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https://www.readbyqxmd.com/read/29778019/phoenix-dactylifera-protects-against-oxidative-stress-and-hepatic-injury-induced-by-paracetamol-intoxication-in-rats
#1
Gamal A Salem, Ahmed Shaban, Hussain A Diab, Wesam A Elsaghayer, Manal D Mjedib, Aomassad M Hnesh, Ravi P Sahu
The current studies were sought to determine effects of antioxidant potential of aqueous and methanolic extracts of Phoenix dactylifera leaves (PLAE and PLME) against the widely-used analgesic paracetamol (PCM) induced hepatotoxicity. Groups of rats were treated with or without PCM (1500 mg/kg), PLAE and PLME (300 mg/kg) and n-acetylcysteine (NAC, 50 mg/kg) followed by assessments of liver function tests, oxidative stress, antioxidant defenses, and hepatotoxicity. We observed that PCM significantly elevated serum liver markers, aspartate aminotransferase (AST), alanine aminotransferase (ALT), alkaline phosphatase (ALP), gamma glutamyl transferase (GGT), and bilirubin compared to control (untreated) group...
May 16, 2018: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29778018/phytochemistry-and-pharmacology-of-anti-depressant-medicinal-plants-a-review
#2
REVIEW
Jeanette Martins, Brijesh S
Stress renders an individual to experience mental pressure and exhaustion which brings about feelings of anxiety, depression, anger and/or other negative emotions. Depression affects a person's state of mind, behaviour, health and is often associated with suicide. The use of anti-depressant drugs as therapeutic agents is associated with symptoms such as, delayed onset of action, side-effects, drug-drug and dietary interactions, sexual dysfunction, cardiac toxicity, etc. Thus, there is need to target these issues and improve current treatment options...
May 16, 2018: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29777941/characterization-of-the-binding-of-a-novel-antitumor-drug-ibrutinib-with-human-serum-albumin-insights-from-spectroscopic-calorimetric-and-docking-studies
#3
Bin Tang, Peixiao Tang, Jiawei He, Hongqin Yang, Hui Li
Ibrutinib (IBR) is a novel Bruton's tyrosine kinase inhibitor and shows good efficacy for several B-cell malignancies. In the current study, the molecular mechanism of the interaction between IBR and the transport protein human serum albumin (HSA) was ascertained by spectroscopic, calorimetric, and docking studies. Detailed investigations on affinity parameter, binding model, conformational change, and site selectivity were implemented by receptor-based and ligand-based analysis. An unusual fluorescence co-quenching (mutual quenching) was observed in the binding of IBR to HSA, followed by a static mechanism...
May 16, 2018: Journal of Photochemistry and Photobiology. B, Biology
https://www.readbyqxmd.com/read/29777930/experimental-and-theoretical-study-of-fingerprint-spectra-of-2-4-fluorophenyl-benzimidazole-and-2-4-chlorophenyl-benzimidazole-in-terahertz-range
#4
Maojiang Song, Fei Yang, Liping Liu, Li Shen, Pengfei Hu, Caixia Su
Due to wide variety of biological and pharmacological activities of benzimidazole derivatives, the terahertz fingerprint spectra of 2-(4-fluorophenyl)benzimidazole and 2-(4-chlorophenyl)benzimidazole are researched by employing terahertz time-domain spectroscopy and density functional theory systematically. Although the substituent at the para position on the benzene moiety are the same family elements (F, Cl) in the periodic table, both experimental and theoretical results show that there are substantial differences in their fingerprint spectra in the range of 0...
