders related to the degeneration of central neurons that gradually lead to various, severe alterations of cognitive and/or motor functions. Currently, for no such diseases does any pharmacological treatment exist able to arrest its progression. Riluzole (1) is a small molecule able to interfere with multiple cellular and molecular mechanisms of neurodegeneration, and is the only approved treatment of amyotrophic lateral sclerosis (ALS), the progression of which proved to significantly slow, thus increasing somewhat average survival...
November 27, 2016: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27923191/a-highly-specific-ratiometric-two-photon-fluorescent-probe-to-detect-dipeptidyl-peptidase-iv-in-plasma-and-living-systems
#3
Li-Wei Zou, Ping Wang, Xing-Kai Qian, Lei Feng, Yang Yu, Dan-Dan Wang, Qiang Jin, Jie Hou, Zhi-Hong Liu, Guang-Bo Ge, Ling Yang
In this study, a highly specific ratiometric two-photon fluorescent probe GP-BAN was developed and well-characterized to monitor dipeptidyl peptidase IV in plasma and living systems. GP-BAN was designed on the basis of the catalytic properties and substrate preference of DPP-IV, and it could be readily hydrolyzed upon addition of DPP-IV under physiological conditions. Both reaction phenotyping and inhibition assays demonstrated that GP-BAN displayed good reactivity and high selectivity towards DPP-IV over other human serine hydrolases including FAP, DPP-VIII, and DPP-IX...
November 30, 2016: Biosensors & Bioelectronics
https://www.readbyqxmd.com/read/27923157/adjuvant-neuronal-nitric-oxide-synthase-inhibition-for-combined-treatment-of-epilepsy-and-comorbid-depression
#4
Tanveer Singh, Rajesh Kumar Goel
BACKGROUND: Elevated nitric oxide (NO) levels in the brain have been apparently associated with depression in kindled animals. Owing to the major role of neuronal nitric oxide synthase (nNOS) in brain and ineffectiveness of antiepileptic drugs (AEDs) in restoring nitrosative stress, the present study was envisaged to evaluate the adjuvant nNOS inhibitor, 7-nitroindazole (7-NI) with valproic acid for combined treatment of epilepsy and associated depression. METHODS: Pentylenetetrazole kindled animals associated with depression were treated with vehicle, valproate (300mg/kg/day ip), valproate with 7-NI (10mg/kg; 20mg/kg; 40mg/kg)/day ip and 7-NI (40mg/kg/day ip) for 15days...
October 4, 2016: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/27923151/a-novel-role-for-the-kr%C3%A3-ppel-like-factor-14-on-macrophage-inflammatory-response-and-atherosclerosis-development
#5
Xiao Wei, Ruomei Yang, Chengpan Wang, Xun Jian, Ling Li, Hua Liu, Gangyi Yang, Zhiyong Li
Genome-wide association studies have shown that Krüppel-like factor 14 (KLF14) is associated with both Type 2 diabetes mellitus and lipid metabolism. However, its role in chronic inflammatory responses and the pathogenesis of atherosclerosis remains unknown. The present study was designed to investigate both in vivo and in vitro the impact of KLF14 on chronic inflammatory responses and atherosclerosis. ApoE KO mice, a well-established animal model of atherosclerosis, had higher expressions of KLF14 in aorta tissues than that in C57BL/6 J mice when fed the high-fat diet (HFD) or standard chow diet...
November 14, 2016: Cardiovascular Pathology: the Official Journal of the Society for Cardiovascular Pathology
https://www.readbyqxmd.com/read/27923139/plga-peg-plga-triblock-copolymeric-micelles-as-oral-drug-delivery-system-in-vitro-drug-release-and-in-vivo-pharmacokinetics-assessment
#6
Xiufen Chen, Jianzhong Chen, Bowen Li, Xiang Yang, Rongjie Zeng, Yajun Liu, Tao Li, Rodney J Y Ho, Jingwei Shao
Poly (d,l-lactide-co-glycolide)-poly (ethylene glycol)-poly (d,l-lactide-co-glycolide) triblock copolymers (PLGA-PEG-PLGA) has been proven to be desirable for anti-cancer drug delivery by intravenous administration. But till now there is no report of developing this micelle as a sustained oral formulation for cancer therapy. 3β-acetoxy-urs-12-en-28-oic acid hexamethylenediamine (US597), a derivative of natural product ursolic acid has been developed as a novel cancer metastasis chemopreventive agent by us...
