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https://www.readbyqxmd.com/read/28074653/the-essential-medicinal-chemistry-of-curcumin
#1
Kathryn M Nelson, Jayme L Dahlin, Jonathan Bisson, James Graham, Guido F Pauli, Michael A Walters
Curcumin is a constituent (up to ∼5%) of the traditional medicine known as turmeric. Interest in the therapeutic use of turmeric and the relative ease of isolation of curcuminoids has led to their extensive investigation. Curcumin has recently been classified as both a PAINS (pan-assay interference compounds) and an IMPS (invalid metabolic panaceas) candidate. The likely false activity of curcumin in vitro and in vivo has resulted in >120 clinical trials of curcuminoids against several diseases. No double-blinded, placebo controlled clinical trial of curcumin has been successful...
January 11, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28068053/surface-modification-of-gold-nanoparticles-with-small-molecules-for-biochemical-analysis
#2
Yiping Chen, Yunlei Xianyu, Xingyu Jiang
As one of the major tools for and by chemical science, biochemical analysis is becoming increasingly important in fields like clinical diagnosis, food safety, environmental monitoring, and the development of chemistry and biochemistry. The advancement of nanotechnology boosts the development of analytical chemistry, particularly the nanoparticle (NP)-based approaches for biochemical assays. Functional NPs can greatly improve the performance of biochemical analysis because they can accelerate signal transduction, enhance the signal intensity, and enable convenient signal readout due to their unique physical and chemical properties...
January 9, 2017: Accounts of Chemical Research
https://www.readbyqxmd.com/read/28054632/a-sensitive-three-monoclonal-antibodies-based-automatic-latex-particle-enhanced-turbidimetric-immunoassay-for-golgi-protein-73-detection
#3
Yanyan Xia, Han Shen, Yefei Zhu, Hongpan Xu, Zhiyang Li, Jin Si
Golgi protein 73 (GP73) is a novel and potential marker for diagnosing hepatocellular carcinoma (HCC) that has been found to be abnormally elevated in liver disease. A latex particle-enhanced turbidimetric immunoassay (LTIA) was recently introduced and licensed for application in a variety of automated clinical chemistry analyzers. However, no studies have reported sufficient data on analytical performance of this method when using 3 monoclonal antibodies for GP73 measurement. The experimental conditions were firstly optimized and range of linearity, diagnostic potential, clinical relevance were compared with the LTIA based on polyclonal antibodies and ELISA...
January 5, 2017: Scientific Reports
https://www.readbyqxmd.com/read/27992181/multiparametric-assessment-of-gold-nanoparticle-cytotoxicity-in-cancerous-and-healthy-cells-the-role-of-size-shape-and-surface-chemistry
#4
Manjari Bhamidipati, Laura Fabris
In recent years we and others have become interested in evaluating the use of surface-enhanced Raman scattering (SERS)-tags for early cancer detection and in designing new approaches to demonstrate the applicability of this spectroscopic technique in the clinic. SERS-based imaging, in particular, offers ultra sensitivity up to the single molecule, multiplexing capability, increased photostability, and has been shown to outperform fluorescence. However, in order to employ SERS tags for early cancer detection, it is important to understand their interaction with cells and determine their cytotoxicity...
December 19, 2016: Bioconjugate Chemistry
https://www.readbyqxmd.com/read/27978469/highly-sensitive-lc-ms-ms-methods-for-the-determination-of-seven-human-cyp450-activities-using-small-oral-doses-of-probe-drugs-in-human
#5
Alexia Grangeon, Sophie Gravel, Fleur Gaudette, Jacques Turgeon, Veronique Michaud
Cocktails composed of several Cytochrome P450 (CYP450)-selective probe drugs have been shown of value to characterize in vivo drug-metabolism activities. Our objective was to develop and validate highly sensitive and selective LC-MS/MS assays allowing the determination of seven major human CYP450 isoenzyme activities following administration of low oral doses of a modified CYP450 probe-drug cocktail in patients. The seven-drug cocktail was composed of caffeine, bupropion, tolbutamide, omeprazole, dextromethorphan, midazolam (all administered concomitantly) and chlorzoxazone (administered separately) to phenotype for CYP1A2, 2B6, 2C9, 2C19, 2D6, 3A4/5 and 2E1, respectively...