May 10, 2018: Spectrochimica Acta. Part A, Molecular and Biomolecular Spectroscopy
https://www.readbyqxmd.com/read/29777865/a-prospective-non-interventional-registry-study-of-patients-initiating-a-course-of-drug-therapy-for-overactive-bladder-perspective-rationale-design-and-methodology
#5
Eric S Rovner, Kevin V Carlson, Anna S Deal, Kavita V Nair, Eva E Oakkar, Julie Park, Eric Gemmen, Rita M Kristy, Katherine L Gooch, Carol R Schermer
INTRODUCTION: Pharmacotherapy of overactive bladder (OAB) typically involves treatment with an antimuscarinic or mirabegron, a β3-adrenoceptor agonist, but real-world evidence on their use, including treatment access, persistence, and switching, is limited. Here, we describe the design of a prospective, multicenter, non-interventional registry of patients beginning a new course of OAB pharmacological therapy in routine clinical practice. METHODS: Adults with an OAB diagnosis for at least 3 months who either initiated a new course of mirabegron or antimuscarinic, or who switched therapy were enrolled into PERSPECTIVE (A Prospective, Non-intErventional Registry Study of Patients Initiating a Course of Drug Therapy for OveractIVE Bladder)...
May 16, 2018: Contemporary Clinical Trials
https://www.readbyqxmd.com/read/29777848/effects-on-mortality-and-cardiovascular-events-of-adherence-to-guideline-recommended-therapy-4-years-after-lower-extremity-arterial-revascularization
#6
M Thiney, N Della Schiava, R Ecochard, P Feugier, P Lermusiaux, A Millon, A Long
OBJECTIVES: All patients with lower extremity peripheral arterial disease (LE-PAD) should benefit from recommended pharmacologic therapies including antiplatelet agents, angiotensin converting enzyme inhibitors (ACE) or Angiotensin receptor blockers (ARB), and HMG-CoA-reductase inhibitors (statins). In the present study, this triple therapy was defined as the best medical treatment. This study was designed to determine the current risk for cardiovascular (CV) events and mortality and also to evaluate the effect of pharmacologic treatment on patient's survival, CV events and additional vascular surgery in vascularized LE-PAD patients...
May 16, 2018: Annals of Vascular Surgery
https://www.readbyqxmd.com/read/29777797/polypharmacy-defined-as-taking-five-or-more-drugs-is-inadequate-in-the-cardiovascular-setting
#7
Nazanin Abolhassani
BACKGROUND: By how much polypharmacy (defined by number of drugss) differs from polyactive ingredient use (defined by the number of pharmacologically active ingredients) has not been assessed. OBJECTIVES: to compare the extent of polypharmacy vs. polyactive ingredients among patients taking CV medicines. METHODS: Prospective, 10-year follow-up study conducted among 880 participants of the CoLaus study taking CV drugs at baseline. Polypharmacy was defined as the use of 5 or more CV medicines; polyactive ingredient use was defined as the use of 5 or more pharmacologically active CV ingredients...
May 16, 2018: Journal of Clinical Epidemiology
https://www.readbyqxmd.com/read/29777752/chemical-profile-and-pharmacological-effects-of-the-resin-and-essential-oil-from-bursera-slechtendalii-a-medicinal-copal-tree-of-southern-mexico
#8
Nemesio Villa-Ruano, Yesenia Pacheco-Hernández, Elvia Becerra-Martínez, José Alejo Zarate-Reyes, Ramiro Cruz-Duran
This study reports on the volatile profile and pharmacological activities of the essential oil and resin from Bursera slechtendalii, an aromatic medicinal tree commercialized in southern Mexico. The essential oil contained 25 volatiles including p-cymen-8-ol (25.4-35.7%), n-hexyl hexanoate (6.8-17.6%) and n-octyl hexanoate (7.6-14.8%), whereas the crystallized resin contained 14 volatiles, including n-octyl acetate (29.6-34.2%), limonene (15.8-18.7%) and n-octyl butyrate (12.6-17-6%). The inhalation of vapors from the resin and essential oil caused a significant anxiolytic-like effect (p < ...
