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https://www.readbyqxmd.com/read/27926950/c6-and-c7-substituted-3-4-dihydro-2-1h-quinolinones-as-inhibitors-of-monoamine-oxidase
#1
L Meiring, J Petzer, A Petzer
Purpose Monoamine oxidase (MAO) inhibitors are considered to be useful therapeutic agents and isoform specific inhibitors are employed for the treatment of depression and Parkinson's disease. MAO inhibitors are also under investigation for the treatment of disorders ranging from Alzheimer's disease, prostate cancer and certain cardiomyopathies. While a number of irreversible MAO inhibitors are available in the clinic, reversible inhibitors, particularly of the MAO-B isoform are still being developed. Based on our interest in discovering reversible inhibitors with specificity for MAO-B, we have recently reported that, among a series of 10 3,4-dihydro-2(1H)-quinolinone derivatives, are high potency MAO-B inhibitors, with a number of homologues displaying good selectivities for MAO-B over the MAO-A isoform...
December 7, 2016: Drug Research
https://www.readbyqxmd.com/read/27926846/alamethicin-supramolecular-organization-in-lipid-membranes-from-19-f-solid-state-nmr
#2
Evgeniy S Salnikov, Jesus Raya, Marta De Zotti, Ekaterina Zaitseva, Cristina Peggion, Gema Ballano, Claudio Toniolo, Jan Raap, Burkhard Bechinger
Alamethicins (ALMs) are antimicrobial peptides of fungal origin. Their sequences are rich in hydrophobic amino acids and strongly interact with lipid membranes, where they cause a well-defined increase in conductivity. Therefore, the peptides are thought to form transmembrane helical bundles in which the more hydrophilic residues line a water-filled pore. Whereas the peptide has been well characterized in terms of secondary structure, membrane topology, and interactions, much fewer data are available regarding the quaternary arrangement of the helices within lipid bilayers...
December 6, 2016: Biophysical Journal
https://www.readbyqxmd.com/read/27926729/intracellular-allosteric-antagonism-of-the-ccr9-receptor
#3
Christine Oswald, Mathieu Rappas, James Kean, Andrew S Doré, James C Errey, Kirstie Bennett, Francesca Deflorian, John A Christopher, Ali Jazayeri, Jonathan S Mason, Miles Congreve, Robert M Cooke, Fiona H Marshall
Chemokines and their G-protein-coupled receptors play a diverse role in immune defence by controlling the migration, activation and survival of immune cells. They are also involved in viral entry, tumour growth and metastasis and hence are important drug targets in a wide range of diseases. Despite very significant efforts by the pharmaceutical industry to develop drugs, with over 50 small-molecule drugs directed at the family entering clinical development, only two compounds have reached the market: maraviroc (CCR5) for HIV infection and plerixafor (CXCR4) for stem-cell mobilization...
December 7, 2016: Nature
https://www.readbyqxmd.com/read/27926611/enhanced-anticancer-activity-of-drug-nanoparticles-formulated-with-%C3%AE-cyclodextrin
#4
Honglei Zhan, Tina Jagtiani, Jun F Liang
Camptothecin (CPT) is a potent chemotherapeutic agent that shows a broad spectrum of anticancer activities. However, it is clinically inactive because of poor aqueous solubility, rapid aqueous hydrolysis, and unexpected side effects. Three strategies have extensively been adopted to improve its dissolution rate including reduction of drug particle size to a nanoscale, use of an amorphous state, and the formation of inclusion compounds. In our study, we combined these three strategies together by constructing CPT nanoparticles by creating an inclusion complex with β-cyclodextrin (BCD)...
December 6, 2016: Anti-cancer Drugs
https://www.readbyqxmd.com/read/27926533/andrographolide-impedes-cancer-stemness-and-enhances-radio-sensitivity-in-oral-carcinomas-via-mir-218-activation
#5
Po-Yu Yang, Pei-Ling Hsieh, Tong Hong Wang, Cheng-Chia Yu, Ming-Yi Lu, Yi-Wen Liao, Tzu-Hsin Lee, Chih-Yu Peng
Current evidence suggests that oral cancer stem cells (OCSCs) possess high tumorigenic and metastatic properties as well as chemo- and radioresistance. In this study, we demonstrated that andrographolide, the main bioactive component in the medicinal plant Andrographis, significantly reduced oncogenicity and restored radio-sensitivity of ALDH1+CD44+ OCSCs. Mechanistic studies showed that andrographolide treatment increased the expression of microRNA-218 (miR-218), leading to the downregulation of Bmi1. We showed that knockdown of miR-218 in ALDH1-CD44- non-OCSCs enhanced cancer stemness, while silencing of Bmi1 significantly counteracted it...
