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https://www.readbyqxmd.com/read/29777772/improving-maraviroc-oral-bioavailability-by-formation-of-solid-drug-nanoparticles
#1
Alison C Savage, Lee M Tatham, Marco Siccardi, Trevor Scott, Manoli Vourvahis, Andrew Clark, Steve P Rannard, Andrew Owen
Oral drug administration remains the preferred approach for treatment of HIV in most patients. Maraviroc (MVC) is the first in class co-receptor antagonist, which blocks HIV entry into host cells. MVC has an oral bioavailability of approximately 33%, which is limited by poor permeability as well as affinity for CYP3A and several drug transporters. While once-daily doses are now the favoured option for HIV therapy, dose-limiting postural hypotension has been of theoretical concern when administering doses high enough to achieve this for MVC (particularly during coadministration of enzyme inhibitors)...
May 16, 2018: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/29777769/a-combined-approach-for-the-early-recognition-of-acute-kidney-injury-after-adult-cardiac-surgery
#2
Cédrick Zaouter, Julien Potvin, Marie-Lise Bats, Marie-Christine Beauvieux, Alain Remy, Alexandre Ouattara
BACKGROUND: Cardiac surgery-associated acute kidney injury (CSA-AKI) is a frequent complication. The current criteria to detect CSA-AKI rise only when organic dysfunction has occurred. The Doppler Renal Resistive Index (RRI) and the urinary G1 cell cycle arrest proteins (TIMP-2 and IGFBP7) have been advocated to predict CSA-AKI at an early stage after cardiac surgery. The primary objective was to determine the predictive value of these new markers to detect CSA-AKI after elective heart surgery in patients at risk to develop AKI...
May 16, 2018: Anaesthesia, Critical Care & Pain Medicine
https://www.readbyqxmd.com/read/29777228/effects-of-clomiphene-citrate-on-male-obesity-associated-hypogonadism-a-randomized-double-blind-placebo-controlled-study
#3
Andressa Heimbecher Soares, Nidia Celeste Horie, Lucas Augusto Piccinin Chiang, Bruno Caramelli, Mariana Gomes Matheus, Alexandre Holthausen Campos, Luciana Cavalheiro Marti, Fernanda Agostini Rocha, Marcio C Mancini, Elaine Maria Frade Costa, Cintia Cercato
BACKGROUND: Obesity causes secondary hypogonadism (HG) in men. Standard testosterone (T) replacement therapy improves metabolic parameters but leads to infertility. OBJECTIVE: To evaluate clomiphene citrate (CC) treatment of adult men with male obesity-associated secondary hypogonadism (MOSH). DESIGN: Single-center, randomized, double-blind, placebo-controlled trial. PARTICIPANTS: Seventy-eight men aged 36.5 ± 7...
May 17, 2018: International Journal of Obesity: Journal of the International Association for the Study of Obesity
https://www.readbyqxmd.com/read/29776952/activity-based-concept-to-screen-biological-matrices-for-opiates-and-synthetic-opioids
#4
Annelies Cannaert, Lakshmi Vasudevan, Melissa Friscia, Amanda L A Mohr, Sarah M R Wille, Christophe P Stove
BACKGROUND: Detection of new highly potent synthetic opioids is challenging as new compounds enter the market. Here we present a novel screening method for the detection of opiates and (synthetic) opioids based on their activity. METHODS: A cell-based system was set up in which activation of the μ -opioid receptor (MOR) led to recruitment of β-arrestin 2, resulting in functional complementation of a split NanoLuc luciferase and allowing readout via bioluminescence...
