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https://www.readbyqxmd.com/read/28934265/comparative-effectiveness-of-different-transarterial-embolization-therapies-alone-or-in-combination-with-local-ablative-or-adjuvant-systemic-treatments-for-unresectable-hepatocellular-carcinoma-a-network-meta-analysis-of-randomized-controlled-trials
#1
Konstantinos Katsanos, Panagiotis Kitrou, Stavros Spiliopoulos, Ioannis Maroulis, Theodore Petsas, Dimitris Karnabatidis
BACKGROUND: The optimal transcatheter embolization strategy for patients with unresectable hepatocellular carcinoma (HCC) remains elusive. We conducted a systematic review and network meta-analysis (NMA) of different embolization options for unresectable HCC. METHODS: Medical databases were searched for randomized controlled trials evaluating bland transarterial embolization (TAE), conventional TACE, drug-eluting bead chemoembolization (DEB-TACE), or transarterial radioembolization (TARE), either alone or combined with adjuvant chemotherapy, or local liver ablation, or external radiotherapy for unresectable HCC up to June 2017...
2017: PloS One
https://www.readbyqxmd.com/read/28933564/%C3%AE-glucosidase-inhibition-by-flavonoids-an-in-vitro-and-in-silico-structure-activity-relationship-study
#2
Carina Proença, Marisa Freitas, Daniela Ribeiro, Eduardo F T Oliveira, Joana L C Sousa, Sara M Tomé, Maria J Ramos, Artur M S Silva, Pedro A Fernandes, Eduarda Fernandes
α-Glucosidase inhibitors are described as the most effective in reducing post-prandial hyperglycaemia (PPHG) from all available anti-diabetic drugs used in the management of type 2 diabetes mellitus. As flavonoids are promising modulators of this enzyme's activity, a panel of 44 flavonoids, organised in five groups, was screened for their inhibitory activity of α-glucosidase, based on in vitro structure-activity relationship studies. Inhibitory kinetic analysis and molecular docking calculations were also applied for selected compounds...
December 2017: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/28933337/the-polymorphism-of-cyp2d6-affects-the-pharmacokinetics-and-dose-escalation-of-paroxetine-controlled-release-tablet-in-healthy-chinese-subjects%C3%A2
#3
Rui Chen, Kai Shen, Pei Hu
PURPOSE: This study evaluated the effects of CYP2D6 polymorphisms on the pharmacokinetics and dose escalation of controlled-release paroxetine over the dose range of 12.5 - 37.5 mg in healthy Chinese subjects. MATERIALS AND METHODS: This was a phase I, open-label, single-dose, three-period crossover study in which 12 healthy subjects received single oral doses of 12.5, 25, and 37.5 mg paroxetine controlled-release tablets with 10-day washout between doses. Serial venous blood samples were collected for 96 hours after study-drug administration and analyzed with LC-MS/MS...
September 21, 2017: International Journal of Clinical Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/28933336/bioavailability-of-oxycodone-after-administration-of-a-new-prolonged-release-once-daily-tablet-formulation-in-healthy-subjects-in-comparison-to-an-established-twice-daily-tablet%C3%A2
#4
Bernhard Scheidel, Martina A Maritz, Yves J Gschwind, Kerstin Steigerwald, Volker Guth, Peter Kovacs, Helene Rey
OBJECTIVE: To evaluate and to compare the bioavailability, the influence of food intake on the bioavailability, and the safety and tolerability of a newly-developed oxycodone once-daily (OOD) prolonged-release tablet with an established oxycodone twice-daily (OTD) prolonged-release tablet after single-dose administration under fasting or fed conditions as well as after multiple-dose administration. MATERIALS AND METHODS: Three single-center, open-label, randomized, balanced, two-treatment, two-period, two-sequence crossover studies were conducted...
September 21, 2017: International Journal of Clinical Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/28933096/-in-vitro-and-in-vivo-recoveries-of-cutaneous-micro-dialysis-probe-of-paeonol-eugenol-and-piperine
#5
Chang Yang, Jie Bai, Shou-Ying Du, Ya-Hua Cui, Qin-Shuai Zhang, Jun-Ming Ma
To establish a method for detecting micro-dialysis recovery of paeonol, eugenol and piperine in Huoxue Zhitong patch, in order to provide the basis for further percutaneous pharmacokinetics studies. The concentrations of paeonol, eugenol and piperine in dialysates were determined by HPLC, and probe deliveries were calculated respectively. The effects of concentration and calibration approaches on the micro-dialysis probe deliveries of the three components were investigated, and their probe absorbability, in vitro and in vivo probe stability and repeatability were also studied...