January 1, 2017: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
https://www.readbyqxmd.com/read/27916120/development-and-statistical-assessment-of-a-paper-based-immunoassay-for-detection-of-tumor-markers
#6
Thiago Mazzu-Nascimento, Giorgio Gianini Morbioli, Luis Aparecido Milan, Fabiana Cristina Donofrio, Carlos Alberto Mestriner, Emanuel Carrilho
Paper-based assays are an attractive low-cost option for clinical chemistry testing, due to characteristics such as short time of analysis, low consumption of samples and reagents, and high portability of assays. However, little attention has been given to the evaluation of the performance of these simple tests, which should include the use of a statistical approach to define the choice of best cut-off value for the test. The choice of the cut-off value impacts on the sensitivity and specificity of the bioassay...
January 15, 2017: Analytica Chimica Acta
https://www.readbyqxmd.com/read/27912126/evaluation-of-the-inactivation-effect-of-triton-x-100-on-ebola-virus-infectivity
#7
Francesca Colavita, Serena Quartu, Eleonora Lalle, Licia Bordi, Daniele Lapa, Silvia Meschi, Antonella Vulcano, Antonietta Toffoletti, Eugenio Bordi, Maria Grazia Paglia, Antonino Di Caro, Giuseppe Ippolito, Maria Rosaria Capobianchi, Concetta Castilletti
BACKGROUND: The recent Ebola virus disease outbreak occurred in West Africa since December 2013 highlighted the need of appropriate virus inactivation procedures to be set up to allow the necessary processing of specimens outside BSL-4 facilities and to perform laboratory tests without affecting clinical decisions. For this purpose, international guidelines suggest the pre-treatment of the samples with Triton X-100. OBJECTIVES: Due to the limited scientific evidence about the efficacy of Triton X-100 on enveloped-viruses, the aim of this work was to evaluate the effect of Triton X-100 on the virus infectivity and to establish the optimal conditions for its use...
January 2017: Journal of Clinical Virology: the Official Publication of the Pan American Society for Clinical Virology
https://www.readbyqxmd.com/read/27899562/the-chembl-database-in-2017
#8
Anna Gaulton, Anne Hersey, Michał Nowotka, A Patrícia Bento, Jon Chambers, David Mendez, Prudence Mutowo, Francis Atkinson, Louisa J Bellis, Elena Cibrián-Uhalte, Mark Davies, Nathan Dedman, Anneli Karlsson, María Paula Magariños, John P Overington, George Papadatos, Ines Smit, Andrew R Leach
ChEMBL is an open large-scale bioactivity database (https://www.ebi.ac.uk/chembl), previously described in the 2012 and 2014 Nucleic Acids Research Database Issues. Since then, alongside the continued extraction of data from the medicinal chemistry literature, new sources of bioactivity data have also been added to the database. These include: deposited data sets from neglected disease screening; crop protection data; drug metabolism and disposition data and bioactivity data from patents. A number of improvements and new features have also been incorporated...
January 4, 2017: Nucleic Acids Research
https://www.readbyqxmd.com/read/27884478/vaccine-provision-delivering-sustained-widespread-use
#9
Scott Preiss, Nathalie Garçon, Anthony L Cunningham, Richard Strugnell, Leonard R Friedland
The administration of a vaccine to a recipient is the final step in a development and production process that may have begun several decades earlier. Here we describe the scale and complexity of the processes that brings a candidate vaccine through clinical development to the recipient. These challenges include ensuring vaccine quality (between 100 and 500 different Quality Control tests are performed during production to continually assess safety, potency and purity); making decisions about optimal vaccine presentation (pre-filled syringes versus multi-dose vials) that affect capacity and supply; and the importance of maintaining the vaccine cold chain (most vaccines have stringent storage temperature requirements necessary to maintain activity and potency)...
December 20, 2016: Vaccine
https://www.readbyqxmd.com/read/27872506/harmonising-adult-reference-intervals-in-australia-and-new-zealand-the-continuing-story
#10
REVIEW
Gus Koerbin, Jillian R Tate
Reference intervals (RIs) are used to help clinicians determine if a patient can be classified as being in a diseased or healthy state and there are often sound scientific and clinical reasons for differences in RIs. One of the current strategic priorities for the Australasian Association of Clinical Biochemists is to encourage and assist laboratories to achieve harmonisation of RIs for common clinical chemistry analytes where sound calibration and traceability are in place. This need is based on good laboratory practice, providing the clinician with results that allow appropriate and reliable clinical interpretation and progression further toward the national e-health framework and a single electronic health record...