May 18, 2018: Clinical Chemistry
https://www.readbyqxmd.com/read/29776409/calcitriol-downregulates-fibroblast-growth-factor-receptor-1-through-histone-deacetylase-activation-in-hl-1-atrial-myocytes
#5
Ting-Wei Lee, Ting-I Lee, Yung-Kuo Lin, Yu-Hsun Kao, Yi-Jen Chen
BACKGROUND: Fibroblast growth factor (FGF)-2 plays a crucial role in the pathophysiology of cardiovascular diseases (CVDs). FGF-2 was reported to induce cardiac hypertrophy through activation of FGF receptor 1 (FGFR1). Multiple laboratory findings indicate that calcitriol may be a potential treatment for CVDs. In this study, we attempted to investigate whether calcitriol regulates FGFR1 expression to modulate the effects of FGF-2 signaling in cardiac myocytes and explored the potential regulatory mechanism...
May 18, 2018: Journal of Biomedical Science
https://www.readbyqxmd.com/read/29775925/exposure-to-tris-1-3-dichloro-2-propyl-phosphate-for-two-generations-decreases-fecundity-of-zebrafish-at-environmentally-relevant-concentrations
#6
Yongkang Zhang, Meng Li, Shuying Li, Qiangwei Wang, Guonian Zhu, Guanyong Su, Robert J Letcher, Chunsheng Liu
Previous studies reported that exposure to environmentally relevant concentrations of TDCIPP significantly decreased the number of cumulative eggs in zebrafish, but effects on the quantity of eggs and sperms remained unknown. Therefore, in this study, effects of TDCIPP on yolk diameter, surface morphology of eggs, sperm density and total motility were evaluated. First generation (F0) zebrafish larvae (Danio rerio) were exposed to 0, 50, 500 or 5000 ng/L tris(1,3-dichloro-2-propyl) phosphate (TDCIPP) from 14 days post fertilization (dpf) to 120 dpf...
May 14, 2018: Aquatic Toxicology
https://www.readbyqxmd.com/read/29775016/-effect-of-salvianolic-acid-b-on-proliferation-and-apoptosis-of-human-nasal-polyps-fibroblasts
#7
D Luo, Y X Zhao, Y H Zhang, Y Zhou, J Ding, Z F Sun
Objective: The aim of this study is to discuss the effects and mechanism of salvianolic acid B (SAB) on the proliferation and apoptosis of human nasal polyps fibroblasts (NPFs). Method: The NPFs were treated with SAB at different concentrations (5, 10, 20, 40 μmol/L). CCK-8 assay was used to determine the inhibition of SAB on the proliferation of NPFs and determined the optimum concentration for the following experiments. The NPFs were divided into four groups: a) control group: the cells were cultured in DMEM without TGF-β1 or salvianolic acid B; b) the TGF-β1 group: the cells were cultured in DMEM containing 5 ng/ml TGF-β1; c) the SAB group: the cells were cultured in DMEM containing SAB at the optimum concentration by CCK-8 assay; d) the TGF-β1+SAB treatment groups: the cells were cultured in DMEM containing 5 ng/ml TGF-β1 and SAB at the optimum concentration by CCK-8 assay...
February 2018: Journal of Clinical Otorhinolaryngology, Head, and Neck Surgery
https://www.readbyqxmd.com/read/29774240/mannan-induced-nos2-in-macrophages-enhances-il-17-driven-psoriatic-arthritis-by-innate-lymphocytes
#8
Jianghong Zhong, Tatjana Scholz, Anthony C Y Yau, Simon Guerard, Ulrike Hüffmeier, Harald Burkhardt, Rikard Holmdahl
Previous identification of the inducible nitric oxide synthase (NOS2) gene as a risk allele for psoriasis (Ps) and psoriatic arthritis (PsA) suggests a possible pathogenic role of nitric oxide (NO). Using a mouse model of mannan-induced Ps and PsA (MIP), where macrophages play a regulatory role by releasing reactive oxygen species (ROS), we found that NO was detectable before disease onset in mice, independent of a functional nicotinamide adenine dinucleotide phosphate oxidase 2 complex. MIP was suppressed by either deletion of Nos2 or inhibition of NO synthases with NG-nitro-l-arginine methyl ester, demonstrating that Nos2-derived NO is pathogenic...