December 1, 2016: Oncotarget
https://www.readbyqxmd.com/read/27925846/characteristics-sources-and-cytotoxicity-of-atmospheric-polycyclic-aromatic-hydrocarbons-in-urban-roadside-areas-of-hangzhou-china
#6
Hongzhen Bai, Hongjian Zhang
The primary objective of this study is to understand the profiles, sources and cytotoxic effects of atmospheric polycyclic aromatic hydrocarbons (PAHs), which are closely related to urban air contamination and public health, in urban roadside environments. On-road sampling campaigns were conducted from 2014 to 2015 at three urban road sites in Hangzhou, China. Sixteen gaseous and particulate matter (PM) 2.5-bound PAHs were identified and quantified using gas chromatography-mass spectrometry (GC-MS). The total PAH concentrations at the three sites ranged from 750 to1142 ng/m(3) and 1050 to 1483 ng/m(3) in summer and winter, respectively...
December 7, 2016: Journal of Environmental Science and Health. Part A, Toxic/hazardous Substances & Environmental Engineering
https://www.readbyqxmd.com/read/27925711/evaluation-of-susceptibility-of-polymer-and-rubber-materials-intended-into-contact-with-drinking-water-on-biofilm-formation
#7
Maciej Szczotko, Agnieszka Stankiewicz, Małgorzata Jamsheer-Bratkowska
Background: Plumbing materials in water distribution networks and indoor installations are constantly evolving. The application of new, more economical solutions with plastic materials eliminates the corrosion problems, however, do not fully protect the consumer against secondary microbial contamination of water intended for human consumption caused by the presence of a biofilm on the inner surface of materials applied. National Institute of Public Health - National Institute of Hygiene conducts research aimed at a comprehensive assessment of this type of materials, resulting their further marketing authorization in Poland...
2016: Roczniki Państwowego Zakładu Higieny
https://www.readbyqxmd.com/read/27925499/non-adherence-to-psychotropic-medication-among-adolescents-a-systematic-review-of-the-literature
#8
Alexander Häge, Lisa Weymann, Lucia Bliznak, Viktoria Märker, Konstantin Mechler, Ralf W Dittmann
INTRODUCTION: Whether patients take their medication as prescribed is of increasing importance in adolescent psychiatry since both the number of efficacious pharmaceutical treatments and the rate of prescriptions of psychotropic compounds are on the rise. Previous research showed high rates of medication nonadherence among both adolescents with medical disorders and adult patients with psychiatric disorders. METHODS: The present review was performed according to PRISMA guidelines and evaluates existing scientific literature concerning adherence to psychotropic medication among adolescents...
December 7, 2016: Zeitschrift Für Kinder- und Jugendpsychiatrie und Psychotherapie
https://www.readbyqxmd.com/read/27925497/anti-inflammatory-and-anticancer-effects-of-flavonol-glycosides-from-diplotaxis-harra-through-gsk3%C3%AE-regulation-in-intestinal-cells
#9
Imen Nasri, Rachid Chawech, Cynthia Girardi, Emmanuel Mas, Audrey Ferrand, Nathalie Vergnolle, Nicolas Fabre, Raoudha Mezghani-Jarraya, Claire Racaud-Sultan
CONTEXT AND OBJECTIVE: Diplotaxis harra (Forssk.) Boiss. (Brassicaceae) is traditionally used as an antidiabetic, anti-inflammatory or anticancer agent. In these pathologies, the glycogen synthase kinase 3 β (GSK3β) is overactivated and represents an interesting therapeutic target. Several flavonoids can inhibit GSK3β and the purpose of this study was to search for the compounds in Diplotaxis harra which are able to modulate GSK3β. MATERIALS AND METHODS: Methanol extracts from D...
December 2017: Pharmaceutical Biology
https://www.readbyqxmd.com/read/27925471/lc-ms-ms-and-gc-ms-analyses-of-biologically-active-extracts-and-fractions-from-tunisian-juniperus-phoenice-leaves
#10
Henda Keskes, Sahla Belhadj, Lobna Jlail, Abdelfattah El Feki, Mohamed Damak, Sami Sayadi, Noureddine Allouche
CONTEXT: Despite some studies related to Juniperus phoenicea L. (Cupressaceae), phytochemical and biological investigations of this plant remain unexplored. OBJECTIVE: This work is the first report dealing with the identification and characterization of volatile components and flavonoids in hexane and methanol extracts from J. phoenicea leaves Materials and methods: Antioxidant activity of hexane, and methanol extracts from J. phoenicea leaves were determined by DPPH-radical scavenging assay...