August 2016: Clinical Biochemist. Reviews
https://www.readbyqxmd.com/read/27867948/supra-therapeutic-plasma-concentrations-of-haloperidol-induce-moderate-inhibition-of-lipopolysaccharide-induced-interleukin-8-release-in-human-monocytes
#11
Herbert Bosshart
BACKGROUND: The clinical use of antipsychotics and mood-stabilizing drugs with proven efficacy is largely determined by the occurrence of treatment-emergent adverse events and routine clinical chemistry and haematology data, which together define the safety and tolerability profile of these psychopharmaceuticals. Whereas the effects of mood-stabilizing drugs on functional properties of blood cells have been poorly investigated, the effects of antipsychotics have received more attention...
October 2016: Annals of Translational Medicine
https://www.readbyqxmd.com/read/27858150/coffee-and-oxidative-stress-a-human-intervention-study
#12
Sergey Shaposhnikov, Thomas Hatzold, Naouale El Yamani, Philip Mark Stavro, Yolanda Lorenzo, Maria Dusinska, Astrid Reus, Wilrike Pasman, Andrew Collins
PURPOSE: Coffee is known to contain phytochemicals with antioxidant potential. The aim of this study was to investigate possible antioxidant effects of coffee in healthy human volunteers. METHODS: A placebo-controlled intervention trial was carried out on 160 healthy human subjects, randomised into three groups, receiving 3 or 5 cups of study coffee or water per day, for 8 weeks. Blood samples were taken before, during, and after the intervention. Serum was used for analysis of blood lipids and standard clinical chemistry analytes...
November 17, 2016: European Journal of Nutrition
https://www.readbyqxmd.com/read/27797468/host-cell-interactions-are-a-significant-barrier-to-the-clinical-utility-of-peptide-antibiotics
#13
Charles G Starr, Jing He, William C Wimley
Despite longstanding promise and many known examples, antimicrobial peptides (AMPs) have failed, thus far, to impact human medicine. On the basis of the physical chemistry and mechanism of action of AMPs, we hypothesized that host cell interactions could contribute to a loss of activity in vivo where host cells are highly concentrated. To test this idea, we characterized AMP activity in the presence of human red blood cells (RBC). Indeed, we show that most of a representative set of natural and synthetic AMPs tested are significantly inhibited by preincubation with host cells and would be effectively inactive at physiological cell density...
December 16, 2016: ACS Chemical Biology
https://www.readbyqxmd.com/read/27784162/multicomponent-chemistry-in-the-synthesis-of-carbonic-anhydrase-inhibitors
#14
Stanislav Kalinin, Claudiu T Supuran, Mikhail Krasavin
Carbonic anhydrase inhibitors (CAIs) are of growing interest since various isoforms of the enzyme are identified as promising drug targets for treatment of disease. The principal drawback of the clinically used CAIs is the lack of isoform selectivity, which may lead to observable side effects. Studies aiming at the design of isoform-selective CAIs entail generation and biological testing of arrays of compounds, which is a resource- and time-consuming process. Employment of multicomponent reactions is an efficient synthetic strategy in terms of gaining convenient and speedy access to a range of scaffolds with a high degree of molecular diversity...
2016: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/27779667/lipopolysaccharide-induced-cytokine-expression-pattern-in-peripheral-blood-mononuclear-cells-in-childhood-obesity
#15
Yu Wu, Bin Yue, Jia Liu
Obesity is characterized by the abnormal or excessive fat accumulation that may impair health and extensive increase in body mass index (BMI). Childhood obesity may occur due to disturbances in metabolic regulation, which lead to metabolic syndrome and other diseases. Peripheral blood suspended immune cells are responsible for immune surveillance. The aim of the present study was to map the inflammatory cytokine expression pattern of isolated peripheral blood mononuclear cells (PBMCs) following lipopolysaccharide (LPS) stress in vitro and clinical chemistry parameters in the plasma of subjects...