May 2018: Science Advances
https://www.readbyqxmd.com/read/29773188/the-toxic-effect-of-gallic-acid-on-biochemical-factors-viability-and-proliferation-of-rat-bone-marrow-mesenchymal-stem-cells-was-compensated-by-boric-acid
#9
Mohammad Hussein Abnosi, Somayeh Yari
OBJECTIVE: Gallic acid (GA) and boron are found in many plants. Our previous studies showed 6 ng/ml boric acid (BA) had positive effect on biochemistry of rat bone marrow mesenchymal stem cells (MSCs) and their osteogenic differentiation. Therefore, we investigate the effect of different doses of GA alone and in the presence of BA on MSCs. MATERIALS AND METHODS: the viability of MSCs was assayed using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) and trypan blue at 12, 24 and 36 h in presence of different concentration of GA...
July 2018: Journal of Trace Elements in Medicine and Biology
https://www.readbyqxmd.com/read/29772299/biophenols-enzymes-%C3%AE-secretase-cholinesterases-histone-deacetylase-and-tyrosinase-inhibitors-from-olive-olea-europaea-l
#10
Syed Haris Omar, Christopher J Scott, Adam S Hamlin, Hassan K Obied
The focus of this study was on inhibition of enzymes involved in the pathogenesis Alzheimer's disease (AD) including prime amyloid beta (Aβ) producing enzyme (β-secretase: BACE-1) and disease progression enzymes including acetylcholinesterase (AChE), butyrylcholinesterase (BChE), histone deacetylase (HDAC), and tyrosinase along with the catecholamine L-DOPA, by using olive biophenols. Here we report the strongest inhibition of BACE-1 from rutin (IC50 : 3.8 nM) followed by verbascoside (IC50 : 6.3 nM) and olive fruit extract (IC50 : 18 ng), respectively...
May 14, 2018: Fitoterapia
https://www.readbyqxmd.com/read/29772029/prolyl-carboxypeptidase-activity-in-the-circulation-and-its-correlation-with-body-weight-and-adipose-tissue-in-lean-and-obese-subjects
#11
Kaat Kehoe, Heidi Noels, Wendy Theelen, Emilie De Hert, Shenguan Xu, An Verrijken, Thierry Arnould, Erik Fransen, Nina Hermans, Anne-Marie Lambeir, Per Venge, Luc Van Gaal, Ingrid De Meester
BACKGROUND: Prolyl carboxypeptidase (PRCP) is involved in the regulation of body weight, likely by hydrolysing alpha-melanocyte-stimulating hormone and apelin in the hypothalamus and in the periphery. A link between PRCP protein concentrations in plasma and metabolic disorders has been reported. In this study, we investigated the distribution of circulating PRCP activity and assessed its relation with body weight and adipose tissue in obese patients and patients who significantly lost weight...
2018: PloS One
https://www.readbyqxmd.com/read/29770951/requirement-of-tgf%C3%AE-signaling-for-effect-of-fluoride-on-osteoblastic-differentiation
#12
Jingmin Zhang, Ningning Jiang, Haolan Yu, Xiuhua Yu, Fengyang Guo, Zhitao Zhao, Hui Xu
Research focused on transforming growth factor β (TGFβ) signaling in osteoblast is gradually increasing, whereas literature is rare in terms of fluorosis. This work aimed to investigate how TGFβ signaling participated in regulation of the osteoblast by different doses of fluoride treatment. Bone marrow stem cells (BMSCs) were developed into osteoblastic cells and exposed to 1, 4, and 16 mg/L F- with and without 10 ng/mL of TGFβ. Cell viability and differentiation state of osteoblast under different settings were measured by means of cell counting kit and analysis of alkaline phosphatase (ALP) activity as well as formation of mineral nodules...