May 16, 2018: Fitoterapia
https://www.readbyqxmd.com/read/29777683/probing-the-binding-site-of-novel-selective-positive-allosteric-modulators-at-the-m-1-machr
#9
Elham Khajehali, Celine Valant, Manuela Jörg, Andrew B Tobin, P Jeffrey Conn, Craig W Lindsley, Patrick M Sexton, Peter J Scammells, Arthur Christopoulos
Subtype-selective allosteric modulation of the M1 muscarinic acetylcholine (ACh) receptor (M1 mAChR) is an attractive approach for the treatment of numerous disorders, including cognitive deficits. The discovery of benzyl quinolone carboxylic acid, BQCA, a selective M1 mAChR positive allosteric modulator (PAM), spurred the subsequent development of newer generation M1 PAMs representing diverse chemical scaffolds, different pharmacodynamic properties and, in some instances, improved pharmacokinetics. Key exemplar molecules from such efforts include PF-06767832 (N-((3R,4S)-3-hydroxytetrahydro-2H-pyran-4-yl)-5-methyl-4-(4-(thiazol-4-yl)benzyl)pyridine-2-carboxamide), VU6004256 (4,6-difluoro-N-(1S,2S)-2-hydroxycyclohexyl-1-((6-(1-methyl-1H-pyrazol-4-yl)pyridine-3-yl)methyl)-1H-indole-3-carboxamide) and MIPS1780 (3-(2-hydroxycyclohexyl)-6-(2-((4-(1-methyl-1H-pyrazol-4-yl)-benzyl)oxy)phenyl)pyrimidin-4(3H)-one)...
May 16, 2018: Biochemical Pharmacology
https://www.readbyqxmd.com/read/29777569/improving-metabolic-stability-with-deuterium-the-discovery-of-hwl-066-a-potent-and-long-acting-free-fatty-acid-receptor-1-agonists
#10
Chunxia Liu, Zheng Li, Wei Shi, Huilan Li, Nasi Wang, Yuxuan Dai, Chen Liao, Wenlong Huang, Hai Qian
The free fatty acid receptor 1 (FFA1) is a potential target due to its function in enhancing of glucose-stimulated insulin secretion. The FFA1 agonist GW9508 has great potential for the treatment of type 2 diabetes mellitus, but it has been suffering from high plasma clearance probably because the phenylpropanoic acid is vulnerable to β-oxidation. To identify orally available analog without influence on the unique pharmacological mechanism of GW9508, we tried to interdict the metabolically labile group by incorporating two deuterium atoms at the α-position of phenylpropionic acid affording compound 4 (HWL-066)...
May 18, 2018: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/29777521/an-early-view-of-real-world-patient-response-to-sacubitril-valsartan-a-retrospective-study-of-patients-with-heart-failure-with-reduced-ejection-fraction
#11
Dana Drzayich Antol, Adrianne Waldman Casebeer, Richard W DeClue, Stephen Stemkowski, Patricia A Russo
INTRODUCTION: Sacubitril/valsartan has been established as an effective treatment for heart failure (HF) with reduced ejection fraction based on clinical trial data; however, little is known about its use or impact in real-world practice. METHODS: This study included data from medical and pharmacy claims and medical records review for patients (n = 200) who initiated sacubitril/valsartan between August 2015 and March 2016 preceding issuance of American College of Cardiology (ACC)/American Heart Association (AHA)/Heart Failure Society of America (HFSA) focused update on new pharmacological therapy for HF (May 2016), which included recommendations for sacubitril/valsartan...
May 17, 2018: Advances in Therapy
https://www.readbyqxmd.com/read/29777519/combination-glucose-lowering-therapy-plans-in-t2dm-case-based-considerations
#12
REVIEW
Lawrence Blonde, Susana Dipp, Daniel Cadena
Type 2 diabetes mellitus (T2DM) is a complex disease, and while lifestyle interventions remain the cornerstone of therapy, most patients will also require pharmacotherapy. Current diabetes treatment guidelines and algorithms recommend an individualized approach to setting glycemic goals and selecting treatment. Although a single antihyperglycemic agent may be appropriate as the initial T2DM pharmacotherapy, the progressive nature of the disease due to declining pancreatic β-cell function will result in the vast majority of T2DM patients eventually requiring two or more antihyperglycemic agents...
