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https://www.readbyqxmd.com/read/29668114/-%C3%AE-2-adrenoceptors-inhibit-neutrophil-extracellular-traps-in-human-polymorphonuclear-leukocytes
#1
Franca Marino, Angela Scanzano, Laura Pulze, Monica Pinoli, Emanuela Rasini, Alessandra Luini, Raffaella Bombelli, Massimiliano Legnaro, Magda de Eguileor, Marco Cosentino
This study tests the hypothesis that in isolated human polymorphonuclear leukocytes (PMN) adrenergic ligands can affect neutrophil extracellular trap (NET) formation. We have previously shown that, in PMN, adrenaline (A), through the activation of adrenergic receptors (AR), reduces stimulus-dependent cell activation; we have, therefore, planned to investigate if AR are involved in NET production. PMN were obtained from venous blood of healthy subject. The ability of adrenergic ligands to affect reactive oxygen species (ROS) production, NET production, and cell migration was investigated in cells cultured under resting conditions or after activation with N-formyl-methionyl-leucyl-phenylalanine (fMLP), LPS, or IL-8...
April 18, 2018: Journal of Leukocyte Biology
https://www.readbyqxmd.com/read/29667820/identification-of-ingol-and-rhamnofolane-diterpenoids-from-euphorbia-resinifera-and-their-abilities-to-induce-lysosomal-biosynthesis
#2
Ning-Dong Zhao, Xiao Ding, Yu Song, Dong-Qiong Yang, Hai-Li Yu, Tiwalade Adegoke Adelakun, Wen-Dan Qian, Yu Zhang, Ying-Tong Di, Fang Gao, Xiao-Jiang Hao, Shun-Lin Li
The phytochemical study of Euphorbia resinifera afforded 18 structurally diverse diterpenoids, including 14 new ingol-type diterpenoids, euphorblins A-N (1-14), a new rhamnofolane diterpenoid, euphorblin O (15), and three known analogues (16-18). The structures of these compounds were deduced using 2D NMR spectroscopy and NOE experiments. The structure of compound 1 was confirmed by single-crystal X-ray crystallography. The abilities of the compounds to enhance lysosomal biosynthesis were evaluated through LysoTracker Red staining...
April 18, 2018: Journal of Natural Products
https://www.readbyqxmd.com/read/29667768/quinazoline-based-hydroxamic-acids-design-synthesis-and-evaluation-of-histone-deacetylase-inhibitory-effects-and-cytotoxicity
#3
Doan Thanh Hieu, Duong Tien Anh, Hai Pham-The, Le-Thi-Thu Huong, Eun Jae Park, Jeong Eun Choi, Jong Soon Kang, Sang-Bae Han, Phan Thi Phuong Dung, Nguyen-Hai Nam
In our search for novel histone deacetylases inhibitors, we have designed and synthesized a series of novel hydroxamic acids and N-hydroxybenzamides incorporating quinazoline heterocycles (4a-i, 6a-i). Bioevaluation showed that these quinazoline-based hydroxamic acids and N-hydroxybenzamides were potently cytotoxic against three human cancer cell lines (SW620, colon; PC-3, prostate; NCI-H23, lung). In term of cytotoxicity, several compounds, e.g. 4g, 4c, 4g-i, 6c, and 6h, displayed from 5- up to 10-fold higher potency than SAHA (suberoylanilidehydroxamic acid, vorinostat)...
April 18, 2018: Chemistry & Biodiversity
https://www.readbyqxmd.com/read/29667758/synthesis-of-enantiomerically-enriched-drug-precursors-by-lactobacillus-paracasei-bd87e6-as-a-biocatalyst
#4
Selda Öksüz, Engin Şahin, Enes Dertli
Global sales of single enantiomeric drug products are growing at an alarming rate every year. A total of 7 bacterial strains were screened for their ability to reduce acetophenones to its corresponding alcohol. Among these strain Lactobacillus paracasei BD87E6 was found to be the most successful biocatalyst to reduce the ketones to the corresponding alcohols. The reaction conditions were systematically optimized for the reducing agent Lactobacillus paracasei BD87E6, which showed high enantioselectivity and conversion for the bioreduction...
April 18, 2018: Chemistry & Biodiversity
https://www.readbyqxmd.com/read/29667756/pharmacokinetic-profiling-of-anticancer-phytocompounds-using-computational-approach
#5
Ashish Sharma, Shilpa Sharma, Mansi Gupta, Shehnaz Fatima, Ravi Saini, Subhash Mohan Agarwal
INTRODUCTION: Natural products exhibit diverse scaffolds and are considered as suitable candidates for development of leads. However, poor pharmacokinetics often acts as a hindrance during the drug discovery process. OBJECTIVE: With a view of exploring the absorption, distribution, metabolism, excretion and toxicity (ADMET) profile of plant-based anticancer compounds, open-access databases (NPACT, CancerHSP and TaxKB) were analysed to identify molecules having properties favourable for drug ability...