May 16, 2018: Biological Trace Element Research
https://www.readbyqxmd.com/read/29770747/cd16-expressing-monocytes-correlate-with-arterial-stiffness-in-hiv-infected-art-na%C3%A3-ve-men
#13
Ling Luo, Yang Han, Xiaojing Song, Ting Zhu, Yong Zeng, Taisheng Li
Objectives To determine the association of the markers of monocyte activation and arterial stiffness among HIV-infected antiretroviral therapy (ART)-naïve men. Methods Sixty HIV-infected ART-naïve men and 20 HIV-uninfected male controls without symptoms or history of cardiovascular disease were recruited. Pulse wave velocity (PWV) were used as the marker of arterial stiffness and determined using a pulse pressure analyzer. The percentage of CD16-expressing monocytes was used as a marker of monocyte activation...
April 2018: HIV Clinical Trials
https://www.readbyqxmd.com/read/29769428/myokine-irisin-induced-protection-against-oxidative-stress-in-vitro-involvement-of-heme-oxygenase-1-and-antioxidazing-enzymes-superoxide-dismutase-2-and-glutathione-peroxidase
#14
A I Mazur-Bialy, K Kozlowska, E Pochec, J Bilski, T Brzozowski
Irisin is a recently discovered myokine reported as protective protein released from exercising skeletal muscles. Although myokines were recently reported to possess the antioxidizing properties, the impact of irisin on the functions of macrophages with respect to its anti-inflammatory potential has not been fully elucidated. Here, we determined the ability of irisin to interact with reactive oxygen species (ROS) in RAW 264.7 murine macrophages. The macrophages were pre-incubated with irisin (0 - 50 nM), some of which had undergone additional co-incubation with bacterial lipopolysaccharide (LPS) (100 ng/ml)...
February 2018: Journal of Physiology and Pharmacology: An Official Journal of the Polish Physiological Society
https://www.readbyqxmd.com/read/29768025/the-post-injury-inflammatory-state-and-the-bone-marrow-response-to-anemia
#15
Tyler J Loftus, Juan C Mira, Elizabeth S Miller, Kolenkode B Kannan, Jessica M Plazas, Daniel Delitto, Julie A Stortz, Jennifer E Hagen, Hari K Parvataneni, Kalia K Sadasivan, Scott C Brakenridge, Frederick A Moore, Lyle L Moldawer, Philip A Efron, Alicia M Mohr
RATIONALE: The pathophysiology of persistent injury-associated anemia is incompletely understood, and human data are sparse. OBJECTIVE: To translate pre-clinical findings by characterizing injury-associated anemia among critically ill trauma patients. This study compared elective hip repair patients with an acute stress response to severely injured trauma patients with a prolonged stress response and evaluated the bone marrow response to anemia. METHODS: A translational prospective observational cohort study comparing severely injured, blunt trauma patients who had operative fixation of a hip or femur fracture (n=17) with elective hip repair patients (n=22) and healthy donors (n=8)...
May 16, 2018: American Journal of Respiratory and Critical Care Medicine
https://www.readbyqxmd.com/read/29767851/risk-factors-for-vitamin-d-deficiency-in-sickle-cell-disease
#16
Jin Han, Xu Zhang, Santosh L Saraf, Michel Gowhari, Robert E Molokie, Johara Hassan, Shivi Jain, Binal N Shah, Taimur Abbasi, Roberto F Machado, Victor R Gordeuk
Vitamin D deficiency (VDD), 25-OHD levels <20 ng/ml, is prevalent among patients with sickle cell disease (SCD) and is linked to acute and chronic pain and bone fracture in this population. There is limited literature regarding VDD-associated risk factors for SCD. We examined potential clinical and genomic parameters associated with VDD in 335 adults with SCD in a cross-sectional study. VDD was present in 65% of adult SCD patients, and 25-OHD levels independently and positively correlated with older age (P < 0·001) and vitamin D supplementation (P < 0·001)...