May 18, 2018: Advances in Therapy
https://www.readbyqxmd.com/read/29777343/the-effects-of-pre-treatment-depressive-symptoms-on-quality-of-life-across-cognitive-behavioral-therapy-for-chronic-pain
#13
Justin M Hughes, Eric A Seemann, J Michael George, K Dean Willis
Recent studies suggest that chronic pain affects millions and carries significant physical, financial, and social burdens, and thus adversely affects quality of life (QOL). Cognitive behavioral therapy for chronic pain (CBTp) is a non-pharmacological treatment method which has been shown to reduce a sufferer's experience of chronic pain and improve overall QOL. These and other studies also indicate that affective symptoms likely impact the effectiveness of CBTp. The current study focused on the effects of depressive symptoms on changes in QOL ratings across a 12-session CBT for chronic pain...
May 17, 2018: Journal of Clinical Psychology in Medical Settings
https://www.readbyqxmd.com/read/29777277/impact-of-muscle-atrophy-on-bone-metabolism-and-bone-strength-implications-for-muscle-bone-crosstalk-with-aging-and-disuse
#14
REVIEW
T Bettis, B-J Kim, M W Hamrick
Bone fractures in older adults are often preceded by a loss of muscle mass and strength. Likewise, bone loss with prolonged bed rest, spinal cord injury, or with exposure to microgravity is also preceded by a rapid loss of muscle mass. Recent studies using animal models in the setting of hindlimb unloading or botulinum toxin (Botox) injection also reveal that muscle loss can induce bone loss. Moreover, muscle-derived factors such as irisin and leptin can inhibit bone loss with unloading, and knockout of catabolic factors in muscle such as the ubiquitin ligase Murf1 or the myokine myostatin can reduce osteoclastogenesis...
May 18, 2018: Osteoporosis International
https://www.readbyqxmd.com/read/29777255/inhibition-of-sialidase-activity-and-cellular-invasion-by-the-bacterial-vaginosis-pathogen-gardnerella-vaginalis
#15
G Govinden, J L Parker, K L Naylor, A M Frey, D O C Anumba, G P Stafford
Bacterial vaginosis is a genital tract infection, thought to be caused by transformation of a lactobacillus-rich flora to a dysbiotic microbiota enriched in mixed anaerobes. The most prominent of these is Gardnerella vaginalis (GV), an anaerobic pathogen that produces sialidase enzyme to cleave terminal sialic acid residues from human glycans. Notably, high sialidase activity is associated with preterm birth and low birthweight. We explored the potential of the sialidase inhibitor Zanamavir against GV whole cell sialidase activity using methyl-umbelliferyl neuraminic acid (MU-NANA) cleavage assays, with Zanamavir causing a 30% reduction in whole cell GV sialidase activity (p < 0...
May 18, 2018: Archives of Microbiology
https://www.readbyqxmd.com/read/29777171/mll-fusion-driven-leukemia-requires-setd2-to-safeguard-genomic-integrity
#16
Anna Skucha, Jessica Ebner, Johannes Schmöllerl, Mareike Roth, Thomas Eder, Adrián César-Razquin, Alexey Stukalov, Sarah Vittori, Matthias Muhar, Bin Lu, Martin Aichinger, Julian Jude, André C Müller, Balázs Győrffy, Christopher R Vakoc, Peter Valent, Keiryn L Bennett, Johannes Zuber, Giulio Superti-Furga, Florian Grebien
MLL-fusions represent a large group of leukemia drivers, whose diversity originates from the vast molecular heterogeneity of C-terminal fusion partners of MLL. While studies of selected MLL-fusions have revealed critical molecular pathways, unifying mechanisms across all MLL-fusions remain poorly understood. We present the first comprehensive survey of protein-protein interactions of seven distantly related MLL-fusion proteins. Functional investigation of 128 conserved MLL-fusion-interactors identifies a specific role for the lysine methyltransferase SETD2 in MLL-leukemia...