December 2017: Pharmaceutical Biology
https://www.readbyqxmd.com/read/27925394/markovnikov-selective-radical-addition-of-s-nucleophiles-to-terminal-alkynes-through-a-photoredox-process
#11
Huamin Wang, Qingquan Lu, Chien-Wei Chiang, Yi Luo, Jiufu Zhou, Guangyu Wang, Aiwen Lei
Direct radical additions to terminal alkynes have been widely employed in organic synthesis, providing credible access to the anti-Markovnikov products. Because of the Kharasch effect, regioselective control for the formation of Markovnikov products still remains a great challenge. Herein, we develop a transition-metal-free, visible light-mediated radical addition of S-nucleophiles to terminal alkynes, furnishing a wide array of α-substituted vinyl sulfones with exclusive Markovnikov regioselectivity. Mechanistic investigations demonstrated that radical/radical cross-coupling might be the key step in this transformation...
December 7, 2016: Angewandte Chemie
https://www.readbyqxmd.com/read/27925320/three-dimensional-fibrous-network-of-na0-21mno2-for-aqueous-sodium-ion-hybrid-supercapacitor
#12
Natarajan Karikalan, Chelladurai Karuppiah, Shen-Ming Chen, Murugan Velmurugan, Periyasami Gnanaprakasam
Sodium ion hybrid supercapacitors are the potential energy storage devices and recently received an enormous interest. However, the development of desired cathode material and the use of non-aqueous electrolyte remains a great challenge. Hence, we developed the aqueous Na-ion hybrid supercapacitor based on three dimensional fibrous network of NaMnO2. The described cathode material was synthesized by the electro-oxidation of potassium manganese hexacyanoferrate (KMnHCF) nanocubes. The oxidized compound was confirmed as Na0...
December 7, 2016: Chemistry: a European Journal
https://www.readbyqxmd.com/read/27925311/the-chemistry-of-a-non-interacting-vicinal-frustrated-phosphane-borane-lewis-pair
#13
Lisa-Maria Elmer, Gerald Kehr, Constantin G Daniliuc, Melanie Siedow, Hellmut Eckert, Matthias Tesch, Armido Studer, Kamille Williams, Timothy H Warren, Gerhard Erker
The dimesitylphosphinocyclopentene/HB(C6 F5 )2 -derived vicinal trans-1,2-P/B frustrated Lewis pair (FLP) 4 shows no direct phosphane-borane interaction. Toward some reagents it behaves similar to an intermolecular FLP; it cleaves dihydrogen, deprotonates terminal alkynes, and adds to organic carbonyl compounds including CO2 . It shows typical intramolecular FLP reaction modes (cooperative 1,1-additions) to mesityl azide, to carbon monoxide, and to NO. The latter reaction yields a persistent P/B FLPNO nitroxide radical, which undergoes H-atom abstraction reactions...
December 7, 2016: Chemistry: a European Journal
https://www.readbyqxmd.com/read/27925279/method-to-account-for-the-effect-of-hydrodynamics-on-polar-organic-compound-uptake-by-passive-samplers
#14
Kees Booij, Natasja L Maarsen, Matthijs Theeuwen, Ronald van Bommel
Mass transfer coefficients of the water boundary layer (kw ) were measured using alabaster dissolution kinetics in a diffusion cell that was operated at stirring rates between 90 and 600 min(-1) , aiming to provide a more robust characterisation of the effect of hydrodynamics on the uptake of polar compounds by passive samplers, as compared with characterisations in terms of stirring rates and water flow velocities. The measured kw helped to quantitatively understand calcium sulphate transport through a poly(ethersulfone) membrane and two water boundary layers (at both sides of the membrane)...
December 7, 2016: Environmental Toxicology and Chemistry
https://www.readbyqxmd.com/read/27925269/lifecycle-exposure-of-fathead-minnows-to-environmentally-relevant-concentrations-of-the-%C3%AE-blocker-drug-propranolol
#15
Joanne L Parrott, Vimal K Balakrishnan
Propranolol is a human pharmaceutical β-blocker that has been detected in municipal wastewater effluents at ng/L to low µg/L. To assess the potential of this compound to affect fish, fathead minnow (Pimephales promelas) were exposed for a lifecycle in a flow-through system to nominal propranolol concentrations of 0.87, 8.7, 87, 870 and 8,700 ng/L. Measured propranolol concentrations were below detection for the two lowest exposure concentrations, and were 76, 580, and 7,800 ng/L for the three highest exposure concentrations...