May 16, 2018: British Journal of Haematology
https://www.readbyqxmd.com/read/29765446/inhibitory-effect-of-pdgf-bb-and-serum-stimulated-responses-in-vascular-smooth-muscle-cell-proliferation-by-hinokitiol-via-up-regulation-of-p21-and-p53
#17
Jiun-Yi Li, Chun-Ping Liu, Wei-Cheng Shiao, Thanasekaran Jayakumar, Yi-Shin Li, Nen-Chung Chang, Shih-Yi Huang, Cheng-Ying Hsieh
Introduction: Vascular smooth muscle cell (VSMC) proliferation plays a major role in the progression of vascular diseases. In the present study, we established the efficacy and the mechanisms of action of hinokitiol, a tropolone derivative found in Chamaecyparis taiwanensis , Cupressaceae, in relation to platelet-derived growth factor-BB (PDGF-BB) and serum-dependent VSMC proliferation. Material and methods: Primary cultured rat VSMCs were pre-treated with hinokitiol and then stimulated by PDGF-BB (10 ng/ml) or serum (10% fetal bovine serum)...
April 2018: Archives of Medical Science: AMS
https://www.readbyqxmd.com/read/29765199/the-development-of-a-reference-database-with-the-topcon-3d-oct-1-maestro
#18
Michael Chaglasian, Murray Fingeret, Pinakin Gunvant Davey, Wei-Chieh Huang, Danny Leung, Edmund Ng, Charles A Reisman
Importance: The paper presents the range for measurements taken with a new spectral domain optical coherence tomography (OCT) device to establish a reference database for discrimination purposes. Objective: To report the range of thickness values for the new Topcon Maestro 3D OCT device with 2 scan size settings: the 12×9 mm wide field and 6×6 mm scans. Design: Prospective, multicenter cohort study conducted at 7 clinical sites across the USA...
2018: Clinical Ophthalmology
https://www.readbyqxmd.com/read/29764763/direct-recovery-of-mangostins-from-garcinia-mangostana-pericarps-using-cellulase-assisted-aqueous-micellar-biphasic-system-with-recyclable-surfactant
#19
Hui-Suan Ng, Grace Yin Tze Tan, Ka-Heng Lee, Wolfgang Zimmermann, Hip Seng Yim, John Chi-Wei Lan
The α- and γ-mangostins from Garcinia mangostana pericarps (GMP) exhibit antioxidant, anti-bacterial, anti-inflammatory and anti-tumor properties. The extraction yields α- and γ-mangostins are often limited by the presence of the GMP cell walls. Therefore, the extraction and recovery of mangostins from GMP with an Aspergillus niger cellulase-assisted aqueous micellar biphasic system (CA-AMBS) was developed for enhanced yield of mangostins. Effects of the concentration of cellulase, the incubation time and the temperature of the system on the recovery of mangostins were investigated...
May 12, 2018: Journal of Bioscience and Bioengineering
https://www.readbyqxmd.com/read/29764547/-comparison-of-lung-protection-for-hydrochloric-acid-or-oleic-acid-induced-rat-acute-respiratory-distress-syndrome-models-pretreated-with-penehyclidine
#20
Yumei Cheng, Zhou Yang, Feng Shen, Bo Liu, Yahui Wang, Yanqi Wu, Ling Yao, Yuqing Liu
OBJECTIVE: To compare the lung protection roles of intraperitoneal pre-injection with penehyclidine for two kinds of rat models with pulmonary and extrapulmonary acute respiratory distress syndrome (ARDSp and ARDSexp). METHODS: Forty healthy adult Sprague-Dawley (SD) rats were randomly divided into five groups (each n = 8): the rats in sham group received only tracheotomy; the ARDS rat models were reproduced by intratracheal inhalation of 0.1 mol/L hydrochloric acid (HCl) 2 mL/kg to simulate ARDSexp (HCl group) and 0...
May 2018: Zhonghua Wei Zhong Bing Ji Jiu Yi Xue
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