November 2016: Zhongguo Zhong Yao za Zhi, Zhongguo Zhongyao Zazhi, China Journal of Chinese Materia Medica
https://www.readbyqxmd.com/read/28932620/distinct-roles-of-catalytic-cysteine-and-histidine-in-the-protease-and-ligase-mechanisms-of-human-legumain-as-revealed-by-dft-based-qm-mm-simulations
#6
Brigitta Elsässer, Florian B Zauner, Johann Messner, Wai Tuck Soh, Elfriede Dall, Hans Brandstetter
The cysteine protease enzyme legumain hydrolyzes peptide bonds with high specificity after asparagine and under more acidic conditions after aspartic acid [Baker E. N.J. Mol. Biol.1980, 141, 441-484; Baker E. N.; J. Mol. Biol.1977, 111, 207-210; Drenth J.; Biochemistry1976, 15, 3731-3738; Menard R.; J. Cell. Biochem.1994, 137; Polgar L.Eur. J. Biochem.1978, 88, 513-521; Storer A. C.; Methods Enzymol.1994, 244, 486-500. Remarkably, legumain additionally exhibits ligase activity that prevails at pH > 5.5. The atomic reaction mechanisms including their pH dependence are only partly understood...
September 1, 2017: ACS Catalysis
https://www.readbyqxmd.com/read/28932549/statins-may-be-beneficial-for-patients-with-pulmonary-hypertension-secondary-to-lung-diseases
#7
Ming-Zhou Zhang, De-Hui Qian, Jian-Cheng Xu, Wei Yao, Ye Fan, Chang-Zheng Wang
BACKGROUND: Previous animal studies and clinical trials report inconsistent findings regarding the role of statins in pulmonary hypertension (PH). Systematic reviews have shown no use of statins on pulmonary arterial hypertension (PAH). This is the first meta-analysis of randomized controlled trials (RCTs) determining the clinical impacts of statin therapy on patients with PH secondary to lung diseases. METHODS: Electronic databases and manual bibliographical searches were conducted...
August 2017: Journal of Thoracic Disease
https://www.readbyqxmd.com/read/28931899/energetics-and-mechanism-of-anion-permeation-across-formate-nitrite-transporters
#8
Kalina Atkovska, Jochen S Hub
Formate-nitrite transporters (FNTs) facilitate the translocation of monovalent polyatomic anions, such as formate and nitrite, across biological membranes. FNTs are widely distributed among pathogenic bacteria and eukaryotic parasites, but they lack human homologues, making them attractive drug targets. The mechanisms and energetics involved in anion permeation across the FNTs have remained largely unclear. Both, channel and transporter mode of function have been proposed, with strong indication of proton coupling to the permeation process...
September 20, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28931533/inflammatory-potential-of-the-diet-and-colorectal-tumor-risk-in-persons-with-lynch-syndrome
#9
Jesca Gm Brouwer, Maureen Makama, Geertruida J van Woudenbergh, Hans Fa Vasen, Fokko M Nagengast, Jan H Kleibeuker, Ellen Kampman, Fränzel Jb van Duijnhoven
Background: Persons with Lynch syndrome (LS) have high lifetime risk of developing colorectal tumors (CRTs) because of a germline mutation in one of their mismatch repair (MMR) genes. An important process in the development of CRTs is inflammation, which has been shown to be modulated by diet.Objective: We aimed to investigate the association between the inflammatory potential of the diet and the risk of CRTs in persons with LS.Design: We used the dietary intake of 457 persons with LS from a prospective cohort study to calculate the adapted dietary inflammatory index (ADII)...
September 20, 2017: American Journal of Clinical Nutrition
https://www.readbyqxmd.com/read/28931062/factors-associated-with-hepatitis-c-prevalence-differ-by-the-stage-of-liver-fibrosis-a-cross-sectional-study-in-the-general-population-in-poland-2012-2016
#10
Magdalena Rosińska, Natalia Parda, Agnieszka Kołakowska, Paulina Godzik, Karolina Zakrzewska, Kazimierz Madaliński, Andrzej Zieliński, Anna Boguradzka, Rafał Gierczyński, Małgorzata Stępień
BACKGROUND & AIMS: There is a considerable burden of hepatitis C in Europe related to the lack of prompt diagnosis. We aimed to estimate the prevalence and related risk factors of HCV infections by the stages of liver fibrosis, using non-invasive methods, to understand testing needs in Poland. METHODS: A cross-sectional study was conducted in 2012-2016 adopting a stratified random sampling of primary health care units followed by systematic sampling of patients within each unit...