May 18, 2018: Nature Communications
https://www.readbyqxmd.com/read/29777164/mrna-treatment-produces-sustained-expression-of-enzymatically-active-human-adamts13-in-mice
#17
Susan Liu-Chen, Brendan Connolly, Lei Cheng, Romesh R Subramanian, Zhaozhong Han
Thrombotic thrombocytopenic purpura (TTP) is primarily caused by deficiency of ADAMTS13 within the blood stream due to either genetic defects or presence of inhibitory autoantibodies. Preclinical and clinical studies suggest that enzyme replacement therapy with recombinant human ADAMTS13 protein (rhADAMTS13) is effective and safe in treatment of TTP. However, frequent dosing would be required due to the relatively short half-life of rhADAMTS13 in circulation as well as the presence of inhibitory autoantibodies that collectively result in the poor pharmacological profile of rhADAMTS13...
May 18, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29777149/stretching-reduces-tumor-growth-in-a-mouse-breast-cancer-model
#18
L Berrueta, J Bergholz, D Munoz, I Muskaj, G J Badger, A Shukla, H J Kim, J J Zhao, H M Langevin
There is growing interest in developing non-pharmacological treatments that could boost natural defenses against cancer and contribute to primary and secondary cancer prevention. Recent studies have shown that gentle daily stretching for 10 minutes can reduce local connective tissue inflammation and fibrosis. Because mechanical factors within the stroma can influence the tumor microenvironment, we hypothesized that stretching would reduce the growth of tumors implanted within locally stretched tissues and tested this hypothesis in a mouse orthotopic breast cancer model...
May 18, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29777128/comparison-of-the-serum-metabolic-signatures-based-on-1-h-nmr-between-patients-and-a-rat-model-of-deep-vein-thrombosis
#19
Jie Cao, Qian-Qian Jin, Gui-Ming Wang, Hong-Lin Dong, Yong-Ming Feng, Jun-Sheng Tian, Ke-Ming Yun, Ying-Yuan Wang, Jun-Hong Sun
Deep vein thrombosis (DVT) and pulmonary embolism (PE) have high morbidity, reduce quality of life, and can cause death. Biomarkers or genetic risk factors have not been identified in patients with DVT. In present study, serum of 61 patients suffering from DVT and a rat DVT model (n = 10) were assayed by a proton nuclear magnetic resonance (1 H NMR) metabolomics technique combing with multivariate statistical analysis to identify the metabolites. The MetPA platform was used to identify differences in the metabolic pathways between the rat model and patients...
May 18, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29777108/factor-xiiia-expressing-inflammatory-monocytes-promote-lung-squamous-cancer-through-fibrin-cross-linking
#20
Alessandro Porrello, Patrick L Leslie, Emily B Harrison, Balachandra K Gorentla, Sravya Kattula, Subrata K Ghosh, Salma H Azam, Alisha Holtzhausen, Yvonne L Chao, Michele C Hayward, Trent A Waugh, Sanggyu Bae, Virginia Godfrey, Scott H Randell, Cecilia Oderup, Liza Makowski, Jared Weiss, Matthew D Wilkerson, D Neil Hayes, H Shelton Earp, Albert S Baldwin, Alisa S Wolberg, Chad V Pecot
Lung cancer is the leading cause of cancer-related deaths worldwide, and lung squamous carcinomas (LUSC) represent about 30% of cases. Molecular aberrations in lung adenocarcinomas have allowed for effective targeted treatments, but corresponding therapeutic advances in LUSC have not materialized. However, immune checkpoint inhibitors in sub-populations of LUSC patients have led to exciting responses. Using computational analyses of The Cancer Genome Atlas, we identified a subset of LUSC tumors characterized by dense infiltration of inflammatory monocytes (IMs) and poor survival...
May 18, 2018: Nature Communications
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