April 18, 2018: Phytochemical Analysis: PCA
https://www.readbyqxmd.com/read/29667556/ultrasound-promoted-green-synthesis-docking-study-of-indole-spliced-thiadiazole-%C3%AE-amino-phosphonates-as-anticancer-agents-and-anti-tyrosinase-agents
#6
Anna Pratima G Nikalje, Pramod Gawhane, Shailee Tiwari, Jaiprakash Sangshetti, Manoj Damale
In this work, a new series of diethyl ((1H-indole-3-yl)((5-phenyl-1,3,4-thiadiazole-2- yl)amino)methyl)phosphonate derivatives 6(a-j) were designed and synthesized in Ultrasound by green protocol using Kabachnik-Fields reaction. The structures of the synthesized compounds were confirmed by spectral analysis such as elemental analyses, IR, 1H NMR, 13C NMR, 31P NMR and mass spectra. The synthesized compounds 6(a-j) were appraised for their in vitro anticancer activity against human cancer cell lines such as SK-MEL-2 (melanoma), IMR-32 (Neuroblastoma), HT-29(Colon) and also on normal murine embryonic fibroblast NIH/3T3 by Sulforhodamine B (SRB) assay, using Adriamycin as a standard drug...
April 17, 2018: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/29667177/adverse-placental-effects-of-valproic-acid-studies-in-perfused-human-placentas
#7
Miriam Rubinchik-Stern, Miriam Shmuel, Jacob Bar, Michal Kovo, Sara Eyal
OBJECTIVE: In utero exposure to valproic acid (VPA) has been associated with worse pregnancy outcomes compared to all other antiepileptic drugs. We have previously shown that VPA alters the expression of placental transporters for hormones and nutrients in vitro and in pregnant mice. Here, our aim was to characterize the effects of short exposure to VPA on the expression of carriers for compounds essential for fetal development in human placentas ex vivo, under controlled conditions...
April 17, 2018: Epilepsia
https://www.readbyqxmd.com/read/29667062/comparison-of-different-advanced-degradation-processes-for-the-removal-of-the-pharmaceutical-compounds-diclofenac-and-carbamazepine-from-liquid-solutions
#8
Andrea G Capodaglio, Anna Bojanowska-Czajka, Marek Trojanowicz
Carbamazepine and diclofenac are two examples of drugs with widespread geographical and environmental media proliferation that are poorly removed by traditional wastewater treatment processes. Advanced oxidation processes (AOPs) have been proposed as alternative methods to remove these compounds in solution. AOPs are based on a wide class of powerful technologies, including UV radiation, ozone, hydrogen peroxide, Fenton process, catalytic wet peroxide oxidation, heterogeneous photocatalysis, electrochemical oxidation and their combinations, sonolysis, and microwaves applicable to both water and wastewater...
April 18, 2018: Environmental Science and Pollution Research International
https://www.readbyqxmd.com/read/29667047/investigation-of-the-mechanism-of-therapeutic-protein-drug-interaction-between-methotrexate-and-golimumab-an-anti-tnf%C3%AE-monoclonal-antibody
#9
Weirong Wang, Jocelyn Leu, Rebecca Watson, Zhenhua Xu, Honghui Zhou
A prominent example of human therapeutic protein-drug interaction (TP-DI) is between methotrexate (MTX) and anti-TNFα mAbs. One plausible mechanism for this TP-DI is through the pharmacodynamic effect of MTX on immunogenicity. However, there is no definitive evidence to substantiate this mechanism, and other competing hypotheses, such as MTX suppressing FcγRI expression thereby affecting mAb PK, have also been proposed. In order to understand this mechanism, a cynomolgus monkey study was conducted using golimumab as a model compound...
April 17, 2018: AAPS Journal
https://www.readbyqxmd.com/read/29667003/chemical-genomics-reveals-inhibition-of-breast-cancer-lung-metastasis-by-ponatinib-via-c-jun
#10
Wei Shao, Shasha Li, Lu Li, Kequan Lin, Xinhong Liu, Haiyan Wang, Huili Wang, Dong Wang
Metastasis is the leading cause of human cancer deaths. Unfortunately, no approved drugs are available for anti-metastatic treatment. In our study, high-throughput sequencing-based high-throughput screening (HTS2 ) and a breast cancer lung metastasis (BCLM)-associated gene signature were combined to discover anti-metastatic drugs. After screening of thousands of compounds, we identified Ponatinib as a BCLM inhibitor. Ponatinib significantly inhibited the migration and mammosphere formation of breast cancer cells in vitro and blocked BCLM in multiple mouse models...