November 26, 2016: Journal of Colloid and Interface Science
https://www.readbyqxmd.com/read/27923055/a-novel-rrm3-function-in-restricting-dna-replication-via-an-orc5-binding-domain-is-genetically-separable-from-rrm3-function-as-an-atpase-helicase-in-facilitating-fork-progression
#7
Salahuddin Syed, Claus Desler, Lene J Rasmussen, Kristina H Schmidt
In response to replication stress cells activate the intra-S checkpoint, induce DNA repair pathways, increase nucleotide levels, and inhibit origin firing. Here, we report that Rrm3 associates with a subset of replication origins and controls DNA synthesis during replication stress. The N-terminal domain required for control of DNA synthesis maps to residues 186-212 that are also critical for binding Orc5 of the origin recognition complex. Deletion of this domain is lethal to cells lacking the replication checkpoint mediator Mrc1 and leads to mutations upon exposure to the replication stressor hydroxyurea...
December 2016: PLoS Genetics
https://www.readbyqxmd.com/read/27923046/mitochondria-and-caspases-tune-nmnat-mediated-stabilization-to-promote-axon-regeneration
#8
Li Chen, Derek M Nye, Michelle C Stone, Alexis T Weiner, Kyle W Gheres, Xin Xiong, Catherine A Collins, Melissa M Rolls
Axon injury can lead to several cell survival responses including increased stability and axon regeneration. Using an accessible Drosophila model system, we investigated the regulation of injury responses and their relationship. Axon injury stabilizes the rest of the cell, including the entire dendrite arbor. After axon injury we found mitochondrial fission in dendrites was upregulated, and that reducing fission increased stabilization or neuroprotection (NP). Thus axon injury seems to both turn on NP, but also dampen it by activating mitochondrial fission...
December 6, 2016: PLoS Genetics
https://www.readbyqxmd.com/read/27923040/a-low-correlation-resting-state-of-the-striatum-during-cortical-avalanches-and-its-role-in-movement-suppression
#9
Andreas Klaus, Dietmar Plenz
During quiet resting behavior, involuntary movements are suppressed. Such movement control is attributed to cortico-basal ganglia loops, yet population dynamics within these loops during resting and their relation to involuntary movements are not well characterized. Here, we show by recording cortical and striatal ongoing population activity in awake rats during quiet resting that intrastriatal inhibition maintains a low-correlation striatal resting state in the presence of cortical neuronal avalanches. Involuntary movements arise from disturbed striatal resting activity through two different population dynamics...
December 2016: PLoS Biology
https://www.readbyqxmd.com/read/27923036/cotargeting-of-cyp-19-aromatase-and-emerging-pivotal-signalling-pathways-in-metastatic-breast-cancer
#10
REVIEW
Stine Daldorff, Randi Margit Ruud Mathiesen, Olav Erich Yri, Hilde Presterud Ødegård, Jürgen Geisler
Aromatase inhibition is one of the cornerstones of modern endocrine therapy of oestrogen receptor-positive (ER+) metastatic breast cancer (MBC). The nonsteroidal aromatase inhibitors anastrozole and letrozole, as well as the steroidal aromatase inactivator exemestane, are the preferred drugs and established worldwide in all clinical phases of the disease. However, although many patients suffering from MBC experience an initial stabilisation of their metastatic burden, drug resistance and disease progression occur frequently, following in general only a few months on treatment...