December 7, 2016: Environmental Toxicology and Chemistry
https://www.readbyqxmd.com/read/27925266/marine-mollusk-derived-agents-with-antiproliferative-activity-as-promising-anticancer-agents-to-overcome-chemotherapy-resistance
#16
REVIEW
Maria Letizia Ciavatta, Florence Lefranc, Marianna Carbone, Ernesto Mollo, Margherita Gavagnin, Tania Betancourt, Ramesh Dasari, Alexander Kornienko, Robert Kiss
The chemical investigation of marine mollusks has led to the isolation of a wide variety of bioactive metabolites, which evolved in marine organisms as favorable adaptations to survive in different environments. Most of them are derived from food sources, but they can be also biosynthesized de novo by the mollusks themselves, or produced by symbionts. Consequently, the isolated compounds cannot be strictly considered as "chemotaxonomic markers" for the different molluscan species. However, the chemical investigation of this phylum has provided many compounds of interest as potential anticancer drugs that assume particular importance in the light of the growing literature on cancer biology and chemotherapy...
December 7, 2016: Medicinal Research Reviews
https://www.readbyqxmd.com/read/27925257/volatile-compounds-produced-by-lactobacillus-paracasei-during-oat-fermentation
#17
Sang Mi Lee, Jieun Oh, Byung-Serk Hurh, Gwi-Hwa Jeong, Young-Keum Shin, Young-Suk Kim
This study investigated the profiles of volatile compounds produced by Lactobacillus paracasei during oat fermentation using gas chromatography-mass spectrometry coupled with headspace solid-phase microextraction method. A total of 60 compounds, including acids, alcohols, aldehydes, esters, furan derivatives, hydrocarbons, ketones, sulfur-containing compounds, terpenes, and other compounds, were identified in fermented oat. Lipid oxidation products such as 2-pentylfuran, 1-octen-3-ol, hexanal, and nonanal were found to be the main contributors to oat samples fermented by L...
December 2016: Journal of Food Science
https://www.readbyqxmd.com/read/27925249/inhibition-of-glucuronidation-and-oxidative-metabolism-of-buprenorphine-using-gras-compounds-or-dietary-constituents-supplements-in-vitro-proof-of-concept
#18
Neha V Maharao, Anand A Joshi, Phillip M Gerk
The present study investigated the potential of generally recognized as safe compounds or dietary substances to inhibit the presystemic metabolism of buprenorphine and increase its oral bioavailability. Using IVIVE, the buprenorphine extraction ratios in intestine and liver were predicted as 96% and 71%, respectively. In addition, the relative fraction of buprenorphine metabolized by oxidation and glucuronidation in these two organs was estimated using pooled human intestinal and liver microsomes. In both organs, oxidation appeared to be the major metabolic pathway with a six and four fold higher intrinsic clearance than glucuronidation in intestine and liver, respectively...
December 7, 2016: Biopharmaceutics & Drug Disposition
https://www.readbyqxmd.com/read/27925246/analytical-method-for-urinary-metabolites-as-biomarkers-for-monitoring-exposure-to-phthalates-by-gas-chromatography-mass-spectrometry
#19
Toshiaki Yoshida
Phthalates, widely being used as plasticizers, have been detected from the indoor air of residences, but there have been few reports on methods of analyzing urinary metabolites as biomarkers to monitor exposure to di-n-pentyl phthalate or di-n-hexyl phthalate. Presented here is a cost-effective and sensitive analytical method for the determination of urinary metabolites of phthalates containing these two compounds. Nine urinary phthalate metabolites were enzymatically hydrolyzed and extracted with toluene: monomethyl phthalate, monoethyl phthalate, monoisobutyl phthalate, mono-n-butyl phthalate, mono-n-pentyl phthalate, mono-n-hexyl phthalate, monocyclohexyl phthalate, monobenzyl phthalate and mono(2-ethyl-5-carboxypentyl) phthalate...
December 7, 2016: Biomedical Chromatography: BMC
https://www.readbyqxmd.com/read/27925210/effects-of-steam-microwave-blanching-and-different-drying-processes-on-drying-characteristics-and-quality-attributes-of-thunbergia-laurifolia-linn-leaves
#20
Traiphop Phahom, Singhanat Phoungchandang, William L Kerr
BACKGROUND: Dried Thunbergia laurifolia leaves are usually prepared using tray drying, resulting in products that have lost substantial amounts of bioactive compounds and antioxidant activity. The maturity of the raw material, blanching techniques and drying methods were investigated in order to select the best condition to produce high qualities of dried T. laurifolia leaves. RESULTS: The 1(st) stage of maturity was selected and steam-microwave blanching (SMB) for 4 min was adequate for blanching leading to the maximum recovery of bioactive compounds...
December 7, 2016: Journal of the Science of Food and Agriculture
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