April 17, 2018: Protein & Cell
https://www.readbyqxmd.com/read/29666865/preparation-of-lactic-acid-and-glucose-responsive-poly-%C3%AE%C2%B5-caprolactone-b-poly-ethylene-oxide-block-copolymer-micelles-using-phenylboronic-ester-as-a-sensitive-block-linkage
#11
David Vrbata, Mariusz Uchman
The present study describes the synthesis, self-assembly and responsiveness to glucose and lactic acid of biocompatible and biodegradable block copolymer micelles using phenylboronic ester as the linkage between hydrophobic poly(ε-caprolactone) (PCL) and hydrophilic poly(ethylene oxide) (PEO). The PCL block with pendant phenylboronic acid (PCLBA) was synthesized by combining ε-caprolactone (ε-CL) ring-opening polymerisation (ROP), using 4-hydroxymethyl(phenylboronic) acid pinacolate as the initiator, and pinacol deprotection...
April 18, 2018: Nanoscale
https://www.readbyqxmd.com/read/29666792/steady-state-linear-and-non-linear-optical-spectroscopy-of-organic-chromophores-and-bio-macromolecules
#12
REVIEW
Marco Marazzi, Hugo Gattuso, Antonio Monari, Xavier Assfeld
Bio-macromolecules as DNA, lipid membranes and (poly)peptides are essential compounds at the core of biological systems. The development of techniques and methodologies for their characterization is therefore necessary and of utmost interest, even though difficulties can be experienced due to their intrinsic complex nature. Among these methods, spectroscopies, relying on optical properties are especially important to determine their macromolecular structures and behaviors, as well as the possible interactions and reactivity with external dyes-often drugs or pollutants-that can (photo)sensitize the bio-macromolecule leading to eventual chemical modifications, thus damages...
2018: Frontiers in Chemistry
https://www.readbyqxmd.com/read/29666146/identification-of-circadian-clock-modulators-from-existing-drugs
#13
T Katherine Tamai, Yusuke Nakane, Wataru Ota, Akane Kobayashi, Masateru Ishiguro, Naoya Kadofusa, Keisuke Ikegami, Kazuhiro Yagita, Yasufumi Shigeyoshi, Masaki Sudo, Taeko Nishiwaki-Ohkawa, Ayato Sato, Takashi Yoshimura
Chronic circadian disruption due to shift work or frequent travel across time zones leads to jet-lag and an increased risk of diabetes, cardiovascular disease, and cancer. The development of new pharmaceuticals to treat circadian disorders, however, is costly and hugely time-consuming. We therefore performed a high-throughput chemical screen of existing drugs for circadian clock modulators in human U2OS cells, with the aim of repurposing known bioactive compounds. Approximately 5% of the drugs screened altered circadian period, including the period-shortening compound dehydroepiandrosterone (DHEA; also known as prasterone)...
April 17, 2018: EMBO Molecular Medicine
https://www.readbyqxmd.com/read/29665654/hypericin-affects-cancer-side-populations-via-competitive-inhibition-of-bcrp
#14
Jana Vargová, Jaromír Mikeš, Rastislav Jendželovský, Lucia Mikešová, Barbora Kuchárová, Ľubomír Čulka, Radek Fedr, Ján Remšík, Karel Souček, Alois Kozubík, Peter Fedoročko
OBJECTIVE: Cancer stem-like cells (CSLCs) are considered a root of tumorigenicity and resistance. However, their identification remains challenging. The use of the side population (SP) assay as a credible marker of CSLCs remains controversial. The SP assay relies on the elevated activity of ABC transporters that, in turn, can be modulated by hypericin (HYP), a photosensitizer and bioactive compound of St. John's Wort (Hypericum perforatum), a popular over-the-counter antidepressant. Here we aimed to comprehensively characterize the SP phenotype of cancer cells and to determine the impact of HYP on these cells...
March 2018: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29665554/inhibition-by-non-steroidal-anti-inflammatory-drugs-of-compound-action-potentials-in-frog-sciatic-nerve-fibers
#15
Rika Suzuki, Tsugumi Fujita, Kotaro Mizuta, Eiichi Kumamoto
AIMS: Although antinociception produced by non-steroidal anti-inflammatory drugs (NSAIDs) is partly attributed to nerve conduction inhibition, this has not been thoroughly examined yet. The aim of the present study was to reveal quantitatively how various types of NSAIDs affect compound action potentials (CAPs), a measure of nerve conduction. MAIN METHODS: CAPs were recorded from the frog sciatic nerve by using the air-gap method. KEY FINDINGS: Soaking the sciatic nerve with acetic acid-based NSAIDs (diclofenac and aceclofenac) reduced the peak amplitude of CAP in a concentration-dependent manner; their IC50 values were 0...