December 2016: Molecular Medicine Reports
https://www.readbyqxmd.com/read/27777860/the-study-of-statistical-methods-for-evaluating-the-comparability-of-routine-chemistry-analytes-among-3-routine-laboratory-measurement-systems-in-china
#16
Kun Zhong, Wei Wang, Chuanbao Zhang, Falin He, Shuai Yuan, Zhiguo Wang
BACKGROUND: Clinical laboratory tests are important for clinicians to make diagnostic decisions, but discrepancies may directly lead to incorrect diagnosis. We would like to introduce some statistical methods to evaluate the comparability of chemistry analytes while comparing the performances of different measurement systems. METHODS: We used a panel of 10 fresh-frozen single donation serum samples to assess assays for the measurement of glucose and other 13 analytes...
2016: SpringerPlus
https://www.readbyqxmd.com/read/27768244/detection-limits-of-quantitative-and-digital-pcr-assays-and-their-influence-in-presence-absence-surveys-of-environmental-dna
#17
Margaret E Hunter, Robert M Dorazio, John S S Butterfield, Gaia Meigs-Friend, Leo G Nico, Jason A Ferrante
A set of universal guidelines is needed to determine the limit of detection (LOD) in PCR-based analyses of low-concentration DNA. In particular, environmental DNA (eDNA) studies require sensitive and reliable methods to detect rare and cryptic species through shed genetic material in environmental samples. Current strategies for assessing detection limits of eDNA are either too stringent or subjective, possibly resulting in biased estimates of species' presence. Here, a conservative LOD analysis grounded in analytical chemistry is proposed to correct for overestimated DNA concentrations predominantly caused by the concentration plateau, a nonlinear relationship between expected and measured DNA concentrations...
October 21, 2016: Molecular Ecology Resources
https://www.readbyqxmd.com/read/27750201/antitubercular-activity-of-1-2-3-triazolyl-fatty-acid-derivatives
#18
Diego G Ghiano, Agustina de la Iglesia, Nina Liu, Peter J Tonge, Héctor R Morbidoni, Guillermo R Labadie
A collection of 1,2,3-triazoles unsaturated fatty acid mimics were efficiently synthesized by click chemistry. The 1,4-disubstituted analogs prepared covered different alkyl chain lengths and triazole positions. The compounds were subsequently tested against Mycobacterium tuberculosis, being most of them active with some of the analogs displaying activity at micromolar concentration. The most potent member of the series has the triazole moiety on the C-2 position with a carbon chain of eight or ten carbon atoms...
January 5, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27750199/potent-anticancer-activity-of-photo-activated-oxo-bridged-diiron-iii-complexes
#19
S Binita Chanu, Samya Banerjee, Mithun Roy
Cancer-specific anticancer drugs are still an elusive goal. Using light as the temporal control to generate cytotoxic species from photo-activated prodrug in the presence or absence of molecular oxygen has shown potential application targeted chemotherapy as in photodynamic therapy (PDT). In the present work we explored the chemistry of several photo-active (μ-oxo)diiron(III) complexes of the following formulation [{Fe(μ-O) (L-his)(B)}2](ClO4)2 (1a-1c), [Fe2(μ-O)(H2O)2B4](ClO4)4 (2b, 2c) and [Fe2(μ-O)(μ-O2CMe)B4](ClO4)3 (3b, 3c), L-his = l-histidine, B is 2,2'-bipyridine, 1,10-phenanthroline (phen) and dipyrido[3,2-d:2',3'-f]quinoxaline (dpq) complexes for tumor-specific anticancer activity...
January 5, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27718484/progress-and-impact-of-enzyme-measurement-standardization
#20
Ilenia Infusino, Erika Frusciante, Federica Braga, Mauro Panteghini
International Federation of Clinical Chemistry and Laboratory Medicine (IFCC) has established reference measurement procedures (RMPs) for the most popular enzymes. Manufacturers should assign values to commercial calibrators traceable to these RMPs to achieve equivalent results in clinical samples, independent of reagent kits, instruments, and laboratory where the measurement is carried out. The situation is, however, far from acceptable. Some manufacturers continue to market assays giving results that are not traceable to internationally accepted RMPs...
October 8, 2016: Clinical Chemistry and Laboratory Medicine: CCLM
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