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Baomin Liu, Hui Qin, Yinsheng Zhang
Bendamustine hydrochloride is an alkylating agent which was developed for the treatment of various human cancers. The stable isotope-labeled bendamustine was required to support clinic studies. An effective and operationally simple method for the synthesis of [D6 ] bendamustine hydrochloride was developed using DCl as a catalyst and D2 O as a deuterium source. Under the present condition, regioselectively deuterated bendamustine hydrochloride with high deuterium incorporation is achieved.
May 17, 2018: Journal of Labelled Compounds & Radiopharmaceuticals
Long Yuan, Shenita Basdeo, Qin C Ji
BMS-986104 is a S1P1 R modulator drug candidate under development and has been evaluated in Phase I clinical trials. BMS-986104 functions as a prodrug and undergoes enzymatic transformations in vivo to form the pharmacologically active phosphate drug, BMS-986104-P. Here, we report approaches to overcome the stability, solubility and extraction challenges in developing a sensitive, accurate and rugged LC-MS/MS method for the simultaneous quantification of the phosphate drug and its prodrug in blood lysate. An effective stabilization strategy using a cocktail of phosphatase and kinase inhibitors was developed to ensure the stability of both analytes during sample collection, storage, and processing...
May 5, 2018: Journal of Pharmaceutical and Biomedical Analysis
Ren-Tsung Wu, Xiaodong Chi, Takehiro Hirao, Vincent M Lynch, Jonathan L Sessler
A new carboxylic acid-functionalized "Texas-sized" molecular box TxSB-CO2H has been prepared by combining two separate build-ing blocks via an iodide-catalyzed macrocyclization reaction. A single crystal X-ray diffraction analysis revealed a paired "clip-like" dimer in the solid state. Concentration-dependent behavior is seen for samples of TxSB-CO2H as prepared, as inferred from 1H NMR spectroscopic studies carried out in DMSO-d6. However, in the presence of excess acid (1% by weight of deuterated trifluo-racetic acid; TFA-d1), little evidence of aggregation is seen in DMSO-d6 except at the highest accessible concentrations...
May 14, 2018: Journal of the American Chemical Society
Miguel Quiliano, Adriana Pabón, Ernest Moles, Leonardo Bonilla-Ramirez, Isabelle Fabing, Kim Y Fong, Diego A Nieto-Aco, David W Wright, Juan C Pizarro, Ariane Vettorazzi, Adela López de Cerain, Eric Deharo, Xavier Fernández-Busquets, Giovanny Garavito, Ignacio Aldana, Silvia Galiano
Design, synthesis, structure-activity relationship, cytotoxicity studies, in silico drug-likeness, genotoxicity screening, and in vivo studies of new 1-aryl-3-substituted propanol derivatives led to the identification of nine compounds with promising in vitro (55, 56, 61, 64, 66, and 70-73) and in vivo (66 and 72) antimalarial profiles against Plasmodium falciparum and Plasmodium berghei. Compounds 55, 56, 61, 64, 66 and 70-73 exhibited potent antiplasmodial activity against chloroquine-resistant strain FCR-3 (IC50 s < 0...
April 24, 2018: European Journal of Medicinal Chemistry
Mette Kragh, Erik Roj Larsen, Klaus Martiny, Dorthe Norden Møller, Camilla Schultz Wihlborg, Tove Lindhardt, Poul Videbech
There is growing evidence for combined chronotherapeutic interventions as adjunctive treatments for major depression. However, as the treatments can be demanding, we need to identify predictors of response. This study aimed to describe predictors of response, remission and deterioration in the short-term phase, as well as predictors of long-term response. The predictors investigated were gender, type of depression, severity of depression, treatment resistance, quetiapine use, general self-efficacy, educational level and positive diurnal variation...
May 11, 2018: Chronobiology International
Nguyen Ngoc Quang, Marina Chavchich, Chu Xuan Anh, Geoffrey W Birrell, Karin van Breda, Thomas Travers, Kerryn Rowcliffe, Michael D Edstein
The pharmacokinetics (PK) and ex vivo activity (pharmacodynamics [PD]) of two artemisinin combination therapies (ACTs) (artemisinin-piperaquine [ARN-PPQ] [Artequick® ] and artesunate-amodiaquine [ARS-AQ] [Coarsucam™ ]) in healthy Vietnamese volunteers were compared following 3-day courses of the ACTs for the preselection of the drugs for falciparum malaria therapy. For PK analysis, serial plasma samples were collected from two separate groups of 22 volunteers after ACT administration. Of these volunteers, ex vivo activity was assessed in plasma samples from seven volunteers who received both ACTs...