April 14, 2018: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29665526/novel-hydrazide-hydrazone-and-amide-substituted-coumarin-derivatives-synthesis-cytotoxicity-screening-microarray-radiolabeling-and-in-vivo-pharmacokinetic-studies
#16
Tamer Nasr, Samir Bondock, Hassan M Rashed, Walid Fayad, Mahmoud Youns, Tamer M Sakr
The current work presents the synthesis and biological evaluation of new series of coumarin hydrazide-hydrazone derivatives that showed in vitro broad spectrum antitumor activities against resistant pancreatic carcinoma (Panc-1), hepatocellular carcinoma (HepG2) and leukemia (CCRF) cell lines using doxorubicin as reference standard. Bromocoumarin hydrazide-hydrazone derivative (BCHHD) 11b showed excellent anticancer activity against all tested cancer cell lines. Enzyme assays showed that BCHHD 11b induced apoptosis due to activation of caspases 3/7...
April 9, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29665471/comparison-between-liquid-chromatography-and-supercritical-fluid-chromatography-coupled-to-mass-spectrometry-for-beta-agonists-screening-in-feeding-stuff
#17
L Herpin, E Bichon, L Rambaud, F Monteau, B Le Bizec
β-agonistic drugs have been forbidden as growth promoters in rearing animals in Europe since the late 1980s (Dir 96/22/EC). Specific and sensitive analytical methods based on UHPLC-MS/MS allow to monitor a large set of these substances. However, optimal performances are not observed for all the target analytes, especially for those exhibiting the highest polarities. We developed an SFC-MS/MS approach to cover the huge elution window of β-agonists, from the most polar which are usually eluted in the void volume when using reversed phase chromatography in conventional HPLC to the most apolar ones...
April 11, 2018: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
https://www.readbyqxmd.com/read/29665289/a-whole-body-physiologically-based-pharmacokinetic-model-for-colistin-and-colistin-methanesulfonate-cms-in-rat
#18
Salim Bouchene, Sandrine Marchand, William Couet, Lena E Friberg, Patrice Gobin, Isabelle Lamarche, Nicolas Grégoire, Sven Björkman, Mats O Karlsson
Colistin is a polymyxin antibiotic used to treat patients infected with multidrug-resistant Gram negative bacteria (MDR-GNB). The objective of this work was to develop a whole-body physiologically based pharmacokinetic (WB-PBPK) model to predict tissue distribution of colistin in rat. The distribution of a drug in a tissue is commonly characterized by its tissue-to-plasma partition coefficient, Kp . Colistin and its prodrug, colistin methanesulfonate (CMS) Kp priors were measured experimentally from rat tissue homogenates or predicted in silico...
April 17, 2018: Basic & Clinical Pharmacology & Toxicology
https://www.readbyqxmd.com/read/29664808/trends-in-pharmacological-emergency-treatment-of-patients-suffering-from-schizophrenia-over-a-16-year-observation-period
#19
Monika Edlinger, Anna-Sophia Welte, Nursen Yalcin-Siedentopf, Georg Kemmler, Felix Neymeyer, W Wolfgang Fleischhacker, Alex Hofer
Patients suffering from schizophrenia are often treated in locked psychiatric units because of psychomotor agitation, hostility and aggressive behavior, or suicidality. Because of legal conditions, investigations on these acutely ill patients are difficult, and many studies do not represent 'real-life psychiatry'. This retrospective survey was conducted at the Department of Psychiatry, Psychotherapy and Psychosomatics of the Medical University, Innsbruck, Austria. Data were collected from the records of all adult inpatients suffering from a schizophrenia spectrum disorder according to the International Classification of Diseases, 10th ed...
April 16, 2018: International Clinical Psychopharmacology
https://www.readbyqxmd.com/read/29664601/difluorocarbene-as-a-building-block-for-consecutive-bond-forming-reactions
#20
Alexander D Dilman, Vitalij V Levin
Compounds containing a difluoromethylene unit have gained increasing attention due to their utility in drug design. Classic methods for the synthesis of these compounds rely on either harsh deoxofluorination reactions or laborious functional group manipulation sequences. In 2013, we proposed a method for assembling gem-difluorinated molecules from a difluorocarbene, a nucleophile, and an electrophile. In this process, a difluorocarbene can be considered an equivalent of a bipolar CF2 unit. Performing consecutive bond-forming reactions by sequential attachment of a nucleophile and an electrophile to a difluorocarbene provides the opportunity for the synthesis of a wide variety of organofluorine compounds...
April 17, 2018: Accounts of Chemical Research
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