2017: PloS One
https://www.readbyqxmd.com/read/28930827/comparative-efficacy-and-safety-of-oral-antidiabetic-drugs-and-insulin-in-treating-gestational-diabetes-mellitus-an-updated-prisma-compliant-network-meta-analysis
#11
Hui-Ling Liang, Shu-Juan Ma, Yan-Ni Xiao, Hong-Zhuan Tan
BACKGROUND: The safety and efficacy of different drugs in treatment of gestational diabetes mellitus (GDM) patients who could not maintain normal glucose level only through diet and exercise remains to be debated. We performed this network meta-analysis (NAM) to compare and rank different antidiabetic drugs in glucose level control and pregnancy outcomes in GDM patients. METHODS: We searched PubMed, Cochrane Library, Web of Science, and Embase up to December 31, 2016...
September 2017: Medicine (Baltimore)
https://www.readbyqxmd.com/read/28930692/palbociclib-in-hormone-receptor-positive-advanced-breast-cancer-a-cost-utility-analysis
#12
J Raphael, J Helou, K I Pritchard, D M Naimark
INTRODUCTION: The addition of palbociclib to letrozole improves progression-free survival in the first-line treatment of hormone receptor positive advanced breast cancer (ABC). This study assesses the cost-utility of palbociclib from the Canadian healthcare payer perspective. METHODS: A probabilistic discrete event simulation (DES) model was developed and parameterised with data from the PALOMA 1 and 2 trials and other sources. The incremental cost per quality-adjusted life-month (QALM) gained for palbociclib was calculated...
September 17, 2017: European Journal of Cancer
https://www.readbyqxmd.com/read/28929693/-intestinal-absorption-of-ginseng-radix-et-rhizoma-extract-combined-with-acori-tatarinowii-rhizoma-in-rats
#13
Meng-Cheng Zheng, Shou-Ying Du, Shan Jia, Jun-Ming Ma, Qing Zhang, Jie Bai, Yang Lu
To investigate the changes in intestinal absorption of ginsenosides Rg₁, ginsenosides Re and ginsenosides Rd after combined administration of Ginseng Radix et Rhizoma extract and Acori Tatarinowii Rhizoma, in order to confirm whether the combined administration is scientific and rational, and provide experimental basis for pharmaceutical studies of the formula. An in vivo single-pass perfusion method was performed to study the effect of various concentrations of ginsenosides Rg₁, ginsenosides Re, ginsenosides Rd on the intestinal absorption at duodenum, jejunum, ileum and colon...
November 2016: Zhongguo Zhong Yao za Zhi, Zhongguo Zhongyao Zazhi, China Journal of Chinese Materia Medica
https://www.readbyqxmd.com/read/28927869/what-have-we-learned-from-best
#14
Cornelia F Allaart, Iris M Markusse, Willem F Lems
BACKGROUND: How have the long term outcomes of RA improved in the last decade? METHODS: Patients with DMARD naïve RA were randomized to 4 treatment strategies: 1. sequential DMARD monotherapy, 2. step-up combination therapy, 3. initial combination therapy including prednisone or 4. including infliximab. Treatment-to-target was aimed at DAS≤2.4 (three-monthly calculations). Functional ability (HAQ), radiologic damage progression (Sharp/vanderHeijde Score) and overall survival were reported...
September 16, 2017: Clinical Immunology: the Official Journal of the Clinical Immunology Society
https://www.readbyqxmd.com/read/28927791/design-and-synthesis-of-novel-prmt1-inhibitors-and-investigation-of-their-binding-preferences-using-molecular-modelling
#15
Hao Yang, Yifan Ouyang, Hao Ma, Hui Cong, Chunlin Zhuang, Wun-Taai Lok, Zhe Wang, Xuanli Zhu, Yutong Sun, Wei Hong, Hao Wang
Protein arginine methyltransferase 1 (PRMT1) catalyses the methylation of substrate arginine by transferring the methyl group from SAM (S-adenosyl-l-methionine), which leads to the formation of S-adenosyl homocysteine (SAH) and methylated arginine. We have shown previously that the Asp84 on PRMT1 could be a potential inhibitor binding site. In the current study, 28 compounds were designed and synthesized that were predicted to bind the Asp84 and substrate arginine sites together. Among them, 6 compounds were identified as potential PRMT1 inhibitors, and showed strong inhibitory effects on cancer cell lines, especially HepG2...