May 7, 2018: American Journal of Tropical Medicine and Hygiene
X J Zhang, Q Lv, L H Min, X H Cao, X J Li
  Purpose Our objective was to evaluate the birth outcomes of FET from different developmental stage of embryo at freezing (Day 3, Day 5 and Day 6). Methods All vitrified-warmed day 3 (D3) and day 5/6 (D5, D6) embryo transfers during the time period from January 2013 until December 2015 were included in the study. The Birthweight, Low birthweight (LBW), sexual distinction, gestation and for singleton births and twins conceived by FET were compared retrospectively between three cryopreservation strategies utilizing either D3, D5 or D6 embryo freezing...
September 2017: Cryo Letters
Liqin Zhi, Lin Xu, Xudan He, Chunhui Zhang, Yaqi Cai
In the present study, the occurrence and distribution of methylsiloxanes (D4-D6, L5-L16) in the surface water and sediment collected from the Daqing oilfield were explored. For wastewater samples from an oilfield combination station, the concentrations of total cyclic methylsiloxanes (∑CMS, D4-D6) and total linear methylsiloxanes (∑LMS, L5-L16) ranged from 137-1911ng/L to 49.4-190ng/L, respectively. Cyclic methylsiloxanes were the predominant methylsiloxanes in the analyzed wastewater samples from the oilfield combination station...
August 1, 2018: Science of the Total Environment
Sandeep R Kunati, Shuming Yang, Basem M William, Yan Xu
Curcumin, a principal curcuminoid of turmeric, gained a lot of attention recently due to its wide spectrum of pharmacological activities in prevention and treatment of various human conditions. The current clinical study is focused on the determination of efficacy and tolerability of curcumin and vitamin D3 combination in patients with early-stage chronic lymphocytic leukemia (CLL) or small lymphocytic lymphoma (SLL). To support this work, an LC-MS/MS method has been developed for simultaneous determination of curcumin and its metabolites, curcumin glucuronide (COG) and curcumin sulfate (COS), in human plasma using curcumin-d6 as an internal standard for curcumin and BPAG-d6 as an internal standard for COG and COS...
April 23, 2018: Journal of Pharmaceutical and Biomedical Analysis
Ivan H Yoshida, Monise Santos, Caroline Z Berton, Caroline L Chiarella, Michelli S Tanada, Emerson BCordts, Waldemar P de Carvalho, Caio P Barbosa
OBJECTIVE: Euploid embryo transfers yield better implantation rates. In Brazil, morphological evaluation is performed to select the best embryos, since genetic analysis is still an expensive procedure. This study aimed to evaluate whether there is an association between trophectoderm morphology and ploidy status. METHODS: The study included 113 blastocysts formed in D5/D6 from 58 in vitro fertilization cycles held from January/2016 to May/2017. All patients with indication for PGD/PGS were included in the study...
May 3, 2018: JBRA Assisted Reproduction
Ahilanandan Dushianthan, Rebecca Cusack, Michael P W Grocott, Anthony D Postle
Acute respiratory distress syndrome (ARDS) is associated with a severe pro-inflammatory response; although decreased plasma cholesterol concentration has been linked to systemic inflammation, any association of phospholipid metabolic pathways with ARDS has not been characterized. Plasma phosphatidylcholine (PC), the major phospholipid of circulating lipoproteins, is synthesized in human liver by two biologically diverse pathways: the CDP:choline and phosphatidylethanolamine-N-methyltransferase (PEMT) pathways...
May 1, 2018: Journal of Lipid Research
Per Bech, Nina Timmerby
INTRODUCTION: Measurement-based care (MBC) transfers the scientific principle from controlled clinical trials to the daily routine treatment to improve the care of patients with anxiety and depression. AIM: Within the pharmacopsychometric triangle in which the domain of desired clinical effect of treatment is balanced against the domain of undesired treatment side effects in terms of the domain of restored well-being. The relevance of these domains both in the controlled clinical trials and in the MBC trials will be tested...
May 1, 2018: Nordic Journal of Psychiatry
Yvonne W S Jauw, Dennis F Heijtel, Josée M Zijlstra, Otto S Hoekstra, Henrica C W de Vet, Danielle J Vugts, Henk M Verheul, Ronald Boellaard, Sonja Zweegman, Guus A M S van Dongen, C Willemien Menke-van der Houven van Oordt, Adriaan A Lammertsma, Marc C Huisman
PURPOSE: Positron emission tomography (PET) with Zirconium-89 (Zr-89)-labeled antibodies can be used for in vivo quantification of antibody uptake. Knowledge about measurement variability is required to ensure correct interpretation. However, no clinical studies have been reported on measurement variability of Zr-89 immuno-PET. As variability due to low signal-to-noise is part of the total measurement variability, the aim of this study was to assess noise-induced variability of Zr-89 -immuno-PET using count-reduced clinical images...