December 6, 2016: British Journal of Cancer
https://www.readbyqxmd.com/read/27922949/the-neurological-safety-of-an-epidurally-administered-lipo-pge1-agonist-in-rats
#11
Eunjoo Choi, Sun Min Im, Hyung-Seok Yoo, Francis Sahngun Nahm, Yang Hyun Kim, Gheeyoung Choe, Pyung Bok Lee
BACKGROUND AND OBJECTIVE: Liposomal prostaglandin E1 (Lipo-PGE1) can inhibit platelet aggregation and vasodilatation and has been found to be therapeutic in ischemia and spinal diseases including stenosis. However, the neurologic safety of epidural administration of lipo-PGE1 requires further study. We investigated the neurotoxicity of epidurally administered lipo-PGE1 agonist in rats. METHODS: Twenty-seven rats were randomly divided into three groups: Epidural isotonic sodium chloride solution administration (negative control, group N, n = 9); epidural lipo-PGE1 agonist (group L, n = 9); and epidural alcohol (positive control, group A, n = 9)...
December 5, 2016: Regional Anesthesia and Pain Medicine
https://www.readbyqxmd.com/read/27922847/apolipoprotein-e-metabolism-and-functions-in-brain-and-its-role-in-alzheimer-s-disease
#12
Fan Liao, Hyejin Yoon, Jungsu Kim
PURPOSE OF REVIEW: APOE4 genotype is the strongest genetic risk factor for Alzheimer's disease. Prevailing evidence suggests that amyloid β plays a critical role in Alzheimer's disease. The objective of this article is to review the recent findings about the metabolism of apolipoprotein E (ApoE) and amyloid β and other possible mechanisms by which ApoE contributes to the pathogenesis of Alzheimer's disease. RECENT FINDINGS: ApoE isoforms have differential effects on amyloid β metabolism...
December 5, 2016: Current Opinion in Lipidology
https://www.readbyqxmd.com/read/27922761/%C3%AE-6%C3%AE-4-integrin-regulates-the-collective-migration-of-epithelial-cells
#13
Zachary T Colburn, Jonathan C R Jones
α6β4 integrin is localized in a unique punctate distribution at the cell-substratum interface along the leading front of single, front-rear polarized, A549 cells. These puncta are interspersed between focal adhesions and lack association with the actin cytoskeleton. Knockdown of β4 integrin in A549 cells inhibits their directed migration, with knockdown cells exhibiting large focal adhesions and reduced actin dynamics. Despite these changes, the speed of knockdown cells is equivalent to controls cells. Interestingly, in such cells, α6 integrin retains its punctate distribution...
December 6, 2016: American Journal of Respiratory Cell and Molecular Biology
https://www.readbyqxmd.com/read/27922746/plant-extracts-initial-screening-identification-of-bioactive-compounds-and-effect-against-candida-albicans-biofilms
#14
Fernanda Lourenção Brighenti, Marcos José Salvador, Aline Vidal Lacerda Gontijo, Alberto Carlos Botazzo Delbem, Ádina Cléia Botazzo Delbem, Cristina Pacheco Soares, Maria Alcionéia Carvalho de Oliveira, Camila Miorelli Girondi, Cristiane Yumi Koga-Ito
AIM: This study screened plants from Brazilian Pantanal for Candida albicans antibiofilm activity. MATERIAL & METHODS: Sixty extracts were obtained from ten plants using different extraction methods. Antifungal activity was assessed. Effects on biofilm inhibition and disruption and cytotoxicity were also evaluated. The most active extract was chemically characterized. RESULTS:  Buchenavia tomentosa ethanolic extract showed noticeable antifungal activity and was selected for biofilm experiments...
December 6, 2016: Future Microbiology
https://www.readbyqxmd.com/read/27922739/tyrosine-kinase-aurora-kinase-and-leucine-aminopeptidase-as-attractive-drug-targets-in-anticancer-therapy-characterisation-of-their-inhibitors
#15
Joanna Ziemska, Jolanta Solecka
Cancers are the leading cause of deaths all over the world. Available anticancer agents used in clinics exhibit low therapeutic index and usually high toxicity. Wide spreading drug resistance of cancer cells induce a demanding need to search for new drug targets. Currently, many on-going studies on novel compounds with potent anticancer activity, high selectivity as well as new modes of action are conducted. In this work, we describe in details three enzyme groups, which are at present of extensive interest to medical researchers and pharmaceutical companies...