September 8, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28927738/dmard-use-is-associated-with-a-higher-risk-of-dementia-in-patients-with-rheumatoid-arthritis-a-propensity-score-matched-case-control-study
#16
Ming-Hsien Chou, Jong-Yi Wang, Cheng-Li Lin, Wei-Sheng Chung
BACKGROUND: Patients with rheumatoid arthritis (RA) exhibit an increased risk of dementia. Disease-modifying antirheumatic drugs (DMARDs) are commonly used to slow RA progression, but studies investigating the relationship between DMARDs and dementia in patients with RA are lacking. We investigated the relationship between DMARDs and dementia in patients with RA. METHODS: Using the National Health Insurance Research Database, patients aged ≥20years, who were newly diagnosed with RA between 2000 and 2011 were identified...
September 16, 2017: Toxicology and Applied Pharmacology
https://www.readbyqxmd.com/read/28927283/proposed-anti-hsv-compounds-isolated-from-simira-species
#17
Jessica F Cavalcanti, Marcelo F de Araujo, Priscila B Gonçalves, Nelilma C Romeiro, Maria T Villela Romanos, Ivo J Curcino Vieira, Raimundo Braz-Filho, Mário G de Carvalho
Secondary metabolites isolated from Simira eleiezeriana and Simira glaziovii were evaluated against herpes simplex virus (HSV-1) and (HSV-2). The 50% effective concentrations values (EC50) were calculated from the dose-response curve and the selectivity index (SI) against the virus. The physicochemical data LogP, (PSA), (NRB), (HBA) and (HBD) were obtained using Marvin Sketch. Among the tested compounds, conipheraldeyde, harman and simirane A showed better results with EC50 6.39; 4.90; 4.61 µg/mL and SI 78...
September 19, 2017: Natural Product Research
https://www.readbyqxmd.com/read/28927275/proton-coupled-conformational-allostery-modulates-the-inhibitor-selectivity-for-%C3%AE-secretase
#18
Robert C Harris, Cheng-Chieh Tsai, Christopher R Ellis, Jana Shen
Many important pharmaceutical targets, such as aspartyl proteases and kinases, exhibit pH-dependent dynamics, functions and inhibition. Accurate prediction of their binding free energies is challenging because current computational techniques neglect the effects of pH. Here we combine free energy perturbation calculations with continuous constant pH molecular dynamics to explore the selectivity of a small-molecule inhibitor for β-secretase (BACE1), an important drug target for Alzheimer's disease. The calculations predicted identical affinity for BACE1 and the closely related cathepsin D at high pH; however, at pH 4...
September 21, 2017: Journal of Physical Chemistry Letters
https://www.readbyqxmd.com/read/28926716/broadband-acoustic-resonance-dissolution-spectroscopy-bards-a-novel-approach-to-investigate-the-wettability-of-pharmaceutical-powder-blends
#19
Raghu V G Peddapatla, M Rizwan Ahmed, Caroline A Blackshields, M J Sousa-Gallagher, Sean McSweeney, J Krüse, Abina M Crean, Dara Fitzpatrick
The ability of Broadband Acoustic Resonance Dissolution Spectroscopy (BARDS) to assess the wettability of powder blends is investigated. BARDS is a novel analytical technology developed based on the change in acoustic phenomenon observed when material is added into a solvent under resonance. Addition of solid material to the solvent results in the introduction of gas (air) into the solvent, changing the compressibility of the solvent system and reducing the velocity of sound in the solvent. As a material is wetted and dissolved, the gas is released from the solvent and resonance frequency is altered...
September 19, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/28925560/apremilast-in-psoriasis-a-prospective-real-world-study
#20
I Vujic, R Herman, M Sanlorenzo, C Posch, B Monshi, K Rappersberger, L Richter
BACKGROUND: Apremilast is a novel oral phosphodiesterase-4 inhibitor approved for psoriasis treatment. Randomized trials have documented its efficacy and safety, but data on real-world patients are scarce. OBJECTIVES: We aim to characterize psoriasis patients treated with apremilast in a real-world setting and calculate drug survival as an important measure of efficacy and compliance. METHODS: All psoriasis patients that received apremilast between April 1(st) 2015 and January 19(th) 2017 were evaluated every 4 weeks and we documented: age, weight, height, smoking status, family history of psoriasis, joint involvement, previous treatments, psoriasis area severity index (PASI) scores, and the onset and duration of adverse events (AE)...
September 19, 2017: Journal of the European Academy of Dermatology and Venereology: JEADV
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