April 30, 2018: Molecular Imaging and Biology: MIB: the Official Publication of the Academy of Molecular Imaging
Jianrong Steve Zhou, Xiaolei Huang, William Ray Jun Jie Oh
Enantioselective α-arylation of racemic ketones containing existing α'-stereocenters is realized for the first time under base-assisted dynamic kinetic resolution. Bridged bicyclic rings are formed in good ee values, which are difficult to obtain otherwise. Furthermore, reactions in DMSO-d6 resulted in extensive deuteration of both α and α' positions in the products, supporting a pathway involving rapid, reversible deprotonation of ketones under the catalytic conditions.
April 30, 2018: Angewandte Chemie
Guillermo Carlos Bazan, Cheng Zhou, Geraldine Chia, James Ho, Thomas Seviour, Talgat Sailov, Bo Liedberg, Staffan Kjelleberg, Jamie Hinks
Membrane-intercalating conjugated oligoelectrolytes (COEs) are emerging as potential alternatives to conventional, yet increasingly ineffective, antimicrobial agents. Three readily accessible COEs, belonging to an unreported series containing a stilbene core, namely COE-D4, COE-D6 and COE-D8, were designed and synthesized so that hydrophobicity increased with increasing side-chain length. A decrease in solubility in aqueous media correlated with an increase in uptake by E. coli. The longest COE, COE-D8, achieved a Minimum Inhibitory Concentration (MIC) value of 4 μg/mL against both E...
April 29, 2018: Angewandte Chemie
Micah Oyaro, John Wylie, Chien-Yu Chen, Raphael O Ondondo, Anna Kramvis
Background: Drug users act as reservoirs and transmission channels for hepatitis B virus (HBV), hepatitis C virus (HCV) and human immunodeficiency virus (HIV) infections to the general population worldwide. Periodic epidemiological studies to monitor the prevalence and genetic diversity of these infections to inform on interventions are limited. Objective of the study: The objective of this study was to determine the predictors of HIV infection and genetic diversity of HBV and HCV among drug users in Kenya...
2018: Southern African Journal of HIV Medicine
Hesam Mirmohammadi, Monika Sitarz, Hagay Shemesh
Introduction: Manufacturers offer gutta-percha (GP) cones matched with different sizes of endodontic files as an attempt to simplify the obturation process and create a tight seal in the canal. The purpose of this study was to evaluate whether intra-manufacture GP diameters matched the diameters of their corresponding files at different levels using laser micrometre. Methods and Materials: Twenty files and corresponding GP master cones of Reciproc R40 (40/0.06) (VDW, Munich, Germany), WaveOne Large(40/0...
2018: Iranian Endodontic Journal
Wenji Li, Hilly Yang, Brian Buckley, Lujing Wang, Ah-Ng Kong
Even through more sensitive methods for quantifying trace levels of curcumin in plasma were urgently needed, beyond tandem mass spectrometry, the Paul trap MS/MS/MS has never been tested for curcumin quantification. Because of its unique trap function to accumulate target compounds selectively by optimizing multiple stage MS experiments, it showed great potential to remove background issues reported at low concentration ranges. A novel Triple stage Ion Trap Mass Spectrometry coupled with High Performance Liquid Chromatography (HPLC-ITMS/MS/MS) method has been developed and validated as a curcumin quantification method, for the first time...
April 17, 2018: Journal of Pharmaceutical and Biomedical Analysis
Lauren Bottorf, Indra D Sahu, Robert M McCarrick, Gary A Lorigan
Electron spin echo envelope modulation (ESEEM) spectroscopy in combination with site-directed spin labeling (SDSL) has been established as a valuable biophysical technique to provide site-specific local secondary structure of membrane proteins. This pulsed electron paramagnetic resonance (EPR) method can successfully distinguish between α-helices, β-sheets, and 310 -helices by strategically using 2 H-labeled amino acids and SDSL. In this study, we have explored the use of 13 C-labeled residues as the NMR active nuclei for this approach for the first time...
April 22, 2018: Biochimica et Biophysica Acta
Ji Kun Xu, Zhen Wen Yu, Yu Shi, Jun Ye Zhao, Xi Zhi Wang, Yu Qiu Wang
A two-year field experiment was conducted in 2014-2015 and 2015-2016 wheat growing seasons to study the effects of micro-sprinkling hose length and width on field water condition, and flag leaf chlorophyll fluorescence characteristics in different sampling districts (D1 to D6 along with the hose laying direction). Six micro-sprinkling hose treatments were set: 60 m (T1 ), 80 m (T2 ) and 100 m (T3 ) lengths under 65 mm width; 60 m (T4 ), 80 m (T5 ) and 100 m (T6 ) lengths under 80 mm width. The results showed that after irrigation at jointing, the Christiansen uniformity coefficient (Cu ) of T1 was significantly higher than T2 and T3 under 65 mm hose width...
November 2017: Ying Yong Sheng Tai Xue Bao, the Journal of Applied Ecology
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