2016: Roczniki Państwowego Zakładu Higieny
https://www.readbyqxmd.com/read/27922734/population-pharmacokinetics-of-ceritinib-in-adult-patients-with-tumors-characterized-by-genetic-abnormalities-in-anaplastic-lymphoma-kinase
#16
Ying Hong, Vanessa Q Passos, Pai-Hsi Huang, Yvonne Y Lau
Ceritinib is a second-generation selective and potent oral anaplastic lymphoma kinase (ALK) inhibitor approved for ALK-positive advanced non-small cell lung cancer previously treated with crizotinib. Population pharmacokinetic (PK) analysis was performed to describe the PK of ceritinib and was used to evaluate the covariate effects on systemic exposure at its label dose (750 mg orally once daily). Ceritinib concentration-time data from 4 clinical studies were described by a 1-compartment model with delayed first-order absorption and time-dependent elimination...
December 6, 2016: Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/27922693/a-novel-pdgf-receptor-inhibitor-eluting-stent-attenuates-in-stent-neointima-formation-in-a-rabbit-carotid-model
#17
Chen Huang, Haijun Mei, Min Zhou, Xiaobing Zheng
A novel drug-eluting stent (DES) is required to target vascular smooth muscle cells (SMCs) without harming endothelial cells (ECs). Platelet-derived growth factor (PDGF) is critical for the proliferation and migration of SMCs. Sunitinib [a PDGF receptor (PDGFR) tyrosine kinase inhibitor]‑eluting stents may therefore inhibit neointimal formation. The aim of the present study was to examine the stent‑based delivery of sunitinib in a rabbit carotid model; in addition, the effects of sunitinib were evaluated in vitro...
December 5, 2016: Molecular Medicine Reports
https://www.readbyqxmd.com/read/27922692/mir-195-inhibits-the-proliferation-and-migration-of-chondrocytes-by-targeting-git1
#18
Yang-Lin Gu, Xiao-Xu Rong, Li-Ting Wen, Guo-Xing Zhu, Ming-Quan Qian
Previous studies have demonstrated that G-protein coupled receptor kinase interacting protein-1 (GIT1) and microRNAs (miRNAs) serve an important role in chondrocyte proliferation and migration. However, a limited number of studies conducted thus far have investigated the association between GIT1 and miRNAs. In the present study, putative miR‑195 binding sites in the GIT1 3'‑untranslated region were identified using common bioinformatic algorithms (miRanda, TargetScan, miRBase and miRWalk), and it was demonstrated that they may be involved in regulating GIT1 expression...
December 5, 2016: Molecular Medicine Reports
https://www.readbyqxmd.com/read/27922690/microrna-152-inhibits-tumor-cell-growth-by-directly-targeting-rtkn-in-hepatocellular-carcinoma
#19
Jiejing Zhou, Yanjun Zhang, Yuhong Qi, Dequan Yu, Qiuju Shao, Jun Liang
Hepatocellular carcinoma (HCC) is the most common form of adult liver cancer and accounts for approximately 90% of all cases of primary liver cancer annually. Rhotekin (RTKN), which functions as a cancer promoter, can be frequently detected in many human cancers, including gastric cancer, colorectal carcinoma and bladder carcinoma. The aim of this study was to investigate the role of RTKN in HCC. Using HCC cells and tissues from patients with liver cancer, we demonstrated that RTKN was significantly increased in HCC...
December 5, 2016: Oncology Reports
https://www.readbyqxmd.com/read/27922689/rb-knockdown-accelerates-bladder-cancer-progression-through-e2f3-activation
#20
Jiang-Ping Wang, Yong Jiao, Cheng-Yuan Wang, Zhi-Bin Xu, Bo Zhang
Bladder cancer is one of the most common cancers diagnosed in the world and leads to significant mortality and morbidity among affected patients. The retinoblastoma (Rb) protein is a main tumor suppressor, controlling cellular responses to potentially oncogenic stimulation. E2F3 was invariably disrupted in different human cancers for its central role in the control of cellular proliferation. Here, we investigated how Rb is integrated to control bladder cancer progression through E2F3 and p53 regulation. The results exhibit that Rb expression is lower in patients with bladder tumor, while E2F3 level is high...
December 6, 2016: International Journal of Oncology
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